KR890000458A - 티오펜설폰아미드 녹내장 치료제 - Google Patents

티오펜설폰아미드 녹내장 치료제 Download PDF

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KR890000458A
KR890000458A KR1019880006786A KR880006786A KR890000458A KR 890000458 A KR890000458 A KR 890000458A KR 1019880006786 A KR1019880006786 A KR 1019880006786A KR 880006786 A KR880006786 A KR 880006786A KR 890000458 A KR890000458 A KR 890000458A
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South Korea
Prior art keywords
compound
thiophene
hydrogen
alkyl
glaucoma
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KR1019880006786A
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English (en)
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KR960005954B1 (ko
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제이ㆍ발드원 존
엠ㆍ하베커 찰스
엘ㆍ그래함 사무엘
할크젠코 와실
디ㆍ하트만 조오지
샴 하비
에스ㆍ폰티셀로 제랄드
엘ㆍ쉐파드 케네드
Original Assignee
제임스 에프ㆍ노오턴
머크 앤드 캄파니, 인코포레이티드
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

티오펜설폰아미드 녹내장 치료제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
내용 없음

Claims (11)

  1. 하기 일반식의 화합물 또는 이의 안과학적으로 허용되는 염.
    상기식에서, Ar은 벤젠, 티오펜 및 푸란 중에서 선택되는 방향족 부분이고; R은 수소, 하이드록시, C1-3알콕시, C1-3알킬 또는 할로이며; R1은 수소, 할로 또는 -X-NR3R4(여기에서 X는 C1-5알킬렌이다)이고; R3는 수소 또는 C1-5알킬이며; R4는 a) 수소 b) i)하이드록시, ii)C1-3알콕시카보닐, iii)카복시, iv)5또는 6-원 헤테로 사이클 또는, V)C3-6사이클로알킬 치환되거나 비치환된 C1-5알킬이거나; 또는 R3및 R4가 저급 알킬인 경우, 이들은 직접 또는 헤테로 원자를 통하여 이들이 결합되어 있는 질소원자와 함께 결합되어 5또는 6-원 포화 헤테로 사이클을 형성할 수 있고; R2는 수소이거나, 또는 -OH 또는 -NR5R6(여기에서 R5및 R6는 수소 및 직쇄 또는 측쇄 C1-5알킬중에서 독립적으로 선택되거나, 또는 저급 알킬인 경우, N5및 R6는 서로 결합되어 5- 또는 6-헤테로 사이클을 형성할 수 있다)로 치환되거나 비치환된 직쇄 또는 측쇄 C1-5알킬이고; Y는 a)결합, b)X 또는 c)X-NR5R6이고; 단, R1, R2및 Y중 적어도 하나는 염기성 치환체 -NR3R4또는 -NR5R6를 포함하고 티오펜의 3위치는 비치환된다.
  2. 제1항에 있어서, Ar이 벤젠인 화합물.
  3. 제2항에 있어서, R2가 수소 또는 C1-5알킬인 화합물.
  4. 제3항에 있어서, 하기 일반식의 화합물.
  5. 제4항에 있어서, 하기 일반식의 화합물 또는 이의 안과학적으로 허용되는 염.
  6. 제5항에 있어서, 5-(3-디에틸아미노 메틸-4-하이드록시페닐설포닐)티오펜-2-설포아미드; 5-[3-(2-메틸프로필)아미노메틸페닐설포닐]티오펜-2-설폰아미드; 5-[에틸아미노-3-(4-하이드록시페닐)프로필설포닐]티오펜-2-설폰아미드; 5-[3-(3-디메틸아미노메틸-4-하이드록시페닐)프로필설포닐]티오펜-2-설폰아미드; 또는 5-(3-디메틸아미노메틸-4-하이드록시페닐설포닐)티오펜-2-설폰아미드; 또는 이의 안과학적으로 허용되는 염인 화합물.
  7. 제6항에 있어서, 5-(3-디메틸아미노메틸-4-하이드록시페닐설포닐)-티오펜-2-설폰아미드 또는 이의 안과학적으로 허용되는 염인 화합물.
  8. 하기 일반식의 화합물.
    상기식에서, R은 수소, 하이드록시, C1-3알콕시, C1-3알킬 또는 할로이고; n은 0.1 또는 2이고 : R2′는 C1-5하이드록시알킬이다.
  9. 제8항에 있어서, R이 하이드록시 또는 메톡시이고, n은 0또는 2이고, R2′은 1-하이드록시에틸인 화합물.
  10. 안과학적으로 허용되는 담체 및 제1항의 화합물의 안내압 저하 유효량 및/또는 녹내장 치료량을 함유함을 특징으로 하는, 상승된 안내압 및/또는 녹내장을 치료하기 위한 안과용 조성물.
  11. 제1항의 화합물의 안내압 저하 유호량 및/또는 녹내장 치료량을 상승된 안내압 및/또는 녹내장을 치료할 필요가 있는 환자에게 국부적으로 눈에 투여함을 특징으로 하여, 상승된 안내압 및/또는 녹내장을 치료하는 방법.
    ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880006786A 1987-06-08 1988-06-07 티오펜 설폰아미드 녹내장 치료제 KR960005954B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US059,084 1987-06-08
US07/059,084 US4847289A (en) 1987-06-08 1987-06-08 Thiophene sulfonamide antiglaucoma agents

Publications (2)

Publication Number Publication Date
KR890000458A true KR890000458A (ko) 1989-03-14
KR960005954B1 KR960005954B1 (ko) 1996-05-06

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KR1019880006786A KR960005954B1 (ko) 1987-06-08 1988-06-07 티오펜 설폰아미드 녹내장 치료제

Country Status (16)

Country Link
US (1) US4847289A (ko)
EP (1) EP0295049B1 (ko)
JP (1) JPH0637488B2 (ko)
KR (1) KR960005954B1 (ko)
AT (1) ATE68182T1 (ko)
AU (1) AU606165B2 (ko)
CA (1) CA1328261C (ko)
DE (1) DE3865368D1 (ko)
DK (1) DK308588A (ko)
ES (1) ES2037829T3 (ko)
GR (1) GR3002957T3 (ko)
IE (1) IE62107B1 (ko)
IL (1) IL86550A (ko)
NZ (1) NZ224830A (ko)
PT (1) PT87620B (ko)
ZA (1) ZA884039B (ko)

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US5153192A (en) * 1990-04-09 1992-10-06 Alcon Laboratories, Inc. Thiophene sulfonamides useful as carbonic anhydrase inhibitors
US5585377A (en) * 1990-04-09 1996-12-17 Alcon Laboratories, Inc. Sulfonamides useful as carbonic anhydrase inhibitors
US5932572A (en) * 1992-02-21 1999-08-03 Alcon Laboratories, Inc. Topical anti-glaucoma compositions
US5300499A (en) * 1992-09-02 1994-04-05 Allergan, Inc. 5-substituted 3-thiophene sulfonamides as antiglaucoma agents
US5629345A (en) * 1993-07-23 1997-05-13 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
US5555804A (en) * 1993-06-25 1996-09-17 Akiyama Printing Machine Manufacturing Company Ltd. Perfecting sheet rotary offset press
US5965620A (en) * 1993-07-23 1999-10-12 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
JP4776113B2 (ja) 2001-08-02 2011-09-21 三菱重工印刷紙工機械株式会社 枚葉両面多色刷り印刷機用印刷ユニットおよび枚葉両面多色刷り印刷機ならびに製造方法
EP1899294B1 (en) * 2005-06-13 2015-03-18 Merck Sharp & Dohme Limited Therapeutic agents
CA2647862A1 (en) 2006-03-31 2007-10-11 Takeda Pharmaceutical Company Limited Acid secretion inhibitor
LT5504B (lt) 2006-08-02 2008-06-25 Biotechnologijos Institutas Benzimidazo[1,2-c][1,2,3]tiadiazolo sulfonamidai - karboanhidrazių slopikliai ir tarpiniai junginiai jiems gauti
WO2008017932A2 (en) * 2006-08-09 2008-02-14 Pfizer Products Inc. Heterocycles useful as inhibitors of carbonic anhydrase
MA33214B1 (fr) 2009-03-26 2012-04-02 Takeda Pharmaceutical Compose pyrazole
US9801813B2 (en) 2013-10-17 2017-10-31 Sentiss Pharma Private Limited Preservative-free ophthalmic pharmaceutical formulation
GB201602934D0 (en) 2016-02-19 2016-04-06 Cancer Res Inst Royal Compounds
WO2021262878A1 (en) * 2020-06-24 2021-12-30 Oregon Health & Science University Novel molecule for modulation of innate immune responses controlled by sting protein

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Also Published As

Publication number Publication date
NZ224830A (en) 1990-04-26
AU606165B2 (en) 1991-01-31
IL86550A0 (en) 1988-11-15
US4847289A (en) 1989-07-11
JPH0637488B2 (ja) 1994-05-18
IE62107B1 (en) 1994-12-14
PT87620A (pt) 1988-06-01
IL86550A (en) 1995-01-24
DE3865368D1 (de) 1991-11-14
EP0295049A3 (en) 1989-03-08
KR960005954B1 (ko) 1996-05-06
DK308588D0 (da) 1988-06-07
GR3002957T3 (en) 1993-01-25
AU1745388A (en) 1988-12-08
ZA884039B (en) 1989-01-25
CA1328261C (en) 1994-04-05
ES2037829T3 (es) 1993-07-01
IE881691L (en) 1988-12-08
DK308588A (da) 1988-12-09
ATE68182T1 (de) 1991-10-15
JPS6456672A (en) 1989-03-03
EP0295049A2 (en) 1988-12-14
PT87620B (pt) 1992-09-30
EP0295049B1 (en) 1991-10-09

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