KR910000600A - 프로판올아민 유도체 - Google Patents

프로판올아민 유도체 Download PDF

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KR910000600A
KR910000600A KR1019890007915A KR890007915A KR910000600A KR 910000600 A KR910000600 A KR 910000600A KR 1019890007915 A KR1019890007915 A KR 1019890007915A KR 890007915 A KR890007915 A KR 890007915A KR 910000600 A KR910000600 A KR 910000600A
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compound
hydrogen
phenyl
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group
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킨즐 프랑크
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쟝-쟈끄 오가이, 프리돌린 클라우스너
에프.호프만-라 로슈 앤드 캄파니 아크티엔게젤샤프트
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Publication of KR910000600A publication Critical patent/KR910000600A/ko

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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/48—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
    • C07C215/52—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/56—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
    • C07C217/60—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

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Abstract

내용 없음

Description

프로판올아민 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 하기 일반식(I)의 프로판올아민 유도체 및 생리학적으로 허용되는 이의 염.
    상기식에서, R1은 수소 또는 일반식(a)의 그룹이고,(a)
    n은 0 또는 1이며, R2및 R5은 페닐, m-할로페닐, m-트리플루오로 메틸페닐. 티에닐 또는 피리딜이고, R3은 수소 또는 메틸이며, R4은 수소, -CH2COOH, -CH2COO-C1-4-알킬, -(CH2)2O-C1-4-알킬 또는 -(CH|2)2O(CH2)1-4-C6H5이다.
  2. 제1항에 있어서, R1이 수소인 화합물.
  3. 제1항에 있어서, R1이 그룹(a) [여기서, n 및 R5은 제1항에서 정의한 바와 같다]인 화합물.
  4. 제1항 또는 제2항에 있어서, R1이 수소이고, R2는 페닐, m-할로페닐, 특히 m-클로로페닐 또는 m-트리플루오로메틸페닐, 티에닐 또는 피리딜, 특히 2- 또는 3-피리딜이며, R4는 수소, 2-에톡시에틸, 2-펜에톡시에틸 또는 에톡시카보닐메틸이고, 특히 존재할 수 있는 그룹 R3에 결합된 탄소원자가 R-배위인 화합물.
  5. 제1항 또는 제3항에 있어서, R1이 일반식(a)의 그룹(여기서, n이 1이고, R5는 페닐 또는 m-할로페닐, 특히 m-클로로페닐이거나, n이 0이고, R5는 페닐, 특히 그룹R5에 결합된 탄소원자R-배위이다)이고 R2는 페닐 또는 m-할로페닐, 특히 m-클로로페닐이며, R3은 수소이고, R4는 2-에톡시에틸인 화합물.
  6. 제4항에 있어서, R2가 페닐 또는 2-티에닐이고, R4는 2-에톡시에틸 또는 에톡시카보닐메틸인 화합물.
  7. 제5항에 있어서, R1이 β-하이드록시펜에틸, 특히(R)-β-하이드록시펜에틸이고, R2는 m-클로로페닐이며, R3은 수소이고, R4는 2-에톡시에틸인 화합물.
  8. (RS)-m-클로로-β-[p-(2-에톡시에톡시)펜에틸][[[(R)-β-하이드록시펜에틸]아미노]메틸]펜에틸 알콜.
  9. 제6항에 있어서, (R 또는 S)-β-[[[p-(2-에톡시에톡시)펜에틸]아미노]메틸]펜에틸 알콜, 에틸[p-[2-[[β-(하이드록시메틸)펜에틸]아미노]에틸]펜옥시]아세테이트, β-[[[p-(2-에톡시에톡시)-α-메틸렌에틸]아미노]메틸]펜에틸 알콜 및 β-[[[p-(2-에톡시에톡시)펜에틸]아미노]메틸]-2-티오펜에탄올 화합물.
  10. 치료학적 활성 물질로서, 특히 비만증, 당뇨병 및 고단백질 분해를 수반하는 상태를 치료하기 위한 활성 물질로서 제1항 내지 제9항 중 어느 한 항에 따르는 화합물.
  11. 제1항 내지 제9항중의 어느 한 항에 따르는 화합물을 함유하는 약제학적 제제.
  12. 제1항 내지 제9항중의 어느 한 항에 따르는 화합물을 함유하는 동물비육용 사료.
  13. a)하기 일반식(II) 또는 (III)의 아미드를 환원시키고, b)경우에 따라 R4가 수소인 일반식(I)의 페놀을 R4가 그룹 -CH2-COOH 또는 -CH2COOC1-4-알킬인 일반식(I)의 화합물을 염으로 전환시키는 공정을 포함함을 특징으로 하여, 제1항 내지 제9항중의 어느 한 항에 따르는 화합물의 제조하는 방법.
    상기식에서, R1, R2및 R3은 제1항에서 정의한 바와 같고, R6은 수소, -(CH2)2O-C1-4-알킬 또는 -(CH2)2O(CH2)1-4-C6H5이다.
  14. 비만증, 당뇨병 및 고단백질 분해를 수반하는 상태의 치료용 약제학적 제제를 제조하기 위한, 제1항 내지 제9항 중의 어느 한 항에 따른 화합물의 용도.
  15. 상기에 기술된 발명, 특히 실시예를 참조로 한 발명.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890007915A 1988-06-10 1989-06-09 프로판올아민 유도체 KR910000600A (ko)

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CH224588 1988-06-10
CH2245/88-2 1988-06-10

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US (1) US5045567A (ko)
EP (1) EP0345591B1 (ko)
JP (1) JPH0236158A (ko)
KR (1) KR910000600A (ko)
AT (1) ATE87610T1 (ko)
AU (1) AU622907B2 (ko)
DE (1) DE58903919D1 (ko)
DK (1) DK284289A (ko)
ES (1) ES2053866T3 (ko)
FI (1) FI892341A (ko)
HU (1) HUT55344A (ko)
IE (1) IE891855L (ko)
IL (1) IL90528A0 (ko)
MC (1) MC2042A1 (ko)
NO (1) NO170011C (ko)
NZ (1) NZ229456A (ko)
PH (1) PH26237A (ko)
PT (1) PT90802B (ko)
YU (1) YU118389A (ko)
ZA (1) ZA894210B (ko)

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Publication number Priority date Publication date Assignee Title
US5563171A (en) * 1993-11-05 1996-10-08 American Cyanamid Company Treatment of glaucoma and ocular hypertension with β3-adrenergic agonists
US5578638A (en) * 1993-11-05 1996-11-26 American Cyanamid Company Treatment of glaucoma and ocular hypertension with β3 -adrenergic agonists
EP0869121B1 (de) * 1997-04-04 2004-06-09 Aventis Pharma Deutschland GmbH Hypolipidämische Propanolaminderivate
DE19845403B4 (de) 1998-10-02 2005-02-10 Aventis Pharma Deutschland Gmbh Mit Gallensäuren verknüpfte Propanolaminderivate, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
DE19845405C2 (de) * 1998-10-02 2000-07-13 Aventis Pharma Gmbh Arylsubstituierte Propanolaminderivate und deren Verwendung

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7112938A (ko) * 1970-09-30 1972-04-05
HU163935B (ko) * 1971-06-25 1973-11-28
CA1145767A (en) * 1978-07-03 1983-05-03 Jack Mills Phenethanolamines, compositions containing the same, and method for effecting weight control
EP0070134B1 (en) * 1981-07-11 1985-11-13 Beecham Group Plc Secondary phenyl ethanol amines and their pharmaceutical use
CA1258454A (en) * 1982-08-10 1989-08-15 Leo Alig Phenethanolamines
WO1984000956A1 (en) * 1982-08-27 1984-03-15 Beecham Group Plc Secondary arylethanolamines
EP0139921B1 (en) * 1983-08-17 1987-03-25 Beecham Group Plc 2-phenylethylamine derivatives
DE3466387D1 (en) * 1983-11-04 1987-10-29 Beecham Group Plc Tertiary amines
CA1249992A (en) * 1983-11-10 1989-02-14 Marcel Muller Oxazolidines
FR2588556B1 (fr) * 1985-10-11 1988-01-08 Sanofi Sa Derives du naphtalene substitues par un groupement (omega-amino) alcanol a activite antimicrobienne, leur preparation et les compositions les contenant
CA1287061C (en) * 1986-06-27 1991-07-30 Roche Holding Ltd. Pyridine ethanolamine derivatives
DE3866984D1 (en) * 1987-07-21 1992-01-30 Hoffmann La Roche Phenoxypropanolamine.

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DK284289A (da) 1989-12-11
NZ229456A (en) 1992-02-25
JPH0236158A (ja) 1990-02-06
IE891855L (en) 1989-12-10
EP0345591A1 (de) 1989-12-13
ES2053866T3 (es) 1994-08-01
PH26237A (en) 1992-04-01
IL90528A0 (en) 1990-01-18
NO892387D0 (no) 1989-06-09
DK284289D0 (da) 1989-06-09
MC2042A1 (fr) 1990-05-30
FI892341A (fi) 1989-12-11
EP0345591B1 (de) 1993-03-31
ATE87610T1 (de) 1993-04-15
ZA894210B (en) 1990-03-28
US5045567A (en) 1991-09-03
PT90802B (pt) 1994-11-30
NO170011C (no) 1992-09-02
FI892341A0 (fi) 1989-05-16
NO892387L (no) 1989-12-11
YU118389A (en) 1991-06-30
AU622907B2 (en) 1992-04-30
DE58903919D1 (en) 1993-05-06
NO170011B (no) 1992-05-25
AU3602689A (en) 1989-12-14
HUT55344A (en) 1991-05-28
PT90802A (pt) 1989-12-29

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