Eli Lilly and Company

Lilly Industries, Inc.

William M Owton

Peter Thaddeus Gallagher

Colin W Smith

Colin P Dell

Michael Brunavs

Martin Victor Miles

Terence Alan Hicks

Andrew Caerwyn Williams

John Fairhurst

Jai P Singh

Dustin James Mergott

Jeremy Gilmore

Fionna Mitchell Martin

David R Dobson

The present invention provides compounds of Formula I useful as BACE inhibitors in the treatment of e.g. Alzheimer's disease: wherein A is selected from the group consisting of; of; Ris H or F; Ris H, &#x2014;OCH, C1-C3 alkyl; Ris H, &#x2014;CH, or &#x2014;OCH; and Ris H or F; or a pharmaceutically acceptable salt thereof. 

BACE inhibitors

Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, &gt;C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R'N--SO.sub.2 --, --COOR', --CONR'R', --NR'R', --N(OR')COOR', --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl, R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl, X is oxygen or sulphur, the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.

Indole compounds

A pharmaceutical compound of the formula ##STR1## in which X is --CR'R'-- or --C(O)-- where R' and R' are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, Y is oxygen or sulphur, R.sup.1, R.sup.2 and R.sup.7 are each selected from halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, nitro, cyano, amino, phenyl, phenoxy, benzyl, benzyloxy, acylamino, C.sub.1-4 alkylsulphonylamino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, carboxamido, sulphonamido, hydroxy, methylenedioxy, carboxy, and heteroaryl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, n, m and p are each 0, 1, 2 or 3; or a salt or ester thereof.

5HT receptor binding benzimidazolylpiperidines

A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--; or a salt, amide or ester thereof.

Pharmaceutical compounds

A pharmaceutical compound of the formula ##STR1## and salts and esters thereof.

A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--; or a salt, amide or ester thereof, useful in the treatment of skeletal diseases.

Anthraquinone pharmaceutical compounds and uses therefor

Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;

Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1 -4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an alkyl group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;

5,6-dihydronaphtho [1,2-b]pyrans and their use as pharmaceutical

This invention provides novel, optionally substituted tetrahydropyridoindoles which are useful serotonergic agents for the treatment of central nervous system disorders.

Serotonerbic tetrahydropyridoindoles

Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.3 are each C.sub.1-4 alkyl or C.sub.1-4 alkyl-carbonyl, and R.sup.2 is carboxy, tetrazolyl, C.sub.1-4 alkyl-sulphonamido or --CR.sup.4 R.sup.5 CO.sub.2 H where R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl; provided that when R.sup.1 and R.sup.3 are both methyl and when R.sup.1 and R.sup.3 are both methylcarbonyl, R.sup.2 is not carboxy; and salts and esters thereof.

Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkoxy;

Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.

Methods of using dihydropyrans

This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are variables.

Growing community of inventors

Lightwater, United Kingdom

William M Owton