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1. 发明授权

US06951848B2 Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor 有权
标题翻译：功能化杂环作为趋化因子受体功能的调节剂及其使用方法
公开(公告)号：US06951848B2
公开(公告)日：2005-10-04
申请号：US10096361
申请日：2002-03-12
申请人： Geraldine C. B. Harriman , Kenneth G. Carson , Daniel L. Flynn , Michael E. Solomon , Yuntao Song , Bharat K. Trivedi , Bruce D. Roth , Christine N. Kolz , Ly Pham , Kuai-lin Sun
发明人： Geraldine C. B. Harriman , Kenneth G. Carson , Daniel L. Flynn , Michael E. Solomon , Yuntao Song , Bharat K. Trivedi , Bruce D. Roth , Christine N. Kolz , Ly Pham , Kuai-lin Sun
IPC分类号： A61P31/18 , C07D209/42 , C07D235/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D487/04 , C07D491/04 , C07D491/08 , A61K31/33 , A61K31/40 , A61K31/405 , C07D209/04
CPC分类号： C07D401/04 , C07D209/42 , C07D235/26 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D487/04 , C07D491/04 , C07D491/08
摘要： Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disclosed is a method for treating a patient having an inflammatory disease and/or viral infection comprising administering an effective amount of a compound of Formula I. In particular embodiments, the invention is a method for treating a patient infected with HIV.
摘要翻译：公开了具有下式的新化合物或其生理上可接受的盐，酰胺，酯或前药。该化合物可用于调节（拮抗，激动）趋化因子受体功能。还公开了一种治疗患有炎性疾病和/或病毒感染的患者的方法，其包括施用有效量的式I化合物。在具体实施方案中，本发明是用于治疗感染HIV的患者的方法。

2. 发明授权

US06270957B1 Non-Imuunosuppressive cyclosporins and their use in the prevention and treatment of HIV infection 失效
标题翻译：非免疫抑制环孢菌素及其在预防和治疗艾滋病毒感染中的应用
公开(公告)号：US06270957B1
公开(公告)日：2001-08-07
申请号：US09242723
申请日：1999-02-22
申请人： Daniel H. Rich , Michael E. Solomon
发明人： Daniel H. Rich , Michael E. Solomon
IPC分类号： C12Q170
CPC分类号： C07K7/645 , A61K38/00 , C07K5/1008
摘要： Disclosed are cyclosporin analogs having amino acid residue substitutions at positions 1, 3, or 7 of the cyclosporin peptide backbone. Also disclosed are conjugates of these cyclosporin analogs in which an HIV protease inhibitor moiety is conjugated to the position-7 amino acid residue of the cyclosporin. These compounds simultaneously bind to and inhibit cyclophilin and HIV protease. The compounds have good bioavailability and potent HIV inhibitory activity. They are useful in the treatment and prevention of HIV-mediated disorders, including AIDS.
摘要翻译：公开了在环孢菌素肽骨架的1,3或7位上具有氨基酸残基取代的环孢菌素类似物。还公开了这些环孢菌素类似物的缀合物，其中HIV蛋白酶抑制剂部分与环孢菌素的位置7氨基酸残基缀合。这些化合物同时结合并抑制亲环蛋白和HIV蛋白酶。该化合物具有良好的生物利用度和有效的HIV抑制活性。它们可用于治疗和预防艾滋病毒介导的疾病，包括艾滋病。

3. 发明授权

US06316405B1 Cyclosporin a conjugates and uses therefor 失效
标题翻译：环孢菌素是一种共轭物及其用途
公开(公告)号：US06316405B1
公开(公告)日：2001-11-13
申请号：US09242724
申请日：1999-02-22
申请人： Daniel H. Rich , Michael E. Solomon
发明人： Daniel H. Rich , Michael E. Solomon
IPC分类号： A61K3800
CPC分类号： C07K5/1008 , A61K38/00 , C07K7/645
摘要： Disclosed are conjugates of A&bgr;-binding peptides and CsA analogs and conjugates of A&bgr;-binding peptides and FK506 Binding Peptide inhibitors. These conjugates chemically induce dimerization of either cyclophilin or FK506 Binding Peptide with A&bgr; peptide, a major component of amyloid plaques found in neurological disorders such as Alzheimer's disease, multiple sclerosis, and amyotrophic lateral sclerosis. The conjugates are useful in the treatment of neurological diseases involving the formation of amyloid plaques because they inhibit and/or prevent the aggregation and deposition of A&bgr; peptide into plaques.
摘要翻译：公开了Abeta结合肽和CsA类似物和Abeta结合肽和FK506结合肽抑制剂的缀合物的缀合物。这些缀合物化学诱导亲环蛋白或FK506结合肽与Abeta肽的二聚，Abeta肽是神经系统疾病如阿尔茨海默病，多发性硬化和肌萎缩性侧索硬化中发现的淀粉样蛋白斑的主要成分。缀合物可用于治疗涉及淀粉样蛋白斑形成的神经疾病，因为它们抑制和/或阻止Aβ肽聚集和沉积到斑块中。

4. 发明授权

US07790719B2 Modulators of melanocortin receptor 失效
标题翻译：黑皮质素受体的调节剂
公开(公告)号：US07790719B2
公开(公告)日：2010-09-07
申请号：US11878708
申请日：2007-07-26
申请人： Tricia J. Vos , Michael Patane , Michael E. Solomon , Christopher Blackburn , Mihaela D. Danca
发明人： Tricia J. Vos , Michael Patane , Michael E. Solomon , Christopher Blackburn , Mihaela D. Danca
IPC分类号： A61K31/505 , A61K31/535 , A61K31/517 , A61K31/445 , C07D239/02 , C07D233/88 , C07D413/14 , C07D239/70
CPC分类号： C07C279/22 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/22 , C07D209/14 , C07D211/26 , C07D211/34 , C07D211/60 , C07D211/62 , C07D213/40 , C07D217/02 , C07D231/12 , C07D233/56 , C07D233/88 , C07D239/16 , C07D239/42 , C07D249/08 , C07D295/13 , C07D295/185 , C07D307/79 , C07D333/20 , C07D333/38 , C07D401/06 , C07D407/12 , C07D409/12 , C07D451/04 , C07D453/02 , C07D471/10
摘要： This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.
摘要翻译：本发明提供了用于治疗黑皮质素受体相关疾病的化合物和方法，例如包括由癌症和其它慢性疾病引起的恶病质的体重减轻障碍。化合物由式I表示：其中X是氧或硫; G是G1或G2：L1，L2，L3和Q是连接基团，环A，B和C以及R 1 -R 14在本说明书中描述。这些化合物是黑皮质素受体的拮抗剂。

5. 发明授权

US07375125B2 Melanocortin-4 receptor binding compounds and methods of use thereof 失效
标题翻译：黑皮质素-4受体结合化合物及其使用方法
公开(公告)号：US07375125B2
公开(公告)日：2008-05-20
申请号：US10462436
申请日：2003-06-16
申请人： Tricia J. Vos , Michael E. Solomon , Christopher F. Claiborne , Martin P. Maguire , Mingshi Dai , Michael Patane , Thomas H. Marsilje
发明人： Tricia J. Vos , Michael E. Solomon , Christopher F. Claiborne , Martin P. Maguire , Mingshi Dai , Michael Patane , Thomas H. Marsilje
IPC分类号： C07D233/20 , A61K31/4164
CPC分类号： C07D471/04 , A61K31/4164 , A61K31/4174 , A61K31/4184 , A61K31/505 , A61K31/5377 , C07C211/27 , C07C211/29 , C07C211/30 , C07C237/38 , C07C257/18 , C07C271/20 , C07C275/26 , C07D233/06 , C07D233/10 , C07D233/18 , C07D233/20 , C07D233/22 , C07D233/26 , C07D233/30 , C07D233/42 , C07D233/48 , C07D235/12 , C07D235/18 , C07D239/06 , C07D295/073 , C07D295/088 , C07D295/13 , C07D295/135 , C07D401/04 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/12 , C07D487/04 , C07D513/04
摘要： Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.
摘要翻译：提供式XVII的MC4-R结合化合物：其中L 2是连接基团，P 1，P 2， Z 4，Z 4，Z 3，Z 3，Z 3，Z 3， SUP> 4，Z 5，t，s和R如说明书中所述。还提供了使用该化合物治疗MC4-R相关疾病（例如与体重减轻相关的疾病）的方法。

6. 发明申请

US20080269217A1 Melanocortin-4 receptor binding compounds and methods of use thereof 审中-公开
公开(公告)号：US20080269217A1
公开(公告)日：2008-10-30
申请号：US12149440
申请日：2008-05-01
申请人： Tricia J. Vos , Michael E. Solomon , Christopher F. Claiborne , Martin P. Maguire , Mingshi Dai , Michael Patane , Thoma H. Marsilje
发明人： Tricia J. Vos , Michael E. Solomon , Christopher F. Claiborne , Martin P. Maguire , Mingshi Dai , Michael Patane , Thoma H. Marsilje
IPC分类号： A61K31/5377 , A61K31/505 , C07D239/06 , A61K31/4184 , C07D235/02 , C07D233/24 , A61K31/4174 , C07D413/02
CPC分类号： C07D471/04 , A61K31/4164 , A61K31/4174 , A61K31/4184 , A61K31/505 , A61K31/5377 , C07C211/27 , C07C211/29 , C07C211/30 , C07C237/38 , C07C257/18 , C07C271/20 , C07C275/26 , C07D233/06 , C07D233/10 , C07D233/18 , C07D233/20 , C07D233/22 , C07D233/26 , C07D233/30 , C07D233/42 , C07D233/48 , C07D235/12 , C07D235/18 , C07D239/06 , C07D295/073 , C07D295/088 , C07D295/13 , C07D295/135 , C07D401/04 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/12 , C07D487/04 , C07D513/04
摘要： Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.

7. 发明授权

US07365070B2 Modulators of melanocortin receptor 失效
标题翻译：黑皮质素受体的调节剂
公开(公告)号：US07365070B2
公开(公告)日：2008-04-29
申请号：US10727997
申请日：2003-12-04
申请人： Tricia J. Vos , Michael Patane , Michael E. Solomon , Christopher Blackburn , Mihaela D. Danca
发明人： Tricia J. Vos , Michael Patane , Michael E. Solomon , Christopher Blackburn , Mihaela D. Danca
IPC分类号： A61K31/40 , A61K31/415 , A61K31/381 , A61K31/535 , A61K31/445 , C07D211/26 , C07D207/04 , C07D333/22 , C07D265/30 , C07D233/66 , C07D241/04 , C07D409/12 , C07D221/20
CPC分类号： C07C279/22 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/22 , C07D209/14 , C07D211/26 , C07D211/34 , C07D211/60 , C07D211/62 , C07D213/40 , C07D217/02 , C07D231/12 , C07D233/56 , C07D233/88 , C07D239/16 , C07D239/42 , C07D249/08 , C07D295/13 , C07D295/185 , C07D307/79 , C07D333/20 , C07D333/38 , C07D401/06 , C07D407/12 , C07D409/12 , C07D451/04 , C07D453/02 , C07D471/10
摘要： This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.
摘要翻译：本发明提供了用于治疗黑皮质素受体相关疾病的化合物和方法，例如包括由癌症和其它慢性疾病引起的恶病质的体重减轻障碍。化合物由式I表示：其中X是氧或硫; G是G1或G2：L 1，L 2，L 3和Q是连接基，环A，B和C和在说明书中描述了R 1〜R 14。这些化合物是黑皮质素受体的拮抗剂。

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