Allergan, Inc.

Allergan Sales, Inc.

Allergen, Inc.

Mark Holoboski

Robert M Burk

Mari F Posner

David W Old

Yariv Donde

Michael E Garst

David Frederick Woodward

Vinh X Ngo

Larry Allen Wheeler

Wha-Bin Im

Scott M Whitcup

Jeremiah H Nguyen

June Chen

Achim H Krauss

Yanbin Liang

Achim H-p Krauss

Disclosed herein are compounds having formula (I) wherein a dashed line represents the presence or adsence of a bond; Y is an organic acid functional group, or an amide or ester thereof; or Y is hydroxymethyl or an ester thereof; or Y is a tetrazolyl functional group; A is &#x2014;(CH)&#x2014;, cis &#x2014;CHCH&#x2550;CH&#x2014;(CH)&#x2014;, or &#x2014;CHC&#x2550;C&#x2014;(CH)&#x2014;, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is &#x2014;(CH)&#x2014;Ar&#x2014;(CH)&#x2014;, wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 &#x2014;CH&#x2014; may be replaced by S or O, and 1 &#x2014;CH&#x2014;CH&#x2014; may be replaced by &#x2014;CH&#x2550;CH&#x2014; or &#x2014;C&#x2261;C&#x2014;; Uand Uare independently selected from &#x2014;H, &#x2550;O, &#x2014;OH, &#x2014;F, &#x2014;Cl, and &#x2014;CN; and B is aryl or heteroaryl, for use as acular hypotensive agent.

Therapeutic substituted cyclopentanes

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 &#x2014;(CH)&#x2014;, cis &#x2014;CHCH&#x2550;CH&#x2014;(CH)&#x2014;, or &#x2014;CHC&#x2550;C&#x2014;(CH)&#x2014;, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is &#x2014;(CH)&#x2014;Ar&#x2014;(CH)&#x2014; wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 &#x2014;CH&#x2014; may be replaced by S or O, and 1 &#x2014;CH&#x2014;CH&#x2014; may be replaced by &#x2014;CH&#x2550;CH&#x2014; or &#x2014;C&#x2261;C&#x2014;; Uand Uare independently selected from &#x2014;H, &#x2550;O, &#x2014;OH, &#x2014;F, &#x2014;Cl, and &#x2014;CN; and B is aryl or heteroaryl, for use as acular hypotensive agent. 

Disclosed herein are compounds represented by the formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Substituted cyclopentanes having prostaglandin activity

Compound having the formula below are disclosed herein: formula (I). Therapeutic methods, compositions, and medicaments related thereto are also disclosed. 

Therapeutic compounds

Compounds having a structure are disclosed herein. Compositions, methods, and medicaments related to the therapeutic use of these compounds are also disclosed.

Compounds comprising  Methods, compositions, and medicaments related thereto are also disclosed.

A method is disclosed herein comprising administering a compound and a second drug to an eye of a mammal for the treatment of glaucoma or the reduction of intraocular pressure, said compound represented by the general formula I; wherein A, B, D, X, Y, Z, R, Rand Rare as defined in the specification.

Combination therapy for glaucoma treatment

Disclosed herein are methods and compositions related to compound 1 or compound 2 or pharmaceutically acceptable salts, or prodrugs thereof, which are antagonists of a prostaglandin EPreceptor, or are prostaglandin EPantagonists.

[object Object]

The invention relates to the use of derivatives of E-type prostaglandins as EPagonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an &#x3b1; bonds, the solid triangle represents a &#x3b2; bond, the wavy segments represent &#x3b1; or &#x3b2; bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, Ris heteroaryl or a substituted heteroaryl radical, Rand Rare independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of COR, CONR, CHOR, CONRSOR, P(O)(OR) and wherein Ris selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.

Omega cycloalkyl 17-heteroaryl prostaglandin E2 analogs as EP2-receptor agonists

Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof;wherein Y, A, B, J, and E are further described. Methods, compositions, and medicaments related thereto are also disclosed.

2,3,4-substituted cyclopentanones as therapeutic agents

The invention relates to the use of derivatives of E-type prostaglandins as EPagonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I:wherein the hatched segment represents an &#x3b1; bonds, the solid triangle represents a &#x3b2; bond, the wavy segments represent &#x3b1; or &#x3b2; bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, Ris heteroaryl or a substituted heteroaryl radical, Rand Rare independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of COR, CONR, CHOR, CONRSOR, P(O)(OR) andwherein Ris selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.

&#x3c9;-cycloalkyl 17-heteroaryl prostaglandin E2 analogs as EP2-receptor agonists

The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound which is a EPagonist.

Growing community of inventors

Laguna Niguel, CA, United States of America

Mark Holoboski