Abstract: A process for preparing 4-haloalkylnicotinic esters of the formula (I), where RF is (C1-C4)-haloalkyl and R is (C1-C6)-alkyl; which comprises a) reacting an aminoketone of the formula (II), RF—C(O)—CH?CH—NH2 ??(II) ?in a condensation reaction under reduced pressure with a compound of the formulae (III) to (V), (R1Z)CH?CH—COOR??(III), (R1Z)2CH—CH2—COOR??(IV), HC?C—COOR??(V), where R1 is (C1-C6)-alkyl and Z is O, S, NR1 or C(O)O, ?to give a compound of the formulae (VI) and/or (VII), RF—C(O)—CH?CH—NH—CH?CH—COOR??(VI) RF—C(O)—CH?CH—NH—CH(ZR1)—CH2—COOR??(VII) b) and subjecting the reaction product to a ring closure reaction.

Abstract: Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, n, A, E, X, G, G?, M and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.

Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.

Abstract: The present invention relates to the synthesis and biological application of piperidinoyl carboxylic acid integrin antagonists affinity moiety of IFormula (I): 1

Abstract: Halo-alkoxycarbonyl derivatives are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing functionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment.

Abstract: Use of a compound of formula (A), wherein: 1

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.

Abstract: Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiating compound of Formula I or Formula II, or a physiologically acceptable salt.

Abstract: A process for preparing compounds of the formula I in which R is hydrogen, C1-C6-alkoxy, —NHC1-C6-alkyl, —N(C1-C6-alkyl)2, OH, NH2 R1 is hydrogen, C1-C6-alkyl, Me3Si, C1-C6-alkyl-S R2 is Boc, C1-C6-acyl, mesyl, benzenesulfonyl, tosyl, trifluoroacetyl, A1-A3-peptide n is 1, 2 R4 is H, C1-C6-alkyl, is described.

Abstract: Disclosed are novel compounds and novel pharmaceutical compositions for use in medical therapy, as well as intermediates and processes for preparing such compounds. Therapeutic methods for preventing or treating glutamate-related disorders in a mammal and methods to inhibit or prevent glutamate binding in mammalian tissue are also disclosed.

Abstract: Intermediates represented by the following formula: (wherein R1 is a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or the like; X is a carboxyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group, a formyl group, —CH2—Y, —CHZ1Z2, —CH(OR4)OR5 or the like), in the synthesis of biphenylamidine derivatives to be used as inhibitors for an activated blood coagulation factor X, and a process for preparing the same.

Abstract: A biocatalytic process to obtain optically enriched derivatives of trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidines, based on the enzymatic resolution of racemic precursors of formula III (where R3 is preferably phenyl or benzyl) by acylation of the hydroxyl group. Depending on the enzyme and the reaction conditions, either of the two enantiomers may be obtained with high enantiomeric purity. These compounds are important intermediates in the synthesis of the paroxetine anti-depressive agent.

Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.

Abstract: The disclosed invention comprises a compound having the formula: in which R1 and R2 independently represent a hydrogen or an alkyl group of 4 carbon atoms or greater. Further disclosed is a process for the preparation of the disclosed chiral amino alcohols from a starting amine compound and a limonene oxide.

Abstract: The present invention relates to the potentiation of glutamate receptor function using certain heterocyclyl sulphonamide derivatives. It also relates to novel heterocyclyl sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: A process for preparing an enantiomerically-enriched form of threo-ritalinic acid, which comprises resolving a mixture of enantiomers of a salt of the acid, said salt being formed with an achiral acid or base, using a chiral resolving agent. The resolved salt can be esterified, to give the therapeutic agent d-threo-methylphenidate.

Abstract: An aldehyde compound is reacted with an amino compound and hydrogen cyanate in the presence of a chiral zirconium catalyst obtained by mixing a zirconium alkoxide with an optically active binaphthol compound.

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

Abstract: Compounds of structure (2) are prepared by reaction of an arecoline analogue of structure(4) with an organometallic compound containing an X-substituted phenyl group, such as a compound of structure (3). Suitably the compound of structure (3) is a Grignard reagent, where M is magnesium and Y is a halogen atom, or M may be a Group II metal and Y is a halogen atom or a second X-substituted phenyl group. When structure (3) is a Grignard reagent, the reaction is carried out either in a suitable non-ether solvent, typically a hydrocarbon or a non-reactive chlorinated hydrocarbon, or in a mixture of such a solvent with diethyl ether. Compounds of structure (2) are important intermediates in the preparation of inter alia paroxetine.

Abstract: There are disclosed a process for producing the optically active cyclic amino acid ester derivative of the formula (I): by optical resolution method, a process for producing the same and a process for producing an optically active cyclic amino acid using the compound of the formula (I).

Abstract: A poly(oxyalkylene)pyridyl or piperidyl ester having the formula: ##STR1## or a fuel-soluble salt thereof; wherein A is a nitrogen-containing ring selected from the group consisting of 3-pyridyl, 4-pyridyl, 3-piperidyl and 4-piperidyl; R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and each R.sub.1 and R.sub.2 is independently selected in each --O--CHR.sub.1 --CHR.sub.2 -- unit; R.sub.3 is hydrogen, alkyl having 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms or alkaryl having about 7 to about 100 carbon atoms; x is an integer from 0 to 4; and n is an integer from about 5 to about 100.The poly(oxyalkylene)pyridyl and piperidyl esters of the present invention are useful as fuel additives for the prevention and control of engine deposits.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: The present invention relates to new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded form an unsubstituted or substituted 5- to 7-membered ring which is interrupted by at least one hetero atom,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or one of the groups ##STR2## E represents a metal ion equivalent or an ammonium ion, L represents oxygen or sulphur,M represents oxygen or sulphur andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description, to processes for their preparation, and to their use as pesticides.

Abstract: 4-Substituted-4-piperidinecarboxamides of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Abstract: Pyridyl and piperidyl esters of polyalkylphenoxyalkanols having the formula: ##STR1## or a fuel soluble salt thereof, wherein A is selected from the group consisting of 3-pyridyl, 4-pyridyl, 3-piperidyl, and 4-piperidyl;R.sub.1 is a polyalkyl group having an average molecular weight in the range of from about 450 to 5,000; andR.sub.2 and R.sub.3 are independently hydrogen or lower alkyl having from about 1 to 6 carbon atoms.The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.

Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.

Abstract: The present invention is concerned with a novel process for the preparation of a compound of the formula: ##STR1## This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Abstract: Cyclopropyl derivatives of formula (I) wherein R is cyclopropyl or methyllopropyl are prepared by reaction of 2,6-dibromohexanoyl chloride with 2,6-dimethylaniline in the presence of a base at 0.degree.-25.degree. C. to give 2,6-dibromohexanoyl-2,6-dimethylanilide which subsequently is reacted with R--NH.sub.2 (wherein R is cyclopropyl or methylcyclopropyl) at 70.degree.-100.degree. C. The compounds are useful as antiarrhythmic agents and as local anaesthetic agents.

Abstract: The present invention provides a stabilizer comprising a substituted cyclohexene compound of a hindered piperidine type wherein the 1- and 2-positions on a cyclohexene ring are doubly bonded, a carbon atom situated at the 4-position and/or the 5-position of the cyclohexene ring contains a substituent having a C.dbd.O group at its alpha-position, at least one carbon atom of the cyclohexene ring located adjacent to said carbon atom having the C.dbd.O group has a hydrogen atom as a substituent, and at least one group containing a 2,2,6,6-tetramethyl-4-piperidyl group attached to the 3-, 4-, 5- or 6-position of the cyclohexene ring; and/or other substituted cyclohexene compound of a hindered piperidine and/or a compound of a hindered piperidine. The stabilizers of the present invention can exhibit improved properties in light stability and in bleed out resistance even without a phenol type antioxidant.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which R.sub.1, R.sub.2 and R.sub.3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy;ALK.sup.1 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups;Y represents a piperidine ring which is attached through nitrogen to ALK.sup.1 ;R.sub.4 represents hydrogen or a C.sub.1-4 alkyl group; the broken line in --- represents a bond, or is absent and the free valency on Y is taken up by hydrogen and the free valency on CR.sub.4 is taken up by hydrogen or a C.sub.1-4 alkyl group;ALK.sup.2 is absent or represents a C.sub.1-4 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups; andR.sub.5 and R.sub.6 independently represent hydrogen, alkyl, phenyl, alkyl (optionally substituted) or R.sub.5 and R.sub.

Abstract: Benzly-piperidine derivatives of formula I and their pharmaceutically acceptable salts are used in the control of psychotic disorders which are caused by damage to the dopamine system, especially schizophrenia. ##STR1## A is ##STR2## B is ##STR3## R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, amino, nitro, halogen, lower-alkly or lower-alkoxy. R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen, nitro, halogen, lower-alkyl, lower-alkoxy, cyano, trifluoromethyl, amino, lower-alkylamino or di-lower-alkylamino. R.sup.7, R.sup.2 and R.sup.9 are independently hydrogen, amino or nitro.

Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.

Abstract: Compounds which suppress human T-lymphocyte proliferation are disclosed.

Abstract: Disclosed herein are peptide of the formulaR--CONH--CH.sub.2 --CONH--CH(R')--CH.sub.2 COOH Iwherein R and R' are as defined herein. The claimed peptide derivatives inhibit platelet aggregation and as such are useful in the treatment of thrombosis.

Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is a 2-R.sub.A -3-R.sub.B -phenyl radical, a 2-R.sub.A -4-R.sub.C -phenyl radical, a 2-R.sub.A -pyridin-3-yl radical, a 3-R.sub.A -pyridin-2-yl radical or a 1-R.sub.D -indol-3-yl radical, wherein one of the radicals R.sub.A and R.sub.B is an aliphatic or heterocycloaliphatic-aliphatic radical or free or aliphatically, araliphatically or heteroaraliphatically etherified hydroxy and the other is hydrogen, an aliphatic radical or free or esterified or amidated carboxy, R.sub.C is hydrogen, an aliphatic radical, free or aliphatically, araliphatically, heteroaraliphatically or heteroarylaliphatically etherified hydroxy or an unsubstituted or heteroaliphatically substituted amino group, and R.sub.D is an aliphatic, araliphatic or heteroaliphatic radical, one of the radicals X.sub.1 and X.sub.2 is carbonyl and the other is methylene, R.sub.2 is an aliphatic radical, R.sub.3 is unsubstituted or aliphatically substituted amino, R.sub.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a trans-substituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'--L).sub.q -- S--C(O)--L'--II' Iwherein:S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. Compounds which contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula :Y--A--CO--R.sup.1are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.