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    • 1. 发明申请
    • 4-ARYL PIPERIDINES
    • WO2005069834A3
    • 2006-04-27
    • PCT/US2005001131
    • 2005-01-13
    • LUNDBECK & CO AS HMARZABADI MOHAMMAD RWETZEL JOHN MCHEN CHIEN-ANDELEON JOHN EJIANG YULU KAI
    • MARZABADI MOHAMMAD RWETZEL JOHN MCHEN CHIEN-ANDELEON JOHN EJIANG YULU KAI
    • C07D211/26A61K31/445C07D211/68C07D401/04C07D401/10C07D401/14
    • C07D211/26
    • This invention is directed to 4-aryl piperidines and related heterocyclic compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.
    • 本发明涉及作为黑色素浓缩激素-1(MCH1)受体的选择性拮抗剂的4-芳基哌啶和相关的杂环化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。 本发明还提供了制备药物组合物的方法,其包括将治疗有效量的本发明化合物与药学上可接受的载体组合。 本发明还提供减少受试者体重的方法,其包括向受试者施用一定量的有效减少受试者体重的本发明化合物。 本发明进一步提供了治疗患有抑郁症和/或焦虑症的受试者的方法,其包括给予受试者一定量的有效治疗受试者的抑郁症和/或焦虑症的本发明化合物。
    • 8. 发明申请
    • 4-ARYL PIPERIDINES
    • WO2005069834A2
    • 2005-08-04
    • PCT/US2005/001131
    • 2005-01-13
    • H. LUNDBECK A/SMARZABADI, Mohammad, R.WETZEL, John, M.CHEN, Chien-AnDELEON, John, E.JIANG, YuLU, Kai
    • MARZABADI, Mohammad, R.WETZEL, John, M.CHEN, Chien-AnDELEON, John, E.JIANG, YuLU, Kai
    • C07D211/26
    • C07D211/26
    • This invention is directed to 4-aryl piperidines and related heterocyclic compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject’s depression and/or anxiety.
    • 本发明涉及作为黑色素浓缩激素-1(MCH1)受体的选择性拮抗剂的4-芳基哌啶和相关的杂环化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。 本发明还提供了制备药物组合物的方法,其包括将治疗有效量的本发明化合物与药学上可接受的载体组合。 本发明还提供减少受试者体重的方法,其包括向受试者施用一定量的有效减少受试者体重的本发明化合物。 本发明进一步提供了治疗患有抑郁症和/或焦虑症的受试者的方法,其包括向受试者施用有效治疗受试者的抑郁症和/或焦虑的量的本发明化合物。
    • 10. 发明申请
    • DIHYDROPYRIDINES AND NEW USES THEREOF
    • 二氢吡啶类及其新用途
    • WO1994022829A2
    • 1994-10-13
    • PCT/US1994003852
    • 1994-04-05
    • SYNAPTIC PHARMACEUTICAL CORPORATIONGLUCHOWSKI, CharlesWETZEL, John, M.CHIU, GeorgeMARZABADI, Mohammad, R.WONG, Wai, C.NAGARATHNAM, Dhanapalan
    • SYNAPTIC PHARMACEUTICAL CORPORATION
    • C07D211/90
    • C07D401/12C07D211/90C07D401/14C07D405/14C07D471/04C07D471/10C07F7/0812
    • The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having structure (I) wherein Y is -(CH2)n-, where n is 1, 2, 3, 4 or 5; -(CH2)h-O-(CH2)k-, where h and k are independently the same or different and are 2, 3 or 4; -(CH2)h-CH=CH-(CH2)k-; or -(CH2)h-CC-(CH2)k-, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is 0, NH, or CH2; wherein R is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R and R are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R and R are independently the same or different and are H, OH, Cl, Br, F, No2, CN, CF3, or NH2, or a linear or branched chain alkyl, alkoxy, alkoxycarbonyl, acyl, alkylsulfoxide, alkylsulfone, or mono- or dialkylamino group. Other active compounds containing one, two or three rings are also disclosed as well as pharmaceutical compositions prepared therefrom and methods of use in the treatment of BPH, inhibition of cholesterol synthesis, and reduction of intraocular pressure.
    • 本发明提供一种治疗受试者的良性前列腺增生的方法,其包括向受试者施用治疗有效量的具有结构(I)的化合物,其中Y为 - (CH 2)n - ,其中n为1,2,3, 4或5; - (CH 2)h -O-(CH 2)k - ,其中h和k独立地相同或不同,为2,3或4; - (CH 2)H-CH = CH-(CH 2)K-; 或 - (CH 2)h-CC-(CH 2)k - ,其中h和k独立地相同或不同,并且是1,2,3或4; 其中Z为0,NH或CH 2; 其中R 1是直链或支链烷基,烷氧基烷基或芳基烷基; 其中R 2和R 4独立地相同或不同,为H或直链或支链烷基; 其中R 3是H,直链或支链烷基,烷氧基,烷氧基烷基或酰基; 并且其中R 5和R 6独立地相同或不同,为H,OH,Cl,Br,F,No2,CN,CF3或NH2,或直链或支链烷基,烷氧基,烷氧基羰基, 酰基,烷基亚砜,烷基砜或单或二烷基氨基。 还公开了含有一个,两个或三个环的其它活性化合物以及由其制备的药物组合物和用于治疗BPH,抑制胆固醇合成和降低眼内压的方法。