[EN] HIGHLY EFFICIENT MYELOPEROXIDASE ACTIVATABLE IMAGING AGENTS<br/>[FR] AGENTS D'IMAGERIE EXTRÊMEMENT EFFICACES POUVANT ÊTRE ACTIVÉS PAR MYÉLOPEROXYDASE
申请人:MASSACHUSETTS GEN HOSPITAL
公开号:WO2021127013A1
公开(公告)日:2021-06-24
Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using magnetic resonance or nuclear imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using the compounds are also provided.
Propanolamine derivatives of the formula: ##STR1## wherein R.sup.2 is CH.sub.3 SO or CH.sub.3 SO.sub.2 ; R.sup.3 is hydrogen, methyl or methoxy; or R.sup.2 and R.sup.3 are together --S(O).sub.m (CH.sub.2).sub.4 --when S is attached at R.sup.2 or --(CH.sub.2).sub.n S(O).sub.m -- when S is attached at R.sup.3 (where m=1 or 2 and n=3 or 4); R.sup.4 is hydrogen or alkyl C.sub.1-4 ; Z is --(CH.sub.2).sub.2 -- or ##STR2## and their non-toxic salts. Processes for the preparation and pharmaceutical compositions thereof. The compounds exhibit both .beta.-adrenoreceptor antagonist activity and vasodilator activity and are indicated for use in the treatment of hypertension.
Propanolamine derivatives, their salts, processes for preparation and pharmaceutical compositions
申请人:RECKITT AND COLMAN PRODUCTS LIMITED
公开号:EP0043736A1
公开(公告)日:1982-01-13
Propanolamine derivatives of the formula:
wherein R2 is CH3SO or CH3S02; R3 is hydrogen, methyl or methoxy; or R2 and R3 are together -S(O)m(CH2)4- or -(CH2)nS(O)m- (where m = 1 or 2 and n = 3 or 4); R4 is hydrogen or alkyl C1-4; Z is -(CH2)2- or
and their non-toxic salts.
Processes for the preparation and pharmaceutical compositions thereof. The compounds exhibit both β-adrenoreceptor antagonist activity and vasodilator activity and are indicated for use in the treatment of hyperten- sion.
Aromachemical alkoxyalkyl sulfanyl compounds or a mixtures thereof having the formula:
R
1
O—C
6
H
5
OH—SR
wherein: R is a straight or branched chain, saturated or unsaturated hydrocarbyl group; preferably, alkyl or alkenyl, having 1-8 carbon atoms; and
R
1
is a straight or branched chain, saturated or unsaturated hydrocarbyl group; preferably, alkyl or alkenyl, having 1-8 carbon atoms and their use as aromachemicals and in articles of manufacture.
芳香族烷氧基烷基硫化合物或其混合物,具有以下式子
R
1
O-C
6
H
5
OH-SR
其中R 是直链或支链、饱和或不饱和的烃基,最好是具有 1-8 个碳原子的烷基或烯基;以及
R
1
是直链或支链、饱和或不饱和的烃基,最好是具有 1-8 个碳原子的烷基或烯基。