TWI912295B - Ｐｈｄ抑制劑化合物、組成物及使用方法 - Google Patents

Ｐｈｄ抑制劑化合物、組成物及使用方法

Info

Publication number
TWI912295B
TWI912295B TW110109980A TW110109980A TWI912295B TW I912295 B TWI912295 B TW I912295B TW 110109980 A TW110109980 A TW 110109980A TW 110109980 A TW110109980 A TW 110109980A TW I912295 B TWI912295 B TW I912295B
Authority
TW
Taiwan
Prior art keywords
alkyl
compound
group
mmol
pharmaceutically acceptable
Prior art date
Application number
TW110109980A
Other languages
English (en)
Chinese (zh)
Other versions
TW202140442A (zh
Inventor
保羅 Ｅ 佛來明
湯馬士 Ｐ 布雷斯黛爾
杉卡拉 拉烏 雅魯
Original Assignee
美商阿克比治療有限公司
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 美商阿克比治療有限公司 filed Critical 美商阿克比治療有限公司
Publication of TW202140442A publication Critical patent/TW202140442A/zh
Application granted granted Critical
Publication of TWI912295B publication Critical patent/TWI912295B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P1/04—Drugs 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
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D417/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW110109980A 2020-03-20 2021-03-19 Ｐｈｄ抑制劑化合物、組成物及使用方法 TWI912295B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202062992606P 2020-03-20 2020-03-20
US62/992,606 2020-03-20

Publications (2)

Publication Number Publication Date
TW202140442A TW202140442A (zh) 2021-11-01
TWI912295B true TWI912295B (zh) 2026-01-21

Family

ID=75639963

Family Applications (1)

Application Number Title Priority Date Filing Date
TW110109980A TWI912295B (zh) 2020-03-20 2021-03-19 Ｐｈｄ抑制劑化合物、組成物及使用方法

Country Status (15)

Country Link
US (1) US20230159489A1 (https=)
EP (1) EP4121426A1 (https=)
JP (1) JP2023518262A (https=)
KR (1) KR20220156890A (https=)
CN (3) CN121085892A (https=)
AR (1) AR121621A1 (https=)
AU (1) AU2021240044A1 (https=)
BR (1) BR112022018878A2 (https=)
CA (1) CA3176142A1 (https=)
CO (1) CO2022014587A2 (https=)
IL (1) IL296632A (https=)
MX (1) MX2022011392A (https=)
PH (1) PH12022552461A1 (https=)
TW (1) TWI912295B (https=)
WO (1) WO2021188938A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11713298B2 (en) 2018-05-09 2023-08-01 Akebia Therapeutics, Inc. Process for preparing 2-[[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino]acetic acid
WO2021117767A1 (ja) 2019-12-10 2021-06-17 田辺三菱製薬株式会社 含窒素ヘテロアリールカルボキサミド酢酸誘導体の製造方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101213189A (zh) * 2005-04-28 2008-07-02 拜耳医药保健股份公司 4－(吡啶－3－基)－2－(吡啶－2－基)－1,2－二氢－3h－吡唑啉－3－酮衍生物作为用于治疗心血管和血液学疾病的转录因子－脯氨酰－4－羟化酶的特异性抑制剂
TW200833330A (en) * 2006-10-26 2008-08-16 Bayer Healthcare Ag Substituted dihydropyrazolones and their use
WO2008121861A2 (en) * 2007-03-28 2008-10-09 Xenon Pharmaceuticals Inc. Pyrazole and pyrrole compounds useful in treating iron disorders
CN101541785A (zh) * 2006-10-26 2009-09-23 拜耳先灵制药股份公司 取代二氢吡唑啉酮和它们作为hif-脯氨酰-4-羟化酶抑制剂的用途
CN101600710A (zh) * 2006-10-26 2009-12-09 拜耳先灵制药股份公司 取代的二吡啶基二氢吡唑啉酮和它们的应用

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4663327A (en) * 1984-05-23 1987-05-05 Bayer Aktiengesellschaft 1-heteroaryl-4-aryl-pyrazolin-5-ones
DE3443308A1 (de) * 1984-11-28 1986-05-28 Bayer Ag, 5090 Leverkusen 1-heteroaryl-4-aryl-pyrazolin-5-one zur verwendung als arzneimittel
WO2010005851A1 (en) * 2008-07-08 2010-01-14 Xenon Pharmaceuticals Inc. Combination therapy for treating iron disorders
MA32976B1 (fr) * 2008-12-29 2012-01-02 Sanofi Sa Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one, leur preparation et leur application en therapeutique comme activateurs de hif
CA2894399A1 (en) * 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
EA031647B1 (ru) * 2013-03-29 2019-02-28 Такеда Фармасьютикал Компани Лимитед 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd
CN106831735B (zh) * 2017-01-23 2019-10-11 牡丹江医学院 一种治疗骨质疏松的杂环化合物及其制备方法和用途

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101213189A (zh) * 2005-04-28 2008-07-02 拜耳医药保健股份公司 4－(吡啶－3－基)－2－(吡啶－2－基)－1,2－二氢－3h－吡唑啉－3－酮衍生物作为用于治疗心血管和血液学疾病的转录因子－脯氨酰－4－羟化酶的特异性抑制剂
TW200833330A (en) * 2006-10-26 2008-08-16 Bayer Healthcare Ag Substituted dihydropyrazolones and their use
CN101541785A (zh) * 2006-10-26 2009-09-23 拜耳先灵制药股份公司 取代二氢吡唑啉酮和它们作为hif-脯氨酰-4-羟化酶抑制剂的用途
CN101600710A (zh) * 2006-10-26 2009-12-09 拜耳先灵制药股份公司 取代的二吡啶基二氢吡唑啉酮和它们的应用
WO2008121861A2 (en) * 2007-03-28 2008-10-09 Xenon Pharmaceuticals Inc. Pyrazole and pyrrole compounds useful in treating iron disorders

Also Published As

Publication number Publication date
US20230159489A1 (en) 2023-05-25
AU2021240044A1 (en) 2022-11-17
CN121085893A (zh) 2025-12-09
JP2023518262A (ja) 2023-04-28
CN121085892A (zh) 2025-12-09
BR112022018878A2 (pt) 2022-11-29
KR20220156890A (ko) 2022-11-28
CN115515948B (zh) 2025-09-09
CA3176142A1 (en) 2021-09-23
IL296632A (en) 2022-11-01
MX2022011392A (es) 2022-12-15
TW202140442A (zh) 2021-11-01
CN115515948A (zh) 2022-12-23
CO2022014587A2 (es) 2022-10-21
WO2021188938A1 (en) 2021-09-23
AR121621A1 (es) 2022-06-22
PH12022552461A1 (en) 2024-01-22
EP4121426A1 (en) 2023-01-25

Similar Documents

Publication Publication Date Title
CN104822672B (zh) 治疗性化合物和组合物以及其作为pkm2调节剂的用途
CN115605467B (zh) Phd抑制剂化合物、组合物和其用途
JP2015523402A (ja) タンパク質キナーゼ阻害薬
JP2008523103A (ja) Ｅｒｋプロテインキナーゼのピリミジンインヒビターおよびその使用
KR20230043885A (ko) 트리시클릭 헤테로사이클
JP7278945B2 (ja) 抗癌剤としてのベンゾイミダゾール誘導体
TWI912295B (zh) Ｐｈｄ抑制劑化合物、組成物及使用方法
CN106795152B (zh) 蛋白激酶抑制剂
JP2026021443A (ja) Ｐｈｄ阻害剤化合物、組成物、および使用
WO2022063333A1 (zh) 一种嘧啶甲酰胺类化合物及其应用
JP7832179B2 (ja) Ｐｈｄ阻害剤化合物、組成物、及び使用方法
CN104936950B (zh) 1h‑吲哚‑3‑羧酰胺衍生物及其作为p2y12拮抗剂的用途
TWI917364B (zh) Ｐｈｄ抑制劑化合物、組成物及使用方法
BR122025027329A2 (pt) Compostos, composição farmacêutica e uso
TW202529740A (zh) Ｐｈｄ抑制劑化合物、組成物及使用方法
TW202613096A (zh) 氘代的Ｈｅｄｇｅｈｏｇ通路ＳＭＯ受體抑制劑