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1. 发明申请

WO2010111626A2 POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS 审中-公开
标题翻译： POLY（ADP-RIBOSE）聚合酶（PARP）抑制剂
公开(公告)号：WO2010111626A2
公开(公告)日：2010-09-30
申请号：PCT/US2010/028878
申请日：2010-03-26
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , BROWN, Jason, W. , GANGLOFF, Anthony, R. , JENNINGS, Andrew, John , VU, Phong, H.
发明人： BROWN, Jason, W. , GANGLOFF, Anthony, R. , JENNINGS, Andrew, John , VU, Phong, H.
IPC分类号： C07D265/36
CPC分类号： C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D473/12
摘要： Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
摘要翻译：提供下式的化合物用于抑制聚（ADP-核糖）聚合酶（PARP）：其中变量在本文中定义。还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物的方法。

2. 发明申请

WO2009129401A8 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2009129401A8
公开(公告)日：2009-10-22
申请号：PCT/US2009/040832
申请日：2009-04-16
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , BROWN, Jason, W. , DONG, Qing , GANGLOFF, Anthony, R. , PARASELLI, Bheema, R. , STAFFORD, Jeffrey, A. , SCORAH, Nicholas , SALSBURY, Jonathon, S. , DAS, Sanjib
发明人： BROWN, Jason, W. , DONG, Qing , GANGLOFF, Anthony, R. , PARASELLI, Bheema, R. , STAFFORD, Jeffrey, A. , SCORAH, Nicholas , SALSBURY, Jonathon, S. , DAS, Sanjib
IPC分类号： A61K31/437 , C07D471/04 , A61P25/00 , A61P35/00
摘要： Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

3. 发明申请

WO2006023931A3 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006023931A3
公开(公告)日：2006-03-02
申请号：PCT/US2005/029990
申请日：2005-08-18
申请人： TAKEDA SAN DIEGO, INC. , CAO, Sheldon X. , GANGLOFF, Anthony R. , PARASELLI, Bheema R. , STAFFORD, Jeffrey A. , WIJESEKERA, Hasanthi P.
发明人： CAO, Sheldon X. , GANGLOFF, Anthony R. , PARASELLI, Bheema R. , STAFFORD, Jeffrey A. , WIJESEKERA, Hasanthi P.
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/4709
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound of the formula (I): In particular 4-(quinolin-2(1H)-ylidene)-1H-pyrazol-5(4H)-one derivatives are disclosed.

4. 发明申请

WO2005061519A1 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2005061519A1
公开(公告)日：2005-07-07
申请号：PCT/US2004/042631
申请日：2004-12-17
申请人： SYRRX, INC. , GANGLOFF, Anthony, R. , NOWAKOWSKI, Jacek , PARASELLI, Bheema, R. , STAFFORD, Jeffrey, A. , TENNANT, Michael, G.
发明人： GANGLOFF, Anthony, R. , NOWAKOWSKI, Jacek , PARASELLI, Bheema, R. , STAFFORD, Jeffrey, A. , TENNANT, Michael, G.
IPC分类号： C07D513/04
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D471/04 , C07D513/04
摘要： The invention relates to compounds of the following formula (I) that may be used to inhibit kinases, as well as compositions of matter and kits comprising these compounds. The present invention also relates to methods for inhibiting kinases, as well as treatment methods using compounds according to the present invention.
摘要翻译：本发明涉及可用于抑制激酶的下式（I）化合物，以及包含这些化合物的物质组合物和试剂盒。本发明还涉及抑制激酶的方法，以及使用根据本发明的化合物的治疗方法。

5. 发明申请

WO2004082638A3 HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：WO2004082638A3
公开(公告)日：2005-05-06
申请号：PCT/US2004008342
申请日：2004-03-17
申请人： SYRRX INC , BRESSI JEROME C , BROWN JASON W , CAO SHELDON X , GANGLOFF ANTHONY R , JENNINGS ANDREW J , STAFFORD JEFFREY A , VU PHONG H , XIAO XIAO-YI
发明人： BRESSI JEROME C , BROWN JASON W , CAO SHELDON X , GANGLOFF ANTHONY R , JENNINGS ANDREW J , STAFFORD JEFFREY A , VU PHONG H , XIAO XIAO-YI
IPC分类号： A61K20060101 , A61K31/4184 , A61K31/454 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/535 , C07D235/18 , C07D413/02 , C07D417/02
CPC分类号： C07D235/18 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/10
摘要： Compounds that may be used to inhibit histone deacetylase having the formula (I) or formula (II) wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
摘要翻译：可用于抑制具有式（I）或式（II）的组蛋白脱乙酰酶的化合物，其中M是能够与脱乙酰酶催化位点和/或金属离子络合的取代基; L是在M取代基和化合物的其余部分之间分离0-10个原子之间的取代基; Z和Q如本文所定义。

6. 发明申请

WO2011014681A1 Poly (ADP-Ribose) Polymerase (PARP) INHIBITORS 审中-公开
标题翻译：聚（ADP-核糖）聚合酶（PARP）抑制剂
公开(公告)号：WO2011014681A1
公开(公告)日：2011-02-03
申请号：PCT/US2010/043751
申请日：2010-07-29
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , BROWN, Jason W. , GANGLOFF, Anthony R. , KIRYANOV, Andre A.
发明人： BROWN, Jason W. , GANGLOFF, Anthony R. , KIRYANOV, Andre A.
IPC分类号： C07D471/14 , A61K31/519 , A61P35/00
CPC分类号： C07D471/14
摘要： Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
摘要翻译：提供下式的化合物用于PARP：其中变量如本文所定义。还提供了包含这些化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物的方法。

7. 发明申请

WO2010085570A1 Poly (ADP-Ribose) Polymerase (PARP) Inhibitors 审中-公开
标题翻译：聚（ADP-核糖）聚合酶（PARP）抑制剂
公开(公告)号：WO2010085570A1
公开(公告)日：2010-07-29
申请号：PCT/US2010/021669
申请日：2010-01-21
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , GANGLOFF, Anthony R. , JENNINGS, Andrew John , JONES, Benjamin , KIRYANOV, Andre A.
发明人： GANGLOFF, Anthony R. , JENNINGS, Andrew John , JONES, Benjamin , KIRYANOV, Andre A.
IPC分类号： C07D471/04 , C07D471/14 , C07D498/14 , C07D513/14 , A61K31/4985 , A61K31/5365 , A61K31/542 , A61P25/00 , A61P35/00 , A61P9/00 , A61P29/00
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: (I) in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译：公开了下列化学式：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X和t在本说明书中定义的（I）。还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。

8. 发明申请

WO2005105788A1 INDOLE DERIVATIVES AND USE THEREOF AS KINASE INHIBITORS 审中-公开
标题翻译：作为激素抑制剂，其衍生物及其用途
公开(公告)号：WO2005105788A1
公开(公告)日：2005-11-10
申请号：PCT/US2005/013410
申请日：2005-04-20
申请人： TAKEDA SAN DIEGO, INC. , BRESSI, Jerome C. , GANGLOFF, Anthony R. , HOSFIELD, David J. , JENNINGS, Andrew John , PARASELLI, Bheema R. , STAFFORD, Jeffrey Alan
发明人： BRESSI, Jerome C. , GANGLOFF, Anthony R. , HOSFIELD, David J. , JENNINGS, Andrew John , PARASELLI, Bheema R. , STAFFORD, Jeffrey Alan
IPC分类号： C07D403/04
CPC分类号： C07D471/04 , C07D401/14 , C07D403/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D513/04
摘要： The invention relates to compounds comprising the below formula that may be used to inhibit kinases as well as compositions of matter, kits and methods comprising these compounds.
摘要翻译：本发明涉及可用于抑制激酶的下式的化合物以及包含这些化合物的物质组合物，试剂盒和方法。

9. 发明申请

WO1998045275A1 COMPOUNDS AND COMPOSITIONS FOR TREATING DISEASES ASSOCIATED WITH SERINE PROTEASE, PARTICULARLY TRYPTASE, ACTIVITY 审中-公开
标题翻译：用于治疗与丝氨酸蛋白酶，特异性TRYPTASE，活性相关的疾病的化合物和组合物
公开(公告)号：WO1998045275A1
公开(公告)日：1998-10-15
申请号：PCT/US1997021849
申请日：1997-12-01
申请人： AXYS PHARMACEUTICALS CORPORATION , CHURCH, Timothy, J. , CUTSHALL, Neil, Scott , GANGLOFF, Anthony, R. , JENKINS, Thomas, E. , LINSELL, Martin, S. , LITVAK, Joane , RICE, Kenneth, D. , SPENCER, Jeffrey, R. , WANG, Vivian, R.
发明人： AXYS PHARMACEUTICALS CORPORATION
IPC分类号： C07D235/20
CPC分类号： C07D231/12 , C07D233/56 , C07D235/20 , C07D249/08 , C07D401/14 , C07D403/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07F7/0812
摘要： Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. A preferred aspect of the invention are compounds of Formula (II) in which: the dashed lines independently represent optional bonds; each R independently is (C1-6)alkyl, (C1-6)alkyloxy, halo or hydroxy; each R independently is (C1-6)alkyl, (C1-6)alkyloxy, halo or hydroxy; X is -C(O)- or -CR R -, X is -CH(R )n1- or -C(R )n1=, wherein R is amino(N1-4)azolidinyl, amino(N1-4)azolyl, (N1-4)azolidinyl, (N1-4)azolyl, -NHC(NH)NR R , -C(NR )R , -C(NH)NHR , -C(NH)NR R or -(CR R )yNH2, or X is -N= or -NH(R )n1-, wherein R is -C(NR )R , -C(NH)NHR or -C(NH)NR R , wherein each R independently is hydrogen or (C1-6)alkyl and each R independently is (C1-6)alkyl; and X is -CH(R )- or -C(R )=, wherein R is -R , -OR , -N(R )R , -SR , -S(O)R , -S(O)2R , -S(O)2OR , -S(O)2N(R )R , -N(R )S(O)2R , -C(O)R , -C(O)OR , -C(O)N(R )R , -N(R )C(O)R , -OC(O)N(R )R , -N(R )C(O)OR , -(CH2)n4N(R )C(O)N(R )R , -OP(O)(OR )OR or -C(O)N(R )CH(COOH)R , or X is -N= or -N(R )-, wherein R is -C(O)R , -C(O)OR , -C(O)N(R )R , -OC(O)N(R )R or -C(O)N(R )CH(COOH)R , wherein R , R and R are as defined in the Summary of the Invention; R is hydrogen or (C1-4)alkyl, R is hydrogen or (C1-4) alkyl, which alkyl optionally is substituted with one to two substituents independently selected from (C1-4)alkyloxy, hydroxy and sulfo, R is hydrogen or methyl and R is hydrogen, methyl or hydroxy. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
摘要翻译：描述了有效预防和治疗肥大细胞介导的炎症性疾病的新型化合物，组合物和方法。本发明的优选方面是式（II）的化合物，其中：虚线独立地表示任选的键; 每个R 2独立地为（C 1-6）烷基，（C 1-6）烷氧基，卤素或羟基; 每个R 3独立地为（C 1-6）烷基，（C 1-6）烷氧基，卤素或羟基; X 3为-C（O） - 或-CR 7 R 8 - ，X 8为-CH（R 1）n1或-C（R 1）n1 = 其中R 1是氨基（N1-4）唑烷基，氨基（N1-4）唑基，（N1-4）唑烷基，（N1-4）唑基，-NHC（NH）NR9R9， -C（NR 9）R 9，-C（NH）NHR 10，-C（NH）NR 10 R 10或 - （CR 11 R 11）y NH 2，或X 8是-N =或-NH（R 1）n1-，其中R 1是-C（NR 9）R 9，-C（NH）NHR 10或 -C（NH）NR 10 R 10，其中每个R 9独立地是氢或（C 1-6）烷基，每个R 10独立地是（C 1-6）烷基; 并且X 9为-CH（R 4） - 或-C（R 4）=，其中R 4为-R 12，-OR 12，-N（R 13））R 12，-SR 12，-S（O）R 12，-S（O）2 R 12，-S（O）2OR 12，-S（O）2 N（ R 13），-N（R 13）S（O）2 R 12，-C（O）R 12，-C（O）OR 12，-C（ O）N（R 13）R 12，-N（R 13）C（O）R 12，-OC（O）N（R 13）R 12，-N （R 13）C（O）OR 12， - （CH 2）n 4 N（R 13）C（O）N（R 13）R 12，-OP（O） 13）或OR 12或-C（O）N（R 14）CH（COOH）R 12或X 9是-N =或-N（R 4） - ，其中 R 4是-C（O）R 12，-C（O）OR 12，-C（O）N（R 13）R 12，-OC（O） R 12或-C（O）N（R 14）CH（COOH）R 12，其中R 12，R 13和R 14如发明概述; R 5为氢或（C 1-4）烷基，R 6为氢或（C 1-4）烷基，该烷基任选被一至两个独立地选自（C 1-4）烷氧基，羟基和磺基，R 7是氢或甲基，R 8是氢，甲基或羟基。化合物，组合物和方法对于预防和治疗与呼吸道相关的炎性疾病如哮喘和过敏性鼻炎以及其它类型的免疫性炎症性疾病如类风湿性关节炎，结膜炎和炎性肠病是有效的，各种皮肤病学条件，以及某些病毒状况。这些化合物包括肥大细胞蛋白酶类胰蛋白酶的有效和选择性抑制剂。用于治疗这些病症的组合物包括口服，吸入，局部和肠胃外制剂以及包含这些制剂的装置。

10. 发明申请

WO2006122319A3 HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：WO2006122319A3
公开(公告)日：2007-11-15
申请号：PCT/US2006018645
申请日：2006-05-10
申请人： TAKEDA SAN DIEGO INC , BRESSI JEROME C , BROWN JASON W , GANGLOFF ANTHONY R , STAFFORD JEFFREY A , VU PHONG H
发明人： BRESSI JEROME C , BROWN JASON W , GANGLOFF ANTHONY R , STAFFORD JEFFREY A , VU PHONG H
IPC分类号： C07D285/24 , A61K31/549 , A61P35/00 , C07D239/80 , C07D417/04 , C07D417/06 , C07D417/12 , C07D513/04
CPC分类号： C07D513/04 , C07D239/80 , C07D285/24 , C07D417/04 , C07D417/06 , C07D417/12
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of : formula (I) and formula (II) wherein the variables are as defined herein.
摘要翻译：提供化合物，药物组合物，试剂盒和方法用于HDAC，其包含选自式（I）和式（II）的化合物，其中变量如本文所定义。

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