公开(公告)号：US20040209871A1

公开(公告)日：2004-10-21

申请号：US10720844

申请日：2003-11-21

申请人： Tularik Inc. ,  Japan Tobacco Inc.

发明人： Brian M. Fox ,  Noboru Furukawa ,  Xiaolin Hao ,  Kiyosei Iio ,  Takashi Inaba ,  Simon M. Jackson ,  Frank Kayser ,  Marc Labelle ,  Kexue Li ,  Takuya Matsui ,  Dustin L. McMinn ,  Nobuya Ogawa ,  Steven M. Rubenstein ,  Shoichi Sagawa ,  Kazuyuki Sugimoto ,  Masahiro Suzuki ,  Masahiro Tanaka ,  Guosen Ye ,  Atsuhito Yoshida ,  Jian Zhang

IPC分类号： A61K031/542 ,  A61K031/538 ,  A61K031/519 ,  C07D498/02 ,  C07D491/02

CPC分类号： C07D491/04

摘要： Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.

摘要翻译： 本文提供了可用于治疗或预防代谢和细胞增殖性疾病或病症的化合物，药物组合物和方法。 特别地，本发明提供调节参与脂质代谢和细胞增殖的蛋白质的活性的化合物。

公开(公告)号：US20040127705A1

公开(公告)日：2004-07-01

申请号：US10615836

申请日：2003-07-10

申请人： DAIICHI PHARMACEUTICAL CO., LTD.

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

IPC分类号： C07D498/02 ,  A61K031/542 ,  A61K031/554

CPC分类号： C07D513/04 ,  C07D207/36

摘要： A pyrrolesulfonamide derivative having the following formula (I): 1 wherein the ring P represented by 2 is a pyrrole ring having the following structure: 3 wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group 4 in which W represents CH, Cnull or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is Cnull; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

摘要翻译： 具有下式（I）的吡咯磺酰胺衍生物：其中由代表的环P是具有以下结构的吡咯环：其中R表示烷基，环烷基，环烷基 - 烷基或芳烷基; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但当不存在键时，Z1表示H，Z2表示OH或Z1，Z2组合在一起表示O或NOR1基团，其中R1表示 H或烷基，芳烷基或芳基; l代表0或1; A表示亚烷基，亚烯基或亚炔基; Y表示W表示CH，C =或N的基团; 当W为CH或N时，m代表0或1，当W为C =时，m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基。 化合物（I）具有强的5-羟色胺-2受体拮抗作用，毒性低，副作用小，作为循环系统疾病如缺血性心脏病，脑血管障碍和周围循环障碍的治疗有用。

公开(公告)号：US20040053923A1

公开(公告)日：2004-03-18

申请号：US10408220

申请日：2003-04-08

申请人： Banyu Pharmaceutical Co., Ltd.

发明人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-Ichi Eiki

IPC分类号： C07D498/02 ,  C07D491/02 ,  C07D487/02 ,  A61K031/542 ,  A61K031/538 ,  A61K031/501 ,  A61K031/506

CPC分类号： C07D498/04

摘要： This invention relates to compounds represented by the general formula nullInull 1 wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及由通式[I]表示的化合物，其中R表示叠氮基等，R 1和R 2相同或不同，表示氢原子等，R 3， 和R 4相同或不同，表示氢原子等，X 1表示氧原子等，X 2表示氧原子等，Y表示氧原子等，Z表示缩合 芳基等，或其药学上可接受的盐，其制备方法和用于治疗糖尿病的药物，用于糖尿病慢性并发症的预防剂或抗肥胖药物，其含有作为有效成分的化合物或药学上可接受的盐 其可接受的盐。

公开(公告)号：US20040023953A1

公开(公告)日：2004-02-05

申请号：US10381024

申请日：2003-07-30

发明人： Uwe Kausmeier ,  Jochen Heinicke ,  Christoph Arkona

IPC分类号： A61K031/542 ,  A61K031/549 ,  A61K031/519

CPC分类号： C07D513/04

摘要： The invention relates to mercaptomethyl-substituted thiazolonull2,3-bnullquinazolines, oxazolonull2,3-bnullquinazolines and imidazolonull2,1-bnullquinazolines. It is the object of the invention to discover new matrix metalloproteinase inhibitors (MMP) and give a simple synthesis method. The object is achieved by the production of the indicated compounds. By means of them it is possible to achieve progress using them as active substances in pharmaceutical preparations for treating diseases such as inflammatory responses of non-specific causes, sunburn and allergies.

摘要翻译： 本发明涉及巯基甲基取代的噻唑并[2,3-b]喹唑啉，恶唑并[2,3-b]喹唑啉和咪唑并[2,1-b]喹唑啉。 本发明的目的是发现新的基质金属蛋白酶抑制剂（MMP）并提供简单的合成方法。 该目的通过生产所示化合物来实现。 通过它们，可以使用它们作为用于治疗诸如非特异性原因的炎性反应，晒伤和过敏等疾病的药物制剂中的活性物质来实现进展。

公开(公告)号：US20040014748A1

公开(公告)日：2004-01-22

申请号：US10311761

申请日：2003-05-12

发明人： Rudi Grutzmann ,  Ulrich Muller ,  Hilmar Bischoff ,  Siegfried Zaiss

IPC分类号： A61K031/542 ,  A61K031/538 ,  A61K031/517 ,  A61K031/502 ,  A61K031/498 ,  A61K031/4745 ,  A61K031/4709

CPC分类号： A61K31/437

摘要： The invention relates to the use of inhibitors of the microsomal triglyceride transfer protein (MTP) for reducing the number of postprandial triglyceride-rich lipoprotein particles (ppTRL) or for reducing their decomposition products i.e. the cholestcrol-rich nullsmall remnant particlenull (remnants). Said particles are associated with apolipoprotein B-48 (ApoB-48) and are designated as nullppTRLnull in the further course of events.

摘要翻译： 本发明涉及微粒体甘油三酯转运蛋白（MTP）的抑制剂用于减少餐后富含甘油三酯的脂蛋白颗粒（ppTRL）或减少其分解产物，即富含胆固醇的“小残余颗粒”（残余物） 。 所述颗粒与载脂蛋白B-48（ApoB-48）相关，并且在进一步的事件中被指定为“ppTRL”。

公开(公告)号：US20040002492A1

公开(公告)日：2004-01-01

申请号：US10373114

申请日：2003-02-24

申请人： Kudos Pharmaceuticals Ltd

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Stephen Philip Jackson ,  Mark James O'Connor ,  Alan Yin Kai Lau ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffery Hummersone ,  Roger John Griffin

IPC分类号： A61K031/542 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/4436 ,  A61K031/4433 ,  A61K031/382 ,  A61K031/381 ,  C07D417/02 ,  C07D413/02 ,  C07D49/02

CPC分类号： C07D409/04 ,  C07D417/04

摘要： The application concerns a compound of formula I: 1 wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3 group; Y is either O or S; R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; R3 is a phenyl or pyridyl group, attached by a first bridge group selected from nullSnull, nullS(nullO)null, nullS(nullO)2null, nullOnull, nullNRNnull and CRC1RC2null to an optionally substituted C5-20 carboaryl group, the phenyl or pyridyl group and optionally substituted C5-20 carboaryl group being optionally further linked by a second bridge group, so as to form an optionally substituted C5-7 ring, the phenyl or pyridyl group being further optionally substituted.

摘要翻译： 本申请涉及式I化合物：其中P和Q中的一个为O，P和Q中的另一个为CH，其中Q和P中的任一个为CH且具有R 1的碳原子之间为双键， 3>组 Y是O或S; R 1和R 2独立地是氢，任选取代的C 1-7烷基，C 3-20杂环基或C 5-20芳基，或者可以一起形成任选取代的具有4至8个环的杂环 原子 R 3是苯基或吡啶基，其通过选自-S - ， - S（= O） - ， - S（= O）2 - ， - O - ， - NR N - 和任选取代的C 5-20碳芳基，苯基或吡啶基和任选取代的C 5-20碳芳基任选进一步通过第二桥基连接，从而形成任选取代的 C5-7环，苯基或吡啶基进一步任选被取代。

公开(公告)号：US20040002490A1

公开(公告)日：2004-01-01

申请号：US10462326

申请日：2003-06-16

发明人： Daniel Lesieur ,  Frederique Klupsch ,  Gerald Guillaumet ,  Marie-Claude Viaud ,  Michel Langlois ,  Caroline Bennejean ,  Pierre Renard ,  Philippe Delagrange

IPC分类号： A61K031/542 ,  A61K031/538 ,  A61K031/502 ,  A61K031/498 ,  A61K031/4745

CPC分类号： C07D207/27 ,  C04B35/632 ,  C07C233/43 ,  C07C233/62 ,  C07C233/65 ,  C07C237/48 ,  C07C271/20 ,  C07C275/24 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/14 ,  C07D209/20 ,  C07D209/60 ,  C07D213/70 ,  C07D221/10 ,  C07D231/12 ,  C07D233/42 ,  C07D233/56 ,  C07D233/84 ,  C07D235/06 ,  C07D249/08 ,  C07D261/20 ,  C07D307/81 ,  C07D307/92 ,  C07D311/58 ,  C07D311/60 ,  C07D319/18 ,  C07D319/20 ,  C07D333/20 ,  C07D333/38 ,  C07D333/58 ,  C07D333/74 ,  C07D335/06 ,  C07D335/08 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D407/12 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D495/14

摘要： The invention concerns compounds of formula (I): R-A-Rnull wherein: A is as defined in the description; R represent a group (V), (VI), (VII), or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; Rnull represents a null(CH2)tnullR5 group wherein t and R5 are as defined in the description, and medicaments containing the same. 1

摘要翻译： 本发明涉及式（I）化合物：R-A-R'其中：A如说明书中所定义; R代表基团（V），（VI），（VII）或（VIII），其中E，Q，R 1，R 2，R 3，v和R 4如 在说明中; R'表示 - （CH 2）t -R 5基团，其中t和R 5如说明书中所定义，和含有它们的药物。

公开(公告)号：US20030225069A1

公开(公告)日：2003-12-04

申请号：US10096421

申请日：2002-03-12

发明人： Simon N. Haydar

IPC分类号： A61K031/542 ,  A61K031/541 ,  A61K031/538 ,  A61K031/5377 ,  A61K031/519 ,  A61K031/496 ,  A61K031/454 ,  A61K031/416 ,  C07D498/14

CPC分类号： C07D495/16

摘要： The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.

摘要翻译： 本发明涉及一组具有抗肿瘤活性的氮杂蒽环唑类化合物及其制备方法。 还公开了含有氮杂蒽环唑化合物的组合物和用本发明化合物治疗哺乳动物肿瘤和癌症的方法。

公开(公告)号：US20030219483A1

公开(公告)日：2003-11-27

申请号：US10377173

申请日：2003-02-26

发明人： Joaquina Faour ,  Juan Vergez

IPC分类号： A61K031/551 ,  A61K031/55 ,  A61K031/542 ,  A61K031/519 ,  A61K031/445 ,  A61K033/00 ,  A61K031/137

CPC分类号： A61K31/135 ,  A61K9/0004 ,  A61K31/505 ,  A61K31/00 ,  A61K2300/00

摘要： The present invention provides an osmotic device containing controlled release venlafaxine in the core in combination with an anti-psychotic agent in a rapid release external coat. A wide range of anti-psychotic agents can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray-coated rather compression-coated onto the device. The device with spray-coated external core is smaller and easier to swallow than the similar device having a compression-coated external coat. The device is useful for the treatment of depression, anxiety or psychosis related disorders.

公开(公告)号：US20030186971A1

公开(公告)日：2003-10-02

申请号：US10363290

申请日：2003-02-27

发明人： Harihide Kimura ,  Seiichi Tanida ,  Tatsuhiko Kaneko

IPC分类号： A61K031/542

CPC分类号： C07D417/04 ,  A61K31/5415 ,  C07D279/08 ,  C07D279/16

摘要： The present invention is intended to provide excellent preventives and/or remedies for heart diseases. Specifically, the present invention provides heart muscle cell apoptosis inhibitors, preventives and/or remedies for heart diseases, comprising a compound represented by the following formula: 1 wherein R represents an optionally substituted hydrocarbon group, an optionally substituted aromatic heterocyclic group, or an optionally substituted amino group; or a salt thereof.

摘要翻译： 本发明旨在为心脏病提供优异的预防措施和/或补救措施。 具体而言，本发明提供心肌细胞凋亡抑制剂，心脏病的预防剂和/或治疗药物，其包含由下式表示的化合物：其中R表示任选取代的烃基，任选取代的芳族杂环基或任选取代的 氨基; 或其盐。