A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 38/01 (2006.01) C07D 207/02 (2006.01) C07D 207/06 (2006.01) C07D 207/08 (2006.01) C07D 207/09 (2006.01) C07D 207/12 (2006.01) C07D 207/14 (2006.01) C07D 207/16 (2006.01) C07D 211/10 (2006.01) C07D 211/22 (2006.01) C07D 295/00 (2006.01) C07D 403/06 (2006.01) C07K 5/062 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2441822
The present invention provides methods for the asymmetric synthesis of (S.S.R)- (-)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: where R1 is an optionally substituted or halogenated alkyl, aryl, heteroalyl or heteroaryl amine, said R1 further comprising a cyclie or bicyclic structure; R2 is methyl, CH2CH3, (CH2)2CH3, C(CH3)3, phenyl, 3, 4-dichlorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N- Boc-4-piperidine, CH2-(N-Boc-4-piperidine), 4-tetrahydropyran, CH2-4- tetrahydropyran. 3-methyl indolyl, 2-napythyl, 3-pyridyl, 4-pyridyl, 3- thienyl; R3 is R2 or C3-8alkyl, R4 is C1-3alkyl; and R5 is NH2, OH, NHOH, NHOCH3, N(CH3)OH, N(CH3)OCH3, NHCH2CH3, NH(CH2C H 3), NHCH2(2, 4-(OCH3)2pH, NHCH2(4-NO2)Ph, NHN(CH3)2, proline, or 2-hydroxymethyl pyrrolidine. Additionally, a method for the treatment of a neoplastic disease or for the inhibition of tumor cell growth each comprising the step of administering to an individual in need of such treatment a pharmacologically effective dose of the compounds of the present invention are provided.
L'invention concerne des procédés pour la synthèse asymétrique de (S,S,R)-(-)-actinonine et de ses analogues, et les composés ainsi synthétisés de formule structurale (I), dans laquelle R?1¿ représente amine hétéroalkylique ou hétéroarylique, aryle ou alkyle halogéné éventuellement substitué, R?1¿ représentant également une structure cyclique ou bicyclique ; R?2¿ représente méthyle, CH¿2?CH ¿3?, (CH¿2?)¿2?CH¿3?, C(CH¿3?)¿3?, phényle, 3,4-dichlorophényle, biphényle, benzyle, 4-hydroxybenzyle, pipédiridine, N-Boc-4-pipéridine, CH¿2?(N-Boc-4-pipéridine), 4-tétrahydropyrane, CH¿2?-4-tétrahydropyrane, 3-méthyle indolyle, 2-naphtyle, 3-pyridyle, 3-thiényle ; R?3¿ représente R?2¿ ou alkyle C¿3-8?, R?4¿ représente alkyleC¿1-3? ; et R?5¿ représente NH¿2?, OH, NHOH, NHOCH¿3?, N(CH¿3?)OH, N(CH¿3?)OCH¿3?, NHCH¿2?CH¿3?, NH(CH¿2?CH¿3?), NHCH¿2?(2,4-(OCH3)¿2?Ph, NHCH¿2?(4-NO¿2?)Ph, NHN(CH¿3?)¿2?, proline ou 2-hydroxyméthyl pyrrolidine. L'invention porte également sur une méthode de traitement d'une maladie néoplasique ou d'inhibition de la prolifération de cellules tumorales, qui consiste à administrer à une personne en ayant besoin, une dose efficace au plan pharmacologique des composés de l'invention.
Borella Christopher
Bornmann William G.
Scheinberg David
Scher Howard
Sirotnak Francis M.
Borden Ladner Gervais Llp
Sloan Kettering Institute For Cancer Research
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