Abstract: The present invention relates to certain amide derivatives that have the ability to inhibit 11-?-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

Abstract: The present invention relates to bicyclic aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.

Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.

Abstract: Chemoselective isolation of aliphatic hydroxyl group-containing and aromatic hydroxyl group-containing compounds is accomplished via formation of polymeric siloxyl ethers. Chemoselective release of aliphatic hydroxyl group-containing and aromatic hydroxyl group-containing compounds from polymeric siloxyl reagents is described.

Abstract: The present invention is a method for alleviating at least one climacteric symptom in a climacteric subject using an anticholinergic agent. To illustrate the instant invention, homatropine was shown to relieve hot flushes in peri-menopausal and post-menopausal women.

Abstract: Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.

Abstract: To provide a novel method for producing a 2-azaadamantane compound from a bicyclocarbamate compound. In accordance with the following scheme: a bicyclocarbamate compound represented by the formula (1) is reacted with a halogenating agent to produce a 2-azaadamantane carbamate compound represented by the formula (2), and the 2-azaadamantane carbamate compound is subjected to hydrogenolysis to produce a 2-azaadamantane compound represented by the formula (3) (in the formulae, R1 is hydrogen or the like, each of R2 and R3 which are independent of each other, is a hydrogen atom or a C1-6 alkyl group, Ar is an aryl group which may be substituted by Ra, Ra is halogen or the like, X is a halogen atom, and Y is X or a hydrogen atom).

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: This invention relates to novel 8-aza-bicyclo[3.2.1]octane 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: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.

Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

Abstract: Described are various compounds and methods for the treatment of disorders arising from aberrant protein folding, including in particular lysosomal storage diseases. In particular, polyhydroxylated alkaloids and imino sugars which are pharmacoperones of an enzyme and which do not bind to a catalytic site of said enzyme are described.

Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane 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: 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: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

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 present application is directed to a method of synthesis of a bicyclic or polycyclic compound of formula I or formula II: in which E, G, Y, n, m, R, R1, R2, R3, R6, R7, R8 and R9 are as defined.

Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

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 invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

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: Compounds and methods of modulating the activity of P-glycoproteins are disclosed. The method utilizes compounds derived from Erythroxylum pervillei. The compounds overcome multidrug resistance and can be used therapeutically to enhance performance of therapeutic drugs, like chemotherapeutic drugs and antibiotics.

Abstract: A process for preparing tropenol (I) 1

Abstract: The present invention relates compounds of the formula (I): 1

Abstract: A method of improving specific immune responses to small immunogens, haptens, has been developed by changing the linkage between the hapten and carrier being used for immunization. High affinity antibodies to the hapten cotinine have been produced using this method. Antibodies to a glycated protein have also been developed, utilizing an immunogen which is composed of a glycated peptide mimic of the glycated peptide sequence which is the target epitope, wherein the peptide mimic is constructed to conformationally mimic the conformation of the peptide in the native protein, the peptide mimic contains no charged groups or other immunodominant group, and the peptide mimic is connected to a spacer sequence equivalent to a peptide spacer of between one and thirty amino acids in length, which serves to position the peptide epitope in a conformation that approximates its conformation in the native protein. In a further embodiment the peptide mimic and spacer are linked to a carrier molecule.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

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: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.

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: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

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 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 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: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.1]-oct-8-yl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

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: Compounds are provided for the preparation of reagents, including labels which can be used in immunoassays of cocaine and cocaine metabolites. The compounds are derivatives of cocaine which are conjugated to antigenic proteins or polypeptides for the formation of antibodies for use in immunoassays. The compounds also may be conjugated to labels for use in immunoassays.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH=CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: 3-Bromo-2,6-dimethoxybenzamides useful as neuroleptic agents are described.

Abstract: 3.alpha.-Benzylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with enzylamine in the presence of phenol.