公开(公告)号：EP2585444B1

公开(公告)日：2014-10-22

申请号：EP11726792.2

申请日：2011-06-22

申请人： Boehringer Ingelheim International GmbH

发明人： HIMMELSBACH, Frank

IPC分类号： C07D265/12 ,  C07D265/18 ,  C07D413/08 ,  C07D413/10 ,  C07D413/14 ,  A61K31/537

CPC分类号： C07D221/20 ,  C07D265/12 ,  C07D265/18 ,  C07D413/10

公开(公告)号：EP2720546A4

公开(公告)日：2014-10-08

申请号：EP12800913

申请日：2012-06-15

申请人： GLAXOSMITHKLINE IP NO 2 LTD

发明人： BROOKS CARL ,  CHEUNG MUI ,  EIDAM HILARY SCHENCK ,  GOODMAN KRISTA B ,  HAMMOND MARLYS ,  HILFIKER MARK A ,  PATTERSON JACLYN R ,  STOY PATRICK ,  YE GUOSEN

IPC分类号： A61K31/422 ,  A61P9/04 ,  C07D413/08 ,  C07D413/14

CPC分类号： C07D413/14 ,  C07D263/52 ,  C07D413/06 ,  C07D413/08

公开(公告)号：EP2074105A4

公开(公告)日：2010-10-06

申请号：EP07815978

申请日：2007-10-12

申请人： NEUROMED PHARMACEUTICALS LTD

发明人： PAJOUHESH HASSAN ,  PAJOUHESH HOSSEIN ,  KAUL RAMESH

IPC分类号： C07D295/182 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61P1/00 ,  A61P3/00 ,  A61P3/10 ,  A61P9/00 ,  A61P13/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P35/00 ,  C07D401/08 ,  C07D403/08 ,  C07D403/12 ,  C07D413/08 ,  C07D413/14

CPC分类号： A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/09 ,  C07D211/16 ,  C07D211/58 ,  C07D213/75 ,  C07D241/04 ,  C07D295/185

公开(公告)号：EP1845981A4

公开(公告)日：2008-02-06

申请号：EP06718694

申请日：2006-01-17

申请人： ARIZONA BOARD REGENTS A BODY C

发明人： PETTIT GEORGE R ,  MELODY NOELEEN

IPC分类号： A61K31/443 ,  C07D413/08 ,  C07D471/04 ,  C07F9/28

CPC分类号： C07D491/04 ,  C07F9/65744

摘要： The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species Narcissus (Amaryllidaceae), as precursors in a novel synthesis method in which each of these compounds are selectively hydrogenated to produce trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c). Also described herein is a novel synthesis method for producing sodium narcistatin (11) from narciclasine (2a). Further described herein are certain novel 3,4-cyclic phosphate prodrugs, including sodium-7-deoxynarcistatin (8), sodium-7-deoxy-transdihydronarcistatin (9), and sodium transdihydronarcistatin (10).

公开(公告)号：EP1581515B1

公开(公告)日：2007-10-10

申请号：EP03814074.5

申请日：2003-12-16

申请人： Merck & Co., Inc.

发明人： WADDELL, Sherman, T. ,  SANTORELLI, Gina, M. ,  MALETIC, Milana, M. ,  LEEMAN, Aaron, H. ,  GU, Xin ,  GRAHAM, Donald, W. ,  BALKOVEC, James, M. ,  ASTER, Susan, D.

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D407/04 ,  C07D409/04 ,  C07D413/08 ,  A61K31/4196 ,  A61K31/4245 ,  A61P3/10

CPC分类号： C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D403/08 ,  C07D405/04 ,  C07D409/04 ,  C07D413/08 ,  C07D417/08

摘要： Triazole derivatives of structural formula (I) are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

公开(公告)号：EP1760079A1

公开(公告)日：2007-03-07

申请号：EP05745210.4

申请日：2005-05-12

申请人： Shanghai Target Drug Co., Ltd.

发明人： PEI, Gang ,  MA, Dawei ,  CHEN, Li ,  YU, Shanghai ,  LI, Ben ,  DONG, Fang ,  LV, Yanhui ,  CHEN, Renhai ,  ZHANG, Jin

IPC分类号： C07D401/06 ,  C07D403/08 ,  C07D413/08 ,  A61K31/4025 ,  A61K31/435 ,  A61P31/18 ,  A61P1/00 ,  A61P17/00 ,  A61P19/00

CPC分类号： C07D405/14 ,  C07D401/06 ,  C07D405/04

摘要： The present invention discloses the compounds of formula I or their pharmaceutically acceptable salts, which are useful as CCR5 antagonists. The preparation and use of the compounds of formula I, pharmaceutical composition containing the same are also disclosed. Furthermore, the present invention discloses an intermediate for the preparation of the compounds of formula I.

摘要翻译： 本发明公开了可用作CCR5拮抗剂的式I化合物或其药学上可接受的盐。 还公开了式I化合物的制备和使用，其含有该化合物的药物组合物。 此外，本发明公开了制备式I化合物的中间体。

公开(公告)号：EP1678167A1

公开(公告)日：2006-07-12

申请号：EP04795145.4

申请日：2004-10-15

申请人： INCYTE CORPORATION

发明人： LI, Yun-Long ,  ZHOU, Jincong ,  BURNS, David ,  YAO, Wenqing ,  JALLURI ,Ravi ,Kumar

IPC分类号： C07D405/14 ,  C07D401/06 ,  C07D207/08 ,  C07D213/50 ,  C07D403/08 ,  C07D413/08 ,  C07D405/08 ,  C07D401/08 ,  C07D241/04 ,  C07D203/08 ,  C07D407/08 ,  C07D211/32 ,  A61K31/40 ,  A61K31/435 ,  A61K31/495

CPC分类号： C07D401/14 ,  C07D207/06 ,  C07D207/08 ,  C07D211/16 ,  C07D211/32 ,  C07D211/60 ,  C07D213/50 ,  C07D241/04 ,  C07D295/185 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/08 ,  C07D403/12 ,  C07D405/08 ,  C07D405/12 ,  C07D405/14 ,  C07D413/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04

摘要： The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.

公开(公告)号：EP1432701B1

公开(公告)日：2005-12-21

申请号：EP02782863.1

申请日：2002-10-07

申请人： Recordati Ireland Limited ,  RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.

发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  RIVA, Carlo ,  TESTA, Rodolfo ,  CORBETT, Jeff, W.

IPC分类号： C07D401/12 ,  A61K31/47 ,  A61K31/404 ,  A61P13/00 ,  C07D215/12 ,  C07D215/18 ,  C07D215/20 ,  C07D405/12 ,  C07D215/40 ,  C07D215/42 ,  C07D215/26 ,  C07D401/06 ,  C07D417/12 ,  C07D413/12 ,  C07D409/08 ,  C07D413/08 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D409/14

CPC分类号： C07D401/06 ,  C07D215/12 ,  C07D215/18 ,  C07D215/20 ,  C07D215/26 ,  C07D215/40 ,  C07D215/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/08 ,  C07D409/14 ,  C07D413/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Compounds of formula (I) are thus useful for treating disorders of the urinary tract. In the compounds I, R1 = one or more substituents selected from H, halogen, OH, alkyl, haloalkyl, alkoxy, haloalkoxy, NO2, nitro, phenyl, substituted phenyl, heterocycle, substituted heterocycle, NR3R4(R3 and R4 being H, alkyl, acyl or alkoxycarbonyl); R2 = one or two substituents selected from H, alkyl; Y = CH2 or a bond; Q = CO, CS or SO2; A = alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, heterocyclic, alkylamino, dialkylamino, arylamino or arylalkylamino, each of which is optionally substituted; n is 1 or 2; X = an amino moiety selected from formula (a), (b) and -N(R5)-CH2-(R5 = H, methyl, benzyl group; W = bond, N, CH, CH2, C(CN) C(OH) or C(COCH3) (when W represents a nitrogen atom or a CH, C(CN) C(OH) or C(COCH3) group, the group Z-B attaches to the W ring atom); when X is (a) or (b), Z = bond, O, S, CH2, CH2CH2, CO, CHOH, OCH2, NH, NHCO or NHCONHCH2, but when X is -N(R5)-CH2-group, Z represents a CH2CH2 or CH2O group or Z and B together represent a 2,3-dihydro-benzo[1,4]dioxin-2-yl group; and B is a monocyclic or bicyclic aryl group or a monocyclic or bicyclic heterocycle, each of which is optionally substituted.

公开(公告)号：EP1583760A2

公开(公告)日：2005-10-12

申请号：EP04702915.2

申请日：2004-01-16

申请人： CV Therapeutics Inc.

发明人： IBRAHIM, Prabha ,  SHENK, Kevin ,  ELZEIN, Elfatih ,  PALLE, V. ,  ZABLOCKI, Jeff ,  REHDER, Kenneth

IPC分类号： C07D413/08 ,  C07D413/14 ,  C07D417/08 ,  C07D417/14 ,  C07D295/08 ,  A61K31/42 ,  A61P9/00

CPC分类号： C07D233/70 ,  C07D235/04 ,  C07D235/18 ,  C07D263/57 ,  C07D271/06 ,  C07D277/34 ,  C07D277/64 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.

公开(公告)号：EP1387829A1

公开(公告)日：2004-02-11

申请号：EP02728285.4

申请日：2002-04-29

申请人： AstraZeneca AB

发明人： JOHANSSON, Magnus ,  ROSENQUIST, sa ,  SEMPLE, Graeme

IPC分类号： C07D213/64 ,  C07D239/34 ,  C07D237/14 ,  C07D401/08 ,  C07D403/08 ,  C07D413/08 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61P25/04 ,  A61P11/14 ,  A61P23/02 ,  A61P29/00

CPC分类号： C07D213/64 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  C07D213/74 ,  C07D237/14 ,  C07D239/22

摘要： The present invention relates to a compound of formula (1), (2) or (3) having the following structures: Formula 1, 2, 3 wherein X, Y, and Z are independently C or N; A is a direct bond, CH2 or NH;B is a direct bond or NH; n= 0-2; R1 is H, optionally substituted C1-4191 alkyl, C3-7191 cycloalkyl, halogen, cyano, nitro, aryl, or alkylaryl; R2 is H, C1-4191 alkyl, or alkoxy C1-4191 alkyl;or R1 and R2 are taken together to form an unsaturated 6-membered aromatic or heterocyclic ring containing one or two heteroatoms fused to the pyridone; R3 is a direct bond, H, C1-4191 alkyl, substituted C1-4191 alkyl, C3-7191 cycloalkyl, aryl or alkylaryl; R4 is a direct bond or H; R5 is C1-4191 alkyl or aryl; R6 and R7 are independently H or C1-4191 alkyl; R8 and R9 are independently H, C1-4191 alkyl, or tert-butoxycarbonyl or R8 and R9 are taken together with the nitrogen to which they are attached and form optionally, unsubstituted, substituted, fused or unsaturated 5-,6-,7-membered heterocycles containing one or two heteroatoms wherein said substituents are selected from the group consisting of hydroxyl, hydroxymethyl, carboxymethyl, carboxy, methoxy, and tert-butoxy;as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof.