Abstract: Disclosed are compounds of formula I wherein R1, R2, R5 and R6 are as defined in the claims; such compounds have interesting pharmacological properties.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: Neuroprotectant agents are provided which do not contain peptides and axe protected from the degradation that limits the use of peptide-based drugs in systemic circulation. With great selectivity for NMDA receptors, the agents exert an open channel block on NMDA receptors, and protect neuronal cells containing such receptors from excitatoxic cell death.

Abstract: The present invention provides diaryl ether derivatives that exhibit significant immunosuppressive effects with less side effects. The diaryl derivatives of the present invention are represented by the following general formula (1): one example is 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propanediol.

Abstract: A compound of formula 1 wherein: R1 is C1-C4-alkyl; R2 is C1-C4-alkyl; and R3 is C1-C4-alkyl or phenyl, each optionally mono- or polysubstituted, or R2 and R3 together are —CH2—CH2— or —CH2—CH2—CH2—, or the corresponding acid addition salt with a pharmacologically acceptable acid, processes for preparing such compounds, pharmaceutical compositions containing such compounds, and their use in the treatment of inflammatory and obstructive respiratory diseases.

Abstract: Diol-functionalized antioxidants and the process for the preparation thereof are disclosed and have the general formula (I): wherein: R1 is tert-butyl and R2 is C1 to C8 linear or branched alkyl. The invention also pertains to a process for their preparation. Which comprises: Reacting a halo functionalized antioxidant having the general formula (II): wherein: R1 is tert-butyl and X is bromide (Br) with a diol having general formula (IV): wherein R2 is C1 to C8 linear or branched alkyl.

Abstract: Crystalline forms of Venlafaxine hydrochloride were found, referred to hereinafter as polymorphic Forms A, B and D. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the crystalline forms.

Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.

Abstract: Described are cyclobexylamine derivatives of Formula I, Formula II, or Formula III and their pharmaceutically acceptable salts thereof: The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.

Abstract: The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising reaction of a compound of formula II with a diene having the formula wherein X is O, S, SO2, —N═N—, —CO—O—, —O—CO—, or or with a diene having the formula wherein R is alkyl or optionally substituted aryl or arylalkyl. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.

Abstract: Venlafaxine besylate compounds provide certain advantages over venlafaxine hydrochloride and are useful in forming pharmaceutical compositions and n treating venlafaxine-treatable diseases and conditions. Venlafaxine besylate can be easily formulated into an extended release dosage form including a hydrogel tablet as well as other matrix-based tablet compositions. A preferred tablet making process involves hot melt granulation.

Abstract: The invention provides a method for treating a subject with venlafaxine, comprising administering to the subject a formulation having a therapeutically effective amount of venlafaxine or a pharmaceutically acceptable salt thereof, wherein the formulation provides a delayed burst release after at least three hours resulting in dispersion mainly through the colon of the active ingredient into the blood stream as a result of colon absorption over a period of at least 24 hours.

Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Provided herein are polyurethane foams which may be prepared by spray techniques. The foams of the invention are prepared using conventional isocyanates and a novel Mannich condensate polyol having a hydroxy number in the range of 250-340 and a viscosity of 3500 cps or less, and wherein the Mannich condensate polyol is derived from nonylphenol, formaldehyde, an alkanolamine, and propylene oxide as the sole alkoxylating agent. Polyurethane foams prepared according to the invention possess superior physical properties over sprayed polyurethane foams prepared using Mannich condensate polyols which are made using mixtures of propylene oxide and ethylene oxide.

Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.

Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.

Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hyproxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: The present invention is directed to the isolation and bioactive characterization of compounds isolated from the clam Spisula polynyma. These compounds include three sphingoid-type bases, spisulosines 285, 299 and 313 (1-3), each of which shows unique cytotoxicity against L1210 murine lymphocytic leukemia cells. In addition, sphingosine (also referred to as 4-sphingenine or octadeca-4-shpingenine, 4) and two related compounds, nonadeca-4-sphingenine (a one carbon longer homolog, 5) and sphinga-4,10-diene (a dehydrosphingosine deravitive, 6) were also obtained, These compounds also contribute to the cytotoxicity of the Spisula polynyma extracts, but did not cause the morphology changes observed with compounds 1-3.

Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.

Abstract: Hydroxy-substituted hydroxylamine antioxidants can be prepared by reacting hydroxylamine or a mono-substituted hydroxylamine, in free base form, with an epoxide. The antioxidant reaction product can be used without isolation from the reaction solution, and combined with a color developing agent to provide a photographic color developing composition in either concentrated or working strength formulations. The method for preparing the antioxidant is rapid and efficient because of the use of the free base form of the hydroxylamine reactant, higher temperatures (at or above 50.degree. C.) and certain molar ratios of reactants.

Abstract: The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases.

Abstract: The present invention relates to a method for the prevention of growth of algae by incorporating within liquids or coating on surfaces certain substituted amino alcohols. More precisely, this invention provides for algistat end uses for amino alcohol compounds endowed with chain extension which have the general formula: ##STR1## wherein n is 1-1000; and R.sub.1 =R.sub.2, and R.sub.1 and R.sub.2 are from the croup consisting of --CH.sub.2 --CH.sub.2 --; --CH.sub.2 --C(CH.sub.3)H--; and --C(CH.sub.3)H--CH.sub.2 --; R.sub.3, and R.sub.4 are each independently selected from the group consisting of H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 OH, and --CH.sub.2 --CH.sub.2 --OH; and the diasteromeric salts thereof.

Abstract: This invention relates to derivatives of 4,4-(disubstituted)cyclohexan-1-ones and related compounds which are useful for treating allergic and inflammatory diseases.

Abstract: Alkyl-substituted polyarenes of the formula ##STR1## in which R is alkyl and Ar.sub.res is an aryl residue, are prepared from aryl ketones by reaction of the latter with 1-cyclohexenyloxytrimethylsilane in the presence of a Friedel-Crafts catalyst. When R is methyl and Ar.sub.res is a naphthyl residue, the reaction serves as a step in a reaction scheme leading to crisnatol mesylate, a pharmaceutical useful in the treatment of brain cancer.

Abstract: Hydroxyalkyl-substituted aminoalkynes of the general formula I ##STR1## where at least one of the substituents R.sup.1, R.sup.4 or R.sup.5 is hydroxyalkyl are prepared in a reaction with heterogeneous catalysis.

Abstract: A process is claimed for preparing [1S(1(.alpha., 2.beta., 4.beta.)]-4-amino-2-hydroxymethyl -1-cyclopentanol from cis-4-((R)-benzoylamino)-2-cyclopentenecarboxylic acid, methyl ester in five steps. The invention also describes a number of novel intermediates useful in the synthesis of [1S(1.alpha., 2.beta.,4.beta.)]-4-amino-2-hydroxymethyl-1-cyclopentanol.

Abstract: The present invention provides novel aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake.

Abstract: A retroviral protease inhibiting compound of the formulaA--X--Bor a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group;A is(1) substituted amino,(2) substituted carbonyl,(3) functionalized imino,(4) functionalized alkyl,(5) functionalized acyl,(6) functionalized heterocyclic or(7) functionalized (heterocyclic)alkyl; andB is(1) substituted carbonyl independently defined as herein,(2) substituted amino independently defined as herein,(3) functionalized imino independently defined as herein,(4) functionalized alkyl independently defined as herein,(5) functionalized acyl independently defined as herein,(6) functionalized heterocyclic independently defined as herein or(7) functionalized (heterocyclic)alkyl independently defined as herein.

Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.

Abstract: Mannich condensation products prepared by the condensation of a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, alkyl, phenyl, aralkyl, alkaryl, or an acyl group of the formula: ##STR2## wherein R.sub.6 is alkyl, phenyl, aralkyl or alkaryl; R.sub.7 is alkyl; u is an integer from 1 to 10; n is an integer from 5 to 100; and x is an integer from 0 to 10;with an aldehyde and a nitrogen base selected from ammonia, lower alkylamine, a polyamine and mixtures thereof.The Mannich condensation products and their fuel soluble salts are useful as fuel additives for the prevention and control of engine deposits.

Abstract: Disclosed are a process and intermediates of the formulae ##STR1## wherein R is --CH.sub.2 OH or --OH and R.sup.3 is H or C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepines of the formula ##STR2## having activity as selective D1 antangonists.

Abstract: Described herein is a novel method of preparing selectively diastereomers of sphingosine bases and their analogues of general formula (1a) or (1b) ##STR1## where R is an aliphatic or aromatic substituent containing a straight, branched or cyclic chain, which may include one or several heteroatoms as chain members and one or several functional groups as substituents. The method comprises the steps of:a) converting a starting material into an intermediate product in the form of .alpha.,.beta.-unsaturated ketone having the general formula (4a) or (4b) ##STR2## where R is as defined above and PG are any protecting groups compatible with the method,b) reducing said .alpha.,.beta.-unsaturated ketone to an aminoalcohol with DIBAL in toluene to obtain selectively an anti-diastereomer, andc) removing the protecting groups to obtain the free sphingosine base or its analogue according to formula (1a) or (1b).

Abstract: A process is disclosed for the preparation of a substituted diaminodiol.

Abstract: The present invention relates to intermediates useful in a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.2a is hydrogen or loweralkyl, R.sub.2b is hydrogen, loweralkyl, cycloalkyl or phenyl and R.sub.1 is cycloalkyl, cycloalkylalkyl, phenyl or benzyl. These intermediates are compounds of the formula: ##STR2## wherein P.sub.2 is an O-protecting group, P.sub.3 is an N-protecting group and R.sub.1, R.sub.2a and R.sub.2b are defined as above.

Abstract: The present invention realates to anti-neoplastic and anti-psoriasis pharmaceutical bis-hexahydropyrimidinylalkyl compounds, compositions and methods of treatment and to insecticidal compositions and methods of controlling the growth of insects.

Abstract: Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of .alpha.-amino aldehyde derivative [I] and compound [II] in the presence of BF.sub.3.OEt.sub.2, as shown in the following reaction formula, .alpha.-amino-.beta.-hydroxy-.delta.-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R.sup.1 is a protective group on the amino group, R.sup.2 is a lower alkyl group which may be branched, and R.sup.4 is a cyclohexyl group or phenyl group).

Abstract: A process of reforming an alkyleneamine feedstock or a mixture of such feedstocks to an alkyleneamine or a mixture of alkyleneamines which is different from the feedstock or feedstock mixture. The process is catalyzed by one of the following: Group VB metal oxides, Group VB metal phosphates, Group IIA metal silicates, and tungsten oxides. For example, ethylenediamine is contacted with a catalyst of niobic acid or magnesium silicate to yield predominantly diethylenetriamine and non-cyclic triethylenetetramines; whereas high molecular weight polyethylenepolyamines are cracked by the same catalysts to mixtures of lower molecular weight linear and cyclic materials.

Abstract: A method for synthesizing no-carrier-added (NCA) aryl [.sup.18 F] fluoride substituted aromatic aldehyde compositions bearing an electron donating group is described. The method of the present invention includes the step of reacting aromatic nitro aldehydes having a suitably protected hydroxyl substitutent on an electron rich ring. The reaction isThe U.S. Government has rights in this invention pursuant to Contract Number DE-AC02-76CH00016, between the U.S. Department of Energy and Associated Universities Inc.

Abstract: A process for reforming alkyleneamines to predominantly linearly-extended polyalkylenepolyamines comprising contacting an alkyleneamine or mixture thereof with a catalyst under conditions such that a mixture of polyalkylenepolyamines enriched in linearly-extended products is formed, said catalyst containing at least one compound selected from the group consisting of (a) Group VB metal oxides, (b) Group VB metal phosphates, (c) silicates of Groups IIA, IIIB, IVB, VB, and the lanthanide and actinide metals, and (d) tungsten oxides, with the proviso that the silicates and tungsten oxides are essentially free of aluminum. For example, ethylenediamine is contacted with a catalyst of niobium phosphate or niobic acid under reaction conditions to yield predominantly non-cyclic polyethylenepolyamines.

Abstract: This invention relates to a process for making amines by condensing an amino compound in the presence of a condensation catalyst and a condensation catalyst promoter, wherein said condensation catalyst promoter is present in an amount sufficient to promote the condensation catalyst. This invention also relates to an alkyleneamines producers composition rich in triethylenetetramine (TETA), tetraethylenepentamine (TEPA) and pentaethylenehexamine (PEHA).

Abstract: Halogenoalkylphenyl-alcohols, ketones and their hydrates of formula I, ##STR1## wherein R.sub.1 to R.sub.8 are as defined in the description, are useful as acetylcholinesterase inhibitors.

Abstract: The present invention provides novel aryloxy indanamines of the formula ##STR1## wherein n, p and q are each independently 0, 1 or 2,Y and X are each independently lower alkyl, lower alkoxy, hydroxy, CF.sub.3, halogeno or when p or q are 2 and each of the Y or each of the X groups are on adjacent aryl carbon atoms, both of the X or both of the Y groups can be taken together to form a methylenedioxy moiety,R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, aralkyl, or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached are pyrrolidino, morpholino, piperidino, piperazino, or 4-methylpiperazino,or an acid addition salt thereof, which are useful as antidepressants and as inhibitors of synaptic norepinephrine and serotonin uptake.

Abstract: A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.

Abstract: The bis-homotris compounds 4-amino-4-[1-(3-hydroxypropyl)]-1,7-heptanediol and 4-[1-(3-aminopropyl)]-4-[1-(3-hydroxypropyl)]-1, 7-heptanediol, and organic synthetic methods for their preparation are described. Unique multifunctional aminotriols, as well as their percursors, quaternary nitroalkanes are disclosed as building blocks for unimolecular micelles, as well as new series of cascade polymers. The quaternary nitro compounds which are disclosed allow the synthesis of a new aminotriol containing a quaternary carbon.

Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.

Abstract: The present invention is directed to the isolation and bioactive characterization of compounds isolated from the clam Spisula polynyma. These compounds include three sphingoid-type bases, spisulosines 285, 299 and 313 (1-3), each of which shows unique cytotoxicity against L1210 murine lymphocytic leukemia cells. In addition, sphingosine (also referred to as 4-sphingenine or octadeca-4-shpingenine, 4) and two related compounds, nonadeca-4-sphingenine (a one carbon longer homolog, 5) and sphinga-4,10-diene (a dehydrosphingosine deravitive, 6) were also obtained, These compounds also contribute to the cytotoxicity of the Spisula polynyma extracts, but did not cause the morphology changes observed with compounds 1-3.

Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.