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1.发明申请Indolinone derivatives and their use in treating disease-states such as cancer 失效吲哚酮衍生物及其在治疗疾病状态如癌症中的应用公开(公告)号：US20050090541A1
公开(公告)日：2005-04-28
申请号：US10972023
申请日：2004-10-22
申请人： Damian Arnaiz , Judi Bryant , Yuo-Ling Chou , Richard Feldman , Paul Hrvatin , Imadul Islam , Monica Kochanny , Wheeseong Lee , Mark Polokoff , Hongyi Yu , Shendong Yuan
发明人： Damian Arnaiz , Judi Bryant , Yuo-Ling Chou , Richard Feldman , Paul Hrvatin , Imadul Islam , Monica Kochanny , Wheeseong Lee , Mark Polokoff , Hongyi Yu , Shendong Yuan
IPC分类号： A61K31/405 , C07D209/34 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D407/14 , C07D409/06 , C07D413/14 , C07D43/02
CPC分类号： C07D209/34 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06
摘要： Indolinone derivatives, such as compounds of the formula (I): wherein A, m, n, R1, R2, R3, R5 and R6 are described herein, are disclosed herein as being useful in treating mammal having disease-states alleviated by the inhibition of PDK-1 activity.
摘要翻译： 吲哚啉酮衍生物，例如式（I）的化合物：其中A，m，n，R 1，R 2，R 3， 本文所述的本文所述的R 5和R 6 6可用于治疗通过抑制PDK-1活性而减轻疾病的哺乳动物。
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2.发明授权Indolinone derivatives and their use in treating disease-states such as cancer 失效吲哚酮衍生物及其在治疗疾病状态如癌症中的应用公开(公告)号：US07105563B2
公开(公告)日：2006-09-12
申请号：US10972023
申请日：2004-10-22
申请人： Damian Arnaiz , Judi Bryant , Yuo-Ling Chou , Richard Feldman , Paul Hrvatin , Imadul Islam , Monica Kochanny , Wheeseong Lee , Mark Polokoff , Hongyi Yu , Shendong Yuan
发明人： Damian Arnaiz , Judi Bryant , Yuo-Ling Chou , Richard Feldman , Paul Hrvatin , Imadul Islam , Monica Kochanny , Wheeseong Lee , Mark Polokoff , Hongyi Yu , Shendong Yuan
IPC分类号： A61K31/404 , C07D209/34
CPC分类号： C07D209/34 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06
摘要： Indolinone derivatives, such as compounds of the formula (I): wherein A, m, n, R1, R2, R3, R5 and R6 are described herein, are disclosed herein as being useful in treating mammal having disease-states alleviated by the inhibition of PDK-1 activity.
摘要翻译： 吲哚啉酮衍生物，例如式（I）的化合物：其中A，m，n，R 1，R 2，R 3， 本文所述的本文所述的R 5和R 6 6可用于治疗通过抑制PDK-1活性而减轻疾病的哺乳动物。
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公开(公告)号：US20060167044A1
公开(公告)日：2006-07-27
申请号：US11305322
申请日：2005-12-19
申请人： Damian Arnaiz , Yuo-Ling Chou , Monica Kochanny , Wheeseong Lee , Shou-Fu Lu , Anne Mengel , Gary Phillips , Guo Wei , Hongyi Yu
发明人： Damian Arnaiz , Yuo-Ling Chou , Monica Kochanny , Wheeseong Lee , Shou-Fu Lu , Anne Mengel , Gary Phillips , Guo Wei , Hongyi Yu
IPC分类号： A61K31/4709 , A61K31/454 , C07D401/02 , C07D409/02
CPC分类号： C07D211/34 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/70 , C07D401/06 , C07D401/12 , C07D409/06 , C07D409/12 , C07D413/12
摘要： Piperidine derivatives of the following formulae I and II: and their pharmaceutically acceptable salts, which are functional antagonists of the CC chemokine receptor CCR1 and are thus useful as anti-inflammatory agents, a pharmaceutical compositions containing said piperidine derivatives or their pharmaceutically acceptable salts, and methods of their use.
摘要翻译： 下式I和II的哌啶衍生物及其药学上可接受的盐，其是CC趋化因子受体CCR1的功能性拮抗剂，因此可用作抗炎剂，含有所述哌啶衍生物或其药学上可接受的盐的药物组合物，以及 使用方法
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公开(公告)号：US20060142363A1
公开(公告)日：2006-06-29
申请号：US11360048
申请日：2006-02-22
申请人： Damian Arnaiz , Yuo-Ling Chou , Brian Griedel , Raju Mohan , Kenneth Shaw
发明人： Damian Arnaiz , Yuo-Ling Chou , Brian Griedel , Raju Mohan , Kenneth Shaw
IPC分类号： A61K31/4166 , C07D233/88
CPC分类号： C07D235/02 , C07D233/76 , C07D233/78 , C07D401/06 , C07D491/04
摘要： A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity. The compound is of the following formula: wherein A, B, R1, R2, R3 and R4 are as defined herein or an isomer or isomeric mixture thereof or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20070155726A1
公开(公告)日：2007-07-05
申请号：US11644244
申请日：2006-12-22
申请人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye
发明人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye
IPC分类号： A61K31/551 , A61K31/495 , A61K31/46 , A61K31/445 , A61K31/407
CPC分类号： C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
摘要翻译： 本发明涉及式（I）化合物：其中r，q，R，R 2，R 3，R 4，R R 5，R 5b，R 5c，R 6a，R 6b，R 6b，R 6b，R 6b，R 6b， 本文描述了作为单一立体异构体或作为其中R 1，R 2，R 8和R 9的混合物 立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药; 其是白三烯A 4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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公开(公告)号：US20100210630A1
公开(公告)日：2010-08-19
申请号：US12771659
申请日：2010-04-30
申请人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
发明人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC分类号： A61K31/551 , C07D487/08 , A61K31/504 , C07D243/08 , C07D263/32 , A61K31/421 , C07D211/58 , A61K31/4468 , C07D207/09 , A61K31/40 , C07D413/00 , A61K31/5377 , A61P29/00
CPC分类号： C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
摘要翻译： 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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公开(公告)号：US07737145B2
公开(公告)日：2010-06-15
申请号：US11644244
申请日：2006-12-22
申请人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
发明人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC分类号： A01N43/60 , A61K31/495 , C07D241/36 , C07D271/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00 , C07D498/00 , C07D513/00
CPC分类号： C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
摘要翻译： 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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公开(公告)号：US20060223833A1
公开(公告)日：2006-10-05
申请号：US11345666
申请日：2006-02-02
申请人： Volker Schulze , Knut Eis , Lars Wortmann , Dirk Kosemund , Olaf Prien , Gerhard Siemeister , Holger Hess-Stumpp , Uwe Eberspaecher , Damian Arnaiz
发明人： Volker Schulze , Knut Eis , Lars Wortmann , Dirk Kosemund , Olaf Prien , Gerhard Siemeister , Holger Hess-Stumpp , Uwe Eberspaecher , Damian Arnaiz
IPC分类号： A61K31/506 , A61K31/4709 , A61K31/4439 , A61K31/427 , C07D417/02
CPC分类号： C07D277/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The invention relates to thiazolidinones of general formula (I) their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.
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