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1. 发明申请

WO2009155606A1 ANTICANCER COMPOUNDS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：反应物化合物及其制备方法和使用方法
公开(公告)号：WO2009155606A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/048167
申请日：2009-06-22
申请人： ST. JUDE CHILDREN'S RESEARCH HOSPITAL , WEBB, Thomas, R. , LAGISETTI, Chandraiah
发明人： WEBB, Thomas, R. , LAGISETTI, Chandraiah
IPC分类号： A61K31/497
CPC分类号： C07D493/10 , A61K31/351 , A61K31/357 , C07D319/06
摘要： In one aspect, the invention relates to compounds having anticancer activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended to be used as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及具有抗癌活性的化合物; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与不受控制的细胞增殖相关的疾病的方法。该摘要旨在用作扫描工具，用于在特定技术中进行搜索，而不意在限制本发明。

2. 发明申请

WO1997029110A1 THIOPHENOPYRIMIDINES 审中-公开
公开(公告)号：WO1997029110A1
公开(公告)日：1997-08-14
申请号：PCT/EP1997000457
申请日：1997-01-30
申请人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES INC. , CHEN, Chen , WEBB, Thomas, R. , McCARTHY, James, R. , MORAN, Terence, J.
发明人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES INC.
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： This invention concerns compounds of formula (I) including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R is NR R or OR ; R is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6 alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of the formula: -Alk-O-CO-Ar ; or R and R taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is a phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的式（I）化合物，其中X是S，SO或SO 2; R 1是NR 4 R 5或OR 5; R 2是C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基; R 3是氢，C 1-6烷基，C 1-6烷基磺酰基，C 1-6烷基磺酰基或C 1-6烷硫基; R 4是氢，C 1-6烷基，一或二（C 3-6环烷基）甲基，C 3-6环烷基，C 3-6烯基，羟基C 1-6烷基，C 1-6烷基羰基氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 5是C 1-8烷基，单或二（C 3-6环烷基）甲基，Ar 1 CH 2，C 1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1 -C 6烷基，（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或下式的基团：-Alk-O-CO-Ar 1; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar是苯基，取代的苯基，吡啶基或取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

3. 发明申请

WO2021195278A1 TRICYCLIC INHIBITORS OF INFLUENZA VIRUS ENDONUCLEASE 审中-公开
公开(公告)号：WO2021195278A1
公开(公告)日：2021-09-30
申请号：PCT/US2021/023980
申请日：2021-03-24
申请人： WEBB, Thomas, R. , LAGISETTI, Chandraiah , BEYLKIN, Diane , PARK, Jaehyeon , ZHOU, Wei , MADRID, Peter , GONG, Leyi , MALERICH, Jeremiah , FUNG, Chat Cheong, Gabriel , NG, Raymond , PERRON, Quentin , BARROS, Vinicius
发明人： WEBB, Thomas, R. , LAGISETTI, Chandraiah , BEYLKIN, Diane , PARK, Jaehyeon , ZHOU, Wei , MADRID, Peter , GONG, Leyi , MALERICH, Jeremiah , FUNG, Chat Cheong, Gabriel , NG, Raymond , PERRON, Quentin , BARROS, Vinicius
IPC分类号： A61P35/00 , C07D471/06 , C07D498/06
摘要： The present disclosure is concerned with 9-hydroxy-6-(pyrrolidin-2-yl)-3,4-dihydro-2H-pyrazino[ 1,2-c]pyrimidine- 1, 8-dione compounds for the treatment of various viral infections such as, for example, influenza virus. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

4. 发明申请

WO1997029109A1 PYRAZOLOPYRIMIDINES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CRF受体拮抗剂的吡唑并嘧啶
公开(公告)号：WO1997029109A1
公开(公告)日：1997-08-14
申请号：PCT/EP1997000459
申请日：1997-01-30
申请人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES INC. , CHEN, Chen , WEBB, Thomas, R. , McCARTHY, James, R. , MORAN, Terence, J. , WILCOXEN, Keith, M.
发明人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES INC.
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D471/10
摘要： This invention concerns compounds of formula (I), including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R is NR R or OR ; R is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of the formula -Alk-O-CO-Ar ; or R and R taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物，包括立体异构体及其药学上可接受的酸加成盐形式，其中R 1为NR 4 R 5或OR 5; R 2是C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基; R 3是氢，C 1-6烷基，C 1-6烷基磺酰基，C 1-6烷基磺酰基或C 1-6烷硫基; R 4是氢，C 1-6烷基，一或二（C 3-6环烷基）甲基，C 3-6环烷基，C 3-6烯基，羟基C 1-6烷基，C 1-6烷基羰基氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 5是C 1-8烷基，一或二（C 3-6环烷基）甲基，Ar 1 CH 2，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，吗啉基，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar 1的基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

5. 发明申请

WO1995035280A1 METHODS OF SYNTHESIS OF PEPTIDYL ARGININALS 审中-公开
标题翻译：肽类ARGININALS的合成方法
公开(公告)号：WO1995035280A1
公开(公告)日：1995-12-28
申请号：PCT/US1995007666
申请日：1995-06-19
申请人： CORVAS INTERNATIONAL, INC. , WEBB, Thomas, R. , REINER, John, E. , TAMURA, Susan, Y. , RIPKA, William, C. , DAGNINO, Raymond, Jr. , NUTT, Ruth, F.
发明人： CORVAS INTERNATIONAL, INC.
IPC分类号： C07D211/56
CPC分类号： C07D401/12 , A61K38/00 , C07D207/16 , C07D211/56 , C07K5/0606 , C07K5/06113
摘要： This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein, which have formula (I), wherein R1 is selected from the group consisting of hydrogen, benzyloxycarbonyl, isonicotinyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, t-butoxycarbonyl, t-amyloxycarbonyl, isobornyloxycarbonyl, adamantyloxycarbonyl, 2-(4-biphenyl)-2-propyloxycarbonyl, 9-fluorenylmethoxycarbonyl and methylsulfonylethoxycarbonyl; R2 is selected from the group consisting of alkyl of 1 to about 12 carbon atoms and aralkyl of about 7 to about 15 carbon atoms, either of which is optionally substituted with hydroxy or -CO-Y, wherein Y is hydroxy, alkoxy of 1 to about 12 carbon atoms, aralkoxy of about 7 to about 15 carbon atoms, O-polymeric support or NH-polymeric support; R3 is selected from the group consisting of hydrogen, Fmoc, nitro, benzyloxycarbonyl, t-butoxycarbonyl and adamantyloxycarbonyl; and R4 is selected from the group consisting of hydrogen, alkyl of 1 to about 12 carbon atoms, aryl of about 6 to about 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms; and salts thereof.
摘要翻译：本发明提供用于合成肽基精氨酸的溶液相和固相方法及其中有用的新型试剂，其具有式（I），其中R 1选自氢，苄氧羰基，异烟碱氧基羰基，2-氯苄氧基羰基，丁氧基羰基，叔戊氧基羰基，异冰片氧基羰基，金刚烷基氧基羰基，2-（4-联苯基）-2-丙氧基羰基，9-芴基甲氧基羰基和甲基磺酰基乙氧基羰基; R2选自1至约12个碳原子的烷基和约7至约15个碳原子的芳烷基，其中任一个任选被羟基或-CO-Y取代，其中Y是羟基，1至约12个碳原子，约7至约15个碳原子的芳烷氧基，O-聚合物载体或NH-聚合物载体; R3选自氢，Fmoc，硝基，苄氧基羰基，叔丁氧基羰基和金刚烷氧基羰基; 并且R 4选自氢，1至约12个碳原子的烷基，约6至约14个碳原子的芳基和约7至约15个碳原子的芳烷基; 及其盐。

6. 发明申请

WO2012151567A1 PYRIMIDINONE COMPOUNDS AND METHODS FOR PREVENTING AND TREATING INFLUENZA 审中-公开
标题翻译：吡咯米辛酮化合物和预防和治疗流感病毒的方法
公开(公告)号：WO2012151567A1
公开(公告)日：2012-11-08
申请号：PCT/US2012/036697
申请日：2012-05-05
申请人： ST. JUDE CHILDREN'S RESEARCH HOSPITAL , WEBB, Thomas, R. , BOYD, Vincent, A.
发明人： WEBB, Thomas, R. , BOYD, Vincent, A.
IPC分类号： A01N43/54
CPC分类号： C07D239/54 , A61K31/13 , A61K31/196 , A61K31/215 , A61K31/351 , A61K31/4045 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/59 , A61K31/7012 , A61K38/21 , A61K45/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D487/04 , A61K2300/00
摘要： In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及可用于治疗和/或预防流感的新型广谱抗病毒，嘧啶酮化合物，使用方法，组合物和试剂盒。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

8. 发明申请

WO2008021369A2 TRICYCLIC COMPOUND DERIVATIVES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY DISORDERS AND IMMUNOMODULATORY DISORDERS 审中-公开
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：WO2008021369A2
公开(公告)日：2008-02-21
申请号：PCT/US2007018002
申请日：2007-08-13
申请人： CHEMBRIDGE RES LAB INC , GREGOR VLAD EDWARD , LIU YAHUA , ANIKIN ALEXEY , MCGEE DANNY PETER CLAUDE , MIKEL CHARLES , MCGRATH DOUGLAS ERIC , VAVILALA GOVERDHAN REDDY , PICKENS JASON C , KADUSHKIN ALEXANDER , THIRUVAZHI MOHAN SANTHANAM , ZOZULYA SERGEY , VAIRAGOUNDAR RAJENDRAN , ZHU TONG , CHUCHOLOWSKI ALEXANDER , WEBB THOMAS R , JIANG LUYONG , GANTLA VIDYASAGAR REDDY , YAN ZHENG
发明人： GREGOR VLAD EDWARD , LIU YAHUA , ANIKIN ALEXEY , MCGEE DANNY PETER CLAUDE , MIKEL CHARLES , MCGRATH DOUGLAS ERIC , VAVILALA GOVERDHAN REDDY , PICKENS JASON C , KADUSHKIN ALEXANDER , THIRUVAZHI MOHAN SANTHANAM , ZOZULYA SERGEY , VAIRAGOUNDAR RAJENDRAN , ZHU TONG , CHUCHOLOWSKI ALEXANDER , WEBB THOMAS R , JIANG LUYONG , GANTLA VIDYASAGAR REDDY , YAN ZHENG
CPC分类号： C07D487/04
摘要： Provided are compounds of formula (I) or a stereoisomer, tautomer, salt, hydrate or prodrug thereof, capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.
摘要翻译：提供了能够调节酪氨酸激酶的式（I）化合物或其立体异构体，互变异构体，盐，水合物或前药，包含该化合物的组合物及其使用方法。

9. 发明申请

WO1996039400A1 AMINO-SUBSTITUTED THIADIAZOLES, PYRIMIDINES, TRIAZINES OR TRIAZOLES USEFUL AS CTF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：氨基取代的噻二唑，吡咯烷，三嗪或三唑作为CTF受体拮抗剂有用
公开(公告)号：WO1996039400A1
公开(公告)日：1996-12-12
申请号：PCT/US1996009633
申请日：1996-06-06
申请人： NEUROCRINE BIOSCIENCES, INC. , McCARTHY, James, R. , XIE, Yun, Feng , WHITTEN, Jeffrey, P. , WEBB, Thomas, R. , CHEN, Chen , RAMPHAL, John, Y. , GRIGORIADIS, Dimitri, E. , DAGNINO, Raymond, Jr. , HUANG, Charles, Q. , LIU, Zhengyu
发明人： NEUROCRINE BIOSCIENCES, INC.
IPC分类号： C07D285/08
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D249/14 , C07D251/16 , C07D251/18 , C07D251/22 , C07D285/08
摘要： Compounds having formulae (I) to (VI) wherein X is a substituted (hetero)aryl group and R1-R6 are various possible substituents, are corticotropin-releasing factor (CRF) receptor antagonists.
摘要翻译：具有式（I）至（VI）的化合物，其中X是取代的（杂）芳基和R 1 -R 6是各种可能的取代基，是促肾上腺皮质激素释放因子（CRF）受体拮抗剂。

10. 发明申请

WO1997014684A1 AMINO SUBSTITUTED PYRIMIDINES AND TRIAZINES 审中-公开
标题翻译：氨基取代的吡咯烷和三嗪
公开(公告)号：WO1997014684A1
公开(公告)日：1997-04-24
申请号：PCT/EP1996004478
申请日：1996-10-15
申请人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES INC. , WEBB, Thomas, R. , MORAN, Terence, J. , McCARTHY, James, R.
发明人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES INC.
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D239/49 , C07D251/14
摘要： Pyrimidines and triazines of formula (I), wherein R is C1-6alkyl, amino, mono- or diC1-6alkylamino; R is hydrogen, C1-6alkyl, C3-6alkenyl, hydroxyC1-6alkyl or C1-6alkyloxy-C1-6alkyl; R is C1-6alkyl, mono- or diC3-6cycloalkylmethyl, phenylmethyl, substituted phenylmethyl, C1-6alkyloxy- C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C3-6alkenyl; or R and R taken together with the nitrogen to which they are attached may form a pyrrolidinyl, morpholinyl or piperidinyl group; X is N or CR ; R is hydrogen or C1-6alkyl; R is phenyl or substituted phenyl; A is -C(=O)-, (a), or -CR R - wherein R and R each independently are hydrogen or C1-4alkyl; R is hydrogen or OH, R is hydrogen or C1-6alkyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing these compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：式（I）的嘧啶和三嗪，其中R是C 1-6烷基，氨基，单或二C 1-6烷基氨基; R 1是氢，C 1-6烷基，C 3-6烯基，羟基C 1-6烷基或C 1-6烷氧基-C 1-6烷基; R 2是C 1-6烷基，单或二C 3-6环烷基甲基，苯甲基，取代的苯基甲基，C 1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基羰基C 1-6烷基，C 3-6烯基; 或R 1和R 2与它们所连接的氮一起可以形成吡咯烷基，吗啉基或哌啶基; X是N或CR 3; R 3为氢或C 1-6烷基; R 4是苯基或取代的苯基; A是-C（= O） - ，（a）或-CR 7 R 8 - ，其中R 5和R 6各自独立地是氢或C 1-4烷基; R 7是氢或OH，R 8是氢或C 1-6烷基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

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