Publication number: 20060148849
Abstract: 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.
Type:
Application
Filed:
March 1, 2006
Publication date:
July 6, 2006
Inventors:
Jean D'Angelo, Christophe Benard, Michele Danet, Marc Le Bret, Jean-Francois Mouscadet, Fatima Zouhiri, Marie Bayle, Didier Desmaele, Laurence Jeanson, Herve Leh, Frederic Subra
Patent number: 7064133
Abstract: 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.
Type:
Grant
Filed:
October 14, 2002
Date of Patent:
June 20, 2006
Assignees:
Bioalliance Pharma, Universite Paris SUD (Paris XI), Institut National de la Sante et de la Recherche Medicale (INSERM), Institut Gustave Roussy
Inventors:
Jean D'Angelo, Christophe Benard, Michele Danet, Marc Le Bret, Jean-Francois Mouscadet, Fatima Zouhiri, Marie Bayle, Didier Desmaele, Laurence Jeanson, Herve Leh, Frederic Subra
Patent number: 6670377
Abstract: 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 trisubstitute
Type:
Grant
Filed:
January 16, 2001
Date of Patent:
December 30, 2003
Assignee:
Centre National de la Recherche
Inventors:
Khalid Mekouar, Jean D'Angelo, Didier Desmaele, Jean-Francois Mouscadet, Frèdèric Subra, Christian Auclair
