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21. 发明授权

US06903085B1 Substituted piperidine compounds useful as modulators of chemokine receptor activity 失效
标题翻译：可用作趋化因子受体活性调节剂的取代哌啶化合物
公开(公告)号：US06903085B1
公开(公告)日：2005-06-07
申请号：US10069215
申请日：2000-08-18
申请人： Stephen Thom , Andrew Baxter , Nicholas Kindor , Thomas McInally , Brian Springthorpe , Matthew Perry , David Harden , Richard Evans , David Marriott
发明人： Stephen Thom , Andrew Baxter , Nicholas Kindor , Thomas McInally , Brian Springthorpe , Matthew Perry , David Harden , Richard Evans , David Marriott
IPC分类号： C07D473/34 , A61K31/4468 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/52 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P19/08 , A61P25/00 , A61P25/06 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/04 , C07D487/04 , C07D491/056 , C07D495/04 , C07D513/04 , A61K31/33 , A61K31/435 , A61K31/445 , C07D211/00 , C07D413/00
CPC分类号： C07D401/12 , C07D211/58 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 6， Z，Q，m，n，X 1，X 2，X 3，X 4和T分别为如本说明书中所定义的，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是用于治疗趋化因子受体相关疾病和病症

22. 发明授权

US06566376B1 Diphenyl-piperidine derivative 失效
标题翻译：二苯基 - 哌啶衍生物
公开(公告)号：US06566376B1
公开(公告)日：2003-05-20
申请号：US09623744
申请日：2000-09-08
申请人： Andrew J G Baxter , Stephen J Brough , Thomas McInally
发明人： Andrew J G Baxter , Stephen J Brough , Thomas McInally
IPC分类号： A61K31445
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： The invention provides compounds of general formula (I) wherein R1, R2, R3, R4, A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.
摘要翻译：本发明提供了通式（I）的化合物，其中R 1，R 2，R 3，R 4，A，Q，U，V，W，X，Y和n如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的应用，特别是治疗趋化因子受体相关疾病和病症。

23. 发明授权

US06303659B2 Compounds 失效
公开(公告)号：US06303659B2
公开(公告)日：2001-10-16
申请号：US09745740
申请日：2000-12-26
申请人： Andrew Baxter , Thomas McInally , Michael Mortimore , David Cladingboel
发明人： Andrew Baxter , Thomas McInally , Michael Mortimore , David Cladingboel
IPC分类号： A61K31166
CPC分类号： C07D203/14 , C07C233/65 , C07C235/46 , C07C235/60 , C07C237/30 , C07C323/62 , C07C2603/74 , C07D209/08 , C07D213/82 , C07D233/64 , C07D295/13
摘要： The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

24. 发明授权

US06303613B1 Aminopyrimidine derivatives, processes for their preparation, compositions containing them and their use as pharmaceuticals 失效
标题翻译：氨基嘧啶衍生物，其制备方法，含有它们的组合物及其作为药物的用途
公开(公告)号：US06303613B1
公开(公告)日：2001-10-16
申请号：US09101165
申请日：1998-08-19
申请人： Thomas McInally , Alan Tinker
发明人： Thomas McInally , Alan Tinker
IPC分类号： A61K31519
CPC分类号： C07D471/04 , C07D495/04
摘要： There are provided novel compounds of formula (I) wherein: A represents a five membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S; or a six membered heterocyclic aromatic ring containing 1 to 3 nitrogen atoms; and R1, R2, R3 and R4 are as defined in the Specification and pharmaceutically acceptable salts thereof and enantiomers and tautomers thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
摘要翻译：提供式（I）的新化合物，其中：A表示含有1至3个可以相同或不同并且选自O，N和S的杂原子的五元杂环芳环; 或含有1至3个氮原子的六元杂环芳环; 并且R 1，R 2，R 3和R 4如本说明书及其药学上可接受的盐及其对映异构体和互变异构体中所定义; 以及其制备方法，含有它们的组合物及其在治疗中的用途。这些化合物是一氧化氮合酶的抑制剂，因此特别可用于治疗或预防炎性疾病和疼痛。

25. 发明授权

US5883102A Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
公开(公告)号：US5883102A
公开(公告)日：1999-03-16
申请号：US793713
申请日：1997-03-03
申请人： Peter Hamley , Austen Pimm , Alan Tinker , Haydn Beaton , Thomas McInally
发明人： Peter Hamley , Austen Pimm , Alan Tinker , Haydn Beaton , Thomas McInally
IPC分类号： A61K20060101 , A61K31/00 , A61K31/505 , A61K31/517 , A61K31/529 , A61K31/55 , A61P29/00 , C07D20060101 , C07D239/70 , C07D239/94 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/10 , C07D487/10 , C07F7/08 , A01N43/54 , C07D237/00 , C07D239/72
CPC分类号： C07D401/04 , C07D239/70 , C07D239/94 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D471/10 , C07D487/10 , C07F7/0812
摘要： Compounds of formula (I) wherein: R.sup.1 and R.sup.19 independently represent hydrogen, alkyl C1-6, alkoxy C1-6, alkylthio C1-6, halogen, hydroxyl or amino;R.sup.2 represents H or alkyl;R.sup.3 represents phenyl, a 6-membered heterocyclic aromatic ring containing one or two nitrogen atoms, or a 5-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O,N, and S, which phenyl or heterocyclic aromatic ring may be optionally substituted by alkyl C1-6, alkoxy C1-6, haologen, hydroxyl, alkylthio C1-6, cyano, trifluoromethyl, nitro, hydroxymethyl, amino, a group --(CH.sub.2).sub.c NHCO.sub.2 R.sup.10, a group --(CH.sub.2).sub.c NR.sup.5 R.sup.6, or a group --CO.sub.2 R.sup.11 ; or R.sup.3 represents hydrogen or alkyl C1-8, which alkyl group may be optionally substituted by amino or a group --NHCO.sub.2 R.sup.10 ;R.sup.4 represents hydrogen or alkyl C1-6; orR.sup.3 and R.sup.4 taken together represent a group (CH.sub.2).sub.a Z(CH.sub.2).sub.b ;c represents an integer 0 to 2;and pharmaceutically acceptable salts thereof, have been found to be useful as a pharmaceuticals. The compounds may especially be used in the treatment of inflammatory disorders.
摘要翻译： PCT No.PCT / GB96 / 02496 Sec。 371日期1997年3月3日 102（e）1997年3月3日PCT PCT 1996年10月14日PCT公布。出版物WO97 / 14686 （I）式（I）化合物其中：R 1和R 19独立地表示氢，烷基C 1-6，烷氧基C 1-6，烷硫基C 1-6，卤素，羟基或氨基; R2代表H或烷基; R3表示苯基，含有一个或两个氮原子的6元杂环芳环，或含有1至3个选自O，N和S的杂原子的5元杂环芳环，该苯基或杂环芳环可以任选被取代通过烷基C 1-6，烷氧基C 1-6，羟基，羟基，烷硫基C 1-6，氰基，三氟甲基，硝基，羟甲基，氨基， - （CH 2）c NHCO 2 R 10基团 - （CH 2）c NR 5 R 6， CO2R11; 或R 3表示氢或烷基C 1-8，该烷基可任选被氨基或基团-NHCO 2 R 10取代; R4代表氢或烷基C1-6; 或R 3和R 4一起表示基团（CH 2）a Z（CH 2）b; c表示0〜2的整数，已经发现其药学上可接受的盐可用作药物。该化合物可特别用于治疗炎症性疾病。

26. 发明授权

US08268990B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US08268990B2
公开(公告)日：2012-09-18
申请号：US12274915
申请日：2008-11-20
申请人： Nicholas J. Bennett , Thomas McInally , Stephen Thom
发明人： Nicholas J. Bennett , Thomas McInally , Stephen Thom
IPC分类号： C07D201/16
CPC分类号： C07D239/48 , C07D239/49 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D417/12
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3和R 4如说明书中所定义，及其药学上可接受的盐，以及其制备方法，含有它们的药物组合物及其在治疗中的用途。

27. 发明申请

US20080300244A1 NOVEL COMPOUNDS 失效
标题翻译：新型化合物
公开(公告)号：US20080300244A1
公开(公告)日：2008-12-04
申请号：US11955984
申请日：2007-12-13
申请人： Roger Victor BONNERT , Thomas McInally , Tobias Mochel , Stephen Thom
发明人： Roger Victor BONNERT , Thomas McInally , Tobias Mochel , Stephen Thom
IPC分类号： A61K31/5377 , C07D473/34 , A61P35/00 , A61P11/00
CPC分类号： C07D473/18
摘要： The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供下式的化合物，其中R1，Y1，X1，Z1，X2，Y2，A，n和R2如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

28. 发明申请

US20050250792A1 Substituted piperidine compounds useful as modulators of chemokine receptor activity 审中-公开
标题翻译：可用作趋化因子受体活性调节剂的取代哌啶化合物
公开(公告)号：US20050250792A1
公开(公告)日：2005-11-10
申请号：US11081201
申请日：2005-03-16
申请人： Stephen Thom , Andrew Baxter , Nicholas Kindor , Thomas McInally , Brian Springthorpe , Matthew Perry , David Harden , Richard Evans , David Marriott
发明人： Stephen Thom , Andrew Baxter , Nicholas Kindor , Thomas McInally , Brian Springthorpe , Matthew Perry , David Harden , Richard Evans , David Marriott
IPC分类号： C07D473/34 , A61K31/4468 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/52 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P19/08 , A61P25/00 , A61P25/06 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/04 , C07D487/04 , C07D491/056 , C07D495/04 , C07D513/04 , A61K31/505 , A61K31/455
CPC分类号： C07D401/12 , C07D211/58 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention provides compounds of formula (I): wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.
摘要翻译：本发明提供式（I）化合物：其中R 1，R 2，R 3，R 6，，Z，Q，m，n，X 1，X 2，X 3，X 4和T 如本说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是用于治疗趋化因子受体相关疾病和病症。

29. 发明授权

US06201024B1 Adamantane derivatives 有权
公开(公告)号：US06201024B1
公开(公告)日：2001-03-13
申请号：US09230478
申请日：1999-01-26
申请人： Andrew Baxter , Thomas McInally , Michael Mortimore , David Cladingboel
发明人： Andrew Baxter , Thomas McInally , Michael Mortimore , David Cladingboel
IPC分类号： A61K31166
CPC分类号： C07D203/14 , C07C233/65 , C07C235/46 , C07C235/60 , C07C237/30 , C07C323/62 , C07C2603/74 , C07D209/08 , C07D213/82 , C07D233/64 , C07D295/13
摘要： The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

30. 发明授权

US4607041A Antihypertensive 2-phenyl Hantzsch dihydropyridines 失效
标题翻译：抗高血压2-苯基汉坦二氢吡啶类
公开(公告)号：US4607041A
公开(公告)日：1986-08-19
申请号：US601389
申请日：1984-04-17
申请人： Andrew J. G. Baxter , John Dixon , Thomas McInally , Alan C. Tinker
发明人： Andrew J. G. Baxter , John Dixon , Thomas McInally , Alan C. Tinker
IPC分类号： C07C17/093 , C07C45/00 , C07C47/55 , C07C205/56 , C07D205/04 , C07D211/78 , C07D211/90 , C07D305/08 , C07D309/12 , C07D401/04 , C07D405/04 , C07D413/04 , C07D521/00 , A61K31/445 , C07D413/14
CPC分类号： C07D231/12 , C07C17/093 , C07C205/56 , C07C45/00 , C07C47/55 , C07D205/04 , C07D211/78 , C07D211/90 , C07D233/56 , C07D249/08 , C07D305/08 , C07D309/12 , C07D401/04 , C07D405/04 , C07D413/04
摘要： There are described compounds of formula I, ##STR1## in which R.sub.1 represents benzofurazanyl, pyridyl or phenyl, the pyridyl or phenyl being substituted by one or more of the groups halogen, nitro, --CN, --OR.sub.9, --S(O).sub.p R.sub.9, or alkyl C1 to 6 optionally substituted by halogen,p is 0, 1 or 2,R.sub.2 and R.sub.3, which may be the same or different, each represent hydrogen; alkyl C1 to 6 optionally substituted by one or more of the groups halogen, cyano, --XR.sub.4, --NR.sub.5 R.sub.6 or phenyl; cycloalkyl C3 to 8 optionally substituted by alkyl C1 to 6; a 4, 5 or 6 membered oxygen or nitrogen containing heterocyclic ring which is optionally substituted by alkyl C1 to 6 the alkyl in turn optionally being substituted by one or more phenyl groups;R.sub.5 and R.sub.6, which may be the same or different, each represent alkyl C1 to 6 optionally substituted by phenyl,Y and Z together form a bond, and additionally, when R.sub.8 is an electron withdrawing group Y may be hydrogen and Z may be hydroxy,one of R.sub.7 and R.sub.8 represents alkyl C1 to 6 and the other represents phenyl,or R.sub.7 and R.sub.8 may be the same or different and each represents phenyl optionally substituted by one or more of alkyl C1 to 6, halogen, alkoxy C1 to 6 or nitro; amino; alkyl C1 to 6 substituted by halogen; --CN; --CH.sub.2 OH; --CHO or --CH(OR.sub.9).sub.2,X is O or S,R.sub.4 is alkyl C1 to 6 or phenyl,R.sub.9 is alkyl C1 to 6, with certain provisons.There are also described processes for making the compounds, and their formulation and use as pharmaceuticals for treatment of hypertension, angina, or congestive heart failure.
摘要翻译：描述式Ⅰ化合物，其中R1代表苯并呋喃基，吡啶基或苯基，吡啶基或苯基被一个或多个卤素，硝基，-CN，-OR9，-S（O） pR9或任选被卤素取代的C 1-6的烷基，p为0,1或2，R 2和R 3可以相同或不同，各自表示氢; 任选被一个或多个卤素，氰基，-XR 4，-NR 5 R 6或苯基基团取代的C 1-6烷基; 任选被C1至6的烷基取代的环烷基C3至8; 任选被烷基C1至6取代的4,5或6元含氧或含氮杂环，所述烷基依次可选地被一个或多个苯基取代; R 5和R 6可以相同或不同，各自表示任选被苯基取代的烷基C1至6，Y和Z一起形成键，另外，当R8是吸电子基团时，Y可以是氢，Z可以是羟基 R 7和R 8中的一个表示烷基C1至6，另一个表示苯基，或者R 7和R 8可以相同或不同，表示任选被一个或多个烷基C1至6，卤素，烷氧基C1至6或硝基氨基; 由卤素取代的C1至6烷基; -CN; -CH 2 OH; -CHO或-CH（OR 9）2，X为O或S，R 4为C 1-6烷基或苯基，R 9为烷基C 1-6，具有一定条件。还描述了制备化合物的方法及其制剂和用作治疗高血压，心绞痛或充血性心力衰竭的药物。

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