Richard H Conley

US Patent:

43283420, May 4, 1982

Filed:

Apr 24, 1981

Appl. No.:

6/257436

Inventors:

Richard A. Conley - Annandale NJ
Margaret M. Lam - New York NY
Leroy B. High - Cranbury NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07D21522

US Classification:

546153

Abstract:

A process is provided for preparing pyrazolo[1,5-c]quinazoline derivatives of the structure ##STR1## wherein X is O or S; R. sup. 1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R. sup. 2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R. sup. 3 and R. sup. 4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single mono-lower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure ##STR2## which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)pyrazole which is then cyclized to the product. In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.

US Patent:

42529450, Feb 24, 1981

Filed:

Jul 11, 1979

Appl. No.:

6/056660

Inventors:

Richard A. Conley - Annandale NJ
Margaret M. Lam - New York NY
LeRoy B. High - Cranbury NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07D48704

US Classification:

544250

Abstract:

A process is provided for preparing pyrazolo-[1,5-c]quinazoline derivatives of the structure ##STR1## wherein X is O or S; R. sup. 1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R. sup. 2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R. sup. 3 and R. sup. 4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single monolower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure ##STR2## which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)-pyrazole which is then cyclized to the product. In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.

US Patent:

47314800, Mar 15, 1988

Filed:

Jul 29, 1985

Appl. No.:

6/760003

Inventors:

Richard A. Conley - Annandale NJ
Donald L. Barton - Frenchtown NJ

Assignee:

Ortho Pharmaceutical Corporation - Raritan NJ

International Classification:

C07C10338

US Classification:

564223

Abstract:

A process for preparing 2-acyl-3,4-dialkoxyanilines is described. The 2-acyl-3,4-dialkoxyanilines are useful intermediates in the preparation of 5,6-dialkoxy-4-alkyl-2(1H)-quinazolinones. The substituted quinazolinones are active as cardiotonic agents.

US Patent:

46174176, Oct 14, 1986

Filed:

Jul 29, 1985

Appl. No.:

6/759975

Inventors:

Richard A. Conley - Annandale NJ
Donald L. Barton - Frenchtown NJ

Assignee:

Ortho Pharmaceutical Corporation - Raritan NJ

International Classification:

C07C125065

US Classification:

560 29

Abstract:

A process for the preparation of alkyl 2-carboxy-3,4-dialkoxybenzenecarbamates is described. The carbamates are useful intermediates in the preparation of 8-halo-5,6-dialkoxyquinazoline-2,4-diones. The diones are useful as cardiotonic agents.

US Patent:

48837873, Nov 28, 1989

Filed:

Jun 20, 1988

Appl. No.:

7/209130

Inventors:

Richard A. Conley - Annandale NJ
Donald L. Barton - Frenchtown NJ

Assignee:

Ortho Pharmaceutical Corporation - Raritan NJ

International Classification:

C07C10338

US Classification:

564414

Abstract:

A process for preparing 2-acyl-3,4-dialkoxyanilines is described. The 2-acyl-3,4-dialkoxyanilines are useful intermediates in the preparation of 5,6-dialkoxy-4-alkyl-2(1H)-quinazolinones. The substituted quinazolinones are active as cardiotonic agents.

US Patent:

46458360, Feb 24, 1987

Filed:

Sep 12, 1983

Appl. No.:

6/531138

Inventors:

Richard A. Conley - Annandale NJ

Assignee:

Ortho Pharmaceutical Corporation - Raritan NJ

International Classification:

C07D23980

US Classification:

544286

Abstract:

A process for the preparation of 6,7-dihydroxy-4-alkyl-2(1H) quinazolinone-1-propionic acids is described. The propionic acid compounds are renal vasodilators and thereby increase renal blood flow. They are useful as cardiovascular agents.

US Patent:

43037950, Dec 1, 1981

Filed:

Jul 23, 1980

Appl. No.:

6/171579

Inventors:

Richard A. Conley - Annandale NJ
Margaret M. Lam - New York NY
Leroy B. High - Cranbury NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07C101453

US Classification:

560 43

Abstract:

A process is provided for preparing pyrazolo-[1,5-c]quinazoline derivatives of the structure ##STR1## wherein X is O or S; R. sup. 1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R. sup. 2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R. sup. 3 and R. sup. 4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single mono-lower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure ##STR2## which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)-pyrazole which is then cyclized to the product. In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.

US Patent:

46580549, Apr 14, 1987

Filed:

Jul 29, 1985

Appl. No.:

6/759974

Inventors:

Richard A. Conley - Annandale NJ

Assignee:

Ortho Pharmaceutical Corporation - Raritan NJ

International Classification:

C07C10154

US Classification:

562453

Abstract:

A process for the preparation of 5,6-dialkoxyanthranilic acids is described. The 5,6-dialkoxyanthranilic acids are useful in the preparation of substituted quinazolinediones which are active cardiotonic agents.