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Title:
CAPROLACTAM DERIVATIVES AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO2001068655
Kind Code:
A3
Abstract:
The invention involves derivatives of caprolactam of the formula (I) in which [A<1>], A<2> and R<1> have the meanings indicated in the description, their salts and their prodrugs. The invention also relates to the preparation of such compounds, synthetic intermediates, their use, and in particular, antagonists of the Src SH2 domain and inhibitors of bone resorption and pharmaceutical compounds containing such compounds.

Inventors:
DEPREZ PIERRE (FR)
LESUISSE DOMINIQUE (FR)
BENARD DIDIER (FR)
Application Number:
PCT/US2001/007935
Publication Date:
August 01, 2002
Filing Date:
March 12, 2001
Export Citation:
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Assignee:
ARIAD PHARMA INC (US)
DEPREZ PIERRE (FR)
LESUISSE DOMINIQUE (FR)
BENARD DIDIER (FR)
International Classes:
C07F9/12; C07F9/40; C07F9/553; C07K5/06; C07K5/065; A61K38/00; (IPC1-7): C07K5/065; A61K31/675; A61K38/05; C07C233/47; C07D223/12; C07F9/553; C07K5/06; C07K5/068
Domestic Patent References:
WO1997024339A11997-07-10
WO1999031066A11999-06-24
Foreign References:
FR2781483A12000-01-28
Other References:
NATCHUS M G ET AL: "Design and synthesis of conformationally-constrained MMP inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 8, no. 16, 18 August 1998 (1998-08-18), pages 2077 - 2080, XP004137222, ISSN: 0960-894X
ROBL J A ET AL: "DUAL METALLOPROTEASE INHIBITORS. 6. INCORPORATION OF BICYCLIC AND SUBSTITUTED MONOCYCLIC AZEPINONES AS DIPEPTIDE SURROGATES IN ANGIOTENSIN-CONVERTING ENZYME/NEUTRAL ENDOPEPTIDASE INHIBITORS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 39, no. 2, 19 January 1996 (1996-01-19), pages 494 - 502, XP000749701, ISSN: 0022-2623
CARLSTROM A-S ET AL: "PALLADIUM-CATALYZED SYNTHESIS OF DIDEHYDROAMINO ACID DERIVATIVES", SYNTHESIS, GEORG THIEME VERLAG. STUTTGART, DE, no. 6, 1 June 1989 (1989-06-01), pages 414 - 418, XP000026631, ISSN: 0039-7881
BEAULIEU P L ET AL: "Ligands for the tyrosine kinase p56lck SH2 domain;discovery of potent dipeptide derivatives with monocharge, nonhydrolyzable phosphate replacement", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 10, 20 May 1999 (1999-05-20), pages 1757 - 1766, XP002148488, ISSN: 0022-2623
TONG ET AL: "Carboxymethyl-phenylalanine as a replacement for phosphotyrosine in SH2 domain binding", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, US, vol. 273, no. 32, 7 August 1998 (1998-08-07), pages 20238 - 20242, XP002143951, ISSN: 0021-9258
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