C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 233/54 (2006.01) A61K 31/185 (2006.01) A61K 31/192 (2006.01) A61K 31/195 (2006.01) A61K 31/196 (2006.01) A61K 31/215 (2006.01) A61K 31/222 (2006.01) A61K 31/275 (2006.01) A61K 31/66 (2006.01) C07C 235/16 (2006.01) C07C 237/12 (2006.01) C07C 279/18 (2006.01) C07C 309/51 (2006.01) C07F 9/38 (2006.01)
Patent
CA 2187791
An influenza virus neuraminidase inhibitor, its analogs, its pharmaceutically acceptable salts, derivatives, and mixtures thereof having formula (I), where A is CO2H, CO2CH3, NO2, SO3H or PO3H2, B is CH, N, O or S, R1 and R2 are H, NO2 or (CHm)nX1 where m = 1 or 2, n is an integer from 0 to 4 and X1 is guanidino, OH, NH2, SH, NO2, F, Cl, Br, I, CN, CF3, CO2H, SO3H or PO3H2, R3 and R4 are H, (CHo)pX2, (CHo)pCHX2CH2X2, NH(CHo)pCHX2CH2X2, NHCO(CHo)pCH2X2 or NHCO(CHo)pCHX2CH2X2 where O = 1 or 2, p is an integer from 0 to 4 and X2 is H, guanidino, OH, NH2, SH, NO2, CF3, CO2H, SO3H or PO3H2, R5 = H, OH, NH2, (CHk)lX3, CO(CHk)lX3, SO(CHk)lX3 or SO2(CHk)lX3 where k = 1 or 2, l is an integer from 0 to 4 and X3 is guanidino, OH, NH2, SH, NO2, CF3, CO2H, SO3H or PO3H2, R6 is H, CH(OH)X4, CH(NH2)X4, COX4, SOX4, or SO2X4, where X4 is H, CH3, CH3CH2, CH3CHCH3, CH3CH2CH2 or halogen substituted analogs of X4. The inhibitor in a composition with a pharmaceutically acceptable carrier. A method of inhibiting influenza virus neuraminidase where the inhibitor is administered to a subject in a pharmaceutically acceptable amount along with effective amounts of a pharmaceutically acceptable carrier. Methods of marking a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of treating and preventing a subject infected with influenza virus (type A or B) using the inhibitor.
L~invention porte sur un inhibiteur de la neuraminidase du virus de la grippe de formule (I), ses analogues, ses sels pharmacocompatibles, ses dérivés, et ses mélanges. Dans la formule (I), A représente CO¿2?H, CO¿2?CH¿3?, NO¿2?, SO¿3?H or PO¿3?H¿2?, B représente CH, N, O or S, R¿1? et R¿2? sont H, NO¿2? ou (CH¿m?)¿n?X¿1? où m = 1 ou 2, n est un entier compris entre 0 et 4, et X¿1? représente guanidino, OH, NH¿2?, SH, NO¿2?, F, Cl, Br, I, CN, CF¿3?, CO¿2?H, SO¿3?H ou PO¿3?H¿2?, R¿3? et R¿4? représentent H, (CH¿o?)¿p?X¿2?, (CH¿o?)¿p?CHX¿2?CH¿2?X¿2?, NH(CH¿o?)¿p?CHX¿2?CH¿2?X¿2?, NHCO(CH¿o?)¿p?CH¿2?X¿2? ou NHCO(CH¿o?)¿p?CHX¿2?CH¿2?X¿2? où O = 1 ou 2, p est un entier compris entre 0 et 4 et X¿2? représente H, guanidino, OH, NH¿2?, SH, NO¿2?, CF¿3?, CO¿2?H, SO¿3?H ou PO¿3?H¿2?, R¿5? = H, OH, NH¿2?, (CH¿k?)¿l?X¿3?, CO(CH¿k?)¿l?X¿3?, SO(CH¿k?)¿l?X¿3? ou SO¿2?(CH¿k?)¿l?X¿3? où k = 1 ou 2, l est un entier compris entre 0 to 4 and X¿3? représente guanidino, OH, NH¿2?, SH, NO¿2?, CF¿3?, CO¿2?H, SO¿3?H ou PO¿3?H¿2?, R¿6? représente H, CH(OH)X¿4?, CH(NH¿2?)X¿4?, COX¿4?, SOX¿4?, ou SO¿2?X¿4?, où X¿4? représente H, CH¿3?, CH¿3?CH¿2?, CH¿3?CHCH¿3?, CH¿3?CH¿2?CH¿2? ou des analogues de X¿4? à substitution halogène. L'invention concerne également l'inhibiteur dans un composition à excipient pharmacocompatible, une méthode d'inhibition de la neuraminidase du virus de la grippe selon laquelle ledit inhibiteur est administré en dose pharmacocompatible avec un excipient pharmacocompatible en dose efficace, des procédés de fabrication d'une composition pharmaceutiques constituée desdits inhibiteur et excipient acceptable, et des méthodes de traitement et de prévention à l'aide dudit inhibiteur de sujets infectés par le virus (A ou B) de la grippe.
Air Gillian
Brouillette Wayne J.
Luo Ming
Gowling Lafleur Henderson Llp
University Of Alabama At Birmingham (the)
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