TWI730012B - 化學化合物 - Google Patents

化學化合物 Download PDF

Info

Publication number
TWI730012B
TWI730012B TW105136236A TW105136236A TWI730012B TW I730012 B TWI730012 B TW I730012B TW 105136236 A TW105136236 A TW 105136236A TW 105136236 A TW105136236 A TW 105136236A TW I730012 B TWI730012 B TW I730012B
Authority
TW
Taiwan
Prior art keywords
methyl
pyridine
dihydroimidazo
amino
pyrazol
Prior art date
Application number
TW105136236A
Other languages
English (en)
Chinese (zh)
Other versions
TW201728586A (zh
Inventor
克理佛德 大衛 瓊斯
里察 安德魯 華德
史蒂芬 史瓦洛
馬克 安卓 葛拉漢
安德魯 賀比 都伯森
詹姆士 麥卡貝
Original Assignee
瑞典商阿斯特捷利康公司
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 瑞典商阿斯特捷利康公司 filed Critical 瑞典商阿斯特捷利康公司
Publication of TW201728586A publication Critical patent/TW201728586A/zh
Application granted granted Critical
Publication of TWI730012B publication Critical patent/TWI730012B/zh

Links

Images

Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW105136236A 2015-11-09 2016-11-08 化學化合物 TWI730012B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562252726P 2015-11-09 2015-11-09
US62/252,726 2015-11-09
US201662401351P 2016-09-29 2016-09-29
US62/401,351 2016-09-29

Publications (2)

Publication Number Publication Date
TW201728586A TW201728586A (zh) 2017-08-16
TWI730012B true TWI730012B (zh) 2021-06-11

Family

ID=57241113

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105136236A TWI730012B (zh) 2015-11-09 2016-11-08 化學化合物

Country Status (35)

Country Link
US (2) US9902731B2 (enExample)
EP (1) EP3374359B1 (enExample)
JP (1) JP6877423B2 (enExample)
KR (1) KR20180074788A (enExample)
CN (1) CN108349983B (enExample)
AU (1) AU2016351813B2 (enExample)
BR (1) BR112018008397B1 (enExample)
CA (1) CA3003549A1 (enExample)
CL (1) CL2018001226A1 (enExample)
CO (1) CO2018004857A2 (enExample)
CR (1) CR20180316A (enExample)
CY (1) CY1123627T1 (enExample)
DK (1) DK3374359T3 (enExample)
EA (1) EA038028B1 (enExample)
ES (1) ES2780650T3 (enExample)
HR (1) HRP20200342T1 (enExample)
IL (1) IL258953A (enExample)
LT (1) LT3374359T (enExample)
ME (1) ME03770B (enExample)
MX (1) MX376639B (enExample)
MY (1) MY197626A (enExample)
NI (1) NI201800058A (enExample)
PE (1) PE20181288A1 (enExample)
PH (1) PH12018500987A1 (enExample)
PL (1) PL3374359T3 (enExample)
PT (1) PT3374359T (enExample)
RS (1) RS60155B1 (enExample)
SG (1) SG11201803066VA (enExample)
SI (1) SI3374359T1 (enExample)
SM (1) SMT202000152T1 (enExample)
SV (1) SV2018005687A (enExample)
TN (1) TN2018000119A1 (enExample)
TW (1) TWI730012B (enExample)
WO (1) WO2017080979A1 (enExample)
ZA (1) ZA201803742B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017068412A1 (en) 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
SMT202000152T1 (it) * 2015-11-09 2020-05-08 Astrazeneca Ab Derivati di diidroimidazopirazinone utili nel trattamento di cancro
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
JP7352981B2 (ja) * 2018-10-10 2023-09-29 深▲チェン▼市塔吉瑞生物医薬有限公司 ジヒドロイミダゾピラジノン化合物、該化合物を含む組成物およびその使用
KR20210145773A (ko) 2019-03-28 2021-12-02 지앙수 헨그루이 메디슨 컴퍼니 리미티드 티에노헤테로고리형 유도체, 이의 제조 방법 및 이의 의약적 용도
EP3978498A1 (en) 2019-05-24 2022-04-06 Jiangsu Hengrui Medicine Co., Ltd. Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines
PH12021553058A1 (en) 2019-06-06 2022-07-25 Hutchison Medipharma Ltd Tricyclic compounds and their use
TW202134242A (zh) 2019-12-05 2021-09-16 瑞典商阿斯特捷利康公司 用於生產式(i)之方法及中間體
EP4071155A4 (en) * 2019-12-06 2024-01-17 D3 Bio (Wuxi) Co., Ltd. Thiazololactam compound as erk inhibitor and use thereof
US20230331731A1 (en) 2020-09-29 2023-10-19 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Crystal form of pyrrolo heterocyclic derivative and preparation method therefor
AR126166A1 (es) * 2021-06-18 2023-09-27 Antengene Discovery Ltd Combinación de un inhibidor de erk y un inhibidor de kras y usos de estos
WO2022268065A1 (en) * 2021-06-22 2022-12-29 Fochon Biosciences, Ltd. Compounds as erk inhibitors
EP4378478A4 (en) 2021-07-27 2025-11-12 Toray Industries MEDICINE FOR THE TREATMENT AND/OR PREVENTION OF CANCER
EP4426702A1 (en) 2021-11-04 2024-09-11 Skyhawk Therapeutics, Inc. Condensed-pyrazine amine derivatives for treating sca3
EP4514807B1 (en) 2022-04-27 2025-12-17 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
US20260027118A1 (en) 2022-05-12 2026-01-29 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
WO2024006971A2 (en) * 2022-07-01 2024-01-04 The Scripps Research Institute Antimalarial compounds

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007042784A2 (en) * 2005-10-14 2007-04-19 Cyclacel Limited Pyrimidin-4-yl-3, 4-dihydr0-2h- pyrrolo [1, 2a] pyrazin-1-one compounds

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
WO2004041826A1 (en) * 2002-11-06 2004-05-21 Merck Sharp & Dohme Limited Imidazopyrazinones and imidazotriazinones derivates as gaba-a receptor anxiolytic
CN101611007A (zh) * 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
ES2648143T3 (es) * 2010-12-22 2017-12-28 Janssen Pharmaceutica Nv Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE)
MX381326B (es) * 2011-10-10 2025-03-12 H Lundbeck As Derivados de 7h-imidazo[1-5-a]pirazin-8-ona como inhibidores de la fosfodiesterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativos
JP2013166727A (ja) * 2012-02-16 2013-08-29 Dainippon Sumitomo Pharma Co Ltd ジヒドロイミダゾピラジノン誘導体
PE20150666A1 (es) 2012-03-01 2015-05-06 Array Biopharma Inc Inhibidores de serina/treonina cinasa
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
EA031243B1 (ru) 2013-12-06 2018-12-28 Дженентек, Инк. Ингибиторы серин/треонинкиназ
MX375902B (es) * 2013-12-30 2025-03-07 Genentech Inc Inhibidores de serina/treonina cinasa.
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
CN106659721B (zh) 2014-04-09 2021-01-01 基因泰克公司 用于制备药物的方法
US10412619B2 (en) * 2014-11-14 2019-09-10 Qualcomm Incorporated Buffer status report for eDCS
WO2016162325A1 (en) 2015-04-07 2016-10-13 Astrazeneca Ab Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors
WO2016192064A1 (en) 2015-06-03 2016-12-08 Js Innopharm (Shanghai) Ltd. Heterocyclic compounds for treating psoriasis
WO2016192063A1 (en) 2015-06-03 2016-12-08 Changzhou Jiekai Pharmatech Co. Ltd Heterocyclic compounds as erk inhibitors
SMT202000152T1 (it) * 2015-11-09 2020-05-08 Astrazeneca Ab Derivati di diidroimidazopirazinone utili nel trattamento di cancro

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007042784A2 (en) * 2005-10-14 2007-04-19 Cyclacel Limited Pyrimidin-4-yl-3, 4-dihydr0-2h- pyrrolo [1, 2a] pyrazin-1-one compounds

Also Published As

Publication number Publication date
RS60155B1 (sr) 2020-05-29
KR20180074788A (ko) 2018-07-03
TW201728586A (zh) 2017-08-16
AU2016351813B2 (en) 2019-05-30
CO2018004857A2 (es) 2018-07-19
EA201891063A1 (ru) 2018-12-28
TN2018000119A1 (en) 2019-10-04
SMT202000152T1 (it) 2020-05-08
CN108349983B (zh) 2021-02-26
EP3374359A1 (en) 2018-09-19
US20180237443A1 (en) 2018-08-23
DK3374359T3 (da) 2020-03-30
PT3374359T (pt) 2020-03-27
JP2019503337A (ja) 2019-02-07
BR112018008397B1 (pt) 2023-12-12
ME03770B (me) 2021-04-20
HRP20200342T1 (hr) 2020-06-12
MY197626A (en) 2023-06-29
EP3374359B1 (en) 2020-01-08
EA038028B1 (ru) 2021-06-24
SG11201803066VA (en) 2018-05-30
LT3374359T (lt) 2020-03-25
WO2017080979A1 (en) 2017-05-18
ZA201803742B (en) 2020-08-26
IL258953A (en) 2018-06-28
CY1123627T1 (el) 2022-03-24
MX2018005725A (es) 2018-08-14
ES2780650T3 (es) 2020-08-26
US20170204100A1 (en) 2017-07-20
AU2016351813A1 (en) 2018-06-21
US9902731B2 (en) 2018-02-27
MX376639B (es) 2025-03-07
PH12018500987A1 (en) 2019-01-28
JP6877423B2 (ja) 2021-05-26
CR20180316A (es) 2018-10-05
BR112018008397A2 (pt) 2018-10-23
SI3374359T1 (sl) 2020-04-30
US10202391B2 (en) 2019-02-12
HK1256283A1 (en) 2019-09-20
CN108349983A (zh) 2018-07-31
CL2018001226A1 (es) 2018-10-05
CA3003549A1 (en) 2017-05-18
PE20181288A1 (es) 2018-08-07
SV2018005687A (es) 2018-07-20
PL3374359T3 (pl) 2020-06-29
NI201800058A (es) 2018-10-18

Similar Documents

Publication Publication Date Title
CN108349983B (zh) 治疗癌症有用的二氢咪唑并吡嗪酮衍生物
EP2948447B1 (en) Chemical compounds
WO2017080980A1 (en) Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
RU2664109C2 (ru) ПРОИЗВОДНЫЕ ТЕТРАГИДРОПИРИДО[3,4-b]ИНДОЛА, ПОЛЕЗНЫЕ ПРИ ЛЕЧЕНИИ РАКА
JP6898919B2 (ja) 新規化合物
CN108137546B (zh) 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途
HK1256283B (en) Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
HK1214592B (en) Chemical compounds
HK1254965B (en) New compounds

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees