Claims
- 1. A compound represented by the following formula 1:
- 2. A compound represented by the following formula 1:
- 3. A compound represented by the following formula 1:
- 4. A compound represented by the following formula 1:
- 5. A compound represented by the following formula 1:
- 6. A compound represented by the following formula 1:
- 7. The compound of claim 1 that is 3-(3,5-dimethoxyphenyl)-2-{4-[4-(2,4-dioxothiazolidin-5-ylmethyl)-phenoxy]-phenyl}-acrylic acid.
- 8. The compound of claim 1 that is 3-(3,5-dimethoxy-phenyl)-2-{4-[4-(2,4-dioxothiazolidin-5-ylmethyl)-phenoxy]-phenyl}-acrylamide.
- 9. The compound of claim 1 that is 3-(3,5-dimethoxy-phenyl)-2-{4-[4-(2,4-dioxothiazolidin-5ylmethyl)-phenoxy]-phenyl}-N,N-dimethyl-acrylamide.
- 10. A pharmaceutical composition comprising:
a) a compound represented by the following formula 1: 33 wherein Z is 34n, m, q and r independently represent integers from zero to 4 provided that n+m≦4 and q+r≦4; p and s independently represent integers from zero to 5 provided that p+s≦5; a and b represent double bonds which may be present or absent; when present, the double bonds may be in the E or Z configuration and, when absent, the resulting stereocenters may have the R- or S-configuration; R and R′ each independently represent a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″;
—CONR2″″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R″ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′″ independently represents a linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; or —(CH2)x—Ar, where x represents an integer from 1 to 6 and Ar represents aryl; R″″ independently represents a hydrogen atom; optionally substituted C1-C20 alkyl; optionally substituted C1-C20 alkoxy; optionally substituted C2-C20 alkenyl; optionally substituted C6-C10 aryl; or NR2″″ represents a cyclic moiety; Z′ represents a hydrogen atom or a pharmaceutically acceptable counter-ion; A, A′ and A″ each independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkoxy; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; halo; or hydroxy; B, B′ and B″ each independently represent; C2-C20 alkenoyl; aroyl; aralkanoyl; nitro; optionally substituted, linear or branched C1-C20 alkyl; or optionally substituted, linear or branched C2-C20 alkenyl; or A and B jointly, A′ and B′ jointly, or A″ and B″ jointly, independently represent a methylenedioxy or ethylenedioxy group; and X and X′ independently represent >NH, >NR′″, —O—, or —S—; and b) a physiologically acceptable carrier.
- 11. A pharmaceutical composition comprising:
a) a compound represented by the following formula 1: 35 wherein Z is 36H; A″; or B″; n, m, q and r independently represent integers from zero to 4 provided that n+m≦4 and q+r≦4; p and s independently represent integers from zero to 5 provided that p+s≦5; a and b represent double bonds which may be present or absent; when present, the double bonds may be in the E or Z configuration and, when absent, the resulting stereocenters may have the R- or S-configuration; R and R′ each independently represent a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; —CONR2″″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R″ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′″ independently represents a linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; or —(CH2)x—Ar, where x represents an integer from 1 to 6 and Ar represents aryl; R″″ independently represents a hydrogen atom; optionally substituted C1-C20 alkyl; optionally substituted C1-C20 alkoxy; optionally substituted C2-C20 alkenyl; optionally substituted C6-C10 aryl; or NR2″″ represents a cyclic moiety; Z′ represents a hydrogen atom or a pharmaceutically acceptable counter-ion; A, and A′ each independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkoxy; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; halo; or hydroxy; A″ independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; or halo; B, B′ and B″ each independently represent; C2-C20 alkenoyl; aroyl; aralkanoyl; nitro; optionally substituted, linear or branched C1-C20 alkyl; or optionally substituted, linear or branched C2-C20 alkenyl; or A and B jointly, A′ and B′ jointly, or A″ and B″ jointly, independently represent a methylenedioxy or ethylenedioxy group; and X and X′ independently represent >NH, >NR′″, —O—, or —S—; and b) a physiologically acceptable carrier.
- 12. A pharmaceutical composition comprising:
a) a compound represented by the following formula 1: 37 wherein Z is 38 or 39n, m, q and r independently represent integers from zero to 4 provided that n+m≦4 and q+r≦4; p and s independently represent integers from zero to 5 provided that p+s≦5; a, b and c represent double bonds which may be present or absent; when present, the double bonds may be in the E or Z configuration and, when absent, the resulting stereocenters may have the R- or S-configuration; R independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; —CONR2″″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OR′″; —CONR2″″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R″ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′″ independently represents a linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; or —(CH2)x—Ar, where x represents an integer from 1 to 6 and Ar represents aryl; R″″ independently represents a hydrogen atom; optionally substituted C1-C20 alkyl; optionally substituted C1-C20 alkoxy; optionally substituted C2-C20 alkenyl; optionally substituted C6-C10 aryl; or NR2″″ represents a cyclic moiety; Z′ represents a hydrogen atom or a pharmaceutically acceptable counter-ion; A, A′ and A″ each independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkoxy; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; halo; or hydroxy; B, B′ and B″ each independently represent; C2-C20 alkenoyl; aroyl; aralkanoyl; nitro; optionally substituted, linear or branched C1-C20 alkyl; or optionally substituted, linear or branched C2-C20 alkenyl; or A and B jointly, A′ and B′ jointly, or A″ and B″ jointly, independently represent a methylenedioxy or ethylenedioxy group; and X and X′ independently represent >NH, >NR′″, —O—, or —S—; and b) a physiologically acceptable carrier.
- 13. A pharmaceutical composition comprising:
a) a compound represented by the following formula 1: 40 wherein Z is 41n, m, q and r independently represent integers from zero to 4 provided that n+m≦4 and q+r≦4; p and s independently represent integers from zero to 5 provided that p+s≦5; a and b represent double bonds which may be present or absent; when present, the double bonds may be in the E or Z configuration and, when absent, the resulting stereocenters may have the R- or S-configuration; R and R′ each independently represent a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R″ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′″ independently represents a linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; or —(CH2)x—Ar, where x represents an integer from 1 to 6 and Ar represents aryl; Z′ represents a hydrogen atom or a pharmaceutically acceptable counter-ion; A, A′ and A″ each independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkoxy; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; halo; or hydroxy; B, B′ and B″ each independently represent; C2-C20 alkenoyl; aroyl; aralkanoyl; nitro; optionally substituted, linear or branched C1-C20 alkyl; or optionally substituted, linear or branched C2-C20 alkenyl; or A and B jointly, A′ and B′ jointly, or A″ and B″ jointly, independently represent a methylenedioxy or ethylenedioxy group; and X and X′ independently represent >NH, >NR′″, —O—, or —S—; and b) a physiologically acceptable carrier.
- 14. A pharmaceutical composition comprising:
a) a compound represented by the following formula 1: 42 wherein Z is 43H; A″; or B″; n, m, q and r independently represent integers from zero to 4 provided that n+m≦4 and q+r≦4; p and s independently represent integers from zero to 5 provided that p+s≦5; a and b represent double bonds which may be present or absent; when present, the double bonds may be in the E or Z configuration and, when absent, the resulting stereocenters may have the R- or S-configuration; R and R′ each independently represent a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R″ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′″ independently represents a linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; or —(CH2)x—Ar, where x represents an integer from 1 to 6 and Ar represents aryl; Z′ represents a hydrogen atom or a pharmaceutically acceptable counter-ion; A, and A′ each independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkoxy; C1C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; halo; or hydroxy; A″ independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; or halo; B, B′ and B″ each independently represent; C2-C20 alkenoyl; aroyl; aralkanoyl; nitro; optionally substituted, linear or branched C1-C20 alkyl; or optionally substituted, linear or branched C2-C20 alkenyl; or A and B jointly, A′ and B′ jointly, or A″ and B″ jointly, independently represent a methylenedioxy or ethylenedioxy group; and X and X′ independently represent >NH, >NR′″, —O—, or —S—; and b) a physiologically acceptable carrier.
- 15. A pharmaceutical composition comprising:
a) a compound represented by the following formula 1: 44 wherein Z is 45n, m, q and r independently represent integers from zero to 4 provided that n+m≦4 and q+r≦4; p and s independently represent integers from zero to 5 provided that p+s≦5; a, b and c represent double bonds which may be present or absent; when present, the double bonds may be in the E or Z configuration and, when absent, the resulting stereocenters may have the R- or S-configuration; R independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OR′″; —CONR2″″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R″ independently represents a hydrogen atom; linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; —CO2Z′; —CO2R′″; —NH2; —NHR′″; —NR2′″; —OH; —OR′″; halogen atom; optionally substituted linear or branched C1-C20 alkyl; optionally substituted linear or branched C2-C20 alkenyl; R′″ independently represents a linear or branched C1-C20 alkyl; linear or branched C2-C20 alkenyl; or —(CH2)x—Ar, where x represents an integer from 1 to 6 and Ar represents aryl; Z′ represents a hydrogen atom or a pharmaceutically acceptable counter-ion; A, A′ and A″ each independently represent a hydrogen atom; C1-C20 acylamino; C1-C20 acyloxy; C1-C20 alkanoyl; C1-C20 alkoxycarbonyl; C1-C20 alkoxy; C1-C20 alkylamino; C1-C20 alkylcarboxylamino; carboxyl; cyano; halo; or hydroxy; B, B′ and B″ each independently represent; C2-C20 alkenoyl; aroyl; aralkanoyl; nitro; optionally substituted, linear or branched C1-C20 alkyl; or optionally substituted, linear or branched C2-C20 alkenyl; or A and B jointly, A′ and B′ jointly, or A″ and B″ jointly, independently represent a methylenedioxy or ethylenedioxy group; and X and X′ independently represent >NH, >NR′″, —O—, or —S—; and b) a physiologically acceptable carrier.
- 16. The pharmaceutical composition of claim 10, wherein said compound represented by formula I is 3-(3,5-dimethoxyphenyl)-2-{4-[4-(2,4-dioxothiazolidin-5-ylmethyl)-phenoxy]-phenyl}-acrylic acid.
- 17. The pharmaceutical composition of claim 10, wherein said compound represented by formula I is 3-(3,5-dimethoxy-phenyl)-2-{4-[4-(2,4-dioxothiazolidin-5-ylmethyl)-phenoxy]-phenyl}-acrylamide.
- 18. The pharmaceutical composition of claim 10, wherein said compound represented by formula I is 3-(3,5-dimethoxy-phenyl)-2-{4-[4-(2,4-dioxo-thiazolidin-5ylmethyl)-phenoxy]-phenyl}-N,N-dimethyl-acrylamide.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This is a continuation of U.S. Ser. No. 09/843,167, filed Apr. 27, 2001, which is further a continuation-in-part of U.S. Ser. No. 09/785,554, filed Feb. 20, 2001, which is a continuation-in-part of U.S. Ser. No. 09/591,105, filed on Jun. 9, 2000, which is a continuation-in-part of Ser. No. 09/287,237, filed on Apr. 6, 1999, which is a continuation-in-part of Ser. No. 09/074,925, filed on May 8, 1998, the disclosures of said earlier applications being incorporated, in their entirety, herein by reference.
Continuations (1)
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Number |
Date |
Country |
Parent |
09843167 |
Apr 2001 |
US |
Child |
10808519 |
Mar 2004 |
US |
Continuation in Parts (4)
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Number |
Date |
Country |
Parent |
09785554 |
Feb 2001 |
US |
Child |
09843167 |
Apr 2001 |
US |
Parent |
09591105 |
Jun 2000 |
US |
Child |
09785554 |
Feb 2001 |
US |
Parent |
09287237 |
Apr 1999 |
US |
Child |
09591105 |
Jun 2000 |
US |
Parent |
09074925 |
May 1998 |
US |
Child |
09287237 |
Apr 1999 |
US |