公开(公告)号：US20060009454A1

公开(公告)日：2006-01-12

申请号：US11152650

申请日：2005-06-14

申请人： Zhen-wei Cai ,  Louis Lombardo ,  Rajeev Bhide ,  Ligang Qian ,  Donna Wei ,  Stephanie Barbosa

发明人： Zhen-wei Cai ,  Louis Lombardo ,  Rajeev Bhide ,  Ligang Qian ,  Donna Wei ,  Stephanie Barbosa

IPC分类号： A61K31/53 ,  C07D487/04

CPC分类号： C07D487/04

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 and 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.

公开(公告)号：US20050124621A1

公开(公告)日：2005-06-09

申请号：US11035248

申请日：2005-01-13

申请人： Rajeev Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

发明人： Rajeev Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

IPC分类号： A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/662 ,  A61K45/00 ,  A61K45/06 ,  A61P1/04 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  A61P7/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/10 ,  A61P31/12 ,  A61P31/18 ,  A61P31/22 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/00 ,  A61P37/02 ,  A61P37/04 ,  A61P37/06 ,  A61P43/00 ,  C07D487/02 ,  C07D487/04 ,  C07F9/6561

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

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 and 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和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。

公开(公告)号：US20070299075A1

公开(公告)日：2007-12-27

申请号：US11832976

申请日：2007-08-02

申请人： Rajeev Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

发明人： Rajeev Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

IPC分类号： A61K31/4196 ,  A61P43/00 ,  C07D253/06

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

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 and 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和FGFR-1的酪氨酸激酶活性，从而使其用作抗癌剂。 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。

公开(公告)号：US20090170853A1

公开(公告)日：2009-07-02

申请号：US12399429

申请日：2009-03-06

申请人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

发明人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

IPC分类号： A61K31/53 ,  C07D487/04 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

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 and 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和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。

公开(公告)号：US07521450B2

公开(公告)日：2009-04-21

申请号：US11832976

申请日：2007-08-02

申请人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

发明人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P19/02 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

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 and 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和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。

公开(公告)号：US07265113B2

公开(公告)日：2007-09-04

申请号：US11035248

申请日：2005-01-13

申请人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

发明人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

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 and 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和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。

公开(公告)号：US07820814B2

公开(公告)日：2010-10-26

申请号：US12399429

申请日：2009-03-06

申请人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

发明人： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa ,  Louis Lombardo ,  Jeffrey Robl

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

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 and 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和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。

公开(公告)号：US20050222119A1

公开(公告)日：2005-10-06

申请号：US11128732

申请日：2005-05-13

申请人： Eugene Thorsett ,  Christopher Semko ,  Dimitrios Sarantakis ,  Michael Pleiss ,  Anthony Kreft ,  Andrei Konradi ,  Francine Grant ,  Darren Dressen ,  Susan Ashwell ,  Reinhardt Baudy ,  Louis Lombardo

发明人： Eugene Thorsett ,  Christopher Semko ,  Dimitrios Sarantakis ,  Michael Pleiss ,  Anthony Kreft ,  Andrei Konradi ,  Francine Grant ,  Darren Dressen ,  Susan Ashwell ,  Reinhardt Baudy ,  Louis Lombardo

IPC分类号： A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078

CPC分类号： A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/0215 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：US20060069101A1

公开(公告)日：2006-03-30

申请号：US11235507

申请日：2005-09-26

申请人： Kyoung Kim ,  Francis Lee ,  Louis Lombardo ,  Feng Luo ,  John Wityak

发明人： Kyoung Kim ,  Francis Lee ,  Louis Lombardo ,  Feng Luo ,  John Wityak

IPC分类号： A61K31/506 ,  C07D417/14

CPC分类号： C07D417/12 ,  C07D417/14

摘要： Novel compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as oncologic and immunologic disorders.

摘要翻译： 新颖的化合物及其盐，含有这些化合物的药物组合物，以及使用这些化合物治疗蛋白质酪氨酸激酶相关疾病例如肿瘤和免疫疾病的方法。

公开(公告)号：US08741958B2

公开(公告)日：2014-06-03

申请号：US12505283

申请日：2009-07-17

申请人： Louis Lombardo ,  Michael E. Lankin ,  Kenya Ishida ,  Shigeru Tanaka ,  Hideo Ujihara ,  Kenji Yagi ,  Jennifer B. Mei ,  Carter B. Green ,  Amrit S. Mankoo

发明人： Louis Lombardo ,  Michael E. Lankin ,  Kenya Ishida ,  Shigeru Tanaka ,  Hideo Ujihara ,  Kenji Yagi ,  Jennifer B. Mei ,  Carter B. Green ,  Amrit S. Mankoo

IPC分类号： A23L1/221

CPC分类号： A61K8/42 ,  A23G1/32 ,  A23G3/36 ,  A23G4/06 ,  A23L27/202 ,  A61Q5/00 ,  A61Q11/00 ,  A61Q15/00 ,  C07C43/303 ,  C07C45/41 ,  C07C57/66 ,  C07C231/12 ,  C07C233/09 ,  C07C235/28 ,  C07C309/66 ,  C12P13/02 ,  C07C47/21

摘要： The present application provides a synthetic spilanthol flavor composition that includes (2E,6Z,8E)-N-(2-methylpropyl)-2,6,8-decatrienamide. The synthetic spilanthol composition can also contain, and at least one of (2E,6E,8E)-N-(2-methylpropyl)-2,6,8-decatrienamide and (2E,6Z,8Z)-N-(2-methylpropyl)-2,6,8-decatrienamide, the (N-(2-methylpropyl)-2,6,8-decatrienamide being present in amounts effective to impart a salivating or tingle effect while reducing the perception of off notes, as compared to the off-notes perceived upon consumption of natural spilanthol (e.g. spilanthol obtained from jambu oleoresin). Methods of increasing salivation and/or providing a tingling sensation upon consuming an orally consumable product that include adding to the product a synthetic spilanthol flavor composition are also provided. Synthetic spilanthol flavor compositions can be added to orally consumed products, such as, but not limited to, foods, beverages, pharmaceuticals, nutraceuticals, or therapeutic compositions, oral personal care products, gums (e.g. chewing gum or bubble gum), candy or lozenges.

摘要翻译： 本申请提供了包括（2E，6Z，8E）-N-（2-甲基丙基）-2,6,8-十一三烯酰胺的合成稀释剂风味组合物。 （2E，6E，8E）-N-（2-甲基丙基）-2,6,8-十一三烯酰胺和（2E，6Z，8Z）-N-（2- 甲基丙基）-2,6,8-十一三烯酰胺，（N-（2-甲基丙基）-2,6,8-癸三酰胺以有效赋予唾液或叮咬效果同时减少脱落感觉的量存在，相比之下 在消费口服消耗品时，增加唾液分泌和/或提供刺痛感的方法包括向产品中加入合成的稀释剂风味组合物的方法也是 合成的稀释剂风味组合物可以添加到口服食品中，例如但不限于食品，饮料，药物，营养保健品或治疗组合物，口腔个人护理产品，牙龈（例如口香糖或泡泡糖），糖果 或锭剂。