JP6553629B2 - 線維芽細胞増殖因子受容体阻害剤としてのキノロン誘導体 - Google Patents

線維芽細胞増殖因子受容体阻害剤としてのキノロン誘導体 Download PDF

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JP6553629B2
JP6553629B2 JP2016550703A JP2016550703A JP6553629B2 JP 6553629 B2 JP6553629 B2 JP 6553629B2 JP 2016550703 A JP2016550703 A JP 2016550703A JP 2016550703 A JP2016550703 A JP 2016550703A JP 6553629 B2 JP6553629 B2 JP 6553629B2
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JP2017505782A (ja
JP2017505782A5 (enExample
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バーナー,エリック
アルバート ブラメルド,ケネス
アルバート ブラメルド,ケネス
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プリンシピア バイオファーマ インコーポレイテッド
プリンシピア バイオファーマ インコーポレイテッド
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

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  • 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)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016550703A 2014-02-07 2015-02-04 線維芽細胞増殖因子受容体阻害剤としてのキノロン誘導体 Active JP6553629B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201461937211P 2014-02-07 2014-02-07
US61/937,211 2014-02-07
US201462007562P 2014-06-04 2014-06-04
US62/007,562 2014-06-04
US201462069932P 2014-10-29 2014-10-29
US62/069,932 2014-10-29
PCT/US2015/014460 WO2015120049A1 (en) 2014-02-07 2015-02-04 Quinolone derivatives as fibroblast growth factor receptor inhibitors

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JP2017505782A JP2017505782A (ja) 2017-02-23
JP2017505782A5 JP2017505782A5 (enExample) 2018-02-01
JP6553629B2 true JP6553629B2 (ja) 2019-07-31

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US (6) US9815834B2 (enExample)
EP (1) EP3102577B1 (enExample)
JP (1) JP6553629B2 (enExample)
KR (1) KR102046448B1 (enExample)
CN (1) CN106459034B (enExample)
AU (1) AU2015214328B2 (enExample)
BR (1) BR112016017137B1 (enExample)
CA (1) CA2937746C (enExample)
CY (1) CY1121444T1 (enExample)
DK (1) DK3102577T3 (enExample)
ES (1) ES2689421T3 (enExample)
HU (1) HUE041594T2 (enExample)
IL (1) IL246933B (enExample)
MX (1) MX369369B (enExample)
PL (1) PL3102577T3 (enExample)
PT (1) PT3102577T (enExample)
RU (1) RU2721723C2 (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018522928A (ja) * 2015-08-11 2018-08-16 プリンシピア バイオファーマ インコーポレイテッド Fgfr阻害剤の合成方法

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106459034B (zh) 2014-02-07 2018-01-12 普林斯匹亚生物制药公司 作为成纤维细胞生长因子受体抑制剂的喹诺酮衍生物
CN105294681B (zh) 2014-07-26 2017-07-07 广东东阳光药业有限公司 Cdk类小分子抑制剂的化合物及其用途
TWI695831B (zh) 2014-09-13 2020-06-11 香港商南北兄弟藥業投資有限公司 Crth2拮抗劑化合物及其用途
CN108264510A (zh) * 2017-01-02 2018-07-10 上海喆邺生物科技有限公司 一种选择性抑制激酶化合物及其用途
WO2018153373A1 (zh) * 2017-02-27 2018-08-30 贝达药业股份有限公司 Fgfr抑制剂及其应用
AU2018229148B2 (en) * 2017-03-03 2022-08-04 Auckland Uniservices Limited FGFR kinase inhibitors and pharmaceutical uses
WO2019015593A1 (zh) * 2017-07-19 2019-01-24 江苏奥赛康药业股份有限公司 嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用
WO2019029541A1 (zh) * 2017-08-08 2019-02-14 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂及其用途
CN110016026B (zh) * 2018-01-08 2022-11-25 上海凌济生物科技有限公司 一类具有抗肿瘤活性的嘧啶并吡啶酮类化合物、制备方法和用途
KR102531596B1 (ko) * 2018-09-14 2023-05-11 아비스코 테라퓨틱스 컴퍼니 리미티드 Fgfr억제제, 그 제조 방법 및 용도
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
AU2020260018A1 (en) * 2019-04-19 2021-11-04 Pfizer Inc. Anti-proliferative agents for treating PAH
JP7121218B1 (ja) 2019-08-08 2022-08-17 ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 ピラジン-2(1h)-オン系化合物の製造方法
WO2021108803A1 (en) 2019-11-26 2021-06-03 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as jak inhibitors
KR20240170936A (ko) * 2022-03-31 2024-12-05 에이스랜드 테라퓨틱스 (홍콩) 리미티드 스피로비시클릭 화합물
CN115368219B (zh) * 2022-10-25 2022-12-27 苏州康纯医药科技有限公司 一种fgfr抑制剂关键中间体的制备方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5620981A (en) 1995-05-03 1997-04-15 Warner-Lambert Company Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
US20050009849A1 (en) 2003-01-03 2005-01-13 Veach Darren R. Pyridopyrimidine kinase inhibitors
JP4616839B2 (ja) 2003-11-13 2011-01-19 エフ.ホフマン−ラ ロシュ アーゲー ヒドロキシアルキル置換ピリド−7−ピリミジン−7−オン類
WO2005105097A2 (en) 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
US20090036472A1 (en) 2005-02-02 2009-02-05 Palle Venkata P Azabicyclo derivatives as anti-inflammatory agents
WO2008150260A1 (en) 2007-06-06 2008-12-11 Gpc Biotech, Inc. 8-oxy-2-aminopyrido (2, 3-d) pyrimidin-7-one derivatives as kinase inhibitors and anticancer agents
IT1395724B1 (it) 2009-02-25 2012-10-19 Neuroscienze Pharmaness S C A R L Composti farmaceutici
AU2012255759C1 (en) 2011-05-17 2025-10-23 Principia Biopharma, Inc. Kinase inhibitors
CN102219860B (zh) * 2011-05-20 2012-09-12 烟台荣昌生物工程有限公司 FGFR-Fc融合蛋白及其用途
BR112014010631A2 (pt) * 2011-11-04 2017-04-25 Afraxis Holdings Inc inibidores de pak para o tratamento da síndrome do x frágil
BR112015000653A2 (pt) * 2012-07-11 2019-11-05 Blueprint Medicines Corp compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos
WO2014182829A1 (en) * 2013-05-09 2014-11-13 Principia Biopharma Inc. Quinolone derivatives as fibroblast growth factor inhibitors
US9851834B2 (en) 2013-09-10 2017-12-26 Alsentis, Llc Time domain differential techniques to characterize various stimuli
CN106459034B (zh) 2014-02-07 2018-01-12 普林斯匹亚生物制药公司 作为成纤维细胞生长因子受体抑制剂的喹诺酮衍生物
EP3298011B1 (en) 2015-05-22 2021-11-17 Principia Biopharma Inc. Quinolone derivatives as fibroblast growth factor receptor inhibitors
JP6940480B2 (ja) 2015-08-11 2021-09-29 プリンシピア バイオファーマ インコーポレイテッド Fgfr阻害剤の合成方法

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018522928A (ja) * 2015-08-11 2018-08-16 プリンシピア バイオファーマ インコーポレイテッド Fgfr阻害剤の合成方法

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KR102046448B1 (ko) 2019-11-19
ES2689421T3 (es) 2018-11-14
US9815834B2 (en) 2017-11-14
US20180065960A1 (en) 2018-03-08
WO2015120049A1 (en) 2015-08-13
CN106459034B (zh) 2018-01-12
US20190233418A1 (en) 2019-08-01
CN106459034A (zh) 2017-02-22
AU2015214328B2 (en) 2019-04-18
AU2015214328A1 (en) 2016-08-04
US11078199B2 (en) 2021-08-03
PL3102577T3 (pl) 2019-03-29
US20210292323A1 (en) 2021-09-23
MX2016010106A (es) 2016-11-15
US20160200725A1 (en) 2016-07-14
IL246933B (en) 2021-05-31
JP2017505782A (ja) 2017-02-23
BR112016017137A2 (enExample) 2017-08-08
US20240092777A1 (en) 2024-03-21
IL246933A0 (en) 2016-09-29
KR20160121520A (ko) 2016-10-19
EP3102577A1 (en) 2016-12-14
US9567334B2 (en) 2017-02-14
CY1121444T1 (el) 2020-05-29
RU2721723C2 (ru) 2020-05-21
SI3102577T1 (sl) 2019-03-29
CA2937746C (en) 2020-09-01
US20160229849A1 (en) 2016-08-11
CA2937746A1 (en) 2015-08-13
US10294223B2 (en) 2019-05-21
BR112016017137B1 (pt) 2022-10-11
US12162882B2 (en) 2024-12-10
RU2016130932A (ru) 2018-03-13
RU2016130932A3 (enExample) 2018-06-19
HUE041594T2 (hu) 2019-05-28
DK3102577T3 (en) 2018-11-12
EP3102577B1 (en) 2018-07-18
MX369369B (es) 2019-11-06
PT3102577T (pt) 2018-10-23

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