TWI864071B - 2-羥環烷-1-胺甲醯基衍生物 - Google Patents

2-羥環烷-1-胺甲醯基衍生物 Download PDF

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Publication number
TWI864071B
TWI864071B TW109127800A TW109127800A TWI864071B TW I864071 B TWI864071 B TW I864071B TW 109127800 A TW109127800 A TW 109127800A TW 109127800 A TW109127800 A TW 109127800A TW I864071 B TWI864071 B TW I864071B
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Taiwan
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triazol
hydroxymethyl
hydroxycyclohexyl
pyran
carboxamide
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TW109127800A
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English (en)
Chinese (zh)
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TW202115039A (zh
Inventor
馬汀 波利
約翰 加菲歐
康妮雅 克索湯米
路伯斯 雷曼
克里斯湯佛 撒爵
柯奈利亞 宗布倫
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瑞士商愛杜西亞製藥有限公司
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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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (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)
TW109127800A 2019-08-15 2020-08-14 2-羥環烷-1-胺甲醯基衍生物 TWI864071B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
WOPCT/EP2019/071921 2019-08-15
EP2019071921 2019-08-15

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TW202115039A TW202115039A (zh) 2021-04-16
TWI864071B true TWI864071B (zh) 2024-12-01

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US (1) US12291519B2 (enExample)
EP (1) EP4013751B1 (enExample)
JP (1) JP7604457B2 (enExample)
KR (1) KR102832308B1 (enExample)
CN (1) CN114269737A (enExample)
AU (1) AU2020329609B2 (enExample)
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CA (1) CA3147454A1 (enExample)
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HU (1) HUE070924T2 (enExample)
IL (1) IL289197B2 (enExample)
MA (1) MA56883B1 (enExample)
MX (1) MX2022001789A (enExample)
PH (1) PH12022550338A1 (enExample)
PL (1) PL4013751T3 (enExample)
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TW (1) TWI864071B (enExample)
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KR102863667B1 (ko) 2019-08-09 2025-09-23 이도르시아 파마슈티컬스 리미티드 (2-아세트아미딜)티오-베타-d-갈락토피라노시드 유도체
US12404295B2 (en) 2019-08-09 2025-09-02 Idorsia Pharmaceuticals Ltd (Hetero)aryl-methyl-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
CN115244045A (zh) * 2019-12-24 2022-10-25 糖模拟物有限公司 抑制半乳凝素-3的c-糖苷酮、醚和醇
WO2022073969A1 (en) 2020-10-06 2022-04-14 Idorsia Pharmaceuticals Ltd Spiro derivatives of alpha-d-galactopyranosides
US12291520B2 (en) 2020-11-02 2025-05-06 Idorsia Pharmaceuticals Ltd Galectin-3 inhibiting 2-hydroxycycloalkane-1-carbamoyl derivatives
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
WO2022184755A1 (en) 2021-03-03 2022-09-09 Idorsia Pharmaceuticals Ltd Triazolyl-methyl substituted alpha-d-galactopyranoside derivatives
WO2022189459A2 (en) * 2021-03-10 2022-09-15 Galecto Biotech Ab Novel galactoside inhibitor of galectins
WO2022241183A1 (en) * 2021-05-14 2022-11-17 Glycomimetics, Inc. Galectin-3 inhibiting c-glycosides
WO2022250976A1 (en) * 2021-05-28 2022-12-01 Glycomimetics, Inc. Galectin-3 inhibiting c-glycoside oximes

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CN107406478A (zh) * 2015-01-30 2017-11-28 格莱克特生物技术公司 半乳糖凝集素的α‑D‑半乳糖苷抑制剂
WO2018209276A1 (en) * 2017-05-12 2018-11-15 Galectin Sciences, Llc Compounds for the treatment of systemic insulin resistance disorders and the use thereof

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KR102626669B1 (ko) 2017-05-12 2024-01-17 갈랙틴 사이언시즈, 엘엘씨 질환의 예방 및 치료를 위한 화합물 및 이의 용도
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JP7674276B2 (ja) 2019-07-03 2025-05-09 ガレクト バイオテック エービー ガレクチンの新規なガラクトシド阻害剤
CA3143078A1 (en) 2019-07-05 2021-01-14 Galecto Biotech Ab Novel galactoside inhibitor of galectins
US12404295B2 (en) 2019-08-09 2025-09-02 Idorsia Pharmaceuticals Ltd (Hetero)aryl-methyl-thio-beta-D-galactopyranoside derivatives
KR102863667B1 (ko) 2019-08-09 2025-09-23 이도르시아 파마슈티컬스 리미티드 (2-아세트아미딜)티오-베타-d-갈락토피라노시드 유도체
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
WO2022073969A1 (en) 2020-10-06 2022-04-14 Idorsia Pharmaceuticals Ltd Spiro derivatives of alpha-d-galactopyranosides
US12291520B2 (en) 2020-11-02 2025-05-06 Idorsia Pharmaceuticals Ltd Galectin-3 inhibiting 2-hydroxycycloalkane-1-carbamoyl derivatives
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
WO2022184755A1 (en) 2021-03-03 2022-09-09 Idorsia Pharmaceuticals Ltd Triazolyl-methyl substituted alpha-d-galactopyranoside derivatives

Patent Citations (3)

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WO2005113569A1 (en) * 2004-05-21 2005-12-01 Forskapatent I Syd Ab Novel 3-triazolyl-galactoside inhibitors of galectins
CN107406478A (zh) * 2015-01-30 2017-11-28 格莱克特生物技术公司 半乳糖凝集素的α‑D‑半乳糖苷抑制剂
WO2018209276A1 (en) * 2017-05-12 2018-11-15 Galectin Sciences, Llc Compounds for the treatment of systemic insulin resistance disorders and the use thereof

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US12291519B2 (en) 2025-05-06
PH12022550338A1 (en) 2023-02-06
EP4013751B1 (en) 2025-01-22
EP4013751A1 (en) 2022-06-22
KR20220047585A (ko) 2022-04-18
HRP20250372T1 (hr) 2025-06-06
IL289197B1 (en) 2025-10-01
RS66695B1 (sr) 2025-05-30
MX2022001789A (es) 2022-03-11
HUE070924T2 (hu) 2025-07-28
JP2022544248A (ja) 2022-10-17
MA56883B1 (fr) 2025-04-30
UA128909C2 (uk) 2024-11-20
CA3147454A1 (en) 2021-02-18
TW202115039A (zh) 2021-04-16
KR102832308B1 (ko) 2025-07-10
AU2020329609B2 (en) 2025-10-02
US20220324847A1 (en) 2022-10-13
EP4013751C0 (en) 2025-01-22
JP7604457B2 (ja) 2024-12-23
BR112021026829A2 (pt) 2022-02-22
AU2020329609A1 (en) 2022-02-24
IL289197A (en) 2022-02-01
CN114269737A (zh) 2022-04-01
IL289197B2 (en) 2026-02-01
PL4013751T3 (pl) 2025-05-19
ES3015725T3 (en) 2025-05-07
WO2021028570A1 (en) 2021-02-18

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