Abstract: Provided are compounds that can act as a modulator of a farnesoid X receptor (FXR) and that can be useful in the treatment of diseases and/or disorders associated with the FXR such as bile acid related disorders, metabolic syndrome, type-2-diabetes, hyperlipidemia, hypertriglyceridemia, primary biliary cirrhosis (PBC), fatty liver disease, nonalcoholic steatohepatitis (NASH), inflammatory autoimmune diseases, Crohn's disease, multiple sclerosis, atherosclerosis, kidney disorders (including chronic kidney disease), hepatic and colon cancers, and other disorders. The compounds are in the class of sulfinic acid compounds and can be an enantiomer, stereoisomer, tautomer, solvate, hydrate, prodrug, metabolite, or pharmaceutically acceptable salt thereof. Compositions including such compounds are also provided along with methods for preparing compounds of the present invention and their use.

Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.

Abstract: The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.

Abstract: Disclosed are benztropine analogs having the formula (I) in which Ar is a C6-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl, heterocyclic, or arylheterocyclic group having 2 to 12 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, P, and any combination thereof; m=1 to 5; n=1 to 3; and R1 to R4 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.

Abstract: The present invention relates to the use of an anesthetic agent for killing clinically latent microorganisms associated with microbial infections and to novel combinations comprising an anesthetic agent and an antimicrobial agent for the treatment of microbial infections.

Abstract: The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.

Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.

Abstract: The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.

Abstract: The present invention relates to anti-drug vaccines based on conjugates between the drug and a non-immunogenic carrier protein. In preferred embodiments, it provides for anti-cocaine vaccines and their use to diminish the effects and/or use of cocaine in a subject.

Abstract: Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.

Abstract: There is provided a process for the preparation of a single enantiomer of anhydroecgonine (of formula I): or a salt thereof, in which R1 is as defined in the description. Such single enantiomers may, for example, be useful intermediates in the synthesis of pharmaceuticals, in which the enantioselectivity is important.

Abstract: The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.

Abstract: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.

Abstract: This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.

Abstract: A compound of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R1 and R2 are each independently a C1-C4-alkyl optionally substituted with hydroxy or halogen; and R3, R4, R5, R6, R7, and R8 are each independently hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, CF3, CN, NO2, or halogen, with the proviso that at least one of the groups R3, R4, R5, R6, R7, and R8 is not hydrogen, processes for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as pharmaceutical compositions.

Abstract: Processes for preparing tropine derivatives of the following Formula B are provided where LG represents a leaving group. The tropine derivatives may be used to prepare Retapamulin, preferably in substantially pure form.

Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Disclosed are (i) compounds of a steroid, a ?-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, ?-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO?), or as the neutral species, nitric oxide (NO.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

Abstract: A mixture of isolated or synthetic affinity molecules in a liquid carrier is disclosed. The mixture comprises at least two different affinity molecules, each with affinity for a predetermined analyte, for use in a single or multi flow cell piezoelectric crystal micro balance apparatus. Each isolated or synthetic affinity molecule forms together with the predetermined analyte an interaction pair selected from the group consisting of anion-cation, antibody-antigen, receptor-ligand, enzyme-substrate, oligonucleotide-oligonucleotide with complementary sequence, oligonucleotide-protein, oligonucleotide-cell, and peptide nucleic acid (PNA) oligomer-polynucleotide, wherein the polynucleotide may be selected from the group consisting of RNA, DNA and PNA polymers complementary to PNA oligomer. Use of the mixture for introduction into the liquid flow of a single or multi flow cell piezoelectric crystal micro balance apparatus is also described, as well as a kit containing the mixture.

Abstract: The present invention relates to new compounds of general formula 1 wherein X? and the groups A, B, R, R1, R2, R3, R3?, R4, R4?, Rx and Rx? may have the meanings given in the claims and in the specification, processes for preparing them and their use as pharmaceutical compositions.

Abstract: A compound of formula 1 wherein X?, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.

Abstract: The invention disclosed herein relates to novel a 8-azabicyclo[3.2.1]oct-2-ene compound of Formula II, wherein R is hydrogen, methyl, ethyl or benzyl; and R1 is 3-thienyl, 2-thienyl, 2-(3-methoxymethyl), 3-quinolinyl, 3-benzofuryl, 2-benzofuryl, 3-benzothienyl, 2-benzothienyl, 2-benzothiazolyl, 2-thieno[3.2-b]thienyl, thieno[2.3-b]thienyl, 2-(3-bromo)benzofuryl or 2-(3-bromo)benzothienyl. These compounds are useful for the treatment of conditions or disorders involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and in the cessation of chemical substance abuse.

Abstract: A compound of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R1 and R2 are each independently a C1-C4-alkyl optionally substituted with hydroxy or halogen; and R3, R4, R5, R6, R7, and R8 are each independently hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, CF3, CN, NO2, or halogen, with the proviso that at least one of the groups R3, R4, R5, R6, R7, and R8 is not hydrogen, processes for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as pharmaceutical compositions.

Abstract: This invention provides a method for preparing a benzoylecgonine composition comprising the steps of: (a) contacting benzoylmethylecgonine and propylene glycol in the presence or absence of water to form a reaction mixture; (b) maintaining the reaction mixture at a temperature between about 50° and 100° C.; and (c) subsequently or simultaneously removing water from the reaction mixture. This invention also provides novel benzoylecgonine and methods for producing them.

Abstract: The present invention relates to new anticholinergics of general formula 1: wherein A, X− and the groups R1, R2, R3, R4, R5, R6 and R7 may have the meanings given in the claims and in the specification, processes for preparing them and their use as pharamaceutical compositions.

Abstract: The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of chemical substances.

Abstract: The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein - - - - is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; or aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalklyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen,

Abstract: The ethyl ester of derivatives of benzoyl ecgonine are provided having a linking group at the para position of the benzoyl group. The derivatives are used to bond to immunogenic polypeptides for production of antisera and monoclonal antibodies. The antisera and antibodies find use in assays, for treatment of cocaine overdose and detoxification.

Abstract: An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee.

Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.

Abstract: The ethyl ester of derivatives of benzoyl ecgonine are provided having a linking group at the para position of the benzoyl group. The derivatives are used to bond to immunogenic polypeptides for production of antisera and monoclonal antibodies. The antisera and antibodies find use in assays, for treatment of cocaine overdose and detoxification.

Abstract: An anti-cocaine vaccine employs a cocaine hapten conjugated to a carrier protein. The anti-cocaine vaccine elicits an immune response which reduces the psychoactive effects of cocaine consumption by the production of anti-cocaine polyclonal antibodies. The antibodies may be employed in an ELISA test for assaying cocaine. The immune response elicited by the anti-cocaine vaccine produces antibody producing cells which may be isolated and cloned for producing anti-cocaine monoclonal antibodies.

Abstract: A method for preparing a cocaine-protein conjugate easily by using a cocaine derivative having a methoxy carbonyl group and benzoyl group. This conjugate is useful for the detection of cocaine or cocaine derivatives.

Abstract: A method for preparing a cocaine-protein conjugate easily by using a cocaine derivative having a methoxy carbonyl group and benzoyl group. This conjugate is useful for the detection of cocaine or cocaine derivatives. A monoclonal antibody, a monoclonal antibody producing cell line, and a method for producing the monoclonal antibody producing cell line by using the above cocaine-protein conjugate as an immunogen is also described.

Abstract: The ethyl ester of derivatives of benzoyl ecgonine are provided having a linking group at the para position of the benzoyl group. The derivatives are used to bond to immunogenic polypeptides for production of antisera and monoclonal antibodies. The antisera and antibodies find use in assays, for treatment of cocaine overdose and detoxification.

Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.

Abstract: Hapten-carrier conjugates capable of eliciting anti-hapten antibodies in vivo are disclosed. Methods of preparing the hapten-carrier conjugates and therapeutic compositions are also disclosed. Where the hapten is a drug of abuse, a therapeutic composition containing the hapten-carrier conjugate is particularly useful in the treatment of drug addiction, more particularly, cocaine addiction. Passive immunization using antibodies raised against conjugates of the instant invention is also disclosed. The therapeutic composition is suitable for co-therapy with other conventional drugs.

Abstract: Hapten-carrier conjugates capable of eliciting anti-hapten antibodies in vivo are disclosed. Methods of preparing the hapten-carrier conjugates and therapeutic compositions are also disclosed. Where the hapten is a drug of abuse, a therapeutic composition containing the hapten-carrier conjugate is particularly useful in the treatment of drug addiction, more particularly, cocaine addiction. Passive immunization using antibodies raised against conjugates of the instant invention is also disclosed. The therapeutic composition is suitable for co-therapy with other conventional drugs.

Abstract: Hapten-carrier conjugates capable of eliciting anti hapten antibodies in vivo by administering, in a therapeutic composition, are disclosed. Anti-hapten antibodies elicited compete with free hapten upon subsequent challenge of a vaccinated individual. Methods of preparing said conjugates and therapeutic compositions are also disclosed. Where the hapten is a drug of abuse, a therapeutic composition containing the hapten-carrier conjugate is particularly useful in the treatment of drug addiction, more particularly, cocaine addiction. Passive immunization using antibodies raised against conjugates of the instant invention is also disclosed. The therapeutic composition is suitable for co-therapy with other conventional drugs.

Abstract: The synthesis and the application of new dyes is described. In particular said new dyes can be incorporated in non-migratory state in hydrophilic colloid layers of photographic materials wherefrom they can be rapidly removed after being quickly decolorized in alkaline aqueous liquids used in the processing of said materials. In photographic applications dyes of the general formula (I) are provided with at least one ionisable group which permits solubilization in aqueous and/or alkaline medium. ##STR1## The meanings of the symbols are as defined in the claims and in the description.

Abstract: A benzoylecgonine conjugate represented by the following formula: ##STR1## wherein, R is H or CH.sub.3 ; R' is --NH--NH--, --(NH).sub.2 --CO--(CH.sub.2).sub.n --CO--NH--NH--, or related linear chains wherein at least one (CH.sub.2) is replaced with a substituent selected from the group consisting of an ether, an amide, a sulfide, a disulfide, an alkyl, an aryl, an alkoxy, an aryloxy or an alkylhalide; and T is a targeting substance selected from the group consisting of proteins, peptides, antigens, polypeptides, dyes, biotins, enzymes, antibodies, hormones, carbohydrates, polysaccharide supports, and filter paper.

Abstract: Disclosed are bridge-substituted analogs of tropanes and benztropines as well as methods for: imaging of cocaine receptors; treatment of cocaine abuse; and imaging and treatment of Parkinson's disease.

Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.

Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.

Abstract: The present invention relates to a novel class of benzoylecgonine, ecgonine and ecgonidine derivatives which are useful for preventing and treating immunoregulatory disorders, neuromuscular. disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. The compounds of this invention are conveniently obtained by chemical synthesis. Accordingly, this invention also relates to methods for preparing the benzoylecgonine, ecgonine and ecgonidine derivatives and to pharmaceutical compositions containing these derivatives.

Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.

Abstract: Compounds of general formula: ##STR1## where: Ar=phenyl or beta-naphtyl, or aromatic heterocyclic 6-membered ring containing one or two nitrogen atoms;R.sub.1 =one or more substituents of the Ar nucleus, preferably in para position, and selected out of the group consisting of H, CH.sub.3, CH.sub.2 --CH--(CH.sub.3).sub.2, O--CH.sub.3, Cl, F, Br, CF.sub.3, NH.sub.2, S--CH.sub.3, CN, NO.sub.2 R.sub.2 =H, CH.sub.3, C.sub.2 H.sub.5, CH(CH.sub.3).sub.2 ;R.sub.3 = ##STR2## Where R.sub.4 =H, CH.sub.3, C.sub.2 H.sub.5 R.sub.5 =H, CH.sub.3X=none O, S, NH, NCH.sub.3, --CH=CH--, --C.ident.C--Y=O, NH,both in the racemic Form and in the isomeric enantiomeric forms,which produce a nootropic effect, i.e. memory enhancement and learning facilitation, as well as an analgesic effect.

Abstract: The present invention relates to a novel class of benzoylecgonine, ecgonine and ecgonidine derivatives which are useful for preventing and treating immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. The compounds of this invention are conveniently obtained by chemical synthesis. Accordingly, this invention also relates to methods for preparing the benzoylecgonine, ecgonine and ecgonidine derivatives and to pharmaceutical compositions containing these derivatives.

Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.