James F Macdonald

US Patent:

6489322, Dec 3, 2002

Filed:

May 21, 1998

Appl. No.:

09/068945

Inventors:

James Macdonald - Rochester NY
James Matz - Rochester NY
William Shakespeare - Framingham MA

Assignee:

AstraZeneca AB - Sodertalje

International Classification:

A61K 3155

US Classification:

51421109, 540552

Abstract:

There are provided novel compounds of formula (I) wherein R represents a 2-thienyl or 3-thienyl ring and R represents hydrogen or C 1 to 4 alkyl and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are selective inhibitors of the neuronal isoform of nitric oxide synthase.

US Patent:

59290854, Jul 27, 1999

Filed:

Jan 22, 1997

Appl. No.:

8/776221

Inventors:

James MacDonald - Pittsford NY
James Matz - Fairport NY
William Shakespeare - Rochester NY

Assignee:

Astra Aktiebolag - Sodertalje

International Classification:

A61K 3147
C07D21722

US Classification:

514310

Abstract:

There are provided novel compounds of formula (I) ##STR1## wherein X, R. sup. 1, R. sup. 2, R. sup. 3, R. sup. 4 and R. sup. 5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.

US Patent:

60309857, Feb 29, 2000

Filed:

Jul 8, 1998

Appl. No.:

9/111926

Inventors:

Robert James Gentile - Scotsville NY
Robert John Murray - Brighton NY
James Edwin MacDonald - Pittsford NY
William Calvin Shakespeare - Rochester NY

Assignee:

Astra Aktiebolag - Sodertalje

International Classification:

A61K 3147
A61K 31445
A61K 3140
A61K 3138
A61K 31155

US Classification:

514307

Abstract:

The present invention relates to methods and compositions useful for treating and preventing conditions in which inhibition of nitric oxide synthetase is beneficial. These conditions include stroke, schizophrenia, anxiety, and pain.

US Patent:

58859853, Mar 23, 1999

Filed:

Sep 21, 1995

Appl. No.:

8/525663

Inventors:

James E. Macdonald - Pittsford NY
Robert Gentile - Scottsville NY
Robert J. Murray - Brighton NY

Assignee:

Astra Aktiebolag

International Classification:

C07D20504
C07D40114
C07D40314
A61K 3140

US Classification:

514217

Abstract:

Guanidine derivatives of formula I ##STR1## wherein R. sup. 8 represents hydrogen, halogen, alkyl C1 to 6, nitro, trifluoromethyl, thioalkyl C1 to 6, hydroxy, alkoxy C1 to 6, or a group selected from --NR. sup. 4 R. sup. 5, --O(CH. sub. 2). sub. p Q, --(CH. sub. 2). sub. m OQ, --(CH. sub. 2). sub. m NR. sup. 1 R. sup. 2, --O(CH. sub. 2). sub. m NR. sup. 1 R. sup. 2, --NHCO(CH. sub. 2). sub. m NH(CH. sub. 2). sub. n Q or --(CH. sub. 2). sub. p CONR. sup. 1 R. sup. 2, or R. sup. 8 represents the group A--CO--B; R. sup. 9 represents hydrogen, halogen, alkyl C1 to 6, nitro or trifluoromethyl; and R. sup. 1, R. sup. 2, R. sup. 4, R. sup. 5, n, m, p, Q, A, B, and W are as defined in the specification, are described together with processes for their manufacture and compositions containing them. Compounds of formula I are useful in therapy.

US Patent:

57863644, Jul 28, 1998

Filed:

Mar 8, 1996

Appl. No.:

8/615254

Inventors:

James MacDonald - Pittsford NY

Assignee:

Astra Aktiebolag - Sodertalje

International Classification:

C07D21702
C07C33502
A61K 3147
A61K 31155

US Classification:

514307

Abstract:

There are provided novel compounds of formula I ##STR1## wherein D represents alkyl C1 to 6; T represents a C. sub. 3-5 saturated or unsaturated alkylene chain substituted by --(CH. sub. 2). sub. m --NXY; --O--(CH. sub. 2). sub. 2 --NH-- substituted by --(CH. sub. 2). sub. m --NXY; or --U--(CH. sub. 2). sub. a --N(X)--(CH. sub. 2). sub. b --; and a, b, m, X and Y are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.

US Patent:

57212473, Feb 24, 1998

Filed:

Nov 14, 1995

Appl. No.:

8/535102

Inventors:

James Edwin Macdonald - Pittsford NY

Assignee:

Astra Aktiebolag - Sodertalje

International Classification:

C07C33532
C07D21706
A61K 31155
A61K 3147

US Classification:

514307

Abstract:

There are provided novel compounds of formula I ##STR1## wherein D, R. sup. 1, R. sup. 2, R. sup. 3, X and p are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.

US Patent:

58078860, Sep 15, 1998

Filed:

Nov 5, 1996

Appl. No.:

8/737286

Inventors:

James Edwin MacDonald - Pittsford NY
William Calvin Shakespeare - Rochester NY
Robert John Murray - Brighton NY
James Russell Matz - Fairport NY

Assignee:

Astra Aktiebolag - Sodertalje

International Classification:

A61K 3138
A61K 3134
A61K 3155
A61K 3147

US Classification:

514438

Abstract:

Compounds of the formula (I) ##STR1## wherein D represents a 5-membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O, N or S, optionally substituted at a carbon atom by halogen, trifluoromethyl, alkyl C1 to 6, nitro, cyano, and which is connected to the remainder of the compound of formula (I) through a carbon atom; A represents (N(X) or CH(--(CH. sub. 2). sub. m --NXY); U represents NH, O or CH. sub. 2 ; V represents (CH. sub. 2). sub. b ; a, b,m, X and Y are as defined in the specification, together with processes for their preparation and compositions containing them. Compounds of formula (I) are nitric oxide synthetase inhibitors and are useful in therapy.

US Patent:

5998399, Dec 7, 1999

Filed:

Nov 16, 1998

Appl. No.:

9/193333

Inventors:

James E. Macdonald - Pittsford NY
Robert Gentile - Scottsville NY
Robert J. Murray - Brighton NY

Assignee:

Astra Aktiebolag - Sodertalje

International Classification:

A61K 31445
C07D295215
C07D21706
C07D22322
C07D20504

US Classification:

514210

Abstract:

Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.