Abstract: Administration of Oxybutynin directly to a patient's lungs for treating urinary incontinence, respiratory disease or IBD.

Abstract: The present invention relates to a crystalline oxybutynin base and process for preparing the same. Further, this invention discloses a process for preparing an acid addition salt of oxybutynin employing the crystalline oxybutynin base.

Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different as compared to the characteristics of the small molecule drug not attached to the water-soluble oligomer.

Abstract: The present application describes deuterium-enriched saxagliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.

Abstract: The present invention relates to a crystalline oxybutynin base and process for preparing the same. Further, this invention discloses a process for preparing an acid addition salt of oxybutynin employing the crystalline oxybutynin base.

Abstract: The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.

Abstract: The invention provides anticholinergic agents that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different as compared to the characteristics of the anticholinergic agent not attached to the water-soluble oligomer.

Abstract: Disclosed herein are substituted phenylcyclohexylglycolate-based muscarinic acetylcholine receptor modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group -R5 or a group, -Z-Y—R5, or a group -Z-NR9R10, or a group -Z-N(R9)C(O)R11; and R3 is a lone pair, or C1-C6-alkyl; R4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R5 is an C1-C6-alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R6 is C1-C6-alkyl or a hydrogen atom; R7a and R7b area C1-C6-alkyl group or halogen; n and m are independently 0, 1, 2 or 3; R8a and R8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl and hydrogen; R8c is —OH, C1-C6-alkyl, hydroxy-C1-C6-alkyl, or a hydrogen atom; R8d is C1-C6

Abstract: The present application describes deuterium-enriched oxybutynin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present application describes deuterium-enriched bazedoxifene, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Administration of Oxybutynin in nebulized dry powder form directly to a patient's lungs for treating urinary incontinence or respiratory disease.

Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: An oxybutynin and its derivatives are produced by reacting a phenylketone with a silylcyanide in the presence of a specified asymmetric catalyst to obtain a siloxynitrile, and then reacting the siloxynitrile with a reducing agent and oxidizing the resulting aldehyde, or subjecting the siloxynitrile to a hydrolysis.

Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.

Abstract: A urethane (meth)acrylate metal salt obtained by reacting (A) one or more polyisocyanates, (B) one or more hydroxy functional (meth)acrylates, and (C) one or more metal salt polyols which are the reaction product of a metal oxide and a half ester containing a hydroxy group and a carboxylic acid group. Processes of preparing such salts and polymers prepared from such salts are also disclosed. The polymers are useful for coating and adhesive compositions prepared by radiation or peroxide curing processes.

Abstract: A process for the preparation of optically active cyclohexylphenylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.

Abstract: Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.

Abstract: A universal linker for solid-phase nucleic acid synthesis that is cleaved under conditions orthogonal to those used during the synthesis and deprotection of nucleic acids such as dsDNA or RNA fragments is disclosed. The invention includes compounds of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of OH, OR.sub.2 and an amino functionalized support and n is an integer ranging from about 1 to about 1000 or more preferably from about 1 to about 100 or greater and R.sub.2 is an alkyl (C.sub.1-20) or greater.

Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.

Abstract: New chromoionophores of the formula IV ##STR1## wherein a=0-3, b=0 or 1, c =0 or 1, x=0 or 1, y=0 or 1, z=0 or 1,R', which may be the same or different in each aryl group, is H, halogen, hydrocarbyl, aryl, hydrocarbylaryl or a substituted derivative thereof;R, which may be the same or different, is hydrocarbyl, aryl, hydrocarbylaryl, or a substituted derivative thereofare useful in optical sensors or colourmetric reagents for clinical use particularly for lithium, When complexed with lithium, the chromoionophores of the invention and other calixarene derivatives can be used for detecting amines, particularly trimethylamine, as an indicator of fish spoilage.

Abstract: The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.

Abstract: Allylaminoesters of the formula (I): ##STR1## in which: R.sub.1 is H or low-molecular-weight alkyl,R.sub.2 is low-molecular-weight alkyl, cycloalkyl, or low-molecular-weight phenylcycloalkyl, pyridyl or phenyl, low-molecular-weight phenylalkyl, low-molecular-weight diphenylalkyl, low-molecular-weight phenylalkenyl, in which the phenyl cycle may be mono-, di- or trisubstituted by chlorine atoms, low-molecular-weight alkyl radicals, low-molecular-weight alkoxy, or trifluoromethyl, acetamide or acetyloxy radicals, their racemic forms, their (S) enantiomers and their addition salts. Also, antiallergic drugs containing the same.

Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.

Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.

Abstract: Pesticidal substituted acrylic esters of the formula ##STR1## in which R.sup.1 represents alkyl, or represents unsubstituted or substituted aralkyl,R.sup.2 represents dialkylamino, or represents a radical --Z--R.sup.3,R.sup.3 represents alkyl, or represents unsubstituted or substituted aralkyl,Z represents oxygen or sulphur,A represents ##STR2## where n represents a number from 0 to 6,R.sup.4 and R.sup.5 in each case independently of one another represent alkyl, or together represent an alkylene chain having 2 to 7 carbon atoms, andR.sup.6 represents alkyl, or represents a radical ##STR3## where R.sup.7 represents alkyl, alkoxy or dialkylamino,B represents the group CH--R.sup.8 or, whereR.sup.9 represents unsubstituted or substituted alkyl, alkenyl, alkynyl, aralkyl, aryl or hetaryl, andR and Q independently of one another represent hydrogen, alkyl, halogenoalkyl or alkoxy.

Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.

Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.

Abstract: A method for synthesizing an acyloxycarboxylic acid by providing a reaction chamber, establishing sources of an .alpha.-hydroxycarboxylic acid and an acid chloride, and repeatedly contacting substantially equal molar amounts of the .alpha.-hydroxycarboxylic acid and the acid chloride within the reaction chamber. The acyloxycarboxylic acid so synthesized is useful as a starting material for conversion to various esters which, when placed in aqueous solution with a source of hydrogen peroxide, result in a peracid and are useful for bleaching applications.

Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.

Abstract: Novel carbaphens are provided of the formula ##STR1## wherein R is OH, OCON(CH.sub.3).sub.2 or OCONHCH.sub.3, and R' is H, OH or sub.2 OCON(CH.sub.3).sub.2, stereoisomers thereof, pharmaceutically-acceptable salts thereof or mixtures thereof.Compositions comprise the carbaphens with pharmaceutically acceptable carriers, and they may further comprise other drugs as well.Methods of treating patients either prophylactically or therapeutically which suffer from organophosphate poisoning, coronary insufficiency, cerebral vasospasms, spastic cholitis and cholecystitis comprise the administration of the carbaphens of the invention.

Abstract: This invention discloses the use of muscarinic anti-cholinergic agents for reducing or preventing the toxic or lethal effects (such as seizures and brain damage) caused by cholinergic neurotoxins. The parent application disclosed that certain muscarinic anti-cholinergics classified as aryl-cycloalkyl-alkanolamines are effective in reducing or preventing the neurotoxicity of soman, a powerful nerve gas. This invention extends that discovery and identifies other muscarinic anti-cholinergic agents, including scopolamine, benactyzine, and benztropine, as highly effective and useful agents to protect against two major classes of cholinergic neurotoxins (acetylcholine receptor agonists, and cholinesterase inhibitors). Analogs of those compounds may also be effective in protecting against cholinergic neurotoxicity, as can be determined through routine screening tests using rats.

Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.

Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein N represents a tertiary aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.

Abstract: Novel hindered phenolic compounds derived from oxamides are disclosed which are useful as stabilizers of synthetic polymer resins.

Abstract: The present invention relates to new tricyclic compounds of the formula: ##STR1## having valuable CNS and cardiovascular properties.

Abstract: The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.

Abstract: Novel compounds of the formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are different lower alkyls and R.sup.3 is a lower alkyl or a methyl pyridine group, and the acid addition salts of formula (1) compounds when R.sup.3 is methyl pyridine. The novel compounds have an asymmetric C-atom and may be in the form of the D,L racemates or the D or L stereoisomers.These compounds are useful in the treatment of hypercholesterolemia and hyperlipidemia because of their high effectiveness in reducing the level of cholesterol and lipids in the blood combined with very low general toxicities and substantially reduced hepatomegalitic effects.

Abstract: Novel di-(substituted phenyl)methoxy acetic acids, alkyl homologues and related salts, ester and amides thereof, together with processes for their manufacture, and pharmaceutical compositions. A representative compound is di-(4-chlorophenyl)methyloxy acetic acid. The compounds possess anti-arthritic properties and in some cases, in addition, an effect on a factor involved in atherosclerotic disease.

Abstract: Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.

Abstract: The invention provides novel phenoxyalkylcarboxylic acids which are useful in therapy as metabolic regulators and in agriculture as selective herbicides.

Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholesterolaemiant and cholagogic agents or in the preparation of such agents.