Robert Martin Guthrie

US Patent:

44436190, Apr 17, 1984

Filed:

Aug 7, 1981

Appl. No.:

6/290989

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
Francis A. Mennona - Nutley NJ
Ann C. Sullivan - Cedar Grove NJ

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

C07D30102

US Classification:

549518

Abstract:

The present invention relates to chlorocitric acids of the formula ##STR1## and stereoisomers, optical antipodes and pharmaceutically acceptable salts thereof, to methods of preparation thereof, including intermediates involved therein, and to their use as anorectic agents for the treatment of obesity in mammals.

US Patent:

43128858, Jan 26, 1982

Filed:

Dec 26, 1978

Appl. No.:

5/973504

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
Francis A. Mennona - Nutley NJ
Ann C. Sullivan - Cedar Grove NJ

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

A61K 3119
C07C 59265

US Classification:

424317

Abstract:

The present invention relates to chlorocitric acids of the formula ##STR1## and stereoisomers, optical antipodes and pharmaceutically acceptable salts thereof, to methods of preparation thereof, including intermediates involved therein, and to their use as anorectic agents for the treatment of obesity in mammals.

US Patent:

47866462, Nov 22, 1988

Filed:

Jul 10, 1987

Appl. No.:

7/072390

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
Jefferson W. Tilley - North Caldwell NJ

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

A61K 3144
C07D41300

US Classification:

514346

Abstract:

The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH. sub. 2). sub. n --(X). sub. m --(CH. sub. 2). sub. r --, X is O, S or --CH. dbd. CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R. sub. 1 and R. sub. 2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH. sub. 2). sub. k -- wherein k is an integer from 0 to 4, R. sub. 3, R. sub. 4 and R. sub. 8 are independently hydrogen or lower alkyl, R. sub. 5 and R. sub. 6, independently are hydrogen or lower alkyl, R. sub. 7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and their enantiomers, diastereomers and racemic mixtures thereof, as well as when *E is ##STR3## their geometric isomers, and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.

US Patent:

49278380, May 22, 1990

Filed:

Jul 5, 1988

Appl. No.:

7/215464

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
John G. Mullin - Hawthorne NJ
Jefferson W. Tilley - North Caldwell NJ

Assignee:

Hoffman-La Roche Inc. - Nutley NJ

International Classification:

A61K 3144
C07D40912

US Classification:

514337

Abstract:

The invention relates to compounds of the formula ##STR1## wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH. sub. 2). sub. n --(X). sub. s --(CH. sub. 2). sub. r ----, X is O, S or --CH. dbd. CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R. sub. 1 and R. sub. 2, independently, are lower alkyl, lower alkenyl or aryl, or one of R. sub. 1 or R. sub. 2 is hydrogen and the other is ##STR2## wherein W is ##STR3## --CH. sub. 2 --CH. sub. 2 --, --CH. sub. 2 --, O, S, or ##STR4## and X. sub. 1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X. sub. 2, X. sub. 3 and X. sub. 4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R. sub. 3 is hydrogen, lower alkyl or aryl, R. sub.

US Patent:

45956898, Jun 17, 1986

Filed:

Feb 9, 1984

Appl. No.:

6/578726

Inventors:

Alfred Boris - Parsipanny NJ
Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ

Assignee:

Hoffmann-LaRoche Inc. - Nutley NJ

International Classification:

C07D40704

US Classification:

514337

Abstract:

A method of treating inflammation which comprises topically administering to the affected area a compound of the formula ##STR1## or a pharmaceutically acceptable addition salt thereof, is described.

US Patent:

49754386, Dec 4, 1990

Filed:

Sep 6, 1988

Appl. No.:

7/241174

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
Jefferson W. Tilley - North Caldwell NJ

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

A61K 3147
C07D21704

US Classification:

514307

Abstract:

Compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH. sub. 2). sub. n --(X). sub. m --(CH. sub. 2). sub. r --, X is O, S or --CH. dbd. CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R. sub. 1 and R. sub. 2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, Aryl, R. sub. 3, R. sub. 4 and R. sub. 8, independently, are hydrogen, lower alkyl, aryl, R. sub. 5 and R. sub. 6, independently, are hydrogen or lower alkyl, R. sub. 7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R. sub. 6 and R. sub. 7 are different, their enantiomers and racemic mixtures thereof, when R. sub. 1 and R. sub. 2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described.

US Patent:

43527582, Oct 5, 1982

Filed:

Aug 7, 1981

Appl. No.:

6/290988

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
Francis A. Mennona - Nutley NJ
Ann C. Sullivan - Cedar Grove NJ

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

C07D30312

US Classification:

549521

Abstract:

The present invention relates to chlorocitric acids of the formula ##STR1## and stereoisomers, optical antipodes and pharmaceutically acceptable salts thereof, to methods of preparation thereof, including intermediates involved therein, and to their use as anorectic agents for the treatment of obesity in mammals.

US Patent:

43407544, Jul 20, 1982

Filed:

Sep 21, 1981

Appl. No.:

6/304282

Inventors:

Robert W. Guthrie - Saddle Brook NJ
Richard W. Kierstead - North Caldwell NJ
Francis A. Mennona - Nutley NJ
Ann C. Sullivan - Cedar Grove NJ

Assignee:

Hoffmann-La Roche Inc. - Nutley NJ

International Classification:

C07C 59265
C07C 59125

US Classification:

562584

Abstract:

The present invention relates to chlorocitric acids of the formula ##STR1## and stereoisomers, optical antipodes and pharmaceutically acceptable salts thereof, to methods of preparation thereof, including intermediates involved therein, and to their use as anorectic agents for the treatment of obesity in mammals.