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1. 发明申请

WO1995021161A1 CHLOROPYRIMIDE INTERMEDIATES 审中-公开
标题翻译：氯仿中间体
公开(公告)号：WO1995021161A1
公开(公告)日：1995-08-10
申请号：PCT/GB1995000225
申请日：1995-02-03
申请人： THE WELLCOME FOUNDATION LIMITED , DALUGE, Susan, Mary , MARTIN, Michael, Tolar , FUGETT, Michelle, Joanne, Ferry
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D239/48
CPC分类号： C07D239/48 , C07D239/50 , C07D473/40
摘要： The present invention relates to certain novel pyrimidine intermediates and their salts, processes for their preparation and processes for their conversion to 9-substituted-2-aminopurines which are useful in medical therapy.
摘要翻译：本发明涉及某些新颖的嘧啶中间体及其盐，其制备方法及其转化为可用于医学治疗的9-取代-2-氨基嘌呤的方法。

2. 发明申请

WO9856761A2 BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO9856761A2
公开(公告)日：1998-12-17
申请号：PCT/EP9803380
申请日：1998-06-08
申请人： GLAXO GROUP LTD , UNIV MICHIGAN , DRACH JOHN CHARLES , TOWNSEND LEROY B , BOYD FRANK LESLIE JR , CHAMBERLAIN STANLEY DAWES , DALUGE SUSAN MARY , DEATON DAVID NORMAN , ANDERSEN MARC W , FREEMAN GEORGE ANDREW
发明人： DRACH JOHN CHARLES , TOWNSEND LEROY B , BOYD FRANK LESLIE JR , CHAMBERLAIN STANLEY DAWES , DALUGE SUSAN MARY , DEATON DAVID NORMAN , ANDERSEN MARC W , FREEMAN GEORGE ANDREW
IPC分类号： C07D235/06 , A61K31/4184 , A61K31/7056 , A61P31/12 , A61P31/22 , C07C20060101 , C07D235/18 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D405/04 , C07H20060101 , C07H19/052 , C07D
CPC分类号： C07D235/24 , C07D235/30 , C07D405/04 , C07H19/052
摘要： The present invention relates to certain bezimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
摘要翻译：本发明涉及某些苯扎咪唑衍生物及其在药物治疗中的用途，特别是用于治疗或预防由疱疹病毒引起的病毒感染。本发明还涉及苯并咪唑衍生物的制备和含有它们的药物制剂。

3. 发明申请

WO1996006844A1 4-(2-AMINO-6-(CYCLOPROPYLAMINO)-9H-PURIN-9-YL)-2-CYCLOPENTENE-1-METHANOL SUCCINATE AS ANTIVIRAL AGENT 审中-公开
标题翻译： 4-（2-氨基-6-（环丙基氨基）-9H-嘌呤-9-基）-2-环戊烯-1-甲醇磺酸酯作为抗病毒剂
公开(公告)号：WO1996006844A1
公开(公告)日：1996-03-07
申请号：PCT/GB1995002014
申请日：1995-08-25
申请人： THE WELLCOME FOUNDATION LIMITED , DALUGE, Susan, Mary , WILSON, Jeffrey, Douglas
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D473/00
CPC分类号： C07D473/00 , A61K31/52
摘要： The present invention relates to the succinate salt of (1S,4R)- cis -[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol or a solvate thereof, to pharmaceutical formulations containing such a compound or pharmaceutical formulations, and to its use in medical therapy or in methods of treatment or prophylaxis of a viral infection, specifically human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infection.
摘要翻译：本发明涉及（1S，4R） - 顺式 - [2-氨基-6-（环丙基氨基）-9H-嘌呤-9-基] -2-环戊烯-1-酮的琥珀酸盐，甲醇或其溶剂合物，含有这种化合物或药物制剂的药物制剂，以及其在药物治疗或治疗或预防病毒感染的方法中的用途，特别是人类免疫缺陷病毒（HIV）和乙型肝炎病毒（HBV）感染。

4. 发明申请

WO1996004280A1 PHENYL XANTHINE DERIVATIVES 审中-公开
标题翻译：苯胺衍生物
公开(公告)号：WO1996004280A1
公开(公告)日：1996-02-15
申请号：PCT/GB1995001808
申请日：1995-07-31
申请人： THE WELLCOME FOUNDATION LIMITED , DALUGE, Susan, Mary , WHITE, Helen, Lyng
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D473/06
CPC分类号： C07D473/06
摘要： The present invention relates to novel compounds of formula (I), processes for their preparation, pharmaceutical formulations containing them, and their use in medicine, particularly in the prophylaxis and treatment of septic shock, allergic, and inflammatory conditions, as well as neurodegeneration.
摘要翻译：本发明涉及新的式（I）化合物，其制备方法，含有它们的药物制剂及其在医药中的用途，特别是涉及脓毒性休克，过敏性和炎症性疾病以及神经变性的预防和治疗。

5. 发明申请

WO1997025316A1 2-AMINO-5,6-DICHLOROBENZIMIDAZOLE DERIVATIVES HAVING ANTIVIRAL ACTIVITY 审中-公开
标题翻译：具有抗病毒活性的2-氨基-5,6-二氯苯并咪唑衍生物
公开(公告)号：WO1997025316A1
公开(公告)日：1997-07-17
申请号：PCT/EP1997000018
申请日：1997-01-03
申请人： GLAXO GROUP LIMITED , DALUGE, Susan, Mary , ANDERSON, Marc, W.
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D235/30
CPC分类号： C07D235/24 , C07D235/30 , C07D403/04
摘要： The present invention relates to benzimidazole derivatives of formula (I) wherein: R represents H, C1-4 alkyl, C3-5 cycloalkyl; R represents H, C1-4 alkyl; or R and R together form with the nitrogen a 4 or 5 membered heterocyclic ring; R represents BR or R wherein B represents a bridging group -C(O)NH-, -C(O)NC1-4alkyl-, or -C(O)O- and R represents H, C1-4alkyl, C2-6alkenyl or halo (preferably fluoro); and each n is an integer independently selected from 0, 1, or 2 (preferably 0 or 1); and geometric isomers or mixtures thereof; and physiologically functional derivatives thereof, and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to their preparation and pharmaceutical formulations containing them.
摘要翻译：本发明涉及式（I）的苯并咪唑衍生物，其中：R 1表示H，C 1-4烷基，C 3-5炔基; R 2表示H，C 1-4烷基; 或R 1和R 2一起与氮一起形成4或5元杂环; R 3表示BR 4或R 4，其中B表示桥基-C（O）NH-，-C（O）NC1-4烷基 - 或-C（O）O-和R 4 >表示H，C 1-4烷基，C 2-6烯基或卤素（优选氟）; 并且每个n是独立地选自0,1或2（优选0或1）的整数; 和几何异构体或其混合物; 及其生理功能衍生物，以及它们在医学治疗中的用途，特别是用于治疗或预防由疱疹病毒引起的病毒感染。本发明还涉及它们的制备和含有它们的药物制剂。

6. 发明申请

WO1996007646A1 ANTIVIRAL NUCLEOSIDE ANALOGUES CONTAINING A SUBSTITUTED BENZIMIDAZOLE BASE ATTACHED TO A CARBOCYCLIC RING 审中-公开
标题翻译：含有取代的苯并咪唑基的偶氮核苷类似物与碳环结合
公开(公告)号：WO1996007646A1
公开(公告)日：1996-03-14
申请号：PCT/US1995011366
申请日：1995-09-11
申请人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DALUGE, Susan, Mary
发明人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07D235/20
CPC分类号： C07D403/04 , C07D235/30
摘要： Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue. In formulae (I) and (I-1), R is H, CH3 or CH2OH; R is H or OH; R is H or OH; or R and R together form a bond; R is amino, cyclopropylamino, cyclobutylamino, isopropylamino, tert-butylamino or -NR R where R and R together with the nitrogen atom to which they are attached form a 4, 5 or 6-membered heterocyclic ring; R is H and R and R are Cl, excluding the compound (+/-)-(1R*, 2S*, 3S*, 5S*)-5-[5,6-Dichloro-2-(cyclopropylamino)-1 H -benzimidazol-1-yl]-3-(hydroxymethyl)-1,2-cyclopentanediol and provided that at least one of R , R and R is or contains OH. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.
摘要翻译：抗病毒核苷类似物包含与碳环连接的取代的苯并咪唑碱代替常规的糖残基。在式（I）和（I-1）中，R 1是H，CH 3或CH 2 OH; R 2是H或OH; R 3是H或OH; 或R 2和R 3一起形成键; R 4是氨基，环丙基氨基，环丁基氨基，异丙基氨基，叔丁基氨基或-NR 8 R 9，其中R 8和R 9与它们所连接的氮原子一起形成4， 5或6元杂环; 不包括化合物（+/-） - （1R *，2S *，3S *，5S *） - 5- [5,6-二氯苯基]，R 5为H且R 6和R 7为Cl -2-（环丙基氨基）-1H-苯并咪唑-1-基] -3-（羟基甲基）-1,2-环戊二醇，条件是R 1，R 2， >和R 3是或含有OH。该化合物具有抗疱疹病毒特异性巨细胞病毒和乙型肝炎病毒感染的活性。

7. 发明申请

WO1993018009A1 ANTIVIRAL NUCLEOSIDE ANALOGUES 审中-公开
标题翻译：抗病毒核苷酸类似物
公开(公告)号：WO1993018009A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000479
申请日：1993-03-08
申请人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, Charles , GOOD, Steven, Spencer , DALUGE, Susan, Mary , MARTIN, Michael, Tolar
发明人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07D235/06
CPC分类号： C07D235/06 , C07D235/08 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30
摘要： Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in a place of the conventional sugar residue. Particularly preferred compounds include those in which the 2-,5- and 6- positions of the benzimidazole base are substituted by halogen. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.
摘要翻译：抗病毒核苷类似物在常规糖残基的位置含有连接到碳环上的取代的苯并咪唑碱。特别优选的化合物包括其中苯并咪唑碱的2-，5-和6-位被卤素取代的化合物。该化合物具有抗疱疹病毒特异性巨细胞病毒和乙型肝炎病毒感染的活性。

8. 发明申请

WO1993017020A2 THERAPEUTIC NUCLEOSIDES 审中-公开
标题翻译：治疗性核素
公开(公告)号：WO1993017020A2
公开(公告)日：1993-09-02
申请号：PCT/GB1993000378
申请日：1993-02-24
申请人： THE WELLCOME FOUNDATION LIMITED , DALUGE, Susan, Mary , LIVINGSTON, Douglas, Alan
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D473/00
CPC分类号： C07D473/00 , A61K31/52 , C07C213/00 , C07C229/48 , C07C2601/10
摘要： The present invention relates to certain purine nucleoside analogues containing a carbocyclic ring in place of the sugar residue, salts, esters and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment or prophylaxis of certain viral infections.
摘要翻译：本发明涉及含有碳环的某些嘌呤核苷类似物代替糖残基，其盐，酯和药学上可接受的衍生物，其制备方法，含有它们的药物制剂以及这些化合物在治疗中的用途，特别是治疗或预防某些病毒感染。

9. 发明申请

WO1993013778A1 THERAPEUTIC NUCLEOSIDES 审中-公开
标题翻译：治疗性核素
公开(公告)号：WO1993013778A1
公开(公告)日：1993-07-22
申请号：PCT/GB1993000005
申请日：1993-01-05
申请人： THE WELLCOME FOUNDATION LIMITED , BURNS, Charlene, Louise , KOSZALKA, George, Walter , KRENITSKY, Thomas, Anthony , DALUGE, Susan, Mary
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/70
CPC分类号： C07H19/16
摘要： Compounds of formula (I), wherein R represents an n-propoxy, cyclobutoxy, cyclopropylamino, piperidino or pyrrolidino group; or a physiologically functional derivative thereof. The invention further includes methods for the preparation of compounds of formula (I), compositions containing them and the use of these compounds as antiviral agents.
摘要翻译：式（I）化合物，其中R 1表示正丙氧基，环丁氧基，环丙基氨基，哌啶子基或吡咯烷子基; 或其生理功能衍生物。本发明还包括制备式（I）化合物，含有它们的组合物和这些化合物作为抗病毒剂的用途的方法。

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