摘要:
The invention relates to the use of 8-hydroxyquinoline 7-carboxylic acid derivatives in order to produce integrase-inhibiting medicaments, capable of blocking viral replication in the stages preceding integration, and if appropriate at the level of this integration stage, these medicaments being usable for the treatment of retroviral pathologies, in particular for the treatment of AIDS.
摘要:
The invention relates to derivatives corresponding to formula I: in which X is an alkyl-(CH2)n— chain with n=0, 1 or 2, or O or N, Z is an aromatic which may contain heteroatoms chosen from O, N or S, as substitutions for the carbon atoms constituting said aromatic ring, this ring being substituted or otherwise with Rb, Rb represents 1 to 3 substituents chosen from —OH, —OR, —COOH, —COOR, —COH, —COR, —NH2, —NH(R), —NH(R,R′), —SH, —SR and CN, Ra is H or —(CH2)n′—Y, with n′=0, 1, 2 or 3 and Y and —CH3, —COOH, —COOR, —CN, —OH, —OR, SR, or an aryl group optionally substituted with Rb, R and R′ represent a linear or branched alkyl chain of 1 to 4 C, and their pharmaceutically acceptable salts. Application as active ingredient of medicaments inhibiting retrovirus integrases.
摘要:
The invention relates to derivatives corresponding to formula I: in which X is an alkyl-(CH2)n— chain with n=0, 1 or 2, or O or N, Z is an aromatic which may contain heteroatoms chosen from O, N or S, as substitutions for the carbon atoms constituting said aromatic ring, this ring being substituted or otherwise with Rb, Rb represents 1 to 3 substituents chosen from —OH, —OR, —COOH, —COOR, —COH, —COR, —NH2, —NH(R), —NH(R,R′), —SH, —SR and CN, Ra is H or —(CH2)n′—Y, with n′=0, 1, 2 or 3 and Y and —CH3, —COOH, —COOR, —CN, —OH, —OR, SR, or an aryl group optionally substituted with Rb, R and R′ represent a linear or branched alkyl chain of 1 to 4 C, and their pharmaceutically acceptable salts. Application as active ingredient of medicaments inhibiting retrovirus integrases.
摘要:
The present invention is directed to a rhenium complex of general Formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is Se; Y is NH, O or S or is a methylene group; Z is halogen; m=0, 1, or 2 and p=0, 1, or 2, provided that m and p are both different from zero when Y is NH, O or S; n=3; R′ is a phenyl group or a group of general Formula —(CH2)q—COOH wherein q=1 or 2, a pharmaceutical composition comprising a therapeutically effective amount of at least one of such rhenium complex where X is additionally S or Te, a method for preparing said rhenium complex and a method for treating a proliferative growth related-disorder using a therapeutically effective amount of at least one of said rhenium complex where X is additionally S or Te. Also claimed is the use of compounds of formula (II) in the preparation of compounds of formula (I).
摘要翻译:本发明涉及通式(I)的铼络合物或其药学上可接受的盐或溶剂化物,其中X为Se; Y是NH,O或S,或是亚甲基; Z是卤素; m = 0,1或2,p = 0,1或2,条件是当Y是NH,O或S时,m和p都不同于0; n = 3; R'是苯基或其中q = 1或2的通式 - (CH 2)q -COOH的基团,药物组合物包含治疗有效量的至少一种这样的铼络合物,其中X另外是S或Te, 制备所述铼配合物的方法和使用治疗有效量的至少一种所述铼配合物治疗增殖性生长相关障碍的方法,其中X另外是S或Te。 还要求保护的是式(II)化合物在制备式(I)化合物中的用途。
摘要:
The invention relates to the use of 8-hydroxyquinoline 7-carboxylic acid derivatives in order to produce integrase inhibiting medicaments, capable of blocking viral replication in the stages preceding integration, and if appropriate, at the level of this integration stage, these medicaments being usable for the treatment of retroviral pathologies, in particular for the treatment of AIDS.
摘要:
New tetra-alkyl-2,2,5,5-cyclohexanone-4-ol-1-compounds and their sulphonyl derivatives with the general formula: ##STR1## in which: each of R and R', identical or different, represents an alkyl radical (1-5 carbons) and R" represents a hydrogen atom or a radical SO.sub.2 R"' in which R"' represents an alkyl radical (1-5 carbons) or an aryl radical (6-14 carbons), the process and the intermediates for their preparation, as well as their use in the synthesis of cyclopropane lactones of cis structure.
摘要:
The present invention is directed to a rhenium complex of general Formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is Se; Y is NH, O or S or is a methylene group; Z is halogen; m=0, 1, or 2 and p=0, 1, or 2, provided that m and p are both different from zero when Y is NH, O or S; n=3; R′ is a phenyl group or a group of general Formula —(CH2)q—COOH wherein q=1 or 2, a pharmaceutical composition comprising a therapeutically effective amount of at least one of such rhenium complex where X is additionally S or Te, a method for preparing said rhenium complex and a method for treating a proliferative growth related-disorder using a therapeutically effective amount of at least one of said rhenium complex where X is additionally S or Te. Also claimed is the use of compounds of formula (II) in the preparation of compounds of formula (I).
摘要翻译:本发明涉及通式(I)的铼络合物或其药学上可接受的盐或溶剂化物,其中X为Se; Y是NH,O或S,或是亚甲基; Z是卤素; m = 0,1或2,p = 0,1或2,条件是当Y是NH,O或S时,m和p都不同于0; n = 3; R'是苯基或其中q = 1或2的通式 - (CH 2)q -COOH的基团,药物组合物包含治疗有效量的至少一种这样的铼络合物,其中X另外是S或Te, 制备所述铼配合物的方法和使用治疗有效量的至少一种所述铼配合物治疗增殖性生长相关障碍的方法,其中X另外是S或Te。 还要求保护的是式(II)化合物在制备式(I)化合物中的用途。
摘要:
The invention relates to the use of 8-hydroxyquinoline 7-carboxylic acid derivatives in order to produce integrase-inhibiting medicaments, capable of blocking viral replication in the stages preceding integration, and if appropriate at the level of this integration stage, these medicaments being usable for the treatment of retroviral pathologies, in particular for the treatment of AIDS.
摘要:
##STR1## New tetra-alkyl-2,2,5,5 cyclohexanone-4-ol-1 and their sulfonated derivatives of the general formula (I), wherein R and R', which may be the same or different, represent an alkyl radical (1-5 atoms of carbon) and R' represents a hydrogen atom or a radical SO--R'" wherein R'" represents an alkyl radical (1-5 atoms of carbon) or an aryl radical (6-14 atoms of carbon), their preparation intermediaries and process, as well as their application to the synthesis of cyclopropanic lactones having the cis structure.
摘要:
The invention concerns quinoline derivatives of formula (I) in which: Ra, Rb and Rc, identical or different represent one or several substituents, themselves identical or different, in any position on the cycles, this or these substituents being selected among a —(CH2)n—Y or —CH═CH—Y group, in which Y is halogen, —OH, —OR, —COH, —COR, —COOH, COOR, —COH, —COR, —CONH2, —CON(Rx, Ry)—CH═NOH, —CO— —CH═NOH, —NH2, —N(Rx, Ry), —NO2, —PO(OR)2—SH2, —SR, —SO2R, —SO2NHR, CN, or Z(Rc) in which R is a C1-C8 alkyl, or aryl or a heterocyclic compound, Rx and Ry, identical or different are C1-C5 alkyl, an aryl or heterocyclic compound and n is nil or a whole number between 1 and 5 Rb can further represent a hydrogen, and when Y is —COOH or —COOR in Rc, Z, if it represents an aryl, comprises at least 3 substituents or the quinoline ring is trisubstituted; X is an ethylene double bond; a —(CH2)n— group in which n is a whole number between 1 and 5: or a —CH(Rd—CH(Re) group, Rd and Re, identical or different, representing a hydrogen, a halogen, hydroxy or epoxy; or a —(CH2)n, —O—C—(CH2)m—, —(CH2)n, —C(O)—O—(CH2)m, —(CH2)n, —O—(CH2)m—, (CH2)n, —N(Q)—(CH2)m—, or (CH2)n, —S(O)—(CH2)m—, group, in which n=1 to 8, m=0 to 8, t=0, 1 or 2, and Q=h, aryl or alkyl. The invention also concerns the pharmaceutically acceptable salts of these derivatives, the diastereoisomeric and the enantiomeric forms thereof. The invention is useful as medicines with HIV anti-integrase inhibiting effect.