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：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：US08212045B2

公开(公告)日：2012-07-03

申请号：US12678995

申请日：2008-09-15

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

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：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：US20100204240A1

公开(公告)日：2010-08-12

申请号：US12678995

申请日：2008-09-15

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. Tumer ,  Eli M. Wallce

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. Tumer ,  Eli M. Wallce

IPC分类号： A61K31/501 ,  C07D417/14 ,  A61K31/444 ,  C07D417/12 ,  A61K31/4439 ,  A61K31/4709 ,  C07D471/04 ,  A61K31/437 ,  A61K31/517 ,  C07D491/052 ,  A61K31/436 ,  A61P3/10

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：US20100099713A1

公开(公告)日：2010-04-22

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： A61K31/4439 ,  C07D417/12 ,  A61P3/10 ,  C07D417/14

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：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。

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。