Abstract: A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atheroclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.

Abstract: Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2  (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.

Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.

Abstract: Novel C3A ligands are provided. Methods of using the present compounds to treat immune and inflammation disease are also provided.

Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: The present invention relates to compounds of the general formula (1) 1

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated

Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: A 1,4-diazacycloheptane derivative and an oxidative hair colorant containing the derivative as a primary intermediate is presented. The 1,4-diazacycloheptane derivative is of the formula: ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently of one another represent hydrogen, a C.sub.1-4 alkyl or hydroxyalkyl group or a C.sub.2-4, dihydroxyalkyl group, X and Y independently of one another represent hydrogen, chlorine, fluorine, a C.sub.1-4 alkyl, hydroxyalkyl, aminoakyl or alkoxy group, a C.sub.2-4 dihydroxyalkyl group or an allyl group and R.sup.5 and R.sup.6 independently of one another represent hydrogen or a C.sub.1-4 alkyl group. Natural color tones can be obtained in keratin fibers with oxidative hair colorants containing the 1,4-diazacycloheptane derivative, without the use of additional primary intermediates.

Abstract: The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R.sup.3 or CH--R.sup.4,Y=CH.sub.2 or (CH.sub.2).sub.2,Z=O or H.sub.2 ;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.

Abstract: The invention relates to intermediates and processes for producing benzothiophenes employing hydroxylamines.

Abstract: Isocyanato compounds with capped, isocyanate-reactive groups are those of the formula I ##STR1## where R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.10 -aryl or C.sub.7 -C.sub.10 -aralkyl or together form C.sub.3 -C.sub.10 -alkanediyl,X and Y are --O--, --S-- or ##STR2## where R.sup.4 is hydrogen, C.sub.1 -C.sub.20 -alkyl which is uninterrupted or interrupted by oxygen atoms in ether function, or is C.sub.6 -C.sub.10 -aryl or C.sub.7 -C.sub.10 -aralkyl,R.sup.3 is C.sub.1 -C.sub.10 -alkanediyl which together with --X--CR.sup.1 R.sup.2 --Y-- forms a 4-7-membered ring,in which either one hydrogen in R.sup.3 or the radical R.sup.4 in ##STR3## is replaced by an allophanate group R.sup.Ia ##STR4## in which R.sup.5 is a divalent aliphatic, alicyclic, araliphatic or aromatic C.sub.2 -C.sub.20 hydrocarbon unit,R.sup.6 is a single bond or a divalent aliphatic, alicyclic, araliphatic or aromatic C.sub.1 -C.sub.20 hydrocarbon unit or a mono- or poly(C.sub.2 -C.sub.

Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, selected from H; C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from H, halogen, --NO.sub.2, alkyl, alkoxy, C.sub.1 -C.sub.6 perfluorinated alkyl, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, --CN, --O--R.sup.1, --O--Ar, --S--R.sup.1, --S--Ar, --SO--R.sup.1, --SO--Ar, --SO.sub.2 --R.sup.1, --SO.sub.2 --Ar, --CO--R.sup.1, --CO--Ar, --CO.sub.2 --R.sup.1, or --CO.sub.2 --Ar; and Y is selected from a) the moiety: ##STR2## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.

Abstract: The invention provides benzo[b]thiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies.

Abstract: The present invention provides a class of substituted indene compounds and their pharmaceutically acceptable salts which possess selective estrogen receptor modulator (SERM) activity and are thus useful in the treatment of osteoporosis and cardiovascular disease, particularly hyperlipidemia in women. The compounds possess the structure ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.2 is hydrogen, hydroxy, halo, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexa-methyleneimino, and n is 2 or 3. The dashed line bond between the carbon atoms at positions 1 and 2 of the indene nucleus represent an optional double bond with the proviso that when the double bond is absent, the parenthetic hydroxy group at position 1 is present and vice versa.

Abstract: Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.

Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.

Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.

Abstract: The instant invention provides dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods for use in the treatment of bone loss or bone resorption.

Abstract: The present invention provides compounds of formula I ##STR1## wherein R.sub.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOO(C.sub.1 -C.sub.6 alkyl), --OCOAr, --OCOOAr, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sub.2 is --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOO(C.sub.1 -C.sub.6 alkyl), --OCOAr, --OCOOAr, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sub.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt or solvate thereof.

Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.

Abstract: The present invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; having activity as a selective estrogen receptor modulator, pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for treating conditions resulting from estrogen deprivation or the inappropriately high presence of estrogen. Also provided are methods and chemical intermediates for the production of a compound of formula I above.

Abstract: Amino alcohol derivatives with a primary amino group or a substituted amino group influence the synthesis of glycolipids and have antiviral, antitumor, metastasis inhibiting and neural cell growth enhancing functions. The amino alcohol derivatives are useful in preparing 2-acylamino alcohol derivatives.

Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.

Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O);Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.

Abstract: The invention provides tetrahydrobenzo?a!fluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia.

Abstract: The present invention provides compounds of formula ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.7 cycloalkyl which is optionally substituted with 1 to 3 substitutents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, amino, nitro, and halo;X is --CH(OH)-- or --CH.sub.2 --;M is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Also provided are methods of using the compounds of the present invention for the treatment of various medical indications associated with post-menopausal syndrome, uterine fibroid disease, endometriosis, and aortal smooth muscle cell proliferation.

Abstract: A novel cyclobutenedione derivative prepared in accordance with the following reaction formula, a process for the preparation thereof, and a nonlinear optical element comprising such a derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 each represents an alkyl group, an alkenyl group or an alkynyl group; R.sup.3 and R.sup.4 each represents a hydrogen atom, an alkyl group, an alkenyl group or an alkynyl group; and C.sup.* represents an asymmetric carbon atom, with the proviso that R.sup.1, R.sup.2 and the nitrogen atom to which they are connected may form a cyclic structure larger than 3-membered ring, R.sup.1 and R.sup.3, and R.sup.2 and R.sup.4 each may be connected to each other to form a methylene chain --(CH.sub.2).sub.n -, and the hydrogen atoms in R.sup.1 and R.sup.2 may be substituted by halogen atom, alkyloxy group or cyano group.

Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.

Abstract: A process for the preparation of tertiary diphenyl carbinols containing a primary or secondary amine substituent on the aliphatic moiety attached to the carbinol function which consists in contacting a Grignard phenyl reagent with an aminoacid wherein the mobile protons are not masked in an aprotic inert organic solvent or a mixture thereof at a temperature between 20.degree. C. and the boiling temperature by the reaction mixture.The reaction products are useful as active ingredients of medicaments and intermediates for the manufacture thereof.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is H, OH, halo, OCO(C.sub.1 -C.sub.6 alkyl), OCO(aryl), OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), OCOO(C.sub.1 -C.sub.6 alkyl), OCOO(aryl), OCONH (C.sub.1 -C.sub.6 alkyl), or OCON(C.sub.1 -C.sub.6 alkyl).sub.2 ;R.sub.2 is aryl, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or 4-cyclohexanol;R.sub.3 is O(CH.sub.2).sub.2 or O(CH.sub.2).sub.3 ;R.sub.4 and R.sub.5 are optionally CO(CH.sub.2).sub.3,CO(CH.sub.2).sub.4, C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrollidine, 3-methylpyrollidine, 3,3-dimethylpyrollidine, 3,4-dimethylpyrollidine, azepine, or pipecoline;R.sub.6 is>CH(C.sub.1 -C.sub.5 alkyl), >CH(C.sub.2 -C.sub.5 alkenyl), >C.dbd.CH(C.sub.1 -C.sub.5 alkyl), >CH(aryl), >C(OH)(C.sub.1 -C.sub.5 alkyl), >C(OH)(C.sub.2 -C.sub.5 alkenyl), C(OH)aryl;and phamaceutically acceptable salts thereof.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.

Abstract: The present invention comprises analogs of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sub.1 A.sub.2 X analogs inhibit the farnesylation of Ras. Furthermore, these CA.sub.1 A.sub.2 X analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they have a prolyl like moiety in the A.sub.1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl) or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof, for inhibiting endometriosis.

Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl) or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof, for treating restenosis.

Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl) or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof, for inhibiting aortal smooth muscle cell proliferation.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

Abstract: This invention relates to a method of inhibiting platelet aggregation, and compounds which are mimics of the peptide sequence Arg-Gly-Asp.

Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.

Abstract: In one aspect, compounds, methods of using them, compositions comprising such compounds, and uses of such compositions.These objects, and others which will become apparent from the following disclosure, are achieved by the present invention which comprises in one aspect compounds of the formula ##STR1## wherein R is alkyl, cycloalkyl, aryl, substituted aryl, alkaryl optionally substituted on the aryl portion or aralkyl optionally substituted on the aryl portion, R having up to 20 carbon atoms and is optionally branched, andA is (CH.sub.2).sub.p, (CH.sub.2).sub.q --O--(CH.sub.2).sub.r, or (CH.sub.2).sub.q --S--(CH.sub.2).sub.r,wherein p=2 to 8, q=1 to 8, and r=1 to 8.R.sub.1 =--(CH.sub.2).sub.m --, --(CH.sub.2 CH.sub.2 --O).sub.n --CH.sub.2 CH.sub.2 --, or --(CH.sub.2 CH.sub.2 CH.sub.2 --O).sub.n --CH.sub.2 CH.sub.2 CH.sub.2 --.

Abstract: Ortho-amides of the formula ##STR1## can be prepared by reacting salts of the formula ##STR2## with alcoholates of the formulaM.sup.1 OR.sup.1 (III)where the radicals R.sup.1 to R.sup.4, M.sup.1 and X.sup..crclbar. have the meaning given in the description. The alcoholates are employed in highly active form with an effective content of 98-100% M.sup.1 OR.sup.1.