Lilly Industries, Inc.

Eli Lilly and Company

Eli Lilly Industries Limited

Delme Evans

Terence Alan Hicks

David William Dunwell

William J Ross

Michael Ralph Jolley

Brian Picton Swann

John Christopher Saunders

William R Williamson

Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 5-membered ring containing a single heteroatom, which may be oxygen, or sulphur, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.

Acylamino furan derivatives

Acylamino derivatives

Novel benzophenone derivatives having anti-allergy activity, and pharmaceutical formulations and methods of treatment utilizing benzophenone derivatives.

Benzophenone derivatives

Novel heteroaryl ketone derivatives, specifically a class of phenyl heteroaryl methanone derivatives, having anti-allergy activity, pharmaceutical formulations containing diphenylmethane derivatives and methods of treatment utilizing such derivatives.

Heteroaryl ketone derivatives

An aryl sulphur compound of formula (I) : ##STR1## where R.sup.1 is C.sub.1-4 alkyl; Ar is a phenyl group optionally substituted by halogen or C.sub.1-4 alkyl and wherein Z is S or SO, having antiallergy activity.

Aryl sulphur compounds as antiasthmatics

Benzoxazoles substituted in the 2-position with sulfhydryl or halogen and substituted in the 5- or 6-position with an acetic or propionic acid group or a salt or ester thereof or a nitrile convertible thereto useful as intermediates in the preparation of 5- or 6-Substituted benzoxazole propionic or acetic acid derivatives, substituted in the 2-position of the oxazole nucleus by a group of the formula AR.sup.4 wherein A is --CH.sub.2 --, --CO--, --CHOR--, or --NR--, wherein R is hydrogen, C.sub.1-6 alkyl or C.sub.2-7 acyl, and R.sup.4 is optionally substituted phenyl, useful as non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.

2,5 OR 2,6-Disubstituted benzoxazoles

Acylamino pyrrole compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.

5- or 6-Substituted benzoxazole propionic or acetic acid derivatives, substituted in the 2-position of the oxazole nucleus by a group of the formula AR.sup.4 wherein A is --CH.sub.2 --, --CO--, --CHOR--, or --NR--, wherein R is hydrogen, C.sub.1.sub.-6 alkyl or C.sub.2.sub.-7 acyl, and R.sup.4 is optionally substituted phenyl, useful as non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.

2,5 OR 2,6 Disubstituted benzoxazoles

2-(Optionally substituted)phenyl-benzoxazoles having a carboxy alkyl, a tetrazolyl, or oxazolinyl group at the 5 or 6 position useful as aspirin-like non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.

2-(Optionally substituted)phenyl-5 or 6-substituted benzoxazoles

The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclizing an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.

Cyanomethyl substituted benzoxazoles

The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclising an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.

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Chalfont St. Peter, United Kingdom

Delme Evans