Abstract: 4-amino-2,2,6,6-tetramethylpiperidine is prepared by reacting 2,2,6,6-tetramethylpiperidine-4-one with ammonia and hydrogen in the presence of nickel and/or cobalt catalyst and water. The main reaction is carried out at a pressure of at most 50 bar and a temperature of at most 120° C. up to a conversion of the 2,2,6,6-tetramethylpiperidine-4-one of at least 80%. Then, an after-reaction takes place at a higher temperature and at a higher pressure compared to the pressure and temperature of the main reaction.

Abstract: Sterically hindered alkoxyamine and hydroxy substituted alkoxyamine stabilizer compounds are made water compatible via certain backbones with affinity towards water. The sterically hindered amines are for example of the formula where for example E and E? are 2-hydroxycyclohexyloxy, 2-hydroxy-2-methylpropoxy, benzyloxy, methoxy, propoxy, hexyloxy, heptyloxy, octyloxy or cyclohexyloxy, Rx is for example —NH2+CH2CH2OH Cl?, —NH3+?OAc, ?NOH, —NHCH(CH3)COO?K+, —NHCH2CH2N(CH3)2+?OAc, —NHCH2CH2SO3?K+, —NHCH(COO?K+)CH2CH2SCH3, —NHCH2COO?K+, —OCH(CH3)COO?K+, —OCH2CH2N(CH3)2+?OAc, —OCH2CH2SO3?K+, —OCH(COO?K+)CH2CH2SCH3 or —OCH2COO31K+, and where R5 comprises repeating units of —(OCH2CH2)—, —(OCH2CH2(CH3))—, —(CH2CHCOOH)—, —(CH2C(CH3)COOH)—, —(CH2CHCOOCH3)—, —(NHCH2CH2)—, —(CH2CHOH)—, —(CH2CHCONH2)— or —(CH2CH(NHCOH))—. These compounds are particularly effective in stabilizing aqueous polymer systems against the deleterious effects of oxidative, thermal and actinic radiation.

Abstract: The present invention relates to polyamide oligomers with linear or branched chain structure with a number average molar mass of 800 to 5000 g/mol, with basic end groups which are at least partially NH2 end groups and carboxyl end groups, produced by condensation of polyamide-forming monomers, the concentration of NH2 end groups being at most 300 mmol/kg and in that these end groups are present in excess in a ratio to the carboxyl end groups.

Abstract: Disclosed herein are isolated forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.

Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.

Abstract: A compound represented by the formula (I): [In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms, C2 to C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom, one of the ring-constituting carbon atoms may be replaced with V, V represents nitrogen atom, or carbon atom substituted with Zx, Zx represents a saturated alkyl group having 1 to 4 carbon atoms and the like, Rs represents -D-Rx etc., D represents a single bond, oxygen atom and the like, Rx represents a saturated alkyl group having 3 to 8 carbon atoms and the like, AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms and the like] or a salt thereof. A compound having prostaglandin production-suppressing action and leukotriene production-suppressing action is provided.

Abstract: Piperazinyl- or piperidinylamine-sulfamic acid amides and their use for the manufacture of a medicament in diseases mediated by the action of steroid sulfatase.

Abstract: The present invention relates to a crystalline polymorphic form of remifentanil hydrochloride. The invention also describes methods of preparing a polymorphic form of remifentanil hydrochloride.

Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

Abstract: A process for synthesizing remifentanil or carfentanil, as well as intermediates for use in the preparation of synthetic opiate or opioid compounds. The process comprising reacting a 4-amino 4-carbamyl piperidine with a base in a closed reaction chamber at elevated temperature and pressure to form to intermediate which may be esterified with an alcohol, alkylated, and acylated to produce a synthetic opiate or opioid compound.

Abstract: The invention concerns a novel method for preparing N-aminopiperidine of formula (I):

Abstract: The present invention relates to a process for the preparation of compounds of the general formula (I). These are used as important intermediates in the preparation of bioactive substances. Preparation is carried out starting from dicarbonyl compounds of the general formula (II), which are reacted with appropriate hydrazine derivatives of the general formula (III) and subsequently hydrogenated. The present invention also relates to advantageous intermediate compounds.

Abstract: Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.

Abstract: One aspect of the present invention relates to novel peptidomometic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize ? opioid receptors. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels and agonize or antagonize ?-opioid receptors.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

Abstract: Disclosed are urea compounds, stereoisomer, or pharmaceutical acceptable salt thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

Abstract: Disclosed are urea compounds of formula I, stereoisomer, or pharmaceutical acceptable salts thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CHNH2, R1 and R2 each is a hydrogen or a C1 to C20 aliphatic; aliphatic amine; an alicyclic; aromatic; heterocycle; and halogenated forms thereof; and wherein, a, b and c are integers from 0 to 12; R1, R2, R3, and R4 each is a hydrogen or a C1 to C20; aliphatic amine; an alicyclic; aromatic; a heterocycle; and halogenated forms thereof.

Abstract: To provide a novel compound which inhibits the generation of AGE and an AGE generation inhibitor containing the compound. A compound represented by the following formula or a pharmaceutically acceptable salt thereof, a medicinal composition containing the compound or such a salt thereof, and an additive composition containing the compound.

Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.

Abstract: The present invention relates to selected 4-imino-N-alkoxy-polyalkyl-peperidine compounds preparation, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 4-imino-N-alkoxy-polyalkyl-piperidine compound. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 4-imino-N-alkoxy-polyalkyl-piperidine compounds for controlled polymerization.

Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.

Abstract: Viscoelastic surfactants are described for use in aqueous systems to generate thickened fluids. The surfactants are alkyl amidoamine salts of inorganic acids and/or organic acids. The fluids may also contain inorganic salts, organic salts or mixtures thereof. Additionally, the fluids may contain a co-surfactant. These fluids are particularly useful in oilfield applications such as hydraulic fracturing, gravel packing, drilling, completion, etc. Viscoelastic fluids of the invention are also useful in industrial and consumer product fluid applications as rheology control agents.

Abstract: This invention relates to 3-amino piperidine derivatives, their intermediates and methods of manufacture. As such, the present invention includes methods of making a compound of the formulas (Ia) and (Ib) wherein R1, R2, R3, R4, R14, and n are herein defined. The present invention also relates to the compounds used in such processes, as well as the compounds made by the processes.

Abstract: The invention relates to a process for preparing a 4-amino-4-phenylpiperidine (I): in which R is hydrogen or a (C1–C3)alkyl group, characterized in that a 1-protected 4-piperidone (II): in which Pr? represents a removable N-protecting group, is treated sequentially first with an alkali metal cyanide and then with an amine ENHPr? (III) in which E represents a group R?=(C1–C3)alkyl, or an N-protecting group and Pr? is an N-protecting group, the protecting group(s) being removable under the same conditions as Pr?; then the compound thus obtained (IV) is subjected to a Grignard reaction with a phenylmagnesium halide, the two or three protecting groups are removed from the compound thus obtained (V) and compound (I) is isolated or in the form of the free base, which is converted into one of its salts.

Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.

Abstract: The present invention relates to a photo-stabilizer of the general formula (I): wherein R1 is hydrogen, halogen, C1 to C12 alkyl, alkoxy (linear and branched), R2 is hydrogen, C1-C8 alkyl, cyclopentyl, cyclohexyl or cumyl, R3 is hydrogen, C1-C4 alkyl, R4 is methyl or ethyl, R5 is C1-C8 alkyl, alkyl phenyl, alkoxy, acyl, cycloalkyl and allyl, X is O, NH, C1-C8 alkyloxy and alkylamino (linear or branched), to derivatives and intermediates thereof

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF? and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF? and/or one or more other involved cytokines, alone or in combination with other agents.

Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.

Abstract: A novel process for the asymmetric synthesis of substituted cyclic &bgr;-amino-carboxylates of the type shown in the specification from appropriate &bgr;-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE inhibitors.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): or pharmaceutically acceptable salt forms thereof, which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scanted candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.

Abstract: The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1 denotes 3-hydroxypropyl, 1,3-dihydroxyprop-2-yl or C3-C6-cycloalkylmethyl, and R2, R3, R4 and Ar have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: Vinylic hindered amine light stabilizers as novel polylmerizable light stabilizers are disclosed and have the general formula (I): wherein: R1 is C1 to C8: alkyl, alkoxy, alkyl phenyl, hydroxy alkyl (all linear and branched), allyl, acyl, cycloalkyl (cyclopentyl, cyclohexyl or curnyl: linear and branched); R2 is hydrogen and methyl, R3 is vinyl, C1-C4 vinyl alkyl [H2C═C(R4)C1-C4], R4 is H, C1-C4 alky and alkyl phenyl and R5 is H, C1-C4 alkyl, X is O, NH, C1-C8 alkyloxy and alkylamino: (linear or branched).

Abstract: Polymeric articles containing at least one polymeric material and a sufficient amount of at least one novel hindered amine light stabilizers to inhibit at least one of photo- or thermal degradation. The hindered amine light stabilizer may be a monomeric or an oligomeric hindered amine light stabilizer.

Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract: The invention relates to a compound comprising a reaction product of (A) an isocyanate functional compound of which at least 40 wt. %, relative to the total amount of (A), has a molecular weight of at least about 500, and (B) a nitrogen-containing compound capable of reacting with said isocyanate functional compound (A). The reaction product has a molecular weight of less then about 20,000 and comprises an effective amount of groups that are able to form reversible intermolecular physical interactions such that a resulting compound shows polymeric mechanical properties at a temperature below a transition temperature. The nitrogen-containing compound is, for instance, melamine, urea, acetoguanamine, benzoguanamine, cyanamide, dicyanamide, thiourea, isocytosine, pyrimidone or aminopyridine. The supramolecular compound comprising a suitable amount of the reaction products exhibits a relatively high elongation at break.

Abstract: Process for removing a residual fragment of a chiral auxiliary from a diastereomeric compound with formula (2) 1

Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

Abstract: A process for preparing an &agr;-haloketone of the formula (1) where R1 is an optionally heteroatom-containing and optionally substituted hydrocarbon radical, R2 is a hydrogen, alkyl, aralkyl or aryl radical, and X is a halogen radical, by reacting a carboxylic acid derivative of the general formula (2) where L is a leaving group, with a mono- or dienolate of a silyl ester of the formula (3) where R3 and R4 are identical or different alkyl, aryl, alkenyl or aralkyl radicals; and hydrolyzing the reaction product immediately afterwards by adding acid and decarboxylating to (1). The product &agr;-haloketone may be reduced to the corresponding &agr;-haloalcohol.

Abstract: Compounds of formula wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen an unsubstituted or substituted C1-C6alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(═O)—R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH—NO2, N—CN or N—NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se

Abstract: The present invention relates to selected 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 trimethyl piperidine derivatives which are substituted in the 4 position by an oxygen or nitrogen atom; a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) said piperidine derivatives. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,6 dimethyl piperidine derivatives which are substituted in the 4 position by an oxygen or nitrogen atom for controlled polymerization. The intermediate N-oxyl derivatives, a composition of the N-oxyl derivatives with ethylenically unsaturated monomers and a free radical initiator, as well as a process for polymerization are also subjects of the present invention.

Abstract: This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower &ohgr;-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.