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1. 发明申请

WO2008010985A3 PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：磷酸衍生物作为组蛋白脱乙酰酶抑制剂
公开(公告)号：WO2008010985A3
公开(公告)日：2008-04-03
申请号：PCT/US2007016123
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： A61K31/66 , A61K31/662 , C07F9/32 , C07F9/40 , C07F9/547 , C07F9/6564
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：本发明涉及一类新的磷衍生物。磷化合物可用于治疗癌症。磷化合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这些药物组合物的磷衍生物和安全给药方案的药物组合物，其易于追踪，并且导致治疗有效量的体内磷衍生物。

2. 发明申请

WO2007087130A3 HYDROXYALKYLARYLAMIDE DERIVATIVES 审中-公开
标题翻译：羟基甲酰胺衍生物
公开(公告)号：WO2007087130A3
公开(公告)日：2007-12-13
申请号：PCT/US2007000183
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： A01N43/00 , A61K31/33
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基酰胺衍生物。本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，并且适用于选择性诱导终末分化，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进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

3. 发明申请

WO2007087129A2 FLUORINATED ARYLAMIDE DERIVATIVES 审中-公开
标题翻译：氟化芳酰胺衍生物
公开(公告)号：WO2007087129A2
公开(公告)日：2007-08-02
申请号：PCT/US2007000182
申请日：2007-01-08
申请人： MERCK & CO INC , MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
发明人： MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
IPC分类号： A61K31/5377
CPC分类号： C07D231/40 , C07D333/20 , C07D333/70 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The present invention relates to a novel class of fluorinated arylamide 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：本发明涉及新型氟化芳基酰胺衍生物。本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，并且适用于选择性诱导终末分化，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疾病（CNS），例如神经退行性疾病本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

4. 发明申请

WO2007087129A8 FLUORINATED ARYLAMIDE DERIVATIVES 审中-公开
标题翻译：氟化芳酰胺衍生物
公开(公告)号：WO2007087129A8
公开(公告)日：2010-05-14
申请号：PCT/US2007000182
申请日：2007-01-08
申请人： MERCK & CO INC , MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
发明人： MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
IPC分类号： A61K31/38
CPC分类号： C07D231/40 , C07D333/20 , C07D333/70 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The present invention relates to a novel class of fluorinated arylamide 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：本发明涉及一类新型氟化芳基酰胺衍生物。本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，并且适用于选择性诱导终末分化，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进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

5. 发明申请

WO2014052563A3 NOVEL COMPOUNDS THAT ARE ERK INHIBITORS 审中-公开
标题翻译：新的化合物是ERK抑制剂
公开(公告)号：WO2014052563A3
公开(公告)日：2015-07-16
申请号：PCT/US2013061878
申请日：2013-09-26
申请人： MERCK SHARP & DOHME , WILSON KEVIN J , WITTER DAVID J , SILIPHAIVANH PHIENG , LIPFORD KATHRYN , SLOMAN DAVID , FALCONE DANIELLE , O'BOYLE BRENDAN , MANSOOR UMAR FARUK , LIM JONGWON , METHOT JOEY L , BOYCE CHRISTOPHER , CHEN LEI , DANIELS MATTHEW H , FEVRIER SALEM , HUANG XIANHAI , KURUKULASURIYA RAVI , TONG LING , ZHOU WEI , KOZLOWSKI JOSEPH , MALETIC MILANA M , SHINKRE BIDHAN A , THATAI JAYANTH THIRUVELLORE , BAKSHI RAMAN KUMAR , KARUNAKARAN GANESH BABU
发明人： WILSON KEVIN J , WITTER DAVID J , SILIPHAIVANH PHIENG , LIPFORD KATHRYN , SLOMAN DAVID , FALCONE DANIELLE , O'BOYLE BRENDAN , MANSOOR UMAR FARUK , LIM JONGWON , METHOT JOEY L , BOYCE CHRISTOPHER , CHEN LEI , DANIELS MATTHEW H , FEVRIER SALEM , HUANG XIANHAI , KURUKULASURIYA RAVI , TONG LING , ZHOU WEI , KOZLOWSKI JOSEPH , MALETIC MILANA M , SHINKRE BIDHAN A , THATAI JAYANTH THIRUVELLORE , BAKSHI RAMAN KUMAR , KARUNAKARAN GANESH BABU
IPC分类号： A61K31/4745 , A61K9/66
CPC分类号： C07D498/18 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/16 , C07D498/14 , C07D498/16 , C07D519/00 , A61K2300/00
摘要： Disclosed are the ERK inhibitors of formula (1), having a pyrazolopyndine bas compound, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译：公开了具有吡唑并噻吩基化合物的式（1）的ERK抑制剂及其药学上可接受的盐。还公开了使用式（1）的化合物治疗癌症的方法。

6. 发明申请

WO2014179154A3 NOVEL COMPOUNDS THAT ARE ERK INHIBITORS 审中-公开
标题翻译：新的化合物是ERK抑制剂
公开(公告)号：WO2014179154A3
公开(公告)日：2015-01-29
申请号：PCT/US2014035384
申请日：2014-04-25
申请人： MERCK SHARP & DOHME , LIM JONGWON , HUANG XIANHAI , FERGUSON RONALD D , ZHOU WEI , BOYCE CHRISTOPHER W , SILIPHAIVANH PHIENG , WITTER DAVID J , MALETIC MILANA M , KOZLOWSKI JOSEPH A , WILSON KEVIN J
发明人： LIM JONGWON , HUANG XIANHAI , FERGUSON RONALD D , ZHOU WEI , BOYCE CHRISTOPHER W , SILIPHAIVANH PHIENG , WITTER DAVID J , MALETIC MILANA M , KOZLOWSKI JOSEPH A , WILSON KEVIN J
IPC分类号： A61K31/655
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
摘要翻译：公开了式（I）的ERK抑制剂及其药学上可接受的盐。还公开了使用式（I）化合物治疗癌症的方法。本发明还提供了包含有效量的至少一种式（I）化合物和药学上可接受的载体的药物组合物。本发明还提供一种药物组合物，其包含有效量的至少一种式（I）化合物和有效量的至少一种其它药物活性成分（例如化学治疗剂）和药学上可接受的载体。本发明还提供了在需要这种治疗的患者中抑制ERK的方法（即，抑制ERK2的活性），包括向所述患者施用有效量的至少一种式（I）的化合物。

7. 发明专利

AU2008269154A1 4-carboxybenzylamino derivatives as histone deacetylase inhibitors 未知
公开(公告)号：AU2008269154A1
公开(公告)日：2008-12-31
申请号：AU2008269154
申请日：2008-06-24
申请人： MERCK & CO INC
发明人： SILIPHAIVANH PHIENG , WITTER DAVID J , WILSON KEVIN J , MILLER THOMAS A , TEMPEST PAUL , OTTE KARIN M , KATTAR SOLOMON , HARRINGTON PAUL , HEIDEBRECHT RICHARD W JR
IPC分类号： A01N47/28 , A61K31/17
摘要： The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino 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 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

8. 发明专利

CA2635210A1 HYDROXYALKYLARYLAMIDE DERIVATIVES 未知
公开(公告)号：CA2635210A1
公开(公告)日：2007-08-02
申请号：CA2635210
申请日：2007-01-08
申请人： MERCK & CO INC
发明人： HEIDEBRECHT RICHARD W JR , MILLER THOMAS A , WILSON KEVIN J , GRIMM JONATHAN , WITTER DAVID J
IPC分类号： A01N43/00 , A61K31/33
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.

9. 发明专利

CA2635209A1 FLUORINATED ARYLAMIDE DERIVATIVES 未知
公开(公告)号：CA2635209A1
公开(公告)日：2007-08-02
申请号：CA2635209
申请日：2007-01-09
申请人： MERCK & CO INC
发明人： MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
IPC分类号： A61K31/38
摘要： The present invention relates to a novel class of fluorinated arylamide 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.

10. 发明专利

CA2657288A1 PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 未知
公开(公告)号：CA2657288A1
公开(公告)日：2008-01-24
申请号：CA2657288
申请日：2007-07-16
申请人： MERCK & CO INC
发明人： KATTAR SOLOMON , HEIDEBRECHT RICHARD W JR , MILLER THOMAS A , WILSON KEVIN J , TEMPEST PAUL , WITTER DAVID J , OTTE KARIN M , SILIPHAIVANH PHIENG , CLOSE JOSHUA , PETERSON SCOTT , GRIMM JONATHAN
IPC分类号： A61K31/66 , A61K31/662 , C07F9/32 , C07F9/40 , C07F9/547 , C07F9/6564
摘要： The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compou nds can also inhibit histone deacetylase and are suitable for use in selecti vely inducing terminal differentiation, and arresting cell growth and/or apo ptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patien t having a tumor characterized by proliferation of neoplastic cells. The com pounds of the invention may also be useful in the prevention and treatment o f TRX-mediated diseases, such as autoimmune, allergic and inflammatory disea ses, and in the prevention and/or treatment of diseases of the central nervo us system (CNS), such as neurodegenerative diseases. The present invention f urther provides pharmaceutical compositions comprising the phosphorus deriva tives and safe dosing regimens of these pharmaceutical compositions, which a re easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.

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