Abstract: Synthetic, novel dimeric cinchona alkaloid compounds having potent cytotoxic activity against human cancer cells. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds cause apoptotic cell death in and cause inhibition of clonogenic growth of human breast cancer, prostate cancer, leukemia, lymphoma cells at nanomolar concentrations. The chemical structure of the compound includes dimeric cinchona alkaloid and derivatives containing various groups attached in their structure. The compounds also possess hydroxy group functionality in the structure to enable the preparation of pharmaceutically applicable salts to enhance their solubility for ease of systemic administration in animals and in humans, for example, in cancer patients.

Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.

Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.

Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.

Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.

Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.

Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.

Abstract: The present invention relates to cinchona-based bifunctional organocatalysts and methods for preparing chiral hemiesters using the same. More specifically, the present invention relates to methods for preparing chiral hemiesters from prochiral or meso cyclic acid anhydrides via desymmetrization, using bifunctional cinchona alkaloid catalysts comprising sulfonamide functional groups.

Abstract: Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C4-C50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones.

Abstract: Compounds of formula (I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive and inflammatory diseases.

Abstract: Disclosed is the chemical synthesis of chiral alkaloid monomers, liquid crystal compositions comprising the chiral alkaloid monomers, and polymerization of the liquid crystal compositions to provide polymer networks with useful cholesteric optical properties and stability.

Abstract: The present invention relates to cinchona-based bifunctional organocatalysts and methods for preparing chiral hemiesters using the same. More specifically, the present invention relates to methods for preparing chiral hemiesters from prochiral or meso cyclic acid anhydrides via desymmetrization, using bifunctional cinchona alkaloid catalysts comprising sulfonamide functional groups.

Abstract: Disclosed is the chemical synthesis of chiral alkaloid monomers, liquid crystal compositions comprising the chiral alkaloid monomers, and polymerization of the liquid crystal compositions to provide polymer networks with useful cholesteric optical properties and stability.

Abstract: One aspect of the present invention relates to cinchona-alkaloid-based catalysts. A second aspect of the invention relates to a method of preparing a derivatized cinchona alkaloid catalyst by reacting a cinchona-alkaloid with base and a compound that has a suitable leaving group. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral cyclic anhydride or a meso cyclic anhydride, comprising the step of: reacting a prochiral cyclic anhydride or a meso cyclic anhydride with a nucleophile in the presence of a catalyst; wherein said prochiral cyclic anhydride or meso cyclic anhydride comprises an internal plane of symmetry or point of symmetry or both; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized cinchona-alkaloid.

Abstract: Optically active diphenylalanine compounds may be conveniently prepared in a good yield by reacting a diphenylalanine compound represented by formula (1) with an optically active amine compound represented by formula (2) in the presence of an organic solvent to give a diastereomeric salt represented by formula (5) and then treating the diastereomeric salt under acidic conditions to give an optically active diphenylalanine compound represented by formula (3): wherein each symbol is as defined in the specification.

Abstract: One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the invention relates to a method of preparing a derivatized quinine-based or quinidine-based catalyst comprising 1) reacting quinine or quinidine with base and a compound that has a suitable leaving group, and 2) converting the ring methoxy group to a hydroxy group. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone, comprising the step of: reacting a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone with a nucleophile in the presence of a catalyst; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized quinine or quinidine.

Abstract: A process for producing a compound represented by the following formula (IV): (wherein R denotes a hydrogen atom, an alkyl group, or an aryl group), comprising reducing a compound selected from the group consisting of: a compound represented by the following formula (I): (wherein R is as defined in the formula); a compound represented by the following formula (II): (wherein R is as defined in the formula); and a compound represented by the following formula (III): (wherein R is as defined in the formula), by reacting the compound with a cell of a microorganism and/or a cell preparation thereof capable of stereo-selectively reducing a keto group.

Abstract: A method for the manufacture of a substance having an apoptosis-inducing ability characterized in including a step of subjecting at least one compound selected from the following (a), (b), (c) and (d) [excluding uronic acid and/or uronic acid derivatives; and compounds which contain uronic acid and/or uronic acid derivatives] to a heating treatment: (a) pentose; (b) pentose derivatives; (c) compounds containing pentose; (d) compounds containing pentose derivatives.

Abstract: A stable crystalline chloride or bromide salt of swainsonine is disclosed.

Abstract: Compounds having the following structure: 1

Abstract: Compounds having the general structure: 1

Abstract: One aspect of the present invention relates to methods of asymmetric synthesis, e.g., asymmetric hydride reductions of carbonyl groups, using a chiral, non-racemic phase transfer catalyst, a helper nucleophile, and a sterically bulky reagent nucleophile, e.g., an alkoxyhydride derived from a sacrificial ketone and a hydride reagent. Moreover, the sterically bulky reagent nucleophile may be generated in situ or prepared in a prior step. Another aspect of the present invention relates to chiral non-racemic phase transfer catalysts, and their use in the subject methods.

Abstract: &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.

Abstract: Enantioseparation methods using chemical compounds which contain the chiral 9,11-substituted-10,11-dihydro-cinchonan skeleton (9,11-Subst.-DHC) and the precursors thereof with the 9-substituted cinchonan skeleton (9-Subst.-C) are described and discussed. The chiral compounds of the present invention are based on cinchonan derivatives containing amide structure elements which support effectively and co-operatively the enantioseparation of chiral acidic selectands involving also ion-pair and ion-exchange binding mechanism between the strong amino group of the selector and the acidic group of the selectand. The methods of enantioseparation of the present invention are related to stereoselective liquid-liquid and liquid-solid type extraction principles and fractionated crystallization employing cinchonan derivative type selectors.

Abstract: There are disclosed compounds of formula (I) 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: Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.

Abstract: There are disclosed compounds of formula (I) 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: This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.

Abstract: 4-(N,N-Dialkylamino)aniline compounds of the following general formula (I): wherein R1 represents an alkyl group, an aryl group or a heterocyclic group, R2 to R5 each represent a hydrogen atom or a substituent, and R2 and R3, R1 and R2, or R4 and R5 may form a ring together; a processing composition for color photography, which contains at least one of these compounds; and a color image-forming method wherein at least one of these aniline compounds is used.

Abstract: There are disclosed compounds of formula (I) and pharmaceutical 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 conditions.

Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein Ar represents an optionally substituted aromatic group; Q represents a divalent aliphatic hydrocarbon group; R.sub.1 represents hydrogen, cyano, an optionally substituted hydrocarbon group, a group of the formula: ##STR2## wherein R.sup.3 and R.sub.4 independently represent hydrogen, acyl or an optionally substituted hydrocarbon group, or R.sup.3 and R.sup.4 jointly form a ring, or acyl; R.sup.2 represents acyl; ......... represents a single bond or a double bond; m represents 1 or 2 or a salt, a process of producing thereof and an anti-neurodegenerative composition.

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: A process for cleaving cinchona alkaloids to a quinoline derivative and an enantiomerically pure, functionalized 1-azabicyclo(2.2.2)octane, includes treating a cinchona alkaloid with a complex metal hydride while simultaneously oxidizing by exposure to air in an ether or tetrahydrofuran. Enantiomerically pure 1-azabicyclo(2.2.2)octanes of the formula ##STR1## in which R is hydrogen, a straight-chain or branched alkoxycarbonyl group with 1 to 12 carbon atoms, a straight-chain or branched alkyl group with 1 to 12 carbon atoms, alkylated silyl groups, or a substituted phenyl or benzyl substituent, are also provided.

Abstract: Quinuclidine compounds of the formula I: ##STR1## R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen;or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond;X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 S--, --SCH.sub.

Abstract: Sulfonic acid esters are used as (a) compounds for forming a strong acid on irradiation in radiation-sensitive, positive or negative working mixtures also comprising (b) either a compound with at least one acid-decomposable C--O--C or C--O--Si bond (for positive working mixtures) or a compound with at least acid-cross-linkable groups (for negative working mixtures) and c) a binder which is insoluble in water but soluble or at least swellable in aqueous alkaline solutions, wherein said sulfonic acid esters are formula?R.sup.1 --CR.sup.2 (CF.sub.3)--O--SO.sub.2 --!.sub.n R.sup.3(I)orR.sup.1 ?--CR.sup.2 (CF.sub.3)--O--SO.sub.2 --R.sup.3 !m (II)wherein R.sup.1, R.sup.2, R.sup.3, n and n are defined with the body of the disclosure. These mixtures are particularly suitable for exposure to deep UV radiation in the formation of recording materials suitable for the production of photoresists, electronic components, and printing plates.

Abstract: Compounds of the formula ##STR1## wherein W, Ar.sup.1, Ar.sup.2 and Ar.sup.3 are defined as below; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Abstract: Quinuclidine compounds of the formula I: ##STR1## R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen;or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond;X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 S--, --SCH.sub.

Abstract: Osmium-catalyzed methods of addition to an olefin are discussed. In the method of asymmetric dihydroxylation of the present invention, an olefin, a chiral ligand, an organic solvent, water, an oxidant and an osmium-containing compound are combined. In the method of asymmetric oxyamination of the present invention, an olefin, a chiral ligand, an organic solvent, water, a metallochloramine derivative, an osmium-containing compound and, optionally, a tetraalkyl ammonium compound are combined. In the method of asymmetric diamination of the present invention, an olefin, a chiral ligand, an organic solvent, a metallo-chloramine derivative, an amine and an osmium-containing compound are combined. In one embodiment, an olefin, a chiral ligand which is a polymeric dihydroquinidine derivative or a dihydroquinine derivative, acetone, water, a base, an oxidant and osmium tetroxide are combined to effect asymmetric dihydroxylation of the olefin.

Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

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 process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines is described where N-protected DL-3,3-diphenylalanine or N-protected-DL-substituted 3,3-diphenylalanine are treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

Abstract: A series of cis-3-[(cyclic)methylamino]-2-[(.alpha.-substituted)arylmethyl]quinuclidin es, 3-[(cyclic)methylimino]-2-[(.alpha.-substituted)-arylmethyl]quinuclidines and cis-3-[(cyclic)-methyleneamino]-2-[(.alpha.-substituted)arylmethyl]-quinuc lidines, including their pharmaceutically acceptable salts, are disclosed. These particular compounds are found to be useful as substance P antagonists and therefore, are of value in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases and pain or migraine. Preferred member compounds include cis-3-[(2-chlorophenyl)methylamino]-2-benzhydryl-quinuclidine, cis-3-[(2-trifluorophenyl)methylamino]2-benzhydrylquinuclidine and cis-[(2-methoxyphenyl)methylamino]-2-benzhydrylquinuclidine. Methods for preparing these compounds from known starting materials are provided.

Abstract: A method for resolving (.+-.)-(.alpha.)-(3-benzoylphenyl) propionic acid is disclosed. The method comprises:i) converting said propionic acid with (-)-cinchonidine in a solvent comprising a mixture of an aliphatic ester and an alkyl alcohol;ii) separating teh diastereomeric salt from such conversion;iii) purifying said separated diastereomeric salt by a single recrystallization; andiv) isolating highly pure (+)-.alpha.-(3-benzoylphenyl) propionic acid without any further recrystallization.

Abstract: Antibacterial quinolone derivatives represented by the following formula and salts thereof are disclosed. ##STR1## wherein R.sup.1 meawns a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted phenyl group, R.sup.2 denotes a hydrogen atom or a carboxyl-protecting group, R.sup.3 represents a hydrogen or halogen atom or an amino, mono- or di-(lower alkyl)amino, hydroxyl or lower alkoxyl group, X is a hydrogen or halogen atom, Y means a nitrogen atom or a group C-R.sup.4 in which R.sup.4 is a hydrogen or halogen atom or a lower alkyl or lower alkoxyl group or is a group ##STR2## which forms a ring together with R.sup.1 (i.e., the asterisked carbon atoms are linked to the N(1) atom of the quinolone skeleton), and A denotes a specific N-containing group. Preparation processes of the quinolone derivatives and antibacterial agents containing the same are also disclosed.

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 thereof and their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.

Abstract: 3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.

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.