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41. 发明申请

US20100144787A1 Quinolines and Their Therapeutic Use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US20100144787A1
公开(公告)日：2010-06-10
申请号：US12531935
申请日：2008-04-03
申请人： John Gary Montana , Harry Finch , George Hynd , Michael Colin Cramp , Rosa Arienzo , Neville McLean
发明人： John Gary Montana , Harry Finch , George Hynd , Michael Colin Cramp , Rosa Arienzo , Neville McLean
IPC分类号： A61K31/4709 , C07D215/233 , C07D215/227 , C07D215/12 , A61P11/06 , A61P11/08 , A61P11/16 , A61P11/02
CPC分类号： C07D401/10 , C07D215/227 , C07D215/233 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(═O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.
摘要翻译：式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R1是卤素或氰基; R2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6烷基或C 3 -C 6环烷基，后两个基团任选被一个或多个卤素原子取代; R5是氢或卤素; R6是C1C6烷基或C3-C6环烷基，其任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y1中的一个是氢，另一个是选自本说明书中提到的那些的OR 6，-C（= O）R 7，NR 8 SO 2 R 6或杂环基; R6，R7和R8如说明书中所定义。

42. 发明申请

US20100144786A1 QUINOLINE DERIVATIVES AS CRTH2 RECEPTOR LIGANDS 审中-公开
标题翻译：喹啉衍生物作为CRTH2受体配体
公开(公告)号：US20100144786A1
公开(公告)日：2010-06-10
申请号：US12531367
申请日：2007-03-29
申请人： Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
发明人： Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
IPC分类号： A61K31/47 , C07D215/233 , A61P17/02 , A61P11/06 , A61P37/06 , A61P17/06
CPC分类号： C07D215/233 , C07D215/20 , C07D215/227
摘要： Specific quinoline derivatives are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component.
摘要翻译：特定的喹啉衍生物是可用于治疗具有炎性成分的病症的CRTH2拮抗剂。

43. 发明授权

US07705027B2 Isoxazole compounds as inhibitors of heat shock proteins 有权
标题翻译：异恶唑化合物作为热休克蛋白的抑制剂
公开(公告)号：US07705027B2
公开(公告)日：2010-04-27
申请号：US10544443
申请日：2004-02-09
申请人： Martin James Drysdale , Brian William Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen Elizabeth James , Kwai Ming Cheung , Thomas Peter Matthews
发明人： Martin James Drysdale , Brian William Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen Elizabeth James , Kwai Ming Cheung , Thomas Peter Matthews
IPC分类号： C07D261/06 , A01N43/80
CPC分类号： A61K31/541 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D261/08 , C07D261/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D495/04
摘要： Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
摘要翻译：式（A）或（B）的异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症：（A），（B）其中R1是式（IA）的基团：-Ar1-（Alk1 ）对 - （Z）r-（Alk 2）sQ，其中在任何相容的组合中，Ar 1是任选取代的芳基或杂芳基，Alk1和Alk2是任选取代的C 1 -C 6亚烷基或C 2 -C 6亚烯基，p，r和 s是独立的0或1，Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O）其中RA为氢或C 1 -C 6烷基，Q为氢或任选地为（C 1 -C 6）烷基，取代的碳环或杂环基; R2是（i）上述式（IA）的基团或（ii）甲酰胺基团; 或（iii）非芳族碳环或杂环，其中环碳任选被取代，和/或环氮任选被式 - （Alk1）对（Z）r-（Alk2）sQ基团取代，其中Q ，Alk1，Alk2，Z，p，r和s如上文关于组（IA）所定义; 并且R 3是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团。

44. 发明申请

US20090182033A1 Cyclic Amine Derivatives and Their Uses 审中-公开
标题翻译：环胺衍生物及其用途
公开(公告)号：US20090182033A1
公开(公告)日：2009-07-16
申请号：US12096563
申请日：2006-12-14
申请人： Harry Finch , Nicholas Charles Ray , Monique Bodil Van Niel , Phillip Smith
发明人： Harry Finch , Nicholas Charles Ray , Monique Bodil Van Niel , Phillip Smith
IPC分类号： A61K31/381 , C07D409/06 , C07C211/40 , C07C69/76 , C07D311/84 , A61K31/352 , A61K31/24 , A61K31/135 , A61P1/00 , A61P11/00 , A61P9/00 , A61P11/06 , A61P11/08 , A61P11/02
CPC分类号： C07C271/38 , C07C217/52 , C07C219/24 , C07C2602/42 , C07D311/86 , C07D333/24
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group -R5 or a group, -Z-Y—R5, or a group -Z-NR9R10, or a group -Z-N(R9)C(O)R11; and R3 is a lone pair, or C1-C6-alkyl; R4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R5 is an C1-C6-alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R6 is C1-C6-alkyl or a hydrogen atom; R7a and R7b area C1-C6-alkyl group or halogen; n and m are independently 0, 1, 2 or 3; R8a and R8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl and hydrogen; R8c is —OH, C1-C6-alkyl, hydroxy-C1-C6-alkyl, or a hydrogen atom; R8d is C1-C6-alkyl or a hydrogen atom; R9 and R10 are independently a hydrogen atom, C1-C6-alkyl, aryl aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C1-C6-alkyl)-, or heteroaryl(C1-C6-alkyl)-group; or R9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 4-8 atoms, optionally containing a further nitrogen or oxygen atom; R11 is C1-C6-alkyl or a hydrogen atom; Ar1 is aryl, heteroaryl or cycloalkyl; Ar2 are independently aryl, heteroaryl or cycloalkyl; and Q is an oxygen atom, —CH2—, —CH2CH2— or a bond.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中R 1是C 1 -C 6 - 烷基或氢原子; 并且R 2是氢原子或基团-R 5或基团-Z-Y-R 5或基团-Z-NR 9 R 10或基团-Z-N（R 9）C（O）R 11; 且R 3为孤对或C 1 -C 6 - 烷基; R4选自式（a），（b），（c）或（d）中的一个; 式（a），（b），（c），（d），Z是C 1 -C 16亚烷基，C 2 -C 16亚烯基或C 2 -C 16亚炔基; Y是键或氧原子; R5是C1-C6烷基，芳基，芳基烷基; 芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C1-C8-烷基） - ，杂芳基（C1-C8-烷基） - ，环烷基或杂环烷基; R6是C1-C6-烷基或氢原子; R7a和R7b区域C1-C6-烷基或卤素; n和m独立地为0,1,2或3; R8a和R8b独立地选自芳基，芳基稠合的杂环烷基，杂芳基，C1-C6-烷基，环烷基和氢; R8c是-OH，C1-C6-烷基，羟基-C1-C6-烷基或氢原子; R8d是C1-C6-烷基或氢原子; R9和R10独立地为氢原子，C1-C6-烷基，芳基芳基稠合 - 杂环烷基，芳基 - 稠合 - 环烷基，杂芳基，芳基（C1-C6-烷基） - 或杂芳基（C1-C6-烷基）组; 或R 9和R 10与它们所连接的氮原子一起形成4-8个原子的杂环，任选地含有另外的氮或氧原子; R11是C1-C6-烷基或氢原子; Ar1是芳基，杂芳基或环烷基; Ar2独立地为芳基，杂芳基或环烷基; 且Q为氧原子，-CH 2 - ， - CH 2 CH 2 - 或键。

45. 发明申请

US20090111795A1 Multimers of Heterocyclic Compounds and Their Use 审中-公开
标题翻译：多元杂环化合物及其用途
公开(公告)号：US20090111795A1
公开(公告)日：2009-04-30
申请号：US11814615
申请日：2006-02-03
申请人： Harry Finch , Christine Edwards , Nicholas Charles Ray , Anne O'Connor , Mary F. Fitzgerald
发明人： Harry Finch , Christine Edwards , Nicholas Charles Ray , Anne O'Connor , Mary F. Fitzgerald
IPC分类号： A61K31/551 , C07D403/14 , A61K31/497 , A61P11/00
CPC分类号： C07D239/22 , A61K31/513 , A61K47/55 , C07D401/12 , C07D403/14
摘要： A compound of formula (I): M-L-M, wherein L is a linker and each M is independently a group of formula (II): is useful in therapy, e.g. of respiratory diseases.
摘要翻译：式（I）的化合物：M-L-M，其中L是连接基，每个M独立地是式（II）的基团：可用于治疗，例如，的呼吸系统疾病。

46. 发明申请

US20080318913A1 Combination of Methylxanthine Compounds and Steroids to Treat Chronic Respiratory Diseases 有权
标题翻译：甲基黄嘌呤化合物和类固醇联合治疗慢性呼吸道疾病
公开(公告)号：US20080318913A1
公开(公告)日：2008-12-25
申请号：US11883635
申请日：2006-02-13
申请人： Justian Craig Fox , Mary Frances Fitzgerald , Harry Finch
发明人： Justian Craig Fox , Mary Frances Fitzgerald , Harry Finch
IPC分类号： A61K31/56 , A61P11/08
CPC分类号： A61K31/58 , A61K31/52 , A61K2300/00
摘要： There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery.
摘要翻译：提供甲基黄嘌呤衍生物如茶碱和类固醇在协同组合中用于治疗慢性阻塞性肺疾病的用途，其中所述组合由吸入途径施用用于肺部递送。

47. 发明申请

US20080318912A1 Medicaments for Treating Chronic Respiratory Disease 审中-公开
标题翻译：治疗慢性呼吸道疾病的药物
公开(公告)号：US20080318912A1
公开(公告)日：2008-12-25
申请号：US11659458
申请日：2005-08-03
申请人： Craig Fox , Harry Finch , Mary Fitzgerald
发明人： Craig Fox , Harry Finch , Mary Fitzgerald
IPC分类号： A61K31/58 , A61P11/00
CPC分类号： A61K31/52 , A61K31/573 , A61K2300/00
摘要： There is provided the use of a methylxanthine compound and a steroid in a synergistic combination for the treatment of a respiratory disease, wherein the methylxanthine compound is administered at a dose, which, in isolation, is not effective to treat said disease.
摘要翻译：提供了用于治疗呼吸系统疾病的协同组合中的甲基黄嘌呤化合物和类固醇的用途，其中所述甲基黄嘌呤化合物以分开的方式施用，所述剂量不能有效地治疗所述疾病。

48. 发明授权

US06228853B1 Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase 失效
标题翻译：吡咯并吡咯啉酮衍生物作为嗜中性粒细胞弹性蛋白酶抑制剂
公开(公告)号：US06228853B1
公开(公告)日：2001-05-08
申请号：US09508326
申请日：2000-06-02
申请人： Michael Dennis Dowle , Harry Finch , Lee Andrew Harrison , Graham George Adam Inglis , Martin Redpath Johnson , Simon John Fawcett MacDonald
发明人： Michael Dennis Dowle , Harry Finch , Lee Andrew Harrison , Graham George Adam Inglis , Martin Redpath Johnson , Simon John Fawcett MacDonald
IPC分类号： C07D48702
CPC分类号： C07D487/04
摘要： According to the invention are provided compounds of formula (I) (relative stereochemistry indicated) wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (I) are useful inter alia in the treatment of inflammatory diseases of the respiratory tract.
摘要翻译：根据本发明，提供式（I）化合物（所示的相对立体化学），其中R1，R2和R3如说明书中所定义。式（I）化合物特别可用于治疗呼吸道炎症性疾病。

49. 发明授权

US5994344A Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase 失效
标题翻译：吡咯并吡咯啉酮衍生物作为嗜中性粒细胞弹性蛋白酶抑制剂
公开(公告)号：US5994344A
公开(公告)日：1999-11-30
申请号：US155323
申请日：1998-09-25
申请人： Michael Dennis Dowle , Harry Finch , Lee Andrew Harrison , Graham George Inglis , Martin Redpath Johnson , Simon John Fawcett Macdonald , Pritom Shah , Robin Andrew Smith
发明人： Michael Dennis Dowle , Harry Finch , Lee Andrew Harrison , Graham George Inglis , Martin Redpath Johnson , Simon John Fawcett Macdonald , Pritom Shah , Robin Andrew Smith
IPC分类号： A61K20060101 , A61K31/00 , A61K31/40 , A61K31/407 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P1/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/00 , A61P13/12 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D207/14 , C07D487/04
CPC分类号： C07D487/04 , C07D207/14
摘要： There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.
摘要翻译： PCT No.PCP / EP97 / 01530 Sec。 371日期：1998年9月25日 102（e）日期1998年9月25日PCT 1997年3月26日PCT公布。公开号WO97 / 36903 日本1997年10月9日根据本发明描述了式（I）化合物（所示的相对立体化学），其中R1，R2，R3和X如说明书中所定义，以及其制备方法，含有它们的组合物和它们用作药物。式（I）的化合物尤其用于治疗慢性支气管炎。

50. 发明授权

US5646140A 1,5-benzodiazepine derivatives having CCK antagonistic or agonistic activity 失效
标题翻译：具有CCK拮抗或激动活性的1,5-苯并二氮杂衍生物
公开(公告)号：US5646140A
公开(公告)日：1997-07-08
申请号：US525659
申请日：1995-10-13
申请人： Elizabeth Ellen Sugg , Christopher Joseph Aquino , Jerzy Ryszard Szewczyk , Harry Finch , Robin Arthur Ellis Carr
发明人： Elizabeth Ellen Sugg , Christopher Joseph Aquino , Jerzy Ryszard Szewczyk , Harry Finch , Robin Arthur Ellis Carr
IPC分类号： A61K38/00 , A61K31/551 , A61K38/02 , A61P3/00 , A61P5/00 , A61P43/00 , C07D243/12 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097 , A61K31/55
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/0207 , C07K5/06139 , C07K5/06191 , C07K5/0827 , A61K38/00
摘要： This invention pertains to novel benzodiazepine compounds of formula (I) ##STR1## which exhibit agonistic activity for CCK-A receptors, enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals for use in medicine as anorectic agents in the regulation of appetite, the treatment of obesity and the maintenance of weight loss.

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