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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。
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公开(公告)号:US20090291965A1
公开(公告)日:2009-11-26
申请号:US12084268
申请日:2006-10-30
申请人: Joshua Close , Richard W. Heidebrecht , Solomon Kattar , Thomas A. Miller , David Sloman , Matthew G. Stanton , Paul Tempest , David J. Witter
发明人: Joshua Close , Richard W. Heidebrecht , Solomon Kattar , Thomas A. Miller , David Sloman , Matthew G. Stanton , Paul Tempest , David J. Witter
IPC分类号: A61K31/496 , C07D401/02 , A61K31/4439 , C07D231/10 , A61K31/415 , C07D271/10 , A61K31/4245 , C07D403/14 , A61P35/00
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。
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公开(公告)号:US20070117824A1
公开(公告)日:2007-05-24
申请号:US11600426
申请日:2006-11-16
申请人: Scott Berk , Joshua Close , Christopher Hamblett , Richard Heidebrecht , Solomon Kattar , Laura Kliman , Dawn Mampreian , Joey Methot , Thomas Miller , David Sloman , Matthew Stanton , Paul Tempest , Anna Zabierek
发明人: Scott Berk , Joshua Close , Christopher Hamblett , Richard Heidebrecht , Solomon Kattar , Laura Kliman , Dawn Mampreian , Joey Methot , Thomas Miller , David Sloman , Matthew Stanton , Paul Tempest , Anna Zabierek
IPC分类号: A61K31/4747 , C07D471/10
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。
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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。
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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。
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公开(公告)号:US20150266895A1
公开(公告)日:2015-09-24
申请号:US14431462
申请日:2013-09-26
申请人: Kevin J. WILSON , David J. WITTER , Phieng SILIPHAIVANH , Kathryn KIPFORD , David SLOMAN , Danielle FALCONE , Brendan O'BOYLE , Umar Faruk MANSOOR , Jongwon LIM , Joey L. METHOT , Christopher BOYCE , Lei CHEN , Matthew H. DANIELS , Salem FEVRIER , Xianhai HUANG , Ravi KURUKULASURIYA , Ling TONG , Wei ZHOU , Joseph KOZLOWSKI , Milana M. MALETIC , Bidhan A. SHINKRE , Jayanth Thiruvellore THATAI , Raman Kumar BAKSHI , Ganesh Babu KARUNAKARAN , MERCK SHARP & DOHME CORP.
发明人: Kevin J. Wilson , David J. Witter , Phieng Siliphaivanh , Kathryn Lipford , David Sloman , Danielle Falcone , Brendan O'Boyle , Umar Faruk Mansoor , Jongwon Lim , Joey L. Methot , Christopher Boyce , Lei Chen , Matthew H. Daniels , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Ling Tong , Wei Zhou , Joseph Kozlowski , Milana M. Maletic , Bidhan A. Shinkre , Jayanth Thiruvellore Thatai , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号: C07D498/18 , A61K31/437 , A61K31/5377 , A61K31/496 , A61K45/06 , A61K31/4375 , C07D498/14 , A61K31/553 , C07D519/00 , C07D471/04 , C07D471/14
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): 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。
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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。
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