Abbott Laboratories Corporation

Bruce W Horrom

Daniel A Dickman

Hormoz Mazdiyasni

Ronald R Rasmussen

Thomas John Perun

William Douglas Barta

Dee W Brooks

Rodger F Henry

Howard E Morton

Sanjay R Chemburkar

William R Baker

M Robert Leanna

Herman H Stein

Harold Elmer Zaugg

Karen E Rodriques

Stephen L Condon

Thomas M Zydowsky

Chi-nung W Hsiao

John J Kyncl

Wayne R Heitmann

Anthony Mannino

Frederick Nelson Minard

Brian A Roden

A process for the preparation of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride (terazosin hydrochloride dihydrate comprises the steps of reacting 4-amino-2-chloro-6,7-dimethoxy-quinazoline with N-(2-tetrahydrofuroyl)piperazine in an anhydrous polar organic solvent in the absence of an added acid scavenger to produce anhydrous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride (Form IV) and thereafter converting the product of that step to 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)-piperazine hydrochloride dihydrate.

Process and intermediate for the preparation of terazosin hydrochloride

Intermediates and a process for their preparation are disclosed which are useful for the preparation of a renin inhibiting compound of the formula: ##STR1## wherein R is a nitrogen-containing heterocycle which is bonded via a nitrogen atom to the sulfonyl group, R.sub.6 is hydrogen, alkoxy, halogen or loweralkyl, R.sub.7 is loweralkyl having 2 to 7 carbon atoms, and R.sub.8 is loweralkyl, cycloalkyl, or aryl or a pharmaceutically acceptable acid addition salt thereof.

Process for the preparation of a renin inhibiting compound

R(+)-2-[4-[(tetrahydro-2-furanyl)carbonyl]-1-piperazinyl]-6,7-dimethoxy-4-q uinazolinamine hydrochloride or a pharmaceutically acceptable salt or hydratet hereof (terazosin), substantially free of the S(-)-enantiomer.

R(+)-terazosin

A process for the production in high yield of 2-acetylbenzo[.beta.]thiophene and its alkyl and alkoxy substituted derivatives by converting a 2-halobenzaldehyde to a 2,2'-dithiobis(benzaldehyde) intermediate and reacting that intermediate successively with 2,4-pentanedione and chloroacetone in the presence of base.

Process for the production of 2-acetylbenzo [.beta.]thiophenes

Certain carbocyclic aryl- and heterocyclic aryl- substituted cyclopropyl N-hydroxyureas, N-hydroxy-carboxamides, and N-acyl-N-hydroxyamines inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.

Cyclopropyl derivative lipoxygenase inhibitors

Described are compounds of the formula ##STR1## wherein Y and Z independently of one another denote hydrogen, halo or trihalomethyl, with the proviso that Y and Z cannot both be hydrogen, R is hydrogen or loweralkyl, n is 5 to 19, and pharmaceutically acceptable salts thereof. The compounds are active hypocholesterolemic agents.

Aminobenzoic acid derivatives

This invention provides dibenzodiazepines represented by the formula ##STR1## The compounds of this invention are useful as antischizophrenics.

Dibenzodiazepines

N-vinyloxyethyl-.alpha.-methyl-.beta.-phenethylamines represented by the formula ##STR1## wherein R is H, halo or CF.sub.3 and acid addition salts thereof have been found to be useful as alcohol intake suppressing agents.

N-vinyloxyethyl-.alpha.-methyl-.beta.-phenethylamines as alcohol intake

A compound represented by the formula ##STR1## wherein R is H, loweralkyl, hydroxyloweralkyl or ##STR2## where R.sub.2 is an alkyl group of 1 to 15 carbon atoms; and R.sub.1 is H or ##STR3## where R.sub.2 is an alkyl group of 1 to 15 carbon atoms. These compounds are useful as antischizophrenics.

Dibenzo�b,e!�1,4!diazepines

This invention provides dibenzodiazepines represented by the formula ##STR1## wherein R is ##STR2## The compounds of this invention are useful as antischizophrenics.

This invention provides 2,4-diamino-5-benzylpyrimidines represented by the formula ##STR1## wherein R.sub.1 is H or loweralkyl; R.sub.2 is H, loweralkyl or R.sub.3 CO-- wherein R.sub.3 is H, alkyl, or cycloalkyl-lowerakyl; and X is a halogen; and the acid addition salts thereof. These pyrimidine compounds are useful as antibacterial agents, and as potentiators of the anti-bacterial activity of sulfonamides.

2,4-Diamino-5-benzylpyrimidines

This invention provides 2,4-diamino-5-benzylpyrimidines represented by the formula ##STR1## wherein R.sub.1 is H or loweralkyl; R.sub.2 is H, loweralkyl or R.sub.3 CO-- wherein R.sub.3 is H, alkyl, or cycloalkyl-loweralkyl; and X is a halogen; and the acid addition salts thereof. These pyrimidine compounds are useful as antibacterial agents, and as potentiators of the antibacterial activity of sulfonamides.

Novel N-vinyloxyethyl-.alpha.-methyl-.beta. -phenethylamines represented by the formula ##STR1## wherein R is H, halo or CF.sub.3 and acid addition salts thereof. The compounds are useful as appetite depressants.

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Waukegan, IL, United States of America

Bruce W Horrom