公开(公告)号：US20080221186A1

公开(公告)日：2008-09-11

申请号：US12070297

申请日：2008-02-16

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 ,  A61K31/4166 ,  A61P29/00 ,  A61P25/04 ,  A61P25/02 ,  A61P11/02 ,  A61P21/00

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 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：US20080103175A1

公开(公告)日：2008-05-01

申请号：US11969196

申请日：2008-01-03

申请人： Ken Chow ,  Todd Heidelbaugh ,  Phong Nguyen ,  Dale Harcourt

发明人： Ken Chow ,  Todd Heidelbaugh ,  Phong Nguyen ,  Dale Harcourt

IPC分类号： A61K31/47

CPC分类号： C07D401/06

摘要： A compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

摘要翻译： 本文公开了具有结构或其药学上可接受的盐或其前药的化合物。 还公开了与之相关的治疗方法，组合物和药物。

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：US20070004790A1

公开(公告)日：2007-01-04

申请号：US11458731

申请日：2006-07-20

申请人： Ken Chow ,  Todd Heidelbaugh ,  John Donello ,  Daniel Gil

发明人： Ken Chow ,  Todd Heidelbaugh ,  John Donello ,  Daniel Gil

IPC分类号： A61K31/4166 ,  C07D233/02

CPC分类号： A61K31/4164 ,  C07D233/84

摘要： The present invention provides an α-2A/α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. The present invention further provides a pharmaceutical composition that contains a pharmaceutical carrier and a therapeutically effective amount of an α-2A/α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof.

摘要翻译： 本发明提供α-2A /α-1A选择性激动剂，其包括由结构1表示的化合物或其药学上可接受的盐，酯，酰胺，消旋异构体或外消旋混合物。 本发明还提供了含有药物载体和治疗有效量的α-2A /α-1A选择性激动剂的药物组合物，其包括由结构1表示的化合物或其药学上可接受的盐，酯，酰胺，消旋异构体或外消旋 的混合物。

公开(公告)号：US20070004789A1

公开(公告)日：2007-01-04

申请号：US11172229

申请日：2005-06-29

申请人： Ken Chow ,  Todd Heidelbaugh ,  Phong Nguyen

发明人： Ken Chow ,  Todd Heidelbaugh ,  Phong Nguyen

IPC分类号： A61K31/4166 ,  C07D235/24

CPC分类号： C07D233/84

摘要： A compound is disclosed herein comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein R is OH or NH2. Methods, compositions, and medicaments related thereto are also disclosed.

摘要翻译： 本文公开的化合物包含其药学上可接受的盐或其前药; 其中R是OH或NH 2。 还公开了与之相关的方法，组合物和药物。

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：US20050075366A1

公开(公告)日：2005-04-07

申请号：US10950376

申请日：2004-09-24

申请人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello

发明人： Todd Heidelbaugh ,  Ken Chow ,  Phong Nguyen ,  Daniel Gil ,  John Donello

IPC分类号： C07D233/70 ,  C07D233/84 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/08 ,  A61K31/4709 ,  C07D43/02

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

摘要： The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and/or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.

摘要翻译： 下式的化合物，其中*表示不对称碳，优先于α2A和α2C肾上腺素能受体的α2B肾上腺素能受体特异性，因此没有或仅有最小的血管内和/或镇静作用。 该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α2B肾上腺素能受体激动剂治疗有反应的病症。

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。

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