Disclosed herein are compounds having the formula (I) wherein a dashed line represents the presence or absence of a bond; Y is an organic acid functional group, or an amide or ester thereof; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2CH═C
Disclosed herein are compounds having the formula (I) wherein a dashed line represents the presence or absence of a bond; Y is an organic acid functional group, or an amide or ester thereof; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2CH═CH—(CH2)3—, or —CH2C═C—(CH2)3—, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 —CH2— may be replaced by S or O, and 1 —CH2—CH2— may be replaced by —CH═CH— or —C≡C—; U1 and U2 are independently selected from —H, ═O, —OH, —F, —Cl, and —CN; and B is aryl or heteroaryl, for use as acular hypotensive agent.
대표청구항▼
1. A compound having a formula or a pharmaceutically acceptable salt thereof, wherein a dashed line represents the presence or absence of a bond;Y is COR4 or CONR5R6, wherein R4, R5, and R6 are independently H or C2-C6 alkyl; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional
1. A compound having a formula or a pharmaceutically acceptable salt thereof, wherein a dashed line represents the presence or absence of a bond;Y is COR4 or CONR5R6, wherein R4, R5, and R6 are independently H or C2-C6 alkyl; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group;A is cis —CH2CH═CH—(CH2)3— or —CH2C≡C—(CH2)3—, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 —CH2— may be replaced by S or O, and 1 —CH2—CH2— may be replaced by —CH═CH— or —C≡C—;U1 and U2 are independently selected from —H, ═O, —OH, —F, —Cl, and —CN; andB is aryl or heteroaryl,provided that if U1 is ═O, U2 is not —OH or —H. 2. A compound having a formula or a pharmaceutically acceptable salt thereof, wherein a dashed line represents the presence or absence of a bond;Y is CO2R4 or CONR5R6, wherein R4, R5, and R6 are independently H or C2-C6 alkyl; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group;A is cis —CH2CH═CH—(CH2)3— or —CH2C≡C—(CH2)3—, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 —CH2— may be replaced by S or O, and 1 —CH2—CH2— may be replaced by —CH═CH— or —C≡C—;U1 is —H, —OH, —F, —Cl, or —CN;U2 is —H, ═O, —OH, —F, —Cl, or —CN; andB is aryl or heteroaryl. 3. A compound having a formula or a pharmaceutically acceptable salt thereof, wherein a dashed line represents the presence or absence of a bond;Y is CO2R4 or CONR5R6, wherein R4, R5, and R6 are independently H or C2-C6 alkyl; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group;U1 and U2 are independently selected from —H, ═O, —OH, —F, —Cl, and —CN; andB is aryl or heteroaryl. 4. The compound according to claim 1, wherein B is substituted phenyl or pyridinyl. 5. The compound according to claim 1, wherein U1 is ═O. 6. The compound according to claim 1, wherein U1 is —H. 7. The compound according to claim 1, wherein U1 is —OH. 8. The compound according to claim 1, wherein U1 is —F. 9. The compound according to claim 1, wherein U1 is —Cl. 10. The compound according to claim 1, wherein U1 is —CN. 11. The compound according to claim 5, wherein U2 is ═O. 12. The compound according to claim 6, wherein U2 is —H. 13. The compound according to claim 6, wherein U2 is —OH. 14. The compound according to claim 5, wherein U2 is —F. 15. The compound according to claim 5, wherein U2 is —Cl. 16. The compound according to claim 5, wherein U2 is —CN. 17. The compound of claim 2 having a formula 18. The compound according to claim 4 wherein B is substituted with substituents selected from F, Cl, C1-3 alkyl, and hydroxyalkyl having from 1 to 3 carbon atoms. 19. The compound of claim 17, wherein B is selected from 20. The compound of claim 19, said compound selected from: 21. A compound wherein the compound is selected from the group consisting of: 5-(3-((1R,2R,3R,5R)-5-chloro-2-(3,5-dichlorostyryl)-3-hydroxycyclopentyl)prop-1-enyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-(3-chloro-5-(hydroxymethyl)styryl)-3-hydroxycyclopentyl)propyl)-thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((E)-2-(5-chloropyridin-3-yl)vinyl)-3-hydroxycyclopentyl)propyl)-thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((E)-2-(2,6-dichloropyridin-4-yl)vinyl)-3-hydroxycyclopentyl)propyl)-thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((Z)-2-(2,6-dichloropyridin-4-yl)vinyl)-3-hydroxycyclopentyl)propyl)-thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((E)-3,5-difluorostyryl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((Z)-3,5-difluorostyryl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-(3,5-dimethylstyryl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-2-(3-(but-3-enyl)styryl)-5-chloro-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((E)-3-chloro-5-((E)-prop-1-enyl)styryl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-2-((Z)-3-chloro-5-((E)-prop-1-enyl)styryl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-3-hydroxy-2-(3-methylstyryl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2R,3R,5R)-5-chloro-3-hydroxy-2-((E)-2-(2-propylpyridin-4-yl)vinyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;2-(2-((1R,2R,3R,5R)-5-chloro-2-(3,5-dichlorostyryl)-3-hydroxycyclopentyl)ethylthio)thiazole-4-carboxylic acid;2-(2-((1R,2R,3R,5R)-2-((E)-3-(but-3-enyl)-5-chlorostyryl)-5-chloro-3-hydroxycyclopentyl)ethylthio)thiazole-4-carboxylic acid;2-(2-((1R,2R,3R,5R)-2-((Z)-3-(but-3-enyl)-5-chlorostyryl)-5-chloro-3-hydroxycyclopentyl)ethylthio)thiazole-4-carboxylic acid;5-(3-((1R,2S,3R)-3-hydroxy-5-oxo-2-(phenylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1S,2S,3R)-3-hydroxy-5-oxo-2-(phenylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-fluoro-3-hydroxy-2-(phenylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(phenylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;Isopropyl 5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(phenylethynyl)cyclopentyl)propyl)thiophene-2-carboxylate;5-(3-((1S,2S,3R,5R)-5-cyano-3-hydroxy-2-(phenylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R)-3-hydroxy-2-(phenylethynyl)-5-(trifluoromethyl)cyclopentyl)propyl)thiophene-2-carboxylic acid (faster eluting HPLC diastereomer);5-(3-((1R,2S,3R)-3-hydroxy-2-(phenylethynyl)-5-(trifluoromethyl)cyclopentyl)propyl)thiophene-2-carboxylic acid (slower eluting HPLC diastereomer);5-(3-((1R,2S,3R,5R)-5-chloro-2-((3,5-dichlorophenyl)ethynyl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-2-(3-ethylphenyl)ethynyl)-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-2-((3-(but-3-enyl)phenyl)ethynyl)-5-chloro-3-hydroxycyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(thiophen-2-ylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(thiophen-3-ylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(pyridin-2-ylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(pyridin-3-ylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(pyridin-4-ylethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;5-(3-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-((3-(3-hydroxypropyl)phenyl)ethynyl)cyclopentyl)propyl)thiophene-2-carboxylic acid;2-(2-((1R,2S,3R,5R)-5-chloro-2-((3,5-dichlorophenyl)ethynyl)-3-hydroxycyclopentyl)ethylthio)thiazole-4-carboxylic acid; and,2-(2-((1R,2S,3R,5R)-5-chloro-3-hydroxy-2-(phenylethynyl)cyclopentyl)ethylthio)thiazole-4-carboxylic acid;or a pharmaceutically acceptable salt thereof.
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이 특허에 인용된 특허 (12)
Buckler Robert T. (Edwardsburg MI) Garling David L. (Elkhart IN), C14Phenyl-substituted derivatives of prostaglandin analogues.
Cullen Thomas G. (Milltown NJ) Henrie ; II Robert N. (East Windsor NJ) Peake Clinton J. (Trenton NJ) Bennett Brian D. (Morrisville PA), Insecticidal substituted-2,4-diamino-5,6,7,8-tetrahydroquinazolines.
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