IL86822A - 6-alkyl-4-amino-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxides and antiglaucoma compositions containing them - Google Patents

6-alkyl-4-amino-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxides and antiglaucoma compositions containing them

Info

Publication number
IL86822A
IL86822A IL86822A IL8682288A IL86822A IL 86822 A IL86822 A IL 86822A IL 86822 A IL86822 A IL 86822A IL 8682288 A IL8682288 A IL 8682288A IL 86822 A IL86822 A IL 86822A
Authority
IL
Israel
Prior art keywords
thiopyran
dioxides
thieno
sulfonamide
dihydro
Prior art date
Application number
IL86822A
Other languages
English (en)
Other versions
IL86822A0 (en
Original Assignee
Merck & Co Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26747752&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL86822(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US07/067,326 external-priority patent/US4797413A/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of IL86822A0 publication Critical patent/IL86822A0/xx
Publication of IL86822A publication Critical patent/IL86822A/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D307/64—Sulfur atoms
    • 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
    • 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
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Non-Silver Salt Photosensitive Materials And Non-Silver Salt Photography (AREA)
  • Lubricants (AREA)
  • Photosensitive Polymer And Photoresist Processing (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heat Sensitive Colour Forming Recording (AREA)
  • Dental Preparations (AREA)
IL86822A 1987-06-26 1988-06-21 6-alkyl-4-amino-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxides and antiglaucoma compositions containing them IL86822A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/067,326 US4797413A (en) 1986-05-14 1987-06-26 Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
US07/208,314 US4863922A (en) 1984-12-12 1988-06-15 Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use

Publications (2)

Publication Number Publication Date
IL86822A0 IL86822A0 (en) 1988-11-30
IL86822A true IL86822A (en) 1992-01-15

Family

ID=26747752

Family Applications (1)

Application Number Title Priority Date Filing Date
IL86822A IL86822A (en) 1987-06-26 1988-06-21 6-alkyl-4-amino-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxides and antiglaucoma compositions containing them

Country Status (18)

Country Link
US (1) US4863922A (pt)
EP (1) EP0296879B1 (pt)
JP (1) JPH0631247B2 (pt)
AT (1) ATE86998T1 (pt)
AU (1) AU616664B2 (pt)
CA (2) CA1328262C (pt)
CY (1) CY1772A (pt)
DE (2) DE19575017I2 (pt)
DK (1) DK167684B1 (pt)
ES (1) ES2053738T4 (pt)
GR (1) GR3007407T3 (pt)
IE (1) IE62255B1 (pt)
IL (1) IL86822A (pt)
LU (1) LU88633I2 (pt)
NL (1) NL950006I2 (pt)
NZ (1) NZ225166A (pt)
PT (1) PT87832B (pt)
SG (1) SG24394G (pt)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
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CA1320487C (en) * 1987-08-03 1993-07-20 George D. Hartman Substituted thieno[2,3-.beta.]thiophene-2-sulfonamides as antiglaucoma agents
US5260453A (en) * 1988-09-23 1993-11-09 Ortho Pharmaceutical Corporation Substituted thienopyrans as antihypertensive agents
US4876271A (en) * 1988-12-20 1989-10-24 Merck & Co., Inc. Substituted thieno[3,2-b]thiophene-2-sulfonamides as topically active carbonic anhydrase inhibitors
US4929549A (en) * 1989-02-08 1990-05-29 Merck & Co., Inc. 5-carbamoylthieno[2,3-b]thiophene-2-sulfon-amides as topically active carbonic anhydrase inhibitors
US4946859A (en) * 1989-07-31 1990-08-07 Merck & Co., Inc. 4-(2-methyl-2-hydroxypropylamino)-5,6-dihydrothieno-[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide
US5120757A (en) * 1989-07-31 1992-06-09 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
CA2028496A1 (en) * 1989-10-31 1991-05-01 Tohru Nakao Thiophene compounds and their pharmaceutical uses
IE911192A1 (en) * 1990-04-12 1991-10-23 Merck & Co Inc Substituted aromatic sulfonamides as antiglaucoma agents
JP3031498B2 (ja) * 1990-04-12 2000-04-10 メルク エンド カムパニー インコーポレーテッド 抗緑内障剤としての置換芳香族スルホンアミド類
US5045561A (en) * 1990-04-12 1991-09-03 Merck & Co., Inc. Substituted furan sulfonamides as antiglaucoma agents
US5157129A (en) * 1990-04-18 1992-10-20 Merck & Co., Inc. Enantiospecific synthesis of s-(+)-5,6-dihydro-4-(r-amino)-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide
US5091409A (en) * 1990-05-17 1992-02-25 Merck & Co., Inc. 4-alkylamino-6-(C3-5 -hydrocarbyl)thieno[2,3-B]thiopyran-2-sulfonamide-7,7-dioxides
US5093332A (en) * 1990-10-01 1992-03-03 Merck & Co., Inc. Substituted thieno(2,3-b)(1,4)thiazine-6-sulfonamides as antiglaucoma agents
EP0480745A3 (en) * 1990-10-12 1992-07-29 Merck & Co. Inc. Substituted dihydrothieno-thiophene-2-sulfonamides and dioxides thereof
US5216020A (en) * 1990-10-12 1993-06-01 Merck & Co., Inc. Substituted 4,5-dihydrothieno(2,3-b)thiophene-2-sulfonamides and 6,6-dioxides thereof
SK282039B6 (sk) * 1991-04-17 2001-10-08 Merck & Co., Inc. Oftalmický prípravok na liečenie očnej hypertenzie obsahujúci kombináciu inhibítora karboanhydrázy a beta-adrenergného antagonistu
SG84487A1 (en) 1991-04-17 2001-11-20 Merck & Co Inc Ophthalmic compositions comprising combinations of a carbonic anhydrase inhibitor and a b-adrenergic antagonist
CA2080403A1 (en) * 1991-10-15 1993-04-16 John J. Baldwin Tricyclic thienothiopyrans
WO1993016701A2 (en) * 1992-02-21 1993-09-02 Alcon Laboratories, Inc. Topical antiglaucoma compositions comprising carbonic anhydrase inhibitors and beta-blockers
US5932572A (en) * 1992-02-21 1999-08-03 Alcon Laboratories, Inc. Topical anti-glaucoma compositions
ES2093980T3 (es) * 1992-08-28 1997-01-01 Zeneca Ltd Proceso de reduccion asimetrica, enzimatica, para producir derivados de 4h-tieno(2,3-6)tiopirano.
JP3279671B2 (ja) * 1992-09-28 2002-04-30 鐘淵化学工業株式会社 チエノチオピラン誘導体の製造方法
TW265343B (pt) * 1993-03-22 1995-12-11 Merck & Co Inc
US6316443B1 (en) 1994-08-04 2001-11-13 Merck & Co., Inc. Ophthalmic compositions comprising combinations of a carbonic anhydrase inhibitor and a β-adrenergic antagonist
TW438587B (en) * 1995-06-20 2001-06-07 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
FR2754712B1 (fr) 1996-10-17 1999-09-03 Merck Sharp Dohme Chibret Lab Compositions ophtalmiques
TWI290470B (en) 1999-12-01 2007-12-01 Sankyo Co The composition for treating glaucoma
CA2396319A1 (en) * 2000-01-18 2001-07-26 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
US6548535B2 (en) 2000-01-18 2003-04-15 Merck & Co., Inc. Method for treating ocular hypertension
ES2177415B1 (es) * 2000-09-04 2004-10-16 Ragactives, S.L. Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios.
US20040254230A1 (en) * 2001-12-03 2004-12-16 Ogidigben Miller J. Method for treating ocular hypertension
WO2003077845A2 (en) * 2002-03-15 2003-09-25 Merck & Co., Inc. Compositions and methods for treating glaucoma and ocular hypertension
JP2005534653A (ja) * 2002-06-06 2005-11-17 メルク フロスト カナダ アンド カンパニー 眼及び骨疾患の治療に於いてｅｐ４受容体作動薬として使用するための１，５−二置換イミダゾリジン−２−オン誘導体
WO2003105847A1 (en) * 2002-06-14 2003-12-24 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
EP1515974A4 (en) * 2002-06-17 2007-02-28 Merck & Co Inc NOVEL MAXI K CHANNEL BLOCKERS, METHODS OF USE, AND METHODS OF MANUFACTURING THE SAME
US7279490B2 (en) * 2002-06-17 2007-10-09 Merck & Co, Inc. Ophthalmic compositions for treating ocular hypertension
JP2005538061A (ja) * 2002-06-17 2005-12-15 メルク　エンド　カムパニー　インコーポレーテッド 新規ｍａｘｉ−ｋチャネルブロッカー、その使用方法および製造方法
EP1545517A1 (en) * 2002-08-28 2005-06-29 Merck Frosst Canada & Co. Oxazolidin-2-one and thiazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of glaucoma
JP2006505572A (ja) * 2002-10-25 2006-02-16 メルク フロスト カナダ アンド カンパニー Ｅｐ４受容体アゴニストとしての２−ピロリドン
AU2004226479A1 (en) * 2003-03-27 2004-10-14 Evotec Oai Ophthalmic compositions for treating ocular hypertension
EP1828198B1 (en) 2004-12-20 2011-02-09 SK Holdings Co., Ltd. Method for separating of optically pure thiophene compounds using simulated moving bed chromatography
US7109353B2 (en) * 2004-12-28 2006-09-19 Council Of Scientific And Industrial Research Process for preparing 5,6-dihydro-4-(S)-(ethylamino)-6-(S) methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide HCl
WO2006070387A1 (en) * 2004-12-28 2006-07-06 Council Of Scientific And Industrial Research PROCESS FOR PREPARING 5,6-DIHYDRO-4-(S)-(ETHYLAMINO)-6-(S) METHYL-4H-THIENO[2,3b]THIOPYRAN-2-SULPHONAMIDE-7,7-DIOXIDE HCI
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CN101622243B (zh) 2007-02-28 2013-12-04 旭化成制药株式会社 磺酰胺衍生物
EP2152718A2 (en) 2007-05-07 2010-02-17 Cipla Limited Process for preparing dorzolamide
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WO2012120086A1 (en) 2011-03-10 2012-09-13 Zach System S.P.A. Asymmetric reduction process
ITMI20121165A1 (it) * 2012-07-03 2014-01-04 Zach System Spa Processo di riduzione asimmetrica
CN103497202B (zh) * 2013-10-23 2015-12-02 武汉武药科技有限公司 盐酸多佐胺中间体的合成方法

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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
US4499103A (en) * 1983-03-17 1985-02-12 Merck & Co., Inc. Benzothiazole-2-sulfonamide derivatives for the topical treatment of elevated intraocular pressure
ATE41002T1 (de) * 1984-12-12 1989-03-15 Merck & Co Inc Substituierte aromatische sulfonamide, ihre herstellung und diese enthaltende ophthalmische zubereitungen.
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
US4731368A (en) * 1986-12-08 1988-03-15 Merck & Co., Inc. Thienopyridine sulfonamides and their ophthalmological formulation

Also Published As

Publication number Publication date
US4863922A (en) 1989-09-05
CY1772A (en) 1995-10-20
SG24394G (en) 1994-06-10
DK167684B1 (da) 1993-12-06
IE62255B1 (en) 1995-01-11
ES2053738T3 (es) 1994-08-01
DK348588D0 (da) 1988-06-24
ES2053738T4 (es) 2011-12-29
PT87832B (pt) 1992-10-30
ATE86998T1 (de) 1993-04-15
NL950006I2 (nl) 1997-02-03
NZ225166A (en) 1991-05-28
PT87832A (pt) 1989-05-31
IE881933L (en) 1988-12-26
DE19575017I2 (de) 2008-11-20
DE3879292D1 (de) 1993-04-22
AU616664B2 (en) 1991-11-07
AU1838788A (en) 1989-01-05
NL950006I1 (nl) 1995-06-16
EP0296879B1 (en) 1993-03-17
DE3879292T2 (de) 1993-09-09
EP0296879A1 (en) 1988-12-28
GR3007407T3 (pt) 1993-07-30
LU88633I2 (fr) 1995-09-01
CA1329211C (en) 1994-05-03
IL86822A0 (en) 1988-11-30
DK348588A (da) 1989-02-24
JPH01100174A (ja) 1989-04-18
CA1328262C (en) 1994-04-05
JPH0631247B2 (ja) 1994-04-27

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