JP6709786B2 - Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体 - Google Patents

Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体 Download PDF

Info

Publication number
JP6709786B2
JP6709786B2 JP2017530208A JP2017530208A JP6709786B2 JP 6709786 B2 JP6709786 B2 JP 6709786B2 JP 2017530208 A JP2017530208 A JP 2017530208A JP 2017530208 A JP2017530208 A JP 2017530208A JP 6709786 B2 JP6709786 B2 JP 6709786B2
Authority
JP
Japan
Prior art keywords
cancer
pharmaceutically acceptable
methyl
solvate
indol
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
JP2017530208A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017537114A (ja
JP2017537114A5 (enExample
Inventor
ペン，ジュロン
コスタンゾ，マイケル，ジョン
グレコ，マイケル，ニコラス
グリーン，マイケル，アラン
ワイルド，ビクトリア，リン
チャン，ドン
Original Assignee
ベータ ファーマ，インコーポレイテッド
ベータ ファーマ，インコーポレイテッド
ベータ ファーマ（シャンハイ）カンパニー，リミテッド
ベータ ファーマ（シャンハイ）カンパニー，リミテッド
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 ベータ ファーマ，インコーポレイテッド, ベータ ファーマ，インコーポレイテッド, ベータ ファーマ（シャンハイ）カンパニー，リミテッド, ベータ ファーマ（シャンハイ）カンパニー，リミテッド filed Critical ベータ ファーマ，インコーポレイテッド
Publication of JP2017537114A publication Critical patent/JP2017537114A/ja
Publication of JP2017537114A5 publication Critical patent/JP2017537114A5/ja
Application granted granted Critical
Publication of JP6709786B2 publication Critical patent/JP6709786B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • C07D403/14—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 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
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017530208A 2014-12-11 2015-12-11 Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体 Active JP6709786B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462090869P 2014-12-11 2014-12-11
US62/090,869 2014-12-11
US201562166883P 2015-05-27 2015-05-27
US62/166,883 2015-05-27
PCT/US2015/065286 WO2016094821A2 (en) 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as egfr modulators

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2020090467A Division JP7181558B2 (ja) 2014-12-11 2020-05-25 Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体

Publications (3)

Publication Number Publication Date
JP2017537114A JP2017537114A (ja) 2017-12-14
JP2017537114A5 JP2017537114A5 (enExample) 2019-01-17
JP6709786B2 true JP6709786B2 (ja) 2020-06-17

Family

ID=56108380

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2017530208A Active JP6709786B2 (ja) 2014-12-11 2015-12-11 Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体
JP2020090467A Active JP7181558B2 (ja) 2014-12-11 2020-05-25 Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2020090467A Active JP7181558B2 (ja) 2014-12-11 2020-05-25 Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体

Country Status (17)

Country Link
US (2) US10590111B2 (enExample)
EP (1) EP3229798A4 (enExample)
JP (2) JP6709786B2 (enExample)
KR (1) KR20170098865A (enExample)
CN (3) CN112375067B (enExample)
AU (1) AU2015360360B2 (enExample)
BR (1) BR112017012272A2 (enExample)
CA (1) CA2970185C (enExample)
CO (1) CO2017006962A2 (enExample)
EA (1) EA036453B1 (enExample)
HK (1) HK1245634A1 (enExample)
IL (1) IL252554A0 (enExample)
MX (1) MX382869B (enExample)
PH (1) PH12017501057A1 (enExample)
SG (2) SG11201704685TA (enExample)
TW (1) TWI618704B (enExample)
WO (1) WO2016094821A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020143131A (ja) * 2014-12-11 2020-09-10 ベータ ファーマ，インコーポレイテッド Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US11052086B2 (en) * 2016-05-11 2021-07-06 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
EP3471730B1 (en) 2016-06-17 2021-10-20 Beta Pharma, Inc. Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof
CN106243044A (zh) * 2016-06-30 2016-12-21 浙江大学 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用
CN108602802B (zh) * 2016-07-26 2020-01-21 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
MX2019015177A (es) * 2017-06-16 2020-02-07 Beta Pharma Inc Formulaciones farmaceuticas de n-(2-(2-(dimetilamino)etoxi)-4-meto xi-5((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilam ida y las sales de ellas.
CN109503573A (zh) * 2017-09-14 2019-03-22 昆明圣加南生物科技有限公司 2-取代苯胺基嘧啶衍生物及其用途
CN107935995A (zh) * 2017-11-28 2018-04-20 中山大学 一种新型2‑苯胺基嘧啶衍生物及其在制备抗肿瘤药物中的应用
CN108017633A (zh) * 2018-01-30 2018-05-11 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用
PT3806898T (pt) * 2018-06-18 2025-12-02 UCB Biopharma SRL Antagonista de gremlin-1 para utilização no tratamento do cancro
IL281344B2 (en) 2018-09-10 2025-09-01 Mirati Therapeutics Inc Combination of adagrasib and cetuximab for cancer treatment
US12390464B2 (en) 2019-09-23 2025-08-19 Beta Pharma, Inc. Treatment of EGFR mutant-related cancers using a combination of EGFR and CDK4/6 inhibitors
WO2021094379A1 (en) 2019-11-12 2021-05-20 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
CA3166980A1 (en) 2020-01-20 2021-07-29 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
US20250136576A1 (en) * 2021-07-13 2025-05-01 ACEA Therapeutics, Inc. Heterocyclic Compounds and Uses Thereof
CN119278041A (zh) 2022-03-31 2025-01-07 阿斯利康(瑞典)有限公司 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体（egfr）酪氨酸激酶抑制剂
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
AU2023262556A1 (en) 2022-04-28 2024-12-05 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
MA71241A (fr) 2022-06-27 2025-04-30 Astrazeneca Ab Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer
JP2025522965A (ja) 2022-07-08 2025-07-17 アストラゼネカ・アクチエボラーグ 癌の治療のためのｈｇｆ受容体阻害剤と組み合わせた上皮成長因子受容体チロシンキナーゼ阻害剤
WO2025238661A1 (en) * 2024-05-17 2025-11-20 Bdr Lifesciences Private Limited An improved process for the preparation of osimertinib

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001047922A2 (en) * 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
JP5179509B2 (ja) * 2006-12-08 2013-04-10 エフ．ホフマン−ラ ロシュ アーゲー 置換ピリミジン類及びｊｎｋモジュレーターとしてのこれらの使用
WO2010059711A1 (en) * 2008-11-18 2010-05-27 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
BR112013027734A2 (pt) * 2011-05-04 2017-08-08 Ariad Pharma Inc compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica
EP2736895B1 (en) * 2011-07-27 2016-01-06 Astrazeneca AB 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer
AU2013204563B2 (en) * 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
PE20170268A1 (es) 2014-06-19 2017-04-21 Ariad Pharma Inc Compuestos de heteroarilo para la inhibicion de cinasa
CN106458969A (zh) * 2014-08-25 2017-02-22 四川海思科制药有限公司 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途
CN105461695B (zh) * 2014-09-29 2018-03-27 齐鲁制药有限公司 嘧啶或三嗪衍生物及其制备方法和用途
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US10590111B2 (en) * 2014-12-11 2020-03-17 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as EGFR modulators

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020143131A (ja) * 2014-12-11 2020-09-10 ベータ ファーマ，インコーポレイテッド Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体
JP7181558B2 (ja) 2014-12-11 2022-12-01 ベータ ファーマ，インコーポレイテッド Ｅｇｆｒモジュレーターとしての置換２－アミノピリミジン誘導体

Also Published As

Publication number Publication date
US11414401B2 (en) 2022-08-16
AU2015360360A1 (en) 2017-06-08
CA2970185C (en) 2023-10-17
CN112457298B (zh) 2024-05-07
CN112375067A (zh) 2021-02-19
CN112457298A (zh) 2021-03-09
SG10201909060SA (en) 2019-11-28
EA201790921A1 (ru) 2017-12-29
JP2017537114A (ja) 2017-12-14
IL252554A0 (en) 2017-07-31
CN112375067B (zh) 2024-03-15
EP3229798A4 (en) 2018-05-30
TW201632512A (zh) 2016-09-16
PH12017501057A1 (en) 2018-03-05
EA036453B1 (ru) 2020-11-12
AU2015360360B2 (en) 2020-06-25
BR112017012272A2 (pt) 2018-01-30
JP7181558B2 (ja) 2022-12-01
KR20170098865A (ko) 2017-08-30
CN108024993A (zh) 2018-05-11
US20170362203A1 (en) 2017-12-21
CO2017006962A2 (es) 2017-10-20
US10590111B2 (en) 2020-03-17
MX382869B (es) 2025-03-13
WO2016094821A2 (en) 2016-06-16
TWI618704B (zh) 2018-03-21
EP3229798A2 (en) 2017-10-18
JP2020143131A (ja) 2020-09-10
MX2017007664A (es) 2018-01-23
CA2970185A1 (en) 2016-06-16
SG11201704685TA (en) 2017-07-28
WO2016094821A3 (en) 2016-08-25
CN108024993B (zh) 2020-11-06
HK1245634A1 (zh) 2018-08-31
US20200216421A1 (en) 2020-07-09

Similar Documents

Publication Publication Date Title
JP6709786B2 (ja) Ｅｇｆｒモジュレーターとしての置換２−アミノピリミジン誘導体
JP6431593B2 (ja) ピリジニルアミノピリミジン誘導体、その製造方法、および用途
JP6101341B2 (ja) 置換ピリドピリミジン化合物およびｆｌｔ３阻害剤としてのこれらの使用
JP7337395B2 (ja) Ｃｄｋ４およびｃｄｋ６阻害剤としての２ｈ－インダゾール誘導体およびその治療上の使用
CN105315285B (zh) 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
CN105377835A (zh) 酪氨酸蛋白激酶调节剂及其应用方法
CN108503627A (zh) 用作egfr抑制剂的2,4-二取代苯-1,5-二胺衍生物及其应用
CN103936762A (zh) 吗啉并喹啉类化合物，其制备方法和用途
JP2025081599A (ja) Ｅｇｆｒキナーゼを阻害する化合物、調製方法、及びその使用
JP6943886B2 (ja) 縮合ピリミジノピペリジン誘導体、ならびにその製造方法および適用
OA18657A (en) Substituted 2-anilinopyrimidine derivatives as EGFR modulators.
HK40081466A (en) Efgr inhibitor, preparation method therefor, and application thereof
HK1221953A1 (zh) 酪氨酸蛋白激酶调节剂及其应用方法
KR20160030296A (ko) 단백질 티로신 키나제 조절자 및 사용 방법

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171026

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181130

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20181130

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190829

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190910

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20191209

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: 20200428

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20200525

R150 Certificate of patent or registration of utility model

Ref document number: 6709786

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250