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1. 发明申请

WO2014031581A1 PROCESS FOR THE SYNTHESIS OF SUBSTITUTED GAMMA LACTAMS 审中-公开
标题翻译：用于合成取代的游离乳杆菌的方法
公开(公告)号：WO2014031581A1
公开(公告)日：2014-02-27
申请号：PCT/US2013055685
申请日：2013-08-20
申请人： ALLERGAN INC , DINH DANNY T , GARST MICHAEL E , OLD DAVID W , SYAGE ELIZABETH T , GORIN BORIS I , LANTHIER CHRISTOPHER M , OUDENES JAN
发明人： DINH DANNY T , GARST MICHAEL E , OLD DAVID W , SYAGE ELIZABETH T , GORIN BORIS I , LANTHIER CHRISTOPHER M , OUDENES JAN
IPC分类号： C07D409/12
CPC分类号： C07D409/12 , H04N5/23229 , H04N5/23293
摘要： The present invention provides synthetic processes for the preparation of a variety of well-defined substituted gamma lactams. The compounds that can be prepared by the process of the invention are useful for treating a variety of conditions. In some embodiments of the invention, the compounds are useful for treating ocular disorders, such as, for example, glaucoma, lowering of elevated intraocular pressure, and the like. In other embodiments, the compounds are useful for treating irritable bowel disease. In further embodiments, the compounds are useful in promoting hair growth. In still further embodiments, the compounds are useful in promoting wound healing, scar reduction, and the like.
摘要翻译：本发明提供用于制备各种明确定义的取代的γ-内酰胺的合成方法。可以通过本发明的方法制备的化合物可用于治疗各种病症。在本发明的一些实施方案中，所述化合物可用于治疗眼部疾病，例如青光眼，降低眼内压升高等。在其它实施方案中，所述化合物可用于治疗肠易激综合征。在另外的实施方案中，这些化合物可用于促进毛发生长。在另外的实施方案中，所述化合物可用于促进伤口愈合，瘢痕减少等。

2. 发明申请

WO2006107598A2 AGENTS AND METHODS FOR ENHANCING PHOTODYNAMIC THERAPY 审中-公开
标题翻译：用于增强光动力治疗的药剂和方法
公开(公告)号：WO2006107598A2
公开(公告)日：2006-10-12
申请号：PCT/US2006010359
申请日：2006-03-22
申请人： ALLERGAN INC , BURKE JAMES A , SYAGE ELIZABETH T , GARST MICHAEL E , WHEELER LARRY A
发明人： BURKE JAMES A , SYAGE ELIZABETH T , GARST MICHAEL E , WHEELER LARRY A
IPC分类号： A61K41/00 , A61K47/48
CPC分类号： A61K41/0071 , A61K41/0057 , A61K47/543 , A61K47/61
摘要： A chemical conjugate for administration to a patient undergoing photodynamic therapy includes a photoactive compound coupled to a leakage reducing agent that is structured to reduce leakage of the photoactive compound from a patient ' s vasculature . The leakage reducing agent may be a bulking agent to sterically reduce the permeability of the photoactive compound through the blood vessel, or it may be a ligand that binds to endothelial cells of a patient's choriocapillaries . The conjugate may be used in methods of reducing secondary damage associated with photodynamic therapy.
摘要翻译：用于给予经历光动力疗法的患者的化学共轭物包括偶联到泄漏还原剂的光活性化合物，其被构造为减少光活性化合物从患者脉管系统的泄漏。渗漏还原剂可以是空间上降低光活性化合物通过血管的渗透性的填充剂，或者它可以是与患者绒毛膜毛细血管的内皮细胞结合的配体。缀合物可用于减少与光动力疗法相关的次级损伤的方法。

3. 发明申请

WO03074481A8 PREPARATION OF PROSTAMIDES 审中-公开
标题翻译：前列腺素的制备
公开(公告)号：WO03074481A8
公开(公告)日：2004-10-21
申请号：PCT/US0306071
申请日：2003-02-28
申请人： ALLERGAN INC , GARST MICHAEL E , OUDENES JAN , ANTCZAK CASIMIR GREGORY , MORTIMER RICHARD DONALD , LU YEE-FUNG , HOCHFELLNER BRIAN GEORGE , ARSENAULT EDWARD ARMAND , YEH WEN-LUNG
发明人： GARST MICHAEL E , OUDENES JAN , ANTCZAK CASIMIR GREGORY , MORTIMER RICHARD DONALD , LU YEE-FUNG , HOCHFELLNER BRIAN GEORGE , ARSENAULT EDWARD ARMAND , YEH WEN-LUNG
IPC分类号： C07C405/00
CPC分类号： C07C405/0041 , Y02P20/55
摘要： The present invention provides a process for the preparation of a prostamide which comprises the steps of (d) reacting first intermediate having the general formula (I) with DIBAL wherein Z is a protecting group and the dotted line represents the presence or absence of a double bond to yield a second intermediate having the general Formula (II) (b) reacting said second intermediate with Na(TMS)2N and (C6H5)3P (CH2)6CONR2X wherein R is a C1-5 alkyl or hydrogen and X is an anion to yield a third intermediate having the general formula (III) (c) reacting said third intermediate with a protecting agent to yield a fourth intermediate having the general formula IV (e) reacting said fourth intermediate to remove said protecting groups and yield a prostamide having the general formula V
摘要翻译：本发明提供了制备前列腺酰胺的方法，其包括以下步骤：（d）使具有通式（I）的第一中间体与DIBAL反应，其中Z是保护基，虚线表示存在或不存在双（II）（b）使所述第二中间体与Na（TMS）2 N和（C 6 H 5）3 P +（CH 2）6 CONR 2 X反应，其中R为C 1-5烷基或氢且X 是产生具有通式（III）的第三中间体的阴离子（c）使所述第三中间体与保护剂反应以产生具有通式IV的第四中间体（e）使所述第四中间体反应以除去所述保护基并产生具有通式V的前列腺酰胺

4. 发明申请

WO03074481A2 PREPARATION OF PROSTAMIDES 审中-公开
标题翻译： PROSTAMIDES的制备
公开(公告)号：WO03074481A2
公开(公告)日：2003-09-12
申请号：PCT/US0306071
申请日：2003-02-28
申请人： ALLERGAN INC , GARST MICHAEL E , OUDENES JAN , ANTCZAK CASIMIR GREGORY , MORTIMER RICHARD DONALD , LU YEE-FUNG
发明人： GARST MICHAEL E , OUDENES JAN , ANTCZAK CASIMIR GREGORY , MORTIMER RICHARD DONALD , LU YEE-FUNG , HOCHFELLNER BRIAN GEORGE , ARSENAULT EDWARD ARMAND , YEH WEN-LUNG
IPC分类号： C07C405/00
CPC分类号： C07C405/0041 , Y02P20/55
摘要： The present invention provides a process for the preparation of a prostamide which comprises the steps of (d) reacting first intermediate having the general formula (I) with DIBAL wherein Z is a protecting group and the dotted line represents the presence or absence of a double bond to yield a second intermediate having the general Formula (II) (b) reacting said second intermediate with Na(TMS)2N and (C6H5)3P+(CH2)6CONR2X wherein R is a C1-5 alkyl or hydrogen and X is an anion to yield a third intermediate having the general formula (III) (c) reacting said third intermediate with a protecting agent to yield a fourth intermediate having the general formula IV (e) reacting said fourth intermediate to remove said protecting groups and yield a prostamide having the general formula V
摘要翻译：本发明提供了一种制备前列腺酰胺的方法，其包括以下步骤：（d）使具有通式（I）的第一中间体与DIBAL反应，其中Z为保护基，虚线表示存在或不存在双键合以产生具有通式（II）的第二中间体（b）使所述第二中间体与Na（TMS）2N和（C6H5）3P +（CH2）6CONR2X反应，其中R是C1-5烷基或氢，X是阴离子以产生具有通式（III）的第三中间体（c）使所述第三中间体与保护剂反应，得到具有通式IV的第四中间体（e）使所述第四中间体反应以除去所述保护基团并产生具有通式V

5. 发明申请

WO2009089284A3 SUBSTITUTED 2-AMINOTETRALIN DERIVATIVES AS SELECTIVE ALPHA 2B AGONIST 审中-公开
标题翻译：取代的2-氨基嘌呤衍生物作为选择性ALPHA 2B AGONIST
公开(公告)号：WO2009089284A3
公开(公告)日：2009-10-15
申请号：PCT/US2009030337
申请日：2009-01-07
申请人： ALLERGAN INC , CAPPIELLO JOHN R , GOMEZ DARIO G , CHOW KEN , GARST MICHAEL E , GIL DANIEL W , WHEELER LARRY A
发明人： CAPPIELLO JOHN R , GOMEZ DARIO G , CHOW KEN , GARST MICHAEL E , GIL DANIEL W , WHEELER LARRY A
IPC分类号： C07D213/38 , A61K31/435 , A61P25/00 , A61P27/00
CPC分类号： C07D213/38
摘要： Substituted 2-aminotetralin derivatives as selective alpha 2B agonists includes a compound represented by Formula (I): wherein R1 = H, methyl, ethyl, propyl, or cyclobutyl; R2 = methyl or H; R3 = pyridinyl X= C or O. The compounds of Formula 1 can be incorporated in a pharmaceutical compositions and can be used in methods of treating an alpha 2B receptor mediated diseases or conditions.
摘要翻译：作为选择性α2B激动剂的取代的2-氨基四氢萘衍生物包括由式（I）表示的化合物：其中R1 = H，甲基，乙基，丙基或环丁基; R2 =甲基或H; R3 =吡啶基X = C或O.式1的化合物可以掺入药物组合物中，并且可以用于治疗α2B受体介导的疾病或病症的方法。

6. 发明申请

WO2007041048A2 SYNTHESIS OF IMIDAZOLE-2-THIONES VIA THIOHYDANTOINS 审中-公开
标题翻译：咪唑二酮合成咪唑-2-酮
公开(公告)号：WO2007041048A2
公开(公告)日：2007-04-12
申请号：PCT/US2006037181
申请日：2006-09-22
申请人： ALLERGAN INC , GARST MICHAEL E , DOLBY LLOYD J , ESDANDIARI SHERVIN , AVEY ALFRED ARTHUR , MAC KENZIE VIVIAN ROSE , MUCHMORE DAVID CHARLES
发明人： GARST MICHAEL E , DOLBY LLOYD J , ESDANDIARI SHERVIN , AVEY ALFRED ARTHUR , MAC KENZIE VIVIAN ROSE , MUCHMORE DAVID CHARLES
IPC分类号： C07D233/20
CPC分类号： C07D233/84
摘要： The present invention provides a method of making an imidazole 2-thione which comprises the step(s) of reducing a thiohydantoin to said imidazole- 2-thione.
摘要翻译：本发明提供了制备咪唑2-硫酮的方法，其包括将硫代乙内酰脲还原为所述咪唑-2-硫酮的步骤。

7. 发明申请

WO2010006117A3 CYCLOSPORIN DERIVATIVES FOR TREATING OCULAR AND DERMAL DISEASES AND CONDITIONS 审中-公开
标题翻译：用于治疗眼睛和眼睛疾病和病症的环磷酰胺衍生物
公开(公告)号：WO2010006117A3
公开(公告)日：2010-03-04
申请号：PCT/US2009050038
申请日：2009-07-09
申请人： ALLERGAN INC , GARST MICHAEL E
发明人： GARST MICHAEL E
IPC分类号： A61K9/00 , A61K38/13 , A61P27/00
CPC分类号： A61K38/13 , A61K9/0014 , A61K9/0048 , A61K38/00 , C07K7/645
摘要： The present invention provides a method for the treatment of ocular or dermal diseases and/or conditions, e.g. an aqueous deficient dry eye state, uveitis or phacoanaphylactic endophthalmitis in an eye, or balanitis, psoriasis, or atopic dermatitis of the skin, said method comprising administering, topically to the eye or the skin, a therapeutically effective amount of a novel cyclosporin A derivative selected from the group consisting of compounds represented by the formula: wherein R1 is S-Alk-R wherein Alk is an alkylene linkage, preferably a methylene or poly methylene linkage, e.g. a C2 to C6 polymethylene linkage, or a polyalkenylene linkage, e.g. a C3 to C6 alkenylenyl linkage, R is -N=C(NR3R4)(NR5R6) or -NR7[(NR3R4)C=NR5], i.e. guanidines or -N=C(R8)(NR9R10), i.e. amidines wherein R3-R7 10 is H, Alk, Ar or (CH2)nAr wherein Ar is an aryl group and n is an integer of from 1 to 13 or R3 and R4 or R4 and R5 or R5 and R7 or R3 and R7, or R9 and R10, together may be -CH2-CH2- or -CH2-CH2-CH2- and R2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl-substituted lower alkyl and R2 is selected from the group consisting of hydroxy and lower alkyl.
摘要翻译：本发明提供了用于治疗眼部或皮肤疾病和/或病症的方法，例如，所述方法包括向眼睛或皮肤局部施用治疗有效量的新型环孢菌素A衍生物，所述方法包括向所述眼睛或皮肤局部施用治疗有效量的新的环孢菌素A衍生物选自由下式表示的化合物：其中R 1是S-Alk-R，其中Alk是亚烷基键，优选亚甲基或聚亚甲基键，例如 C2-C6聚亚甲基连接，或聚亚烯基键，例如。 C 3 -C 6亚烯基键，R是-N = C（NR 3 R 4）（NR 5 R 6）或-NR 7 [（NR 3 R 4）C = NR 5]，即胍或-N = C（R 8）（NR 9 R 10） R710是H，Alk，Ar或（CH2）nAr，其中Ar是芳基，n是1至13的整数，R3或R4或R4和R5或R5和R7或R3和R7，或R9和R10 一起可以是-CH 2 -CH 2 - 或-CH 2 -CH 2 -CH 2 - ，并且R 2选自羟基，低级烷基和羟基取代的低级烷基，R 2选自羟基和低级烷基。

8. 发明申请

WO2013101911A3 BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT 审中-公开
标题翻译：苯并咪唑衍生物作为持续性钠电流的选择性阻隔剂
公开(公告)号：WO2013101911A3
公开(公告)日：2013-08-22
申请号：PCT/US2012071784
申请日：2012-12-27
申请人： ALLERGAN INC , EHRING GEORGE R , CHAO ELLEN , NG HERMAN , TON HAU , LI JIA CHIAN , ADORANTE JOSEPH S , GARST MICHAEL E , RIND HOWARD B , HANSEN MARK R , AVEY JR ALFRED A , DOLBY LLOYD J , ESFANDIARI SHERVIN , MACKENZIE VIVIAN R , MARSDEN JEREMIAH A , MUCHMORE DAVID C
发明人： EHRING GEORGE R , CHAO ELLEN , NG HERMAN , TON HAU , LI JIA CHIAN , ADORANTE JOSEPH S , GARST MICHAEL E , RIND HOWARD B , HANSEN MARK R , AVEY JR ALFRED A , DOLBY LLOYD J , ESFANDIARI SHERVIN , MACKENZIE VIVIAN R , MARSDEN JEREMIAH A , MUCHMORE DAVID C
IPC分类号： C07D235/06 , A61K31/4184 , A61P25/00 , A61P25/08 , A61P27/02 , A61P29/00 , C07D235/08 , C07D235/12 , C07D235/20 , C07D401/12 , C07D403/06
CPC分类号： C07D235/12 , C07D235/06 , C07D235/08 , C07D235/14 , C07D235/20 , C07D401/12 , C07D403/06 , C07D403/12
摘要： The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐; 其中R，R 1，R 2，R 3，R 4，m和n如本文所定义，包含所述化合物的药物组合物，以及治疗由升高的持续性钠电流介导的疾病或病症的方法，所述疾病或病症例如眼部病症，，癫痫症和慢性疼痛。

9. 发明申请

WO2006036512A2 UNSUBSTITUTED AND SUBSTITUTED 4-BENZYL-1,3-DIHYDRO-IMIDAZOLE-2-THIONES ACTING AS SPECIFIC OR SELECTIVE ALPHA2 ADRENERGIC AGONISTS AND METHODS FOR USING THE SAME 审中-公开
标题翻译：作为特异性或选择性ALPHA2 ADRENERGIC AGONISTS的不考虑和取代的4-苄氧基-1,3-二氢-1H-咪唑-2-酮及其使用方法
公开(公告)号：WO2006036512A2
公开(公告)日：2006-04-06
申请号：PCT/US2005032221
申请日：2005-09-07
申请人： ALLERGAN INC , HEIDELBAUGH TODD M , CHOW KEN , NGUYEN PHONG X , GIL DANIEL W , DONELLO JOHN E , GARST MICHAEL E , WHEELER LARRY A , CAPPIELLO JOHN R
发明人： HEIDELBAUGH TODD M , CHOW KEN , NGUYEN PHONG X , GIL DANIEL W , DONELLO JOHN E , GARST MICHAEL E , WHEELER LARRY A , CAPPIELLO JOHN R
IPC分类号： C07D233/84 , A61K31/4174 , A61P1/12 , A61P7/12 , A61P9/12 , A61P29/00 , A61P37/00
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 alpha 2 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 alpha 2 adrenergic receptors.
摘要翻译：变量具有本说明书中定义的含义的式1化合物用于活化α2肾上腺素能受体。式1的化合物掺入药物组合物中，并且用作哺乳动物（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。

10. 发明申请

WO2009152052A8 METHODS OF TREATING ALPHA ADRENERGIC MEDIATED CONDITIONS 审中-公开
标题翻译：治疗ALPHA ADRENERGIC MEDIATED条件的方法
公开(公告)号：WO2009152052A8
公开(公告)日：2010-11-11
申请号：PCT/US2009046432
申请日：2009-06-05
申请人： ALLERGAN INC , FANG WENKUI K , NGUYEN PHONG X , CHOW KEN , HEIDELBAUGH TODD M , GOMEZ DARIO G , GARST MICHAEL E , SINHA SANTOSH C
发明人： FANG WENKUI K , NGUYEN PHONG X , CHOW KEN , HEIDELBAUGH TODD M , GOMEZ DARIO G , GARST MICHAEL E , SINHA SANTOSH C
IPC分类号： A61K31/4168 , A61P9/12
CPC分类号： A61K31/4168
摘要： Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an a-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.
摘要翻译：本文描述了通过向受试者施用含有有效量的α-肾上腺素能调节剂的药物组合物来治疗受试者的病症或疾病的化合物和方法。化合物和方法也可用于缓解急性和慢性疼痛的类型。

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