KR970065521A - 아미노알킬 에테르 및 아실아미노알킬 에테르, 이들의 제조방법, 및 브라디키닌 수용체 길항제로서의 이들의 용도 - Google Patents

아미노알킬 에테르 및 아실아미노알킬 에테르, 이들의 제조방법, 및 브라디키닌 수용체 길항제로서의 이들의 용도 Download PDF

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KR970065521A
KR970065521A KR1019970008175A KR19970008175A KR970065521A KR 970065521 A KR970065521 A KR 970065521A KR 1019970008175 A KR1019970008175 A KR 1019970008175A KR 19970008175 A KR19970008175 A KR 19970008175A KR 970065521 A KR970065521 A KR 970065521A
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aryl
compound
alkanoyl
alkyl
formula
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홀거 하이취
아달베르트 바그너
클라우스 비르트
베른바르트 쉘켄스
게르하르트 뇔켄
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야코비, 루츠 위르겐
훽스트 아크티엔게젤사프트
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Publication of KR970065521A publication Critical patent/KR970065521A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/24—Oxygen atoms attached in position 8
    • C07D215/26—Alcohols; Ethers thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/18—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Abstract

브라디키닌 B2수용체에 대해 높은 친화력을 갖고 수용성이 향상된 아미노알킬 에테르 및 아실아미노알킬 에케르를 기술한다. 이러한 아미노알킬 에테르 및 아실아미노알킬 에테르를 화학실(1)로 나타낼 수 있다
상기 화학식(1)에서, R1, R2및 R3은 알킬, 아릴 알킬아릴, 할로겐, 수소, 사이클로알킬, CHO, CO-O-알킬 또는 COOH이고; R4및 R5은 수소, 할로겐, 알콕시, 니트로, 시아노 또는 S-알킬이며; n 은 1 내지 8의 수이고; R6은 수소, 알킬, 알킬알케닐 또는 알킬아릴이며; R7은 수소 및 치환되거나 치환되지 않은 아실 라디칼이다. 화학식(1)의 화합물의 제조방법은 명세서에서 기술하는 바와 같다.

Description

아미노알킬 에테르 및 아실아미노알킬 에테르, 이들의 제조방법, 및 브라디키닌 수용체 길항제로서의 이들의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 화학식(1) 화합물 및 생리학적으로 허용되는 이의 염.
    상기 화학식(1)에서, R1,R2및 R3은 동일하거나 상이하고, (C1-C5)-알킬, (C6-C10)-아릴, (C1-C3)-알킬-(C6-C10)-아릴, 할로겐 수소, (C3-C8)-사이클로알킬, CHO, CO-O-(C1-C3)-알킬 또는 COOH이며; R4및 R5는 동일하거나 상이하고, 수소, 할로겐, (C1-C3)-알콕시, 니트로, 시아노 또는 S-(C1-C3)-알킬이고;n은 1 내지 8의 수이며; R6은 수소, (C1-C3)-알킬, (C3-C5)-알킬알케닐 또는 (C1-C3)-알킬-(C6-C10)-아릴이고; R7은 수소; 및 (C1-C6)-알카노일, (C1-C3)-알콕시-(C2-C6)-알카노일, (C1-C6)-알킬카바모일-(C2-C6)-알카노일, (C6-C12)-아릴-(C2-C6)-알카노일, (C3-C7)-알케노일,(C3-C8)-사이클로알킬카보닐, (C5-C7)-사이클로알케닐카보닐, (C1-C3)-알콕시카보닐, (C6-C12)-아릴옥시카보닐, (C6-C12)-아로일, (C1-C3)-알콕시-(C6-C12)-아로일, 할로겐(-(C6-C12)-아로일, (C6-C1)-아릴-(C3-C6)-알케노일, (C1-C3)-알콕시-(C6-C12)-아릴-(C3-C6)-알케노일,(C1-C3)-알킬렌디옥시-(C6-C12)-아릴-(C3-C6)-알케노일, 니트로-(C6-C12)-아릴-(C3-C6)-앞케노일, 시아노-(C6-C12)-아릴-(C3-C6)-알케노일, 할로-(C6-C12)-아릴-(C3-C6)-알케노일, 할로-(C1-C3)-알킬-(C6-C12)-아릴-(C3-C6)-알케노일, 헤테로-(C3-C8)-사이클로알킬-(C6-C12)-아릴-(C3-C6)-알케노일,아미노-(C6-C12)-아릴-(C3-C6)-알케노일,(C1-C4)-알킬아미노-(C6-C12)-아릴-(C3-C6)-알케노일,(C2-C5)-아실아미노-(C6-C12)-아릴신나모일, (C1-C3)-알콕시카보닐아미노-(C6-C12)-아릴신나모일, (C1-C4)-알킬아미노카보닐아미노신나모일, 헤테로-(C6-C12)-아릴-(C2-C6)-알카노일아미노-(C6-C12)-아릴-(C3-C6)-알케노일, (C6-C12)-아로일아미노-(C6-C12)-아릴-(C3-C6)-알케노일, 헤테로-(C6-C12)-아릴카보닐암미노-(C6-C12)-아릴-(C3-C6)-알케노일,(C1-C5)-알킬설포닐아미노-(C6-C12)-아릴-(C3-C6)-알케노일, (C1-C5)-알킬우레이도-(C6-C12)-아릴-(C3-C6)-알케노일,(C2-C6)-알카노일-(C6-C12)-아릴-(C3-C6)-알케노일,(C1-C5)-알콕시카보닐-(C6-C12)-아릴-(C3-C6)-알케노일,(C1-C5)-알킬카바모일-(C6-C12)-아릴-(C3-C6)-알케노일,(C6-C12)-아릴카바모일-(C6-C12)-아릴-(C3-C6)-알케녹실, (C6-C12)-아릴-(C1-C5)-알콕시카보닐,(C1-C5)-알킬카바모일,(C6-C12)-아릴카바모일, (C6-C12)-아로일카바모일,(C1-C6)-알킬설포닐, (C6-C12)-알릴설포닐, (C6-C12)-아릴-(C1-C6)-알킬설포닐 및 프탈로일 (R6=R7일때)인 치환되거나 치환되지 않은 아실라디칼이다.
  2. 제1항에 있어서, R1,R2및 R3이 동일하거나 상이하고, 수소 또는 (C1-C3)-알킬이며 R4및 R5가 할로겐이고 R6이 수소, 메틸, 에틸 또는 벤질인 화학식(1)의 화합물.
  3. 제1항 또는 제2항에 있어서, R7이 수소 또는 아실 라디칼인 화학식(1)의 화합물.
  4. 제1항 내지 제3항 중의 어느 한 항에 있어서, R1,R2및R3이 동일하거나 상이하고, 수소, 메틸, 에틸 또는 프로필이며 R4및 R5가 염소이고 n이 1 내지 4이며 R6이 수소이고 R7이 수소, (C2-C3)-알카노일, (C3-C5)-알케노일, (C1-C5)-알킬아미노카보닐, (C6-C10)-아릴-(C1-C3)-알킬아미노카보닐, (C1-C5)-알킬옥시카보닐, (C6-C10)-아릴-(C1-C3)-알킬옥시카보닐, (C6-C10)-아릴-(C3-C7)-사이클로알킬카보닐 또는 페닐환이 수소, (C1-C3)-알킬, 아미노, (C1-C3)-모노아미노와 (C1-C3)-디알킬아미노, 할로겐,(C1-C3)-할로알킬, (C2-C5)-아실아미노 및 (C1-C3)-알콕시로부터 선택된 두개 이하의 동일하거나 상이한 리디칼로 치환된 트랜스-신남산 잔기인 화학식(1)의 화합물.
  5. 화학식(2)의 화합물을 수소화리튬, 수소화칼륨 또는 수소화나트륨과 같은 금속 수소화물, 또는 탄산나트륨, 탄산칼륨 또는 탄산세슘과 같은 알칼리 금속 탄산염의 존재하에 DMF 또는 DMSO와 같은 불활성 용매속에서 0℃ 내지 60℃의 온도에서 화학식(3)의 화합물과 반응시켜 화학식(4)의 화합물을 수득하는 단계 a),화학식(4)의 화합물을 에탄올 속에서 환류하에 가하이드라진 분해반응시켜 화학식 (1a)의 화합물로 전환시키는 단계 b),화학식(1a)의 화합물을 공지된 방법에 따라 적절히 아실화 및/또는 알킬화시키는 단계 c) 및 생성된 화학식(1)의 화합물을 공지된 방법에 따라 생리학적으로 허용되는 이의 염으로 적절히 전환시키는 단계 d)를 포함하여, 제1항 내지 제4항 중의 어느 한 항에 따르는 화학식(1)의 화합물을 제조하는 방법.
    상기 화학식 (2),(3),(4) 및 (1a)에서, R1, R2, R3,R4, R5및 n은 제1항에서 정의한 바와 같다.
  6. 제1항 내지 제4항 중의 어느 한 항에 따르는 화학식(1)의 화합물의 약제로서의 용도.
  7. 제1항 내지 제4항 중의 어느 한 항에 따르는 화학식(1)의 화합물을 하나 이상 함유하는 약제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019970008175A 1996-03-13 1997-03-12 아미노알킬 에테르 및 아실아미노알킬 에테르, 이들의 제조방법, 및 브라디키닌 수용체 길항제로서의 이들의 용도 KR970065521A (ko)

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DE19609827A DE19609827A1 (de) 1996-03-13 1996-03-13 Aminoalkyl- und Acylaminoalkylether, Verfahren zu deren Herstellung und ihre Verwendung als Bradykinin-Rezeptorantagonisten
DE19609827.0 1996-03-13

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Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
JP2002505689A (ja) 1997-06-19 2002-02-19 セプレイコー インコーポレイテッド キノリン−インドール抗菌剤、それらに関する用途及び組成物
US6376670B1 (en) 1997-06-19 2002-04-23 Sepracor Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
US6103905A (en) * 1997-06-19 2000-08-15 Sepracor, Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
EP1914236A1 (en) 2002-04-10 2008-04-23 Ortho-McNeil Pharmaceutical, Inc. Novel heteroaryl alkylamide derivatives useful as bradykinin receptor modulators
ITMI20021247A1 (it) * 2002-06-07 2003-12-09 Menarini Ricerche Spa Antagonisti basici non peptidici della bradichinina e loro impiego informulazioni farmaceutiche
TWI407960B (zh) 2007-03-23 2013-09-11 Jerini Ag 小分子緩激肽ｂ２受體調節劑
AU2008319397B2 (en) 2007-11-01 2013-01-31 Acucela, Inc. Amine derivative compounds for treating ophthalmic diseases and disorders
MA50804B1 (fr) 2017-11-24 2022-05-31 Pharvaris Netherlands B V Nouveaux antagonistes des récepteurs de bradykinine b2
AR118982A1 (es) 2019-05-23 2021-11-17 Pharvaris Gmbh Antagonistas cíclicos del receptor b2 de bradiquinina
UY38707A (es) 2019-05-23 2020-12-31 Pharvaris Gmbh Nuevos antagonistas cíclicos del receptor b2 de bradiquinina
DK4203919T3 (da) 2021-08-05 2024-04-29 Pharvaris Gmbh Lipidbaseret sammensætning til oral administration af bradykinin-b2-receptorantagonister
WO2023180577A1 (en) 2022-03-25 2023-09-28 Pharvaris Gmbh Therapeutic uses of bradykinin b2-receptor antagonists
WO2023180575A1 (en) 2022-03-25 2023-09-28 Pharvaris Gmbh Solid composition comprising solubilised bradykinin b2-receptor antagonists
TW202345810A (zh) 2022-03-25 2023-12-01 瑞士商帕法瑞斯有限責任公司 包含緩激肽ｂ２受體拮抗劑之固態延長釋放組成物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5216165A (en) * 1990-10-03 1993-06-01 American Home Products Corporation N-substituted aminoquinolines as analgesic agents
US5288725A (en) * 1992-10-15 1994-02-22 Merck & Co., Inc. Pyrroloquinoline Bradykinin antagonist
AU680870B2 (en) * 1993-04-28 1997-08-14 Astellas Pharma Inc. New heterocyclic compounds
US6756388B1 (en) * 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
ATE269310T1 (de) * 1994-10-27 2004-07-15 Fujisawa Pharmaceutical Co Pyridopyrimidinone, chinoline und anellierte n- heterozyklen als bradykinin-antagonisten
FR2735128B1 (fr) * 1995-06-07 1997-07-25 Fournier Ind & Sante Nouveaux composes de benzenesulfonamide, leur procede de preparation et utilisation en therapeutique.
FR2737892B1 (fr) * 1995-08-17 1997-10-24 Fournier Ind & Sante Nouveaux composes de benzenesulfonamide, procede de preparation et utilisation en therapeutique

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HRP970138A2 (en) 1998-04-30
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TR199700184A2 (xx) 1997-10-21
ATE192738T1 (de) 2000-05-15
SI0795547T1 (en) 2000-10-31
ID16217A (id) 1997-09-11
HUP9700566A1 (hu) 2000-08-28
AR006189A1 (es) 1999-08-11
CA2199771A1 (en) 1997-09-13
PL318923A1 (en) 1997-09-15
BR9701267A (pt) 1999-01-12
JPH101472A (ja) 1998-01-06
NO971136L (no) 1997-09-15
IL120427A0 (en) 1997-07-13
DE59701617D1 (de) 2000-06-15
NO971136D0 (no) 1997-03-12
DK0795547T3 (da) 2000-09-18
EP0795547B1 (de) 2000-05-10
GR3033415T3 (en) 2000-09-29
AU1621797A (en) 1997-09-18
ES2148858T3 (es) 2000-10-16
PT795547E (pt) 2000-10-31
HU9700566D0 (en) 1997-04-28
CZ76697A3 (en) 1997-10-15
SK32097A3 (en) 1998-01-14
MX9701857A (es) 1997-09-30
JP4317597B2 (ja) 2009-08-19
EP0795547A1 (de) 1997-09-17
TW363891B (en) 1999-07-11
US6140341A (en) 2000-10-31
ZA972129B (en) 1997-09-15

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