公开(公告)号：WO2006068992A1

公开(公告)日：2006-06-29

申请号：PCT/US2005/045907

申请日：2005-12-16

Applicant: ELI LILLY AND COMPANY ,  AICHER, Thomas, Daniel ,  CHICARELLI, Mark, Joseph ,  GAUTHIER, Cassandra, A. ,  HINKLIN, Ronald, Jay ,  TIAN, Hongqi ,  WALLACE, Owen, Brendan ,  KRASUTSKY, Alexei, Pavlovych ,  ALLEN, John, Gordon

Inventor： AICHER, Thomas, Daniel ,  CHICARELLI, Mark, Joseph ,  GAUTHIER, Cassandra, A. ,  HINKLIN, Ronald, Jay ,  TIAN, Hongqi ,  WALLACE, Owen, Brendan ,  KRASUTSKY, Alexei, Pavlovych ,  ALLEN, John, Gordon

IPC: A61K31/4015 ,  C07D207/27 ,  C07D211/76 ,  C07D401/12 ,  A61K31/4025 ,  A61K31/4412 ,  A61P3/04

CPC classification number: C07D207/26 ,  C07D207/267 ,  C07D207/27 ,  C07D401/10

Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention compositions containing these compounds for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula I wherein G 1 is methylene or ethylene; L is-(C 1 -C 4 )alkylene-, -S-, -CH(OH)-, or -O-; R 0 is Formula II or Formula III and the other substituents are as defined in the claims.

Abstract translation: 本发明提供可用作11-β羟基类固醇脱氢酶1的有效和选择性抑制剂的式I化合物。本发明还提供了一种药物组合物，其包含式I化合物或其药学上可接受的盐 载体，稀释剂或赋形剂。 此外，含有这些化合物用于治疗代谢综合征，糖尿病，高血糖症，肥胖症，高血压，高脂血症，与高血糖症有关的其它症状以及相关疾病的本发明组合物。 式I其中G 1是亚甲基或亚乙基; L是 - （C 1 -C 4 -C 4）亚烷基 - ， - S - ， - CH（OH） - 或-O-; R 0是式II或式III，其它取代基如权利要求中所定义。

公开(公告)号：WO2007077961A2

公开(公告)日：2007-07-12

申请号：PCT/JP2006326367

申请日：2006-12-27

Applicant: TAKEDA PHARMACEUTICAL ,  FUKUMOTO SHOJI ,  MATSUNAGA NOBUYUKI ,  OHRA TAIICHI ,  OHYABU NORIO ,  HASUI TOMOAKI ,  MOTOYAJI TAKASHI ,  SIEDEM CHRISTOPHER STEPHEN ,  TANG TONY PISAL ,  DEMEESE LISA A ,  GAUTHIER CASSANDRA

Inventor： FUKUMOTO SHOJI ,  MATSUNAGA NOBUYUKI ,  OHRA TAIICHI ,  OHYABU NORIO ,  HASUI TOMOAKI ,  MOTOYAJI TAKASHI ,  SIEDEM CHRISTOPHER STEPHEN ,  TANG TONY PISAL ,  DEMEESE LISA A ,  GAUTHIER CASSANDRA

IPC: C07D403/04 ,  A61K31/423 ,  A61K31/538 ,  A61K31/542 ,  A61P9/04 ,  A61P9/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D417/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.

Abstract translation: 本发明涉及其中每个符号如说明书中所定义的。 该化合物具有优异的矿物质皮质激素受体拮抗作用，可用作预防或治疗高血压，心力衰竭等的药剂，具有稠合杂环的化合物或其前药或其盐; 以及预防或治疗高血压，心力衰竭等的药剂。

公开(公告)号：WO2004032882A3

公开(公告)日：2004-07-08

申请号：PCT/US0333317

申请日：2003-10-10

Applicant: SMITHKLINE BEECHAM CORP ,  BROWN MATTHEW LEE ,  CHEUNG MUI ,  DICKERSON SCOTT HOWARD ,  GAUTHIER CASSANDRA ,  HARRIS PHILIP ANTHONY ,  HUNTER ROBERT NEIL III ,  PACOFSKY GREGORY ,  PEEL MICHAEL ROBERT ,  STAFFORD JEFFREY ALAN

Inventor： BROWN MATTHEW LEE ,  CHEUNG MUI ,  DICKERSON SCOTT HOWARD ,  GAUTHIER CASSANDRA ,  HARRIS PHILIP ANTHONY ,  HUNTER ROBERT NEIL III ,  PACOFSKY GREGORY ,  PEEL MICHAEL ROBERT ,  STAFFORD JEFFREY ALAN

IPC: A61K20060101 ,  A61K31/421 ,  A61K31/422 ,  C07D263/30 ,  C07D263/48 ,  C07D413/02 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

CPC classification number: C07D263/48 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

Abstract: Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Abstract translation: 本文描述了用作VEGFR2，CDK2和CDK4抑制剂的恶唑衍生物。 所描述的本发明还包括制备这种恶唑衍生物的方法以及使用它们治疗过度增殖性疾病的方法。

公开(公告)号：WO2007077961A3

公开(公告)日：2007-07-12

申请号：PCT/JP2006/326367

申请日：2006-12-27

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  FUKUMOTO, Shoji ,  MATSUNAGA, Nobuyuki ,  OHRA, Taiichi ,  OHYABU, Norio ,  HASUI, Tomoaki ,  MOTOYAJI, Takashi ,  SIEDEM, Christopher, Stephen ,  TANG, Tony, Pisal ,  DEMEESE, Lisa, A. ,  GAUTHIER, Cassandra

Inventor： FUKUMOTO, Shoji ,  MATSUNAGA, Nobuyuki ,  OHRA, Taiichi ,  OHYABU, Norio ,  HASUI, Tomoaki ,  MOTOYAJI, Takashi ,  SIEDEM, Christopher, Stephen ,  TANG, Tony, Pisal ,  DEMEESE, Lisa, A. ,  GAUTHIER, Cassandra

IPC: C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/423 ,  A61K31/538 ,  A61K31/542 ,  A61P9/04 ,  A61P9/12

Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.

公开(公告)号：WO2004032882A2

公开(公告)日：2004-04-22

申请号：PCT/US2003/033317

申请日：2003-10-10

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BROWN, Matthew, Lee ,  CHEUNG, Mui ,  DICKERSON, Scott, Howard ,  GAUTHIER, Cassandra ,  HARRIS, Philip, Anthony ,  HUNTER, Robert, Neil, III ,  PACOFSKY, Gregory ,  PEEL, Michael, Robert ,  STAFFORD, Jeffrey, Alan

Inventor： BROWN, Matthew, Lee ,  CHEUNG, Mui ,  DICKERSON, Scott, Howard ,  GAUTHIER, Cassandra ,  HARRIS, Philip, Anthony ,  HUNTER, Robert, Neil, III ,  PACOFSKY, Gregory ,  PEEL, Michael, Robert ,  STAFFORD, Jeffrey, Alan

IPC: A61K

CPC classification number: C07D263/48 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

Abstract: Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Abstract translation: 本文描述了可用作VEGFR2，CDK2和CDK4抑制剂的恶唑衍生物。 所述的发明还包括制备这种恶唑衍生物的方法以及使用它们在治疗过度增殖性疾病中的方法。