Beecham Group Plc

Smithkline Beecham Corporation

Beecham Group P.l.c. of Beecham House

Robert William Ward

Roger Edward Markwell

Mervyn Thompson

Alexander C Goudie

David Glynn Smith

Ian Hughes

David Haigh

John Liddle

Jason Witherington

Stephen Garland

David J Hunter

Deidre Mary Bernadette Hickey

Robert John Ife

Michael S Hadley

John David Harling

David Kenneth Dean

Lee James Beeley

Stephen A Smith

John Michael Berge

Frank Peter Harrington

Nikesh R Kotecha

Antonio Kuok Keong Vong

Howard E Rosenberg

Alastair David Reith

Ashley Edward Fenwick

Matthew Paul Coghlan

Julie Caroline Holder

Carol R De Mello

Peter David Edwards

The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; Ris unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and Ris unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

Pyrazolopyridines and pyrazolopyridazines as antidiabetics

The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; Ris unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and Ris unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

This invention relates to substituted isoquinoline derivatives and their use as anticonvulsants.

Substituted isoquinoline derivatives and their use as anticonvulsants

Method and compounds

Compounds of formula (I) and pharmaceutically acceptable salts thereof, where G is a methylene or ethylene linkage; R is hydrogen, C alkylO&mdash;; R is hydrogen, halogen, CN, N , trifluoromethyldiazirinyl, CF , CF O&mdash;, CF S&mdash;, CF CO&mdash;, C alkyl, C cycloalkyl, C cycloalkyl-C alkyl-, C alkylO&mdash;, C alkylCO&mdash;, C cycloalkylCO&mdash;, C cycloalkyl-C -alkylCO&mdash;, phenyl, phenoxy, benzyloxy, benzoyl and substituted benzoyl, phenyl-C alkyl-, C alkylSO &mdash;, (C alkyl) NSO &mdash; or (C alkyl)NHSO &mdash;; R is hydrogen, halogen, CN, N , trifluoromethyldiazirinyl, C alkylO&mdash;, C alkylS&mdash;, C alkyl, C cycloalkyl, C cycloalkyl-C alkyl-, C alkenyl, C alkynyl, CF CO&mdash;, C alkylCO&mdash;, C cycloalkylCO&mdash;, C cycloalkyl-C alkylCO&mdash;, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C alkyl-, or &mdash;NR R where R is hydrogen or C alkyl; and R is hydrogen, C alkyl, &mdash;CHO, &mdash;CO C alkyl or &mdash;COC alkyl; R is hydrogen, C alkyl, C alkenyl, or C alkynyl, are useful in the prevention and treatment of anxiety, mania, depression disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines, disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy including post-traumatic epilepsy, Parkinson's disease, psychosis, migraine, etc.

Substituted benzamide derivatives and pharmaceutical compositions containing them

Compounds of formula (I) and pharmaceutically acceptable salts thereof:

1,6-naphthyridine anti-convulsants

A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein,

Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic

Novel compounds of formula (I) and salts, solvates and hydrates thereof, processes for their preparation and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R is hydrogen, C.sub.1-6 alkyl or optionally substituted benzyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2 is C.sub.3-6 alkyl; R.sub.3 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.3 is a group ##STR2## where R.sub.7 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl and R.sub.8 is hydrogen or alkyl; and R.sub.4 is --CH.sub.2 --(CH.sub.2).sub.n OR.sub.5 or --CH.sub.2 --(CH.sub.2).sub.n OCOR.sub.6 or --CH(R.sub.9)COR.sub.10, where n is an integer from 1 to 6; R.sub.5, R.sub.6 and R.sub.9 are hydrogen or C.sub.1-6 alkyl; and R.sub.10 is hydroxy or --O--C.sub.1-6 alkyl or --NR.sub.5 R.sub.6 (where R.sub.5 and R.sub.6 may be linked to form a heterocyclic ring; or R.sub.3 and R.sub.4 are joined together as --(CH.sub.2).sub.m -- where m is an integer from 4 to 12.

Compounds

Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen or alkyl; R.sub.3 is C.sub.3-6 alkyl; R.sub.4 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.4 is a group ##STR2## where R.sub.8 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.9 is hydrogen or alkyl; and R.sub.5 is hydrogen or alkyl.

Phosphorus containing peptides, pharmaceutical compositions and method

Compounds of the formula (I): ##STR1## wherein: X is NR wherein R is hydrogen, C.sub.1-6 alkyl; oxygen; sulphur; SO; or SO.sub.2 ; or R and R.sub.3 taken together are C.sub.4-6 polymethylene;

Pharmacologically useful pyrazolopyridines

A compound of the formula (I) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl; or together with R.sub.3 is C.sub.4-6 polymethylene;

Pharmaceutically useful pyrazolo[4,3-b]pyridines

A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;

Certain anti-inflammatory pyrazolo [4,3-b] pyridine 7-amines

Compounds of formula (I) ##STR1## wherein: R is hydrogen or C.sub.1-6 alkyl;

Certain 7-amino-pyrazolo[4,3-b]pyridines useful in treating inflammatory

A compound of formula (I) or a salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl;

Pyrazolopyridine derivatives useful in treating inflammation and

Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is NR wherein R is hydrogen or C.sub.1-6 alkyl, oxygen, sulphur, SO or SO.sub.2 ;

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Harlow, United Kingdom

Robert William Ward