Charles A Nichol

US Patent:

47014555, Oct 20, 1987

Filed:

Jun 21, 1985

Appl. No.:

6/747671

Inventors:

Charles A. Nichol - Durham NC
John F. Reinhard - Durham NC
Gary K. Smith - Raleigh NC
Eric C. Bigham - Chapel Hill NC

Assignee:

Burroughs Wellcome Co. - Research Triangle Park NC

International Classification:

A61K 31505
C07D47504

US Classification:

514249

Abstract:

This invention provides the pterin compounds of formula (I) and use in human and veterinary medicine. ##STR1## wherein R represents lower alkyl groups (straight or branched) of 1-8 carbons (for this formula and all other formulas herein) including all stereo isomers thereof or a pharmaceutically acceptable salt thereof.

US Patent:

46651829, May 12, 1987

Filed:

Nov 19, 1985

Appl. No.:

6/799285

Inventors:

Charles A. Nichol - Durham NC
John F. Reinhard - Durham NC
Gary K. Smith - Raleigh NC
Eric C. Bigham - Chapel Hill NC

Assignee:

Burroughs Wellcome Co. - Rearch Triangle Park NC

International Classification:

C07D47504
A61K 31505

US Classification:

544258

Abstract:

The compounds of formula (I) ##STR1## wherein R. sup. 1 is hydrogen, lower alkyl of 1-4 carbons, lower alkenyl of 2-4 carbons, --B--X--R. sup. 5). sub. n, or --B--Z--B--X--R. sup. 5 --. sub. n ; n=0 when X is halogen or n=1 when X is --O--, --NR. sup. 6 -- (where R. sup. 6 is hydrogen or lower alkyl of 1-4 carbons) or --S(O)q-- (where q=0 to 2); B is lower alkanyl (straight or branched) of 1-5 carbons; R. sup. 5 is hydrogen, aralkyl of 7 to 12 carbons or alkyl of 1-10 carbons; Z is --O--, NR. sup. 6 --, or --S(O)q--; R. sup. 2 is hydrogen or lower alkyl of 1-4 carbons or lower alkenyl of 2-4 carbons or either R. sup. 1 and R. sup. 2 together with the carbon atom in the pteridine ring structures to which they are attached, form a spirocycloalkyl ring system having 3 to 7 carbon atoms; R. sup. 3 and R. sup. 4 are hydrogen or methyl; R. sup. 2 and R. sup. 3, together with the carbon atoms in the pteridine ring structure to which they are attached, form a cycloalkyl ring system having 5 to 7 carbon atoms; provided that at least one of R. sup. 1, R. sup. 2, R. sup. 3 and R. sup.

US Patent:

40052036, Jan 25, 1977

Filed:

Feb 12, 1975

Appl. No.:

5/549454

Inventors:

Dwight R. Stickney - Durham NC
William S. Simmons - Durham NC
Charles A. Nichol - Durham NC
George H. Hitchings - Durham NC
Gertrude B. Elion - Chapel Hill NC

Assignee:

Burroughs Wellcome Co. - Research Triangle Park NC

International Classification:

A61K 31505

US Classification:

424251

Abstract:

Method and pharmaceutical preparations for treating meningeal leukemia, CNS Iymphoma and neoplasma in the brain which comprises treating an infected mammal such as a human with a dose of an effective treatment amount of a compound of Formula I ##STR1## where R is a straight or branched chain lower alkyl of 1 to 4 carbon atoms, and X is a halogen atom (fluorine, chlorine, bromine or iodine) and pharmaceutically acceptable salts thereof. Preferred compounds for treatment of the aforementioned diseases are 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine and 2,4-diamino-5-(3',4'-dichlorophenyl)-6-ethylpyrimidine.

US Patent:

40062350, Feb 1, 1977

Filed:

Feb 12, 1975

Appl. No.:

5/549452

Inventors:

Dwight R. Stickney - Durham NC
William S. Simmons - Durham NC
Charles A. Nichol - Durham NC
George H. Hitchings - Durham NC
Gertrude B. Elion - Chapel Hill NC

Assignee:

Burroughs Wellcome Co. - Research Triangle Park NC

International Classification:

A61K 31505

US Classification:

424251

Abstract:

Method and pharmaceutical preparations for treating meningeal leukemia, CNS lymphoma and neoplasms in the brain which comprises treating an infected mammal such as a human with a dose of an effective treatment amount of a compound of Formula I ##STR1## where R is a straight or branched chain lower alkyl of 1 to 4 carbon atoms, and X is a halogen atom (fluorine, chlorine, bromine or iodine) and pharmaceutically acceptable salts thereof. Preferred compounds for treatment of the aforementioned diseases are 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methyl-pyrimidine and 2,4-diamino-5-(3',4'-dichlorophenyl)-6-ethyl-pyrimidine.

US Patent:

45873402, May 6, 1986

Filed:

Jun 13, 1984

Appl. No.:

6/620152

Inventors:

Charles A. Nichol - Durham NC
John F. Reinhard - Durham NC
Gary K. Smith - Raleigh NC
Eric C. Bigham - Chapel Hill NC

Assignee:

Burroughs Wellcome Co. - Research Triangle Park NC

International Classification:

C07D47504
A61K 31505

US Classification:

544258

Abstract:

This invention provides the intermediates of formula II-A below, useful to make the pterin compounds of formula I below. The pterin compounds are used in human and veterinary medicine. ##STR1## wherein R represents a lower alkyl of 1 to 8 carbons.

US Patent:

43729576, Feb 8, 1983

Filed:

Jan 23, 1981

Appl. No.:

6/228164

Inventors:

David S. Duch - Cary NC
Charles A. Nichol - Durham NC
Carl W. Sigel - Raleigh NC

Assignee:

Burroughs Wellcome Co. - Research Triangle Park NC

International Classification:

A61K 31505

US Classification:

424251

Abstract:

Potent psoriasis activity in combination with low inhibition of histamine N-methyltransferase has been found in a class of 2,4-diamino-6-(2,5-dialkoxybenzyl)-5-methylpyrido[2,3-d]pyrimidines.

US Patent:

40052044, Jan 25, 1977

Filed:

Feb 12, 1975

Appl. No.:

5/549453

Inventors:

Dwight R. Stickney - Durham NC
William S. Simmons - Durham NC
Charles A. Nichol - Durham NC
George H. Hitchings - Durham NC
Gertrude B. Elion - Chapel Hill NC

Assignee:

Burroughs Wellcome Co. - Triangle Park NC

International Classification:

A61K 31505

US Classification:

424251

Abstract:

Method and pharmaceutical preparations for treating meningeal leukemia, CNS Iymphoma and neoplasms in the brain which comprises treating an infected mammal such as a human with a dose of an effective treatment amount of a compound of Formula I ##STR1## where R is a straight or branched chain lower alkyl of 1 to 4 carbon atoms, and X is a halogen atom (fluorine, chlorine, bromine or iodine) and pharmaceutically acceptable salts thereof. Preferred compounds for treatment of the aforementioned diseases are 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine and 2,4-diamino-5-(3',4'-dichlorophenyl)-6-ethylpyrimidine.

US Patent:

45129924, Apr 23, 1985

Filed:

Feb 6, 1981

Appl. No.:

6/231977

Inventors:

David S. Duch - Gary NC
Charles A. Nichol - Durham NC
Carl W. Sigel - Raleigh NC

Assignee:

Burroughs Wellcome Co. - NC

International Classification:

A61K 31505

US Classification:

514258

Abstract:

This application is directed to treatment of psoriasis with a pyrido pyrimidine compound such as 2,4-diamino-6-(3,4-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidine.