公开(公告)号：US20210188863A1

公开(公告)日：2021-06-24

申请号：US16755172

申请日：2018-10-08

申请人： David Annunziato CANDITO ,  Thomas, H. GRAHAM ,  John ACTON ,  Ryan Wing-Kun CHAU ,  Joanna L. CHEN ,  J. Michael ELLIS ,  Peter H. FULLER ,  Anmol GULATI ,  Hakan GUNAYDIN ,  Solomon KATTAR ,  Mitchell Henry KEYLOR ,  Blair T. LAPOINTE ,  Ping LIU ,  Weiguo LIU ,  Joey L. METHOT ,  Santhosh F. NEELAMKAVIL ,  Vladimir SIMOV ,  Ling TONG ,  Harold B. WOOD ,  Merck Sharp & Dohme Corp.

发明人： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC分类号： C07D491/10 ,  C07D403/14 ,  C07D487/08 ,  C07D405/14 ,  C07D401/14 ,  C07D413/14 ,  C07D498/10 ,  C07D519/00 ,  C07D498/04 ,  C07D403/04

摘要： The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US08389553B2

公开(公告)日：2013-03-05

申请号：US12666384

申请日：2008-06-24

申请人： Paul Harrington ,  Solomon Kattar ,  Thomas A. Miller ,  Matthew G. Stanton ,  Paul Tempest ,  David J. Witter

发明人： Paul Harrington ,  Solomon Kattar ,  Thomas A. Miller ,  Matthew G. Stanton ,  Paul Tempest ,  David J. Witter

IPC分类号： A01N43/40 ,  A01N47/10 ,  A61K31/44 ,  A61K31/27 ,  C07D213/55 ,  C07D213/00 ,  C07D211/30 ,  C07D211/32 ,  C07D217/00

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.

公开(公告)号：US20110207711A1

公开(公告)日：2011-08-25

申请号：US13057325

申请日：2009-07-27

申请人： Jason Katz ,  James Jewell ,  Joon Jung ,  Solomon Kattar ,  Yongquan Hou ,  Rachel MacCoss ,  Satoru Ito

发明人： Jason Katz ,  James Jewell ,  Joon Jung ,  Solomon Kattar ,  Yongquan Hou ,  Rachel MacCoss ,  Satoru Ito

IPC分类号： A61K31/397 ,  C07D471/04 ,  A61K31/437 ,  C07D403/14 ,  A61K31/496 ,  C07D413/14 ,  A61K31/5377 ,  C07D401/14 ,  A61K31/517 ,  A61K31/5386 ,  A61P35/00 ,  A61P25/28 ,  A61P19/02 ,  A61P3/10 ,  A61P1/00

CPC分类号： A61K45/06 ,  A61K31/535 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.

摘要翻译： 本发明涉及作为激酶PDK1的抑制剂的吡唑并吡啶和咪唑并吡啶，因此可用于治疗骨髓增生性疾病或癌症。 该化合物也可用作其它激酶如FGFR3，NTRK3，RP-S6K和WEE1的抑制剂。 此外，本发明化合物还选择性地抑制微管亲和调节激酶（MARK），因此可用于治疗或预防阿尔茨海默氏病。

公开(公告)号：US11161854B2

公开(公告)日：2021-11-02

申请号：US16755172

申请日：2018-10-08

申请人： Merck Sharp & Dohme Corp. ,  David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

发明人： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC分类号： C07D491/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/08 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

摘要： The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US08551984B2

公开(公告)日：2013-10-08

申请号：US12968608

申请日：2010-12-15

申请人： Michael D. Altman ,  Brian M. Andresen ,  Kenneth L. Arrington ,  Jason Burch ,  Kaleen Konrad Childers ,  Bernard Cote ,  Maria Emilia Di Francesco ,  Anthony Donofrio ,  Kristina Dupont-Gaudet ,  John Michael Ellis ,  Christian Fischer ,  Daniel Guay ,  David Joseph Guerin ,  Andrew M. Haidle ,  Solomon Kattar ,  Sandra Lee Knowles ,  Chaomin Li ,  Jongwon Lim ,  Michelle R. Machacek ,  Alan B. Northrup ,  Brendan M. O'Boyle ,  Ryan D. Otte ,  Michael H. Reutershan ,  Eric Romeo ,  Adam J. Schell ,  Tony Siu ,  Kerrie B. Spencer ,  Brandon M. Taoka ,  B. Wesley Trotter ,  Hua Zhou

发明人： Michael D. Altman ,  Brian M. Andresen ,  Kenneth L. Arrington ,  Jason Burch ,  Kaleen Konrad Childers ,  Bernard Cote ,  Maria Emilia Di Francesco ,  Anthony Donofrio ,  Kristina Dupont-Gaudet ,  John Michael Ellis ,  Christian Fischer ,  Daniel Guay ,  David Joseph Guerin ,  Andrew M. Haidle ,  Solomon Kattar ,  Sandra Lee Knowles ,  Chaomin Li ,  Jongwon Lim ,  Michelle R. Machacek ,  Alan B. Northrup ,  Brendan M. O'Boyle ,  Ryan D. Otte ,  Michael H. Reutershan ,  Eric Romeo ,  Adam J. Schell ,  Tony Siu ,  Kerrie B. Spencer ,  Brandon M. Taoka ,  B. Wesley Trotter ,  Hua Zhou

IPC分类号： C07D417/12 ,  A61K31/497

CPC分类号： C07D417/12 ,  C07D417/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  C07D495/04 ,  C07F9/65583

摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.

摘要翻译： 本发明提供了新颖的式（I）嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎。

公开(公告)号：US08158825B2

公开(公告)日：2012-04-17

申请号：US11922740

申请日：2006-06-21

申请人： Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, Jr. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

发明人： Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, Jr. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

IPC分类号： C07C233/02 ,  C07C255/60 ,  C07C311/46 ,  C07C311/08 ,  C07C235/84 ,  A61K31/519 ,  A61K31/44 ,  C07D265/30 ,  C07D495/04 ,  C07D215/06 ,  C07D211/06 ,  C07D213/82

CPC分类号： C07C235/78 ,  C07C233/75 ,  C07C233/80 ,  C07C235/42 ,  C07C235/56 ,  C07C235/74 ,  C07C235/84 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C311/46 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/327 ,  C07D209/14 ,  C07D209/20 ,  C07D211/06 ,  C07D213/40 ,  C07D213/56 ,  C07D213/82 ,  C07D215/06 ,  C07D215/12 ,  C07D215/40 ,  C07D231/40 ,  C07D249/08 ,  C07D261/14 ,  C07D265/30 ,  C07D277/28 ,  C07D277/46 ,  C07D277/56 ,  C07D295/135 ,  C07D295/155 ,  C07D295/185 ,  C07D307/68 ,  C07D319/16 ,  C07D319/18 ,  C07D333/20 ,  C07D333/38 ,  C07D333/70 ,  C07D413/14 ,  C07D495/04

摘要： The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate 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 modified malonate derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the modified malonate derivatives in vivo.

摘要翻译： 本发明涉及一类新型改性丙二酸衍生物。 修饰的丙二酸酯化合物可用于治疗癌症。 修饰的丙二酸酯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 本发明还提供包含改性丙二酸酯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修饰的丙二酸酯衍生物。

公开(公告)号：US08026260B2

公开(公告)日：2011-09-27

申请号：US12084268

申请日：2006-10-30

申请人： Joshua Close ,  Richard W. Heidebrecht, Jr. ,  Solomon Kattar ,  Thomas A. Miller ,  David Sloman ,  Matthew G Stanton ,  Paul Tempest ,  David J. Witter

发明人： Joshua Close ,  Richard W. Heidebrecht, Jr. ,  Solomon Kattar ,  Thomas A. Miller ,  David Sloman ,  Matthew G Stanton ,  Paul Tempest ,  David J. Witter

IPC分类号： A61K31/4439 ,  A61K31/415 ,  A61K31/423 ,  A61K31/425 ,  A61K31/4245 ,  C07D401/02 ,  C07D271/10 ,  C07D277/20 ,  C07D231/10

CPC分类号： C07D401/12 ,  C07D231/40 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention 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 present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.

摘要翻译： 本发明涉及新一类具有芳基 - 吡唑基基序的组蛋白脱乙酰酶抑制剂。 本发明的化合物可用于治疗癌症。 本发明的化合物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。 本发明进一步提供包含本发明化合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本发明化合物。

公开(公告)号：US20100160327A1

公开(公告)日：2010-06-24

申请号：US11922740

申请日：2006-06-21

申请人： Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, JR. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

发明人： Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, JR. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

IPC分类号： A61K31/5375 ,  A61K31/519 ,  A61K31/47 ,  A61K31/4453 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/426 ,  A61K31/42 ,  A61K31/4196 ,  A61K31/404 ,  A61K31/402 ,  A61K31/381 ,  A61K31/357 ,  A61K31/34 ,  A61K31/277 ,  A61K31/18 ,  A61K31/167 ,  C07D265/30 ,  C07D495/04 ,  C07D215/06 ,  C07D211/06 ,  C07D213/82 ,  C07D213/56 ,  C07D277/46 ,  C07D277/56 ,  C07D261/14 ,  C07D249/08 ,  C07D209/20 ,  C07D207/327 ,  C07D333/70 ,  C07D319/16 ,  C07D307/68 ,  C07C255/60 ,  C07C311/46 ,  C07C311/08 ,  C07C235/84 ,  A61P35/00

CPC分类号： C07C235/78 ,  C07C233/75 ,  C07C233/80 ,  C07C235/42 ,  C07C235/56 ,  C07C235/74 ,  C07C235/84 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C311/46 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/327 ,  C07D209/14 ,  C07D209/20 ,  C07D211/06 ,  C07D213/40 ,  C07D213/56 ,  C07D213/82 ,  C07D215/06 ,  C07D215/12 ,  C07D215/40 ,  C07D231/40 ,  C07D249/08 ,  C07D261/14 ,  C07D265/30 ,  C07D277/28 ,  C07D277/46 ,  C07D277/56 ,  C07D295/135 ,  C07D295/155 ,  C07D295/185 ,  C07D307/68 ,  C07D319/16 ,  C07D319/18 ,  C07D333/20 ,  C07D333/38 ,  C07D333/70 ,  C07D413/14 ,  C07D495/04

摘要： The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate 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 modified malonate derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the modified malonate derivatives in vivo.

摘要翻译： 本发明涉及一类新型改性丙二酸衍生物。 修饰的丙二酸酯化合物可用于治疗癌症。 修饰的丙二酸酯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 本发明还提供包含改性丙二酸酯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修饰的丙二酸酯衍生物。

公开(公告)号：US20100160309A1

公开(公告)日：2010-06-24

申请号：US12530648

申请日：2008-03-10

申请人： Tony Siu ,  Jonathan Young ,  Micheal Altman ,  Alan Northrup ,  Ekaterina Kozina ,  Christopher Dinsmore ,  David J. Guerin ,  Kevin A. Keenan ,  Joon O. Jung ,  Solomon Kattar ,  Rachel N. MacCoss

发明人： Tony Siu ,  Jonathan Young ,  Micheal Altman ,  Alan Northrup ,  Ekaterina Kozina ,  Christopher Dinsmore ,  David J. Guerin ,  Kevin A. Keenan ,  Joon O. Jung ,  Solomon Kattar ,  Rachel N. MacCoss

IPC分类号： A61K31/4375 ,  C07D471/04 ,  C07D471/14 ,  A61P35/00 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/506

CPC分类号： C07D471/04 ,  C07D471/14

摘要： The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.

摘要翻译： 本发明提供抑制JAK2酪氨酸激酶和/或PDK1的化合物。 本发明还提供了包含这种抑制化合物的组合物以及通过将该化合物给予需要治疗或预防骨髓增生性疾病或癌症的患者来抑制JAK2酪氨酸激酶活性和/或PDK1激酶抑制活性的方法。

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。