Abstract: A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

Abstract: There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of ?-lactamase inhibitors.

Abstract: A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

Abstract: A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

Abstract: A process for making an N1-(2?-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R? wherein R and R? are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.

Abstract: A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R′ wherein R and R′ are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.

Abstract: This invention provides compounds of formula VI wherein Y is hydrogen, methyl, methoxy, methylthio or trifluoromethyl; R is hydrogen, C1-3alkyl or (CH2)nAr; n is 0, 1 or 2; and Ar is phenyl or methoxyphenyl, or a pharmaceutically acceptable salt thereof. These compounds are selective dopamine autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems. The invention also comprises intermediate compounds, compositions and methods related to the compounds of formula VI.

Abstract: A process for formation of N-aryl piperazines with chiral N′-1-[benzoyl(2-pyridyl)amino]-2-propane side-chains having the structure shown in formula below, and for making intermediate compounds therefor. In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N,N′ disubstituted piperazines act on the central nervous system at 5HT receptors.

Abstract: A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: 1

Abstract: A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R′ 1

Abstract: A process for formation of N-aryl piperazines with chiral N′-1-[benzoyl(2-pyridyl)amino]-2-propane side-chains having the structure shown in formula below, and for making intermediate compounds therefor.

Abstract: This invention provides compounds of formula VI 1

Abstract: This invention provides estrogens and antiestrogens of formula I having the structure wherein X, Y, Z, and R are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: This invention is concerned with a new and improved process for the large scale production of 4-?6-(hexylcarbamoyloxy)hexylcarbainoyloxy!-piperidine-1-carboxylic acid 4-phenoxyphenyl ester, disclosed in European Patent Application 0 635 501 A1, published Jan. 25, 1995, a compound that inhibits cholesterol ester hydrolase (CEH) and acylcoenzyme A cholesterol acyltransferase (ACAT). In the invention process, 1-benzyl-4-hydroxypiperidine or 1-methyl-4-hydroxypiperidine is reacted with a carbonylating reagent such as carbonyldiimidazole (CDI) and 6-aminohexanol forming the intermediate 1-benzyl (or methyl)-4-(6-hydroxyhexylcarbamoyloxy)piperidine. Reaction of this intermediate with CDI and hexylamine gives the corresponding 1-benzyl (or methyl)-4-?6-(hexylcarbamoyloxy)-hexylcarbamoyloxy!piperidine. The N-benzyl or methyl group is concomitantly removed and replaced with the 4-phenoxyphenyloxycarbonyl group using 4-phenoxyphenyl chloroformate.

Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.

Abstract: Disclosed herein are 1- or 2-thio, thiomethylene, and sulfonylnaphthalene derivatives of formulas I and II ##STR1## or a pharmaceutically acceptable cationic salt thereof, wherein n is 0 or 1R.sub.5 is hydrogen, bromo, chloro, trifluoromethyl or difluoroethyl;R.sub.6 is hydrogen, hydroxy, methoxy or ethoxy; andR.sub.7 is hydrogen or R.sub.7 and R.sub.6 are both methyl or ethyl carbonate,provided that, when S(O).sub.2 is in the 2 position of the naphthalene ring, R.sub.5, R.sub.6 and R.sub.7 are each hydrogen. The disclosed compounds possess blood-glucose lowering actions and are useful in the treatment of diabetes mellitus.

Abstract: Disclosed herein are 1- or 2-thio, thiomethylene, and sulfonylnaphthalene derivatives of formulas I and II ##STR1## or a pharmaceutically acceptable catonic salt thereof, wherein n is 0 or 1R.sub.5 is hydrogen, bromo, chloro, trifluoromethyl or difluoroethyl;R.sub.6 is hydrogen, hydroxy, methoxy or ethoxy; andR.sub.7 is hydrogen or R.sub.7 and R.sub.6 are both methyl or ethyl carbonate,provided that, when S(O).sub.2 is in the 2 position of the naphthalene ring, R.sub.5, R.sub.6 and R.sub.7 are each hydrogen. The disclosed compounds possess blood-glucose lowering actions and are useful in the treatment of diabetes mellitus.

Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.

Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.

Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl;R.sup.2 is hydrogen or lower alkyl having one to three carbon atoms; andR.sup.5 is benzyl or lower alkyl;and a compound of the formula ##STR2## in which R.sup.1 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl;R.sup.2 is hydrogen or lower alkyl having one to three carbon atoms; andX is bromo or chloro, or hydrogen;as intermediates for pyrazino(2,3-3,4) pyrido (1,2-a) indoles which are useful for treating hypertension in mammals.