Invention Grant
- Patent Title: Isoxazole compounds as inhibitors of heat shock proteins
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Application No.: US16528278Application Date: 2019-07-31
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Publication No.: US11234987B2Publication Date: 2022-02-01
- Inventor: Martin James Drysdale , Brian William Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen Elizabeth James , Kwai Ming Cheung , Thomas Peter Matthews
- Applicant: Vernalis (R&D) Ltd. , The Institute of Cancer Research , Cancer Research Technology Limited
- Applicant Address: GB Great Abington; GB London; GB London
- Assignee: Vernalis (R&D) Ltd.,The Institute of Cancer Research,Cancer Research Technology Limited
- Current Assignee: Vernalis (R&D) Ltd.,The Institute of Cancer Research,Cancer Research Technology Limited
- Current Assignee Address: GB Great Abington; GB London; GB London
- Agency: Banner & Witcoff, Ltd.
- Priority: GB0303105 20030211,GB0306560 20030321,GB0313751 20030613
- Main IPC: A61P25/14
- IPC: A61P25/14 ; A61P25/28 ; A61P17/06 ; A61P17/00 ; A61P9/10 ; A61P15/00 ; A61P43/00 ; A61P25/00 ; A61P3/10 ; A61P35/00 ; A61P19/02 ; A61P29/00 ; A61P27/02 ; A61P11/06 ; A61P1/00 ; C07D495/04 ; C07D261/10 ; C07D261/08 ; C07D417/04 ; C07D413/04 ; C07D413/10 ; A61K31/42 ; A61K31/4439 ; A61K31/427 ; A61K31/541 ; A61K31/4709 ; A61K31/496 ; A61K31/5377 ; A61K31/454 ; A61K31/422 ; A61P31/12

Abstract:
Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO.sub.2-, —C(═O)O—, —C(═O)NRA—, —C(═S) NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
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