公开(公告)号：US07968548B2

公开(公告)日：2011-06-28

申请号：US11464053

申请日：2006-08-11

申请人： Shubh D. Sharma ,  Yi-Qun Shi ,  Kevin D. Burris ,  Zhijun Wu ,  Papireddy Purma ,  Yadi Reddy Bonuga

发明人： Shubh D. Sharma ,  Yi-Qun Shi ,  Kevin D. Burris ,  Zhijun Wu ,  Papireddy Purma ,  Yadi Reddy Bonuga

IPC分类号： A61K31/495 ,  C07D241/04

CPC分类号： C07D241/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12

摘要： Melanocortin receptor-specific compounds with diamine groups of the general formula and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L1, L2, L3, R1a, R1b, R2a, R2b and X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

摘要翻译： 具有通式的二胺基的黑皮质素受体特异性化合物及其药学上可接受的盐，其中W是具有至少一个阳离子中心，氢键供体或氢键受体的二胺杂原子单元，J，Q，L1，L2，L3， R1a，R1b，R2a，R2b和X如本说明书中所定义，并且带有星号的碳原子可具有任何立体化学构型。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

公开(公告)号：US07727991B2

公开(公告)日：2010-06-01

申请号：US11464051

申请日：2006-08-11

申请人： Shubh D. Sharma ,  Yi-Qun Shi ,  Kevin D. Burris ,  Zhijun Wu ,  Papireddy Purma ,  Yadi Reddy Bonuga

发明人： Shubh D. Sharma ,  Yi-Qun Shi ,  Kevin D. Burris ,  Zhijun Wu ,  Papireddy Purma ,  Yadi Reddy Bonuga

IPC分类号： A61K31/495 ,  C07D295/10

CPC分类号： C07D241/04 ,  C07D403/12

摘要： Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q is a substituted or unsubstituted aromatic carbocyclic ring group, L, R2a, R2b, R3a, R3b, r, x and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

摘要翻译： 其中J是取代或未取代的单环或双环结构，W是具有至少一个阳离子中心，氢键给体或氢键受体的杂原子单元，Q是通式的黑皮质素受体特异性化合物及其药学上可接受的盐 取代或未取代的芳族碳环基，L，R2a，R2b，R3a，R3b，r，x和y如说明书中所定义，并且带有星号的碳原子可以具有任何立体化学构型。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

公开(公告)号：US07727990B2

公开(公告)日：2010-06-01

申请号：US11464069

申请日：2006-08-11

申请人： Shubh D. Sharma ,  Yi-Qun Shi ,  Kevin D. Burris ,  Zhijun Wu ,  Papireddy Purma ,  Yadi Reddy Bonuga

发明人： Shubh D. Sharma ,  Yi-Qun Shi ,  Kevin D. Burris ,  Zhijun Wu ,  Papireddy Purma ,  Yadi Reddy Bonuga

IPC分类号： A61K31/497 ,  C07D295/067

CPC分类号： C07D241/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12

摘要： Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where X, W, J, Q, L1, L2, L3, R1a, R1b, R2a, and R2b are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

摘要翻译： 通式的黑皮质素受体特异性化合物及其药学上可接受的盐，其中X，W，J，Q，L1，L2，L3，R1a，R1b，R2a和R2b如本说明书中所定义， 星号可以具有任何立体化学构型。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

公开(公告)号：US20060287331A1

公开(公告)日：2006-12-21

申请号：US11464053

申请日：2006-08-11

申请人： Shubh SHARMA ,  Yi-Qun SHI ,  Kevin BURRIS ,  Zhijun WU ,  Papireddy PURMA ,  Yadi Reddy BONUGA

发明人： Shubh SHARMA ,  Yi-Qun SHI ,  Kevin BURRIS ,  Zhijun WU ,  Papireddy PURMA ,  Yadi Reddy BONUGA

IPC分类号： A61K31/495 ,  C07D241/04

CPC分类号： C07D241/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12

摘要： Melanocortin receptor-specific compounds with diamine groups of the general formula and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L1, L2, L3, R1a, R1b, R2a, R2b and X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

摘要翻译： 具有通式的二胺基的黑皮质素受体特异性化合物及其药学上可接受的盐，其中W是具有至少一个阳离子中心，氢键给体或氢键受体的二胺杂原子单元，J，Q，L 1， L 2，L 3，R 3，R 1a，R 1b，R 2a， R 2，R 2和X如说明书中所定义，并且用星号标记的碳原子可以具有任何立体化学构型。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

公开(公告)号：US07834017B2

公开(公告)日：2010-11-16

申请号：US11836897

申请日：2007-08-10

申请人： Kevin Burris ,  Yi-Qun Shi ,  Shubh D. Sharma ,  Yadi Reddy Bonuga ,  Papireddy Purma

发明人： Kevin Burris ,  Yi-Qun Shi ,  Shubh D. Sharma ,  Yadi Reddy Bonuga ,  Papireddy Purma

IPC分类号： A61K31/497 ,  C07D403/00 ,  C07D295/00

CPC分类号： C07D241/04 ,  A61K31/495 ,  A61K31/496 ,  C07D403/06 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.

摘要翻译： 提供具有结构式I的化合物：其中基团-C（R 8）（CH 2）v CH（R 9）（CH 2）y Q和-C（R 8）（CH 2）v CH（R 9）（CH 2） ，R1a，R1b，R2a，R2b，R8，R9，J，Q，W，X，L2，v和y具有说明书中给出的含义。 使用这些化合物治疗对人或非人哺乳动物（例如男性性功能障碍，女性性功能障碍，进食障碍，超过最佳体重，肥胖，低于最佳）的黑色素皮质素受体功能变化的病症 体重或恶病质）也被描述。

公开(公告)号：US20060287332A1

公开(公告)日：2006-12-21

申请号：US11464069

申请日：2006-08-11

申请人： Shubh SHARMA ,  Yi-Qun SHI ,  Kevin BURRIS ,  Zhijun WU ,  Papireddy PURMA ,  Yadi Reddy BONUGA

发明人： Shubh SHARMA ,  Yi-Qun SHI ,  Kevin BURRIS ,  Zhijun WU ,  Papireddy PURMA ,  Yadi Reddy BONUGA

IPC分类号： A61K31/496 ,  C07D241/04

CPC分类号： C07D241/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12

摘要： Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where X, W, J, Q, L1, L2, L3, R1a, R1b, R2a, and R2b are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

摘要翻译： 通式的黑皮质素受体特异性化合物及其药学上可接受的盐，其中X，W，J，Q，L 1，L 2，L 3， R 1a，R 1a，R 1b，R 2a和R 2b如本说明书中所定义 ，并且带有星号的碳原子可以具有任何立体化学构型。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

公开(公告)号：US20060287330A1

公开(公告)日：2006-12-21

申请号：US11464051

申请日：2006-08-11

申请人： Shubh SHARMA ,  Yi-Qun SHI ,  Kevin BURRIS ,  Zhijun WU ,  Papireddy PURMA ,  Yadi Reddy BONUGA

发明人： Shubh SHARMA ,  Yi-Qun SHI ,  Kevin BURRIS ,  Zhijun WU ,  Papireddy PURMA ,  Yadi Reddy BONUGA

IPC分类号： A61K31/496 ,  A61K31/495 ,  C07D403/02

CPC分类号： C07D241/04 ,  C07D403/12

摘要： Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q is a substituted or unsubstituted aromatic carbocyclic ring group, L, R2a, R2b, R3a, R3b, r, x and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

摘要翻译： 其中J是取代或未取代的单环或双环结构，W是具有至少一个阳离子中心，氢键供体或氢键受体的杂原子单元，Q是通式的黑皮质素受体特异性化合物及其药学上可接受的盐 取代或未取代的芳族碳环基团，L，R 2a，R 2b，R 3a，R 3b， ，r，x和y如说明书中所定义，并且用星号标记的碳原子可以具有任何立体化学构型。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。