CN106164076B - 作为ros1抑制剂的化合物 - Google Patents

作为ros1抑制剂的化合物 Download PDF

Info

Publication number
CN106164076B
CN106164076B CN201580016470.XA CN201580016470A CN106164076B CN 106164076 B CN106164076 B CN 106164076B CN 201580016470 A CN201580016470 A CN 201580016470A CN 106164076 B CN106164076 B CN 106164076B
Authority
CN
China
Prior art keywords
alkyl
hydrogen
group
replaced
oxy
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
CN201580016470.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN106164076A (zh
Inventor
L.A.梅维勒奇
E.T.J.帕基尔
S.德康
G.J.M.梅塞
B.弗罗布洛夫斯基
J.E.维亚拉尔
L.米尔佩尔
M.L.让蒂
T.F.A.J.茹索姆
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.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of CN106164076A publication Critical patent/CN106164076A/zh
Application granted granted Critical
Publication of CN106164076B publication Critical patent/CN106164076B/zh
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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C07D487/10—Spiro-condensed 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
    • C07D487/12—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 three hetero rings
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201580016470.XA 2014-03-27 2015-03-26 作为ros1抑制剂的化合物 Active CN106164076B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161950 2014-03-27
EP14161950.2 2014-03-27
PCT/EP2015/056498 WO2015144799A1 (en) 2014-03-27 2015-03-26 SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS

Publications (2)

Publication Number Publication Date
CN106164076A CN106164076A (zh) 2016-11-23
CN106164076B true CN106164076B (zh) 2019-03-26

Family

ID=50389872

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580016470.XA Active CN106164076B (zh) 2014-03-27 2015-03-26 作为ros1抑制剂的化合物

Country Status (13)

Country Link
US (1) US10280170B2 (enExample)
EP (1) EP3129376B1 (enExample)
JP (1) JP6522646B2 (enExample)
KR (1) KR102455519B1 (enExample)
CN (1) CN106164076B (enExample)
AU (1) AU2015238296B2 (enExample)
BR (1) BR112016022105B1 (enExample)
CA (1) CA2940918C (enExample)
EA (1) EA032255B1 (enExample)
ES (1) ES2715676T3 (enExample)
IL (1) IL247947B (enExample)
MX (1) MX367914B (enExample)
WO (1) WO2015144799A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6116782B1 (ja) * 2015-08-28 2017-04-19 積水メディカル株式会社 ベンジル化合物
TWI782056B (zh) * 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有ｍｇａｔ２抑制活性的縮合環衍生物
WO2019233456A1 (zh) * 2018-06-08 2019-12-12 贝达药业股份有限公司 Erk抑制剂及其应用
KR20210114001A (ko) * 2019-01-11 2021-09-17 시오노기 앤드 컴파니, 리미티드 Mgat2 저해 활성을 갖는 다이하이드로피라졸로피라지논 유도체
JP7068743B2 (ja) * 2019-01-11 2022-05-17 塩野義製薬株式会社 Ｍｇａｔ２阻害活性を有する縮合環誘導体を含有する医薬組成物
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN114315866B (zh) * 2020-09-30 2023-10-31 烟台药物研究所 一种盐酸左旋咪唑的合成方法
TW202229282A (zh) * 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
WO2022127756A1 (en) * 2020-12-15 2022-06-23 Gritscience Biopharmaceuticals Co., Ltd. Compounds as casein kinase inhibitors
CN114957259A (zh) * 2021-02-25 2022-08-30 南京明德新药研发有限公司 氰基取代的芳香双环类化合物及其应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1747949A (zh) * 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
CN101889012A (zh) * 2007-12-12 2010-11-17 杜邦公司 杀真菌二环吡唑
CN102056927A (zh) * 2008-05-13 2011-05-11 Irm责任有限公司 作为激酶抑制剂的稠合含氮杂环及其组合物
CN102083835A (zh) * 2008-02-29 2011-06-01 惠氏有限责任公司 吡唑并[1，5-a]嘧啶的桥联双环杂环或螺双环杂环衍生物、其制备方法和用途
WO2011153553A2 (en) * 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
US7662826B2 (en) 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
CA2494700C (en) 2002-08-26 2011-06-28 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
JP2005343889A (ja) 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
EP2235020A1 (en) 2007-12-21 2010-10-06 Wyeth LLC Pyrazolo [1,5-a] pyrimidine compounds
KR101238585B1 (ko) 2008-04-07 2013-02-28 노파르티스 아게 단백질 키나제 억제제로서의 화합물 및 조성물
EP2271645A1 (en) * 2008-04-07 2011-01-12 Irm Llc Compounds and compositions as kinase inhibitors
CN102459264A (zh) * 2009-05-27 2012-05-16 雅培制药有限公司 激酶活性的嘧啶抑制剂
EP2434960A1 (en) 2009-05-28 2012-04-04 Cook Medical Technologies LLC Tacking device and methods of deployment
WO2013017989A1 (en) * 2011-08-02 2013-02-07 Pfizer Inc. Crizotinib for use in the treatment of cancer
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1747949A (zh) * 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
CN101889012A (zh) * 2007-12-12 2010-11-17 杜邦公司 杀真菌二环吡唑
CN102083835A (zh) * 2008-02-29 2011-06-01 惠氏有限责任公司 吡唑并[1，5-a]嘧啶的桥联双环杂环或螺双环杂环衍生物、其制备方法和用途
CN102056927A (zh) * 2008-05-13 2011-05-11 Irm责任有限公司 作为激酶抑制剂的稠合含氮杂环及其组合物
WO2011153553A2 (en) * 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition

Also Published As

Publication number Publication date
ES2715676T3 (es) 2019-06-05
IL247947B (en) 2019-03-31
JP2017508779A (ja) 2017-03-30
CA2940918A1 (en) 2015-10-01
CN106164076A (zh) 2016-11-23
KR102455519B1 (ko) 2022-10-14
US10280170B2 (en) 2019-05-07
US20170174690A1 (en) 2017-06-22
EA032255B1 (ru) 2019-04-30
MX2016012668A (es) 2016-12-14
MX367914B (es) 2019-09-11
KR20160137576A (ko) 2016-11-30
EP3129376A1 (en) 2017-02-15
BR112016022105B1 (pt) 2023-01-31
WO2015144799A1 (en) 2015-10-01
AU2015238296A1 (en) 2016-09-08
BR112016022105A2 (enExample) 2017-08-15
CA2940918C (en) 2023-10-24
JP6522646B2 (ja) 2019-05-29
AU2015238296B2 (en) 2018-10-18
EP3129376B1 (en) 2018-12-26
EA201691930A1 (ru) 2017-02-28

Similar Documents

Publication Publication Date Title
CN106164076B (zh) 作为ros1抑制剂的化合物
TWI871397B (zh) Ｋｒａｓ突變蛋白抑制劑
TWI727981B (zh) 氧雜螺環類衍生物、其製備方法及其在醫藥上的應用
CN104910148B (zh) 氨基三唑并吡啶和其作为激酶抑制剂的用途
CN106132967B (zh) 作为ros1抑制剂的化合物
CN104109151B (zh) N‑(2‑{2‑二甲氨基乙基‑甲氨基}‑4‑甲氧基‑5‑{[4‑(1‑甲基吲哚‑3‑基)嘧啶‑2‑基]氨基}苯基)丙‑2‑烯酰胺的甲磺酸盐的多晶型
CN109563043A (zh) 作为dnmt1的抑制剂的取代的吡啶
CN109219604A (zh) 四氢异喹啉雌激素受体调节剂及其用途
CN113382986A (zh) 酪氨酸激酶抑制剂组合物、其制备方法和使用方法
JP2017508779A5 (enExample)
CN109641885A (zh) 作为免疫调节剂的杂环化合物
BR112016020621B1 (pt) Composto, composição farmacêutica, inibidor de atividade da enzima ezh1 e/ou ezh2, agente terapêutico para tumores, e, agente antitumor
CN102858765A (zh) 吡唑基喹唑啉激酶抑制剂
TW201625305A (zh) 用於癌症治療之組合療法
CN114213415A (zh) 大环嘧啶衍生物
CN109641882A (zh) 作为nik抑制剂的杂芳族衍生物
SA518391217B1 (ar) Mdm2-p53 مثبطات أيزو إندولينون لتفاعل ذات نشاط مضاد للسرطان
TW202340196A (zh) 含有雜環的化合物及其應用
CN106279160B (zh) N‑苯基‑2‑氨基嘧啶类化合物制备方法和用途
CN109311846A (zh) 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物
CN109689645A (zh) 作为nik抑制剂的氰基吲哚啉衍生物
TW202110848A (zh) 取代的稠合雙環類衍生物、其製備方法及其在醫藥上的應用
CN113518779A (zh) 噻吩并杂环类衍生物、其制备方法及其在医药上的应用
TW202016093A (zh) Ｏｇａ抑制劑化合物
CN107108633B (zh) 作为PI3Kβ抑制剂的杂环基连接的咪唑并哒嗪衍生物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant