American Cyanamid Company

American Cyanamid

Other

Wyeth Holdings Corporation

Middleton B Floyd, Jr

Martin J Weiss

Charles V Grudzinskas

Sow-Mei L Chen

Allan Wissner

Robert E Schaub

Vern G DeVries

John F Poletto

Karel F Bernady

Hwei-Ru Tsou

Semiramis Ayral-Kaloustian

Nan Zhang

Dan Maarten Berger

Philip Frost

Thomas H Claus

Philip R Hamann

Douglas Bruce Kitchen

Bernard D Johnson

Sow-Mei Lai Chen

Jo A Goidl

Mark E Salvati

Marvin Fred Reich

William J McGahren

Philip Ross Hamann

Charles V Gredeinskas

Sow-mei C Chen

This invention provides compounds of formula I having the structure wherein G, G, R, R, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

Substituted 3-cyanoquinolines

This invention provides compounds of formula I having the structure

This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;

Substituted 3-cyano quinolines

This invention provides a compound having the formula ##STR1## wherein: X is phenyl which is optionally substituted;

4-aminoquinazoline EGFR Inhibitors

Novel compounds are disclosed of the derivatives of furan having the formula ##STR1## wherein R.sub.4 consists essentially of hydrogen and C.sub.1 -C.sub.6 alkyl, and W is either carbonyl or carbinol and N is from 3-5.

Precursors and synthesis of D1-(methyl)-16,16-(dimethyl)-11-alpha,

Novel compounds are disclosed of the classes: ##STR1## wherein the subscript n is an integer from 3-5, inclusive, R.sub.1 is hydrogen or R.sub.2 ; R.sub.2 and R.sub.3 consist essentially of C.sub.1 -C.sub.6 alkyl and R.sub.2 may be the same as or different from R.sub.3, and wherein Aryl consists essentially of phenyl and phenyl substituted with halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, and trifluoromethyl;

Precursors and synthesis of

Phosphates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These phosphates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the phosphates are also disclosed.

Antidiabetic phosphates

Novel precursors for the synthesis of methyl-9-oxo-11.alpha.,16-dihydroxy-16-vinyl-5-cis-13-trans prostadienoates having the formulae ##STR1## wherein R.sub.1 is H or C.sub.1 -C.sub.4 alkyl; R.sub.2 is C.sub.1 -C.sub.4 alkyl, R.sub.3 is H, C.sub.1 -C.sub.4 trialkylsilyl or C.sub.1 -C.sub.6 alkyl; X.sub.1 is halogen, cyano, C.sub.1 -C.sub.4 alkoxycarbonyl, carboxy or tri (C.sub.1 -C.sub.4 alkoxy)methyl; n is 2-4 inclusive; and P.sub.1 is H or a blocking or protective group; congeners and racemic mixture of these compounds and processes of synthesizing them.

Precursors and synthesis of methyl-9-oxo-11.alpha.,

Phosphonates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These phosphonates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the phosphonates are also disclosed.

Antidiabetic phosphonates

Alpha-substituted phosphonates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These alpha-substituted phosphonates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the alpha-substituted phosphonates are also disclosed.

Antidiabetic alpha-substituted phosphonates

This disclosure describes novel 4-oxy-2-substituted-cyclopent-2-en-1-ones useful as intermediates for the preparation of homo and nor prostaglandins of the E.sub.2, E.sub.3 and F series.

Novel 2-substituted-3,4-epoxycyclopentan-1-ones,

This disclosure describes novel 15-deoxy-16-hydroxy-16-substituted prostanoic acids and congeners thereof having utility as bronchodilators as hypotensive agents, and as agents for the control of excessive gastric secretion.

15-deoxy-16-hydroxy-16-substituted prostanoic acids and congeners

A new process is disclosed for preparing 1-(methyl)-16,16-(dimethyl)-11-alpha-15-alpha-dihydroxy-9-oxo-2,13,trans, trans-prostadienoate, and congeners thereof, including racemic mixtures.

Precursors and synthesis of d1-(methyl)-16,16-(dimethyl)-11-alpha,

A method of treating diabetes mellitus using arylglyoxals which are known compounds.

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Suffern, NY, United States of America

Middleton B Floyd, Jr