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1. 发明授权

US07713979B2 Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效
标题翻译：环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶1的抑制剂
公开(公告)号：US07713979B2
公开(公告)日：2010-05-11
申请号：US11718111
申请日：2005-10-26
申请人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , John Gordon Allen , Zhaogen Chen , Thomas Edward Mabry , Jefferson Ray McCowan , Nancy June Snyder , Leonard Larry Winneroski, Jr.
发明人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , John Gordon Allen , Zhaogen Chen , Thomas Edward Mabry , Jefferson Ray McCowan , Nancy June Snyder , Leonard Larry Winneroski, Jr.
IPC分类号： C07D207/00 , A61K31/40 , A61K31/497 , A61K31/445 , C07D211/06 , C07D403/00
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 Formula 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，以及式I和组合物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用途。

2. 发明申请

US20090023917A1 Selective Estrogen Receptor Modulators for the Treatment of Vasomotor Symptoms 审中-公开
标题翻译：选择性雌激素受体调节剂治疗血管舒缩症状
公开(公告)号：US20090023917A1
公开(公告)日：2009-01-22
申请号：US10597241
申请日：2005-01-18
申请人： Robert Dean Dally , Jeffrey Alan Dodge , Scott Alan Frank , Ronald Jay Hinklin , Timothy Alan Shepherd , Owen Brendan Wallace
发明人： Robert Dean Dally , Jeffrey Alan Dodge , Scott Alan Frank , Ronald Jay Hinklin , Timothy Alan Shepherd , Owen Brendan Wallace
IPC分类号： C07D223/04 , C07D211/22 , C07D405/12 , C07D409/12 , C07D401/12
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。

3. 发明申请

US20080214621A1 Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 审中-公开
标题翻译：环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶抑制剂1
公开(公告)号：US20080214621A1
公开(公告)日：2008-09-04
申请号：US11722090
申请日：2005-12-16
申请人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Cassandra A. Gauthier , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , Alexei Pavlovych Krasutsky , John Gordon Allen
发明人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Cassandra A. Gauthier , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , Alexei Pavlovych Krasutsky , John Gordon Allen
IPC分类号： A61K31/4439 , C07D207/02 , C07D211/74 , C07D401/10 , A61K31/4015 , A61K31/4412 , A61P3/10
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 G1 is methylene or ethylene; L is —(C1-C4)alkylene-, —S—, —CH(OH)—, or —O—; R0 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，含有这些化合物的本发明组合物用于治疗代谢综合征，糖尿病，高血糖肥胖症，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。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. 发明授权

US08217032B2 Selective estrogen receptor modulators for the treatment of vasomotor symptoms 有权
标题翻译：选择性雌激素受体调节剂用于治疗血管舒缩症状
公开(公告)号：US08217032B2
公开(公告)日：2012-07-10
申请号：US13167343
申请日：2011-06-23
申请人： Robert Dean Dally , Jeffrey Alan Dodge , Scott Alan Frank , Ronald Jay Hinklin , Timothy Alan Shepherd , Owen Brendan Wallace
发明人： Robert Dean Dally , Jeffrey Alan Dodge , Scott Alan Frank , Ronald Jay Hinklin , Timothy Alan Shepherd , Owen Brendan Wallace
IPC分类号： A61P15/12 , A61K31/4453 , A61K31/4523 , A61K31/55 , C07D295/08 , C07D311/78 , C07D335/04 , C07D221/18
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。

5. 发明授权

US07834194B2 Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效
标题翻译：环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶1的抑制剂
公开(公告)号：US07834194B2
公开(公告)日：2010-11-16
申请号：US11722101
申请日：2005-12-16
申请人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace
发明人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace
IPC分类号： C07D411/06 , A61K31/4025
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, R0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) 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）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。

6. 发明申请

US20090156571A1 BIPHENYL AMIDE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权
标题翻译：作为11-羟基脱氢酶脱氢酶1的抑制剂的二苯胺衍生物衍生物
公开(公告)号：US20090156571A1
公开(公告)日：2009-06-18
申请号：US12297349
申请日：2007-04-19
申请人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
发明人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/453 , C07D405/14 , C07D403/08 , C07D413/08 , C07D417/08 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/553
CPC分类号： C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention discloses novel compounds of Formula I: possessing 11 β-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 β-HSD type 1 activity.
摘要翻译：本发明公开了具有11个β-HSD 1型拮抗剂活性的新颖的式I化合物，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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍和与11β相关的其它病症的方法 -HSD类型1活动。

7. 发明授权

US08088776B2 Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权
标题翻译：联苯酰胺内酰胺衍生物作为11-β-羟基类固醇脱氢酶的抑制剂1
公开(公告)号：US08088776B2
公开(公告)日：2012-01-03
申请号：US12297349
申请日：2007-04-19
申请人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
发明人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/496 , A61K31/453 , C07D403/02 , C07D405/14
CPC分类号： C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention discloses novel compounds of Formula I: possessing 11 β-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 β-HSD type 1 activity.
摘要翻译：本发明公开了具有11＆amp; b -HSD 1型拮抗剂活性的式I化合物，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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍以及与其相关的其它病症的方法 ; -HSD 1型活动。

8. 发明授权

US07271264B2 Pentacyclic oxepines and derivatives thereof, compositions and methods 失效
标题翻译：五环氧基及其衍生物，组合物和方法
公开(公告)号：US07271264B2
公开(公告)日：2007-09-18
申请号：US10521998
申请日：2003-07-18
申请人： Ronald Jay Hinklin , Owen Brendan Wallace
发明人： Ronald Jay Hinklin , Owen Brendan Wallace
IPC分类号： C07D211/22 , C07D405/12 , C07D409/12
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 R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC═CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; 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）的化合物，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（C 2 -C 6烷基）;和（C 2 -C 6）烷基）。 R 0，R 2和R 3各自独立地为-H，-OH，-O（C 1 H 3） -C≡C4烷基），-OCOC 6 H 5，-OCO（C 1 -C 4烷基） 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; 和Y是-O - ， - S - ， - NH-，-NMe - 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。

9. 发明申请

US20110281847A1 SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS 有权
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：US20110281847A1
公开(公告)日：2011-11-17
申请号：US13167343
申请日：2011-06-23
申请人： Robert Dean Dally , Jeffrey Alan Dodge , Scott Alan Frank , Ronald Jay Hinklin , Timothy Alan Shepherd , Owen Brendan Wallace
发明人： Robert Dean Dally , Jeffrey Alan Dodge , Scott Alan Frank , Ronald Jay Hinklin , Timothy Alan Shepherd , Owen Brendan Wallace
IPC分类号： A61K31/55 , C07D211/22 , A61K31/4453 , C07D405/12 , A61P43/00 , A61K31/4545 , C07D401/12 , A61K31/4535 , C07D223/04 , C07D409/12 , A61K31/453
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。

10. 发明申请

US20080207691A1 Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 失效
标题翻译：环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶抑制剂1
公开(公告)号：US20080207691A1
公开(公告)日：2008-08-28
申请号：US11722101
申请日：2005-12-16
申请人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace
发明人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace
IPC分类号： A61K31/4535 , C07D409/06 , A61K31/4436 , A61K31/4025 , A61P3/08
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, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) 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。

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