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91. 发明申请

WO2005070042A3 NOVEL CHEMICAL COMPOUNDS 审中-公开
标题翻译：新化学化合物
公开(公告)号：WO2005070042A3
公开(公告)日：2005-09-29
申请号：PCT/US2005000303
申请日：2005-01-06
申请人： SMITHKLINE BECKMAN CORP , HASEGAWA MASAICHI , KANO KAZUYA , NAKANO MASATO , YAMABE MARIKO
发明人： HASEGAWA MASAICHI , KANO KAZUYA , NAKANO MASATO , YAMABE MARIKO
IPC分类号： A61K31/425 , C07D277/04 , C07D277/38 , C07D277/56 , C07D417/04 , C07D417/14
CPC分类号： C07D277/56 , C07D417/04 , C07D417/14
摘要： This invention relates to newly identified compounds for inhibiting hYAK3 and/or CK2 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 and/or CK2 proteins.
摘要翻译：本发明涉及新鉴定的用于抑制hYAK3和/或CK2蛋白的化合物和用于治疗与hYAK3和/或CK2蛋白的不平衡或不适当活性相关的疾病的方法。

92. 发明申请

WO2004099170A3 PHENYL SUBSTITUTED CARBOXYLIC ACIDS AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE-1B 审中-公开
标题翻译：作为蛋白酪氨酸磷酸化酶1B的抑制剂的苯基取代的羧酸
公开(公告)号：WO2004099170A3
公开(公告)日：2005-09-15
申请号：PCT/US2004013701
申请日：2004-04-30
申请人： INST OF PHARMACEUTICAL DISCOVE , WHITEHOUSE DARREN , HU SHAOJING , FANG HAIQUAN , VAN ZANDT MICHAEL
发明人： WHITEHOUSE DARREN , HU SHAOJING , FANG HAIQUAN , VAN ZANDT MICHAEL
IPC分类号： C07C311/19 , C07C311/29 , C07D209/08 , C07D233/62 , C07D277/38 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/91 , C07D401/04 , A61K31/343 , A61P3/10 , C07C307/00
CPC分类号： C07D307/79 , C07C311/19 , C07C311/29 , C07D209/08 , C07D307/80 , C07D307/81 , C07D307/91 , C07D401/04
摘要： Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译：公开了式（A）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗，瘦素抗性或高血糖相关的代谢紊乱。本发明的化合物包括可用于治疗糖尿病和其它PTP介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶抑制剂，特别是蛋白质酪氨酸磷酸酶-1B（PTP-1B）。还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。

93. 发明申请

WO2004021997A8 INHIBITORS OF FUNGAL INVASION 审中-公开
标题翻译：真菌侵入抑制剂
公开(公告)号：WO2004021997A8
公开(公告)日：2004-07-29
申请号：PCT/US0327911
申请日：2003-09-08
申请人： MICROBIA INC , TALLEY JOHN JEFFREY , FRETZEN ANGELIKA , ZIMMERMAN CRAIG , BARDEN TIMOTHY , YANG JING JING , MARTINEZ EDUARDO , BUSBY ROBERT , CORDERO ETCHELL A , CIPRIANO FARIBA HOUMAN , PIERCE CHRISTINE M , SUMMERS ERIC F
发明人： TALLEY JOHN JEFFREY , FRETZEN ANGELIKA , ZIMMERMAN CRAIG , BARDEN TIMOTHY , YANG JING JING , MARTINEZ EDUARDO , BUSBY ROBERT , CORDERO ETCHELL A , CIPRIANO FARIBA HOUMAN , PIERCE CHRISTINE M , SUMMERS ERIC F
IPC分类号： A01N43/80 , A61K31/42 , C07D261/14 , C07D261/16 , C07D277/38 , C07D277/56 , C07D413/12 , C07D417/12 , A01N25/00 , C07D277/04 , C07D277/18 , C07D277/20
CPC分类号： C07D413/12 , A01N43/80 , C07D261/16 , C07D417/12
摘要： This invention relates to isoxazole-based inhibitors of fungal invasion.
摘要翻译：本发明涉及基于异恶唑的真菌侵入抑制剂。

94. 发明申请

WO2004001059A2 HETEROCYCLIC INHIBITORS OF KINASES 审中-公开
标题翻译： KINASES的杂环抑制剂
公开(公告)号：WO2004001059A2
公开(公告)日：2003-12-31
申请号：PCT/US0319243
申请日：2003-06-18
申请人： SQUIBB BRISTOL MYERS CO , BORZILLERI ROBERT M , TOKARSKI JOHN S , BHIDE RAJEEV S
发明人： BORZILLERI ROBERT M , TOKARSKI JOHN S , BHIDE RAJEEV S
IPC分类号： C07D277/20 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P35/00 , A61P43/00 , C07D233/70 , C07D233/84 , C07D233/88 , C07D263/28 , C07D263/46 , C07D263/48 , C07D277/34 , C07D277/36 , C07D277/38 , C07D277/42 , C07D417/12 , C07D417/14 , C12Q
CPC分类号： C07D277/42 , C07D417/12 , C07D417/14
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式（I）化合物抑制生长因子受体如VEGFR-2，FGFR-1的酪氨酸激酶活性，从而使其成为抗癌剂。式（I）化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。

95. 发明申请

WO03002530A2 PYRROLIDINES AS DIPEPTIDYL PEPTIDASE INHIBITORS 审中-公开
标题翻译：吡咯啉作为DIPEPTIDYL PEPTIDASE抑制剂
公开(公告)号：WO03002530A2
公开(公告)日：2003-01-09
申请号：PCT/US0220466
申请日：2002-06-26
申请人： SMITHKLINE BEECHAM CORP , HAFFNER CURT DALE , MCDOUGALD DARRYL LYNN , RANDHAWA AMARJIT SAB , REISTER STEVEN MICHAEL , DEATON DAVID N , LENHARD JAMES MARTIN
发明人： HAFFNER CURT DALE , MCDOUGALD DARRYL LYNN , RANDHAWA AMARJIT SAB , REISTER STEVEN MICHAEL , DEATON DAVID N , LENHARD JAMES MARTIN
IPC分类号： A61K31/40 , A61K31/401 , A61K31/426 , A61P1/04 , A61P1/10 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/04 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/06 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/18 , A61P25/24 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/16 , C07D207/26 , C07D207/273 , C07D207/48 , C07D277/06 , C07D277/38 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D451/04 , C07D207/00
CPC分类号： C07D207/273 , C07D207/16 , C07D207/48 , C07D277/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D451/04
摘要： The present invention relates to novel compounds of formula (I):, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.
摘要翻译：本发明涉及式（I）的新型化合物：它们用于抑制丝氨酸蛋白酶的用途，例如二肽基肽酶如二肽基肽酶IV（DPP-IV）及其制备方法及其治疗效用。

96. 发明申请

WO0174793A3 SUBSTITUTED THIAZOLES AND THE USE THEREOF AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 审中-公开
标题翻译：取代的THIAZOLES及其作为PLASMINOGEN ACTIVATOR INHIBITOR-1的抑制剂的用途
公开(公告)号：WO0174793A3
公开(公告)日：2002-05-16
申请号：PCT/US0110307
申请日：2001-04-02
申请人： DIMENSIONAL PHARM INC , DHANOA DALE S , RYAN DECLAN E , DECKMAN INGRID , SAPIENZA ANTHONY
发明人： DHANOA DALE S , RYAN DECLAN E , DECKMAN INGRID , SAPIENZA ANTHONY
IPC分类号： C07D277/38 , C07D277/42 , C07D417/04 , A61K31/425 , C07D277/22
CPC分类号： C07D417/04 , C07D277/38 , C07D277/42
摘要： The present invention relates to the use of aminothiazole derivatives of Formula (I) of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as inhibitors of PAI-1. It has been discovered that compounds of Formula (I): or a solvate, hydrate or a pharmaceutically acceptable salt thereof, wherein Y, Ar , Ar , R , R , Z, m and n are described in the specification, inhibit plasminogen activator inhibitor-1 (PAI-1). These compounds can be used in the prophylaxis or for the treatment of thrombosis, angina pectoris, cerebral infarction, myocardial infarction, pulmonary infarction, intra-atrial thrombus in atrial fibrillation, deep venous thrombus, disseminated intravascular coagulation syndrome, diabetic complications, restenosis and stroke.
摘要翻译：本发明涉及式（I）的氨基噻唑衍生物作为PAI-1抑制剂的用途，以及新类别的氨基噻唑衍生物的用途及其作为PAI-1抑制剂的用途。已经发现式（I）化合物或其溶剂化物，水合物或其药学上可接受的盐，其中Y，Ar 1，Ar 2，R 1，R 2，Z，m 和n在本说明书中描述，抑制纤溶酶原激活物抑制剂-1（PAI-1）。这些化合物可用于预防或治疗血栓形成，心绞痛，脑梗死，心肌梗塞，肺梗死，心房颤动中的心房内血栓，深静脉血栓，弥散性血管内凝血综合征，糖尿病并发症，再狭窄和中风。

97. 发明申请

WO02014291A1 PPAR delta ACTIVATORS 审中-公开
公开(公告)号：WO02014291A1
公开(公告)日：2002-02-21
申请号：PCT/JP2001/006836
申请日：2001-08-09
IPC分类号： A61P3/04 , A61P3/06 , A61P3/10 , A61P5/38 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D233/64 , C07D233/70 , C07D233/88 , C07D233/90 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/38 , C07D413/04 , A61K31/4164 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , C07D263/34 , C07D263/48 , C07D417/04
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24
摘要： Compounds of the general formula (¦) or salts thereof; and activators of PPAR delta (peroxisome proliferator activated receptor delta ) containing the compounds or the salts as the active ingredient: (I) wherein R and R are each hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X and X are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(=O), C(=O)NH, NHC(=O), CH=CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R and R are each optionally substituted C1-8 alkyl; and R is hydrogen or C1-8 alkyl, with the proviso that when X is a free valency, X is not O or S(O)p, while when X is C(=O)NH, X is not a free valency.
摘要翻译：通式（|）的化合物或其盐; 和含有化合物或盐的PPARδ（过氧化物酶体增殖物激活受体δ）的活化剂作为活性成分：（I）其中R 1和R 2各自为氢，C 1-8烷基，芳基或杂环基其可以被取代;等等; A是氧，硫等; X 1和X 2各自为自由价，氧，S（O）p（其中p为0至2的整数），C（= O），C（= O）NH，NHC（= O），CH = CH等; Y是任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基，条件是当X 1是自由价时，X 2不是O或S（O）p，而当X 1是C（O） = O）NH，X 2不是自由价。

98. 发明申请

WO01051487A1 NON-PEPTIDYL INHIBITORS OF VLA-4 DEPENDENT CELL BINDING USEFUL IN TREATING INFLAMMATORY, AUTOIMMUNE, AND RESPIRATORY DISEASES 审中-公开
标题翻译： VLA-4依赖性细胞结合的非肽抑制剂有助于治疗炎症，自身免疫和呼吸道疾病
公开(公告)号：WO01051487A1
公开(公告)日：2001-07-19
申请号：PCT/IB2000/001893
申请日：2000-12-15
IPC分类号： A61K31/135 , A61K31/137 , A61K31/198 , A61K31/275 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/436 , A61K31/519 , A61K31/522 , A61K31/56 , A61K31/58 , A61K31/606 , A61K31/635 , A61K31/675 , A61K38/00 , A61K38/21 , A61P1/00 , A61P3/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P11/08 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/04 , A61P37/06 , C07C229/34 , C07C233/47 , C07C275/42 , C07C311/06 , C07D233/64 , C07D235/10 , C07D235/14 , C07D261/08 , C07D277/22 , C07D277/38 , C07D413/04
CPC分类号： C07D413/04 , C07C229/34 , C07C233/47 , C07C311/06 , C07D235/14 , C07D261/08
摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of formula (1.0.0) and pharmaceutically acceptable salts and other prodrug derivatives thereof.
摘要翻译：公开了一种非肽基化合物，其中所述化合物是可用于治疗炎性，自身免疫性和呼吸系统疾病的VLA-4抑制剂，其中所述化合物包含式（1.0.0）化合物及其药学上可接受的盐和其它其前药衍生物。

99. 发明申请

WO00033841A1 MYT1 KINASE INHIBITORS 审中-公开
标题翻译： MYT1激酶抑制剂
公开(公告)号：WO00033841A1
公开(公告)日：2000-06-15
申请号：PCT/US1999/028990
申请日：1999-12-07
IPC分类号： C12N9/99 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4439 , A61P9/00 , A61P17/06 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D277/20 , C07D277/38 , C07D277/42 , C07D417/04 , C07D417/14 , C12Q1/04 , A61K31/44 , C07D417/10
CPC分类号： C07D417/14 , C07D277/42
摘要： Novel myt1 kinase receptor antagonists and methods of using them are provided.
摘要翻译：本发明涉及新型myt1激酶受体拮抗剂及其使用方法。

100. 发明申请

WO99046253A1 HETEROCYCLYL ANTHRACYCLINONE DERIVATIVES 审中-公开
标题翻译：杂环烷基蒽醌衍生物
公开(公告)号：WO99046253A1
公开(公告)日：1999-09-16
申请号：PCT/EP1999/001554
申请日：1999-03-04
IPC分类号： A61K31/65 , A61P25/00 , A61P25/28 , C07D233/88 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D417/04 , A61K31/415 , A61K31/425
CPC分类号： C07D417/04 , C07D233/88 , C07D277/40 , C07D277/42
摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy; R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
摘要翻译：式（1）的化合物，其中R 1是氢，羟基，式OR 5的基团，其中R 5是C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 8环烷基，卤素，可被未被取代或被C1单或二取代的氨基 C 6烷基，C 2 -C 6烯基，芳烷基，酰基或三氟乙酰基; R 2是氢，羟基，NR 6 R 7基团，其中R 6和R 7独立地表示氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或与氮原子一起代表任选取代的C 3 -C 8 杂环 R3是氢，羟基; R4是2-取代的噻唑基或咪唑基系统及其药学上可接受的盐，可用于治疗淀粉样变性。还描述了制备方法和药物组合物。

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