Rhone Poulenc Rorer

Rhone-poulenc Sante

Bernard Yvon Vacher

Andrew David Morley

Garry Fenton

Malcolm Norman Palfreyman

Andrew James Ratcliffe

Terance W Hart

Brian William Sharp

Sukanthini Thurairatnam

Michael John Ashton

Brian W Sharp

Nigel Vicker

Ian Michael McFarlane

David Charles Cook

Susan Jacqueline Hills

Keith Alfred Stuttle

Roger J Walsh

Michael Thomas Withnall

Sven Jan-Anders Karlsson

This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic-

Compounds containing phenyl linked to aryl or heteroaryl by an

Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- o

Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.

Antiinflammatory, immunosuppressive and antialleric 16,

Thioformamide derivatives

A thioformamide derivative of the formula: ##STR1## wherein R represents alkyl, A represents optionally substituted pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]pyridin-6-yl, or phenyl and Y represents a valency bond, methylene or ethylene, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aryloxyalkyl, aromatic heterocyclylalkyl or aromatic heterocyclyloxyalkyl group or a group ZC(.dbd.O)-- in which Z represents optionally substituted alkyl, aryl, or aromatic heterocyclic, n represents 0 or 1, and when n represents 0, R.sup.1 may represent a hydrogen atom, optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aryloxyalkyl, aromatic heterocyclylalkyl or aromatic heterocyclyloxyalkyl group or a group ZC(.dbd.O)-- or ZSO.sub.2 --, and when n represents 1, R.sup.1 represents optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl radical and pharmaceutically acceptable salts thereof possess pharmacological properties.

Thioformamide derivative, process for its preparation, pharmaceutical

Thioformamide derivatives of the formula (I) ##STR1## wherein R represents an alkyl group; A represents either:

This invention relates to a thioformamide derivative of the formula I ##STR1## wherein: R and R.sup.1 each independently represent an alkyl group;

Pyrid-3-yl thioformamide compounds which have useful pharmaceutical

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Dagenham, United Kingdom

Bernard Yvon Vacher