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1. 发明申请

WO1993011756A1 MEDICAMENT FOR TREATMENT OF PROTOZOAL INFECTIONS 审中-公开
标题翻译：用于治疗原发性感染的药物
公开(公告)号：WO1993011756A1
公开(公告)日：1993-06-24
申请号：PCT/GB1992002344
申请日：1992-12-17
申请人： THE WELLCOME FOUNDATION LIMITED , GUTTERIDGE, Winston, Edward , HUDSON, Alan, Thomas , LATTER, Victoria, Susan , PUDNEY, Mary
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/12
CPC分类号： A61K31/12 , Y02A50/409 , Y02A50/492
摘要： The present invention relates to pharmaceutical compositions for the treatment and/or prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Microsporidia comprising 2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other functional derivative thereof as active ingredient and to a method of treating or preventing said protozoal infections in an animal which comprises administering to said animal an effective amount of said compound.
摘要翻译：本发明涉及用于治疗和/或预防由包括2- [4-（4-氯苯基）环己基] -3-羟基-1,4-萘醌在内的活细胞，起绒复合物，厌氧原生动物和微孢子虫引起的原生动物感染的药物组合物或其生理上可接受的盐或其它功能性衍生物作为活性成分，以及治疗或预防动物中所述原生动物感染的方法，其包括向所述动物施用有效量的所述化合物。

2. 发明申请

WO1991005550A1 MEDICAMENT FOR THE TREATMENT OF CRYPTOSPORIDIOSIS 审中-公开
标题翻译：治疗结缔组织病的药物
公开(公告)号：WO1991005550A1
公开(公告)日：1991-05-02
申请号：PCT/GB1989001287
申请日：1989-10-26
申请人： THE WELLCOME FOUNDATION LIMITED , LATTER, Victoria, Susan
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/12
CPC分类号： A61K31/12 , Y02A50/488
摘要： The present invention relates to the use of 2-[4-(4-chlorophenyl) cyclohexyl]-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other physiologically functional derivative thereof for the manufacture of a medicament for the treatment and/or prophylaxis of cryptosporidiosis in animals, to pharmaceutical compositions for the treatment and/or prophylaxis of cryptosporidiosis, comprising said compound as active ingredient and to a method of treating or preventing cryptosporidiosis in an animal which comprises administering to said animal an effective amount of said compound.
摘要翻译：本发明涉及2- [4-（4-氯苯基）环己基] -3-羟基-1,4-萘醌或其生理上可接受的盐或其他生理功能衍生物在制备用于治疗的药物中的用途和/或预防动物中的隐孢子虫病，用于治疗和/或预防隐孢子虫病的药物组合物，其包含所述化合物作为活性成分，以及治疗或预防动物隐孢子虫病的方法，其包括向所述动物施用有效量的说化合物。

3. 发明申请

WO1994012164A1 COMBINATION OF ATOVAQUONE WITH PROGUANIL FOR THE TREATMENT OF PROTOZOAL INFECTIONS 审中-公开
标题翻译： ATOVAQUONE与PROGUANIL的联合用于治疗原发性感染
公开(公告)号：WO1994012164A1
公开(公告)日：1994-06-09
申请号：PCT/GB1993002425
申请日：1993-11-25
申请人： THE WELLCOME FOUNDATION LIMITED , GUTTERIDGE, Winston, Edward , HUTCHINSON, David, Brian, Ashton , LATTER, Victoria, Susan , PUDNEY, Mary
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： A61K31/155
CPC分类号： A61K31/155 , Y02A50/411 , Y10S514/895 , A61K31/12 , A61K2300/00
摘要： The invention relates to combinations of atovaquone and proguanil, their use in the treatment and prophylaxis of parasitic infections, such as protozoal parasitic infections, e.g. malaria and toxoplasmosis, and infections caused by P.carinii and their use in the manufacture of medicaments for the treatment and/or prophylaxis of such infections. The combinations can conveniently be administered in a single pharmaceutical formulation. Preferably, atovaquone and proguanil are administered in a potentiating ratio so that they act in synergy.
摘要翻译：本发明涉及阿托伐醌和氯胍的组合，它们用于治疗和预防寄生虫感染，例如原生动物寄生虫感染，例如，疟疾和弓形虫病，以及由卡氏菌引起的感染及其在制备用于治疗和/或预防这种感染的药物中的用途。这些组合可以方便地以单一药物制剂施用。优选地，阿托伐醌和氯胍以增强比例施用，使得它们协同作用。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO1996009294A1 SUBSTITUTED HETEROAROMATIC COMPOUNDS AND THEIR USE IN MEDICINE 审中-公开
标题翻译：取代的异种化合物及其在医学中的应用
公开(公告)号：WO1996009294A1
公开(公告)日：1996-03-28
申请号：PCT/GB1995002202
申请日：1995-09-18
申请人： THE WELLCOME FOUNDATION LIMITED , HUDSON, Alan, Thomas , VILE, Sadie , BARRACLOUGH, Paul , FRANZMANN, Karl, Witold , MC KEOWN, Stephen, Carl , PAGE, Martin, John
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D239/94
CPC分类号： C07D405/12 , C07D215/44 , C07D239/88 , C07D239/94 , C07D239/95 , C07D409/12
摘要： The invention is directed towards substituted heteroaromatic compounds which are protein tyrosine kinase inhibitors, in particular substituted quinolines and quinazolines. Methods of their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.
摘要翻译：本发明涉及作为蛋白质酪氨酸激酶抑制剂，特别是取代的喹啉和喹唑啉的取代杂芳族化合物。其制备方法，包括这些化合物的药物组合物及其在医学中的应用，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，过敏，哮喘，移植排斥，炎症，血栓形成，神经系统疾病，和癌症。

8. 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。

9. 发明申请

WO1995034534A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：WO1995034534A1
公开(公告)日：1995-12-21
申请号：PCT/GB1995001378
申请日：1995-06-14
申请人： THE WELLCOME FOUNDATION LIMITED , HODSON, Harold, Francis , PALMER, Richard, Michael, John , SAWYER, David, Alan , KNOWLES, Richard, Graham , FRANZMANN, Karl, Witold , DRYSDALE, Martin, James , SMITH, Steven , DAVIES, Patricia, Ifeyinwa , CLARK, Helen, Alice, Rebecca , SHEARER, Barry, George
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07C317/48
CPC分类号： C07C323/60 , C07C317/48 , Y02P20/55
摘要： A compound of formula (I), wherein R is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkyl C1-6alkyl group, each optionally substituted by one to three groups independently selected from: -CN; -NO2; a group -COR wherein R is hydrogen, C1-6alkyl, -OR wherein R is hydrogen or C1-6alkyl, or NR R , wherein R and R are independently selected from hydrogen or C1-6alkyl; a group -S(O)mR , wherein m is 0, 1 or 2, R is hydrogen, C1-6 alkyl, hydroxy or NR R , wherein R and R are independently hydrogen or C1-6 alkyl; a group PO(OR )2, wherein R is hydrogen or C1-6 alkyl; a group NR R , wherein R and R are independently selected from hydrogen, C1-6 alkyl, -COR , wherein R is hydrogen or C1-6alkyl, or -S(O)m'R , wherein m' is 0, 1 or 2 and R is hydrogen or C1-6alkyl; halo; or a group -OR , wherein R is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or -COR wherein R is hydrogen or C1-6 alkyl; p is 2 or 3, q is 1 or 2 and n is 0 or 1 and all salts, esters, amides and physiologically acceptable prodrugs thereof; pharmaceutical uses and formulations therefor; and processes for their preparation are disclosed.
摘要翻译：式（I）化合物，其中R 1为C 1-6直链或支链烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或C 3-6环烷基C 1-6烷基各自任选被一至三个独立地选自：-CN的基团取代; NO 2; 基团-COR 2其中R 2是氢，C 1-6烷基，-OR 3，其中R 3是氢或C 1-6烷基或NR 4 R 5，其中R 4 >和R 5独立地选自氢或C 1-6烷基; 基团-S（O）m R 6，其中m为0,1或2，R 6为氢，C 1-6烷基，羟基或NR 7 R 8，其中R 7和 R 8独立地是氢或C 1-6烷基; 基团PO（OR 9）2，其中R 9是氢或C 1-6烷基; NR 10 R 11基团，其中R 10和R 11独立地选自氢，C 1-6烷基，-COR 12，其中R 12是氢或C 1-6烷基，或-S（O）m'R 13，其中m'为0,1或2，R 13为氢或C 1-6烷基; 光环; 或基团-OR 14，其中R 14是氢，任选被一至三个卤素原子取代的C 1-6烷基，C 6-10芳基或-COR 15，其中R 15是氢或C1- 6烷基; p为2或3，q为1或2，n为0或1，所有的盐，酯，酰胺和其生理上可接受的前药; 药用及其制剂; 并公开了其制备方法。

10. 发明申请

WO1995023134A1 THERAPEUTIC BENZONITRILES 审中-公开
标题翻译：治疗苯丙胺
公开(公告)号：WO1995023134A1
公开(公告)日：1995-08-31
申请号：PCT/GB1995000376
申请日：1995-02-23
申请人： THE WELLCOME FOUNDATION LIMITED , CHAN, Joseph, Howing
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07C323/37
CPC分类号： C07C317/48 , C07C323/63
摘要： Arylthiobenzonitrile compounds of formula (I) wherein, R is hydrogen, nitro, trifluoromethyl, halogen, carboxy, C1-4 carboxyamido, nitrile, C1-4 alkanoyl, C1-4 alkylsulfonyl, C1-4 alkylsulfinyl, trifluoromethylsulfonyl, trifluoromethylsulfinyl, C2-7 alkenyl or C2-7 alkynyl; R , R , m and n have the meanings given in the description; or a physiologically acceptable derivative thereof, pharmaceutical formulations containing them, processes for their preparation and their use in therapy and their use in the treatment or prophylaxis of an HIV infection or inflammation are disclosed.
摘要翻译：式（I）的芳硫基苄腈化合物，其中R是氢，硝基，三氟甲基，卤素，羧基，C 1-4羧酰胺基，腈，C 1-4烷酰基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基，三氟甲基磺酰基，三氟甲基亚磺酰基，烯基或C 2-7炔基; R 1，R 2，m和n具有说明书中给出的含义; 或其生理上可接受的衍生物，含有它们的药物制剂，其制备方法及其在治疗中的用途及其在治疗或预防HIV感染或炎症中的用途。

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