JP7604457B2 - ２－ヒドロキシシクロアルカン－１－カルバモイル誘導体 - Google Patents

２－ヒドロキシシクロアルカン－１－カルバモイル誘導体 Download PDF

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Publication number
JP7604457B2
JP7604457B2 JP2022508567A JP2022508567A JP7604457B2 JP 7604457 B2 JP7604457 B2 JP 7604457B2 JP 2022508567 A JP2022508567 A JP 2022508567A JP 2022508567 A JP2022508567 A JP 2022508567A JP 7604457 B2 JP7604457 B2 JP 7604457B2
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triazol
pyran
hydroxymethyl
hydroxycyclohexyl
carboxamide
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Japanese (ja)
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JP2022544248A5 (enExample
JP2022544248A (ja
Inventor
ボリ マーティン
ガットフィールド ジョン
グリソストミ コリンナ
レメン ルボス
ザーガー クリストフ
ツムブルン コルネリア
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Idorsia Pharmaceuticals Ltd
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Idorsia Pharmaceuticals Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12—Triazine radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2022508567A 2019-08-15 2020-08-14 ２－ヒドロキシシクロアルカン－１－カルバモイル誘導体 Active JP7604457B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EPPCT/EP2019/071921 2019-08-15
EP2019071921 2019-08-15
PCT/EP2020/072865 WO2021028570A1 (en) 2019-08-15 2020-08-14 2-hydroxycycloalkane-1-carbamoyl derivatives

Publications (3)

Publication Number Publication Date
JP2022544248A JP2022544248A (ja) 2022-10-17
JP2022544248A5 JP2022544248A5 (enExample) 2023-08-23
JP7604457B2 true JP7604457B2 (ja) 2024-12-23

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JP2022508567A Active JP7604457B2 (ja) 2019-08-15 2020-08-14 ２－ヒドロキシシクロアルカン－１－カルバモイル誘導体

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Country Link
US (1) US12291519B2 (enExample)
EP (1) EP4013751B1 (enExample)
JP (1) JP7604457B2 (enExample)
KR (1) KR102832308B1 (enExample)
CN (1) CN114269737A (enExample)
AU (1) AU2020329609B2 (enExample)
BR (1) BR112021026829A2 (enExample)
CA (1) CA3147454A1 (enExample)
ES (1) ES3015725T3 (enExample)
HR (1) HRP20250372T1 (enExample)
HU (1) HUE070924T2 (enExample)
IL (1) IL289197B2 (enExample)
MA (1) MA56883B1 (enExample)
MX (1) MX2022001789A (enExample)
PH (1) PH12022550338A1 (enExample)
PL (1) PL4013751T3 (enExample)
RS (1) RS66695B1 (enExample)
TW (1) TWI864071B (enExample)
UA (1) UA128909C2 (enExample)
WO (1) WO2021028570A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024506182A (ja) * 2021-02-09 2024-02-09 イドーシア ファーマシューティカルズ リミテッド ヒドロキシヘテロシクロアルカン－カルバモイル誘導体

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CN114206893A (zh) 2019-08-09 2022-03-18 爱杜西亚药品有限公司 (杂)芳基-甲基-硫代-β-D-吡喃半乳糖苷衍生物
WO2021028323A1 (en) 2019-08-09 2021-02-18 Idorsia Pharmaceuticals Ltd (2-acetamidyl)thio-beta-d-galactopyranoside derivatives
CN114585619B (zh) 2019-08-29 2024-09-27 爱杜西亚药品有限公司 α-D-吡喃半乳糖苷衍生物
JP2023508363A (ja) * 2019-12-24 2023-03-02 グリコミメティクス， インコーポレイテッド ガレクチン－３阻害性ｃ－グリコシドケトン、エーテル、およびアルコール
US12312362B2 (en) 2020-10-06 2025-05-27 Idorsia Pharmaceuticals Ltd Spiro derivatives of Alpha-D-galactopyranosides
EP4237419A1 (en) 2020-11-02 2023-09-06 Idorsia Pharmaceuticals Ltd Galectin-3 inhibiting 2-hydroxycycloalkane-1 -carbamoyl derivatives
RS67032B1 (sr) 2021-03-03 2025-08-29 Idorsia Pharmaceuticals Ltd Alfa-d-galaktopiranozidni derivati supstituisani triazolil-metilom
WO2022189459A2 (en) * 2021-03-10 2022-09-15 Galecto Biotech Ab Novel galactoside inhibitor of galectins
JP2024517936A (ja) * 2021-05-14 2024-04-23 グリコミメティクス， インコーポレイテッド ガレクチン－３阻害性ｃ－グリコシド
US20240287121A1 (en) * 2021-05-28 2024-08-29 Glycomimetics, Inc. Galectin-3 inhibiting c-glycoside oximes

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JP2016501849A (ja) 2012-11-15 2016-01-21 タフツ ユニバーシティー ガレクチンタンパク質阻害剤を用いて被験体の眼の血管新生または繊維症を処置し、調節し、または、予防する方法、組成物、およびキット
JP2018503660A (ja) 2015-01-30 2018-02-08 ガレクト・バイオテック・エイビイ ガレクチンの新規なガラクトシド阻害剤
WO2018209276A1 (en) 2017-05-12 2018-11-15 Galectin Sciences, Llc Compounds for the treatment of systemic insulin resistance disorders and the use thereof
WO2019067702A1 (en) 2017-09-27 2019-04-04 Bristol-Myers Squibb Company INHIBITORS WITH SMALL MOLECULES OF GALECTIN-3

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PL3456717T3 (pl) 2015-07-06 2021-10-25 Gilead Sciences, Inc. Pochodna 4,6-diaminochinolino-3-karbonitrylu jako modulator cot (cancer osaka thyroid) do leczenia choroby zapalnej
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JP2022508720A (ja) 2018-10-15 2022-01-19 ガレクト バイオテック エービー ガレクチンのガラクトシド阻害剤
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WO2021004940A1 (en) 2019-07-05 2021-01-14 Galecto Biotech Ab Novel galactoside inhibitor of galectins
WO2021028323A1 (en) 2019-08-09 2021-02-18 Idorsia Pharmaceuticals Ltd (2-acetamidyl)thio-beta-d-galactopyranoside derivatives
CN114206893A (zh) 2019-08-09 2022-03-18 爱杜西亚药品有限公司 (杂)芳基-甲基-硫代-β-D-吡喃半乳糖苷衍生物
CN114585619B (zh) 2019-08-29 2024-09-27 爱杜西亚药品有限公司 α-D-吡喃半乳糖苷衍生物
US12312362B2 (en) 2020-10-06 2025-05-27 Idorsia Pharmaceuticals Ltd Spiro derivatives of Alpha-D-galactopyranosides
EP4237419A1 (en) 2020-11-02 2023-09-06 Idorsia Pharmaceuticals Ltd Galectin-3 inhibiting 2-hydroxycycloalkane-1 -carbamoyl derivatives
CN116806219A (zh) 2021-02-09 2023-09-26 爱杜西亚药品有限公司 羟基杂环烷-氨甲酰基衍生物
RS67032B1 (sr) 2021-03-03 2025-08-29 Idorsia Pharmaceuticals Ltd Alfa-d-galaktopiranozidni derivati supstituisani triazolil-metilom

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005113569A1 (en) 2004-05-21 2005-12-01 Forskapatent I Syd Ab Novel 3-triazolyl-galactoside inhibitors of galectins
JP2016501849A (ja) 2012-11-15 2016-01-21 タフツ ユニバーシティー ガレクチンタンパク質阻害剤を用いて被験体の眼の血管新生または繊維症を処置し、調節し、または、予防する方法、組成物、およびキット
JP2018503660A (ja) 2015-01-30 2018-02-08 ガレクト・バイオテック・エイビイ ガレクチンの新規なガラクトシド阻害剤
WO2018209276A1 (en) 2017-05-12 2018-11-15 Galectin Sciences, Llc Compounds for the treatment of systemic insulin resistance disorders and the use thereof
WO2019067702A1 (en) 2017-09-27 2019-04-04 Bristol-Myers Squibb Company INHIBITORS WITH SMALL MOLECULES OF GALECTIN-3

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024506182A (ja) * 2021-02-09 2024-02-09 イドーシア ファーマシューティカルズ リミテッド ヒドロキシヘテロシクロアルカン－カルバモイル誘導体
JP7844491B2 (ja) 2021-02-09 2026-04-13 イドルシア・ファーマシューティカルズ・リミテッド ヒドロキシヘテロシクロアルカン－カルバモイル誘導体

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AU2020329609A1 (en) 2022-02-24
KR102832308B1 (ko) 2025-07-10
HUE070924T2 (hu) 2025-07-28
CA3147454A1 (en) 2021-02-18
HRP20250372T1 (hr) 2025-06-06
EP4013751A1 (en) 2022-06-22
WO2021028570A1 (en) 2021-02-18
US12291519B2 (en) 2025-05-06
IL289197B1 (en) 2025-10-01
CN114269737A (zh) 2022-04-01
EP4013751C0 (en) 2025-01-22
EP4013751B1 (en) 2025-01-22
RS66695B1 (sr) 2025-05-30
KR20220047585A (ko) 2022-04-18
IL289197B2 (en) 2026-02-01
PH12022550338A1 (en) 2023-02-06
PL4013751T3 (pl) 2025-05-19
BR112021026829A2 (pt) 2022-02-22
IL289197A (en) 2022-02-01
US20220324847A1 (en) 2022-10-13
JP2022544248A (ja) 2022-10-17
TWI864071B (zh) 2024-12-01
AU2020329609B2 (en) 2025-10-02
MX2022001789A (es) 2022-03-11
MA56883B1 (fr) 2025-04-30
UA128909C2 (uk) 2024-11-20
TW202115039A (zh) 2021-04-16
ES3015725T3 (en) 2025-05-07

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