JP2023518262A - Ｐｈｄ阻害剤化合物、組成物、及び使用 - Google Patents

Ｐｈｄ阻害剤化合物、組成物、及び使用 Download PDF

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JP2023518262A
JP2023518262A JP2022556196A JP2022556196A JP2023518262A JP 2023518262 A JP2023518262 A JP 2023518262A JP 2022556196 A JP2022556196 A JP 2022556196A JP 2022556196 A JP2022556196 A JP 2022556196A JP 2023518262 A JP2023518262 A JP 2023518262A
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alkyl
compound
cycloalkyl
halogen
optionally substituted
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JP2023518262A5 (https=
Inventor
イー． フレミング ポール
ピー． ブライスデル トーマス
ラオ アッル センカラ
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Akebia Therapeutics Inc
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    • 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

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  • 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)
JP2022556196A 2020-03-20 2021-03-19 Ｐｈｄ阻害剤化合物、組成物、及び使用 Pending JP2023518262A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062992606P 2020-03-20 2020-03-20
US62/992,606 2020-03-20
PCT/US2021/023222 WO2021188938A1 (en) 2020-03-20 2021-03-19 Phd inhibitor compounds, compositions, and use

Publications (2)

Publication Number Publication Date
JP2023518262A true JP2023518262A (ja) 2023-04-28
JP2023518262A5 JP2023518262A5 (https=) 2024-05-24

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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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60255788A (ja) * 1984-05-23 1985-12-17 バイエル・アクチエンゲゼルシヤフト １‐ヘテロアリール‐４‐アリール‐ピラゾリン‐５‐オン
JPS61137878A (ja) * 1984-11-28 1986-06-25 バイエル・アクチエンゲゼルシヤフト 薬剤用１‐ヘテロアリール‐４‐アリール‐ピラゾリン‐５‐オン類
WO2008121861A2 (en) * 2007-03-28 2008-10-09 Xenon Pharmaceuticals Inc. Pyrazole and pyrrole compounds useful in treating iron disorders
JP2010507605A (ja) * 2006-10-26 2010-03-11 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト 置換ジピリジル−ジヒドロピラゾロン類およびそれらの使用
JP2012513976A (ja) * 2008-12-29 2012-06-21 サノフイ ２−ピリジン−２−イル−ピラゾール−３（２ｈ）−オンの誘導体、これらの調製およびｈｉｆ活性化剤としての治療用途
JP2016501882A (ja) * 2012-12-06 2016-01-21 クオンティセル ファーマシューティカルズ，インク． ヒストンデメチラーゼ阻害剤
JP2016515582A (ja) * 2013-03-29 2016-05-30 武田薬品工業株式会社 ６−（５−ヒドロキシ−１ｈ−ピラゾール−１−イル）ニコチンアミド誘導体およびｐｈｄ阻害剤としてのそれらの使用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102005019712A1 (de) * 2005-04-28 2006-11-09 Bayer Healthcare Ag Dipyridyl-dihydropyrazolone und ihre Verwendung
DE102006050516A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dihydropyrazolone und ihre Verwendung
DE102006050513A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substitiuierte Dihydropyrazolone und ihre Verwendung
WO2010005851A1 (en) * 2008-07-08 2010-01-14 Xenon Pharmaceuticals Inc. Combination therapy for treating iron disorders
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 (7)

* Cited by examiner, † Cited by third party
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JPS60255788A (ja) * 1984-05-23 1985-12-17 バイエル・アクチエンゲゼルシヤフト １‐ヘテロアリール‐４‐アリール‐ピラゾリン‐５‐オン
JPS61137878A (ja) * 1984-11-28 1986-06-25 バイエル・アクチエンゲゼルシヤフト 薬剤用１‐ヘテロアリール‐４‐アリール‐ピラゾリン‐５‐オン類
JP2010507605A (ja) * 2006-10-26 2010-03-11 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト 置換ジピリジル−ジヒドロピラゾロン類およびそれらの使用
WO2008121861A2 (en) * 2007-03-28 2008-10-09 Xenon Pharmaceuticals Inc. Pyrazole and pyrrole compounds useful in treating iron disorders
JP2012513976A (ja) * 2008-12-29 2012-06-21 サノフイ ２−ピリジン−２−イル−ピラゾール−３（２ｈ）−オンの誘導体、これらの調製およびｈｉｆ活性化剤としての治療用途
JP2016501882A (ja) * 2012-12-06 2016-01-21 クオンティセル ファーマシューティカルズ，インク． ヒストンデメチラーゼ阻害剤
JP2016515582A (ja) * 2013-03-29 2016-05-30 武田薬品工業株式会社 ６−（５−ヒドロキシ−１ｈ−ピラゾール−１−イル）ニコチンアミド誘導体およびｐｈｄ阻害剤としてのそれらの使用

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Title
BUECHI, J. ET AL.: ""Synthesis and pharmacological properties of certain pyridylpyrazol-5-ones"", HELVETICA CHIMICA ACTA, vol. 49, no. 1, JPN6025005428, 1966, pages 272 - 280, ISSN: 0005525612 *
CADIEUX, J. A. ET AL.: ""Synthesis and biological evaluation of substituted pyrazoles as blockers of divalent metal transpo", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 22, no. 1, JPN6025005429, 2012, pages 90 - 95, ISSN: 0005525611 *

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US20230159489A1 (en) 2023-05-25
AU2021240044A1 (en) 2022-11-17
CN121085893A (zh) 2025-12-09
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
TWI912295B (zh) 2026-01-21

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