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92. 发明授权

EP2941425B1 AMINOPYRIDINE DERIVED COMPOUNDS AS LRRK2 INHIBITORS 有权
标题翻译：氨基吡啶衍生的化合物，如LRRK2抑制剂
公开(公告)号：EP2941425B1
公开(公告)日：2017-07-12
申请号：EP13815781.3
申请日：2013-12-30
申请人： H. Lundbeck A/S , Vernalis (R&D) Ltd.
发明人： MIKKELSEN, Gitte Kobberøe , DAVID, Laurent , WATSON, Stephen , SMITH, Garrick Paul , WILLIAMSON, Douglas Stewart , CHEN, I-Jen
IPC分类号： C07D401/14 , C07D413/14 , C07D401/04 , C07D403/14 , C07D413/04 , A61K31/4439 , A61K31/444 , A61K31/497 , A61P25/16 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/4439 , A61K31/4545 , A61K31/497 , C07D401/04 , C07D401/14 , C07D403/14 , C07D413/04 , C07D413/14

93. 发明授权

EP2207780B1 THIENOPYRIMIDINE COMPOUNDS AND COMPOSITIONS 有权
标题翻译：噻吩并嘧啶化合物和组合物
公开(公告)号：EP2207780B1
公开(公告)日：2013-05-15
申请号：EP08806335.9
申请日：2008-09-19
申请人： Vernalis (R&D) Ltd.
发明人： JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
IPC分类号： C07D495/04 , A61K31/33 , A61P11/00
CPC分类号： C07D495/04

94. 发明授权

EP1722798B1 PYRIMIDINE COMPOUNDS AS PURINE RECEPTOR ANTAGONISTS 有权
标题翻译：嘧啶化合物嘌呤受体拮抗剂
公开(公告)号：EP1722798B1
公开(公告)日：2010-10-20
申请号：EP05708320.6
申请日：2005-02-11
申请人： VERNALIS (R&D) LTD
发明人： GILLESPIE, Roger John, Vernalis (R & D) Ltd , WILLIAMSON, Douglas Stewart, Vernalis (R & D) Ltd
IPC分类号： A61K31/496 , A61K31/506 , A61P21/00 , C07D239/48
CPC分类号： C07D409/14 , C07D401/12 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of formula (1); wherein R1 is optionally substituted C1-C3alkyl C2-C3alkenyl, or C2-C3alkynyl, or -NR6R1, -ORB, -SR9 or halogen; R3 is H; optionally substituted C,-Csalkyl, C2-C6alkenyl, C2C6alkynyl, or C3-C7 cycloalkyl, halogen; OH or OR10; R4 is H, optionally substituted C1C6alkyl, C3-C6alkenyl, C3-C6alkynyl, C3-C7 cycloalkyl, aryl or heteroaryl, R5 is H or Optionally substituted C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, or C3-C7 cycloalkyl; or R4 and R5 together form a 5 or 6-membered heterocyclic ring; and R7, R8, R9 and R10 are optionally substituted C1-C3alkyl, C2-C3alkenyl, C2-C3alkynyl, or C3-C7 cycloalkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease.

95. 发明公开

EP2207780A1 THIENOPYRIMIDINE COMPOUNDS AND COMPOSITIONS 有权
标题翻译：噻吩并嘧啶化合物和组合物
公开(公告)号：EP2207780A1
公开(公告)日：2010-07-21
申请号：EP08806335.9
申请日：2008-09-19
申请人： Vernalis (R&D) Ltd.
发明人： JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
IPC分类号： C07D495/04 , A61K31/33 , A61P11/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6 alkoxy-( C1-C6 )-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-( C1-C6 )-alkyl, or heteroaryl-( C1-C6 )-alkyl; or R-1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-( C1-C6 )-alkyl, C3- C8 cycloalkyl, aryl, heteroaryl, aryl-( C1-C6 )-alkyl, or heteroaryl- C1-C6 )-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-( C1-C6 )-alkyl, - NHR7 -N(-R8)-R9, -NH-(C=O)-R10, -(C=O)-NH-R11, -(C=O)-O-R12, or halo; and R7, R8, R9, R10, R-11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-( C1-C6 )-alkyl and heteroaryl.
摘要翻译：式（I）化合物是其中R 1和R 2独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - -C 6） - 烷基或杂芳基 - （C 1 -C 6） - 烷基; 或者R-1和R 2与它们所连接的氮原子一起形成任选取代的5元或6元环; （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C 1 -C 6） - 烷基或杂芳基-C 1 -C 6） - 烷基; 或者R 3和R 4与它们所连接的氮原子一起形成任选取代的5元或6元环; R 5和R 6独立地选自氢，C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基，-NHR 7 -N（-R 8）-R 9，-NH-（C = O）-R 10， - C = O）-NH-R11， - （C = O）-O-R12或卤素; 和R 7，R 8，R 9，R 10，R 11和R 12独立地选自C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基和杂芳基。

96. 发明公开

EP1833797A1 AZACYCLIC COMPOUNDS AS INHBITORS OF SENSORY NEURONE SPECIFIC CHANNELS (SNS) 审中-公开
标题翻译：氮杂化合物作为抑制剂SNS（感觉神经元特异性的）信道
公开(公告)号：EP1833797A1
公开(公告)日：2007-09-19
申请号：EP06700329.3
申请日：2006-01-06
申请人： VERNALIS (R&D) LTD
发明人： HAMLYN, Richard, Ionix Pharmaceuticals Limited , HUCKSTEP, Mike, Ionix Pharmaceuticals Limited , EARNSHAW, Christopher G., Ionix Pharm. Limited , STOKES, Stephen, Ionix Pharmaceuticals Limited , TICKLE, David, Ionix Pharmaceuticals Limited , ALLART, Brigitte, Ionix Pharmaceuticals Limited , BOYD, Joseph William, Ionix Pharm. Limited , KNUTSEN, Lars Jacob S., Ionix Pharm. Limited , LYNCH, Rosemary, Ionix Pharmaceuticals Limited , PATIENT, Lee, Ionix Pharmaceuticals Limited
IPC分类号： C07D217/04 , A61K31/472 , C07D209/48 , A61K31/4035 , A61P25/04 , A61P25/06 , C07D401/12 , A61K31/4725 , C07D417/04 , A61K31/5415 , C07D413/04 , A61K31/538 , C07D405/12 , C07D495/04 , A61K31/4365
CPC分类号： C07D495/04 , C07D209/48 , C07D217/04 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06
摘要： Compounds of the formula (I) , and pharmaceutically acceptable salts thereof , are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents. wherein: - Ar represents a phenyl ring or a 5 - to 6- membered heteroaryl group; - m is 1 , 2 or 3 .

97. 发明申请

WO2014106612A1 AMINOPYRIDINE DERIVED COMPOUNDS AS LRRK2 INHIBITORS 审中-公开
标题翻译：氨基吡啶衍生化合物作为LRRK2抑制剂
公开(公告)号：WO2014106612A1
公开(公告)日：2014-07-10
申请号：PCT/EP2013/078105
申请日：2013-12-30
申请人： H. LUNDBECK A/S , VERNALIS (R&D) LTD.
发明人： MIKKELSEN, Gitte Kobberøe , DAVID, Laurent , WATSON, Stephen , SMITH, Garrick Paul , WILLIAMSON, Douglas Stewart , CHEN, I-Jen
IPC分类号： C07D401/14 , C07D413/14 , C07D401/04 , C07D403/14 , C07D413/04 , A61K31/4439 , A61K31/444 , A61K31/497 , A61P25/16 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/4439 , A61K31/4545 , A61K31/497 , C07D401/04 , C07D401/14 , C07D403/14 , C07D413/04 , C07D413/14
摘要： The present invention is directed to aminopyridine derived compounds of formula (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such a Lewy body dementia, Parkinson's disease or cancer.
摘要翻译：本发明涉及氨基吡啶衍生的式（A）化合物。该化合物被认为可用于治疗与LRRK2相关的疾病如路易体痴呆，帕金森病或癌症。

98. 发明申请

WO2011010083A1 INDOLYL-PYRIDONE DERIVATIVES 审中-公开
标题翻译：吲哚基吡啶衍生物
公开(公告)号：WO2011010083A1
公开(公告)日：2011-01-27
申请号：PCT/GB2010/001360
申请日：2010-07-16
申请人： VERNALIS (R & D) LTD , STOKES, Stephen , FOLOPPE, Nicolas , FIUMANA, Andrea , DRYSDALE, Martin , BEDFORD, Simon , WEBB, Paul
发明人： STOKES, Stephen , FOLOPPE, Nicolas , FIUMANA, Andrea , DRYSDALE, Martin , BEDFORD, Simon , WEBB, Paul
IPC分类号： C07D401/14 , A61K31/4412 , A61P35/00
CPC分类号： C07D401/14
摘要： Compounds of formula (I) are inhibitors of Chk1, useful in the treatment of, inter alia, cancers: wherein R 1 , R 2 , R 5 and R 6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxy methyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R 3 , and R 4 are independently selected from hydrogen, hydroxy, C 1 -C 3 alkyl, fluoro-(C 1 -C 3 )-alkyl, hydroxy-(C 1 -C 3 )-alkyl, C 1 -C 3 alkoxy, fluoro-(C 1 -C 3 )-alkoxy, hydroxy-(C 1 -C 3 )-alkoxy, -N(R 11 )-R 12 , -AIk-N(R 11 )-R 12 , -0-AIk-N(R 11 )-R 12 , -C(=O)OH, carboxy-(C 1 -C 3 )-alkyl, or -C(=O)-NH-R 13 ; AIk is a straight or branched chain divalent C 1 -C 6 alkylene radical; R 7 and R 8 are independently selected from hydrogen, hydroxy, or C 1 -C 3 alkoxy; X is a straight chain divalent C 1 -C 3 alkylene radical, optionally substituted on one or more carbons by R 9 and/or R 10 ; W is selected from -C(=O)-N(-R 16 )- or -N(-R 17 )-C(=O)-; Y is hydrogen, C 1 -C 3 alkyl, C 1 -C 3 alkoxy, or halo; and Q is an optionally substituted 5-membered monocyclic heteroaryl ring.
摘要翻译：式（I）化合物是Chk1的抑制剂，可用于治疗尤其是癌症：其中R1，R2，R5和R6独立地选自氢，羟基，甲基，三氟甲基，羟基甲基，甲氧基，三氟甲氧基，甲基氨基和二甲基氨基; R3和R4独立地选自氢，羟基，C1-C3烷基，氟 - （C1-C3） - 烷基，羟基 - （C1-C3） - 烷基，C1-C3烷氧基，氟 - （C1-C3）烷氧基，羟基 - （C 1 -C 3） - 烷氧基，-N（R 11）-R 12，-A 1 k -N（R 11）-R 12，-O-Alk-N（R 11）-R 12，-C（= O）羧基 - （C 1 -C 3） - 烷基或-C（= O）-NH-R 13; Alk是直链或支链二价C1-C6亚烷基; R 7和R 8独立地选自氢，羟基或C 1 -C 3烷氧基; X是直链的二价C1-C3亚烷基，任选地被一个或多个碳上被R9和/或R10取代; W选自-C（= O）-N（-R 16） - 或-N（-R 17）-C（= O） - ; Y是氢，C 1 -C 3烷基，C 1 -C 3烷氧基或卤素; 且Q为任选取代的5元单环杂芳基环。

99. 发明申请

WO2008104595A1 ACID ADDITION SALTS, HYDRATES AND POLYMORPHS OF 5-(2,4-DIHYDROXY-5-ISOPROPYL-PHENYL)-4-(4-MORPHOLIN-4-YLMETHYL-PHENYL)-ISOXAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE AND FORMULATIONS COMPRISING THESE FORMS 审中-公开
标题翻译： 5-（2,4-二羟基-5-异丙基苯基）-4-（4-吗啉-4-基 - 甲基 - 苯基） - 异恶唑-3-羧酸乙酰胺和包含这些形式的制剂的酸加成盐，水合物和多元醇
公开(公告)号：WO2008104595A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/052443
申请日：2008-02-28
申请人： NOVARTIS AG , VERNALIS (R & D) LTD. , DRYSDALE, Martin James , DYMOCK, Brian William , KRELL, Christoph , MUTZ, Michael , PETERSEN, Holger , ZHENG, Weijia
发明人： DRYSDALE, Martin James , DYMOCK, Brian William , KRELL, Christoph , MUTZ, Michael , PETERSEN, Holger , ZHENG, Weijia
IPC分类号： A61K31/5377 , C07D295/00 , A61P35/00
CPC分类号： C07D295/155 , A61K31/5377 , C07D261/18
摘要： The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4- morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4- ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.
摘要翻译：本发明涉及5-（2,4-二羟基-5-异丙基 - 苯基）-4-（4-吗啉-4-基甲基 - 苯基） - 异恶唑-3-甲酸乙酰胺的新盐形式，特别是甲磺酸盐，盐酸盐，酒石酸盐，磷酸盐和半富马酸盐; 到这种盐的结晶形式; （4-二羟基-5-异丙基 - 苯基）-4-（4-吗啉-4-基甲基 - 苯基） - 异恶唑-3-甲酸乙酰胺的多晶型物; 到上述新盐形式的水合物和多晶型物; 使用上述新的盐形式来制备用于治疗由Hsp90介导的病症的药物; 涉及使用新的盐形式治疗由Hsp90介导的病症的方法; 包括这种盐形式的制剂，特别是适于静脉内施用的水溶液; 以及填充这种制剂的琥珀色玻璃容器。

100. 发明申请

WO2008025947A1 1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES USEFUL AS HSP90 INHIBITORS 审中-公开
标题翻译： 1H-PYRROLO [2,3-B]吡啶衍生物作为HSP90抑制剂有用
公开(公告)号：WO2008025947A1
公开(公告)日：2008-03-06
申请号：PCT/GB2007/003133
申请日：2007-08-17
申请人： VERNALIS (R & D) LTD. , BROUGH, Paul , DRYSDALE, Martin
发明人： BROUGH, Paul , DRYSDALE, Martin
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) have HSP90 inhibitory activity: ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-Alk 1 -(Z) m -(Alk 2 ) n -Q (IA) wherein X is a bond, -O-, -S-, -S(O)-, -SO 2 -, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO 2 -, -NR A -, or, in either orientation -C(=O)O-, -C(=O)NR A -, -C(=S)NR A -, -SO 2 NR A -, -NR A C(=O)-, or -NR A SO 2 - wherein R A is hydrogen or C 1 -C 6 alkyl in which one or more hydrogens is optionally substituted by fluorine;Alk 1 and AIk 2 are optionally substituted divalent C 1 -C 3 alkylene:or C 2 -C 3 alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH 2 OH, -C(=O)NH 2 ,-C(=O)H, -C(=O)CH 3 , or -NH 2 ; R 3 and R 4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C 1 -C 3 alkyl optionally substituted with one or more fluorine substituents, C 1 -C 3 alkoxy optionally substituted with one or more fluorine substituents, -CH=CH 2 , -C≡CH, cyclopropyl and -NH 2 , or R 3 and R 4 together represent methylenedioxy (-OCH 2 O-) or ethylenedioxy (-OCH 2 CH 2 O-) in either of which one or more hydrogens are optionally replaced by fluorine; S 1 is as defined in the description.
摘要翻译：式（I）化合物具有HSP90抑制活性：环A是芳基或杂芳基环或环系; R 1是氢，氟，氯，溴或式（1A）的基团：-X-Alk - （Z）m - （Alk 2）其中X为键，-O - ， - S - ， - S（O） - ， - SO 2 - ，或-NH-，Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - S（O） - ， - SO 2 - ，或者在任一取向-C（= O）O - ， - C（= O）NR A - ， - C（= S），C（= O） - ， - NR 2 - ， - C（= O） - ， - 其中R A是氢或C 1 -C 6 - ，其中R A是氢或C 1 -C 6 - 其中一个或多个氢任选被氟取代的烷基; Alk 1和Alk 2是任选取代的二价C 1 -C 1烷基，亚烷基：或C 2 -C 3亚烯基，m和n独立地为0或1，Q为氢或任选取代的碳环或杂环基; R 2是氰基（-CN），氟，氯，溴，甲基，乙基，-OH，-CH 2 OH，-C（= O）NH _{如说明书中所定义。}

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