Abstract: The present invention provides selective kinase inhibitors of formula (I).

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention is directed to 1,2,3,4,10,10a,-hexahydro-pyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

Abstract: The present invention provides a compound of formula I 1

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl2). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I):

Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.

Abstract: This invention is directed to compounds of the formula 1

Abstract: Disclosed are novel compounds represented by the following structural formula:

Abstract: A compound having the formula 1

Abstract: 1

Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): 1

Abstract: The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.

Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.

Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

Abstract: The present invention provides novel compounds exemplified by pyrrolic nitrogens used as anion and neutral species recognition elements with an aromatic core as a signal group. Described are methods for the synthesis of various pyrrole aryl compounds as well as various applications for these compounds. Methods of use include the binding and detection of specific analytes in a mixture and, in some examples, the separation of the analyte from the mixture. Additional methods of use include the transport of therapeutic agents and the sensing of components, degradants, and impurities in foodstuffs.

Abstract: Piperazine derivatives, as well as pharmaceutically acceptable salts, solvates and esters thereof, can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, type II diabetes, obesity and sleep apnoea.

Abstract: The present invention provides inhibitors of protein kinase C, of formula (I) wherein: one of: R1 and R2, R2 and R3 or R3 and R4, together form a 5 or 6 membered ring and the two groups of R1, R2, R3 and R4 not forming a ring, are H; and salts thereof, formulations comprising said inhibitors of protein kinase C of formula (I), processes for preparation thereof and use thereof in the manufacture of a medicament for the treatment of inflammatory, immunological, bronchopulmonary, cardiovascular, oncological or CNS-degenerative disorders.

Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: 1

Abstract: The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc. ), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N—R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C—RA; and D1, D2, D3 and D4 each independently represent C—RB, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N—R2A, an oxygen atom, a sulfur atom, etc.

Abstract: Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract: Novel spiropyran compounds, particularly with photochromic properties, are disclosed, as well as photochromic compositions and ophthalmic articles containing said compounds. The photochromes have been designed so as to have a high colorability, a high sensitivity to activating radiation breaking the pyran ring, to be entirely or practically free from coloration in a non activated non exposed state, to have an intense coloration following activation and a high coverage of the visible spectrum in combination with at least one other photochrome, and to have high rates of coloration/decoloration. The spiropyrans are easily produced and photochemically stable, and are, e.g., of formula (i), wherein L=(a); (b).

Abstract: Novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them.

Abstract: Pyrrolylquinoxalinediones of the formula I and their tautomeric and isomeric forms, and their physiologically tolerated salts, where the variables have the following meanings: R1 hydrogen, cyclohexyl an aliphatic radical which has 1 to 4 carbon atoms and can carry the radical —COOR5, where R5 is hydrogen or C1-C4-alkyl, R2 —COOH, —COO—C1-C4, —COO—(CH2)m—Ph, —CONR6R7 and where m can be an integer from 1 to 6, R6 can be hydrogen, C1-C4-alkyl or OH and R7 can be hydrogen, C1-C4-alkyl, where all the phenyl or pyridyl rings present in R2 can also be substituted by up to 3 of the following radicals: C1-C4-alkyl, halogen, —O—C1-C4-alkyl, —OCF3, —NO2, —CN, —COOR5 or —CONHR5, R3 —CF3, —NO2, —CN, and R4 hydrogen or R3 and R4 can together be a fused-on benzene ring. The compounds are suitable as drugs for human and veterinary medicine.

Abstract: A compound of the formula 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The present invention relates-to compounds of the general formula (I) 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a] indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

Abstract: A preparation of a tyrphostin including a compound of a general formula: 1

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention relates to tricyclic quinoxaline compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein tyrosine kinases and therefore should be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention provides optionally substituted and/or annulated compounds of formula (I) wherein X, Y, Z and A is each independently carbon or nitrogen, and at least two of X, Y, Z and A are carbon; and pharmaceutically acceptable salts thereof with the proviso that: 3-(1H-Indol-3-yl)-1H-quinoxalin-2-one, 3-(2-Methyl-1H-indol-3-yl)-1H-quinoxalin-2-one, and 3-(1,2-Diphenyl-1H-indol-3-yl)-1H-quinoxalin-2-one are excluded from compounds of formula (I). The invention includes the use of compounds of formula (I) in medical therapy, particularly in the therapy of conditions requiring inhibition of protein kinase C.

Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.

Abstract: Fluorinated phenanthrene derivatives and their use in liquid-crystalline mixtures Fluorinated phenanthrene derivatives of the formula (I) in which G is —CHF—CH2— or —CF═CH—, E1, E2, E3, E4, E5 and E6 are identical or different and are —CH—, —CF— or —N— and R1(—A1—M1)a(—A2—M2)b, (M3—A3—)c(M4—A4—)d R2 denote mesogenic radicals are suitable as components for liquid-crystalline mixtures, especially ferroelectric mixtures.

Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

Abstract: Compounds of formula A are disclosed: ##STR1## wherein R.sup.1 is aralkyl or cycloalkyl; R.sup.2 is cycloalkylmethyl, alkyl, or aralkyl;R.sup.3 is hydrogen, alkyl, substituted phenyl (including p-phenoxy-phenyl), or fluorene;R.sup.4 is hydrogen, alkyl, substituted phenyls (including 1-alkyl-4-carboxy-substituted phenyls), alkyl carboxylic acids;R.sup.5 is hydrogen or R.sup.1 and R.sup.5 taken together forming a tetrahydroisoquinoline ring or a piperidine ring.These compounds exhibit inhibitory action against fructose-1,6-bisphosphatase (FBPase) and are indicated in the treatment or management of Type II diabetes.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: The disclosure relates to quinoxaline derivatives of Formula I ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined in the disclosure, as well as their production and use in medicinal agents.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors and the method of preparing these compounds are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: Fibrinogen receptor antagonist alcohol prodrugs having the structure, for example, of ##STR1## more particularly, ##STR2##

Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: PDGF receptor kinase inhibitory compounds of the quinoxaline family, methods for their synthesis and containment is slow release pharmaceutical preparations, and their use for treatment of proliferative malignant and non-malignant diseases or disorders by local or systemic application. A compound according to the invention includes a tyrphostin of the general formula: ##STR1## wherein R1 and R2 are each independently selected from the group consisting of alkyl, alkoxy, halogen, nitro and amine and Ar is selected from the group consisting of phenyl, ferrocene, thiophene, furane, pyrrole, indole, thiazole, imidazole and pyridine.

Abstract: Compounds of formula (I): ##STR1## wherein R represents a CR.sub.4 R.sub.5, CHR.sub.6, or C.dbd.R.sub.7 radical and R.sub.3 represents an oxygen atom, salts thereof, the preparation thereof and drugs containing same. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-osoxaziepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R.sub.1 -R.sub.4 represent organic or inorganic groups;A represents an alkylene group of 2 to 6 carbon atoms optionally substituted with one or more, alkyl groups having from 1 to 4 carbon atoms;Y represents methylene, oxygen, sulfur, or NH; andX is either N, C or CH,which compounds are, useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

Abstract: A process for preparing a compound of formula (I) or a phamaceutically-acceptable salt thereof, comprising: 1) reacting a compound. of formula (III), in which R is a straight or branched chain alkyl having from one to four carbon atoms, with an alkali metal hydroxide in an aqueous medium at a temperature of about 80.degree. to 120.degree. C. and time of about 20 to 100 hours to form a reaction product; 2) cyclizing the reaction product of step 1) with formic acid and formaldehyde to form a formiate compound; and 3) neutralizing the formiate compound of step 2) with an aqueous base.