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    CYCLOSPORIN DERIVATIVES FOR ENHANCING THE GROWTH OF HAIR
    91.
    发明申请
    CYCLOSPORIN DERIVATIVES FOR ENHANCING THE GROWTH OF HAIR 审中-公开
    CYCLOSPORIN衍生物，用于增强头发的生长

    公开(公告)号：US20100305047A1

    公开(公告)日：2010-12-02

    申请号：US12785158

    申请日：2010-05-21

    申请人： David F. Woodward ,  Michael E. Garst

    发明人： David F. Woodward ,  Michael E. Garst

    IPC分类号： A61K38/13 ,  A61P17/14

    CPC分类号： A61K38/13 ,  A61K9/0014 ,  A61K9/0017 ,  A61K9/06 ,  A61K9/08 ,  A61K9/10 ,  A61K9/107 ,  A61K9/12 ,  A61K9/124 ,  A61K9/143 ,  A61K47/02 ,  A61K47/06 ,  A61K47/10 ,  A61K47/22

    摘要： The present invention provides a method for the treatment of alopecia and/or enhancing hair growth in a patient, wherein said method comprises administering, preferably topically, to the skin, e.g. the scalp or the eyelid, a therapeutically effective amount of a 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 or alkylenyl linkage, R is a hydrogen or a unsubstituted or substituted hydrocarbyl group and R2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl substituted lower alkyl.

    摘要翻译： 本发明提供了一种治疗患者脱发和/或增强头发生长的方法，其中所述方法包括给皮肤施用，优选局部给予皮肤。 头皮或眼睑，治疗有效量的选自由下式表示的化合物的环孢菌素A衍生物：其中R1是S-Alk-R，其中Alk是亚烷基或亚烷基键，R是氢或 未取代或取代的烃基，R2选自羟基，低级烷基和羟基取代的低级烷基。

    4-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
    92.
    发明授权
    4-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists 有权
    作为α2肾上腺素能激动剂的4-（缩合环状甲基） - 咪唑-2-硫酮

    公开(公告)号：US07838545B2

    公开(公告)日：2010-11-23

    申请号：US12166964

    申请日：2008-07-02

    申请人： Todd M. Heidelbaugh ,  Ken Chow ,  Phong X. Nguyen ,  Daniel W. Gill ,  John E. Donello ,  Michael E. Garst ,  Larry A. Wheeler

    发明人： Todd M. Heidelbaugh ,  Ken Chow ,  Phong X. Nguyen ,  Daniel W. Gill ,  John E. Donello ,  Michael E. Garst ,  Larry A. Wheeler

    IPC分类号： A61K31/4174 ,  C07D233/42

    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 cardiovascular 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： 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开的几种化合物优选α2B和/或α2C肾上腺素能受体是优于α2A肾上腺素能受体的特异性或选择性的。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的化合物可用作哺乳动物（包括人）中用于治疗疾病的药物和/或缓解对α2肾上腺素能受体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。

    4-(Phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists
    94.
    发明授权
    4-(Phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists 失效
    作为特定α2肾上腺素能激动剂的4-（苯基甲基和取代的苯基甲基） - 咪唑-2-硫酮

    公开(公告)号：US07683089B1

    公开(公告)日：2010-03-23

    申请号：US11232341

    申请日：2005-09-20

    申请人： Todd M. Heidelbaugh ,  Ken Chow ,  Phong X. Nguyen ,  Daniel W. Gil ,  John E. Donello ,  Michael E. Garst ,  Larry A. Wheeler

    发明人： Todd M. Heidelbaugh ,  Ken Chow ,  Phong X. Nguyen ,  Daniel W. Gil ,  John E. Donello ,  Michael E. Garst ,  Larry A. Wheeler

    IPC分类号： A61K31/4164 ,  C07D233/30

    CPC分类号： C07D233/84

    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： 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开的几种化合物优选α2B和/或α2C肾上腺素能受体是优于α2A肾上腺素能受体的特异性或选择性的。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的化合物可用作哺乳动物（包括人）中用于治疗疾病的药物和/或缓解对α2肾上腺素能受体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。

    QUINOLYNYLMETHYLIMIDIZOLES AS THERAPEUTIC AGENTS
    95.
    发明申请
    QUINOLYNYLMETHYLIMIDIZOLES AS THERAPEUTIC AGENTS 审中-公开
    喹诺酮类药物作为治疗药物

    公开(公告)号：US20090286829A1

    公开(公告)日：2009-11-19

    申请号：US12436837

    申请日：2009-05-07

    申请人： Todd M. Heidelbaugh ,  Phong X. Nguyen ,  Ken Chow ,  Michael E. Garst

    发明人： Todd M. Heidelbaugh ,  Phong X. Nguyen ,  Ken Chow ,  Michael E. Garst

    IPC分类号： A61K31/4709 ,  A61P25/00

    CPC分类号： A61K31/4709

    摘要： Disclosed herein are methods for treating a disorder associated with selective subtype modulation of alpha 2B and alpha 2C adrenergic receptors. Such methods can be performed, for example, by administering to a subject in need thereof a pharmaceutical composition containing a therapeutically effective amount of at least one compound having the structure: Compositions and medicaments related thereto are also disclosed.

    摘要翻译： 本文公开了治疗与α2B和α2C肾上腺素能受体的选择性亚型调节相关的病症的方法。 这样的方法可以例如通过向有需要的受试者施用含有治疗有效量的至少一种具有以下结构的化合物的药物组合物：还公开了与其有关的组合物和药物。

    2,3,4-substituted cyclopentanones as therapeutic agents
    99.
    发明授权
    2,3,4-substituted cyclopentanones as therapeutic agents 有权
    2,3,4-取代环戊酮作为治疗剂

    公开(公告)号：US07101906B2

    公开(公告)日：2006-09-05

    申请号：US10991284

    申请日：2004-11-16

    申请人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst ,  Jeremiah H. Nguyen

    发明人： Yariv Donde ,  Robert M. Burk ,  Michael E. Garst ,  Jeremiah H. Nguyen

    IPC分类号： A61K31/881 ,  C07D333/56 ,  C07D333/62

    CPC分类号： C07D333/62 ,  C07C405/0025 ,  C07D333/56

    摘要： Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein a dashed line represents the presence or absence of a bond; Y is a carboxylic acid, sulfonic acid, or phosphonic acid functional group; or an amide or ester thereof comprising from 0 to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising from 0 to 12 carbon atoms; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2—CH═CH—(CH2)3—, or —CH2—C≡C—(CH2)3— wherein 1 or 2 carbons may be substituted with S or O; B is hydrogen, C1-6 hydrocarbyl, CN, CO2H, or —(CH2)mX(CH2)pH, wherein m is at least 1 and the sum of m and p is from 1 to 5; X is S or O; J is H, CH3, or CF3; D is a covalent bond, CH2, O, or S; and E is an aromatic heterobicyclic ring system which may have substituents comprising up to 6 non-hydrogen atoms each. Methods, compositions, and medicaments related thereto are also disclosed.

    摘要翻译： 本文公开了包含其药学上可接受的盐或其前药的化合物，其中虚线表示存在或不存在键; Y是羧酸，磺酸或膦酸官能团; 或其包含0至12个碳原子的酰胺或酯; 或Y是含有0至12个碳原子的羟甲基或其醚; 或Y为四唑基官能团; A是 - （CH 2 CH 2）6 - ，顺式-CH 2 -CH-CH-（CH 2 CH 2） ）3 - 或 - CH 2-C≡C-（CH 2）3 - 其中1或 2个碳可以被S或O取代; B是氢，C 1-6烃基，CN，CO 2 H或 - （CH 2 CH 2）m H 其中m至少为1，m和p之和为1至5; X是S或O; J是H，CH 3或CF 3; D是共价键，CH 2，O或S; 并且E是芳族杂双环系统，其可以具有各自包含多达6个非氢原子的取代基。 还公开了与之相关的方法，组合物和药物。

    Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2&agr; antagonists
    100.
    发明授权
    Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2&agr; antagonists 有权
    亚麻基7-氧杂双环[2.2.1]庚烷恶唑作为前列腺素F2α拮抗剂

    公开(公告)号：US06509364B2

    公开(公告)日：2003-01-21

    申请号：US10087547

    申请日：2002-02-28

    申请人： Robert M. Burk ,  Yariv Donde ,  Michael E. Garst

    发明人： Robert M. Burk ,  Yariv Donde ,  Michael E. Garst

    IPC分类号： C07D41310

    CPC分类号： C07D493/08

    摘要： The present invention provides novel compounds represented by the general formula I. and pharmaceutically acceptable salts thereof wherein m, n, X, R, R1 and R2 are as defined in the specification. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.

    摘要翻译： 本发明提供由通式I表示的新化合物及其药学上可接受的盐，其中m，n，X，R 1，R 2和R 2如说明书中所定义。 新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病 ，血小板聚集和血栓形成。