DK167684B1 - Substitueret aromatisk sulfonamid og farmaceutisk praeparat til behandling af glaucom indeholdende en saadan forbindelse - Google Patents

Substitueret aromatisk sulfonamid og farmaceutisk praeparat til behandling af glaucom indeholdende en saadan forbindelse Download PDF

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Publication number
DK167684B1
DK167684B1 DK348588A DK348588A DK167684B1 DK 167684 B1 DK167684 B1 DK 167684B1 DK 348588 A DK348588 A DK 348588A DK 348588 A DK348588 A DK 348588A DK 167684 B1 DK167684 B1 DK 167684B1
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DK
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Prior art keywords
dihydro
sulfonamide
thiopyran
mixture
solution
Prior art date
Application number
DK348588A
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Danish (da)
English (en)
Other versions
DK348588A (da
DK348588D0 (da
Inventor
John J Baldwin
Gerald S Ponticello
Marcia E Christy
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
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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=DK167684(B1) "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 DK348588D0 publication Critical patent/DK348588D0/da
Publication of DK348588A publication Critical patent/DK348588A/da
Application granted granted Critical
Publication of DK167684B1 publication Critical patent/DK167684B1/da

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    • 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)
  • Dental Preparations (AREA)
  • Heat Sensitive Colour Forming Recording (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)
DK348588A 1987-06-26 1988-06-24 Substitueret aromatisk sulfonamid og farmaceutisk praeparat til behandling af glaucom indeholdende en saadan forbindelse DK167684B1 (da)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US6732687 1987-06-26
US07/067,326 US4797413A (en) 1986-05-14 1987-06-26 Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
US20831488 1988-06-15
US07/208,314 US4863922A (en) 1984-12-12 1988-06-15 Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use

Publications (3)

Publication Number Publication Date
DK348588D0 DK348588D0 (da) 1988-06-24
DK348588A DK348588A (da) 1989-02-24
DK167684B1 true DK167684B1 (da) 1993-12-06

Family

ID=26747752

Family Applications (1)

Application Number Title Priority Date Filing Date
DK348588A DK167684B1 (da) 1987-06-26 1988-06-24 Substitueret aromatisk sulfonamid og farmaceutisk praeparat til behandling af glaucom indeholdende en saadan forbindelse

Country Status (18)

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

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CA1320487C (fr) * 1987-08-03 1993-07-20 George D. Hartman Thieno (2,3-.beta.)thiophen-2-sulfonamides utilises comme agents antig laucome
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
US5120757A (en) * 1989-07-31 1992-06-09 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
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
CA2028496A1 (fr) * 1989-10-31 1991-05-01 Tohru Nakao Composes de thiophene et leurs applications pharmaceutiques
IE911192A1 (en) * 1990-04-12 1991-10-23 Merck & Co Inc Substituted aromatic sulfonamides as antiglaucoma agents
US5045561A (en) * 1990-04-12 1991-09-03 Merck & Co., Inc. Substituted furan 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
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
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
EP0480745A3 (en) * 1990-10-12 1992-07-29 Merck & Co. Inc. Substituted dihydrothieno-thiophene-2-sulfonamides and dioxides thereof
IL101537A (en) * 1991-04-17 1997-11-20 Merck & Co Inc OPHTHALMIC COMPOSITIONS COMPRISING COMBINATIONS OF A CARBONIC ANHYDRASE INHIBITOR AND A b-ADRENERGIC ANTAGONIST
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
JPH0830067B2 (ja) * 1991-10-15 1996-03-27 メルク エンド カムパニー インコーポレーテッド 三環チエノチオピラン類
US5932572A (en) * 1992-02-21 1999-08-03 Alcon Laboratories, Inc. Topical anti-glaucoma compositions
ES2118941T3 (es) * 1992-02-21 1998-10-01 Alcon Lab Inc Composiciones antiglaucoma topicas que comprenden inhibidores de anhidrasa carbonica y bloqueantes beta.
ATE144795T1 (de) * 1992-08-28 1996-11-15 Zeneca Ltd Enzymatisches asymetrisches reduktionsverfahren zur herstellung von 4h thieno (2,3-6) thiopyren derivaten.
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 (fr) * 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
ATE409491T1 (de) 2000-01-18 2008-10-15 Merck & Co Inc Orhthalmologische zusammenstellungen zur behandlung von ocularer 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 (fr) * 2002-03-15 2003-09-25 Merck & Co., Inc. Compositions et methodes de traitement du glaucome et de l'hypertension oculaire
CA2487977A1 (fr) * 2002-06-06 2003-12-18 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Derives d'imidazolidine-2-one disubstitues en 1,5 utiles en tant qu'agonistes du recepteur ep4 dans le traitement de troubles oculaires et de maladies osseuses
AU2003239972B2 (en) * 2002-06-14 2008-02-28 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
CA2488884A1 (fr) * 2002-06-17 2003-12-24 Merck & Co., Inc. Nouveaux inhibiteurs de canaux maxi k, methodes d'utilisation et procede de fabrication associe
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AU2003258433A1 (en) * 2002-08-28 2004-03-19 Merck Frosst Canada Ltd Oxazolidin-2-one and thiazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of glaucoma
CA2502914A1 (fr) * 2002-10-25 2004-05-06 Merck Frosst Canada & Co. Agonistes des recepteurs ep<sb>4</sb>
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MX2007007923A (es) * 2004-12-28 2007-11-14 Usv Ltd Procedimiento para preparar clorhidrato de 5,6-dihidro-4-(s)- (etilamino)-6-(s)metil-4h-tieno[2,3b]tiopiran-2-sulfonamida-7,7- dioxido.
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EP1918293A1 (fr) * 2006-10-02 2008-05-07 Sandoz AG Procédé pour la préparation d'acide 4-oxo-thieno[2,3b]thiopyran-2-yl-sulfonique
CA2679263A1 (fr) 2007-02-28 2008-09-04 Asahi Kasei Pharma Corporation Derive de sulfonamide
AU2008247144B2 (en) * 2007-05-07 2013-02-28 Cipla Limited Process for preparing dorzolamide
JP2011517313A (ja) 2007-12-11 2011-06-02 ビアメト ファーマシューティカルズ，インク． 金属結合部分を標的化部分と組み合わせて使用する金属酵素阻害剤
WO2010061398A1 (fr) * 2008-11-27 2010-06-03 Suven Life Sciences Limited Procédé pour la préparation de chlorhydrate de dorzolamide et ses intermédiaires
EP2683724B1 (fr) 2011-03-10 2015-05-06 ZaCh System S.p.A. Procédé de réduction asymétrique
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
EP0189690B1 (fr) * 1984-12-12 1989-03-01 Merck & Co. Inc. Sulfonamides aromatiques substitués, leur préparation et compositions ophtalmiques les contenant
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
CY1772A (en) 1995-10-20
ES2053738T4 (es) 2011-12-29
SG24394G (en) 1994-06-10
DK348588A (da) 1989-02-24
IE881933L (en) 1988-12-26
IL86822A (en) 1992-01-15
ES2053738T3 (es) 1994-08-01
PT87832A (pt) 1989-05-31
AU1838788A (en) 1989-01-05
JPH0631247B2 (ja) 1994-04-27
LU88633I2 (fr) 1995-09-01
GR3007407T3 (fr) 1993-07-30
EP0296879A1 (fr) 1988-12-28
DE3879292D1 (de) 1993-04-22
ATE86998T1 (de) 1993-04-15
NZ225166A (en) 1991-05-28
DE19575017I2 (de) 2008-11-20
CA1328262C (fr) 1994-04-05
JPH01100174A (ja) 1989-04-18
DK348588D0 (da) 1988-06-24
CA1329211C (fr) 1994-05-03
EP0296879B1 (fr) 1993-03-17
NL950006I2 (nl) 1997-02-03
IL86822A0 (en) 1988-11-30
US4863922A (en) 1989-09-05
DE3879292T2 (de) 1993-09-09
NL950006I1 (nl) 1995-06-16
AU616664B2 (en) 1991-11-07
PT87832B (pt) 1992-10-30
IE62255B1 (en) 1995-01-11

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Legal Events

Date Code Title Description
CTFF Application for supplementary protection certificate (spc) filed

Free format text: PRODUCT NAME: DORZOLAMID

Spc suppl protection certif: CA 1995 00005

Filing date: 19950428

CTFG Supplementary protection certificate (spc) issued

Spc suppl protection certif: CA 1995 00005

Filing date: 19950428

PUP Patent expired