JP6506742B2 - Ｗｎｔ経路モジュレーターとしてのプリンジオン - Google Patents

Ｗｎｔ経路モジュレーターとしてのプリンジオン Download PDF

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Publication number
JP6506742B2
JP6506742B2 JP2016515318A JP2016515318A JP6506742B2 JP 6506742 B2 JP6506742 B2 JP 6506742B2 JP 2016515318 A JP2016515318 A JP 2016515318A JP 2016515318 A JP2016515318 A JP 2016515318A JP 6506742 B2 JP6506742 B2 JP 6506742B2
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thiazol
compound
dioxo
phenyl
dimethyl
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JP2016519165A (ja
JP2016519165A5 (https=
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スー・イェイ・ホ
ステファニー・エリアーヌ・ブランシャール
アティサヤマニ・ジェヤラジ・ドゥライスワミー
ジェネファー・アラム
ヴィクラント・アルン・アドスール
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Agency for Science Technology and Research Singapore
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016515318A 2013-05-23 2014-05-19 Ｗｎｔ経路モジュレーターとしてのプリンジオン Active JP6506742B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1309333.1A GB201309333D0 (en) 2013-05-23 2013-05-23 Purine diones as WNT pathway modulators
GB1309333.1 2013-05-23
PCT/SG2014/000217 WO2014189466A1 (en) 2013-05-23 2014-05-19 Purine diones as wnt pathway modulators

Publications (3)

Publication Number Publication Date
JP2016519165A JP2016519165A (ja) 2016-06-30
JP2016519165A5 JP2016519165A5 (https=) 2017-04-06
JP6506742B2 true JP6506742B2 (ja) 2019-04-24

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JP2016515318A Active JP6506742B2 (ja) 2013-05-23 2014-05-19 Ｗｎｔ経路モジュレーターとしてのプリンジオン

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US (6) US9926320B2 (https=)
EP (1) EP2999699B1 (https=)
JP (1) JP6506742B2 (https=)
KR (2) KR102062262B1 (https=)
CN (2) CN109776537B (https=)
AU (2) AU2014269134B2 (https=)
BR (1) BR112015029182B1 (https=)
CA (1) CA2912757C (https=)
DK (1) DK2999699T3 (https=)
ES (1) ES2802923T3 (https=)
GB (1) GB201309333D0 (https=)
SG (1) SG11201509593TA (https=)
WO (1) WO2014189466A1 (https=)

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GB201309333D0 (en) 2013-05-23 2013-07-10 Agency Science Tech & Res Purine diones as WNT pathway modulators
GB201322334D0 (en) * 2013-12-17 2014-01-29 Agency Science Tech & Res Maleimide derivatives as modulators of WNT pathway
TWI676626B (zh) * 2014-04-23 2019-11-11 美商美國禮來大藥廠 抑制瞬時受體電位ａ１離子通道
HUE049253T2 (hu) * 2014-09-19 2020-09-28 Lilly Co Eli A tranziens receptor potenciál A1 ion csatorna gátlása
CN105440034B (zh) * 2015-11-16 2017-08-15 山东罗欣药业集团股份有限公司 一种利格列汀及其中间体的制备方法
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
CN106632332B (zh) * 2016-09-26 2018-07-06 杭州新博思生物医药有限公司 一种伊曲茶碱的制备方法
CN111247148B (zh) * 2017-09-14 2022-12-20 新加坡科技研究局 Wnt通路调节剂
WO2019152465A1 (en) 2018-01-31 2019-08-08 Eli Lilly And Company Inhibiting the transient receptor potential a1 ion channel
US10961534B2 (en) 2018-07-13 2021-03-30 University of Pittsburgh—of the Commonwealth System of Higher Education Methods of treating porphyria
US12534762B2 (en) 2018-09-28 2026-01-27 Children's Medical Center Corporation Treating atopic dermatitis by targeting the WNT pathway
CN114025764A (zh) * 2019-05-22 2022-02-08 新加坡科技研究局 药物组合
CN114072131B (zh) * 2019-05-22 2024-03-19 新加坡科技研究局 口服制剂、其制备方法及其用途
US12365686B2 (en) * 2019-07-08 2025-07-22 Jiangsu Kanion Pharmaceutical Co., Ltd. Compound as porcupine inhibitor and use thereof
CN115279377A (zh) * 2020-01-08 2022-11-01 新加坡科技研究局 联合疗法
BR112023025403A2 (pt) 2021-06-25 2024-02-20 Korea Res Inst Chemical Tech Composto heterocíclico bifuncional tendo função de degradação de btk por meio da via ubiquitina proteassoma e uso do mesmo
KR20240073960A (ko) * 2021-10-29 2024-05-27 지앙수 카니온 파마수티컬 씨오., 엘티디. 5-치환된 피리딘-2(1h)-케톤계 화합물 및 이의 용도
CN114671875A (zh) * 2022-04-27 2022-06-28 成都施贝康生物医药科技有限公司 新型二氢嘧啶类化合物、异构体或盐及其制备方法和用途
CN120737092B (zh) * 2025-09-05 2025-11-14 利诚检测认证集团股份有限公司 别嘌醇半抗原及其制备方法、人工抗原、抗体及其应用

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GB201309333D0 (en) 2013-05-23 2013-07-10 Agency Science Tech & Res Purine diones as WNT pathway modulators

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JP2016519165A (ja) 2016-06-30
US11555037B2 (en) 2023-01-17
BR112015029182A8 (pt) 2020-03-17
DK2999699T3 (da) 2020-07-13
US20230174533A1 (en) 2023-06-08
SG11201509593TA (en) 2015-12-30
AU2014269134A1 (en) 2015-12-10
GB201309333D0 (en) 2013-07-10
US10472360B2 (en) 2019-11-12
BR112015029182A2 (pt) 2017-07-25
US10844063B2 (en) 2020-11-24
KR102062262B1 (ko) 2020-01-03
US10526335B2 (en) 2020-01-07
US20160090386A1 (en) 2016-03-31
AU2014269134B2 (en) 2017-06-15
US12559495B2 (en) 2026-02-24
US9926320B2 (en) 2018-03-27
AU2017219132B2 (en) 2019-04-18
US20180170932A1 (en) 2018-06-21
EP2999699A4 (en) 2016-10-26
WO2014189466A1 (en) 2014-11-27
US20210155623A1 (en) 2021-05-27
BR112015029182B1 (pt) 2023-10-03
ES2802923T3 (es) 2021-01-21
CN105452248A (zh) 2016-03-30
EP2999699B1 (en) 2020-04-29
CN109776537A (zh) 2019-05-21
US20200190086A1 (en) 2020-06-18
CN109776537B (zh) 2021-12-14
EP2999699A1 (en) 2016-03-30
KR20200000504A (ko) 2020-01-02
KR102153989B1 (ko) 2020-09-09
AU2017219132A1 (en) 2017-09-14
KR20160029024A (ko) 2016-03-14
CA2912757C (en) 2021-11-30
CA2912757A1 (en) 2014-11-27
US20170334912A1 (en) 2017-11-23

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