WO2000018741A3 - Pyrazole compounds as cox-2 inhibitors - Google Patents

Pyrazole compounds as cox-2 inhibitors Download PDF

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Publication number
WO2000018741A3
WO2000018741A3 PCT/JP1999/005289 JP9905289W WO0018741A3 WO 2000018741 A3 WO2000018741 A3 WO 2000018741A3 JP 9905289 W JP9905289 W JP 9905289W WO 0018741 A3 WO0018741 A3 WO 0018741A3
Authority
WO
WIPO (PCT)
Prior art keywords
optionally substituted
hydroxy
halogen
hydrogen
substituted
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
PCT/JP1999/005289
Other languages
French (fr)
Other versions
WO2000018741A2 (en
Inventor
Nobukiyo Konishi
Katsuya Nakamura
Hirofumi Yamamoto
Takashi Manabe
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.)
Fujisawa Pharmaceutical Co Ltd
Original Assignee
Fujisawa Pharmaceutical Co Ltd
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
Priority claimed from AUPP6231A external-priority patent/AUPP623198A0/en
Priority claimed from AUPQ2243A external-priority patent/AUPQ224399A0/en
Application filed by Fujisawa Pharmaceutical Co Ltd filed Critical Fujisawa Pharmaceutical Co Ltd
Publication of WO2000018741A2 publication Critical patent/WO2000018741A2/en
Publication of WO2000018741A3 publication Critical patent/WO2000018741A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings 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
    • C07D231/16—Halogen atoms or nitro radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A compound of formula (I), wherein R1 is halo(lower)alkyl, halogen or cyano, R2 is aryl optionally substituted with substituent(s) selected from the group consisting of halogen, lower alkoxy, cyano, nitro, lower alkenyl, amino, acyl and hydroxyimino, R3 is hydrogen, hydroxy, acyloxy, lower alkoxy optionally substituted with lower alkoxy, amino optionally substituted with hydroxy or lower alkyl, lower alkylthio, or lower alkylsulfonyl, R4 is hydrogen or halogen, Q is pyrazolyl, A is lower alkylene optionally substituted with oxo or hydroxy, and n is 0, 1 or 2, provided that when R3 is hydrogen, R2 is aryl substituted with lower alkenyl or A is lower alkylene substituted with oxo, or its salt, processes for their preparation and pharmaceutical compositions.
PCT/JP1999/005289 1998-09-30 1999-09-27 Pyrazole compounds as cox-2 inhibitors Ceased WO2000018741A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
AUPP6231A AUPP623198A0 (en) 1998-09-30 1998-09-30 Novel compounds
AUPP6231 1998-09-30
AUPQ2243 1999-08-16
AUPQ2243A AUPQ224399A0 (en) 1999-08-16 1999-08-16 Novel compounds

Publications (2)

Publication Number Publication Date
WO2000018741A2 WO2000018741A2 (en) 2000-04-06
WO2000018741A3 true WO2000018741A3 (en) 2000-06-08

Family

ID=25645886

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1999/005289 Ceased WO2000018741A2 (en) 1998-09-30 1999-09-27 Pyrazole compounds as cox-2 inhibitors

Country Status (1)

Country Link
WO (1) WO2000018741A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7172769B2 (en) 1999-12-08 2007-02-06 Pharmacia Corporation Cyclooxygenase-2 inhibitor compositions having rapid onset of therapeutic effect

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030100594A1 (en) * 2001-08-10 2003-05-29 Pharmacia Corporation Carbonic anhydrase inhibitor
JP2006502980A (en) * 2002-06-25 2006-01-26 ファルマシア・コーポレーション Arylsulfonylhydroxamic acid and amide derivatives and their use as protease inhibitors
JP2005535642A (en) * 2002-06-28 2005-11-24 ニトロメッド インコーポレーティッド Nitrosated and / or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use containing oximes and / or hydrazones
ES2379076T3 (en) 2002-12-02 2012-04-20 Astellas Pharma Inc. Useful pyrazole derivatives as COX-I inhibitors
CA3010445A1 (en) * 2016-01-05 2017-07-13 The Regents Of The University Of California Benzothiazole amphiphiles
CN107827820B (en) * 2017-11-10 2020-01-07 山东大学 Pyrazoline aminopeptidase N inhibitor and preparation method and application thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5486534A (en) * 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
WO1997013755A1 (en) * 1995-10-09 1997-04-17 Fujisawa Pharmaceutical Co., Ltd. 1,3,5-trisubstituted pyrazoles for treament of inflammation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5486534A (en) * 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
WO1997013755A1 (en) * 1995-10-09 1997-04-17 Fujisawa Pharmaceutical Co., Ltd. 1,3,5-trisubstituted pyrazoles for treament of inflammation

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
TSUJI ET AL: "Studies on anti- inflammatory agents. IV. Synthesis and pharmacological properties of 1,5-diarylpyrazoles and related derivatives", CHEMICAL AND PHARMACEUTICAL BULLETIN,JP,PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, vol. 45, no. 6, June 1997 (1997-06-01), pages 987 - 995, XP002112608, ISSN: 0009-2363 *
TSUJI ET AL: "Studies on anti- inflammatory agents. V. Synthesis and pharmacological properties of 3-(difluoromethyl)-1-(4-methoxyphenyl)- 5-[4-(methylsulfinyl)phenyl]pyrazole and related compounds", CHEMICAL AND PHARMACEUTICAL BULLETIN,JP,PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, vol. 45, no. 9, September 1997 (1997-09-01), pages 1475 - 1481, XP002112607, ISSN: 0009-2363 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7172769B2 (en) 1999-12-08 2007-02-06 Pharmacia Corporation Cyclooxygenase-2 inhibitor compositions having rapid onset of therapeutic effect

Also Published As

Publication number Publication date
WO2000018741A2 (en) 2000-04-06

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