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21. 发明专利

CA2428802A1 CAMPTOTHECIN COMPOUNDS WITH A SULFHYDRYL GROUP 未知
公开(公告)号：CA2428802A1
公开(公告)日：2002-05-23
申请号：CA2428802
申请日：2001-11-16
申请人： RES TRIANGLE INST , UNIV DUKE , NAT INST HEALTH
发明人： ADAMS DAVID J , GAMCSIK MICHAEL P , WALL MONROE E , COLVIN O MICHAEL , WANI MANSUKH C , POMMIER YVES , MANIKUMAR GOVINDARAJAN
IPC分类号： A61K31/4745 , A61K38/00 , A61K47/48 , C07D491/22 , C07K5/02 , A61K33/44
摘要： Camptothecin compounds which are effective anti-tumor compounds are disclosed. These conjugates inhibit the enzyme topoisomerase I and enhance the stability of the topoisomerase I-DNA cleavable complex.

22. 发明专利

NZ235792A METHOD FOR INHIBITING THE ENZYME TOPOISOMERASE I USING CAMPTOTHECIN ANALOGUES 未知
公开(公告)号：NZ235792A
公开(公告)日：1992-04-28
申请号：NZ23579290
申请日：1990-10-23
申请人： RES TRIANGLE INST
发明人： WALL MONROE E , WANI MANSUKH , NICHOLAS ALLEN W , MANIKUMAR GOVINDARAJAN
IPC分类号： A61K31/47 , A61K20060101 , A61K31/44 , A61P35/00 , A61P43/00 , C07D20060101 , C07D471/04 , C07D491/14 , C07D491/20 , C07D491/22 , C12N9/00 , C12N9/90 , C12N9/99
摘要： A method for synthesizing camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase.

23. 发明专利

PT95324A Process for preparation of 20(S) or 20(RS)-camptothecins, the salts thereof, and pharmaceutical compositions that contain them, and for inhibition of the enzyme topoisomerase I 未知
公开(公告)号：PT95324A
公开(公告)日：1991-05-22
申请号：PT9532490
申请日：1990-09-14
申请人： RES TRIANGLE INST
发明人： WALL MONROE E , WANI MANSUKH C , NICHOLAS ALLAN W , MANIKUMAR GOVINDARAJAN
IPC分类号： A61K31/335 , A61K31/435 , A61K31/47 , C07D491/00 , C07D491/22 , C07K5/06 , C07K5/08 , C07K5/10
摘要： The present invention relates to the process for preparation of a 20(S) or 20(RS) camptothecin having the structure shown below in which Z is H or C1-8 alkyl and R is NO2, NH2, N3, H, halogen, COOH, OH, C1-3 O-alkyl, SH, C1-3 S-alkyl, CN, CH2NH2, C1-3 NH-alkyl, C1-3 CH2-NH-alkyl, N-(C1-3 alkyl)2, CH2N(C1-3 alkyl)2, O-, NH- or S-CH2CH2N(CH2CH2OH)2, O-, NH- or S-CH2CH2CH2N(CH2CH2OH)2, O-, NH- or S-CH2CH2N(CH2CH2CH2OH)2, O-, -NH- or S-CH2CH2CH2N(CH2CH2CH2OH2)2, O-, NH- or S-CH2CH2N(C1-3 alkyl)2, O-, NH- or S-CH2CH2CH2N(C1-3 alkyl)2, CHO, C1-3 alkyl or NHCOCHR1NR2R3, in which R1 is a side chain of an α-amino acid and R2 and R3 are, independently of each other, hydrogen or a lower alkyl group or R3 is a peptide unit containing l-3 amino acid units bound to nitrogen, via a peptide bond; NHCO-alkyleno-C2-8-X or NHCO-alkenyleno-C2-8-X, in which X is COOH, CONR2-(CH2)n- NR2R3, where n = 1-10 and R2 and R3 are defined as above; NHCO-B-(CH2)n-NR2R3, where B = oxygen or NH; or where m + y = 3-6. The process involves, when appropriate: diazotizing a 9-amino-10,11-methylenedioxy-20(S)- or 20(RS)-camptothecin and displacing the diazo group with a corresponding nucleophil, or reducing the group R = CN; or alkylating the group R = OH, SH, NH2 or CH2NH2 with an alkylating agent; or reacting 10,11-methylenedioxy-20(S) or 20(RS)- camptothecin with a mixture of concentrated sulphuric and nitric acid; or nitrating 10,11-methylenedioxy-20(S)- or 20(RS)- camptothecin in order to obtain 9-nitro-10,11- methylenedioxy-20(S) or 20(RS)-camptothecin and then reducing the 9-nitro group; or reacting 9-amino or 9-amino-7-alkyl C1-8-10,11- methylenedioxy-20(S)- or 20(RS)-camptothecin with an amino acid with a protected amino group or peptide containing 1-4 amino acid units, a saturated or unsaturated C4-10 carboxylic acid anhydride or phosgene, and then with a primary or secondary straight, branched- chain or cyclic diamine, or with a tertiary amino- alcohol. The invention also relates to the process for preparation of salts of the abovementioned compounds, as well as the process for preparation of pharmaceutical compositions containing the compounds or salts.

24. 发明专利

DE60022095D1 CAMPTOTHECIN-BETA-ALANIN-ESTER MIT TOPOISOMERASE I HEMMUNG 未知
公开(公告)号：DE60022095D1
公开(公告)日：2005-09-22
申请号：DE60022095
申请日：2000-06-14
申请人： RES TRIANGLE INST RES TRIANGLE , BRISTOL MYERS SQUIBB CO
发明人： WALL MONROE E , WANI MANSUKH C , MANIKUMAR GOVINDARAJAN , BALASUBRAMANIAN NEELAKANTAN , VYAS DOLATRAI
IPC分类号： C12N9/99 , A61K38/00 , A61P35/00 , A61P35/02 , C07D491/22 , C07K5/023 , A61K31/4741 , A61K31/4745 , A61K31/435
摘要： beta-Alanine esters of camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.

25. 发明专利

CA2530046A1 7-SUBSTITUTED CAMPTOTHECIN AND CAMPTOTHECIN ANALOGS AND METHODS FOR PREPARING SAME 未知
公开(公告)号：CA2530046A1
公开(公告)日：2005-02-03
申请号：CA2530046
申请日：2004-06-25
申请人： RES TRIANGLE INST
发明人： WALL MICHAEL A , WANI MANSUKH C , MANIKUMAR GOVINDARAJAN
IPC分类号： C07D491/147 , A61K31/47 , C07D491/22
摘要： Methods of forming camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex .

26. 发明专利

ES2165346T3 未知
公开(公告)号：ES2165346T3
公开(公告)日：2002-03-16
申请号：ES90310085
申请日：1990-09-14
申请人： RES TRIANGLE INST
发明人： WALL MONROE E , NICHOLAS ALLAN W , MANIKUMAR GOVINDARAJAN , WANI MANSUKH C
IPC分类号： C07D491/22 , C07K5/06 , C07K5/08 , C07K5/10 , A61K31/47
摘要： A camptothecin analog having the structure shown below: where Z is H or C1-8 alkyl, R is NO2, NH2 N3, hydrogen, halogen, COOH, OH, O-C1-3 alkyl, SH, S-C1-3 alkyl, CN, CH2NH2, NH-C1-3 alkyl, CH2-NH-C1-3 alkyl, N(C1-3 alkyl)2, CH2N(C1-3 alkyl)2, O-, NH- or S-CH2CH2N(CH2CH2OH)2, O-, NH- or S-CH2CH2CH2N(CH2CH2OH)2, O-, NH- or S-CH2CH2N(CH2CH2CH2OH)2, O-, NH- or S-CH2CH2CH2N(CH2CH2CH2OH2)2, O-, NH- or S-CH2CH2N(C1-3 alkyl)2, O-, NH- or S-CH2CH2CH2N(C1-3 alkyl)2, CHO, C1-3 alkyl or NHCOCHR NR R , where R is the side-chain of an alpha -amino acid and R and R , independently, are hydrogen or a lower alkyl group or R is a peptide unit containing 1-3 amino acid units bonded to the nitrogen through a peptide bond; NHCO-C2-8-alkylene-X or NHCO-C2-8-alkenylene-X, where X is COOH; CONR -(CH2)n-NR R , where n = 1-10 and R and R are as defined above; NHCO-B-(CH2)n-NR R , where B = oxygen or NH; or where m + y = 3-6, and salts thereof. B

28. 发明专利

ZA907360B 10,11-METHYLENEDIOXY-20(RS)-CAMPTOTHECIN AND 10,11-METHYLENEDIOXY-20(S)-CAMPTOTHECIN ANALOGS 未知
公开(公告)号：ZA907360B
公开(公告)日：1991-07-31
申请号：ZA907360
申请日：1990-09-14
申请人： RES TRIANGLE INST
发明人： WALL MONROE E , MONROE E WALL , WANI MANSUKH C , MANSUKH C WANI , NICHOLAS ALLAN W , ALLAN W NICHOLAS , MANIKUMAR GOVINDARAJAN , GOVINDARAJAN MANIKUMAR
IPC分类号： A61K31/4745 , A61K31/47 , A61P35/00 , A61P43/00 , C07D491/22 , C07K1/113 , C07K5/06 , C07K5/08 , C07K5/10 , C07D
摘要： A camptothecin analog having the structure shown below: wherein R is NO2, NH2, NHCOCHR1NR2R3, where R1 is the side-chain of an alpha -amino acid and R2 and R3, independently are hydrogen or a lower alkyl group or R3 is a peptide unit containing 1-3 amino acid units bonded to the nitrogen through a peptide bond, NHCO-C2-8-alkylene-X or NHCO-C2-8-alkenylene-X, where X is COOH or CONR2-(CH2)n-NR2R3, n=1-10 and R2 and R3 are as defined above, NHCO-Z-(CH2)n-NR2R3, where z=oxygen or NH, or where m+y=3-6 and salts thereof.

29. 发明专利

ZA9007360B 10,11-METHYLENEDIOXY-20(RS)-CAMPTOTHECIN AND 10,11-METHYLENEDIOXY-20(S)-CAMPTOTHECIN ANALOGS 未知
公开(公告)号：ZA9007360B
公开(公告)日：1991-07-31
申请号：ZA9007360
申请日：1990-09-14
申请人： RES TRIANGLE INST
发明人： WALL MONROE E , MONROE E WALL , WANI MANSUKH C , MANSUKH C WANI , NICHOLAS ALLAN W , ALLAN W NICHOLAS , MANIKUMAR GOVINDARAJAN , GOVINDARAJAN MANIKUMAR
IPC分类号： A61K31/47 , A61K31/4745 , A61P35/00 , A61P43/00 , C07D491/22 , C07K1/113 , C07K5/06 , C07K5/08 , C07K5/10 , C07D
CPC分类号： C07D491/22

30. 发明专利

AU4418789A SYNTHESIS OF CAMPTOTHECIN AND ANALOGS THEREOF 未知
公开(公告)号：AU4418789A
公开(公告)日：1990-04-18
申请号：AU4418789
申请日：1989-09-28
申请人： RES TRIANGLE INST
发明人： WALL MONROE E , WANI MANSUKH C , NICHOLAS ALLAN W , MANIKUMAR GOVINDARAJAN
IPC分类号： C07D491/147 , C07D491/22 , A61K31/47
摘要： A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anti-tumor activity.

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