Propanobicyclic amine derivatives for CNS disorders
    21.
    发明授权
    Propanobicyclic amine derivatives for CNS disorders 失效
    中枢神经系统疾病的丙酰胆碱胺衍生物

    公开(公告)号:US5098916A

    公开(公告)日:1992-03-24

    申请号:US501216

    申请日:1990-03-29

    Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.17 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R.sup.3, R.sup.4, ring-position two, ring-position three and ring-position four; or the pharmaceutically-acceptable salts thereof.

    Methods ad compositions of (-) ketoconazole for treating fungal yeast
and dermatophyte infections
    23.
    发明授权
    Methods ad compositions of (-) ketoconazole for treating fungal yeast and dermatophyte infections 失效
    ( - )酮康唑用于治疗真菌酵母和皮肤癣菌感染的方法和组成

    公开(公告)号:US6040307A

    公开(公告)日:2000-03-21

    申请号:US314229

    申请日:1999-05-18

    CPC classification number: A61K31/495

    Abstract: Methods and compositions are disclosed utilizing the optically pure (-) isomer of ketoconazole. This compound is a potent drug for the treatment of local and systemic fungal, yeast, and dermatophyte infections, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ketoconazole.

    Abstract translation: 公开利用光学纯的( - )酮康唑异构体的方法和组合物。 该化合物是用于治疗局部和全身真菌,酵母和皮肤癣菌感染的有效药物,同时避免与酮康唑外消旋混合物相关的副作用的伴随责任。

    Methods and compositions for treating androgen-dependant diseases using
optically pure R-(-) casodex
    24.
    发明授权
    Methods and compositions for treating androgen-dependant diseases using optically pure R-(-) casodex 失效
    使用光学纯的R - ( - )casodex治疗雄激素依赖性疾病的方法和组合物

    公开(公告)号:US5985868A

    公开(公告)日:1999-11-16

    申请号:US107628

    申请日:1998-06-30

    Applicant: Nancy M. Gray

    Inventor: Nancy M. Gray

    CPC classification number: A61K31/277 A61K31/275 Y10S514/859

    Abstract: Methods and compositions are disclosed utilizing optically pure R-(-)-casodex for the treatment of androgen-dependent prostate cancer, while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of casodex. R-(-)-casodex is an antiandrogen and is therefore useful in the treatment of other conditions supported by androgen or caused by elevated androgen levels. Such conditions include benign prostatic hypertrophy or hyperplasia, acne and hirsutism.

    Abstract translation: 公开了使用光学纯的R - ( - ) - casodex用于治疗雄激素依赖性前列腺癌的方法和组合物,同时显着降低与casodex的外消旋混合物相关的副作用的伴随的责任。 R - ( - ) - casodex是一种抗雄激素,因此可用于治疗由雄激素支持或由升高的雄激素水平引起的其他病症。 这些病症包括良性前列腺肥大或增生,痤疮和多毛症。

    Nitrogen-containing cyclohetero cycloalkylaminoaryl derivatives for CNS
disorders
    25.
    发明授权
    Nitrogen-containing cyclohetero cycloalkylaminoaryl derivatives for CNS disorders 失效
    用于CNS疾病的含氮环杂环烷基氨基芳基衍生物

    公开(公告)号:US5739158A

    公开(公告)日:1998-04-14

    申请号:US877190

    申请日:1992-07-01

    CPC classification number: C07D295/135

    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

    Abstract translation: PCT No.PCT / US91 / 00688 Sec。 371日期:1992年7月1日 102(e)日期1992年7月1日PCT 1991年1月31日PCT PCT。 WO91 / 12247 PCT出版物 日期1991年8月22日描述了含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血,精神障碍,抽搐和帕金森综合征。 特别感兴趣的化合物具有式为四氟化烷基,四至六个碳原子的环烷基烷基和低级链烯基低级烷基; 其中R2和R3各自独立地选自氢和低级烷基; 其中R 4至R 7,R 10和R 11各自独立地选自氢,羟基,低级烷基,苄基,苯氧基,苄氧基和卤代低级烷基; 其中n是选自四至六的数字; 其中p是选自零至四的数字; 其中q是选自三至五的数; 其中A选自苯基,萘基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢,羟基,低级烷基,低级烷氧基,卤素,卤代低级烷基,氨基,单低级烷基氨基和二低级烷基氨基的取代基取代。 或其药学上可接受的盐。

    N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury
    26.
    发明授权
    N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury 失效
    用于治疗神经毒性损伤的N-(1-噻吩基环烷基)烯基胺

    公开(公告)号:US5604255A

    公开(公告)日:1997-02-18

    申请号:US344433

    申请日:1994-11-23

    CPC classification number: C07D409/06 C07D333/20

    Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein R.sup.1 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; wherein each of R.sup.2 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl, oxo and alkoxy; wherein R.sup.5 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; and wherein the broken line within the N-containing ring represents a double bond between any two adjacent carbon atoms

    Abstract translation: 描述了治疗的化合物,组合物和方法以控制与缺氧或缺血相关的脑损伤,其通常在中风,心脏骤停或围产期窒息之后。 治疗包括施用N-(1-噻吩基环烷基)链烯基胺化合物作为拮抗剂,以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。 最感兴趣的化合物是下式的化合物,其中R 1是一个或多个选自氢,烷基一至约五个碳原子,三至五个碳原子的环烷基,二至五个碳原子的烯基, 羟基和烷氧基; 其中R2各自为选自氢化物,1至约5个碳原子的烷基,3至约5个碳原子的环烷基,2至约5个碳原子的链烯基,羟基,氧代和烷氧基; 其中R5是一个或多个选自氢化的,一至五个碳原子的烷基,三个至五个碳原子的环烷基,二个至五个碳原子的烯基,羟基和烷氧基的基团; 并且其中所述含N环内的虚线表示任意两个相邻碳原子之间的双键

    Antipyretic and analgesic methods of using optically pure R-etodolac
    27.
    发明授权
    Antipyretic and analgesic methods of using optically pure R-etodolac 失效
    使用光学纯的R-乙哚乙酸的解热镇痛方法

    公开(公告)号:US5561151A

    公开(公告)日:1996-10-01

    申请号:US368735

    申请日:1995-01-04

    CPC classification number: A61K31/40

    Abstract: Methods are disclosed utilizing optically pure R(-) etodolac for the treatment of pain, including but not limited to pain associated with toothaches, headaches, sprains, joint pain and surgical pain, for example dental pain and ophthalmic pain, while substantially reducing adverse effects which are associated with the administration of the racemic mixture of etodolac. The optically pure R(-) etodolac is also useful in treating pyrexia while substantially reducing the adverse effects associated with the administration of the racemic mixture of etodolac.

    Abstract translation: 公开了利用光学纯的R( - )依托度酸治疗疼痛的方法,包括但不限于与牙痛,头痛,扭伤,关节疼痛和手术疼痛相关的疼痛,例如牙痛和眼痛,同时显着降低不良反应 其与依托度酸的外消旋混合物的施用相关联。 光学纯的R( - )依托度酸也可用于治疗发热,同时显着减少与依托度酸的外消旋混合物的施用相关的不利影响。

    Compositions containing indole-2-carboxylate compounds for treatment of
CNS disorders
    30.
    发明授权
    Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders 失效
    含有吲哚-2-羧酸盐化合物的组合物,用于治疗中枢神经系统疾病

    公开(公告)号:US5229413A

    公开(公告)日:1993-07-20

    申请号:US830108

    申请日:1992-02-03

    CPC classification number: A61K31/405

    Abstract: Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.

    Abstract translation: 含有某些吲哚-2-羧酸酯化合物和衍生物的组合物被描述为治疗由神经毒性损伤或神经变性疾病,特别是由缺血事件引起的CNS障碍引起的CNS障碍的治疗有效性。 优选的化合物具有式“IMAGE”,其中R 5和R 6各自独立地选自氢,溴,氯和氟,并且其中R 10和R 12各自独立地选自氢和低级烷基及其药学上可接受的盐。

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