Abstract: The present disclosure is concerned with a process for the preparation of the above disclosed compounds, pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, or mixtures thereof which comprises subjecting a 17-substituted-3,14-dihydroxypyridomorphinan to dialkylation at the phenolic hydroxyl at the 3-position and the tertiary alcohol at the 14-position followed by selective dealkylation of the phenolic ether function.

Abstract: A morphinan derivative represented by the following general formula (I): (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

Abstract: The present invention relates to a new amorphous form of rifaximin and to methods for the preparation thereof by means of high energy milling or Spray drying. The present invention further relates to a new amorphous form for use as medicament and to the pharmaceutical compositions composing it.

Abstract: The present invention discloses an application of koumine and homologue thereof in preparation of drugs for treating autoimmune diseases involving bones and joints including rheumatoid arthritis, spondylitis ankylopoietica or the like, in particular an application of Gelsemium alkaloid monomer koumine and homologue thereof or pharmaceutically acceptable salt thereof as active ingredient in preparation of drugs for treating autoimmune diseases involving bones and joints including rheumatoid arthritis, spondylitis ankylopoietica or the like.

Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.

Abstract: The invention relates to novel fluorescent dyes with phosphorylated hydroxymethyl groups, a method for preparing the same as well as to their use in imaging techniques. The fluorescent dyes are coumarin, rhodamine or BODIPY dyes having of one of the following general formulae I-III: wherein W=OP(O) Y1Y2 or P(O) Y1Y2, where Y1 and Y2 independently denote any of the following residues: OH, O(?), ORa and ORb, NHRa and NHRb, NRaRb and NRcRd, ORa and NHRb, ORa and NRbRc, NHRa and NRbRc; and any salt thereof.

Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.

Abstract: The present invention discloses a stable amorphous form of Rifaximin characterised by having X-ray powder diffraction pattern as given in FIG. 1, having a 2? peaks at 7.2 and having moisture content in the range of 3% to 4% preferably, 3.4% to 3.7%. This invention also discloses a novel process for its preparation.

Abstract: The present invention relates to new rifaximin forms kappa, theta, rifaximin:piperazine cocrystal 1 and rifaximin:piperazine cocrystal 2, methods of making same and to their use in medicinal preparations and therapeutic methods.

Abstract: A topical foam pharmaceutical composition for rectal administration comprising rifaximin is described. Also described is a method of making the composition and the use of the composition as a medicament.

Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin ? and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.

Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.

Abstract: The present invention relates to a new amorphous form of rifaximin and to methods for the preparation thereof by means of high energy milling or Spray drying. The present invention further relates to a new amorphous form for use as medicament and to the pharmaceutical compositions composing it.

Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin ? and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: A method for identifying the redox activity of a subject compound is disclosed. The method can be performed aerobically and can include forming a mixture comprising a free-radical precursor and a compound to be tested, and converting the free-radical precursor into a free-radical anion and a free-radical cation. After the free radical cation and the free radical anion have been formed, the relative redox activity of the subject compound may cause a difference in the rate of photo-bleaching of the mixture and/or the rate of superoxide generation. These differences can be quantified and used to identify the redox activity of the subject compound. This sensitive technique for measuring redox activity can be used to screen compounds for various biological applications. Drugs also can be developed based on the relationship between redox activity and biological activity for particular biological applications.

Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.

Abstract: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to ? agonists.

Abstract: This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates and to processes which utilise such intermediates in the synthesis of morphinane compounds.

Abstract: The present invention relates to novel sequences for use in detection, diagnosis and treatment of bowl disease (BD). The invention provides BD-associated polynucleotide sequences whose expression is associated with BD. Provided herein are diagnostic compositions and methods for the detection of BD. The present invention provides monoclonal and polyclonal antibodies specific for the BD polypeptides. The present invention also provides diagnostic tools and therapeutic compositions and methods for screening, prevention and treatment of BD.

Abstract: Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.

Abstract: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to ? agonists.

Abstract: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to ? agonists.

Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: Compounds represented by the formulae: wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is selected from the group consisting of alkyl, aryl, alkaryl, and NH2, and R2 is selected from the group consisting of alkyl, aryl and aralkyl, and provided that at least one of Y, X and R is other than H; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain, as immunomodulators and for treating drug abuse.

Abstract: The present invention relates to an efficient procedure for the synthesis of deserpidine (Ia), starting from reserpic acid lactone (II) via the intermediate 11-O-demethyl reserpic acid lactone (III).

Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin ? and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: The present invention relates to an efficient procedure for the synthesis of deserpidine (Ia), starting from reserpic acid lactone (II) via the intermediate 11-O-demethyl reserpic acid lactone (III).

Abstract: Novel N-oxides of 4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the N-oxides of 4,5-epoxy-morphinanium analogs and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as modulators of opioid receptors.

Abstract: Compounds represented by formula (I) wherein R is C1-6cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence of ? agonists.

Abstract: Tert-alkylphenoxy-substituted polycyclic compounds of the general formula I where P is a conjugated polycyclic radical which is stable to bases and nucleophiles, optionally bears aryl substituents and contains no group from the group consisting of —CO—NH—CO—, —COOH and —CO—O—CO—; R is C1–C8-alkyl, whose carbon chain may be interrupted by one or more groups selected from the group consisting of —O—, —S—, —NR1—, —CO— and/or —SO2— and which may be monosubstituted or polysubstituted by C1–C6-alkoxy or by a 5- to 7-membered heterocyclic radical which is attached via a nitrogen atom and may contain further heteroatoms and be aromatic; C5–C8-cycloalkyl whose carbon chain may be interrupted by one or more groups selected from the group consisting of —O—, —S—, —NR1—, —CO— and/or —SO2— and which may be monosubstituted or polysubstituted by C1–C6-alkyl; R1 is hydrogen or C1–C6-alkyl; Hal is chlorine and/or bromine; m is from 0 to 15; n is from 1 to 16, subject to the proviso that the sum m+n is ?16, are prepared a

Abstract: Compounds represented by the formulae: wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is selected from the group consisting of alkyl, aryl, alkaryl, and NH2, and R2 is selected from the group consisting of alkyl, aryl and aralkyl, and provided that at least one of Y, X and R is other than H; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain, as immunomodulators and for treating drug abuse.

Abstract: Compounds represented by the formulae: wherein each of Y, X and R individually is selected from the group consisting of hydrogen hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is selected from the group consisting of alkyl, aryl, alkaryl, and NH2, and R2 is selected from the group consisting of alkyl aryl, and aralkyl, and provided that at least one of Y, X and R in formula I is other than hydrogen; and pharmaceutically acceptable salts thereof are provided along with uses as immunodulaters and/or treating for drug abuse and/or as analegesics for treating pain.

Abstract: The epindolidione compounds of the general formula (I) 1

Abstract: This invention features ring-substituted pyrrolo-&bgr;-carboline derivatives and ring-substitution and structural derivatives of 3-(1H-indol-3-yl)-1H-pyrrole-2,5-dione of formulas (I-III), which are useful as neuroprotective and anti-proliferative compounds. Also disclosed are methods for the preparation of these compounds, selected biological profiles and uses of these compounds in the treatment of various neurodegenerative and inflammatory diseases of the human nervous system and in the treatment of various other proliferative disorders characterized by loss of growth or cellular differentiation control including, but not limited to, cancer and inflammation.

Abstract: Compounds represented by the formula: 1

Abstract: Compounds represented by the formula: wherein each of Y, X and R individually is H, OH, alkyl, alkoxy, aryl, halo, CF3 and NO2, provided that at least one of Y, X and R is other than H; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain, as immunomodulators and for treating drug abuse.

Abstract: Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.

Abstract: A compound comprising a ligand portion which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group selected from radionuclide chelating agents, fluorochromes, toxins, drugs, polyboron moieties, proteins, biological response modifiers, chemical moieties capable of binding to other molecules of interest, and radioisotopes selected from therapeutically effective alpha and beta emitters, and diagnostically effective gamma emitters. The compound may be used in a method of treating cancer, and in a method of imaging opioid receptors either inside or outside of the central nervous system.

Abstract: The compounds of structural formulae (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents, is disclosed. A compound of formula (I) or (II) is an agonist for the &mgr; and &dgr; opioid receptors, an antagonist for the &kgr; opioid receptor, and has high affinity at all three receptors. A compound of formula (I) or (II) has utility in a variety of therapeutic and research areas where &kgr; opioid receptor antagonism is beneficial, including the treatment of opiate addiction or pain, or in a method of stimulating an immune system of a human.

Abstract: Quaterrylenetetracarboxylic diimides I ##STR1## where R is hydrogen;C.sub.1 -C.sub.30 -alkyl whose carbon chain may be interrupted by one or e of --O--, --S--, --NR.sup.1 --, --CO-- and/or --SO.sub.2 -- and which may be monosubstituted or polysubstituted by cyano, C.sub.1 -C.sub.6 -alkoxy or a 5-, 6- or 7-membered heterocyclic radical which is attached via a nitrogen atom and which may contain further heteroatoms and may be aromatic, whereR.sup.1 is hydrogen or C.sub.1 -C.sub.6 -alkyl;C.sub.5 -C.sub.8 -cycloalkyl whose carbon skeleton may be interrupted by one or more of --O--, --S-- and/or --NR.sup.1 --;aryl or hetaryl, which may each be monosubstituted or poly-substituted by C.sub.1 -C.sub.18 -alkyl, C.sub.1 -C.sub.6 -alkoxy, cyano, --CONHR.sup.2, --NHCOR.sup.2 and/or aryl- or hetaryl-azo, which may each be substituted by C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.6 -alkoxy or cyano, whereR.sup.2 is hydrogen; C.sub.1 -C.sub.18 -alkyl; aryl or hetaryl, which may each be substituted by C.sub.1 -C.sub.

Abstract: Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders.

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: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.

Abstract: A compound of the formula: ##STR1## A process for its preparation and pharmaceutical compositions comprising the compound or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The compound exhibits analgesic activity.

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

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

Abstract: 10-bromosandwicine and 10-bromoisosandwicine and acid addition salts thereof are disclosed. There novel compounds possess valuable pharmacological properties e.g. heart rhythm regulatory properties. Furthermore they are valuable intermediates for the preparation of 10-brominated N.sub.b -quaternary sandwicine derivatives which exhibit heart rhythm regulatory and adrenolytic properties. 10-bromosandwicine is prepared by brominating sandwicine and can subsequently be isomerized into 10-bromoisosandwicine.