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1. (WO2004002956) ASYMMETRIC SYNTHESIS OF AMINO-PYRROLIDINONES AND A CRYSTALLINE, FREE-BASE AMINO-PYRROLIDINONE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2004/002956    International Application No.:    PCT/US2003/007920
Publication Date: 08.01.2004 International Filing Date: 14.03.2003
IPC:
C07D 215/14 (2006.01), C07D 401/12 (2006.01)
Applicants: BRISTOL MYERS SQUIBB COMPANY [US/US]; P. O. Box 4000, Route 206 and Provinceline Road, Princeton, NJ 08543-4000 (US) (For All Designated States Except US).
CAMPAGNA, Silvio [US/US]; (US) (For US Only).
SAVAGE, Scott, A. [US/US]; (US) (For US Only).
BORDAWEKAR, Shaliendra [IN/US]; (US) (For US Only).
MADUSKUIE, Thomas, P. [US/US]; (US) (For US Only).
WALTERMIRE, Robert, E. [US/US]; (US) (For US Only).
DESIKAN, Sridhar [IN/US]; (US) (For US Only).
ANDERSON, Stephen, R. [US/US]; (US) (For US Only)
Inventors: CAMPAGNA, Silvio; (US).
SAVAGE, Scott, A.; (US).
BORDAWEKAR, Shaliendra; (US).
MADUSKUIE, Thomas, P.; (US).
WALTERMIRE, Robert, E.; (US).
DESIKAN, Sridhar; (US).
ANDERSON, Stephen, R.; (US)
Agent: BELFIELD, Jing; Bristol-Myers Squibb Company, P.O. Box 4000, Princeton, NJ 08543-4000 (US)
Priority Data:
60/392,440 28.06.2002 US
60/400,411 01.08.2002 US
Title (EN) ASYMMETRIC SYNTHESIS OF AMINO-PYRROLIDINONES AND A CRYSTALLINE, FREE-BASE AMINO-PYRROLIDINONE
(FR) SYNTHESE ASYMETRIQUE D'AMINO-PYRROLIDINONES ET AMINO-PYRROLIDINONE CRISTALLIN A BASE LIBRE
Abstract: front page image
(EN)A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described.(I) These compounds are useful as intermediates for MMP and TACE inhibitors.Crystalline, free-base form of Compound J ((2R)-2-((3R)-3-amino-3-{-[(2-methyl-4-quinolinyl)methoxy]phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide): (II) which is useful as a TACE inhibitor, pharmaceutical compositions comprising the same, and methods of using the same for treating inflammatory diseases are also described.
(FR)L'invention concerne un nouveau procédé de synthèse asymétrique d'un amino-pyrrolidinone du type indiqué ci-dessous. Ces composés servent d'intermédiaires pour des inhibiteurs de MMP et TACE. L'invention concerne également la forme cristalline à base libre du composé J ((2R)-2-((3R)-3-amino-3-{-[(2-méthyl-4-quinolinyl)méthoxy]phényl}-2-oxopyrrolidinyl)-N-hydroxy-4-méthylpentanamide), qui peut servir d'inhibiteur de TACE, des compositions pharmaceutiques la comprenant, ainsi que leurs procédés d'utilisation pour traiter des maladies inflammatoires.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NI, NO, NZ, OM, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)