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公开(公告)号:US20050020503A1
公开(公告)日:2005-01-27
申请号:US10850101
申请日:2004-05-20
Applicant: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
Inventor: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
CPC classification number: A61K31/4709 , A61K38/06 , A61K38/212 , C07K5/0808 , C07K5/0827 , Y02A50/463 , A61K2300/00
Abstract: Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
Abstract translation: 式(I)化合物:其中B,X,R 3,L 0,L 1,L 2,R 2,R 1和R C如本文所定义。 该化合物可用作用于治疗丙型肝炎病毒感染的HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US20120077737A1
公开(公告)日:2012-03-29
申请号:US12952777
申请日:2010-11-23
Applicant: Montse Llinas-Brunet , Josée Bordeleau , Cédrickx Godbout , Mélissa Leblanc , Benoît Moreau , Jeffrey O'Meara
Inventor: Montse Llinas-Brunet , Josée Bordeleau , Cédrickx Godbout , Mélissa Leblanc , Benoît Moreau , Jeffrey O'Meara
CPC classification number: C07D487/04 , A61K31/4709
Abstract: Compounds of the invention, which are macrocyclic peptide analogs containing an acylsulfonamide moiety, maintain good activity against NS3 proteases containing clinically relevant resistance mutations for this class as represented by genotype 1a R155K, genotype 1b D168V and genotype 1a D168V resistance mutations. The compounds of the invention are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
Abstract translation: 作为含有酰基磺酰胺部分的大环肽类似物的本发明化合物对于含有基因型1a R155K,基因型1b D168V和基因型1a D168V抗性突变所表示的该类临床相关抗性突变的NS3蛋白酶保持良好的活性。 本发明的化合物可用作治疗丙型肝炎病毒感染的HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US20060046965A1
公开(公告)日:2006-03-02
申请号:US11185671
申请日:2005-07-19
Applicant: Murray Bailey , Punit Bhardwaj , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-Andre Poupart , Jean Rancourt
Inventor: Murray Bailey , Punit Bhardwaj , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet , Marc-Andre Poupart , Jean Rancourt
IPC: A61K38/04 , C07K5/04 , C07D403/02
CPC classification number: C07D413/04 , A61K38/00 , C07K5/06139 , C07K5/06191
Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
Abstract translation: 式(I)的化合物:其中R 1,R 2,R 3,R 4,n和 m如本文所定义。 该化合物可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US20050080005A1
公开(公告)日:2005-04-14
申请号:US10945518
申请日:2004-09-20
Applicant: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
Inventor: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
CPC classification number: C07K5/0827 , A61K38/00 , C07K5/0802 , C07K5/0812 , Y02A50/463
Abstract: Compounds of formula I: wherein D, R4, R3, L0, L1, L2, R2 and Rc are defined herein; or a pharmaceutically acceptable salt thereof, useful as inhibitors of the HCV NS3 protease.
Abstract translation: 式I化合物:其中D,R 4,R 3,L 0,L 1,L 2,R 2和R c在本文中定义; 或其药学上可接受的盐,其可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US06268365B1
公开(公告)日:2001-07-31
申请号:US09438629
申请日:1999-11-12
Applicant: Rajashekhar Betageri , Pierre L. Beaulieu , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , Usha Patel , John R. Proudfoot , Mario Cardozo
Inventor: Rajashekhar Betageri , Pierre L. Beaulieu , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , Usha Patel , John R. Proudfoot , Mario Cardozo
IPC: A61K31501
CPC classification number: C07D213/75 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12
Abstract: This invention relates to compounds of formula (1): wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
Abstract translation: 本发明涉及式(1)的化合物:其中环a,A,B,C,D,E,R和Q在本文中定义。 这些化合物具有破坏具有一个或多个SH2结构域及其天然配体的调节蛋白之间相互作用的能力。
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公开(公告)号:US6156784A
公开(公告)日:2000-12-05
申请号:US455633
申请日:1999-12-07
Applicant: Rajashekhar Betageri , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , John R. Proudfoot
Inventor: Rajashekhar Betageri , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , John R. Proudfoot
IPC: A61K31/198 , A61K31/27 , C07D213/75 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/40 , A61K31/215 , A61K31/185 , C07C229/04
CPC classification number: C07D213/75 , A61K31/198 , A61K31/27 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12
Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I). ##STR1##
Abstract translation: 公开了含有下式(I)化合物的组合物,其中A,B,C,G,Q和R在本文中定义。 这些化合物可用作磷酸酪氨酸模拟物,当掺入合适的分子结构时,抑制酪氨酸激酶依赖性调节蛋白与其天然含磷酸酪氨酸的配体或受体的结合。 还公开了制备式(I)化合物的方法。
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公开(公告)号:US6054470A
公开(公告)日:2000-04-25
申请号:US208113
申请日:1998-12-09
Applicant: Rajashekhar Betageri , Pierre L. Beaulieu , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , Usha Patel , John R. Proudfoot , Mario Cardozo
Inventor: Rajashekhar Betageri , Pierre L. Beaulieu , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , Usha Patel , John R. Proudfoot , Mario Cardozo
IPC: C07D237/22 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61K31/50 , A61P1/04 , A61P3/10 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D213/75 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D211/70 , C07D211/72 , C07D211/82 , C07D211/84
CPC classification number: C07D213/75 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12
Abstract: This invention relates to compounds of formula (1): ##STR1## wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
Abstract translation: 本发明涉及式(1)的化合物:其中环a,A,B,C,D,E,R和Q在本文中定义。 这些化合物具有破坏具有一个或多个SH2结构域及其天然配体的调节蛋白之间相互作用的能力。
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