KR880002870A - 신규 키산틴 유도체 - Google Patents

신규 키산틴 유도체 Download PDF

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Publication number
KR880002870A
KR880002870A KR870009453A KR870009453A KR880002870A KR 880002870 A KR880002870 A KR 880002870A KR 870009453 A KR870009453 A KR 870009453A KR 870009453 A KR870009453 A KR 870009453A KR 880002870 A KR880002870 A KR 880002870A
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KR
South Korea
Prior art keywords
hydrogen
compound
hydroxy
methoxy
alkyl
Prior art date
Application number
KR870009453A
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English (en)
Inventor
엘·키스 졸탄
모레이 존
Original Assignee
예안 클라메르 한스 루돌프 하우스
산도즈 리미티드
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB868620825A external-priority patent/GB8620825D0/en
Priority claimed from GB878702129A external-priority patent/GB8702129D0/en
Priority claimed from GB878703435A external-priority patent/GB8703435D0/en
Application filed by 예안 클라메르 한스 루돌프 하우스, 산도즈 리미티드 filed Critical 예안 클라메르 한스 루돌프 하우스
Publication of KR880002870A publication Critical patent/KR880002870A/ko

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C07D473/12—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1, 3, and 7, e.g. caffeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline

Abstract

내용 없음

Description

신규 키산틴 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(Ⅰ)의 화합물 또는 이것의 생리학적 - 가수성 및 - 허용성 에스테르 :
    상기 식에서, R1은 C1- C4알킬, C3-4알케닐 또는 (C3-5시클로알킬)-메틸이며, R2은 C1- C4알킬 [히드록시-또는 (C1-4알콕시) - 치환 C1-3알킬]-메틸, (C3-5시클로알킬)-메틸 또는 하기식(A)의 그룹이며,
    상기 식에서 X는 -CH2-또는 -O-이다. R3및 R4는 각각 수소, 히드록시메틸, 메톡시메틸 또는 N, N-디메틸카르밤오일옥시메틸이며, R5은 히드록시 또는 메톡시이며, R6는 수소, 히드록시, 메톡시 또는 할로겐이며, 및 R7은 2--또는 3-위치에 존재하며 히드록시, 메톡시 또는 할로겐, 또는 R5가 3,4-미텔렌디옥시, 또는 R6가 2, 3-메틸렌디옥시와 함께 존재한다.
  2. 제 1 항에 있어서, 상기 R3는 수소, R5는 CH3O-이고, R6는 수소이고 R7은 3-위치에 존재하는 CH3O-이고, a) R1이 CH3일 때, R4는 수소이고, R2는 CH3-, CH3O-(CH2)2-, HO-(CH2)2-,또는 CH3-CO-O-(CH2)2- ; 또는 b) R2이 CH3=CH-CH2- 일 때, R4는 수소이고, R2는 CH3O-(CH2)2- 또는또는 c) R1이일 때, R4는 수소이고, R2는 CH3O-(CH2)2- 또는; 또는 d) R1이 CH3- 일 때, R4는 HOCH2- R2는 CH3-HO-O-(CH2)2- 또는; 또는 e) R1이 CH3-일 때, R4는 CH3O-CH2이고 R2은 HO-(CH2)2- ; 또는 f) R1이 CH3-일 때, R2는 CH3O-(CH2)2-이고, R4는 CH3-CO-O-CH2- ; 또는 (CH3)2-CO-O-CH2- 또는 g) R1이 CH2=CH-CH2- 일 때, R2는이고, R4는 CH3-CO-O-CH2- 또는 HO-(CH2)2- ; 또는 상기에서 R3는 수소이고, R5는 CH3O-이고, R6는 수소이며, R7는 3위치에 존재하는 CH3O이며, h) R1이 CH3-일 때 R2는 CH3O-(CH2)2-이고, R4는 수소인 것을 특징으로 하는 화합물 또는 에스테르.
  3. 제 1 항에 있어서 상기 R1은 CH3이고, R2은 CH3O-(CH2)2-, R3는 수소이고, R2은 HO-(CH2)2- 이고, R5는 CH3O-이고, R6는 수소이며 R7는 3-위치에 존재하는 CH3O-인것을 특징으로 하는 화합물.
  4. 제 1 항에 있어서, 상기 R1은 CH3이고, R2은 CH3O-(CH2)2-, R3는 수소이고, R4은 CH2O-이고, R5는 CH3O-이고, R6는 수소이며 R7는 3-위치에 존재하는 CH3O-인것을 특징으로 하는 화합물.
  5. 제 1 항에 있어서, 상기 -C(R3)R4-는 (R)-CH(CH3OH)-, (R)-CH(CH3OCH3)- 또는 (R) - CH[CH2-O-CO-N-(CH3)2]- 또는 생리학적-가수성 및 -허용성 에스테르인 것을 특징으로 하는 화합물.
  6. 제 3 항에 있어서, 상기 -C(R3)R4-는 (R)-CH(CH3OH)-인것을 특징으로 하는 화합물.
  7. 제 4 항에 있어서, 상기 -C(R3)R4-는 (R)-CH(CH3OH)-인것을 특징으로 하는 화합물.
  8. 제 1 항에서 청구한 화합물 또느 에스테르에 약리학적 허용성 회석제 또는 담체(carrier)를 함께 포함하는 것을 특징으로 하는 약학적 조성물,
  9. 치료(처방)을 필요로 하는 피검체에서의 폐쇄성 및 염증성 기도(기관)질병의 치료 또는 호산구증다증의 축척 또는 활성의 억제를 위해서 또는 아토피(atopy, 가족성과민증세)의 치료를 위한 방법으로서, 상기 방법은 제 1 항에서 정의한 식(Ⅰ)의 화합물 도는 이것의 생리학적- 가수성 및 허용성 에스테르를 상기 피검체에 효과적인 함량의 투여를 포함하는 것을 특징으로 하는 방법,
  10. 제 9 항에 있어서, 천식을 치료하는 것을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870009453A 1986-08-28 1987-08-27 신규 키산틴 유도체 KR880002870A (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB868620825A GB8620825D0 (en) 1986-08-28 1986-08-28 Organic compounds
GB878702129A GB8702129D0 (en) 1987-01-30 1987-01-30 Organic compounds
GB8703435 1987-02-13
GB8702129 1987-02-13
GB878703435A GB8703435D0 (en) 1987-02-13 1987-02-13 Organic compounds
GB8620825 1987-02-13

Publications (1)

Publication Number Publication Date
KR880002870A true KR880002870A (ko) 1988-05-12

Family

ID=27263135

Family Applications (1)

Application Number Title Priority Date Filing Date
KR870009453A KR880002870A (ko) 1986-08-28 1987-08-27 신규 키산틴 유도체

Country Status (17)

Country Link
EP (1) EP0258191B1 (ko)
JP (1) JPH0631236B2 (ko)
KR (1) KR880002870A (ko)
AU (1) AU600021B2 (ko)
CA (1) CA1289954C (ko)
DE (1) DE3779374D1 (ko)
DK (1) DK169337B1 (ko)
ES (1) ES2033922T3 (ko)
FI (1) FI87356C (ko)
GR (1) GR3004747T3 (ko)
HU (1) HU199840B (ko)
IE (1) IE60512B1 (ko)
IL (1) IL83659A (ko)
MY (1) MY101830A (ko)
NZ (1) NZ221571A (ko)
PH (1) PH24761A (ko)
PT (1) PT85594B (ko)

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GB9210839D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Plc Novel compounds
GB9312853D0 (en) 1993-06-22 1993-08-04 Euro Celtique Sa Chemical compounds
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EP0799040B1 (en) 1994-12-13 2003-08-20 Euroceltique S.A. Trisubstituted thioxanthines
JPH10508032A (ja) 1994-12-13 1998-08-04 ユーロ−セルティーク，エス．エイ． アリールチオキサンチン類
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US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CA2688161C (en) 2007-06-04 2020-10-20 Kunwar Shailubhai Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
ES2522968T3 (es) 2008-06-04 2014-11-19 Synergy Pharmaceuticals Inc. Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
CN108676076A (zh) 2011-03-01 2018-10-19 辛纳吉制药公司 制备鸟苷酸环化酶c激动剂的方法
WO2014131024A2 (en) 2013-02-25 2014-08-28 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
US9486494B2 (en) 2013-03-15 2016-11-08 Synergy Pharmaceuticals, Inc. Compositions useful for the treatment of gastrointestinal disorders
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法
MX2016001714A (es) 2013-08-09 2016-10-03 Ardelyx Inc Compuestos y metodos para inhibir el transporte de fosfato.
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Also Published As

Publication number Publication date
IE60512B1 (en) 1994-07-27
FI87356B (fi) 1992-09-15
NZ221571A (en) 1990-11-27
GR3004747T3 (ko) 1993-04-28
ES2033922T3 (es) 1993-04-01
DK448787D0 (da) 1987-08-27
HUT47111A (en) 1989-01-30
DK448787A (da) 1988-02-29
IL83659A0 (en) 1988-01-31
FI873704A0 (fi) 1987-08-26
DE3779374D1 (en) 1992-07-02
DK169337B1 (da) 1994-10-10
AU600021B2 (en) 1990-08-02
IL83659A (en) 1991-06-10
IE872296L (en) 1988-02-28
EP0258191B1 (en) 1992-05-27
PH24761A (en) 1990-10-01
MY101830A (en) 1992-01-31
CA1289954C (en) 1991-10-01
PT85594B (pt) 1990-05-31
PT85594A (en) 1987-09-01
FI873704A (fi) 1988-02-29
JPS6363679A (ja) 1988-03-22
FI87356C (fi) 1992-12-28
EP0258191A1 (en) 1988-03-02
HU199840B (en) 1990-03-28
AU7744587A (en) 1988-03-03
JPH0631236B2 (ja) 1994-04-27

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