公开(公告)号：US20090286791A1

公开(公告)日：2009-11-19

申请号：US12309493

申请日：2007-07-20

申请人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Tim Turner ,  Yoshihisa Nakada

发明人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Tim Turner ,  Yoshihisa Nakada

IPC分类号： A61K31/4155 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D231/14 ,  A61P3/04 ,  A61P3/10 ,  A61K31/4439 ,  A61K31/4184 ,  A61K31/498 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/506

CPC分类号： C07D401/12 ,  C07D207/08 ,  C07D213/81 ,  C07D233/90 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides compounds represented by the formula (Ia): the formula (Ib): the formula (Ic): and the formula (Id): wherein each symbol is as defined in the specification.According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.

摘要翻译： 本发明提供由式（Ia）表示的化合物：式（Ib）：式（Ic）：和式（Id）：其中每个符号如说明书中所定义。 根据本发明，这些化合物具有DGAT抑制活性，可用于预防，治疗或改善由高表达或高活化DGAT引起的疾病或病理。

公开(公告)号：US20120065196A1

公开(公告)日：2012-03-15

申请号：US12309480

申请日：2007-07-20

申请人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Yoshihisa Nakada

发明人： Shuji Kitamura ,  Thomas Daniel Aicher ,  Steve Gonzales ,  Yvan Le Huerou ,  Scott Alan Pratt ,  Yoshihisa Nakada

IPC分类号： A61K31/541 ,  A61K31/454 ,  A61K31/445 ,  C07D401/12 ,  C07D413/12 ,  A61K31/4245 ,  C07D513/00 ,  A61K31/428 ,  A61K31/497 ,  C07D403/12 ,  A61K31/5377 ,  C07D417/12 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  C07D401/06

CPC分类号： C07D401/12 ,  C07D231/14 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

摘要： The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification.According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.

摘要翻译： 本发明提供由式（Ie）表示的化合物：和式（If）：其中每个符号如说明书中所定义。 根据本发明，这些化合物具有DGAT抑制活性，可用于预防，治疗或改善由高表达或高活化DGAT引起的疾病或病理。

公开(公告)号：US07214673B2

公开(公告)日：2007-05-08

申请号：US10505805

申请日：2003-03-17

申请人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Joseph Herman Krushinski, Jr. ,  Yvan Le Huerou ,  Marta Maria Pineiro-Nunez ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Dennis Charles Thompson ,  David Edward Tupper ,  Ying Chen ,  Margaret Mary Faul ,  Vincent Patrick Rocco

发明人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Joseph Herman Krushinski, Jr. ,  Yvan Le Huerou ,  Marta Maria Pineiro-Nunez ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Dennis Charles Thompson ,  David Edward Tupper ,  Ying Chen ,  Margaret Mary Faul ,  Vincent Patrick Rocco

IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D243/10

CPC分类号： C07D487/04 ,  C07D243/38 ,  C07D495/04 ,  C07D513/04

摘要： Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl, wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl, wherein R7 is hydrogen, (C1-6) alkyl, fluorinated alkyl, or optionally substituted phenyl, R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorder, and pharmaceutical formulations of the compounds of formula (I).

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。

公开(公告)号：US08754226B2

公开(公告)日：2014-06-17

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 ,  David A. Mareska ,  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 ,  David A. Mareska ,  Steven Armen Boyd

IPC分类号： A01N43/40 ,  A61K31/445 ,  A61K31/44 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00

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。

公开(公告)号：US20130184257A1

公开(公告)日：2013-07-18

申请号：US13823041

申请日：2011-09-15

申请人： Thomas Daniel Aicher ,  Josef R. Bencsik ,  Steven Armen Boyd ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt

发明人： Thomas Daniel Aicher ,  Josef R. Bencsik ,  Steven Armen Boyd ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt

IPC分类号： C07D413/14 ,  C07D401/04 ,  C07D401/14 ,  C07D211/76

CPC分类号： C07D413/14 ,  A61K31/4468 ,  A61K31/454 ,  C07D211/76 ,  C07D401/04 ,  C07D401/14

摘要： Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R7 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，R7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，可用于治疗或预防疾病 例如但不限于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。

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。

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。

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。

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。