JP7793529B2 - Kcc2調節剤としての縮合ピリミジン化合物 - Google Patents

Kcc2調節剤としての縮合ピリミジン化合物

Info

Publication number
JP7793529B2
JP7793529B2 JP2022554784A JP2022554784A JP7793529B2 JP 7793529 B2 JP7793529 B2 JP 7793529B2 JP 2022554784 A JP2022554784 A JP 2022554784A JP 2022554784 A JP2022554784 A JP 2022554784A JP 7793529 B2 JP7793529 B2 JP 7793529B2
Authority
JP
Japan
Prior art keywords
alkyl
optionally substituted
pyrimidin
dihydro
cyclohexylphenyl
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.)
Active
Application number
JP2022554784A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023517680A5 (enExample
JP2023517680A (ja
Inventor
エリザベス ジャービス,レベッカ
ヴェルナー ビューリ,ローランド
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.)
AstraZeneca AB
Original Assignee
AstraZeneca AB
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 AstraZeneca AB filed Critical AstraZeneca AB
Publication of JP2023517680A publication Critical patent/JP2023517680A/ja
Publication of JP2023517680A5 publication Critical patent/JP2023517680A5/ja
Priority to JP2025151939A priority Critical patent/JP2025186368A/ja
Application granted granted Critical
Publication of JP7793529B2 publication Critical patent/JP7793529B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2022554784A 2020-03-13 2021-03-12 Kcc2調節剤としての縮合ピリミジン化合物 Active JP7793529B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025151939A JP2025186368A (ja) 2020-03-13 2025-09-12 Kcc2調節剤としての縮合ピリミジン化合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062989104P 2020-03-13 2020-03-13
US62/989,104 2020-03-13
PCT/EP2021/056393 WO2021180952A1 (en) 2020-03-13 2021-03-12 Fused pyrimidine compounds as kcc2

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025151939A Division JP2025186368A (ja) 2020-03-13 2025-09-12 Kcc2調節剤としての縮合ピリミジン化合物

Publications (3)

Publication Number Publication Date
JP2023517680A JP2023517680A (ja) 2023-04-26
JP2023517680A5 JP2023517680A5 (enExample) 2024-03-21
JP7793529B2 true JP7793529B2 (ja) 2026-01-05

Family

ID=74874882

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2022554784A Active JP7793529B2 (ja) 2020-03-13 2021-03-12 Kcc2調節剤としての縮合ピリミジン化合物
JP2025151939A Pending JP2025186368A (ja) 2020-03-13 2025-09-12 Kcc2調節剤としての縮合ピリミジン化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2025151939A Pending JP2025186368A (ja) 2020-03-13 2025-09-12 Kcc2調節剤としての縮合ピリミジン化合物

Country Status (25)

Country Link
US (1) US12617795B2 (enExample)
EP (1) EP4103566B1 (enExample)
JP (2) JP7793529B2 (enExample)
KR (1) KR20220152319A (enExample)
CN (4) CN119684300A (enExample)
AU (1) AU2021234134B2 (enExample)
BR (1) BR112022018173A2 (enExample)
CA (1) CA3171192A1 (enExample)
CL (1) CL2022002386A1 (enExample)
CO (1) CO2022012884A2 (enExample)
DK (1) DK4103566T3 (enExample)
ES (1) ES2962136T3 (enExample)
FI (1) FI4103566T3 (enExample)
HR (1) HRP20231314T1 (enExample)
HU (1) HUE064037T2 (enExample)
IL (1) IL296265B2 (enExample)
LT (1) LT4103566T (enExample)
MX (1) MX2022011354A (enExample)
PE (1) PE20230106A1 (enExample)
PL (1) PL4103566T3 (enExample)
PT (1) PT4103566T (enExample)
RS (1) RS64823B1 (enExample)
SI (1) SI4103566T1 (enExample)
SM (1) SMT202300384T1 (enExample)
WO (1) WO2021180952A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2022407047A1 (en) * 2021-12-08 2024-07-25 Kineta, Inc. Bicyclic heteroarenes and methods of their use
CN117843618A (zh) * 2022-08-29 2024-04-09 北京沐华生物科技有限责任公司 一种ep300/cbp调节剂及其制备方法和用途
CN121548571A (zh) * 2023-04-05 2026-02-17 艾索尼斯治疗公司 Kcc2增强剂及其用途
US20250281497A1 (en) * 2024-03-06 2025-09-11 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of seizure disorders
WO2025188977A1 (en) * 2024-03-06 2025-09-12 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of addiction and insomnia
WO2025188974A1 (en) * 2024-03-06 2025-09-12 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of autism spectrum disorder, obsessive compulsive disorder and tics
WO2025188973A1 (en) * 2024-03-06 2025-09-12 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of 22q11.2 deletion/duplication syndromes
US20260048062A1 (en) * 2024-03-06 2026-02-19 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of psychosis and psychotic disorders
WO2025188952A1 (en) * 2024-03-06 2025-09-12 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of synucleinopathies and tdp-43 proteinopathies
WO2025188953A1 (en) * 2024-03-06 2025-09-12 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of neuropathic and neuro-inflammatory pain
US20250281500A1 (en) * 2024-03-06 2025-09-11 Ovid Therapeutics Inc. Fused amino pyrimidine compounds and pridopidine for treatment of huntington’s disease
US20260048063A1 (en) * 2024-03-06 2026-02-19 Ovid Therapeutics Inc. Fused amino pyrimidine compounds for treatment of neurodegenerative disorders

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010526138A (ja) 2007-05-08 2010-07-29 アストラゼネカ・アクチエボラーグ ピロロピリミジン−7−オン誘導体とその薬剤としての使用
WO2019045824A1 (en) 2017-09-01 2019-03-07 Kadmon Corporation, Llc ALPHA PROPELLER PROTEIN KINASE INHIBITORS ("COILED-COIL") ASSOCIATED WITH RHO

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3398152B2 (ja) 1993-10-12 2003-04-21 ブリストル‐マイヤーズ・スクイブ・ファーマ・カンパニー 1n−アルキル−n−アリールピリミジンアミンおよびその誘導体
HRP20140395T1 (hr) 2008-08-20 2014-06-06 Zoetis Llc SPOJEVI PIROLO[2,3-d]PIRIMIDINA
EP4019518A1 (en) 2014-02-28 2022-06-29 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
US11331313B2 (en) 2017-05-22 2022-05-17 Whitehead Institute For Biomedical Research KCC2 expression enhancing compounds and uses thereof
WO2019226643A1 (en) 2018-05-25 2019-11-28 The Children's Medical Center Corporation Methods for treating spinal cord injury

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010526138A (ja) 2007-05-08 2010-07-29 アストラゼネカ・アクチエボラーグ ピロロピリミジン−7−オン誘導体とその薬剤としての使用
WO2019045824A1 (en) 2017-09-01 2019-03-07 Kadmon Corporation, Llc ALPHA PROPELLER PROTEIN KINASE INHIBITORS ("COILED-COIL") ASSOCIATED WITH RHO

Also Published As

Publication number Publication date
AU2021234134B2 (en) 2025-08-21
PL4103566T3 (pl) 2024-02-05
IL296265A (en) 2022-11-01
ES2962136T3 (es) 2024-03-15
CN115298182A (zh) 2022-11-04
CA3171192A1 (en) 2021-09-16
IL296265B2 (en) 2026-04-01
CO2022012884A2 (es) 2022-10-11
HRP20231314T1 (hr) 2024-02-16
WO2021180952A1 (en) 2021-09-16
CN119684299A (zh) 2025-03-25
RS64823B1 (sr) 2023-12-29
PE20230106A1 (es) 2023-01-25
SMT202300384T1 (it) 2024-01-10
CN119735594A (zh) 2025-04-01
HUE064037T2 (hu) 2024-03-28
CN115298182B (zh) 2025-02-11
AU2021234134A1 (en) 2022-11-03
MX2022011354A (es) 2022-11-30
PT4103566T (pt) 2023-11-09
SI4103566T1 (sl) 2024-04-30
KR20220152319A (ko) 2022-11-15
DK4103566T3 (da) 2023-10-30
JP2023517680A (ja) 2023-04-26
US20230151013A1 (en) 2023-05-18
BR112022018173A2 (pt) 2022-10-25
CN119684300A (zh) 2025-03-25
CL2022002386A1 (es) 2023-04-28
EP4103566B1 (en) 2023-10-04
JP2025186368A (ja) 2025-12-23
EP4103566A1 (en) 2022-12-21
IL296265B1 (en) 2025-12-01
FI4103566T3 (fi) 2023-10-20
WO2021180952A9 (en) 2021-12-16
US12617795B2 (en) 2026-05-05
LT4103566T (lt) 2023-11-10

Similar Documents

Publication Publication Date Title
JP2025186368A (ja) Kcc2調節剤としての縮合ピリミジン化合物
CN104837829B (zh) 抑制剂化合物
US20220127281A1 (en) Heteroaryl compounds that inhibit g12c mutant ras proteins
JP2025532125A (ja) 新規なテトラヘテロサイクル化合物
EP3405192B1 (en) Bruton's tyrosine kinase inhibitors
KR102327917B1 (ko) 신규한 4-아미노피라졸로[3,4-d]피리미디닐아자바이사이클로 유도체 및 이를 포함하는 약학 조성물
AU2014249192A1 (en) BET bromodomain inhibitors and therapeutic methods using the same
AU2019237991B2 (en) JAK inhibitors
JP2022523477A (ja) ピロロピリミジン誘導体及びこれを有効成分として含有するタンパク質キナーゼ関連疾患の予防又は治療用薬学的組成物
JP7851393B2 (ja) 癌の治療のためのhpk1阻害剤としての置換ピラジン-2-カルボキサミド阻害剤
CA2630360A1 (en) Substituted bicyclic pyrimidone derivatives
HK40085963A (en) Fused pyrimidine compounds as kcc2 modulators
HK40085963B (en) Fused pyrimidine compounds as kcc2 modulators
WO2024061118A1 (zh) 大环含氮冠醚化合物及其作为蛋白激酶抑制剂的应用
WO2026099455A1 (en) Dihydropyrrolopyrimidinone compounds as trem2 modulators
JP2023544847A (ja) がんの治療のためのベンゾ[h]キナゾリン-4-アミン及びチエノ[3,2-h]キナゾリン-4-アミン誘導体
AU2006314136A1 (en) Substituted bicyclic pyrimidone derivatives
HK1126204B (en) Substituted bicyclic pyrimidone derivatives

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240311

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20240311

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20250130

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20250204

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250502

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20250513

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250912

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20251209

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20251217

R150 Certificate of patent or registration of utility model

Ref document number: 7793529

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150