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1. 发明申请

WO2006036497A3 4-(CONDENSED CYCLICMETHYL)-IMIDAZOLE-2-THIONES ACTING AS ALPHA2 ADRENERGIC AGONISTS 审中-公开
标题翻译： 4-（CONDENSED CYCLICMETHYL）-IMIDAZOLE-2-THEION作为ALPHA2 ADRENERGIC AGONISTS
公开(公告)号：WO2006036497A3
公开(公告)日：2006-05-04
申请号：PCT/US2005032023
申请日：2005-09-07
申请人： ALLERGAN INC , HEIDELBAUGH TODD M , CHOW KEN , NGUYEN PHONG X , GIL DANIEL , DONELLO JOHN E , GARST MICHAEL E , WHEELER LARRY A
发明人： HEIDELBAUGH TODD M , CHOW KEN , NGUYEN PHONG X , GIL DANIEL , DONELLO JOHN E , GARST MICHAEL E , WHEELER LARRY A
IPC分类号： C07D405/06 , A61K31/4164 , A61K31/4178 , A61P29/02 , C07D233/84 , C07D401/06 , C07D409/06 , C07D417/06
CPC分类号： C07D405/06 , C07D233/84 , C07D401/06 , C07D409/06 , C07D417/06
摘要： Compounds of Formula 1 (I) where the variables have the meaning defined in the specification are agonists of alpha 2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha 2B and/or alpha 2C adrenergic receptors in preference over alpha 2A 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 alpha 2 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：变量具有本说明书中定义的含义的式1（I）化合物是α2肾上腺素能受体的激动剂。本公开内容的若干化合物优先于α2A2肾上腺素能受体是特异性或选择性的α2B2和/或α2C2N2肾上腺素能受体。另外一些所要求保护的化合物没有或只有最小的血管内和/或镇静作用。式1的化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或减轻对α2肾上腺素能受体的激动剂治疗有反应的病症。没有明显的心血管和/或镇静作用的式1化合物可用于治疗疼痛和其他具有最小副作用的病症。

2. 发明专利

JP2011079838A 4-SUBSTITUTED IMIDAZOLE-2-THIONES AND IMIDAZOL-2-ONES AS AGONISTS OF α-2B AND α-2C ADRENERGIC RECEPTORS 审中-公开
标题翻译： 4-取代的咪唑-2-酮和咪唑烷-2-酮作为α-2B和α-2C ADRENERGIC受体的激动剂
公开(公告)号：JP2011079838A
公开(公告)日：2011-04-21
申请号：JP2010249874
申请日：2010-11-08
申请人： Allergan Inc , アラーガン、インコーポレイテッドAllergan,Incorporated
发明人： CHOW KEN , HEIDELBAUGH TODD , GIL DANIEL , GARST MICHAEL , WHEELER LARRY A , NGUYEN PHONG X , GOMEZ DARIO G
IPC分类号： C07D233/84 , A61K31/4164 , A61K31/4166 , A61K31/4178 , A61K31/4709 , A61P1/04 , A61P1/12 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P19/02 , A61P19/06 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P27/06 , A61P27/16 , A61P37/02 , A61P37/06 , A61P43/00 , C07D233/70 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/08
CPC分类号： C07D401/06 , C07D233/70 , C07D233/84 , C07D405/06 , C07D409/06 , C07D409/08
摘要： PROBLEM TO BE SOLVED: To provide medicaments for treating pain and other conditions without accompanying cardiovascular and/or sedative activity. SOLUTION: There are provided compounds represented by formula (I) (wherein, X is S). The compounds of formula (I) 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 α 2B adrenergic receptors. Compounds of formula (I) where X is O are also useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedative activity. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供用于治疗疼痛和其他病症的药物，而不伴随心血管和/或镇静作用。提供由式（I）表示的化合物（其中X为S）。式（I）的化合物可用作哺乳动物（包括人）中用作治疗疾病和/或缓解对α2B2β肾上腺素能受体的激动剂治疗有反应的病症的药物。其中X为O的式（I）化合物也可用于治疗疼痛和其他没有或仅有最小心血管和/或镇静作用的病症。版权所有（C）2011，JPO＆INPIT

3. 发明专利

ES2396269T3 Compuestos adrenérgicos 未知
公开(公告)号：ES2396269T3
公开(公告)日：2013-02-20
申请号：ES08797844
申请日：2008-08-14
申请人： ALLERGAN INC
发明人： SINHA SANTOSH , BHAT SMITA , HEIDELBAUGH TODD , GIL DANIEL , CHOW KEN , GARST MICHAEL
IPC分类号： C07D401/12 , A61K31/435 , A61P29/00 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Un compuesto que tiene una estructura (I) o una sal farmacéuticamente aceptable, o un tautómero o un complejo no covalente del mismo; en el que X es O, S, o NH; y A es un sistema de anillos bicíclicos condensados que comprende: un resto de anillo alquilo C3-5 condensado con un anillo heteroaromático de seis miembros que tiene 1 o 2heteroátomos en el anillo independientemente seleccionados de N, O, o S; en el que el resto de anillo alquilo forma el enlace representado como A-N en la estructura, teniendo dicho resto deanillo alquilo 0 o 1 sustituyentes alquilo C1-4; y el anillo heteroaromático tiene de 0 a 3 sustituyentes que consisten independientemente en: de 0 a 4 átomos decarbono, de 0 a 10 átomos de hidrógeno, de 0 a 2 átomos de oxígeno, de 0 a 1 átomos de azufre, de 0 a 1 átomosde nitrógeno, de 0 a 3 átomos de flúor, de 0 a 1 átomos de cloro, y de 0 a 1 átomos de bromo, donde el compuestose selecciona del siguiente grupo de compuestos (II) y (III): o una sal farmacéuticamente aceptable, o un tautómero o un complejo no covalente del mismo; donde en la fórmula (II): Ra, Rb, y Rd son independientemente hidrógeno, o restos estables que consisten en: de 0 a4 átomos de carbono, de 0 a 10 átomos de hidrógeno, de 0 a 2 átomos de oxígeno, de 0 a 1 átomos de azufre, de 0a 1 átomos de nitrógeno, de 0 a 3 átomos de flúor, de 0 a 1 átomos de cloro, y de 0 a 1 átomos de bromo; y Rc es hidrógeno o alquilo C1-4.

4. 发明专利

ZA200409333B 4-substituted imidazole-2-thiones and imidazol-2-ones as agonists of the alpha-2B and alpha-2C adrenergic receptors. 未知
公开(公告)号：ZA200409333B
公开(公告)日：2005-05-19
申请号：ZA200409333
申请日：2004-11-19
申请人： ALLERGAN INC
发明人： CHOW KEN , HEIDELBAUGH TODD , GIL DANIEL , GARST MICHAEL , WHEELER LARRY A , NGUYEN PHONG X , GOMEZ DARIO G
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 , A61K , C07D
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.

5. 发明专利

AU2010201167A1 4-substituted imidazole-2-thiones and imidazol-2-ones as agonists of the alpha-2B and alpha-2C adrenergic receptors 未知
公开(公告)号：AU2010201167A1
公开(公告)日：2010-04-29
申请号：AU2010201167
申请日：2010-03-24
申请人： ALLERGAN INC
发明人： CHOW KEN , HEIDELBAUGH TODD , GIL DANIEL , GARST MICHAEL , WHEELER LARRY A , NGUYEN PHONG X , GOMEZ DARIO G
IPC分类号： C07D233/84 , 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 , C07D401/06 , 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.

6. 发明专利

AT429216T 未知
公开(公告)号：AT429216T
公开(公告)日：2009-05-15
申请号：AT03774642
申请日：2003-10-07
申请人： ALLERGAN INC
发明人： WHEELER LARRY , GIL DANIEL , DONELLO JOHN
IPC分类号： A61K31/17 , A61K31/00 , A61K31/137 , A61K31/4174 , A61P25/16 , A61P25/28
摘要： Methods of preventing or retarding the degeneration of neurons. Also disclosed are methods for treating Alzheimer's disease or Parkinson's disease through the administration of selective alpha 2B or alpha 2B/2C receptor agonists, hereby incorporated by reference herein.

7. 发明专利

ES2613509T3 Profármacos de ésteres de [3-(1-(1H-imidazol-4-il)etil)-2-metilfenil]metanol 未知
公开(公告)号：ES2613509T3
公开(公告)日：2017-05-24
申请号：ES11760963
申请日：2011-09-16
申请人： ALLERGAN INC
发明人： CHOW KEN , DIBAS MOHAMMED , DONELLO JOHN , GARST MICHAEL , GIL DANIEL , WANG LIMING
IPC分类号： A61K31/4174 , A61P17/04 , A61P27/06 , C07D233/64
摘要： Un compuesto seleccionado de entre los siguientes compuestos o una sal farmacéuticamente aceptable del mismo: 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido iso-butírico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 2,2-dimetil-propiónico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido acético; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido benzoico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 3-metil-butírico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 3-fenil-propiónico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 2-amino-3-metil-butírico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 2-(2-amino-3-metil-butirilamino)-3-metil-butírico; 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 2-(2-amino-acetilamino)-3-metil-butírico; y 3-[(S)-1-(1H-imidazol-4-il)-etil]-2-metil-bencil éster del ácido 2-amino-3-fenil-propiónico.

8. 发明专利

CA2486537C 4-(SUBSTITUTED CYCLOALKYLMETHYL)IMIDAZOLE-2-THIONES, 4-(SUBSTITUTED CYCLOALKENYLMETHYL)IMIDAZOLE-2-THIONES, 4-(SUBSTITUTED CYCLOALKYLMETHYL)IMIDAZOL-2-ONES AND 4-(SUBSTITUTED CYCLOALKENYLMETHYL)IMIDAZOL-2-ONES AND RELATED COMPOUNDS 未知
公开(公告)号：CA2486537C
公开(公告)日：2012-04-24
申请号：CA2486537
申请日：2003-05-16
申请人： ALLERGAN INC
发明人： CHOW KEN , HEIDELBAUGH TODD , GIL DANIEL , GARST MICHAEL , WHEELER LARRY A , NGUYEN PHONG X , GOMEZ DARIO G
IPC分类号： C07D233/84 , 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 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/08
摘要： Compounds of Formula (I): 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 (I) 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 (I) 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.

9. 发明专利

ES2376878T3 Uso de brimonidina para prevenir y reducir la severidad de afecciones asociadas al estres 未知
公开(公告)号：ES2376878T3
公开(公告)日：2012-03-20
申请号：ES04755981
申请日：2004-06-22
申请人： ALLERGAN INC
发明人： GIL DANIEL , WHITCUP SCOTT , BRIN MITCHELL , DONELLO JOHN
IPC分类号： A61K31/498 , A61P25/00
摘要： Brimonidina o una sal, tautómero, solvato, amida o N-óxido farmacéuticamente aceptable de la misma para su uso en la prevención o reducción de la severidad de hipersensibilidad sensorial asociada con una migraña por administración sistémica del compuesto.

10. 发明专利

AT539751T 未知
公开(公告)号：AT539751T
公开(公告)日：2012-01-15
申请号：AT04755981
申请日：2004-06-22
申请人： ALLERGAN INC
发明人： GIL DANIEL , WHITCUP SCOTT , BRIN MITCHELL , DONELLO JOHN
IPC分类号： A61K31/498 , A61P25/00
摘要： The present invention provides a method of reducing the severity of one or more symptoms of an inflammatory dermatological condition in a subject, comprising topically administering to the skin of a subject in need of such reduction an effective amount of brimonidine or a pharmaceutically acceptable salt, ester, amide, stereoisomer or racemic mixture thereof.

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