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公开(公告)号:US08252774B2
公开(公告)日:2012-08-28
申请号:US13120090
申请日:2009-09-22
IPC分类号: A61K31/663 , C07F9/02
CPC分类号: C07F9/6561
摘要: Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
摘要翻译: 公开了新的5-氮杂吲哚双膦酸化合物,以及制备化合物的方法,包括该化合物的药物组合物,以及在治疗异常钙和磷酸盐代谢(包括骨和关节疾病等)疾病的方法中给予化合物。
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公开(公告)号:US20110230443A1
公开(公告)日:2011-09-22
申请号:US13120078
申请日:2009-09-22
IPC分类号: A61K31/675 , C07F9/38 , A61P19/00 , A61P35/00 , A61P19/02 , A61P19/08 , A61P29/00 , A61P33/06 , A61P33/02
CPC分类号: C07D471/04 , C07F9/65068
摘要: Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
摘要翻译: 公开了新的咪唑并[1,2-α]吡啶基双膦酸盐化合物,以及制备化合物的方法,包括该化合物的药物组合物,以及在治疗异常钙和磷酸盐代谢的方法中施用化合物,包括骨和关节疾病 和其他疾病。
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公开(公告)号:US20110237550A1
公开(公告)日:2011-09-29
申请号:US13120090
申请日:2009-09-22
CPC分类号: C07F9/6561
摘要: Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
摘要翻译: 公开了新的5-氮杂吲哚双膦酸化合物,以及制备化合物的方法,包括该化合物的药物组合物,以及在治疗异常钙和磷酸盐代谢(包括骨和关节疾病等)疾病的方法中给予化合物。
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公开(公告)号:US08618079B2
公开(公告)日:2013-12-31
申请号:US13120078
申请日:2009-09-22
IPC分类号: A61K31/675
CPC分类号: C07D471/04 , C07F9/65068
摘要: Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
摘要翻译: 公开了新的咪唑并[1,2-α]吡啶基双膦酸盐化合物,以及制备化合物的方法,包括该化合物的药物组合物,以及在治疗异常钙和磷酸盐代谢的方法中施用化合物,包括骨和关节疾病 和其他疾病。
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公开(公告)号:US06911447B2
公开(公告)日:2005-06-28
申请号:US10121874
申请日:2002-04-12
IPC分类号: C07D241/04 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/496 , A61P3/06 , A61P3/10 , A61P5/00 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P15/00 , A61P15/08 , A61P15/10 , A61P21/04 , A61P29/00 , A61P31/04 , A61P35/00 , C07D207/12 , C07D211/46 , C07D241/06 , C07D241/08 , C07D401/12 , C07D403/06 , A01N25/00 , A61K9/14 , A61K47/00 , A61K47/30 , A61K47/34
CPC分类号: C07D241/08 , C07D207/12 , C07D211/46 , C07D241/06 , C07D401/12 , C07D403/06 , C07K5/06078 , C07K5/06191 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.
摘要翻译: 公开了MC-3 / MC-4受体配体,所述配体具有下式:其中A是选自以下的构象限制性环系:a)非芳族碳环; b)芳族碳环; c)非芳族杂环; d)芳族杂环; 其中所述环包含5至8个原子; W是优选包含D-1-氟苯丙氨酸的单元,Y包含杂原子,Z包括芳族碳环。 还公开了包含本发明配体的药物组合物以及治疗通过MC-3 / MC-4受体介导的疾病的方法。
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公开(公告)号:US07087759B2
公开(公告)日:2006-08-08
申请号:US10856983
申请日:2004-05-28
IPC分类号: C07D261/20 , C07D211/36 , C07D207/48 , A61K31/445
CPC分类号: C07D241/08 , C07D207/12 , C07D211/46 , C07D241/06 , C07D401/12 , C07D403/06 , C07K5/06078 , C07K5/06191 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.
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公开(公告)号:US07132539B2
公开(公告)日:2006-11-07
申请号:US10689022
申请日:2003-10-20
IPC分类号: C07D403/12 , C07D241/04 , A61K31/495 , A61K31/496
CPC分类号: C07D401/12 , C07D241/04 , C07D241/08 , C07D403/12
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。
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公开(公告)号:US07781418B2
公开(公告)日:2010-08-24
申请号:US12001318
申请日:2007-12-11
IPC分类号: A61K31/675 , A61K31/44 , A01N43/42
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。
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9.
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。
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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。
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