IP Library Granted Patent US 8,394,836
Granted Patent B2
US 8,394,836 · App. 12/746,104 · Granted Mar 12, 2013

Indoles and their therapeutic use

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Quick Facts
Patent No.
US 8,394,836
App. No.
12/746,104
Granted
Mar 12, 2013
Kind
B2
Abstract

Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is —SO 2 — or *—SO 2 NR 3 — wherein the bond marked with an asterisk is attached to Ar 1 ; R 1 is hydrogen, fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; R 3 is hydrogen, C 1 C 8 alkyl or C 3 -C 7 cycloalkyl; Ar 1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C 3 -C 7 cycloalkyl, —O(C 1 -C 4 alkyl) or C 1 C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar 2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C 3 -C 3 -C 7 cycloalkyl, —O(C 1 -C 4 alkyl) or C 1 C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.

Claims (4)

1. A compound that is {5-fluoro-2-methyl-3[3-(pyridine-2-sulfonyl)thiophen-2-ylmethyl]indol-1-yl}acetic acid or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound as claimed in claim 1 and a pharmaceutically acceptable carrier.

3. A method for treating a disease selected from asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, comprising administering to a patient having such disease an effective amount of a compound as claimed in claim 1 .

4. A method for treating a disease selected from psoriasis, atopic and non-atopic dermatitis, Crohn's disease, ulcerative colitis, and irritable bowel disease, comprising administering to a patient having such disease an effective amount of a compound as claimed in claim 1 .

Assignments (4)
RELEASE OF SECURITY INTEREST IN INTELLECTUAL PROPERTY COLLATERAL AT REEL/FRAME NO. 49081/0335 Recorded May 3, 2024
From: MIDCAP FINANCIAL TRUST, AS AGENT
To: GOSSAMER BIO, INC.; GOSSAMER BIO SERVICES, INC.; GB001, INC.; GB002, INC.; GB003, INC.; GB004, INC.; GB005, INC.; GB007, INC.; GB008, INC.
Reel/Frame 067310/0307 →
SECURITY INTEREST Recorded May 3, 2019
From: GOSSAMER BIO, INC.; GOSSAMER BIO SERVICES, INC.; GB001, INC.; GB002, INC.; GB003, INC.; GB004, INC.; GB005, INC.; GB006, INC.; GB007, INC.
To: MIDCAP FINANCIAL TRUST, AS AGENT
Reel/Frame 049081/0335 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 23, 2019
From: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
To: GB001, INC.
Reel/Frame 048974/0193 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2011
From: HYND, GEORGE; MONTANA, JOHN GARY; FINCH, HARRY; ARIENZO, ROSA; AVITABILE-WOO, BARBARA; DOMOSTOJ, MATHIAS
To: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
Reel/Frame 025571/0707 →