公开(公告)号：US20090170853A1

公开(公告)日：2009-07-02

申请号：US12399429

申请日：2009-03-06

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

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

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

CPC classification number: C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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：US07420059B2

公开(公告)日：2008-09-02

申请号：US10989138

申请日：2004-11-15

Applicant: Stephen P. O'Connor ,  Jeffrey Robl ,  Yan Shi

Inventor： Stephen P. O'Connor ,  Jeffrey Robl ,  Yan Shi

IPC: C07D221/18 ,  C07D471/02 ,  A61K31/47

CPC classification number: C07D213/80 ,  C07D211/76 ,  C07D401/14 ,  C07D471/04 ,  C07D491/04 ,  C07D498/04 ,  C07D513/04

Abstract: Compounds are provided having the following structure and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, U, V, W, Y, and n are as defined above, which compounds are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis and may be employed as hormone replacement therapy. A method for treating the above diseases employing the above compounds is also provided.

Abstract translation: 提供具有以下结构的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， 其中U，V，W，Y和n如上所定义，这些化合物是HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质的作用，例如降低LDL胆固醇和/或增加 HDL胆固醇，治疗高脂血症，血脂异常，高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及阿尔茨海默病和骨质疏松症，可用作激素替代疗法。 还提供了使用上述化合物治疗上述疾病的方法。

公开(公告)号：US20060287357A1

公开(公告)日：2006-12-21

申请号：US11448947

申请日：2006-06-07

Applicant: James Li ,  Lawrence Hamann ,  Haixia Wang ,  Zheming Ruan ,  Christopher Cooper ,  Jun Li ,  Jeffrey Robl

Inventor： James Li ,  Lawrence Hamann ,  Haixia Wang ,  Zheming Ruan ,  Christopher Cooper ,  Jun Li ,  Jeffrey Robl

IPC: A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L, R3, R3a, R3b and R4 are defined herein.

Abstract translation: 提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。 这些新化合物具有以下结构：或其立体异构体或前药或其药学上可接受的盐，其中W，L，R 3，R 3a，R 3b， >和R 4'在本文中定义。

公开(公告)号：US06995183B2

公开(公告)日：2006-02-07

申请号：US10899641

申请日：2004-07-27

Applicant: Lawrence G. Hamann ,  Ashish Khanna ,  Mark S. Kirby ,  David R. Magnin ,  Ligaya M. Simpkins ,  James C. Sutton ,  Jeffrey Robl

Inventor： Lawrence G. Hamann ,  Ashish Khanna ,  Mark S. Kirby ,  David R. Magnin ,  Ligaya M. Simpkins ,  James C. Sutton ,  Jeffrey Robl

IPC: A61K31/403 ,  A61K31/426 ,  A61K31/4453 ,  C07D209/52 ,  C07D205/04 ,  C07D295/00 ,  C07D279/12 ,  C07D259/03 ,  C07D221/00 ,  C07D295/16

CPC classification number: C07C255/46 ,  C07C255/47 ,  C07C2601/08 ,  C07C2602/18 ,  C07C2603/74 ,  C07D207/16 ,  C07D209/52 ,  C07D277/04 ,  C07D295/185

Abstract: Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n+m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.

Abstract translation: 提供具有下式的化合物

公开(公告)号：US20050171140A1

公开(公告)日：2005-08-04

申请号：US10989138

申请日：2004-11-15

Applicant: Stephen O'Connor ,  Jeffrey Robl ,  Saleem Ahmad ,  Sharon Bisaha ,  Natesan Murugesan ,  Khehyong Ngu ,  Yan Shi ,  Philip Stein ,  Nachimuthu Soundararajan ,  Kenneth Natalie ,  Laxma Kolla ,  Justin Sausker ,  Sandra Quinlan ,  Junying Fan ,  Dejah Petsch ,  Zhenrong Guo

Inventor： Stephen O'Connor ,  Jeffrey Robl ,  Saleem Ahmad ,  Sharon Bisaha ,  Natesan Murugesan ,  Khehyong Ngu ,  Yan Shi ,  Philip Stein ,  Nachimuthu Soundararajan ,  Kenneth Natalie ,  Laxma Kolla ,  Justin Sausker ,  Sandra Quinlan ,  Junying Fan ,  Dejah Petsch ,  Zhenrong Guo

IPC: A61K31/435 ,  A61K31/4745 ,  A61K31/505 ,  C07D211/76 ,  C07D213/80 ,  C07D401/14 ,  C07D471/02 ,  C07D471/04 ,  C07D491/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D213/80 ,  C07D211/76 ,  C07D401/14 ,  C07D471/04 ,  C07D491/04 ,  C07D498/04 ,  C07D513/04

Abstract: Compounds are provided having the following structure and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, U, V, W, Y, and n are as defined above, which compounds are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis and may be employed as hormone replacement therapy. A method for treating the above diseases employing the above compounds is also provided.

Abstract translation: 提供具有以下结构的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， 其中U，V，W，Y和n如上所定义，这些化合物是HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质的作用，例如降低LDL胆固醇和/或增加 HDL胆固醇，治疗高脂血症，血脂异常，高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及阿尔茨海默病和骨质疏松症，可用作激素替代疗法。 还提供了使用上述化合物治疗上述疾病的方法。

公开(公告)号：US20050070589A1

公开(公告)日：2005-03-31

申请号：US10932981

申请日：2004-09-01

Applicant: Khehyong Ngu ,  David Weinstein ,  Jeffrey Robl

Inventor： Khehyong Ngu ,  David Weinstein ,  Jeffrey Robl

IPC: C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D495/04 ,  C07D231/10 ,  A61K31/415 ,  A61K31/416 ,  C07D403/02

CPC classification number: C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D495/04

Abstract: The present invention provides pyrazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.

Abstract translation: 本发明提供15-LO的吡唑基抑制剂，含有这些抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联相关的疾病的方法。

公开(公告)号：US07521450B2

公开(公告)日：2009-04-21

申请号：US11832976

申请日：2007-08-02

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

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

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

CPC classification number: C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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：US20050239839A1

公开(公告)日：2005-10-27

申请号：US11149408

申请日：2005-06-09

Applicant: Lawrence Hamann ,  Ashish Khanna ,  Mark Kirby ,  David Magnin ,  Ligaya Simpkins ,  James Sutton ,  Jeffrey Robl

Inventor： Lawrence Hamann ,  Ashish Khanna ,  Mark Kirby ,  David Magnin ,  Ligaya Simpkins ,  James Sutton ,  Jeffrey Robl

IPC: C07C255/46 ,  C07C255/47 ,  C07D207/16 ,  C07D209/52 ,  C07D277/04 ,  C07D295/185 ,  A61K31/445 ,  A61K31/275 ,  A61K31/401 ,  A61K31/403 ,  A61K31/426

CPC classification number: C07C255/46 ,  C07C255/47 ,  C07C2601/08 ,  C07C2602/18 ,  C07C2603/74 ,  C07D207/16 ,  C07D209/52 ,  C07D277/04 ,  C07D295/185

Abstract: Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n+m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.

公开(公告)号：US20050124621A1

公开(公告)日：2005-06-09

申请号：US11035248

申请日：2005-01-13

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

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

IPC: 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 classification number: C07D487/04 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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：US20050085497A1

公开(公告)日：2005-04-21

申请号：US10946055

申请日：2004-09-21

Applicant: Saleem Ahmad ,  Jeffrey Robl ,  Khehyong Ngu

Inventor： Saleem Ahmad ,  Jeffrey Robl ,  Khehyong Ngu

IPC: A61K31/505 ,  A61K31/506 ,  A61P3/06 ,  C07D213/74 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D45/02

CPC classification number: C07D213/74 ,  C04B35/632 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholsterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis wherein X is N or CR5; and pharmaceutically acceptable salts thereof, wherein R1 to R7 are as defined herein. A method for treating the above diseases employing the above compounds is also provided.

Abstract translation: 提供具有以下结构的化合物，其为HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质，例如降低LDL胆固醇和/或增加HDL胆固醇，以及治疗高脂血症，血脂异常，激素替代疗法， 高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及阿尔茨海默病和骨质疏松症，其中X是N或CR 5; 和其药学上可接受的盐，其中R 1至R 7如本文所定义。 还提供了使用上述化合物治疗上述疾病的方法。