KR910000711A - 크로만 유도체 - Google Patents

크로만 유도체 Download PDF

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KR910000711A
KR910000711A KR1019890008330A KR890008330A KR910000711A KR 910000711 A KR910000711 A KR 910000711A KR 1019890008330 A KR1019890008330 A KR 1019890008330A KR 890008330 A KR890008330 A KR 890008330A KR 910000711 A KR910000711 A KR 910000711A
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South Korea
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formula
compound
oxy
carbon atoms
pyrazinyl
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KR1019890008330A
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English (en)
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호이슬러 귄터
게리케 롤프
브르지거 한스
바움바르트 만프레트
루에스 인게보르그
데 페이어 야케스
베르그만 롤프
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위르겐 호이만, 라인하르트 쉬틀러
메르크 파텐트 게젤샤프트 미트 베슈랭크터 하프퉁
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Priority claimed from DE3820506A external-priority patent/DE3820506A1/de
Priority claimed from DE3835011A external-priority patent/DE3835011A1/de
Application filed by 위르겐 호이만, 라인하르트 쉬틀러, 메르크 파텐트 게젤샤프트 미트 베슈랭크터 하프퉁 filed Critical 위르겐 호이만, 라인하르트 쉬틀러
Publication of KR910000711A publication Critical patent/KR910000711A/ko

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    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/10—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 two hetero rings linked by a carbon chain containing aromatic 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Dermatology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Cosmetics (AREA)

Abstract

내용 없음

Description

크로만 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 다음 일반식(Ⅰ)의 크로만 유도체 및 그의 염.
    상기 식에서,=CH-CO 또는 =CH-CHR8-이거나, 만약 R5기가 전체적 또는 부분적으로도 수소화되어 있지 않으면 =CH4-CR3R8- 또는 =CH-CR8(OA)-이고, R1은 A이고, R2와 R8은 각각 수소 또는 A이고, R1과 R2는 함께 3-6탄소원자를 지닌 알킬렌이고, R3는 OH 또는 OAc이고, R4는 수소이고, R3와 R4는 함께 결합이고, R5는 A, F, Cl, Br, I, OH, OAc, NO2, NH2, AcNH, HOOC 및/또는 AOOC가 하나 또는 둘 치환되어 있거나 치환되지 않는 피리딜-옥시, 피라디진일-옥시, 피리미딘일-옥시, 피라진일-옥시, 옥소-디히드로-피리딜-옥시, 옥소-디히드로-피리다진일-옥시, 옥소-디히드로-피리미딘일-옥시, 옥소-디히드로-피라진일-옥시, 1H-2-피리돈-1-일, 1H-4-피리돈-1-일, 1H-4-피리다진온-1-일, 1H-6-피리다진온-1-일, 1H-2-, 1H-4-4- 또는 1H-6-피리미딘온-1-일, 1H-2-피리진온-1-일, 3H-2-필롤린온-1-일, 5H-2-필롤린온-1-일, 1H-2-퀴놀론-1-일, 2H-1-이소퀴놀론-2-일, 2H-1-프탈라진온-2-일, 3H-4-퀴나졸린온-3-일, 또는 1H-2-티오피리돈-1-일 등의 치환기를 말하며 이들은 전체적 또는 부분적으로 수소화되어 있고, R6와 R7은 각각 H, A, HO, AO, CHO, ACO, ACS, HOOC, AOOC, AO-CS , ACOO, A-CS-O, 1-6탄소원자를 지닌 히드록시알킬, 1-6탄소원자를 지닌 머르캅토알킬, NO2, NH2, NHA, NA2, CN, F, Cl, Br, I, CF3, ASO, ASO2, AO-SO, AO-SO2, AcNH, AO-CO-NH, H2NSO, HANSO, A2NSO, H2NSO2, HANSO2, A2NSO2, H2NCO, HANCO, A2NCO, H2NCS, HANCS, A2NCS, ASONH, ASO2NH, AOSONH, AOSO2NH, ACO-알킬, 니트로알킬, 시아노알킬, 1-C(=NOH)또는 A-C(=NNH2)이고, R7은 피리딜, 피라다진일, 피리미딘일 또는 피라진일이고, A는 1-6탄소원자를 지닌 알킬이고, 알킬은 1-6탄소원자를 지닌 알킬렌이고, Ac는 1-8탄소원자를 지닌 알칸오일 또는 7-11 탄소원자를 지닌 아로일이다.
  2. 제1항에 있어서,,=CH-CO 또는 =CH-CHR8-이고, R5는 A, F, Cl, Br, I, OH,OA, OAc, NO2, NH2, AcNH, HOOC 및/또는 AOOC가 하나 또는 둘 치환되어 있거나/있지않은 1H-4-피리돈-1-일, 1H-4-피리다진온-1-일, 1H-4-피리미딘온-1-일, 1H-2-퀴놀론-1-일, 2H-1-이소퀴놀론-일, 2H-1-프탈라진온-2-일, 3H-4-퀴나졸린-3-일기(이들 치환기는 완전히 또는 부분적으로 수소화 될 수도 있다)이고/이거나 R7은 피리딜, 피리다진일, 피리미딘일 또는 피라진일인 경우 X-Y는 또한 =CR4-CR3R8이고,R5가 전체적 또는 부분적으로 수소화되지 않은 경우 X-Y는 또한 =CH-CR8(OA)-인 경우인 화합물.
  3. a) 2,2-디메틸-4-(1H-2-피리돈-1-일)-6-시아노-크로만-3-올, b) 2,2-디메틸-4-(1H-2-피리돈-1-일)-6-시아노-2H-크로멘, c) 2,2-디메틸-4-(6-히드록시-3-피리다진일옥시)-6-시아노-3-크로만올.
  4. 일반식(Ⅰ)의 크로만 유도체를 제조하는 방법에 있어서, X-Y가 =CH4-CR8R8- 또는 =CH-CHR8인 일반식(Ⅰ)의 화합물을 제조하기 위해서 다음 일반식(Ⅱa)의 3,4-에폭시크로만 또는 일반식(Ⅱb)의 크로만 유도체를 일반식(Ⅲ) 화합물 또는 그의 반응성 유도체와 반응시키고/시키거나, X-Y가 =CH-CR8(OH)-인 일반식(Ⅰ)의 화합물을 탈수하거나 알킬화시키고/시키거나 X-Y가 =C=CR8-인 일반식(Ⅰ)인 화합물을 에폭사이드화 시키고/시키거나, X-Y가 =C-CH인 일반식(Ⅰ)의 화합물을 X-Y가 =CH-CO-인 일반식(Ⅰ)의 화합물로 산촉매를 사용하여 이성질체화 시키고/시키거나, 일반식(Ⅰ)의 R3,R5,R6및/또는 R7기 중 하나 또는 그 이상을 다른 R3,R5,R6및/또는 R7기로 전환시키고/시키거나, 일반식(Ⅰ)의 염기 화합물을 산처리에 의해 그의 산부가염으로 전환시킴을 특징으로 하는 일반식(Ⅰ)의 크로만 유도체의 제조방법.
    상기 식에서 E는 cl, Br, I 또는 반응성 에스테르화 OH그룹이고, R1, R2, R5, R6, R7및 R8은 일반식(Ⅰ)에서 정의한 바와 같다.
  5. 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용되는 염을 적어도 하나의 고형아 액형 또는 반고형 부형제 또는 보조제와 함께, 필요에 따라 하나이상의 다른 활성화합물과 배합하여 적합한 투여 형태로 제조하는 것을 특징으로 하는 약학적 제제의 제조방법.
  6. 적어도 하나의 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용되는 염을 함유함을 특징으로 하는 약학적 제제.
  7. 약품의 제조를 위한 일반식(Ⅰ) 화합물의 용도.
  8. 탈모증 치료용 약품의 제조를 위한 일반식(Ⅰ) 화합물의 용도.
  9. 질병을 치료하는데 있어서의 일반식(Ⅰ) 화합물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890008330A 1988-06-16 1989-06-16 크로만 유도체 KR910000711A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE3820506A DE3820506A1 (de) 1988-06-16 1988-06-16 -n-heterocyclisch substituierte chromanderivate und ihre verwendung als arzneimittel
DEP3820506.8 1988-06-16
DE3835011A DE3835011A1 (de) 1988-10-14 1988-10-14 Chromanderivate
DEP3835011.4 1988-10-14

Publications (1)

Publication Number Publication Date
KR910000711A true KR910000711A (ko) 1991-01-30

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ID=25869185

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Application Number Title Priority Date Filing Date
KR1019890008330A KR910000711A (ko) 1988-06-16 1989-06-16 크로만 유도체

Country Status (11)

Country Link
EP (1) EP0346724A1 (ko)
JP (1) JPH0240375A (ko)
KR (1) KR910000711A (ko)
AU (1) AU626549B2 (ko)
DK (1) DK296789A (ko)
FI (1) FI92824C (ko)
HU (1) HUT56096A (ko)
IL (1) IL90613A0 (ko)
NO (1) NO174391C (ko)
NZ (1) NZ229540A (ko)
PT (1) PT90864B (ko)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3835011A1 (de) * 1988-10-14 1990-04-19 Merck Patent Gmbh Chromanderivate
FR2621587B1 (fr) * 1987-10-12 1990-02-09 Sanofi Sa Derives du dimethyl-2,2 chromene, procede pour leur preparation et composition pharmaceutiques les contenant
AU628331B2 (en) * 1988-05-06 1992-09-17 Merck Patent Gesellschaft Mit Beschrankter Haftung Chroman derivatives
DE3918041A1 (de) * 1989-06-02 1990-12-06 Merck Patent Gmbh Chromanderivate
GB8924376D0 (en) * 1989-10-30 1989-12-20 Beecham Group Plc Novel compounds
EP0430621A3 (en) * 1989-11-29 1992-03-04 Beecham Group P.L.C. Process for the preparation of chiral 3,4-epoxy benzopyrans
JP2575226B2 (ja) * 1990-05-11 1997-01-22 吉富製薬株式会社 光学活性な３，４−ジヒドロ−３，４−エポキシ−２ｈ−１ベンゾピラン化合物の製造法およびその合成中間体
TW257762B (ko) * 1991-06-14 1995-09-21 Nippon Chemicals Pharmaceutical Co Ltd
EP0623129A1 (en) * 1992-11-25 1994-11-09 Novartis AG 2,2-dialkyl- and 2,2-dialkyl-3,4-dihydro-3-hydroxy-2h-1-benzopyr ans, their use as pharmaceuticals
WO1994012493A1 (en) * 1992-11-25 1994-06-09 Sandoz, Ltd. 2,2-dialkyl- and 2,2-dialkyl-3,4-dihydro-3-hydroxy-2h-1-benzopyr ans, their use as pharmaceuticals
IL108841A0 (en) * 1993-03-10 1994-06-24 Pfizer Res & Dev Benzopyrans
GB9316111D0 (en) * 1993-08-04 1993-09-22 Pfizer Ltd Benzopyrans
US5574049A (en) * 1994-07-22 1996-11-12 Sandoz Ltd. 2,2-dialkyl- and 2,2-dialkyl-3,4-dihydro-3-hydroxy-2H-1-benzopyrans
JP2007000772A (ja) * 2005-06-23 2007-01-11 Casio Electronics Co Ltd 二重マイクロカプセル、その製造方法及びマイクロカプセルの表面処理方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3274350D1 (en) * 1981-09-25 1987-01-08 Beecham Group Plc Pharmaceutically active benzopyran compounds
EP0107423B1 (en) * 1982-10-19 1986-07-23 Beecham Group Plc Novel chromans and chromenes
PT84806B (pt) * 1986-05-03 1989-12-29 Beecham Group Plc Processo para a preparacao de benzopiranos
DE3726261A1 (de) * 1986-12-23 1988-07-07 Merck Patent Gmbh Chromanderivate
FR2615191B1 (fr) * 1987-05-16 1991-01-11 Sandoz Sa Nouveaux benzo(b)pyrannes et pyrannopyridines, leur preparation et leur utilisation comme medicaments
FR2621587B1 (fr) * 1987-10-12 1990-02-09 Sanofi Sa Derives du dimethyl-2,2 chromene, procede pour leur preparation et composition pharmaceutiques les contenant
AU628331B2 (en) * 1988-05-06 1992-09-17 Merck Patent Gesellschaft Mit Beschrankter Haftung Chroman derivatives

Also Published As

Publication number Publication date
DK296789A (da) 1989-12-17
NO174391B (no) 1994-01-17
AU626549B2 (en) 1992-08-06
PT90864A (pt) 1989-12-29
NO892494D0 (no) 1989-06-15
FI92824C (fi) 1995-01-10
FI892948A (fi) 1989-12-17
NO174391C (no) 1994-04-27
IL90613A0 (en) 1990-01-18
JPH0240375A (ja) 1990-02-09
HUT56096A (en) 1991-07-29
FI892948A0 (fi) 1989-06-15
PT90864B (pt) 1994-11-30
DK296789D0 (da) 1989-06-15
AU3644089A (en) 1989-12-21
NO892494L (no) 1989-12-18
FI92824B (fi) 1994-09-30
NZ229540A (en) 1991-03-26
EP0346724A1 (de) 1989-12-20

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