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公开(公告)号：WO2012025187A3
公开(公告)日：2012-06-21
申请号：PCT/EP2011003831
申请日：2011-07-29
Applicant: MERCK PATENT GMBH , BURGDORF LARS , SCHULTZ MELANIE , HOFMANN TATJANA , HODOUS BRIAN , POTNICK JUSTIN , SUTTON AMANDA E , HUCK BAYARD R
Inventor： BURGDORF LARS , SCHULTZ MELANIE , HOFMANN TATJANA , HODOUS BRIAN , POTNICK JUSTIN , SUTTON AMANDA E , HUCK BAYARD R
IPC: C07D491/04 , A61K31/4355
CPC classification number: C07D491/048 , A61K31/4355 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D491/04 , C07D519/00
Abstract: Compounds of the formula (I) in which R1 denotes Ar1 or Het1, R2 denotes Ar2, Het2, NH(CH2)nAr2, O(CH2)nAr2 or NH(CH2)nHet2, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupus.
Abstract translation: 其中R 1表示Ar 1或Het 1的式（I）化合物，R 2表示Ar 2，Het 2，NH（CH 2）nAr 2，O（CH 2）n Ar 2或NH（CH 2）n Het 2）是Syk的抑制剂， 尤其用于治疗类风湿性关节炎和/或系统性红斑狼疮。
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公开(公告)号：WO2011017142A1
公开(公告)日：2011-02-10
申请号：PCT/US2010/043467
申请日：2010-07-28
Applicant: MERCK PATENT GMBH , CHEN, Xiaoling , KARRA, Srinivasa R. , HUCK, Bayard R. , LAN, Ruoxi , SUTTON, Amanda E. , GOUTOPOULOS, Andreas , HODOUS, Brian L. , JONES, Reinaldo C.
Inventor： CHEN, Xiaoling , KARRA, Srinivasa R. , HUCK, Bayard R. , LAN, Ruoxi , SUTTON, Amanda E. , GOUTOPOULOS, Andreas , HODOUS, Brian L. , JONES, Reinaldo C.
IPC: A61P35/00 , A61K31/519 , C07D471/04 , C07D498/14
CPC classification number: C07D471/04 , C07D498/14
Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供根据式（I）的新型取代的氮杂环化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：WO2010002779A2
公开(公告)日：2010-01-07
申请号：PCT/US2009/049035
申请日：2009-06-29
Applicant: MERCK SERONO S.A. , XIAO, Yufang , CHEN, Xiaoling , KARRA, Srinivasa R. , HUCK, Bayard R. , SUTTON, Amanda E. , GOUTOPOULOS, Andreas
Inventor： XIAO, Yufang , CHEN, Xiaoling , KARRA, Srinivasa R. , HUCK, Bayard R. , SUTTON, Amanda E. , GOUTOPOULOS, Andreas
IPC: C07D471/04 , A61K31/436 , A61P35/00
CPC classification number: C07D471/04 , A61K31/436 , A61K45/06 , A61K2300/00
Abstract: Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
Abstract translation: 公开了抑制极光激酶的萘吡啶酮衍生物化合物以及包含这些化合物的药物组合物及其合成方法。 这些化合物可用于治疗由不规则和/或扰乱的极光激酶如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。
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4.发明申请BICYCLIC AZAHETEROCYCLIC CARBOXAMIDES AS INHIBITORS OF THE KINASE P70S6K 审中-公开双环氮杂环碳酰胺作为激酶P70S6K的抑制剂
公开(公告)号：WO2012013282A8
公开(公告)日：2012-03-29
申请号：PCT/EP2011003272
申请日：2011-07-01
Applicant: MERCK PATENT GMBH , HUCK BAYARD R , NEAGU CONSTANTIN , JONES REINALDO C , DESELM LIZBETH CELESTE , XIAO YUFANG , KARRA SRINIVASA R , LAN RUOXI , MOCHALKIN IGOR , SUTTON AMANDA E , RICHARDSON THOMAS E
Inventor： HUCK BAYARD R , NEAGU CONSTANTIN , JONES REINALDO C , DESELM LIZBETH CELESTE , XIAO YUFANG , KARRA SRINIVASA R , LAN RUOXI , MOCHALKIN IGOR , SUTTON AMANDA E , RICHARDSON THOMAS E
IPC: C07D239/74 , A61K31/517 , A61P35/00 , C07D403/12
CPC classification number: C07D239/94 , A61K31/517 , A61K45/06 , C07D239/74 , C07D403/12
Abstract: The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供了根据式（I）的新型双环氮杂杂环羧酰胺化合物，它们的制造和用于治疗过度增殖性疾病例如癌症的用途。
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公开(公告)号：WO2012025187A2
公开(公告)日：2012-03-01
申请号：PCT/EP2011/003831
申请日：2011-07-29
Applicant: MERCK PATENT GMBH , BURGDORF, Lars , SCHULTZ, Melanie , HOFMANN, Tatjana , HODOUS, Brian , POTNICK, Justin , SUTTON, Amanda E. , HUCK, Bayard R.
Inventor： BURGDORF, Lars , SCHULTZ, Melanie , HOFMANN, Tatjana , HODOUS, Brian , POTNICK, Justin , SUTTON, Amanda E. , HUCK, Bayard R.
IPC: C07D491/04
CPC classification number: C07D491/048 , A61K31/4355 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D491/04 , C07D519/00
Abstract: Compounds of the formula I in which R 1 and R 2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and / or systemic lupus.
Abstract translation: 其中R1和R2具有权利要求1所述含义的式I化合物是Syk的抑制剂，并且可以用于治疗类风湿性关节炎和/或系统性红斑狼疮。
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Patent Agency Ranking6.发明申请C-RING MODIFIED TRICYCLIC BENZONAPHTHIRIDINONE PROTEIN KINASE INHIBITORS AND USE THEREOF 审中-公开C环改性三苯并噻吩酮蛋白激酶抑制剂及其用途
公开(公告)号：WO2010077530A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/066319
申请日：2009-12-02
Applicant: MERCK PATENT GMBH , XIAO, Yufang , HUCK, Bayard, R. , SUTTON, Amanda, E. , RICHARDSON, Thomas, E. , KARRA, Srinivasa, R.
Inventor： XIAO, Yufang , HUCK, Bayard, R. , SUTTON, Amanda, E. , RICHARDSON, Thomas, E. , KARRA, Srinivasa, R.
IPC: C07D471/04 , C07D471/14 , C07D495/14 , C07D491/147 , A61K31/4375 , A61P35/00
CPC classification number: C07D471/04 , C07D471/14 , C07D491/147 , C07D495/14
Abstract: Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.
Abstract translation: 公开了C环改性的三环苯并萘环酮化合物及其类似物，包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗适于蛋白激酶信号转导抑制，调节和/或调节的疾病。
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公开(公告)号：WO2010002779A3
公开(公告)日：2011-03-03
申请号：PCT/US2009049035
申请日：2009-06-29
Applicant: MERCK PATENT GMBH , XIAO YUFANG , CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS
Inventor： XIAO YUFANG , CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS
IPC: C07D471/04 , A61K31/436 , A61P35/00
CPC classification number: C07D471/04 , A61K31/436 , A61K45/06 , A61K2300/00
Abstract: Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
Abstract translation: 公开了抑制极光激酶的萘吡啶酮衍生物化合物以及包含这些化合物的药物组合物及其合成方法。 这些化合物可用于治疗由不规则和/或扰乱的极光激酶如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。
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公开(公告)号：WO2009108670A1
公开(公告)日：2009-09-03
申请号：PCT/US2009/035089
申请日：2009-02-25
Applicant: MERCK SERONO S.A. , HUCK, Bayard R. , CHEN, Xiaoling , DE SELM, Lizbeth Celeste , JONES, Christopher Charles Victor , KARRA, Srinivasa R. , XIAO, Yufang , GOUTOPOULOS, Andreas , SUTTON, Amanda E.
Inventor： HUCK, Bayard R. , CHEN, Xiaoling , DE SELM, Lizbeth Celeste , JONES, Christopher Charles Victor , KARRA, Srinivasa R. , XIAO, Yufang , GOUTOPOULOS, Andreas , SUTTON, Amanda E.
IPC: C07D471/04 , A61K31/44 , A61K35/00
CPC classification number: C07D471/04
Abstract: Disclosed are benzonaphthyridinyl derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to kinase signal transduction inhibition, regulation or modulation.
Abstract translation: 公开了苯并萘并吡啶基衍生物化合物及其类似物，包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗适于激酶信号转导抑制，调节或调节的疾病。
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9.发明申请BICYCLIC AZAHETEROCYCLIC CARBOXAMIDES AS INHIBITORS OF THE KINASE P70S6K 审中-公开作为激酶P70S6K的抑制剂的双相类AZAHETEROCYCLIC CARBOXAMIDES
公开(公告)号：WO2012013282A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/003272
申请日：2011-07-01
Applicant: MERCK PATENT GMBH , HUCK, Bayard, R. , NEAGU, Constantin , JONES, Reinaldo C. , DESELM, Lizbeth, Celeste , XIAO, Yufang , KARRA, Srinivasa, R. , LAN, Ruoxi , MACHALKIN, Igor , SUTTON, Amanda, E. , RICHARDSON, Thomas, E.
Inventor： HUCK, Bayard, R. , NEAGU, Constantin , JONES, Reinaldo C. , DESELM, Lizbeth, Celeste , XIAO, Yufang , KARRA, Srinivasa, R. , LAN, Ruoxi , MACHALKIN, Igor , SUTTON, Amanda, E. , RICHARDSON, Thomas, E.
IPC: C07D239/74 , C07D403/12 , A61K31/517 , A61P35/00
CPC classification number: C07D239/94 , A61K31/517 , A61K45/06 , C07D239/74 , C07D403/12
Abstract: The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供了根据式（I）的新型双环氮杂胞苷酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：WO2011017009A1
公开(公告)日：2011-02-10
申请号：PCT/US2010/042844
申请日：2010-07-22
Applicant: MERCK PATENT GMBH , SUTTON, Amanda E. , BRUGGER, Nadia , RICHARDSON, Thomas E. , VANDEVEER, Harold George , HUCK, Bayard R. , LAN, Ruoxi , POTNICK, Justin
Inventor： SUTTON, Amanda E. , BRUGGER, Nadia , RICHARDSON, Thomas E. , VANDEVEER, Harold George , HUCK, Bayard R. , LAN, Ruoxi , POTNICK, Justin
IPC: C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P35/00
CPC classification number: C07D471/04 , C07D333/02 , C07D487/04
Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供根据式（I）的新型取代的氮杂环化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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