KR890000458A - 티오펜설폰아미드 녹내장 치료제 - Google Patents
티오펜설폰아미드 녹내장 치료제 Download PDFInfo
- Publication number
- 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
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- thiophene
- hydrogen
- alkyl
- glaucoma
- Prior art date
Links
Classifications
-
- 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
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
내용 없음
Claims (11)
- 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.
- 제1항에 있어서, Ar이 벤젠인 화합물.
- 제2항에 있어서, R2가 수소 또는 C1-5알킬인 화합물.
- 제3항에 있어서, 하기 일반식의 화합물.
- 제4항에 있어서, 하기 일반식의 화합물 또는 이의 안과학적으로 허용되는 염.
- 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.
- 제6항에 있어서, 5-(3-디메틸아미노메틸-4-하이드록시페닐설포닐)-티오펜-2-설폰아미드 또는 이의 안과학적으로 허용되는 염인 화합물.
- 하기 일반식의 화합물.상기식에서, R은 수소, 하이드록시, C1-3알콕시, C1-3알킬 또는 할로이고; n은 0.1 또는 2이고 : R2′는 C1-5하이드록시알킬이다.
- 제8항에 있어서, R이 하이드록시 또는 메톡시이고, n은 0또는 2이고, R2′은 1-하이드록시에틸인 화합물.
- 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.
- 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.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US07/059,084 US4847289A (en) | 1987-06-08 | 1987-06-08 | Thiophene sulfonamide antiglaucoma agents |
US059,084 | 1987-06-08 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR890000458A true KR890000458A (ko) | 1989-03-14 |
KR960005954B1 KR960005954B1 (ko) | 1996-05-06 |
Family
ID=22020751
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
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) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5378703A (en) * | 1990-04-09 | 1995-01-03 | Alcon Laboratories, Inc. | Sulfonamides useful as carbonic anhydrase inhibitors |
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 |
WO2006134341A1 (en) * | 2005-06-13 | 2006-12-21 | Merck Sharp & Dohme Limited | Therapeutic agents |
WO2007114338A1 (ja) | 2006-03-31 | 2007-10-11 | Takeda Pharmaceutical Company Limited | 酸分泌抑制薬 |
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 |
US20100256357A1 (en) * | 2006-08-09 | 2010-10-07 | Agouron Pharmaceuticals, Inc. | Heterocycles useful as inhibitors of carbonic anhydrase |
US8895588B2 (en) | 2009-03-26 | 2014-11-25 | Takeda Pharmaceutical Company Limited | Pyrazole compound |
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 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1459571A (en) * | 1974-09-12 | 1976-12-22 | Pfizer Ltd | Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus |
ZA813332B (en) * | 1980-06-21 | 1982-05-26 | Pfizer | Larvicides and isecticides |
US4416890A (en) * | 1981-07-13 | 1983-11-22 | Merck & Co., Inc. | Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure |
US4386098A (en) * | 1981-11-03 | 1983-05-31 | Merck & Co., Inc. | 6-Hydroxy-2-benzothiazolesulfonamide for the topical treatment of elevated intraocular pressure |
US4426388A (en) * | 1982-04-02 | 1984-01-17 | Merck & Co., Inc. | 5-Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure |
US4477466A (en) * | 1983-05-23 | 1984-10-16 | Merck & Co., Inc. | Acyloxy derivatives of [phenylsulfonyl(or sulfinyl)]thiophenesulfonamide for the topical treatment of elevated intraocular pressure |
US4542152A (en) * | 1983-05-23 | 1985-09-17 | Merck & Co., Inc. | 5-[Phenylsulfonyl(or sulfinyl)]thiophene-2-sulfonamides for the topical treatment of elevated intraocular pressure |
ES8600752A1 (es) * | 1983-06-20 | 1985-10-16 | Merck & Co Inc | Un procedimiento para la preparacion de nuevos derivados de tiosulfonamida. |
US4486444A (en) * | 1983-06-20 | 1984-12-04 | Merck & Co., Inc. | (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof for the topical treatment of elevated intraocular pressure |
US4585787A (en) * | 1983-06-20 | 1986-04-29 | Merck & Co., Inc. | 5-[2(Or 3)-hydroxyphenylsulfonyl]thiophene-2-sulfonamides for the topical treatment of elevated intraocular pressure |
US4668697A (en) * | 1983-10-31 | 1987-05-26 | Merck & Co., Inc. | Elevated intraocular pressure lowering benzo-[b]-thiophene-2-sulfonamide derivatives, compositions, and method of use therefor |
EP0182691B1 (en) * | 1984-11-02 | 1990-07-04 | Merck & Co. Inc. | Substituted thiophene-2-sulfonamides and their preparation |
US4677115A (en) * | 1984-12-12 | 1987-06-30 | Merck & Co., Inc. | Antiglaucoma thieno-thiopyran and thieno-thiepin sulfonamide derivatives, compositions, and method of use thereof |
US4665090A (en) * | 1985-10-09 | 1987-05-12 | Merck & Co., Inc. | Substituted thiophene-2-sulfonamide antiglaucoma agents |
-
1987
- 1987-06-08 US US07/059,084 patent/US4847289A/en not_active Expired - Fee Related
-
1988
- 1988-05-30 IL IL8655088A patent/IL86550A/en not_active IP Right Cessation
- 1988-05-30 NZ NZ224830A patent/NZ224830A/en unknown
- 1988-05-31 PT PT87620A patent/PT87620B/pt not_active IP Right Cessation
- 1988-06-06 EP EP88305178A patent/EP0295049B1/en not_active Expired - Lifetime
- 1988-06-06 DE DE8888305178T patent/DE3865368D1/de not_active Expired - Fee Related
- 1988-06-06 AT AT88305178T patent/ATE68182T1/de not_active IP Right Cessation
- 1988-06-06 ES ES198888305178T patent/ES2037829T3/es not_active Expired - Lifetime
- 1988-06-07 AU AU17453/88A patent/AU606165B2/en not_active Ceased
- 1988-06-07 DK DK308588A patent/DK308588A/da not_active Application Discontinuation
- 1988-06-07 CA CA000568886A patent/CA1328261C/en not_active Expired - Fee Related
- 1988-06-07 ZA ZA884039A patent/ZA884039B/xx unknown
- 1988-06-07 KR KR1019880006786A patent/KR960005954B1/ko not_active IP Right Cessation
- 1988-06-07 IE IE169188A patent/IE62107B1/en not_active IP Right Cessation
- 1988-06-08 JP JP63139590A patent/JPH0637488B2/ja not_active Expired - Lifetime
-
1991
- 1991-10-22 GR GR91401588T patent/GR3002957T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
EP0295049B1 (en) | 1991-10-09 |
GR3002957T3 (en) | 1993-01-25 |
DE3865368D1 (de) | 1991-11-14 |
IL86550A (en) | 1995-01-24 |
IE881691L (en) | 1988-12-08 |
AU1745388A (en) | 1988-12-08 |
IL86550A0 (en) | 1988-11-15 |
ZA884039B (en) | 1989-01-25 |
ES2037829T3 (es) | 1993-07-01 |
DK308588A (da) | 1988-12-09 |
PT87620A (pt) | 1988-06-01 |
JPS6456672A (en) | 1989-03-03 |
EP0295049A3 (en) | 1989-03-08 |
NZ224830A (en) | 1990-04-26 |
JPH0637488B2 (ja) | 1994-05-18 |
ATE68182T1 (de) | 1991-10-15 |
US4847289A (en) | 1989-07-11 |
IE62107B1 (en) | 1994-12-14 |
AU606165B2 (en) | 1991-01-31 |
EP0295049A2 (en) | 1988-12-14 |
DK308588D0 (da) | 1988-06-07 |
CA1328261C (en) | 1994-04-05 |
KR960005954B1 (ko) | 1996-05-06 |
PT87620B (pt) | 1992-09-30 |
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