公开(公告)号：EP2027087A2

公开(公告)日：2009-02-25

申请号：EP07795056.6

申请日：2007-05-18

申请人： MannKind Corporation

发明人： FLYNN, Gary, A. ,  LEE, Sandra, Aeyoung ,  FARIS, Mary ,  BRANDT, David, William ,  CHAKRAVARTY, Subrata

IPC分类号： C07D207/14 ,  C07D307/80 ,  C07D209/44 ,  C07D317/54 ,  C07D211/10 ,  C07D319/18 ,  C07D211/26 ,  C07D333/56 ,  C07D211/30 ,  C07D401/04 ,  C07D217/04 ,  C07D401/06 ,  C07D265/36 ,  C07D295/192 ,  C07D307/52

CPC分类号： A61K31/538 ,  A61K31/137 ,  A61K31/33 ,  A61K31/40 ,  A61K31/4035 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/5377 ,  C07D207/08 ,  C07D207/14 ,  C07D209/44 ,  C07D211/10 ,  C07D211/26 ,  C07D211/30 ,  C07D217/04 ,  C07D265/36 ,  C07D295/108 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D307/52 ,  C07D307/80 ,  C07D317/54 ,  C07D319/18 ,  C07D333/56 ,  C07D401/04 ,  C07D401/06

摘要： Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.

公开(公告)号：EP2014285A1

公开(公告)日：2009-01-14

申请号：EP08014713.5

申请日：2000-11-21

申请人： Shionogi&Co., Ltd.

发明人： Kawanishi, Yasuyuki Shionogi & Co., Ltd ,  Takenaka, Hideyuki Shionogi & Co., Ltd, ,  Hanasaki, Kohji Shionogi & Co., Ltd ,  Okada, Tetsuo Shionogi & Co., Ltd

IPC分类号： A61K31/18 ,  C07C311/06 ,  C07C311/20 ,  C07C311/46 ,  C07C323/40 ,  C07D207/12 ,  C07D209/08 ,  C07D209/48 ,  C07D209/88 ,  C07D211/58 ,  C07D213/75 ,  C07D215/36 ,  C07D217/04 ,  C07D219/10 ,  C07D231/16 ,  C07D231/56 ,  C07D233/68 ,  C07D239/42 ,  C07D277/56 ,  C07D285/06 ,  C07D295/12 ,  C07D307/68 ,  C07D307/91 ,  C07D311/16 ,  C07D317/66 ,  C07D333/38 ,  C07D333/72 ,  A61P3/00

CPC分类号： C07D249/08 ,  A61K31/00 ,  A61K31/18 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/37 ,  A61K31/381 ,  A61K31/4015 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/423 ,  A61K31/425 ,  A61K31/428 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/451 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/5375 ,  A61K31/63 ,  A61K31/635 ,  C07C311/06 ,  C07C311/07 ,  C07C311/08 ,  C07C311/14 ,  C07C311/20 ,  C07C311/21 ,  C07C311/46 ,  C07C323/40 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/44 ,  C07C2603/18 ,  C07D207/09 ,  C07D207/12 ,  C07D207/16 ,  C07D209/08 ,  C07D209/48 ,  C07D209/88 ,  C07D211/58 ,  C07D211/62 ,  C07D213/75 ,  C07D213/82 ,  C07D215/36 ,  C07D215/38 ,  C07D217/04 ,  C07D219/10 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D233/56 ,  C07D233/68 ,  C07D239/42 ,  C07D277/56 ,  C07D277/70 ,  C07D285/06 ,  C07D295/135 ,  C07D307/68 ,  C07D307/91 ,  C07D311/16 ,  C07D317/66 ,  C07D333/38 ,  C07D333/72

摘要： The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I):

wherein R 1 is lower alkyl, cycloalkyl or the like,
R 2 is hydrogen, lower alkyl or the like,
n is 1 or 2,
X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like,
Y is CONR 7 , CSNR 7 , NR 7 CO, NR 7 CS or the like,
Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R 7 is hydrogen or lower alkyl,
prodrug, pharmaceutically acceptable salt or solvate thereof

摘要翻译： 本发明提供一种用作NPY Y5受体拮抗剂的药物组合物，其包含式（I）化合物：其中R 1为低级烷基，环烷基等，R 2为氢，低级烷基等，n为 1或2，X是低级亚烷基，低级亚烯基，亚芳基，亚环烷基等，Y是CONR 7，CSNR 7，NR 7 CO，NR 7 CS等，Z是低级烷基，任选取代的碳环基，任选取代的杂环基 R 7为氢或低级烷基，前药，药学上可接受的盐或溶剂化物

公开(公告)号：EP1827435A2

公开(公告)日：2007-09-05

申请号：EP05849528.4

申请日：2005-11-21

申请人： AMR Technology, Inc.

发明人： MOLINO, Bruce, F. ,  BERKOWITZ, Barry ,  COHEN, Marlene

IPC分类号： A61K31/472 ,  C07D217/04

CPC分类号： A61K31/47

摘要： The present invention relates to a method of treating disorders by administering a compound of the formulae IA-IF. These compounds are tetrahydroisoquinolines of the following structure: wherein R1-R8 for compounds of each of the formulae IA, IB, IC, ID, IE and IF are as described herein.

公开(公告)号：EP1541559A4

公开(公告)日：2007-08-22

申请号：EP03741482

申请日：2003-07-18

申请人： ASAHI KASEI PHARMA CORP

发明人： YAMADA RINTARO ,  SETO MINORU

IPC分类号： C07D401/12 ,  A61K31/472 ,  A61K31/4725 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D409/12

CPC分类号： C07D217/04 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D401/12 ,  C07D409/12

摘要： A compound represented by the following formula (1): (1) wherein R1 represents hydrogen, halogeno, etc.; R2 represents hydrogen, halogeno, C1-6 alkyl, etc.; R3 represents, e.g., -O-X-C(A1)(A11)-C(A2)(A21)-N(A31)(A3) (X represents propylene, etc.; A11 and A21 each represents hydrogen or C1-6 alkyl; A31 represents C1-6 hydroxyalkyl or hydrogen; and A1, A2, and A3 each represents hydrogen, C1-6 alkyl, etc.) or a salt of the compound. The compound or salt has myosin regulatory light-chain phosphorylation inhibitory activity and is useful in treatments for diseases to which contraction of various cells relates.

公开(公告)号：EP1780196A2

公开(公告)日：2007-05-02

申请号：EP06010095.5

申请日：2002-12-10

申请人： Amgen, Inc

发明人： Bo, Yunxin Y. ,  Chakrabarti, Partha P. ,  Chen, Ning ,  Doherty, Elizabeth M. ,  Fotsch, Christopher H. ,  Han, Nianhe ,  Kelly, Michael G. ,  Liu, Qingyian ,  Norman, Mark Henry ,  Ognyanov, Vassil I. ,  Wang, Xianghong ,  Zhu, Jiawang

IPC分类号： C07C233/11 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D265/36 ,  C07D241/40 ,  A61K31/4418 ,  A61K31/47 ,  A61P31/12 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D471/04 ,  C07D417/14

CPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Compounds having the general structure

and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

摘要翻译： 具有一般结构和含有它们的组合物的化合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管综合征，紧张性头痛，一般炎症，关节炎，风湿性 疾病，骨关节炎，炎症性肠病，炎症性眼病，炎性或不稳定性膀胱病，牛皮癣，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛及相关的痛觉过敏和异常性疼痛，糖尿病性神经病痛， 咳嗽痛，交感神经痛，交感综合症，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒症，白癜风，一般胃肠道疾病， G 腹部溃疡，十二指肠溃疡，腹泻，坏死因子诱发的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

公开(公告)号：EP1776119A1

公开(公告)日：2007-04-25

申请号：EP05775926.8

申请日：2005-08-10

申请人： GLAXO GROUP LIMITED

发明人： EDWARDS, Christine Argenta Discovery Limited ,  FENTON, Garry Argenta Discovery Limited ,  MACDONALD, Simon John Fawcett GlaxoSmithKline ,  WEINGARTEN, Gordon Gad GlaxoSmithKline

IPC分类号： A61K31/47 ,  C07D215/04 ,  C07D217/04 ,  A61K31/472 ,  A61P17/00 ,  A61P29/00

CPC分类号： C07C255/34 ,  C07C17/2635 ,  C07C25/24 ,  C07C45/29 ,  C07C45/30 ,  C07C45/69 ,  C07C47/273 ,  C07C49/233 ,  C07C49/237 ,  C07C57/50 ,  C07C255/33 ,  C07C2602/10 ,  C07D215/38 ,  C07D217/02 ,  C07D303/08

摘要： The present invention is directed to compounds of formula (I): wherein R represents a methyl or an ethyl group X represents N, C-H or C-CH3 when X represents C-H or C-CH3, Y represents N when X represents N, Y represents C-H and physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

摘要翻译： 本发明涉及式（I）化合物：其中R表示甲基或乙基，X表示N，C-H或C-CH 3，当X表示C-H或C-CH 3时，Y表示N，当X表示 N，Y表示C-H及其生理功能衍生物，包含该化合物的药物组合物，用于制备特别用于治疗炎症和/或过敏病症的药物的化合物的用途，用于制备化合物的方法和 在制造化合物的过程中的化学中间体。

公开(公告)号：EP1764358A3

公开(公告)日：2007-03-28

申请号：EP06010087.2

申请日：2002-12-10

申请人： Amgen, Inc

发明人： Bo, Yunxin Y. ,  Chakrabarti, Partha, P. ,  Chen, Ning ,  Doherty, Elisabeth M. ,  Fotsch, Cristopher H. ,  Han, Ninanhe ,  Kelly, Michael G. ,  Liu, Qingyian ,  Norman, Mark Henry ,  Ognyanov, Vassil I. ,  Wang, Xianghong ,  Zhu, Jiawang

IPC分类号： C07C233/11 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D265/36 ,  C07D241/40 ,  A61K31/4418 ,  A61K31/47 ,  A61P31/12 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D471/04 ,  C07D417/14

CPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Compounds having the general structure

and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, bums, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

公开(公告)号：EP1045837B1

公开(公告)日：2007-03-14

申请号：EP98966748.0

申请日：1998-12-23

申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

发明人： BRINGMANN, Gerhard ,  BOYD, Michael, R. ,  WENZEL, Matthias

IPC分类号： C07D217/02 ,  C07D217/04 ,  C07D217/24 ,  C07D491/04 ,  A61K31/47

CPC分类号： C07D491/04 ,  A61K31/47 ,  C07D217/02 ,  C07D217/04 ,  C07D217/24

摘要： The present invention provides new monomeric derivatives of the C-8'-7 linked naphthylisoquinoline alkaloid dioncophylline D. The invention also provides new C-4 substituted monomeric arylisoquinoline alkaloid derivatives. The present invention furthermore provides novel dimeric arylisoquinoline alkaloids comprised of coupled first and second arylisoquinoline monomers, wherein either or both of said monomer(s) is (are) monomeric compound(s) of the present invention. Monomeric and dimeric compounds of the present invention have medically useful properties, such as antimicrobial properties, more specifically such as antimalarial and antiviral properties. Monomeric compounds of the present invention are also useful as building blocks or intermediates for synthesis of novel dimeric arylisoquinoline alkaloids. Monomeric and dimeric compounds of the present invention may be obtained in substantially pure form by total synthesis, partial synthesis, or derivatization from known synthetic or naturally occurring compounds, and by isolation and purification from plants of the Dioncophyllaceae and Ancistrocladaceae families.

公开(公告)号：EP1556357A4

公开(公告)日：2006-09-13

申请号：EP03737085

申请日：2003-06-12

申请人： CYTOKINETICS INC ,  SMITHKLINE BEECHAM CORP

发明人： MCDONALD ANDREW ,  LU PU-PING ,  BERGNES GUSTAVE ,  MORGANS DAVID J JR ,  DHANAK DASHYANT ,  KNIGHT STEVEN DAVID

IPC分类号： C07D217/04 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K45/00 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D217/24 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D217/24

公开(公告)号：EP1389611A4

公开(公告)日：2006-06-07

申请号：EP02722849

申请日：2002-04-26

申请人： TAISHO PHARMA CO LTD

发明人： SATO MASAKAZU ,  MIYATA N ,  ISHII TAKAAKI ,  MATSUNAGA Y ,  AMADA HIDEAKI

IPC分类号： A61K31/136 ,  A61K31/402 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/4525 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/55 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P43/00 ,  C07C259/14 ,  C07D207/20 ,  C07D211/22 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D211/70 ,  C07D213/74 ,  C07D213/75 ,  C07D217/04 ,  C07D295/13 ,  C07D295/135 ,  C07D295/15 ,  C07D401/04 ,  C07D491/10 ,  C07D491/113 ,  C07D215/06 ,  C07D241/04 ,  C07D265/30 ,  C07D295/12

CPC分类号： C07D213/75 ,  A61K31/136 ,  A61K31/402 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/4525 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/55 ,  C07C259/14 ,  C07D207/20 ,  C07D211/22 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D211/70 ,  C07D213/74 ,  C07D217/04 ,  C07D295/13 ,  C07D295/135 ,  C07D295/15 ,  C07D401/04 ,  C07D491/10

摘要： Hydroxyformamidine compounds represented by the following general formula or pharmaceutically acceptable salts thereof: wherein R1 represents substituted morpholino, substituted piperidino, piperazin-1-yl, substituted piperazin-1-yl, thiomorpholin-1-yl, perhydroazepin-1-yl, perhydroazocin-1-yl, tetrahydropyridin-1-yl, pyrrolin-1-yl, etc.; X represents nitrogen or CR5; and R2 to R5 are the same or different and each represents hydrogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or halogeno. Drugs inhibiting 20-HETE synthase relating to contraction/dilation of microvessels, induction of cell proliferation, etc. in main organs such as kidney and cerebral vessels.