JP4978464B2 - Vap−1阻害剤活性を有するチアゾール誘導体 - Google Patents

Vap−1阻害剤活性を有するチアゾール誘導体 Download PDF

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Publication number
JP4978464B2
JP4978464B2 JP2007504792A JP2007504792A JP4978464B2 JP 4978464 B2 JP4978464 B2 JP 4978464B2 JP 2007504792 A JP2007504792 A JP 2007504792A JP 2007504792 A JP2007504792 A JP 2007504792A JP 4978464 B2 JP4978464 B2 JP 4978464B2
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Prior art keywords
thiazol
ethyl
amino
phenyl
methyl
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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
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JP2007504792A
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Japanese (ja)
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JP2008508188A5 (cg-RX-API-DMAC7.html
JP2008508188A (ja
Inventor
隆幸 井上
隆 東條
真正 森田
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Astellas Pharma Inc
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Astellas Pharma Inc
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Priority claimed from AU2004904196A external-priority patent/AU2004904196A0/en
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Publication of JP2008508188A5 publication Critical patent/JP2008508188A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/38Nitrogen atoms
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • 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
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    • AHUMAN NECESSITIES
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P37/00Drugs for immunological or allergic disorders
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    • 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
    • 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
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2007504792A 2004-07-27 2005-07-27 Vap−1阻害剤活性を有するチアゾール誘導体 Expired - Fee Related JP4978464B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AU2004904196A AU2004904196A0 (en) 2004-07-27 Thiazole Derivatives Having VAP-1 Inhibitory Activity
AU2004904196 2004-07-27
PCT/JP2005/014136 WO2006011631A2 (en) 2004-07-27 2005-07-27 Thiazole derivatives having vap-1 inhibitory activity

Publications (3)

Publication Number Publication Date
JP2008508188A JP2008508188A (ja) 2008-03-21
JP2008508188A5 JP2008508188A5 (cg-RX-API-DMAC7.html) 2008-08-14
JP4978464B2 true JP4978464B2 (ja) 2012-07-18

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JP2007504792A Expired - Fee Related JP4978464B2 (ja) 2004-07-27 2005-07-27 Vap−1阻害剤活性を有するチアゾール誘導体

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Country Link
US (1) US20070254931A1 (cg-RX-API-DMAC7.html)
EP (1) EP1786792B1 (cg-RX-API-DMAC7.html)
JP (1) JP4978464B2 (cg-RX-API-DMAC7.html)
KR (1) KR20070050932A (cg-RX-API-DMAC7.html)
CN (1) CN101031555A (cg-RX-API-DMAC7.html)
AT (1) ATE427941T1 (cg-RX-API-DMAC7.html)
CA (1) CA2575411A1 (cg-RX-API-DMAC7.html)
DE (1) DE602005013793D1 (cg-RX-API-DMAC7.html)
ES (1) ES2324922T3 (cg-RX-API-DMAC7.html)
WO (1) WO2006011631A2 (cg-RX-API-DMAC7.html)

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JP5369257B2 (ja) 2006-02-15 2013-12-18 アッヴィ・インコーポレイテッド 新規なアセチル−CoAカルボキシラーゼ(ACC)阻害薬およびそれらの糖尿病、肥満および代謝症候群での使用
CA2641766A1 (en) * 2006-02-15 2007-08-23 Abbott Laboratories Novel acetyl-coa carboxylase (acc) inhibitors and their use in diabetes, obesity and metabolic syndrome
TW200913999A (en) 2007-06-25 2009-04-01 R Tech Ueno Ltd Composition for eye diseases acompany hypoxia or ischemia
CN103120690A (zh) * 2007-10-19 2013-05-29 株式会社·R-技术上野 用于治疗白内障的药物组合物
WO2009061830A1 (en) * 2007-11-06 2009-05-14 Massachusetts Eye & Ear Infirmary Methods and compositions for treating conditions associated with angiogenesis using a vascular adhesion protein-1 (vap-1) inhibitor
EP2240468B1 (en) * 2008-01-18 2013-10-16 Allergan, Inc. Selective subtype alpha 2 adrenergic agents and methods for use thereof
TWI437986B (zh) 2008-01-31 2014-05-21 R Tech Ueno Ltd 噻唑衍生物及使用該衍生物作為vap-1抑制劑之用途
TWI490214B (zh) * 2008-05-30 2015-07-01 艾德克 上野股份有限公司 苯或噻吩衍生物及該等作為vap-1抑制劑之用途
NZ592603A (en) * 2008-10-21 2013-02-22 Metabolex Inc Aryl gpr120 receptor agonists and uses thereof
UA112154C2 (uk) 2009-09-08 2016-08-10 Біоті Терапіс Корп. Застосування повністю людського анти-vap-1-антитіла для лікування фіброзних станів
FI20115234A0 (fi) 2011-03-08 2011-03-08 Biotie Therapies Corp Uusia pyridatsinoni- ja pyridoniyhdisteitä
UA110515C2 (ru) 2011-03-15 2016-01-12 Astellas Pharma Inc Гуанідинова сполука
WO2013057944A1 (ja) 2011-10-19 2013-04-25 興和株式会社 新規なスピロインドリン化合物、及びそれを含有する医薬
CA2915163A1 (en) 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors
HUE042625T2 (hu) 2014-04-15 2019-07-29 Pecsi Tudomanyegyetem Szemikarbazid-szenzitiv amin-oxidáz gátlók fájdalomcsillapítóként való alkalmazásra traumás neuropátiában és neurogén gyulladásban
WO2015189534A1 (en) 2014-06-12 2015-12-17 Proximagen Limited Vap-1 inhibitors for treating muscular dystrophy
CN104478828B (zh) * 2014-12-10 2016-07-06 漳州片仔癀药业股份有限公司 2-氨基-7-取代苯并噻唑类化合物及其制备方法与用途
JOP20200093A1 (ar) 2015-01-09 2017-06-16 Kyowa Kirin Co Ltd طريقة لإنتاج مشتق ثيازول
JP2018076236A (ja) 2015-06-05 2018-05-17 株式会社アールテック・ウエノ がんを処置するための医薬組成物
EP3333163A4 (en) 2015-08-06 2019-01-09 UBE Industries, Ltd. SUBSTITUTED GUANIDINE DERIVATIVE
AU2016366635A1 (en) 2015-12-07 2018-06-21 Benevolentai Cambridge Limited VAP-1 inhibitors for treating pain
KR20190003995A (ko) * 2016-05-12 2019-01-10 베링거 인겔하임 인터내셔날 게엠베하 피리디닐 유도체, 약제학적 조성물 및 이의 aoc3 저해제로서의 용도
KR102607007B1 (ko) * 2016-12-28 2023-11-29 유비이 가부시키가이샤 치환 구아니딘 화합물
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Publication number Publication date
KR20070050932A (ko) 2007-05-16
DE602005013793D1 (de) 2009-05-20
EP1786792B1 (en) 2009-04-08
WO2006011631A2 (en) 2006-02-02
CN101031555A (zh) 2007-09-05
ES2324922T3 (es) 2009-08-19
WO2006011631A3 (en) 2006-04-20
EP1786792A2 (en) 2007-05-23
US20070254931A1 (en) 2007-11-01
CA2575411A1 (en) 2006-02-02
ATE427941T1 (de) 2009-04-15
JP2008508188A (ja) 2008-03-21

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