公开(公告)号：EP1036075B1

公开(公告)日：2004-06-23

申请号：EP98918108.6

申请日：1998-04-10

申请人： Dr. Reddy's Laboratories Ltd.

发明人： LOHRAY, Vidya, Bhushan ,  LOHRAY, Braj, Bhushan ,  PARASELLI, Rao, Bheema ,  RAMANUJAM, Rajagopalan ,  CHAKRABARTI, Ranjan

IPC分类号： C07D417/12 ,  A61K31/425 ,  C07D265/22 ,  C07D277/34 ,  C07D239/90

CPC分类号： C07D277/20 ,  C07D265/22 ,  C07D277/34 ,  C07D413/12 ,  C07D417/12

公开(公告)号：EP1360178A4

公开(公告)日：2004-05-26

申请号：EP01944241

申请日：2001-06-05

申请人： CALYX THERAPEUTICS INC

发明人： NEOGI PARTHA ,  NAG BISHWAJIT ,  MEDICHERLA SATYANARAYANA ,  DEY DEBENDRANATH

IPC分类号： A61K31/426 ,  A61P1/04 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/26 ,  A61P9/10 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P21/04 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D277/20 ,  C07D277/24 ,  C07D277/34

CPC分类号： C07D277/20 ,  C07D277/24 ,  C07D277/34

摘要： Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.

摘要翻译： 提供了含有噻唑烷二酮或恶唑烷二酮部分的新型二苯基乙烯化合物及其衍生物，其可有效降低II型糖尿病动物模型中的血糖水平，血清胰岛素，甘油三酯和游离脂肪酸水平。 与先前报道的已知降低瘦素水平的噻唑烷二酮化合物相反，本发明化合物增加瘦素水平并且不具有已知的肝脏毒性。 公开的化合物可用于多种治疗，包括治疗炎症，炎性和免疫性疾病，胰岛素抵抗，高脂血症，冠状动脉疾病，癌症和多发性硬化症。

公开(公告)号：EP1357115A4

公开(公告)日：2004-04-07

申请号：EP01272544

申请日：2001-12-28

申请人： TAKEDA CHEMICAL INDUSTRIES LTD

发明人： MOMOSE YU ,  MAEKAWA TSUYOSHI ,  TAKAKURA NOBUYUKI ,  ODAKA HIROYUKI ,  KIMURA HIROYUKI ,  ITO TATSUYA

IPC分类号： A61P3/06 ,  A61P3/10 ,  A61P9/12 ,  A61P13/12 ,  A61P19/10 ,  A61P27/02 ,  A61P31/04 ,  A61P43/00 ,  C07D263/32 ,  C07D277/24 ,  C07D277/32 ,  C07D277/34 ,  C07D277/42 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

CPC分类号： C07D403/04 ,  C07D263/32 ,  C07D277/24 ,  C07D277/42 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： Alkanoic acid derivatives represented by the general formula (I) or salts thereof, useful as preventive and/or therapeutic agents for diabetes, hyperlipidemia, impaired glucose tolerance, and so on: (I) wherein R1 is an optionally substituted five-membered aromatic heterocyclic group; X is a free valency or the like; Q is a divalent hydrocarbon group containing 1 to 20 carbon atoms; Y is a free valency or the like; A is an aromatic ring which may have one to three substituents; Z is -(CH¿2)n-Z?1- (wherein n is an integer of 1 to 8; and Z1 is oxygen or the like) or the like; B is an optionally mono- to tri-substituted pyridine ring or the like; U is a free valency or the like; W is a divalent hydrocarbon group containing 1 to 20 carbon atoms; and R3 is -OH or the like, with the proviso that when B is an optionally mono- to tri-substituted benzene ring, U is a free valency.

公开(公告)号：EP0783496B9

公开(公告)日：2003-09-03

申请号：EP95927993.6

申请日：1995-08-09

申请人： Takeda Chemical Industries, Ltd.

发明人： SOHDA, Takashi ,  ODAKA, Hiroyuki ,  MOMOSE, Yu

IPC分类号： C07D277/34 ,  C07D417/12 ,  C07D417/10 ,  A61K31/425

CPC分类号： C07D417/12 ,  C07D277/34

公开(公告)号：EP1322647A1

公开(公告)日：2003-07-02

申请号：EP01971336.1

申请日：2001-09-25

申请人： DR. REDDY'S RESEARCH FOUNDATION

发明人： CHEBIYYAM, Prabhakar ,  MAMILLAPALLI, Ramabhadra, Sarma ,  KRISHNAMURTHI, Vyas ,  SEELLA, Vishnuvardhan, Reddy ,  GADDAM, Om, Reddy

IPC分类号： C07D417/12 ,  C07D277/34 ,  A61K31/425 ,  A61P3/10 ,  A61P9/12

CPC分类号： C07D417/12

摘要： This invention relates to novel polymorphic/pseudopolymorphic forms of 5-[4-[2[N-methyl-N-(2-pyridyl)amino]ethoxy]benzyl] thiazolidine-2,4-dione maleate having formula (I). The invention also relates to a pharmaceutical composition comprising the novel polymorphic form or their mixture and a pharmaceutically acceptable carrier. The polymorphic forms of the present invention are more active, as antidiabetic agent, than the hitherto known 5-[4-[2-[N-(2-methyl-N-(2-pyridyl)amino]ethoxy]benzyl] thiazolidine-2,4-dione maleate.

公开(公告)号：EP1313471A1

公开(公告)日：2003-05-28

申请号：EP01963157.1

申请日：2001-08-30

申请人： Oxford GlycoSciences (UK) Limited

发明人： ORCHARD, Michael Glen,Oxford GlycoSci. (UK) Ltd. ,  NEUSS, Judi Charlotte,Oxford GlycoSci. (UK) Ltd. ,  GALLEY, Carl Maurice Swedler

IPC分类号： A61K31/426 ,  A61K31/427 ,  A61P31/10 ,  C07D277/34 ,  C07D277/36 ,  C07D417/12

CPC分类号： C07D277/20 ,  C07D417/12

摘要： A compound of formula I or a salt thereof wherein, A is O or S, X and Y independently represent O, CH2 and may be the same or different, Q is (CH2)m-CH(R1)-(CH2)n, R is OR6, NHR8, R1 is hydrogen, or optionally substituted alkyl, R2 and R3 are independently hydrogen, or specific substituents, provided that R2 and R3 are not both H, and R4 and R5 are hydrogen or specific substituents, m is 0-3; n is 0-2; are useful in the treatment of fungal infections.

公开(公告)号：EP1048659A4

公开(公告)日：2002-11-20

申请号：EP98953024

申请日：1998-11-12

申请人： INST MED MOLECULAR DESIGN INC

发明人： KAGECHIKA HIROYUKI ,  HASHIMOTO YUICHI ,  ITAI AKIKO

IPC分类号： C07D277/34 ,  C07D417/10 ,  A61K31/425 ,  A61K31/55

CPC分类号： C07D417/10 ,  C07D277/34

摘要： Retinoid receptor agonists having retinoic effects or regulatory effects of increasing or suppressing retinoid actions. The agonists include compounds represented by general formulas (I) and (II).

公开(公告)号：EP1243584A1

公开(公告)日：2002-09-25

申请号：EP00956916.1

申请日：2000-09-05

申请人： OTSUKA CHEMICAL COMPANY, LIMITED

发明人： HAYASHI, Masatoshi, Naruto Res. Ctr. ,  ENDO, Yasuhiro, Naruto Res. Ctr. ,  KOMURA, Tomozo, Naruto Res. Ctr.

IPC分类号： C07D277/10 ,  C07D277/30 ,  C07D277/34 ,  C07D279/06 ,  C07D279/08 ,  C07D281/00 ,  C07D291/08 ,  C07D417/04 ,  C07D417/12 ,  A01N43/78

CPC分类号： C07D277/10 ,  A01N43/78 ,  C07D277/30 ,  C07D277/34 ,  C07D279/06 ,  C07D417/04

摘要： The cyanomethylene compound of the invention is a compound represented by the formula (1)
wherein R is C 1-20 straight-chain or branched-chain alkyl, C 3-8 cycloalkyl, aryl or heterocyclic group; and the aryl and the heterocyclic group may be substituted with one or more substituents); R 1 is C 1-8 straight-chain or branched-chain alkyl, C 3-8 cycloalkyl, aryl or heterocyclic group; and the aryl and the heterocyclic group may be substituted with one or more substituents; A is C 1-6 straight-chain or branched-chain alkylene, and Y is a sulfur atom, sulfinyl or sulfonyl. The cyanomethylene compound of the invention exhibits an excellent fungicidal activity against drug resistant fungi as well as drug sensitive fungi, and can be used as a fungicide in agriculture and horticulture.

摘要翻译： 本发明的氰基亚甲基化合物是由式（1） worin R所表示的化合物是C 1-20直链或支链烷基，C 3-8环烷基，芳基或杂环基; 和芳基和杂环基可以被一个或多个取代基）来substituiertem; [R <1>是C 1-8直链或支链烷基，C 3-8环烷基，芳基或杂环基; 和芳基和杂环基可以被一个或多个取代基substituiertem; A是C 1-6的直链或支链亚烷基，且Y为硫原子，亚磺酰基或磺酰基。 发明展品的氰基亚甲基化合物园艺耐药性的真菌以及药物敏感真菌优异的杀真菌活性，并且可以用作农业杀真菌剂和。

公开(公告)号：EP1207157A4

公开(公告)日：2002-09-18

申请号：EP00953477

申请日：2000-08-18

申请人： KYORIN SEIYAKU KK

发明人： MIYACHI HIROYUKI ,  NOMURA MASAHIRO ,  TANASE TAKAHIRO ,  MURAKAMI KOJI ,  TSUNODA MASAKI

IPC分类号： A61P3/06 ,  A61P3/10 ,  A61P43/00 ,  C07D277/34 ,  A61K31/426

CPC分类号： C07D277/34

摘要： Substituted benzylthiazolidine-2,4-dione derivatives capable of, as a ligand of human peroxisome proliferator-activated receptor (PPAR), enhancing the transcriptional activity of the receptor and showing effects of lowering blood sugar level and lowering lipid level; and a process for producing the same. Novel substituted benzamide derivatives represented by general formula (1), pharmaceutically acceptable salts thereof and hydrates of the same wherein A represents optionally substituted phenyl, optionally substituted phenoxy or optionally substituted benzyloxy.

摘要翻译： 取代的苄基噻唑烷-2,4-二酮衍生物能够作为人过氧化物酶体增殖物激活受体（PPAR）的配体，增强受体的转录活性并显示出降低血糖水平和降低血脂水平的效果; 及其制造方法。 由通式（1）表示的新型取代的苯甲酰胺衍生物，其药学上可接受的盐及其水合物，其中A代表任选取代的苯基，任选取代的苯氧基或任选取代的苄氧基。

公开(公告)号：EP1235817A1

公开(公告)日：2002-09-04

申请号：EP00980514.4

申请日：2000-11-17

申请人： Ortho-McNeil Pharmaceutical, Inc.

发明人： ANDRES, Mark, C. ,  BRYN, Stephen, R. ,  NEWMAN, Ann, W. ,  RUSSELL, Catherine

IPC分类号： C07D277/34 ,  A61K31/425

CPC分类号： C07D277/34

摘要： The present invention provides a crystal form, termed E type crystal form, and an amorphous form of 5-[[6-[(2-fluorophenyl)methoxy]-2-naphthalenyl]methyl]-2,4-Thiazolidinedione (MCC-555) that are distinguishable from known crystal forms. The present invention also provides a method for preparation thereof and pharmaceutical compositions comprising the E type crystal form, or amorphous forms of MCC-555.