Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrile is directly formed.

Abstract: A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A═—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered heter

Abstract: Methods for treating sexual dysfunction, such as erectile dysfunction or sexual arousal disorder, with a compound having the generic formula X1—X2-(D)Phe-Arg-(D)Trp-X3. A particularly useful compound is HP-228, which has the formula Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH2. The invention also provides methods for selecting melanocortin receptor-3 ligands by determining whether a compound modulates the activity of MC-3 as an agonist or antagonist. These methods can be used to screen compound libraries for ligands to treat MC-3-associated conditions. Such conditions include sexual dysfunction, including erectile dysfunction and sexual arousal disorder.

Abstract: CRF antagonists of Formulas I-V, wherein the B group in the Formulas contains an oxime The variables in the Formulas have the meanings described herein.

Abstract: Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.

Abstract: Novel compounds that are useful for targeting chemokine receptors are disclosed. These compounds are complex tertiary amines.

Abstract: Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrite is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrite is directly formed.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) 1

Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: 1

Abstract: The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the structure: 1

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Abstract: The present invention provides a simple single step process for the preparation of [2,8-bis (trifluoromethyl)-4-quinolinyl]-2 -pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.

Abstract: Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.

Abstract: This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached may

Abstract: Compounds of formula: in which R represents a CR1R2, C═C(R5)SO2R6 or C═C(R7)SO2alk radical, their preparation and the pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor (“CRF receptor”) and useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.

Abstract: Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.

Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.

Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: Compounds of formula (I) which are optionally substituted 2-(&ohgr;,&ohgr;-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(&ohgr;,&ohgr;-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. Thus, the compounds are useful in the treatment of type 2 diabetes.

Abstract: This invention provides a compound of the formula (I): 1

Abstract: The present application relates to new carboxylic acid amides of general formula 1

Abstract: A chemical compound having the formula:

Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.

Abstract: Squaric acid derivatives of formula (1) are described: 1

Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ar represents substituted or unsubstituted aryl, wherein the optional substituents are selected from alkyl, hydroxy or alkoxy or, if attached to adjacent carbon atoms any two substituents together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; A represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by 1 or 2 C1-6 alkyl groups; R1 represents hydrogen, alkyl, alkenyl or cycloalkyl; one or two of of the group of R2, R3 and R4 represents nitro the remaining members of the group of R2, R3 and R4 represent hydrogen; X represents a —CO—NH— moiety; and Z represents C2-4 n-alkylene group wherein each carbon is optionally substituted 1 or 2 C1-6 alkyl groups; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compo

Abstract: The present application de gibes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.

Abstract: Propanoic acid derivatives of formula (1) are described:

Abstract: To provide a novel compound of the formula: [wherein A1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A2 is an aromatic ring which may be substituted, X is a divalent group, Y is a nitrogen atom or a methine group, Z is an ethenylene which may be substituted or ethynylene, R is a heterocyclic group which may be substituted, provided that 3,4-dihydro-6-[3-(1H-imidazol-1-yl)-1-propenyl]-2(1H)-quinolone and 2-[3-[5-ethyl-6-methyl-2-(benzyloxy)-3-pyridyl]-1-propenyl]benzoxazole are excluded.], or a salt thereof which has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating mammals suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.

Abstract: A novel 1,4-substituted cyclic amine derivative represented by the following formula: 1

Abstract: The invention concerns compounds of formula (I) wherein: A represents either a hydrogen atom or a hydroxyl group; B represents a pyrrolidin-2-yl (D) or 2-piperidyl (E), B capable of being substituted by one or two R5 groups; R1 represents a hydrogen atom, a C1-C6 alkyl, a C2-C6 alkenyl, a C1-C2 perfluoroalkyl or a C1-C6 fluoroalkyl group; R2, R3 or R4, independently of one another, represent a hydrogen atom, a C1-C6 alkyl, group or a C2-C6 alkenyl group, or R1 and R2 can together form a C1-C6 alkylene chain, or a C3-C6 alkenylene chain; R5 represents a C1-C6 alkyl group, and R6 represents a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, C3-C6 cycloalkyl, C3-C6 cycloalkenyl or a benzyl.

Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula 1

Abstract: This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ 1

Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula wherein Z1 and Z2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole; A is selected from —C(X)-amine, —C(O)—SR3, —NH—C(X)R4, and —C(═NR3)—XR7; B is —Wm—Q(R2)3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R4; Q is C, Si, Ge, or Sn; W is —C(R3)pH(2−p)—; or when Q is C, W is selected from —C(R3)pH(2−p)—, —N(R3)mH(1−m)—, —S(O)p—, and —O—; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R is independently selected from a) halo, formyl, cyano, amino, nitro, thiocyanato, isothiocyanato, trimethylsilyl, and hydroxy; b) C1-C4 alkyl, alkenyl, alkynyl,

Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Quinoline compound, zinc halogenide complex and zinc complex suited for use in an electro-luminescence (EL) element, a fluorescent material and an ultraviolet absorption material, and a preparation process for these compounds are described. These compounds and a tautomer of the same has a strong luminescent intensity and is used for an EL material, the compound of zinc halogenide complex and zinc complex and a tautomer of the same has absorption at a wave length of 400 nm or less and is used for an ultraviolet absorption material, and further the quinoline compound and a tautomer has a strong luminescent intensity and is used for a fluorescent material. The zinc halogenide complex and zinc complex can be prepared by related preparation processes directly from a quinoline derivative and a phthalimide derivative, or by way of the quinoline compound which is obtained from these derivatives.

Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.

Abstract: Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.

Abstract: Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.

Abstract: 2-Sulfamoylbenzoic acid derivatives of general formula (I): which have both an antagonistic effect on the leukotriene D4 receptor and an antagonistic effect on the thromboxane A2 receptor and salts thereof, pharmaceuticals, anti-allergic agents and leukotriene-thromboxane A2 antagonistic agents containing them as an active ingredient.

Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formulae Ia and Ib are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2 and R3 are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy-(1-6C)alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.