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1.发明授权N-substituted tricyclic 3-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders 有权N-取代的三环3-氨基吡唑作为治疗细胞增殖性疾病的抑制剂公开(公告)号：US07196110B2
公开(公告)日：2007-03-27
申请号：US10438152
申请日：2003-05-14
申请人： Chih Yung Ho , Bengt Anders Brunmark , Stuart Emanuel , Robert A. Galemmo, Jr. , Dana L. Johnson , Donald W. Ludovici , Umar Maharoof , Jay M. Mei , Jan L. Sechler , Eric D. Strobel , Robert W. Tuman , Hwa Kwo Yen
发明人： Chih Yung Ho , Bengt Anders Brunmark , Stuart Emanuel , Robert A. Galemmo, Jr. , Dana L. Johnson , Donald W. Ludovici , Umar Maharoof , Jay M. Mei , Jan L. Sechler , Eric D. Strobel , Robert W. Tuman , Hwa Kwo Yen
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： C07F9/65038 , C07D231/54 , C07D231/56 , C07D233/64 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D491/04 , C07D495/04
摘要： The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell proliferative disorders.
摘要翻译： 本发明涉及可用作血小板衍生生长因子受体（PDGF-R）激酶抑制剂的N-取代三环3-氨基吡唑衍生物，以及制备所述衍生物的方法。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如肿瘤和其它细胞增殖性疾病的病症的方法。
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公开(公告)号：US06403620B1
公开(公告)日：2002-06-11
申请号：US09393782
申请日：1999-09-10
申请人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
发明人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
IPC分类号： A61K314192
CPC分类号： C07D257/04 , C07D231/14 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12
摘要： The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
摘要翻译： 本申请描述了具有式I的中性P1特异性基团的因子Xa抑制剂或其药学上可接受的盐形式，其中R和E可以是例如甲氧基和卤素的基团。
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3.发明授权Nitrogen containing heteromatics with ortho-substituted P1s as factor Xa inhabitors 有权含有邻位取代的P1的含氮异构体作为因子Xa居民公开(公告)号：US06271237B1
公开(公告)日：2001-08-07
申请号：US09217336
申请日：1998-12-21
IPC分类号： A61K31415
CPC分类号： C07D257/04 , C07D231/14 , C07D231/22 , C07D231/24 , C07D249/04 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.
摘要翻译： 本申请描述了具有式I的邻位取代的P1及其衍生物的含氮杂芳族化合物：或其药学上可接受的盐或前药形式，其中J为N或NH且D与E上的G邻位取代，并且可为CH 2 NH 2，其为 可用作因子Xa的抑制剂。
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4.发明授权
公开(公告)号：US4920131A
公开(公告)日：1990-04-24
申请号：US209428
申请日：1988-06-21
IPC分类号： C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D401/12
CPC分类号： C07D401/12 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20
摘要： This invention relates to quinolinyl compounds of the general formula: ##STR1## and the use of these compounds as pharmacological agents which are lipoxygenase inhibitors and/or leukotriene antagonists possessing anti-inflammatory and anti-allergic properties and their pharmaceutical compositions and processes for this preparation.
摘要翻译： 本发明涉及以下通式的喹啉基化合物：＆lt; IMAGE＆gt;＆gt;图像和这些化合物作为具有抗炎和抗过敏性质的脂氧合酶抑制剂和/或白三烯拮抗剂的药理学及其药物组合物的用途 和该制备方法。
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5.发明授权3- and 5-(bicyclic ether or bicyclic alkylene thioether) alkylene amino thiatriazines 失效3-和5-（双环醚或双环亚烷基硫醚）亚烷基氨基硫杂三嗪
公开(公告)号：US4816583A
公开(公告)日：1989-03-28
申请号：US130393
申请日：1987-12-09
申请人： Donald E. Kuhla , Henry F. Campbell , William L. Studt , Stuart A. Dodson , Robert A. Galemmo, Jr. , Pamela J. Durham
发明人： Donald E. Kuhla , Henry F. Campbell , William L. Studt , Stuart A. Dodson , Robert A. Galemmo, Jr. , Pamela J. Durham
IPC分类号： C07D285/00 , C07D285/15 , C07F7/18
CPC分类号： C07D285/15 , C07F7/1896
摘要： A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including gastrointestinal anti-ulcerogenic and cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
摘要翻译： 一类具有药理活性的包括胃肠道抗溃疡发生和细胞保护活性的药物组合物的药用组合物，以及使用所述组合物治疗哺乳动物胃肠胃酸过多和溃疡性疾病的方法的3-和5-氨基硫代三嗪化合物。
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公开(公告)号：US20110212942A1
公开(公告)日：2011-09-01
申请号：US12974401
申请日：2010-12-21
申请人： Robert A. Galemmo , Dean R. Artis , Xiaocong Michael Ye , Danielle Aubele , Anh Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
发明人： Robert A. Galemmo , Dean R. Artis , Xiaocong Michael Ye , Danielle Aubele , Anh Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
IPC分类号： A61K31/55 , C07D475/00 , C07D471/14 , C07D487/14 , C07D498/14 , A61K31/4985 , A61K31/5383 , A61P35/00 , A61P25/28 , A61P25/16 , A61P35/02 , A61P35/04
CPC分类号： C07D475/00 , A61K31/519 , A61K31/5377 , A61K31/5383 , C07D475/04 , C07D475/12 , C07D487/14 , C07D498/14 , C07D519/00
摘要： The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
摘要翻译： 本发明提供具有式（I）结构的化合物或其盐或溶剂化物，其中环A，X，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。 本发明进一步提供包含本发明化合物的药物组合物以及制备和使用本发明化合物和组合物的方法，例如治疗和预防各种疾病如帕金森病。
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公开(公告)号：US5998424A
公开(公告)日：1999-12-07
申请号：US99752
申请日：1998-06-18
申请人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
发明人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
IPC分类号： C07D231/14 , C07D257/04 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , A01N43/54 , C07D211/32 , C07D277/64
CPC分类号： C07D257/04 , C07D231/14 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12
摘要： The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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8.发明授权Substituted naphthylene compounds exhibiting selective leukotriene B.sub.4 antagonist activity 失效显示出选择性白三烯B4拮抗剂活性的取代的亚萘基化合物
公开(公告)号：US5468898A
公开(公告)日：1995-11-21
申请号：US777246
申请日：1993-04-23
IPC分类号： A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/42 , A61K31/423 , A61K31/47 , A61K31/496 , A61K31/52 , A61P3/00 , A61P25/00 , A61P29/00 , C07C235/34 , C07C259/06 , C07D209/00 , C07D209/12 , C07D209/18 , C07D209/24 , C07D209/32 , C07D209/42 , C07D213/30 , C07D215/12 , C07D215/14 , C07D257/04 , C07D263/56 , C07D263/58 , C07D403/06 , C07D471/04 , C07D473/02 , C07C233/51
CPC分类号： C07D403/06 , C07C235/34 , C07D209/12 , C07D209/24 , C07D209/42
摘要： This invention relates to bicyclic aryl compounds having selective LTB.sub.4 antagonist properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, and to methods for the treatment of disorders which result from LTB.sub.4 activity and pharmaceutical compositions including such compounds.
摘要翻译： PCT No.PCT / US91 / 06447 Sec。 371日期：1993年4月23日 102（e）日期1993年4月23日PCT 1991年9月6日PCT PCT。 公开号WO92 / 04315 本发明涉及具有选择性LTB4拮抗剂性质并包含酰氨基取代基的双环芳基化合物，具有末端羧酸或其衍生物的取代基和亲脂性取代基，以及用于治疗疾病的方法 LTB4活性的结果和包括这些化合物的药物组合物。
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公开(公告)号：US5028615A
公开(公告)日：1991-07-02
申请号：US499513
申请日：1990-04-20
IPC分类号： A61K31/47 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D401/10 , C07D401/12
CPC分类号： C07D401/10 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D401/12
摘要： This invention relates to certain quinoline-diaryl compounds and their use as leukotriene D.sub.4 antagonists for the treatment of hypersensitive disorders.
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10.发明授权N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors 有权N-取代的三环3-氨基吡唑作为抗有丝分裂的微管蛋白聚合抑制剂公开(公告)号：US07816390B2
公开(公告)日：2010-10-19
申请号：US12021535
申请日：2008-01-29
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： C07D231/54 , C07D401/12
摘要： The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol; or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译： 本发明涉及具有以下结构的化合物：N-（3-乙氧基苯基）-1,4-二氢-6-乙氧基-7-（3-羟基丙氧基）-1-甲基茚并[1,2-c]吡唑-3 -胺; 3- [3-（3-溴 - 苯基氨基）-6-乙氧基-1-甲基-1,4-二氢 - 茚并[1,2-c]吡唑-7-基氧基] - 丙-1-醇; 或3- [3-（2-氯 - 吡啶-4-基氨基）-6-乙氧基-1-甲基-1,4-二氢 - 茚并[1,2-c]吡唑-7-基氧基] - 丙-1 - 醇和N-氧化物，其药学上可接受的盐，溶剂合物，互变异构体和立体化学异构体，以及这些化合物作为微管蛋白聚合抑制剂和用于治疗实体瘤的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。
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