Abstract: The present invention concerns compounds of general formula (I): in which the substituents are as described herein.

Abstract: Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Abstract: Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided.

Abstract: The invention relates to compounds of the formula 1 1

Abstract: The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R1, R6a, R6b, R7, R8, R9, X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention is directed to compositions and methods for the treatment of patients with cephalotaxines, for example, homoharringtonine. The invention is also directed to improvements in the purity, manufacturing process, formulation and administration of homoharringtonine for the treatment of cancer and other aberrant cellular diseases. The invention also provides methods and compositions for antiparasitic, antifungal, antiviral and antibacterial treatments.

Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula (I): 1

Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.

Abstract: This invention relates to: an indole derivative or a pharmaceutically acceptable salt thereof represented by formula (I): 1

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention concerns a compound of formula (I) 1

Abstract: The present invention relates generally to compounds that inhibit serine proteases.

Abstract: Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided.

Abstract: The invention relates to benzimidazole derivatives of general formula 1

Abstract: This invention is directed to compounds of the formula (I): 1

Abstract: This invention is directed to compounds of the formula (I): 1

Abstract: Novel compounds of formula (I): wherein X1, X2, X3 and X4, n, R1, R2 and R3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are useful for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea. They are particularly useful for the treatment of obesity.

Abstract: Described herein are compounds selective for a 5-HT1D receptor, which have the general formula:

Abstract: The subject invention involves compounds having the structure: wherein each R1 is independently alkyl, aryl, or heterocycle; each R2-R7 is independently hydrogen or other substituent; B is nil and n is 0-3, or B is ethenyl and n is 0-1; and pharmaceutically acceptable forms thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases or disorders using such compounds.

Abstract: This invention concerns the use of compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X—is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH

Abstract: The subject invention involves compounds having the structure: wherein the C&agr;—N&bgr;, C5-C6, and C6-C7 bonds are each single or double bonds, except that both C5-C6, and C6-C7 are double bonds; R1 is selected from hydrogen, alkyl, aryl, and heterocycle; R2-R15 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable forms thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.

Abstract: It is provided a method for preparing the pyrroloazepine derivatives, especially in optically active form useful as drugs, by low-priced and simple method and in industrial applicable scale, represented by the following formula (I): 1

Abstract: Described are salts of hyperforin and adhyperforin of formula I [A−]m[B]p+  (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A−] is an anion of formula II with n=0 or 1 and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.

Abstract: A process for preparing epinastine hydrochloride of formula (I) the process comprising: (a) suspending and dissolving an epinastine base of formula (II)  in water by the addition of aqueous hydrochloric acid at a pH of ≧7; (b) extracting the aqueous solution obtained from step (a) with an organic, water-immiscible solvent; (c) removing the organic, water-immiscible solvent from the aqueous solution obtained from step (b); and (d) adjusting the pH of the aqueous solution of step (c) to ≦6 using hydrochloric acid to precipitate the product of formula (I), and then drying the product.

Abstract: The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.

Abstract: The invention concerns a method of sulphonation characterised in that it consists in contacting a nucleophile whose nucleophilic atom is a nitrogen atom with a reagent comprising by successive or simultaneous addition: a heavy sulphonyl halide (i.e. whose atomic number is not less than that of chlorine), advantageously suphonyl chloride; and an organic base both not capable of alkylation and lipid soluble; and the organic part of said sulphonyl is perfluorinated on the carbon carried by the sulphur. The invention is applicable to organic synthesis.

Abstract: The present invention relates to compounds of Formula (I): 1

Abstract: The invention concerns a novel method for preparing vinca-alkaloids by reacting a catharantine-type product and a vindoline-type product, characterized in that it consists in selecting the reaction conditions such that the product is oxidized.

Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.

Abstract: The invention is concerned with novel compounds of the formula the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or sulphur; R1 is hydrogen or halo; R2 is hydrogen, C1-4alkyl, phenylmethyl or halophenylmethyl; Alk is C1-4alkanediyl; —Z—A— is a bivalent radical selected from the group consisting of —S—CH2—CH2, —S—CH2—CH2—CH2—, —S—CH═CH—, —CH═CH—CH═CH—, —C(═CHR3)—CH2—CH2—CH2—, —CH═CH—O—, —CHR4—CH2—CH2—, —CHR4—CH2—CH2—CH2—, —CHR4—CH2—CH2—CH2—CH2—; in said bivalent radicals one hydrogen may be replaced by C1-4alkyl; R3 is phenyl or halophenyl; each R4 independently represents hydrogen, hydroxy, phenylmethyl or halophenylmethyl.

Abstract: A novel optically active quarternary ammonium salt with an axial chirality is provided. The quarternary ammonium salt can act as a phase-transfer catalyst to convert glycine derivatives into optically active &agr;-amino acid derivatives by stereoselectively alkylating the glycine derivatives. Furthermore, according to the present invention, intermediates useful for producing the novel quarternary ammonium can be produced.

Abstract: 9-(4-Methylthiazol-2-yl)- 11-(pyridin-4-yl)-6,7-dihydro-5H-2, 7a-diazadibenzo[a,c]cyclohepten-8-one, and pharmaceutically acceptable salts thereof, are selective ligands for GABAA receptors, in particular having high affinity for the a2 and/or a3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Abstract: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, halo, OH, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl and others; R5 is selected from the group consisting of SO2Ar, C(O)Ar, Ar and CH2Ar; R6 and R7 are independently selected from the group consisting of H, C1-6alkyl, optionally substituted phenyl and optionally substituted benzyl; ————— represents a single or double bond; n is selected from an integer of from 1-3; X is selected from the group consisting of CR17 and N; Z is selected from the group consisting of C, CH and N, provided that when ————— is a double bond, Z is C and when ————— is a single bond, Z is selected from CH and N; Ar is an optionally substituted aromatic group selected from the group consisting of phenyl, pyridyl, thienyl,

Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; ═Q is ═O or ═NR3; X is a covalent bond or —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; L is a piperidine derivative of formula (a-1) or a spiro piperidine derivative of formula (a-2); Ar1 is phenyl or substituted phenyl; Ar2 is naphtalenyl; phenyl or substituted phenyl; and Het is a monocyclic or bicyclic heterocycle; each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.

Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X— is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH2&mdas

Abstract: A compound of the general formula I; is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.

Abstract: The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R.sup.1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R.sup.2 represents hydrogen, hydroxy, or halogen; R.sup.3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.

Abstract: Compounds based on the benzoxazine ring system are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating schizophrenia, and for improving memory encoding.

Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.

Abstract: The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.

Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.

Abstract: Crystallized anhydrous zilpaterol hydrochloride having less than 5% of the crystals with a size of less than 15 microns and at least 95% of the crystals having a size of less than 250 microns and a process for its preparation and novel intermediates.

Abstract: The present invention is concerned with novel imidazoazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; --A--B-- is a radical of formula --X--CH.dbd.CH-- (a-1); --CH.dbd.CH--X-- (a-2); or --CH.dbd.CH-- CH.dbd.CH-- (a-3); X represents O, S or NR.sup.1 ; R.sup.1 represents hydrogen or C.sub.1-6 alkyl; -----Y is a radical of formula .dbd.O (b-1); --OH (b-2); or .dbd.N--OH (b-3); and L represents hydrogen, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkyloxycarbonyl, phenylcarbonyl, C.sub.1-6 alkyl or C.sub.1-6 alkyl substituted with C.sub.1-4 alkyloxycarbonyl, hydroxycarbonyl, aryl, aryloxy or a radical of formula ##STR2## --D--Z-- is --S--CH.dbd.CH--, --S--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --; and aryl is phenyl or phenyl substituted with halo, hydroxy or C.sub.1-4 alkyloxy.

Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.

Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: A process for preparation of 2-equivalent 4-arylthio-5-pyrazolone magenta couplers comprises the steps of:(i) reacting a 4-equivalent 5-pyrazolone magenta coupler and a diaryldisulfide compound in the presence of 1,8-diazabicyclo-[5,4,0]-undecen-7-ene and an organic solvent to obtain a reaction product between 4-arylthio-5-pyrazolone magenta coupler and 1,8-diazabicyclo-[5,4,0]-undecen-7-ene, and(ii) converting the reaction product with an inorganic acid into the 4-arylthio-5-pyrazolone magenta coupler.The reaction product between the 4-arylthio-5-pyrazolone magenta coupler and the 1,8-diazabicyclo-[5,4,0]-undecen-7-ene is easily formed in high yield and purity. This reaction product, which is insoluble in the reaction solvent, can be easily isolated from the reaction mixture and converted by acidification into the 2-equivalent 4-arylthio-5-pyrazolone magenta coupler in high yield and purity.