The present invention relates compounds of the formula (I): ##STR1##wherein X represents hydrogen or a C.sub.1-4 alkyl group optionally substituted by a hydroxy group; Y represents hydrogen, C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; Z is --CR.sup.9 R.sup.10 CH.sub.2 -- or --CH.sub.2 CR.sup.9 R.sup.10 --; R represents hydrogen, fluorine, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined herein.The compounds are of particular use in the treatment of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Merck Sharp &amp; Dohme Ltd.

Azabicyclic amine derivatives and their use as therapeutic agents

A problem of the present invention is to provide a new compound which has NK.sub.1 receptor antagonist activity, and thus is useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. A compound represented by the formula (I): ##STR00001## wherein W represents a fluorine atom and the like, ring A represents a cycloalkyl and the like, X.sup.1 represents CH or N, R represents methyl and the like, Y represents 0 to 2, U.sup.1, U.sup.2 and U.sup.3 each independently represents a single bond and the like, or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have an excellent NK.sub.1 receptor antagonist activity, and thus are also useful as an agent for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.

KISSEI PHARMACEUTICAL CO., LTD.

NK1 receptor antagonist

The present invention relates to compounds of the formula (I): ##STR1##wherein R.sup.1 is fluorine or trifluoromethyl; R.sup.2 is fluorine or trifluoromethyl; R.sup.3 is methyl or hydroxymethyl; R.sup.4 represents a variety of substituents; and n is zero, 1 or 2;and pharmaceutically acceptable salts thereof.The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Tetrahydropyran derivatives and their use as therapeutic agents

The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.10 are a variety of substituents defined in the specification; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, emesis and postherpetic neuralgia.

fluorine/wymioty

Azabicyclic amine derivatives and their use as therapeutic agents

NK1 receptor antagonist

Tetrahydropyran derivatives and their use as therapeutic agents

Spiro-piperidine derivatives and their use as tachykinin antagonists

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