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1. 发明申请

WO2007124337A8 BIPHENYL AMIDE LACTAM DERIVATIVES AS INHIBITORS OF 11- BETA-HYDROXYSTEROID DEHYDROGENASE 1 审中-公开
公开(公告)号：WO2007124337A8
公开(公告)日：2007-11-01
申请号：PCT/US2007/066921
申请日：2007-04-19
申请人： ELI LILLY AND COMPANY , AICHER, Thomas, Daniel , CHEN, Zhaogen , HINKLIN, Ronald, Jay , HITE, Gary, Alan , KRASUTSKY, Alexei, Pavlovych , LI, Renhua , MCCOWAN, Jefferson, Ray , SAEED, Ashraf , SNYDER, Nancy, June , TOTH, James, Lee , WALLACE, Owen, Brendan , WINNEROSKI, JUNIOR, Leonard, Larry , XU, Yanping , YORK, Jeremy, Schulenburg
发明人： AICHER, Thomas, Daniel , CHEN, Zhaogen , HINKLIN, Ronald, Jay , HITE, Gary, Alan , KRASUTSKY, Alexei, Pavlovych , LI, Renhua , MCCOWAN, Jefferson, Ray , SAEED, Ashraf , SNYDER, Nancy, June , TOTH, James, Lee , WALLACE, Owen, Brendan , WINNEROSKI, JUNIOR, Leonard, Larry , XU, Yanping , YORK, Jeremy, Schulenburg
IPC分类号： C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D498/04 , A61P3/10 , A61K31/4015
摘要： The present invention discloses novel compounds of Formula I: possessing 11 ß-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ß -HSD type 1 activity.

2. 发明申请

WO2006049952A1 CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 审中-公开
标题翻译：作为11-羟基脱氢酶脱氢酶1的抑制剂的环丙基乳糖衍生物
公开(公告)号：WO2006049952A1
公开(公告)日：2006-05-11
申请号：PCT/US2005/038369
申请日：2005-10-26
申请人： ELI LILLY AND COMPANY , AICHER, Thomas, D. , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan , CHEN, Zhaogen , MABRY, Thomas, Edward , MCCOWAN, Jefferson, Ray , SNYDER, Nancy, June , WINNEROSKI, Leonard, Larry, Junior , ALLEN, John, Gordon
发明人： AICHER, Thomas, D. , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan , CHEN, Zhaogen , MABRY, Thomas, Edward , MCCOWAN, Jefferson, Ray , SNYDER, Nancy, June , WINNEROSKI, Leonard, Larry, Junior , ALLEN, John, Gordon
IPC分类号： A61K31/4015 , C07D207/27 , C07D211/76 , C07D401/10 , C07D403/10 , C07D409/10 , A61K31/4025 , A61K31/4412 , A61P3/04
CPC分类号： C07D403/12 , C07D207/26 , C07D207/267 , C07D207/273 , C07D211/76 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/10
摘要： The present invention discloses compounds of Formula I: (I) having 11beta -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
摘要翻译：本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物：（I），以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及作为药物用于治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，综合征X和与高血糖相关的其它病症的组合物I和组合物的用途。

3. 发明申请

WO2006068992A1 CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 审中-公开
标题翻译：作为11-羟基脱氢酶脱氢酶抑制剂的环丙基乳糖衍生物
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
申请人： 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
发明人： AICHER, Thomas, Daniel , CHICARELLI, Mark, Joseph , GAUTHIER, Cassandra, A. , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan , KRASUTSKY, Alexei, Pavlovych , ALLEN, John, Gordon
IPC分类号： A61K31/4015 , C07D207/27 , C07D211/76 , C07D401/12 , A61K31/4025 , A61K31/4412 , A61P3/04
CPC分类号： C07D207/26 , C07D207/267 , C07D207/27 , C07D401/10
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2006068991A1 CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 审中-公开
标题翻译：作为11-羟基脱氢酶脱氢酶1的抑制剂的环丙基乳糖衍生物
公开(公告)号：WO2006068991A1
公开(公告)日：2006-06-29
申请号：PCT/US2005/045906
申请日：2005-12-16
申请人： ELI LILLY AND COMPANY , AICHER, Thomas, Daniel , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan
发明人： AICHER, Thomas, Daniel , CHICARELLI, Mark, Joseph , HINKLIN, Ronald, Jay , TIAN, Hongqi , WALLACE, Owen, Brendan
IPC分类号： A61K31/4015 , C07D207/27 , C07D211/76 , C07D401/06 , C07D403/06 , C07D495/04 , A61K31/4025 , A61K31/4412 , A61P3/04
CPC分类号： C07D207/26 , C07D405/06 , C07D409/06 , C07D409/14 , C07D495/04
摘要： 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 provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R 0 is (II), or (III) G 1 is methylene or ethylene; L is a divalent linking group selected from -(C 1 -C 4 ) alkylene-, -S-, -CH(OH)-, or -O-; A is methylene, -S-, -O-, or -NH-; and the other substituents are as defined in the claims.
摘要翻译：本发明提供了可用作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，本发明提供包含式I化合物用于治疗代谢综合征，糖尿病，高血糖症，肥胖，高血压，高脂血症，与高血糖症相关的其它症状以及相关疾病的组合物。式（I）其中R 0为（II）或（III）G 1为亚甲基或亚乙基; L是选自 - （C 1 -C 4 -C 4）亚烷基 - ， - S - ， - CH（OH） - 或-O-的二价连接基团。 A是亚甲基，-S-，-O-或-NH-; 而其它取代基如权利要求中所定义。

5. 发明申请

WO2004009578A2 PENTACYCLIC OXEPINES AND DERIVATIVES THEREOF, COMPOSITIONS AND METHODS 审中-公开
标题翻译： PENTACYCLIC OXEPINES及其衍生物，其制备方法及含有它们的药物组合物
公开(公告)号：WO2004009578A2
公开(公告)日：2004-01-29
申请号：PCT/US2003/019561
申请日：2003-07-18
申请人： ELI LILLY AND COMPANY , HINKLIN, Ronald, Jay , WALLACE, Owen, Brendan
发明人： HINKLIN, Ronald, Jay , WALLACE, Owen, Brendan
IPC分类号： C07D313/00
CPC分类号： C07D409/10 , C07D313/06 , C07D313/10 , C07D333/56 , C07D495/04
摘要： The present invention provides a compound of the formula (I) wherein R 1 is -H, -OH, -O(C 1 -C 4 alkyl), -OCOC 6 H 5 , -OCO(C 1 -C 6 alkyl), or -OSO 2 (C 2 -C 6 alkyl); R 0 , R 2 and R 3 are each independently -H, -OH, -O(C 1 -C 4 alkyl), -OCOC 6 H 5 , -OCO(C 1 -C 6 alkyl), -OSO 2 (C 2 -C 6 alkyl) or halo; R 4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is -S- or -HC=CH-; G is -O-, -S-, -SO-, SO 2 , or -N(R 5 )-, wherein R 5 is -H or C 1 -C 4 alkyl; and Y is -O-, -S-, -NH-, -NMe-, or -CH 2 -; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
摘要翻译：本发明提供式（I）化合物，其中R 1是-H，-OH，-O（C 1 -C 4烷基），-OCOC 6 H 5，-OCO（C 1 -C 6烷基）或-OSO 2（C 2 -C 1-6烷基）; R 0，R 2和R 3各自独立地为-H，-OH，-O（C 1 -C 4烷基），-OCOC 6 H 5，-OCO（C 1 -C 6烷基），-OSO 2（C 2 -C 6 烷基）或卤素; R 4是1-哌啶基，1-吡咯烷基，甲基-1-吡咯烷基，二甲基-1-吡咯烷基，4-吗啉代，二甲基氨基，二乙基氨基，二异丙基氨基或1-六亚甲基亚氨基; n为2或3，X为-S-或-HC = CH-; G是-O - ， - S - ， - SO-，SO 2或-N（R 5） - ，其中R 5是-H或C 1 -C 4烷基; 且Y为-O - ， - S - ， - NH - ， - MeMe - 或-CH 2 - ; 或其药学上可接受的盐; 其药物组合物，任选与雌激素和孕激素组合; 抑制与雌激素剥夺有关的疾病的方法; 以及用于抑制与内源性雌激素异常生理反应相关的疾病的方法。

6. 发明申请

WO2005073204A1 SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS 审中-公开
标题翻译：用于治疗VASOMOTOR症状的选择性雌激素受体调节剂
公开(公告)号：WO2005073204A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/000020
申请日：2005-01-18
申请人： ELI LILLY AND COMPANY , DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan
发明人： DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan
IPC分类号： C07D295/08
CPC分类号： C07D295/088 , C07D221/18 , C07D311/78 , C07D335/04
摘要： The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
摘要翻译：本发明涉及式I或Ia的选择性雌激素受体调节剂：（I）（Ia）; 或其药用酸加成盐; 可用于治疗血管舒缩症状，特别是潮热，盗汗等影响更年期周围妇女的症状。

7. 发明申请

WO2005073190A1 SELECTIVE ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性雌激素受体调节剂
公开(公告)号：WO2005073190A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/000018
申请日：2005-01-18
申请人： ELI LILLY AND COMPANY , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , WALLACE, Owen, Brendon
发明人： DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , WALLACE, Owen, Brendon
IPC分类号： C07D209/32
CPC分类号： C07D209/14 , C07D295/084 , C07D311/58 , C07D311/60 , C07D333/64
摘要： The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.
摘要翻译：本发明涉及选自以下的选择性雌激素受体调节剂：（I）或其药用盐; 有用的，例如用于治疗子宫内膜异位和子宫平滑肌瘤。

8. 发明申请

WO2010036497A2 SELECTIVE ESTROGEN RECEPTOR MODULATOR 审中-公开
标题翻译：选择性雌激素受体调节剂
公开(公告)号：WO2010036497A2
公开(公告)日：2010-04-01
申请号：PCT/US2009/055805
申请日：2009-09-03
申请人： ELI LILLY AND COMPANY , DODGE, Jeffrey, Alan , RICHARDSON, Timothy, Ivo , CLARKE, Christian, Alexander , JONES, Scott, Alan , HINKLIN, Ronald, Jay , HUMMEL, Conrad, Wilson , LEWIS, George, Sal
发明人： DODGE, Jeffrey, Alan , RICHARDSON, Timothy, Ivo , CLARKE, Christian, Alexander , JONES, Scott, Alan , HINKLIN, Ronald, Jay , HUMMEL, Conrad, Wilson , LEWIS, George, Sal
IPC分类号： A61K31/4535 , C07D409/02
CPC分类号： C07D333/08 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38
摘要： The present invention is directed to a compound of the formula (A): or a pharmaceutically acceptable salt thereof; and also to compounds of formula (I): or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（A）的化合物或其药学上可接受的盐; 以及式（I）化合物或其药学上可接受的盐。

9. 发明申请

WO2008118718A2 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS 审中-公开
标题翻译： 2-氨基吡啶类似物作为GLUCOKINASE激活剂
公开(公告)号：WO2008118718A2
公开(公告)日：2008-10-02
申请号：PCT/US2008/057543
申请日：2008-03-19
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, Jay , SINGH, Ajay
发明人： AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, Jay , SINGH, Ajay
IPC分类号： C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , A61P3/10 , A61K31/427 , A61K31/4427
CPC分类号： C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04
摘要： Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

10. 发明申请

WO2007117381A2 GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007117381A2
公开(公告)日：2007-10-18
申请号：PCT/US2007/007444
申请日：2007-03-23
申请人： ARRAY BIOPHARMA INC. , AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, Jay , SINGH, Ajay
发明人： AICHER, Thomas, Daniel , BOYD, Steven, Armen , CHICARELLI, Mark, Joseph , CONDROSKI, Kevin, Ronald , HINKLIN, Ronald, Jay , SINGH, Ajay
CPC分类号： C07D417/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
摘要翻译：提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

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