CN112135821B - 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物 - Google Patents

作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物 Download PDF

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Publication number
CN112135821B
CN112135821B CN201980029405.9A CN201980029405A CN112135821B CN 112135821 B CN112135821 B CN 112135821B CN 201980029405 A CN201980029405 A CN 201980029405A CN 112135821 B CN112135821 B CN 112135821B
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indazole
alkyl
mmol
carboxamide
alkoxy
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Chinese (zh)
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CN112135821A (zh
Inventor
G·弗尔洛蒂
C·卡瓦里斯基亚
R·布翁菲戈里欧
R·姆布拉托
T·亚科安杰利
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Angelini Acraf SpA
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Aziende Chimiche Riunite Angelini Francesco ACRAF SpA
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    • 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
    • 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
    • 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non 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
    • A61K31/435Heterocyclic 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201980029405.9A 2018-05-07 2019-05-06 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物 Active CN112135821B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18171084 2018-05-07
EP18171084.9 2018-05-07
PCT/EP2019/061532 WO2019215075A1 (en) 2018-05-07 2019-05-06 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors

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CN112135821A CN112135821A (zh) 2020-12-25
CN112135821B true CN112135821B (zh) 2024-05-31

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US (1) US11472795B2 (https=)
EP (1) EP3790873B1 (https=)
JP (1) JP7411574B2 (https=)
KR (1) KR102778690B1 (https=)
CN (1) CN112135821B (https=)
AU (1) AU2019265606B2 (https=)
BR (1) BR112020021922A2 (https=)
CA (1) CA3094896A1 (https=)
CY (1) CY1125293T1 (https=)
DK (1) DK3790873T3 (https=)
EA (1) EA202092422A1 (https=)
ES (1) ES2913975T3 (https=)
GE (2) GEP20227437B (https=)
HR (1) HRP20220664T1 (https=)
HU (1) HUE058894T2 (https=)
IL (1) IL278330B2 (https=)
LT (1) LT3790873T (https=)
MA (1) MA52557A (https=)
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MX (1) MX2020011882A (https=)
PL (1) PL3790873T3 (https=)
PT (1) PT3790873T (https=)
RS (1) RS63255B1 (https=)
SG (1) SG11202009230WA (https=)
SI (1) SI3790873T1 (https=)
SM (1) SMT202200227T1 (https=)
UA (1) UA128089C2 (https=)
WO (1) WO2019215075A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023506257A (ja) * 2019-12-16 2023-02-15 コリア リサーチ インスティチュート オブ ケミカル テクノロジー 新規なインダゾール誘導体及びその用途
CN114230565B (zh) * 2020-09-09 2023-10-27 成都奥睿药业有限公司 5-取代吲哚3-酰胺衍生物及其制备方法和用途
WO2022125377A1 (en) * 2020-12-08 2022-06-16 Disarm Therapeutics, Inc. Benzopyrazole inhibitors of sarm1

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102239150A (zh) * 2008-12-05 2011-11-09 韩国科学技术研究院 作为用于增殖性疾病治疗的蛋白激酶抑制剂的新型吲唑衍生物或其药学上可接受的盐以及含有其作为活性成分的药物组合物
CN103929963A (zh) * 2011-09-14 2014-07-16 萨穆梅德有限公司 吲唑-3-羧酰胺及其作为WNT/β-CATENIN信号传导通路抑制剂的用途
CN104080781A (zh) * 2012-02-21 2014-10-01 方济各安吉利克化学联合股份有限公司 1H-吲唑-3-甲酰胺化合物作为糖原合酶激酶3β抑制剂的用途
CN104093712A (zh) * 2012-02-21 2014-10-08 方济各安吉利克化学联合股份有限公司 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物
CN106535890A (zh) * 2014-03-20 2017-03-22 萨穆梅德有限公司 5‑取代的吲唑‑3‑羧酰胺及其制备和应用
CN112020501A (zh) * 2018-02-23 2020-12-01 萨穆梅德有限公司 5-杂芳基取代的吲唑-3-基甲酰胺类及其制备和用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ257545A (en) 1992-11-05 1997-01-29 Smithkline Beecham Plc Heterocyclic (especially piperidine) derivatives and pharmaceutical compositions
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
ITMI20030287A1 (it) 2003-02-18 2004-08-19 Acraf Indazolammidi dotate di attivita' analgesica metodo, per
ITMI20030972A1 (it) 2003-05-15 2004-11-16 Acraf Indazolo dotato di attivita' analgesica, metodo per prepararlo e composizione farmaceutica che lo comprende.
TW201040191A (en) 2009-03-27 2010-11-16 Abbott Gmbh & Co Kg Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102239150A (zh) * 2008-12-05 2011-11-09 韩国科学技术研究院 作为用于增殖性疾病治疗的蛋白激酶抑制剂的新型吲唑衍生物或其药学上可接受的盐以及含有其作为活性成分的药物组合物
CN103929963A (zh) * 2011-09-14 2014-07-16 萨穆梅德有限公司 吲唑-3-羧酰胺及其作为WNT/β-CATENIN信号传导通路抑制剂的用途
CN104080781A (zh) * 2012-02-21 2014-10-01 方济各安吉利克化学联合股份有限公司 1H-吲唑-3-甲酰胺化合物作为糖原合酶激酶3β抑制剂的用途
CN104093712A (zh) * 2012-02-21 2014-10-08 方济各安吉利克化学联合股份有限公司 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物
CN106535890A (zh) * 2014-03-20 2017-03-22 萨穆梅德有限公司 5‑取代的吲唑‑3‑羧酰胺及其制备和应用
CN112020501A (zh) * 2018-02-23 2020-12-01 萨穆梅德有限公司 5-杂芳基取代的吲唑-3-基甲酰胺类及其制备和用途

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MA52557A (fr) 2021-03-17
WO2019215075A1 (en) 2019-11-14
UA128089C2 (uk) 2024-04-03
IL278330A (https=) 2020-12-31
EP3790873A1 (en) 2021-03-17
JP7411574B2 (ja) 2024-01-11
JP2021523134A (ja) 2021-09-02
EP3790873B1 (en) 2022-04-27
CN112135821A (zh) 2020-12-25
IL278330B2 (en) 2024-06-01
KR102778690B1 (ko) 2025-03-12
US20210053956A1 (en) 2021-02-25
DK3790873T3 (da) 2022-05-23
SG11202009230WA (en) 2020-11-27
MX2020011882A (es) 2021-01-20
HRP20220664T1 (hr) 2022-06-24
MD3790873T2 (ro) 2022-07-31
SMT202200227T1 (it) 2022-07-21
EA202092422A1 (ru) 2021-02-12
BR112020021922A2 (pt) 2021-01-26
GEAP202215506A (en) 2022-07-11
IL278330B1 (en) 2024-02-01
KR20210005863A (ko) 2021-01-15
AU2019265606A1 (en) 2020-10-15
ES2913975T3 (es) 2022-06-07
AU2019265606B2 (en) 2023-10-12
CA3094896A1 (en) 2019-11-14
SI3790873T1 (sl) 2022-07-29
CY1125293T1 (el) 2025-03-28
LT3790873T (lt) 2022-06-10
US11472795B2 (en) 2022-10-18
HUE058894T2 (hu) 2022-09-28
RS63255B1 (sr) 2022-06-30
PT3790873T (pt) 2022-05-11
PL3790873T3 (pl) 2022-06-27
GEP20227437B (en) 2022-11-10

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