公开(公告)号：US07265113B2

公开(公告)日：2007-09-04

申请号：US11035248

申请日：2005-01-13

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 ,  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：US06969717B2

公开(公告)日：2005-11-29

申请号：US10622593

申请日：2003-07-18

Applicant: Rajeev S. Bhide ,  Rejean Ruel ,  Carl Thibault ,  Alexandre L'Heureux

Inventor： Rajeev S. Bhide ,  Rejean Ruel ,  Carl Thibault ,  Alexandre L'Heureux

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 ,  C07D484/04

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：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：US07053223B2

公开(公告)日：2006-05-30

申请号：US10775438

申请日：2004-02-10

Applicant: Rajeev S. Bhide

Inventor： Rajeev S. Bhide

IPC: C07D233/02

CPC classification number: C07D405/06 ,  C07D405/12 ,  C07D409/14

Abstract: The present invention discloses the identification of the novel inhibitors of farnesyl protein transferase and ras protein farnesylation. The compounds and pharmaceutical compositions disclosed herein are useful in treating diseases associated with farnesyl protein transferase, such as cancer.

Abstract translation: 本发明公开了法呢基蛋白转移酶和ras蛋白法尼基化的新型抑制剂的鉴定。 本文公开的化合物和药物组合物可用于治疗与法呢基蛋白转移酶（例如癌症）相关的疾病。

公开(公告)号：US06933386B2

公开(公告)日：2005-08-23

申请号：US10622280

申请日：2003-07-18

Applicant: Rajeev S. Bhide ,  Junying Fan ,  Luca Parlanti ,  Stephanie Barbosa ,  Ligang Qian ,  Zhen-Wei Cai ,  Francis S. Gibson

Inventor： Rajeev S. Bhide ,  Junying Fan ,  Luca Parlanti ,  Stephanie Barbosa ,  Ligang Qian ,  Zhen-Wei Cai ,  Francis S. Gibson

IPC: A61K31/53 ,  A61K45/06 ,  A61P13/08 ,  A61P29/00 ,  A61P37/00 ,  C07D487/04

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

Abstract: The present invention relates to a process for preparing certain pyrrolotriazine compounds of the formula 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: 本发明涉及制备下式的某些吡咯并三嗪化合物及其药学上可接受的盐的方法。 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：US06869952B2

公开(公告)日：2005-03-22

申请号：US10623171

申请日：2003-07-18

Applicant: Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa

Inventor： Rajeev S. Bhide ,  Zhen-Wei Cai ,  Ligang Qian ,  Stephanie Barbosa

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：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：US07102002B2

公开(公告)日：2006-09-05

申请号：US11152650

申请日：2005-06-14

Applicant: Zhen-wei Cai ,  Louis J. Lombardo ,  Rajeev S. Bhide ,  Ligang Qian ,  Donna D. Wei ,  Stephanie Barbosa

Inventor： Zhen-wei Cai ,  Louis J. Lombardo ,  Rajeev S. Bhide ,  Ligang Qian ,  Donna D. Wei ,  Stephanie Barbosa

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

CPC classification number: C07D487/04

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：US07084160B2

公开(公告)日：2006-08-01

申请号：US10464139

申请日：2003-06-18

Applicant: Robert M. Borzilleri ,  Rajeev S. Bhide ,  John S. Tokarski ,  Peter Zheng ,  Ligang Qian ,  Zhen-Wei Cai

Inventor： Robert M. Borzilleri ,  Rajeev S. Bhide ,  John S. Tokarski ,  Peter Zheng ,  Ligang Qian ,  Zhen-Wei Cai

IPC: A61K31/44 ,  C07D417/12

CPC classification number: C07D277/42 ,  C07D417/12 ,  C07D417/14

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, 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：US06951859B2

公开(公告)日：2005-10-04

申请号：US10633997

申请日：2003-08-04

Applicant: Rajeev S. Bhide ,  Robert M. Borzilleri

Inventor： Rajeev S. Bhide ,  Robert M. Borzilleri

IPC: A61K31/53 ,  A61K45/06 ,  A61P13/08 ,  A61P29/00 ,  A61P37/00 ,  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。