摘要:
The invention relates to the use of selected (R)-2-[(halobenzyloxy)benzylamino]-propanamides and the pharmaceutically acceptable salts thereof for the manufacture of medicament, that are selectively active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, pain, migraine, periferal diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinological systems, gastrointestinal, urogenital, metabolic and seizure disorders, where the above mechanisms have been described as playing a pathological role.
摘要:
The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.
摘要:
3-aminopyrrolidone compounds and pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases.
摘要:
This invention is related to compounds and use of N-Acyl-N′-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role
摘要:
Methods of using certain a-aminoamide derivatives as anti-inflammatory agents. The anti-inflammatory agents of the invention are able to reduce or even stop inflammatory s conditions substantially without side effects.
摘要:
Use of kynurenine-3-hydroxylase inhibitors for the preparation of medicaments for the treatment of L-DOPA induced movement disorders, dyskinesias, drug addiction, pain and cataract.
摘要:
The present invention relates to novel N-(4-substituted-benzyl)-2-aminolactams as therapeutic agents, pharmaceutical compositions and a process of preparation.
摘要:
Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.
摘要:
The invention provides new imidazole containing alkoxyimino derivatives of tetrahydronaphthalene and chroman of general formula (I) ##STR1## wherein Z is --CH.sub.2 --or--O--;m is an integer of 1 to 4;n is zero of 1;T is a straight or branched saturated C.sub.1 -C.sub.6 hydrocarbon chain or C.sub.2 -C.sub.5 alkenylene chain;A is a bond or a divalent group consisting of --Si(R'R")--; --O--CH.sub.2 --,--CF.sub.2 --,C(R'R")--,vinylene or isopropenylene, wherein each of R' and R" being the same or different is hydrogen or C.sub.1 -C.sub.4 alkyl;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, being the same, are hydrogen or methyl, or one of R.sub.1 and R.sub.2 is hydrogen and the other isa) a C.sub.1 -C.sub.8 alkyl group;b) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl group, wherein the cycloalkyl group or moiety is unsubstituted or substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl groups; orc) an aryl or aryl-C.sub.1 -C.sub.4 alkyl group, wherein the aryl group or the aryl moiety is unsubstituted or substituted by 1 to 4 substituents independently chosen from halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio and C.sub.1 -C.sub.4 alkylsulfonyl;R.sub.3 is hydrogen or a substituent chosen from halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio and C.sub.1 -C.sub.4 alkylsulfonyl;R.sub.4 is an --OR.sub.5 or --N(R.sub.5 R.sub.6) group, wherein each of R.sub.5 and R.sub.6 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl;and the pharmaceutically acceptable salts thereof, which are useful in the treatment of a disease state in which an enhancement of TxA.sub.2 synthesis exerts a pathogenic effect.
摘要:
The present invention relates to new N-imidazolyl and N-imidazolylmethyl derivatives of bicyclic compounds having the general formula (I) ##STR1## Wherein A is a .gtoreq.CR.sub.3 or >CHR.sub.3 group, in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a >C.dbd.CR.sub.4 R.sub.5 group, in which each of R.sub.4 and R.sub.5 independently is hydrogen or C.sub.1 -C.sub.5 alkyl;Z is --CH.sub.2 --, --O-- or --S--;n is zero or 1;each of R and R.sub.1 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is --COCH.sub.2 OH, --CH.sub.2 OR', --COOR', --CONR'R" or --CH.dbd.CH--COOR', in which each of R' and R" independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof; and wherein:a) when n is zero, then Z is --CH.sub.2 -- or --O--; whereas when n is one, then Z is --CH.sub.2 --, --O-- or --S--;b) when A is .gtoreq.CR.sub.3 or >CHR.sub.3 in which R.sub.3 is hydrogen, then n is one; andc) when, at the same time, A is >CHR.sub.3 in which R.sub.3 is hydrogen, Z is --CH.sub.2 --, n is one and R.sub.2 is --COOR' wherein R' is as defined above, then at least one of R and R.sub.1 is other than hydrogen,which are useful in the treatment of diseases related to an enhancement of TxA.sub.2 synthesis.