Glaxo Wellcome Inc.

Glaxo Inc.

Smithkline Beecham Corporation

Stephen V Frye

Kenneth William Batchelor

Michael Ross Johnson

James Marvin Veal

Francis Gerard Fang

Michael Luzzio

Karen Elizabeth Lackey

Philip Anthony Harris

David Middlemiss

Robert Anthony Mook

Stephen Thomas Davis

Scott Howard Dickerson

Lee Frederick Kuyper

Curt Dale Haffner

Patrick Reed Maloney

Robert Neil Hunter, Iii

Robert Carl Andrews

Duncan Herrick Walker

Marty C Johnson

George F Dorsey, Jr

Cynthia Markert Cribbs

Compounds of formula (I): wherein X is N, CH, CCF, or C(Caliphatic); Ris sulfonic acid, Caliphatic-sulfonyl, sulfonyl-Caliphatic, Caliphatic-sulfonyl-Caliphatic, Caliphatic-amino, R-sulfonyl, Rsulfonyl-Caliphatic, R-aminosulfonyl, R-aminosulfonyl-Caliphatic, R-sulfonylamino, R-sulfonylamino-Caliphatic, aminosulfonylamino, di-Caliphatic amino, di-Caliphatic aminocarbonyl, di-Caliphatic aminosulfonyl, di-Caliphatic amino, di-Caliphatic aminocarbonyl, di-Caliphatic aminosulfonyl-Caliphatic, (R)-Arylamino, (R)-Arylsulfonyl, (R)-Aryl-aminosulfonyl, (R)-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, Ris hydrogen; and further wherein Rand Rare optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

Substituted oxindole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors and compositions and methods of treating chemotherapy and radiation therapy side effects

Compounds of formula (I): wherein X is N, CH, CCF , or C(C aliphatic); R is sulfonic acid, C aliphatic-sulfonyl, sulfonyl-C aliphatic, C aliphatic-sulfonyl-C aliphatic, C aliphatic-amino, R -sulfonyl, R sulfonyl-C aliphatic, R -aminosulfonyl, R -aminosulfonyl-C aliphatic, R -sulfonylamino, R -sulfonylamino-C aliphatic, aminosulfonylamino, di-C aliphatic amino, di-C aliphatic aminocarbonyl, di-C aliphatic aminosulfonyl, di-C aliphatic amino, di-C aliphatic aminocarbonyl, di-C aliphatic aminosulfonyl-C aliphatic, (R ) -Arylamino, (R ) -Arylsulfonyl, (R ) -Aryl-aminosulfonyl, (R ) -Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R is hydrogen; and further wherein R and R are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

Substituted oxindole derivatives as protein tyrosine kinase and as protein serine/threonine kinase inhibitors

The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (B) wherein X, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases. ##STR1##

Androstenones

The present invention relates to methods for preparing and using compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) wherein X, W, Z, R.sup.4, and R.sup.5, are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.

The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.

Androstenone derivative

Substituted 6-azaandrostenones

Inhibitors of 5-.alpha.-testosterone reductase

There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.

17 .beta.acyl 6 azaandrost-4,6 diazo-4-ene-3-ones

The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are

Heterocyclic inhibitors of 5-.alpha.-testosterone reductase

Cobalt prophyrins of the following formula (l): ##STR1## or a salt or ligand complex thereof and their synthesis, pharmaceutical compositions and use in controlling obesity.

Cobalt porphyrins

Pharmaceutical compositions containing cobalt porphyrins of the following formula (I): ##STR1## wherein R.sup.1 =--CH.sub.2 CH.sub.2 CN and R.sup.2 =--CH.sub.2 CH.sub.2 COOH or R.sup.1 and R.sup.2 =--CH.sub.2 CH.sub.2 COOH or R.sup.1 =--H and R.sup.2 =--CH.sub.2 lCH.sub.2 COOH or a salt or ligand complex thereof and their use in controlling obesity.

Cobalt porphyrin pharmaceutical compositions

Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X.sup.1 and X.sup.2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic acid amide, with a halobenzene in the presence of an alkyllithium reagent.

Growing community of inventors

Durham, NC, United States of America

Stephen V Frye