FI80032B - Foer behandling av oegats inre tryck an- vaendbara 2-sulfamoylbenzo/b/tiofenderivat. - Google Patents

Foer behandling av oegats inre tryck an- vaendbara 2-sulfamoylbenzo/b/tiofenderivat. Download PDF

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Publication number
FI80032B
FI80032B FI842478A FI842478A FI80032B FI 80032 B FI80032 B FI 80032B FI 842478 A FI842478 A FI 842478A FI 842478 A FI842478 A FI 842478A FI 80032 B FI80032 B FI 80032B
Authority
FI
Finland
Prior art keywords
formula
compound
thiophene
sulfamoylbenzo
solution
Prior art date
Application number
FI842478A
Other languages
English (en)
Finnish (fi)
Other versions
FI80032C (sv
FI842478A0 (fi
FI842478A (fi
Inventor
Robert F Czaja
David G Melillo
Kenneth L Shepard
Samuel L Graham
Jr Jacob M Hoffmann
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of FI842478A0 publication Critical patent/FI842478A0/fi
Publication of FI842478A publication Critical patent/FI842478A/fi
Application granted granted Critical
Publication of FI80032B publication Critical patent/FI80032B/fi
Publication of FI80032C publication Critical patent/FI80032C/sv

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Classifications

    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • 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
    • 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
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
    • C07F9/655354—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (6)

1. Förfarande för framställninv av en förening med formeln R ~0O>~s°2m2 och av oftalmologiskt eller farmaceutiskt godtagbara sait 10 därav, varvid X är väte, halogen, säsom klor, brom eller fluor, C^_2~alkyl, hydroxi eller C^_3~alkoxi; och R är 0 0 9 9 1. hydroxi, R^-C-O, R^-O-C-O och R^-O-C-R^-C-O; där R^ är C^_4~alkyl; 15 kännetecknat därav, att man a) ifall R är OH, hydrolyserar motsvarande metyleter; i 2 b) ifall R är R -C-O-, behandlar föreningen
20 Ha_©0>_S°2NH2 med R^-CO-X^, väri R^ är som ovan angivits och X^ är klor, brom, jod, -OCOR1, -OCOCH2(CH3) eller -0C0N(CgH^2; c) ifall R är R^O-CO-O, behandlar föreningen 25 H° —so2nh2 med ett klorformiat med formeln R^-OCOCl eller med ett bis-3 0 karbonat med formeln R"*OCOOR^.
2. Förfarande för framställning av en förening med strukturformeIn 35. il )>— SO NH 58 80032 kännetecknat därav, att man a) reducerar en förening med strukturformeln ho\/\5vo 5 1^JQ>^02NH2 b) oxiderar en förening med strukturformeln 1° s™2 c) dehalogenerar en förening med strukturformeln ^j)3^S02KH2 halo 20 väri halo är Cl, Br eller J; d) aminerar en förening med strukturformeln „ ""Cö-·”·'· e) behandlar en förening med strukturformeln S O 30 väri M är en alkalimetallkatjon, med en elektrofil kväve-förening; II 59 80032 f) behandlar en förening med strukturformeln I | /)-SO,N=v k- 2 n W(C1_4alkyl) med en syra eller bas; g) behandlar en förening med strukturformeln HOtl <^/^^VnvS02NH2 med vattenfri vätehalogenid i flytande svaveldioxid; 15 h) diazotiserar en förening med strukturformeln H., N. 2 xy^>V's\ 20 i) behandlar en förening med strukturformeln 9 van R är väte, C^_4-alkyl, fenyl-C^ _4~alkyl eller f enyl, med ammoniak eller med ammoniumjoner; j) avföretrar en förening med strukturformeln 30 TÖ- S0^NH2 1 o 35 väri R är C^_4~alkyl eller fenyl-C _4~alkyl, 60 80 032 k) deacylerar en förening med strukturformeln O lH 5 s°2NH2 l) reducerar en förening med strukturformeln o II
FI842478A 1983-06-20 1984-06-19 Förfarande för framställning av nya terapeutiskt användbara 2-sulfamoy lbenso/b/tiofenderivat FI80032C (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US50609283A 1983-06-20 1983-06-20
US50609283 1983-06-20
US54719183A 1983-10-31 1983-10-31
US54719183 1983-10-31

Publications (4)

Publication Number Publication Date
FI842478A0 FI842478A0 (fi) 1984-06-19
FI842478A FI842478A (fi) 1984-12-21
FI80032B true FI80032B (fi) 1989-12-29
FI80032C FI80032C (sv) 1990-04-10

Family

ID=27055356

Family Applications (1)

Application Number Title Priority Date Filing Date
FI842478A FI80032C (sv) 1983-06-20 1984-06-19 Förfarande för framställning av nya terapeutiskt användbara 2-sulfamoy lbenso/b/tiofenderivat

Country Status (15)

Country Link
EP (1) EP0129478B1 (sv)
KR (1) KR890000386B1 (sv)
AU (1) AU558665B2 (sv)
CA (1) CA1253151A (sv)
DE (1) DE3481057D1 (sv)
DK (1) DK298584A (sv)
ES (1) ES8600272A1 (sv)
FI (1) FI80032C (sv)
GR (1) GR82372B (sv)
HU (1) HUT37420A (sv)
IE (1) IE57601B1 (sv)
IL (1) IL72070A (sv)
NO (1) NO842467L (sv)
NZ (1) NZ208444A (sv)
PT (1) PT78762A (sv)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0189690B1 (en) * 1984-12-12 1989-03-01 Merck & Co. Inc. Substituted aromatic sulfonamides, their preparation and ophthalmic compositions containing them
US4820848A (en) * 1984-12-12 1989-04-11 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US4731368A (en) * 1986-12-08 1988-03-15 Merck & Co., Inc. Thienopyridine sulfonamides and their ophthalmological formulation
EP0271273A3 (en) * 1986-12-08 1989-07-12 Merck & Co. Inc. Thieno-and furopyridine sulfonamides
US4808595A (en) * 1986-12-24 1989-02-28 Merck & Co., Inc. Furopyridine sulfonamides and their opthalmological compositions
US4894390A (en) * 1987-08-03 1990-01-16 Merck & Co., Inc. Substituted thieno[2,3-b]thiophene-2-sulfonamides as antiglaucoma agents
CA1320487C (en) * 1987-08-03 1993-07-20 George D. Hartman Substituted thieno[2,3-.beta.]thiophene-2-sulfonamides as antiglaucoma agents
US4751231A (en) * 1987-09-16 1988-06-14 Merck & Co., Inc. Substituted thieno[2,3-b]pyrrole-5-sulfonamides as antiglaucoma agents
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
AU3378399A (en) * 1998-04-02 1999-10-25 Ortho-Mcneil Pharmaceutical, Inc. 4-thionaphthyl-1h-imidazoles with alpha-2-adrenergic activity
US6313309B1 (en) * 1999-04-05 2001-11-06 Ortho-Mcneil Pharmaceutical, Inc. 4-thionaphthyl—1H—imidazoles which are usefulα22-adrenoceptoR agonists/ antagonists
NZ561672A (en) 2005-03-28 2010-04-30 Toyama Chemical Co Ltd Process for production of 1-(3-(2-(1-benzothiophen-5-yl)-ethoxy)propyl)azetidin-3-ol or salts thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR241136A1 (es) * 1981-07-13 1991-11-29 Merck E Co Inc Procedimiento para preparar esteres de 6-hidroxi-2-benzotiazolsulfonamida para tratamiento topicode presion intraocular elevada"
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

Also Published As

Publication number Publication date
EP0129478B1 (en) 1990-01-17
AU2949684A (en) 1985-06-13
FI80032C (sv) 1990-04-10
NO842467L (no) 1985-12-21
KR890000386B1 (ko) 1989-03-16
AU558665B2 (en) 1987-02-05
PT78762A (en) 1984-07-01
KR850000428A (ko) 1985-02-27
DK298584A (da) 1984-12-21
ES533390A0 (es) 1985-10-01
GR82372B (sv) 1984-12-13
IL72070A0 (en) 1984-10-31
EP0129478A3 (en) 1987-03-25
DK298584D0 (da) 1984-06-19
EP0129478A2 (en) 1984-12-27
NZ208444A (en) 1987-08-31
IE841536L (en) 1984-12-20
FI842478A0 (fi) 1984-06-19
FI842478A (fi) 1984-12-21
HUT37420A (en) 1985-12-28
IE57601B1 (en) 1993-01-27
DE3481057D1 (de) 1990-02-22
ES8600272A1 (es) 1985-10-01
IL72070A (en) 1988-11-30
CA1253151A (en) 1989-04-25

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Owner name: MERCK & CO., INC.