ПРОИЗВОДНЫЕ АЗАБИЦИКЛООКТАНА, ФАРМАЦЕВТИЧЕСКИЕ ПРЕПАРАТЫ, СПОСОБ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ, СПОСОБЫ ПОЛУЧЕНИЯ СОЕДИНЕНИЙ, СОЕДИНЕНИЯ

Описываются соединения формулы (I), где R1, R2, R3 и Ra-Rh имеют значения, приведенные в описании, которые полезны в профилактике и лечении аритмий, в частности предсердных и желудочковых аритмий, а также способы получения соединений формулы (I) и промежуточные соединения. 14 н. и 27 з.п. ф-лы, 1 табл.

Новые производные азабициклооктана, полезные в лечении сердечных аритмий

Способ получения производных бензиламина или их солей

Способ получения производных бензиламина или их солей

Способ получения производных бензиламина или их солей

Способ получения производных бензиламина или их солей

Способ получения производных бензиламина или их солей

AZEPIN-DERIVATE, DEREN HERSTELLUNG UND VERWENDUNG ALS SIGMA-REZEPTOR- LIGANDEN

PIPERIDIN- ODER 8-AZABICYCLOÄ3.2.1ÜOCT-3-YLDERIVATE, DIE SICH ALS MODULATOREN DER CHEMOKINREZEPTORAKTIVITÄT EIGNEN

PSYCHOTROPIC POLYCYCLIC IMIDES

Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: <CHEM> in which X is -O-, -S-, -SO-, -SO2-, -CR3R4- where R3 and R4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R3 and R4 form a cycloalkyl group of 3 to 5 carbon atoms; n is one of the integers 2, 3, 4 or 5; R is phenyl, alkylphenyl in which the alkyl group contains 1 to 4 carbon atoms, halophenyl, trifluoromethylphenyl, alkoxyphenyl, in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R1 and R2, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R1 and R2 complete a benzene ring, or a group of the formula: <CHEM> where Y is -CH2, -CH2-CH2-, -O- or -S- and the dotted line represents optional unsaturation; or a pharmaceutically acceptable salt thereof. In addition, the intermediate b3-dicarboxylic and the corresponding anhydrides - 2,3,3a,4,5,6,6a,7,7a-decahydro-4,6,7-metheno-1H-cyclopena[a]pentalene-1,3 -dicarboxylic acid and octahydro-1, 5-methano-6,8,9-metheno-pentaleno[1,2,-d]oxepin-2,4(1H, 5H)-dione represent especially significant aspects of the invention.

BENZOIC ACID DERIVATIVES

New camphidine derivatives and processes for their preparation

The invention comprises compounds of the general formula in which R represents an alkyl or dialkylamino-alkyl group where each alkyl group preferably has 1-4 carbon atoms; and acid addition salts and mono- and bis-quaternary ammonium salts thereof; and the preparation thereof by reducing corresponding N-substituted 5-chlorocamphoric acid imides, e.g. with a hydride, particularly lithium aluminium hydride; and, if desired, treating the products with alkylating agents of the general formula Alk-X, in which Alk represents one or two alkyl groups each preferably having not more than 4 carbon atoms and X represents an anion. N - substituted 5 - chloro - camphoric acid imides are prepared by treating 5-chlorocamphoric acid imide with an alkyl halide or a dialkylamino-alkyl halide hydrohalide in alcoholic alkali metal p hydroxide solution.

Formamide derivatives useful as adrenoceptor

Aryl fused azaplycyclic compounds

Aryl fused azapolycyclic compounds.

Compounds of formula and their pharmaceutically acceptable salts, wherein r1, r2, r3 and n are defined as in the specification, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders are claimed.

Aryl fused azapolycyclic compounds.

Aryl fused azapolycyclic compounds

Aryl fused azaplycyclic compounds

Formamide derivatives useful as adrenoceptor.

Formamide derivatives useful as adrenoceptor

Aryl fused azapolycyclic compounds.

A method for manufacturing news dihalogéno-amino-benzylamines.

Aryl fused azapolycyclic compounds.

Aryl fused azapolycyclic compounds

Formamide derivatives useful as adrenoceptor

Aryl fused azapolycyclic compounds

ARYL-CONDENSED AZAPOLYCYCLI DERIVATIVES

5 (2-OXYPHENYL) - PYRROL DERIVATIVES AS DOPAMIN-D3 RECEPTOR ANTAGONIST

BENZODIAZEPINDERIVATE

Procedures for the production of new Amino monohalogenphenyläthanolaminen and from their salts

Procedures for the production of new Amino monohalogenphenyläthanolaminen and from their salts

Amidino derivatives useful as nitric oxide synthase inhibitors

Benzodiazepine derivatives

New azabicyclooctane derivatives useful in the treatment of cardiac arrhythmias

5-(2-oxyphenyl)-pyrrole derivatives as dopamine d3 receptor antagonists

BENZYLAMINES

AMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS

The current invention discloses useful pharmaceutical compositions containing amidino derivatives of formula (I) as nitric oxide synthase inhibitors.

Verfahren zur Darstellung eines neuen basischen Derivates der Kampferreihe.

Verfahren zur Herstellung von neuen Dihalogen-amino-benzylaminen

Verfahren zur Herstellung von neuen Dihalogen-amino-benzylaminen

Verfahren zur Herstellung von Kampferimidderivaten

Verfahren zur Herstellung von neuen Amino-monohalogenphenyläthanolaminen

Amino-monohalophenylethanolamines cns active analgesic

... (A) Cpds. of general formula (I) - Hal=Cl, Br, or I. - R1 and R2=H or (1-3C) alkyl - R3 and R4=H, lower alkyl opt. subst. by OH, Oalkyl or N(alkyl)2, alkenyl, cycloalkyl, Ph, PhCH2, or NR3R4 forms a - or camphidine residue, all opt. subst. by lower alkyl - (B) Salts of (I). - CNS active analgesics. - LD50 (p.o., mouse)= 650 mg/kg for N-ethyl-beta-(4-amino-3-bromophenyl )-beta-hydroxyethylamine.

Verfahren zur Herstellung von neuen Amino-monohalogen-phenyläthanolaminen

Verfahren zur Herstellung von neuen Amino-monohalogen-phenyläthanolaminen

Verfahren zur Herstellung von neuen Dihalogen-amino-benzylaminen

Verfahren zur Herstellung von neuen Amino-monohalogen-phenyläthanolaminen

VERFAHREN ZUR HERSTELLUNG NEUER BASISCH SUBSTITUIERTER TERTIAERER BUTANOLE.

VERFAHREN ZUR HERSTELLUNG NEUER BASISCH SUBSTITUIERTER TERTIAERER BUTANOLE.

VERFAHREN ZUR HERSTELLUNG NEUER BASISCH SUBSTITUIERTER TERTIAERER BUTANOLE.

Verfahren zur Herstellung von Kampferimidderivaten

Verfahren zur Herstellung von neuen Dihalogen-amino-benzylaminen

Verfahren zur Herstellung von neuen Amino-monohalogenphenyläthanolaminen

Process for the preparation of novel benzylamines

Novel benzylamines of the formula I in which the symbols R1 to R5 have the meaning given in Patent Claim 1 and their physiologically tolerable acid addition salts with inorganic or organic acids are prepared. The compounds of the formula I have useful pharmacological properties, in particular an anti-ulcer action, a secretolytic, cough-relieving and augmentative effect on the production of the surfactant or anti-atelectasis factor of the alveoli. The compounds of the formula I are prepared by introduction of the group into appropriate reactive benzyl compounds.

Process for the preparation of novel benzylamines

Preparation of novel benzylamines of the formula I in which the symbols R1 to R5 have the meaning given in Patent Claim 1, and of their physiologically tolerable acid addition salts with inorganic or organic acids. The compounds of the formula I have useful pharmacological properties, in particular an anti-ulcer action, a secretolytic, cough-relieving and an augmenting action on the production of the surfactant or anti-atelectasis factor of the alveoli. The compounds of the formula I are prepared by reaction of an appropriately substituted benzyl alcohol with an amide of the formula R8C(O)NR4R5, in which R8 denotes an alkyl, aryl or aralkyl radical.

Process for the preparation of novel benzylamines

Process for the preparation of novel benzylamines

The preparation of novel benzylamines of the formula I in which the symbols R1 to R5 have the meanings stated in Claim 1, as well as their physiologically tolerated acid addition salts with inorganic or organic acids is described. The compounds of the formula I have valuable pharmacological properties, especially an antiulcer effect, a secretolytic, cough-suppressant effect and an effect enhancing the production of the surfactant or antiatelectasis factor in the alveoli. The compounds of the formula I are prepared by reacting an appropriately substituted benzaldehyde with a nitrogen compound which introduces the group -NR4R5, in the presence of formic acid.

Process for the preparation of novel benzylamines

The preparation of novel benzylamines of the formula I in which the symbols R1 to R5 have the meanings stated in Claim 1, as well as their physiologically tolerated acid addition salts with inorganic or organic acids is described. The compounds of the formula I have valuable pharmacological properties, especially an antiulcer effect, a secretolytic, cough-suppressant effect and an effect enhancing the production of the surfactant or antiatelectasis factor in the alveoli. The compounds of the formula I are prepared by reacting an appropriately substituted benzyl alcohol with an amide of the formula O=P(NR4R5)3.

Process for the preparation of novel benzylamines

Process for the preparation of novel benzylamines

The preparation of novel benzylamines of the formula I in which the symbols R1 to R5 have the meanings stated in Claim 1, as well as their physiologically tolerated acid addition salts with inorganic or organic acids is described. The compounds of the formula I have valuable pharmacological properties, especially an antiulcer effect, a secretolytic, cough-suppressant effect and an effect enhancing the production of the surfactant or antiatelectasis factor in the alveoli. The compounds of the formula I are prepared by introducing the radical R5 into an appropriate compound in which R5 is hydrogen.

Process for the preparation of novel benzylamines

Preparation of novel benzylamines of the formula I <IMAGE> in which the symbols R1 to R5 have the meaning given in Patent Claim 1, and of their hydrolysis products in which R1 denotes hydrogen, and their physiologically tolerable acid addition salts with inorganic or organic acids. The compounds of the formula I have useful pharmacological properties, in particular an anti-ulcer action, a secretolytic, cough-relieving and heightening action on the production of the surfactant or anti-atelectasis factor of the alveoli. The compounds of the formula I are prepared by reaction of a compound of the formula II <IMAGE> in which R9 denotes a hydrogen atom or an aliphatic or aromatic group corresponding to R1 with a nitrogen compound of the formula HNR4R5 and, if appropriate, subsequent hydrolysis of the reaction product.

AROMATIC CARBONIC ACID AND SULFONSAEUREESTER OR - AMIDES.

ARILKONDENSIROVANNYEAZAPOLITsIKLIChESKIE COMPOUNDS

ПОХІДНІ АЗАБІЦИКЛООКТАНУ КОРИСНІ ПРИ ЛІКУВАННІ СЕРЦЕВИХ АРИТМІЙ, СПОСІБ ЇХ ОДЕРЖАННЯ (ВАРІАНТИ), ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ПРОМІЖНА СПОЛУКА

Згідно з винаходом запропоновано сполуки формули (І), де R1, R2, R3 та Ra-Rh визначено в описі, які корисні при профілактиці чи лікуванні серцевих аритмій, зокрема атріальних та вентрикулярних аритмій, способи одержання сполуки формули (І) та інтермедіатів.

КАРБОКСАМІДНІ СПОЛУКИ, ЯКІ МАЮТЬ АНТАГОНІСТИЧНУ У ВІДНОШЕННІ МСН ДІЮ, ЛІКАРСЬКІ ЗАСОБИ, ЯКІ МІСТЯТЬ ЦІ СПОЛУКИ, І СПОСІБ ЇХ ОДЕРЖАННЯ

У заявці описані карбоксамідні сполуки загальної формули (І) (І), у якій групи і залишки А, В, W, X, Y, Z, R1, R2, R3 і k мають вказані в п. 1 формули винаходу значення. У заявці описаний далі спосіб одержання таких карбоксамідних сполук, а також лікарські засоби, які містять принаймні одну запропоновану у винаході карбоксамідну сполуку. Запропоновані у винаході лікарські засоби завдяки наявності в них антагоністичної у відношенні МСН-рецептора активності придатні для лікування пов'язаних з порушенням обміну речовин розладів і/або розладів прийому їжі, насамперед ожиріння, булімії, анорексії, гіперфагії і діабету.

AZAPOLYCYCLIC COMPOUNDS CONDENSATED WITH ARYL

AZAPOLYCYCLIC COMPOUNDS CONDENSED WITH ARYL

USE OF FORMAMIDE DERIVATIVES AS ADRENOCEPTOR

Aryl Fused Azapolycyclic Compounds, Composition Containing the Same and Use Thereof

ALPHA-AMINOALKYLBENZYL ALCOHOLS

A method for manufacturing news dihalogéno-amino-benzylamines

Bis-(4-azatricyclo undecyl)alkoxy fluorenones - interferon promoters, from bis-acyloxyfluorenones and azatricycloalkylhalides

ARYL FUSED AZAPOLYCYCLIC COMPOUNDS

PHENYLTRIAZOLE COMPOUNDS FOR THE TREATMENT OF PAIN

Provided herein are compounds that are useful in the treatment of pain in a subject. Also provided herein is a pharmaceutical composition comprising compounds or pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier and methods of treating pain in a subject in need thereof.

SULPHONAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CNS DISORDERS

Sulphonamide compounds of formula (I) or a salt thereof, wherein: Ar is an optionally substituted mono- or bicyclic aromatic or heteroaromatic ring; R1 and R2 are independently hydrogen, C1-6 alkyl, arylC1-6 alkyl or together with the nitrogen atom to which they are attached form an optionally substituted 5- to 7-membered heterocyclic ring optionally containing a further heteroatom selected from nitrogen, sulphur or oxygen, the nitrogen atom being substituted by hydrogen, C1-6 alkyl, cycloC3-7alkyl, or an optionally substituted aryl, heteroaryl or arylC1-6 alkyl group; R3 is hydrogen or C1-6 alkyl; X is oxygen, sulphur or a bond; n is 2 or 3; and m is 1 or 2, having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of CNS disorders.

Способ получения производных бензиламина или их солей

Benzamidderivate

BENZODIAZEPINDERIVATE

ARYLKONDENSIERTE AZAPOLYCYCLISCHE DERIVATE

Verfahren zur Herstellung organischer Basen

ARYLPIPERIDIN DERIVATIVES

VERFAHREN ZUR HERSTELLUNG VON NEUEN AMINOBENZYLAMINEN SOWIE DEREN SAUREADDITIONSSALZEN

PIPERIDIN OR 8-AZABICYCLO (3.2.1) OCT-3 YLDERIVATE, AS MODULATORS CHEMOKINREZEPTORAKTIVITÄT THEMSELVES BEING SUITABLE

PROCEDURE FOR THE PRODUCTION OF NEW AMINOBENZYLAMINEN AS WELL AS THEIR SOUR ADDITION SALTS

GROWTH PROMOTING AMINOPHENYLETHYLAMINE DERIVATIVES

Aryl fused azapolycyclic compounds

ARYL FUSED AZAPOLYCYCLIC COMPOUNDS

This invention is directed to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

NEW AZABICYCLOOCTANE DERIVATIVES USEFUL IN THE TREATMENT OF CARDIAC ARRHYTHMIAS

There is provided compounds of formula (I), wherein R1, R2, R3 and Ra to Rh have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias, a process for the preparation of compounds of formula (I), and intermediate compounds.

NEW CARBOXAMIDE COMPOUNDS HAVING MCH-ANTAGONISTIC ACTIVITY, PHARMACEUTICAL PREPARATIONS COMPRISING THESE COMPOUNDS AND PROCESS FOR THEIR MANUFACTURE

The invention relates to carboxamide compounds of general formula (I), in which the groups and radicals A, B, W, X, Y, Z, R1, R2, R3, and k have the meanings indicated in claim 1. The invention also relates to methods for producing said carboxamide compounds and medicaments containing at least one inventive carboxamide. The inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, especially obesity, bulimia, anorexia, hyperphagia, and diabetes due to the MCH receptor-antagonistic activity thereof.

AZABICYCLOOCTANE DERIVATIVES USEFUL IN THE TREATMENT OF CARDIAC ARRHYTHMIAS, A METHOD FOR OBTAINING THEREOF (VARIANTS), PHARMACEUTICAL COMPOSITION BASED THEREON AND INTERMEDIARY COMPOUND

DERIVATIVES OF FORMAMIDE, SUITABLE AS THE ADRENORECEPTOR

Manufacture of 4-((1r,3s)-6-chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine and 1-((1r,3s)-6-chloro-3-phenyl-indan-1-yl)-3,3-dimethyl-piperazine

The present invention relates to a process for the manufacture of 4-((1R,3S)-6-Chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine or a pharmaceutically acceptable salt thereof and a process for the manufacture of 1-((1R,3S)-6-Chloro-3-phenyl-indan-1-yl)-3,3-dimethyl-piperazine or a pharmaceutically acceptable salt thereof.

CROSS-LINKED CYCLIC AMINE COMPOUNDS AND AGENTS FOR PEST CONTROL

Cyclic amine compounds represented by formula (1) 116-. (canceled)19. Cyclic amine compounds according to claim 17 , wherein Cyrepresents a pyridazyl group substituted by halogen claim 17 , nitro claim 17 , or haloalkyl.20. Agents for pest control comprising at least one of the cyclic amine compounds of . The present invention relates to novel cyclic amine compounds and agents for pest control which contain these cyclic amine compounds or the like as active ingredients.Priority is claimed on Japanese Patent Application No. 2005-294126, filed Oct. 6, 2005, Japanese Patent Application No. 2005-294127, filed Oct. 6, 2005, Japanese Patent Application No. 2005-297803, filed Oct. 12, 2005, Japanese Patent Application No. 2005-297804, filed Oct. 12, 2005, Japanese Patent Application No. 2006-016877, filed Jan. 25, 2006, and Japanese Patent Application No. 2006-182314, filed Jun. 30, 2006, the contents of which are incorporated herein by reference.Although many compounds which have insecticidal/acaricidal activities are conventionally known, there are problems such as insufficient effect thereof, limitation of use thereof because of drug resistance problems, occurrence of phytotoxicity or contamination in plant bodies, or strong toxicity against mammalians, fish, or the like.As compounds with backbones similar to those of the compounds of the present invention, compounds represented by the formula below are known.In the formula, X represents —O—, —N(R)—, —S—, or the like and Rrepresents a substituted saturated heterocyclic group or the like. As a representative of such compounds, the compound represented by the formula below is known (refer to Patent document 1).Moreover, the compounds represented by the formula below are known.In the formula, X represents —CH— or the like; Z represents a bonding or the like; Rrepresents an optionally substituted aryl or an optionally substituted heteroaryl; and Rand Rrepresent —(CH)— or the like together. However, when Rand Rrepresent —(CH ...

Patch preparation

A patch preparation containing a support and an adhesive layer formed on one surface of the support, wherein the adhesive layer contains 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine or a physiologically acceptable acid addition salt thereof, an acrylic polymer, lactic acid, sesame oil and one or more kinds of stabilizers selected from 2-mercaptobenzimidazole, 2,6-di-tert-butyl-4-methylphenol and propyl gallate. A patch preparation containing a support and an adhesive layer containing lactic acid and magnesium aluminometasilicate and formed on at least one surface of the support, which preparation is superior in both skin permeability and adhesiveness in the presence of water.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 130-. (canceled)321. The composition of claim , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.331. The composition of claim , wherein the acetylcholinesterase inhibitor is donepezil.35. The composition of claim 34 , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.365. The composition of claim claim 34 , wherein the acetylcholinesterase inhibitor is donepezil.38. The method of claim 37 , wherein the treating is for Alzheimer's Disease.39. The method of claim 38 , wherein the treating is for mood disorder.40. The method of claim 39 , wherein the mood disorder is depression.41. The method of claim 38 , further comprising administration of an acetylcholinesterase inhibitor.42. The method of claim 41 , wherein the acetylcholinesterase inhibitor is donepezil.44. The method of claim 43 , wherein the treating is for Alzheimer's Disease.45. The method of claim 43 , wherein the treating is for mood disorder.46. The method of claim 45 , wherein the mood disorder is depression.47. The method of claim 44 , further comprising administration of an acetylcholinesterase inhibitor.48. The method of claim 47 , wherein the acetylcholinesterase inhibitor is donepezil. The invention is directed to certain chromane, isochromane, and dihydroisobenzofuran derivatives, their salts, pharmaceutical compositions comprising them and their use in therapy of the human body. The compounds of the invention have been found to modulate the metabotropic glutamate receptor 2 (mGluR2), and hence are expected to be useful in the treatment of Alzheimer's Disease and other diseases mediated by the mGuR2 receptor.The metabotropic glutamate receptors are known to contain one or more allosteric sites, which may alter the affinity with which glutamate and other metabotropic glutamate (mGuR) ligands bind to the primary binding ...

BICYCLIC ROR-GAMMA MODULATORS

Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds. 11. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein X is —NR— or —C(R)(R)—.12. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at a and b.13. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at c and d.14. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at a and c.15. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at b and d.19. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein each Rand each Rare hydrogen.20. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein t is 1 , 2 , or 3.21. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein t is 1.22. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Ris C-Calkyl , C-Cheteroaryl , (C-Cheteroaryl)-C-Calkylene- , —S(O)R , —C(O)R , —C(O)OR , or —C(O)—C-Calkylene-OR , wherein C-Cheteroaryl and (C-Cheteroaryl)-C-Calkylene- are optionally substituted with 1 or 2 groups each independently selected from halo , C-Calkyl , C-Chaloalkyl , and hydroxyl.23. The compound of any one of - , or a pharmaceutically acceptable salt , solvate ...

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': '2', 'sub': 3', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '2', '3', '2', '3, 'Ris selected from H, cyclopropyl, —CH, —CH(CH), —CH—OH, —CH—OCH, —CHF, —CHF, —CF, —CHCHF, —CHCHF, —CHCF, —CH—O—CHF, —CH—O—CHF, —CH(CH)—O—CHF, —CH(CH)—O—CHF, —CH—NH—CHCF, and —CH—N(CH)—CHCF;'}{'sup': '2A', 'Ris selected from H and methyl;'}{'sup': '3', 'Ris selected from H and methyl; and'}{'sup': '3A', 'Ris selected from H and methyl.'}4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': 2', '2A, 'Rand Rare both methyl; and'}{'sup': 3', '3A, 'Rand Rare both H.'}8. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of phenyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, pyrazolyl, thienyl, thiazolyl, thiadiazolyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, 2, or 3, provided that the value of n does not exceed the maximum number of substitutable hydrogen atoms on ring B; and{'sup': '1', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6, 'each R(when present) is independently selected from the group consisting of halogen, —CN, —OH, —(C-C) alkyl, —O—(C-C) alkyl, —(C-C) haloalkyl, —O—(C-C) haloalkyl, cyclopropyl, cyclobutyl, —NH, —NH(C-C)alkyl, —N(C-Calkyl), —C(O)O(C-C) alkyl, and phenyl.'}9. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of: phenyl, pyrazolyl, pyridinyl, thienyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, or 2; and{'sup': '1', 'sub': 3', '2, 'each R(when present) is independently selected from ...

COMPOUNDS AND METHODS FOR TREATING CANCER, NEUROLOGICAL DISORDERS, ETHANOL WITHDRAWAL, ANXIETY, DEPRESSION, AND NEUROPATHIC PAIN

Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain. 2. (canceled)4. The compound of claim 1 , wherein Ris halogen.1. The compound of claim 1 , wherein Ris halogen claim 1 , —CN claim 1 , —C(O)R claim 1 , —OR claim 1 , —NRR claim 1 , —C(O)OR claim 1 , —C(O)NRR claim 1 , —S(O)R claim 1 , —S(O)OR claim 1 , —S(O)NRR claim 1 , —ONRR claim 1 , —NHC(O)NHNRR claim 1 , substituted or unsubstituted alkyl claim 1 , substituted or unsubstituted heteroalkyl claim 1 , substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted aryl claim 1 , or substituted or unsubstituted heteroaryl.6. (canceled)7. The compound of claim 1 , wherein Ris halogen claim 1 , —NRR claim 1 , substituted or unsubstituted alkyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or unsubstituted heteroaryl.8. (canceled)10. The compound of claim 9 , wherein ring A is aryl or heterocycloalkyl.12. The compound of claim 9 , wherein Ris halogen claim 9 , —CF claim 9 , —CN claim 9 , —OH claim 9 , unsubstituted or R-substituted alkyl or unsubstituted or R-substituted heteroalkyl.1317.-. (canceled)18. The compound of claim 1 , wherein Ris —OR claim 1 , —NRR claim 1 , —C(O)OR claim 1 , substituted or unsubstituted alkyl claim 1 , substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or unsubstituted heteroaryl.19. (canceled)20. The compound of claim 1 , wherein Ris —C(O)OR claim 1 , wherein Ris R-substituted or unsubstituted aryl claim 1 , wherein Ris —CF claim 1 , —CN claim 1 , —OH claim 1 , unsubstituted alkyl or R-substituted or unsubstituted heteroalkyl.21. (canceled)22. The compound of claim 1 , wherein Ris R-substituted or ...

AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS

Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject. 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein each Ris claim 2 , independently at each occurrence claim 2 , halo.4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein each Ris claim 2 , independently at each occurrence claim 2 , halo or —C-Calkyl claim 2 , wherein the alkyl is optionally substituted 1-3 times with halo.7. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , together with a pharmaceutically acceptable carrier.8. A method of treating an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound of .9. A method of reducing the viral load associated with an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound of .10. A method of reducing reoccurrence of an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound of .11. A method of inducing remission of hepatic injury from an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound of .12. The method of claim 8 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor claim 8 , immunomodulatory agents claim 8 , pegylated interferon claim 8 , viral entry inhibitor claim 8 , viral maturation inhibitor claim 8 , literature-described capsid assembly modulator claim 8 , ...

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': '2', 'sub': 3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '2', '3', '2', '3, 'Ris selected from H, cyclopropyl, —CH, —CH(CH), —CH—OH, —CH—OCH, —CF, —CHCHF, —CHCHF, —CHCF, —CH—O—CHF, —CH—O—CHF, —CH(CH)—O—CHF, —CH(CH)—O—CHF, —CH—NH—CHCF, and —CH—N(CH)—CHCF;'}{'sup': '2A', 'Ris selected from H and methyl;'}{'sup': '3', 'Ris selected from H and methyl; and'}{'sup': '3A', 'Ris selected from H and methyl.'}4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': 2', '2A, 'Rand Rare both methyl; and'}{'sup': 3', '3A, 'Rand Rare both H.'}8. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of phenyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, pyrazolyl, thienyl, thiazolyl, thiadiazolyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, 2, or 3, provided that the value of n does not exceed the maximum number of substitutable hydrogen atoms on ring B; and{'sup': '1', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6, 'each R(when present) is independently selected from the group consisting of halogen, —CN, —OH, —(C-C) alkyl, —O—(C-C) alkyl, —(C-C) haloalkyl, —O—(C-C) haloalkyl, cyclopropyl, cyclobutyl, —NH, —NH(C-C)alkyl, —N(C-Calkyl), —C(O)O(C-C) alkyl, and phenyl.'}9. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of: phenyl, pyrazolyl, pyridinyl, thienyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, or 2; and{'sup': '1', 'sub': 3', '2, 'each R(when present) is independently selected from the group consisting of ...

COMPOUNDS AND METHODS FOR TREATING CANCER, NEUROLOGICAL DISORDERS, ETHANOL WITHDRAWAL, ANXIETY, DEPRESSION, AND NEUROPATHIC PAIN

Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain. 153.-. (canceled)55. The compound of claim 54 , wherein Ris halogen.56. The compound of claim 54 , wherein{'sup': 2', '4', '4', '4', '4A', '4', '4', '4A', '4', '4', '4', '4A', '4', '4A', '4', '4A, 'sub': n2', 'n2', 'n2, 'Ris halogen, —CN, —C(O)R, —OR, —NRR, —C(O)OR, —C(O)NRR, —S(O)R, —S(O)OR, —S(O)NRR, —ONRR, —NHC(O)NHNRR, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.'}57. The compound of claim 54 , wherein Ris halogen claim 54 , —OR claim 54 , —NRR claim 54 , —C(O)OR claim 54 , substituted or unsubstituted alkyl claim 54 , substituted or unsubstituted cycloalkyl claim 54 , substituted or unsubstituted heterocycloalkyl claim 54 , substituted or unsubstituted aryl claim 54 , substituted or unsubstituted heteroaryl.58. The compound of claim 54 , wherein Ris halogen claim 54 , —OR claim 54 , —NRR claim 54 , substituted or unsubstituted alkyl claim 54 , substituted or unsubstituted heterocycloalkyl claim 54 , substituted or unsubstituted aryl claim 54 , substituted or unsubstituted heteroaryl.59. The compound of claim 54 , wherein{'sup': 1', '3', '3', '3A', '3', '3', '3', '3, 'sub': 1', '10, 'Ris Cl, F, Br, —OH, —OR, —NRR, R-substituted or unsubstituted C-Calkyl, R-substituted or unsubstituted heterocycloalkyl, R-substituted or unsubstituted aryl, R-substituted or unsubstituted heteroaryl,'}{'sup': '3A', 'Ris hydrogen;'}{'sup': 3', '3B', '3B', '3B', '3B', '3B', '3B, 'sub': 3', '2', '2', '3', '2', '2', '2', '2, 'Ris —CF, —CN, —OH, —NH, —CONH, —S(O)H, —S(O)NH, —NHC(O) NH, —NHC(O)H, —OCHF, R-substituted or unsubstituted alkyl, R-substituted or unsubstituted heteroalkyl, R-substituted or ...

Solid pharmaceutical dispersions with enhanced bioavailability

Dosage form containing two or more active pharmaceutical ingredients in different physical forms

Patch Preparation

Targets, methods, and reagents for diagnosis and treatment of schizophrenia

Process for production of azabicycloalkanol derivative

아자비시클로알칸올 유도체, 특히 농의약 중간체로서 유용한 시스-3-치환-3-아자비시클로[3.2.1]옥탄-8-올 유도체를 수율이 양호하고, 게다가 공업적으로 저렴하게 제조하는 것이다. 수산기로 치환된 메틴을 부제 탄소로서 갖는 아자비시클로C 6-10 알칸올 유도체의 디아스테레오머, 예를 들어 트랜스-3-치환-3-아자비시클로[3.2.1]-8-올 유도체를 천이 금속 착물 존재 하에서 수산기로 치환된 메틴을 이성화시켜, 열역학적으로 안정한 어느 디아스테레오머, 예를 들어 시스-3-치환-3-아자비시클로[3.2.1]-8-올 유도체를 과잉으로 함으로써, 아자비시클로C 6-10 알칸올 유도체 중, 열역학적으로 안정한 어느 디아스테레오머를 제조한다. Azabicycloalkanol derivatives, particularly cis-3-substituted-3-azabicyclo [3.2.1] octan-8-ol derivatives, which are useful as agrochemical intermediates, have good yields and are industrially inexpensive. Diastereomers of azabicycloC 6-10 alkanol derivatives having a methine substituted as a hydroxyl group as a subsidiary carbon, for example trans-3-substituted-3-azabicyclo [3.2.1] -8-ol derivatives Azabicyclo by isomerizing methine substituted with hydroxyl groups in the presence of a complex to excess any thermodynamically stable diastereomer such as cis-3-substituted-3-azabicyclo [3.2.1] -8-ol derivatives Of the C 6-10 alkanol derivatives, any thermodynamically stable diastereomer is prepared.

W-aminoalkanic acid aryl amide

Method of treatment of psychotic disorders

FIELD: medicine, psychiatry, pharmacy. SUBSTANCE: invention relates to novel method of treatment of psychotic disorders by administration in mammal needing in such treatment of effective dose of compound of the formula (1) where Z 1 means sulfur atom; Z 2 means oxygen or sulfur atom; R means hydrogen atom or group Z 2 -R 2 ; R 1 means hydrogen atom or C 1 -C 5 -alkyl; R 2 means C 1 -C 15 -alkyl; R 5 ,R 6 mean hydrogen atoms. EFFECT: valuable medicinal properties of method. 2 cl, 1 tbl озячгегс пы сэ (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ ^”2 191 580 ' ОМК А бл К 31/4462, 31/427, А б1Р 13) С2 25/18 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 96105388/14, 15.08.1994 (24) Дата начала действия патента: 15.08.1994 (30) Приоритет: 19.08.1993 1$ 08/109300 (43) Дата публикации заявки: 10.06.1998 (46) Дата публикации: 27.10.2002 (56) Ссылки: ЕР 0591027 АЛ (ЗУМТНЕЕАВО), 06.04.1994. ЕР 0591026 АЛ (ЗУМТНЕГАВО), 06.04.1994. \МО 9203430 АЛ (МОУМО МОКОЗК А/З), 05.03.1992. ЗЧ 1095878 А (Жансен Фармасетика Н.В.), 30.05.1984. (85) Дата перевода заявки РСТ на национальную фазу: 19.03.1996 (86) Заявка РСТ: ОК 94/00305 (15.08.1994) (87) Публикация РСТ: М/О 95/05174 (23.02.1995) (98) Адрес для переписки: 129010, Москва, ул. Б.Спасская 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", Н.Г. Лебедевой (71) Заявитель: НОВО НОРДИСК А/С (ОК) (72) Изобретатель: БАЙМАСТЕР Франклин Портер (0$), ШЕННОН Харлан И. (1$) (73) Патентообладатель: НОВО НОРДИСК А/С (0К) (74) Патентный поверенный: Лебедева Наталья Георгиевна (54) СПОСОБ ЛЕЧЕНИЯ ПСИХОТИЧЕСКИХ РАССТРОЙСТВ (57) Изобретение относится к новому способу лечения психотических расстройств путем введения млекопитающему, нуждающемуся в этом, эффективного количества соединения формулы |[, где 71 - сера, 72 - кислород или сера; К - водород или группа 7? - В?; К! водород или С1-С5 алкил: В? - С 1-С45 алкил, В $, Вб - водород. 1 з.п.Ф-лы, 1 табл. 2191580 С2 КО озячгегс пы сэ КУЗЗАМ АСЕМСУ ГОК ...

Compounds

Method for preparing benzylamine derivatives or their salts

Patch preparation

지지체 및 해당 지지체의 한 면에 형성된 점착제 층을 함유하는 첩부 제제로서, 여기서 점착제 층은 2-(4-에틸-1-피페라지닐)-4-(4-플루오로페닐)-5,6,7,8,9,10-헥사히드로시클로옥타[b]피리딘 또는 그의 생리학적으로 허용가능한 산부가염, 아크릴계 중합체, 젖산, 참깨유 및 2-메르캅토벤즈이미다졸, 2,6-디-tert-부틸-4-메틸페놀 및 갈산 프로필로부터 선택되는 1종 또는 2종 이상의 안정화제하는 것을 특징으로 하는 첩부 제제를 제공한다. 지지체 및 젖산과 메타규산알루민산 마그네슘을 함유하고 지지체의 적어도 한 면에 형성된 점착제 층을 포함하는 첩부 제제는 피부 투과성과 수분 존재 하에서의 점착성이 모두 우수하다. (4-ethyl-1-piperazinyl) -4- (4-fluorophenyl) -5,6-dihydroxybenzene, and a pressure sensitive adhesive layer formed on one side of the support, wherein the pressure sensitive adhesive layer comprises 2- 7,8,9,10-hexahydrocycloocta [b] pyridine or a physiologically acceptable acid addition salt thereof, an acrylic polymer, lactic acid, sesame oil and 2-mercaptobenzimidazole, 2,6- Butyl-4-methylphenol, and propyl gallate. The present invention also provides an adhesive preparation characterized by comprising at least one stabilizer selected from butyl-4-methylphenol and propyl gallate. A patch preparation comprising a support and a pressure-sensitive adhesive layer containing lactic acid and magnesium metasilicate aluminate and formed on at least one side of the support is excellent in both skin permeability and adhesion in the presence of water.

Modulation and repletion/enhancement of the complement system for treatment of trauma

The present invention features the use of selected complement activation inhibitor(s) for treating an individual who has suffered a severe injury. The complement activation inhibitor acts at or above the level of C3 activation and does not significantly deplete or irreversibly inhibit complement activation. Also provided are compositions and methods for repleting and/or enhancing complement activation capacity in a subject who has suffered a traumatic injury.

Modulation and repletion/enhancement of the complement system for treatment of trauma

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailabilty

DISPOSABLE SOLID PHARMACEUTICAL SUBSTANCES WITH INCREASED BIO AVAILABILITY

Διασπορές στερεού που έχει ξηρανθεί με ψεκασμό που περιλαμβάνουν μερικώς διαλυτό φάρμακο και ηλεκτρική οξεική υδροξυπροπυλμεθυλκυτταρίνη (HPMCAS) παρέχουν αυξημένη υδατική διαλυτότητα ή/και βιοδιαθεσιμότητα σε ένα περιβάλλον ΧΡήσης. Spray-dried solid dispersions comprising partially soluble drug and hydroxypropylmethylcellulose acetate (HPMCAS) provide increased aqueous solubility and / or bioavailability in a USE environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Composition comprising a spray-dried solid dispersion

Solid pharmaceutical dispersions with enhanced bioavailability

含有微溶药物和羟丙基甲基纤维素乙酸琥珀酸酯(HPMCAS)的喷雾干燥固体分散体，它能够在使用环境中提供提高了的水溶解度和/或生物利用度。

Solid pharmaceutical dispersions with increased bioavailability.

Patente de Invenção: <B>"DISPERSõES FARMACêUTICAS SóLIDAS COM UMA BIODISPONIBILIDADE AUMENTADA"<D>. As dispersões sólidas por pulverização que compreendem uma droga fracamente solúvel e succinato de acetato de hidroxipropil-metilcelulose (HPMCAS) fornecem uma acrescida solubilidade aquosa e/ou biodisponibilidade num ambiente de utilização.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with increased bioavailability

Solid pharmaceutical dispersions with increased bioavailability

SOLID PHARMACEUTICAL DISPERSIONS WITH INCREASED BIODISPONIBILITY.

UNAS DISPERSIONES SOLIDAS Y SECAS PARA PULVERIZACION, QUE COMPRENDEN UN FARMACO ESCASAMENTE SOLUBLE Y SUCCINATO DE ACETATO DE HIDROXIPROPILMETILCELULOSA (HPMCAS) PROPORCIONAN UN AUMENTO DE LA SOLUBILIDAD EN AGUA Y/O DE LA BIODISPONIBILIDAD EN EL AMBIENTE EN QUE SE UTILIZA. SOLID AND DRY DISPERSIONS FOR SPRAYING, WHICH INCLUDE A SCASAMENTLY SOLUBLE PHARMACO AND HYDROXYPROPYL-CELLULOSE ACETATE SUCCINATE (HPMCAS) PROVIDE AN INCREASE IN WATER SOLUBILITY AND / OR SEQUENTIALIZABILITY IN SEABILITY.

Solid pharmaceutical dispersions comprising drug and hpmcas and process for their preparation

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Solid pharmaceutical dispersions with enhanced bioavailability

Solid pharmaceutical dispersions with enhanced bioavailability

含有微溶药物和羟丙基甲基纤维素乙酸琥珀酸酯(HPMCAS)的喷雾干燥固体分散体,它能够在使用环境中提供提高了的水溶解度和/或生物利用度。

Solid pharmaceutical dispersions with enhanced bioavailability

含有微溶药物和羟丙基甲基纤维素乙酸琥珀酸酯(HPMCAS)的喷雾干燥固体分散体，它能够在使用环境中提供提高了的水溶解度和/或生物利用度。

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or bioavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Composition including dispersion system of spray-dried solid

(57)【要約】 【課題】 本発明は、噴霧乾燥固体分散系を含む組成物 を提供する。 【解決手段】 難溶性薬物とヒドロキシプロピルメチル セルロースアセテートスクシネート（ＨＰＭＣＡＳ）と を含んだ噴霧乾燥固体分散系は、使用環境において水性 溶解度および／またはバイオアベイラビリティの増大を もたらす。

Solid pharmaceutical dispersions with enhanced bioavailability

Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or biavailability in a use environment.

Solid pharmaceutical dispersions with increased bioavailability

Method for preparing benzylamine derivatives or their salts

Method of obtaining benzylamine derivatives or salts thereof

The method of obtaining benzalamine derivatives or their salts

New dihalo-amino-benzylamines.

O-AMINOALKANOIC ACID ARYLAMIDES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION

Patent FR2321282B1

NOVEL AROMATIC ESTERS AND AMIDES, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

Patent FR2499076B1

Method for producing azabicycloalkanol derivative

アザビシクロアルカノール誘導体、とりわけ、農医薬中間体として有用なシス−３−置換−３−アザビシクロ［３．２．１］オクタン−８−オール誘導体を収率よく、しかも工業的に安価に製造するものである。水酸基に置換されたメチンを不斉炭素として有するアザビシクロＣ６−１０アルカノール誘導体のジアステレオマー、たとえば、トランス−３−置換−３−アザビシクロ［３．２．１］−８−オール誘導体を、遷移金属錯体存在下にて水酸基に置換されたメチンを異性化させ、熱力学的に安定ないずれかのジアステレオマー、たとえば、シス−３−置換−３−アザビシクロ［３．２．１］−８−オール誘導体を過剰にすることにより、アザビシクロＣ６−１０アルカノール誘導体のうち、熱力学的に安定ないずれかのジアステレオマーを製造する。 Azabicycloalkanol derivatives, in particular, cis-3-substituted-3-azabicyclo [3.2.1] octane-8-ol derivatives useful as agricultural and pharmaceutical intermediates with good yield and industrially inexpensive production It is. Diastereomers of azabicyclo C6-10 alkanol derivatives having methine substituted with a hydroxyl group as an asymmetric carbon, such as trans-3-substituted-3-azabicyclo [3.2.1] -8-ol derivatives, transition metals Any methine substituted with a hydroxyl group in the presence of the complex is isomerized and is thermodynamically stable, for example, cis-3-substituted-3-azabicyclo [3.2.1] -8- An excess of the all derivative produces any thermodynamically stable diastereomer of the azabicyclo C6-10 alkanol derivatives.

NOVEL DERIVATIVES OF (3-INDOL-3 YL) AMINO-2-PROPIONYLOXY ACETIC ACID, PROCESSES FOR THEIR PREPARATION AND MEDICAMENTS CONTAINING SAME

NOUVEAUX DERIVES DE L'ACIDE (INDOL-3 YL)-3 AMINO-2 PROPIONYLOXY-2 ACETIQUE, PROCEDES POUR LEUR PREPARATION ET MEDICAMENTS LES CONTENANT. ILS REPONDENT A LA FORMULE GENERALE I CI-APRES: (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN ATOME D'HYDROGENE, UN RADICAL ALKYLE LINEAIRE OU RAMIFIE RENFERMANT 1 A 12 ATOMES DE CARBONE, OU UN RADICAL ALICYCLIQUE MONO- OU POLYCLIQUE RENFERMANT 5 A 16 ATOMES DE CARBONE, EVENTUELLEMENT LIE PAR UN RADICAL METHYLENE, AINSI QUE LEURS SELS D'ADDITION PHARMACEUTIQUEMENT ACCEPTABLES. MEDICAMENTS PALLIANT LA DEFICIENCE DU SYSTEME SEROTONINERGIQUE. NEW DERIVATIVES OF ACID (INDOL-3 YL) -3 AMINO-2 PROPIONYLOXY-2 ACETIC, METHODS FOR THEIR PREPARATION AND MEDICINAL PRODUCTS CONTAINING THEM. THEY COMPLY WITH GENERAL FORMULA I BELOW: (CF DRAWING IN BOPI) IN WHICH R REPRESENTS A HYDROGEN ATOM, A LINEAR OR BRANCHED RADICAL ALKYL CONTAINING 1 TO 12 CARBON ATOMS, OR A MONO- OR POLYCLIC ALICYCLIC RADICAL CONTAINING 5 TO 16 CARBON ATOMS, POSSIBLY BOUND BY A RADICAL METHYLENE, AS WELL AS THEIR PHARMACEUTICALLY ACCEPTABLE ADDITIONAL SALTS. MEDICINES RELATING TO THE DEFICIENCY OF THE SEROTONINERGIC SYSTEM.

Process for manufacturing new dihalo-geno-amino-benzylamines

Process for the preparation of norcamphidin and its homologues substituted in position -2 and products in accordance with those obtained

Bis-(4-azatricyclo undecyl)alkoxy fluorenones - interferon promoters, from bis-acyloxyfluorenones and azatricycloalkylhalides

of formula (I): (where R = 4-azatricyclo- 4,3,1,13,8 - undec-4-yl or 1,8,8-trimethyl-3-azabicyclo 3,2,1 oct-3-yl; alk = 1-7 C alkylene; Z = CH2, CHOH or CO), are useful against viral, bacterial and fungal infections in human and veterinary medicine. Their acute toxicity is lower than that of known interferon-stimulants.

PROCEDURE FOR THE PREPARATION OF PSYCHOTROPIC POLYCLIC IMIDES.

LAS AMIDAS SUSTITUIDAS DE FORMULA (I) DONDE X, R, R1 Y R2 REPRESENTAN SUSTANCIAS CUYA FORMULA SE DESCRIBE SON AGENTES ANTOPSICOTICOS Y ANSIOLITICOS CON MUY PEQUEÑOS EFECTOS SECUNDARIOS EXTRAPIRAMIDALES. THE SUBSTITUTED AMIDES OF FORMULA (I) WHERE X, R, R1 AND R2 REPRESENT SUBSTANCES WHOSE FORMULA IS DESCRIBED ARE ANTOPSYCHOTIC AND ANSIOLITICAL AGENTS WITH VERY SMALL EXTRAPIRAMIDAL SIDE EFFECTS.

ω-aminoalkanoic acid arylamides, processes for producing the same, and medicaments containing the same

Targets, methods, and reagents for diagnosis and treatment of schizophrenia

The present invention provides targets, methods, and reagents for the diagnosis and treatment of schizophrenia and related conditions. The invention provides methods for the diagnosis of schizophrenia and susceptibility to schizophrenia by detection of polymorphisms, mutations, variations, alterations in expression, etc., in calcineurin genes or calcineurin interacting genes, or polymorphisms linked to such genes. The invention provides oligonucleotides, arrays, and antibodies for detection of polymorphisms and variants. The invention provides transgenic mice having alterations in such genes. The invention also provides methods of treating schizophrenia by administering compounds that target these genes. The invention further provides screening methods for identifying such compounds and compounds obtained by performing the screens.

Psychotropic bicyclic imides

Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects:

Quaternary ammonium picolinates - with hypotensive, ganglioplegic and antiseptic activity

Quaternary ammonium picolinates are of formula (I) (where X, X1-3 are 1-20C hydrocarbyl opt. substd. by a halo, CN, OH; 9C acyl, 9C acyloxy or 9C hydroacyloxy; or 2 or 3 of X,X1-3 may be linked to one another directly or via an O-atom to form a heterocyclic ring with the N-atom; R is H, alkyl, alkenyl, cycloalkyl, phenyl, halophenyl, alkylphenyl, or alkoxyphenyl). (I) are hypotensive, ganglioplegic and antiseptic agents.

Patent JPS6136830B2

Camphidine derivative, production thereof, and use thereof

Camphidine derivative of the formula (see formula I) wherein R is the formula (see formula II) in which R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or optionally substituted phenyl, n is 0 or 1, R is cycloalkyl of C 5-8 which is optionally substituted by lower alkyl, norbornyl, bicyclo [3.3.1] nonyl, naphthyl, 1,3-benzodioxolyl, pyridyl or thienyl, m is an integer of 1-4, and C* is an asymmetric carbon, or nontoxic salt thereof.

Method for producing piperidin-4-one-derivative

Provided is a method for producing a piperidin-4-one derivative useful as an intermediate for agricultural chemicals or pharmaceutical products. A piperidin-4-one derivative represented by formula (III-a) or formula (III-b) is produced by reacting a cyclic bis(aminol)ether compound represented by formula (I) and an acetone derivative represented by formula (II) in the presence of at least one substance selected from the group consisting of protonic acids, Lewis acids, acid halides and dialkyl sulfuric acids.

A process for the production of a piperidin -4-one derivative

Modulation and repletion/enhancement of the complement system for treatment of trauma

The present invention features the use of selected complement activation inhibitor(s) for treating an individual who has suffered a severe injury. The complement activation inhibitor acts at or above the level of C3 activation and does not significantly deplete or irreversibly inhibit complement activation. Also provided are compositions and methods for repleting and/or enhancing complement activation capacity in a subject who has suffered a traumatic injury.

3,4-dihydroisoquinoline compounds as muscrinic receptor antagonists for the treatment of respiratory, urinary and gastrointestinal diseases

The present invention generally relates to muscarinic receptor antagonists of formula (I), which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. Formula (I) wherein Formula (II) represents a nitrogen-containing ring having from 5 to 9 carbon atoms is a bridging group selected from the group consisting of -(CH2)n-, -CH(Q)CH2-, -CH2CH(Q)CH2-, -CH2-O-CH2- or -CH2-NH-CH2-), where n is an integer selected from 0-3 (wherein when n is zero then T represents a direct bond); Y is alkylene, alkenylene, alkynylene or no atom; X is -NH or oxygen.

PROCEDURE FOR THE PREPARATION OF 2,7-BIS DERIVATIVES OF FLUORENES

Targets, methods, and reagents for diagnosis and treatment of schizophrenia

The present invention provides targets, methods, and reagents for the diagnosis and treatment of schizophrenia and related conditions. The invention provides methods for the diagnosis of schizophrenia and susceptibility to schizophrenia by detection of polymorphisms, mutations, variations, alterations in expression, etc., in calcineurin genes or calcineurin interacting genes, or polymorphisms linked to such genes. The invention provides oligonucleotides, arrays, and antibodies for detection of polymorphisms and variants. The invention provides transgenic mice having alterations in such genes. The invention also provides methods of treating schizophrenia by administering compounds that target these genes. The invention further provides screening methods for identifying such compounds and compounds obtained by perfoming the screens.

W-aminoalkanoic acid arylamides

ABSTRACT OF THE DISCLOSURE The present invention provides .alpha.-aminoalkanoic acid arylamides having the formula R'(CH2)n CONHR .............(I) wherein R represents a phenyl or naphthyl group which can be substituted with a halogen atom, or anitro, lower alkyl, lower alkoxyl, hydroxyl, acetoamino or lower alkoxycarbonyl group; R' represents an amino group and n is an integer of from 4 to 8 which have a blood platelet aggregation inhibiting effect, and are preventive and therapeutic medicines for thromlosis in encephalo- and cardio-vasculer system. The present invention also provides a process for their preparation.

Antipsychotic method

Patent FI41962B

Psychotropic polycyclic imides

Substituted imides of formula (I) are antipsychotic, anxiolytic agents with very little extrapyramidal side effets, in which X is -O-, -S-, -SO-, -SO2- ,-CR3R4- where R3 and R4 independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R3 and R4 form a cycloalkyl group of 3 to 5 carbon atoms; n is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R1 and R2, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R1 and R2 complete a benzene ring, or a group of formula (II) or (III), where Y is -CH2-, -CH2-CH2-, -O- or -S- and the dotted line represents optional unsaturation; or a pharmaceutically acceptable salt thereof. In addition, the intermediate b3-dicarboxylic and the corresponding anhydrides-2,3,3a,3b,4,5,6,6a,7,7a-decahydro-4,6,7-metheno-1H-cyclopenta[a]pentalene-1,3-dicarboxylic acid and octahydro-1,5-methano-6,8,9-methenopentaleno[1,2-d]oxepin-2,4(1H,5H)-dione represent especially significant aspects of the invention.

Solid preparation for oral administration of cariprazine hydrochloride

Disclosed is a solid preparation for oral administration, which comprises cariprazine hydrochloride, in which lactose is used as the main excipient, and which enables the stable storage of cariprazine hydrochloride contained therein without the need of adding cyclodextrin.

Pyrrolo-pyridine derivatives as dopamine receptor ligands

Compounds of formula (I) are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia wherein Q is (Qa), (Qb), (Qc).

Use of 5-hydroxytryptamine-antagonists in the treatment of mental disorders originating in childhood

The invention relates to the use of a compound which acts as an antagonist of 5-HT at 5-HT₃ receptors in the treatment of autism or another disorder originating in childhood in which there is mental retardation.

Arylpiperidine derivatives

A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl side chain is further substituted by certain heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders and are represented by the formula: wherein Ar is methoxyphenyl or naphthyl; n is an integer of from two to four, inclusive; X is a direct link; and R is 2-amino-4-thiazolylphenyl, 5-oxindolyl, 2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl or 1,8,8-trimethyl-2,4-dioxo-3-azabicyclo-[3.2.1]octan-3-yl. Methods for preparing all these compounds from known starting materials are also disclosed.

A dosage form containing two or more active pharmaceutical ingredients in different physical forms

Aralkyl esters and processes for their preparation

ABSTRACT Compounds with the general formula I I or pharmaceutically acceptable, salts thereof, wherein X and Y are halogen, CF3 or hydrogen, provided that both X and Y are not hydrogen and R is a straight or branched saturated or unsaturated alkyl group having 2-5 carbon atoms in the chain processes for the production of said compounds and the use of the said compounds for the treatment of mental disorders.

5- (2-OXYPHENYL) -PYRROL DERIVATIVES AS DOPAMINE-D3 RECEPTOR ANTAGONISTS

Azepine derivatives production thereof and use thereof as sigma-receptor ligands

Formamide derivatives useful as adrenoceptor

Azepine derivative, production thereof, and use thereof.

An azepine derivative represented by general formula (1) or a nontoxic salt thereof, a process for producing the same, and a therapeutic agent containing the same as the active ingredient for treating diseases related to σ-receptor, wherein R represents a group represented by general formula (2) (wherein R1 represents hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or optionally substituted phenyl, and n represents 0 or 1), C¿5?-C8 cycloalkyl which may be substituted by lower alkyl, norbornyl, bicyclo[3.3.1]nonyl, naphthyl, 1,3-benzodioxolyl, pyridyl or thienyl; m represents an integer of 0 to 4; and C* represents an asymmetric carbon atom. The compound (1) and nontoxic salt thereof have a high affinity for σ-receptor but scarcely any affinity for other receptors, thus being utilized for treating diseases related to σ-receptor, such as schizophrenia.

Treatment of Obsessive-Compulsive Disorders with 5-HT2 Antagonists

The present invention is directed to 5-HT2 antagonists end their use as agents in the treatment of obsessive-compulsive disorders (OCD). The invention is particularly directed to the compound (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol which is a member of a class of 5-HT2 antagonists known as N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5-HT2 receptor site.

Process for production of azabicycloalkanol derivative

The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan- 8-ol derivative which is useful as an intermediate for an agricultural or pharmaceutical agent, with a high degree of efficiency and at an industrially low cost. A methyne having a hydroxyl group as a substituent in a diastereomer of an azabicyclo-C6-10-alkanol derivative having the methyne as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of the diastereomers of the derivative (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of the diastereomers of the azabicyclo-C6-10-alkanol derivative can be produced.