KR960017644A - 신규한 설폰아미드 - Google Patents

신규한 설폰아미드 Download PDF

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KR960017644A
KR960017644A KR1019950042804A KR19950042804A KR960017644A KR 960017644 A KR960017644 A KR 960017644A KR 1019950042804 A KR1019950042804 A KR 1019950042804A KR 19950042804 A KR19950042804 A KR 19950042804A KR 960017644 A KR960017644 A KR 960017644A
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alkyl
alkoxy
phenyl
heterocyclyl
halo
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KR1019950042804A
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KR100415030B1 (ko
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브로이 볼커
부리 카스파
카사 쟝-마리
클로제 마흐틴
허쓰 죠지
뢰플러 베른트-미카엘
뮐러 마르셀
나이드하르트 베르너
라무즈 헨리
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프리돌린 클라우스너·롤란드 보러
에프. 호프만-라 롯슈 아크티엔게젤샤프트
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Organic Chemistry (AREA)
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  • Heart & Thoracic Surgery (AREA)
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  • Urology & Nephrology (AREA)
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  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

본 발명은 엔도텔린 수용체의 저해제인 하기 일반식(Ⅰ)의 화합물에 관한 것이다.
상기 식에서, R1는 헤테로사이클릴을 의미하고; R2은 수소, 저급-알킬, 저급-알콕시, 저급-알킬티오, 저급-알콕시-저급-알킬, 저급-알킬설포닐-저급-알콕시, 페닐, 저급 알킬페닐, 저급-알콕시-페닐, 저급-알킬렌-디옥시페닐, 페닐-저급 알킬, 저급 알킬-페닐-저급 알킬, 저급 알콕시-페닐-저급 알킬, 저급알킬렌디옥시페닐-저급 알킬, 헤테로사이클릴 또는 헤테로사이클릴-저급 알킬을 의미하고; R3은 저급-알킬, 저급-알콕시, 포르밀, 할로-저급-알킬, 히드록시-저급-알킬, 아미노-저급-알킬 또는 -CH2O-A-저급 알킬, -(CH2)m-O-(CRaRb)nOH, -(CH2)m-O-(CRaRb)nOR9, -(CH2)m-O-(CRaRb)nNH2또는 -(CH2)m-O-(CRaRb)n-B-R9잔기를 의미하고; R4내지 R8은 수소, 저급-알콕시 또는 할로겐을 의미하고; R9는 헤테로사이클릴; 페닐; 또는 저급-알킬, 저급-알콕시 및/또는 할로겐으로 치환된 페닐; 또는 저급-알킬을 의미하고; Ra및 Rb는 수소 또는 저급-알킬을 의미하고; A는 케탈화 1,2-디히드록시-에틸렌기를 의미하고; B는 -OC(O)O-, -OC(O)NH-, -NHC(O)NH- 또는 -NHC(O)O-를 의미하고; n은 2,3 또는 4를 의미하며; m은 0 또는 1을 의미한다.
이들은 엔도텔린 활성과 관련된 장애, 특히 순환게 장애(예 : 고혈압, 허혈증, 혈관경련 및 협심증)를 치료하는데 사용할 수 있다.

Description

신규한 설폰아미드
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (2)

  1. 하기 일반식(Ⅰ)의 화합물;
    상기 식에서, R1는 헤테로사이클릴을 의미하고; R2은 수소, 저급-알킬, 저급-알콕시, 저급-알킬티오, 저급-알콕시-저급-알킬, 저급-알킬설포닐-저급-알콕시, 페닐, 저급 알킬페닐, 저급-알콕시-페닐, 저급-알킬렌-디옥시페닐, 페닐-저급 알킬, 저급 알킬-페닐-저급 알킬, 적브 알콕시-페닐-저급 알킬, 저급알킬렌디옥시페닐-저급 알킬, 헤테로사이클릴 또는 헤테로사이클릴-저급 알킬을 의미하고; R3은 저급-알킬, 저급-알콕시, 포르밀, 할로-저급-알킬, 히드록시-저급-알킬, 아미노-저급-알킬 또는 -CH2O-A-저급 알킬, -(CH2)m-O-(CRaRb)nOH, -(CH2)m-O-(CRaRb)nOR9, -(CH2)m-O-(CRaRb)nNH2또는 -(CH2)m-O-(CRaRb)n-B-R9잔기를 의미하고; R4내지 R8은 수소, 저급-알콕시 또는 할로겐을 의미하고; R9는 헤테로사이클릴; 페닐; 또는 저급-알킬, 저급-알콕시 및/또는 할로겐으로 치환된 페닐; 또는 저급-알킬을 의미하고; Ra및 Rb는 수소 또는 저급-알킬을 의미하고; A는 케탈화 1,2-디히드록시-에틸렌기를 의미하고; B는 -OC(O)O-, -OC(O)NH-, -NHC(O)NH- 또는 -NHC(O)O-를 의미하고; n은 2,3 또는 4를 의미하며; m은 0 또는 1을 의미한다.
  2. 제1항에 따른 화합물 및 통상의 담체 및 보강제를 함유하는 약학제재.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950042804A 1994-11-25 1995-11-22 신규한설폰아미드 KR100415030B1 (ko)

Applications Claiming Priority (4)

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CH3559/94 1994-11-25
CH355994 1994-11-25
CH2842/95 1995-10-09
CH284295 1995-10-09

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KR960017644A true KR960017644A (ko) 1996-06-17
KR100415030B1 KR100415030B1 (ko) 2004-05-17

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EP (1) EP0713875B1 (ko)
JP (1) JP2755565B2 (ko)
KR (1) KR100415030B1 (ko)
AT (1) ATE199905T1 (ko)
AU (1) AU691353B2 (ko)
CA (1) CA2162630C (ko)
CZ (1) CZ289920B6 (ko)
DE (1) DE59509107D1 (ko)
DK (1) DK0713875T3 (ko)
ES (1) ES2156179T3 (ko)
FI (1) FI117896B (ko)
GR (1) GR3036065T3 (ko)
HK (1) HK1012345A1 (ko)
HU (1) HU225112B1 (ko)
IL (1) IL116064A (ko)
MA (1) MA23725A1 (ko)
MY (1) MY119409A (ko)
NO (1) NO307606B1 (ko)
NZ (1) NZ280495A (ko)
PT (1) PT713875E (ko)
RU (1) RU2162084C2 (ko)
TW (1) TW394763B (ko)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2217034A1 (en) * 1995-04-03 1996-10-10 Sumitomo Pharmaceuticals Company, Limited Novel pyrimidine derivatives effective as psychotropic drug and process for the production thereof
ES2221696T3 (es) * 1997-08-19 2005-01-01 F. Hoffmann-La Roche Ag Procedimiento para la preparacion de piridinas 2,5.disustituidas.
TWI284642B (en) * 1999-01-18 2007-08-01 Hoffmann La Roche Novel heterocyclic sulfonamides
US6417360B1 (en) 1999-03-03 2002-07-09 Hoffmann-La Roche Inc. Heterocyclic sulfonamides
ES2295048T3 (es) 1999-09-03 2008-04-16 Actelion Pharmaceuticals Ltd. Bis-sulfonamidas.
MXPA02006250A (es) * 1999-12-22 2004-09-06 Actelion Pharmaceuticals Ltd Derivados de butino diol.
WO2001081338A1 (en) * 2000-04-25 2001-11-01 Actelion Pharmaceuticals Ltd Substituted sulfonylaminopyrimidines
US6387915B2 (en) 2000-05-31 2002-05-14 Pfizer Inc. Isoxazole-sulfonamide endothelin antagonists
US6670362B2 (en) 2000-09-20 2003-12-30 Pfizer Inc. Pyridazine endothelin antagonists
WO2003051870A1 (en) * 2001-12-18 2003-06-26 Astrazeneca Ab Novel compounds
TWI328007B (en) 2002-01-16 2010-08-01 Astrazeneca Ab Novel compounds
EP1454625A1 (en) * 2003-03-06 2004-09-08 Speedel Development AG Pyridylsulfonamidyl-pyrimidines for the treatment of diabetic nephropathies
EP1725540B1 (en) * 2004-03-05 2012-09-12 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2086544C1 (ru) * 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
TW287160B (ko) * 1992-12-10 1996-10-01 Hoffmann La Roche
TW394761B (en) * 1993-06-28 2000-06-21 Hoffmann La Roche Novel Sulfonylamino Pyrimidines

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RU2162084C2 (ru) 2001-01-20
JPH08208625A (ja) 1996-08-13
JP2755565B2 (ja) 1998-05-20
AU691353B2 (en) 1998-05-14
EP0713875B1 (de) 2001-03-21
EP0713875A1 (de) 1996-05-29
MA23725A1 (fr) 1996-07-01
KR100415030B1 (ko) 2004-05-17
DK0713875T3 (da) 2001-06-11
FI955669A (fi) 1996-05-26
FI955669A0 (fi) 1995-11-24
HUT75030A (en) 1997-03-28
AU3789595A (en) 1996-05-30
MY119409A (en) 2005-05-31
FI117896B (fi) 2007-04-13
IL116064A (en) 2000-06-29
NO954718D0 (no) 1995-11-22
CZ308895A3 (en) 1997-07-16
TW394763B (en) 2000-06-21
IL116064A0 (en) 1996-01-31
HU225112B1 (en) 2006-06-28
NO954718L (no) 1996-05-28
HU9503311D0 (en) 1996-01-29
CA2162630A1 (en) 1996-05-26
HK1012345A1 (en) 1999-07-30
CA2162630C (en) 2007-05-01
NZ280495A (en) 1996-12-20
ATE199905T1 (de) 2001-04-15
GR3036065T3 (en) 2001-09-28
NO307606B1 (no) 2000-05-02
PT713875E (pt) 2001-09-28
CZ289920B6 (cs) 2002-04-17
DE59509107D1 (de) 2001-04-26
ES2156179T3 (es) 2001-06-16

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