JP4749640B2 - ピラジノン、このような化合物を含む組成物 - Google Patents

ピラジノン、このような化合物を含む組成物 Download PDF

Info

Publication number
JP4749640B2
JP4749640B2 JP2001511433A JP2001511433A JP4749640B2 JP 4749640 B2 JP4749640 B2 JP 4749640B2 JP 2001511433 A JP2001511433 A JP 2001511433A JP 2001511433 A JP2001511433 A JP 2001511433A JP 4749640 B2 JP4749640 B2 JP 4749640B2
Authority
JP
Japan
Prior art keywords
alkyl
aryl
het
halo
optionally 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.)
Expired - Lifetime
Application number
JP2001511433A
Other languages
English (en)
Japanese (ja)
Other versions
JP2003505378A (ja
JP2003505378A5 (cg-RX-API-DMAC10.html
Inventor
ハン，ヨンシン
ジルー，アンドレ
ザンボニー，ロバート
マツケイ，ダニエル・ジエイ
ベイリー，クリストフアー・アイ
グリム，エリツク・エル
コルツチ，ジヨン
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 Canada 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 Canada Inc filed Critical Merck Canada Inc
Publication of JP2003505378A publication Critical patent/JP2003505378A/ja
Publication of JP2003505378A5 publication Critical patent/JP2003505378A5/ja
Application granted granted Critical
Publication of JP4749640B2 publication Critical patent/JP4749640B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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)
JP2001511433A 1999-07-19 2000-07-17 ピラジノン、このような化合物を含む組成物 Expired - Lifetime JP4749640B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US14446699P 1999-07-19 1999-07-19
US60/144,466 1999-07-19
US17061499P 1999-12-14 1999-12-14
US60/170,614 1999-12-14
PCT/CA2000/000833 WO2001005772A1 (en) 1999-07-19 2000-07-17 Pyrazinones, compositions containing such compounds

Publications (3)

Publication Number Publication Date
JP2003505378A JP2003505378A (ja) 2003-02-12
JP2003505378A5 JP2003505378A5 (cg-RX-API-DMAC10.html) 2007-05-24
JP4749640B2 true JP4749640B2 (ja) 2011-08-17

Family

ID=26842025

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2001511433A Expired - Lifetime JP4749640B2 (ja) 1999-07-19 2000-07-17 ピラジノン、このような化合物を含む組成物

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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995035308A1 (en) * 1994-06-17 1995-12-28 Vertex Pharmaceuticals Incorporated INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995035308A1 (en) * 1994-06-17 1995-12-28 Vertex Pharmaceuticals Incorporated INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME

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
AU773317B2 (en) 2004-05-20
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

Similar Documents

Publication Publication Date Title
JP2529825B2 (ja) 新規なペプチダ−ゼ阻害剤
US6699856B2 (en) Pyrazinones, compositions containing such compounds and methods of use
JPWO1998009949A1 (ja) 新規アセトアミド誘導体およびプロテアーゼ阻害剤
WO2003024955A2 (en) Small molecule inhibitors of caspases
US20030096737A1 (en) Caspase inhibitors and uses thereof
WO1991015487A1 (en) Novel 4h-3,1-benzoxazin-4-one derivative
US6225288B1 (en) Gamma-ketoacid dipeptides as inhibitors of caspase-3
CN102822192B (zh) 作为尘螨1型肽酶变应原抑制剂的丙酮酰胺化合物
CA2266639A1 (en) 3,4-disubstituted azetidin-2-one derivatives useful as cysteine proteinase regulators
JPH08503475A (ja) 抗変性活性剤としてのカルボキシ−ペプチジル誘導体
US8119673B2 (en) Compounds 148
JP2002531464A (ja) カスパーゼ−３阻害薬としてのγ−ケト酸テトラペプチド類
US6525025B2 (en) Gamma-ketoacid dipeptides as inhibitors of caspase-3
US20030045478A1 (en) Gamma-ketoacid dipeptide derivatives as inhibitors of caspase-3
CA2386411A1 (en) Nicotinyl aspartyl ketones as inhibitors of caspase-3
KR20010077201A (ko) 4-하이드록실아미노-3-사이클로부텐-1,2-다이온 유도체 및이들의 제조 방법
HUP9903675A2 (hu) Új acetamid-származékok és proteáz inhibitorok

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20060324

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20070322

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20070322

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100720

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20101020

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110510

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110518

R150 Certificate of patent or registration of utility model

Ref document number: 4749640

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140527

Year of fee payment: 3

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

EXPY Cancellation because of completion of term