公开(公告)号：US5281593A

公开(公告)日：1994-01-25

申请号：US54914

申请日：1993-04-29

Applicant: Jeremy Gilmore ,  Alec Todd

Inventor： Jeremy Gilmore ,  Alec Todd

IPC: C07D401/10 ,  C07D401/14 ,  C07D417/14 ,  A61K31/47 ,  C07D401/12

CPC classification number: C07D401/14 ,  C07D401/10 ,  C07D417/14

Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C.sub.1-4 alkyl, aldehydo, --CH.sub.2 Z, --CH.dbd.CH--Z or --CH.sub.2 CH.sub.2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R.sup.2 is halo, nitrile, an optionally protected acid group or --CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl; R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl, or C.sub.1-4 alkyl substituted by --CONR.sup.7 R.sup.8 or an optionally protected acid group; R.sup.5 is ##STR2## where W is --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --O-- or --S--, R.sup.9 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl, and R.sup.10 is hydrogen, C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl; R.sup.6 is hydrogen or C.sub.1-4 alkyl; X is --O--(CH.sub.2).sub.n CR.sup.11 R.sup.12, --CR.sup.11 R.sup.12 --, --CR.sup.11 R.sup.12.(CH.sub.2).sub.n.CR.sup.13 R.sup.14 -- or --CR.sup.11 .dbd.CR.sup.12 -- where R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each hydrogen or C.sub.1-4 alkyl, and n is 0, 1 or 2; and Y is --O--CR.sup.15 R.sup.16 --, --CR.sup.15 .dbd.CR.sup.16 -- or --CR.sup.15 R.sup.16.CR.sup.17 R.sup.18 -- where R.sup.15, R.sup.16, R.sup.17 and R.sup.18 are each hydrogen or C.sub. 1-4 alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.

Abstract translation: 其中R 1为氢，卤素，C 1-4烷基，C 1-4烷氧基，腈，任意保护的羧基，任意保护的四唑基，三卤代甲基，羟基-C 1-4烷基，醛，-CH 2 Z， -CH = CH-Z或-CH 2 CH 2 Z，其中Z为任选保护的羧基或任选保护的四唑基; R 2是卤素，腈，任意保护的酸基或-CONR 7 R 8，其中R 7和R 8各自是氢或C 1-4烷基; R 3和R 4各自为氢，C 1-4烷基，任选取代的苯基或被-CONR 7 R 8或任选保护的酸基取代的C 1-4烷基; R5是 其中W是-CH = CH-，-CH = N-，-N = CH-，-O-或-S-，R9是氢，卤素，C1-4烷基，C1- 4烷氧基或三卤甲基，R 10是氢，C 1-4烷基，C 2-6烯基，C 3-6环烷基或C 1-4烷基-C 3-6环烷基; R6是氢或C1-4烷基; X是-O-（CH 2）n CR 11 R 12，-CR 11 R 12 - ， - CR 11 R 12。（CH 2）n CR 1 R 14 - 或-CR 11 = CR 12 - ，其中R 11，R 12，R 13和R 14各自是氢或C 1-4烷基，n是 0，1或2; 并且Y是-O-CR 15 R 16 - ， - CR 15 = CR 16 - 或-CR 15 R 16 CR 17 R 18 - ，其中R 15，R 16，R 17和R 18各自是氢或C 1-4烷基; 或其盐。 未保护形式的化合物作为白三烯拮抗剂是活性的。

公开(公告)号：US07619096B2

公开(公告)日：2009-11-17

申请号：US10558626

申请日：2004-05-11

Applicant: Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

Inventor： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

IPC: C07D207/00 ,  A61K31/40 ,  C07D295/00 ,  A01N43/36

CPC classification number: C07D207/14 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其可用于抑制一种或多种生理活性单胺（5-羟色胺，去甲肾上腺素和多巴胺）摄取。

公开(公告)号：US20060079554A1

公开(公告)日：2006-04-13

申请号：US10536295

申请日：2003-11-25

Applicant: Peter Barry ,  Manuel Cases-Thomas ,  Peter Gallagher ,  Jeremy Gilmore ,  John Masters ,  Graham Timms ,  Maria Whatton ,  Virginia Wood

Inventor： Peter Barry ,  Manuel Cases-Thomas ,  Peter Gallagher ,  Jeremy Gilmore ,  John Masters ,  Graham Timms ,  Maria Whatton ,  Virginia Wood

IPC: A61K31/445 ,  C07D211/56

CPC classification number: C07D405/12 ,  C07D211/58

Abstract: N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.

Abstract translation: 通式（I）的N，N-二取代的4-氨基 - 哌啶是5-羟色胺和/或去甲肾上腺素和/或多巴胺摄取的抑制剂。 因此，它们可用于治疗中枢和/或周围神经系统的病症。

公开(公告)号：US07335660B2

公开(公告)日：2008-02-26

申请号：US10496535

申请日：2002-12-06

Applicant: Javier Agejas-Chicharro ,  Graham Henry Timms ,  Andrew Caerwyn Williams ,  Nicholas Paul Camp ,  Jeremy Gilmore ,  Ana Belen Bueno Melendo ,  Carlos Lamas-Peteira

Inventor： Javier Agejas-Chicharro ,  Graham Henry Timms ,  Andrew Caerwyn Williams ,  Nicholas Paul Camp ,  Jeremy Gilmore ,  Ana Belen Bueno Melendo ,  Carlos Lamas-Peteira

IPC: A61K31/496 ,  C07D311/76 ,  C07D405/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/06 ,  C07D413/14 ,  C07D413/04 ,  C07D407/06 ,  C07D409/14 ,  C07D405/04 ,  C07D417/12 ,  C07D405/12

CPC classification number: C07D405/06 ,  C07D307/87 ,  C07D311/76 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the treatment of central nervous system disorders, such as depression, bipolar disorder, and anxiety.

Abstract translation: 本发明涉及其中R 1至R 12，-WV-，-XY-，p和n具有权利要求1中定义的值的式（I）化合物， 其制备和用作药物用于治疗中枢神经系统疾病，例如抑郁症，双相性精神障碍和焦虑症。

公开(公告)号：US5410061A

公开(公告)日：1995-04-25

申请号：US962365

申请日：1992-10-16

Applicant: Jeremy Gilmore ,  John R. Harris

Inventor： Jeremy Gilmore ,  John R. Harris

IPC: A61K31/47 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07D401/10 ,  A61K31/475

CPC classification number: C07D401/12 ,  C07D401/14

Abstract: A compound having pharmaceutical activity, of the formula ##STR1## in which A is hydrogen or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 0 or 1 to 4, R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl and R.sup.3 is --CN, --COOH, tetrazolyl or --CONHSO.sub.2 R.sup.4 where R.sup.4 is optionally substituted phenyl, and ##STR2## where R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x, R.sup.1, R.sup.2 and R.sup.3 are as defined above, and R.sup.7 is hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 1 to 4, and R.sup.1, R.sup.2 and R.sup.3 are as defined above;provided that when A is hydrogen at least one of R.sup.5, R.sup.6 and R.sup.7is --(CR.sup.1 R.sup.2).sub.x R.sup.3, and provided that when ##STR3## A is --(CR.sup.1 R.sup.2).sub.x R.sup.3 and x is 1 to 4 then R.sup.3 is --CONHSO.sub.2 R.sup.4 ;and salts and esters thereof.

Abstract translation: 具有药物活性的化合物，其中A为氢或 - （CR 1 R 2）x R 3，其中x为0或1至4，R 1和R 2为氢或C 1-4烷基，R 3为 - CN，-COOH，四唑基或-CONHSO 2 R 4，其中R 4是任选取代的苯基，和其中R 5和R 6各自是氢，C 1-4烷基或 - （CR 1 R 2）x R 3，其中x，R 1，R 2 和R 3如上所定义，并且R 7是氢，C 1-4烷基或 - （CR 1 R 2）x R 3，其中x是1至4，并且R 1，R 2和R 3如上定义; 条件是当A为氢时，R 5，R 6和R 7中的至少一个为 - （CR 1 R 2）x R 3，并且条件是当A为 - （CR 1 R 2）x R 3且x为1至4时，R 3为-CONHSO 2 R 4; 及其盐和酯。

公开(公告)号：US20070066663A1

公开(公告)日：2007-03-22

申请号：US10558588

申请日：2004-05-25

Applicant: Christopher Beadle ,  Manuel Cases-Thomas ,  Barry Clark ,  Peter Gallagher ,  John Masters ,  Graham Timms ,  Magnus Walter ,  Maria Whatton ,  Virginia Wood ,  Jeremy Gilmore

Inventor： Christopher Beadle ,  Manuel Cases-Thomas ,  Barry Clark ,  Peter Gallagher ,  John Masters ,  Graham Timms ,  Magnus Walter ,  Maria Whatton ,  Virginia Wood ,  Jeremy Gilmore

IPC: A61K31/41

CPC classification number: C07D405/12 ,  C07D211/56 ,  C07D453/02

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其可用于抑制一种或多种生理活性单胺（5-羟色胺，去甲肾上腺素和多巴胺）摄取。

公开(公告)号：US5185361A

公开(公告)日：1993-02-09

申请号：US761587

申请日：1991-09-18

Applicant: Jeremy Gilmore

Inventor： Jeremy Gilmore

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P7/10 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/08

CPC classification number: C07D209/08

Abstract: A pharmaceutical compound of the formula ##STR1## in which A is selected from --NHCOR.sup.1, --NHCOOR.sup.1, --NHCONHR.sup.1, --NHCSNHR.sup.1, --CONHR.sup.1, where R.sup.1 is optionally halo-substituted C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl or phenyl-C.sub.1-4 alkyl B is optionally substituted phenyl, and --X--Y-- is --CH=CH-- or --CH.sub.2 --CH.sub.2 --; and salts thereof. The compounds are leukotriene antagonists.

公开(公告)号：US07432280B2

公开(公告)日：2008-10-07

申请号：US10558588

申请日：2004-05-25

Applicant: Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

Inventor： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

IPC: A01N43/90 ,  A01N43/40 ,  A61K31/44 ,  A61K31/445 ,  C07D453/02 ,  C07D211/56 ,  C07D211/98

CPC classification number: C07D405/12 ,  C07D211/56 ,  C07D453/02

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其可用于抑制一种或多种生理活性单胺（5-羟色胺，去甲肾上腺素和多巴胺）摄取。

公开(公告)号：US06509476B1

公开(公告)日：2003-01-21

申请号：US09637434

申请日：2000-08-11

Applicant: Nicholas James Bach ,  Stephen Richard Baker ,  Jeremy Gilmore ,  Russell Andrew Lewthwaite ,  Alexander McKillop ,  Jason Scott Sawyer ,  George Richard Stephenson ,  Michael William John Urquhart

Inventor： Nicholas James Bach ,  Stephen Richard Baker ,  Jeremy Gilmore ,  Russell Andrew Lewthwaite ,  Alexander McKillop ,  Jason Scott Sawyer ,  George Richard Stephenson ,  Michael William John Urquhart

IPC: A61K3140

CPC classification number: C07D401/14 ,  A61K31/4725 ,  C07D209/08

Abstract: This invention relates to a method of making N-benzyl indoles, and to intermediates for use in the method, and to certain substantially optically pure N-benzyl indoles obtained by the method.

Abstract translation: 本发明涉及制备N-苄基吲哚的方法和用于本方法的中间体，以及通过该方法获得的某些基本上光学上纯的N-苄基吲哚。

公开(公告)号：US5563147A

公开(公告)日：1996-10-08

申请号：US462237

申请日：1995-06-05

Applicant: Jeremy Gilmore ,  Peter T. Gallagher ,  Martin V. Miles ,  William M. Owton ,  Colin W. Smith

Inventor： Jeremy Gilmore ,  Peter T. Gallagher ,  Martin V. Miles ,  William M. Owton ,  Colin W. Smith

IPC: C07D471/04 ,  A61K31/44

CPC classification number: C07D471/04

Abstract: This invention provides novel, optionally substituted tetrahydropyridoindoles which are useful serotonergic agents for the treatment of central nervous system disorders.

Abstract translation: 本发明提供了新颖的任选取代的四氢吡啶并吲哚，其是用于治疗中枢神经系统疾病的有用的5-羟色胺能药。