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1. 发明专利

AU2007333243A1 Phosphoinositide 3-kinase inhibitor compounds and methods of use 未知
公开(公告)号：AU2007333243A1
公开(公告)日：2008-06-19
申请号：AU2007333243
申请日：2007-12-05
申请人： GENENTECH INC , DANIEL SUTHERLIN , CASTANEDO GEORGETTE , BAYLISS TRACY , CHUCKOWREE IRINA , DOTSON JENNAFER , FOLKES ADRIAN , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , STABEN STEVEN , ZHU BING-YAN , TSUI VICKIE , WANG SHUMEI , PIRAMED LTD , NAN WAN
发明人： GUNZNER JANET , HEFFRON TIM , GOLDSMITH RICHARD , STABEN STEVEN , CHUCKOWREE IRINA , WANG SHUMEI , DOTSON JENNAFER , FOLKES ADRIAN , SUTHERLIN DANIEL P , BAYLISS TRACY , WAN NAN CHI , MATHIEU SIMON , TSUI VICKIE , CASTANEDO GEORGETTE , ZHU BING-YAN , OLIVERO ALAN
IPC分类号： A61K31/519 , A61P35/00 , C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

2. 发明申请

WO2007106192A2 INHIBITORS OF IAP 审中-公开
标题翻译： IAP的抑制剂
公开(公告)号：WO2007106192A2
公开(公告)日：2007-09-20
申请号：PCT/US2006/062335
申请日：2006-12-19
申请人： GENENTECH, INC. , KOEHLER, Michael F. T. , GAZZARD, Lewis, J. , TSUI, Vickie Hsiao-wei
发明人： KOEHLER, Michael F. T. , GAZZARD, Lewis, J. , TSUI, Vickie Hsiao-wei
IPC分类号： A61K31/52 , C07D473/10
CPC分类号： C07D403/04 , C07D417/04 , C07D417/14 , C07D513/04
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X 1 , X 2 , Y, Z 1 , Z 2 , Z 3 , Z 4 , R 1 , R 2 , R 3 , R 3' , R4, R 4', R 5 , R 6 , R 6' and n are as described herein.
摘要翻译：本发明提供可用作治疗恶性肿瘤的治疗剂的IAP新型抑制剂，其中化合物具有通式（I）：其中Q，X 1，X 2， Y，Z 1，Z 2，Z 3，Z 4，R 1，N 1， R 1，R 2，R 3，R 3'，R 4，R 4'，R“ 5，R 6，R 6'和n如本文所述。

3. 发明申请

WO2013024002A1 PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：吡咯并[3,4-c]吡啶化合物及其使用方法
公开(公告)号：WO2013024002A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/065643
申请日：2012-08-10
申请人： F. HOFFMANN-LA ROCHE AG , DO, Steven , HU, Huiyong , KOLESNIKOV, Aleksandr , LEE, Wendy , TSUI, Vickie Hsiao-Wei , WANG, Xiaojing , WEN, Zhaoyang
发明人： DO, Steven , HU, Huiyong , KOLESNIKOV, Aleksandr , LEE, Wendy , TSUI, Vickie Hsiao-Wei , WANG, Xiaojing , WEN, Zhaoyang
IPC分类号： C07D471/04 , A61K31/437 , A61P9/00 , A61P35/00 , A61P37/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/506 , A61K31/55 , A61K31/551 , A61K45/06 , C07D231/00 , C07D519/00
摘要： Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R 1 and R 2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式I的吡唑并[3,4-c]吡啶化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中R 1和R 2如本文所定义，可用于抑制Pim激酶，由Pim激酶介导的癌症。公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

4. 发明申请

WO2011113802A3 IMIDAZOPYRIDINE AND PURINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
公开(公告)号：WO2011113802A3
公开(公告)日：2011-09-22
申请号：PCT/EP2011/053826
申请日：2011-03-15
申请人： F. HOFFMANN-LA ROCHE AG , LAI, Yingjie , LIANG, Jun , MAGNUSON, Steven R. , TSUI, Vickie H. , ZHANG, Birong , ROBARGE, Kirk
发明人： LAI, Yingjie , LIANG, Jun , MAGNUSON, Steven R. , TSUI, Vickie H. , ZHANG, Birong , ROBARGE, Kirk
IPC分类号： A61K31/437 , A61K31/4406 , A61K31/4409 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K31/541 , C07D471/04 , C07D473/34 , C07D491/107 , A61P1/00 , A61P17/06 , A61P29/00
摘要： The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R 1 , R 2 , R 4 , R 5 and R 16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy., as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illenesses, inflammatory bowel disease or psoriasis.

5. 发明申请

WO2005094818A1 AZABICYCLO-OCTANE INHIBITORS OF IAP 审中-公开
标题翻译：化学文摘AZABICYCLO-OCTANE抑制剂
公开(公告)号：WO2005094818A1
公开(公告)日：2005-10-13
申请号：PCT/US2005/009328
申请日：2005-03-22
申请人： GENENTECH, INC. , COHEN, Frederick , FAIRBROTHER, Wayne , FLYGARE, John , TSUI, Vickie, Hsiao-Wei , KETELTAS, Stephen, Franz
发明人： COHEN, Frederick , FAIRBROTHER, Wayne , FLYGARE, John , TSUI, Vickie, Hsiao-Wei , KETELTAS, Stephen, Franz
IPC分类号： A61K31/403
CPC分类号： C07K5/06026 , C07K14/4747
摘要： The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X 1 and X 2 are independently O or S; L is a bond or -C(X 3 )-, -C(X 3 )NR 12 , -C(X 3 )O- wherein X 3 is O or S and R 12 is H or R 1 ; R 1 is alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; R 2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R 3 is H or alkyl; R 4 and R 4' are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R 5 , and R 5' are each independently H or alkyl; R 6 is H or alkyl; and salts and solvates thereof.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有其中X 1和X 2独立地为O或S的通式（I）; L是键或-C（X3） - ， - C（X3）NR12，-C（X3）O-，其中X3是O或S，R12是H或R1; R 1是烷基，碳环，碳环取代的烷基，杂环或杂环取代的烷基，其中各自任选被卤素，羟基，巯基，羧基，烷基，卤代烷基，烷氧基，烷基磺酰基，氨基，硝基，芳基和杂芳基取代; R2是烷基，环烷基，环烷基烷基，芳基，芳烷基，杂环或杂环基烷基; R3是H或烷基; R 4和R 4'独立地是H，烷基，芳基，芳烷基，环烷基，环烷基烷基，杂芳基或杂芳烷基，其中各自任选被卤素，羟基，巯基，羧基，烷基，烷氧基，氨基和硝基取代; R5和R5'各自独立地为H或烷基; R6是H或烷基; 及其盐和溶剂合物。

6. 发明申请

WO2013045461A1 PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：吡唑-4-基 - 环己基 - 羧酰胺化合物及其使用方法
公开(公告)号：WO2013045461A1
公开(公告)日：2013-04-04
申请号：PCT/EP2012/068899
申请日：2012-09-26
申请人： F. HOFFMANN-LA ROCHE AG , HODGES, Alastair J. , MATTEUCCI, Mizio , SHARPE, Andrew , SUN, Minghua , TSUI, Vickie H. , WANG, Xiaojing
发明人： HODGES, Alastair J. , MATTEUCCI, Mizio , SHARPE, Andrew , SUN, Minghua , TSUI, Vickie H. , WANG, Xiaojing
IPC分类号： C07D401/14 , C07D403/14 , C07D417/12 , C07D417/14 , C07D451/06 , C07D471/10 , C07D487/10 , C07D498/04 , C07D498/08 , C07D498/10 , C07D491/107 , A61P35/00 , A61K31/427 , A61K31/55 , A61K31/4965
CPC分类号： C07D417/14 , A61K31/427 , A61K31/435 , A61K31/454 , A61K31/496 , A61K31/5386 , A61K31/55 , A61K31/551 , A61K31/553 , A61K45/06 , C07D401/14 , C07D403/14 , C07D417/12 , C07D451/06 , C07D471/10 , C07D487/10 , C07D491/107 , C07D498/04 , C07D498/08 , C07D498/10
摘要： Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula (I), including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula (I), for in vitro, in situ , and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）的吡唑-4-基 - 杂环基 - 甲酰胺化合物，其包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中X是噻唑基，吡嗪基，吡啶基或嘧啶基，可用于抑制Pim激酶，并用于治疗诸如由Pim激酶介导的癌症的病症。公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种病症的方法。

7. 发明申请

WO2013041539A1 IMIDAZOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：咪唑吡啶化合物，组合物和使用方法
公开(公告)号：WO2013041539A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/068380
申请日：2012-09-19
申请人： F. HOFFMANN-LA ROCHE AG , LAI, Yingjie , LIANG, Jun , MAGNUSON, Steven, R. , ROBARGE, Kirk, D. , TSUI, Vickie, Hsaio-Wei , ZHANG, Birong
发明人： LAI, Yingjie , LIANG, Jun , MAGNUSON, Steven, R. , ROBARGE, Kirk, D. , TSUI, Vickie, Hsaio-Wei , ZHANG, Birong
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention provides TYK2 inhibitors of Formulas (la-lb), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R a , R 1 , R 2 , R 4 , R 5 and R 16 are defined herein, a pharmaceutical composition that includes a compound of Formulas (la-lb) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in the therapy of inflammatory diseases.
摘要翻译：本发明提供式（Ia-1b）的TYK2抑制剂，其立体异构体或其药学上可接受的盐，其中A，X，Ra，R 1，R 2，R 4，R 5和R 16在本文中定义，药物组合物包括式 1a-1b）和药学上可接受的载体，佐剂或载体，以及在治疗炎性疾病中使用该化合物或组合物的方法。

8. 发明申请

WO2010142752A1 JANUS KINASE INHIBITOR COMPOUNDS AND METHODS 审中-公开
标题翻译：甘油激酶抑制剂化合物和方法
公开(公告)号：WO2010142752A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/058128
申请日：2010-06-10
申请人： F. HOFFMANN-LA ROCHE AG , GOODACRE, Simon Charles , LAI, Yingjie , LIANG, Jun , MAGNUSON, Steven R. , ROBARGE, Kirk D. , STANLEY, Mark S. , TSUI, Vickie Hsiao-Wei , WILLIAMS, Karen , ZHANG, Birong , ZHOU, Aihe
发明人： GOODACRE, Simon Charles , LAI, Yingjie , LIANG, Jun , MAGNUSON, Steven R. , ROBARGE, Kirk D. , STANLEY, Mark S. , TSUI, Vickie Hsiao-Wei , WILLIAMS, Karen , ZHANG, Birong , ZHOU, Aihe
IPC分类号： C07D213/75 , C07D401/12 , A61K31/506 , A61K31/495 , A61K31/4439 , A61K31/444 , A61P37/04
CPC分类号： C07D213/75 , C07D401/12
摘要： The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R 1 , R 2 , R 4 and R 5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I), methods of making those compounds as well as methods of use thereof
摘要翻译：本发明提供式（I）化合物，其立体异构体或其药学上可接受的盐，其中A，B，D，R 1，R 2，R 4和R 5在本文中定义，药物组合物包含式（I）化合物，使这些化合物及其使用方法

9. 发明申请

WO2008073785A2 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：磷酸三辛酯抑制剂化合物及其使用方法
公开(公告)号：WO2008073785A2
公开(公告)日：2008-06-19
申请号：PCT/US2007/086533
申请日：2007-12-05
申请人： GENENTECH, INC. , PIRAMED LIMITED , CASTANEDO, Georgette , DOTSON, Jennafer , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , TSUI, Vickie , WANG, Shumei , ZHU, Bing-Yan , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
发明人： CASTANEDO, Georgette , DOTSON, Jennafer , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , TSUI, Vickie , WANG, Shumei , ZHU, Bing-Yan , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
IPC分类号： C07D491/048 , C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).
摘要翻译：式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的其盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗由脂质激酶介导的癌症等疾病。公开了使用式Ia-d化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种疾病的方法。式（Ic）和（Id）。

10. 发明申请

WO2012066061A1 PYRAZOLOPYRIDINES AND PYRAZOLOPYRIDINES AND THEIR USE AS TYK2 INHIBITORS 审中-公开
标题翻译：吡唑并吡啶和吡唑并吡啶及其作为TY2抑制剂的用途
公开(公告)号：WO2012066061A1
公开(公告)日：2012-05-24
申请号：PCT/EP2011/070313
申请日：2011-11-17
申请人： F. HOFFMANN-LA ROCHE AG , BLENCH, Toby , GOODACRE, Simon , LAI, Yingjie , LIANG, Yun , MACLEOD, Calum , MAGNUSON, Steven , TSUI, Vickie , WILLIAMS, Karen , ZHANG, Birong
发明人： BLENCH, Toby , GOODACRE, Simon , LAI, Yingjie , LIANG, Yun , MACLEOD, Calum , MAGNUSON, Steven , TSUI, Vickie , WILLIAMS, Karen , ZHANG, Birong
IPC分类号： C07D471/04 , C07D487/04 , A61K31/37 , A61K31/519 , A61P11/02 , A61P11/06 , A61P17/06 , A61P19/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R 1 , R 2 , R 4 and R 5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as TYK2 Kinase inhibitors.
摘要翻译：本发明提供式（I）的化合物，其立体异构体或其药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义;药物组合物，其包含式（I）的化合物和药学上可接受的载体，佐剂或载体，以及在治疗中使用该化合物或组合物的方法，作为TYK2激酶抑制剂。

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