Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.

Abstract: Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 or sulfurY is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups;W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; orW is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; andZ.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 whereR.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.

Abstract: Compounds of the formula ##STR1## wherein: Q is naphthyl, heterocyclic or heterobicyclic; R.sup.1 and R.sup.2, when taken separately, are hydrogen, hydroxy, alkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, phenyl, heterocyclic or heterobicyclic; R.sup.1 and R.sup.2, when taken together, form a carbocyclic, carbobicyclic, heterocyclic or heterobicyclic group; R.sup.3 is --(CH.sub.2).sub.n COR.sup.4, tetrazolyl, alkyltetrazolyl, triazolyl, alkyltriazolyl, --(CH.sub.2).sub.n CH.sub.2 OH, --SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6 or --NHSO.sub.2 R.sup.7 ; R.sup.4 is hydrogen, hydroxy, --NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, alkoxy, alkylthio, --NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7 or --OY; n is 0 to 5; Y is a pharmaceutically acceptable cation or a group hydrolyzable under physiological conditions; R.sup.5 and R.sup.6, when taken separately, are hydrogen, alkyl, --CONRR, --COOR or --CO(C.sub.6 H.sub.5); R.sup.5 and R.sup.6, when taken together, form an azacyclic ring; R.sup.

Abstract: Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; andR.sub.5 and R.sub.6 is are optionally substituted organic substituents; orNR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups, which compounds can be used in the treatment of neuropsychological disorders.

Abstract: A process for producing a 6-substituted 2(1H)-quinoxalinone of the formula (I): ##STR1## wherein X is a halogen atom, a trihalogeno-substituted C.sub.1-5 alkyl group or a nitro group, which comprises reacting a 6-substituted 2(1H)-quinoxalinone-N-oxide of the formula (II): ##STR2## wherein X is as defined above, with an alkali metal hydrosulfide and/or an alkali metal sulfide in the presence of from 1 to 20 mol times of an alkali.

Abstract: The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises:(a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage;(b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative;(c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and(d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.

Abstract: A process for producing an dioxoquinazoline of following formula (II): ##STR1## wherein R.sub.1 and R.sub.2 independently represent a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group, an aralkyl group, an alkoxy group, an alkoxylcarbonyl group or a group represented by YNR.sub.3 R.sub.4, wherein Y represents a direct bond, a lower alkylene group or a carbonyl group, and R.sub.3 and R.sub.4 independently represent a lower alkyl group or N, R.sub.3 and R.sub.4 may bond together to form a five- or six-membered heterocycle which comprises reacting an anthranylamide of formula (I): ##STR2## wherein X, R.sub.1 and R.sub.2 are as defined above.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which one of A or B represents N and the other represents N or C--R.sub.3 ; R.sub.1 represents hydrogen, halo, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonylalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy, alkoxycarbonyl, alkanoylamino or carbamoylalkenyl; R.sub.2 represents hydrogen, alkyl, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R.sub.3 represents hydrogen or alkyl; R.sub.4 represents hydrogen, halo, alkoxycarbonyl, cyano, benzyloxycarbonyl, alkanoyl, benzoyl, alkyl, carboxy, alkylthio or carbamoyl; R.sub.5 represents hydrogen or alkyl; R.sub.9 represents hydrogen or alkyl; R.sub.10 represents phenyl, pyridyl or pyrimidinyl substituted by OR.sub.6 and optionally further substituted wherein R.sub.6 represents hydrogen, alkyl, alkoxycarbonyl or carbamoyl, alicyclic hydrocarbon, phenyl, cycloalkylalkyl, arylalkyl or pyridyl; or when R.sub.10 represents phenyl, OR.sub.

Abstract: Quinolin-2-yl benzoic acid compounds which are useful as intermediates of quinoline compounds having angiotensin II antagonist activity prepared by decarboxylating 2-(carboxyphenyl)-4-quinolinecarboxylic acid compounds in which a carboxyl group bonded to a phenyl group may be esterified, while a carboxyl group bonded to a quinoline ring is not esterified, and both rings may have one or more substituents inert to the decarboxylation reaction.

Abstract: A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido?2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts or metal complexes thereof as an effective component: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each of R.sup.1 and R.sup.2 is hydrogen, alkyl or benzyl; R.sup.3 is hydrogen, hydroxyl, dialkylaminomethyleneamino or --NH--X; X is hydrogen, alkyl, alkenyl, hydroxyl, amino, hydroxyalkyl, benzyl or acyl; R.sup.4 is hydrogen, alkyl, halogen, nitro, amino, hydroxyl, benzyloxy, cyano, carboxyl, alkoxycarbonyl, alkoxysulfonyl, aminosulfonyl, dialkylaminosulfonyl or sulfo; and R.sup.5 is hydrogen, alkyl or amino. The rapid-acting remedy for bronchial asthma is capable of relieving the symptom of laboring breath at the onset of asthma due to its excellent bronchodilating action.

Abstract: Novel amido-quinoxalinediones of the formula ##STR1## where R.sup.1 -R.sup.5, n and m have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.

Abstract: Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; andR.sub.5 and R.sub.6 is are optionally substituted organic substituents; orNR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups,which compounds can be used in the treatment of neuropsychological disorders.

Abstract: All purpose cleaning or microemulsion compositions more environmentally friendly, which is especially effective in the removal of a mixture of oil and kaolin soil, contains an analephotropic negatively charged complex, a hydrocarbon ingredient, a cosurfactant, and water.

Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1,2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;R.sup.1 is (1-4C)alkoxy;A is (1-4C)alkylene; andQ is a saturated, monocyclic 4-, 5-, 6- or 7-membered heterocyclic ring containing one or two oxygen heteroatoms, which ring optionally bears up to four (1-4C)alkyl substituents; or a pharmaceutically-acceptable salt thereof;processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.

Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;R.sup.3 is (1-4C)alkoxy; andR.sup.1 is di-?(1-4C)alkyl!amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-?(1-4C)alkoxy-(2-4C)alkyl!amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R.sup.1 substituents comprising a CH.sub.2 (methylene) group which is not attached to a N or O atom optionally bears on said CH.sub.

Abstract: A compound represented by the general formula: ##STR1## wherein Y represents a nitrogen atom or C--G (G represents a carboxyl group which may be esterified); ring R is a nitrogen-containing unsaturated heterocyclic group which may be substituted for; each of rings A and B may have a substituent; n represents an integer from 1 to 4; k represents the integer 0 or 1, or a salt thereof, which serves well as an anti-inflammatory agent, particularly a therapeutic agent for arthritis.

Abstract: The present invention provides anti-neoplastic topoisomerase I inhibitors of the formula: ##STR1## wherein Ar is (C.sub.6 -C.sub.12)aryl or (5- to 12-membered) heteroaryl comprising 1-3 N, S or non-peroxide O, wherein N is unsubstituted or is substituted with (C.sub.1 -C.sub.4)alkyl; X is H, CN, CHO, OH, acetyl, CF.sub.3, O(C.sub.1 -C.sub.4)alkyl, NO.sub.2, NH.sub.2, halogen or halo-(C.sub.1 -C.sub.4)alkyl; each Y is individually H, (C.sub.1 -C.sub.4)alkyl or aralkyl; Y' is H or (C.sub.1 -C.sub.4)alkyl; n is 0 or 1; and each Z is individually H, (C.sub.1 -C.sub.4)alkyl, halogen or halo(C.sub.1 -C.sub.4)alkyl; or a pharmaceutically acceptable salt therein.

Abstract: N.sub.1 -(1,2-cis-2-halogenocydopropyl)-substituted pyridonecarboxylic acid derivatives represented by formula (I) and the salts thereof are disclosed. These compounds have patent antibacterial activities against a wide variety of infectious bacteria, and are useful as antibacterial agents by oral or parenteral administration.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; and g is 0, 1, 2, 3 or 4;R.sub.1, R.sub.2, R.sub.3, R.sub.4, U, Q and T are defined in claim 1.The compounds have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.