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1. 发明申请

WO2007136605A3 ARYL-FUSED SPIROCYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2007136605A3
公开(公告)日：2007-11-29
申请号：PCT/US2007/011540
申请日：2007-05-14
申请人： MERCK & CO., INC. , HAMBLETT, Christopher , KATTAR, Solomon , MAMPREIAN, Dawn , METHOT, Joey , MILLER, Thomas , TEMPEST, Paul
发明人： HAMBLETT, Christopher , KATTAR, Solomon , MAMPREIAN, Dawn , METHOT, Joey , MILLER, Thomas , TEMPEST, Paul
IPC分类号： A61K31/438 , C07D401/04
摘要： The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo .

2. 发明申请

WO2007127137A2 DISUBSTITUTED ANILINE COMPOUNDS 审中-公开
标题翻译：分析苯胺化合物
公开(公告)号：WO2007127137A2
公开(公告)日：2007-11-08
申请号：PCT/US2007/009642
申请日：2007-04-20
申请人： MERCK & CO., INC. , HEIDEBRECHT, Richard , METHOT, Joey , MAMPREIAN, Dawn , MILLER, Thomas , SILIPHAIVANH, Phieng
发明人： HEIDEBRECHT, Richard , METHOT, Joey , MAMPREIAN, Dawn , MILLER, Thomas , SILIPHAIVANH, Phieng
IPC分类号： A61K31/4743
CPC分类号： C07D333/20 , C07C229/60 , C07C237/04 , C07C237/40
摘要： The present invention relates to a novel class of disubstituted aniline compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo .
摘要翻译：本发明涉及一类新的二取代苯胺化合物。这些化合物可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经退行性疾病本发明进一步提供包含本发明化合物和易于遵循的这些药物组合物的安全给药方案的药物组合物，并且其在体内导致治疗有效量的这些化合物。

3. 发明公开

EP2013196A2 DISUBSTITUTED ANILINE COMPOUNDS 有权转让
标题翻译：二取代苯胺类化合物
公开(公告)号：EP2013196A2
公开(公告)日：2009-01-14
申请号：EP07755785.8
申请日：2007-04-20
申请人： Merck & Co., Inc.
发明人： HEIDEBRECHT, Richard , METHOT, Joey , MAMPREIAN, Dawn , MILLER, Thomas , SILIPHAIVANH, Phieng
IPC分类号： C07D333/24 , A61K31/381
CPC分类号： C07D333/20 , C07C229/60 , C07C237/04 , C07C237/40
摘要： The present invention relates to a novel class of disubstituted aniline compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

4. 发明公开

EP2023924A2 ARYL-FUSED SPIROCYCLIC COMPOUNDS 有权转让
标题翻译：芳融合化合物螺
公开(公告)号：EP2023924A2
公开(公告)日：2009-02-18
申请号：EP07777029.5
申请日：2007-05-14
申请人： Merck & Co., Inc.
发明人： HAMBLETT, Christopher , KATTAR, Solomon , MAMPREIAN, Dawn , METHOT, Joey , MILLER, Thomas , TEMPEST, Paul
IPC分类号： A61K31/438 , C07D401/04
CPC分类号： C07D471/10 , C07D401/04 , C07D491/107
摘要： The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

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