Abstract: A new process for the preparation of fexofenadine and of related intermediates, which can be used in the preparation of fexofenadine, is provided.

Abstract: The present invention relates to a novel polymorphic form of Fexofenadine hydrochloride, to a process for preparing it, to pharmaceutical compositions containing it, as well as its use. The invention also relates to intermediates useful for the preparation of Fexofenadine hydrochloride, antihistamine drug used in the treatment of allergy symptoms.

Abstract: [Problem] The object of the present invention is to provide a novel compound having ?2 adrenergic receptor agonist activity and muscarinic receptor antagonist activity. [Means for Solving the Problem] The present invention is a quaternary ammonium salt compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, with superior ?2 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.

Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

Abstract: Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

Abstract: The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.

Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

Abstract: Intermediates useful for the synthesis of fexofenadine, processes for their preparation and processes for the synthesis of fexofenadine are described.

Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.

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 present invention relates to a novel polymorphic form of Fexofenadine hydrochloride, to a process for preparing it, to pharmaceutical compositions containing it, as well as its use. The invention also relates to intermediates useful for the preparation of Fexofenadine hydrochloride, antihistamine drug used in the treatment of allergy symptoms.

Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.

Abstract: Selective bromination of 2-methyl-2-phenylpropanoic acid in aqueous medium is described to obtain pure 2-(4-bromophenyl)-2-methylpropanoic acid, which is a useful key intermediate in the process of manufacturing pure fexofenadine.

Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.

Abstract: A process for the preparation of 4-[1-oxo-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-?,?-dimethylbenzeneacetic acid, useful as an intermediate for the preparation of fexofenadine, is provided.

Abstract: The invention relates to the use of and mainly novel compounds of the formula I wherein the moieties are as defined in the description, which are useful as farnesyl pyrophosphate synthase modulators and e.g. in the treatment of proliferative diseases.

Abstract: The present invention discloses a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-?,?-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl)toluene with 4-chlorobutyryl chloride to provide 4-(4-chloro-1-oxobutyl)-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl)toluene; (2) hydrolyzing said 4-(4-chloro-1-oxobutyl)-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl)toluene to provide 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1 -oxobutyl)-?,?-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1 -oxobutyl)-?,?-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetate with 4-(?,?-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-?,?-dimethylphenylacetate; (5) reducing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-p

Abstract: A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-?,?-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-?,?-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralisation of the solution.

Abstract: Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.

Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.

Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The present invention relates to a use of a specific alpha-arylmethoxyacrylate derivative, or its pharmacologically acceptable salt or solvate for preventing and treating metabolic bone diseases.

Abstract: Process for the preparation of 4-[1-oxo-4-[4-(hydroxyphenylmethyl)-1-piperidinyl]butyl]-?,?-dimethylbenzenacetic acid, which is an intermediate useful in the preparation of fexofenadine, by hydrating asymmetric alkynes.

Abstract: The invention relates to novel crystalline forms of fexofenadine base, a process for the preparation thereof and the use thereof in therapy.

Abstract: The invention relates to non-hydrated fexofenadine hydrochloride which can be obtained from a fexofenadine base and hydrogen chloride, according to the reaction conditions, either in the form of a novel polymorph (“form A”), in an amorphous form, or in the form of a mixture of different polymorphs. Said novel polymorph (“form A”) can be used as a therapeutic active ingredient and can be processed to form a pharmaceutical containing the same and a pharmaceutically acceptable carrier. Said pharmaceutical is suitable for use as an antihistaminic agent, an antiallergic agent and/or a bronchodilating agent.

Abstract: The present invention is related to a novel polymorph of Fexofenadine and processes of preparation thereof.

Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: The present invention is directed to a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-?,?-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl) toluene with N,N-dimethyl cyclopropylcarboxylic acid amide to provide 4-(cyclopropyl-oxo-methyl)-?,?-dimethyl-?-(4,4-dimethyloxozolin-2-yl) toluene; (2) hydrolyzing said 4-(cyclopropyl-oxo-methyl)-?,?-dimethyl-?-(4,4-dimethyloxozolin-2-yl) toluene to provide 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetate with 4-(?,?-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-?,?-dimethylphenylacetate; (5) reducing said methyl 4-[4-[

Abstract: The present invention is related to novel polymorph of Fexofenadine and Fexofenadine hydrochloride of formula 1 and process of preparation thereof. The present invention is also directed to provide pure novel polymorphs of Fexofenadine and its hydrochloride by a simple process which is cost effective, commercially viable and environment friendly.

Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, and alkoxy. This process involves incubating a starting compound having a structure according to Formulae IIA and/or IIB: wherein R3 is —CH3 and R1, R2, A, B, and D are defined above in the presence of a microorganism under conditions effective to produce the product compound.

Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.

Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety,

Abstract: Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.

Abstract: Provided is a crystalline (polymorphic) form of fexofenadine hydrochloride, denominated fexofenadine hydrochloride Form XVI.

Abstract: A process for preparing fexofenadine is described that includes the purification of 4-[4-chloro-1-oxobutyl]-2,2-dimethylphenyl acetic acid alkyl ester by means of suspension in a hydrocarbon, preferably n-heptane. The compound thus obtained is dissolved in a suitable solvent and condensed with azacyclanol to give the compound shown below where R is an alkyl radical, which is then hydrolysed and reduced to give fexofenadine.

Abstract: Compounds of formula (I). Selectively inhibit production of A?(1-42) and hence find use in treatment of diseases associated with deposition of ?-amyloid in the brain.

Abstract: The present invention discloses a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-?,?-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl)toluene with 4-chlorobutyryl chloride to provide 4-(4-chloro-1-oxobutyl)-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl)toluene; (2) hydrolyzing said 4-(4-chloro-1-oxobutyl)-?,?-dimethyl-?-(4,4-dimethylisoxazolin-2-yl)toluene to provide 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-?,?-dimethylphenylacetate with 4-(?,?-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-?,?-dimethylphenylacetate; (5) reducing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-pip

Abstract: The present invention relates the use of compounds having the general Formula I, wherein the definitions or R1 and R2 are provided in the specification. Said compounds of Formula I are useful for the synthesis of a variety of ?-secretase modulators, which are in turn useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: The present invention relates to stable amorphous form of fexofenadine hydrochloride, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of allergic reactions.

Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group repr

Abstract: Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.

Abstract: The present invention provides novel crystal forms of fexofenadine hydrochloride Forms V, VI and VIII through XV and processes for their preparation and preparation of amorphous form and other crystalline forms of fexofenadine hydrochloride. Forms XIV and XV are solvates of ethyl acetate, while Form IX is anhydrous, but can be crystallized as a solvate of MTBE or cyclohexane. The forms are useful for administration to humans and animals to alleviate symptoms caused by histamine. The present invention further provides pharmaceutical compositions of the new crystalline forms.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.

Abstract: The invention provides novel crystalline forms of fexofenadine hydrochloride, a process for the preparation of the novel forms and of the known form A, and their use in therapy.

Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of Het, R0, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: Provided are crystalline forms of fexofenadine hydrochloride and processes for their preparation.

Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.