Abstract: The present invention relates to 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives of formula (I), wherein R1 is as defined in the description, their preparation and their use as pharmaceutically active compounds.

Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.

Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.

Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.

Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: The present invention provides new amino lipids and a convenient method for synthesising these compounds. These (cationic) amino lipids have good properties as transfection agents. The method is an economic versatile two step synthesis allowing the preparation of various amino lipids thus leading to the assembly of a combinatorial library of transfection agents. Moreover, the present invention provides lipid particles (liposomes) containing said amino lipids and their use for delivering bioactive agents into cells. The invention encompasses also the use of lipid particles containing the cationic amino lipids as medicament.

Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

Abstract: An object of the present invention is to provide a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof and to provide a pharmaceutical agent which contains said compound as an active ingredient and has a highly safe neurotrophic factor-like activity or an alleviating action for side effect induced by administration of anti-cancer agents. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof which is the compound of the present invention is specifically represented by the formula (1): (In the formula, Y is —O—, —NR— or —S—, R is hydrogen atom, alkyl group, dialkylaminoalkyl group or the like and W is a substituent such as dialkylaminoalkyl group) and has a quite high usefulness as a pharmaceutical agent such as a preventive or therapeutic agent for dementia, Alzheimer's disease, Parkinson's disease, depression, etc., a treating or repairing agent for spinal cord injury.

Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.

Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.

Abstract: The present invention includes a method of preparing a composition comprising (+)-doxapram or a salt thereof, wherein the composition is essentially free of (?)-doxapram or a salt thereof.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.

Abstract: The invention relates to a continuous method for producing amides of aliphatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—COOR4 (I), wherein R3 represents hydrogen or an optionally substituted aliphatic hydrocarbon group with 1 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, or wherein R3 and R4 form an optionally substituted ring with 5, 6 or 7 ring members, with at least one amine of formula (II) HNR1R2 (II), wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.

Abstract: Disclosed are near IR emitting fluorescent compounds; methods of making and kits containing the described compounds; and their use in fluorescence-based detection of biological materials.

Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.

Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.

Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.

Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Abstract: This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.

Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.

Abstract: The present invention is directed to the compounds of formula wherein R1 to R4 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.

Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.

Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.

Abstract: The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.

Abstract: The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, n, p, and q are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11?-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

Abstract: The present invention provides an organocatalyst of formula (I), wherein R1 is —H, —OH, —O—Si(R4)(R5)(R6) or C1-6alkoxy, in which R4, R5 and R6 are identical or different and independently selected from the group consisting of C1-6alkyl, phenyl and phenyl substituted with C1-6alkyl; R2 is —OH or ?O; X1 is one selected from the group consisting of —NH—, —S— and X2 is one selected from the group consisting of —C(?O)—, —CH2— and and X1 is different from X2. The high yield and enantioselectivity of an addition reaction are obtained by using the organocatalyst of the present invention.

Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: The invention relates to hydroxamic acid derivatives having carbamate linkage with the structural formula that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous systems (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.

Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.

Abstract: The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.

Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: A process for the formation of 2-(methyloxy)-N-[2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]-4,6-bis(trifluoromethyl)benzamide is disclosed, comprising treatment of 2,4-ditrifluoromethyl-6-methoxy-benzoic acid with an arylsulphonyl halide, C1-6alkylsulphonyl halide or di-C1-6alkylphosphoryl chloride, in the presence of a base and an aprotic solvent; followed by reaction with [2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]amine or a salt thereof. Also disclosed is a process for the formation of [2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]amine comprising: i) treatment of an ?-haloketone with an alcohol in the presence of a base followed by reaction with pyrrolidine; ii) treatment of the product of stage i) with Ar—CH(R5)N H2 wherein R5 is C1-4alkyl and Ar is optionally substituted phenyl, followed by reduction with a sodium borohydride derivative; and iii) reduction of the product of stage ii) with hydrogen and a palladium catalyst.

Abstract: Ethoid-containing compounds comprising one or more ethoid moieties (e.g., a methyleneoxy, ?[CH2O]) as a substitutive, isosteric replacement for an amide moiety of a polyaminoacid are disclosed. Universal, modular approaches for preparing such ethoid-containing compounds are also disclosed. Such ethoid-containing compounds can be polyaminoacid analogs, and are useful as food additives, as cosmetics ingredients, as research reagents, as diagnostic agents, and as therapeutic agents.

Abstract: The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.

Abstract: Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.

Abstract: The present invention relates to new substituted benzamide modulators of dopamine receptor, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.

Abstract: The present invention is directed to the compounds of formula wherein R1 to R4 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.