TWI785474B - 用作選擇性Aurora A抑制劑的新型雜環化合物 - Google Patents

用作選擇性Aurora A抑制劑的新型雜環化合物 Download PDF

Info

Publication number
TWI785474B
TWI785474B TW110102296A TW110102296A TWI785474B TW I785474 B TWI785474 B TW I785474B TW 110102296 A TW110102296 A TW 110102296A TW 110102296 A TW110102296 A TW 110102296A TW I785474 B TWI785474 B TW I785474B
Authority
TW
Taiwan
Prior art keywords
methyl
carboxylic acid
chloro
alkyl
amino
Prior art date
Application number
TW110102296A
Other languages
English (en)
Chinese (zh)
Other versions
TW202140449A (zh
Inventor
岱 成
陳明明
李阿敏
李海軍
楊貴群
Original Assignee
大陸商北京加科思新藥研發有限公司
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 大陸商北京加科思新藥研發有限公司 filed Critical 大陸商北京加科思新藥研發有限公司
Publication of TW202140449A publication Critical patent/TW202140449A/zh
Application granted granted Critical
Publication of TWI785474B publication Critical patent/TWI785474B/zh

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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/505—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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • 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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW110102296A 2020-01-22 2021-01-21 用作選擇性Aurora A抑制劑的新型雜環化合物 TWI785474B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CN2020073786 2020-01-22
WOPCT/CN2020/073786 2020-01-22
WOPCT/CN2020/076159 2020-02-21
CN2020076159 2020-02-21
CN2020085922 2020-04-21
WOPCT/CN2020/085922 2020-04-21

Publications (2)

Publication Number Publication Date
TW202140449A TW202140449A (zh) 2021-11-01
TWI785474B true TWI785474B (zh) 2022-12-01

Family

ID=76993163

Family Applications (1)

Application Number Title Priority Date Filing Date
TW110102296A TWI785474B (zh) 2020-01-22 2021-01-21 用作選擇性Aurora A抑制劑的新型雜環化合物

Country Status (13)

Country Link
US (2) US20230128198A1 (enExample)
EP (1) EP4093736A4 (enExample)
JP (1) JP7688646B2 (enExample)
KR (1) KR102828343B1 (enExample)
CN (2) CN114423751B (enExample)
AU (1) AU2021209744B2 (enExample)
CL (1) CL2022001951A1 (enExample)
CO (1) CO2022010878A2 (enExample)
IL (1) IL294247B2 (enExample)
MX (1) MX2022009059A (enExample)
PH (1) PH12022551858A1 (enExample)
TW (1) TWI785474B (enExample)
WO (1) WO2021147974A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA53172A (fr) 2018-07-20 2021-05-26 Hoffmann La Roche Composés de sulfonimidamide en tant qu'inhibiteurs de l'activité de l'interleukine 1
CN112239465A (zh) * 2019-07-16 2021-01-19 微境生物医药科技(上海)有限公司 极光激酶抑制剂及其用途
CN112898292A (zh) 2019-12-03 2021-06-04 微境生物医药科技(上海)有限公司 新型极光激酶抑制剂及其用途
BR112022014480A2 (pt) 2020-01-22 2022-09-13 Hoffmann La Roche Compostos, composições farmacêutica, método para tratar um distúrbio em um paciente, usos de um composto e de uma composição farmacêutica e kit
CN118946560A (zh) * 2022-02-23 2024-11-12 修复治疗公司 Polo样激酶4(plk4)抑制剂、药物组合物、其制备方法和用途
CN115057811B (zh) * 2022-05-26 2024-06-14 安庆朗坤药业有限公司 一种2-溴甲基-3,5-二氟吡啶的制备方法
CN115322143B (zh) * 2022-07-21 2023-07-14 安徽德诺医药股份有限公司 一种4-哌啶甲酸叔丁酯盐酸盐的制备方法
WO2024230647A1 (zh) * 2023-05-05 2024-11-14 苏州信诺维医药科技股份有限公司 杂环类化合物、其药物组合物和其应用
CN116903587B (zh) * 2023-06-01 2024-03-22 三峡大学 一种角鲨烯环氧酶抑制剂及其用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200817363A (en) * 2006-08-31 2008-04-16 Banyu Pharma Co Ltd Novel aminopyridine derivatives having aurora a selective inhibitory action
WO2009104802A1 (en) * 2008-02-22 2009-08-27 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
TW201339150A (zh) * 2012-02-29 2013-10-01 Taiho Pharmaceutical Co Ltd 新穎哌啶化合物或其鹽
TW201629038A (zh) * 2014-11-14 2016-08-16 美國禮來大藥廠 極光ａ激酶抑制劑

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210084555A (ko) * 2018-11-30 2021-07-07 일라이 릴리 앤드 캄파니 신경모세포종의 치료에 사용하기 위한 오로라 a 키나제 억제제
CN112239465A (zh) * 2019-07-16 2021-01-19 微境生物医药科技(上海)有限公司 极光激酶抑制剂及其用途
CN112898292A (zh) * 2019-12-03 2021-06-04 微境生物医药科技(上海)有限公司 新型极光激酶抑制剂及其用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200817363A (en) * 2006-08-31 2008-04-16 Banyu Pharma Co Ltd Novel aminopyridine derivatives having aurora a selective inhibitory action
WO2009104802A1 (en) * 2008-02-22 2009-08-27 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
TW201339150A (zh) * 2012-02-29 2013-10-01 Taiho Pharmaceutical Co Ltd 新穎哌啶化合物或其鹽
TW201629038A (zh) * 2014-11-14 2016-08-16 美國禮來大藥廠 極光ａ激酶抑制劑

Also Published As

Publication number Publication date
IL294247B2 (en) 2025-11-01
KR20220131514A (ko) 2022-09-28
WO2021147974A1 (en) 2021-07-29
US20230128198A1 (en) 2023-04-27
IL294247B1 (en) 2025-07-01
MX2022009059A (es) 2022-08-15
EP4093736A4 (en) 2024-01-10
CO2022010878A2 (es) 2022-08-19
KR102828343B1 (ko) 2025-07-04
AU2021209744B2 (en) 2023-08-31
CA3161268A1 (en) 2021-07-29
CL2022001951A1 (es) 2023-04-14
TW202140449A (zh) 2021-11-01
CN116354936A (zh) 2023-06-30
CN114423751B (zh) 2023-04-21
PH12022551858A1 (en) 2024-01-03
IL294247A (en) 2022-08-01
AU2021209744A1 (en) 2022-07-07
EP4093736A1 (en) 2022-11-30
JP7688646B2 (ja) 2025-06-04
JP2023513419A (ja) 2023-03-31
US11384066B1 (en) 2022-07-12
CN114423751A (zh) 2022-04-29

Similar Documents

Publication Publication Date Title
US12570642B2 (en) GLP-IR modulating compounds
ES3025032T3 (en) Carboxy-benzimidazole glp-1r modulating compounds
CN104428299B (zh) 5-氮杂吲唑化合物及其使用方法
CN114423751B (zh) 用作选择性aurora a抑制剂的新型杂环化合物
KR102851010B1 (ko) 포스파티딜이노시톨 3-키나제 저해제
KR20240127910A (ko) Sos1 억제제 및 항암제를 포함하는 암 치료용 약학 조성물
WO2024067714A1 (zh) 具有抗kras突变肿瘤活性的化合物
KR102609431B1 (ko) Phd 저해제로서의 활성을 갖는 융합된 바이시클릭 헤테로아릴 유도체
TW202214605A (zh) 免疫調節劑、組合物及其方法
WO2025061125A1 (zh) 一种大环化合物及其制备方法和用途
WO2016011390A1 (en) Irak4 inhibiting agents
TW202220987A (zh) 經取代雜環化合物及其治療用途
CA3161268C (en) Heterocyclic compounds useful as aurora a selective inhibitors
HK40066473B (en) Novel heterocyclic compounds useful as aurora a selective inhibitors
HK40129387A (en) Pyridone and pyrimidinone inhibitors of hematopoietic progenitor kinase 1
HK40105619A (en) Rip1 modulators including azetidine cyclic ureas, preparations, and uses thereof
HK40066473A (en) Novel heterocyclic compounds useful as aurora a selective inhibitors
HK1208439B (en) 5-azaindazole compounds and methods of use
HK1249512B (en) Fused bicyclic heteroaryl derivatives having activity as phd inhibitors