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1. 发明申请

WO2005096784A3 BENZOTRIAZINE INHIBITORS OF KINASES 审中-公开
标题翻译：苄基苯并噻嗪类抑制剂
公开(公告)号：WO2005096784A3
公开(公告)日：2009-02-19
申请号：PCT/US2005012057
申请日：2005-04-07
申请人： TARGEGEN INC , NORONHA GLENN , BARRETT KATHY , CAO JIANGUO , GRITZEN COLLEEN , GONG XIANCHANG , HOOD JOHN , MAK CHI CHING , MCPHERSON ANDREW , PATHAK VED PRAKASH , RENICK JOEL , SOLL RICHARD , SPLITTGERBER UTE , WRASIDLO WOLFGANG , ZENG BINQI , ZHAO NINGNING , DNEPROVSKAIA ELENA
发明人： NORONHA GLENN , BARRETT KATHY , CAO JIANGUO , GRITZEN COLLEEN , GONG XIANCHANG , HOOD JOHN , MAK CHI CHING , MCPHERSON ANDREW , PATHAK VED PRAKASH , RENICK JOEL , SOLL RICHARD , SPLITTGERBER UTE , WRASIDLO WOLFGANG , ZENG BINQI , ZHAO NINGNING , DNEPROVSKAIA ELENA
IPC分类号： A61K31/53 , C07D253/08
CPC分类号： C07D253/08 , C07D403/04 , C07D403/12 , C07D413/04
摘要： The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
摘要翻译：本发明提供具有式（I）的苯并三嗪化合物。本发明的苯并三嗪化合物能够抑制激酶，Src激酶家族的成员和各种其它特异性受体和非受体激酶。

2. 发明申请

WO2007053452A1 BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES 审中-公开
标题翻译：二甲基亚氨基嘧啶抑制剂
公开(公告)号：WO2007053452A1
公开(公告)日：2007-05-10
申请号：PCT/US2006/042044
申请日：2006-10-26
申请人： TARGEGEN, INC. , CAO, Jon, Jianguo , HOOD, John , LOHSE, Dan , MAK, Chi, Ching , MC PHERSON, Andrew , NORONHA, Glenn , PATHAK, Ved , RENICK, Joel , SOLL, Richard, M. , ZENG, Binqi
发明人： CAO, Jon, Jianguo , HOOD, John , LOHSE, Dan , MAK, Chi, Ching , MC PHERSON, Andrew , NORONHA, Glenn , PATHAK, Ved , RENICK, Joel , SOLL, Richard, M. , ZENG, Binqi
IPC分类号： C07D239/48 , C07D239/49 , A61K31/505 , C07D207/06
CPC分类号： C07D239/48 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non receptor kinases.
摘要翻译：本发明提供具有一般结构（A）的联芳基间 - 嘧啶化合物。本发明的嘧啶化合物能够抑制激酶，例如Jak激酶家族的成员和各种其它特异性受体和非受体激酶。

3. 发明申请

WO2007056075A3 SIX MEMBERED HETEROAROMATIC INHIBITORS TARGETING RESISTANT KINASE MUTATIONS 审中-公开
公开(公告)号：WO2007056075A3
公开(公告)日：2007-05-18
申请号：PCT/US2006/042838
申请日：2006-10-31
申请人： TARGEGEN, INC. , CAO, Jianguo , HOOD, John , LOHSE, Dan , MAK, Chi, Ching , MC PHERSON, Andrew , NORONHA, Glenn , PATHAK, Ved , RENICK, Joel , SOLL, Richard, M. , ZENG, Binqi , CHOW, Chun , PALANKI, Moorthy , DNEPROVSKAIA, Elena
发明人： CAO, Jianguo , HOOD, John , LOHSE, Dan , MAK, Chi, Ching , MC PHERSON, Andrew , NORONHA, Glenn , PATHAK, Ved , RENICK, Joel , SOLL, Richard, M. , ZENG, Binqi , CHOW, Chun , PALANKI, Moorthy , DNEPROVSKAIA, Elena
IPC分类号： A01N43/54 , A61K31/505
摘要： A compound is provided, havingthe general structure (A): Formula (A) wherein A is an (un)substituted aryl or (un)substituted heteroaryl moiety, G is N, CH, or CR, R is an unsubstituted or substituted lower alkyl, Y is a hydrophobic linking moiety, and L is a substitutent as defined. The compound (A) can be used for treatment of various angiogenic and hematological-associated disorders, such as myeloproliferative disorder in patients who do not respond to kinase-inhibition therapy that comprises administering approved medications.

4. 发明申请

WO2007056075A2 SIX MEMBERED HETEROAROMATIC INHIBITORS TARGETING RESISTANT KINASE MUTATIONS 审中-公开
标题翻译：六种成员杂合抑制剂靶向抗性激酶突变
公开(公告)号：WO2007056075A2
公开(公告)日：2007-05-18
申请号：PCT/US2006042838
申请日：2006-10-31
申请人： TARGEGEN INC , CAO JIANGUO , HOOD JOHN , LOHSE DAN , MAK CHI CHING , MC PHERSON ANDREW , NORONHA GLENN , PATHAK VED , RENICK JOEL , SOLL RICHARD M , ZENG BINQI , CHOW CHUN , PALANKI MOORTHY , DNEPROVSKAIA ELENA
发明人： CAO JIANGUO , HOOD JOHN , LOHSE DAN , MAK CHI CHING , MC PHERSON ANDREW , NORONHA GLENN , PATHAK VED , RENICK JOEL , SOLL RICHARD M , ZENG BINQI , CHOW CHUN , PALANKI MOORTHY , DNEPROVSKAIA ELENA
IPC分类号： A61K31/551 , A61K31/506 , A61K31/53 , C07D403/02
CPC分类号： C07D417/12 , C07D239/42 , C07D253/06 , C07D277/42 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/06 , C07D417/14
摘要： A compound is provided, havingthe general structure (A): Formula (A) wherein A is an (un)substituted aryl or (un)substituted heteroaryl moiety, G is N, CH, or CR, R is an unsubstituted or substituted lower alkyl, Y is a hydrophobic linking moiety, and L is a substitutent as defined. The compound (A) can be used for treatment of various angiogenic and hematological-associated disorders, such as myeloproliferative disorder in patients who do not respond to kinase-inhibition therapy that comprises administering approved medications.
摘要翻译：提供具有通式结构（A）的化合物：其中A是（未）取代的芳基或（未）取代的杂芳基部分，G是N，CH或CR，R是未取代或取代的低级烷基 Y是疏水性连接部分，并且L是如所定义的取代基。化合物（A）可用于治疗各种血管生成和血液学相关疾病，例如对包括给予经批准的药物的激酶抑制疗法无反应的患者的骨髓增殖性疾病。

5. 发明申请

WO2008008234A1 2-AMINO-5-SUBSTITUTED PYRIMIDINE INHIBITORS 审中-公开
标题翻译： 2-氨基-5-取代的吡咯咪嗪抑制剂
公开(公告)号：WO2008008234A1
公开(公告)日：2008-01-17
申请号：PCT/US2007/015357
申请日：2007-07-02
申请人： TARGEGEN, INC. , NORONHA, Glenn , CAO, Jianguo , GRITZEN, Colleen , MAK, Chi, Ching , MCPHERSON, Andrew , PATHAK, Ved, P. , RENICK, Joel , SOLL, Richard, M. , ZENG, Binqi , DNEPROVSKAIA, Elena
发明人： NORONHA, Glenn , CAO, Jianguo , GRITZEN, Colleen , MAK, Chi, Ching , MCPHERSON, Andrew , PATHAK, Ved, P. , RENICK, Joel , SOLL, Richard, M. , ZENG, Binqi , DNEPROVSKAIA, Elena
IPC分类号： C07D403/02 , A61K31/42
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D409/12 , C07D413/12
摘要： Compounds having the general structure (A) are provided. The compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, Vegfr and various other specific receptor and non-receptor kinases. Formula (I):
摘要翻译：提供具有一般结构（A）的化合物。本发明的化合物能够抑制激酶，例如Src激酶家族的成员，Vegfr和各种其它特异性受体和非受体激酶。式（I）：

6. 发明申请

WO2006101977A3 PYRIMIDINE COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2006101977A3
公开(公告)日：2006-09-28
申请号：PCT/US2006/009518
申请日：2006-03-15
申请人： TARGEGEN, INC. , CAO, Jianguo , SOLL, Richard, M. , NORONHA, Glenn , BARRETT, Kathy , GRITZEN, Colleen , HOOD, John , MAK, Chi, Ching , MCPHERSON, Andrew , PATHAK, Ved, Prakash , RENICK, Joel , SPLITTGERBER, Ute , ZENG, Binqi
发明人： CAO, Jianguo , SOLL, Richard, M. , NORONHA, Glenn , BARRETT, Kathy , GRITZEN, Colleen , HOOD, John , MAK, Chi, Ching , MCPHERSON, Andrew , PATHAK, Ved, Prakash , RENICK, Joel , SPLITTGERBER, Ute , ZENG, Binqi
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/44 , A61K31/40 , A61K31/506 , A61P19/02 , A61P29/02 , A61P37/06
摘要： The invention provides pyrimidine compounds having formula (A): The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, and various other specific receptor and non-receptor kinases.

7. 发明申请

WO2006101977A2 PYRIMIDINE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：吡嗪化合物及其使用方法
公开(公告)号：WO2006101977A2
公开(公告)日：2006-09-28
申请号：PCT/US2006009518
申请日：2006-03-15
申请人： TARGEGEN INC , CAO JIANGUO , SOLL RICHARD M , NORONHA GLENN , BARRETT KATHY , GRITZEN COLLEEN , HOOD JOHN , MAK CHI CHING , MCPHERSON ANDREW , PATHAK VED PRAKASH , RENICK JOEL , SPLITTGERBER UTE , ZENG BINQI
发明人： CAO JIANGUO , SOLL RICHARD M , NORONHA GLENN , BARRETT KATHY , GRITZEN COLLEEN , HOOD JOHN , MAK CHI CHING , MCPHERSON ANDREW , PATHAK VED PRAKASH , RENICK JOEL , SPLITTGERBER UTE , ZENG BINQI
IPC分类号： A61K31/506 , C07D403/02 , C07D403/14
CPC分类号： C07D239/48 , C07D239/49 , C07D401/12 , C07D417/12
摘要： The invention provides pyrimidine compounds having formula (A): The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, and various other specific receptor and non-receptor kinases.
摘要翻译：本发明提供具有式（A）的嘧啶化合物：本发明的嘧啶化合物能够抑制激酶，例如Src激酶家族的成员和各种其它特异性受体和非受体激酶。

8. 发明申请

WO2009055674A1 PYRROLOPYRIMIDINE ALKYNYL COMPOUNDS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：吡咯烷基炔丙基化合物及其制备方法和使用方法
公开(公告)号：WO2009055674A1
公开(公告)日：2009-04-30
申请号：PCT/US2008/081119
申请日：2008-10-24
申请人： TARGEGEN INC. , NORONHA, Glenn , CAO, Jianguo , CHOW, Chun , MAK, Chi, Ching , PALANKI, Moorthy , DNEPROVSKAIA, Elena , MCPHERSON, Andrew , PATHAK, Ved, Prakash , RENICK, Joel , ZENG, Binqi
发明人： NORONHA, Glenn , CAO, Jianguo , CHOW, Chun , MAK, Chi, Ching , PALANKI, Moorthy , DNEPROVSKAIA, Elena , MCPHERSON, Andrew , PATHAK, Ved, Prakash , RENICK, Joel , ZENG, Binqi
IPC分类号： C07D487/04 , A61K31/505 , A61P35/02
CPC分类号： C07D487/04
摘要： Provided herein are pyrrolopyrimide alkynyl compounds, and methods of making and using the same. Such compounds may be used in inflammatory or myeloproliferative disorders. The disclosure also provides for treating cancer.
摘要翻译：本文提供吡咯并吡啶酰亚胺炔基化合物及其制备和使用方法。这些化合物可用于炎性或骨髓增生性疾病。本公开还提供治疗癌症。

9. 发明申请

WO2007056023A3 THIAZOLE INHIBITORS TARGETING RESISTANT KINASE MUTATIONS 审中-公开
标题翻译：噻唑抑制剂抵抗性激酶突变
公开(公告)号：WO2007056023A3
公开(公告)日：2007-10-18
申请号：PCT/US2006042697
申请日：2006-10-31
申请人： TARGEGEN INC , CAO JIANGUO , HOOD JOHN , LOHSE DAN , MAK CHI CHING , MC PHERSON ANDREW , NORONHA GLENN , PATHAK VED , RENICK JOEL , SOLL RICHARD M , ZENG BINQI , CHOW CHUN , PALANKI MOORTHY , DNEPROVSKAIA ELENA
发明人： CAO JIANGUO , HOOD JOHN , LOHSE DAN , MAK CHI CHING , MC PHERSON ANDREW , NORONHA GLENN , PATHAK VED , RENICK JOEL , SOLL RICHARD M , ZENG BINQI , CHOW CHUN , PALANKI MOORTHY , DNEPROVSKAIA ELENA
IPC分类号： A61K31/53 , C07D253/08
CPC分类号： C07D417/12 , C07D239/42 , C07D253/06 , C07D277/42 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/06 , C07D417/14
摘要： A compound is provided, having the general structure (A): wherein A is an aryl or heteroaryl group, Y is a hydrophobic linking moiety, and L is a substitutent. The compound (A) can be used for treatment of various angiogenic-associated or hematologic disorders, such as myeloproliferative disorders in patients who do not respond to kinase-inhibition therapy that comprises administering currently used medications.
摘要翻译：提供具有一般结构（A）的化合物：其中A是芳基或杂芳基，Y是疏水连接部分，L是取代基。化合物（A）可用于治疗各种血管生成相关或血液学疾病，例如对不包括对目前使用的药物施用的激酶抑制治疗无反应的患者中的骨髓增生性疾病。

10. 发明申请

WO2009049028A1 PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USE AS JANUS KINASE MODULATORS 审中-公开
标题翻译：吡咯啉化合物及其作为JANUS KINASE调节剂的用途
公开(公告)号：WO2009049028A1
公开(公告)日：2009-04-16
申请号：PCT/US2008/079315
申请日：2008-10-09
申请人： TARGEGEN INC. , NORONHA, Glenn , CAO, Jianguo , CHOW, Chun, P. , MAK, Chi Ching , PALANKI, Moorthy, S.S. , DNEPROVSKAIA, Elena , MCPHERSON, Andrew , PATHAK, Ved, Prakash , RENICK, Joel , ZENG, Binqi
发明人： NORONHA, Glenn , CAO, Jianguo , CHOW, Chun, P. , MAK, Chi Ching , PALANKI, Moorthy, S.S. , DNEPROVSKAIA, Elena , MCPHERSON, Andrew , PATHAK, Ved, Prakash , RENICK, Joel , ZENG, Binqi
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519
CPC分类号： C07D487/04
摘要： Provided herein are pyrrolopyrimidine compounds of Formula (I) wherein R1 is a heteroaryl containing at least one S atom, and optionally substituted on a ring carbon by one, two, or three substituents each independently selected from the group consisting of : halo, hydroxyl, nitro, formyl, formamido, cyano, sulfonyl, carboxy, amino, amido, acylamino, carbamoyl, sulphamoyl, alkyl, alkenyl, CF3, ureido, alkynyl, alkoxy, alkanoyl, alkoxycarbonyl, carbaldehyde oxime, N -alkylsulphamoyl, N-alkylcarbamoyl, -OR13R11 or -R13R11; R2 is phenyl or pyridinyl, wherein R2 optionally substituted on a ring carbon by one, two, or three substituents each indenpendently selected from the group consisting of : halo, hydroxyl, cyano, nitro, formyl, formamido, carboxy, sulfonyl, amino, amido, -N- alkyl -amino, carbamoyl, sulphamoyl, CF3, ureido, alkyl, alkenyl, alkynyl, alkoxy, alkanoyl, alkoxycarbonyl, N-alkylsulphamoyl, N-alkylcarbamoyl, -OR11, -OR12R11, or -R12R11; and methods of making and using the same. Such compounds may be used in inflammatory or myeloproliferative disorders. The disclosure also provides for treating cancer.
摘要翻译：本文提供了式（I）的吡咯并嘧啶化合物，其中R 1是含有至少一个S原子的杂芳基，并且任选地在环碳上被一个，两个或三个取代基取代，所述取代基各自独立地选自：卤素，羟基，硝基，甲酰基，甲酰氨基，氰基，磺酰基，羧基，氨基，酰氨基，酰氨基，氨基甲酰基，氨磺酰基，烷基，烯基，CF 3，脲基，炔基，烷氧基，烷酰基，烷氧羰基，甲醛肟，N-烷基氨磺酰，N-烷基氨基甲酰基， OR13R11或-R13R11; R2是苯基或吡啶基，其中R2任选地在环碳上被一个，两个或三个取代基取代，每个独立地选自：卤素，羟基，氰基，硝基，甲酰基，甲酰氨基，羧基，磺酰基，氨基，酰氨基，-N-烷基氨基，氨基甲酰基，氨磺酰基，CF 3，脲基，烷基，烯基，炔基，烷氧基，烷酰基，烷氧基羰基，N-烷基氨磺酰基，N-烷基氨基甲酰基，-OR 11，-OR 12 R 11或-R 12 R 11; 以及制作和使用它们的方法。这些化合物可用于炎性或骨髓增生性疾病。本公开还提供治疗癌症。

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