Abstract: New compounds of formula I are described: 1

Abstract: Described are cyclohexylamine derivatives of Formula I 1

Abstract: The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R1 represents hydrogen atom, nitro group, cyano group, C1-6 alkylcarbonylamino, R2 and R3 each independently represent C1-6 alkyl group, R4 represents hydroxyl group or C1-6 alkylcarbonyloxy group or represents a bond or oxygen atom together with R5, R5 represents hydrogen atom or represents a bond or oxygen atom together with R4, R6 represents hydrogen atom, hydroxyl group or NR7R8, n means 0 or an integer of 1 to 4, X represents C═O, CH2, SO2 or NR16, Y represents NR17 when X is C═O, CH2 or SO2 and represents C═O when X is NR16, Z is absent when Y represents NR17 or represents NR18 when Y is C═O, W represents aromatic groups or lactam rings, or pharmaceutically acceptable salt thereof.

Abstract: Disclosed are methods of producing of alkoxy arylamine compounds which find particular use in the syntheses of pharmaceutical drug. The alkoxy arylamine compounds generally have the formula: H2N—Ar—OR wherein Ar is an unsubstituted or substituted aromatic group, and R is an unsubstituted or substituted alkyl or aryl group. The methods comprise generally, the steps of (a) alkylating a protected-amino arylalcohol to form a protected-amino arylether; and (b) deprotecting said protected-amino arylether to form an alkoxy arylamine compound.

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 invention relates to organic compounds having a molecular weight of less than 1000 comprising at least one structural unit of the formula (I) 1

Abstract: The present invention relates to a process for the preparation of &agr;′ chloroketones, such as 4-phenyl-3-t-butyloxy-carbonylamino)-2-keto-1-chlorobutane by reacting certain aryl amino acid esters, e.g. N-(2-t-butoxycarbonyl)-L-phenylalanine-4-nitrophenyl ester, with a sulfur ylide compound to form the corresponding keto ylide compound which is then treated with a source of chloride and an organic acid.

Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.

Abstract: Disclosed are compounds of the formula (I) 1

Abstract: Disclosed is a three step synthesis of 11-aryl-5,6-dihydro-11H-dibenz[b,e]azepines from a 2-aminobenzophenone represented by the following structural formula: 1

Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.

Abstract: A novel process for the preparation of compounds of formula I by aminolysis of a p-halophenyl alkyl ketone of formula II with a cyclic amine of formula III in water at a temperature of at least 130° C., in which formulae X is a halogen atom and R1, R2 and R3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.

Abstract: The invention relates to methods for the treatment of central nervous system disorders, neurological 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.

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: Compounds of the formulae I, II, III and IV ##STR1## wherein Ar for example is a phenyl, biphenyl or benzoylphenyl group, which is unsubstituted or substituted; Ar.sub.1, for example, has the same meanings as Ar; Ar.sub.2 is inter alia phenyl; X may be a direct bond; Y hydrogen, etc.; R.sub.1 and R.sub.2 for example C.sub.1 -C.sub.8 alkyl; R.sub.3 inter alia hydrogen or C.sub.1 -C.sub.12 alkyl; R.sub.4 is inter alia C.sub.1 -C.sub.12 alkyl; or R.sub.3 and R.sub.4 together are C.sub.3 -C.sub.7 alkylene; R.sub.5 is for example C.sub.1 -C.sub.6 alkylene; and Z is a divalent radical; provided that at least one of the radicals Ar, Ar.sub.1, Ar.sub.2, Ar.sub.3, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or Y is substituted by 1 to 5 SH groups, or provided that Y contains at least one --SS-- group, are photoinitiators for the polymerization of ethylenically unsaturated compounds.

Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.

Abstract: The present invention discloses a process for the preparation of a compound having formula 4: ##STR1## The process comprises the step of reacting an enolate having the formula: ##STR2## with a Grignard reagent. The enolate salt is formed in situ from the reaction of a protected ester wherein M is an alkali metal. R.sub.6 and R.sub.7 are each hydrogen or are independently selected from ##STR3## wherein R.sub.a and R.sub.b are independently selected from hydrogen, lower alkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, lower alkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR4## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from lower alkyl, trifluoromethyl, alkoxy and halo. Alternatively, R.sub.6 is as defined above and R.sub.7 is R.sub.12 OC(O)-- wherein R.sub.12 is benzyl; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded form ##STR5## wherein R.sub.

Abstract: The present invention provides novel thiadiazole amide derivatives represented by formula I ##STR1## The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis, periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.

Abstract: A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a temperature of at least 130.degree. C., in which formulae X is a halogen atom and R.sub.1, R.sub.2 and R.sub.3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.

Abstract: Disclosed is a benzoylethylene derivative represented by the following formula (I) or a salt thereof. ##STR1## R.sup.1 to R.sup.5 : a hydrogen atom, --OR.sup.9 (R.sup.9 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.), etc.,R.sup.6 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.,R.sup.7 : a hydrogen atom, a cyano group, a C.sub.1 -C.sub.5 alkyl group, --SO.sub.q R.sup.15 (q: 0, 1, 2, R.sup.15 : a thienyl group, a phenyl group, etc.) etc.,R.sup.8 : a cyano group, --CR.sup.22 R.sup.23 X (R.sup.22, R.sup.23 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc., X: --NR.sup.24 R.sup.25 (R.sup.24, R.sup.25 : a C.sub.1 -C.sub.5 alkyl group, etc., an alkylene group by combining, etc.)), etc.The benzoylethylene derivative of the present invention has potent tyrosine kinase inhibiting activity and cancer cell growth inhibiting activity. The tyrosine kinase inhibitor of the present invention is useful as a carcinostatic agent.

Abstract: Compounds of formulas ##STR1## wherein, B is lower alkylene or an optionally substituted aromatic ring system;G.sup.1, G.sup.2 and G.sup.3 each independently signify a residue of a glycopyranoside, a glycopyranose or a derivative thereof, with at least one hydroxy group of residue G.sup.1, G.sup.2 or G.sup.3 being esterified with sulfuric acid, and pharmaceutically usable salts thereof, are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.

Abstract: A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient. In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl. The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.

Abstract: A process for producing a (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative which comprises reacting a (2S)-2-(N,N-dibenzyl)aminophenylalanine ester derivative with acetonitrile in the presence of a lithium compound or a magnesium compound is disclosed, and a process for producing a (2S)-2-(N,N-dibenzyl)amino-5-amino-1,6-diphenyl-4-hexen-3-one derivative which comprises adding a benzylmagnesium halide or a benzyllithium to a reaction solution containing the (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative and reacting the derivative with the benzylmagnesium halide or the benzyllithium is also disclosed. According to these processes, optically pure (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative and (2S)-2-(N,N-dibenzyl)amino-5-amino-1,6-diphenyl-4-hexen-3-one derivative can be produced in a good yield on an industrial scale.

Abstract: Compounds of formula ##STR1## wherein R, R', R", R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m, n and p have the meanings reported in the description;and their pharmaceutically acceptable salts are described.The compounds of formula I are useful in the treatment of arterial hypertension and congestive heart failure, of renal failure, of peripheral arteriopathies, of cerebrovascular insufficiencies and of ischemic cardiopathy.

Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.

Abstract: Compounds structurally related to ethacrynic acid are described. The compounds are useful for controlling intraocular pressure. Unlike ethacrynic acid, the compounds of the present invention are capable of effectively penetrating the cornea. Methods of controlling intraocular pressure via topical application of one or more of the compounds to the eye and topical ophthalmic compositions useful in the treatment of glaucoma are also described.

Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meaning defined in the description which possess valuable herbicidal properties.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.

Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.

Abstract: This invention comprises polyanionic benzylglycosides of benzene triacid amides of the general formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are, independently, H, SO.sub.3 M, or ##STR2## and each oligosaccharide group contains 1 to 3 sugar groups; M is lithium, sodium, potassium, or ammonium;n is 1 or 2;X is a halogen, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms;Y is carbonyl or sulfonyl;or the pharmaceutically acceptable salts thereof, as well as their use as smooth muscle cell antiproliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterized by excessive smooth muscle proliferation.

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: Compounds are described in which a polyamine moiety is linked to a phenolic moiety by a Mannich base linkage involving one of the amino groups of the polyamine moiety, and in which an aminoalkylene-poly(oxyalkylene) moiety is linked to the phenolic moiety by a Mannich base linkage involving an amino group of the alkylene-poly(oxyalkylene) moiety. Compounds of this type have been found to be highly effective in controlling the formation of intake valve deposits in internal combustion engines.

Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)--wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.

Abstract: Compounds of the formula ##STR1## having retinoid like biological activity.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor. An intermediate for preparing the novel compounds have the following formula: ##STR1## wherein R, R.sub.1 and R.sub.9, are as defined in the specification.

Abstract: A new process for the preparation of pyrazolines of formula ##STR1## is provided, in which R.sup.1 and R.sup.3 are identical or different and each represent optionally substituted aryl or optionally substituted and/or benzo-fused heterocyclyl with 5 or 6 ring members of which 1 to 4 are nitrogen atoms and the remainder are carbon atoms, andR.sup.2 represents hydrogen or alkyl, cycloalkyl or aryl, each of which is optionally substituted.In this, in a first reaction stage, ketones of formula (II) ##STR2## are reacted with bis-dialkylaminomethanes of formula (III)(R.sup.4).sub.2 N--CH.sub.2 --N(R.sup.4).sub.2 (III)in whichR.sup.4 represents alkyl,optionally in the presence of a diluent, at temperatures between 0.degree. C. and 100.degree. C. and the substituted dialkylaminoalkyl ketones of general formula (IV) ##STR3## formed in this way are optionally isolated and in a second process stage are reacted with hydrazine (hydrate), optionally in the presence of a diluent, at temperatures between 0.degree. C.

Abstract: The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.

Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X--Y).

Abstract: This invention relates to asymmetric syntheses in which a prochiral or chiral compound is contacted in the presence of an optically active metal-ligand complex catalyst to produce an optically active product.

Abstract: A compound of the formula (VIII): ##STR1## wherein R.sup.1 represents a halo-(C.sub.1 to C.sub.6)-alkoxy group at the ortho or meta position; and W.sup.2 represents a methanesulfonyl group, a methylthio group or ##STR2## wherein R.sup.44 is a (C.sub.1 to C.sub.3)-alkoxy group.

Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X-Y).

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 continuous process employing at least two reaction stages for manufacturing pesticides from methyl isocyanate and oxime or phenol reactants in water.