Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
    26.
    发明授权
    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
    环戊烷庚(烯)酸,2-杂芳基烯基衍生物作为治疗剂

    公开(公告)号:US07183310B2

    公开(公告)日:2007-02-27

    申请号:US10915933

    申请日:2004-08-10

    IPC分类号: A61K31/38 C07D333/16

    CPC分类号: C07D333/28

    摘要: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

    摘要翻译: 公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。 本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐,四唑或前药,所述衍生物在此详细描述。 本文还公开了治疗疾病或病症的方法,包括青光眼和眼内压升高。 还公开了与其相关的药物制备的组合物和方法。

    Ocular treatment using cyclosporin-A derivatives
    28.
    发明授权
    Ocular treatment using cyclosporin-A derivatives 有权
    使用环孢菌素A衍生物进行眼部治疗

    公开(公告)号:US06350442B2

    公开(公告)日:2002-02-26

    申请号:US09870256

    申请日:2001-05-30

    申请人: Michael E. Garst

    发明人: Michael E. Garst

    IPC分类号: A61K3174

    CPC分类号: A61K38/13 A61K9/0048

    摘要: A method of treating a disorder in an eye, for example, an aqueous deficient dry eye state, phacoanaphylactic endophthalmitis, or uveitis, is provided. The method generally includes administering a therapeutically effective amount of a certain cyclosporin A derivative topically to the affected eye. The derivative may be administered as a solution, suspension or ointment in a pharmaceutically acceptable excipient.

    摘要翻译: 提供了治疗眼睛疾病的方法,例如水性缺血性干眼症,超声乳内镜眼内炎或葡萄膜炎。 该方法通常包括向受影响的眼部局部施用治疗有效量的某种环孢菌素A衍生物。 衍生物可以作为药学上可接受的赋形剂中的溶液,悬浮液或软膏施用。

    Combinations of prostaglandins and brimonidine or derivatives thereof
    29.
    发明授权
    Combinations of prostaglandins and brimonidine or derivatives thereof 有权
    前列腺素和溴莫尼定或其衍生物的组合

    公开(公告)号:US06294563B1

    公开(公告)日:2001-09-25

    申请号:US09440379

    申请日:1999-11-15

    申请人: Michael E. Garst

    发明人: Michael E. Garst

    IPC分类号: A61K31415

    摘要: The invention concerns combinations of alpha adrenergic agents such as brimonidine and its derivatives as represented by formula (I) below wherein each Y is independently selected from the group consisting of N, N—CH3, O, S and C—R1; R1 is hydrogen, lower alkyl or oxo; R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, lower alkyl and lower alkenyl; n is an integer from 1 to 3; and a broken line beside a solid line indicates either a single or a double bond with the proviso that when n=1, both bonds from Y to C—R1 cannot be double bonds, and prostaglandins known in the art to cause lowering of intraocular pressure which are useful in compositions, methods of treatment and articles of manufacture for the treatment of glaucoma and alleviation of elevated intraocular pressure and providing neuroprotection.

    摘要翻译: 本发明涉及α型肾上腺素能药物的组合,例如由下式(I)表示的溴莫尼定及其衍生物,其中每个Y独立地选自N,N-CH 3,O,S和C-R 1; R1是氢,低级烷基或氧代; R2,R3和R4独立地选自氢,卤素,低级烷基和低级烯基; n为1〜3的整数, 而实线旁边的虚线表示单键或双键,条件是当n = 1时,Y到C-R1的两个键都不能是双键,而本领域已知的引起眼压降低的前列腺素 可用于治疗青光眼的组合物,治疗方法和制品,并且降低眼内压升高并提供神经保护作用。

    Prodrugs of proton pump inhibitors
    30.
    发明授权
    Prodrugs of proton pump inhibitors 失效
    质子泵抑制剂的前药

    公开(公告)号:US6093734A

    公开(公告)日:2000-07-25

    申请号:US131481

    申请日:1998-08-10

    摘要: Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable sulfinyl or arylsulfonyl group attached to the benzimidazole nitrogen, or include a group that forms a Mannich base with the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.

    摘要翻译: 吡啶基甲基亚磺酰基苯并咪唑型质子泵抑制剂药物的前药具有与苯并咪唑氮连接的可水解亚磺酰基或芳基磺酰基,或包括与苯并咪唑氮形成曼尼希碱的基团。 本发明的前药在生理条件下水解以提供质子泵抑制剂,其半衰期可在几小时内测量,并且能够提供质子泵抑制剂药物的持续血浆浓度比目前使用的药物更长时间。 在生理条件下从本发明前药产生的质子泵抑制剂药物可以更有效地治疗由胃酸分泌引起的几种疾病和病症。