Pennwalt Corporation

Fisons Ltd.

Astra Ab

Other

Astra Aktiebolag

Ronald C Griffith

James J Napier

Robert John Murray

Clyde R Kinsolving

Richard J Schmiesing

Michael Balestra

Edwin S Wu

Thomas A Davidson

John Charles Gordon

James Russell Matz

Donald Mathisen

Robert J Griffith

There are provided new compounds of formula I: ##STR1## wherein R represents hydrogen or methyl; and n represents 1 or 2; or a pharmaceutically acceptable acid addition salt thereof, together with processes for preparing them, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful in the treatment of psychotic disorders, intellectual impairment disorders and anxiety.

Spiro-azabicyclic compounds useful in therapy

Spiro-Azabicyclic Compounds useful in therapy

Compounds of formula (I) ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is hydrogen or C.sub.1-6 alkyl, R.sub.3 and R.sub.4 independently represent one or more radicals selected from hydrogen, NH.sub.2, NO.sub.2, halogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl, X represents S or --CH.dbd.CH-- group and pharmaceutically acceptable salts are NMDA receptor antagonists.

2-phenyl- and 2-thienyl-(2)-piperidine derivatives having

2-heterocyclicethylamine derivatives and their use as pharmaceuticals

There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano; R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl; R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ; R.sub.3 represents hydrogen or C1 to 6 alkyl; in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl; or a pharmaceutically acceptable salt thereof. Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.

Arylalkyl-amines having anticonvulsant and neuroprotective properties

Compounds of general formula I, ##STR1## wherein R.sup.1 represents hydrogen or alkyl C.sub.1-3, R.sup.2 represents hydrogen, alkyl C.sub.1-6, alkenyl C.sub.3-6 or alkynyl C.sub.3-6, n and m are integers from 1 to 3, provided that n+m=4, and one of X and Y represents CH.sub.2 and the other represents CHR.sup.3, C=CHR.sup.4 or C=NR.sup.5, in which R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16 and R.sup.17 are as defined in the specification, and their salts are useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptors. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome, and also as analgesic agents for use in the treatment of severe painful conditions such as rheumatism, arthritis, and terminal illness.

Spirofurane derivatives

There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;

Spiro[cycloalkylbenzene-1,1'-(1',2',3',4'-tetrahydro-isoquinolines)]

(S)-.alpha.-phenyl-2-pyridineethanamine, and its pharmaceutically acceptable derivatives, are useful in the treatment of neurodegenerative disorders, and exhibit linear pharmacokinetics.

Compounds for the treatment of neurodegenerative disorders

There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano; R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl; R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ; R.sub.3 represents hydrogen or C1 to 6 alkyl;

Arylalkyl-amines and -amides having anticonvulsant and neuroprotective

Compounds are provided of the following general structure: ##STR1## wherein B is hydrogen or lower alkyl (C.sub.1 -C.sub.4), R.sub.1 is hydrogen or methyl, R.sub.2 is lower alkyl (C.sub.1 -C.sub.4), phenylmethyl or 2-(aminocarbonyl)ethyl, R.sub.3 is H or lower alkyl (C.sub.1 -C.sub.4) and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

2-aminopropanamide derivatives

Compounds of the formula I, ##STR1## in which: R.sub.1 represents hydrogen or C.sub.1-6 alkyl,

(2-thienyl)alkylamine derivatives having neuroprotective properties

Compounds are provided of the following general structure: ##STR1## wherein R.sub.4 is lower alkyl (C.sub.1 -C.sub.4); R.sub.1 is hydrogen or methyl, R.sub.2 is hydrogen or methyl, R.sub.3 is lower alkyl (C.sub.1 -C.sub.6) or cyclopropyl, and where R.sub.5 and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

2-(alkylamino)acetamide derivatives

Compounds of general formula I, ##STR1## wherein R.sup.1 represents hydrogen or alkyl C.sub.1-3,

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Pittsford, NY, United States of America

Ronald C Griffith