JP4510442B2 - TNF−α発現のN−ヘテロ環インヒビター - Google Patents

TNF−α発現のN−ヘテロ環インヒビター Download PDF

Info

Publication number
JP4510442B2
JP4510442B2 JP2003508925A JP2003508925A JP4510442B2 JP 4510442 B2 JP4510442 B2 JP 4510442B2 JP 2003508925 A JP2003508925 A JP 2003508925A JP 2003508925 A JP2003508925 A JP 2003508925A JP 4510442 B2 JP4510442 B2 JP 4510442B2
Authority
JP
Japan
Prior art keywords
methyl
dimethyl
mmol
alkyl
ylamino
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 - Fee Related
Application number
JP2003508925A
Other languages
English (en)
Japanese (ja)
Other versions
JP2004535447A (ja
JP2004535447A5 (enExample
Inventor
グルザール・アーメッド
アクセル・メッツガー
スティーブン・ティ・ロブルスキー
イアン・ヘンダーソン
ジェイムズ・ウェン
デイビッド・ジェイ・ディラー
カテリナ・レフセリス
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb 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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of JP2004535447A publication Critical patent/JP2004535447A/ja
Publication of JP2004535447A5 publication Critical patent/JP2004535447A5/ja
Application granted granted Critical
Publication of JP4510442B2 publication Critical patent/JP4510442B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • C07D213/85Nitriles in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50Three nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
JP2003508925A 2001-06-26 2002-06-26 TNF−α発現のN−ヘテロ環インヒビター Expired - Fee Related JP4510442B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30102001P 2001-06-26 2001-06-26
PCT/US2002/020341 WO2003002544A1 (en) 2001-06-26 2002-06-26 N-heterocyclic inhibitors of tnf-alpha expression

Publications (3)

Publication Number Publication Date
JP2004535447A JP2004535447A (ja) 2004-11-25
JP2004535447A5 JP2004535447A5 (enExample) 2006-01-05
JP4510442B2 true JP4510442B2 (ja) 2010-07-21

Family

ID=23161582

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003508925A Expired - Fee Related JP4510442B2 (ja) 2001-06-26 2002-06-26 TNF−α発現のN−ヘテロ環インヒビター

Country Status (7)

Country Link
US (3) US20030139435A1 (enExample)
EP (1) EP1406875B1 (enExample)
JP (1) JP4510442B2 (enExample)
AU (1) AU2002316421B2 (enExample)
CA (1) CA2451128A1 (enExample)
HU (1) HUP0401711A3 (enExample)
WO (1) WO2003002544A1 (enExample)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7037916B2 (en) * 1999-07-15 2006-05-02 Pharmacopeia Drug Discovery, Inc. Pyrimidine derivatives as IL-8 receptor antagonists
GB0016877D0 (en) * 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
US6867300B2 (en) * 2000-11-17 2005-03-15 Bristol-Myers Squibb Company Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors
US6670357B2 (en) * 2000-11-17 2003-12-30 Bristol-Myers Squibb Company Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
JP4510442B2 (ja) * 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー TNF−α発現のN−ヘテロ環インヒビター
NZ531854A (en) * 2001-11-01 2006-03-31 Janssen Pharmaceutica Nv Aminobenzamide derivatives as glycogen synthase kinase 3beta inhibitors
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
DE60325469D1 (de) 2002-04-23 2009-02-05 Bristol Myers Squibb Co Als kinase inhibitoren geeignete arylketonpyrrolotriazin-verbindungen
BR0309669A (pt) * 2002-04-23 2005-03-01 Bristol Myers Squibb Co Compostos de anilina de pirrolo-triazina úteis como inibidores de cinase
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
CN1717396A (zh) * 2002-11-28 2006-01-04 舍林股份公司 Chk-、Pdk-和Akt-抑制嘧啶,其制备及作为药物的用途
US6909001B2 (en) 2002-12-12 2005-06-21 Pharmacia Corporation Method of making tricyclic aminocyanopyridine compounds
CA2508780A1 (en) * 2002-12-12 2004-07-01 Pharmacia Corporation Method of using aminocyanopyridine compounds as mitogen activated protein kinase-activated protein kinase-2 inhibitors
WO2004069829A1 (en) * 2003-01-10 2004-08-19 Pharmacopeia Drug Discovery, Inc. (2s)-2-((pyrimidin-4-yl)amino)-4-methylpentanoic acid aminoethylamid derivatives as il-8 receptor modulators for the treatment of atherosclerosis and rheumatoid arthritis
EP1927594A1 (en) * 2003-01-14 2008-06-04 Arena Pharmaceuticals, Inc. 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
BRPI0406761A (pt) * 2003-01-14 2005-12-20 Arena Pharm Inc Derivados de arila e heteroarila 1,2,3-trissubstituìdos como moduladores do metabolismo e a profilaxia e tratamento de distúrbios relacionados a estes tais como diabetes e hiper-glicemia
UA92450C2 (ru) * 2003-01-14 2010-11-10 Арена Фармасьютикалз, Инк. 1,2,3-тризамещенные арильные и гетероарильные производные как модуляторы метаболизма, профилактика и лечение расстройств, связанных с ним, таких как диабет и гипергликемия
KR20050099525A (ko) 2003-02-05 2005-10-13 브리스톨-마이어스 스큅 컴퍼니 피롤로트리아진 키나제 억제제의 제조 방법
US20050014753A1 (en) * 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
ATE522525T1 (de) * 2003-05-01 2011-09-15 Bristol Myers Squibb Co Arylsubstituierte pyrazolamidverbindungen, die als kinase-inhibitoren von nutzen sind
WO2005000298A2 (en) * 2003-06-03 2005-01-06 Novartis Ag 5-membered heterocycle-based p-38 inhibitors
US7465738B2 (en) 2003-06-16 2008-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as promoters of SMN2
US7504396B2 (en) * 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
AR045047A1 (es) * 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
US8178671B2 (en) 2003-07-30 2012-05-15 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds
PT2287156E (pt) * 2003-08-15 2013-08-26 Novartis Ag 2,4-di(fenilamino)-pirimidinas úteis no tratamento de doenças neoplásicas, desordens inflamatórias e do sistema imunitário
PE20050483A1 (es) 2003-10-31 2005-08-25 Arena Pharm Inc Derivados de tetrazol de formula (i), sus composiciones farmaceuticas y procesos para producir composiciones farmaceuticas
EP1687274A1 (en) * 2003-11-20 2006-08-09 Warner-Lambert Company LLC Androgen receptor modulators
US7459562B2 (en) * 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
JP4812763B2 (ja) 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ, インコーポレイテッド シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
EP1598343A1 (de) * 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
MXPA06014129A (es) * 2004-06-04 2007-03-07 Arena Pharm Inc Derivados de arilo y heteroarilo sustituidos como moduladores del metabolismo y profilaxis y tratamiento de trastornos relacionados con los mismos.
US7253167B2 (en) * 2004-06-30 2007-08-07 Bristol-Myers Squibb Company Tricyclic-heteroaryl compounds useful as kinase inhibitors
TW200600513A (en) * 2004-06-30 2006-01-01 Bristol Myers Squibb Co A method for preparing pyrrolotriazine compounds
US7504521B2 (en) * 2004-08-05 2009-03-17 Bristol-Myers Squibb Co. Methods for the preparation of pyrrolotriazine compounds
TW200618803A (en) 2004-08-12 2006-06-16 Bristol Myers Squibb Co Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors
CA2581454A1 (en) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
AU2005289426A1 (en) * 2004-09-27 2006-04-06 Amgen Inc. Substituted heterocyclic compounds and methods of use
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
EP1814878B1 (en) 2004-11-24 2012-01-04 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
MY148521A (en) * 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
EP1856135B1 (en) 2005-01-19 2009-12-09 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US20060247263A1 (en) * 2005-04-19 2006-11-02 Amgen Inc. Substituted heterocyclic compounds and methods of use
US8153791B2 (en) * 2005-12-21 2012-04-10 Janssen Pharmaceutica N.V. Substituted pyrimidinyl oxime kinase inhibitors
US8278446B2 (en) * 2005-12-21 2012-10-02 Janssen Pharmaceutica N.V. Process for preparing substituted diaminopyrimidine oximes
WO2007081630A2 (en) * 2005-12-21 2007-07-19 Janssen Pharmaceutica, N.V. Substituted pyrimidinyl kinase inhibitors
WO2007109783A2 (en) * 2006-03-23 2007-09-27 Janssen Pharmaceutica, N.V. Substituted pyrimidine kinase inhibitors
JP2009545592A (ja) 2006-07-31 2009-12-24 プリーシス・ファーマシューティカルズ・インコーポレイテッド コード化小分子ライブラリーからのオーロラキナーゼ阻害剤
US8119798B2 (en) 2006-08-01 2012-02-21 Glaxosmithkline Llc P38 kinase inhibitors
ES2633318T3 (es) 2006-10-23 2017-09-20 Cephalon, Inc. Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met
US20100137398A1 (en) * 2007-05-04 2010-06-03 Novartis Ag Use of hdac inhibitors for the treatment of gastrointestinal cancers
BRPI0814432A2 (pt) * 2007-07-17 2017-05-09 Rigel Pharmaceuticals Inc pirimidinadiaminas substituídas por amina cíclica como inibidores de pkc
PT2203173E (pt) 2007-10-26 2016-03-15 Academisch Ziekenhuis Leiden Resumo
AU2009215430B2 (en) * 2008-02-22 2015-02-12 Rigel Pharmaceuticals, Inc. Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis
EP2119783A1 (en) 2008-05-14 2009-11-18 Prosensa Technologies B.V. Method for efficient exon (44) skipping in Duchenne Muscular Dystrophy and associated means
US20110245156A1 (en) * 2008-12-09 2011-10-06 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
AT509266B1 (de) * 2009-12-28 2014-07-15 Univ Wien Tech Substituierte pyridine und pyrimidine
MX2012008141A (es) * 2010-01-13 2012-08-03 Glaxosmithkline Llc Compuestos y metodos.
MX2012014158A (es) 2010-06-04 2013-02-07 Hoffmann La Roche Derivados de aminopirimidina como moduladores de proteina cinasa rica repeticiones leucina 2 (lrrk2).
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
PH12013500880A1 (en) 2010-11-10 2013-07-01 Hoffmann La Roche Pyrazole aminopyrimidine derivatives as lrrk2 modulators
CA2862628C (en) 2012-01-27 2021-08-24 Prosensa Technologies B.V. Rna modulating oligonucleotides with improved characteristics for the treatment of duchenne and becker muscular dystrophy
CN102952084A (zh) * 2012-11-15 2013-03-06 大连九信生物化工科技有限公司 一种4,6-二氯-2-甲硫基-5-硝基嘧啶的合成方法
AU2014369031A1 (en) 2013-12-20 2016-07-07 Signal Pharmaceuticals, Llc Substituted Diaminopyrimidyl Compounds, compositions thereof, and methods of treatment therewith
AU2016205361C1 (en) 2015-01-06 2021-04-08 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
CA3002551A1 (en) 2015-06-22 2016-12-29 Arena Pharmaceuticals, Inc. Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(com pound 1)for use in s1p1 receptor-associated disorders
WO2017151409A1 (en) 2016-02-29 2017-09-08 University Of Florida Research Foundation, Incorporated Chemotherapeutic methods
LT3442947T (lt) * 2016-04-15 2023-09-11 Epizyme, Inc. Aminu pakeisti arilo arba heteroarilo junginiai, kaip ehmt1 ir ehmt2 inhibitoriai
CA3053418A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
JP6722365B1 (ja) * 2017-07-18 2020-07-15 ロンザ リミテッドLonza Limited 塩素化s−プロピル−チオバルビツル酸の製造方法
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CA3127373A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
CA3102136A1 (en) 2018-06-06 2019-12-12 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
PT3966206T (pt) 2019-05-10 2023-11-10 Deciphera Pharmaceuticals Llc Inibidores de autofagia de heteroarilaminopirimidina amida e métodos de utilização dos mesmos
US11530206B2 (en) 2019-05-10 2022-12-20 Deciphera Pharmaceuticals, Llc Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
JP7626722B2 (ja) 2019-06-17 2025-02-04 デシフェラ・ファーマシューティカルズ,エルエルシー アミノピリミジンアミドオートファジー阻害剤およびその使用方法

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6110563A (ja) * 1984-06-25 1986-01-18 Hokuriku Seiyaku Co Ltd ピリミジルアミノフエニルプロピオン酸誘導体
GR900100380A (el) * 1989-05-20 1991-10-10 Fisons Plc Μέ?οδος παρασκευής αντι-φλεγμονωδών παραγώγων αμινοφενόλης.
CZ101496A3 (en) 1993-10-12 1996-11-13 Du Pont Merck Pharma N-alkyl-n-aryl-pyrimidinamines and derivatives thereof
DE19651213A1 (de) * 1996-12-10 1998-08-06 Dystar Textilfarben Gmbh & Co Wasserlösliche faserreaktive Farbstoffe, Verfahren zu ihrer Herstellung und ihre Verwendung
DE19715603A1 (de) * 1997-04-15 1998-10-22 Dystar Textilfarben Gmbh & Co Azofarbstoffe, Verfahren zu ihrer Herstellung und ihre Verwendung
MY132496A (en) * 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
WO2001019825A1 (en) * 1999-09-15 2001-03-22 Warner-Lambert Company Pteridinones as kinase inhibitors
GB9924092D0 (en) 1999-10-13 1999-12-15 Zeneca Ltd Pyrimidine derivatives
AU1212501A (en) * 1999-10-21 2001-04-30 Merck & Co., Inc. Gram-positive selective antibacterial compounds, compositions containing such compounds and methods of treatment
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
CA2396693A1 (en) * 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0007371D0 (en) * 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
KR100847169B1 (ko) * 2000-12-21 2008-07-17 글락소 그룹 리미티드 혈관형성 조절제로서의 피리미딘아민
CA2449118A1 (en) * 2001-05-29 2002-12-05 Schering Aktiengesellschaft Cdk inhibiting pyrimidines, production thereof and their use as medicaments
JP4510442B2 (ja) * 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー TNF−α発現のN−ヘテロ環インヒビター
EP2090571B1 (de) * 2001-10-17 2012-05-16 Boehringer Ingelheim Pharma GmbH & Co. KG Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung
EP1453516A2 (de) * 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses

Also Published As

Publication number Publication date
WO2003002544A1 (en) 2003-01-09
US20060276488A1 (en) 2006-12-07
JP2004535447A (ja) 2004-11-25
EP1406875A4 (en) 2005-05-04
EP1406875B1 (en) 2013-07-31
US20080015185A1 (en) 2008-01-17
US8044040B2 (en) 2011-10-25
AU2002316421B2 (en) 2008-05-15
HUP0401711A3 (en) 2009-07-28
US7253174B2 (en) 2007-08-07
US20030139435A1 (en) 2003-07-24
CA2451128A1 (en) 2003-01-09
HUP0401711A2 (hu) 2004-12-28
EP1406875A1 (en) 2004-04-14

Similar Documents

Publication Publication Date Title
JP4510442B2 (ja) TNF−α発現のN−ヘテロ環インヒビター
AU2002316421A1 (en) N-heterocyclic inhibitors of TNF-ALPHA expression
JP4794793B2 (ja) N−ヘテロ環TNF−α発現阻害剤
US7615552B2 (en) Fused heterocyclic compounds
US6906067B2 (en) N-heterocyclic inhibitors of TNF-α expression
US20020065270A1 (en) N-heterocyclic inhibitors of TNF-alpha expression
US20060069110A1 (en) Substituted heterocyclic compounds and methods of use
JP2007500129A (ja) p−38キナーゼ阻害剤
JP5237115B2 (ja) 新規複素環類
EP1689403A2 (en) Heteroaryl-hydrazone compounds
US7037916B2 (en) Pyrimidine derivatives as IL-8 receptor antagonists
Stanetty et al. Synthesis of analogs of the phenylamino-pyrimidine type protein kinase C inhibitor CGP 60474 utilizing a Negishi cross-coupling strategy
BG65128B1 (bg) Заместени пирамидинови съединения и тяхното използване
EP1409463B1 (en) N-heterocyclic inhibitors of tnf-alpha expression
AU2002312590A1 (en) N-heterocyclic inhibitors of TNF-alpha expression
KR20000069328A (ko) 치환된 피리미딘 화합물과 그것의 용도
JPS59227866A (ja) 2,4−ジアルコキシ−6−ヒドロキシピリミジン類の製造法

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20050613

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20050613

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090407

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090615

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090622

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090730

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20090917

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20091027

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A712

Effective date: 20100215

RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20100222

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100223

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20100215

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20100405

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: 20100427

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: 20100430

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

Free format text: PAYMENT UNTIL: 20130514

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

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

Free format text: PAYMENT UNTIL: 20130514

Year of fee payment: 3

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees