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1. 发明申请

US20150258074A1 NOVEL COMPOUNDS THAT ARE ERK INHIBITORS 有权
标题翻译：新的化合物是ERK抑制剂
公开(公告)号：US20150258074A1
公开(公告)日：2015-09-17
申请号：US14431485
申请日：2013-09-26
申请人： Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
发明人： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
CPC分类号： A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
摘要翻译：公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。还公开了使用式（1.0）化合物治疗癌症的方法。

2. 发明授权

US08999957B2 Heterocyclic compounds as ERK inhibitors 有权
标题翻译：杂环化合物作为ERK抑制剂
公开(公告)号：US08999957B2
公开(公告)日：2015-04-07
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, Jr. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, Jr. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D401/14 , C07D405/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07F7/18
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译：本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。这些化合物是ERK抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

3. 发明申请

US20100324046A1 4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权
标题翻译： 4-羧基苯甲酰胺衍生物作为脱乙酰壳多糖酶抑制剂
公开(公告)号：US20100324046A1
公开(公告)日：2010-12-23
申请号：US12666384
申请日：2008-06-24
申请人： Paul Harrington , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , Paul Tempest , Kevin J. Wilson , David J. Witter
发明人： Paul Harrington , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , Paul Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/5375 , C07D213/56 , C07D401/12 , C07D409/12 , C07C271/22 , C07C237/40 , C07D333/24 , C07D213/74 , C07D231/12 , C07D277/30 , C07D233/61 , C07D207/09 , C07D241/04 , C07D265/30 , C07D211/34 , C07D217/04 , C07D209/44 , C07D207/14 , C07D307/22 , C07D263/22 , C07D249/04 , A61K31/4406 , A61K31/444 , A61K31/4436 , A61K31/27 , A61K31/167 , A61K31/381 , A61K31/4025 , A61K31/4409 , A61K31/415 , A61K31/426 , A61K31/4174 , A61K31/40 , A61K31/4965 , A61K31/4453 , A61K31/472 , A61K31/4035 , A61K31/341 , A61K31/4439 , A61K31/421 , A61K31/4192 , A61P35/00
CPC分类号： C07D295/155 , C07C237/40 , C07C237/42 , C07C271/22 , C07C271/38 , C07C271/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/14 , C07D207/16 , C07D209/44 , C07D209/48 , C07D211/14 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/74 , C07D217/04 , C07D231/12 , C07D233/64 , C07D241/12 , C07D263/20 , C07D277/28 , C07D295/125 , C07D307/22 , C07D333/10 , C07D333/20 , C07D401/04 , C07D409/12 , C07D413/12
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.
摘要翻译：本发明涉及一类新的4-羧基苄基氨基衍生物。 4-羧基苄基氨基化合物可用于治疗癌症。 4-羧基苄基氨基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4-羧基苄基氨基衍生物和这些药物组合物的安全投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4-羧基苄基氨基衍生物。

4. 外观设计

USD272290S Fixture cleaner 失效
公开(公告)号：USD272290S
公开(公告)日：1984-01-17
申请号：US246996
申请日：1981-03-24
申请人： Kevin J. Wilson
设计人： Kevin J. Wilson

5. 发明授权

US09200002B2 Compositions useful for treating disorders related to KIT 有权
标题翻译：用于治疗与KIT有关的疾病的组合物
公开(公告)号：US09200002B2
公开(公告)日：2015-12-01
申请号：US14515327
申请日：2014-10-15
申请人： Brian L. Hodous , Joseph L. Kim , Kevin J. Wilson , Douglas Wilson , Yulian Zhang
发明人： Brian L. Hodous , Joseph L. Kim , Kevin J. Wilson , Douglas Wilson , Yulian Zhang
IPC分类号： C07D487/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , A61K31/495 , A61K31/54 , A61P35/00 , A61K31/53 , A61K31/5377 , A61K45/06
CPC分类号： C07D487/04 , A61K31/496 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要： Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
摘要翻译：本文描述了可用于治疗与突变型KIT相关的病症的化合物和组合物。

6. 发明授权

US09096559B2 4-carboxybenzylamino derivatives as histone deacetylase inhibitors 有权
标题翻译： 4-羧基苄基氨基衍生物作为组蛋白脱乙酰酶抑制剂
公开(公告)号：US09096559B2
公开(公告)日：2015-08-04
申请号：US13751789
申请日：2013-01-28
申请人： Paul Harrington , Richard W. Heidebrecht, Jr. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , Matthew G. Stanton , Paul Tempest , Kevin J. Wilson , David J. Witter
发明人： Paul Harrington , Richard W. Heidebrecht, Jr. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , Matthew G. Stanton , Paul Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： C07D333/10 , C07C235/76 , C07C235/84 , C07D295/155 , C07C237/40 , C07C237/42 , C07C271/22 , C07C271/38 , C07C271/54 , C07D207/08 , C07D207/14 , C07D207/16 , C07D209/44 , C07D209/48 , C07D211/14 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/74 , C07D217/04 , C07D231/12 , C07D233/64 , C07D241/12 , C07D263/20 , C07D277/28 , C07D295/125 , C07D307/22 , C07D333/20 , C07D401/04 , C07D409/12 , C07D413/12 , C07D213/55
CPC分类号： C07D295/155 , C07C237/40 , C07C237/42 , C07C271/22 , C07C271/38 , C07C271/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/14 , C07D207/16 , C07D209/44 , C07D209/48 , C07D211/14 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/74 , C07D217/04 , C07D231/12 , C07D233/64 , C07D241/12 , C07D263/20 , C07D277/28 , C07D295/125 , C07D307/22 , C07D333/10 , C07D333/20 , C07D401/04 , C07D409/12 , C07D413/12
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.
摘要翻译：本发明涉及一类新的4-羧基苄基氨基衍生物。 4-羧基苄基氨基化合物可用于治疗癌症。 4-羧基苄基氨基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4-羧基苄基氨基衍生物和这些药物组合物的安全投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4-羧基苄基氨基衍生物。

7. 发明申请

US20130137690A1 4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： 4-羧基苯甲酰胺衍生物作为脱乙酰壳多糖酶抑制剂
公开(公告)号：US20130137690A1
公开(公告)日：2013-05-30
申请号：US13751789
申请日：2013-01-28
申请人： Paul Harrington , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , Matthew G. Stanton , Paul Tempest , Kevin J. Wilson , David J. Witter
发明人： Paul Harrington , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , Matthew G. Stanton , Paul Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： C07D295/155 , A61K31/5377 , C07D213/55 , C07D403/02 , C07D413/14 , A61K31/496 , C07D409/14
CPC分类号： C07D295/155 , C07C237/40 , C07C237/42 , C07C271/22 , C07C271/38 , C07C271/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/14 , C07D207/16 , C07D209/44 , C07D209/48 , C07D211/14 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/74 , C07D217/04 , C07D231/12 , C07D233/64 , C07D241/12 , C07D263/20 , C07D277/28 , C07D295/125 , C07D307/22 , C07D333/10 , C07D333/20 , C07D401/04 , C07D409/12 , C07D413/12
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.
摘要翻译：本发明涉及一类新的4-羧基苄基氨基衍生物。 4-羧基苄基氨基化合物可用于治疗癌症。 4-羧基苄基氨基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4-羧基苄基氨基衍生物和这些药物组合物的安全投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4-羧基苄基氨基衍生物。

8. 发明申请

US20130096084A1 NOVEL HETEROCYCLIC COMPOUNDS AS ERK INHBITORS 有权
标题翻译：新型杂环化合物作为ERK抑制剂
公开(公告)号：US20130096084A1
公开(公告)日：2013-04-18
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/14 , A61K45/06 , C07D405/14 , A61K31/454 , A61K31/55 , A61K31/551 , C07D401/12 , C07D409/14 , C07D417/14 , A61K31/506 , C07D471/04 , C07F7/18 , A61K31/695 , C07D413/14 , A61K31/5377 , A61K31/4545
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译：本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。这些化合物是ERK抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

9. 发明授权

US07834034B2 Benzothiophene derivatives 有权
标题翻译：苯并噻吩衍生物
公开(公告)号：US07834034B2
公开(公告)日：2010-11-16
申请号：US11918913
申请日：2006-04-14
申请人： Dawn M. Mampreian , Thomas A. Miller , David L. Sloman , Matthew G. Stanton , Kevin J. Wilson , David J. Witter
发明人： Dawn M. Mampreian , Thomas A. Miller , David L. Sloman , Matthew G. Stanton , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/445 , C07D409/12
CPC分类号： C07D333/70 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14
摘要： The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide 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 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的苯并噻吩酰胺衍生物。异羟肟酸化合物可用于治疗癌症。苯并噻吩酰胺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。

10. 发明申请

US20090062297A1 Hydroxyalkylarylamide Derivatives 审中-公开
标题翻译：羟烷基芳基酰胺衍生物
公开(公告)号：US20090062297A1
公开(公告)日：2009-03-05
申请号：US12087623
申请日：2007-01-08
申请人： Richard W. Heidebrecht , Thomas A. Miller , Kevin J. Wilson , David J. Witter , Jonathan Grimm
发明人： Richard W. Heidebrecht , Thomas A. Miller , Kevin J. Wilson , David J. Witter , Jonathan Grimm
IPC分类号： A61K31/496 , C07D333/24 , A61K31/381 , A61K31/422 , C07D413/12 , C07D333/70
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，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。

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