KR102977603B1 - 헤테로시클릴 화합물, 이를 포함하는 약제학적 조성물, 이의 제조 방법, 및 이의 용도 - Google Patents

헤테로시클릴 화합물, 이를 포함하는 약제학적 조성물, 이의 제조 방법, 및 이의 용도

Info

Publication number
KR102977603B1
KR102977603B1 KR1020217022806A KR20217022806A KR102977603B1 KR 102977603 B1 KR102977603 B1 KR 102977603B1 KR 1020217022806 A KR1020217022806 A KR 1020217022806A KR 20217022806 A KR20217022806 A KR 20217022806A KR 102977603 B1 KR102977603 B1 KR 102977603B1
Authority
KR
South Korea
Prior art keywords
group
compound
groups
cycloalkyl
alkyl
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
KR1020217022806A
Other languages
English (en)
Korean (ko)
Other versions
KR20210131314A (ko
Inventor
중후이 천
스왕스왕 돤
구이잉 리
룬펑 한
치정 순
리옌둥 징
샤오쥔 한
치앙 티안
홍메이 송
통통 쉐
징이 왕
Original Assignee
쓰촨 케룬-바이오테크 바이오파마수티컬 컴퍼니 리미티드
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 쓰촨 케룬-바이오테크 바이오파마수티컬 컴퍼니 리미티드 filed Critical 쓰촨 케룬-바이오테크 바이오파마수티컬 컴퍼니 리미티드
Publication of KR20210131314A publication Critical patent/KR20210131314A/ko
Application granted granted Critical
Publication of KR102977603B1 publication Critical patent/KR102977603B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • C07D471/08—Bridged systems
    • 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
    • C07D487/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
KR1020217022806A 2019-02-19 2020-02-11 헤테로시클릴 화합물, 이를 포함하는 약제학적 조성물, 이의 제조 방법, 및 이의 용도 Active KR102977603B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201910124584 2019-02-19
CN201910124584.6 2019-02-19
CN201910437878 2019-05-24
CN201910437878.4 2019-05-24
CN201910932095 2019-09-29
CN201910932095.3 2019-09-29
PCT/CN2020/074696 WO2020168939A1 (zh) 2019-02-19 2020-02-11 杂环化合物、包含其的药物组合物及其制备方法和用途

Publications (2)

Publication Number Publication Date
KR20210131314A KR20210131314A (ko) 2021-11-02
KR102977603B1 true KR102977603B1 (ko) 2026-06-12

Family

ID=72143544

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217022806A Active KR102977603B1 (ko) 2019-02-19 2020-02-11 헤테로시클릴 화합물, 이를 포함하는 약제학적 조성물, 이의 제조 방법, 및 이의 용도

Country Status (16)

Country Link
US (1) US20220144847A1 (enExample)
EP (1) EP3929198A4 (enExample)
JP (2) JP7615056B2 (enExample)
KR (1) KR102977603B1 (enExample)
CN (3) CN117327078A (enExample)
AU (1) AU2020226422C1 (enExample)
BR (1) BR112021016299A2 (enExample)
CA (1) CA3130245A1 (enExample)
CL (1) CL2021002205A1 (enExample)
CO (1) CO2021011023A2 (enExample)
IL (1) IL285378B2 (enExample)
MX (1) MX2021009971A (enExample)
PH (1) PH12021552004A1 (enExample)
SA (1) SA521430084B1 (enExample)
SG (1) SG11202107848TA (enExample)
WO (1) WO2020168939A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7688690B2 (ja) * 2020-07-28 2025-06-04 スーチュアン・コールン-バイオテック・バイオファーマシューティカル・カンパニー・リミテッド ピリミジン系化合物の塩、結晶形およびその調製方法
WO2022199503A1 (zh) 2021-03-24 2022-09-29 四川科伦博泰生物医药股份有限公司 杂环化合物治疗与激酶耐药突变相关的疾病的用途和方法
CN114235976B (zh) * 2021-11-09 2023-11-03 暨南大学 一种含氮杂环有机化合物中间产物的合成和分析方法
CN120897743A (zh) 2023-05-19 2025-11-04 四川科伦博泰生物医药股份有限公司 杂环化合物治疗与ret基因改变相关疾病的用途和方法
WO2025256440A1 (zh) * 2024-06-14 2025-12-18 四川科伦博泰生物医药股份有限公司 含杂环化合物富马酸盐的制备方法
WO2026017002A1 (zh) * 2024-07-16 2026-01-22 四川科伦博泰生物医药股份有限公司 以杂环化合物为活性成分的药物组合物、其制备方法及用途
GB202410599D0 (en) * 2024-07-19 2024-09-04 Ellipses Pharma Ltd Therapeutics useful synergistic combinations

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006093247A1 (ja) * 2005-02-28 2006-09-08 Japan Tobacco Inc. Syk阻害活性を有する新規なアミノピリジン化合物
WO2012154518A1 (en) * 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101166734A (zh) * 2005-02-28 2008-04-23 日本烟草产业株式会社 具有Syk抑制活性的新型的氨基吡啶化合物
WO2008013622A2 (en) * 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
US20080234267A1 (en) * 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
JP2010208945A (ja) * 2007-06-01 2010-09-24 Mitsubishi Tanabe Pharma Corp 複素環化合物
CN102812022B (zh) * 2010-01-12 2016-02-03 Ab科学有限公司 噻唑和噁唑激酶抑制剂
JP2013107824A (ja) * 2010-03-17 2013-06-06 Dainippon Sumitomo Pharma Co Ltd 新規単環ピリミジン誘導体
WO2012057262A1 (ja) * 2010-10-28 2012-05-03 日本新薬株式会社 ピリジン誘導体及び医薬
US10202365B2 (en) * 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
TWI704148B (zh) * 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JP6888101B2 (ja) * 2017-01-18 2021-06-16 アレイ バイオファーマ インコーポレイテッド RETキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピラジン化合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006093247A1 (ja) * 2005-02-28 2006-09-08 Japan Tobacco Inc. Syk阻害活性を有する新規なアミノピリジン化合物
WO2012154518A1 (en) * 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors

Also Published As

Publication number Publication date
AU2020226422A1 (en) 2021-09-09
IL285378B1 (en) 2025-07-01
PH12021552004A1 (en) 2022-09-05
NZ778907A (en) 2025-05-30
CN113316578A (zh) 2021-08-27
WO2020168939A1 (zh) 2020-08-27
CO2021011023A2 (es) 2021-09-09
AU2020226422C1 (en) 2026-04-02
JP7615056B2 (ja) 2025-01-16
JP7821259B2 (ja) 2026-02-26
KR20210131314A (ko) 2021-11-02
US20220144847A1 (en) 2022-05-12
IL285378A (en) 2021-09-30
CN117327078A (zh) 2024-01-02
JP2025060928A (ja) 2025-04-10
SG11202107848TA (en) 2021-08-30
SA521430084B1 (ar) 2025-05-01
AU2020226422B2 (en) 2025-07-31
CL2021002205A1 (es) 2022-04-22
EP3929198A1 (en) 2021-12-29
BR112021016299A2 (pt) 2021-10-13
CN113316578B (zh) 2023-10-31
JP2022521859A (ja) 2022-04-12
CN117263945A (zh) 2023-12-22
CN117263945B (zh) 2026-08-11
IL285378B2 (en) 2025-11-01
MX2021009971A (es) 2021-10-13
CA3130245A1 (en) 2020-08-27
EP3929198A4 (en) 2022-11-16

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

A201 Request for examination
PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

D21 Rejection of application intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

D22 Grant of ip right intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D22-EXM-PE0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

F11 Ip right granted following substantive examination

Free format text: ST27 STATUS EVENT CODE: A-2-4-F10-F11-EXM-PR0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

U12 Designation fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U12-OTH-PR1002 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

Q13 Ip right document published

Free format text: ST27 STATUS EVENT CODE: A-4-4-Q10-Q13-NAP-PG1601 (AS PROVIDED BY THE NATIONAL OFFICE)