公开(公告)号：EP3281937A1

公开(公告)日：2018-02-14

申请号：EP16183294.4

申请日：2016-08-09

申请人： Dompé farmaceutici S.p.A.

发明人： DE PIZZOL, Maria ,  SIRICO, Anna ,  ZIPPOLI, Mara ,  BIANCHINI, Gianluca ,  BECCARI, Andrea ,  ARAMINI, Andrea ,  LIBERATI, Chiara Rossana Maria

IPC分类号： C07C311/16 ,  C07C311/21 ,  C07C311/51 ,  C07D231/42 ,  C07D235/30 ,  C07D249/04 ,  C07D249/08 ,  C07D249/14 ,  C07D257/06 ,  C07D261/16 ,  C07D263/50 ,  C07D275/03 ,  C07D277/52 ,  C07D285/04 ,  C07D285/135

CPC分类号： C07D231/42 ,  A61K31/18 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/425 ,  A61K31/433 ,  C07C311/16 ,  C07C311/21 ,  C07C311/51 ,  C07D235/30 ,  C07D249/04 ,  C07D249/08 ,  C07D249/14 ,  C07D257/06 ,  C07D261/16 ,  C07D263/50 ,  C07D275/03 ,  C07D277/52 ,  C07D285/04 ,  C07D285/135

摘要： The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I):

Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabetes (particularly type 2 diabetes), impaired oral glucose tolerance, insulin resistance, obesity, obesity related disorders, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.

摘要翻译： 本发明涉及用作G蛋白偶联受体120（GPR120）和/或40（GPR40）的激动剂的化合物，并且具有式（I）：所述化合物可用于治疗由GPR120调节的疾病或病症和/或 GPR40如糖尿病（特别是2型糖尿病），口服葡萄糖耐量受损，胰岛素抵抗，肥胖，肥胖相关病症，代谢综合征，血脂异常，LDL升高，甘油三酯升高，肥胖诱导的炎症，骨质疏松症和肥胖相关心血管病症。

公开(公告)号：EP2938338A2

公开(公告)日：2015-11-04

申请号：EP13868405.5

申请日：2013-12-27

申请人： Drexel University ,  Baruch S. Blumberg Institute ,  Enantigen Therapeutics, Inc.

发明人： BAUGH, Simon David Peter ,  YE, Hong ,  XU, Xiaodong ,  GUO, Ju-tao ,  XIAO, Tong ,  DU, Yanming ,  BLOCK, Timothy

IPC分类号： A61K31/165 ,  A61K31/18

CPC分类号： C07C311/16 ,  C07B2200/07 ,  C07C233/66 ,  C07C309/89 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/48 ,  C07C317/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D203/26 ,  C07D205/04 ,  C07D211/96 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D215/38 ,  C07D215/42 ,  C07D217/24 ,  C07D231/40 ,  C07D231/42 ,  C07D239/26 ,  C07D261/14 ,  C07D263/48 ,  C07D263/50 ,  C07D263/58 ,  C07D277/46 ,  C07D277/52 ,  C07D295/26 ,  C07D295/30 ,  C07D295/32 ,  C07D305/08 ,  C07D309/04 ,  C07D319/16 ,  C07D319/18

摘要： The present invention provides novel compounds of formula (I) and methods of use thereof. In certain embodiments, the compounds of the invention are useful as nucleocapsid assembly inhibitors. In other embodiments, the compounds of the invention are useful as pregenomic RNA encapsidation inhibitors of Hepatitis B virus (HBV). In yet other embodiments, the compounds of the invention are useful for the treatment of viral infection, including HBV and related viral infections.

摘要翻译： 本发明提供新的式（I）化合物及其使用方法。 在某些实施方案中，本发明的化合物可用作核衣壳组装抑制剂。 在其它实施方案中，本发明的化合物可用作乙型肝炎病毒（HBV）的前基因组RNA包封抑制剂。 在其它实施方案中，本发明的化合物可用于治疗病毒感染，包括HBV和相关病毒感染。

公开(公告)号：EP0946508B1

公开(公告)日：2009-09-23

申请号：EP97952409.7

申请日：1997-12-15

申请人： Bristol-Myers Squibb Pharma Company

发明人： PINTO, Donald, Joseph, Phillip ,  PRUITT, James, Russell ,  CACCIOLA, Joseph ,  FEVIG, John, Matthew ,  HAN, Qi ,  ORWAT, Michael, James ,  QUAN, Mimi, Lifen ,  ROSSI, Karen, Anita

IPC分类号： C07D207/34 ,  C07D231/14 ,  C07D233/90 ,  C07D249/06 ,  C07D257/04 ,  A61K31/40 ,  A61K31/41 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

CPC分类号： C07D257/04 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/40 ,  C07D231/42 ,  C07D233/56 ,  C07D233/90 ,  C07D249/06 ,  C07D249/08 ,  C07D249/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

公开(公告)号：EP1995241A1

公开(公告)日：2008-11-26

申请号：EP08153165.9

申请日：2008-03-20

申请人： ICAgen, Incorporated ,  Pfizer Limited

发明人： Marron, Brian Edward ,  Fritch, Paul Christopher ,  Markworth, Christopher John ,  Maynard, Andrew Thomas ,  Swain, Nigel Alan

IPC分类号： C07D231/42 ,  C07D249/14 ,  C07D257/06 ,  C07D261/16 ,  C07D277/20 ,  C07D417/12 ,  C07D285/135 ,  A61K31/427 ,  A61K31/433 ,  A61P25/00

CPC分类号： C07D471/04 ,  C07D231/42 ,  C07D249/14 ,  C07D257/06 ,  C07D261/16 ,  C07D277/20 ,  C07D277/52 ,  C07D285/08 ,  C07D285/135 ,  C07D417/12

摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

摘要翻译： 提供了可用于通过电压门控钠通道抑制钠离子通量来治疗疾病的化合物，组合物和方法。 更具体地，本发明提供取代的芳基磺酰胺，包含这些化合物的组合物，以及使用这些化合物或组合物治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的方法，其通过阻断与起始相关的钠通道或 指示条件复发。 本发明的化合物，组合物和方法特别用于通过电压门控钠通道抑制离子通量来治疗神经性或炎性疼痛。

公开(公告)号：EP1814860A1

公开(公告)日：2007-08-08

申请号：EP05824911.1

申请日：2005-10-26

申请人： SCHERING CORPORATION

发明人： SHIPPS, Gerald, W., Jr. ,  CURRAN, Patrick, J. ,  ANNIS, D., Allen ,  NASH, Huw, M. ,  COOPER, Alan, B. ,  ZHU, Hugh, Y. ,  WANG, James, J-S. ,  DESAI, Jagdish, A. ,  GIRIJAVALLABHAN, Viyyoor, Moopil

IPC分类号： C07D231/14 ,  A61K31/415 ,  A61P31/14

CPC分类号： C07D249/10 ,  C07D231/14 ,  C07D231/40 ,  C07D231/42 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention provides compounds of formula I wherein X, Y, R1-R7 are as defined herein. Compositions containing these compounds, and methods for inhibiting HCV RNA-dependent RNA polymerase and treating hepatitis C and related disorders using these compounds and compositions are also provided. (I)

公开(公告)号：EP1732884A1

公开(公告)日：2006-12-20

申请号：EP04742190.4

申请日：2004-07-12

申请人： Biotie Therapies Corp.

发明人： SMITH, David ,  MARJAMÄKI, Anne ,  OJALA, Marika ,  PIHLAVISTO, Marjo ,  HEINO, Jyrki ,  KÄPYLÄ, Jarmo ,  PENTIKÄINEN, Olli ,  NYRÖNEN, Tommi ,  JOHNSON, Mark ,  HUHTALA, Mikko

IPC分类号： C07C317/32 ,  A61K31/18 ,  A61P35/00

CPC分类号： C07D239/22 ,  C07C311/21 ,  C07C311/29 ,  C07D207/325 ,  C07D209/08 ,  C07D209/48 ,  C07D209/88 ,  C07D213/61 ,  C07D213/82 ,  C07D231/12 ,  C07D231/16 ,  C07D231/42 ,  C07D233/54 ,  C07D233/68 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/48 ,  C07D239/52 ,  C07D257/04 ,  C07D263/56 ,  C07D271/06 ,  C07D271/08 ,  C07D275/06 ,  C07D277/62 ,  C07D277/64 ,  C07D277/66 ,  C07D277/68 ,  C07D277/74 ,  C07D285/06 ,  C07D295/135 ,  C07D295/30 ,  C07D303/36 ,  C07D317/66 ,  C07D333/34 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14

摘要： The invention relates to sulphonamide derivatives of formula (I), where RC is optionally substituted 4-6-membered heterocyclic ring containing one or more N atoms, or RC forms together with the phenyl ring to which it is attached a benzodioxolyl group, or RC is -NR1R2, RA is a group having the formula (A), (B) or (C) RB is hydrogen or alkyl. The invention also relates to the use of derivatives of formula (I) as inhibitors for collagen receptor integrins and a process for preparing sulphonamides of formula (I).

公开(公告)号：EP1147102B1

公开(公告)日：2004-03-17

申请号：EP00913263.0

申请日：2000-01-27

申请人： Wyeth Holdings Corporation

发明人： LEVIN, Jeremy, Ian ,  CHEN, James, Ming ,  NELSON, Frances, Christy

IPC分类号： C07D333/00

CPC分类号： C07D213/78 ,  C07C309/42 ,  C07C309/87 ,  C07D231/42 ,  C07D333/38

公开(公告)号：EP0934300B1

公开(公告)日：2002-12-18

申请号：EP97910099.7

申请日：1997-10-08

申请人： American Cyanamid Company

发明人： LEVIN, Jeremy, Ian ,  NELSON, Christy, Frances

IPC分类号： C07D333/38 ,  C07D231/42 ,  C07D213/78 ,  C07D409/12 ,  A61K31/38 ,  A61K31/44 ,  A61K31/415

CPC分类号： C07D213/78 ,  C07D231/42 ,  C07D333/38 ,  C07D333/40 ,  C07D409/12

摘要： The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-α converting enzyme (TACE, tumor necrosis factor-α converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection, cachexia, anorexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel diseases, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, ocular inflammation, keratoconus, Sjogren's syndrome, myopia, ocular tumors, ocular angiogenesis/neovascularization. The TACE and MMP inhibiting ortho-sulfonamido aryl hydroxamic acids of the present invention are represented by formula (1) where the hydroxamic acid moiety and the sulfonamido moiety are bonded to adjacent carbons on group A where A is defined as: a 5-6 membered heteroaryl having from 1 to 3 heteroatoms independently selected from N, O, and S and optionally substituted by R?1, R2 and R3¿; and Z, R?1, R2, R3, R4, R5, R6, R7, R8 and R9¿ are described in the specification, and the pharmaceutically acceptable salts thereof and the optical isomers and diastereomers thereof.

公开(公告)号：EP1257539A2

公开(公告)日：2002-11-20

申请号：EP01913034.3

申请日：2001-02-23

申请人： Ortho-McNeil Pharmaceutical, Inc.

发明人： KORDIK, Cheryl, P. ,  DAX, Scott, L. ,  LUO, Chi ,  REITZ, Allen, B. ,  MCNALLY, James, J.

IPC分类号： C07D231/42 ,  A61P25/24

CPC分类号： C07D231/38 ,  C07D231/14 ,  C07D231/42 ,  C07D401/04 ,  C07D403/04

摘要： Amino pyrazole derivatives of the formula (I) which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.

公开(公告)号：EP0192951B1

公开(公告)日：1989-11-08

申请号：EP86100722

申请日：1986-01-21

申请人： BAYER AG

发明人： SCHALLNER, OTTO, DR. ,  GEHRING, REINHOLD, DR. ,  STETTER, JORG, DR. ,  SANTEL, HANS-JOACHIM, DR. ,  SCHMIDT, ROBERT R., DR.

IPC分类号： A01N43/56 ,  C07D231/38 ,  C07D231/42

CPC分类号： C07D231/42