Abstract: The present invention relates to a compound of formula (I) which is useful for inhibiting neoplasms where the resistance is conferred in part or in total by MRP1.

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 formula (I): wherein R is hydrogen or C2-6 alkanoyl; X is halogen; and ring A is benzene ring which is optionally substituted by 1 to 4 substituents selected from {circle around (1)} halogen, {circle around (2)} hydroxy, {circle around (3)} C1-6 alkoxy optionally substituted by halogen or phenyl, {circle around (4)} C1-6 alkylthio optionally substituted by halogen or phenyl, {circle around (5)} C1-6 alkyl optionally substituted by halogen, {circle around (6)} C2-6 alkanoylamino or {circle around (7)} carboxy optionally esterified by C1-6 alkyl, or a salt thereof; which can be used for preventing or treating inflammatory disease, arthritis, chronic rheumatoid arthritis, autoimmune diseases, or rejection after organ transplantation.

Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.

Abstract: A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: Compounds of formula (I) in which the substituents have the meanings mentioned in the specification, are suitable for the prevention and treatment of gastrointestinal diseases.

Abstract: A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein:Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, heterocyclic ring containing at least one nitrogen heteroatom in a 1,3-relationship with the nitrogen atom depicted in formula I, wherein Y may be unsubstituted or substituted with at least one alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, or --COOR.sup.5 group, or a moiety selected from the group consisting of: ##STR2## wherein R.sup.5 and R.sup.7 are independently hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl.

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

Abstract: The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives of the general formula (I) and salts thereof, ##STR1## in which the radicals R.sup.1 to R.sup.5 have the meaning given in the description, and to novel 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives and processes for their preparation.

Abstract: Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also invented are intermediates and processess used in preparing these compounds.

Abstract: There is disclosed a compound of the formula (A): ##STR1## wherein W is C-G or C-G' (G is optionally esterified carboxyl; and G' is halogen); X is oxygen, optionally oxidized sulfur or --(CH.sub.2).sub.q -- (q is 0 to 5); R is optionally substituted amino or heterocyclic group; the ring B is optionally substituted nitrogen-containing 5- to 7-membered ring; L is hydrogen, optionally substituted hydrocarbon residue, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl provided that, when W is C-G, L is hydrogen, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted alkoxycarbonyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl; n is 0 or 1; the ring A may have a substituent. A process for producing the compound (A) and a pharmaceutical composition containing the compound (A) are also disclosed.

Abstract: This invention relates to bicyclic amino group-substituted pyridonecarboxylic acid derivatives of the general formulaA--Priesters thereof and salts thereof, wherein: Pri is a pyridonecarboxylic acid residue, and A is a bicyclic amino group represented by the following formula and joined to the 7-position of the pyridonecarboxylic acid or a position equivalent to the 7-position thereof. ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents a hydrogen atom, a lower alkyl group or an amino-protecting group; R.sub.3 and R.sub.4 may be the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, an oxo group, a lower alkoxy group or a lower alkyl group; and n is an integer of 0 or 1.The above-described pyridonecarboxylic acid derivatives, esters thereof and salts thereof are useful as antibacterial agents.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: Compounds of formula (I), wherein R.sub.1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15 --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: This invention provides an anti-inflammatory agent, particularly an agent for treating arthritis, and a bone resorption inhibiting agent, containing a thienopyridine or thienopyrimidine derivative or a salt thereof. This invention also provides a novel thienopyridine or thienopyrimidine derivative having anti-inflammatory activity and bone resorption inhibiting activity.

Abstract: The present invention relates to new thiazolo?3,2-a!quinoline and thiazolo?3,2-a!naphthyridine derivatives of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, Z and X have the meaning indicated in the description, processes for their preparation and their use in antibacterial compositions.

Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A.sup.1, A.sup.2 and A.sup.3 are independently carbon or nitrogen and R.sup.1, R.sup.3, R.sup.4 and R.sup.6 are known quinolone substituents; and wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety;or a protected form, salt, pharmaceutically-acceptable salt, biohydrolyzable ester, or solvate thereof;the process comprising reacting one or more organosilicon compounds with a compound having a structure according to Formula (II) ##STR2## wherein A.sup.1, A.sup.2 and A.sup.3, R.sup.1, R.sup.3, R.sup.4 and R.sup.6 as described above; wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety; and X is a leaving group;or a protected form, salt, biohydrolyzable ester, or solvate thereof.

Abstract: Compounds of general formula (Ia), (Ib) and (II), wherein R.sup.1 and R.sup.2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R.sup.3 R.sup.4 NS(O).sub.2 -- and R.sup.3 and R.sup.4 signify lower alkyl, and R.sup.2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH.sub.2 NHCH.sub.3, a bicyclic heterocycle with 1-3N atoms or a group --NR.sup.5 R.sup.6 or --OR.sup.5 in which R.sup.5 and R.sup.6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH.dbd.CH--, --CH.dbd.N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II).

Abstract: Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.

Abstract: Disclosed are new quinolone- and naphthyridonecarboxyclic acid derivatives of the formula: ##STR1## wherein T represents a radical of the formula: ##STR2## and the other radicals are as disclosed herein, for example, the compound 7-(3a-amino-1,2,3,7a-tetrahydro-isoindol-2-yl)-1-cyclopropyl-6-fluoro-1,4- dihydro-8-methoxy-4-oxo-3-quinolinecarboxyclic acid, their salts, antibacterial compositions containing them, processes for their preparation, and methods of using them to combat bacterial infections. Disclosed also are intermediates useful in said processes of preparation.

Abstract: Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the dithiocarbamate containing moiety;and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

Abstract: Antimicrobial quinolone thiourea compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the thiourea containing moietyand pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

Abstract: Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.

Abstract: Hypoxia selective cytotoxins having the structural formula ##STR1## wherein D, E, F and G, independently, are carbon or nitrogen, with the proviso that three or more of D, E, F and G are carbon; R.sub.1 and R.sub.2, independently, are selected from the group consisting of methyl, halo, hydro, trifluoromethyl, methoxy, cyano, and methylsulfo; R.sub.3 and R.sub.4, independently, are selected from the group consisting of methyl, ethyl, phenyl, naphthyl, tertiary butyl, halo, halomethylene, hydro, trifluoromethyl, cyano and methylsulfo, or R.sub.3 and R.sub.4 taken together are a substituted or unsubstituted five or six-membered nonaromatic ring system; n is an integer 1 through 5; X is carbon or nitrogen; and Z is a physiologically acceptable anion, are disclosed. The compounds are useful as radiosensitizers or chemosensitizers, especially in the treatment of cancer patients.

Abstract: In accordance with the present invention, there is provided a class of polycyclic fused ring compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.

Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.

Abstract: The present invention provides novel carbonic anhydrase inhibitors represented by the structural formula: ##STR1## wherein

Abstract: A compound of formula ##STR1## in which A represents S;R.sub.1 is selected from the group consisting of OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, phenyl, benzyl (C.sub.1 -C.sub.4)alkyl NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 ;R.sub.2 is selected from the group consisting of OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, and NZ.sub.1 Z.sub.2 ;R.sub.3 is selected from the group consisting of H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl, and benzyl;B is selected from the group consisting of phenyl; pyridyl; phenyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl or --NZ.sub.1 Z.sub.

Abstract: This invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and W are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: Compounds of the formula I ##STR1## in which X.sup.1 and X.sup.2 the same or different, signify hydrogen, a C.sub.1 - to C.sub.6 -alkyl radical or a halogen atom or, insofar as they stand in neighbouring positions, together with the carbon atoms carrying them, form a condensed-on phenyl ring, and R signifies a possibly substituted carbocyclic or heterocyclic saturated or unsaturated radical, as well as their physiologically compatible salts, processes for their preparation, as well as medicaments which contain these compounds for the treatment of allergic diseases.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: A compound of the formula: ##STR1## wherein R is an optionally substituted aryl group or an optionally substituted aromatic heterocycle group; A ring is a 5 to 9 membered alicyclic group, in which one or more of carbon atoms constituting said A ring may be replaced by O, or S and said A ring may have alkyl as a substituent, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a thienoimidazopyridone derivative represented by Formula (I): ##STR1## wherein A and B independently represent --S-- or --CH.dbd., X-Y-Z represents --N(R.sup.2)--CH.dbd.N-- or --N.dbd.CH--N (R.sup.2)-- wherein R.sup.2 is hydrogen, lower alkyl or --CH(R.sup.3)--(CH.sub.2).sub.n --R.sup.4 wherein R.sup.4 is phenyl, n is 0 or 1, and R.sup.3 is hydrogen or lower alkyl, and R.sup.1 represents lower alkyl, or a pharmaceutically acceptable salt thereof.

Abstract: This invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and W are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: Indazole arthropodicides, compositions containing them and a method for controlling arthropods employing these indazoles as the active ingredient. The indazoles have the following general formula wherein Q, X, Y, R.sub.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C.dbd.O, C.dbd.S, C-SCH.sub.3, C.dbd.NH, C-NH.sub.2, C-NHCH.sub.3, C--NHCOOCH.sub.3, or C--NHCN. B is CH.sub.2, CH, C.dbd.O, N, NH or N--CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C.dbd.O, O, N, NH or N--CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.

Abstract: Arylaminocarbonyl compounds of the formula (I) ##STR1## wherein R.sub.2-6, X.sub.1, A and m are as defined in the disclosure, intermediates therefore, synthesis thereof, and the use of said compounds for the control of weeds are described.

Abstract: Compounds selected from the group consisting of 9-amino-4-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-2-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-8-fluoro-4-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-4-oxa-1,2,3,4,5,6,7,8-octahydro-acridine or a pharmaceutical acceptable salt thereof are useful treating Alzheimer's disease.

Abstract: This invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and W are variablesThese compounds are highly selective agonists, antagonists or inverse agonists for GABA.sub.a brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Quinoline derivatives fused to a five-membered heterocyclic ring and of the formula ##STR1## where R.sup.1 is hydrogen, halogen, carboxyl or substituted or unsubstituted alkyl,Y is nitrogen or C--R.sup.2, whereR.sup.2 is hydrogen, halogen, hydroxyl, alkoxy, alkylthio, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted benzyl, phenethyl, phenyl or naphthyl, or a substituted or unsubstituted 5- or 6-membered heterocyclic ring with one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen,X is oxygen or N--R.sup.3, R.sup.3 being hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or subsituted or unsubstituted benzyl,processes for their manufacture and their use for combating unwanted plant growth.

Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 denotesa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by an optionally substituted phenyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical,a 1-piperazinyl radical substituted in the 4-position by an optionally substituted phenyl, 1,2-benzisothiazol-3-yl, 1,2-benzisoxazol-3-yl or 2-pyridyl radical,a piperidino radical substituted in the 4-position by an optionally substituted phenyl, bis(4-fluorophenyl)methylene, 4-fluorobenzoyl, optionally substituted 2-oxo-1-benzimidazolinyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, by two phenyl radicals or a hydroxyl radical and an optionally substituted phenyl radicalR.sub.2 denotes a radical SO.sub.2 R.sub.4 in which R.sub.4 denotes an alkyl or phenyl radical,R.sub.3 denotes a phenyl or naphthyl radical,or else R.sub.2 and R.sub.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treatment allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: The invention concerns pharmaceutically useful novel compounds of the formula I, in which ring B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Abstract: Compounds are disclosed of formula:R.sub.1 --(CH.sub.2).sub.n --Hetin which R.sub.1 represents a residue of formula ##STR1## X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical,Z represents an alkyl radical,n is equal to 2 or 3,Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH.sub.2).sub.m --R.sub.2 or .dbd.CH--R.sub.2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH.sub.2).sub.m --R.sub.2),m is equal to 1 or 2, andR.sub.2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.

Abstract: The present invention relates to substituted azetidinylisothiazolopyridone derivatives which correspond to the general formula I: ##STR1## or its tautomeric formula ##STR2## It also relates to a process for preparing them and to their application as a medicinal product.

Abstract: This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.