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1. 发明申请

WO1996001833A1 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：WO1996001833A1
公开(公告)日：1996-01-25
申请号：PCT/GB1995001597
申请日：1995-07-06
申请人： THE WELLCOME FOUNDATION LIMITED , CHAMBERLAIN, Stanley, Dawes , KOSZALKA, George, Walter
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07H19/052
CPC分类号： C07D235/30 , C07H19/052
摘要： The present invention relates to benzimidazole 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：本发明涉及苯并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诸如由疱疹病毒引起的病毒感染的病毒感染。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。

2. 发明申请

WO1992001456A1 HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO1992001456A1
公开(公告)日：1992-02-06
申请号：PCT/GB1991001196
申请日：1991-07-18
申请人： THE WELLCOME FOUNDATION LIMITED , KRENITSKY, Thomas, Anthony , AVERETT, Devron, Randolph , WILSON, Jeffrey, Douglas , MOORMAN, Allan, Ray , KOSZALKA, George, Walter , CHAMBERLAIN, Stanley, Dawes , PORTER, David , WOLBERG, Gerald
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/70
CPC分类号： C07H19/16 , Y10S514/814 , Y10S514/883 , Y10S514/908
摘要： 6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumour therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.
摘要翻译： Ara-G的6-烷氧基衍生物及其药学上可接受的酯被描述为可用于肿瘤治疗。还公开了新的药学上可接受的酯，其制备方法和含有它们的药物制剂。

3. 发明申请

WO1993006112A1 THERAPEUTIC NUCLEOSIDES 审中-公开
标题翻译：治疗性核素
公开(公告)号：WO1993006112A1
公开(公告)日：1993-04-01
申请号：PCT/GB1992001748
申请日：1992-09-23
申请人： THE WELLCOME FOUNDATION LIMITED , MILLER, Wayne, Howard , CHAMBERLAIN, Stanley, Dawes , BIRON, Karen, Kathleen
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07F09/6561
CPC分类号： C07D473/00 , C07C69/78 , C07F7/1804 , C07F9/65616 , C07H9/04
摘要： The present invention relates to an antiviral phosphonate derivate of an acyclic purine nucleoside analog, to pharmaceutically acceptable derivatives thereof and to their use in medical therapy, particularly in the treatment of cytomegalovirus infections. Methods for preparing the R-enantiomer of the compound of the invention, substantially free from the corresponding S-enantiomer are disclosed.
摘要翻译：本发明涉及无环嘌呤核苷类似物的抗病毒膦酸酯衍生物及其药学上可接受的衍生物，以及它们在医学治疗中的用途，特别是用于治疗巨细胞病毒感染。公开了制备基本上不含相应S-对映体的本发明化合物的R-对映异构体的方法。

4. 发明申请

WO1994001117A1 THERAPEUTIC NUCLEOSIDES 审中-公开
标题翻译：治疗性核素
公开(公告)号：WO1994001117A1
公开(公告)日：1994-01-20
申请号：PCT/GB1993001387
申请日：1993-07-01
申请人： THE WELLCOME FOUNDATION LIMITED , KOSZALKA, George, Walter , VAN DRAANEN, Nanine, Agneta , FREEMAN, George, Andrew , SHORT, Steven, Andersen , SLATER, Martin, John
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/70
CPC分类号： A61K31/70
摘要： The present invention relates to the use of 2'-deoxy-4'-thioribonucleosides and physiologically acceptable salts, esters or salts of such esters thereof, for the manufacture of a medicament for the treatment or prophylaxis of retrovirus, cytomegalovirus, varicella zoster virus, Epstein-Barr virus, human herpes virus 6, hepatitis viral infections, including hepatitis B, coxsackie virus and hepatitis C virus infections.
摘要翻译：本发明涉及2'-脱氧-4'-硫虫核苷及其这些酯的生理学上可接受的盐，酯或盐在制备用于治疗或预防逆转录病毒，巨细胞病毒，水痘带状疱疹病毒，爱泼斯坦 - 巴尔病毒，人类疱疹病毒6，肝炎病毒感染，包括乙型肝炎，柯萨奇病毒和丙型肝炎病毒感染。

5. 发明申请

WO1993014103A1 THERAPEUTIC NUCLEOSIDES 审中-公开
标题翻译：治疗性核素
公开(公告)号：WO1993014103A1
公开(公告)日：1993-07-22
申请号：PCT/GB1993000004
申请日：1993-01-05
申请人： THE WELLCOME FOUNDATION LIMITED , BURNS, Charlene, Louise , KOSZALKA, George, Walter , KRENITSKY, Thomas, Anthony
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07H19/173
CPC分类号： C07H19/16
摘要： The present invention relates to certain novel 2',3'-dideoxy-3'-fluoro-purine nucleoside compounds, salts, esters and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment of prophylaxis of viral infections.
摘要翻译：本发明涉及某些新的2'，3'-二脱氧-3'-氟 - 嘌呤核苷化合物，其盐，酯和生理功能衍生物，其制备方法，含有它们的药物制剂以及这些化合物在治疗，特别是预防病毒感染的治疗。

6. 发明申请

WO1994001443A1 THERAPEUTIC NUCLEOSIDES 审中-公开
标题翻译：治疗性核素
公开(公告)号：WO1994001443A1
公开(公告)日：1994-01-20
申请号：PCT/GB1993001388
申请日：1993-07-01
申请人： THE WELLCOME FOUNDATION LIMITED , KOSZALKA, George, Walter , VAN DRAANEN, Nanine, Agneta , FREEMAN, George, Andrew , SHORT, Steven, Andersen
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07H05/10
CPC分类号： C07H19/16
摘要： The present invention relates to certain novel 2'-deoxy-4'-thio-purine nucleosides, physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to their use in therapy, particularly in the treatment or prophylaxis of viral infections.
摘要翻译：本发明涉及某些新的2'-脱氧-4'-硫嘌呤核苷，其生理功能衍生物，其制备方法，含有它们的药物制剂及其在治疗中的用途，特别是用于治疗或预防病毒感染。

7. 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。

8. 发明申请

WO1997000681A1 PHARMACEUTICAL COMPOSITION CONTAINING LAMOTRIGINE 审中-公开
标题翻译：含有LAMOTRIGINE的药物组合物
公开(公告)号：WO1997000681A1
公开(公告)日：1997-01-09
申请号：PCT/EP1996002759
申请日：1996-06-20
申请人： THE WELLCOME FOUNDATION LIMITED , FLOYD, Alison, Green , JAIN, Sunil
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/53
CPC分类号： A61K31/53 , A61K9/19
摘要： A lyophilized formulation of lamotrigine having been prepared by lyophilizing a frozen sterile aqueous solution of lamotrigine mesylate in which the pH is from 2.5 to 4.
摘要翻译：通过冻干甲磺酸拉莫三嗪的冷冻无菌水溶液制备拉唑三嗪的冻干制剂，其中pH为2.5至4。

9. 发明申请

WO1996019440A1 ACETAMIDINE DERIVATIVES AND THEIR USE AS INHIBITORS FOR THE NITRIC OXIDE SYNTHASE 审中-公开
标题翻译：乙酰胺衍生物及其作为氮氧化物合成酶的抑制剂
公开(公告)号：WO1996019440A1
公开(公告)日：1996-06-27
申请号：PCT/GB1995002978
申请日：1995-12-20
申请人： THE WELLCOME FOUNDATION LIMITED , OPLINGER, Jeffrey, Alan , GARVEY, Edward, Patrick , FURFINE, Eric, Steven , SHEARER, Barry, George , COLLINS, Jon, Loren
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07C257/14
CPC分类号： C07D249/08 , A61K31/155 , A61K31/416 , C07C257/14 , C07C257/18 , C07C311/46 , C07C323/41 , C07C323/60 , C07C335/36 , C07C2602/08 , C07D213/74 , C07D217/04 , C07D217/22 , C07D231/12 , C07D231/56 , C07D233/56 , C07D277/40 , C07D333/20
摘要： A class of acetamidine derivatives of general formula (I), methods for the manufacture thereof in therapy, particularly as inhibitors of nitric oxide synthase, is disclosed or a salt thereof, wherein R is hydrogen, a C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR wherein R is hydrogen or C1-6 alkyl; and R is hydrogen, C1-6 alkyl, or a group NR R wherein R and R are independently hydrogen or C1-6 alkyl, provided that R is not NR R when X is oxygen or S(O)n; R and R are independently selected from hydrogen or halo; R is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR wherein Z is oxygen, C(O)m', wherein m' is 1 or 2, S(O)n', wherein n' is 0, 1 or 2, or a group NR wherein R is hydrogen or C1-6 alkyl and R is hydrogen, C1-6 alkyl or a group NR R wherein R and R are independently hydrogen or C1-6 alkyl; or R is substituted by a group (a), wherein R has a definition the same as for R ; with the proviso that when R is a C1-6 alkyl group and R is a C1-14 hydrocarbyl substituted by two groups ZR wherein one group ZR is CO2H, the other group ZR is not NH2.
摘要翻译：公开了一类通式（I）的乙脒衍生物，其在治疗中的制备方法，特别是作为一氧化氮合酶抑制剂的方法，或其盐，其中R 1为氢，任选地为C 1-6烃基被卤素，卤素，硝基，氰基或XR 3基团取代，其中X是氧，C（O）m，其中m是1或2，S（O）n，其中n是0,1或2， NR 4其中R 4是氢或C 1-6烷基; 并且R 3是氢，C 1-6烷基或NR 5 R 6基团，其中R 5和R 6独立地是氢或C 1-6烷基，条件是R 3是当X为氧或S（O）n时，不为NR 5 R 6; R 1a和R 1b独立地选自氢或卤素; R 2是可任选地含有一个或两个杂原子的C 1-14烃基，R 2任选被一个或多个独立地选自卤素的基团取代; N3; 硝基; CF3; ZR 7其中Z是氧，C（O）m'，其中m'是1或2，S（O）n'，其中n'是0,1或2，或NR 8的基团其中R 8是氢或C 1-6烷基，R 7是氢，C 1-6烷基或NR 9 R 10基团，其中R 9和R 10独立地是氢或C 1-6 烷基; 或R 2由基团（a）取代，其中R 11具有与R 1相同的定义; 条件是当R 1为C 1-6烷基且R 2为被两个ZR 7基团取代的C 1-14烃基时，其中一个基团ZR 7为CO 2 H，另一组ZR < 7>不是NH2。

10. 发明申请

WO1996016990A1 HUMANIZED ANTIBODIES TO CD38 审中-公开
标题翻译：人类抗体CD38
公开(公告)号：WO1996016990A1
公开(公告)日：1996-06-06
申请号：PCT/GB1995002777
申请日：1995-11-28
申请人： THE WELLCOME FOUNDATION LIMITED , ELLIS, Jonathan, Henry , LEWIS, Alan, Peter
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07K16/46
CPC分类号： C07K16/2896 , A61K38/00 , C07K16/465 , C07K2317/24 , C07K2319/00
摘要： The present invention relates to a monoclonal antibody, preferably with specificity for CD38, having CDRs of foreign origin and a recipient framework region having a sequence of human or primate origin, wherein the original amino acid residues in position 29 and/or 78 of the sequence of the recipient framework region of the heavy chain is replaced by a replacement amino acid residue that is the same or similar to that in the corresponding position of the sequence of the corresponding framework region of the heavy chain of the antibody from which the CDRs are derived. Method of preparation of said antibody. Pharmaceutical composition containing said antibody. Use of said antibody for the treatment of cancer and autoimmune diseases.
摘要翻译：本发明涉及优选具有CD38特异性的单克隆抗体，其具有国外起源的CDR和具有人或灵长类来源序列的受体框架区，其中序列的位置29和/或78的原始氨基酸残基重链的接收者框架区的替换氨基酸残基被替换为相同或相似于CDR衍生自抗体重链的相应构架区的序列相应位置的氨基酸残基。所述抗体的制备方法。含有所述抗体的药物组合物。使用所述抗体治疗癌症和自身免疫性疾病。

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