Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Ar have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meaning indicated in the description, are novel active bronchial therapeutics

Abstract: A compound of the formula 1

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.

Abstract: Compounds of the formula 1

Abstract: The invention relates to novel substituted 2-amino-4-alkylamino-1,3,5-triazines of the formula (I) in which R1 represents in each case optionally substituted alkyl having 2 to 6 carbon atoms or cycloalkyl having 3 to 6 carbon atoms, R2 represents hydrogen or represents alkyl having 1 to 4 carbon atoms, A represents oxygen or methylene, Ar represents in each case optionally substituted phenyl, naphthyl or heterocyclyl, and Z represents hydrogen, represents halogen or represents in each case optionally substituted alkyl, alkoxy, alkylcarboxyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl or alkinyl, to processes and to novel intermediates for their preparation and to their use as herbicides.

Abstract: A novel compound N-demethyl-sinomenine, a metabolite of the anti-arthritic alkaloid sinomenine, has been identified and characterized. The compound may be incorporated in a pharmaceutical composition and may be administered to patients for treatment of various disorders, such as rheumatoid arthritis. The novel compound has superior biological activity and water solubility as compared to sinomenine.

Abstract: Magenta ink exhibiting excellent coloration on various recording materials is provided according to the present invention. The magenta ink can realize high image densities and can produce images having superior light resistance. The magenta ink contains first and second coloring materials represented by the following general formulae 1 and 2, respectively, and a water-based medium.

Abstract: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.

Abstract: Novel chemical analogs are disclosed for the essential heroin metabolite 6-O-acetyl morphine (6MAM). The analogs optionally can be made to contain protein reactive groups, and can be used to form protein conjugates, fluorescently labeled compounds, and solid-phase adsorbants. The proteins conjugates can be used in turn to raise antibodies reactive with 6MAM and having a low cross-reactivity with the closely related opiates, morphine and codeine. The antibodies can be used in combination with labeled analogs in exquisitely sensitive immunoassays suitable for testing for heroin abuse.

Abstract: This invention provides an antipruritic comprising an opiate &kgr; receptor agonist as an effective component, a new morphinan quaternary ammonium salt derivative and a new morphinan-N-oxide derivative which are useful in treating pruritus complicated with some diseases.

Abstract: Compounds of the formula I in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel efficacious bronchial therapeutics.

Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): ##STR1## wherein a, b, A, R.sup.1, L.sup.1, D, R.sup.3, R.sup.4, R.sup.2, L.sup.2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.

Abstract: The invention provides processes for the conversion of normorphinone and its derivatives, which can be synthesized from morphine, to the corresponding 14-hydroxynormorphinone and its derivatives including oxycodone, oxymorphone, noroxymorphone and naltrexone. Noroxymorphone is a key intermediate for the production of important narcotic analgesics and antagonists. The invention also provides certain novel intermediates.

Abstract: Normorphine and normorphinone derivatives are provided as compositions of matter.

Abstract: (9.alpha., 13.alpha.,14.alpha.)-1-(3-Methoxymorphinan-17-yl)alkanones of the formula ##STR1## wherein R signifies lower alkanoyl, are valuable intermediates for the manufacture of dextromethorphan of the formula ##STR2## They can be produced in an advantageous manner by cyclization of a (R)- or (S)-1-?1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydro-isoquinolin-2-yl!alka none of the formula ##STR3## with an alkylsulfonic acid or a mixture of alkylsulfonic acids at a temperature between about 5.degree. and 50.degree. C., but above the melting point of the alkylsulfonic acid used or of the alkylsulfonic acid mixture used, and can be converted into dextromethorphan in a manner known per se by cleavage or the residue R and N-methylation.

Abstract: The present invention is directed to certain novel compounds identified as bridged piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.3, R.sup.3a,R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: A process for the preparation of a .gamma.-lactone of the formula ##STR1## which can be used to produce a single enantiomer of aminoazanoradamantane which is coupled to aromatic acid moieties to produce compounds useful as 5-HT agonists or antagonists.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D-DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine .revreaction. pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.2 or OH functional group to the carbonyl function of [DHC], then [D] must be other than a sympathetic-stimulant, steroid sex hormone or long chain alkanol; and(b) non-toxic pharmaceutically acceptable salts of compounds of formula (I). The corresponding ionic pyridinium salt type drug/carrier entities [D-QC].sup.+ X.sup.- are also disclosed.

Abstract: Process for the preparation of 3,14.beta.-dihydroxy-17-normorphinan ##STR1## A suitable economic process for the preparation of 3,14.beta.-dihydroxy-17-normorphinan of a general formula (I) is being solved, which is a key intermediate of a semisynthetic synthesis of an effective analgesic of Butorphanol from thebaine.Synthesis includes a two step N-demethylation, and concerted dephenoxylation of 4-phenoxy-14.beta.-hydroxy-3-methoxymorphinan in the first step by means of a chloroformate, then, in the second step, by means of sodium action in a liquid ammonia, and by means of the following O-demethylation under action of a complex of aluminium chloride - dialkylsulfide.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: There are disclosed compounds having the formula ##STR1## wherein R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; R.sub.2 and R.sub.3 are independently H or CH.sub.3 ; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6 where R.sub.4 is hydrogen or loweralkyl, and R.sub.5 and R.sub.6 are independently hydrogen, loweralkyl or cycloalkyl; Y and Z are independently a direct bond, CR.sub.7 R.sub.8 or CR.sub.7 R.sub.8 --CR.sub.9 R.sub.10 ; and L and Q are independently CR'.sub.7 R'.sub.8, CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10, CR'.sub.7 .dbd.CR'.sub.9 or CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10 --CR.sub.11 R.sub.12, where each of R.sub.7 through R.sub.12 and R'.sub.7 through R'.sub.

Abstract: Anthraquinone dyes of the formula ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3 and n are as defined in claim 1, produce dyeings having good fastness properties on nitrogen-containing or hydroxyl-containing fibre materials.

Abstract: It has been discovered that certain (+)-3-substituted-N-alkylmorphinans are ffective anticonvulsant and neuroprotective agents. Novel compounds having these biological properties are presented in a method of use for preventing, treating or controlling convulsions in mammals having a need for such treatment. The compounds do not lead to dependency, have low toxicity, and provide effective anticonvulsant or neuroprotective treatment with little or no behavioral detriment to the recipient. A number of pharmacological formulations and methods of administering compounds of the invention are suitable for anticonvulsive or neuroprotective treatments.

Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl;Y is CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.

Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.

Abstract: Compounds of formula I ##STR1## wherein X and Y each denotes hydrogen or together denote -0-,R.sub.1 denotes allyl optionally substituted by 1 to 3 alkyl groups, the substituent or substituents having in total a maximum of 3 carbon atoms, cyclopropyl-methyl or 3-furylmethyl,R.sub.2 denotes hydrogen, alkyl with 1 to 10 C-atoms, cycloalkyl with 5 or 6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl-alkyl with 7 to 12 C-atoms,R.sub.3 denotes hydrogen, alkyl with 1 to 10 C-atoms or phenyl,R.sub.4 denotes hydrogen, OH, NR.sub.6 R.sub.7, NHCOR, NHSO.sub.2 R' or NHCOOR",R.sub.6 and R.sub.7, independently of one another, denote hydrogen or alkyl with 1 to 3 C-atoms,R denotes alkyl with 1 to 6 C-atoms, phenyl or --A--COOR",A denotes alkylene or alkenylene each with 2 to 4 C-atoms,R' denotes alkyl with 1 to 6 C-atoms or phenyl,R" denotes methyl or ethyland wherein either R.sub.3 is in the .alpha.-positionand R.sub.4 is in the .beta.-position, or R.sub.3 is in the .beta.position and R.sub.

Abstract: There are disclosed compounds having the formula ##STR1## wherein R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; R.sub.2 and R.sub.3 are independently H or CH.sub.3 ; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sup.6 where R.sup.4 is hydrogen or loweralkyl, and R.sub.5 and R.sub.6 are independently hydrogen, loweralkyl or cycloalkyl; Y and Z are independently a direct bond, CR.sub.7 R.sub.8 or CR.sub.7 R.sub.8 -CR.sub.9 R.sub.10 ; and P and Q are independently CR.sub.7 'R.sub.8 ', CR.sub.7 'R.sub.8 '-CR.sub.9 'R.sub.10 ' or CR.sub.7 'R.sub.8 '-CR.sub.9 'R.sub.10 '--CR.sub.11 R.sub.12, where each of R.sub.7 through R.sub.12 and R.sub.7 ' through R.sub.10 ' is independently H or CH.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: Dihydromorphinone compound of the general formulaHDM.dbd.N--Rwherein ##STR1## where * indicates binding carbon R1 is an optionally substituted alkyl, alkylene, cycloalkyl, or cycloalkyleneR2 is OH or HR3 is OH or OCH3 andR is N.dbd.R4, N--R4, ##STR2## R4 is an optionally substituted alkyl, alkylene, cycloalkyl, cycloalkylene, aryl, heterocycloalkyl, heterocycloalkylene, or alkenyl, andn is 1-10, and use thereof as an opiate receptor blocker.

Abstract: Fluorescent reagents useful as opioid receptor probes. Opioids labeled at the 3 position with fluorescers are useful in various in vivo and in vitro methods for the detection and quantification of receptor sites in tissue cells and subcellular particles.

Abstract: Methyllevallorphanium salts having peripheral antagonistic activity of formula ##STR1## wherein Y.sup.n(-) represents the anion a pharmaceutically acceptable acid other than halogen and n represents the number of negative charges of said anion; a process for their preparation by exchange of the halogen ion with the Y.sup.n(-) anion; and pharmaceutical compositions containing them as active ingredients.

Abstract: Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans are useful as analgesics or narcotic antagonists and provide enhanced bioavailability of 3-hydroxymorphinans from orally administered doses.

Abstract: An improved process for the dealkylation of alkyl aryl ethers to aryl phenols is provided. In this process, an alkyl aryl ether, such as a methyl ether of an opioid, is contacted with an aqueous acid selected from HBr, HCl, or HI which contains at least one equivalent weight, based on the ether, of boric acid or an inorganic salt of a metal selected from Li, Na, K, Al, Mg, Ca, Mn and Ni. MgBr.sub.2 in aqueous HBr is preferred in dealkylating an N-substituted 14-hydroxydihydronorcodeine.

Abstract: There is disclosed herewith a method of producing morphinan compounds by total synthesis which incorporates utilization of N-cycloalkylcarbonyl compounds, which show certain advantages over the prior art which has been previously expressed in U.S. Pat. No. 4,368,326.

Abstract: Dihydromorphinone compound of the general formulaHDM.dbd.N--RwhereinHDM is ##STR1## where * indicates binding carbonR1 is an optionally substituted alkyl, alkylene, cycloalkyl, or cycloalkyleneR2 is OH or HR3 is OH or OCH3 andR is N.dbd.R4, N--R4, ##STR2## R4 is an optionally substituted alkyl, alkylene, cycloalkyl, cycloalkylene, aryl, heterocycloalkyl, heterocycloalkylene, or alkenyl, andn is 1-10, and use thereof as an opiate receptor blocker.

Abstract: Novel substituted and bridged pyridine compounds useful as calcium channel blockers and analgesics, pharmaceutical compositions thereof, and methods of treatment are disclosed.

Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.

Abstract: The present invention is concerned with dextrorotatory morphinans, which are illustrated by (+)-4-methoxy-6-keto-N-methylmorphinan. Related compounds which also have been introduced as cough-suppressing agents include the (+)-3-methoxy-N-methylmorphinans (ROMILAR-Roche).

Abstract: This invention relates to compounds which may be described as the unnatural enantiomers of morphine agonists and antagonists, which are useful as antitussives. The synthesis utilized is capable of producing all of the unnatural enantiomers of medically important opium derivatives of the morphinan type, including thebaine.

Abstract: A complex of 3-methoxy-N-methylmorphinan with 7-theophyllineacetic acid (1:2) is prepared by reacting the reactive materials in a polar solvent. The complex has antitussive activity.

Abstract: A method for the synthesis of particular isoquinoline compounds which are useful intermediates in the preparation of members of the family of opium alkaloids, such as morphine and codeine. Steps in the process include the acylation of the isoquinoline nitrogen; reaction of the acylated isoquinoline with a phosphorous compound; and condensation with a benzaldehyde derivative to yield a 1-benzyl isoquinoline.

Abstract: An improved method for preparing a compound having the formula ##STR1## which is an intermediate in the preparation of dextromethorphan, the improved method comprises the steps of(A) hydrogenating a compound having the formula ##STR2## in the presence of a hydrogenation catalyst to obtain a compound having the formula ##STR3## (B) hydrogenating the product of Step (A) in the presence of a hydrogen treated rhodium catalyst to obtain a compound having the formula ##STR4## (C) reacting the product of Step (B) with 4-methoxyphenylacetic acid to obtain a mixture of compounds comprising ##STR5## (D) dehydrating the product mixture of Step (C).

Abstract: Dyes of the formula ##STR1## in which D is an organic dye radical which contains at least one group conferring solubility in water, R is a halogenoalkyl radical having 1 to 2 C atoms or a halogenoacryl radical and n is an integer from 1 to 4 and each group of the formula ##STR2## is bonded to D via an aromatic carbon atom, are prepared by reacting the corresponding dye compounds of the formula D--H).sub.n with halogenoalkanoylamidoglycolic or halogenoacryloylamidoglycolic acids and are suitable for dyeing cellulose and polyamide materials.

Abstract: The present invention involves 7-carboethoxymorphinan-6-one compounds of the formula: ##STR1## These compounds are useful as analgesic and/or narcotic antagonists.

Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.

Abstract: 6-Keto-hydroxymorphinans having at the 4 position a substituent which is R.sub.1 =H, O lower alkyl, or O lower acyl, and N may be substituted by R.sub.2, which for agonist properties may be lower alkyl, lower alkenyl, cyclopropylmethyl, or phenyl lower alkyl, etc. Additionally, the nitrogen may be substituted by R.sub.2, which is allyl, cyclopropylmethyl, cyclobutylmethyl, dimethylallyl, etc., which function as antagonists to the morphine-like activity of the compound. Such activity is known as antinociceptive.

Abstract: This patent application describes the preparation and properties of novel and highly potent morphinan analgesics. The compounds include narcotic agnoists as well as narcotic antagonists and are represented by the following formula: ##STR1## R.sub.1 =OCH.sub.3, OCOCH.sub.3, H R.sub.2 =CH.sub.3, CH.sub.2 --CH.dbd.CH.sub.2, ##STR2## CH.sub.2 CH.sub.2 C.sub.6 H.sub.

Abstract: Levorotatory N-substituted acylmorphinans of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl-lower alkyl, cyano-lower alkyl, aryl-lower alkyl, or 5- or 6-membered heterocyclic-lower alkyl, and one of R.sub.2 or R.sub.3 is hydrogen and the other of R.sub.2 or R.sub.3 is alkanoyl of 2 to 7 carbon atoms, aroyl, trifluoromethylcarbonyl or ##STR2## wherein R is hydrogen or lower alkyl and n is an integer of 0 to 6, and salts thereof with pharmaceutically acceptable acid addition salts, are described. The compounds of formula I are useful as analgesic agents.