AU648938B2 - Novel 2-saccharinylmethyl and 4,5,6,7-tetrahydro -2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof - Google Patents

Novel 2-saccharinylmethyl and 4,5,6,7-tetrahydro -2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof Download PDF

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Publication number
AU648938B2
AU648938B2 AU28294/92A AU2829492A AU648938B2 AU 648938 B2 AU648938 B2 AU 648938B2 AU 28294/92 A AU28294/92 A AU 28294/92A AU 2829492 A AU2829492 A AU 2829492A AU 648938 B2 AU648938 B2 AU 648938B2
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AU
Australia
Prior art keywords
alkyl
hydrogen
mol
phenyl
compound according
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU28294/92A
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English (en)
Other versions
AU2829492A (en
Inventor
John Joseph Court
Ranjit Chimanlal Desai
Dennis John Hlasta
Chakrapani Subramanyam
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi SA
Original Assignee
Sterling Winthrop 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 Sterling Winthrop Inc filed Critical Sterling Winthrop Inc
Publication of AU2829492A publication Critical patent/AU2829492A/en
Application granted granted Critical
Publication of AU648938B2 publication Critical patent/AU648938B2/en
Assigned to SANOFI reassignment SANOFI Alteration of Name(s) in Register under S187 Assignors: STERLING WINTHROP INC.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings
    • C07F9/6541—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65742—Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
    • 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
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65744—Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems

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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)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
AU28294/92A 1991-12-27 1992-11-12 Novel 2-saccharinylmethyl and 4,5,6,7-tetrahydro -2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof Ceased AU648938B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/814,741 US5187173A (en) 1991-12-27 1991-12-27 2-saccharinylmethyl and 4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
US814741 1991-12-27

Publications (2)

Publication Number Publication Date
AU2829492A AU2829492A (en) 1993-07-01
AU648938B2 true AU648938B2 (en) 1994-05-05

Family

ID=25215883

Family Applications (1)

Application Number Title Priority Date Filing Date
AU28294/92A Ceased AU648938B2 (en) 1991-12-27 1992-11-12 Novel 2-saccharinylmethyl and 4,5,6,7-tetrahydro -2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof

Country Status (22)

Country Link
US (1) US5187173A (enExample)
EP (1) EP0549073B1 (enExample)
JP (1) JPH05271262A (enExample)
AT (1) ATE150755T1 (enExample)
AU (1) AU648938B2 (enExample)
CA (1) CA2085427A1 (enExample)
CZ (1) CZ371692A3 (enExample)
DE (1) DE69218568T2 (enExample)
DK (1) DK0549073T3 (enExample)
ES (1) ES2100274T3 (enExample)
FI (1) FI925875L (enExample)
GR (1) GR3023632T3 (enExample)
HU (1) HUT63630A (enExample)
IL (3) IL104229A (enExample)
MX (1) MX9207542A (enExample)
MY (1) MY106897A (enExample)
NO (1) NO303639B1 (enExample)
NZ (1) NZ245585A (enExample)
RU (1) RU2091377C1 (enExample)
SG (1) SG48310A1 (enExample)
SK (1) SK371692A3 (enExample)
TW (1) TW225538B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU670635B2 (en) * 1992-12-08 1996-07-25 Sanofi Novel 2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5236917A (en) * 1989-05-04 1993-08-17 Sterling Winthrop Inc. Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
AU653279B2 (en) * 1991-12-30 1994-09-22 Sanofi Novel 2-saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
US5541168A (en) * 1994-12-02 1996-07-30 Sterling Winthrop Inc. Substituted 2-(phosphinyloxymethyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
IL163748A0 (en) * 2002-03-05 2005-12-18 Merck Frosst Canada Inc Cathepsin cysteine protease inhibitors
CA2479256A1 (en) * 2002-03-20 2003-10-02 Bristol-Myers Squibb Company Phosphate prodrugs of fluorooxindoles
DK1865940T3 (da) * 2005-03-21 2013-03-04 Virobay Inc Alfaketoamidforbindelser som cysteinproteasehæmmere

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2534092A (en) * 1991-11-15 1993-05-20 Sanofi 2-substituted saccharin derivative proteolytic enzyme inhibitors
AU642537B2 (en) * 1990-11-01 1993-10-21 Sanofi 2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3002884A (en) * 1959-04-15 1961-10-03 Rohm & Haas Horticultural process with n-halomethyl-1,2-benzisothiazolin - 3 - one-1,1-dioxides for controlling fungus diseases
US3314960A (en) * 1964-08-25 1967-04-18 American Home Prod Benzisothiazol glutarimides
FR1451417A (fr) * 1965-07-15 1966-01-07 Roussel Uclaf Nouveaux esters d'acides cycliques et leur procédé de préparation
US4195023A (en) * 1975-08-20 1980-03-25 Merck & Co., Inc. 2-(2-Furoyl)1,2-benzisothiazole-3-one, 2-(2-furoyl) saccharin, and 2-(2-thenoyl) saccharin
US4276298A (en) * 1978-03-24 1981-06-30 Merck & Co., Inc. 2-Aryl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective protease inhibitors
US4263393A (en) * 1979-09-06 1981-04-21 Eastman Kodak Company Novel electron donor precursors and photographic element containing them
US4350752A (en) * 1980-12-29 1982-09-21 Eastman Kodak Company Photographic elements and film units containing imidomethyl blocked photographic reagents
US4363865A (en) * 1981-03-04 1982-12-14 Eastman Kodak Company Imido methyl blocked photographic dyes and dye releasing compounds
US4410618A (en) * 1982-06-11 1983-10-18 Eastman Kodak Company Blocked photographic reagents
US4547371A (en) * 1983-04-18 1985-10-15 Merck & Co., Inc. Substituted cephalosporin sulfones as anti-inflammatory and anti-degenerative agents
US4623645A (en) * 1983-04-18 1986-11-18 Merck & Co., Inc. Substituted cephalosporin sulfoxides as anti-inflammatory and antidegenerative agents
US4659855A (en) * 1983-05-09 1987-04-21 Georgia Tech Research Corporation Aryl sulfonyl fluoride compounds
JPH026496A (ja) * 1988-06-27 1990-01-10 Ishihara Sangyo Kaisha Ltd 有機リン酸アミド系化合物、それらの製造方法及びそれらを含有する有害動物防除剤
NZ233521A (en) * 1989-05-04 1992-05-26 Sterling Drug Inc 2-substituted saccharin derivatives, preparation and pharmaceutical compositions thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU642537B2 (en) * 1990-11-01 1993-10-21 Sanofi 2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
AU2534092A (en) * 1991-11-15 1993-05-20 Sanofi 2-substituted saccharin derivative proteolytic enzyme inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU670635B2 (en) * 1992-12-08 1996-07-25 Sanofi Novel 2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof

Also Published As

Publication number Publication date
TW225538B (enExample) 1994-06-21
FI925875A7 (fi) 1993-06-28
FI925875L (fi) 1993-06-28
AU2829492A (en) 1993-07-01
ATE150755T1 (de) 1997-04-15
DE69218568D1 (de) 1997-04-30
MY106897A (en) 1995-08-30
MX9207542A (es) 1993-06-01
DE69218568T2 (de) 1997-11-13
EP0549073B1 (en) 1997-03-26
DK0549073T3 (da) 1997-10-06
CA2085427A1 (en) 1993-06-28
GR3023632T3 (en) 1997-08-29
IL116601A (en) 1997-04-15
HUT63630A (en) 1993-09-28
CZ371692A3 (en) 1994-04-13
RU2091377C1 (ru) 1997-09-27
IL104229A (en) 1997-02-18
NO924991L (no) 1993-06-28
JPH05271262A (ja) 1993-10-19
HU9204123D0 (en) 1993-04-28
NZ245585A (en) 1995-05-26
EP0549073A1 (en) 1993-06-30
FI925875A0 (fi) 1992-12-23
US5187173A (en) 1993-02-16
IL116601A0 (en) 1996-03-31
NO303639B1 (no) 1998-08-10
SK371692A3 (en) 1995-05-10
SG48310A1 (en) 1998-04-17
NO924991D0 (no) 1992-12-23
IL104229A0 (en) 1993-05-13
ES2100274T3 (es) 1997-06-16

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Legal Events

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired