Abstract: It has now been found that certain novel N-(substituted aryl)-4(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein.

Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.

Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.

Abstract: Piperidine derivatives represented by formula (I) or nontoxic salts thereof (wherein symbols are defined in the description): Since the compound represented by formula (I) has a PDE4 inhibitory activity, it is useful for preventing and/or treating inflammatory diseases, diabetic diseases, allergic diseases, autoimmune diseases, osteoporosis, bone fracture, obesity, depression, Parkinson's disease, dementia, ischemia-reperfusion injury, leukemia and the like.

Abstract: Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.

Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.

Abstract: The Present invention relates to a process for the preparation of (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine of formula 1. (RS) 3-Methyl-1-(2-piperidinyl phenyl butyl amine having formula 1 is an important key intermediate for the synthesis of repaglinide of formula 2 an oral hypoglycemic agent.

Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings, each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: The present invention provides a process for the preparation of threo-methylphenidate hydrochloride. According to a preferred embodiment, the process comprises the following steps: (a) contacting 1-(phenylglyoxylyl)piperidine arenesulfonylhydrazone of the formula wherein Ar denotes an aryl group, where the aryl group may be substituted by a C1–C6 alkyl, halo or nitro group; with an inorganic base in the presence of a water immiscible organic solvent and a phase transfer catalyst to obtain (R*,R*)-enriched 7-phenyl-1-azabicyclo [4.2.0]octan-8-one of the formula: (b) reacting the (R*,R*)-enriched 7-phenyl-1-azabicyclo[4.2.0]octan-8-one prepared in step (a) with a solution of hydrogen chloride in methanol to obtain threo-enriched methylphenidate hydrochloride; (c) crystallizing the threo-enriched methylphenidate hydrochloride prepared in step (b) to give the desired threo-methylphenidate hydrochloride.

Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.

Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.

Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: 1

Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: The invention discloses deuterated 3-piperidinopropiophenones as well as their physiologically tolerated salts. Furthermore, the invention concerns the use of deuterated 3-piperidinopropiophenones for the treatment of muscular illnesses as well as for the preparation of pharmaceutical drugs for the treatment of muscular illnesses.

Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.

Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1

Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder. Furthermore, the invention provides methods of treating sleep disorders using compositions that remain active for a discrete period of time to reduce side effects. More specifically, the invention is directed to the compositions and use of derivatized, e.g., ester or carboxylic acid derivatized, antihistamine antagonists for the treatment of sleep disorders.

Abstract: An improved process for the manufacture of fexofenadine is described in which a compound of formula (F): wherein R2 represents COOH, COO—C1-6 alkyl or CN; and R3 represents hydrogen, mesylate, triflate, tosylate or carboxy-C1-6-alkyl, or a salt thereof is prepared by: (I) reacting a compound of formula (B): wherein R1 represents hydrogen or carboxy-C1-6-alkyl; and R2 is a hereinbefore defined, with a copper and/or silver compound in the presence of palladium or a compound thereof to yield a compound of formula (C): wherein R1, and R2 are as hereinbefore defined; (II) converting said compound of formula (C) into a compound of formula (E): wherein R2 and R3 are as hereinbefore defined and R4 represents a halogen atom, and (III) reacting said compound of formula (E) with azacyclonol.

Abstract: The present in to s directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1

Abstract: Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a therapeutically effective amount of a selective muscarinic m1 agonist compound is administered to a patient in need of such treatment.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: 1

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and a process for their preparation are described. The compounds are suitable, for example, for treating type II diabetes.

Abstract: Compounds of the formula B—X—(CH2)m—CR1R2—(CH2)n—CO—Y  (I) have therapeutic utility as inhibitors of metalloproteinases etc.

Abstract: Compounds of the formula wherein R1 R2, R7, R8, X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from. dementia and Alzheimer's disease.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.

Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.

Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: A process for preparing an enantiomerically-enriched form of threo-ritalinic acid, which comprises resolving a mixture of enantiomers of a salt of the acid, said salt being formed with an achiral acid or base, using a chiral resolving agent. The resolved salt can be esterified, to give the therapeutic agent d-threo-methylphenidate.

Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.

Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB: 1

Abstract: The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO2X)m wherein  is a carrier, X is a leaving group, Y is a bond or spacer, Z is a bivalent group, when Z is a bivalent electron attractive group, W is an aromatic ring which may be substituted and when Z is a bivalent non-electron attractive group, W is an aromatic ring which is substituted by an electron attractive group and may be further substituted and m is 1 or 2, or a salt thereof, which is useful for synthesizing a novel organic compound.

Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.