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1. 发明申请

WO1996001827A1 TETRACYCLIC DERIVATIVES AND THEIR USE AS ANTITUMOUR AGENTS 审中-公开
标题翻译：四环衍生物及其作为抗菌剂的用途
公开(公告)号：WO1996001827A1
公开(公告)日：1996-01-25
申请号：PCT/GB1995001598
申请日：1995-07-06
申请人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED , MILLER, David, Drysdale , BARRACLOUGH, Paul , VILE, Sadie , WALKER, Ann, Louise , SHANNON, Patrick, Vivian, Richard , CHUNCHATPRASERT, Laddawan , DEBONT, Pierre, Philippe, Marc , HUDSON, Alan, Thomas
发明人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds of formula (I) wherein A) is (a), (b), (c) or (d), X and Y are O, S, SO, SO2, CH2, CO or NR7, R is an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms wherein the 5- or 6-membered ring may be aromatic or non-aromatic. The compounds have been found to have anti-tumour activity. More specifically, the invention concerns pyrrolo (3,2-b) carbazoles, 1H-benzofuro (3,2-f) indoles and 1H-(1) benzothieno (2,3-f) indoles, methods of their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents.
摘要翻译：其中A）为（a），（b），（c）或（d）的式（I）化合物，X和Y为O，S，SO，SO 2，CH 2，CO或NR 7，R 1为任选取代的含有1至4个杂原子的5-或6-元杂环，其中5-或6-元环可以是芳族或非芳族的。发现这些化合物具有抗肿瘤活性。更具体地，本发明涉及吡咯（3,2-b）咔唑，1H-苯并呋喃（3,2-f）吲哚和1H-（1）苯并噻吩并（2,3-f）吲哚，其制备方法，药物制剂含有它们及其作为抗肿瘤剂的用途。

2. 发明申请

WO1995021170A1 ANTITUMOUR TETRACYCLIC COMPOUNDS 审中-公开
标题翻译：抗菌四环化合物
公开(公告)号：WO1995021170A1
公开(公告)日：1995-08-10
申请号：PCT/GB1995000190
申请日：1995-01-31
申请人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED , MILLER, David, Drysdale , VILE, Sadie , SHANNON, Patrick, Vivian, Richard , CHUNCHATPRASERT, Laddawan , HUDSON, Alan, Thomas
发明人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D495/04 , C07F7/0812
摘要： The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns compounds of formula (I), wherein A is (a), (b), (c) or (d), X is O, S, SO, SO2, CH2, CO or NR , wherein R is H, alkyl, aralkyl, aryl, alkenyl, acyl, alkynyl, sulphonyl or substituted sulphonyl; Y is O, S, SO, SO2, CH2, CO or NR , with the proviso that Y is not O when X is O; methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents. The compounds have low toxicity against normal cell lines whilst exhibiting anti-tumour cell activity.
摘要翻译：本发明涉及已被发现具有抗肿瘤活性的杂环化合物。更具体地，本发明涉及式（I）化合物，其中A是（a），（b），（c）或（d），X是O，S，SO，SO 2，CH 2，CO或NR 7 其中R 7是H，烷基，芳烷基，芳基，烯基，酰基，炔基，磺酰基或取代的磺酰基; Y是O，S，SO，SO2，CH2，CO或NR7，条件是当X是O时，Y不为O; 其制备方法，含有它们的药物制剂及其作为抗肿瘤剂的用途。该化合物对正常细胞系具有低毒性，同时具有抗肿瘤细胞活性。

3. 发明申请

WO1994002483A1 TETRACYCLIC COMPOUNDS PROCESS AND INTERMEDIATES FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOUR AGENTS 审中-公开
标题翻译：四环化合物的制备方法及其制备及其作为抗菌剂的用途的中间体
公开(公告)号：WO1994002483A1
公开(公告)日：1994-02-03
申请号：PCT/GB1993001512
申请日：1993-07-19
申请人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED , FRANZMANN, Karl, Witold , STABLES, Jeremy, Nigel , SHANNON, Patrick, Vivian, Richard , RAO, Nagaraja, Kodanda, Ranganatha , CHUNCHATPRASERT, Laddawan
发明人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D207/333 , C07D207/34 , C07D209/94 , C07D403/06 , C07D409/06 , C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to heterocyclic compounds of formula (I), which have been found to have anti-tumour activity. More specifically, the invention concerns Pyrrolo (3,2-bŸ ) carbazoles, 1H-Benzofuro (3,2-fŸ ) indoles and 1H-(1) Benzothieno (2,3-fŸ ) indoles, methods for their preparation, intermediates, pharmaceutical formulations containing them and their use as anti-tumour agents.
摘要翻译：本发明涉及已发现具有抗肿瘤活性的式（I）的杂环化合物。更具体地，本发明涉及吡咯（3,2-by）咔唑，1H-苯并呋喃（3,2-fy）吲哚和1H-（1）苯并噻吩并（2,3-f））吲哚，其制备方法，含有它们的药物制剂及其作为抗肿瘤剂的用途。

4. 发明申请

WO9945926B1 CONDENSED HETEROCYCLIC COMPOUNDS AS ANTI-INFLAMMATORY AND IMMUNOMODULATORY AGENTS 审中-公开
标题翻译：作为抗炎和免疫调节剂的稠合杂环化合物
公开(公告)号：WO9945926B1
公开(公告)日：1999-11-04
申请号：PCT/GB9900580
申请日：1999-02-25
申请人： UNIV CARDIFF , SHANNON PATRICK VIVIAN RICHARD , EICHHOLTZ THOMAS , LINSTEAD DAVID , MASDIN PHILIP , SKINNER RICHARD
发明人： SHANNON PATRICK VIVIAN RICHARD , EICHHOLTZ THOMAS , LINSTEAD DAVID , MASDIN PHILIP , SKINNER RICHARD
IPC分类号： A61K31/41 , A61K31/422 , A61K31/4245 , A61K31/454 , A61K31/7056 , A61K31/44 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/445 , A61K31/535 , A61K31/70
CPC分类号： A61K31/403 , A61K31/41 , A61K31/422 , A61K31/4245 , A61K31/454 , A61K31/5377 , A61K31/7056
摘要： The present invention relates to use of a compound of formula (1) as an immunomodulatory or anti-inflammatory drug or for use in the treatment of a therapeutic indication in which inhibition of dehydro-orate dehydrogenase (DHODH) is beneficial and salts and physiologically functional salts thereof, wherein X, R , R , A, Z and Z have the meanings given in Claim 1.
摘要翻译：本发明涉及式（1）化合物作为免疫调节剂或抗炎药的用途或用于治疗其中抑制脱氢酸盐脱氢酶（DHODH）是有益的治疗适应症和盐和生理功能的用途其中X，R 5，R 6，A，Z 1和Z 2具有权利要求1中给出的含义。

5. 发明申请

WO1995021171A1 TRICYCLIC DERIVATIVES AND THEIR USE AS ANTI-CANCER AGENTS 审中-公开
标题翻译：三肽衍生物及其作为抗癌剂的用途
公开(公告)号：WO1995021171A1
公开(公告)日：1995-08-10
申请号：PCT/GB1995000203
申请日：1995-02-01
申请人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED , MILLER, David, Drysdale , CHUNCHATPRASERT, Laddawan , SHANNON, Patrick, Vivian, Richard
发明人： THE WELLCOME FOUNDATION LIMITED , UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound of formula (I) or a salt or physiologically functional derivative thereof, wherein A is (a), (b), (c), (d), X is O, S, SO, SO2, CH2, CO or NR , wherein R is H, alkyl, aralkyl, aryl, alkenyl, acyl, alkynyl, sulphonyl, substituted sulphonyl, or COOMe; Y is O, S, SO, SO2, CH2, CO or NR ; R is COR , CHO, CH2OH, CH2OR , CONH2, COOR , CONHR , CONR R , CSOR , CSSR , COSR , CSNHR , CSNR R , CNHOR wherein R and R are independently hydrogen, alkoxyalkyl, heterocycloalkyl, heteroaralkyl, or C1-10 optionally substituted hydrocarbyl group which may optionally contain one or two oxygen atoms in the chain; or R and R are a sugar group. R is H, halo, cyano, COOR , alkyl, aryl, alkenyl, alkynyl, alkoxy, (wherein alkyl, aryl, alkenyl, alkynyl and alkoxy can be substituted) or CH2CH2CO2R wherein R is alkyl or aryl; R is H, alkyl, halogen, cyano, amino, COOR , CONHR , COR , CH2OH, CH2OR , CONH2, CONR R , CSOR , CSSR , COSR , CSNHR , CSNR R or CNHOR ; R is H, halogen, cyano, amino, alkyl, COOR , CONHR , COR , CH2OH, CH2OR , CONH2, CONR R , CSOR , CSSR , COSR , CSNHR , CSNR R or CNHOR ; R is H, hydroxy, aryloxy, aralkyloxy, alkyl, substituted alkyl, aralkyl, nitro, amino, halo, cyano COOR or CHO; R is H, aryl, alkyl, aralkyl, nitro, halogen, CHO or COR wherein R is alkyl or aryl; wherein R is not H when R is H and R is not H or Me when A is (c). Processes for their preparation are described, together with their use in medicine, particularly cancer therapy and pharmaceutical formulations comprising the compounds.
摘要翻译：式（I）化合物或其盐或生理功能衍生物，其中A为（a），（b），（c），（d），X为O，S，SO，SO 2，CH 2，CO或NR 其中R 7为H，烷基，芳烷基，芳基，烯基，酰基，炔基，磺酰基，取代的磺酰基或COOMe; Y是O，S，SO，SO 2，CH 2，CO或NR 7; R 1是COR 8，CHO，CH 2 OH，CH 2 O 9，CONH 2，COOR 8，CONHR 8，CONR 8 R 9，CSOR 8，CSSR 8， COSR 8，CSNHR 8，CSNR 8 R 9，CNHOR 8，其中R 8和R 9独立地是氢，烷氧基烷基，杂环烷基，杂芳烷基或C 1-10任选取代的烃基该基团可任选地在链中含有一个或两个氧原子; 或R 8和R 9为糖基团。 R 2是H，卤素，氰基，COOR 8，烷基，芳基，烯基，炔基，烷氧基，（其中烷基，芳基，烯基，炔基和烷氧基可以被取代）或CH 2 CH 2 CO 2 R 12其中R 12 >是烷基或芳基; R 3是H，烷基，卤素，氰基，氨基，COOR 8，CONHR 8，COR 8，CH 2 OH，CH 2 OR 8，CONH 2，CONR 8 R 9， 8，CSSR 8，COSR 8，CSNHR 8，CSNR 8 R 9或CNHOR 8; R 4是H，卤素，氰基，氨基，烷基，COOR 8，CONHR 8，COR 8，CH 2 OH，CH 2 O 8，CONH 2，CONR 8 R 9， 8，CSSR 8，COSR 8，CSNHR 8，CSNR 8 R 9或CNHOR 8; R 5是H，羟基，芳氧基，芳烷氧基，烷基，取代的烷基，芳烷基，硝基，氨基，卤素，氰基COOR 8或CHO; R 6是H，芳基，烷基，芳烷基，硝基，卤素，CHO或COR 13，其中R 13是烷基或芳基; 当A为（c）时，当R 2为H且R 3不为H或Me时，R 8不为H。描述了其制备方法及其在药物中的用途，特别是癌症治疗和包含该化合物的药物制剂。

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