Debra Lou Allison

US Patent:

43806457, Apr 19, 1983

Filed:

Dec 11, 1981

Appl. No.:

6/329842

Inventors:

Bruce E. Witzel - Rahway NJ
Paul E. Finke - Metuchen NJ
Debra L. Allison - Scotch Plains NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D491044
C07D49504

US Classification:

548430

Abstract:

Improved yields of Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids have been achieved from processes based on modifications performed on a pyrrole carboxylic ester rather than on a pyrrole-. alpha. -oxoacetate.

US Patent:

49994360, Mar 12, 1991

Filed:

Aug 22, 1989

Appl. No.:

7/397325

Inventors:

Bruce E. Witzel - Westfield NJ
Debra L. Allison - Basking Ridge NJ
Charles G. Caldwell - Scotch Plains NJ
Kathleen Rupprecht - Cranford NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D33374

US Classification:

549 45

Abstract:

Aryl substituted thiophenes 3-ols, its dihydro derivatives, 1-oxide and 1,1-dioxide analogs, as well as aryl substituted furans, are 5-lipoxygenase inhibitors useful in the treatment of inflammation and other leukotriene-mediated diseases.

US Patent:

43749976, Feb 22, 1983

Filed:

Jun 4, 1981

Appl. No.:

6/270317

Inventors:

James B. Doherty - New Milford NJ
Debra L. Allison - Scotch Plains NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D207337
C07D20731

US Classification:

548539

Abstract:

Zomepirac and its analogs have been prepared from a 5-aroyl-3-hydroxycarbonyl-4-substituted pyrrole-2-acetic acid via acidic decarboxylation.

US Patent:

47600861, Jul 26, 1988

Filed:

Feb 27, 1985

Appl. No.:

6/705115

Inventors:

Allan N. Tischler - Westfield NJ
Bruce E. Witzel - Westfield NJ
Philippe L. Durette - New Providence NJ
Kathleen M. Rupprecht - Cranford NJ
Timothy F. Gallagher - Harleysville PA
Debra L. Allison - Scotch Plains NJ
Marvin M. Goldenberg - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3138
C07D33362

US Classification:

514443

Abstract:

N-Alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by: (1) treating a substituted 2-halobenzoate with thioacetamide followed by N-alkenylation with appropriate agents, such as aldehydes, ketones, enol ethers, epoxides, acetals or ketals; (2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide, followed by dehydration; and (3) further synthetic modification of compounds prepared above. These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases. Furthermore, these compounds have been found to exhibit cytoprotective activity which does not involve the inhibition of gastric acid secretion but can be used at relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants.

US Patent:

47205032, Jan 19, 1988

Filed:

Aug 2, 1985

Appl. No.:

6/761946

Inventors:

Bruce E. Witzel - Westfield NJ
Allan N. Tischler - Westfield NJ
Debra L. Allison - Scotch Plains NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3138
A61K 3134
C07D49502
C07D49300

US Classification:

514443

Abstract:

N-substituted fused-heterocyclic carboxamide derivatives, for example, N-(2,2-diphenylethenyl)-3-hydroxythieno[3,2-b]thiophene-2-carboxamide can be prepared by ring closure between an appropriately substituted halo-thiophene ester, e. g. , methyl 3-bromo-thiophene-2-carboxylate, and mercaptoacetamide followed by condensation with diphenylacetaldehyde. Alternatively, the ring closure can be carried out between an appropriately substituted mercaptothiophene ester, e. g. , methyl 3-mercaptothiophene-2-carboxylate and a haloacetamide to afford the fused-heterocyclic intermediate, 3-hydroxythieno[3,2-b]thiophene-2-carboxamide. N-alkenylation of the intermediate will then lead to the final products. These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, eye inflammation caused by glaucoma or other eye diseases, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, or other prostaglandin and/or leukotriene mediated diseases.

US Patent:

44407793, Apr 3, 1984

Filed:

Jun 4, 1982

Appl. No.:

6/385232

Inventors:

James B. Doherty - New Milford NJ
Conrad P. Dorn - Plainfield NJ
Bruce E. Witzel - Westfield NJ
Debra L. Allison - Scotch Plains NJ
Tsung-Ying Shen - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3155
C07D20994
C07D491044

US Classification:

424274

Abstract:

Tricyclic derivatives of substituted pyrrole acids, e. g. , substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.

US Patent:

50682482, Nov 26, 1991

Filed:

Jun 22, 1989

Appl. No.:

7/369982

Inventors:

Allan N. Tischler - Oakland CA
Philippe L. Durette - New Providence NJ
Bruce E. Witzel - Westfield NJ
Kathleen M. Rupprecht - Cranford NJ
Timothy F. Gallagher - Harleysville PA
Marvin M. Goldenberg - Westfield NJ
Debra L. Allison - Basking Ridge NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3138

US Classification:

514443

Abstract:

Method for increasing resistance to gastro-intestinal irritation, and for the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandin and/or leukotriene mediated diseases comprising the administration to a subject in need of such treatment, a non-toxic therapeutically effective amount of compound of formula I: ##STR1##.