Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.

Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.

Abstract: A hydrazine compound of the formula (I) or its salt: ##STR1## wherein A is a benzofuranyl group which may be substituted, a quinolinyl group which may be substituted, a benzothienyl group which may be substituted, a benzothiazolyl group which may be substituted, a thienothienyl group which may be substituted, a dihydrothienothienyl group which may be substituted, a dihydrocyclopentathienyl group which may substituted, a tetrahydrobenzothienyl group which may be substituted, an indanyl group which may be substituted, or a hexahydroindanyl group which may be substituted, W is a hydrogen atom, a cyano group, --COCOOR', --S--N(R")COOR' or --CH.sub.

Abstract: The present disclosure describes novel peptidomimetic compounds which contain a novel class of isosteres and which inhibit the proteolytic activity of HIV protease and further describes therapeutic compositions comprising said compounds, a method of treatment for patients having the AIDS virus involving administering a therapeutically effective amount of the novel compounds of the present invention, and a method of preparation for said isosteres.

Abstract: Bifunctional chelating agents based on substituted 8-hydroxy-2-carboxamidoquinolines and their chelates are provided together with processes for their preparation. The agents can react with a variety of biological substrates and/or chelate with a variety of transition metals providing useflu in vivo agents for localizing radioactivity where needed for diagnostic or therapeutic purposes.

Abstract: Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclylcarboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.

Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the nitrogen and carbon atoms to which it is bound, a heterocycle,B represents, with the nitrogen atom to which it is bound, a heterocycle,R.sub.1 represents alkoxy, benzyloxy, phenoxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or substituted or unsubstituted cycloalkyl,their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid, medicinal products containing the same.

Abstract: Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.

Abstract: Compounds having the Formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## wherein X represents ##STR2## R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group, an alkoxyl group, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group, ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom or an alkyl group which may be substituted by a hydroxyl group; R.sub.7 represents a hydrogen atom, an alkyl group, an alkyoxyl group, a hydroxyl group, a halogen atom, a nitro group, a cyano group, ##STR4## wherein -A represents ##STR5## and R and R' represent independently a hydrogen atom or an alkyl group; and R.sub.10 to R.sub.12 represent independently a hydrogen atom or an alkyl group, a process for producing such compounds, and a medium for recording optical information using these compounds.

Abstract: Quinolinecarboxylic acid derivatives of the formula: ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is independently of the other hydrogen or halogen,R.sup.3 is C.sub.1 -C.sub.13 -alkoxy, C.sub.1 -C.sub.8 -monoalkylamino or di(C.sub.1 -C.sub.8 alkyl)amino andR.sup.4 and R.sup.5 are identical or different and each is independently of the other hydrogen, C.sub.1 -C.sub.13 -alkyl or C.sub.1 -C.sub.13 -alkoxy,with the proviso that R.sup.3 is not methoxy or ethoxy when at the same time R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each hydrogen, are useful as color formers for preparing pressure-sensitive papers.

Abstract: The present invention relates to novel dihydroquinoline derivatives, pharmaceutical compositions and methods of use of dihydroquinoline derivatives as modulators of the arachidonic acid cascade. The novel dihydroquinoline derivatives of this invention are useful for the treatment of diseases, such as asthma, where products of the arachidonic acid cascade contribute to the disease.

Abstract: Compounds of formula ##STR1## in which R.sub.1 represents H, an alkyl or a substituted alkyl, R.sub.2 represents H or alkyl and R.sub.3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R.sub.2 and R.sub.3 considered together represent the group ##STR2## which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases.Use of these compounds as medicaments.No figure.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulphonyl, arylsulphonyl, monoaralkylcarbamoyl, cinnamoyl or .alpha.-aralkoxycarbonylaminoalkanoyl and R.sup.2 is hydrogen or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a cyclic imide group of the formula ##STR2## in which P and Q together represent an aromatic system; R.sup.3 is alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkyl- sulphinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl or, when n stands for zero, R.sup.3 can also represent alkylthioalkyl or, when n stands for 1, R.sup.3 can also represent alkylsulphonylalkyl; R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R.sup.5 is hydrogen and R.sup.6 is hydroxy or R.sup.5 and R.sup.6 together represent oxo; R.sup.7 and R.sup.

Abstract: A dihydropyridine.revreaction.pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain. A chelating agent capable of chelating with a radionuclide and having a reactive hydroxyl, carboxyl, amino, amide or imide group is coupled to a carrier moiety comprising a dihydropyridinie.revreaction.pyridinium salt nucleus and then complexed with a radionuclide to provide a new radionuclide pharmaceutial that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier (`BBB`) and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated. This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.

Abstract: This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.

Abstract: Novel antibacterial compounds are disclosed having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amide and prodrugs thereof,wherein R.sup.1 is selected from the group consisting of (a) lower alkyl, (b) halo(lower alkyl), (c) lower alkyl(alkynyl), (d) lower cycloalkyl, (e) lower alkylamino, (f) nitrogen-containing aromatic heterocycle, (g) bicyclic alkyl and (h) phenyl;R.sup.2 is selected from the group consisting of hydrogen, lower alkyl, a pharmaceutically acceptable cation, and a prodrug ester group;R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, amino, and lower alkyl;R.sup.5 is either a nitrogen-containing heterocycle or a nitrogen-containing spiro-bicyclic-heterocycle; andA is N or C--R.sup.6, wherein R.sup.6 is selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy, or R.sup.1 and R.sup.

Abstract: A dihydropyridine.revreaction. pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine.revreaction. pyridinium salt redox system and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated. This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.

Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.

Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.

Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.

Abstract: The invention relates to a quinoline of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, halogeno, hydroxy, cyano, carbamoyl, nitro or amino, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino or alkanoylamino each of up to 4 carbon atoms, or substituted alkyl or alkoxy each of up to 3 carbon atoms, provided that both R.sup.1 and R.sup.2 are not hydrogen; the quinoline ring may bear further substituents; R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms; R.sup.4 is hydrogen, alkyl, alkenyl or alkynyl each of up to 4 carbon atoms or substituted alkyl of up to 3 carbon atoms; Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or which bears one or more substituents; R.sup.5 is such that R.sup.5 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.

Abstract: Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.

Abstract: Quinoline-4-carboxylic acids derivatives are useful as dye-forming components for pressure- and heat-sensitive recording materials and have of the general formula I ##STR1## where one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen while the other two are each independently of each other hydrogen, fluorine, chlorine, bromine, linear or branched C.sub.1 -C.sub.5 -alkyl, hydroxyl, C.sub.1 -C.sub.10 -alkoxy, which may be interrupted in the alkyl by 1 or 2 oxygen atoms, or is ##STR2## R.sup.7 is hydrogen, methyl or ethyl and R.sup.8 is C.sub.1 -C.sub.4 -alkanoyl, benzoyl, p-chlorobenzoyl, C.sub.1 -C.sub.6 -alkyl, benzyl or p-chlorobenzyl, orR.sup.1 and R.sup.2 together are a fused-on benzene ring,R.sup.2 and R.sup.3 together are unsubstituted or C.sub.1 -C.sub.4 -alkyl-substituted methylenedioxy or ethylenedioxy,R.sup.4 is hydroxyl, C.sub.1 -C.sub.10 -alkoxy, which may be interrupted by 1-4 oxygen atoms, or unsubstituted or chlorine-substituted phenyl-C.sub.1 -C.sub.2 -alkoxy,R.sup.5 is hydroxyl or C.sub.1 -C.sub.

Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Abstract: The invention relates to the compounds of general formula: ##STR1## in which: X denotes either an oxygen atom, or two hydrogen atoms;Y denotes either a hydrogen atom, or a hydroxyl group;or Y denotes an amino group on condition that X denotes two hydrogen atoms;R denotes a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms, optionally substituted with one or more hydroxy, amino, mercapto, methylthio or carboxy groups, or aryl groups such as phenyl, pyridyl or thienyl; ##STR2## denotes a polycyclic nitrogenous structure; their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.

Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## (wherein X represents ##STR2## Y represents C.dbd.O, C.dbd.C(CN).sub.2 or SO.sub.2 ; R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group which may be substituted, an alkoxyl group which may be substituted, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group which may be substituted, --A--R or ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom, an alkyl group which may be substituted, an aryl group which may be substituted or a cyclohexyl group; R.sub.5 and R.sub.6 may be combined to form a ring or may form a ring with a hetero atom; R.sub.7 and R.sub.

Abstract: The present invention provides linear, cyclic and trifurcate tri- and tetramine backbone multidentate chelating agents based on the 8-hydroxyquinoline chelating unit. The chelating agents may optionally be substituted with a substate reactive moiety and antibody-metal ion conjugates may be produced for in vivo diagnostic and therapeutic methods.

Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.

Abstract: In general, the invention features compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein AR is an indolyl, quinolyl, naphthyl or a mono- or di- R.sup.1 substituted naphthyl in which R.sup.1 is, independently, an alkyl group having 1-5, inclusive, carbon atoms, an alkoxy group having 1-5, inclusive, carbon atoms, a halogen, amino, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, ethyl carboxylate, or a hydrogen; m is an integer between 0 and 2, inclusive; and A is either ##STR2## where n is an integer between 1 and 5, inclusive, and R.sup.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.

Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.

Abstract: The present invention are novel 3-aminopropoxyaryl derivatives, compositions and methods of use thereof for treating congestive heart failure, coronary heart disease, or myocardial ischemia.

Abstract: A compound of the formual (I) ##STR1## or 1-oxide or salt thereof, whereinR.sub.1 is a C.sub.1-11 alkyl group, a lower alkenyl group, a phenyl or group which may be substituted, an aralkyl group whose nucleus may be substituted, a haloalkyl or a 5- or 6-membered heterocycle group;R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are, the same or different, hydrogen atom, a halogen atom, cyano group, nitro group, amino group, a lower alkyl group, a lower haloalkyl group, hydroxy group, a lower alkoxy group, an aryloxy group, carboxy group or a lower alkoxycarbonyl group;R.sub.7 is hydrogen atom, a halogen atom, a lower alkyl group, a phenyl group which may be substituted, an aralkyl group whose nucleus may be substituted, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group or a haloalkyl group;R.sub.8 is a C.sub.

Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.

Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein Y is S or O;R is hydrogen or alkyl having from about 1 to about 4 carbon atoms;R.sup.1 is hydrogen, alkyl having from about 1 to about 4 carbon atoms, alkoxy having from about 1 to about 4 carbon atoms, halogen or trifluoromethyl;R.sup.2 is hydrogen or unsubstituted or substituted alkyl having from about 1 to about 4 carbon atoms; andR.sup.3 is hydrogen, alkyl having from about 1 to about 6 carbon atoms, cycloalkyl having from about 3 to about 6 carbon atoms, alkoxy having from about 1 to about 4 carbon atoms, aryloxy having from about 6 to about 10 carbon atoms, alkylthio having from about 1 to about 4 carbon atoms, hydroxyalkoxy having from about 1 to about 4 carbon atoms, or unsubstituted or substituted phenyl is useful to obtain inhibition of aldose reduction in animals, including humans.

Abstract: A hydroquinoline compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, A, l, m and n are as defined or its pharmaceutically acceptable salt, composition containing the compound and processes for preparing same are disclosed. The compound is useful as an antiulcer agent.

Abstract: A method of preparing a labelled specific binding partner, such as a biological probe in the form of an antibody or oligonucleotide probe, using a protected label (the corresponding unprotected label being susceptible to inactivation, such as by hydrolysis to yield a non-chemiluminescent form of the label). The specific binding partner is linked to the label, and an adduct of the label is prepared using a protective adduct former which produces a protected label which is less susceptible to inactivation. Particularly preferred labels are the acridiniums and acridans, most preferably the former having the general structure: ##STR1## wherein the phenyl rings are optionally additionally substituted, R.sub.1 is preferably an alkyl, and R.sub.5 is an optionally substituted hydrocarbon, most preferably a phenyl moiety which is either linked to the specific binding partner, or capable of being linked thereto.

Abstract: A quinoline derivative represented by the following formula is disclosed. ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group which may contain a substituent and R.sub.2 represents an alkyl group which may contain a substituent, or R.sub.1 and R.sub.2 in combination with each other and with the adjacent nitrogen atom from a ring which may contain a nitrogen atom other than said adjacent nitrogen atom, an oxygen atom, or a substituent, and R.sub.3 represents a cyano group, a carbamoyl group, or a lower alkoxycarbonyl group. The compound exhibits superior cardiotonic activity and vasodilative activity, and thus is effective as a medicine.

Abstract: A compound of the formula I ##STR1## where A is nitro, amino, halocarbonyl or halosulfonyl, R is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkanoylamino, hydroxyl, C.sub.1 -C.sub.4 -alkoxy phenoxy which is unsubstituted by methyl or chloro, mercapto, C.sub.1 -C.sub.4 -alkylthio, phenylthio which is unsubstituted or substituted by ethyl, fluoro, or methoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, phenoxycarbonyl which is unsubstituted or substituted by isopropyl, bromo, or methoxy, carbamoyl, hydroxysulfonyl, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl which is unsubstituted or substituted by ethyl, chloro, or isopropoxy, sulfamoyl or trifluoromethyl or is C.sub.1 -C.sub.4 -alkyl which may be substituted by hydroxyl, C.sub.1 -C.sub.4 -alkoxy or halogen, and X and Y are each, independently of one another, halogen, hydroxysulfonyl, C.sub.1 -C.sub.

Abstract: The present invention provides an improved process for the preparation of o-carboxypyridyl- and o-carboxyquinolylimidazolinones from their 2-methyl-o-carboxylate pyridine and quinoline precursors.

Abstract: According to the present invention, there are provided novel carboxystyrene derivatives of the general formula (I): wherein the symbols are as defined hereinabove. Also provided herein are leukotriene antagonists and phospholipase inhibitors containing the carboxystyrene derivative or pharmaceutically acceptable salt thereof as an effective ingredient.

Abstract: The invention is novel 2-carbamoylnicotinic and 3-quinolinecarboxylic acids and esters which are intermediate compounds for the preparation of 2-(2-imidazolin-2-yl)pyridine and quinoline herbicides.

Abstract: The novel class of substituted quinolines represented by the general formula (I): ##STR1## where each of R.sub.1 and R.sub.2 separately represents H or up to three of the groups lower alkyl, halogen, CF.sub.3, CN, SO.sub.2 CH.sub.3, NO.sub.2, OH, NH.sub.2, NHSO.sub.2 R.sub.3, NHCOOR.sub.3, OR.sub.3, SR.sub.3, NHR.sub.3 or NR.sub.3 R.sub.3 (where R.sub.3 is lower alkyl optionally substituted with hydroxy, amino or ether functions), and each of R.sub.1 and R.sub.2 may additionally separately represent the substitution of an aza (--N.dbd.) group for one or two of the methine (--CH.dbd.) groups in each of the carbocyclic rings, and R.sub.1 may also represent, at positions 2', 3' or 4' only, a phenyl ring optionally further substituted with lower alkyl, halogen, CF.sub.3, CN, SO.sub.2 CH.sub.3, NO.sub.2, OH, NH.sub.2, NHCOR.sub.3, NHCOOR.sub.3, OR.sub.3, SR.sub.3, NHR.sub.3 or NR.sub.3 R.sub.3 (where R.sub.3 is lower alkyl optionally substituted with hydroxy, amino or ether functions);Y represents C(NH)NH.sub.

Abstract: New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.

Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R is hydrogen, lower alkyl, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di-lower alkylamino, nitro, hydroxy, carboxy, lower alkoxycarbonyl, lower alkoxy or halo;R.sup.2 is hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other inflammatory conditions.

Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.