公开(公告)号：EP1053350A1

公开(公告)日：2000-11-22

申请号：EP99903891.2

申请日：1999-02-08

Applicant: YEDA RESEARCH AND DEVELOPMENT COMPANY, LTD.

Inventor： LAPIDOT, Aviva ,  IAKOBASHVILI, Robert ,  MALIN, Gennady

IPC: C12Q1/68

CPC classification number: C12Q1/6848 ,  C12Q1/6869 ,  C12Q2527/125 ,  C12Q2531/113

Abstract: The osmoprotectants proline, 2- methyl- 4- carboxy- 3,4,5,6- tetrahydropyrimidine ('THP(B)'), and 2-methyl-4-carboxy-5-hydroxy-3,4,5,6-tetrahydropyrimidine ('THP(A)') are capable of increasing the thermal stability of DNA polymerases at elevated temperatures. THP(B) is further effective in lowering the melting temperature of double-stranded DNA. Proline, THP(A) and THP(B) are thus useful in procedures involving melting of double-stranded DNA and/or polymerase-mediated DNA synthesis, such as in primer extension, in PCR (polymerase chain reaction) amplification and in DNA sequencing.

公开(公告)号：EP1140958B1

公开(公告)日：2006-03-15

申请号：EP99961263.3

申请日：1999-12-28

Applicant: YEDA RESEARCH AND DEVELOPMENT COMPANY, LTD.

Inventor： LAPIDOT, Aviva ,  LITOVCHICK, Alexander.Harvard Univer. Med. School ,  EVDOKIMOV, Artem. Building 538,Room 200C

IPC: C07H7/00 ,  C07H3/04 ,  C07H3/06 ,  C07H15/04 ,  A61K31/70

CPC classification number: C07H15/04 ,  C07H3/04 ,  C07H3/06 ,  C07H7/00

Abstract: Conjugates of saccharide and an acetamidino- or guanidino- compounds of formula (I), wherein A is CH3 or NH2; X is a linear or branched C1-C8 alkyl chain optionally containing hydroxy, amino and/or oxo groups; n is an integer from 1 to 6, and Sac is the residue of a mono- or oligo-saccharide are useful as antiviral, particularly as antiretroviral, agents, and can be used either alone or together with other compounds used in AIDS treatment such as AZT and/or protease inhibitors, for the treatment of HIV-infection, AIDS and manifestations of AIDS such as Kaposi sarcoma. Particularly preferred compounds are aminoglycoside-arginine conjugates in which the saccharide is a natural aminoglycoside antibiotic such as kanamycin, gentamycin and neomycin that is conjugated to arginine residues.