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    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
    1.
    发明授权
    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
    使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法

    公开(公告)号：US5418234A

    公开(公告)日：1995-05-23

    申请号：US298494

    申请日：1994-08-30

    申请人： Charles Gluchowski ,  Michael E. Garst ,  James A. Burke ,  Larry A. Wheeler ,  Michael E. Garst

    发明人： Charles Gluchowski ,  Michael E. Garst ,  James A. Burke ,  Larry A. Wheeler ,  Michael E. Garst

    IPC分类号： A61K31/495 ,  C07D403/12 ,  A61K31/50

    CPC分类号： C07D403/12 ,  A61K31/495 ,  Y10S514/816 ,  Y10S514/854 ,  Y10S514/93

    摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8-positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain and reduction in or prevention of at least one effect of ischemia.

    摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供所需治疗效果，所述化合物选自下列化合物：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物， 其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-，6-或7-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个，并且独立地选自Cl，Br，H和具有1至 3个碳原子。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛和减少或预防至少一种局部缺血的作用。

    Cyclosporin derivatives for treating ocular and dermal diseases and conditions
    3.
    发明授权
    Cyclosporin derivatives for treating ocular and dermal diseases and conditions 有权
    用于治疗眼部和皮肤疾病和病症的环孢菌素衍生物

    公开(公告)号：US08716238B2

    公开(公告)日：2014-05-06

    申请号：US12499911

    申请日：2009-07-09

    申请人： Michael E. Garst

    发明人： Michael E. Garst

    IPC分类号： A61K38/13

    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 R is —N═C(NR3R4)(NR5R6) or —NR7[(NR3R4)C═NR5], i.e. guanidines or —N═C(R8)(NR9R10), i.e. amidines wherein R3-R10 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 3是-N = C（NR 3 R 4）（NR 5 R 6）或-NR 7 [（NR 3 R 4）C≡NR5]，即胍或-N = C（R 8）（NR 9 R 10） R 10是H，Alk，Ar或（CH 2）n Ar，其中Ar是芳基，n是1至13的整数，或者R 3和R 4或R 4和R 5或R 5和R 7或R 3和R 7或R 9和R 10， 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。

    Cyclosporin derivatives for treating inflammatory diseases and conditions
    5.
    发明授权
    Cyclosporin derivatives for treating inflammatory diseases and conditions 有权
    用于治疗炎性疾病和病症的环孢菌素衍生物

    公开(公告)号：US08524671B2

    公开(公告)日：2013-09-03

    申请号：US12785133

    申请日：2010-05-21

    申请人： Michael E. Garst ,  Michael E. Stern

    发明人： Michael E. Garst ,  Michael E. Stern

    IPC分类号： A61K38/13

    CPC分类号： C07K7/645 ,  A61K38/13

    摘要： The present invention provides a method for the treatment of inflammatory diseases and/or conditions, e.g. allergic conjunctivitis, uveitis or phacoanaphylactic endophthalmitis in an eye of a mammal, said method comprising administering to said mammal in need of treatment 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, or a polyalkenylene linkage, e.g. a C3 to C6 alkenylenyl linkage and R is a hydrogen or a unsubstituted or substituted hydrocarbyl group.

    摘要翻译： 本发明提供了治疗炎性疾病和/或病症的方法，例如， 过敏性结膜炎，葡萄膜炎或哺乳动物眼中的眼内炎眼内炎，所述方法包括向需要治疗的所述哺乳动物施用治疗有效量的新型环孢菌素A衍生物，其选自由下式表示的化合物：其中R1为 S-Alk-R其中Alk是亚烷基键，优选亚甲基或聚亚甲基键，或聚亚烯基键，例如 C3至C6链烯基，R为氢或未取代或取代的烃基。