KR960010681A - 17-데옥시코르티코스테로이드-21-(o)- 카복실산 에스테르, 이의 제조방법 및 이를 함유하는 약제 - Google Patents

17-데옥시코르티코스테로이드-21-(o)- 카복실산 에스테르, 이의 제조방법 및 이를 함유하는 약제 Download PDF

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KR960010681A
KR960010681A KR1019950030850A KR19950030850A KR960010681A KR 960010681 A KR960010681 A KR 960010681A KR 1019950030850 A KR1019950030850 A KR 1019950030850A KR 19950030850 A KR19950030850 A KR 19950030850A KR 960010681 A KR960010681 A KR 960010681A
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methyl
hydrogen
carboxylic acid
formula
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KR100406627B1 (ko
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슈타체 울리히
알페르만 한스-게오르크
본 만프레트
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로제르트, 루츠
훽스트 아크티엔게젤샤프트
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J17/00Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J33/00Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

본 발명은 다음 일반식(Ⅰ)의 17-데옥시코르티코스테로이드-21-[0]-카복실산 에스테르, 이의 제조방법 및 이를 함유한느 약제에 관한 것이다.
상기 식에서, A,Y,Z,R(1)및 R(2)는 명세서에서 정의한 바와 같다.
일반식(Ⅰ)의 화합물은 매우 강력한 국부 및 국소 소염 작용을 나타내며, 소염 효능의국부/전신 비가 매우우수하며, 종종 이 비는, 구조적으로 관련된, 21-에스테르 잔기에 어떠한 아릴 또는 헤트아릴 그룹도 수반하지 않는 코르티코이드 21-에스테르 또는 에스테르화되지 않은, 즉 유리21-하이드록실 그룹을 포함하는 유사한 17-뎅고시크르티코이드의 비에 의해 매우 우수하다.

Description

17-데옥시코르티코스테로이드-21-[0]-카복실산 에스테르, 이의 제조방법 및 이를 함유하는 약제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 일반식 (Ⅰ)의 17-데옥시크로티코이드-21-카복실산 에스테르.
    상기 식에서, A는 임의의 입체 배열 상태로 존재하는 CHOH 및 CHCl, CH2, C=O 또는 9(11) 이중결합이고, Y는 수소, 불소 또는 염소이며, Z는 수소, 불소 또는 메틸이고, R(1)은 임의로 치환되거나 융합된 아릴 또는 헤트아릴이거나, 포화되거나, C2에서 1회 불포화되거나, C3에서 1회 이상 불포화되거나 또는 추가의 알킬그룹에 의해 환식으로 측쇄화되거나 헤테로 원자 O, S 또는 N에 의해 치환되거나 삽입된 [(C1-C4)-알킬][여기서, 1, 2위치는 포화되거나 불포화된(1,2-이중결합) 상태로 존재한다]이고, R(2)는 수소, α-메틸 또는 β-메틸이다.
  2. 제1항에 있어서, R(1)이 제1항에서 정의한 바와 동일하고, A가(β배열 상태로 존재하는)CHOH이고, Y가 F이며, Z가 수소이고, R(2)가 α-메틸인 17-데옥시코르티코이드-21-카복실산 에스테르.
  3. (a)일반식 (Ⅱ)의 화합물을 (a1) 일반식(Ⅲ)의 활성화 카복실산, 바람직하게는 할라이드 또는 무수물 또는 아졸리드와 반응시키거나 또는 (a2)탈수제 (DCCI등)의 존재하에 일반식(Ⅲ)의 카복실산 자체와 반응시키거나, (b)일반식(Ⅱ)의 화합물을 일반식 (Ⅲ)의 카복실산의 염, 바람직하게는 K또는 Na염 또는 트리알킬암모늄 염과 반응시켜 제1항에ㅣ서 청구한 일반식(Ⅰ)의 화합물을 제조하는 방법.
    상기 식에서, A는임의의 입체 배열 상태로 존재하는 CHOH 및 CHCl, CH2, C=O 또는 9(11) 이중결합이고, Y는 수소, 불소 또는 염소이며, Z는 수소, 불소 또는 메틸이고, R(1)은 임의로 치환되거나 융합된 아릴 또는 헤트아릴이거나, C2에서 1회 포화되거나,불포화되거나, C3에서 1회 이상 불포화되거나 또는 추가의 알킬그룹에 의해 환식으로 측쇄화되거나 헤테로원자 O, S또는 N에 의해 치환되거나 삽입된 [(C1-V4)-알킬][여기서, 1,2위치는 포화되거나 불포화되거나 불포화된 (1,2-이중결합) 상태로 존재한다.]이고, R(2)는 수소, α-메틸 또는 β-메틸이며, R(4)는 방법 (a)에서는 OH이고, 방법 (b)에서는 Br, I또는 설폰산 아릴 에스테르 그룹 또는 설폰산 알킬 에스테르 그룹이며, R(5)는 방법(a1)에서는 C1, Br, -O[-CO-[(C1-C4)알킬]-R(1)]1-,-OC(O)CF3또는 다른 활성 산 라디칼이고,방법(a2)에서는 OH이며, 방법(b)에서는 -[O-Me+](여기서, Me+는 바람직하게는 알칼리 금속염 또는 트리알킬암모늄 염의 양이온이다)이다.
  4. 제1항 에서 청구한 일반식(Ⅰ)의 화합물을 유효량 함유하는 약재.
  5. 약제학적으로 통상적인 첨가제와 배합된 제1항에서 청구한 일반식 (Ⅰ)의 화합물 유효량을 손상된 피부부위에 처리하여 피부 질환을 치료하는 방법.
  6. 피부 질환 치료용 약제를 제조하기 위한, 제 1항에서 청구한 일반식 (Ⅰ)의 화합물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950030850A 1994-09-20 1995-09-20 17-데옥시코르티코스테로이드-21-[0]-카복실산에스테르,이의제조방법및이를함유하는약제 Expired - Fee Related KR100406627B1 (ko)

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DEP4433374.9 1994-09-20
DE4433374A DE4433374A1 (de) 1994-09-20 1994-09-20 17-Desoxi-corticosteroid-21-/O/-Carbonsäure- ester, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel

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DE (2) DE4433374A1 (ko)
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US12209988B2 (en) 2019-05-24 2025-01-28 Electronics And Telecommunications Research Institute Sensor and method of manufacturing the same

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US12209988B2 (en) 2019-05-24 2025-01-28 Electronics And Telecommunications Research Institute Sensor and method of manufacturing the same

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SI9500295B (en) 2001-12-31
CZ242595A3 (en) 1996-04-17
JP3902255B2 (ja) 2007-04-04
NZ280038A (en) 1997-03-24
ATE188480T1 (de) 2000-01-15
DE4433374A1 (de) 1996-03-21
DE59507565D1 (de) 2000-02-10
DK0708111T3 (da) 2000-06-13
PT708111E (pt) 2000-04-28
CN1124250A (zh) 1996-06-12
JPH0899992A (ja) 1996-04-16
FI954394L (fi) 1996-03-21
HUT72969A (en) 1996-06-28
CA2158610C (en) 2007-07-17
EP0708111A1 (de) 1996-04-24
HU217438B (hu) 2000-01-28
EP0708111B1 (de) 2000-01-05
RU2161624C2 (ru) 2001-01-10
HU9502735D0 (en) 1995-11-28
AU695710B2 (en) 1998-08-20
CA2158610A1 (en) 1996-03-21
PL186071B1 (pl) 2003-10-31
FI114708B (fi) 2004-12-15
ZA957877B (en) 1996-04-03
AU3172895A (en) 1996-04-04
PL310544A1 (en) 1996-04-01
CN1056151C (zh) 2000-09-06
GR3032688T3 (en) 2000-06-30
CZ288297B6 (en) 2001-05-16
NO305210B1 (no) 1999-04-19
KR100406627B1 (ko) 2004-02-19
IL115331A0 (en) 1995-12-31
ES2140596T3 (es) 2000-03-01
FI954394A0 (fi) 1995-09-18
SI9500295A (en) 1996-04-30
US5824670A (en) 1998-10-20
NO953695D0 (no) 1995-09-19
NO953695L (no) 1996-03-21
TW424094B (en) 2001-03-01
IL115331A (en) 2002-07-25

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