Merck + Co., Inc.

Arthur F Wagner

Tsung-Ying Shen

Nathaniel Grier

Richard L Tolman

John J Baldwin

Malcolm MacCoss

Adolph M Pietruszkiewicz

Ralph F Hirschmann

John Hannah

Norman P Jensen

Frederick W Holly

Tsung-Ting Shen

Tsau-Yen Lin

Certain piperazinylpyrimidines have pronounced .beta.-adrenergic blocking properties and some of the compounds are particularly useful in the treatment of elevated intraocular pressure and glaucoma.

Piperazinylpyrimidines as .beta.-adrenergic receptor blockers

Novel hypoglycemic agents having the formula (I) are disclosed. ##STR1##

Piperazinylalkylpyrimidines as hypoglycemic agents

7,8-Dihydro-4-(1-piperazinyl)-6H-thiopyranopyrimidines have .beta.-adrenergic blocking properties and are thus useful in the treatment of cardiovascular ailments known to be amenable to .beta.-blocker therapy. Certain of the compounds are useful in the treatment of elevated intraocular pressure by topical ocular administration.

7,8-dihydro-4-(1-pierazinyl)-6H-thiopyrano-[3,2-d] pyrimidines as

A process for preparing 9-substituted guanine-containing acyclonucleosides comprising selective alkylation at the 9-position of the purine by utilizing a blocking group at the 6-position.

Regioselective synthesis of 9-substituted purine acyclonucleoside

Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising quaternized nitrogen atoms linked to each other through trimethylene groups. By the term 'linear backbone' is meant that the polymer has only acyclic groups, i.e. trimethylene, linking the nitrogen atoms in a single continuous chain; the polymer is free from 'branching' when it has no repeating monomer units extending from the polymer backbone; and it is free from 'cross-linking' when there is no joining of two linear backbones. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of dihydro-oxazine, reductive alkylation of the resulting polymer, followed by quaternization.

Poly-[(methylimino)trimethylene]

Process of preparing poly[{alkyl-(3-ammoniopropyl)iminio}trimethylene

Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising quaternized nitrogen atoms linked to each other through trimethylene groups. By the term 'linear backbone' is meant that the polymer has only acyclic groups, i. e. trimethylene, linking the nitrogen atoms in a single continuous chain; the polymer is free from 'branching' when it has no repeating monomer units extending from the polymer backbone; and it is free from 'cross-linking' when there is no joining of two linear backbones. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of dihydro-oxazine, reductive alkylation of the resulting polymer, followed by quaternization.

Bile acid sequestering composition containing

The invention disclosed herein relates to novel non-adhesive, free-flowing, pharmacologically acceptable compositions comprising ionene quaternary polymers effective as bile acid sequestrants, such as poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], adsorbed on a pulverulent, solid aggregate of large surface to mass ratio, such as fumed silicas and silica aerogels. It also relates to the novel process for preparing such adsorbate compositions which comprises forming a substantially, uniform suspension of the finely-divided solid aggregate in an aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], evaporatively removing the water from the suspension, and drying the adsorbate thus produced.

Non-adhesive ionene quaternary polymer compositions useful as bile acid

Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising either tertiary or quaternized nitrogen atoms linked to each other through ethylene groups. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of an oxazoline, hydrolysis or direct reduction, nitrogen substitution, and optional quaternization of the resulting polymer.

Poly-[(dialkyl and hydroxy-dialkyl-imino)ethylene halides] and process

Poly[{alkyl-(3-ammoniopropyl)iminio}trimethylene dihalides] and process

The invention disclosed herein relates to novel partially cross-linked, fully quaternized poly-[(methylimino)trimethylene] polymers wherein a minor proportion (1% to 20%) of the nitrogen atoms in adjacent poly-[(methylimino)trimethylene] linear chains are, by quaternization, joined through trimethylene or 2-hydroxy-trimethylene bridges, the non-cross-linked nitrogens in the said linear chains being fully quaternized with lower alkyl or trialkylammoniopropyl groupings; and to the novel process for preparing these partially cross-linked, fully quaternized polymers which comprises reacting poly-[(methylimino)trimethylene] with 0.01 to 0.2 equivalents of 1,3-dihalo-propane or 1,3-dihalo-2-hydroxypropane per equivalent of tertiary amine in said poly-[(methylimino)trimethylene], and subsequently reacting the resulting product with excess alkyl halide or 3-halopropyltrialkylammonium halide. These partially cross-linked fully quaternized poly-[(methylimino) trimethylene] polymers are useful as highly-efficient bile acid sequestrants.

Controlled partially cross-linked 3,3-ionenes

Novel linear, unbranched, non-cross-linked polymers particularly poly-[{methyl-(3-trimethylammoniopropyl)imino} trimethylene dihalide] are prepared by the polymerization of the novel monomer, 3-[N'-(3-halopropyl)-N'-methylamino]-N,N,N-trimethyl-l-propanaminium halide, or an acid addition salt thereof preferably in an oxygen excluded environment, e.g., under nitrogen or argon. The polymer, especially after modification of terminal groups, is an excellent oral anticholesterolemic.

3-[N'-(3-Halopropyl)-N-'-methylamino]-N,N,N-trimethyl-1-propanaminium

Novel derivatives of 3,6-bis(2-piperidinyl)-2,5-piperazinedione and processes for preparing the same. The new compounds exhibit activity in inhibiting the growth of tumors in mammals and birds, and in inhibiting the growth of certain microorganisms.

3,6-Bis(2-piperidinyl)-2,5-piperazinedione compounds

Hexa- and heptapeptides of formula W-[X-Pro-Phe-Phe-Y-Z].sub.n H prepared by standard synthetic peptide techniques are anti-inflammatory, anti-rheumatoid arthritic and anti-ulcer agents.

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Princeton, NJ, United States of America

Arthur F Wagner