AU773317B2 - Pyrazinones, compositions containing such compounds - Google Patents

Pyrazinones, compositions containing such compounds Download PDF

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Publication number
AU773317B2
AU773317B2 AU61432/00A AU6143200A AU773317B2 AU 773317 B2 AU773317 B2 AU 773317B2 AU 61432/00 A AU61432/00 A AU 61432/00A AU 6143200 A AU6143200 A AU 6143200A AU 773317 B2 AU773317 B2 AU 773317B2
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AU
Australia
Prior art keywords
alkyl
cooh
aryl
het
halo
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.)
Expired
Application number
AU61432/00A
Other languages
English (en)
Other versions
AU6143200A (en
Inventor
Christopher I. Bayly
John Colucci
Andre Giroux
Erich L Grimm
Yongxin Han
Daniel J. Mckay
Robert Zamboni
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.)
Merck Canada Inc
Original Assignee
Merck Frosst Canada and Co
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 Frosst Canada and Co filed Critical Merck Frosst Canada and Co
Publication of AU6143200A publication Critical patent/AU6143200A/en
Application granted granted Critical
Publication of AU773317B2 publication Critical patent/AU773317B2/en
Assigned to MERCK FROSST CANADA LTD. reassignment MERCK FROSST CANADA LTD. Alteration of Name(s) in Register under S187 Assignors: MERCK FROSST CANADA & CO.
Assigned to MERCK CANADA INC. reassignment MERCK CANADA INC. Request to Amend Deed and Register Assignors: MERCK FROSST CANADA LTD.
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
AU61432/00A 1999-07-19 2000-07-17 Pyrazinones, compositions containing such compounds Expired AU773317B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US14446699P 1999-07-19 1999-07-19
US60/144466 1999-07-19
US17061499P 1999-12-14 1999-12-14
US60/170614 1999-12-14
PCT/CA2000/000833 WO2001005772A1 (en) 1999-07-19 2000-07-17 Pyrazinones, compositions containing such compounds

Publications (2)

Publication Number Publication Date
AU6143200A AU6143200A (en) 2001-02-05
AU773317B2 true AU773317B2 (en) 2004-05-20

Family

ID=26842025

Family Applications (1)

Application Number Title Priority Date Filing Date
AU61432/00A Expired AU773317B2 (en) 1999-07-19 2000-07-17 Pyrazinones, compositions containing such compounds

Country Status (9)

Country Link
US (2) US6444811B1 (cg-RX-API-DMAC10.html)
EP (1) EP1202976B1 (cg-RX-API-DMAC10.html)
JP (1) JP4749640B2 (cg-RX-API-DMAC10.html)
AT (1) ATE344249T1 (cg-RX-API-DMAC10.html)
AU (1) AU773317B2 (cg-RX-API-DMAC10.html)
CA (1) CA2378834C (cg-RX-API-DMAC10.html)
DE (1) DE60031686T2 (cg-RX-API-DMAC10.html)
ES (1) ES2274795T3 (cg-RX-API-DMAC10.html)
WO (1) WO2001005772A1 (cg-RX-API-DMAC10.html)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE344249T1 (de) * 1999-07-19 2006-11-15 Merck Frosst Canada Ltd Pyrazinone, diese verbindungen enthaltende zusammenstellungen
US20020155172A1 (en) * 2000-04-07 2002-10-24 Junying Yuan Methods and compounds for decreasing cell toxicity or death
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
AU2002246065A1 (en) * 2001-01-26 2002-08-06 Evotec Oai Ag Methods and means for detecting enzymatic cleavage and linkage reactions
FR2827288B1 (fr) * 2001-07-12 2003-10-31 Servier Lab Nouveaux derives d'octahydro-2h-pyrido[1,2-a]pyrazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP1485107A1 (en) 2002-02-11 2004-12-15 Vertex Pharmaceuticals Incorporated Phospholipids as caspase inhibitor prodrugs
EP1499898A2 (en) * 2002-04-19 2005-01-26 Vertex Pharmaceuticals Incorporated Regulation of tnf-alpha
CA2526467C (en) 2003-05-20 2015-03-03 Kagutech Ltd. Digital backplane recursive feedback control
AU2005223767B2 (en) * 2004-03-12 2011-12-01 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
CN1980658A (zh) 2004-05-27 2007-06-13 沃泰克斯药物股份有限公司 治疗自身炎性疾病的ice抑制剂
KR20080038369A (ko) 2005-07-28 2008-05-06 버텍스 파마슈티칼스 인코포레이티드 카스파제 억제제 프로드럭
KR20080042286A (ko) * 2006-11-09 2008-05-15 주식회사 엘지생명과학 피리다지논 구조를 포함하는 캐스파제 저해제
MY148484A (en) 2007-08-03 2013-04-30 Sanofi Aventis Caspase imaging probes
EP2262783A2 (en) * 2008-02-21 2010-12-22 Sanofi-Aventis Covalently binding imaging probes
JP6006908B2 (ja) 2010-11-05 2016-10-12 ブランダイス ユニバーシティＢｒａｎｄｅｉｓ Ｕｎｉｖｅｒｓｉｔｙ Ｉｃｅ阻害化合物およびその使用
CN109180690A (zh) * 2018-10-15 2019-01-11 烟台显华化工科技有限公司 一类用作蓝色荧光材料的氮杂芳香化合物及其应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
PL329441A1 (en) * 1996-04-23 1999-03-29 Merck & Co Inc Pyrasinone-type thrombin inhibitors
US5981546A (en) * 1996-08-29 1999-11-09 Merck & Co., Inc. Integrin antagonists
JP2002511052A (ja) 1996-08-29 2002-04-09 メルク エンド カンパニー インコーポレーテッド インテグリンアンタゴニスト
BR9712000A (pt) * 1996-09-06 1999-08-24 Nippon Kayaku Kk Derivados de acetamida sais dos mesmos composi-Æo farmac-utica inibidores de protease de quimase de desgranula-Æo de mastÄcitos ou de libera-Æo de histamina de mastÄcitos e de ativa-Æo de eosinÄfilo ou de libera-Æo de oxig-nio ativo de eosinÄfilo e processo para produzir os dervados de acetamida
AU728006B2 (en) 1997-03-24 2001-01-04 Merck & Co., Inc. Thrombin inhibitors
US5866573A (en) 1997-04-21 1999-02-02 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1017393A4 (en) 1997-09-05 2002-01-23 Merck & Co Inc PYRAZINONE THROMBINE INHIBITORS
ATE344249T1 (de) * 1999-07-19 2006-11-15 Merck Frosst Canada Ltd Pyrazinone, diese verbindungen enthaltende zusammenstellungen

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
6444811 *

Also Published As

Publication number Publication date
DE60031686D1 (de) 2006-12-14
ES2274795T3 (es) 2007-06-01
WO2001005772A1 (en) 2001-01-25
JP2003505378A (ja) 2003-02-12
DE60031686T2 (de) 2007-08-30
JP4749640B2 (ja) 2011-08-17
CA2378834C (en) 2009-07-07
EP1202976B1 (en) 2006-11-02
CA2378834A1 (en) 2001-01-25
ATE344249T1 (de) 2006-11-15
US20030236402A1 (en) 2003-12-25
EP1202976A1 (en) 2002-05-08
US6444811B1 (en) 2002-09-03
AU6143200A (en) 2001-02-05
US6699856B2 (en) 2004-03-02

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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired