CN114269737A - 2-羟环烷-1-胺甲酰基衍生物 - Google Patents

2-羟环烷-1-胺甲酰基衍生物 Download PDF

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Publication number
CN114269737A
CN114269737A CN202080057325.7A CN202080057325A CN114269737A CN 114269737 A CN114269737 A CN 114269737A CN 202080057325 A CN202080057325 A CN 202080057325A CN 114269737 A CN114269737 A CN 114269737A
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China
Prior art keywords
pyran
hydroxycyclohexyl
hydroxymethyl
triazol
hydroxy
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Pending
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CN202080057325.7A
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English (en)
Chinese (zh)
Inventor
马丁·博利
约翰·加特菲尔德
考里纳·格里索斯托米
卢博斯·雷门
克里斯托夫·萨格尔
科妮莉亚·朱姆布鲁恩
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Actelion Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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Publication of CN114269737A publication Critical patent/CN114269737A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41921,2,3-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12Triazine 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)
CN202080057325.7A 2019-08-15 2020-08-14 2-羟环烷-1-胺甲酰基衍生物 Pending CN114269737A (zh)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CN114269737A true CN114269737A (zh) 2022-04-01

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080057325.7A Pending CN114269737A (zh) 2019-08-15 2020-08-14 2-羟环烷-1-胺甲酰基衍生物

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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP4010348B1 (en) 2019-08-09 2023-12-20 Idorsia Pharmaceuticals Ltd (2-acetamidyl)thio-beta-d-galactopyranoside derivatives
CA3148365A1 (en) 2019-08-29 2021-03-04 Martin Bolli Alpha-d-galactopyranoside derivatives
CA3161794A1 (en) * 2019-12-24 2021-07-01 John L. Magnani Galectin-3 inhibiting c-glycoside ketones, ethers, and alcohols
ES3014851T3 (en) 2020-10-06 2025-04-25 Idorsia Pharmaceuticals Ltd Spiro derivatives of alpha-d-galactopyranosides
KR20230104190A (ko) 2020-11-02 2023-07-07 이도르시아 파마슈티컬스 리미티드 갈렉틴-3 억제 2-히드록시시클로알칸-1-카르바모일 유도체
KR20230145111A (ko) * 2021-02-09 2023-10-17 이도르시아 파마슈티컬스 리미티드 히드록시헤테로시클로알칸-카르바모일 유도체
PL4301748T3 (pl) 2021-03-03 2025-09-08 Idorsia Pharmaceuticals Ltd Triazolilo-metylo podstawione pochodne alfa-d-galaktopiranozydu
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
WO2022250976A1 (en) * 2021-05-28 2022-12-01 Glycomimetics, Inc. Galectin-3 inhibiting c-glycoside oximes

Citations (5)

* 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
WO2016120403A1 (en) * 2015-01-30 2016-08-04 Galecto Biotech Ab Alpha-d-galactoside inhibitors of galectins
WO2018209255A1 (en) * 2017-05-12 2018-11-15 Galectin Sciences, Llc Compounds for the prevention and treatment of diseases and the use thereof
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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JP2015535233A (ja) 2012-10-31 2015-12-10 ガレクト・バイオテック・エイビイ ガレクチン−3のガラクトシド阻害剤及び肺線維症のためのその使用
WO2014078655A1 (en) 2012-11-15 2014-05-22 Tufts University Methods, compositions and kits for treating, modulating, or preventing ocular angiogenesis or fibrosis in a subject using a galectin protein inhibitor
KR101974793B1 (ko) 2015-07-06 2019-05-02 길리애드 사이언시즈, 인코포레이티드 Cot 조정제 및 그의 사용 방법
CA3025867A1 (en) 2016-07-12 2018-01-18 Galecto Biotech Ab Alpha-d-galactoside inhibitors of galectins
WO2019075045A1 (en) 2017-10-11 2019-04-18 Bristol-Myers Squibb Company INHIBITORS WITH SMALL MOLECULES OF GALECTIN-3
AU2018361991A1 (en) 2017-10-31 2020-05-14 Galectin Sciences, Llc Selenogalactoside compounds for the treatment of systemic insulin resistance disorders and the use thereof
CN113366007A (zh) 2018-10-15 2021-09-07 格莱克特生物技术公司 半乳糖凝集素的半乳糖苷抑制剂
JP2022508719A (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のプロドラッグ
JP7486484B2 (ja) 2018-11-21 2024-05-17 ガレクト バイオテック エービー ガレクチンのα-D-ガラクトシド阻害剤
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CA3141436A1 (en) 2019-07-03 2021-01-07 Fredrik Zetterberg Novel galactoside inhibitor of galectins
CN114450282A (zh) 2019-07-05 2022-05-06 格莱克特生物技术公司 半乳糖凝集素的新型半乳糖苷抑制剂
EP4010348B1 (en) 2019-08-09 2023-12-20 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
CA3148365A1 (en) 2019-08-29 2021-03-04 Martin Bolli Alpha-d-galactopyranoside derivatives
ES3014851T3 (en) 2020-10-06 2025-04-25 Idorsia Pharmaceuticals Ltd Spiro derivatives of alpha-d-galactopyranosides
KR20230104190A (ko) 2020-11-02 2023-07-07 이도르시아 파마슈티컬스 리미티드 갈렉틴-3 억제 2-히드록시시클로알칸-1-카르바모일 유도체
KR20230145111A (ko) 2021-02-09 2023-10-17 이도르시아 파마슈티컬스 리미티드 히드록시헤테로시클로알칸-카르바모일 유도체
PL4301748T3 (pl) 2021-03-03 2025-09-08 Idorsia Pharmaceuticals Ltd Triazolilo-metylo podstawione pochodne alfa-d-galaktopiranozydu

Patent Citations (5)

* 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
WO2016120403A1 (en) * 2015-01-30 2016-08-04 Galecto Biotech Ab Alpha-d-galactoside inhibitors of galectins
WO2018209255A1 (en) * 2017-05-12 2018-11-15 Galectin Sciences, Llc Compounds for the prevention and treatment of diseases and the use thereof
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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IL289197A (en) 2022-02-01
IL289197B2 (en) 2026-02-01
CA3147454A1 (en) 2021-02-18
RS66695B1 (sr) 2025-05-30
JP2022544248A (ja) 2022-10-17
IL289197B1 (en) 2025-10-01
JP7604457B2 (ja) 2024-12-23
ES3015725T3 (en) 2025-05-07
PL4013751T3 (pl) 2025-05-19
AU2020329609A1 (en) 2022-02-24
MA56883B1 (fr) 2025-04-30
EP4013751B1 (en) 2025-01-22
WO2021028570A1 (en) 2021-02-18
HRP20250372T1 (hr) 2025-06-06
UA128909C2 (uk) 2024-11-20
EP4013751A1 (en) 2022-06-22
US12291519B2 (en) 2025-05-06
MX2022001789A (es) 2022-03-11
BR112021026829A2 (pt) 2022-02-22
AU2020329609B2 (en) 2025-10-02
PH12022550338A1 (en) 2023-02-06
KR102832308B1 (ko) 2025-07-10
TW202115039A (zh) 2021-04-16
US20220324847A1 (en) 2022-10-13
TWI864071B (zh) 2024-12-01
KR20220047585A (ko) 2022-04-18
HUE070924T2 (hu) 2025-07-28
EP4013751C0 (en) 2025-01-22

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