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1. 发明授权

US06277861B1 Anti-convulsant isoquinolyl-benzamide derivatives 失效
标题翻译：抗惊厥异喹啉基 - 苯甲酰胺衍生物
公开(公告)号：US06277861B1
公开(公告)日：2001-08-21
申请号：US09381369
申请日：1999-12-21
申请人： John David Harling , Barry Sidney Orlek , Mervyn Thompson
发明人： John David Harling , Barry Sidney Orlek , Mervyn Thompson
IPC分类号： A61K3147
CPC分类号： C07D217/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, where R1 is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), C1-6alkenyl, C1-6alkynyl, C1-6alkylCO—, formyl, CF3CO— or C1-6alkylSO2—; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3CO—, trifluoromethyldiazirinyl, C 1-6?alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO—, C1-6alkylCO—, C3-6cycloalkylO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS—, C1-6alkylSO2—, (C1-4alkyl)2NSO2—, (C1-4alkyl)NHSO2—, (C1-4alkyl)2NCO—, (C1-4alkyl)NHCO— or CONH2; or —NR5R6 where R5 is hydrogen or C1-4alkyl, and R6 is hydrogen, C1-4alkyl, formyl, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups together form a carbocyclic ring that is saturated or unsaturated and unsubstituted or substituted by —OH or ═O; and the two R3 groups and the two R4 groups are each independently hydrogen or C1-6alkyl or the two R3 groups and/or the two R4 groups together form a C3-6spiroalkyl group provided that at least one R3 and R4 group is not hydrogen, are useful in the treatment and prophylaxis of epilepsy and other disorders.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1为氢，C 1-6烷基（任选被羟基或C 1-4烷氧基取代），C 1-6烯基，C 1-6炔基，C 1-6烷基CO-，甲酰基，CF 3 CO-或C 1 烷基SO2-; R 2是氢或至多三个选自卤素，NO 2，CN，N 3，CF 3 O-，CF 3 S-，CF 3 CO-，三氟甲基二氮丙烯基，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6全氟烷基， C 1-6烷基，C 3-6环烷基-C 1-4烷基 - ，C 1-6烷基O - ，C 1-6烷基CO-，C 3-6环烷基O-，C 3-6环烷基CO-，C 3-6环烷基-C 1-4烷基O - ，C 3-6环烷基-C 1-4烷基CO-，苯基，苯氧基，苄氧基，苯甲酰基，苯基-C 1-4烷基 - ，C 1-6烷基-S-，C 1-6烷基SO 2 - ，（C 1-4烷基）2NSO 2 - ，（C 1-4烷基）NHSO 2 - ，（C 1-4烷基）2 CO-， -4-烷基）NHCO-或CONH 2; 或-NR5R6，其中R5是氢或C1-4烷基，R6是氢，C1-4烷基，甲酰基，-CO2C1-4烷基或-COC1-4烷基; 或两个R 2基团一起形成饱和或不饱和且未被取代或被-OH或= O取代的碳环; 并且两个R 3基团和两个R 4基团各自独立地为氢或C 1-6烷基，或者两个R 3基团和/或两个R 4基团一起形成C 3-6螺环烷基，条件是至少一个R 3和R 4

2. 发明授权

US5773463A Indane and tetrahydronaphthalene derivatives as calcium channel antagonists 失效
标题翻译：吲哚和四氢萘衍生物作为钙通道拮抗剂
公开(公告)号：US5773463A
公开(公告)日：1998-06-30
申请号：US583026
申请日：1996-01-22
申请人： John David Harling , Barry Sidney Orlek
发明人： John David Harling , Barry Sidney Orlek
IPC分类号： C07D307/84 , A61K31/135 , A61K31/275 , A61K31/34 , A61P3/00 , A61P3/14 , A61P9/10 , A61P25/00 , C07C211/38 , C07C211/53 , C07C215/44 , C07C217/52 , C07C255/54 , C07C271/24 , C07C323/30 , C07C323/62 , C07D307/79
CPC分类号： C07D307/79 , A61K31/135 , A61K31/275 , A61K31/34 , C07C211/53 , C07C217/52 , C07C255/54 , C07C323/30 , C07C2102/08 , C07C2102/10
摘要： This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.
摘要翻译： PCT No.PCT / EP94 / 02409 Sec。 371日期1996年1月22日 102（e）日期1996年1月22日PCT 1994年7月21日PCT公布。出版物WO95 / 0402800 日期1995年2月9日本发明描述了通式（I）的化合物（I）的氨基茚满和氨基四氢萘衍生物在其中Ar，X，R 1，R 2和n如权利要求1中定义的用于制备用于治疗其中指示钙通道拮抗剂的病症的药物。落入式（I）中的新化合物也被要求保护。

3. 发明授权

US5863952A Enantiomers of 1-(3,4-dichlorobenzyl)-2-methylaminoindane 失效
标题翻译： 1-（3,4-二氯苄基）-2-甲基氨基茚满对映异构体
公开(公告)号：US5863952A
公开(公告)日：1999-01-26
申请号：US860764
申请日：1997-07-11
申请人： Barry Sidney Orlek , John David Harling
发明人： Barry Sidney Orlek , John David Harling
IPC分类号： A61K31/135 , A61P3/00 , A61P3/14 , A61P9/10 , A61P25/00 , C07C211/42 , C07C271/24
CPC分类号： C07C211/42 , C07C2102/08
摘要： The single enantiomers of formula (I) and salts thereof ##STR1## are calcium channel antagonists useful in the treatment of ischaemic conditions e.g., stroke.
摘要翻译： PCT No.PCT / EP96 / 00206 Sec。 371日期：1997年6月11日 102（e）日期1997年6月11日PCT 1996年1月10日PCT PCT。公开号WO96 / 21641 日期：1996年7月18日式（I）的单一对映体及其盐式（I）是可用于治疗缺血性疾病例如中风的钙通道拮抗剂。

4. 发明授权

US6110934A Substituted benzamide derivatives and their use as anticonvulsants 失效
标题翻译：取代的苯甲酰胺衍生物及其作为抗惊厥药的用途
公开(公告)号：US6110934A
公开(公告)日：2000-08-29
申请号：US202524
申请日：1998-12-16
申请人： John David Harling , Barry Sidney Orlek , Mervyn Thompson
发明人： John David Harling , Barry Sidney Orlek , Mervyn Thompson
IPC分类号： A61K31/472 , C07D209/44 , C07D217/04 , C07D223/16 , C07D401/12 , A61K31/47
CPC分类号： C07D223/16 , A61K31/472 , C07D209/44 , C07D217/04 , C07D401/12
摘要： This invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at positions C4 and C5, being optionally substituted on the N atom of the heterocyclic system, and where the unsaturated ring of the heterocyclic system is a 5,6, 7 or 8-membered ring. Also to the use of these compounds as anticonvulsants in certain medical conditions, and to processes for making them.
摘要翻译： PCT No.PCT / EP97 / 03131 Sec。 371日期1998年12月16日第 102（e）日期1998年12月16日PCT提交1997年6月13日PCT公布。出版物WO97 / 48683 日期1997年12月24日本发明涉及通式（I）的取代苯甲酰氨基 - 杂环化合物，其在苯甲酰氨基的C2位具有烷氧基取代基和C4和C5位的各种取代基，任选在并且其中杂环体系的不饱和环是5,6,7或8元环。还涉及在某些医疗条件下使用这些化合物作为抗惊厥药，以及制备它们的方法。

5. 发明授权

US5817698A Substituted cycloalkylamine derivatives and their use as calcium channel antagonists 失效
标题翻译：取代的环烷基胺衍生物及其作为钙通道拮抗剂的用途
公开(公告)号：US5817698A
公开(公告)日：1998-10-06
申请号：US704585
申请日：1996-09-20
申请人： Thomas Henry Brown , John David Harling , Barry Sidney Orlek
发明人： Thomas Henry Brown , John David Harling , Barry Sidney Orlek
IPC分类号： A61K31/135 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07C211/35 , C07C211/37 , C07C217/52 , C07C225/20 , C07C255/49 , C07C323/26 , C07C323/30 , C07C323/50
CPC分类号： C07C225/20 , C07C217/52 , C07C323/26 , C07C2101/08
摘要： A method of treatment of a condition or disease related to the accumulation of calcium in the brain cells of a mammal which comprises administering to a subject in need thereof an effective amount of a compound of formula (I), wherein X is O, S, C.dbd.O or a bond; p and q are independently 0-4; R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkylC.sub.1-4 alkyl; n is 1, 2, 3 or 4; and Ar is phenyl optionally substituted by 1 to 3 substituents selected from; halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di- alkylamino and Ph(Alk.sup.1).sub.r Y(Alk.sup.2).sub.s -- where Ph is optionally substituted phenyl, Y is a bond, oxygen or a carbonyl group, Alk.sup.1 and Alk.sup.2 are independently C.sub.1-4 alkyl which may be straight or branched and r and s are independently 0 or 1, provided that the length of (Alk.sup.1).sub.r Y(Alk.sup.2).sub.s does not exceed 5 atoms, and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for the treatment of a disorder wherein a calcium channel antagonist is indicated, e.g. ischaemic stroke. Certain novel compounds within formula (I) are also claimed.
摘要翻译： PCT No.PCT / EP95 / 00964 Sec。 371日期：1996年9月20日 102（e）1996年9月20日PCT PCT 1995年3月14日PCT公布。公开号WO95 / 26327 日期1995年10月5日式（I）治疗与哺乳动物脑细胞中钙累积相关的病症或疾病的方法，其包括向有需要的受试者施用有效量的化合物式（I）的化合物，其中X为O，S，C = O或键; p和q独立地为0-4; R 1和R 2各自独立地选自氢，C 1-6烷基，C 3-6环烷基或C 3-6环烷基C 1-4烷基; n为1,2,3或4; 并且Ar是任选被1至3个选自下列的取代基取代的苯基; 卤素，C 1-4烷基，C 1-4烷氧基，C 1-2亚烷基二氧基，三氟甲基，三氟甲氧基，CN，NO 2，氨基，单 - 或二 - 烷基氨基和Ph（Alk 1）rY（Alk 2）s-，其中Ph是任选取代的苯基，Y是键，氧或羰基，Alk1和Alk2独立地为可以是直链或支链的C 1-4烷基，r和s独立地为0或1，条件是（Alk1）rY（Alk2）s的长度不超过5 原子及其药学上可接受的盐; 在制备用于治疗其中指示钙通道拮抗剂的病症的药物中，例如，缺血性中风。还要求公式（I）中的某些新化合物。

6. 发明申请

US20120058984A1 PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS 审中-公开
标题翻译：用作ITK抑制剂的吡咯烷酮衍生物
公开(公告)号：US20120058984A1
公开(公告)日：2012-03-08
申请号：US13257098
申请日：2010-03-15
申请人： Catherine Mary Alder , Ian Robert Baldwin , Nicholas Paul Barton , Amanda Jennifer Campbell , Aurelie Cecile Champigny , John David Harling , Aoife Caitriona Maxwell , Juliet Kay Simpson , Ian Edward David Smith , Christopher John Tame , Caroline Wilson , James Michael Woolven
发明人： Catherine Mary Alder , Ian Robert Baldwin , Nicholas Paul Barton , Amanda Jennifer Campbell , Aurelie Cecile Champigny , John David Harling , Aoife Caitriona Maxwell , Juliet Kay Simpson , Ian Edward David Smith , Christopher John Tame , Caroline Wilson , James Michael Woolven
IPC分类号： A61K31/506 , C07D417/14 , A61K31/5377 , A61K31/541 , A61P11/00 , A61P37/08 , A61P37/00 , A61P37/06 , A61P29/00 , A61P31/18 , A61P7/06 , A61P25/00 , A61P11/06 , A61P11/08 , A61P17/00 , A61P17/06 , A61P3/10 , A61P5/16 , A61P27/02 , A61P1/00 , C07D417/12
CPC分类号： C07D513/04 , C07D417/12 , C07D417/14
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是激酶活性的抑制剂，特别是Itk活性。

7. 发明授权

US07199239B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US07199239B2
公开(公告)日：2007-04-03
申请号：US10518778
申请日：2003-06-18
申请人： Paul John Beswick , John David Harling , Savvas Kleanthous , Millard Hurst Lambert, III , Vipulkumar Kantibhai Patel , Juliet Simpson
发明人： Paul John Beswick , John David Harling , Savvas Kleanthous , Millard Hurst Lambert, III , Vipulkumar Kantibhai Patel , Juliet Simpson
IPC分类号： C07D211/70 , C07D239/02 , C07D241/04 , C07C69/74
CPC分类号： C07D213/74 , C07C217/58 , C07C217/80 , C07C233/18 , C07C255/58 , C07C311/08 , C07C311/29 , C07C323/25 , C07C2601/02 , C07D239/42 , C07D241/20
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, Wherein: R1 and R2 are independently hydrogen or C1-3 alkyl; X represents a bond, CH2 or O; R3 and R4 are independently hydrogen, C1-6 alkyl, OCH3, CF3, allyl or halogen; X1 is CH2, SO2, or CO; R5 is —C1-6 alkyl (optionally substituted by C1-6alkoxy or C1-6alkylthio), —C2-6 alkenyl, —C0-6 alkyl phenyl (wherein the phenyl is optionally substituted by one or more CF3, halogen, C1-3 alkyl, C1-3 alkoxy), —COC1-6 alkyl, SO2C1-6 alkyl; R6 is phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 N atoms wherein the phenyl or heteroaryl group is optionally substituted with 1, 2 or 3 moieties selected from the group consisting of C1-6 alkyl, halogen, —OC1-6 alkyl, —SO2C1-3 alkyl, phenyl (optionally substituted by one or more groups selected from halogen, CF3, C1-3 alkyl, OC1-3 alkyl, acetyl, CN).
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂化物或可水解的酯，

8. 发明授权

US06245778B1 1,6-naphthyridine anti-convulsants 失效
标题翻译： 1,6-萘啶抗惊厥药
公开(公告)号：US06245778B1
公开(公告)日：2001-06-12
申请号：US09424399
申请日：1999-11-23
申请人： Michael Stewart Hadley , John David Harling , Frank Peter Harrington , Mervyn Thompson , Robert William Ward
发明人： Michael Stewart Hadley , John David Harling , Frank Peter Harrington , Mervyn Thompson , Robert William Ward
IPC分类号： A61K314375
CPC分类号： C07D471/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: where R1 is hydrogen, C1-6 alkyl optionally substituted by hydroxy or C1-4alkoxy, or C1-6 alkylphenyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, C1-6 alkylO-, C1-6 alkylS-, C1-6 alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3, CF3O, CF3CO—, C1-6alkylCO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR3R4 where R3 is hydrogen or C1-4 alkyl, and R4 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups form a saturated carbocyclic ring optionally interrupted by oxygen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy; are useful in the treatment and prophylaxis of inter alia epilepsy.
摘要翻译：式（I）化合物及其药学上可接受的盐：其中R 1是氢，任选被羟基或C 1-4烷氧基取代的C 1-6烷基或C 1-6烷基苯基; R 2是氢或至多三个选自卤素，NO 2，CN的取代基，N 3，C 1-6烷基，C 1-6烷基，C 1-6烷基，C 3-6环烷基，C 3-6环烷基-C 1-4烷基 - ，C 1-6烯基，C 1-6炔基，CF 3，CF 3 O，CF 3 CO-， C 3-6烷基CO-，C 3-6环烷基CO-，C 3-6环烷基-C 1-4烷基CO-，苯基，苯氧基，苄氧基，苯甲酰基，苯基-C 1-4烷基 - 或-NR 3 R 4，其中R 3是氢或C 1-4烷基，R 4是氢， 4个烷基，-CHO，-CO 2 C 1-4烷基或-COC 1-4烷基;或两个R 2基团形成任选被氧中断的饱和碳环; X选自氢，卤素，氰基，烷基和烷氧基;可用于处理和特别是癫痫预防。

9. 发明授权

US07235544B2 3-sulfonylamino-pyrrolidine-2-one derivatives as inhibitors of factor Xa 失效
标题翻译： 3-磺酰基氨基 - 吡咯烷-2-酮衍生物作为因子Xa的抑制剂
公开(公告)号：US07235544B2
公开(公告)日：2007-06-26
申请号：US10561328
申请日：2004-06-17
申请人： Alan David Borthwick , John David Harling , Wendy Rebecca Irving , Savvas Kleanthous , Nigel Stephen Watson , Robert John Young
发明人： Alan David Borthwick , John David Harling , Wendy Rebecca Irving , Savvas Kleanthous , Nigel Stephen Watson , Robert John Young
IPC分类号： A61K31/5377 , A61K31/381 , A61K31/397 , A61K31/402 , C07D411/10 , C07D401/10 , C07D207/12
CPC分类号： C07D207/273 , C07D401/10 , C07D403/10 , C07D409/12
摘要： The invention relates to compounds of formula (I): wherein substituents are as defined.
摘要翻译：本发明涉及式（I）的化合物：其中取代基如所定义。

10. 发明授权

US06410555B1 Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity 失效
标题翻译：具有抗惊厥活性的四氢萘并吡喃基甲酰胺
公开(公告)号：US06410555B1
公开(公告)日：2002-06-25
申请号：US09719335
申请日：2001-02-16
申请人： John David Harling , Frank Peter Harrington , Mervyn Thompson
发明人： John David Harling , Frank Peter Harrington , Mervyn Thompson
IPC分类号： A61K31435
CPC分类号： C07D471/04 , C07D471/10
摘要： Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1 is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), phenyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl; R2 is hydrogen or, up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3SO2—, CF3CO—, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkyl, C1-6alkylCO—, C3-6cycloalkylO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS—, C1-6alkylSO2—, (C1-4alkyl)2NSO2—, (C1-4alkyl)NHSO2—, (C1-4alkyl)2NCO—, (C1-4alkyl)NHCO— or CONH2; or —NR5R6 where R5 is hydrogen or C1-4alkyl, and R6 is hydrogen, C1-4alkyl, formyl, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups together form a carbocyclic ring that is saturated or unsaturated, optionally interrupted by O or NH; R3 groups and R4 groups are each independently hydrogen or C1-6alkyl and/or the two R3 groups and/or the two R4 groups together form a C3-6spiroalkyl group, provided that at least one R3 or R4 group is not hydrogen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy, are useful in the treatment and prophylaxis of epilepsy, migraine, and other disorders.
摘要翻译：式（I）化合物及其药学上可接受的盐和溶剂化物：其中R 1是氢，C 1-6烷基（任选被羟基或C 1-4烷氧基取代），苯基-C 1-4烷基 - ，C 1-6烯基，C 1-6炔基; R2是氢或最多三个选自卤素，NO 2，CN，N 3，CF 3 O-，CF 3 S-，CF 3 SO 2 - ，CF 3 CO-，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6全氟烷基，C 3-6环烷基，C 3-6环烷基-C 1-4烷基 - ，C 1-6烷基，C 1-6烷基CO-，C 3-6环烷基O-，C 3-6环烷基CO-，C 3-6环烷基-C 1-4烷基O - ，C 3-6环烷基-C 1-4烷基CO-，苯基，苯氧基，（C 1-4烷基）2 NSO 2 - ，（C 1-4烷基）NHSO 2 - ，（C 1-4烷基）2 NCO - ，（C 1-4烷基），C 1-4烷基）NHCO-或CONH 2; 或-NR5R6，其中R5是氢或C1-4烷基，R6是氢，C1-4烷基，甲酰基，-CO2C1-4烷基或-COC1-4烷基; 或两个R 2基团一起形成饱和或不饱和的碳环，任选被O或NH中断; R 3基团和R 4基团各自独立地为氢或C 1-6烷基和/或两个R 3基团和/或两个R 4基团一起形成C 3-6螺环烷基，条件是至少一个R 3或R 4基团不是氢; X选自氢，卤素，氰基，烷基和烷氧基

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