Melanocortin receptor ligands
    7.
    发明授权
    Melanocortin receptor ligands 失效
    黑皮质素受体配体

    公开(公告)号:US07132539B2

    公开(公告)日:2006-11-07

    申请号:US10689022

    申请日:2003-10-20

    摘要: The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.

    摘要翻译: 本发明涉及包含由选自C 1 -C 12烷基的R 1烷基单元取代的含氮环支架的化合物, 直链或支链烷基,C 3 -C 8环烷基,C 2 -C 12直链状 或支链烯基或卤代烷基,例如具有下式的2-酮-3-烷基哌嗪:其中R选自苯基,3-氟苯基,4-氟苯基,3,5-二氟苯基和4-氟苯基, 氯苯基; R 1选自甲基,乙基,丙基,异丙基,丁基,异丁基,仲丁基,叔丁基,环丙基,环丙基甲基,环戊基,环戊基甲基,环己基, 环己基甲基,苄基,烯丙基,1-甲基烯丙基,2-甲基烯丙基,丁-2-烯基和炔丙基; R 7a选自氢,-CO 2 H,-CONH 2,-CONHCH 3,/ SUB >和-CON(CH 3 3)2。 R 8是苄基,取代的苄基或萘-2-基甲基。

    Composition for treating bone disorders
    8.
    发明授权
    Composition for treating bone disorders 有权
    用于治疗骨骼疾病的组合物

    公开(公告)号:US07781418B2

    公开(公告)日:2010-08-24

    申请号:US12001318

    申请日:2007-12-11

    CPC分类号: C07F9/5765

    摘要: Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis.

    摘要翻译: 公开了一种新的物质组合物,基本上为对映异构体纯的(1R,6S)-2-氮杂双环[4.3.0]壬烷-8,8-二膦酸,制备这种新的物质组合物的方法,包含新的 组合物和组合物在治疗骨质疏松症,溶骨性骨转移,类风湿性关节炎和骨关节炎等骨病的方法中的用途。

    2-decarboxy-2-phosphinico Prostaglandin F analogs
    9.
    发明授权
    2-decarboxy-2-phosphinico Prostaglandin F analogs 有权
    2-decarboxy-2-phosphinico前列腺素F类似物

    公开(公告)号:US06372730B1

    公开(公告)日:2002-04-16

    申请号:US09632256

    申请日:2000-08-03

    IPC分类号: A61K3166

    CPC分类号: C07F9/303

    摘要: The invention provides novel Prostaglandin F analogs. In particular, the present invention is directed to compounds having a structure according to the following formula: wherein R1, R2, X, Y, V, a, b, W, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically—acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.

    摘要翻译: 本发明提供了新型前列腺素F类似物。 特别地,本发明涉及具有下式结构的化合物:其中R1,R2,X,Y,V,a,b,W和Z定义如下。本发明还包括光学异构体,非对映异构体 和上式的对映异构体及其药学上可接受的盐,生物可水解的酰胺,酯和酰亚胺。本发明的化合物可用于治疗多种疾病和病症,例如骨骼疾病和青光眼。 因此,本发明还提供包含这些化合物的药物组合物。 本发明还提供了使用这些化合物或含有它们的组合物治疗骨病和青光眼的方法。

    Melanocortin receptor ligands
    10.
    发明授权
    Melanocortin receptor ligands 失效
    黑皮质素受体配体

    公开(公告)号:US07026335B2

    公开(公告)日:2006-04-11

    申请号:US10410775

    申请日:2003-04-09

    IPC分类号: A61K31/445 C07D401/04

    CPC分类号: C07D401/06 C07D211/26

    摘要: The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein preferably R is substituted aryl, W is a pendant unit having the formula: -L-Q L is a linking unit, Q is preferably a cyclic hydrocarbyl unit; W1 is preferably a carbocyclic unit and W2 is a heteroatom comprising unit.

    摘要翻译: 本发明涉及包含与取代或未取代的烃基环连接的4-取代的哌啶环的化合物。 化合物,包括所有对映异构体和非对映体形式及其药学上可接受的盐,具有下式:其中优选R是取代的芳基,W是具有下式的侧链单元:<?in-line-formula description =“In-line Formulas” - =“lead”?> - LQ <?in-line-formula description =“In-line Formulas”end =“tail”?> L是连接单元,Q优选为环状烃基单元; W 1优选是碳环单元,W 2是含杂原子的单元。