公开(公告)号：EP1062950A2

公开(公告)日：2000-12-27

申请号：EP00118103.1

申请日：1991-05-02

申请人： BIOCHEM PHARMA INC

发明人： Coates, Jonathan Alan Victor ,  Mutton, Ian Martin ,  Williamson, Christopher ,  Penn, Charles Richard ,  Storer, Richard

IPC分类号： A61K31/513 ,  A61P31/18

CPC分类号： A61K31/7068 ,  A61K31/505 ,  A61K31/506 ,  A61K31/70 ,  A61K45/06 ,  C07D411/04 ,  A61K2300/00

摘要： (-)-4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one, its pharmaceutically acceptable derivatives, pharmaceutical formulations thereof, methods for its preparation and its use as an antiviral agent are described.

摘要翻译： （ - ） - 4-氨基-1-（2-羟甲基-1,3-氧硫杂环戊烷-5-基） - （1H） - 嘧啶-2-酮，其药学上可接受的衍生物，其药物制剂，其制备方法和 描述其作为抗病毒剂的用途。

公开(公告)号：EP0984967A1

公开(公告)日：2000-03-15

申请号：EP97906955.6

申请日：1997-03-14

申请人： BIOCHEM PHARMA INC.

发明人： JIN, Haolun ,  CHAN, Laval, Chun-Kong ,  WANG, Wei ,  STEFANAC, Tomislav ,  MANSOUR, Tarek, S. ,  NGUYEN-BA, Paul ,  LAVALLEE, Jean-François ,  FALARDEAU, Guy

IPC分类号： C07D471/06 ,  A61K31/495

CPC分类号： C07D471/04 ,  C07D215/48

摘要： The present invention relates to heterocyclic compounds, more particularly naphthyridine compounds having antiviral activity. In particular, compounds of formula (I) wherein B, W, X, Y, R1, R2, R3, R4, and n are as defined herein, are useful in the therapy and prophylaxis of cytomegalovirus (CMV) infection in mammals.

公开(公告)号：EP0485458B1

公开(公告)日：1997-10-22

申请号：EP90911857.2

申请日：1990-08-03

申请人： BIOCHEM PHARMA INC.

发明人： BRILLON, Denis ,  SAUVE, Gilles ,  ZACHARIE, Boulos ,  BELLEAU, Bernard

IPC分类号： C07D235/26 ,  C07C327/40 ,  C07C233/43 ,  C07K5/08 ,  C07K5/10 ,  C07K5/06

CPC分类号： C07D403/12 ,  A61K38/00 ,  C07D235/26 ,  C07K5/02 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/1013 ,  C07K14/66

摘要： Thioacylating reagents are provided for the introduction of thioamide bonds into growing peptides represented by structure (I), where the substituents are disclosed herein. Intermediate precursors for preparing these thioacylating reagents are also provided. A process for preparing the thioacylating reagents and the intermediate precursors is further provided. Thiopeptides, and salts thereof, that exhibit pharmacological utility are provided and are represented by formula (II), wherein R?1, R3, R4¿, X and n are as defined herein. Methods for preparing these thiopeptides from solution and solid phase syntheses, utilizing the thioacylating reagents disclosed herein, are also provided.

公开(公告)号：EP0711771A3

公开(公告)日：1996-07-10

申请号：EP95120531.9

申请日：1990-02-08

申请人： BIOCHEM PHARMA INC.

发明人： Belleau, Bernard ,  Nguyen-Ba, Nghe ,  Belleau, Pierette

IPC分类号： C07D473/00 ,  C07D411/04

CPC分类号： C07D411/14 ,  C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07D473/00 ,  C07D473/40

摘要： Disclosed are compounds of the formula

wherein R₁ is hydrogen;
   R₂ is a purine or pyrimidine base or an analogue or derivative thereof;
   Z is S, S=O or SO₂; and
   pharmaceutically acceptable derivatives thereof. Also described are use of the compounds as antiviral agents, pharmaceutical formulations, and methods for the preparation of the compounds.

公开(公告)号：EP0565549B1

公开(公告)日：1995-04-05

申请号：EP92901354.8

申请日：1992-01-03

申请人： BIOCHEM PHARMA INC.

发明人： NGUYEN-BA, Nghe ,  BELLEAU, Bernard

IPC分类号： A61K31/505

CPC分类号： A61K31/70 ,  A61K31/505

摘要： Use of a compound of formula (I) or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of hepatitis B is disclosed.

公开(公告)号：EP0635026A1

公开(公告)日：1995-01-25

申请号：EP93907719.0

申请日：1993-04-02

申请人： BIOCHEM PHARMA INC.

发明人： PENNEY, Christopher ,  ZACHARIE, Boulos

IPC分类号： A61K38 ,  A61K31 ,  A61P31 ,  C07C327 ,  C07K1 ,  C07K5

CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07C327/42 ,  C07K5/0215 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06104

摘要： New, small and structurally simple immunomodulating oligopeptides are disclosed. The oligopeptides of this invention possess a long, lipophilic alkyl chain. These immunododulating oligopeptides can be used in conjunction with anti-viral or anti-cancer agents in the treatment of human and animal diseases. Processes for the syntheses of immunomodulating chemicals are also disclosed.

公开(公告)号：EP0382526A2

公开(公告)日：1990-08-16

申请号：EP90301335.7

申请日：1990-02-08

申请人： BIOCHEM PHARMA INC.

发明人： Belleau, Bernard (deceased) ,  Belleau, Pierette ,  Nguyen-Ba, Nghe

IPC分类号： C07D473/00 ,  C07D411/04 ,  C07D411/14 ,  C07D327/04 ,  A61K31/52 ,  A61K31/505

CPC分类号： C07D411/14 ,  C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07D473/00 ,  C07D473/40

摘要： Disclosed are compounds of the formula
wherein R₁ is hydrogen;
R₂ is a purine or pyrimidine base or an analogue or derivative thereof;
Z is S, S=O or SO₂; and
pharmaceutically acceptable derivatives thereof.
Also described are use of the compounds as antiviral agents, pharmaceutical formulations, and methods for the preparation of the compounds.

摘要翻译： 公开了式CHEM的化合物，其中R 1是氢; R2是嘌呤或嘧啶碱基或其类似物或衍生物; Z是S，S = O或SO 2; 及其药学上可接受的衍生物。 还描述了化合物作为抗病毒剂，药物制剂和制备化合物的方法的用途。

公开(公告)号：EP1115724A1

公开(公告)日：2001-07-18

申请号：EP99969413.6

申请日：1999-09-21

申请人： BIOCHEM PHARMA INC

发明人： LAMOTHE, Serge ,  ZACHARIE, Boulos ,  ATTARDO, Giorgio ,  LABRECQUE, Denis ,  COURCHESNE, Marc ,  FALARDEAU, Guy ,  REJ, Rabindra ,  ABBOTT, Shaun

IPC分类号： C07D455/02 ,  A61K31/435

CPC分类号： C07D455/02

摘要： The present invention comprises novel compounds that are effective inhibitors of integrins, particularly αIIbβ3 or αv integrins such as αvβ3 and αvβ5. The present invention, according to one embodiment, comprises a compound of formula (I) or formula (II), or a pharmaceutically acceptable salt, solvate, or metabolic precursor thereof. Wherein R1, R2, R3 and R4 are as defined herein.

摘要翻译： 本发明包含作为整联蛋白的有效抑制剂的新型化合物，特别是αIIbβ3或αv整联蛋白如αvβ3和αvβ5。 根据一个实施方案，本发明包含式（I）或式（II）的化合物或其药学上可接受的盐，溶剂合物或代谢前体。 其中R1，R2，R3和R4如本文所定义。

公开(公告)号：EP0970074A1

公开(公告)日：2000-01-12

申请号：EP96941539.7

申请日：1996-12-13

申请人： BIOCHEM PHARMA INC.

发明人： MANSOUR, Tarek ,  CIMPOIA, Alex ,  BEDNARSKI, Krzysztof

IPC分类号： C07D411/04 ,  C07H19/06

CPC分类号： C07D405/04 ,  Y02P20/55

摘要： The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10 °C, wherein R1 and L are as defined herein.

公开(公告)号：EP0654031B1

公开(公告)日：1999-12-29

申请号：EP94918252.1

申请日：1994-06-07

申请人： BIOCHEM PHARMA INC.

发明人： MANSOUR, Tarek, S. ,  EVANS, Colleen, A. ,  JIN, Haolun ,  SIDDIQUI, Arshad, M. ,  TSE, Allan, H., L.

IPC分类号： C07D411/04 ,  C07D473/00 ,  C07D497/08

CPC分类号： C07D473/00 ,  C07D411/04 ,  C07D497/08

摘要： The present invention relates to a process for producing predominantly pure cis nucleoside analogues using a novel bicyclic intermediate of formula (III), wherein X is S, or O; Y is S, CH2, O or CH(R); wherein R is azido or halogen; and Z is S or O.