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1. 发明申请

US20050171158A1 Melanocortin receptor ligands 审中-公开
标题翻译：黑皮质素受体配体
公开(公告)号：US20050171158A1
公开(公告)日：2005-08-04
申请号：US11092100
申请日：2005-03-29
申请人： Frank Ebetino , Xuewei Liu , Mark Solinsky , John Wos
发明人： Frank Ebetino , Xuewei Liu , Mark Solinsky , John Wos
IPC分类号： C07D211/16 , A61K31/445 , A61K31/454 , A61K31/4545 , A61P1/14 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P5/24 , A61P7/00 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P15/00 , A61P15/10 , A61P19/02 , A61P19/06 , A61P21/02 , A61P25/00 , A61P29/00 , A61P31/10 , A61P35/00 , C07D211/26 , C07D211/58 , C07D401/06 , C07D401/14 , C07D211/06 , C07D41/02
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。

2. 发明申请

US20050239835A1 Melanocortin receptor ligands 审中-公开
标题翻译：黑皮质素受体配体
公开(公告)号：US20050239835A1
公开(公告)日：2005-10-27
申请号：US11172059
申请日：2005-06-30
申请人： Frank Ebetino , Xuewei Liu , Mark Solinsky , John Wos , Rashid Mumin
发明人： Frank Ebetino , Xuewei Liu , Mark Solinsky , John Wos , Rashid Mumin
IPC分类号： A61K31/451 , A61K31/454 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P15/08 , A61P15/10 , A61P17/00 , A61P19/02 , A61P19/06 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D211/26 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/06 , C07D417/12 , A61K31/445 , C07D417/02 , C07D43/02
CPC分类号： C07D409/06 , C07D211/26 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12
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 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 2是含杂原子的单元。

3. 发明申请

US20060128613A1 Melanocortin receptor ligands 审中-公开
标题翻译：黑皮质素受体配体
公开(公告)号：US20060128613A1
公开(公告)日：2006-06-15
申请号：US10386962
申请日：2003-03-12
申请人： Frank Ebetino , Adam Mazur , Jeffrey Hayes , Feng Wang , Mark Solinsky , Anny-Odile Colson , Qishen Lin
发明人： Frank Ebetino , Adam Mazur , Jeffrey Hayes , Feng Wang , Mark Solinsky , Anny-Odile Colson , Qishen Lin
IPC分类号： A61K38/12 , C07K7/64
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/0827 , C07K5/1016 , C07K5/1027 , C07K7/64
摘要： Disclosed are MC-4 and/or MC-3 receptor ligands, the ligands having a structure according to Formula (I): wherein R2, R4, R4′, R5, R6, R6′, R7, R8, R8′, R9, R9′, R10, Ar, Z1, Z2, Z3, X, B, D, p, q, r and s are as described in the specification and claims, and optical isomers, diastereomers or enantiomers thereof; pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides or imides thereof. Also disclosed are pharmaceutical compositions comprising the ligands of Formula (I), as well as methods of treating diseases mediate by the MC-4/MC-3 receptors, as described in the Detailed Descriptions section of the specification.
摘要翻译：公开了MC-4和/或MC-3受体配体，所述配体具有根据式（I）的结构：其中R 2，R 4，R SUP R 4，R 5，R 6，R 6，R 7，R 7，R 7， R 8，R 9，R 9，R 9，R 10，R 9，，Ar，Z 1，Z 2，Z 3，X，B，D，p，q，r和s如说明书和权利要求书及其光学异构体，非对映异构体或其对映异构体; 药学上可接受的盐，水合物和生物可水解的酯，酰胺或其酰亚胺。还公开了包含式（I）的配体的药物组合物，以及治疗由MC-4 / MC-3受体介导的疾病的方法，如说明书的详细描述部分所述。

4. 发明申请

US20060247224A1 Melanocortin receptor ligands 审中-公开
公开(公告)号：US20060247224A1
公开(公告)日：2006-11-02
申请号：US11473972
申请日：2006-06-23
申请人： Frank Ebetino , Xinrong Tian , Wieslaw Mazur , Anny-Odile Colson
发明人： Frank Ebetino , Xinrong Tian , Wieslaw Mazur , Anny-Odile Colson
IPC分类号： A61K31/496 , C07D409/02 , C07D405/02 , C07D403/02
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.

5. 发明授权

US11497813B2 Bortezomib conjugates and methods using same 有权
公开(公告)号：US11497813B2
公开(公告)日：2022-11-15
申请号：US15772910
申请日：2016-11-02
申请人： Frank EBETINO et al.
发明人： Frank Ebetino , Robert Boeckman , Lianping Xing , Lifeng Xiao , Brendan Boyce
IPC分类号： A61K47/00 , A61K47/54 , C07F9/6561 , A61K49/00 , C07K5/078 , C07F9/6558 , C07K5/062 , A61P19/00 , A61P35/00 , A61K31/69 , C07K5/06
摘要： The present invention provides compositions and methods for providing controllable local delivery of a conjugate of bortezomib (Btz) and a bisphosphonate to promote bone formation. In certain embodiments, the invention is used as a treatment for a subject with diseases and disorders characterized by bone loss.

6. 发明申请

US20060106059A1 Melanocortin receptor ligands 审中-公开
标题翻译：黑皮质素受体配体
公开(公告)号：US20060106059A1
公开(公告)日：2006-05-18
申请号：US11328330
申请日：2006-01-09
申请人： Wieslaw Mazur , Xinrong Tian , Xiufeng Hu , Frank Ebetino
发明人： Wieslaw Mazur , Xinrong Tian , Xiufeng Hu , Frank Ebetino
IPC分类号： C07D217/12 , A61K31/47
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 has the formula: W is a unit which preferable comprises D-(4-fluorophenyl)alanine, Y comprises at least one nitrogen 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，配体具有下式：其中A具有下式：W是优选包含D-（4-氟苯基）丙氨酸的单元，Y包含至少一个氮杂原子，和 Z包含芳族碳环。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。

7. 发明申请

US20050010031A1 Melanocortin receptor ligands 失效
标题翻译：黑皮质素受体配体
公开(公告)号：US20050010031A1
公开(公告)日：2005-01-13
申请号：US10689022
申请日：2003-10-20
申请人： Frank Ebetino , Xinrong Tian , Wieslaw Mazur , Anny-Odile Colson
发明人： Frank Ebetino , Xinrong Tian , Wieslaw Mazur , Anny-Odile Colson
IPC分类号： C07D241/04 , C07D241/08 , C07D401/12 , C07D403/12 , C07K14/72
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, isopropyl, butyl, isobutyl, 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直链或支链烷基，C 3 -C 8环烷基，C 2 -C 12直链或支链烯基的C 1 -C 12烷基单元取代的含氮环支架的化合物或卤代烷基，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-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和-CON（CH 3）2; R 8是苄基，取代的苄基或萘-2-基甲基。

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