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公开(公告)号：NO20064351L
公开(公告)日：2006-11-20
申请号：NO20064351
申请日：2006-09-26
Applicant: VERTEX PHARMA
Inventor： STUDLEY JOHN , CHARRIER JEAN-DAMIEN , MORTIMORE MICHAEL , DURRANT STEVEN , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , RAMAYA SHARN , TRUDEAU MARTIN , LOOKER ADAM
IPC: C07D207/16 , A61K31/439 , A61K38/04 , A61K38/06 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04
Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
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公开(公告)号：CA2768700A1
公开(公告)日：2005-09-29
申请号：CA2768700
申请日：2005-03-11
Applicant: VERTEX PHARMA
Inventor： TANOURY GERALD J , CHEN MINZHANG , JONES ANDREW D , NYCE PHILIP L , TRUDEAU MARTIN , GUERIN DAVID J , SNOONIAN JOHN R
IPC: C07D405/12 , C07B43/04 , C07B57/00
Abstract: The invention relates to processes such as that shown in the scheme and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
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公开(公告)号：AU2005223767A1
公开(公告)日：2005-09-29
申请号：AU2005223767
申请日：2005-03-11
Applicant: VERTEX PHARMA
Inventor： CHEN MINZHANG , JONES ANDREW D , TANOURY GERALD J , SNOONIAN JOHN R , NYCE PHILIP L , TRUDEAU MARTIN , GUERIN DAVID J
IPC: C07B43/04 , C07B57/00 , C07D405/12
Abstract: The invention relates to a process of producing a compound of comprising purifying a mixture of wherein R 8 is a protecting group, and purifying includes chromatographing, selectively crystallizing, or dynamically crystallizing the mixture.
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公开(公告)号：EA005680B1
公开(公告)日：2005-04-28
申请号：EA200200769
申请日：2001-01-16
Applicant: VERTEX PHARMA
Inventor： CHARIFSON PAUL , STAMOS DEAN , BADIA MICHAEL , GRILLOT ANNE-LAURE , RONKIN STEVEN , TRUDEAU MARTIN
IPC: C07D231/38 , A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/08 , A61P25/00 , A61P31/04 , A61P31/06 , A61P43/00 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14
Abstract: Настоящееизобретениеотноситсяк соединениямформулы (I)вкоторыхкольцоА означаеттиазол, оксазол, имидазолилипиразол, азаместителиявляютсятакими, какопределенов описании, ик егофармацевтическиприемлемымсолям. Соединениеингибируетактивностьбактериальнойгиразыи поэтомуиспользуетсядлялечениябактериальныхинфекционныхзаболеваниймлекопитающих.
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公开(公告)号：PT1251848E
公开(公告)日：2004-10-29
申请号：PT01903077
申请日：2001-01-16
Applicant: VERTEX PHARMA
Inventor： CHARIFSON PAUL , STAMOS DEAN , BADIA MICHAEL , GRILLOT ANNE-LAURE , RONKIN STEVEN , TRUDEAU MARTIN
IPC: C07D231/38 , A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/08 , A61P25/00 , A61P31/04 , A61P31/06 , A61P43/00 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14
Abstract: The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.
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Patent Agency Ranking
公开(公告)号：DK1251848T3
公开(公告)日：2004-10-18
申请号：DK01903077
申请日：2001-01-16
Applicant: VERTEX PHARMA
Inventor： RONKIN STEVEN , CHARIFSON PAUL , STAMOS DEAN , BADIA MICHAEL , GRILLOT ANNE-LAURE , TRUDEAU MARTIN
IPC: C07D231/38 , A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/08 , A61P25/00 , A61P31/04 , A61P31/06 , A61P43/00 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14
Abstract: The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.
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公开(公告)号：NZ520628A
公开(公告)日：2004-05-28
申请号：NZ52062801
申请日：2001-01-16
Applicant: VERTEX PHARMA
Inventor： CHARIFSON PAUL , STAMOS DEAN , BADIA MICHAEL , GRILLOT ANNE-LAURE , RONKIN STEVEN , TRUDEAU MARTIN
IPC: C07D231/38 , A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/08 , A61P25/00 , A61P31/04 , A61P31/06 , A61P43/00 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14
Abstract: A thiazol-5-yl pyrazole derivative or a pharmaceutically acceptable salt thereof has formula IA wherein: R1 is aliphatic, -C(R4)2(CH2)nNRCOR, -C(R4)=N-OR, -C(R4)=N-OC(=O)-aliphatic, -C(R4)=NNRCO2-aliphatic, -C(R4)=NNRCOR, -C(R4)=NN(R)2, -C(R4)2(CH2)nNRCO2-aliphatic, -CO2-aliphatic, -CON(R)2, -C(R4)2(CH2)nCON(R)2, -C(R4)2(CH2)nSO2N(R)2, -CONH-OR, -SO2N(R)2 or -C(R4)2(CH2)nNRSO2-aliphatic wherein the -CH2- and the aliphatic group can be optionally substituted group; n is 0 or 1; each R is independently hydrogen or an optionally substituted aliphatic group; R2 is hydrogen or, when R1 is -CO2-aliphatic or-CONH-aliphatic, R2 can be -halo, -CN, aliphatic, a three to five-membered heterocyclic, or a five-membered heteroaryl; Ring A is thiazole, oxazole, imidazole or pyrazole, with the imidazole being optionally attached by a C1-3 bridge from an imidazole ring nitrogen to Ar to form a five-to seven membered fused ring; Z is C-R3 or N-R3; R3 is- (CH2)pN(R5)2 or an optionally substituted aliphatic, heterocyclic, heterocyclylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; each R4 is independently hydrogen, an optionally substituted aliphatic group, or two R4 taken together with the carbon to which they are attached form a three to six membered aliphatic ring; each R5 is independently hydrogen, an optionally substituted aliphatic group, or two R5 taken together with the nitrogen to which they are attached form a five or six membered heterocyclic ring; p is 0 to 4 when Z is C-R3 or 1 to 4 when Z is N-R3 and Ar is an optionally substituted aryl, heteroaryl, or heterocyclic ring. The compounds are useful in treating bacterial infections.
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公开(公告)号：NO20032668L
公开(公告)日：2003-06-12
申请号：NO20032668
申请日：2003-06-12
Applicant: VERTEX PHARMA
Inventor： GRILLOT ANNE-LAURE , CHARIFSON PAUL S , STAMOS DEAN , LIAO YUSHENG , BADIA MICHAEL C , TRUDEAU MARTIN
IPC: C07D235/32 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/4245 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , A61P31/00 , A61P31/04 , A61P43/00 , C07D213/00 , C07D221/00 , C07D235/00 , C07D235/30 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/056 , C07D498/04 , C07D521/00 , C07F9/6558 , C07F9/6561
Abstract: The present invention relates to compounds of the formula I or a pharmaceutically acceptable derivative thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
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公开(公告)号：NO20032668A
公开(公告)日：2003-06-12
申请号：NO20032668
申请日：2003-06-12
Applicant: VERTEX PHARMA
Inventor： GRILLOT ANNE-LAURE , CHARIFSON PAUL S , STAMOS DEAN , LIAO YUSHENG , BADIA MICHAEL C , TRUDEAU MARTIN
IPC: C07D235/32 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/4245 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , A61P31/00 , A61P31/04 , A61P43/00 , C07D213/00 , C07D221/00 , C07D235/00 , C07D235/30 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/056 , C07D498/04 , C07D521/00 , C07F9/6558 , C07F9/6561
CPC classification number: C07D403/12 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07F9/65583 , C07F9/6561 , Y02A50/393 , Y02A50/473 , A61K2300/00
Abstract: The present invention relates to compounds of the formula I or a pharmaceutically acceptable derivative thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
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公开(公告)号：CZ20013349A3
公开(公告)日：2002-03-13
申请号：CZ20013349
申请日：2000-03-17
Applicant: VERTEX PHARMA
Inventor： STAMOS DEAN , TRUDEAU MARTIN , BETHIEL SCOTT , BADIA MICHAEL , SAUNDERS JEFFREY
IPC: C07D307/20 , A61K31/27 , A61K31/275 , A61K31/341 , A61K31/421 , A61K31/422 , A61K31/454 , A61K31/5377 , A61K31/541 , A61K45/00 , A61P1/18 , A61P9/10 , A61P11/06 , A61P19/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/02 , A61P43/00 , C07C275/40 , C07C275/42 , C07D263/32 , C07D413/12 , C07D417/12 , C07F9/653 , C07F9/143 , C07C275/30 , C07C275/34 , A61K31/17 , A61P31/00
Abstract: The present invention relates to compounds which inhibit JMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting JMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of I1VIPDH using the compounds of this invention and related compounds.
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