CN118488838A - 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途 - Google Patents

含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途 Download PDF

Info

Publication number
CN118488838A
CN118488838A CN202280086990.8A CN202280086990A CN118488838A CN 118488838 A CN118488838 A CN 118488838A CN 202280086990 A CN202280086990 A CN 202280086990A CN 118488838 A CN118488838 A CN 118488838A
Authority
CN
China
Prior art keywords
alkyl
compound
pharmaceutically acceptable
stereoisomer
acceptable salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202280086990.8A
Other languages
English (en)
Chinese (zh)
Inventor
丁晓
秦烈娜
任峰
徐剑宇
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.)
Yingsi Intelligent Technology Intellectual Property Co ltd
Original Assignee
Yingsi Intelligent Technology Intellectual Property Co ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Yingsi Intelligent Technology Intellectual Property Co ltd filed Critical Yingsi Intelligent Technology Intellectual Property Co ltd
Publication of CN118488838A publication Critical patent/CN118488838A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/505—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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202280086990.8A 2021-10-28 2022-10-28 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途 Pending CN118488838A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2021127023 2021-10-28
CNPCT/CN2021/127023 2021-10-28
CN2022112270 2022-08-12
CNPCT/CN2022/112270 2022-08-12
PCT/CN2022/128220 WO2023072240A1 (en) 2021-10-28 2022-10-28 Prolyl hydroxylase domain-containing protein (phd) inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
CN118488838A true CN118488838A (zh) 2024-08-13

Family

ID=86159087

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202280086990.8A Pending CN118488838A (zh) 2021-10-28 2022-10-28 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途
CN202280086996.5A Pending CN118591533A (zh) 2021-10-28 2022-10-28 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202280086996.5A Pending CN118591533A (zh) 2021-10-28 2022-10-28 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途

Country Status (11)

Country Link
US (6) US20250034132A1 (https=)
EP (2) EP4422623A4 (https=)
JP (2) JP2024539946A (https=)
KR (2) KR20240095274A (https=)
CN (2) CN118488838A (https=)
AR (3) AR127501A1 (https=)
AU (1) AU2022378858A1 (https=)
CA (1) CA3235718A1 (https=)
IL (1) IL312220A (https=)
TW (3) TW202334158A (https=)
WO (3) WO2023072246A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20240095274A (ko) 2021-10-28 2024-06-25 인실리코 메디신 아이피 리미티드 프롤릴 히드록실라제 도메인-함유 단백질 (phd) 억제제 및 그의 용도
GB202301059D0 (en) 2023-01-25 2023-03-08 Univ Oxford Innovation Ltd PHD inhibitors
EP4702023A1 (en) * 2023-04-28 2026-03-04 Insilico Medicine IP Limited Crystalline prolyl hydroxylase domain-containing protein (phd) inhibitor and uses thereof
AU2024261389A1 (en) * 2023-04-28 2025-10-30 Insilico Medicine Ip Limited Prolyl hydroxylase domain-containing protein (phd) inhibitors, combinations and uses thereof
CN121057737A (zh) * 2023-04-28 2025-12-02 英矽智能科技知识产权有限公司 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂结晶及其用途
CN117402178B (zh) * 2023-12-15 2024-03-08 英矽智能科技(上海)有限公司 作为jak抑制剂和phd抑制剂的嘧啶类化合物
CN117603230B (zh) * 2023-12-15 2025-03-21 英矽智能科技(上海)有限公司 作为jak抑制剂和phd抑制剂的三并环类化合物
CN117756822B (zh) * 2023-12-20 2025-04-18 英矽智能科技(上海)有限公司 作为jak抑制剂和phd抑制剂的嘧啶氨基类化合物
CN117736227B (zh) * 2023-12-20 2025-01-21 英矽智能科技(上海)有限公司 抑制jak和phd的一类化合物
CN117924326B (zh) * 2024-01-23 2025-01-21 英矽智能科技(上海)有限公司 一类抑制jak和phd的三并环类化合物

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6730682B2 (en) * 2000-07-12 2004-05-04 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
AU2003262946A1 (en) * 2002-08-30 2004-03-19 Pharmacia And Upjohn Company Method of preventing or treating atherosclerosis or restenosis
US8614204B2 (en) 2003-06-06 2013-12-24 Fibrogen, Inc. Enhanced erythropoiesis and iron metabolism
GB0505621D0 (en) * 2005-03-18 2005-04-27 Glaxo Group Ltd Novel compounds
US8962530B2 (en) 2007-06-27 2015-02-24 Regents Of The University Of Colorado Inflammatory bowel disease therapies
KR20100045480A (ko) * 2007-08-10 2010-05-03 크리스탈지노믹스(주) 피리딘 유도체 및 이들의 사용방법
EP2536709A4 (en) 2010-02-17 2013-11-27 Univ Cornell PROLYL HYDROXYLASE HEMMER AND USE METHOD THEREFOR
WO2013134660A1 (en) * 2012-03-09 2013-09-12 Fibrogen, Inc. 4 -hydroxy- isoquinoline compounds as hif hydroxylase inhibitors
GB201504565D0 (en) 2015-03-18 2015-05-06 Takeda Pharmaceutical Novel compounds
CN106146490B (zh) 2015-03-27 2018-10-23 沈阳三生制药有限责任公司 被芳氧基或杂芳氧基取代的5-羟基-1,7-萘啶化合物、其制备方法及其制药用途
CN106146491B (zh) * 2015-03-27 2017-12-12 沈阳三生制药有限责任公司 被芳基或杂芳基取代的5‑羟基‑1,7‑萘啶化合物、其制备方法及其制药用途
CN108341777A (zh) 2017-01-23 2018-07-31 四川科伦博泰生物医药股份有限公司 异喹啉酮类化合物及其应用
WO2018218042A1 (en) * 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
TW201920108A (zh) * 2017-09-25 2019-06-01 日商武田藥品工業有限公司 N-(氰基取代之苄基或吡啶基甲基)-3-羥基吡啶醯胺衍生物
AU2018340475B2 (en) * 2017-09-28 2023-01-19 Transthera Sciences (Nanjing), Inc. PDE9 inhibitor and use thereof
CN110878096A (zh) 2018-09-05 2020-03-13 石药集团中奇制药技术（石家庄）有限公司 一种1,7-萘啶类衍生物及其制备方法和用途
CN112979541B (zh) 2019-12-17 2022-11-11 浙江大学 一种基于n-(3-羟基吡啶-2-羰基)甘氨酸的抗肿瘤药物增敏剂及其应用
WO2021163344A1 (en) * 2020-02-12 2021-08-19 Amgen Inc. Novel prmt5 inhibitors
GB202004960D0 (en) * 2020-04-03 2020-05-20 Kinsenus Ltd Inhibitor compounds
KR20240095274A (ko) 2021-10-28 2024-06-25 인실리코 메디신 아이피 리미티드 프롤릴 히드록실라제 도메인-함유 단백질 (phd) 억제제 및 그의 용도

Also Published As

Publication number Publication date
US11780854B2 (en) 2023-10-10
JP2024539946A (ja) 2024-10-31
US20240002406A1 (en) 2024-01-04
EP4422623A4 (en) 2025-10-29
JP2024541910A (ja) 2024-11-13
AR127488A1 (es) 2024-01-31
AR127501A1 (es) 2024-01-31
AR127500A1 (es) 2024-01-31
TW202334134A (zh) 2023-09-01
US20250034132A1 (en) 2025-01-30
EP4422623A1 (en) 2024-09-04
US12209101B2 (en) 2025-01-28
KR20240095274A (ko) 2024-06-25
TW202334158A (zh) 2023-09-01
WO2023072257A1 (en) 2023-05-04
EP4423074A1 (en) 2024-09-04
CN118591533A (zh) 2024-09-03
US20230192688A1 (en) 2023-06-22
CA3235718A1 (en) 2023-05-04
US11731987B2 (en) 2023-08-22
WO2023072246A1 (en) 2023-05-04
US12071443B2 (en) 2024-08-27
TW202332677A (zh) 2023-08-16
US20240067661A1 (en) 2024-02-29
AU2022378858A1 (en) 2024-05-02
KR20240093899A (ko) 2024-06-24
US20230192723A1 (en) 2023-06-22
IL312220A (en) 2024-06-01
EP4423074A4 (en) 2025-09-03
WO2023072240A1 (en) 2023-05-04
US20260015349A1 (en) 2026-01-15

Similar Documents

Publication Publication Date Title
CN118488838A (zh) 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途
JP7794989B2 (ja) Ｐａｒｐ１阻害薬及びその使用
CN118556053A (zh) 赖氨酸乙酰基转移酶6a(kat6a)抑制剂及其用途
CN118434722A (zh) 甲硫氨酸腺苷转移酶2a(mat2a)抑制剂及其用途
JP7813374B2 (ja) Ｐａｒｐ１阻害薬及びその使用
JP7680619B2 (ja) Ｐａｒｐ１阻害薬及びその使用
JP7728989B2 (ja) 三環式ｐａｒｐ１阻害剤及びその使用
US20250145624A1 (en) Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (pkmyt1) inhibitors and uses thereof
US20250188094A1 (en) Pyrazole membrane-associated tyrosine-and threonine-specific cdc2-inhibitory kinase (pkmyt1) inhibitors and uses thereof
WO2023165528A1 (en) Diacylglycerol kinase (dgk) alpha inhibitors and uses thereof
WO2023165525A1 (en) Diacylglycerol kinase (dgk) alpha inhibitors and uses thereof
CN118871439A (zh) 外核苷酸焦磷酸酶-磷酸二酯酶(enpp1)抑制剂及其用途
KR20250023339A (ko) 페닐 트라이아졸 mll1-wdr5 단백질-단백질 상호작용 저해제
HK40114409A (zh) 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂及其用途
WO2025252075A1 (en) Novel compounds as salt-inducible kinases inhibitors and uses thereof
WO2025232848A1 (en) Salt-inducible kinases (sik) inhibitors and methods of uses thereof
WO2025232877A1 (en) Salt-inducible kinases (sik) inhibitors
WO2025026377A1 (en) Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp1) inhibitors and uses thereof
WO2024061300A1 (en) Inhibitors of trex1 and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40114409

Country of ref document: HK