公开(公告)号：US20080097103A1

公开(公告)日：2008-04-24

申请号：US11873500

申请日：2007-10-17

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

IPC分类号： C07D233/84 ,  C07D401/02 ,  C07D405/06 ,  C07D409/02

CPC分类号： C07D233/84 ,  C07D233/70 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.

摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的心血管和/或镇静活性。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。 其中X为O的式1的化合物也具有它们没有或只有最小的心血管和/或镇静活性的有利特性，并且可用于治疗没有或仅有最小的心血管和/或镇静活性的疼痛和其它状况。

公开(公告)号：US20060069144A1

公开(公告)日：2006-03-30

申请号：US11232383

申请日：2005-09-20

申请人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello ,  Michael Garst ,  Larry Wheeler

发明人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello ,  Michael Garst ,  Larry Wheeler

IPC分类号： A61K31/4178 ,  A61K31/4166 ,  C07D405/02

CPC分类号： C07D405/06 ,  C07D233/84 ,  C07D401/06 ,  C07D409/06 ,  C07D417/06

摘要： Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

摘要翻译： 式1的化合物

公开(公告)号：US20060069142A1

公开(公告)日：2006-03-30

申请号：US11232287

申请日：2005-09-20

申请人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello ,  Michael Garst ,  Larry Wheeler ,  John Cappiello

发明人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello ,  Michael Garst ,  Larry Wheeler ,  John Cappiello

IPC分类号： A61K31/4166 ,  C07D233/84

CPC分类号： A61K31/4166 ,  C07D233/84

摘要： Compounds of Formula 1 where the variables have the meaning defined in the specification are used to activate alpha2 adrenergic receptors. The compounds of Formula 1 are incorporated in pharmaceutical compositions and are used as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors.

摘要翻译： 式1的化合物

公开(公告)号：US20060149072A1

公开(公告)日：2006-07-06

申请号：US11371612

申请日：2006-03-09

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler ,  Phong Nguyen ,  Dario Gomez

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler ,  Phong Nguyen ,  Dario Gomez

IPC分类号： C07D409/02 ,  C07D403/02

CPC分类号： C07D401/06 ,  C07D233/70 ,  C07D233/84 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。 其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

公开(公告)号：US20060069143A1

公开(公告)日：2006-03-30

申请号：US11232323

申请日：2005-09-20

申请人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello ,  Michael Garst ,  Larry Wheeler

发明人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello ,  Michael Garst ,  Larry Wheeler

IPC分类号： A61K31/4178 ,  C07D403/02 ,  C07D405/02

CPC分类号： C07D471/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

摘要： Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

摘要翻译： 式1的化合物

公开(公告)号：US20080091028A1

公开(公告)日：2008-04-17

申请号：US11873537

申请日：2007-10-17

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

IPC分类号： C07D215/12 ,  C07D215/02 ,  C07D215/22 ,  C07D233/06 ,  C07D233/30

CPC分类号： C07D233/84 ,  C07D233/70 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。 其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

公开(公告)号：US20050267186A1

公开(公告)日：2005-12-01

申请号：US11143334

申请日：2005-06-02

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler ,  Phong Nguyen ,  Dario Gomez

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler ,  Phong Nguyen ,  Dario Gomez

IPC分类号： A61K31/4164 ,  A61K31/4166 ,  A61K31/4178 ,  A61K31/4709 ,  A61P1/04 ,  A61P1/12 ,  A61P9/02 ,  A61P9/04 ,  A61P9/12 ,  A61P13/02 ,  A61P19/02 ,  A61P19/06 ,  A61P21/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P27/16 ,  A61P37/06 ,  C07D233/70 ,  C07D233/84 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08 ,  C07D233/66

CPC分类号： C07D401/06 ,  C07D233/70 ,  C07D233/84 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗对α2B2肾上腺素能受体的激动剂治疗有反应的疾病和/或缓解的病症。 其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

公开(公告)号：US20070072926A1

公开(公告)日：2007-03-29

申请号：US11555831

申请日：2006-11-02

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

IPC分类号： A61K31/4166

CPC分类号： C07D233/84 ,  C07D233/70 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。 其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

公开(公告)号：US20060148872A1

公开(公告)日：2006-07-06

申请号：US11368990

申请日：2006-03-06

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry Wheeler

IPC分类号： A61K31/4166 ,  C07D233/70

CPC分类号： C07D233/70 ,  A61K9/0019 ,  A61K31/4164 ,  C07D233/84 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed.

摘要翻译： 本文公开了下式的化合物或其药学上可接受的盐。 还公开了与其相关的方法和组合物。

公开(公告)号：US07345077B2

公开(公告)日：2008-03-18

申请号：US11143334

申请日：2005-06-02

申请人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry A. Wheeler ,  Phong X. Nguyen ,  Dario G. Gomez

发明人： Ken Chow ,  Todd Heidelbaugh ,  Daniel Gil ,  Michael Garst ,  Larry A. Wheeler ,  Phong X. Nguyen ,  Dario G. Gomez

IPC分类号： A61K31/4164 ,  C07D233/30

CPC分类号： C07D401/06 ,  C07D233/70 ,  C07D233/84 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08

摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

摘要翻译： 式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。 式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗对α2B2肾上腺素能受体的激动剂治疗有反应的疾病和/或缓解的病症。 其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。