David J Walsh

US Patent:

46705660, Jun 2, 1987

Filed:

Jan 19, 1984

Appl. No.:

6/572006

Inventors:

David A. Walsh - Richmond VA

Assignee:

A. H. Robins Company, Incorporated - Richmond VA

International Classification:

C07D20934

US Classification:

548485

Abstract:

This invention relates to novel compounds having the formula: ##STR1## wherein; R. sup. 1 is fluoro, chloro, bromo, lower-alkyl or nitro, R. sup. 2 is lower alkyl, lower alkoxy, fluoro, chloro, bromo, nitro or trifluoromethyl, and m and n are 0-2 with the proviso that when R. sup. 1 or R. sup. 2 are tertiary butyl or a sterically hindering lower alkyl radical, m and/or n are 1. These compounds are intermediates in the preparation of 2-aminobiphenylacetic acids, esters and metal salts thereof.

US Patent:

49607766, Oct 2, 1990

Filed:

Jan 28, 1987

Appl. No.:

7/007592

Inventors:

David A. Walsh - Richmond VA
Albert D. Cale - Mechanicsville VA

Assignee:

A. H. Robins Company, Inc. - Richmond VA

International Classification:

A61K 31495
A61K 31445
C07D40112
C07D40312

US Classification:

514252

Abstract:

Novel 4-aryl-N-[2-(dialkylamino and heterocyclicamino)alkyl]-1-piperazinecarboxamides of the formula: ##STR1## wherein B is oxygen or sulfur; Ar is selected from ##STR2## or 2, 3 or 4-pyridyl; X is selected from hydrogen, halogen, loweralkyl, loweralkoxy, amino, dimethylamino, nitro, trifluoromethyl, cyano, acetyl, acetylamino, aminocarbonyl, carboxy or loweralkylcarboxylic acid ester; Y is selected from hydrogen, halogen, loweralkyl, loweralkoxy, nitro, trifluoromethyl, cyano, acetylamino, aminocarbonyl, carboxy or loweralkyl carboxylic acid ester; Z is selected from hydrogen, loweralkyl or loweralkoxy; Q is selected from ##STR3## m is 1 to 3 inclusive; n is zero or 1; p is zero to 3 inclusive; R. sup. 1, R. sup. 2 and R. sup. 3 are loweralkyl and may be the same or different, or R. sup. 1 and R. sup. 2 taken together with the adjacent nitrogen atom may be form a heterocyclic residue; and the pharmaceutically acceptable salts thereof are disclosed.

US Patent:

42307180, Oct 28, 1980

Filed:

Jan 9, 1979

Appl. No.:

6/002150

Inventors:

David A. Walsh - Richmond VA
William J. Welstead - Richmond VA

Assignee:

A. H. Robins Company, Inc. - Richmond VA

International Classification:

C07D29502
C07D20900

US Classification:

424274

Abstract:

3,4-Epoxypyrrolidines substituted in the 1-position with alkyl, cycloalkyl and phenylalkyl are disclosed which have pharmaceutical application in cataract prevention in animals and as intermediates in preparation of trans-3-aryloxy-4-hydroxypyrrolidines. The epoxypyrrolidines are prepared by a novel route involving chlorination of pyrrolines in aqueous medium.

US Patent:

50632353, Nov 5, 1991

Filed:

Apr 30, 1990

Appl. No.:

7/516570

Inventors:

David A. Walsh - Richmond VA

Assignee:

A. H. Robins Company, Inc. - Richmond VA

International Classification:

A61K 31445
C07D21122

US Classification:

514317

Abstract:

Novel compounds of the formula: ##STR1## are disclosed wherein Ar and Ar. sup. 1 are phenyl, sustituted phenyl or pyridinyl, "alk" is a C. sub. 1 -C. sub. 12 straight or branched hydrocarbon chain, and R is H, loweralkylcarbonyl, arylcarbonyl, or aminocarbonyl where the amino is unsubstituted or substituted by one or two groups selected from loweralkyl or aryl. The compounds of this invention are useful in the treatment of allergic disorders.

US Patent:

48107131, Mar 7, 1989

Filed:

Dec 20, 1985

Appl. No.:

6/811799

Inventors:

John M. Yanni - Chesterfield VA
David A. Walsh - Richmond VA

Assignee:

A. H. Robins Company, Incorporated - Richmond VA

International Classification:

A61K 31445

US Classification:

514317

Abstract:

A method of treating allergy with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain novel compounds: ##STR1## wherein p is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, --CH. sub. 2 -- or ##STR2## n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the. alpha. carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one, 4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one or 1,4-benzodioxan-loweralkyl-2-yl, and the pharmaceutically acceptable salts thereof.

US Patent:

50575244, Oct 15, 1991

Filed:

Feb 8, 1990

Appl. No.:

7/476803

Inventors:

David A. Walsh - Richmond VA

Assignee:

A. H. Robins Company Incorporated - Richmond VA

International Classification:

A61K 31445
C07D21132

US Classification:

514317

Abstract:

Novel compounds useful in the treatment of allergic disorders and having the formula: ##STR1## where Ar and Ar. sup. 1 are pyridinyl, phenyl, or substituted phenyl and where Y is --OH,--O. sup. crclbar. M. sup. sym. m,--O--loweralkyl, --O--Aryl, or NR. sup. 1 R. sup. 2 (R. sup. 1, R. sup. 2. dbd. H, loweralkyl, aryl) are herein disclosed.

US Patent:

48554472, Aug 8, 1989

Filed:

Aug 8, 1988

Appl. No.:

7/229932

Inventors:

David A. Walsh - Richmond VA

Assignee:

A. H. Robins Company, Incorporated - Richmond VA

International Classification:

C07D20918

US Classification:

548494

Abstract:

2-Amino-3-aroyl-. gamma. -oxobenzenebutanoic acids and derivatives having the formula: ##STR1## wherein X is hydrogen, halogen, or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxyl, nitro, or trifluoromethyl; n is 1 or 2; and R is hydrogen lower-alkyl, or a pharmaceutically acceptable cation, are disclosed having anti-inflammatory activity.

US Patent:

48823309, Nov 21, 1989

Filed:

Apr 6, 1989

Appl. No.:

7/333673

Inventors:

David A. Walsh - Richmond VA
John M. Yanni - Chesterfield VA

Assignee:

A. H. Robins Company, Incorporated - Richmond VA

International Classification:

A61K 31495

US Classification:

514255

Abstract:

1-Aryloxy-4-[(4-aryl)-1-piperazinyl]-2-butanols of the formula: ##STR1## wherein Ar is selected fro ##STR2## or 2, 3 or 4-pyridyl); X and X' are selected from the group of hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, nitro, acetylamino, phenyl or ##STR3## acetyl, cyano, aminocarbonyl, carboxy, or loweralkyl carboxylic acid ester; Y, Y', Y" are selected from the same group as X and X' except phenyl and substituted phenyl are excluded; Z and Z' are selected from hydrogen, loweralkyl or loweralkoxy and the pharmaceutically acceptable salt thereof are employed in a method of inhibiting or combatting allergic response associated with anaphylactic sensitivity in animals and humans.