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![4-heterocyclo-pyrrolo[2,3d] pyrimidine compositions and their use](/abs-image/US/2008/09/30/US07429574B2/abs.jpg.150x150.jpg)
31.发明授权公开(公告)号：US07429574B2
公开(公告)日：2008-09-30
申请号：US10816329
申请日：2004-03-31
IPC分类号： C07F9/02 , C07D487/04 , A61K31/519 , A61K31/685 , A61P11/06 , A61P11/08 , A61P7/12 , A61P11/00 , A61P9/00
CPC分类号： C07D487/04 , A61K31/519
摘要： Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.
摘要翻译： 公开了可用于治疗腺苷受体刺激的疾病的新型脱氮嘌呤。
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![4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof](/abs-image/US/2003/12/16/US06664252B2/abs.jpg.150x150.jpg)
32.发明授权4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof 失效对腺苷A2a受体特异性的4-氨基吡咯并[2,3-d]嘧啶化合物及其用途公开(公告)号：US06664252B2
公开(公告)日：2003-12-16
申请号：US09728607
申请日：2000-12-01
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： This invention pertains to compounds having the structure: wherein NR1R2 is a substituted or unsubstituted 4-8 membered ring; wherein R3 is a substituted or unsubstituted four to six membered ring; wherein R5 is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl; wherein R6 is H, alkyl, substituted alkyl, or cycloalkyl; with the proviso that NR1R2 is not 3-acetamido piperadino, 3-hydroxy pyrrolidino, 3-methyloxy carbonylmethyl pyrolidino, or 3-aminocarbonylmethyl pyrrolidino; with the proviso that NR1R2 is 3-hydroxymethyl piperadino only when R3 is 4-pyridyl; which specifically inhibit the adenosine A2a receptor and the use of these compounds to treat a disease associated with A2a adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译： 本发明涉及具有以下结构的化合物：其中NR1R2是取代或未取代的4-8元环; 其中R3是取代或未取代的四至六元环; 其中R 5是H，烷基，取代的烷基，芳基，芳基烷基，氨基，取代的芳基; 其中R6是H，烷基，取代的烷基或环烷基; 条件是NR1R2不是3-乙酰氨基哌啶子基，3-羟基吡咯烷子基，3-甲氧羰基甲基吡咯烷基或3-氨基羰基甲基吡咯烷子基; 条件是仅当R 3是4-吡啶基时，NR 1 R 2是3-羟甲基哌啶子基; 其特异性抑制腺苷A2a受体以及这些化合物用于治疗受试者中与A2a腺苷受体相关的疾病的用途，其包括向受试者施用治疗有效量的化合物。
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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。
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![Pyrrolo[2,3d]pyrimidine compositions and their use](/abs-image/US/2009/03/26/US20090082369A1/abs.jpg.150x150.jpg)
公开(公告)号：US20090082369A1
公开(公告)日：2009-03-26
申请号：US12228867
申请日：2008-08-15
IPC分类号： A61K31/519 , C07D487/04 , A61P9/00 , A61P25/00
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds having the structure: wherein R1 and R2 together form a substituted or unsubstituted heterocyclic ring; R3 is a substituted or unsubstituted aryl moiety; R4 is a hydrogen atom, an unsubstituted alkyl, or a substituted or unsubstituted aryl moiety; and R5 and R6 are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, or a pharmaceutically acceptable salt thereof, 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R1和R2一起形成取代或未取代的杂环; R3是取代或未取代的芳基部分; R4是氢原子，未取代的烷基或取代或未取代的芳基部分; 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或其药学上可接受的盐，以及这些化合物用于治疗与腺苷水平升高相关的疾病的用途 在一个主题
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公开(公告)号：US20090069391A1
公开(公告)日：2009-03-12
申请号：US11918912
申请日：2006-04-14
申请人： Jed Lee Hubbs , Sam Kattar , Joey Methot , Thomas Miller , Phieng Siliphaivanh , Matthew Stanton , Kevin Wilson , David J. Witter
发明人： Jed Lee Hubbs , Sam Kattar , Joey Methot , Thomas Miller , Phieng Siliphaivanh , Matthew Stanton , Kevin Wilson , David J. Witter
IPC分类号： A61K31/381 , C07D333/52 , A61K31/4245 , A61P25/00 , A61P35/00 , C07D271/10
CPC分类号： C07D333/70 , A61K31/38 , A61K31/381 , A61K31/41
摘要： The present invention relates to a novel class of hydroxamic acid derivatives. 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 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 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： 本发明涉及一类新型异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸化合物也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，例如神经变性 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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公开(公告)号：US06680324B2
公开(公告)日：2004-01-20
申请号：US10000280
申请日：2001-11-30
IPC分类号： A61K31505
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
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公开(公告)号：US06680322B2
公开(公告)日：2004-01-20
申请号：US09728316
申请日：2000-12-01
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/505 , A61K2300/00
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
摘要翻译： 本发明涉及特异性抑制腺苷A1受体的化合物以及这些化合物用于治疗受试者中与腺苷受体A1相关的疾病的用途。
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公开(公告)号：US06686366B1
公开(公告)日：2004-02-03
申请号：US09454075
申请日：1999-12-02
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译： 本发明涉及特异性抑制腺苷A3受体的化合物以及这些化合物用于治疗受试者中与A3腺苷受体有关的疾病的用途，其包括向受试者施用治疗有效量的化合物。
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公开(公告)号：US07772238B2
公开(公告)日：2010-08-10
申请号：US11918912
申请日：2006-04-14
申请人： Jed Lee Hubbs , Sam Kattar , Joey Methot , Thomas Miller , Phieng Siliphaivanh , Matthew Stanton , Kevin Wilson , David J. Witter
发明人： Jed Lee Hubbs , Sam Kattar , Joey Methot , Thomas Miller , Phieng Siliphaivanh , Matthew Stanton , Kevin Wilson , David J. Witter
IPC分类号： A61K31/496 , A61K31/381 , C07D405/04 , C07D333/56
CPC分类号： C07D333/70 , A61K31/38 , A61K31/381 , A61K31/41
摘要： The present invention relates to a novel class of hydroxamic acid derivatives. 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 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 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： 本发明涉及一类新型异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸化合物也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，例如神经变性 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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公开(公告)号：US07598252B2
公开(公告)日：2009-10-06
申请号：US10718280
申请日：2003-11-20
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
摘要翻译： 本发明涉及特异性抑制腺苷A1受体的化合物以及这些化合物用于治疗受试者中与腺苷受体A1相关的疾病的用途。
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