公开(公告)号：EP2744788A1

公开(公告)日：2014-06-25

申请号：EP12825316.8

申请日：2012-08-13

申请人： Merck Sharp & Dohme Corp.

发明人： ANAND, Rajan ,  COLANDREA, Vincent, J. ,  REITER, Maud ,  VACHAL, Petr ,  ZWICKER, Aaron ,  WILSON, Jonathan, E. ,  ZHANG, Fengqi ,  ZHAO, Kake

IPC分类号： C07D243/00 ,  C07D498/00 ,  C07D487/00

CPC分类号： C07D409/06 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D241/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06

摘要： Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

摘要翻译： 具有式Ia结构的化合物（包括所述化合物的药学上可接受的盐）是CETP抑制剂，并且可用于提高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

公开(公告)号：EP2489657A3

公开(公告)日：2012-11-28

申请号：EP11187842.7

申请日：2007-10-26

申请人： MethylGene Inc. ,  Envivo Pharmaceuticals, Inc.

发明人： Deziel, Robert ,  Leit, Silvana ,  Beaulieu, Patrick ,  Chantigny, Yves Andre ,  Mancuso, John ,  Tessier, Pierre ,  Shapiro, Gideon ,  Chesworth, Richard ,  Smil, David

IPC分类号： C07D209/00 ,  C07D223/00 ,  C07D239/00 ,  C07D243/00 ,  C07D267/00 ,  C07D279/00 ,  A61K31/55 ,  A61P43/00 ,  C07D403/00 ,  C07D413/00 ,  C07D471/00

CPC分类号： C07D498/04 ,  C07C259/06 ,  C07C259/10 ,  C07D209/02 ,  C07D209/08 ,  C07D209/52 ,  C07D209/94 ,  C07D221/12 ,  C07D223/16 ,  C07D223/20 ,  C07D223/22 ,  C07D223/24 ,  C07D223/26 ,  C07D223/28 ,  C07D225/08 ,  C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D243/24 ,  C07D243/38 ,  C07D265/38 ,  C07D267/14 ,  C07D267/18 ,  C07D267/20 ,  C07D279/22 ,  C07D279/26 ,  C07D281/16 ,  C07D285/36 ,  C07D291/08 ,  C07D295/155 ,  C07D313/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D491/08 ,  C07D495/04 ,  C07D513/04 ,  C07H13/10

摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein (B), Q, J, L and Z are as defined in the specification.

公开(公告)号：EP2083014A2

公开(公告)日：2009-07-29

申请号：EP09004786.1

申请日：1996-12-26

申请人： Vertex Pharmceuticals Incorporated

发明人： Batchelor, Mark J. ,  Bebbington, David ,  Bemis, Guy, W. ,  Fridman, Wolf, Herman ,  Gillespie, Roger, J. ,  Golec, Julian M. C. ,  Gu, Yong ,  Laufer, David J. ,  Livingston, David J. ,  Matharu, Saroop S. ,  Mullican, Michael D. ,  Murcko, Mark A. ,  Murdoch, Robert ,  Nyce, Philip L. ,  Robidoux, Andrea L. ,  Su, Michael ,  Wannamaker, M. Woods ,  Wilson, Keith P. ,  Zelle, Robert E.

IPC分类号： C07K5/023 ,  C07D487/04 ,  C07D498/04 ,  A61K38/04 ,  A61K31/55 ,  C07D243/00 ,  C07D237/00

CPC分类号： C07D243/12 ,  A61K38/00 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07K5/0202 ,  C07K5/06139 ,  C07K5/0821

摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physiochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases and decreasing IGIF, and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

摘要翻译： 本发明涉及作为白细胞介素-1转化酶抑制剂的新型化合物。 本发明的ICE抑制剂的特征在于具体的结构和生理化学特征。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适合于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-3介导的疾病，炎性疾病，自身免疫疾病 ，破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，用于治疗白介素-1-，细胞凋亡，IGIF和IFN-3介导的疾病并减少IGIF和IFN-3产生的方法。 本发明还涉及制备N-酰基氨基化合物的方法。

公开(公告)号：EP1537114B8

公开(公告)日：2007-10-03

申请号：EP03784194.7

申请日：2003-08-06

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： MC KENNA, Jeffrey

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5517 ,  A61P5/40 ,  C07D241/00 ,  C07D235/00 ,  C07D243/00

CPC分类号： C07D487/04 ,  C07D471/04

公开(公告)号：EP1785425A2

公开(公告)日：2007-05-16

申请号：EP07101576.2

申请日：2003-09-29

申请人： NEUROSEARCH A/S

发明人： Peters, Dan ,  Olsen, Gunnar, M. ,  Nielsen, Elsebet, Østergaard ,  Jørgensen, Tino, Dyhring ,  Ahring, Philip, K.

IPC分类号： C07D471/08 ,  A61K31/55 ,  A61P25/00 ,  C07D221/00 ,  C07D243/00

CPC分类号： C07D471/08 ,  C07D487/04

摘要： This invention relates to novel 1,4-diazabicycloalkane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters.
Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

摘要翻译： 本发明涉及新的1,4-二氮杂双环烷烃衍生物及其在制备药物组合物中的用途。 发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。 由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或病症 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状有关的疾病或病症。

公开(公告)号：EP1776160A1

公开(公告)日：2007-04-25

申请号：EP05791680.1

申请日：2005-08-12

申请人： OMEROS CORPORATION

发明人： TEDFORD, Clark, E. ,  RAJAGOPALAN, Raghavan

IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D267/02 ,  C07D281/08 ,  C07D243/00 ,  C07D487/00

CPC分类号： C07D471/14

摘要： The present invention discloses novel 5-HT receptor binding agents of Formula 3, wherein X is -CH or -N-. Y is selected from the group consisting of -CR10R11, -NR12, -0-, -S-, -SO-, and -SO2-. R1 to R12 are various substituents selected to optimize the physicochemical and biological properties such as receptor binding, receptor selectivity, tissue penetration, lipophilicity, toxicity, bioavailability, and pharmacokinetics of compounds of Formula 3. These include hydrogen, alkyl, acyl, hydroxyl, hydroxyalkyl, aryl, amino, aminoalkyl, alkoxyl, aryloxyl, carboxyl, alkoxycarbonyl, halogen, cyano, and other suitable electron donating or electron withdrawing groups. R2 and R3, R3 and R4, or R5 and R6 may optionally be tethered together to form fused alicyclic or heterocyclic ring. R1 and R2, R4 and R5, or R6 and R7 may also optionally be tethered together to form spiro carbo- or heterocyclic ring.

公开(公告)号：EP1537114B1

公开(公告)日：2006-08-09

申请号：EP03784194.7

申请日：2003-08-06

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： MC KENNA, Jeffrey

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5517 ,  A61P5/40 ,  C07D241/00 ,  C07D235/00 ,  C07D243/00

CPC分类号： C07D487/04 ,  C07D471/04

摘要： Compounds of formula (I), provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention, delay of progression, or treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis, and remodeling following hypertension and endothelial dysfunction. Preferred are the compounds of formula (I) which are selective inhibitors of aldosterone synthase devoid of undesirable side effects due to general inhibition of cytochrome P450 enzymes.

公开(公告)号：EP1597260A1

公开(公告)日：2005-11-23

申请号：EP04709303.4

申请日：2004-02-09

申请人： Pfizer Limited ,  PFIZER INC.

发明人： BRYANS, Justin Stephen,Pfizer Global R & D ,  JOHNSON, Patrick Stephen,Pfizer Global R & D ,  RYCKMANS, Thomas,Pfizer Global R & D ,  STOBIE, Alan,Pfizer Global R & D ,  RUSSELL, Rachel, Jane,Pfizer Global R & D ,  WAYMAN, Christopher, PeterPfizer Global R & D

IPC分类号： C07D487/04 ,  A61K31/55 ,  A61K31/501 ,  A61K31/4427 ,  A61P29/00 ,  C07D498/04 ,  C07D401/04 ,  C07D413/14 ,  C07D513/04 ,  C07D249/00 ,  C07D243/00 ,  C07D267/00

CPC分类号： A61K31/41 ,  A61K31/4196 ,  G01N2333/72 ,  G01N2500/04

摘要： A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein V represents -(CH2)d(O)e-, -CO-, or -CH(C1-6 alkyl)-; W is -0-, -S(O)a , or -N(R1')-R1 represents H, C 1-6 alkyl, (CH2)bCOR2, CO(CH2)bNR2R3, S02R2, (CH2 )cOR2, (CH2)c,NR2R3, or (CH2)bhet1; het1 represents a saturated or unsaturated heterocycle of from 3 to 8 atoms containing one or more heteroatoms selected from O, N, or S, optionally substituted with C 1-6 alkyl; X and Y independently represent H, C 1-6 alkyl, halogen, OH, CF3, OCF3, OR4; Z represents -(CH2)f(O)g , -CO- or -CH(C 1-6 alkyl)-; Ring A represents a 4-7 membered, saturated N-containing heterocycle, optionally substituted with OH, and in which optionally at least one ring N is substituted with O;Ring B represents phenyl or a 4-7 membered unsaturated N-containing heterocycle, optionally substituted with OH, halogen, CN, CONH2, CF3, OCF3, and in which optionally at least one ring N is substituted with O; R2 and R3 independently represent H, C 1-6 alkyl [optionally substituted with OH, halogen,N(C 1.6 alkyl)2, or C 1.6 alkyloxy], C 1.6 alkyloxy, N(C 1-6 alkyl)2, or [C 3-8 cycloalkyl]; or R2 and R3, together with the nitrogen atom to which they are attached independently represent a heterocycle of from 3 to 8 atoms, optionally substituted with C 1-6 alkyl;R4 represents straight or branched C 1-6 alkyl, a and c independently represent 0, 1, or 2; b, e and g independently represent 0 or 1; d and f independently represent 1 or 2;are useful in the treatment of dysmenorrhoea.

公开(公告)号：EP0253571B1

公开(公告)日：1989-08-23

申请号：EP87306067.7

申请日：1987-07-09

申请人： Merck & Co., Inc.

发明人： Reider, Paul J. ,  Grabowski, Edward J.J.

IPC分类号： C07B55/00 ,  C07B57/00 ,  C07C85/00 ,  C07D243/00 ,  C07D243/26

CPC分类号： C07D243/24

公开(公告)号：EP0221463A3

公开(公告)日：1987-12-02

申请号：EP86114748

申请日：1986-10-23

申请人： Dainippon Pharmaceutical Co., Ltd.

发明人： Matsumoto, Jun-ichi ,  Miyamoto, Teruyuki ,  Egawa, Hiroshi ,  Nakamura, Shinichi

IPC分类号： C07D215/56 ,  C07D401/04 ,  A61K31/47 ,  A61K31/53 ,  A61K31/55 ,  C07D243/00 ,  C07D215/00 ,  C07D241/00

CPC分类号： C07D401/04 ,  C07D215/56

摘要： The present invention relates to a quinoline derivative of the formula
wherein Z is an amino group or a halogen atom, R, is a hydrogen atom or a methyl or ethyl group, R 2 is a hydrogen atom or a methyl or fluoromethyl group, R 3 and R 4 are the same or different and each represents a hydrogen atom or a methyl group, and n is 1 or 2;
and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.