发明名称 4-(or 5-) substituted catechol derivatives
摘要 Compounds of the formula:; are disclosed. The compounds act as phosphodiesterase-4 modulators, and useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions. Other embodiments are also disclosed.
申请公布号 US8877816(B2) 申请公布日期 2014.11.04
申请号 US200812275168 申请日期 2008.11.20
申请人 Decode Genetics EHF 发明人 Singh Jasbir;Gurney Mark E.;Burgin Alex;Sandanayaka Vincent;Kiselyov Alexander
分类号 A61K31/165;C07C233/02;A61P29/00;C07C311/08;C07C275/32;C07C43/295;C07D213/73;C07C45/71;C07C43/29;C07C205/38;C07D213/81;C07D213/83 主分类号 A61K31/165
代理机构 Heslin Rothenberg Farley & Mesiti P.C. 代理人 Heslin Rothenberg Farley & Mesiti P.C.
主权项 1. A compound of formula I: or a salt thereof, wherein: R1 is chosen from H, (C1-C8)alkyl and halo(C1-C8)alkyl; R2 is chosen from H and halo; Ar1 is selected from optionally substituted phenyl and optionally substituted heteroaryl, wherein substituted phenyl and substituted heteroaryl refer to phenyl and heteroaryl residues wherein up to three H atoms in each residue are individually replaced with halogen, alkyl, haloalkyl, haloalkoxy, hydroxy, loweralkoxy, oxaalkyl, carboxy, carboalkoxy, carboxamido, alkylaminocarbonyl, alkoxycarbonyl, alkoxycarbonylamino, acyl, alkoxyalkyl, benzenesulfonyl, cyano, carbonyl, nitro, amino, urea, alkylurea, hydroxyalkyl, alkylamino, dialkylamino, aminoalkyl, (alkyl)(aryl)aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, dialkylaminoalkoxy, heterocyclylalkoxy, mercapto, alkylthio, alkylsulfinyl, alkylsulfonyl, acylamino, acylaminoalkyl, acylaminoalkoxy, amidino, acetoxy, sulfoxide, alkylsulfoxide, sulfone, alkylsulfone, sulfonylamino, alkylsulfonylamino, aryl, heterocyclyl, hydroxyimino, alkoxyimino, aminosulfonyl, trityl, amidino, guanidino, ureido, benzyloxyphenyl, benzyl, heteroaryl, heterocyclylalkyl, phenoxy, benzyloxy, heteroaryloxy, —NH(tBoc), or —NHSO2NH2 ; and Ar2 is selected from: (a) phenyl substituted in the para position with a single substituent selected from halogen, alkyl, haloalkyl, haloalkoxy, hydroxy, loweralkoxy, oxaalkyl, carboxy, carboalkoxy, carboxamido, alkylaminocarbonyl, alkoxycarbonyl, alkoxycarbonylamino, acyl, alkoxyalkyl, benzenesulfonyl, cyano, carbonyl, nitro, amino, urea, alkylurea, hydroxyalkyl, alkylamino, dialkylamino, aminoalkyl, (alkyl)(aryl)aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, dialkylaminoalkoxy, heterocyclylalkoxy, mercapto, alkylthio, alkylsulfinyl, alkylsulfonyl, acylamino, acylaminoalkyl, acylaminoalkoxy, amidino, acetoxy, sulfoxide, alkylsulfoxide, sulfone, alkylsulfone, sulfonylamino, alkylsulfonylamino, aryl, heterocyclyl, hydroxyimino, alkoxyimino, aminosulfonyl, trityl, amidino, guanidino, ureido, benzyloxyphenyl, benzyl, heteroaryl, heterocyclylalkyl, phenoxy, benzyloxy, heteroaryloxy, —NH(tBoc), and —NHSO2NH2; and(b) pyridinyl substituted in the para position with a single substituent selected from halogen, alkyl, haloalkyl, haloalkoxy, hydroxy, loweralkoxy, oxaalkyl, carboxy, carboalkoxy, carboxamido, alkylaminocarbonyl, alkoxycarbonyl, alkoxycarbonylamino, acyl, alkoxyalkyl, benzenesulfonyl, cyano, carbonyl, nitro, amino, urea, alkylurea, hydroxyalkyl, alkylamino, dialkylamino, aminoalkyl, (alkyl)(aryl)aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, dialkylaminoalkoxy, heterocyclylalkoxy, mercapto, alkylthio, alkylsulfinyl, alkylsulfonyl, acylamino, acylaminoalkyl, acylaminoalkoxy, amidino, acetoxy, sulfoxide, alkylsulfoxide, sulfone, alkylsulfone, sulfonylamino, alkylsulfonylamino, aryl, heterocyclyl, hydroxyimino, alkoxyimino, aminosulfonyl, trityl, amidino, guanidino, ureido, benzyloxyphenyl, benzyl, heteroaryl, heterocyclylalkyl, phenoxy, benzyloxy, heteroaryloxy, —NH(tBoc), and —NHSO2NH2.
地址 Reykjavik IS