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WO2008093674A1 - キナーゼ阻害活性を有する新規チアジアゾール誘導体 - Google Patents

キナーゼ阻害活性を有する新規チアジアゾール誘導体 Download PDF

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Publication number
WO2008093674A1
WO2008093674A1 PCT/JP2008/051308 JP2008051308W WO2008093674A1 WO 2008093674 A1 WO2008093674 A1 WO 2008093674A1 JP 2008051308 W JP2008051308 W JP 2008051308W WO 2008093674 A1 WO2008093674 A1 WO 2008093674A1
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French (fr)
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Takahiro Honda
Koushi Fujisawa
Hiroyuki Aono
Masakazu Ban
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Santen Pharmaceutical Co Ltd
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Santen Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

　式(I)で表される化合物又はその塩。式中、環Ａはベンゼン環、チオフェン環又はピリジン環を示し；Ｒａは水素原子、ハロゲン原子、アルキル基又はアルコキシ基を示し；環Ｂはピリジン環、ピリミジン環、ベンゼン環又はキノリン環を示し；Ｒ１は水素原子、ハロゲン原子、アミノ基、アルキル基、カルボキシル基等を示し；ＺはＣＨ２又は酸素原子を示し；Ｗは単結合、ＮＨ又は酸素原子を示し；Ｒｂは水素原子、アルキル基又はアリール基を示し；環Ｃはベンゼン環、ピリジン環、キノリン環又はイソキノリン環を示し；Ｒ２とＲ２’は同一又は異なって水素原子、ハロゲン原子、ニトロ基、アミノ基、アルキル基等を示す。 　【化１】
PCT/JP2008/051308 2007-01-29 2008-01-29 キナーゼ阻害活性を有する新規チアジアゾール誘導体 Ceased WO2008093674A1 (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2007-018059 2007-01-29
JP2007018059 2007-01-29
JP2007-083153 2007-03-28
JP2007083153 2007-03-28

Publications (1)

Publication Number Publication Date
WO2008093674A1 true WO2008093674A1 (ja) 2008-08-07

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Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/JP2008/051308 Ceased WO2008093674A1 (ja) 2007-01-29 2008-01-29 キナーゼ阻害活性を有する新規チアジアゾール誘導体
PCT/JP2008/051312 Ceased WO2008093677A1 (ja) 2007-01-29 2008-01-29 血管新生阻害活性を有する新規オキサジアゾール誘導体およびチアジアゾール誘導体

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PCT/JP2008/051312 Ceased WO2008093677A1 (ja) 2007-01-29 2008-01-29 血管新生阻害活性を有する新規オキサジアゾール誘導体およびチアジアゾール誘導体

Country Status (7)

Country Link
US (1) US8063034B2 (ja)
EP (1) EP2128156A4 (ja)
JP (2) JP5216341B2 (ja)
KR (1) KR101475540B1 (ja)
CN (2) CN103224493A (ja)
CA (1) CA2676163A1 (ja)
WO (2) WO2008093674A1 (ja)

Cited By (6)

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JP5146623B2 (ja) * 2011-03-18 2013-02-20 東洋紡株式会社 フレキシブルブーツ用ポリエステルブロック共重合体組成物
JP2017071634A (ja) * 2010-03-24 2017-04-13 アミテック セラピューティック ソリューションズ，インク． キナーゼ阻害に役立つ複素環式化合物
US10112935B2 (en) 2015-02-27 2018-10-30 Lycera Corporation Indazolyl thiadiazolamines and related compounds for inhibition of Rho-associated protein kinase and the treatment of disease
WO2018230713A1 (ja) 2017-06-16 2018-12-20 学校法人同志社 カスパーゼ阻害活性を有する化合物、これらの化合物を含む、角膜内皮の症状、障害または疾患を治療または予防するための医薬およびその応用
US10556898B2 (en) 2016-08-26 2020-02-11 Lycera Corporation Indazolyl-1,2,4-thiadiazolamines and related compounds for inhibition of Rho-associated protein kinase and the treatment of disease
US11433090B2 (en) 2017-06-16 2022-09-06 The Doshisha mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof

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DE602006016564D1 (de) * 2005-03-03 2010-10-14 Santen Pharmaceutical Co Ltd Neue cyclische verbindung mit chinolylalkylthiogruppe
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CN102584639B (zh) * 2011-12-22 2013-09-18 山东京博控股股份有限公司 对三氟甲氧基苯胺基甲酰肼的合成方法
JP2013177372A (ja) 2012-01-31 2013-09-09 Santen Pharmaceut Co Ltd 非水性液体組成物
EP2865747B1 (en) * 2012-06-25 2018-08-22 Kyowa Hakko Kirin Co., Ltd. 4,6-hexadecadiene-2,4-dicarboxylic acid derivative
CN103288817A (zh) * 2013-07-02 2013-09-11 天津理工大学 一种基于1,3,4-噻二唑和1,3,4-噁二唑的希夫碱衍生物及其制备方法和应用
CN103408540B (zh) * 2013-08-22 2016-05-18 中国药科大学 2-唑环取代噻吩类plk1抑制剂及其用途及其用途
TW201609145A (zh) 2013-12-25 2016-03-16 參天製藥股份有限公司 注射劑及形成緩釋（ｄｅｐｏｔ）之方法
CN108794460B (zh) * 2018-05-11 2021-05-28 贵州医科大学 一种1,2,4-噁二唑-3,4-二氢喹啉型化合物及其制备方法和用途
CN108774215A (zh) * 2018-08-15 2018-11-09 翟学旭 含氮杂环类衍生物及其在视网膜新生血管疾病中的应用

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Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017071634A (ja) * 2010-03-24 2017-04-13 アミテック セラピューティック ソリューションズ，インク． キナーゼ阻害に役立つ複素環式化合物
US10214513B2 (en) 2010-03-24 2019-02-26 Amitech Therapeutic Solutions, Inc. Heterocyclic compounds useful for kinase inhibition
JP5146623B2 (ja) * 2011-03-18 2013-02-20 東洋紡株式会社 フレキシブルブーツ用ポリエステルブロック共重合体組成物
US10112935B2 (en) 2015-02-27 2018-10-30 Lycera Corporation Indazolyl thiadiazolamines and related compounds for inhibition of Rho-associated protein kinase and the treatment of disease
US10556898B2 (en) 2016-08-26 2020-02-11 Lycera Corporation Indazolyl-1,2,4-thiadiazolamines and related compounds for inhibition of Rho-associated protein kinase and the treatment of disease
WO2018230713A1 (ja) 2017-06-16 2018-12-20 学校法人同志社 カスパーゼ阻害活性を有する化合物、これらの化合物を含む、角膜内皮の症状、障害または疾患を治療または予防するための医薬およびその応用
US11433090B2 (en) 2017-06-16 2022-09-06 The Doshisha mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof
US12343356B2 (en) 2017-06-16 2025-07-01 The Doshisha mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof

Also Published As

Publication number Publication date
US8063034B2 (en) 2011-11-22
JP2008266295A (ja) 2008-11-06
KR101475540B1 (ko) 2014-12-22
EP2128156A4 (en) 2011-05-18
CN101600712A (zh) 2009-12-09
CN103224493A (zh) 2013-07-31
KR20090104087A (ko) 2009-10-05
WO2008093677A1 (ja) 2008-08-07
JP2008266294A (ja) 2008-11-06
US20100016354A1 (en) 2010-01-21
EP2128156A1 (en) 2009-12-02
JP5216341B2 (ja) 2013-06-19
CA2676163A1 (en) 2008-08-07

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