Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.

Abstract: Compounds of formula (I) in which the substituents as defined in the description are useful for preventing and treating gastrointestinal disorders.

Abstract: Novel polycyclic compounds of the formula [I], wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.

Abstract: N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R6 is an R7- and R8-substituted phenyl radical, they are active bronchial therapeutics.

Abstract: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its op

Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, arm novel active bronchial therapeutics.

Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Ar have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meaning indicated in the description, are novel active bronchial therapeutics

Abstract: Compounds of the formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are novel active bronchial therapeutics.

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 oxypyrone 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: This application relates to long-wavelength acridinium compounds having electron-donating groups, which may either be: (a) Part of an extended conjugation system attached by appropriate functional groups to the acridinium nucleus, with coplanarity of the attached functional group and the acridone moiety during light emission (geometry requirement), said functional group consisting of at least one aromatic ring and one electron-donating atom or group with an extra pair of electrons which can readily delocalize into the extended &pgr; system to which the heteroatom is directly attached or built into, and establish stable extended resonance with the electron-withdrawing carbonyl moiety of the light emitting acridone.

Abstract: Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: N-oxides of formula 1 wherein R1, R2, R3 and R4 have the meanings given in the description, are selective inhibitors of types 3 and 4 of cyclic nucleotide phosphodiesterase (PDE3, PDE4); they are useful on the one hand as bronchial therapeutics but on the other hand especially for the treatment of disorders of inflammatory nature.

Abstract: Compounds of formula I pharmaceutically acceptable salts thereof and compositions of either are useful for treating conditions amenable to treatment with a phosphodiesterase inhibitor type 4.

Abstract: The invention relates to novel dipyrano-quinolinone class of compounds having the general formula: Wherein R is hydrogen, alkyl optionally substituted about C-1 to C-10 alkenyl optionally substituted about C-1 to C-10 with one or more double bounds, alkynyl optionally substituted about C-1 to C-10 with one or more triple bonds, aryl, hetero aryl, carbocyclic aryl, alkyl aryl, alcyclic compounds, C-1 to C-6 alkyl with terminal dialkyl amino group, thio alkyl, hydroxyl alkyl groups; R1 is H, lower dialkyl amino alkyls such as methyl, ethyl, propyl, and other alkyl groups or b-amino acid moieties, hydroxy alkyl groups having optionally substituted about C-1 to C-10 carbons, acid amides such as aliphatic acids, aromatic acids, sulphonic acids trihalo acids.

Abstract: Compounds of formula (I), where R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings given in the description, are new active bronchial therapeutic agents.

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: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.

Abstract: Compounds of the formula I in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel efficacious bronchial therapeutics.

Abstract: A compound which is a bis(acridinecarboxamide) or bis(phenazinecarboxamide) derivative of formula (I): ##STR1## wherein each X, which may be the same or different in a given molecule, is --CH.dbd. or --N.dbd. each of R.sub.1 to R.sub.4 which may be the same or different, H, C.sub.1 -C.sub.4 alkyl, OH, SH, NH.sub.2, C.sub.1 -C.sub.4 alkoxy, aryloxy, NHR, N(R).sub.2, SR, SO.sub.2 R wherein R is C.sub.1 -C.sub.4 alkyl, CF.sub.3, NO.sub.2 or halogen, or R.sub.1 and R.sub.2 together form a methylenedioxy group; each of R.sub.5 and R.sub.6, which may be the same or different, is H or C.sub.1 -C.sub.4 alkyl; Z is (CH.sub.2).sub.n, (CH.sub.2).sub.n O(CH.sub.2).sub.n, (CH.sub.2).sub.n N(R.sub.7)(CH.sub.2).sub.n, (CH.sub.2).sub.n N(R.sub.7)(CH.sub.2).sub.m N(R.sub.7)(CH.sub.2).sub.n or (CH.sub.2).sub.n N(CH.sub.2 CH.sub.2).sub.2 N(CH.sub.2).sub.n wherein R.sub.7 is H or C.sub.1 -C.sub.

Abstract: This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, and cancer in a mammal.

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: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula: ##STR1## wherein: A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.

Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.

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: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: A compound of formula (I): ##STR1## in which R.sup.1, R.sup.2, X and Y are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of certain cancers.

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: New compounds of formula: ##STR1## wherein A-B, X, Y, R and n are as defined in the description. The geometric isomers, racemate and optical isomers thereof and the addition salts with pharmaceutically acceptable acids, and medicinal products containing the same are useful for treating psychotic disorders, depression, Parkinson's disease, memory disorders and disorders associated with drug abuse.

Abstract: This is described an improved process for the asymetric synthesis of (+)-Pancratistatin utilizing aziridines as the starting materials.

Abstract: A tetracyclic compound of the formula: ##STR1## wherein A and the atoms to which it is attached and the optional double bond represent a mono- or di-heterocyclic ring selected from: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are specifically defined, which compounds are useful in the treatment of dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of substance abuse and other addictive behavior disorders, cognitive impairment and attention deficit disorder.

Abstract: New compounds of formula: ##STR1## wherein A--B, X, Y, R and n are as defined in the description. The geometric isomers, racemate and optical isomers thereof and the addition salts with pharmaceutically acceptable acids, and medicinal products containing the same are useful for treating psychotic disorders, depression, Parkinson's disease, memory disorders and disorders associated with drug abuse.

Abstract: A class of 1,2,3,4,4a,5,6,10b-octahydrobenz[f]isoquinoline compounds and pharmaceutically acceptable salts of formula I: ##STR1## wherein, R.sup.1 represents hydrocarbon;R.sup.2 and R.sup.3 independently represent hydrogen, hydrocarbon, halogen, cyano, trifluoromethyl, nitro, --OR.sup.x, --SR.sup.x, --NR.sup.x R.sup.y, --CO.sub.2 R.sup.x or together represent methylenedioxy; andR.sup.x and R.sup.y independently represent hydrogen or hydrocarbon.The compounds disclosed herein are selective ligands at sigma recognition sites and are therefore useful in the treatment of psychiatric disorders.

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: A class of 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridine and 2,3,4,4a,5,6,7,11b-octahydro-1H-benzo[3,4]cyclohepta[1,2-c]pyridine derivatives are selective ligands at sigma recognition sites and are therefore useful in the treatment and/or prevention of psychiatric and/or gastrointestinal disorders.

Abstract: Compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein m is 0, 1 or 2 and n is 0 or 1;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is C.sub.1 -C.sub.6 -alkyl substituted with a heterocyclic group or C.sub.7 -C.sub.16 -arylalkyl, wherein the aryl group is unsubstituted or substituted with from one to three non-hydrogen members independently selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkyl, halo-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxy, amino and C.sub.1 -C.sub.6 -alkylamino;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, halogen, and halo-C.sub.1 -C.sub.6 -alkyl, or any two of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 taken together form a methylenedioxy group; andR.sup.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl.

Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O--or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl,andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereofand their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.

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: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

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 relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogues, and to the preparation of these compounds.The new compounds can be represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are hydrogen, or R+R.sub.1 or R.sub.1 +R.sub.2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms;R.sub.3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group;R.sub.4 is a group of the formula --C(R.sub.11).sub.2 --X--R.sub.12, wherein the groups R.sub.11 are hydrogen, or both groups R.sub.11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR.sub.14, wherein R.sub.14 is hydrogen or alkyl having 1-4 C-atoms, and R.sub.12 is hydrogen, alkyl having 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the carbamoyl group or mono- or dialkylcarbamoyl group having 1-4 C-atoms per alkyl group;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: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.

Abstract: A new antineoplastic substance denominated "pancratistatin". Methods of isolating natural and synthetic pancratistatin and 7-deoxynarciclasine and the pharmaceutically acceptable derivatives thereof to make a pharmaceutical preparation therefrom and methods for treating a host afflicted with a neoplasm with said preparations.

Abstract: A pyridine derivative represented by formula (I): ##STR1## wherein the symbols are as defined in the specification, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A.sub.2 and is useful in the treatment and prevention of a broad range of diseases.

Abstract: Certain substituted indazoles, including all geometric and stereoisomers thereof, agricultural compositions containing the indazoles and use of the indazoles as insecticides.

Abstract: A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): ##STR1## whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuration (II) over the cis configuration (III) as defined in the following formulae: ##STR2## The preferred reaction conditions include use of a borane complex as the reducing agent and an acidic solvent such as trifuloroacetic acid.

Abstract: A new antineoplastic substance denominated "pancratistatin". Methods of isolating natural and synthetic pancratistatin and 7-deoxynarciclasine and the pharmaceutically acceptable derivatives thereof to make a pharmaceutical preparation therefrom and methods for treating a host afflicted with a neoplasm with said preparations.