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1. 发明申请

US20050187267A1 Sulfonylpyrrolidine modulators of androgen receptor function and method 有权
公开(公告)号：US20050187267A1
公开(公告)日：2005-08-25
申请号：US11048439
申请日：2005-02-01
申请人： Lawrence Hamann , Yingzhi Bi , Mark Manfredi , Alexandra Nirschl , James Sutton
发明人： Lawrence Hamann , Yingzhi Bi , Mark Manfredi , Alexandra Nirschl , James Sutton
IPC分类号： A61K31/4015 , A61K31/433 , C07D207/48 , C07D285/06 , C07D285/14 , C07D498/04
CPC分类号： C07D285/14 , C07D207/48
摘要： Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, arylalkyl or substituted arylalkyl, CO2R4a, CONR4aR4b, and CH2OR4a; R2 is hydrogen (H), OR3, SR3, halo, NHR3, NHCOR4c1, NHCO2R4c1, NHCONR4cR4d and NHSO2R4c; R3 in each functional group is hydrogen (H), alkyl or substituted alkyl, CHF2, CF3 and CON4e; R4, R4a, R4b, R4c, R4c1, R4d, R4e, R4f, R4g, or R4h in each functional group are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R5 and R5′ are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl, wherein at least one of R5 and R5′ is hydrogen, or R5 and R5′ taken together form a double bond with oxygen (O), sulfur (S), NR7 or CR7R7′; where R7 and R7′ are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (—O—) or NR4h, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.

2. 发明申请

US20080108691A1 OPEN-CHAIN PROLYL UREA-RELATED MODULATORS OF ANDROGEN RECEPTOR FUNCTION 审中-公开
标题翻译： OPEN-CHAIN PROLYL URA-related MODULATORS OF ANDROGEN RECEPTOR FUNCTION
公开(公告)号：US20080108691A1
公开(公告)日：2008-05-08
申请号：US11931498
申请日：2007-10-31
申请人： Lawrence Hamann , David Augeri , Mark Manfredi
发明人： Lawrence Hamann , David Augeri , Mark Manfredi
IPC分类号： A61K31/4015 , A61P5/26 , C07D207/12
CPC分类号： C07D207/16 , C07D401/12
摘要： There are provided nuclear hormone receptor modulating compounds of formula I wherein R1, R2, R3, X, Y, n and G are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds. Other embodiments are also disclosed.
摘要翻译：提供了式I的核激素受体调节化合物，其中R 1，R 2，R 3，X，Y，n和G分别为如本文所述。还提供了使用这些化合物治疗核激素受体相关病症（如与年龄相关的疾病，例如肌肉减少症）的方法，并且还提供含有这些化合物的药物组合物。还公开了其他实施例。

3. 发明申请

US20050153968A1 Monocyclic N-aryl hydantoin modulators of androgen receptor function 有权
标题翻译：单环N-芳基乙内酰脲调节剂雄激素受体功能
公开(公告)号：US20050153968A1
公开(公告)日：2005-07-14
申请号：US10984502
申请日：2004-11-09
申请人： Yingzhi Bi , Lawrence Hamann , Mark Manfredi , Ligaya Simpkins
发明人： Yingzhi Bi , Lawrence Hamann , Mark Manfredi , Ligaya Simpkins
IPC分类号： A61K31/4178 , A61K31/4709 , A61K31/498 , A61K31/502 , C07D233/72 , C07D233/76 , C07D233/78 , C07D233/96 , C07D43/02
CPC分类号： C07D233/72 , C07D233/76 , C07D233/78 , C07D233/96
摘要： The present invention relates to novel compounds useful in the treatment of androgen receptor associated conditions, such as age-related diseases, pharmaceutical compositions containing at least one of the compounds of the present invention and methods of treating a patient in need of therapy for an androgen receptor associated condition by administering a therapeutically effective amount of at least compound of the present invention.
摘要翻译：本发明涉及可用于治疗雄激素受体相关病症例如年龄相关疾病的新化合物，含有至少一种本发明化合物的药物组合物和治疗需要雄激素治疗的患者的方法受体相关病症，通过施用治疗有效量的至少本发明化合物。

4. 发明申请

US20050059652A1 Open chain prolyl urea-related modulators of androgen receptor function 有权
标题翻译：开链脯氨酰脲相关调节剂的雄激素受体功能
公开(公告)号：US20050059652A1
公开(公告)日：2005-03-17
申请号：US10712456
申请日：2003-11-13
申请人： Lawrence Hamann , David Augeri , Mark Manfredi
发明人： Lawrence Hamann , David Augeri , Mark Manfredi
IPC分类号： A61K31/401 , A61K31/4025 , A61K31/445 , A61K31/454 , A61K31/55 , A61P3/04 , A61P3/10 , A61P9/12 , A61P25/22 , A61P25/24 , C07D207/16 , C07D211/06 , C07D401/12 , C07D43/02
CPC分类号： C07D207/16 , C07D401/12
摘要： The invention provides for a pharmaceutical composition capable of modulating the androgen receptor comprising a compound of formula I wherein R1, R2, R3, X, Y, Z and G are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.
摘要翻译：本发明提供能够调节包含式I化合物的雄激素受体的药物组合物，其中R 1，R 2，R 3，X，Y，Z和G如本文所述。还提供了使用这些化合物治疗核激素受体相关病症（如与年龄有关的疾病，例如肌肉减少症）的方法，并且还提供含有这些化合物的药物组合物。

5. 发明申请

US20100183601A1 Combination of Aurora Kinase Inhibitors and Anti-CD20 Antibodies 审中-公开
标题翻译： Aurora激酶抑制剂和抗CD20抗体的组合
公开(公告)号：US20100183601A1
公开(公告)日：2010-07-22
申请号：US12638018
申请日：2009-12-15
申请人： Mark Manfredi
发明人： Mark Manfredi
IPC分类号： A61K39/395 , A61P35/00 , A61P35/02
CPC分类号： A61K31/55 , A61K39/00 , A61K39/395 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/2887 , C07K2317/24 , A61K2300/00
摘要： The present invention relates to methods for the treatment of hematological malignancies. In particular, the invention provides methods for treatment of hematological malignancies by administering Aurora kinase inhibitors in combination with anti-CD20 antibodies.
摘要翻译：本发明涉及治疗血液恶性肿瘤的方法。特别地，本发明提供了通过将Aurora激酶抑制剂与抗CD20抗体组合施用来治疗血液恶性肿瘤的方法。

6. 发明申请

US20070093509A1 Non-basic melanin concentrating hormone receptor-1 antagonists 有权
标题翻译：非基本黑色素浓缩激素受体-1拮抗剂
公开(公告)号：US20070093509A1
公开(公告)日：2007-04-26
申请号：US11586255
申请日：2006-10-25
申请人： William Washburn , Mark Manfredi , Jeffrey Robi , Andres Hernandez
发明人： William Washburn , Mark Manfredi , Jeffrey Robi , Andres Hernandez
IPC分类号： A61K31/519 , C07D498/02 , A61K31/675
CPC分类号： C07D495/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
摘要翻译：本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

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