Abstract: The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.

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: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.

Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an H1 receptor antagonist, whereby endogenous BMP-2 up-regulation is stimulated in said subject. Also provided is a pharmaceutical formulation including an H1 receptor antagonist present in an effective amount to stimulate BMP-2 up-regulation in a subject and a kit.

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: 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: 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: 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: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.

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 various processes for the preparation of (R)-?-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.

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: 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: Compounds or their salts having general formula: A-B—C—NO2 wherein: A is a drug radical; B is a linker; and C is a bivalent radical.

Abstract: The present invention relates to a process for the production of piperidine derivatives with microorganisms. This is carried out by incubating starting compounds in the presence of a microorganism under conditions effective to produce piperidine derivative products. Suitable microorganisms can be from any one of the genus of Stemphylium, Gliocladium, Bacillus, Botrytis, Cyathus, Rhizopus, Pycniodosphora, Pseudomonas, Helicostylum, Mucor, Gelasinospora, Rhodotorula, Candida, Mycobacterium, and Penicillium. In another aspect of the invention, starting compounds are incubated in the presence of Cunninghamella bainieria under conditions effective to produce piperidine derivative products.

Abstract: Nitric acid salts with medicines active in the respiratory system pathology treatment.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: The present invention is directed to the method of isolation of sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.

Abstract: Nitric acid salts with medicines active in the respiratory system pathology treatment.

Abstract: The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them.

Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.

Abstract: The present invention provides various processes for the preparation of (R)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.

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: This invention relates to novel piperidine derivatives of formula (I) and a process for the preparation thereof. wherein R1 is H or C1-C6alkyl wherein the C1-C6alkyl moiety is straight or branched; R2 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; or stereoisomers or pharmaceutically acceptable acid addition salt thereof.

Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1

Abstract: A process comprising allowing a peroxide compound represented by following Formula (2): 1

Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: 1

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 invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.

Abstract: The present invention relates to processes for preparing certain piperidine derivatives, including fexofenadine (F), the active ingredient in the non-sedating antihistamine sold in the U.S. under the designation “Allegra®”. This invention also relates to novel synthetic intermediates useful in the processes of the present invention.

Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.

Abstract: This invention relates to novel substituted piperidine derivatives. More particularly, this invention relates to substituted phenyl 4-substituted-piperidinoalkanol derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.

Abstract: The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydroxy-methyl)-2-methoxy-phenyl]ester a metabolite of the 5HT2A antagonist (+)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol and a processes for its preparation and its use in the treatment for a number of disease states.

Abstract: This invention relates to novel piperidine derivatives of formula (I) and a process for the preparation thereof. wherein R1 is H or C1-C6alkyl wherein the C1-C6alkyl moiety is straight or branched; R2 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; or stereoisomers or pharmaceutically acceptable acid addition salt thereof.

Abstract: Disclosed is the use of a compound with Formula (I) wherein n is 2, 3, or 4, and R1, R2, R3, and R4 are each independently hydrogen, C1-6 alkyl, halogen, trifluoromethyl, hydroxy, C1-6 alkoxy or amino, or an optical isomer or a pharmaceutically acceptable salt thereof for the production of a pharmaceutical composition for treatment of a neurodevelopmental disorder. Also a method for treatment of neurodevelopmental disorders wherein a therapeutically effective amount of said compound is administered to a patient is disclosed.

Abstract: This invention relates to novel substituted piperidine derivatives. More particularly, this invention relates to substituted phenyl 4-substituted-piperidinoalkanol derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R)-trihexyphenidyl. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R)-trihexyphenidyl, or a pharmaceutically acceptable salt thereof, substantially free of the (S)-trihexyphenidyl enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (R)-trihexyphenidyl, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.

Abstract: Arylmetal compounds are prepared by deprotonation of aromatics which have a hydrogen atom in the ortho position relative to a halogen atom or a trifluoromethoxy group, using a suitable base or by halogen-metal exchange of haloaromatics using a suitable metalating reagent. The arylmetal compounds are prepared in a continuous-flow reactor. The arylmetal compound can be further reacted with an electrophilic reagent.

Abstract: 4-(3-Heterocyclyl-1-benzoyl)pyrazoles of the formula I ##STR1## where: R.sup.1 and R.sup.3 are each hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl, N-alkylaminosulfonyl, N,N-dialkyl)aminosulfonyl, N-alkylsulfonylamino, N-haloalkylsulfonylamino, N-alkyl-N-alkylsulfonylamino or N-alkyl-N-haloalkylsulfonylamino;R.sup.2 is a 5- or 6-membered heterocyclyl radical with or without substitution which comprises 1 to 4 identical or different hetero atoms from the following group: oxygen, sulfur or nitrogen;R.sup.4 is hydrogen, halogen or alkyl;R.sup.5 is substituted pyrazole which is attached in position 4;and agriculturally useful salts thereof; processes for preparing the 4-(3-heterocyclyl-1-benzoyl)pyrazoles; compositions comprising them; and the use of these derivatives or these compositions comprising them for controlling undesirable plants.

Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.

Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, and its use in the treatment of a number of disease states.

Abstract: The invention relates to the preparation of the compound 4-(4-(4-(hydroxydiphenyl)-1-piperidinyl)-1-hydroxybutyl)-.alpha.,.alpha.-d imethylphenylacetic acid and its phosphorylated derivatives. These compounds can be prepared from .alpha.-(p-tert-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-pi peridinylbutanol with the aid of fungi of the genus Cunninghamella or Absidia. The compounds according to the present invention can be used as pharmaceuticals for the treatment of allergic disorders, allergic rhinitis or asthma. Compounds of the formula II in which R.sup.1 is --CH.sub.2 --O--P(O)(OH).sub.2 and R.sup.2 is --OH; R.sup.1 is --CH.sub.3 and R.sup.2 is --O--P(O)(OH).sub.2 ; orR.sup.1 is --COOH and R.sup.2 is --O--P(O)(OH).sub.2 are produced by the process according to the present invention and are suitable as pharmaceuticals with antihistamine action.

Abstract: The invention concerns a compound of formula (I): ##STR1## wherein R.sup.1 -R.sup.6, A, B, and D have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, and methods of treating a bacterial infection by administering such a compound or salt.

Abstract: A process for the preparation of tertiary diphenyl carbinols containing a primary or secondary amine substituent on the aliphatic moiety attached to the carbinol function which consists in contacting a Grignard phenyl reagent with an aminoacid wherein the mobile protons are not masked in an aprotic inert organic solvent or a mixture thereof at a temperature between 20.degree. C. and the boiling temperature by the reaction mixture.The reaction products are useful as active ingredients of medicaments and intermediates for the manufacture thereof.

Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.

Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.

Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.

Abstract: Novel tricyclic triazolo derivatives and pharmaceutically acceptable salts thereof, which are useful as anti-inflammation agents, anti-allergy agents or anti-PAF agents as well as processes for producing the same are disclosed. The triazolo derivatives of the present invention are represented by the formula (I): ##STR1## ?wherein R.sup.1 represents hydrogen, lower alkyl or C.sub.3 -C.sub.5 cycloalkyl; R.sup.2 and R.sup.3 respectively represent hydrogen, lower alkyl, lower alkoxy or halogen; W represents C.dbd.O or CR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 respectively represents hydrogen or lower alkyl); A represents C.sub.1 -C.sub.5 straight or branched saturated or unsaturated alkylene which may contain one or more hetero atoms; l represents 0 to 2, n represents 1 to 3, . . . represents single bond or double bond; Y represents N or C; Z represents C(B)Ar.sup.1 Ar.sup.2 (wherein B represents hydrogen, hydroxy or methoxy, Ar.sup.1 and Ar.sup.

Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.

Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.