-
1.Heterocyclic compounds useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders 有权
标题翻译: 可用于治疗肿瘤性疾病,炎症性疾病和免疫调节性疾病的杂环化合物公开(公告)号:US08629147B2
公开(公告)日:2014-01-14
申请号:US11593191
申请日:2006-11-02
申请人: Alexey Vyacheslavovich Anikin , Vidyasagar Reddy Gantla , Vlad Edward Gregor , Luyong Jiang , Yahua Liu , Danny Peter Claude McGee , Charles Chamchoumis Mikel , Jason Conrad Pickens , Thomas Roy Webb , Zheng Yan , Tong Zhu , Aleksander Kadushkin , Sergey Sviridov , Sergey Zozulya , Alexander Chucholowski , Douglas Eric McGrath
发明人: Alexey Vyacheslavovich Anikin , Vidyasagar Reddy Gantla , Vlad Edward Gregor , Luyong Jiang , Yahua Liu , Danny Peter Claude McGee , Charles Chamchoumis Mikel , Jason Conrad Pickens , Thomas Roy Webb , Zheng Yan , Tong Zhu , Aleksander Kadushkin , Sergey Sviridov , Sergey Zozulya , Alexander Chucholowski , Douglas Eric McGrath
IPC分类号: A61K31/497 , A61K31/47 , A61K31/445
CPC分类号: C07D401/04 , C07D235/18 , C07D235/20 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/04 , C07D495/04
摘要: The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.
摘要翻译: 本发明提供了能够调节酪氨酸激酶的化合物,包含该化合物的组合物及其使用方法。
-
2.Heterocyclic compounds useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders 有权
标题翻译: 可用于治疗肿瘤性疾病,炎症性疾病和免疫调节性疾病的杂环化合物公开(公告)号:US20080207635A1
公开(公告)日:2008-08-28
申请号:US11593191
申请日:2006-11-02
申请人: Alexey Vyacheslavovich Anikin , Vidyasagar Reddy Gantla , Vlad Edward Gregor , Luyong Jiang , Yahua Liu , Danny Peter Claude McGee , Charles Chamchoumis Mikel , Jason Conrad Pickens , Thomas Roy Webb , Zheng Yan , Tong Zhu , Aleksander Kadushkin , Sergey Sviridov , Sergey Zozulya , Alexander Chucholowski , Douglas Eric McGrath
发明人: Alexey Vyacheslavovich Anikin , Vidyasagar Reddy Gantla , Vlad Edward Gregor , Luyong Jiang , Yahua Liu , Danny Peter Claude McGee , Charles Chamchoumis Mikel , Jason Conrad Pickens , Thomas Roy Webb , Zheng Yan , Tong Zhu , Aleksander Kadushkin , Sergey Sviridov , Sergey Zozulya , Alexander Chucholowski , Douglas Eric McGrath
IPC分类号: A61K31/497 , C07D401/14 , C12N9/12 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61P35/00 , A61P3/10 , A61P9/10
CPC分类号: C07D401/04 , C07D235/18 , C07D235/20 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/04 , C07D495/04
摘要: The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.
摘要翻译: 本发明提供了能够调节酪氨酸激酶的化合物,包含该化合物的组合物及其使用方法。
-
公开(公告)号:US08815906B2
公开(公告)日:2014-08-26
申请号:US12922891
申请日:2009-03-18
申请人: Yahua Liu , Alexey Vyacheslavovich Anikin , Charles Chamchoumis Mikel , Douglas Eric McGrath , Goverdhan Reddy Vavilala , Jason Conrad Pickens , Aleksander Kadushkin , Luyong Jiang , Mohan Santhanam Thiruvazhi , Sergey Zozulya , Rajendran Vairagoundar , Tong Zhu , Alexander Chucholowski , Zheng Yan , Alisher Khasanov , Christina Gregor
发明人: Vlad Edward Gregor , Yahua Liu , Alexey Vyacheslavovich Anikin , Charles Chamchoumis Mikel , Douglas Eric McGrath , Goverdhan Reddy Vavilala , Jason Conrad Pickens , Aleksander Kadushkin , Luyong Jiang , Mohan Santhanam Thiruvazhi , Sergey Zozulya , Rajendran Vairagoundar , Tong Zhu , Alexander Chucholowski , Zheng Yan , Alisher Khasanov
IPC分类号: C07D401/14 , A61K31/4439 , A61K31/4545
CPC分类号: C07D401/14 , A61K31/4439 , A61K31/4545 , C07D487/04
摘要: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
摘要翻译: 提供式(I)化合物或其调节酪氨酸激酶活性的立体异构体,互变异构体,盐,水合物或前药,包含化合物的组合物及其使用方法。
-
公开(公告)号:US20130053376A1
公开(公告)日:2013-02-28
申请号:US12922891
申请日:2009-03-18
申请人: Yahua Liu , Alexey Vyacheslavovich Anikin , Charles Chamchoumis Mikel , Douglas Eric McGrath , Goverdhan Reddy Vavilala , Jason Conrad Pickens , Aleksander Kadushkin , Luyong Jiang , Mohan Santhanam Thiruvazhi , Sergey Zozulya , Rajendran Vairagoundar , Tong Zhu , Alexander Chucholowski , Zheng Yan , Alisher Khasanov , Christina Gregor
发明人: Vlad Edward Gregor , Yahua Liu , Alexey Vyacheslavovich Anikin , Charles Chamchoumis Mikel , Douglas Eric McGrath , Goverdhan Reddy Vavilala , Jason Conrad Pickens , Aleksander Kadushkin , Luyong Jiang , Mohan Santhanam Thiruvazhi , Sergey Zozulya , Rajendran Vairagoundar , Tong Zhu , Alexander Chucholowski , Zheng Yan , Alisher Khasanov
IPC分类号: A61K31/4545 , C07D401/14 , A61K31/4439 , C07D413/14 , C12N9/99 , A61K31/541 , C07D405/14 , A61K31/5377 , A61P35/00 , C07D487/04 , C07D417/14
CPC分类号: C07D401/14 , A61K31/4439 , A61K31/4545 , C07D487/04
摘要: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
-
公开(公告)号:US06646137B1
公开(公告)日:2003-11-11
申请号:US09717072
申请日:2000-11-22
IPC分类号: C07D30702
CPC分类号: C07D213/82 , C07C279/12 , C07D207/34 , C07D209/42 , C07D215/12 , C07D231/14 , C07D231/16 , C07D261/10 , C07D307/00 , C07D307/68 , C07D307/71 , C07D307/91 , C07D317/68 , C07D319/18 , C07D333/38 , C07D333/70 , C07D405/12 , C07D409/12
摘要: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
摘要翻译: 能够抑制促性腺激素释放激素作用的非肽GnRH剂具有以下通式,其中X1,X2,Y和Z是定义的变量:这些化合物及其药学上可接受的盐,多聚体,前药和活性代谢物 适合于治疗哺乳动物生殖障碍和类固醇激素依赖性肿瘤以及调节生育能力,其中指出促性腺激素释放的抑制。 还描述了合成化合物的方法和可用于其制备的中间体。
-
公开(公告)号:US06218426B1
公开(公告)日:2001-04-17
申请号:US09259206
申请日:1999-03-01
IPC分类号: A01N4306
CPC分类号: C07D213/82 , C07C279/12 , C07D207/34 , C07D209/42 , C07D215/12 , C07D231/14 , C07D231/16 , C07D261/10 , C07D307/00 , C07D307/68 , C07D307/71 , C07D307/91 , C07D317/68 , C07D319/18 , C07D333/38 , C07D333/70 , C07D405/12 , C07D409/12
摘要: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
摘要翻译: 能够抑制促性腺激素释放激素作用的非肽GnRH剂具有以下通式,其中X1,X2,Y是定义的变量:这些化合物及其药学上可接受的盐,多聚体,前药和活性代谢物是 适用于治疗哺乳动物生殖障碍和类固醇激素依赖性肿瘤以及调节生育能力,其中指出促性腺激素释放的抑制。 还描述了合成化合物的方法和可用于其制备的中间体。
-
公开(公告)号:US06469021B1
公开(公告)日:2002-10-22
申请号:US09831572
申请日:2001-10-26
申请人: Larry Kenneth Truesdale , Richard A. Bychowski , Javier Gonzalez , Atsuo Kuki , Ranjan Jagath Rajapakse , Min Teng , Dan Kiel , Daljit S. Dhanoa , Yufeng Hong , Tso-sheng Chou , Anthony L. Ling , Michael David Johnson , Vlad Edward Gregor
发明人: Larry Kenneth Truesdale , Richard A. Bychowski , Javier Gonzalez , Atsuo Kuki , Ranjan Jagath Rajapakse , Min Teng , Dan Kiel , Daljit S. Dhanoa , Yufeng Hong , Tso-sheng Chou , Anthony L. Ling , Michael David Johnson , Vlad Edward Gregor
IPC分类号: A61K31437
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要: Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
摘要翻译: 作为肠激素胰高血糖素样肽1(GLP-1)的拮抗剂的非肽化合物具有9H-b-咔啉中心基序。 该化合物表现出有利的物理,化学和生物学特性,并且抑制GLP-1肽与GLP-1受体的结合和/或通过结合的GLP-1阻止受体活化。 本发明还涉及抑制GLP-1与GLP-1受体结合的方法以及抑制GLP-1受体活化的方法。 还描述了可用于制备非肽GLP-1受体拮抗剂的中间体化合物。
-
8.TRICYCLIC COMPOUND DERIVATIVES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY DISORDERS AND IMMUNOMODULATORY DISORDERS 失效
标题翻译: 用于治疗神经疾病,炎症性疾病和免疫缺陷性疾病的三分子化合物衍生物公开(公告)号:US20120071473A1
公开(公告)日:2012-03-22
申请号:US13242272
申请日:2011-09-23
申请人: Vlad Edward Gregor , Nelson Levy
发明人: Vlad Edward Gregor , Nelson Levy
IPC分类号: A61K31/4545 , A61K31/5377 , A61P35/00 , C12N9/99 , A61P9/10 , A61P17/06 , A61P37/00 , C07D487/04 , A61P3/10
CPC分类号: C07D487/04
摘要: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
摘要翻译: 提供式(I)化合物或其调节酪氨酸激酶活性的立体异构体,互变异构体,盐,水合物或前药,包含化合物的组合物及其使用方法。
-
公开(公告)号:US06849733B1
公开(公告)日:2005-02-01
申请号:US08916527
申请日:1997-08-22
IPC分类号: C07D295/12 , A61K31/17 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/407 , A61K31/4164 , A61K31/4184 , A61K31/439 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/5375 , A61P3/04 , A61P9/10 , A61P9/12 , A61P11/08 , A61P15/00 , A61P25/22 , A61P43/00 , C07C279/00 , C07C279/24 , C07D205/00 , C07D205/04 , C07D207/09 , C07D207/27 , C07D207/335 , C07D211/26 , C07D211/62 , C07D211/72 , C07D213/38 , C07D213/40 , C07D217/02 , C07D217/26 , C07D233/61 , C07D235/16 , C07D239/42 , C07D295/20 , C07D307/14 , C07D307/52 , C07D309/14 , C07D319/12 , C07D333/20 , C07D409/12 , C07D413/00 , C07D453/02 , C07D487/08
CPC分类号: C07C279/24 , C07D213/40 , C07D307/14
摘要: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
摘要翻译: 公开了在说明书中进一步定义的符号W,A,D,R 1,R 2,R 3,R 4中具有通式IW的新型神经肽Y配体。 式I化合物是神经肽Y的激动剂和拮抗剂,因此可用作调节剂。
-
-
-
-
-
-
-
-