Abstract: The present invention relates to a new process for the preparation of compounds of the formulae and their pharmaceutically acceptable acid addition salts, which are NMDA (N-methyl-D-aspartate)-receptor-subtype selective blockers.

Abstract: Process for the synthesis of FLECAINIDE comprising the reaction between 2,5-dihydroxybenzoic acid with trifluoroethanol perfluorobutanesulphonate to give the intermediate trifluoroethanol 2,5-bis-trifluoroethoxybenzoate, the reaction of said intermediate with 2-aminomethylpiperidine to give FLECAINIDE.

Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl, CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

Abstract: A process for the production of paroxetine is described, wherein N-substituted derivatives of 4-(p-fluorophenyl)-3-hydroxymethyl-1,2,3,6-tetrahydropyridine are treated according to the following sequence of reactions: (a) hydrogenation catalyzed by transition metal complexes with chiral diphosphinic ligands; (b) —OH derivatisation and nucleophilic substitution, the substituent being sesamol; (c) N-dealkylation. The process is highly stereospecific and brings about the formation of intermediates enriched with the desired isomeric components, which are converted into paroxetine in quantitative yields.

Abstract: Novel liquid crystal compound having a negative and absolutely large value of dielectric anisotropy, being excellent in compatibility with other liquid crystalline compounds at a low temperature and being stable chemically and physically, as well as a liquid crystal composition comprising this compound, and a liquid crystal display device comprising this liquid crystal composition are provided, said compound is expressed by the general formula (1): R1—A1—B1—A2—B2—A3—B3—Z—B4—A4—R2  (1) wherein A1, A2, A3 and A4 represent a single bond, 1,4-cyclohexylene, 1,4-phenylene which may be substituted with a fluorine atom(s) or the like; B1, B2, B3 and B4 represent a single bond, 1,2-ethylene, 1,2-ethenylene, 1,2-ethynylene, oxymethylene, methyleneoxy or the like; R1 and R2 represent an alkyl group having 1 to 10 carbon atoms or the like; and Z represents (I) to (VI): wherein X represents H or F, and Y represents difluoromethyl gr

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

Abstract: A process for producing an optically active propargyl alcohol represented by the following formula (4): 1

Abstract: A process and diastereomeric salts useful for the optical resolution of racemic &agr;-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(−)-di-paratoluoyltartaric acid or (−)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.

Abstract: The present in to s directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

Abstract: Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

Abstract: Tosylate salts are useful in purifying 4-(fluorophenyl)-3-carbinol-piperidines from the corresponding des-fluoro impurity. The purified compounds are advantageously used in paroxetine synthesis.

Abstract: New 4-substituted piperidines of the following general formula (I) are disclosed in which R1 and R2 are substituted in unsubstituted aryl radicals, which compounds are obtained as racemic mixtures and as pure enantiomers. The compounds, and their pharmaceutically acceptable salts, inhibit the serotonin and/or noradrenaline reuptake, and are useful as medicaments in disorders in which an increase of levels of those neurotransmitters is necessary.

Abstract: Benzopiperidine derivatives represented by formula (I), salts thereof or hydrates thereof, processes for producing the same and drugs comprising the same: wherein the variables are as described in the specification. These compounds are useful as drugs efficacious in the prevention and treatment of these various inflammatory diseases and immunologic diseases, such as rheumatoid arthritis, atopic dermatitis, psoriasis, asthma, and rejection reaction accompanying organ transplantation.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

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: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with &bgr;-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases.

Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.

Abstract: The tosylate ester of the formula (6) and its salts, are convenient intermediates in the synthesis of paroxetine.

Abstract: There is provided a compound of formula I, 1

Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.

Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB: 1

Abstract: 3-amino-3-arylpropan-1-ol compounds of formula I: R1 and R2 independently denoting C1-6 alkyl, or together denoting a (CH2)2-6 ring optionally substituted by phenyl, R3 denoting C3-6 alkyl, C3-6 cycloalkyl, aryl optionally containing heteroatoms and optionally substituted by R6 to R8, or a substituted C1-3 alkylphenyl of formula XII:  R4 and R5 independently denoting C1-6 alkyl, C3-6 cycloalkyl, phenyl, benzyl, or phenethyl, or together forming a (CH2)3-6 or CH2CH2OCH2CH2 ring, R6 to R8 independently denoting H, F, Cl, Br, CHF2, CF3, OH, OCF3, OR14, NR15R16, SR14, phenyl, SO2CH3, SO2CF3, C1-6 alkyl, CN, COOR14, or CONR15R16, or together forming a OCH2O, OCH2CH2O, CH═CHO, CH═C(CH3)O or (CH2)4 ring, R14 denoting C1-6 alkyl, phenyl, benzyl, or phenethyl, R15 and R16 independently denoting H, C1-6 alkyl, phenyl, benzyl or phenethyl, and A denoting optionally substituted aryl optionally containing heteroatoms, or a diastereomer or enantiomer or pharmaceutica

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO2X)m wherein  is a carrier, X is a leaving group, Y is a bond or spacer, Z is a bivalent group, when Z is a bivalent electron attractive group, W is an aromatic ring which may be substituted and when Z is a bivalent non-electron attractive group, W is an aromatic ring which is substituted by an electron attractive group and may be further substituted and m is 1 or 2, or a salt thereof, which is useful for synthesizing a novel organic compound.

Abstract: New 4-substituted piperidines of the following general formula (I) are disclosed in which R1 and R2 are substituted in unsubstituted aryl radicals, which compounds are obtained as racemic mixtures and as pure enantiomers.

Abstract: The invention relates to compounds of the general formula wherein R1 signifies hydrogen or hydroxy; R2 signifies hydrogen or methyl; and X signifies —O— or —CH2— and their pharmaceutically acceptable acid addition salts. It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

Abstract: The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: 1

Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1 2

Abstract: Novel compounds of the formula 1

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: N-(Hydroxyalkoxy) hindered amine stabilizers are prepared by reacting the corresponding N-oxyl compound with a peroxide or organic hydroperoxide and a catalytic amount of a metal salt or metal-ligand complex in an alcohol solvent. These N-(hydroxyalkoxy) hindered amines are particularly useful as stabilizers for polyolefins, thermoplastic polyolefins and automotive coating compositions.

Abstract: Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula IV ##STR2## wherein R.sup.1 and R.sup.2 are as defined in the specification.

Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.

Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

Abstract: Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartatc (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, amioglycoside antibiotics-induced hearing loss, migraine headaches, chronic pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

Abstract: Compounds selected from the group of compounds represented by Formula I: ##STR1## as an individual isomer or as a racemic or non-racemic mixture of isomers, and their pharmaceutically acceptable salts and N-oxides thereof; are sodium channel blockers, and thus exhibit useful pharmacological properties, including utility for the treatment of neuropathic pain conditions.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists Substance P and NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The subject invention pertains to optically-enriched compounds of formula (1), wherein Ar is a C.sub.6-20 aryl group; and R.sup.1 and R.sup.2 are independently H, alkyl or aryl. The subject invention also pertains to method of preparing these compounds. The subject compounds can be prepared by reduction of the corresponding 1,4-dihydropyridine-3-aldehyde, e.g., using hydrogen an a catalyst. The aldehyde can be prepared by hydrolytic cleavage of an aminal obtainable by the reaction of 3-pyridinecarboxaldehyde and a chiral C-2 symmetric diamine, an then stereoselective introduction of the Ar and COOCHR.sup.1 R.sup.2 groups.

Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.

Abstract: A medicine having the following basic structure, for the alleviation or treatment of symptoms derived from ischemic diseases and seizures, epilepsy, and migraine, having a powerful action in suppressing cytotoxic Ca.sup.2+ overload and free from side-effects: ##STR1## wherein Z.dbd.C, CH, or N, X.dbd.O or CH.sub.2, E and Y.dbd.H, OH, a halogen, alkoxy, alkyl, or a halogen-substituted alkyl.

Abstract: Compositions containing compounds of the following structure, some of which are novel, and the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: ##STR1## in which U is --(CH.sub.2).sub.n --;Q is hydroxy;R is ##STR2## in which V, W, and Z are each hydrogen; X is selected from alkoxy, haloalkoxy, alkoxyalkyl, cycloalkylalkoxy, halocycloalkylalkoxy, alkoxycarbonyl, haloalkoxycarbonyl, cycloalkylalkoxycarbonyl, halocycloalkylalkoxycarbonyl, alkoxyalkoxycarbonyl, alkoxycarbonylamino, haloalkoxycarbonylamino, cycloalkylalkoxycarbonylamino, halocycloalkylalkoxycarbonylamino, alkylaminocarbonyl, haloalkylaminocarbonyl, cyanoalkoxycarbonylamino, phenylcarbonylamino, and phenoxycarbonyl, each cycloalkyl moiety or phenyl ring optionally substituted with halogen; Y is selected from hydrogen and halogen; n is 1, 2, or 3; R.sup.1 and R.sup.

Abstract: Products are described which can be obtained by reacting components a), b) and c), where component a) is a compound of the formula I or a mixture of compounds of the formula I, component b) is a compound of the formula II or a mixture of compounds of the formula II and component c) is a compound of the formula III or a mixture of compounds of the formula III, ##STR1## in which the general symbols are as defined in claim 1, the compound of the formula I being, for example, pentaerythritol, thiodiethylene glycol, 1,4-butanediol, 1,4-propanediol, diethylene glycol, triethylene glycol, diethanolamine or glycerol, the compound of the formula II being, for example, sunflower oil or coconut fat, and the compound of the formula III being, for example, methyl 3-(3',5'-di-tert-butyl-4'-hydroxyphenyl)propionate. The abovementioned products can be used as liquid antioxidants in polymers and lubricants.

Abstract: A compound of the formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently represent H, an optionally acylated hydroxyl group, an optionally substituted amino group, an optionally substituted alkoxy group or an optionally substituted hydrocarbon group, or R.sup.2 and R.sup.3 may form an optionally substituted hydrocarbon ring; R.sup.4 represents an alkyl group; R.sup.5 represents an optionally substituted hydroxyl group; R.sup.6 and R.sup.7 independently represent an optionally substituted hydrocarbon group or R.sup.6 and R.sup.7 form an optionally substituted ring; m represents 1 or 2; and n represents an integer of 1 to 5; or a hydroquinone derivative or a salt thereof has lipoperoxide formation inhibitory effect and is useful as a medicine for treating or preventing central nervous system disorders, diseases in the circulatory system, etc.

Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

Abstract: This invention relates to new stereoselective processes for preparing 3-substituted-4-aryl piperidines and methods for controlling the absolute stereochemistry at the C-3 and C-4 positions of the piperidine ring. Compounds of this type are key intermediates in the preparation of paroxetine, femoxetine, and other medicaments.

Abstract: A novel substituted benzenedithiol metal complex represented by the general formula (1) is provided. The substituted benzenedithiol metal complex is useful as a singlet oxygen quencher and as an optical data recording medium per se. ##STR1## wherein M is a transition metal; A.sup.+ is a quaternary ammonium group; and R is an organic group selected from the group consisting of organic groups represented by the formulae (i), (ii), (iii) and (iv): ##STR2## (wherein R.sup.1 is an alkyl group having 1 to 4 carbon atoms) ##STR3## (wherein n is 3, 4 or 5), ##STR4## (wherein R.sup.2 is one of a hydrogen atom and a substitutent having 1 to 4 carbon atoms).