Abstract: The present invention relates to novel 4-substituted quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: wherein R1, R2, R3, R4, R5, R6, R7, R9, and Y, have the meanings provided.

Abstract: It has been found that one of the enantiomers of 8-aminoquinoline antiparasitic compounds is surprisingly more active than the other enantiomer against parasitic infections including opportunistic parasitic infections. These enantiomers as well as pharmaceutical compositions containing pure enantiomers are disclosed. Also disclosed is a novel class of 8-aminoquinolines which contain a tri-substituted phenoxy substitution.

Abstract: The invention relates to compound of formula (I): 1

Abstract: 1,3 Diazines according to formula (I): and pharmaceutically acceptable salts thereof inhibit phosphorylation of platelet-derived growth factor receptor and thereby hinder abnormal cell growth and cell wandering. The compounds may be used to treat or prevent cell-proliferative disorders such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

Abstract: A heterocyclic derivative of the formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.

Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The invention relates to a pharmaceutical composition for ophthalmic administration comprising a compound of the formula: wherein X1, X2, X3, R1, R2, R3, R4, R5, Q and A are as defined in the disclosure. This invention also relates to methods of using the pharmaceutical composition in the prevention and/or treatment of bradykinin or its analogues mediated diseases in the eye, such as allergy, inflammation and pain of the eye.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B.sub.2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) ##STR1## in which R.sup.1,R.sup.2,R.sup.3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, CO--O-alkyl, COOH; R.sup.4, R.sup.5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R.sup.6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R.sup.7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.

Abstract: The present invention relates to an improved Skraup reaction process wherein pressure is applied during the reaction and the number of equivalents of sulfuric acid utilized is reduced.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: This invention relates to a quinoline compound of the formula: ##STR1## wherein R.sup.1 is a pyridyl group or aryl, each of which may be substituted with suitable substituent(s),A is --COHN-- or --NHCO--,n is an integer of 0 or 1, and ##STR2## is a group of the formula: ##STR3## In which R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined,and pharmaceutically acceptable salt thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prevention and/or the treatment of bone diseases caused by abnormal bone metabolism in human being or animals.

Abstract: A method for forming a color image comprises the step of developing an image-wise exposed silver halide color photographic photosensitive material at the presence of a 6-aminotetrahydroquinoline color developing agent which is the following compound or its analoge. According to this method, the rapid process can be attained and an image of a low fog density can be obtained.

Abstract: Disclosed are 4-(N,N-dialkylamino)aniline compounds having a 4-N substituent which is a polyethyleneoxy group and which forms a condensed ring with benzene ring, such as aniline compounds having the following structure, a processing composition containing such a compound and a method for forming a color image with the processing solution. The aniline compound is useful as a color developing agent capable of having a low fog density and sufficient yellow and cyan image densities and suitable for the rapid process.

Abstract: The invention concerns compounds of formula I ##STR1## wherein the substituents have various meanings, and their use in the prevention or treatment of inflammatory and proliferative skin diseases and cancer.

Abstract: New isoquinoline derivatives and pharmaceutically acceptable acid addition salts represented by the following general formula (I) ##STR1## wherein Ar is an aromatic ring which may be substituted, and n shows 0, 1 or 2, have an inhibitory activity against apoptotic neuronal cell death. These compounds are useful for agents of prevention and treatment of neuronal neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, Huntington's chorea and amyotrophic lateral sclerosis, cerebral ischemic injury such as stroke, and peripheral neuropathy in diabetes mellitus.

Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

Abstract: The invention relates to novel heteroaryl-oxazolidinones of the general formula (I): ##STR1## in which the substituents are as defined in the description, to processes for their preparation and to their use as drugs, especially as antibacterial drugs.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: The present invention relates to novel photosensitive quinolone compounds, specifically novel 3-diazo 2,4-quinolinedione compounds, that may be used in a variety of applications, such as, photosensitive coating compositions, pharmaceuticals, agricultural, amongst others. The invention further relates to a process for making the novel photosensitive 3-diazo 2,4-quinolinedione compounds. These compounds are particularity useful as a photoactive component in a positive working photoresist composition, particularity for use as a deep ultraviolet (UV) photoresist.

Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.

Abstract: Methine dyes of the formula ##STR1## where K is a carbocyclic or heterocyclic radical,X is nitrogen or a radical of the formula C--Q.sup.1, andQ.sup.1, Q.sup.2 and Q.sup.3 are hydrogen, substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, substituted or unsubstituted phenoxy, C.sub.1 -C.sub.6 -alkylthio, halogen, cyano, formylamino or a radical of the formula R.sup.3, --CO--OR.sup.1, --CO--NHR.sup.1, --CO--NH--CO--R.sup.1, --CO--NH--CO--R.sup.3, --CO--NH--SO.sub.2 R.sup.3, --NH--CO--R.sup.1, --NH--CO--OR.sup.1, --NH--CO--NR.sup.1 R.sup.2, NH--CS--OR.sup.1, --NH--CS--NR.sup.1 R.sup.2, --NH--CO--R.sup.3, --NH--SO.sub.2 --R.sup.1, --NH--SO.sub.2 --R.sup.3 or --NH--SO.sub.2 --NR.sup.1 R.sup.2, wherein R.sup.1 and R.sup.2 are substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl or substituted or unsubstituted phenyl, or else --NR.sup.1 R.sup.2 is amino, and R.sup.

Abstract: Azamethine dyes of the formula ##STR1## where W is oxygen, sulfur or a radical of the formula --NH--CO--, --NH--COO-- oder --NH--SO.sub.2 --,Z.sup.1 is C.sub.1 -C.sub.4 -alkyl with or without substitution, phenyl or C.sub.1 -C.sub.4 -alkoxy,Z.sup.2 and Z.sup.3 are each hydrogen or C.sub.1 -C.sub.4 -alkyl with or without substitution, provided --CZ.sup.1 Z.sup.2 Z.sup.3 is not linear and is not isopropyl,Z.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,Z.sup.5 and Z.sup.6 are each C.sub.1 -C.sub.10 -alkyl with or without substitution, C.sub.3 -C.sub.4 -alkenyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl or tolyl, or together with the nitrogen atom joining them together a heterocyclic radical or Z.sup.4 and Z.sup.5 are together a bridge member, andT is a radical of a cyclic acidic--CH compound H.sub.2 T,are useful for thermal transfer.

Abstract: The subject invention relates to compounds having the structure: ##STR1## as defined in the claims, and to pharmaceutical compositions containing such compounds, and the use of such compounds for preventing or treating of disorders modulated by alpha-2 adrenoceptors.

Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.

Abstract: Substituted quinoline compounds, processes for their preparation, composition containing them, and their use as safenersCompounds of the formula I and salts thereof ##STR1## in which R.sup.1 ?lacuna! CN, C(.dbd.Z)--Q(A.sub.i X.sub.i).sub.q --R, --C(.dbd.Z)--QR*, 1,2,3,4-tetrazol-5-yl, 1,3,4-triazol-2-yl, 1,3-oxazol-2-yl,and the remaining radicals are as defined in claim 1, are suitable for use as safeners for protecting crop plants such as, for example, cereals, rice and maize, against herbicide damage.Some of the compounds are known and some are novel and they can be prepared from quinolin-8-oxy derivatives by the processes of claim 7.

Abstract: Quinoline analogs of mevalonolactone of the following formula are useful as anti-cholesterol synthesis agents: ##STR1## where the substituents are as defined in the specification.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: Methine dyes of the formula I ##STR1## where R is hydrogen, unsubstituted or substituted C.sub.1 -C.sub.10 -alkyl or unsubstituted or substituted phenyl,X is nitrogen or a radical of the formula CQ.sup.1, CH.dbd.CQ.sup.1 --CH, CH.dbd.CH--CH.dbd.CH--CH, ##STR2## where Q.sup.1 is hydrogen, C.sub.1 -C.sub.4 -alkyl, chlorine or bromine and Q.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl, andY is a radical of the aniline, aminonaphthalene, indole, aminoquinoline, aminothiazole or aminothiophene series,the use thereof in nonlinear optics, and novel thiazole derivatives.

Abstract: A compound of the formula: ##STR1## or its salt is prepared by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## Wherein the variables are all defined in claim 1.

Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.

Abstract: Pyridone dyes useful for thermal transfer have the formula ##STR1## where R.sup.1 is hydrogen or C.sub.1 -C.sub.4 - alkyl,R.sup.2 and R.sup.3 are identical or different and each is, independently of the other, hydrogen, substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl, substituted or unsubstituted C.sub.1 -C.sub.12 -alkanoyl, C.sub.1 -C.sub.12 -alkoxycarbonyl, substituted or unsubstituted C.sub.1 -C.sub.12 -alkylsulfonyl, C.sub.5 -C.sub.7 -cycloalkylsulfonyl, substituted or unsubstituted phenylsulfonyl, substituted or unsubstituted pyridylsulfonyl, substituted or unsubstituted benzoyl, pyridylcarbonyl or thienylcarbonyl or are together with the nitrogen atom to which they are bonded unsubstituted or C.sub.1 -C.sub.4 - alkyl-substituted succinimido, unsubstituted or C.sub.1 -C.sub.

Abstract: Novel benzene derivatives are provided of the general formula (I): ##STR1## [wherein R.sup.1 represents an amino group, a substituted amino group, a protected amino group, or a nitro group; R.sup.2 represents an amino group, a substituted amino group, a protected amino group, a hydroxy group, a substituted hydroxy group, or a protected hydroxy group; R.sup.3 represents an amino group, a substituted amino, a heterocyclyl group having a ring nitrogen atom as the point of binding, or a substituted heterocyclyl group having a ring nitrogen atom as the point of binding; m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n represents an integer from 2 to 6] and salts thereof.Compounds of formula (I) except those wherein R.sup.1 is a nitro group have activity in promoting production of nerve growth factor. Compounds of formula (I) wherein R.sup.1 is a nitro group are intermediates for compounds of formula (I) wherein R.sup.1 is an amino group.

Abstract: Fungicidal 2-imidazolin-5-ones and 2-imidazoline-5-thiones, processes for their preparation, fungicidal compositions containing them and methods of using them to treat or prevent fungal disease in crops.

Abstract: Amide Derivatives of formula (I) wherein R.sup.1 is a mono or bicyclic heteroaryl radical, R.sup.2 is cycloalkyl, R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl, and R.sup.5 is a group of formula (A) or (B) or (C): R.sup.8 --CH.sub.2 --CH.sub.2 -- or (D) or (E): R.sup.9 OCH.sub.2 CHOHCH.sub.2 -- or (F): R.sup.9 OCH.sub.2 CH.sub.2 -- and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.

Abstract: The invention relates to 6-membered nitrogen-containing heteroaryloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.

Abstract: The invention is herbicide 3-substituted quinoline intermediates and a method for the synthesis of the herbicide intermediates 3-alkoxymethyl substituted quinolines.

Abstract: Substituted tetrahydropyridines and hydroxypiperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.

Abstract: The compounds of formula I are smooth muscle relaxants: ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.

Abstract: Pyridone dyes useful for thermal transfer have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, Y, X and Z are defined in the specification.

Abstract: The subject invention relates to compounds having the structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl;(b) R' is selected from unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; and halo; and(c) R" is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; methyl monosubstituted with hydroxy, thiol or amino; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; amino; unsubstituted amide; unsubstituted or C.sub.1 -C.sub.3 substituted amido; halo; unsubstituted sulfoxide; unsubstituted sulfonyl; and cyano;pharmaceutical compositions containing such compounds, and the use of such compounds for preventing or treating respiratory, ocular, and/or gastrointestinal disorders.

Abstract: The subject invention involves methods of treating nasal congestion comprising administration, to a human or lower animal in need of such treatment of a safe and effective amount of a compound having the following structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; and(b) R' is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; cyano; and halo.The subject invention also involves the use of such compounds for preventing or treating other respiratory, ocular and/or gastrointestinal disorders. The subject invention also involves novel compounds having the above structure wherein R' is hydrogen or fluoro or cyano.

Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.

Abstract: Novel 5,6-dihydro-4H-imidazo[4,5,1-ij]quinolines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.

Abstract: This invention relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof. More particularly, this invention relates to new heterocyclic compounds and salts thereof which display bradykinin antagonist activity, to processes for preparing these compounds, to a pharmaceutical composition comprising these compounds, and to methods of using same in the prevention and/or the treatment of bradykinin- or bradykinin analogue-mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, in human beings or in animals.

Abstract: The present invention relates to benzenesulfonamide derivatives represented by Formula (I): ##STR1## in which R.sup.1 and R.sup.2 independently represent hydrogen or lower alkanoyl; and R.sup.3 and R.sup.4 independently represent hydrogen, lower alkyl, cycloalkyl, substituted or unsubstituted polycycloalkyl, substituted aryl, or a substituted or unsubstituted heterocyclic group, or R.sup.3 and R.sup.4 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted aliphatic heterocyclic group, or a pharmaceutically acceptable salt thereof. The derivatives are useful as therapeutic agents for osteoporosis.

Abstract: The present invention provides a dye-donor element for use according to thermal dye sublimation transfer, said dye-donor element comprising a support provided with a dye layer containing a dye and a polymeric binder, characterized in that said dye corresponds to the following formula: ##STR1## wherein R.sup.1 to R.sup.12 are as set out in the claims and the description.

Abstract: Novel compounds having potassium channel activating activity and useful, for example, as antiischemic agents are disclosed. These compounds have the general formula ##STR1## wherein A is ##STR2## or a single bond to complete an indoline nucleus; X is --O--, --S-- or --NCN; and the R groups are as defined herein.