Warner-lambert Company

Schering Corporation

Merck Sharp + Dohme Corp.

Warner Lambert LLC

Neil A Lindo

Harold Zinnes

Bernard R Neustadt

William J Greenlee

Samuel Chackalamannil

Yan Xia

Craig D Boyle

Deen Tulshian

John Shavel, Jr

Lisa S Silverman

Dhiru B Vashi

Jeffrey N Clark

Brian Alexander Mc Kittrick

Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein

Adenosine Areceptor antagonists

Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or &#x2014;C(O)CH&#x2014;; Y is &#x2014;N(R)CHCHN(R)&#x2014;, &#x2014;OCHCHN(R)&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;CHS&#x2014;, &#x2014;(CH)&#x2014;NH&#x2014;, or optionally substituted m and n are 2&#x2013;3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R&#x2014;C(O)&#x2014;, R&#x2014;SO&#x2014;, R&#x2014;OC(O)&#x2014;, R&#x2014;N(R)&#x2014;C(O)&#x2014;, R&#x2014;N(R)&#x2014;C(S)&#x2014;, phenyl-CH(OH)&#x2014;, or phenyl-C(&#x2550;NOR)&#x2014;; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R, R, R, R, and Rare as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.

Adenosine A2a receptor antagonists

Compounds having the structural formula Ior a pharmaceutically acceptable salt thereof, wherein

Polycyclic guanine derivatives

This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.

Organic acid-substituted guanidine anthelmintics

N-((2-nitro)phenyl)-N' (organic acid) guanidine anthelmintics

3,3'-Thiodimethylenebis 2-[(dialkylamino)methyl]indole compounds having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups. The compounds of this invention exhibit antifungal and CNS depressant properties and can be used as antifungal agents or CNS depressant agents.

Bis 2-[(dialkylamino)methyl]indoles

.beta.-[2-[(DIALKYLAMINO)METHYL]-1H-indol-3-yl]-.alpha.,.alpha.-diphenylpro pionitriles and 4-[[2-[(dialkylamino)methyl]-1H-indol-3-yl]methyl]-2,4-dihydro-5-lower alkyl-2-phenyl-3H-pyrazol-3-ones and acid addition salts thereof which are useful pharmacological agents, especially as central nervous system depressants, are disclosed. The compounds can be produced by reacting an anion of an acetonitrile or a pyrazol-3-one with the appropriate quatenary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.

3-(3H-Pyrazol-3-one)-2-(disubstituted aminomethyl)indoles and

N,N-dialkyl-3-[(phenylthio)methyl]-1H-indole-2-methanamines or 3-(1H-imidazol-1-ylmethyl)-N,N,-dimethyl-1H-indole-2-methanamines and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a thiophenols or imidazoles with the appropriate 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.

3-(1H-imidazol-1-ylmethyl)-2-(disubstitutedaminomethyl)indoles and a

Bis(2-[(disubstitutedamino)methyl]-1H-indole) compounds wherein said 2-[(disubstitutedamino)methyl]-1H-indol-3-ylmethylene moieties are linked together through a piperazine or 1,3-dihydro-2H-indol-2-one fragment and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a piperazine or 1,3-dihydro-2H-indole-2-one compound with the appropriate quaternary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo-[3,4-b]indole.

Bis(2-[(disubstituted amino)methyl]-1H-indole) compounds

A novel process for preparing 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides is disclosed. The process involves the base catalyzed rearrangement of a saccharinacetamide of structure I to give II, ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, aryl or a heterocyclic ring selected from the group consisting of pyridyl, substituted-pyridyl, and thiazolyl. Compounds of the formula II have useful anti-inflammatory properties. In addition, they can be used as intermediates in the preparation of known anti-inflammatory agents.

2-[(N-2-pyridylcarbamoyl)methyl]saccharin

A novel process for preparing 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides is disclosed. The process involves the base catalyzed rearrangement of a saccharinacetamide of structure I to give II, ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, aryl or a heterocyclic ring selected from the group consisting of pyridyl, substituted-pyridyl, and thiazolyl. Compounds of the formula II have useful anti-inflammatory properties. In addition, they can be used as intermediate in the preparation of known anti-inflammatory agents.

Process for the preparation of

Processes for the production of the compounds of the formula: ##STR1## are disclosed. In the above formula, R.sub.1 is aryl which may be substituted or unsubstituted; R.sub.2 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like. These compounds are prepared by the following reaction schemes: ##STR2## These compounds are useful as anti-inflammatory agents.

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New Providence, NJ, United States of America

Neil A Lindo