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1. 发明授权

US10442819B2 Tricyclic compounds as inhibitors of mutant IDH enzymes 有权
公开(公告)号：US10442819B2
公开(公告)日：2019-10-15
申请号：US15532549
申请日：2015-12-01
申请人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
IPC分类号： A61K31/351 , A61K31/4353 , A61K31/5355 , A61K31/551 , C07D471/04 , C07D471/14 , C07D498/08 , C07D471/08 , C07D498/04 , C07D498/10 , A01N43/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

2. 发明授权

US09023865B2 Compounds that are ERK inhibitors 有权
标题翻译： ERK抑制剂的化合物
公开(公告)号：US09023865B2
公开(公告)日：2015-05-05
申请号：US14353381
申请日：2012-10-25
申请人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
发明人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
IPC分类号： C07D401/14 , A61K31/437 , C07D471/04 , C07D519/00 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (1): 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。

3. 发明申请

US20090082308A1 Benzothiophene derivatives 有权
标题翻译：苯并噻吩衍生物
公开(公告)号：US20090082308A1
公开(公告)日：2009-03-26
申请号：US11918913
申请日：2006-04-14
申请人： Jed Lee Hubbs , Dawn M. Mampreian , Joey L. Methot , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , David L. Sloman , Matthew G. Stanton , Kevin J. Wilson , David J. Witter
发明人： Jed Lee Hubbs , Dawn M. Mampreian , Joey L. Methot , Thomas A. Miller , Karin M. Otte , Phieng Siliphaivanh , David L. Sloman , Matthew G. Stanton , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/695 , C07D333/56 , A61K31/381 , C07D409/12 , A61K31/4709 , C07D409/10 , A61K31/4025 , C07D409/06 , A61K31/496 , C07D413/12 , A61P25/00 , A61P35/00 , A61K31/4155 , A61K31/506 , C07F7/08 , A61K31/5377 , C07D409/14 , A61K31/4178 , A61K31/404 , A61K31/4436 , A61K31/4245 , A61K31/4192
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

US20090209566A1 Spirocyclic Compounds 有权
标题翻译：螺环化合物
公开(公告)号：US20090209566A1
公开(公告)日：2009-08-20
申请号：US12085396
申请日：2006-11-17
申请人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
发明人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
IPC分类号： A61K31/438 , C07D471/10 , C07D491/107 , C07D498/10 , C07D487/10 , A61K31/4439 , A61K31/506 , A61P35/00
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin 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：本发明涉及由下列结构式表示的新一类取代的螺环化合物：其中A，B和D独立地选自CR12，NR1a，C（O）和O; E选自键，CR12，NR1a，C（O）和O; 其中A，B，D或E中的至少一个为CR 12; 并且条件是当A为O时，则E不为O; G是CR12; R选自NH 2和OH; 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疾病（CNS），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。

5. 发明申请

US20170267695A1 ERK INHIBITORS 有权
公开(公告)号：US20170267695A1
公开(公告)日：2017-09-21
申请号：US15531771
申请日：2015-12-10
申请人： Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
发明人： Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
IPC分类号： C07D498/18 , C07D471/22 , C07D471/18
CPC分类号： C07D498/18 , A61K31/437 , A61K31/444 , C07D471/18 , C07D471/22
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting 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). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).

6. 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。

7. 发明申请

US20090012075A1 Fluorinated Arylamide Derivatives 审中-公开
标题翻译：氟化芳酰胺衍生物
公开(公告)号：US20090012075A1
公开(公告)日：2009-01-08
申请号：US12087624
申请日：2007-01-08
申请人： Thomas A. Miller , David L. Sloman , Matthew G. Stanton , Kevin J. Wilson , David J. Witter
发明人： Thomas A. Miller , David L. Sloman , Matthew G. Stanton , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/381 , C07D409/12 , C07D333/50 , C07D409/14 , C07D413/10 , C07D413/14 , A61K31/4436 , A61K31/5377 , A61K31/4025 , A61K31/4245 , A61P35/00 , A61K31/415 , A61K31/496
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。

8. 发明授权

US07834026B2 Spirocyclic compounds 有权
标题翻译：螺环化合物
公开(公告)号：US07834026B2
公开(公告)日：2010-11-16
申请号：US12085396
申请日：2006-11-17
申请人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
发明人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
IPC分类号： A01N43/42 , A01N43/12 , A01N43/26 , A61K31/44 , A61K31/34 , A61K31/335 , C07D237/00 , C07D239/00 , C07D241/00 , C07D491/10 , C07D491/20 , C07D495/10 , C07D495/20 , C07D497/10 , C07D497/20 , C07D311/96 , C07D313/06 , C07D313/20 , C07D315/00
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin 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：本发明涉及由下列结构式表示的新一类取代的螺环化合物：其中A，B和D独立地选自CR12，NR1a，C（O）和O; E选自键，CR12，NR1a，C（O）和O; 其中A，B，D或E中的至少一个为CR 12; 并且条件是当A为O时，则E不为O; G是CR12; R选自NH 2和OH; 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，并且其在体内产生治疗有效量的这些化合物。

9. 发明授权

US07544695B2 Spirocyclic compounds 有权
标题翻译：螺环化合物
公开(公告)号：US07544695B2
公开(公告)日：2009-06-09
申请号：US11600426
申请日：2006-11-16
申请人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
发明人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
IPC分类号： A61K31/438 , C07D498/10
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to a novel class of substituted 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.
摘要翻译：本发明涉及一类新的取代的螺环化合物。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。

10. 发明授权

US10975084B2 KDM5 inhibitors 有权
公开(公告)号：US10975084B2
公开(公告)日：2021-04-13
申请号：US16341313
申请日：2017-10-06
申请人： Merck Sharp & Dohme Corp. , Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
发明人： Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.

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