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1. 发明授权

US08853409B2 Pyridin-2yl-amino-1, 2, 4-thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus 有权
标题翻译：吡啶-2-基 - 氨基-1,2,4-噻二唑衍生物作为葡萄糖激酶活化剂用于治疗糖尿病
公开(公告)号：US08853409B2
公开(公告)日：2014-10-07
申请号：US13493616
申请日：2012-06-11
申请人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Jay Bradford Fell , John P. Fischer , Indrani W. Gunawardana , Ronald Jay Hinklin , Ajay Singh , Timothy M. Turner , Eli M. Wallace
发明人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Jay Bradford Fell , John P. Fischer , Indrani W. Gunawardana , Ronald Jay Hinklin , Ajay Singh , Timothy M. Turner , Eli M. Wallace
IPC分类号： A61K31/44 , C07D417/00 , C07D417/14 , C07D417/12 , C07D213/75
CPC分类号： C07D401/14 , C07D213/75 , C07D401/12 , C07D417/12 , C07D417/14
摘要： Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
摘要翻译：提供式（I）的化合物：其中R2，R3，R13，L和D2如说明书中所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可以通过激活葡糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损））以及其它疾病和病症如本文讨论的疾病和病症。

2. 发明授权

US08431713B2 2-aminopyridine derivatives as glucokinase activators 有权
标题翻译： 2-氨基吡啶衍生物作为葡糖激酶活化剂
公开(公告)号：US08431713B2
公开(公告)日：2013-04-30
申请号：US12524327
申请日：2008-01-16
申请人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Rustam Ferdinand Garrey , Ronald Jay Hinklin , Ajay Singh , Timothy M. Turner
发明人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Rustam Ferdinand Garrey , Ronald Jay Hinklin , Ajay Singh , Timothy M. Turner
IPC分类号： A61K31/44 , C07D213/55
CPC分类号： C07D495/04 , C07D417/14
摘要： Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, 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：提供具有式I的化合物或其盐，其中R2，L，R3，R11，D2和R13如本文所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病，例如糖尿病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。

3. 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。

4. 发明申请

US20110281874A1 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS 有权
标题翻译： 2-氨基吡啶类似物作为GLUCOKINASE激活剂
公开(公告)号：US20110281874A1
公开(公告)日：2011-11-17
申请号：US13191994
申请日：2011-07-27
申请人： Thomas D. AICHER , Steven Armen BOYD , Mark Joseph CHICARELLI , Kevin Ronald CONDROSKI , Ronald Jay HINKLIN , Ajay SINGH
发明人： Thomas D. AICHER , Steven Armen BOYD , Mark Joseph CHICARELLI , Kevin Ronald CONDROSKI , Ronald Jay HINKLIN , Ajay SINGH
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/519 , A61K31/506 , A61K31/437 , A61P3/10 , A61K31/4439 , C07D495/04 , C07D471/04 , C07D417/14 , C07D498/04 , C07D417/12 , A61K31/496 , A61K31/4545
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。

5. 发明申请

US20100105659A1 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS 失效
标题翻译： 2-氨基吡啶类似物作为GLUCOKINASE激活剂
公开(公告)号：US20100105659A1
公开(公告)日：2010-04-29
申请号：US12532374
申请日：2008-03-19
申请人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Ronald Jay Hinklin , Ajay Singh
发明人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Ronald Jay Hinklin , Ajay Singh
IPC分类号： A61K31/55 , C07D403/14 , A61K31/4545 , C07D495/02 , A61K31/4365 , C07D471/02 , A61K31/4355 , C07D239/02 , A61K31/506 , A61K31/519 , C07D215/16 , A61K31/47 , C07D401/02 , A61K31/439 , C07D401/14 , A61P3/00
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。

6. 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。

7. 发明申请

US20130158009A1 PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS 失效
标题翻译：作为GPR119调节剂的哌啶取代的LACTAMS
公开(公告)号：US20130158009A1
公开(公告)日：2013-06-20
申请号：US13698257
申请日：2011-05-13
申请人： Thomas Daniel Aicher , Josef Roland Bencsik , Kevin Ronald Condroski , Jay Bradford Fell , John P. Fischer , Ronald Jay Hinklin , Scott Alan Pratt , Ajay Singh , Timothy M. Turner , Steven Armen Boyd
发明人： Thomas Daniel Aicher , Josef Roland Bencsik , Kevin Ronald Condroski , Jay Bradford Fell , John P. Fischer , Ronald Jay Hinklin , Scott Alan Pratt , Ajay Singh , Timothy M. Turner , Steven Armen Boyd
IPC分类号： C07D413/14 , C07D405/14 , C07D401/14
CPC分类号： C07D413/14 , C07D401/14 , C07D405/14
摘要： Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
摘要翻译：其中X1，X2，L，R3，R4，R5，R6，R6a，R7，R9，R9a和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂并且可用于治疗或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。

8. 发明授权

US08362037B2 2-aminopyridine analogs as glucokinase activators 失效
标题翻译： 2-氨基吡啶类似物作为葡糖激酶活化剂
公开(公告)号：US08362037B2
公开(公告)日：2013-01-29
申请号：US12532374
申请日：2008-03-19
申请人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Ronald Jay Hinklin , Ajay Singh
发明人： Thomas Daniel Aicher , Steven Armen Boyd , Mark Joseph Chicarelli , Kevin Ronald Condroski , Ronald Jay Hinklin , Ajay Singh
IPC分类号： A61K31/445 , C07D417/14
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。

9. 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。

10. 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。

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