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1. 发明申请

US20120028953A1 Azetidine Derivatives 有权
标题翻译：氮杂环丁烷衍生物
公开(公告)号：US20120028953A1
公开(公告)日：2012-02-02
申请号：US12920181
申请日：2009-02-27
申请人： Stephen Roughley , Steven Walls , Terance Hart , Rachel Parsons , Paul Brough , Christopher Graham , Alba Macias
发明人： Stephen Roughley , Steven Walls , Terance Hart , Rachel Parsons , Paul Brough , Christopher Graham , Alba Macias
IPC分类号： A61K31/397 , C07D401/12 , C07D401/14 , C07D413/14 , A61K31/4427 , A61K31/506 , A61K31/497 , A61K31/501 , A61K31/444 , A61K31/4439 , A61P29/00 , A61P1/08 , A61P25/00 , A61P25/08 , A61P9/00 , A61P9/10 , A61P35/00 , A61P37/00 , A61P37/08 , A61P33/00 , A61P31/12 , A61P31/04 , A61P19/10 , A61P1/00 , C07D205/04
CPC分类号： A61K31/506 , A61K31/397 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/497 , A61K31/501 , C07D205/04 , C07D401/12 , C07D401/14 , C07D413/14
摘要： Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
摘要翻译：式（I）化合物是脂肪酰胺水解酶（FAAH）的抑制剂，它们可用于治疗由于抑制FAAH活性而引起的疾病或医学病症，例如焦虑，抑郁症，炎症和饮食，睡眠，神经变性和运动障碍：式（I）其中Ar1是任选取代的苯基或具有5或6个环原子的任选取代的单环杂芳基; Ar2是任选取代的苯基，任选取代的具有5或6个环原子的单环杂芳基或在每个稠环中具有5或6个环原子的任选取代的稠合双环杂芳基; 并且Ar 3是选自任选取代的亚苯基和具有5或6个环原子的任选取代的单环亚芳基的二价基团。

2. 发明授权

US08450346B2 Azetidine derivatives as FAAH inhibitors 有权
标题翻译：氮杂环丁烷衍生物作为FAAH抑制剂
公开(公告)号：US08450346B2
公开(公告)日：2013-05-28
申请号：US12920181
申请日：2009-02-27
申请人： Stephen Roughley , Steven Walls , Terance Hart , Rachel Parsons , Paul Brough , Christopher Graham , Alba Macias
发明人： Stephen Roughley , Steven Walls , Terance Hart , Rachel Parsons , Paul Brough , Christopher Graham , Alba Macias
IPC分类号： A61K31/397 , A61K31/4427 , A61K31/495 , C07D205/00 , C07D213/24 , C07D237/10
CPC分类号： A61K31/506 , A61K31/397 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/497 , A61K31/501 , C07D205/04 , C07D401/12 , C07D401/14 , C07D413/14
摘要： Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
摘要翻译：式（I）化合物是脂肪酰胺水解酶（FAAH）的抑制剂，它们可用于治疗由于抑制FAAH活性而引起的疾病或医学病症，例如焦虑，抑郁症，炎症和饮食，睡眠，神经变性和运动障碍：式（I）其中Ar1是任选取代的苯基或具有5或6个环原子的任选取代的单环杂芳基; Ar2是任选取代的苯基，任选取代的具有5或6个环原子的单环杂芳基或在每个稠环中具有5或6个环原子的任选取代的稠合双环杂芳基; 并且Ar 3是选自任选取代的亚苯基和具有5或6个环原子的任选取代的单环亚芳基的二价基团。

3. 发明申请

US20070112192A1 3-(2-Hydroxy-phenyl)-1h-pyrazole-4-carboxylic acid amide derivatives as hsp90 inhibitors for the treatment of cancer 失效
标题翻译： 3-（2-羟基 - 苯基）-1H-吡唑-4-羧酸酰胺衍生物作为治疗癌症的hsp90抑制剂
公开(公告)号：US20070112192A1
公开(公告)日：2007-05-17
申请号：US10536898
申请日：2003-12-04
申请人： Mandy Beswick , Paul Brough , Martin Drysdale , Brian Dymock
发明人： Mandy Beswick , Paul Brough , Martin Drysdale , Brian Dymock
IPC分类号： C07D413/00
CPC分类号： C07D231/14 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Compounds of formula (IA) or (IB) or salts, N-oxides. hydrates or solvates thereof are Inhibitors of HSP90, and useful in the treatment of, for example, cancer: formula (IA), formula (IB) wherein Ar is an aryl or heteroaryl radical which is linked via a ring carbon, and which is substituted by a hydroxy group on a carbon in the 2-position, and which is otherwise either unsubstituted or optionally substituted; R1 is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and R3 is a carboxamide group.
摘要翻译：式（IA）或（IB）的化合物或其盐，N-氧化物。水合物或溶剂化物是HSP90的抑制剂，可用于治疗例如癌症：式（IA），式（IB）其中Ar是通过环碳连接且被取代的芳基或杂芳基通过2-位上的碳上的羟基，其另外是未取代的或任选被取代的; R 1是氢或任选取代的C 1 -C 6烷基; R 2是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C C 6链烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团; R 3是甲酰胺基。

4. 发明申请

US20100010037A1 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：US20100010037A1
公开(公告)日：2010-01-14
申请号：US12438809
申请日：2007-08-17
申请人： Paul Brough , Martin Drysdale
发明人： Paul Brough , Martin Drysdale
IPC分类号： A61K31/437 , C07D471/02 , A61P35/04
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-Alk1-(Z)m-(Alk2)n-Q (IA) wherein X is a bond, —O—, —S—, —S(O)—, —SO2—, or —NH—, Z is —O—, —S—, —(C═O)—, —(C═S)—, —S(O)—, —SO2—, —NRA—, or, in either orientation —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (—CN), fluoro, chloro, bromo, methyl, ethyl, —OH, —CH2OH, —C(═O)NH2, —C(═O)H, —C(═O)CH3, or —NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (—CN), C1-C3alkyl optionally substituted with one or more fluorine substituents, C1-C3alkoxy optionally substituted with one or more fluorine substituents, —CH═CH2, —C≡CH, cyclopropyl and —NH2, or R3 and R4 together represent methylenedioxy (—OCH2O—) or ethylenedioxy (—OCH2CH2O—) in either of which one or more hydrogens are optionally replaced by fluorine; S1 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-Alk1-（Z）m-（Alk2）nQ（IA）其中X是键，-O - ， - S-， -S（O） - ， - SO 2 - 或-NH-，Z是-O-，-S-， - （CO） - ， - （CS） - ， - （S） - ， - SO 2 - NR - ， - 取代-C（ - O）O-，-C（ - ） - NRA，-C（ - ） - NRA - ， - SO2NRA-，-NRAC（-O） - 或-NRASO2 - 其中RA是氢或其中一个或多个氢任选被氟取代的C 1 -C 6烷基; Alk1和Alk2是任选取代的二价C1-C3亚烷基或C2-C3亚烯基，m和n分别为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 2，-C（-O）H，-C（-O） NH2; R 3和R 4独立地选自氢，氟，氯，溴，氰基（-CN），任选被一个或多个氟取代基取代的C 1 -C 3烷基，任选被一个或多个氟取代基取代的C 1 -C 3烷氧基，-CH-CH 2， -C≡CH，环丙基和-NH 2，或者R 3和R 4一起代表亚甲二氧基（-OCH 2 O-）或亚乙二氧基（-OCH 2 CH 2 O-），其中一个或多个氢任选被氟取代; S1如说明书中所定义。

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