[EN] FUSED TETRACYCLIC PYRIDO[4,3-B]INDOLE AND PYRIDO[3,4-B]INDOLE DERIVATIVES AND METHODS OF USE [FR] DÉRIVÉS DE PYRIDO[4,3-B]INDOLE ET PYRIDO[3,4-B]INDOLE TÉTRACYCLIQUE CONDENSÉS ET PROCÉDÉS D'UTILISATION
Pyrazol-1-ylphenylacetic acids of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and denote a hydrogen atom or a halogen atom, R.sup.4 denotes a hydrogen atom or an alkyl group, A B denotes a carbon-carbon single or double bond, and their salts are pharmacologically active and are useful as medicaments. Medicament compositions are produced therefrom. Their functional carboxylic acid derivatives and other new intermediates are used in their preparation.
Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A
1
, is hydrogen or methyl; ring Ar
1
is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA
1
CHO— and L2 are linked to adjacent ring atoms; rings Are
2
, Ar
3
each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.
Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis:
wherein A represents a carboxyl group —COOH, or a carboxyl bioisostere; A
1
is hydrogen or methyl; ring Ar
1
is an optionally substituted phenyl ring or 5- or 6-membered monocyclic heteroaryl ring, in which AA
1
CHO— and L2 are linked to adjacent ring atoms; rings Ar
2
, Ar
3
each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.
FUSED TETRACYCLIC PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE
申请人:Chakravarty Sarvajit
公开号:US20130210803A1
公开(公告)日:2013-08-15
This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.