ПРОИЗВОДНОЕ 2-АМИНОПРОПАН-1,3-ДИОЛА, ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ ДЛЯ ИХ СИНТЕЗА

Описывается производное 2-аминопропан-1,3-диола общей формулы где R1, R2, R3 и R4 одинаковы или различны, и каждый обозначает водород или прямой или разветвленный алканоил, содержащий от 1 до 6 атомов углерода; его фармацевтически приемлемая соль добавления кислоты или гидрат; фармацевтическая композиция, обладающая иммуносупрессивной активностью; 2-амино-2-(2-(4-(1-гидрокси-5-фенилпентил)фенил)этил) пропан-1,3-диол или его производное, где аминогруппа защищена алифатической ацильной группой и/или гидроксигруппа защищена трет-бутилдиметилсилильной группой, а также 2-амино-2-(2-(4-формилфенил)этил)-пропан-1,3-диол, его производное, где аминогруппа и/или гидроксигруппа защищены алифатической группой и/или гидроксигруппа защищена трет-бутилдиметилсилильной группой. Ввиду небольшой токсичности, высокой безопасности и иммуносупрессивного действия, эти производные могут использоваться в качестве предупреждающих или подавляющих реакцию отторжения при пересадке органов и для профилактики или лечения ...

Способ получения N-замещенных аминоацетиладамантанов

USE FROM PHENALKYLAMINEN TO THE PRODUCTION OF CHOLESTERINSENKENDEN DRUGS

USE OF PHENALKYLAMINES

Use of compounds of the formula (see formula I) wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl, L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene, n = 0 or, where L contains an O atom, n = 0 or 1; Q is C1-7-alkyl, C2-10-alkenyl or a group of formula Q': R is H, halogen, CF3, CN or NO2, R3 and R4 are H, C1-4-alkyl or halogen and R5 is H or, where R is H, H or halogen, and their pharmaceutically acceptable acid addition salts for the manufacture of cholesterol-lowering medicaments, as well as novel compounds falling under formula I.

PROCESS FOR PREPARING ( ) TRANS-4-P-FLUOROPHENYL-3-HYDROXYMETHYL-1

The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX') methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

PROCEDURE FOR THE PRODUCTION OF (+) - TRANS-4-PFLUOROPHENYL-3-HYDROXYMETHYL-1-METHYLPIPERIDIN

2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME

SYNTHETIC ION CHANNELS

2-Aminopropan-1,3-diol-Verbindungen, ihre medizinische Anwendung und Zwischenprodukte zu ihrer Synthese

Synthetic ion channels

Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.

2-Aminopropan-1,3-diol-Verbindungen, ihre medizinische Anwendung und Zwischenprodukte zu ihrer Synthese

2-AMINOPROPAN-1,3-DIOL-VERBINDUNGEN, YOUR MEDICAL APPLICATION AND INTERMEDIATE PRODUCTS TO YOUR SYNTHESIS

2-AMINOPROPAN-1,3-DIOL-VERBINDUNGEN, YOUR MEDICAL APPLICATION AND INTERMEDIATE PRODUCTS TO YOUR SYNTHESIS

ПРИМЕНЕНИЕ ФЕНАЛКИЛАМИНОВ

Применение соединений формулы Iгде один из R1 и R2 представляет собой С1-7 алкил, а другой представляет собой С1-7-алкил либо С2-6-алкенилметил, L представляет собой при определенных условиях связанный через О-атом с фенильной группой С1-11-алкилен либо С2-11-алкенилен, или L представляет собой 1,4-фенилен, n обозначает 0 либо, если L содержит O-атом, n обозначает 0 или 1, Q представляет собой С1-7-алкил, C2-10-алкенил либо группу формулы Q':R представляет собой Н, галоген, СF3, CN либо NO2, R3 и R4 представляют собой Н, С1-4-алкил либо галоген и R5 представляет собой Н либо, если R - водород, Н или галоген, и их приемлемых в фармацевтике аддитивных солей кислот для изготовления лекарственных средств, снижающих содержание холестерина, а также новые соединения, соответствующие формуле I.

2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

METHOD OF MODULATING MEMBRANE POTENTIAL OF A CELL

Use of phenalkylamines

Use of phenalkylamines

USE OF PHENALKYLAMINES

Use of compounds of the formula I wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl, L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene, n = 0 or, where L contains an O atom, n = 0 or 1; Q is C1-7-alkyl, C2-10-alkenyl or a group of formula Q': Q' R is H, halogen, CF3, CN or NO2, R3 and R4 are H, C1-4-alkyl or halogen and R5 is H or, where R is H, H or halogen, and their pharmaceutically acceptable acid addition salts for the manufacture of cholesterol-lowering medicaments, as well as novel compounds falling under formula I.

2-Aminopropane-1,3-diol compound, pharmaceutical use thereof and synthetic intermediates therefor

PROCESS FOR PREPARING (.PLUSMN.) TRANS-4-P-FLUOROPHENYL-3-HYDROXYMETHYL-1-METHYLPIPERIDINE

The present invention relates to a process for preparing (.plusmn.)-trans-4-p- fluorophenyl-3-hydroxymethyl-1-methylpiperidine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX') methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

Verfahren zur Herstellung von (+)-trans-4-p-Fluorophenyl-3-hydroxymethyl-1-methylpiperidin

Pharmaceutical composition for lowering cholesterol containing phenalkylamines and certain novel phenalkylamines

Use of compounds of the formula wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl, L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene, n=0 or, where L contains an O atom, n=0 or 1; Q is C1-7-alkyl, C2-10-alkenyl or a group of formula Q, R is H, halogen, CF3, CN or NO2, R3 and R4 are H, C1-4-alkyl or halogen and R5 is H or, where R is H, H or halogen, and their pharmaceutically acceptable acid addition salts for the manufacture of cholesterol-lowering medicaments, as well as novel compounds falling under formula 1.

2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

タペンタドールおよびその中間体を調製するための新しい方法

VERFAHREN ZUR HERSTELLUNG VON (+)-TRANS-4-P-FLUOROPHENYL-3-HYDROXYMETHYL-1-METHYLPIPERIDIN

SYNTHETIC ION CHANNELS

Use of phenylalkylamines for producing cholesterol lowering agents

Use of compounds of the formula in which one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenylmethyl, L is C1-11-alkylene or C2-11-alkenylene which is optionally bonded via an O atom to the phenyl group, or L is 1,4-phenylene, n is 0 or, if L contains an O atom, n is 0 or 1, Q is C1-7-alkyl, C2-10-alkenyl or a group of the formula Q : R is H, halogen, CF3, CN or NO2, R3 and R4 are H, C1-4-alkyl or halogen, and R5 is H or, if R is H, H or halogen, and their pharmaceutically acceptable acid addition salts for producing cholesterol-lowering medicinal agents, and compounds covered by formula I.

2-氨基丙烷-1，3-二醇化合物、其作为医药的用途及其合成中间体

... 本发明涉及用通式(I)表示的2-氨基丙烷-1，3-二醇化合物、其制药上可容许的酸加成盐或者它们的水合物，由含有该化合物的医药、含有该化合物和制药上容许的载体的药物组合物以及作为合成中间体有用的2-氨基-2-(2-(4-(1-羟基-5-苯基戊基)苯基)乙基)丙烷-1，3-二醇或者2-氨基-2-(2-(4-甲酰基苯基)乙基)丙烷-1，3-二醇、其氨基和/或羟基被保护了的化合物或者它们的盐。(式中，R#+[1]、R#+[2]、R#+[3]、R#+[4]相同或不同，分别地表示氢原子或者酰基)本发明的化合物显示了毒性小、安全性高的优良免疫抑制作用，作为脏器移植时的排斥反应的预防或抑制剂、或者作为自身免疫疾病或过敏性疾病的预防或治疗剂是有用的。 ...

Verwendung von Phenalkylaminen zur Herstellung von cholesterinsenkenden Arzneimitteln

COMPOSITION 2-AMINOPROPANO-1, 3-DIOL, ITS PHARMACEUTICAL JOB AND INTERMEDIATE SYNTHETIC FOR The same

Process for the preparation of (±) - trans-4-p-fluorofenil-3-hidroximetil-1-metilpiperi dina

2-AMINOPROPAN-1,3-DIOL-VERBINDUNGEN, IHRE MEDIZINISCHE ANWENDUNG UND ZWISCHENPRODUKTE ZU IHRER SYNTHESE

Fluorine compound, surfactant, aqueous coating composition and silver halide photographic light-sensitive material using them

Disclosed is a silver halide photographic light-sensitive material having one or more layers including a light-sensitive silver halide emulsion layer on a support, wherein any of the layers contains the specific fluorine compound. The silver halide photographic light-sensitive material can be stably produced and is imparted with antistatic property.

METHOD OF MODULATING MEMBRANE POTENTIAL OF A CELL

Provided herein are methods of modulating membrane potential of a cell membrane using self-assembling compounds. Also provided herein are methods of regulating a natural voltage-dependent ion channel in a cell membrane using the self-assembling compounds disclosed herein. Further provided herein are methods of treating, preventing and /or managing a disease that is related to the abnormal membrane potential responses by using the self-assembling compounds disclosed herein.

Method of modulating membrane potential of a cell

Provided herein are methods of modulating membrane potential of a cell membrane using self-assembling compounds. Also provided herein are methods of regulating a natural voltage-dependent ion channel in a cell membrane using the self-assembling compounds disclosed herein. Further provided herein are methods of treating, preventing and /or managing a disease that is related to the abnormal membrane potential responses by using the self-assembling compounds disclosed herein.

2-aminopropane-1,3-glycol compound, its use as medicine and its synthetic intermediate

2-AMINOPROPAN-1,3-DIOL-VERBINDUNGEN, IHRE MEDIZINISCHE ANWENDUNG UND ZWISCHENPRODUKTE ZU IHRER SYNTHESE

Method of modulating membrane potential of a cell

PROCESS FOR PREPARING (±) TRANS-4-P-FLUOROPHENYL-3-HYDROXYMETHYL-1

The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX') methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

SYNTHETIC ION CHANNELS

Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.

Composto 2-aminopropano-1,3-diol, seu emprego farmacêutico e intermediários sintéticos para o mesmo

2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

The present invention relates to a compound of the general formulawherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME

2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

The present invention relates to a compound of the general formula wherein R¹, R², R³ and R⁴ are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

Use of phenylalkylamines for producing cholesterol lowering agents

METHOD OF MODULATING MEMBRANE POTENTIAL OF A CELL

Amino alkenyloxybenzene derivatives

A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula см. иллюстрацию в PDF-документе wherein one of R1 and R2 is C1-7 -alkyl and the other is C1-7 -alkyl or C2-6 -alkenyl-methyl; L is C1-11 -alkylene or C2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7 -alkyl, C2-10 -alkenyl or a group of formula см. иллюстрацию в PDF-документе wherein R is H, halogen, CF3, CN or NO2 ; R3 and R4 are H, C1-4 -alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.

USE OF PHENALKYL AMINE

PURPOSE: To provide a novel compound exhibiting cholesterol-lowering activity and useful for treatment and prevention of hypercholesterolemia and athetosclerosis. CONSTITUTION: There is provided a compound of formula I [wherein one of R1 and R2 is 1-7C alkyl and the other is 1-7C alkyl or 2-6C alkenylmethyl; L can be linked to phenyl via O or is 1-11C alkylene or the like; R3 and R4 are each H, 1-4C alkyl or the like; (d) is 0 or 1; and Q is 1-7C alkyl, 2-10C alkenyl or Q' (wherein R is H, CF3, CN or the like; and R5 is H, halogen or the like)], e.g. 4-{[6-(allylmethylamino)hexyl]oxy}-3-chlorobenzophenone. The compound of formula I is obtained by reacting, e.g. dibromohexane with 3- chloro-4-hydroxybenzophenone in the presence of tetrabutylammonium bromide to obtain 4-[(6-bromohexyl)oxy]-3-chlorobenzophenone and subsequently reacting the resultant compound with N-allylmethyl amine. COPYRIGHT: (C)1995,JPO ...

COMPOSITION 2-AMINOPROPANO-1,3-DIOL, ITS PHARMACEUTICAL USE AND ITS SYNTHETIC INTERMEDIATE

Compound useful for lowering cholesterol

A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula I wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl; L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7-alkyl, C2-10-alkenyl or a group of formula Q' wherein R is H, halogen, CF3, CN or NO2; R3 and R4 are H, C1-4-alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.

Process for preparing (+)trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine

The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX') methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

PROCESS FOR THE PREPARATION OF (+) - TRANS-4-P-FLUOROFENIL-3-HIDROXIMETIL-1-METILPIPERIDINA

PROCESS FOR PREPARING (+) TRANS-4-P-FLUOROPHENYL-3-HYDROXYMETHYL-1

Amino alkenyloxybenzene derivatives

A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula I wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl; L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7-alkyl, C2-10-alkenyl or a group of formula Q' wherein R is H, halogen, CF3, CN or NO2; R3 and R4 are H, C1-4-alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.

Compound useful for lowering cholesterol

A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula см. иллюстрацию в PDF-документе wherein one of R1 and R2 is C1-7 -alkyl and the other is C1-7 -alkyl or C2-6 -alkenyl-methyl; L is C1-11 -alkylene or C2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7 -alkyl, C2-10 -alkenyl or a group of formula см. иллюстрацию в PDF-документе wherein R is H, halogen, CF3, CN or NO2 ; R3 and R4 are H, C1-4 -alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.

Method of lowering cholesterol

A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula I wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl; L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7-alkyl, C2-10alkenyl or a group of formula Q' wherein R is H, halogen, CF3, CN or NO2; R3 and R4 are H, C1-4-alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.

2-氨基丙烷-1,3-二醇化合物、其作为医药的用途及其合成中间体

... 本发明涉及用通式(I)表示的2-氨基丙烷-1，3-二醇化合物、其制药上可容许的酸加成盐或者它们的水合物，由含有该化合物的医药、含有该化合物和制药上容许的载体的药物组合物以及作为合成中间体有用的2-氨基-2-(2-(4-(1-羟基-5-苯基戊基)苯基)乙基)丙烷-1，3-二醇或者2-氨基-2-(2-(4-甲酰基苯基)乙基)丙烷-1，3-二醇、其氨基和/或羟基被保护了的化合物或者它们的盐。∴(式中，R#+[1]、R#+[2]、R#+[3]、R#+[4]相同或不同，分别地表示氢原子或者酰基)本发明的化合物显示了毒性小、安全性高的优良免疫抑制作用，作为脏器移植时的排斥反应的预防或抑制剂、或者作为自身免疫疾病或过敏性疾病的预防或治疗剂是有用的。 ...

Process for preparing (±)-trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine

The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine of formula I. The present invention also relates to novel intermediates of the formula IX and IX', methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

Processo para a preparação de (±)-trans-4-p-fluorofenil-3-hidroximetil-1-metilpiperi dina

2-aminopropane-1,3-diol compounds medicinal use thereof and intermediates in synthesizing the same

Use of phenalkylamines

Synthetic ion channels

Process for preparing (±)trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine

The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX') methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

Method of lowering cholesterol

A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula см. иллюстрацию в PDF-документе wherein one of R1 and R2 is C1-7 -alkyl and the other is C1-7 -alkyl or C2-6 -alkenyl-methyl; L is C1-11 -alkylene or C2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7 -alkyl, C2-10 alkenyl or a group of formula см. иллюстрацию в PDF-документе wherein R is H, halogen, CF3, CN or NO2 ; R3 and R4 are H, C1-4 -alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.

Use of phenalkylamines