Dihydropyrimidone inhibitors of calcium channel function Number:7,166,603 from the United States Patent and Trademark Office (PTO) owispatent Compounds having the formula, ##STR00001## enantiomers, diastereomers, solvates and salts thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4, A, X, and J are described herein, are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.<H Dihydropyrimidone, inhibitors, Dihydropyrimido, 7166603.html, Patent, pto, 7166603

Title: Dihydropyrimidone inhibitors of calcium channel function

Abstract: Compounds having the formula, ##STR00001## enantiomers, diastereomers, solvates and salts thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4, A, X, and J are described herein, are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.

Patent Number: 7,166,603 Issued on 01/23/2007 to Murugesan, et al.

Inventors: Murugesan; Natesan (Princeton Junction, NJ), Bisacchi; Gregory S. (Newtown Highlands, MA), Ewing; William R. (Yardley, PA), Yu; Guixue (Lawrenceville, NJ), Gu; Zhengxiang (Princeton, NJ), Friends; Todd (Bordentown, NJ), Zhang; Minsheng (Warren, NJ)
Assignee: Bristol-Myers Squibb Co. (Princeton, NJ)

Appl. No.: 10/897,215

Filed: July 22, 2004

Current U.S. Class: 514/249 ; 514/269; 544/295; 544/316

Current International Class: C07D 239/22 (20060101); A61K 31/513 (20060101); C07D 403/06 (20060101)

Field of Search: 544/295,316 514/249,269

References Cited [Referenced By]

U.S. Patent Documents


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4684655	August 1987	Atwal
4684656	August 1987	Atwal
4689414	August 1987	Atwal
4728652	March 1988	Atwal
4753946	June 1988	Atwal et al.
4769371	September 1988	Atwal
4824831	April 1989	Atwal
4855301	August 1989	Atwal et al.
5202330	April 1993	Atwal et al.
5403847	April 1995	Gluchowski et al.
5889016	March 1999	Bruce et al.
5942517	August 1999	Nagarathnam et al.
6143750	November 2000	Patane et al.
6172066	January 2001	Nagarathnam et al.
6207444	March 2001	Sidler et al.
6228861	May 2001	Nagarathnam et al.
6245773	June 2001	Wong et al.
6255315	July 2001	Patane et al.
6268369	July 2001	Nagarathnam et al.
6274585	August 2001	Cui et al.
6387893	May 2002	Evans et al.
2002/0010186	January 2002	Wong et al.
2005/0043322	February 2005	Murugesan et al.

Foreign Patent Documents


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WO 96/14846	May., 1996	WO
WO 97/17969	May., 1997	WO
WO 97/42956	Nov., 1997	WO
WO 98/33791	Aug., 1998	WO
WO 98/51311	Nov., 1998	WO
WO 98/57638	Dec., 1998	WO
WO 98/57641	Dec., 1998	WO
WO 99/23072	May., 1999	WO
WO 99/48530	Sep., 1999	WO
WO 00/02455	Jan., 2000	WO
WO 00/06565	Feb., 2000	WO
WO 00/15845	Mar., 2000	WO
WO 00/37026	Jun., 2000	WO
WO 00/59882	Oct., 2000	WO
WO 01/02561	Jan., 2001	WO
WO 01/19845	Mar., 2001	WO
WO 01/22919	Apr., 2001	WO
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WO 02/078639	Oct., 2002	WO
WO 02/079149	Oct., 2002	WO
WO 02/079169	Oct., 2002	WO
WO 03/007953	Jan., 2003	WO

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Primary Examiner: Rao; Deepak
Attorney, Agent or Firm: Duncan; Laurelee A.

Parent Case Text

This application claims the benefit of priority from U.S. Provisional Application Ser. No. 60/489,365 filed Jul. 23, 2003, the entirety of which is incorporated herein by reference.

Claims

What is claimed is:

1. A compound having the formula, ##STR00348## or an enantiomer, diastereomer, or salt, thereof, wherein ##STR00349## A is a group of formula X is oxygen or sulfur; J is n-propylene; R.sup.1 is alkyl optionally substituted with Z.sup.1b, Z.sup.2b and/or one or more Z.sup.3b; R.sup.2 is CO.sub.2R.sup.5; R.sup.3 is --N(R.sup.6)C(O)R.sup.7; R.sup.4 is hydrogen or alkyl, R.sup.5 is alkyl; R.sup.6 is hydrogen or alkyl; R.sup.7 is selected from ##STR00350## ##STR00351## ##STR00352## ##STR00353## ##STR00354## ##STR00355## ##STR00356## ##STR00357## Z.sup.1 and 1b, and 1g, Z.sup.2b, and Z.sup.3b are optional substituents independently selected from (1) R.sup.10, where R.sup.10 is (i) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl; (ii) a group (i) which is itself substituted by one or more of the same or different groups (i); or (iii) a group (i) or (ii) which is independently substituted by one or more of the following groups (2) to (13) of the definition of Z.sup.1, (2) --OH or --OR.sup.10, (3) --SH or --SR.sup.10, (4) --C(O).sub.tH, --C(O).sub.tR.sup.10, or --O--C(O)R.sup.10, where t is 1 or 2, (5) --SO.sub.3H, --S(O).sub.tR.sup.10, or S(O).sub.tN(R.sup.11)R.sup.10, (6) halo, (7) cyano, (8) nitro, (9) --U.sup.1--N R.sup.12R.sup.13, (10) --U.sup.1--N(R.sup.11)--U.sup.2--N R.sup.12R.sup.13, (11) --U.sup.1--N(R.sup.14)--U.sup.2--R.sup.10, (12) --U.sup.1--N(R.sup.14)--U.sup.2--H, (13) oxo; U.sup.1 and U.sup.2 are each independently (1) a single bond, (2) --U.sup.3--S(O).sub.t--U.sup.4--, (3) --U.sup.3--C(O)--U.sup.4--, (4) --U.sup.3--C(S)--U.sup.4--, (5) --U.sup.3--O--U.sup.4--, (6) --U.sup.3--S--U.sup.4--, (7) --U.sup.3--O--C(O)--U.sup.4--, (8) --U.sup.3--C(O)--O--U.sup.4--, (9) --U.sup.3--C(.dbd.NR.sup.15)--U.sup.4--, or (10) --U.sup.3--C(O)--C(O)--U.sup.4; R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 (1) are each independently hydrogen or a group provided in the definition of Z.sup.1; or (2) R.sup.12 and R.sup.13 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (3) R.sup.12 or R.sup.13, together with R.sup.11, may be alkylene or alkenylene completing a 3- to 8-membered saturated or unsaturated ring together with the nitrogen atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (4) R.sup.12 and R.sup.13 together with the nitrogen atom to which they are attached may combine to form a group --N.dbd.C R.sup.16R.sup.17 where R.sup.16 and R.sup.17 are each independently H or a group provided in the definition of R.sup.10; and U.sup.3 and U.sup.4 are each independently (1) a single bond, (2) alkylene, (3) alkenylene, (4) alkynylene.

2. A compound of claim 1, or an enantiomer, diastereomer, or salt, thereof, wherein R.sup.1 is methyl; and R.sup.2 is C(O)O(alkyl) wherein alkyl is selected from methyl, ethyl and isopropyl.

3. A compound of claim 1, or an enantiomer, diastereomer, or salt, thereof, wherein R.sup.1 is ##STR00358## R.sup.2 is C(O)O(alkyl) wherein alkyl is selected from methyl, ethyl and isopropyl.

4. A compound having the formula, ##STR00359## or an enantiomer, diastereomer, or salt, thereof, wherein ##STR00360## A is a group of formula X is oxygen or sulfur; J is alkylene; R.sup.1 is alkyl optionally substituted with Z.sup.1b, Z.sup.2b and/or one or more Z.sup.3b; R.sup.2 is CO.sub.2R.sup.5; R.sup.3 is --N(R.sup.6)C(O)OR.sup.7; R.sup.4 is hydrogen or alkyl, R.sup.5 is alkyl; R.sup.6 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1g, Z.sup.2g and one or more Z.sup.3g; R.sup.7 selected from ##STR00361## Z.sup.1, 1b, and 1g, Z.sup.2b and 2g, and Z.sup.3b and 3g are optional substituents independently selected from (1) R.sup.10, where R.sup.10 is (i) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl; (ii) a group (i) which is itself substituted by one or more of the same or different groups (i); or (iii) a group (i) or (ii) which is independently substituted by one or more of the following groups (2) to (13) of the definition of Z.sup.1, (2) --OH or --OR.sup.10, (3) --SH or --SR.sup.10, (4) --C(O).sub.tH, --C(O).sub.tR.sup.10, or --O--C(O)R.sup.10, where t is 1 or 2, (5) --SO.sub.3H, --S(O).sub.tR.sup.10, or S(O).sub.tN(R.sup.11)R.sup.10, (6) halo, (7) cyano, (8) nitro, (9) --U.sup.1--N R.sup.12R.sup.13, (10) --U.sup.1--N(R.sup.11)--U.sup.2--N R.sup.12R.sup.13, (11) --U.sup.1--N(R.sup.14)--U.sup.2--R.sup.10, (12) --U.sup.1--N(R.sup.14)--U.sup.2--H, (13) oxo; U.sup.1 and U.sup.2 are each independently (1) a single bond, (2) --U.sup.3--S(O).sub.t--U.sup.4--, (3) --U.sup.3--C(O)--U.sup.4--, (4) --U.sup.3--C(S)--U.sup.4--, (5) --U.sup.3--O--U.sup.4--, (6) --U.sup.3--S--U.sup.4--, (7) --U.sup.3--O--C(O)--U.sup.4--, (8) --U.sup.3--C(O)--O--U.sup.4--, (9) --U.sup.3--C(.dbd.NR.sup.15)--U.sup.4--, or (10) --U.sup.3--C(O)--C(O)--U.sup.4--; R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 (1) are each independently hydrogen or a group provided in the definition of Z.sup.1; or (2) R.sup.12 and R.sup.13 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (3) R.sup.12 or R.sup.13, together with R.sup.11, may be alkylene or alkenylene completing a 3- to 8-membered saturated or unsaturated ring together with the nitrogen atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (4) R.sup.12 and R.sup.13 together with the nitrogen atom to which they are attached may combine to form a group --N.dbd.C R.sup.16R.sup.17 where R.sup.16 and R.sup.17 are each independently H or a group provided in the definition of R.sup.10; and U.sup.3 and U.sup.4 are each independently (1) a single bond, (2) alkylene, (3) alkenylene, (4) alkynylene.

5. A compound having the formula, ##STR00362## or an enantiomer, diastereomer, or salt, thereof, wherein ##STR00363## A is a group of formula X is oxygen or sulfur; J is alkylene; R.sup.1 is alkyl optionally substituted with Z.sup.1b, Z.sup.2b and/or one or more Z.sup.3b; R.sup.2 is CO.sub.2R.sup.5; R.sup.3 is --N(R.sup.6)S(O).sub.2R.sup.7; R.sup.5 is alkyl; R.sup.6 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1g, Z.sup.2g and one or more Z.sup.3g; R.sup.7 selected from ##STR00364## ##STR00365## Z.sup.1, 1b, and 1g, Z.sup.2b and 2g, and Z.sup.3b and 3g are optional substituents independently selected from (1) R.sup.10, where R.sup.10 is (i) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl; (ii) a group (i) which is itself substituted by one or more of the same or different groups (i); or (iii) a group (i) or (ii) which is independently substituted by one or more of the following groups (2) to (13) of the definition of Z.sup.1, (2) --OH or --OR.sup.10, (3) --SH or --SR.sup.10, (4) --C(O).sub.tH, --C(O).sub.tR.sup.10, or --O--C(O)R.sup.10, where t is 1 or 2, (5) --SO.sub.3H, --S(O).sub.tR.sup.10, or S(O).sub.tN(R.sup.11)R.sup.10, (6) halo, (7) cyano, (8) nitro, (9) --U--N R.sup.12R.sup.13, (10) --U--N(R.sup.11)--U.sup.2--N R.sup.12R.sup.13, (11) --U.sup.1--N(R.sup.14)--U.sup.2--R.sup.10, (12) --U.sup.1--N(R.sup.14)--U.sup.2--H, (13) oxo; U.sup.1 and U.sup.2 are each independently (1) a single bond, (2) --U.sup.3--S(O).sub.t--U.sup.4--, (3) --U.sup.3--C(O)--U.sup.4--, (4) --U.sup.3--C(S)--U.sup.4--, (5) --U.sup.3--O--U.sup.4--, (6) --U.sup.3--S--U.sup.4--, (7) --U.sup.3--O--C(O)--U.sup.4--, (8) --U.sup.3--C(O)--O--U.sup.4--, (9) --U.sup.3--C(.dbd.NR.sup.15)--U.sup.4--, or (10) U.sup.3--C(O)--C(O)--U.sup.4--; R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 (1) are each independently hydrogen or a group provided in the definition of Z.sup.1; or (2) R.sup.12 and R.sup.13 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (3) R.sup.12 or R.sup.13, together with R.sup.11, may be alkylene or alkenylene completing a 3- to 8-membered saturated or unsaturated ring together with the nitrogen atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (4) R.sup.12 and R.sup.13 together with the nitrogen atom to which they are attached may combine to form a group --N.dbd.C R.sup.16 R.sup.17 where R.sup.16 and R.sup.17 are each independently H or a group provided in the definition of R.sup.10; and U.sup.3 and U.sup.4 are each independently (1) a single bond, (2) alkylene, (3) alkenylene, (4) alkynylene.

6. A compound having the formula, ##STR00366## or an enantiomer, diastereomer, or salt, thereof, wherein ##STR00367## A is a group of formula X is oxygen or sulfur; J is alkylene; R.sup.1 is alkyl optionally substituted with Z.sup.1b, Z.sup.2b and/or one or more Z.sup.3b; R.sup.2 is CO.sub.2R.sup.5; R.sup.3is selected from ##STR00368## ##STR00369## R.sup.5 is alkyl; Z.sup.1 and 1b, Z.sup.2b, and Z.sup.3b optional substituents independently selected from (1) R.sup.10, where R.sup.10 is (i) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl; (ii) a group (i) which is itself substituted by one or more of the same or different groups (i); or (iii) a group (i) or (ii) which is independently substituted by one or more of the following groups (2) to (13) of the definition of Z.sup.1, (2) --OH or --OR.sup.10, (3) --SH or --SR.sup.10, (4) --C(O).sub.tH, --C(O).sub.tR.sup.10, or --O--C(O)R.sup.10, where t is 1 or 2, (5) --SO.sub.3H, --S(O).sub.tR.sup.10, or S(O).sub.tN(R.sup.11)R.sup.10, (6) halo, (7) cyano, (8) nitro, (9)--U--N R.sup.12R.sup.13, (10) --U.sup.1--N(R.sup.11)--U.sup.2--N R.sup.12R.sup.13, (11) --U.sup.1--N(R.sup.14)--U.sup.2--R.sup.10, (12) --U.sup.1--N(R.sup.14)--U.sup.2--H, (13) oxo; U.sup.1 and U.sup.2 are each independently (1) a single bond, (2) --U.sup.3--S(O).sub.t--U.sup.4--, (3) --U.sup.3--C(O)--U.sup.4--, (4) --U.sup.3C(S)--U.sup.4--, (5) --U.sup.3--O--U.sup.4--, (6) --U--S--U.sup.4--, (7) --U.sup.3--O--C(O)--U.sup.4--, (8) --U.sup.3--C(O)--O--U.sup.4--, (9) --U--C(.dbd.NR.sup.15)--U.sup.4--, or (10) --U.sup.3--C(O)--C(O)--U.sup.4--; R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 (1) are each independently hydrogen or a group provided in the definition of Z.sup.1; or (2) R.sup.12 and R.sup.13 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (3) R.sup.12 or R.sup.13, together with R.sup.11, may be alkylene or alkenylene completing a 3- to 8-membered saturated or unsaturated ring together with the nitrogen atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (4) R.sup.12 and R.sup.13 together with the nitrogen atom to which they are attached may combine to form a group --N.dbd.C R.sup.16R.sup.17 where R.sup.16 and R.sup.17 are each independently H or a group provided in the definition of R.sup.10; and U.sup.3 and U.sup.4 are each independently (1) a single bond, (2) alkylene, (3) alkenylene, (4) alkynylene.

7. A compound having the formula, ##STR00370## or an enantiomer, diastereomer, or salt, thereof, wherein A is aryl optionally substituted with Z.sup.1, Z.sup.2 and/or one or more Z.sup.3; X is oxygen or sulfur; J is alkylene, alkenylene, or alkynylene any of which may be optionally substituted with Z.sup.1a, Z.sup.2a and/or one or more Z.sup.3a; R.sup.1 is hydrogen, alkyl, alkenyl or alkynyl any of which may be optionally substituted with Z.sup.1b, Z.sup.2b and/or one or more Z.sup.3b; R.sup.2 is (a) alkyl, alkoxy or aryloxy, each group optionally substituted with Z.sup.1c, Z.sup.2c and/or one or more Z.sup.3c; (b) cyano or nitro; or (c) --C(O)R.sup.5 or C(O)OR.sup.5; R.sup.3 is a group of formula ##STR00371## R.sup.4 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1e, Z.sup.2e and/or one or more Z.sup.3e; R.sup.5 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1f, Z.sup.2f and/or one or more Z.sup.3f; R.sup.6, R.sup.7 and R.sup.8 are independently (a) hydrogen; (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1g, Z.sup.2g and one or more Z.sup.3; or (c) R.sup.6 and R.sup.7 are optionally taken together to form (i) an alkylene or alkenylene group; (ii) --N.dbd.CR.sup.9--; (iii) --N.dbd.N--; or R.sup.9 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1g, Z.sup.2g and/or one or more Z.sup.3g; Z.sup.1-1g, Z.sup.2-2g, and Z.sup.3-3g are optional substituents independently selected from (1) R.sup.10, where R.sup.10 is (i) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl; (ii) a group (i) which is itself substituted by one or more of the same or different groups (i); or (iii) a group (i) or (ii) which is independently substituted by one or more of the following groups (2) to (13) of the definition of Z.sup.1, (2) --OH or --OR.sup.10, (3) --SH or --SR.sup.10, (4) --C(O).sub.tH, --C(O).sub.tR.sup.10, or --O--C(O)R.sup.10, where t is 1 or 2, (5) --SO.sub.3H, --S(O).sub.tR.sup.10, or S(O).sub.tN(R.sup.11)R.sup.10, (6) halo, (7) cyano, (8) nitro, (9) --U.sup.1--N R.sup.12R.sup.13, (10) --U.sup.1--N(R.sup.11)--U.sup.2--N R.sup.12R.sup.13, (11) --U.sup.1--N(R.sup.14)--U.sup.2--R.sup.10, (12) --U.sup.1--N(R.sup.14)--U.sup.2--H, (13) oxo; U.sup.1 and U.sup.2 are each independently (1) a single bond, (2) --U.sup.3--S(O).sub.t--U.sup.4--, (3) --U.sup.3--C(O)--U.sup.4--, (4) --U.sup.3--C(S)--U.sup.4--, (5) --U.sup.3--O--U.sup.4--, (6) --U.sup.3--S--U.sup.4--, (7) --U.sup.3--O--C(O)--U.sup.4--, (8) --U.sup.3--C(O)--O--U.sup.4--, (9) --U.sup.3--C(.dbd.NR.sup.15)--U.sup.4--, or (10) --U.sup.3--C(O)--C(O)--U.sup.4--; R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 (1) are each independently hydrogen or a group provided in the definition of Z.sup.1; or (2) R.sup.12 and R.sup.13 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (3) R.sup.12 or R.sup.13, together with R.sup.11, may be alkylene or alkenylene completing a 3- to 8-membered saturated or unsaturated ring together with the nitrogen atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (4) R.sup.12 and R.sup.13 together with the nitrogen atom to which they are attached may combine to form a group --N.dbd.C R.sup.16 R.sup.17 where R.sup.16 and R.sup.17 are each independently H or a group provided in the definition of R.sup.10; and U.sup.3 and U.sup.4 are each independently (1) a single bond, (2) alkylene, (3) alkenylene, (4) alkynylene.

8. A compound having the formula, ##STR00372## or an enantiomer, diastereomer, or salt, thereof, wherein A is aryl optionally substituted with Z.sup.1, Z.sup.2 and/or one or more z.sup.3; X is oxygen or sulfur; J is alkylene, alkenylene, or alkynylene any of which may be optionally substituted with Z.sup.1a, Z.sup.2a and/or one or more Z.sup.3a; R.sup.1 is hydrogen, alkyl, alkenyl or alkynyl any of which may be optionally substituted with Z.sup.1b, Z.sup.2b and/or one or more Z.sup.3b; R.sup.2 is (a) alkyl, alkoxy or aryloxy, each group optionally substituted with Z.sup.1c, Z.sup.2c and/or one or more Z.sup.3c; (b) cyano or nitro; or (c) --C(O)R.sup.5 or C(O)OR.sup.5; R.sup.3 is a group of formula ##STR00373## ##STR00374## R.sup.4 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1e, Z.sup.2e and/or one or more Z.sup.3e; R.sup.5 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1f, Z.sup.2f and/or one or more Z.sup.3f; R.sup.6, R.sup.7 and R.sup.8 are independently (a) hydrogen; (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1g, Z.sup.2g and one or more Z.sup.3g; or (c) R.sup.6 and R.sup.7 are optionally taken together to form (i) an alkylene or alkenylene group; (ii) N.dbd.CR.sup.9--; (iii) N.dbd.N--; or R.sup.9 is (a) hydrogen; or (b) alkyl, cycloalkyl, aryl, heterocyclo, heteroaryl, (aryl)alkyl, (cycloalkyl)alkyl, (heterocyclo)alkyl or (heteroaryl)alkyl, any of which may be optionally substituted with Z.sup.1g, Z.sup.2g and/or one or more Z.sup.3g; Z.sup.1-1g, Z.sup.2-2g, and Z.sup.3-3g are optional substituents independently selected from (1) R.sup.10, where R.sup.10 is (i) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl; (ii) a group (i) which is itself substituted by one or more of the same or different groups (i); or (iii) a group (i) or (ii) which is independently substituted by one or more of the following groups (2) to (13) of the definition of Z.sup.1, (2) --OH or --OR.sup.10, (3) --SH or --SR.sup.10, (4) --C(O).sub.tH, --C(O).sub.tR.sup.10, or --O--C(O)R.sup.10, where t is 1 or 2, (5) --SO.sub.3H, --S(O).sub.tR.sup.10, or S(O).sub.tN(R.sup.11)R.sup.10, (6) halo, (7) cyano, (8) nitro, (9) --U.sup.1--N R.sup.12R.sup.13, (10) --U.sup.1--N(R.sup.11)--U.sup.2--N R.sup.12R.sup.13, (11) --U.sup.1--N(R.sup.14)--U.sup.2--R.sup.10, (12) --U.sup.1--N(R.sup.14)--U.sup.2--H, (13) oxo; U.sup.1 and U.sup.2 are each independently (1) a single bond, (2) --U.sup.3--S(O).sub.t--U.sup.4--, (3) --U.sup.3--C(O)--U.sup.4--, (4) --U.sup.3--C(S)--U.sup.4--, (5) --U.sup.3--O--U.sup.4--, (6) --U.sup.3--S--U.sup.4--, (7) --U.sup.3--O--C(O)--U.sup.4--, (8) --U.sup.3--C(O)--O--U.sup.4--, (9) --U.sup.3--C(.dbd.NR.sup.15)--U.sup.4--, or (10) --U.sup.3--C(O)--C(O)--U.sup.4--; R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 (1) are each independently hydrogen or a group provided in the definition of Z.sup.1; or (2) R.sup.12 and R.sup.13 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (3) R.sup.12 or R.sup.13, together with R.sup.11, may be alkylene or alkenylene completing a 3- to 8-membered saturated or unsaturated ring together with the nitrogen atoms to which they are attached, which ring is unsubstituted or substituted with one or more groups listed in the definition of Z.sup.1, or (4) R.sup.12 and R.sup.13 together with the nitrogen atom to which they are attached may combine to form a group --N.dbd.C R.sup.16R.sup.17 where R.sup.16 and R.sup.17 are each independently H or a group provided in the definition of R.sup.10; and U.sup.3 and U.sup.4 are each independently (1) a single bond, (2) alkylene, (3) alkenylene, (4) alkynylene; provided that if R.sup.3 is ##STR00375## then J is methylene.

9. A compound of claim 8, or an enantiomer, diastereomer, or salt thereof, wherein: J is methylene; and R.sup.3 is selected from ##STR00376##

10. A compound selected from (i) 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-phenoxybenzoyl)amino]propyl]-6- -(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[[4-(2-pyridinyloxy)phenyl]sulfon- yl]amino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester, trifluoroacetic acid salt (1:1); 4-[(2-Aminoethoxy)methyl]-6-(2-chlorophenyl)-1,2,3,6-tetrahydro-1-[3-[met- hyl(1-oxo-3-phenylpropyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, ethyl ester; 4-[(2-Aminoethoxy)methyl]-6-(2-chlorophenyl)-1,2,3,6-tetrahydro-1-[3-[met- hyl(4-phenoxybenzoyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, ethyl ester; 4-[(2-Aminoethoxy)methyl]-6-(3,5-dichlorophenyl)-1,2,3,6-tetrahydro-1-[3-- [methyl(4-phenoxybenzoyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 4-[(2-Aminoethoxy)methyl]-6-(3,5-dichlorophenyl)-1,2,3,6-tetrahydro-1-[3-- [methyl(4-phenoxybenzoyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, methyl ester; 4-[(2-Aminoethoxy)methyl]-6-(3,5-dichlorophenyl)-1,2,3,6-tetrahydro-1-[3-- [methyl(4-phenoxybenzoyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, ethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[[3-[[methyl(3-phenylpro- pyl)amino]carbonyl]phenyl]methyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-(Benzoylmethylamino)propyl]-1,2,3,6-tetrahydro-4-methyl-6-(3-nitroph- enyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(phenylacetyl)amino]propyl]-6-(3-- nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(Diphenylacetyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-6-(- 3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(1-oxo-3-phenylpropyl)amino]propy- l]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(4-Chlorophenyl)acetyl]methylamino]propyl]-1,2,3,6-tetrahyd- ro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-pyridinylcarbonyl)amino]propyl- ]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(3-pyridinylcarbonyl)amino- ]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(2-Furanylcarbonyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-- 6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[(5-isoxazolylcarbonyl)methylamino]propyl]-4-meth- yl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(Cyclopentylacetyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-- methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(Cyclohexylcarbonyl)methylamino]propyl]-1,2,3,6-tetrahydro-4- -methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(2-methylbenzoyl)amino]pro- pyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3-Fluorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-me- thyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(2-Fluorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-me- thyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(4-Fluorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-me- thyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(2-thienylacetyl)amino]pro- pyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3-Cyclopentyl-1-oxopropyl)methylamino]propyl]-1,2,3,6-tetra- hydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3-Cyanobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-6-(- 3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(4-Cyanobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-6-(- 3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(2E)-1-oxo-3-phenyl-2-propenyl]a- mino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(4-Ethylbenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-6-(- 3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[(2-methoxybenzoyl)methylamino]propyl]-4-methyl-6- -(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[(3-methoxybenzoyl)methylamino]propyl]-4-methyl-6- -(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(phenoxyacetyl)amino]propyl]-6-(3- -nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(4-Fluorophenyl)acetyl]methylamino]propyl]-1,2,3,6-tetrahydro-4-me- thyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3-Chlorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-me- thyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(2,4-Difluorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-- 4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(2,3-Difluorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methy- l-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(2-phenylcyclopropyl)carb- onyl]amino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-propylbenzoyl)amino]propyl]-6-- (3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(1-oxo-2-phenylbutyl)amino]propyl- ]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(1,3-Benzodioxol-5-ylcarbonyl)methylamino]propyl]-1,2,3,6-te- trahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[[((3-methoxyphenyl)acetyl]methylamino]propyl]-4-- methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[[(4-methoxyphenyl)acetyl]methylamino]prop- yl]-4-methyl-6-(3nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(phenylmethoxy)acetyl]amino]prop- yl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(2-quinoxalinylcarbonyl)am- ino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(Benzo[b]thien-2-ylcarbonyl)methylamino]propyl]-1,2,3,6-tetrahydro-- 4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[4-(1,1-Dimethylethyl)benzoyl]methylamino]propyl]-1,2,3,6-tetrahydr- o-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3,5-Dimethoxybenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-meth- yl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(4-Chlorophenoxy)acetyl]methylamino]propyl]-1,2,3,6-tetrahy- dro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[3-(trifluoromethyl)benzoyl]amino- ]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3,4-Dichlorobenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methy- l-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[([1,1'-Biphenyl]-4-ylcarbonyl)methylamino]propyl]-1,2,3,6-te- trahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[[1-(4-Chlorophenyl)cyclopentyl]carbonyl]methylamino]propyl]-1,2,3,- 6-tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[(4-iodobenzoyl)methylamino]propyl]-4-methyl-6-(3- -nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(3,4-Dimethylbenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-4-methy- l-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[(2,3-Dimethylbenzoyl)methylamino]propyl]-1,2,3,6-tetrahydro-- 4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[[6-(4-methylphenoxy)-3-pyridinyl- ]carbonyl]amino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(1-oxo-4-phenoxybutyl)amino]propy- l]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(1-naphthalenylacetyl)amin- o]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[Acetyl(phenylmethyl)amino]propyl]-1,2,3,6-tetrahydro-4-methyl-6-(3-- nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(3-phenoxybenzoyl)amino]propyl]-6- -(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(3-phenoxyphenyl)acetyl]amino]pr- opyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-phenoxybenzoyl)amino]pr- opyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-phenoxybenzoyl)amino]pr- opyl]-2-oxo-6-(2-pyridinyl)-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-phenoxybenzoyl)amino]pr- opyl]-6-(6-methyl-2-pyridinyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(4-phenoxybenzoyl)amino]propyl]-6- -(2-methyl-4-thiazolyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[4-(2-p- henoxyethoxy)benzoyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-1-[3-[[4-(4-hydroxyphenoxy)benzoyl]- methylamino]propyl]-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[4-(4-Chlorophenoxy)benzoyl]methylamino]propyl]-6-(3-chlorophenyl)-- 1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[4-(4-methylph- enoxy)benzoyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(cyclohexyloxy)benzoyl]methylamino]propyl]-1,- 2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[(4'-ethyl[1,1'-biphenyl]-4-yl)carbonyl]m- ethylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxyli- c acid, 1-methylethyl ester; 1-[3-[(4-Benzoylbenzoyl)methylamino]propyl]-6-(3-chlorophenyl)-1,2,3,6-te- trahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[(2,3-dihydro-5-benzofuranyl)carbonyl]methylamin- o]propyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[(2-dibenzofuranylcarbonyl)methylamino]propyl]-1,- 2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[4-[[2-- oxo-5-(trifluoromethyl)-1(2H)-pyridinyl]methyl]benzoyl]amino]propyl]-2-oxo- -5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[(4-ethoxybenzoyl)methylamino]propyl]-1,2,3,6-tet- rahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(1,1-dimethylethoxy)benzoyl]methylamino]propy- l]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[4-(trifluorom- ethoxy)benzoyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[4-(phenylmeth- oxy)benzoyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(4-phen- oxybenzoyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(2-cyclohexen-1-yloxy)benzoyl]methylam- ino]propyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-2-oxo-1-[3-[(4-phenoxybenz- oyl)amino]propyl]-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(phenoxyacetyl- )amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[(5-methyl-3-p- henyl-4-isoxazolyl)carbonyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[(2-phenylcycl- opropyl)carbonyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(2,4-difluorophenoxy)benzoyl]methylamino]prop- yl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[(4-ethoxybenzoyl)methylamino]propyl]-1,2,3,6-tet- rahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[4-[[(phenylam- ino)carbonyl]amino]benzoyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)benzo- yl]methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarbo- xylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(4-fluorophenoxy)benzoyl]methylamino]propyl]-- 1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(1-oxo-3,3-dip- henylpropyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(1-oxo-- 4-phenylbutyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(1-oxo-3-pheno- xypropyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(1-oxo-- 3-phenylpropyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[4-(4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)b- enzoyl]methylamino]propyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinec- arboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl(4-phenoxybenz- oyl)amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-1-[3-(2-oxo-3-phenyl-- 1-imidazolidinyl)propyl]-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-1-[3-(2-oxo-3-phenyl-- 1(2H)-pyridinyl)propyl]-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[2,3-Dihydro-2-oxo-3-(phenylmethyl)-1H-imidazol-1-yl]propyl]-1,2,3,6- -tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-(1,5-Dihydro-5-oxo-1-phenyl-4H-1,2,4-triazol-4-yl)propyl]-1,2,3,6-te- trahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-(4,5-Dihydro-5-oxo-4-phenyl-1H-1,2,4-triazol-1-yl)propyl]-1,2,3,6-te- trahydro-4-methyl-6-(3-mtrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester;

1-[3-(4,5-Dihydro-5-oxo-4-phenyl-1H-tetrazol-1-yl)propyl]-1,2,3,6-tetrahy- dro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-1-[3-[2-oxo-3-(phenyl- methyl)-1-imidazolidinyl]propyl]-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-(1,3-Dihydro-1,3-dioxo-2H-isoindol-2-yl)propyl]-1,2,3,6-tetrahydro-4- -methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[3-(4-Ethoxyphenyl)-2-oxo-1-imidazolidinyl]propyl]-1,2,3,6-te- trahydro-4-methyl-6-(nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-1-[3-(4-phenyl-1H-imi- dazol-1-yl)propyl]-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-1-[3-(2-oxo-3-phenyl-- 1-imidazolidinyl)propyl]-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[3-(2,4-difluorophenyl)-2-oxo-1-imidazolidinyl]pr- opyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[3-[4-(1,1-dimethylethyl)phenyl]-2-oxo-1-imidazol- idinyl]propyl]1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[3-[3-(1,1-dimethylethyl)phenyl]-2-oxo-1-imidazol- idinyl]propyl]1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[3-[4-(4-Chlorophenoxy)phenyl]-2-oxo-1-imidazolidinyl]propyl]-6-(3-c- hlorophenyl)-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1-[3-[[[(4-fluorophenyl)amino]carbonyl]methylamino]pro- pyl]-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(phenylamino)carbonyl]amino]prop- yl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[([1,1'-Biphenyl]-4-ylamino)carbonyl]methylamino]propyl]-6-(- 3-chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-1-(3-[[[[(4-methoxyphenyl)methyl]am- ino]carbonyl]methylamino]propyl]-4-methyl-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[[(4-phenoxyph- enyl)amino]carbonyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(phenoxycarbonyl)amino]propyl]-6-- (3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(1,1-Dimethylethoxy)carbonyl](phenylmethyl)amino]propyl]-1,2,3,6-t- etrahydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-4-methyl-1-[3-[methyl[(phenylmethox- y)carbonyl]amino]propyl]-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 6-(3-Chlorophenyl)-1,2,3,6-tetrahydro-1-[3-[[(4-methoxyphenoxy)car- bonyl]methylamino]propyl]-4-methyl-2-oxo-5pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(phenylsulfonyl)amino]propyl]-6-(- 3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(phenylmethyl)sulfonyl]amino]pro- pyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl(2-thienylsulfonyl)amino]p- ropyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(3-methylphenyl)sulfonyl]- amino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(2-methylphenyl)sulfonyl]amino]p- ropyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[(4-methylphenyl)sulfonyl]- amino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(2-Fluorophenyl)sulfonyl]methylamino]propyl]-1,2,3,6-tetrahydro-4-- methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(3-Fluorophenyl)sulfonyl]methylamino]propyl]-1,2,3,6-tetrah- ydro-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-4-methyl-1-[3-[methyl[[(E)-2-phenylethenyl]sulfonyl]am- ino]propyl]-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1-[3-[[(2,5-Dimethylphenyl)sulfonyl]methylamino]propyl]-1,2,3,6-tetrahydr- o-4-methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinecarboxylic acid, 1-methylethyl ester; 1,2,3,6-Tetrahydro-1-[3-[[(4-methoxyphenyl)sulfonyl]methylamino]propyl]-4- -methyl-6-(3-nitrophenyl)-2-oxo-5-pyrimidinec