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    • 98. 发明申请
    • Amino substituted aryloxybenzylpiperidine derivatives
    • 氨基取代的芳氧基苄基哌啶衍生物
    • US20060079522A1
    • 2006-04-13
    • US10962099
    • 2004-10-08
    • Mohammad MarzabadiChien-An ChenYu JiangKai LuKim Andersen
    • Mohammad MarzabadiChien-An ChenYu JiangKai LuKim Andersen
    • A61K31/5377A61K31/496A61K31/4545C07D403/14C07D413/14
    • C07D211/26C07D401/12C07D403/12
    • This invention is directed to Amino substituted Aryloxybenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also 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 subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention.
    • 本发明涉及作为MCH1受体的配体的氨基取代的芳氧基苄基哌啶衍生物。 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。 本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。 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和药学上可接受的载体组合。 本发明还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本发明化合物。 本发明还提供了治疗患有肥胖症的受试者的方法,其包括给予受试者一定量的本发明化合物。
    • 99. 发明授权
    • Silanol enzyme inhibitors
    • 硅烷醇酶抑制剂
    • US06960678B2
    • 2005-11-01
    • US10171560
    • 2002-06-11
    • Scott McN. SieburthAlfred M. MutahiChien-An Chen
    • Scott McN. SieburthAlfred M. MutahiChien-An Chen
    • C12N9/99A61K31/695A61P43/00C07F7/08C07F7/10C07F7/21C07K5/06C07F7/02
    • C07F7/0836C07F7/081C07F7/0838C07F7/21
    • Compounds of formula (I, II or III), wherein X is OH; Y is OH, H, lower alkyl of one to six carbons or heteroatoms or F; Z and Z′ are independently H, lower alkyl or Q3Si where Q is lower alkyl or aryl; n is 3-50; n′ is 2-50; A and B are independently a) alkyl of one to ten carbons or heteroatoms, b) aryl of four to seven carbons or heteroatoms, c) cyclic of three to ten carbons or heteroatoms, or moieties of the formulas (d, e, or f); R1-R11 groups are each independently hydrogen, alkyl of one to ten carbons or heteroatoms, aryl of 4 to 14 carbons or heteroatoms, arylalkyl of five to twenty carbons or heteroatoms; unsubstituted carbonyl or substituted carbonyl. Heteroatoms are nitrogen, oxygen, silicon or sulfur. At least one of A or B, or both A and B are d), e), or f). The compounds of formula (I) inhibit protease enzymes and can be used as pharmaceuticals.
    • 式(I,II或III)的化合物,其中X是OH; Y是OH,H,1至6个碳原子的低级烷基或杂原子或F; Z和Z'独立地为H,低级烷基或Q 3 Si,其中Q为低级烷基或芳基; n为3-50; n'为2-50; A和B独立地为a)1-10个碳原子或杂原子的烷基,b)4至7个碳原子或杂原子的芳基,c)具有3至10个碳原子或杂原子或式(d,e或f ); R 1〜11个基团各自独立地为氢,1至10个碳原子的烷基或杂原子,4至14个碳原子的芳基或杂原子,5至20个碳的芳基烷基或 杂原子 未取代的羰基或取代羰基。 杂原子是氮,氧,硅或硫。 A或B中的至少一个,或A和B两者均为d),e)或f)。 式(I)化合物抑制蛋白酶,可用作药物。
    • 100. 发明申请
    • 4-Aryl piperidines
    • 4-芳基哌啶
    • US20050154020A1
    • 2005-07-14
    • US10757962
    • 2004-01-14
    • Mohammad MarzabadiJohn WetzelChien-An ChenJohn DeleonYu JiangKai Lu
    • Mohammad MarzabadiJohn WetzelChien-An ChenJohn DeleonYu JiangKai Lu
    • C07D211/26A61K31/4545C07D41/14
    • 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和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。