CA2084857A1 - Saccharin derivative proteolytic enzyme inhibitors - Google Patents

Saccharin derivative proteolytic enzyme inhibitors

Info

Publication number
CA2084857A1
CA2084857A1 CA002084857A CA2084857A CA2084857A1 CA 2084857 A1 CA2084857 A1 CA 2084857A1 CA 002084857 A CA002084857 A CA 002084857A CA 2084857 A CA2084857 A CA 2084857A CA 2084857 A1 CA2084857 A1 CA 2084857A1
Authority
CA
Canada
Prior art keywords
alkyl
alkoxy
compound
phenyl
formula
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.)
Abandoned
Application number
CA002084857A
Other languages
English (en)
French (fr)
Inventor
Dennis J. Hlasta
James H. Ackerman
Albert J. Mura
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 Aventis France
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 CA2084857A1 publication Critical patent/CA2084857A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D275/00Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Cosmetics (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Beans For Foods Or Fodder (AREA)
  • Bakery Products And Manufacturing Methods Therefor (AREA)
  • Fertilizers (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CA002084857A 1991-12-19 1992-12-08 Saccharin derivative proteolytic enzyme inhibitors Abandoned CA2084857A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81026591A 1991-12-19 1991-12-19
US810,265 1991-12-19

Publications (1)

Publication Number Publication Date
CA2084857A1 true CA2084857A1 (en) 1993-06-20

Family

ID=25203432

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002084857A Abandoned CA2084857A1 (en) 1991-12-19 1992-12-08 Saccharin derivative proteolytic enzyme inhibitors

Country Status (19)

Country Link
EP (1) EP0547708B1 (US06251921-20010626-C00395.png)
JP (1) JP3179600B2 (US06251921-20010626-C00395.png)
KR (2) KR100292995B1 (US06251921-20010626-C00395.png)
AT (1) ATE233250T1 (US06251921-20010626-C00395.png)
AU (1) AU668694B2 (US06251921-20010626-C00395.png)
CA (1) CA2084857A1 (US06251921-20010626-C00395.png)
CZ (1) CZ283257B6 (US06251921-20010626-C00395.png)
DE (1) DE69232929D1 (US06251921-20010626-C00395.png)
FI (1) FI925787A (US06251921-20010626-C00395.png)
HU (1) HU219950B (US06251921-20010626-C00395.png)
IL (1) IL104154A (US06251921-20010626-C00395.png)
MX (1) MX9207449A (US06251921-20010626-C00395.png)
MY (1) MY110104A (US06251921-20010626-C00395.png)
NO (1) NO300770B1 (US06251921-20010626-C00395.png)
NZ (1) NZ245518A (US06251921-20010626-C00395.png)
RU (1) RU2107685C1 (US06251921-20010626-C00395.png)
SG (1) SG52659A1 (US06251921-20010626-C00395.png)
SK (1) SK374692A3 (US06251921-20010626-C00395.png)
TW (1) TW225532B (US06251921-20010626-C00395.png)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
US8013001B2 (en) 2001-12-21 2011-09-06 Exelixis, Inc. Modulators of LXR

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5378720A (en) * 1991-12-19 1995-01-03 Sterling Winthrop Inc. Saccharin derivative proteolytic enzyme inhibitors
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
US5512576A (en) * 1994-12-02 1996-04-30 Sterling Winthrop Inc. 2-substituted 1,2,5,-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
DE19533643A1 (de) * 1995-09-12 1997-03-13 Nycomed Arzneimittel Gmbh Neue cyclische Derivate von Benzolsulfonamiden
US5750550A (en) * 1995-09-15 1998-05-12 Sanofi 2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof
ES2334990T3 (es) 2002-02-14 2010-03-18 Pharmacia Corporation Piridinonas sustituidas como moduladores de p38 map quinasa.
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-二取代之3-氰基-吡啶酮衍生物及其作為mGluR2-受體之正向異位性調節劑之用途
NZ575685A (en) * 2006-10-04 2012-04-27 Bionomics Ltd Novel benzofuran potassium channel blockers and uses thereof
CA2672656C (en) 2006-12-18 2012-03-20 Amgen Inc. Naphthalenone compounds exhibiting prolyl hydroxylase inhibitory activity, compositions, and uses thereof
EP2097416B1 (en) 2006-12-18 2012-09-12 Amgen, Inc Azaquinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, compositions, and uses thereof
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
US8048894B2 (en) 2007-04-18 2011-11-01 Amgen Inc. Quinolones and azaquinolones that inhibit prolyl hydroxylase
WO2008130508A1 (en) 2007-04-18 2008-10-30 Amgen Inc. Indanone derivatives that inhibit prolyl hydroxylase
AU2008248165B2 (en) 2007-05-04 2011-12-08 Amgen Inc. Diazaquinolones that inhibit prolyl hydroxylase activity
AU2008248234B2 (en) 2007-05-04 2011-02-03 Amgen Inc. Thienopyridine and thiazolopyridine derivatives that inhibit prolyl hydroxylase activity
US9114138B2 (en) 2007-09-14 2015-08-25 Janssen Pharmaceuticals, Inc. 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones
WO2010025890A1 (en) 2008-09-02 2010-03-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
WO2010060589A1 (en) 2008-11-28 2010-06-03 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
SG10201402250TA (en) 2009-05-12 2014-07-30 Janssen Pharmaceuticals Inc 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
MX2011011962A (es) 2009-05-12 2012-02-28 Janssen Pharmaceuticals Inc Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostericos positivos de receptores de glutamato metabotropico (mglur2).
WO2012062750A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
ES2552879T3 (es) 2010-11-08 2015-12-02 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
EA201891617A3 (ru) 2014-01-21 2019-04-30 Янссен Фармацевтика Нв Комбинации, содержащие положительные аллостерические модуляторы или ортостерические агонисты метаботропного глутаматергического рецептора 2 подтипа, и их применение
HUE053734T2 (hu) 2014-01-21 2021-07-28 Janssen Pharmaceutica Nv 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE3617976A1 (de) * 1986-05-28 1988-01-14 Alter Sa 1,4-dihydropyridin, verfahren zu dessen herstellung und dessen verwendung in antithrombotischen medikamenten
ATE159720T1 (de) * 1989-05-04 1997-11-15 Sanofi Sa Saccharinderivate zur verwendung als proteolytische enzyminhibitoren sowie verfahren zur herstellung
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
AU656027B2 (en) * 1991-11-15 1995-01-19 Sanofi Saccharin derivative proteolytic enzime inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
US8013001B2 (en) 2001-12-21 2011-09-06 Exelixis, Inc. Modulators of LXR

Also Published As

Publication number Publication date
HU9204029D0 (en) 1993-04-28
NO924915L (no) 1993-06-21
NO300770B1 (no) 1997-07-21
SG52659A1 (en) 1998-09-28
JPH05345771A (ja) 1993-12-27
FI925787A (fi) 1993-06-20
MY110104A (en) 1998-01-27
CZ283257B6 (cs) 1998-02-18
IL104154A (en) 1996-09-12
ATE233250T1 (de) 2003-03-15
JP3179600B2 (ja) 2001-06-25
IL104154A0 (en) 1993-05-13
EP0547708B1 (en) 2003-02-26
EP0547708A1 (en) 1993-06-23
SK278390B6 (en) 1997-02-05
HU219950B (hu) 2001-09-28
FI925787A0 (fi) 1992-12-18
CZ374692A3 (en) 1993-08-11
NZ245518A (en) 1995-06-27
DE69232929D1 (de) 2003-04-03
AU2829292A (en) 1993-07-08
KR100292995B1 (ko) 2001-09-17
RU2107685C1 (ru) 1998-03-27
NO924915D0 (no) 1992-12-18
TW225532B (US06251921-20010626-C00395.png) 1994-06-21
KR100378968B1 (ko) 2003-04-08
AU668694B2 (en) 1996-05-16
HUT67039A (en) 1995-01-30
SK374692A3 (en) 1997-02-05
MX9207449A (es) 1994-03-31

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued