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91. 发明授权

US06288068B1 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06288068B1
公开(公告)日：2001-09-11
申请号：US09482168
申请日：2000-01-12
申请人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Javaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
发明人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Javaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
IPC分类号： C07D31495
CPC分类号： C07D211/20 , C07C2601/14 , C07D211/22 , C07D211/24 , C07D211/32 , C07D211/58 , C07D213/643 , C07D213/65 , C07D213/68 , C07D237/14 , C07D239/34 , C07D239/38 , C07D257/04 , C07D277/34 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D295/26 , C07D307/33 , C07D333/20 , C07D335/02 , C07D405/12 , C07D405/14 , C07D409/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X ，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和制备方法。还公开了上述化合物或能够与乙酰胆碱酯酶抑制剂一起增强乙酰胆碱释放的其它化合物的协同组合。

92. 发明授权

US5977138A Ether muscarinic antagonists 失效
标题翻译：醚类毒蕈碱拮抗剂
公开(公告)号：US5977138A
公开(公告)日：1999-11-02
申请号：US910616
申请日：1997-08-13
申请人： Yuguang Wang , Wei K. Chang , Sundeep Dugar , Samuel Chackalamannil
发明人： Yuguang Wang , Wei K. Chang , Sundeep Dugar , Samuel Chackalamannil
IPC分类号： A61K45/06 , C07D211/46 , C07D211/96 , C07D405/12 , C07D405/14 , C07D409/14 , A61K31/445 , C07D401/04
CPC分类号： C07D405/12 , A61K45/06 , C07D211/46 , C07D211/96 , C07D405/14 , C07D409/14
摘要： 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or an isomer, pharmaceutically acceptable salt, ester or solvate thereof, whereinX is a bond, --O--, --S--, --SO--, --SO.sub.2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O-- CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 -C.sub.6 alkyl)-, --C(C.sub.1 -C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --O--C(O)NR.sup.17 --, --NR.sup.17 C(O)--O--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --;R is cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl;R.sup.2 is H, alkyl, optionally substituted cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted piperidinyl; and the remaining variables are as defined in the specification, are disclosed. Compounds of formula I are useful for treating cognitive disorders such as Alzheimer's disease. Also disclosed are pharmaceutical compositions, methods of preparation and combinations of compounds of formula I with ACh'ase inhibitors.
摘要翻译： 1,4-二取代的式I的哌啶毒蕈碱拮抗剂或其异构体，药学上可接受的盐，酯或溶剂化物，其中X是键，-O - ， - S - ， - SO - ， - SO 2 - ， - ，-C（OR 7）2 - ， - CH 2 -O - ， - CH 2 - ， - CH = CH - ， - CH 2 - ， - CH（C 1 -C 6烷基） - ， - CONR 17 - ， - NR 17 CO - ， - OC（O）NR 17 - ， - NR 17 C（O）-O-，-SO 2 NR 17 - 或-NR 17 SO 2 - R是环烷基，任选取代的苯基或任选取代的吡啶基; R2是H，烷基，任选取代的环烷基，环烯基，叔丁氧羰基或任选取代的哌啶基; 并且其余变量如说明书中所定义。式I化合物可用于治疗认知障碍如阿尔茨海默病。还公开了药物组合物，制备方法和式I化合物与ACh酶抑制剂的组合。

93. 发明授权

US5883096A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US5883096A
公开(公告)日：1999-03-16
申请号：US602403
申请日：1996-02-16
申请人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
发明人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
IPC分类号： C07D295/08 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/365 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P25/28 , C07D211/14 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/32 , C07D211/58 , C07D211/62 , C07D239/34 , C07D257/04 , C07D271/06 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/14 , C07D295/145 , C07D295/15 , C07D307/33 , C07D309/12 , C07D317/28 , C07D317/62 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D307/81 , C07D333/58
CPC分类号： C07D211/20 , C07D211/22 , C07D211/24 , C07D211/32 , C07D211/58 , C07D213/643 , C07D213/65 , C07D213/68 , C07D237/14 , C07D239/34 , C07D239/38 , C07D257/04 , C07D277/34 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D295/26 , C07D307/33 , C07D333/20 , C07D335/02 , C07D405/12 , C07D405/14 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl;X is --O--, --SO.sub.0-2 --, amino, substituted amino, --CO--, --CH.sub.2 --, mono or di-substituted methylene, --CS--, --CONR.sup.20 --, --NR.sup.20 --SO.sub.2 --, --NR.sup.20 CO--, --SO.sub.2 NR.sup.20 --, --CH.dbd.CH--, --C.tbd.C-- or --NHC(O)NH--;R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification;R.sup.1 and R.sup.21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification;R.sup.2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; andR.sup.3, R.sup.4, R.sup.5, R.sup.20, R.sup.27 and R.sup.28 are as defined in the specification; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease; pharmaceutical compositions and methods of preparation are also disclosed, as well as synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
摘要翻译：式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物其中Y和Z之一是N，另一个是N，CH或C-烷基; X是-O - ， - SO 2 - ， - 氨基，取代的氨基，-CO - ， - CH 2 - ，单或二取代的亚甲基，-CS-，-CONR 20 - ，-NR 20 SO 2 - ， - -SO 2 NR 20 - ， - CH = CH - ， - C 3 CF 3 - 或-NHC（O）NH-; R是任选取代的苯基，芳基或环烷基，或说明书中定义的其它取代基; R1和R21是H，CN或任选取代的烷基，或说明书中定义的其它取代基; R2是任选取代的环烷基或哌啶基，或说明书中定义的其它取代基; R3，R4，R5，R20，R27和R28如说明书中所定义; 是可用于治疗认知障碍如阿尔茨海默病的毒蕈碱拮抗剂; 还公开了药物组合物和制备方法，以及上述化合物或能够与乙酰胆碱酯酶抑制剂一起增强乙酰胆碱释放的其它化合物的协同组合。

94. 发明授权

US5608067A 4-substituted pyrazoloquinoline derivatives 失效
标题翻译： 4-取代的吡唑并喹啉衍生物
公开(公告)号：US5608067A
公开(公告)日：1997-03-04
申请号：US234695
申请日：1994-04-28
申请人： Adriano Afonso , Joseph M. Kelly , Samuel Chackalamannil
发明人： Adriano Afonso , Joseph M. Kelly , Samuel Chackalamannil
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed herein are compounds of the formula ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.11, and c are as set forth herein are described. These compounds are useful as agents for the treatment of mammals infected with herpes group virus. Certain of these compounds are useful as antitumor agents.
摘要翻译：本文公开的是其中R 1，R 3，R 4，R 11和c如本文所述的式Ⅺ的化合物。这些化合物可用作治疗感染疱疹病毒的哺乳动物的药剂。这些化合物中的某些可用作抗肿瘤剂。

95. 发明授权

US5476847A Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors 失效
标题翻译：次膦酸的衍生物可用作内皮素转化酶抑制剂
公开(公告)号：US5476847A
公开(公告)日：1995-12-19
申请号：US267630
申请日：1994-06-29
申请人： Brian A. McKittrick , Michael F. Czarniecki , Samuel Chackalamannil , Shin Chung , Shawn DeFrees , Andrew W. Stamford
发明人： Brian A. McKittrick , Michael F. Czarniecki , Samuel Chackalamannil , Shin Chung , Shawn DeFrees , Andrew W. Stamford
IPC分类号： A61K31/66 , A61P1/00 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07F9/30 , C07F9/572 , C07F9/6558 , A61K31/405 , C07D209/14 , C07F9/36
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728
摘要： Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.7, wherein A.sub.2 is a divalent .alpha.-aminoacyl radical, and R.sub.7 is a substituent on the .alpha.-amino atom selected from H, R.sub.8 OCO--, R.sub.8 SO.sub.2 -- and R.sub.8 NHCO--, wherein R.sub.8 is aryl, arylmethyl or (C.sub.1 -C.sub.8)alkyl;are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R.sup.3 and R.sup.4 form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.
摘要翻译：结构式为“IMAGE”的次膦酸衍生物或其药学上可接受的盐，其中R为H，烷基或烷酰氧基亚甲基; R 1，R 2，R 3和R 4是H，烷基，烯基，链烯基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，羟基烷基，羧基烷基，硫代烷基，烷氧基硫代烷基，氨基烷基，烷基氨基烷基，环烷基取代的烷基或杂环烷基。或R 1和R 2形成3-8成员的环烷基环，并且R 3和R 4如所定义; 或R 3和R 4形成3-7成员的环烷基环，并且R 1和R 2如所定义; 或R 1和R 2一起，并且R 3和R 4一起形成环烷基环; R5是-OR9或-NHR9，其中R9是氢或烷基; n为0或1; A1是对氨基苯甲酰基或对氨基苯磺酰基，或者A1和R5一起形成α-氨基酰基衍生物的基团; R6为苯基甲氧基羰基，芳基羰基，杂芳基羰基或-A2-R7，其中A2为二价α-氨基酰基，R7为选自H，R8OCO-，R8SO2-和R8NHCO-的α-氨基原子上的取代基，其中R8 是芳基，芳甲基或（C1-C8）烷基; 被公开用作内皮素转化酶抑制剂; 还公开了一种其中R3和R4形成环烷基环的新化合物，以及包含所述新化合物的药物组合物。

96. 发明授权

US5089609A 4-benzoyl azetidinones 失效
标题翻译： 4-苯甲酰基氮杂环丁酮
公开(公告)号：US5089609A
公开(公告)日：1992-02-18
申请号：US621158
申请日：1990-11-30
申请人： Samuel Chackalamannil
发明人： Samuel Chackalamannil
IPC分类号： A47F5/02 , C07D205/08 , C07D303/48 , C07F7/18
CPC分类号： A47F5/02 , C07D205/08 , C07D303/48 , C07F7/1852
摘要： Compounds of the formula ##STR1## wherein each R' is independently hydrogen, one, two or three of halogen, lower alkyl or lower alkoxy and R" is methyl, ethyl, allyl or a phenyl, are described. These compounds are useful as intermediates in preparing penems and carbapenems.
摘要翻译：描述式VIII的化合物，其中每个R'独立地是氢，一个，两个或三个卤素，低级烷基或低级烷氧基，R“是甲基，乙基，烯丙基或苯基。这些化合物可用作制备青霉烯和碳青霉烯类的中间体。

97. 发明授权

US08815876B2 Bicyclic heterocycle derivatives and methods of use thereof 有权
标题翻译：双环杂环衍生物及其使用方法
公开(公告)号：US08815876B2
公开(公告)日：2014-08-26
申请号：US13003716
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Bernard R. Neustadt , Samuel Chackalamannil , William J. Greenlee
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Bernard R. Neustadt , Samuel Chackalamannil , William J. Greenlee
IPC分类号： C07D519/00 , A61K31/519 , A61P13/12 , A61P3/04
CPC分类号： C07D519/00
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
摘要翻译：本发明涉及双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖症，糖尿病，糖尿病并发症，代谢紊乱，心血管疾病或与该活动相关的病症的方法的G蛋白偶联受体（GPCR）。化合物为结构（I）。

98. 发明申请

US20140219989A1 FACTOR IXA INHIBITORS 有权
标题翻译：因子IXA抑制剂
公开(公告)号：US20140219989A1
公开(公告)日：2014-08-07
申请号：US14131469
申请日：2012-07-03
申请人： Craig Boyle , William Greenlee , Samuel Chackalamannil , Claire Lankin
发明人： Craig Boyle , William Greenlee , Samuel Chackalamannil , Claire Lankin
IPC分类号： C07D401/12 , A61K31/167 , C07D261/20 , A61K31/423 , C07D217/22 , A61K31/472 , C07D295/192 , A61K31/5375 , A61K31/5377 , C07D215/38 , A61K31/47 , C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07C235/16
CPC分类号： A61K31/167 , A61K31/423 , A61K31/47 , A61K31/472 , A61K31/505 , A61K31/506 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07C235/16 , C07C235/38 , C07C257/18 , C07D215/38 , C07D217/22 , C07D239/42 , C07D261/20 , C07D295/192 , C07D401/12
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：本发明提供本文所述的式（I）化合物或其药学上可接受的盐。本发明还提供包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。

99. 发明授权

US08389532B2 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-E]-[1,2,4]-triazolo-[1,5-C]-pyrimidin-5-amine 有权
标题翻译： 7- [2- [4-（6-氟-3-甲基-1,2-苯并异恶唑-5-基）-1-哌嗪基]乙基] -2-（1-丙炔基）-7H-吡唑并[4， 3-E] - [1,2,4] - 三唑并 - [1,5-C] - 嘧啶-5-胺
公开(公告)号：US08389532B2
公开(公告)日：2013-03-05
申请号：US12498013
申请日：2009-07-06
申请人： Craig D. Boyle , Samuel Chackalamannil , Unmesh Shah , Jean E. Lachowicz
发明人： Craig D. Boyle , Samuel Chackalamannil , Unmesh Shah , Jean E. Lachowicz
IPC分类号： A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D487/14
摘要： The compound having the structural formula I or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular Parkinson's disease, Extra Pyramidal Syndrome, restless legs syndrome and attention deficit hyperactivity disorder, pharmaceutical compositions comprising it, and combinations with other agents.
摘要翻译：公开了具有结构式I的化合物或其药学上可接受的盐，以及其用于治疗中枢神经系统疾病，特别是帕金森病，额外金字塔综合征，不宁腿综合征和注意缺陷多动障碍，药物包含它的组合物，以及与其它试剂的组合。

100. 发明申请

US20110237559A1 6-SUBSTITUTED SULFONYL AZABICYCLO[3.2.1]OCTANES USEFUL TO INHIBIT 11Beta-HYDROXYSTEROID DEHYDROGENASE TYPE-1 有权
标题翻译： 6-取代的亚磺酰氨基胆碱[3.2.1]有用于抑制11Beta羟化酶脱氢酶1型
公开(公告)号：US20110237559A1
公开(公告)日：2011-09-29
申请号：US12672817
申请日：2008-08-12
申请人： Craig D. Boyle , Samuel Chackalamannil , Unmesh Shah , Claire M. Lankin
发明人： Craig D. Boyle , Samuel Chackalamannil , Unmesh Shah , Claire M. Lankin
IPC分类号： A61K31/56 , C07D209/02 , A61K31/403 , A61P3/06 , A61P3/04 , A61P3/10 , A61P9/10 , C07D409/12 , A61K31/422 , C07D413/12 , C07D405/12 , C07D401/12 , A61K31/4439 , A61K31/4245 , C07D403/12 , A61K31/4155 , A61K31/5377 , C07D413/14 , A61K31/433 , C07D417/12 , C12N5/02
CPC分类号： C07D487/08
摘要： In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11β-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11β-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明涉及可用于抑制11-羟基类固醇脱氢酶I型药物的新一类6-取代磺酰基-1,3,3-三烷基-6-氮杂双环[3.2.1]辛烷化合物含有该化合物的组合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与表达11β-羟基类固醇脱氢酶I相关的一种或多种病症的方法。

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