公开(公告)号：WO2008106692B1

公开(公告)日：2008-10-30

申请号：PCT/US2008055724

申请日：2008-03-03

Applicant: NOVARTIS VACCINES & DIAGNOSTIC ,  BURGER MATTHEW ,  LINDVALL MIKA ,  HAN WOOSEOK ,  LAN JIONG ,  NISHIGUCHI GISELE ,  SHAFER CYNTHIA ,  BELLAMACINA CORNELIA ,  HUH KAY ,  ATALLAH GORDANA ,  MCBRIDE CHRISTOPHER ,  ANTONIOS-MCCREA WILLIAM JR ,  ZAVOROTINSKAYA TATIANA ,  WALTER ANNETTE ,  GARCIA PABLO

Inventor： BURGER MATTHEW ,  LINDVALL MIKA ,  HAN WOOSEOK ,  LAN JIONG ,  NISHIGUCHI GISELE ,  SHAFER CYNTHIA ,  BELLAMACINA CORNELIA ,  HUH KAY ,  ATALLAH GORDANA ,  MCBRIDE CHRISTOPHER ,  ANTONIOS-MCCREA WILLIAM JR ,  ZAVOROTINSKAYA TATIANA ,  WALTER ANNETTE ,  GARCIA PABLO

IPC: C07D213/78 ,  A61K31/44 ,  A61P35/00 ,  C07D239/28 ,  C07D401/12

CPC classification number: C07D401/12 ,  C07D213/78 ,  C07D239/28

Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase- mediated disorder, such as cancer.

Abstract translation: 提供了在人或动物受试者中抑制与肿瘤发生相关的激酶活性的新化合物，组合物和方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：WO2014039831A1

公开(公告)日：2014-03-13

申请号：PCT/US2013/058527

申请日：2013-09-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  CHERUVALLATH, Zacharia ,  KOMANDLA, Mallareddy ,  LAWSON, John David ,  MCBRIDE, Christopher ,  TANG, Mingnam

Inventor： CHERUVALLATH, Zacharia ,  KOMANDLA, Mallareddy ,  LAWSON, John David ,  MCBRIDE, Christopher ,  TANG, Mingnam

IPC: C07D487/14 ,  A61K31/4162 ,  A61P3/04

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  C07D487/14 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (1), and pharmaceutically acceptable salts thereof, wherein L, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Abstract translation: 公开了式（1）的化合物及其药学上可接受的盐，其中L，R 1，R 2，R 3，R 4，R 5，R 6和R 7在说明书中定义。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗与MetAP2相关的肥胖症和相关疾病，病症和病症的用途。

公开(公告)号：WO2006113498A3

公开(公告)日：2007-01-11

申请号：PCT/US2006014194

申请日：2006-04-14

Applicant: CHIRON CORP ,  MACHAJEWSKI TIMOTHY D ,  GAO ZHENHAI ,  LEVINE BARRY H ,  ANTONIOS-MCCREA WILLIAM ,  BELLAMACINA CORNELIA R ,  COSTALES ABRAN ,  DOUGHAN BRANDON M ,  FONG SUSAN ,  HENDRICKSON THOMAS ,  LIN XIAODONG ,  MCBRIDE CHRISTOPHER ,  MCKENNA MAUREEN ,  RICO ALICE C ,  SHAFER CYNTHIA M ,  WANG X MICHAEL ,  ZHOU YASHEEN ,  XIA YI ,  MENDENHALL KRIS G

Inventor： MACHAJEWSKI TIMOTHY D ,  GAO ZHENHAI ,  LEVINE BARRY H ,  ANTONIOS-MCCREA WILLIAM ,  BELLAMACINA CORNELIA R ,  COSTALES ABRAN ,  DOUGHAN BRANDON M ,  FONG SUSAN ,  HENDRICKSON THOMAS ,  LIN XIAODONG ,  MCBRIDE CHRISTOPHER ,  MCKENNA MAUREEN ,  RICO ALICE C ,  SHAFER CYNTHIA M ,  WANG X MICHAEL ,  ZHOU YASHEEN ,  XIA YI ,  MENDENHALL KRIS G

IPC: C07D239/84 ,  A61K31/517 ,  A61P35/00 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12

CPC classification number: C07D401/14 ,  C07D239/84 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

Abstract: 2-Amino-quinazolin-5-one compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cell proliferative diseases.

Abstract translation: 2-氨基 - 喹唑啉-5-酮化合物，立体异构体，互变异构体，其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种2-氨基 - 喹唑啉-5-酮化合物的组合物，单独或与至少一种另外的治疗剂组合。 单独使用2-氨基 - 喹唑啉-5-酮化合物或与至少一种其它治疗剂组合使用的方法用于预防或治疗细胞增殖性疾病。

公开(公告)号：WO2009042711A4

公开(公告)日：2009-06-04

申请号：PCT/US2008077558

申请日：2008-09-24

Applicant: TAKEDA PHARMACEUTICAL ,  CAO SHELDON X ,  FEHER VICTORIA ,  ICHIKAWA TAKASHI ,  JONES BENJAMIN ,  KALDOR STEPHEN W ,  KIRYANOV ANDRE A ,  LIU YAN ,  MCBRIDE CHRISTOPHER ,  NATALA SRINIVASA REDDY ,  NIE ZHE ,  STAFFORD JEFFREY A ,  LAM BETTY

Inventor： CAO SHELDON X ,  FEHER VICTORIA ,  ICHIKAWA TAKASHI ,  JONES BENJAMIN ,  KALDOR STEPHEN W ,  KIRYANOV ANDRE A ,  LIU YAN ,  MCBRIDE CHRISTOPHER ,  NATALA SRINIVASA REDDY ,  NIE ZHE ,  STAFFORD JEFFREY A ,  LAM BETTY

IPC: A61K31/4545 ,  A61P11/00 ,  A61P37/08 ,  C07D487/04 ,  C07D487/14

CPC classification number: C07D487/04 ,  C07D487/14 ,  C07D519/00

Abstract: Compounds of the following formula are provided for use with kinases: (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 提供下式的化合物用于激酶：（I），其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：WO2009067547A1

公开(公告)日：2009-05-28

申请号：PCT/US2008/084078

申请日：2008-11-19

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  CAO, Sheldon X. ,  FEHER, Victoria ,  ICHIKAWA, Takashi ,  JONES, Benjamin ,  KALDOR, Stephen W. ,  KIRYANOV, Andre A. ,  LAM, Betty ,  LIU, Yan ,  MCBRIDE, Christopher ,  NATALA, Srinivasa Reddy ,  NIE, Zhe ,  STAFFORD, Jeffrey A.

Inventor： CAO, Sheldon X. ,  FEHER, Victoria ,  ICHIKAWA, Takashi ,  JONES, Benjamin ,  KALDOR, Stephen W. ,  KIRYANOV, Andre A. ,  LAM, Betty ,  LIU, Yan ,  MCBRIDE, Christopher ,  NATALA, Srinivasa Reddy ,  NIE, Zhe ,  STAFFORD, Jeffrey A.

IPC: C07D487/04 ,  A61K31/551 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: Compounds of the following formula are provided for use with kinases, wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 提供下式的化合物用于激酶，其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：WO2009042806A1

公开(公告)日：2009-04-02

申请号：PCT/US2008/077746

申请日：2008-09-25

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  MCBRIDE, Christopher ,  ZHIE, Nie

Inventor： MCBRIDE, Christopher ,  ZHIE, Nie

IPC: A61K31/4545 ,  C07D487/04 ,  A61P37/08 ,  A61P11/00

CPC classification number: C07D487/04 ,  C07D487/14 ,  C07D519/00

Abstract: The present invention relates generally to processes of making 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl benzamide and Form A of 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl benzamide.

Abstract translation: 本发明一般涉及制备4-（9-环戊基-7,7-二氟-5-甲基-6-氧代-6,7,8,9-四氢-5H-嘧啶并[4,5-b] [1,4]二氮杂-2-基氨基）-3-甲氧基-N-（1-甲基哌啶-4-基苯甲酰胺）和4-（9-环戊基-7,7-二氟-5-甲基-6- -4-氧代-6,7,8,9-四氢-5H-嘧啶并[4,5-b] [1,4]二氮杂-2-基氨基）-3-甲氧基-N-（1-甲基哌啶-4-基苯甲酰胺）

公开(公告)号：WO2007030377A1

公开(公告)日：2007-03-15

申请号：PCT/US2006/034088

申请日：2006-08-30

Applicant: NOVARTIS AG ,  AIKAWA, Mina E. ,  AMIRI, Payman ,  DOVE, Jeffrey H. ,  LEVINE, Barry Haskell ,  MCBRIDE, Christopher ,  PICK, Teresa E. ,  POON, Daniel J. ,  RAMURTHY, Savithri ,  RENHOWE, Paul A. ,  SHAFER, Cynthia ,  STUART, Darrin ,  SUBRAMANIAN, Sharadha

Inventor： AIKAWA, Mina E. ,  AMIRI, Payman ,  DOVE, Jeffrey H. ,  LEVINE, Barry Haskell ,  MCBRIDE, Christopher ,  PICK, Teresa E. ,  POON, Daniel J. ,  RAMURTHY, Savithri ,  RENHOWE, Paul A. ,  SHAFER, Cynthia ,  STUART, Darrin ,  SUBRAMANIAN, Sharadha

IPC: C07D401/14 ,  A61K31/435 ,  A61P35/00

CPC classification number: C07D401/14 ,  Y02P20/55

Abstract: New substituted benzimidazole compounds of formula (I), compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase or receptor tyrosine kinase mediated disorder, such as cancer.

Abstract translation: 提供式（I）的新取代的苯并咪唑化合物，组合物和抑制与人或动物受试者的肿瘤发生相关的激酶活性的方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：WO2006113498A2

公开(公告)日：2006-10-26

申请号：PCT/US2006/014194

申请日：2006-04-14

Applicant: CHIRON CORPORATION ,  MACHAJEWSKI, Timothy, D. ,  GAO, Zhenhai ,  LEVINE, Barry, H. ,  ANTONIOS-MCCREA, William ,  BELLAMACINA, Cornelia, R. ,  COSTALES, Abran ,  DOUGHAN, Brandon, M. ,  FONG, Susan ,  HENDRICKSON, Thomas ,  LIN, Xiaodong ,  MCBRIDE, Christopher ,  MCKENNA, Maureen ,  RICO, Alice, C. ,  SHAFER, Cynthia, M. ,  WANG, X., Michael ,  ZHOU, Yasheen ,  XIA, Yi ,  MENDENHALL, Kris, G.

Inventor： MACHAJEWSKI, Timothy, D. ,  GAO, Zhenhai ,  LEVINE, Barry, H. ,  ANTONIOS-MCCREA, William ,  BELLAMACINA, Cornelia, R. ,  COSTALES, Abran ,  DOUGHAN, Brandon, M. ,  FONG, Susan ,  HENDRICKSON, Thomas ,  LIN, Xiaodong ,  MCBRIDE, Christopher ,  MCKENNA, Maureen ,  RICO, Alice, C. ,  SHAFER, Cynthia, M. ,  WANG, X., Michael ,  ZHOU, Yasheen ,  XIA, Yi ,  MENDENHALL, Kris, G.

CPC classification number: C07D401/14 ,  C07D239/84 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

Abstract: 2-Amino-quinazolin-5-one compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cell proliferative diseases.

Abstract translation: 2-氨基 - 喹唑啉-5-酮化合物，立体异构体，互变异构体，药用盐和前药; 包括药学上可接受的载体和一种或多种2-氨基 - 喹唑啉-5-酮化合物的组合物，单独或与至少一种另外的治疗剂组合。 将2-氨基 - 喹唑啉-5-酮化合物单独使用或与至少一种另外的治疗剂组合使用的方法用于预防或治疗细胞增殖性疾病。

公开(公告)号：WO2004018419A2

公开(公告)日：2004-03-04

申请号：PCT/US2003/025990

申请日：2003-08-19

Applicant: CHIRON CORPORATION ,  BARSANTI, Paul, A. ,  BUSSIERE, Dirksen ,  HARRISON, Stephen, D. ,  HEISE, Carla, C. ,  JANSEN, Johanna, M. ,  JAZAN, Elisa ,  MACHAJEWSKI, Timothy, D. ,  McBRIDE, Christopher ,  McCREA, William, R. ,  NG, Simon ,  NI, Zhi-Jie ,  PECCHI, Sabina ,  PFISTER, Keith ,  RAMURTHY, Savithri ,  RENHOWE, Paul, A. ,  SHAFER, Cynthia, M. ,  SILVER, Joel, B. ,  WAGMAN, Allan ,  WEISMANN, Marion

Inventor： BARSANTI, Paul, A. ,  BUSSIERE, Dirksen ,  HARRISON, Stephen, D. ,  HEISE, Carla, C. ,  JANSEN, Johanna, M. ,  JAZAN, Elisa ,  MACHAJEWSKI, Timothy, D. ,  McBRIDE, Christopher ,  McCREA, William, R. ,  NG, Simon ,  NI, Zhi-Jie ,  PECCHI, Sabina ,  PFISTER, Keith ,  RAMURTHY, Savithri ,  RENHOWE, Paul, A. ,  SHAFER, Cynthia, M. ,  SILVER, Joel, B. ,  WAGMAN, Allan ,  WEISMANN, Marion

IPC: C07D

CPC classification number: C07D401/04 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/52 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D453/02 ,  C07D453/06 ,  C07D471/04

Abstract: Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.

Abstract translation: 提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或1B的化合物，其药学上可接受的盐，其互变异构体或其药学上可接受的盐 互变异构体。 具有结构I和IB的化合物具有以下结构并且具有本文所述的变量。 此类化合物可用于制备用于抑制各种酶的药物和用于治疗由这些酶介导的病症的药物。

公开(公告)号：WO2013130855A1

公开(公告)日：2013-09-06

申请号：PCT/US2013/028386

申请日：2013-02-28

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  CHERUVALLATH, Zacharia ,  ERICKSON, Philip ,  FENG, Jun ,  KOMANDLA, Mallareddy ,  LAWSON, John David ,  MCBRIDE, Christopher ,  MIURA, Joanne ,  MURPHY, Sean ,  TANG, Mingnam ,  TON-NU, Huong-Thu

Inventor： CHERUVALLATH, Zacharia ,  ERICKSON, Philip ,  FENG, Jun ,  KOMANDLA, Mallareddy ,  LAWSON, John David ,  MCBRIDE, Christopher ,  MIURA, Joanne ,  MURPHY, Sean ,  TANG, Mingnam ,  TON-NU, Huong-Thu

IPC: C07D401/14 ,  C07D413/14 ,  C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D407/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/416 ,  A61P3/04

CPC classification number: C07D498/04 ,  A61K31/416 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D407/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和R 6在本说明书中定义。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗与MetAP2相关的肥胖症和相关疾病，病症和病症的用途。