专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

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。

3. 发明授权

US08026260B2 Histone deacetylase inhibitors with aryl-pyrazolyl-motifs 有权
标题翻译：组蛋白脱乙酰酶抑制剂与芳基 - 吡唑基 - 基序
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。

4. 发明申请

US20090023718A1 Diamine and Iminodiacetic Acid Hydroxamic Acid Derivatives 审中-公开
标题翻译：二胺和亚氨基二乙酸羟肟酸衍生物
公开(公告)号：US20090023718A1
公开(公告)日：2009-01-22
申请号：US10580480
申请日：2004-11-23
申请人： Thomas A. Miller , David J. Witter , Sandro Belvedere
发明人： Thomas A. Miller , David J. Witter , Sandro Belvedere
IPC分类号： A61K31/5355 , A61K31/416 , A61K31/47 , A61K31/4965 , C07D231/54 , C07D215/38 , C07D265/30 , C07D241/04 , A61P35/00
CPC分类号： C07D211/16 , C07C259/06 , C07C2601/14 , C07D209/14 , C07D215/38 , C07D215/40 , C07D217/06 , C07D231/56 , C07D277/82 , C07D295/185 , C07D317/66
摘要： The present invention relates to a novel class of hydroxamic acid derivatives having a diamine or iminodiacetic acid backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively including terminal differentiation, arresting cell growth and/or apoptosis of neo-plastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compound of the invention are also 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：本发明涉及具有二胺或亚氨基二乙酸骨架的新一类异羟肟酸衍生物。异羟肟酸化合物可用于治疗癌症。异羟肟酸化合物还可以抑制组蛋白脱乙酰酶，并且适用于选择性地包括末端分化，阻止新塑料细胞的细胞生长和/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，例如神经变性疾病本发明进一步提供包含异羟肟酸衍生物的药物组合物，以及易于遵循的这些药物组合物的安全的给药方案，并且其在体内导致治疗有效量的异羟肟酸衍生物。

5. 发明授权

US06800633B2 Pyrrolo[2,3d]pyrimidine compositions and their use 失效
标题翻译：吡咯并[2,3d]嘧啶组合物及其用途
公开(公告)号：US06800633B2
公开(公告)日：2004-10-05
申请号：US09728229
申请日：2000-12-01
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds having the structure: wherein R1 and R2 are each independently a hydrogen atom, substituted alkyl, or a substituted or unsubstituted aryl, or alkylaryl moiety or together form a substituted or unsubstituted heterocyclic ring, provided that both R1 and R2 are both not hydrogen atoms or that neither R1 or R2 is 1-phenylethyl; R3 is a substituted or unsubstituted aryl, or alkylaryl moiety; R4 is a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety; and R5 and R6 are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, and the use of these compounds to treat a disease associated with increased levels of adenosine in a subject.
摘要翻译：本发明涉及具有以下结构的化合物：其中R 1和R 2各自独立地为氢原子，取代的烷基或取代或未取代的芳基或烷基芳基部分，或一起形成取代或未取代的杂环，条件是R 1和R 2均为不是氢原子，也不是R1或R2都是1-苯基乙基; R3是取代或未取代的芳基或烷基芳基部分; R4是氢原子或取代或未取代的烷基，芳基或烷芳基部分; 并且R 5和R 6各自独立地为卤素原子，氢原子或取代或未取代的烷基，芳基或烷基芳基部分，以及这些化合物用于治疗与受试者中腺苷水平升高相关的疾病的用途。

6. 发明申请

US20160068532A1 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：US20160068532A1
公开(公告)日：2016-03-10
申请号：US14787280
申请日：2014-04-25
申请人： Jongwon LIM , Xianhai HUANG , Ronald D. FERGUSON , Wei ZHOU , Christopher W. BOYCE , Phieng SILIPHAIVANH , David J. WITTER , Milana M. MALETIC , Joseph A. KOZLOWSKI , Kevin J. WILSON , MERCK SHARP & DOHME CORP.
发明人： Jongwon Lim , Xianhai Huang , Ronald D. Ferguson , Wei Zhou , Christopher W. Boyce , Phieng Siliphaivanh , David J. Witter , Milana M. Maletic , Joseph A. Kozlowski , Kevin J. Wilson
IPC分类号： C07D487/04 , C07D471/14 , C07D471/04
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学活性成分（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（即，抑制ERK2的活性）的方法，包括向所述患者施用有效量的至少一种式（I）化合物。

7. 发明授权

US07981874B2 Phosphorus derivatives as histone deacetylase inhibitors 失效
标题翻译：磷衍生物作为组蛋白脱乙酰酶抑制剂
公开(公告)号：US07981874B2
公开(公告)日：2011-07-19
申请号：US12309459
申请日：2007-07-16
申请人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, Jr. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
发明人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, Jr. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/662 , A61K31/683 , A61K31/67 , A61K31/675 , A61K31/4747 , A61K31/4545 , A61K31/4436 , A61K31/415 , A61K31/427 , C07F9/28 , C07F9/53 , C07F9/40 , C07F9/32 , C07F9/6571 , C07F9/6584 , C07D333/20 , C07D277/50 , C07D231/40 , C07D221/20 , C07F9/58 , C07F9/59
CPC分类号： C07F9/655345 , C07F9/5304 , C07F9/5325 , C07F9/65031 , 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：本发明涉及一类新型的磷衍生物。磷化合物可用于治疗癌症。磷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磷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磷衍生物。

8. 发明申请

US20110130361A1 SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：硅酮衍生物作为脱乙酰壳多糖抑制剂
公开(公告)号：US20110130361A1
公开(公告)日：2011-06-02
申请号：US12672441
申请日：2008-08-05
申请人： Jonathan Grimm , Richard W. Heidebrecht, JR. , Dawn M. Mampreian , Joey L. Methot , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Kevin J. Wilson , David J. Witter
发明人： Jonathan Grimm , Richard W. Heidebrecht, JR. , Dawn M. Mampreian , Joey L. Methot , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/695 , C07C271/28 , C07D333/22 , C07D209/32 , C07F7/02 , A61K31/24 , A61K31/381 , A61K31/4015 , A61P35/00
CPC分类号： C07F7/0812
摘要： The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon 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 Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo.
摘要翻译：本发明涉及一类新型的硅衍生物。硅化合物可用于治疗癌症。硅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疾病（CNS），例如神经退行性疾病本发明还提供包含硅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硅衍生物。

9. 发明授权

US07795304B2 Histone deacetylase inhibitors 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US07795304B2
公开(公告)日：2010-09-14
申请号：US11660718
申请日：2005-08-22
申请人： Sandro Belvedere , Christopher Laurence Hamblett , Thomas A. Miller , David J. Witter , Jiaming Yan
发明人： Sandro Belvedere , Christopher Laurence Hamblett , Thomas A. Miller , David J. Witter , Jiaming Yan
IPC分类号： C07C271/20 , C07D295/088 , C07D277/46 , C07D213/30 , A61K31/5375 , A61K31/4402 , A61K31/4168 , A61K31/40 , A61K31/325
CPC分类号： C07D295/088 , C07C271/22 , C07D277/46
摘要： The invention relates to hydroxamic acid derivatives having carbamate linkage with the structural formula that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous systems (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.
摘要翻译：本发明涉及具有结构式的具有氨基甲酸酯键的异羟肟酸衍生物，其为组蛋白脱乙酰酶（HDAC）的抑制剂，可用于预防和/或治疗细胞增殖性疾病，例如癌症，自身免疫性，过敏性和炎性疾病，中枢神经系统疾病（CNS）如神经变性疾病，以及预防和/或治疗再狭窄。

10. 发明申请

US20090270351A1 PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 失效
标题翻译：作为组蛋白脱乙酰酶抑制剂的磷酸衍生物
公开(公告)号：US20090270351A1
公开(公告)日：2009-10-29
申请号：US12309459
申请日：2007-07-16
申请人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
发明人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/675 , A61K31/67 , C07F9/28 , C07D333/04
CPC分类号： C07F9/655345 , C07F9/5304 , C07F9/5325 , C07F9/65031 , 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：本发明涉及一类新型的磷衍生物。磷化合物可用于治疗癌症。磷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疾病（CNS），例如神经退行性疾病本发明进一步提供包含磷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磷衍生物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式