KR890012952A - Phenoxyethylamine Derivatives And Preparation Methods And Compositions Showing Excellent α_1-Blocking Activity Containing The Same - Google Patents

Phenoxyethylamine Derivatives And Preparation Methods And Compositions Showing Excellent α_1-Blocking Activity Containing The Same Download PDF

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KR890012952A
KR890012952A KR1019890001736A KR890001736A KR890012952A KR 890012952 A KR890012952 A KR 890012952A KR 1019890001736 A KR1019890001736 A KR 1019890001736A KR 890001736 A KR890001736 A KR 890001736A KR 890012952 A KR890012952 A KR 890012952A
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acid addition
pharmaceutically
cited
phenoxyethylamine
represented
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KR1019890001736A
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KR930011150B1 (en
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야스오 이또
히데오 가또
에이이찌 고시나까
노부오 오가와
가즈야 미다니
슌이찌로 사꾸라이
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이또 겐지
호꾸리꾸 세이야꾸 가부시기가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/23—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/27—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음.No content.

Description

페녹시에틸아민 유도체와 그 제조방법 및 이를 함유하는 우수한 α1-블로킹 활성을 나타내는 조성물Phenoxyethylamine derivatives and preparation methods thereof, and compositions having excellent α1-blocking activity containing the same

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (16)

다음식 (I)에 의하여 표시되는 것들로부터 선정된 페녹시에틸아민 유도체 및 약학적으로 인용할 수 있는 그 산부가염.Phenoxyethylamine derivatives selected from those represented by the following formula (I) and pharmaceutically usable acid addition salts thereof. 식중, R1및 R5는 저급알킬이고, R2및 R3은 동일 또는 상이하며, 각각 수소 또는 저급알킬이고, 또는은 환멤버원자로서 질소, 산소 또는 유황원자를 포함하는 5- 또는 6-멤버 환 시스템의 기이고, R4는 수소 또는 저급알킬이고, n은 1 내지 3의 정수이다.Wherein R 1 and R 5 are lower alkyl, R 2 and R 3 are the same or different and are each hydrogen or lower alkyl, or Is a group of a 5- or 6-membered ring system containing nitrogen, oxygen or sulfur atoms as ring member atoms, R 4 is hydrogen or lower alkyl and n is an integer from 1 to 3. 제1항에 있어서, (+)-5-[2-[2-(5-플루오로-2-메톡시페녹시)에틸아미노]-프로필]-2-메톡시벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.The compound and pharmaceutical according to claim 1, which is (+)-5- [2- [2- (5-fluoro-2-methoxyphenoxy) ethylamino] -propyl] -2-methoxybenzenesulfonamide Acid addition salts, which can be cited as. 제1항에 있어서, R-(-)-5-[2-[2-(5-플루오로-2-메톡시페녹시)에틸아미노]-프로필]-2-메톡시벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.A compound according to claim 1 which is R-(-)-5- [2- [2- (5-fluoro-2-methoxyphenoxy) ethylamino] -propyl] -2-methoxybenzenesulfonamide and Pharmacologically cited acid addition salts. 제1항에 있어서, 5-[2-[2-(4-플루오로-2-메톡시페녹시)에틸아미노]-프로필]-2-메톡시벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.A compound according to claim 1, which is 5- [2- [2- (4-fluoro-2-methoxyphenoxy) ethylamino] -propyl] -2-methoxybenzenesulfonamide and may be pharmaceutically recited. That acid addition salt. 제1항에 있어서, 5-[2-[2-(2-에톡시-5-플루오로페녹시)에틸아미노]-프로필 ]-2-메톡시벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.A compound according to claim 1, which is 5- [2- [2- (2-ethoxy-5-fluorophenoxy) ethylamino] -propyl] -2-methoxybenzenesulfonamide and may be pharmaceutically recited. That acid addition salt. 제1항에 있어서, 5-[2-[2-(5-플루오로-2-메톡시페녹시)에틸아미노]-프로필 ]-2-메톡시-N-메틸벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.The compound according to claim 1, which is 5- [2- [2- (5-fluoro-2-methoxyphenoxy) ethylamino] -propyl] -2-methoxy-N-methylbenzenesulfonamide Acid addition salts, which can be cited as. 제1항에 있어서, 5-[2-[2-(5-플루오로-2-메톡시페녹시)에틸아미노]-프로필 ]-2-메톡시-N,N-디메틸벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.A compound according to claim 1, which is 5- [2- [2- (5-fluoro-2-methoxyphenoxy) ethylamino] -propyl] -2-methoxy-N, N-dimethylbenzenesulfonamide and Pharmacologically cited acid addition salts. 제1항에 있어서, 5-[2-[2-(2-에톡시-5-플루오로페녹시)에틸아미노]-프로필 ]-2-메톡시-N,N-디메틸벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.A compound according to claim 1 which is 5- [2- [2- (2-ethoxy-5-fluorophenoxy) ethylamino] -propyl] -2-methoxy-N, N-dimethylbenzenesulfonamide and Pharmacologically cited acid addition salts. 제1항에 있어서, 5-[2-[2-(5-플루오로-2-메톡시페녹시)에틸아미노]-프로필]-2-에톡시벤젠술폰아미드인 화합물 및 약학적으로 인용할 수 있는 그 산부가염.The compound according to claim 1, which is 5- [2- [2- (5-fluoro-2-methoxyphenoxy) ethylamino] -propyl] -2-ethoxybenzenesulfonamide and may be pharmaceutically recited. That acid addition salt. 다음식(II)에 의하여 표시되는 페녹시에틸아민과Phenoxyethylamine represented by the following formula (II) 식중, R5는 상기 정의와 같은 것이고, 다음식(III)에 의하여 표시되는 카르보닐화합물과를 반응시키고,Wherein R 5 is the same as defined above and reacts with a carbonyl compound represented by the following formula (III), 식중, R1,R2,R3,R4및 n은 상기 정의와 같은 것이고, 그 다음에 이와같이 얻어진 화합물을 환원시킴으로써 이루어지는 일반식(I)에 의하여 표시되는 페녹시에틸아민 화합물과 약학적으로 인용할 수 있는 그 산부가염의 제조방법.Wherein R 1 , R 2 , R 3 , R 4 and n are the same as the above definitions, and are then pharmaceutically as phenoxyethylamine compounds represented by the general formula (I) formed by reducing the compound thus obtained. The manufacturing method of the acid addition salt which can be quoted. 다음식(VIII)에 의하여 표시되는 페녹시아세트 알데히드와Phenoxyacetaldehyde represented by the following formula (VIII) 식중, R5는 상기 정의와 같은 것이고, 다음식(IX)에 의하여 표시되는 아민화합물을 반응시키고,In formula, R <5> is the same as the said definition, Reacting the amine compound represented by following formula (IX), 식중, R1,R2,R3,R4및 n은 상기 정의와 같은 것이고, 그 다음에 이와같이 얻어진 화합물을 환원시킴으로써 이루어지는 일반식(I)에 의하여 표시되는 페녹시에틸아민 화합물과 약학적으로 인용할 수 있는 그 산부가염의 제조방법.Wherein R 1 , R 2 , R 3 , R 4 and n are the same as the above definitions, and are then pharmaceutically as phenoxyethylamine compounds represented by the general formula (I) formed by reducing the compound thus obtained. The manufacturing method of the acid addition salt which can be quoted. 다음식(VI)에 의하여 표시되는 플루오로페녹시알칸 화합물과A fluorophenoxyalkane compound represented by the following formula (VI); 식중, X는 할로겐원자를 표시하고, R5는 상기 정의와 같은 것이고, 다음식(IX)에 의하여 표시되는 아민화합물을 반응시키고,Wherein X represents a halogen atom, R5 is as defined above, and reacts the amine compound represented by the following formula (IX), 식중, R1,R2,R3,R4및 n은 상기 정의와 같은 것으로 이루어지는 일반식(I)에 의하여 표시되는 페녹시에틸아민 화합물과 약학적으로 인용할 수 있는 그 산부가염의 제조방법.Wherein R 1 , R 2 , R 3 , R 4 and n are phenoxyethylamine compounds represented by the general formula (I) having the same definitions as above and a method for producing the acid addition salts thereof which can be pharmaceutically cited. . 용해약제의 수단에 의하여 라세메이트를 용해하여 이루어지는 일반식(Ⅰ)에 의하여 표시되는 광학적 활성인 페녹시에틸아민 화합물과 약학적으로 인용할 수 있는 그 산부가염의 제조방법.An optically active phenoxyethylamine compound represented by the general formula (I) formed by dissolving racemate by means of a dissolving agent, and a method for producing the acid addition salt thereof, which can be pharmaceutically cited. 일반식(Ⅰ)에 의하여 표시되는 페녹시에틸아민 화합물 또는 약학적으로 인용할 수 있는 그 산부가염의 유효량 및 약학적으로 인용할 수 있는 증량제 또는 희석제로 이루어지는 고혈압 및 배뇨곤란의 치료에 유용한 α1-블로킹약제.Α1- useful for the treatment of hypertension and dysuria, consisting of an effective amount of a phenoxyethylamine compound represented by the general formula (I) or a pharmaceutically recited acid addition salt and a pharmaceutically cited extender or diluent Blocking agent. 일반식(Ⅰ)에 의하여 표시되는 페녹시에틸아민 유도체 또는 약학적으로 인용할 수 있는 그 산부가염의 유효량 및 약학적으로 인용할 수 있는 증량제 또는 희석제로 이루어지는 고혈압 및 배뇨곤란의 치료를 위하여 유용한 약제 조성물.Pharmaceutical agents useful for the treatment of hypertension and dysuria, consisting of an effective amount of a phenoxyethylamine derivative represented by formula (I) or a pharmaceutically cited acid addition salt and a pharmaceutically cited extender or diluent Composition. 일반식(Ⅰ)에 의하여 표시되는 페녹시에틸아민 유도체 또는 약학적으로 인용할 수 있는 그 산부가염 또는 이를 포함하는 약제 조성물의 유효량을 환자에게 투약하는 단계로 이루어지는 고혈압 또는 배뇨곤란의 치료방법.A method of treating hypertension or difficulty in urination, comprising administering to a patient an effective amount of a phenoxyethylamine derivative represented by the general formula (I) or a pharmaceutically recited acid addition salt or a pharmaceutical composition comprising the same. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019890001736A 1988-02-19 1989-02-15 Phenoxyethylamine derivatives process, for preparing the same, and composition for exhibiting excellent alpha-1-blocking activity containing the same KR930011150B1 (en)

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
JP3506388 1988-02-19
JP88-35063 1988-02-19
JP?63-35063? 1988-02-19
JP?63-138345? 1988-06-07
JP88-138345 1988-06-07
JP13834588 1988-06-07
JP?63-192162? 1988-08-02
JP88-192162 1988-08-02
JP19216288 1988-08-02
JP88-303897 1988-12-02
JP?63-303897? 1988-12-02
JP63303897A JP2696363B2 (en) 1988-02-19 1988-12-02 Phenoxyethylamine derivative

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KR890012952A true KR890012952A (en) 1989-09-20
KR930011150B1 KR930011150B1 (en) 1993-11-24

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ES2200699B1 (en) * 2002-07-12 2005-10-01 Ragactives, S.L PROCEDURE FOR THE SEPARATION OF R (-) AND S (+) - 5- (2 - ((2- (ETOXIFENOXI) ETIL) AMINO) PROPIL-2-METOXIBENCENO-SULFONAMIDE.
US7329780B2 (en) * 2003-12-09 2008-02-12 Cj Corporation Method of preparing optically pure phenethylamine derivatives
SI21655A (en) * 2003-12-29 2005-06-30 LEK farmacevtska dru�ba d.d. Synthesis of optically pure (r)-5-(2-aminopropyl)-methoxybenzene sulphonamide
JP4653966B2 (en) * 2004-04-19 2011-03-16 ダイセル化学工業株式会社 Method for producing 2-benzoyloxyacetaldehyde derivative
JP2006232757A (en) * 2005-02-25 2006-09-07 Ohara Yakuhin Kogyo Kk Method for producing phenoxyethyl halide and its derivative
DE102007028925A1 (en) * 2007-06-22 2008-12-24 Saltigo Gmbh Preparing 2-phenoxy-acetal compound, useful e.g. to prepare 2-alkyl-5-nitrobenzofuran, which is useful as precursor to prepare pharmaceutical active agent, comprises reacting a 2-hydroxyacetal compound with a substituted aromatic compound

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JPH02149554A (en) 1990-06-08
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