Abstract: The present application relates to a new process for the asymmetric production of 3-(pyridin-4-yl)-3-hydroxy-pentanoic acid derivatives, which are useful intermediates in the manufacture of compounds that are known to show antiproliferative activity.

Abstract: 4-pyridone (4-pyridinone) derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.

Abstract: The present invention is directed to novel pyridine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels.

Abstract: 3-Chloro-6-(hydroxymethyl)-2-methyl-5-[4-({4-[(trifluoromethyl)oxy]phenyl}oxy)phenyl]-4(1H)-pyridinone, having the following formula: is described along with its pharmaceutically acceptable salts, processes for its preparation, pharmaceutical formulations thereof and its uses in treatment of certain parasitic infections such as malaria.

Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.

Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper-triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.

Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Compounds having a formula: or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.

Abstract: The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

Abstract: Compounds of the general formula (I); wherein the substituents are as defined in claim 1, are useful as fungicides.

Abstract: The present invention relates to new compounds of formula (I), (II), or (III) wherein R1, R2, R3, R4, R5 and W are as defined herein, and methods of using the compounds to inhibit PAI-1 and to treat PAI-1 related disorders.

Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

Abstract: Disclosed is a liquid-crystal composition capable of providing a functional film that exhibits useful optical properties. The composition comprises a compound of the following formula (1) that exhibits a smectic liquid-crystal phase. R1—(Ar1)p—C?C—(Ar2)m—C?C—(Ar3)n—R2??(1) wherein R1 and R2 represent alkyl; R3, R4, R5 and R6 represent hydrogen or alkyl; Ar1, Ar2 and Ar3 represent divalent aromatic hydrocarbon or aromatic heterocyclic group; and p, m and n are 1 or 2.

Abstract: Fungicidal compounds of the general formula (I): wherein X and Y are independently H, halo, C1-8 alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkoxy, C1-8 alkylthio, nitro, amino, mono- or di-(C1-6)alkylamino, mono- or di-(C2-6)alkenylamino, mono- or di-(C2-6)alkynylamino, formylamino, C1-4 alkyl(formyl)amino, C1-4 alkylcarbonylamino, C1-4 alkyl(C1-4 alkylcarbonyl)amino, cyano, formyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-4)alkylaminocarbonyl, carboxy, C1-4 alkylcarbonyloxy, aryl(C1-4)alkylcarbonyloxy, C1-4 alkylsulphinyl, C1-4 alkylsulphonyl, C1-4 alkylsulphonyloxy, aryl, heteroaryl, aryloxy, arylthio, heteroaryloxy or heteroarylthio wherein any of the foregoing alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, groups or moieties are optionally substituted; R1 is phenyl, cyano, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl in which the alkyl, alkenyl and alkynyl groups are optionally substituted on their terminal carbon atom with one, two or three halogen atoms,

Abstract: The present invention relates to a process for preparing pyridinyl and pyrimidinyl mono-fluorinated beta keto esters of formula (I): wherein: R1 represents a pyridine ring or a pyrimidine ring, the rings being optionally substituted by a C3-6 cycloalkyl group, a C1-4 alkyl group, a C1-4 alkoxy group, a benzyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or ahalogenatom; and R3 represents a C1-6 alkyl group; by reacting with fluorine a compound of formula (II) wherein R1, R2 and R3 have the same meaning as defined above.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

Abstract: The invention relates method of combating undesired plant growth at a locus, comprising application to the locus of an effective amount of at least one compound of formula (I): wherein R1, R3, A, X, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and to novel compounds of formula I as well as to herbicidal compositions containing such compounds as active ingredients.

Abstract: The compound (1) having 2,3-bis(trifluoromethyl)-1,4-phenylene is stable chemically and has excellent miscibility with other liquid crystal compounds, large and negative dielectric anisotropy and proper optical anisotropy. A liquid crystal composition comprising the compound has large specific resistance and a large voltage holding ratio, and that the composition is useful for a liquid crystal display element.

Abstract: A compound of the formula (I) wherein A is O, S, CHR1 or NR2, R1 and R2 are H, lower alkyl, X1 and X2 are H, halogen, nitro, cyano, etc., Y1 is H, lower alkyl, Z1 and Z2 are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.

Abstract: Compounds are provided having the formula: wherein A, Q, and X are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such compounds alone or in combination with other antidiabetic agents such as metformin, glyburide, troglitazone and/or insulin.

Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.

Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.

Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Abstract: A production method of an ether compound given by formula (3): which comprises making an alcohol compound given by formula (4): wherein R1 represents a 3,3-dihalo-2-propenyl group or a benzyl group optionally substituted with a halogen atom(s), react with a pyridine compound given by formula (5): wherein R2 represents a hydrogen atom or halogen atom, in a hydrocarbon compound in the presence of an alkali hydroxide or alkaline earth hydroxide with distilling off water from the reaction mixture, provides the ether compound, which is useful as an active ingredient of insecticide/acaricide or production intermediate thereof, in high yield.

Abstract: Compounds of structure (1) are obtained by reduction of compounds of the structures Compounds of structure (1), especially where Z is a hydrogen atom or a 3,4-methylenedioxyphenyl group, are important intermediates for inter alia paroxetine.

Abstract: The compound of the formula I is suitable for the preparation of pharmaceuticals for the treatment of fungal disorders caused by azole-resistant fungi.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: The invention relates to a method for producing optically pure compounds of 3(R)- and 3(S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine or its carboxylic acid esters by reacting the enantiomer mixtures stereoselectively, using an enzyme.

Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (±)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Abstract: Substituted 2-(2′-pyridyloxy)phenylacetamides I, where R1 is fluorine, chlorine, CH3 or halomethyl; R2 is fluorine, bromine, alkyl or halomethyl; R3 is hydrogen or one of the radicals mentioned under R2; and R2 is 6-chloro if R3 is hydrogen, R3 is 5-chloro if R2 is fluorine and the compound in which R1, R2 and R3 are each chlorine with the proviso that R1 may not be chlorine if R2 is 5-trifluoromethyl and R3 is hydrogen, and processes for their preparation and their use for controlling harmful fungi and animal pests are described.

Abstract: This invention relates to a process for converting 2,4-dichloropyridines into 2-aryloxy-4-chloropyridines, comprising reacting a compound of formula (I), wherein R1 is (C1-C4)alkyl; R2 is methyl or ethyl; and R3, R4 and R5 are selected, independently, from (C1-C4)alkyl and (C1-C4)alkoxy; or a pharmaceutically acceptable salt thereof; comprising reacting a compound of formula (II), wherein R1 and R2 are defined as above, with a compound of formula (III), wherein R3, R4 and R5 are defined as above, in the presence of a base that is capable of deprotonating the compound of formula (III), optionally in the presence of an organometallic halide or oxide and a suitable solvent, and then optionally converting the resulting compound of formula (I) into a pharmaceutically acceptable salt of such compound.

Abstract: A process for condensing at least one carbonyl compound carrying at least one electron-withdrawing group with an aromatic derivative carrying at least one hydroxyl functional group, wherein the electron-withdrawing group present on the carbonyl compound is selected from fluoroalkyl derivatives, esters, including orthoesters, and nitrites and said condensation is carried out in a basic medium.

Abstract: This invention discloses and claims novel intermediates and procedures for the synthesis of camptothecin derivatives, such as irinotecan, and other compounds related to the synthesis of CPT-11. Related procedures and compounds are also disclosed, such as a novel method of making mappicine.

Abstract: A process for the preparation of carbonates containing aromatic ester groups is disclosed. The process entails reacting aromatic monohydroxy componds with phosgene or with chlorocarbonic acid esters of aromatic monohydroxy compounds at a temperature of 50 to 350° C. and in the presence of active carbon as catalyst.

Abstract: (R)(+)-2-[4-(5-chloro 3-fluoropyridin-2-yloxy)-phenoxy]-propionic acid propinyl ester is produced by converting a compound of formula II in an inert organic solvent, without isolation of the intermediate products, with M2CO3, in which M is sodium or potassium, into the compound of formula III reacting this with the compound of formula IV to form the compound of formula V and converting this with a compound of formula VI wherein Z signifies phenylsulphonyl, tosyl, methylsulphonyl, nosyl, bromophenyl, Cl-, Br- or CICO-, into the compound of formula I.

Abstract: A fungicidal compound having general formula (I) or a stereoisomer thereof, wherein A is CH or N, B is OCH3 or NHCH3, R1 is H, chloro or methyl and R2 is H, fluoro, chloro or methyl.

Abstract: The invention relates to compounds of formula (1) ##STR1## wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder is carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1) or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.

Abstract: This invention relates to intermediates and processes for the synthesis of camtothecin derivatives, such as irinotecan. Related procedures and compounds are disclosed, such as a method of making mappicine.

Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.

Abstract: This invention relates to a process for preparing 2-substituted pyridines via metal halogen exchange with sec-butyllithium on optionally substituted 2-bromo or 2-iodopyridines. The resulting lithopyridine intermediate is reacted with an electrophile to provide the desired 2-substituted pyridine. The substitution of sec-butyllithium for n-butyllithium in such a process results in an enhanced yield and purity of the desired 2-substituted pyridine.

Abstract: A pyridone derivative represented by the general formula: ##STR1## {wherein R is an alkyl group or a haloalkyl group, R.sup.1 is a hydrogen atom, an alkyl group, a haloalkyl group, an acetyl group, an amino group, an alkoxycarbonylamino group, an alkylcarbonylamino group or the like, R.sup.2 is a hydrogen atom, an alkyl group, a carboxyl group or an alkoxycarbonyl group, R.sup.19 is a hydrogen atom, a halogen atom, a cyano group or the like, Q is a phenyl group which may be substituted or a condensed hetero ring which may be substituted}, a herbicide containing it and an intermediate for its production, are provided.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (.+-.)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.