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：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：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：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：US20050059721A1

公开(公告)日：2005-03-17

申请号：US10891953

申请日：2004-07-15

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： A61K31/4164 ,  A61P1/00 ,  A61P9/00 ,  C07D233/84

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：US20080070945A1

公开(公告)日：2008-03-20

申请号：US11858191

申请日：2007-09-20

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： A61K31/4709 ,  A61P21/00 ,  A61P25/28 ,  A61P27/06

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，优选α2 B 2肾上腺素能受体比α2A和α2 N 2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。 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α2B2肾上腺素能受体的激动剂治疗有反应的病症。

公开(公告)号：US20050058696A1

公开(公告)日：2005-03-17

申请号：US10881901

申请日：2004-06-30

申请人： John Donello ,  Daniel Gil

发明人： John Donello ,  Daniel Gil

IPC分类号： A61K9/00 ,  A61K31/135 ,  A61K31/4168 ,  A61K31/433 ,  A61K31/498 ,  A61K31/513 ,  A61K31/517 ,  A61K45/06 ,  A61K47/02 ,  A61K47/20 ,  A61K9/70 ,  A61K9/20

CPC分类号： A61K31/513 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K31/135 ,  A61K31/4168 ,  A61K31/433 ,  A61K31/498 ,  A61K31/517 ,  A61K45/06 ,  A61K47/02 ,  A61K47/20 ,  A61K2300/00

摘要： Methods and compositions for the treatment of pain and other conditions in a mammal using a composition which directly or indirectly stimulates alpha 2 adrenoreceptor agonist activity with a minimum of sedation or other side effects.

摘要翻译： 用于使用直接或间接刺激α2肾上腺素受体激动剂活性的组合物治疗哺乳动物疼痛和其它病症的方法和组合物，其具有最小的镇静作用或其它副作用。

公开(公告)号：US20050059664A1

公开(公告)日：2005-03-17

申请号：US10891740

申请日：2004-07-15

申请人： Daniel Gil ,  John Donello

发明人： Daniel Gil ,  John Donello

IPC分类号： A61K31/4164 ,  A61K31/498

CPC分类号： A61K31/4164 ,  A61K31/498

摘要： The present invention provides methods of preventing or alleviating sympathetically-enhanced conditions, neurological conditions, ocular conditions and chronic pain without concomitant sedation by peripherally administering to a subject an effective amount of an α-2A/α-1A selective agonist, thereby preventing or alleviating the condition or chronic pain without concomitant sedation, where the selective agonist has an α-1A efficacy less than that of brimonidine or a ratio of α-1A/α-2A potency greater than that of brimonidine.

摘要翻译： 本发明提供了通过向受试者周边施用有效量的α-2A /α-1A选择性激动剂来预防或减轻交感神经增强的病症，神经病症，眼部病症和慢性疼痛而不伴随镇静的方法，从而预防或减轻 该情况或慢性疼痛而没有伴随的镇静，其中选择性激动剂的α-1A功效小于溴莫尼定或α-1A /α-2A效力的比值大于溴莫尼定的效力。

公开(公告)号：US20050164992A1

公开(公告)日：2005-07-28

申请号：US11084454

申请日：2005-03-17

申请人： Yariv Donde ,  Jeremiah Nguyen ,  Karen Kedzie ,  Daniel Gil ,  John Donello ,  Wha-Bin Im

发明人： Yariv Donde ,  Jeremiah Nguyen ,  Karen Kedzie ,  Daniel Gil ,  John Donello ,  Wha-Bin Im

IPC分类号： A61K31/5575 ,  C07C405/00 ,  C07D333/56 ,  C07D333/62 ,  C07D409/08 ,  A61K31/557 ,  A61K31/66

CPC分类号： C07D333/56 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/559 ,  C07C57/26 ,  C07C57/48 ,  C07C59/90 ,  C07C69/732 ,  C07C69/738 ,  C07D333/62 ,  C07D409/08

摘要： Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.

摘要翻译： 本文公开了一种方法，其包括向患有炎症性肠病的哺乳动物施用化合物用于治疗所述疾病，所述化合物具有式I的结构，其中X，Y，B，R 2， R 3，R 4，R 5，R 6和n具有本文找到的含义。