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1. 发明申请

US20060211695A1 Fused heterocyclic kinase inhibitors 有权
标题翻译：融合的杂环激酶抑制剂
公开(公告)号：US20060211695A1
公开(公告)日：2006-09-21
申请号：US11292358
申请日：2005-12-01
申请人： Robert Borzilleri , Zhong Chen , Tram Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung Kim , Zhen-wei Cai
发明人： Robert Borzilleri , Zhong Chen , Tram Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung Kim , Zhen-wei Cai
IPC分类号： A61K31/53 , A61K31/52 , A61K31/519 , C07D498/02 , C07D487/02 , C07D473/02
CPC分类号： C07D487/04 , C07D471/04 , C07D495/04
摘要： In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要翻译：通常，本发明包括式I和II的化合物，包括其药学上可接受的盐。本发明的化合物可用作蛋白激酶抑制剂，因此可用于治疗癌症和其它蛋白激酶介导的疾病。

2. 发明申请

US20050239820A1 Bicyclic heterocycles as kinase inhibitors 有权
标题翻译：双环杂环作为激酶抑制剂
公开(公告)号：US20050239820A1
公开(公告)日：2005-10-27
申请号：US11113838
申请日：2005-04-25
申请人： Robert Borzilleri , Kyoung Kim , Zhen-Wei Cai
发明人： Robert Borzilleri , Kyoung Kim , Zhen-Wei Cai
IPC分类号： A61K31/4745 , C07D471/02 , C07D471/04
CPC分类号： C07D471/04
摘要： The compounds of the instant invention can be used as anticancer agents. More specifically, the invention comprises a compound having Formula I or II,
摘要翻译：本发明的化合物可用作抗癌剂。更具体地，本发明包括具有式I或II的化合物，

3. 发明申请

US20070123534A1 Pyrrolotriazine kinase inhibitors 有权
标题翻译：吡咯并三嗪激酶抑制剂
公开(公告)号：US20070123534A1
公开(公告)日：2007-05-31
申请号：US11605168
申请日：2006-11-28
申请人： Zhen-Wei Cai , Kyoung Kim , Robert Borzilleri
发明人： Zhen-Wei Cai , Kyoung Kim , Robert Borzilleri
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： In general, the instant invention comprises compounds having Formulae I and II: including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要翻译：通常，本发明包括具有式I和II的化合物：包括其药学上可接受的盐。本发明的化合物可用作蛋白激酶抑制剂，因此可用于治疗癌症和其它蛋白激酶介导的疾病。

4. 发明申请

US20050288290A1 Fused heterocyclic kinase inhibitors 审中-公开
标题翻译：融合的杂环激酶抑制剂
公开(公告)号：US20050288290A1
公开(公告)日：2005-12-29
申请号：US11167043
申请日：2005-06-24
申请人： Robert Borzilleri , Zhong Chen , Tram Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung Kim , Zhen-wei Cai
发明人： Robert Borzilleri , Zhong Chen , Tram Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung Kim , Zhen-wei Cai
IPC分类号： A61K31/519 , A61K31/52 , A61K31/53 , C07D471/04 , C07D473/14 , C07D487/02 , C07D487/04 , C07D495/04
CPC分类号： C07D471/04 , C07D473/00 , C07D473/30 , C07D487/04 , C07D495/04
摘要： In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要翻译：通常，本发明包括式I和II的化合物，包括其药学上可接受的盐。本发明的化合物可用作蛋白激酶抑制剂，因此可用于治疗癌症和其它蛋白激酶介导的疾病。

5. 发明申请

US20070117802A1 Met kinase inhibitors 有权
标题翻译： Met激酶抑制剂
公开(公告)号：US20070117802A1
公开(公告)日：2007-05-24
申请号：US11521035
申请日：2006-09-14
申请人： Robert Borzilleri , Zhen-wei Cai , Donna Wei , John Tokarski
发明人： Robert Borzilleri , Zhen-wei Cai , Donna Wei , John Tokarski
IPC分类号： A61K31/53 , A61K31/519 , C07D487/04 , C07D491/02
CPC分类号： C07D213/75 , C07D471/04
摘要： The invention is directed to compounds that are useful for the treatment of cancer having the following Formula:
摘要翻译：本发明涉及可用于治疗具有下式的癌症的化合物：

6. 发明申请

US20060135576A1 Heterocyclic inhibitors of kinases 有权
公开(公告)号：US20060135576A1
公开(公告)日：2006-06-22
申请号：US11349767
申请日：2006-02-08
申请人： Robert Borzilleri , Rajeev Bhide , John Tokarski , Peter Zheng , Ligang Qian , Zhen-Wei Cai
发明人： Robert Borzilleri , Rajeev Bhide , John Tokarski , Peter Zheng , Ligang Qian , Zhen-Wei Cai
IPC分类号： A61K31/426 , A61K31/421
CPC分类号： C07D277/42 , C07D417/12 , C07D417/14
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, 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.

7. 发明申请

US20050245530A1 Monocyclic heterocycles as kinase inhibitors 有权
标题翻译：单环杂环作为激酶抑制剂
公开(公告)号：US20050245530A1
公开(公告)日：2005-11-03
申请号：US11111144
申请日：2005-04-21
申请人： Robert Borzilleri , Lyndon Cornelius , Robert Schmidt , Gretchen Schroeder , Kyoung Kim
发明人： Robert Borzilleri , Lyndon Cornelius , Robert Schmidt , Gretchen Schroeder , Kyoung Kim
IPC分类号： A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/501 , A61K31/506 , A61P35/00 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/46 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/02 , C07D417/02 , C07D417/12 , C07D43/02
CPC分类号： C07D213/82 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/47 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12
摘要： The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
摘要翻译：本发明涉及具有下式的化合物及其用于治疗癌症的方法。

8. 发明申请

US20060128709A1 Pyrrolotriazine inhibitors of kinases 有权
公开(公告)号：US20060128709A1
公开(公告)日：2006-06-15
申请号：US11345845
申请日：2006-02-02
申请人： John Hunt , Rajeev Bhide , Robert Borzilleri , Ligang Qian
发明人： John Hunt , Rajeev Bhide , Robert Borzilleri , Ligang Qian
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D519/00 , 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, 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.

9. 发明申请

US20070255055A1 EPOTHILONE DERIVATIVES 有权
公开(公告)号：US20070255055A1
公开(公告)日：2007-11-01
申请号：US11763636
申请日：2007-06-15
申请人： Gregory Vite , Soong-Hoon Kim , Robert Borzilleri , James Johnson
发明人： Gregory Vite , Soong-Hoon Kim , Robert Borzilleri , James Johnson
IPC分类号： C07D225/02
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to compounds of the formula Q is selected from the group consisting of G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, W is O or NR15; X is O or H,H; Y is selected from the group consisting of O; H,OR16; OR17,OR17; NOR18; H,NOR19; H,NR20R21; H,H; or CHR22; OR17OR17 can be a cyclic ketal; Z1 and Z2 are selected from the group consisting of CH2, O, NR23, S, or SO2, wherein only one of Z and Z2 is a heteroatom; B1 and B2 are selected from the group consisting of OR24, or OCOR25, or O2CNR26R27; when B1 is H and Y is OH, H they can form a six-membered ring ketal or acetal; D is selected from the group consisting of NR28R29, NR30COR31 or saturated heterocycle; R1, R2, R3, R4, R5, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26, and R27 are selected from the group H, alkyl, substituted alkyl, or aryl and when R1 and R2 are alkyl can be joined to form a cycloalkyl; R3 and R4 are alkyl can be joined to form a cycloalkyl; R9, R10, R16, R17, R24, R25, and R31 are selected from the group H, alkyl, or substituted alkyl; R8, R11, R12, R28, R30, R32, R33, and R30 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R15, R23 and R29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R32C═O, R33SO2, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein W and X are both O; and R1, R2, R7, are H; and R3, R4, R6, are methyl; and R8, is H or methyl; and Z1, and Z2, are CH2; and G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and Q is as defined above are excluded.

10. 发明申请

US20070078140A1 MET kinase inhibitors 有权
标题翻译： MET激酶抑制剂
公开(公告)号：US20070078140A1
公开(公告)日：2007-04-05
申请号：US11529875
申请日：2006-09-28
申请人： Robert Borzilleri , Xiao-Tao Chen , David Williams , John Tokarski , Robert Kaltenbach
发明人： Robert Borzilleri , Xiao-Tao Chen , David Williams , John Tokarski , Robert Kaltenbach
IPC分类号： A61K31/506 , A61K31/501 , A61K31/4965 , A61K31/497 , C07D403/04
CPC分类号： C07D401/12 , C07D213/82 , C07D471/04
摘要： The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.
摘要翻译：本发明涉及具有式I或II的化合物：包括其盐，以及用于治疗癌症的方法。

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