Claims
- 1. A compound of the formula ##STR36## wherein X.sub.1 is (C(R.sub.1).sub.2).sub.n where R.sub.1 is independently H or alkyl of 1 to 6 carbons, and n is an integer between 0 and 2;
- Z is --(CR.sub.1 .dbd.CR.sub.1).sub.n' -- where n' is an integer having the value 3-5,
- R.sub.2 is hydrogen, lower alkyl of 1 to 6 carbons, F, Cl, Br, I, CF.sub.3, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons;
- R.sub.3 is hydrogen, lower alkyl of 1 to 6 carbons or F;
- m is an integer having the value of 0-3;
- o is an integer having the value of 0-3;
- A is (CH.sub.2).sub.q where q is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;
- B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or Si(C.sub.1-6 alkyl).sub.3, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons;, and
- R.sub.14 is (R.sub.15).sub.r -thienyl, and
- R.sub.15 is independently H, F, Cl, Br, I, NO.sub.2, N(R.sub.8).sub.2, N(R.sub.8)COR.sub.8, NR.sub.8 CON(R.sub.8).sub.2, OH, OCOR.sub.8, OR.sub.8, CN, COOH, COOR.sub.8 an alkyl group having 1 to 10 carbons, fluoro substituted alkyl group having 1 to 10 carbons, an alkenyl group having 1 to 10 carbons and 1 to 3 double bonds, alkynyl group having 1 to 10 carbons and 1 to 3 triple bonds, or a trialkylsilyl or trialkylsilyloxy group where the alkyl groups independently have 1 to 6 carbons with the proviso that when R.sub.14 is 2-thienyl then Z is not C(CH.sub.3).dbd.CH--CH.dbd.CH--C(CH.sub.3).dbd.CH--.
- 2. A compound in accordance with claim 1 where n is 1.
- 3. A compound in accordance with claim 1 where A is (CH.sub.2).sub.q.
- 4. A compound in accordance with claim 1 where B is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, or CONR.sub.9 R.sub.10.
- 5. A compound of the formula ##STR37## where R.sub.1 is independently H or alkyl of 1 to 6 carbons;
- Z is --(CR.sub.1 .dbd.CR.sub.1).sub.n' - where n' is an integer having the value of 3,
- R.sub.2 is hydrogen, lower alkyl of 1 to 6 carbons;
- R.sub.3 is hydrogen, lower alkyl of 1 to 6 carbons or F;
- m is an integer having the value of 0-3;
- o is an integer having the value of 0-4;
- A is (CH.sub.2).sub.q where q is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;
- B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or Si(C.sub.1-6 alkyl).sub.3, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons or (trimethylsilyl)alkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, and
- R.sub.14 is alkyl of 1-6 carbons, CH.sub.2 COOH, CH.sub.2 COOR.sub.8 or (R.sub.15).sub.r -heteroaryl where the heteroaryl group has 1 to 3 heteroatoms selected from the group consisting of O, S and N, r is an integer having the values of 0-5, and
- R.sub.15 is independently H, F, Cl, Br, I, NO.sub.2, N(R.sub.8).sub.2, OH, OCOR.sub.8, OR.sub.8, CN, COOH, COOR.sub.8, an alkyl group having 1 to 10 carbons, or fluoro substituted alkyl group having 1 to 10 carbons with the proviso that when R.sub.14 is 2-thienyl then Z is not C(CH.sub.3).dbd.CH--CH.dbd.CH--C(CH.sub.3).dbd.CH--.
- 6. A compound in accordance with claim 5 where A is (CH.sub.2).sub.q where q is 0 and where B is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, or CONR.sub.9 R.sub.10.
- 7. A compound in accordance with claim 5 where the R.sub.14 group is 2-thienyl.
BACKGROUND OF THE INVENTION
1. Cross Reference to Related Application
The present application is a divisional of application Ser. No. 08/667,663 filed on Jun. 21, 1996, to be issued as U.S. Pat. No. 5,773,594.
US Referenced Citations (113)
Foreign Referenced Citations (2)
Number |
Date |
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170105A |
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EPX |
0098591 |
Jan 1984 |
EPX |
Divisions (1)
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Number |
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Parent |
667663 |
Jun 1996 |
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