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1. 发明申请

WO2014176210A1 THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：噻唑替代氨基酸作为分离型酪氨酸激酶抑制剂
公开(公告)号：WO2014176210A1
公开(公告)日：2014-10-30
申请号：PCT/US2014/034909
申请日：2014-04-22
申请人： MERCK SHARP & DOHME CORP. , MERCK CANADA INC. , ANTHONY, Neville, J. , ANDRESEN, Brian, M. , NORTHRUP, Alan, B. , CHILDERS, Kaleen, K. , DONOFRIO, Anthony , MILLER, Thomas, A. , LIU, Yuan , MACHACEK, Michelle, R. , WOO, Hyun Chong , SPENCER, Kerrie, B. , ELLIS, John Michael , ALTMAN, Michael, D. , ROMEO, Eric, T. , GUAY, Daniel , GRIMM, Jonathan , LEBRUN, Marie-Eve , ROBICHAUD, Joel, S. , WANG, Liping , DUBOIS, Byron , DENG, Qiaolin
发明人： ANTHONY, Neville, J. , ANDRESEN, Brian, M. , NORTHRUP, Alan, B. , CHILDERS, Kaleen, K. , DONOFRIO, Anthony , MILLER, Thomas, A. , LIU, Yuan , MACHACEK, Michelle, R. , WOO, Hyun Chong , SPENCER, Kerrie, B. , ELLIS, John Michael , ALTMAN, Michael, D. , ROMEO, Eric, T. , GUAY, Daniel , GRIMM, Jonathan , LEBRUN, Marie-Eve , ROBICHAUD, Joel, S. , WANG, Liping , DUBOIS, Byron , DENG, Qiaolin
IPC分类号： A61K31/44 , A61K31/53 , A61K31/426
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , and R 4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译：本发明提供式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和R 4如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。

2. 发明申请

WO2015095444A1 THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：噻唑替代氨基酸作为分离型酪氨酸激酶抑制剂
公开(公告)号：WO2015095444A1
公开(公告)日：2015-06-25
申请号：PCT/US2014/071024
申请日：2014-12-18
申请人： MERCK SHARP & DOHME CORP. , MILLER, Thomas, A. , PETROCCHI, Alessia , ROMEO, Eric, T. , VITHARANA, Dilrukshi , KATTAR, Solomon, D. , NORTHRUP, Alan, B. , ALTMAN, Michael, D. , ANTHONY, Neville, J.
发明人： MILLER, Thomas, A. , PETROCCHI, Alessia , ROMEO, Eric, T. , VITHARANA, Dilrukshi , KATTAR, Solomon, D. , NORTHRUP, Alan, B. , ALTMAN, Michael, D. , ANTHONY, Neville, J.
IPC分类号： C07D213/72
CPC分类号： C07D417/12 , A61K31/437 , A61K31/444 , A61K31/517 , A61K31/519 , C07D413/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R 1 , R 2 , R 3 , R 4 , ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译：本发明提供了式（I）（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，环A和下标n 1，n 2和r如上定义于此。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。

3. 发明申请

WO2014153280A1 2-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS 审中-公开
标题翻译：含吡啶二羧酸的酪氨酸激酶（SYK）抑制剂
公开(公告)号：WO2014153280A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/030131
申请日：2014-03-17
申请人： MERCK SHARP & DOHME CORP. , ANDRESEN, Brian, M. , ANTHONY, Neville, J. , HAIDLE, Andrew, M. , MILLER, Thomas, A. , OSIMBONI, Ekundayo
发明人： ANDRESEN, Brian, M. , ANTHONY, Neville, J. , HAIDLE, Andrew, M. , MILLER, Thomas, A. , OSIMBONI, Ekundayo
IPC分类号： A61K31/167 , A61K31/4192 , A61K31/44
CPC分类号： C07D213/81 , C07D401/14 , C07D487/04
摘要： The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译：本发明提供了具有式（I）的某些含2-吡啶甲酰胺的化合物或其药学上可接受的盐，其中A和B如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。

4. 发明申请

WO2014074422A1 AMINO-PYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS 审中-公开
标题翻译：含氨基吡啶类的吡咯啉类激酶（SYK）抑制剂
公开(公告)号：WO2014074422A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/068190
申请日：2013-11-04
申请人： MERCK SHARP & DOHME CORP. , ANDRESEN, Brian, M. , ANTHONY, Neville, J. , MILLER, Thomas, A.
发明人： ANDRESEN, Brian, M. , ANTHONY, Neville, J. , MILLER, Thomas, A.
IPC分类号： A61K31/44
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/008 , A61K9/08 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K31/444 , A61K45/06 , A61K47/10 , A61K47/186 , A61K47/24 , A61K47/26 , A61K47/38 , A61K2300/00
摘要： The invention provides certain amino-pyridine-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R 3 , R 4 , R 5 , R 6 , and the subscript n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译：本发明提供某些含有氨基 - 吡啶的式（I）（I）化合物或其药学上可接受的盐，其中R3，R4，R5，R6和下标n如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。

5. 发明公开

EP2988744A1 THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：甲硫氨酸硫酸酯酶
公开(公告)号：EP2988744A1
公开(公告)日：2016-03-02
申请号：EP14788026.4
申请日：2014-04-22
申请人： Merck Sharp & Dohme Corp. , Merck Canada Inc.
发明人： ANTHONY, Neville, J. , ANDRESEN, Brian, M. , NORTHRUP, Alan, B. , CHILDERS, Kaleen, K. , DONOFRIO, Anthony , MILLER, Thomas, A. , LIU, Yuan , MACHACEK, Michelle, R. , WOO, Hyun Chong , SPENCER, Kerrie, B. , ELLIS, John Michael , ALTMAN, Michael, D. , ROMEO, Eric, T. , GUAY, Daniel , GRIMM, Jonathan , LEBRUN, Marie-Eve , ROBICHAUD, Joel, S. , WANG, Liping , DUBOIS, Byron , DENG, Qiaolin
IPC分类号： A61K31/44 , A61K31/53 , A61K31/426
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

6. 发明申请

WO2008010985A2 PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：作为组蛋白脱乙酰酶抑制剂的磷酸衍生物
公开(公告)号：WO2008010985A2
公开(公告)日：2008-01-24
申请号：PCT/US2007/016123
申请日：2007-07-16
申请人： MERCK & CO., INC. , CLOSE, Joshua , GRIMM, Jonathan , HEIDEBRECHT, Richard, W., Jr. , KATTAR, Solomon , MILLER, Thomas, A. , OTTE, Karin, M. , PETERSON, Scott , SILIPHAIVANH, Phieng , TEMPEST, Paul , WILSON, Kevin, J. , WITTER, David, J.
发明人： CLOSE, Joshua , GRIMM, Jonathan , HEIDEBRECHT, Richard, W., Jr. , KATTAR, Solomon , MILLER, Thomas, A. , OTTE, Karin, M. , PETERSON, Scott , SILIPHAIVANH, Phieng , TEMPEST, Paul , WILSON, Kevin, J. , WITTER, David, J.
IPC分类号： A61K31/675
CPC分类号： C07F9/655345 , C07F9/5304 , C07F9/5325 , C07F9/65033 , C07F9/65586 , C07F9/657154 , C07F9/657181 , C07F9/6584
摘要： The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also 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 phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.
摘要翻译：本发明涉及一类新型的磷衍生物。磷化合物可用于治疗癌症。磷化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导末端分化，阻止肿瘤细胞的细胞生长和/或细胞凋亡，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磷衍生物和这些药物组合物的安全给药方案的药物组合物，其易于遵循，并且其在体内导致治疗有效量的磷衍生物。

7. 发明申请

WO2009020589A1 SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：硅酮衍生物作为脱乙酰壳多糖酶抑制剂
公开(公告)号：WO2009020589A1
公开(公告)日：2009-02-12
申请号：PCT/US2008/009390
申请日：2008-08-05
申请人： MERCK & CO., INC. , GRIMM, Jonathan , HEIDEBRECHT, Richard, W., Jr. , MAMPREIAN, Dawn, M. , METHOT, Joey, L. , MILLER, Thomas, A. , OTTE, Karin, M. , PETERSON, Scott , SILIPHAIVANH, Phieng , WILSON, Kevin, J. , WITTER, David, J.
发明人： GRIMM, Jonathan , HEIDEBRECHT, Richard, W., Jr. , MAMPREIAN, Dawn, M. , METHOT, Joey, L. , MILLER, Thomas, A. , OTTE, Karin, M. , PETERSON, Scott , SILIPHAIVANH, Phieng , WILSON, Kevin, J. , WITTER, David, J.
IPC分类号： C07D471/00
CPC分类号： C07F7/0812
摘要： The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also 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 Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo.
摘要翻译：本发明涉及一类新型的硅衍生物。硅化合物可用于治疗癌症。硅化合物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导末端分化，并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还提供包含硅衍生物和这些药物组合物的安全给药方案的药物组合物，其易于遵循，并且其在体内导致治疗有效量的硅衍生物。

8. 发明申请

WO2007087130A2 HYDROXYALKYLARYLAMIDE DERIVATIVES 审中-公开
标题翻译：羟基烷基酰胺衍生物
公开(公告)号：WO2007087130A2
公开(公告)日：2007-08-02
申请号：PCT/US2007/000183
申请日：2007-01-08
申请人： MERCK & CO., INC. , HEIDEBRECHT, Richard, W., Jr. , MILLER, Thomas, A. , WILSON, Kevin, J. , WITTER, David, J. , GRIMM, Jonathan
发明人： HEIDEBRECHT, Richard, W., Jr. , MILLER, Thomas, A. , WILSON, Kevin, J. , WITTER, David, J. , GRIMM, Jonathan
IPC分类号： C07D403/02
CPC分类号： C07D333/70 , C07D333/20 , C07D413/12
摘要： The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also 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 hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
摘要翻译：本发明涉及一类新的羟烷基芳酰胺衍生物。本发明化合物可用于治疗癌症。氟化芳基酰胺衍生物还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。本发明化合物还可用于预防和治疗TRX介导的疾病，如自身免疫性疾病，变应性疾病和炎性疾病，以及用于预防和/或治疗中枢神经系统（CNS）疾病，例如神经退行性疾病。本发明进一步提供了包含异羟肟酸衍生物和这些药物组合物的安全给药方案的药物组合物，所述药物组合物易于追踪，并且导致体内治疗有效量的异羟肟酸衍生物。

9. 发明授权

EP2170339B1 PYRIDYL AND PYRIMIDINYL DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权转让
标题翻译：吡啶和PYRIMIDINYLDERIVATE ALS蛋白去乙酰化酶
公开(公告)号：EP2170339B1
公开(公告)日：2014-10-15
申请号：EP08794377.5
申请日：2008-06-24
申请人： Merck Sharp & Dohme Corp.
发明人： HEIDEBRECHT, Richard, W., Jr. , MILLER, Thomas, A. , STANTON, Matthew, G. , WITTER, David, J.
IPC分类号： A01N43/40
CPC分类号： C07D213/75 , C07D409/04 , C07D409/14

10. 发明公开

EP2205070A1 N-HYDROXY-NAPHTHALENE DICARBOXAMIDE AND N-HYDROXY-BIPHENYL-DICARBOXAMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： N-羟基萘DICARBOXAMID-和N-羟基 - 联苯DICARBOXAMIDVERBINDUNGEN ALS蛋白脱乙酰酶
公开(公告)号：EP2205070A1
公开(公告)日：2010-07-14
申请号：EP08836352.8
申请日：2008-09-30
申请人： Merck Sharp & Dohme Corp.
发明人： KATTAR, Solomon , MILLER, Thomas, A. , OTTE, Karin, M. , SILIPHAIVANH, Phieng , SURDI, Laura , TEMPEST, Paul , ZABIEREK, Anna, A.
IPC分类号： A01N37/18 , A61K31/16
CPC分类号： C07D319/18 , C07C259/10 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/323 , C07D207/335 , C07D213/40 , C07D231/56 , C07D233/61 , C07D261/08 , C07D265/30 , C07D277/28 , C07D307/14 , C07D307/52 , C07D307/81 , C07D409/04 , C07D417/04 , C07D471/04
摘要： The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can also 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 N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.

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