CN114710956A - 抑制perk的吡咯并嘧啶化合物 - Google Patents

抑制perk的吡咯并嘧啶化合物 Download PDF

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Publication number
CN114710956A
CN114710956A CN202080073530.2A CN202080073530A CN114710956A CN 114710956 A CN114710956 A CN 114710956A CN 202080073530 A CN202080073530 A CN 202080073530A CN 114710956 A CN114710956 A CN 114710956A
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CN
China
Prior art keywords
amino
alkyl
pyrrolo
pyrimidin
methyl
Prior art date
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Pending
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CN202080073530.2A
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English (en)
Chinese (zh)
Inventor
M.J.穆尔维希尔
A-H.李
M.D.苏尔曼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hebsel Co ltd
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Hebsel Co ltd
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Publication date
Application filed by Hebsel Co ltd filed Critical Hebsel Co ltd
Publication of CN114710956A publication Critical patent/CN114710956A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202080073530.2A 2019-08-29 2020-08-28 抑制perk的吡咯并嘧啶化合物 Pending CN114710956A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962893528P 2019-08-29 2019-08-29
US62/893,528 2019-08-29
PCT/US2020/048621 WO2021041975A1 (en) 2019-08-29 2020-08-28 Perk inhibiting pyrrolopyrimidine compounds

Publications (1)

Publication Number Publication Date
CN114710956A true CN114710956A (zh) 2022-07-05

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ID=72470610

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080073530.2A Pending CN114710956A (zh) 2019-08-29 2020-08-28 抑制perk的吡咯并嘧啶化合物

Country Status (12)

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US (1) US20220356186A1 (https=)
EP (1) EP4021908A1 (https=)
JP (1) JP2022546414A (https=)
KR (1) KR20220066290A (https=)
CN (1) CN114710956A (https=)
AU (1) AU2020336975A1 (https=)
BR (1) BR112022003584A2 (https=)
CA (1) CA3152508A1 (https=)
IL (1) IL290889A (https=)
MX (1) MX2022002446A (https=)
PH (1) PH12022550491A1 (https=)
WO (1) WO2021041975A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114585606A (zh) 2019-08-29 2022-06-03 希伯塞尔股份有限公司 抑制perk的化合物
RS65962B1 (sr) 2020-05-08 2024-10-31 Halia Therapeutics Inc Inhibitori nek7 kinaze
CN117597346A (zh) * 2021-04-05 2024-02-23 哈利亚治疗公司 Nek7抑制剂
WO2022216680A1 (en) * 2021-04-05 2022-10-13 Halia Therapeutics, Inc. Nek7 inhibitors
US20240287081A1 (en) * 2021-06-09 2024-08-29 Icahn School Of Medicine At Mount Sinai Perfluoroalkane substituted pyrazolo[3,4-d]pyrimidin and pyrrolo[2,3-d]pyrimidin compounds and uses thereof
US20250000859A1 (en) 2021-08-25 2025-01-02 Alesta Therapeutics BV Use of gcn2 inhibitors in treating cancer
GB202407386D0 (en) 2024-05-24 2024-07-10 Apollo Ap45 Ltd 1H-pyrazolo(4,3-D)pyrimidine derivatives

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998041525A1 (en) * 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
US20030187001A1 (en) * 1997-03-19 2003-10-02 David Calderwood 4-aminopyrrolopyrimidines as kinase inhibitors
WO2016085160A2 (ko) * 2014-11-28 2016-06-02 (주)네오팜 발모촉진용 또는 탈모방지용 조성물
EP3067356A1 (en) * 2013-11-08 2016-09-14 ONO Pharmaceutical Co., Ltd. Pyrrolo pyrimidine derivative
WO2018009017A1 (en) * 2016-07-07 2018-01-11 Daewoong Pharmaceutical Co., Ltd. NOVEL 4-AMINOPYRAZOLO[3,4-d]PYRIMIDINYLAZABICYCLO DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
WO2018194885A1 (en) * 2017-04-18 2018-10-25 Eli Lilly And Company Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
US3903297A (en) 1973-11-01 1975-09-02 Upjohn Co Method of treatment and prophylaxis of gastric hypersecretion and gastric and duodenal ulcers using prostaglandin analogs
CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
WO2016004254A1 (en) 2014-07-01 2016-01-07 The Regents Of The University Of California Combined modulation of ire1
GB201508747D0 (en) * 2015-05-21 2015-07-01 Univ Edinburgh Compounds
WO2017046739A1 (en) * 2015-09-15 2017-03-23 Glaxosmithkline Intellectual Property (No.2) Limited Imidazolidinone derivatives as inhibitors of perk
TW201722957A (zh) * 2015-09-15 2017-07-01 葛蘭素史克智慧財產（第二）有限公司 化學化合物

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998041525A1 (en) * 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
US20030187001A1 (en) * 1997-03-19 2003-10-02 David Calderwood 4-aminopyrrolopyrimidines as kinase inhibitors
EP3067356A1 (en) * 2013-11-08 2016-09-14 ONO Pharmaceutical Co., Ltd. Pyrrolo pyrimidine derivative
WO2016085160A2 (ko) * 2014-11-28 2016-06-02 (주)네오팜 발모촉진용 또는 탈모방지용 조성물
WO2018009017A1 (en) * 2016-07-07 2018-01-11 Daewoong Pharmaceutical Co., Ltd. NOVEL 4-AMINOPYRAZOLO[3,4-d]PYRIMIDINYLAZABICYCLO DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
WO2018194885A1 (en) * 2017-04-18 2018-10-25 Eli Lilly And Company Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
CHAPMAN E，等: "A small molecule inhibitor selective for a variant ATP­binding site of the chaperonin GroEL", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL,, vol. 19, no. 03, 7 December 2008 (2008-12-07) *
JEFFREY M. AXTEN，等: "Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development", ACS MEDICINAL CHEMISTRY LETTERS, vol. 04, no. 10, 23 August 2013 (2013-08-23), pages 964 - 968 *
SUJATA CHAKRABORTY，等: "Targeting Dynamic ATP-Binding Site Features Allows Discrimination between Highly Homologous Protein Kinases", ACS CHEMICAL BIOLOGY, vol. 14, no. 06, 30 April 2019 (2019-04-30), pages 1249 - 1259 *
XUE YUAN，等: "Identification of Pyrrolo[2, 3-d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia", JOURNAL OF MEDICINAL CHEMISTRY, vol. 62, no. 08, 2 April 2019 (2019-04-02), pages 4158 - 4173, XP055742629, DOI: 10.1021/acs.jmedchem.9b00223 *
YUESHAN LI，等: "Identification of 5-(2, 3-Dihydro-1 H -indol-5-yl)-7 H -pyrrolo[2, 3- d ]pyrimidin-4-amine Derivatives as a New Class of Receptor­Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61, no. 24, 27 November 2018 (2018-11-27), pages 11398 - 11414, XP055676382, DOI: 10.1021/acs.jmedchem.8b01652 *

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Publication number Publication date
US20220356186A1 (en) 2022-11-10
IL290889A (en) 2022-04-01
KR20220066290A (ko) 2022-05-24
PH12022550491A1 (en) 2023-02-06
EP4021908A1 (en) 2022-07-06
BR112022003584A2 (pt) 2022-05-24
MX2022002446A (es) 2022-06-02
JP2022546414A (ja) 2022-11-04
WO2021041975A1 (en) 2021-03-04
AU2020336975A1 (en) 2022-03-31
CA3152508A1 (en) 2021-03-04

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