Abstract: A process for the racemization of optically active amines of the formula (I), where Ar is an unsubstituted or substituted aryl and R is alkyl, in whicha) (I) is reacted with the ketone (II) in which Ar and R have the same meanings as for (I), to give the condensation product (III), ##STR1## b) (III) is racemized by treatment with base, ##STR2## c) the arylalkylamine (I) is liberated as racemate from racemic (III) by reaction with optically active (I).

Abstract: The present invention relates to a process for preparing N-methyl-3-(p-trifluoromethylphenoxy)-3-phenyl-propylamine and pharmaceutically acceptable acid addition salts thereof. The process in accordance with the present invention comprises reacting 1-phenyl-3-(N-methylamine) propane-1-ol with 1-chloro-4-trifluoromethylbenzene, in the presence of an hydroxide of an alkaline metal in a dipolar aprotic solvent non saponifiable in reaction conditions. The process in accordance with the present invention further comprises a final crystallization step which allows to obtain the active ingredient in a highly pure crystalline form.

Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein A is an optionally substituted phenyl naphthyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidyl, thienyl, thiazolyl, oxazolyl, thiadiazolyl having at least two adjacent ring carbon atoms or a bicyclic ring system, provided that the --CH(R.sup.3)N(R.sup.2)B--R.sup.1 and --OCH(R.sup.4 --)--D linking groups arm positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the --OCHR.sup.4 -- linking group (and therefore in the 3-position relative to the --CHR.sup.3 NR.sup.2 -- linking group) is not substituted; B is an optionally substituted ring system; D is an optionally substituted ring system; R.sup.1 is a variety of group as defined in the description; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenylC.sub.1-3 alkyl or 5- or 6-membered heteroarylC.sub.1-3 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is hydrogen or C.sub.1-4 alkyl; and N-oxides of NR.

Abstract: In accordance with the present invention, there is provided a phenanthrylenediamine derivative represented by the general formula (1). The derivative is excellent in the electric charge transferring capability, the compatibility with a binding resin and the stability, thereby providing a photosensitive material which is highly sensitive and excellent in the durability. ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent a halogen atom, an alkyl group, an alkoxy group or an aryl group; and a, b, c and d each represent an integer from 0 to 5!.

Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or radiation therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH agonist, either simultaneous with or subsequent to LHRH antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH antagonist. Methods for inhibiting the LHRH agonist-induced hormone surge, whatever its clinical setting, are also disclosed. These methods generally involve administration of an LHRH-antagonist in combination with the LHRH agonist.

Abstract: The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy dihydrobenzindole oligopeptides and prodrugs thereof wherein the monomeric constituents are derived from monocyclic or bicyclic heterocyclic aromatic residues.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

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

Abstract: A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, ##STR1## wherein W represents sulfur or oxygen and X represents --N(R.sup.1)--, or alternatively X represents sulfur or oxygen and W represents --N(R.sup.1)--, and R.sup.1 represents hydrogen, alkyl or substituted alkyl; R.sup.2 and R.sup.3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R.sup.4 represents hydrogen, alkyl or substituted C.sub.1 -C.sub.4 alkyl; R.sup.5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include --B--ONO.sub.2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.

Abstract: A diamine compound of the following formula (1): ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group, each of A.sub.1, A.sub.2 and A.sub.3 which are independent of one another, is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a group of the following formula (2): ##STR2## wherein R.sub.1 is as defined above, and X is a substituted or unsubstituted arylene group or a substituted or unsubstituted heterocyclic bivalent group.

Abstract: Odor formation during storage of (hydrocarbylthio)aromatic amines due to formation and release of odoriferous sulfur-containing species such as dihydrocarbyldisulfides, is suppressed. To accomplish this, a small amount of N,N-dihydrocarbylhydroxylamine odor-inhibitor (e.g., N,N-diethylhydroxylamine) is blended with the (hydrocarbylthio)aromatic amine. This enables products such as a mixture of 3,5-di(methylthio)-2,4-diaminotoluene and 3,5-di(methylthio)-2,6-diaminotoluene) to be stored for long periods of time with significantly reduced formation and release of odoriferous sulfur-containing species.

Abstract: The invention provides compounds, several of which belong to a class having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concents a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effective to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity.

Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIII, General Formula CIV, and General Formula CVI. In one embodiment, the reagents of General Formula CIII may be used to produce, after condensation with a bioactive species (BAS), the reagent of General Formula CIV. The reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI.

Abstract: The invention is directed to phosphoramidite derivatives of macrocycles, such as porphyrins and expanded porphyrins, including sapphyrins and texaphyrins. The phosphoramidite derivatives are useful as intermediates in the preparation of macrocycle-oligonucleotide conjugates.

Abstract: A drug containing a calmodulin inhibitor as an active ingredient is disclosed. This drug is useful in the suppression of neuronal cell death, in particular brain neuronal cell death, due to, for example, cerebral ischemia.Also, a drug containing a compound capable of inhibiting binding of calmodulin to a cytoskeltal protein as an active ingredient and a drug containing a compound suppressing the breakdown of a cytoskeltal protein as an active ingredient are disclosed.These drugs are useful in the treatment and prevention of various diseases in the brain and sequelae thereof as well as in the prevention of relapses of these diseases.

Abstract: The present invention relates to a triazole compound represented by the formula (1): ##STR1## wherein R.sup.1 represents a lower alkyl group which may have a substituent; R.sup.2 and R.sup.3 represent respectively hydrogen, an aryl group, a benzoyl group, a tosyl group, a lower alkoxy carbonyl group, or an aryl sulfonyl group, each of which except for hydrogen may have a substituent; provided that when R.sup.2 is hydrogen, the triazole compound is represented by the formula (2): ##STR2## wherein R.sup.1 and R.sup.3 have the same as defined above.

Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.

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.