公开(公告)号：US06458783B1

公开(公告)日：2002-10-01

申请号：US09556740

申请日：2000-04-21

Applicant: Charles Z. Ding ,  John T. Hunt ,  Katerina Leftheris ,  Rajeev S. Bhide

Inventor： Charles Z. Ding ,  John T. Hunt ,  Katerina Leftheris ,  Rajeev S. Bhide

IPC: A61K31675

CPC classification number: C07D401/06 ,  C07D243/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof.

Abstract translation: 对参与ras癌基因表达的酶的法呢基转移酶的抑制是由formulastheir对映异构体，非对映异构体及其药学上可接受的盐，前药和溶剂化物的化合物进行的。

公开(公告)号：US07820814B2

公开(公告)日：2010-10-26

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: 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：US07547711B2

公开(公告)日：2009-06-16

申请号：US11349767

申请日：2006-02-08

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.

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，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：US07244733B2

公开(公告)日：2007-07-17

申请号：US11345845

申请日：2006-02-02

Applicant: John T. Hunt ,  Rajeev S. Bhide ,  Robert Michael Borzilleri ,  Ligang Qian

Inventor： John T. Hunt ,  Rajeev S. Bhide ,  Robert Michael Borzilleri ,  Ligang Qian

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

CPC classification number: C07D519/00 ,  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, FGFR-1, PDGFR, HER-1, HER-2, 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，FGFR-1，PDGFR，HER-1，HER-2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：US06982265B1

公开(公告)日：2006-01-03

申请号：US09573829

申请日：2000-05-18

Applicant: John T. Hunt ,  Rajeev S. Bhide ,  Robert Michael Borzilleri ,  Ligang Qian

Inventor： John T. Hunt ,  Rajeev S. Bhide ,  Robert Michael Borzilleri ,  Ligang Qian

IPC: C07D487/04 ,  A61K31/153 ,  A61P35/00 ,  A61P27/02 ,  A61P29/00

CPC classification number: C07D519/00 ,  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, FGFR-1, PDGFR, HER-1, HER-2, 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，FGFR-1，PDGFR，HER-1，HER-2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：US08148361B2

公开(公告)日：2012-04-03

申请号：US12513928

申请日：2007-11-07

Applicant: Rajeev S. Bhide ,  Anne Marinier

Inventor： Rajeev S. Bhide ,  Anne Marinier

IPC: A61K31/437 ,  A61K31/397 ,  C07D471/04 ,  A61P35/00 ,  A61P7/00

CPC classification number: C07D471/04

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, FGFR-1 and IGFR-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）的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，FGFR-1和IGFR-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：US20100041636A1

公开(公告)日：2010-02-18

申请号：US12513928

申请日：2007-11-07

Applicant: Rajeev S. Bhide ,  Anne Marinier

Inventor： Rajeev S. Bhide ,  Anne Marinier

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/397 ,  A61P35/00 ,  A61P7/00

CPC classification number: C07D471/04

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, FGFR-1 and IGFR-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）的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，FGFR-1和IGFR-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：US07112675B2

公开(公告)日：2006-09-26

申请号：US11190412

申请日：2005-07-27

Applicant: John T. Hunt ,  Rajeev S. Bhide ,  Robert Michael Borzilleri ,  Ligang Qian

Inventor： John T. Hunt ,  Rajeev S. Bhide ,  Robert Michael Borzilleri ,  Ligang Qian

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

CPC classification number: C07D519/00 ,  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, FGFR-1, PDGFR, HER-1, HER-2, 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：US07030118B2

公开(公告)日：2006-04-18

申请号：US10441848

申请日：2003-05-20

Applicant: Louis J. Lombardo ,  Rajeev S. Bhide ,  Kyoung S. Kim ,  Songfeng Lu

Inventor： Louis J. Lombardo ,  Rajeev S. Bhide ,  Kyoung S. Kim ,  Songfeng Lu

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

CPC classification number: C07D487/04 ,  A61K31/53

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，其用于诱导有丝分裂停滞，从而使其可用作抗癌剂和可通过诱导有丝分裂停止治疗的其它疾病。

公开(公告)号：US06602883B1

公开(公告)日：2003-08-05

申请号：US09566396

申请日：2000-05-05

Applicant: Rajeev S. Bhide ,  Charles Z. Ding ,  John T. Hunt ,  Soong-Hoon Kim ,  Katerina Leftheris

Inventor： Rajeev S. Bhide ,  Charles Z. Ding ,  John T. Hunt ,  Soong-Hoon Kim ,  Katerina Leftheris

IPC: A61K3147

CPC classification number: C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D409/14

Abstract: Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.