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: 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: 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: 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: 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: 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: 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: 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: 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: A method of preparing an arylamine compound includes reacting a metal amide comprising a metal selected from the group consisting of tin, boron, zinc, magnesium, indium and silicon, with an aromatic compound comprising an activated substituent in the presence of a transition metal catalyst to form an arylamine. The method is useful in preparing mixtures of arylamines for use in screening for pharmaceutical and biological activity and in preparing poly(anilines).

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: 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: 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: 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: Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.

Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difiuorophenyl]-2-oxazolid inone.

Abstract: Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a tetrahydro-quinolinyl or tetrahydro-isoquinolinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

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: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH.dbd.CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.c is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl and these compounds are useful in preventing and treating skin disorders.

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 patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.3, R.sup.4, R.sup.6 and R.sup.7 each have the meanings set forth in the specification.The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.

Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.

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: There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.

Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.

Abstract: This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines.

Abstract: This invention is directed to certain 2-(alkoxycarbonylamino)- and 2-(alkoxycarbonylimino)benzlmidazole derivatives which are useful in the topical, oral or parenteral treatment of animals suffering from helminth infections.

Abstract: Compounds of formula I or I', ##STR1## wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;R.sup.1 is selected from(A) (1-6C)alkyl;(B) phenyl and naphthyl or substituted versions thereof;(C) phenyl (1-3C)alkyl and naphthyl (1-3C) alkyl;(D) five- and six-membered heteroaryl rings;(E) heteroaryl (1-3C)alkyl and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I or I' and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I or I', or a pharmaceutically acceptable salt thereof are claimed. The invention also relates to novel processes for producing enantiomeric methanoanthracenyl sulfoxides.

Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## The compounds and their pharmaceutically acceptable salts can be used as antihypertensives, agents for the treatment of glaucoma, or for increasing the flow of the retinal ocular fluid.

Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.

Abstract: The invention relates to cyclic imino derivatives of general formulaB--X.sub.5 --X.sub.4 --X.sub.3 --X.sub.2 --X.sub.1 --A--Y--E(I)whereinA, B, E, X.sub.2 to X.sub.5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.

Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: A method of treatment of Cryptococcus neoformans infection by administering to a patient in need thereof an effective amount of a benzimidazile compound.

Abstract: Compounds characterized as quinolinyl- or isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension and are of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; X is selected from oxygen atom and methylene; G is a quinolinyl or isoquinolinyl group; R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; R.sub.2 is phenylmethyl; each of R.sub.3 and R.sub.5 is hydrido; R.sub.4 is--(CH.sub.2).sub.q --C--V;V is selected from hydrido and methyl; R.sub.6 is cyclohexylmethyl; R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; q is a number selected from zero through three, inclusive; and n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

Abstract: Compounds of the formula I: ##STR1## wherein X, Y, Z, a, b, c, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined in the specification are provided. The compounds are useful as inhibitors of retroviral protease enzymes.

Abstract: The present invention relates to new pyrazole derivatives possessing an amide group substituted with an amino acid or one of its derivatives at position 3 and variously substituted in positions 1, 2, 4 or 5 of the pyrazole ring, to a process for preparing these and to pharmaceutical compositions containing the said pyrazole derivatives as an active ingredient.

Abstract: Described are guanidinocarbonyl isoquinolines of the formula I, ##STR1## wherein R(1) is hydrogen, (amino) (cyclo) (aryl)alk(en)yl (heteroaryl); R(2) is hydrogen, halogen, alkyl, or aryl; G is a radical of the formula VII: ##STR2## X(2), X(3) and X(4) are hydrogen, halogen, nitro, amino, alkyl, sulfonamide, (mono) (di) (lower alkyl) (amino), benzyloxy, hydroxy; X(1) hydrogen, oxygen, sulfur and NR(7)R(8), and their pharmaceutically acceptable salts; described is also a process for their preparation, their use as medicaments, and medicaments containing them for treating congestive heart failure, and arrhythmic conditions as well as cardioprotective agents in mammals.

Abstract: This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of using them are also covered.

Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.

Abstract: This invention provides certain novel substituted tetrahydroisoquinoline opticulisomers of the formula: ##STR1## wherein A represents the formula ##STR2## wherein R is hydrogen or halogen; R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R.sup.4 is a hydrogen atom or a lower alkylsulfonyl;with the proviso that when R.sup.1 is hydroxyl, R.sup.2 and R.sup.3 are all not hydrogen, or salts thereof.

Abstract: This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders.

Abstract: Disclosed are benzothiophene and thienothiophene derivatives useful for inhibiting urokinase activity.

Abstract: The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 (sulfonyl) or CO (carbonyl); A represents .sub.0 (oxygen), S (sulfur), or a direct bond; B represents lower alkylene; or B represents lower alkenylene or lower alkynylene provided that A represents a direct bond; X represents oxygen or sulfur, R.sub.

Abstract: A process for the preparation of isoquinolines of the formula ##STR1## wherein R is methyl or benzyl and R' is phenyl, p-hydroxyphenyl or p-methoxyphenyl, by reacting a solution of an enamine of the formula ##STR2## wherein R and R' are as described above, in a hydrocarbon with an anhydrous solution of p-toluenesulphonic acid in toluene or xylene at an elevated temperature.

Abstract: Tetrahydroisoquinoline derivatives of the following formula [I] and acid addition salts thereof, and ##STR1## (wherein in all of these formulae, R.sup.1 represents C.sub.1 -C.sub.5 straight or branched alkyl, C.sub.2 -C.sub.5 straight or branched alkenyl or C.sub.2 -C.sub.5 straight or branched alkynyl; R.sup.2 represents hydrogen atom, C.sub.1 -C.sub.10 straight or branched alkyl, C.sub.2 -C.sub.10 straight or branched alkenyl, C.sub.2 -C.sub.10 straight or branched alkynyl, C.sub.1 -C.sub.10 straight or branched alkoxy, C.sub.2 -C.sub.10 straight or branched alkenyloxy, C.sub.2 -C.sub.10 straight or branched alkynyloxy, or C.sub.1 -C.sub.10 straight or branched halogenated alkyl; R.sup.3, R.sup.4 R.sup.5 and R.sup.6, the same or different represent hydrogen atom, C.sub.1 -C.sub.10 straight or branched alkyl, C.sub.2 -C.sub.10 straight or branched alkenyl, C.sub.2 -C.sub.10 straight or branched alkynyl, C.sub.1 -C.sub.10 straight or branched alkoxy, C.sub.2 -C.sub.10 straight or branched alkenyloxy, C.sub.

Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).

Abstract: Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensinBACKGROUND OF THE INVENTIONThe United States government has rights in this invention as a result of a grant from the NIAID of the National Institute of Health, Bethesda, Md.

Abstract: 1,4-dihydropyridine derivatives of formula (I): ##STR1## wherein Ar.sup.1 and Ar.sup.2 each represent an unsubstituted or substituted aromatic hydrocarbon or aromatic heterocyclic group; and R.sup.1 represents --CO.sub.2 R.sup.2, --SO.sub.2 R.sup.3, --COR.sup.4, --CON(R.sup.5).sub.2, --CH--or --NO.sub.2 in which R.sup.2 is hydrogen, a straight chain, branched chain or cyclic saturated hydrocarbon group, which may have a substituent or a straight chain, branched chain or cyclic unsaturated hydrocarbon group having 2 to 10 carbon atoms, which may have a substituent, R.sup.3 is an alkyl group having 1 to 4 carbon atoms, R.sup.4 is an alkyl group having 1 to 4 carbon atoms or a phenyl group; and R.sup.5 is an alkyl group having 1 to 4 carbon atoms.