公开(公告)号：EP2132188A2

公开(公告)日：2009-12-16

申请号：EP08731517.2

申请日：2008-03-06

申请人： Janssen Pharmaceutica N.V.

发明人： GAUL, Michael ,  SEARLE, Lily Lee ,  RENTZEPERIS, Dionisios

IPC分类号： C07D277/34

CPC分类号： C07D277/34 ,  C07D417/06

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

公开(公告)号：EP1367111B1

公开(公告)日：2009-07-22

申请号：EP02701690.6

申请日：2002-03-04

申请人： Japan Science and Technology Agency

发明人： IRIE, Masahiro

IPC分类号： C09K9/02 ,  C07D307/58 ,  G03C1/73 ,  C07D333/32 ,  C07D277/34

CPC分类号： C07D333/32 ,  C07D277/34 ,  C07D307/58 ,  C09K9/02 ,  C09K2211/1051 ,  C09K2211/1092 ,  G03C1/73

摘要： A photochromic material which has a quantum yield in ring-opening reaction of 10-3 or lower and suffers no color fading in the ambient light. This material comprises a diheteroarylethene compound, in which each heteroaryl group has an alkoxyl group and an aryl group.

公开(公告)号：EP2004601A1

公开(公告)日：2008-12-24

申请号：EP07734152.7

申请日：2007-03-30

申请人： Matrix Laboratories Limited

发明人： GOPALAN, Balasubramanian ,  RAVI, Dhamjewar ,  RASHEED, Mohammed ,  SREEDHARA, Swamy, Keshavapura, Hosamane ,  ISHTIYAQUE, Ahmad

IPC分类号： C07D207/16 ,  C07D207/26 ,  C07D207/32 ,  C07D209/48 ,  C07D233/36 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D275/02 ,  C07D277/34 ,  C07D295/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4196

CPC分类号： C07D249/08 ,  C07D207/16 ,  C07D207/27 ,  C07D207/323 ,  C07D209/48 ,  C07D233/36 ,  C07D257/04 ,  C07D271/06 ,  C07D275/02 ,  C07D277/34 ,  C07D295/13 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined.The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.

公开(公告)号：EP1907347A2

公开(公告)日：2008-04-09

申请号：EP06787368.7

申请日：2006-07-12

申请人： Acadia Pharmaceuticals Inc.

发明人： OLSSON, Roger ,  PIU, Fabrice ,  GUNDERSEN, Birgitte

IPC分类号： C07C63/06 ,  C07D277/34 ,  C07D233/60 ,  C07D249/14

CPC分类号： C07C243/38 ,  C07C63/06 ,  C07C255/14 ,  C07C259/10 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/18 ,  C07D213/30 ,  C07D213/40 ,  C07D213/75 ,  C07D233/54 ,  C07D239/26 ,  C07D277/34 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52

摘要： Disclosed herein are novel compounds with activity at RARβ 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.

摘要翻译： 本文公开了对RARβ2受体具有活性的新化合物。 还公开了这些化合物用于治疗或缓解癌症症状，神经障碍如记忆缺陷和精神分裂症，神经退行性病症如帕金森病和阿尔茨海默病，炎性病症如牛皮癣和类风湿性关节炎，眼部病症和抑郁症的用途。

公开(公告)号：EP1877406A1

公开(公告)日：2008-01-16

申请号：EP06753498.2

申请日：2006-04-24

申请人： Bayer Schering Pharma Aktiengesellschaft

发明人： PRIEN, Olaf ,  SCHULZE, Volker ,  EIS, Knut ,  WORTMANN, Lars ,  KOSEMUND, Dirk ,  SIEMEISTER, Gerhard ,  EBERSPAECHER, Uwe ,  GUENTHER, Judith ,  BRITTAIN, Dominic E., A.

IPC分类号： C07D417/06 ,  C07D277/34 ,  A61K31/427 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07D277/34 ,  C07D417/06

摘要： The invention relates to thiazolidinones of general formula (I): as well as to their production and to their use as inhibitors of the polo-like kinase (PIk) for treating various diseases, as well as to intermediate products for the production of the compounds according to the invention.

公开(公告)号：EP1688138A4

公开(公告)日：2008-01-16

申请号：EP04799921

申请日：2004-11-26

申请人： TAKEDA PHARMACEUTICAL

发明人： FUKATSU KOHJI ,  FUJII RYO ,  KOBAYASHI MAKOTO ,  YONEMORI JINICHI ,  TANAKA TOSHIO

IPC分类号： A61K31/192 ,  A61K31/216 ,  A61K31/341 ,  A61K31/4453 ,  A61K31/5375 ,  A61P3/04 ,  A61P3/06 ,  A61P3/08 ,  A61P43/00 ,  C07C45/68 ,  C07C45/71 ,  C07C59/68 ,  C07C69/734 ,  C07D213/64 ,  C07D213/643 ,  C07D277/34 ,  C07D295/08 ,  C07D295/092 ,  C07D295/096 ,  C07D307/12 ,  C07D307/16 ,  C07D317/54 ,  C07D333/32 ,  C07F7/18 ,  G01N33/15 ,  G01N33/50

CPC分类号： C07D213/643 ,  A61K31/192 ,  A61K31/216 ,  A61K31/341 ,  A61K31/4453 ,  A61K31/5375 ,  C07C45/68 ,  C07C45/71 ,  C07C59/68 ,  C07C69/734 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D213/64 ,  C07D277/34 ,  C07D295/088 ,  C07D295/096 ,  C07D307/12 ,  C07D317/54 ,  C07D333/32 ,  C07F7/1852 ,  C07C49/697 ,  C07C49/67 ,  C07C49/84 ,  C07C49/755 ,  C07C47/575

摘要： A 14273 receptor function regulating agent useful as a preventive/therapeutic agent for diabetes, hyperlipemia, etc. There is provided a 14273 receptor function regulating agent comprising a compound having a group capable of releasing an aromatic ring and a cation.

公开(公告)号：EP1848700A1

公开(公告)日：2007-10-31

申请号：EP06735487.8

申请日：2006-02-17

申请人： Bexel Pharmaceuticals Inc

发明人： NAG, Bishwajit ,  NAG, Abhijeet ,  DEY, Debendranath ,  AGARWAL, Shiv Kumar ,  NEOGI, Partha ,  REDDY, Gaddam Om ,  BADIGER, Sangamesh ,  SINGH, Gajendra ,  PANDEY, Surendra Kumar ,  CHITHRA, Santhanagopalan

IPC分类号： C07D277/20 ,  C07D277/34 ,  C07D277/36 ,  A61P3/10

CPC分类号： C07D277/20 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  C07D277/34 ,  C07D277/36

摘要： Diphenyl ether compounds of the formula (I) are provided th-it exhibit activity useful for reducing glucose, cholesterol, and/or triglyceride levels in plasma, and for treatment of obesity, inflammation, immunological diseases, autoimmune diseases, diabetes and disorders associated with insulin resistance. (I) wherein represents an optional bond; W represents O or S; Z represents CR10, O or S; G represents O, S or together with R10 forms a 5 or 6 membered aromatic or heteroaromatic ring system containing 1 or 2 heteroatoms selected from the group consisting of O, S and N; R8 represents OR13 or NR14R15; where R13 is selected from the group consisting of hydrogen, substituted and unsubstituted (C1-C20) alkyl, (C2-C20) alkenyl, (C5-C14) aryl, (C6-C34) aralkyl, (C1C13) heteroaryl, and a counter ion; and where R14 and R15 are independently selected from the group consisting of H, substituted and unsubstituted (C1-C20) alkyl, (C2-C20) alkenyl and (C5-C14) aryl; the other substituents are defined in the claims.

公开(公告)号：EP1798216A1

公开(公告)日：2007-06-20

申请号：EP05785694.0

申请日：2005-09-26

申请人： Sankyo Company, Limited

发明人： KAJINO, Hisaki c/o Sankyo Company Limited ,  MIYAMOTO, Hiroshi c/o Sankyo Company Limited ,  IKEUCHI, Yutaka c/o Sankyo Company Limited

IPC分类号： C07C217/84 ,  C07C211/52 ,  C07C209/10 ,  C07C213/00 ,  C07C271/28 ,  C07D277/20 ,  C07D277/34 ,  C07D417/12

CPC分类号： C07D277/34 ,  C07C217/90 ,  C07C271/28 ,  C07C323/36 ,  C07D417/12

摘要： [Subject]
The object of the present invention is to provide new intermediates (IIa) and (III) of the 6-substituted-1-methyl-1-H-benzimidazol derivatives (I) which are publicly known pharmaceutically active ingredients, and a preparation procedure suitable for a large scale synthesis of N-(5-substituted-2-nitrophenyl)-N-methylamines (II) which are synthetic intermediates.
Additionally, another object of the present invention is to provide an efficient procedure for the preparation of the 6-substituted-1-methyl-1-H-benzimidazole derivative (I) from said synthetic intermediates (II) in a shorter number of steps.
[Measures to solve the subject]
The present invention relates to a procedure for the preparation of a compound (I) represented by the following formula and synthetic intermediates of said compound (I).

(In the above reaction scheme, R 2 represents a phenyl group which may optionally be substituted with substituents such as a C 1 -C 6 alkyl group or the like, and X represents an oxygen atom, a sulfur atom or a nitrogen atom).

摘要翻译： [主题]本发明的目的是提供一种高级的中间体（IIa）和（III）的6- substituiertem -1-甲基-1H-苯并咪唑衍生物（I），其是公知的药学活性成分，和一个的 适合的N-大规模合成制备程序（5-取代的-2-硝基苯基）-N-甲基胺（II），其是合成的中间体。 另外，本发明的另一目的是提供高效程序为6- substituiertem -1-甲基-1H-苯并咪唑从在更短的多个步骤，所述合成中间体（II）衍生物（Ⅰ）的制备方法。 [处理方法来解决所述对象本发明涉及一种用于由下式和所述化合物（I）的合成中间体表示的化合物（I）的制备过程。 （在上述反应路线中，R 2表示可以任选被检查为C 1 -C 6烷基或类似物，且X darstellt到氧原子，硫原子或氮原子的取代基substituiertem苯基）。

公开(公告)号：EP1753734A1

公开(公告)日：2007-02-21

申请号：EP05737588.3

申请日：2005-05-05

申请人： RENOPHARM LTD.

发明人： ASSAF, Peter ,  GAZALEEN-MARIEE, Elham ,  NAVEH, Michael

IPC分类号： C07D277/24 ,  C07D277/34 ,  C07D277/40 ,  C07D417/04 ,  C07D277/50 ,  C07D417/12 ,  C07D277/46 ,  A61K31/426 ,  A61K31/4439

CPC分类号： A61K31/427 ,  C07D277/22 ,  C07D277/24 ,  C07D277/34 ,  C07D277/36 ,  C07D277/42 ,  C07D417/04 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D495/04

摘要： Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.

公开(公告)号：EP1253145B1

公开(公告)日：2006-09-20

申请号：EP01948982.2

申请日：2001-01-30

申请人： KYORIN PHARMACEUTICAL CO., LTD.

发明人： OHNODA, Michiro ,  ORITA, Kazuo ,  YOSHIDA, Noriyuki

IPC分类号： C07D277/34 ,  A61K31/426

CPC分类号： C07D277/34

摘要： A method of industrially advantageously purifying 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[4-(trifluoromethyl)phenylmethyl]benzamide (KRP-297), which improves insulin resistance and is highly effective in lowering blood sugar and in lipid diminution. The method comprises the steps of: forming an alkali metal salt of KRP-297 and a hydrate thereof in a reaction system for producing KRP-297; isolating and purifying them; and then liberating the KRP-297 from the salt. Also provided are an alkali metal salt of KRP-297 and a hydrate of the salt.