ES2925212T3 - Compuesto heterocíclico sustituido con alquinilo, método de preparación y uso médico del mismo - Google Patents

Compuesto heterocíclico sustituido con alquinilo, método de preparación y uso médico del mismo Download PDF

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Publication number
ES2925212T3
ES2925212T3 ES17849992T ES17849992T ES2925212T3 ES 2925212 T3 ES2925212 T3 ES 2925212T3 ES 17849992 T ES17849992 T ES 17849992T ES 17849992 T ES17849992 T ES 17849992T ES 2925212 T3 ES2925212 T3 ES 2925212T3
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Prior art keywords
mmol
ethynyl
compound
cancer
dimethoxyphenyl
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ES17849992T
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English (en)
Spanish (es)
Inventor
Xiangyang Chen
Yingxiang Gao
Norman Xianglong Kong
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Beijing Innocare Pharma Tech Co Ltd
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Beijing Innocare Pharma Tech Co Ltd
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    • 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
    • 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
    • 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
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/435—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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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

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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES17849992T 2016-09-19 2017-01-25 Compuesto heterocíclico sustituido con alquinilo, método de preparación y uso médico del mismo Active ES2925212T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610833890.3A CN107840842A (zh) 2016-09-19 2016-09-19 炔代杂环化合物、其制备方法及其在医药学上的应用
PCT/CN2017/072570 WO2018049781A1 (zh) 2016-09-19 2017-01-25 炔代杂环化合物、其制备方法及其在医药学上的应用

Publications (1)

Publication Number Publication Date
ES2925212T3 true ES2925212T3 (es) 2022-10-14

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ES17849992T Active ES2925212T3 (es) 2016-09-19 2017-01-25 Compuesto heterocíclico sustituido con alquinilo, método de preparación y uso médico del mismo

Country Status (12)

Country Link
US (3) US10710981B2 (enExample)
EP (1) EP3517535B1 (enExample)
JP (1) JP6906811B2 (enExample)
KR (1) KR102783517B1 (enExample)
CN (2) CN107840842A (enExample)
AU (1) AU2017327954B2 (enExample)
CA (1) CA3036594C (enExample)
ES (1) ES2925212T3 (enExample)
MX (1) MX390747B (enExample)
RU (1) RU2729069C1 (enExample)
SG (1) SG10202102822RA (enExample)
WO (1) WO2018049781A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7497357B2 (ja) * 2018-12-13 2024-06-10 インターベット インターナショナル ベー． フェー． １－［（３ｒ，４ｓ）－４－シアノテトラヒドロピラン－３－イル］－３－［（２－フルオロ－６－メトキシ－４－ピリジル）アミノ］ピラゾール－４－カルボキサミドの調製方法
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
MX2022007988A (es) * 2019-12-26 2022-07-11 Beijing Innocare Pharma Tech Co Ltd Formas cristalinas de (s)-1-(1-acriloilpirrolidin-3-il)-3-((3,5-di metoxifenil)etinil)-5-(metilamino)-1h-pirazol-4-carboxamida.
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
US11345681B1 (en) * 2020-06-05 2022-05-31 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
WO2022042613A1 (zh) * 2020-08-27 2022-03-03 上海和誉生物医药科技有限公司 一种1h-吡唑-4-酰胺衍生物，其制备方法和应用
AU2022206989A1 (en) 2021-01-12 2023-08-24 Beijing Innocare Pharma Tech Co., Ltd. Process for preparing (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl) ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide
CN115433190B (zh) * 2021-06-02 2024-09-20 药雅科技(上海)有限公司 不可逆杂环化合物fgfr抑制剂的制备方法和用途
CN114853739B (zh) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN115043832B (zh) * 2021-03-08 2023-08-22 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
AU2022381641A1 (en) * 2021-11-03 2024-06-20 Beijing Innocare Pharma Tech Co., Ltd. Amorphous solid dispersion comprising (s) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1h-pyrazole-4-carboxamide
CA3238193A1 (en) * 2021-11-16 2023-05-25 Jisong Cui Method for treating head and neck cancer
KR20240119095A (ko) * 2021-12-08 2024-08-06 킨네이트 바이오파마 인크. Fgfr 저해제의 고체 상태 형태
AU2022407439A1 (en) * 2021-12-08 2024-06-27 Kinnate Biopharma Inc. Treatment of cancer with an fgfr kinase inhibitor
WO2023107870A1 (en) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
US20250332105A1 (en) * 2024-04-25 2025-10-30 Beijing Innocare Pharma Tech Co., Ltd. Amorphous solid dispersion comprising (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl)ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2833948B1 (fr) * 2001-12-21 2004-02-06 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et leur utilisation en tant que medicament
RU2340605C2 (ru) 2002-06-27 2008-12-10 Ново Нордиск А/С Арилкарбонильные производные в качестве терапевтических средств
CN1508130A (zh) 2002-12-18 2004-06-30 中国科学院大连化学物理研究所 N-苯基-n’-嘧啶基取代脲类衍生物的合成方法
US7150894B2 (en) * 2003-05-01 2006-12-19 Kraft Foods Holdings, Inc. Acid whey texture system
PT1761520E (pt) 2004-06-23 2008-09-15 Lilly Co Eli Inibidores de quinase
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
EP1966222A2 (en) 2005-11-16 2008-09-10 SGX Pharmaceuticals, Inc. Pyrazolothiazole protein kinase modulators
FR2908409B1 (fr) 2006-11-10 2009-01-09 Sanofi Aventis Sa Pyrazoles substituees,compositions les contenant,procede de fabrication et utilisation
ES2364864T3 (es) * 2006-12-21 2011-09-15 Astrazeneca Ab Acilaminopirazoles como inhibidores de fgfr.
US7737149B2 (en) * 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
MX2010014066A (es) 2008-06-16 2011-06-01 Univ Tennessee Res Foundation Compuestos para el tratamiento del cancer.
FR2947546B1 (fr) 2009-07-03 2011-07-01 Sanofi Aventis Derives de pyrazoles, leur preparation et leur application en therapeutique
GB2474748B (en) * 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
JP5879273B2 (ja) 2010-03-01 2016-03-08 ジーティーエックス・インコーポレイテッド 癌を処置するための化合物
JP6016915B2 (ja) * 2011-07-28 2016-10-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール
WO2013024427A1 (en) 2011-08-16 2013-02-21 Glenmark Pharmaceuticals S.A. Novel urea derivatives as tec kinase inhibitors and uses thereof
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
AU2014291161B2 (en) * 2013-07-18 2018-04-26 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of FGFR inhibitor
US10124003B2 (en) * 2013-07-18 2018-11-13 Taiho Pharmaceutical Co., Ltd. Therapeutic agent for FGFR inhibitor-resistant cancer
TN2016000115A1 (en) 2013-10-25 2017-07-05 Novartis Ag Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors.
AU2016238436A1 (en) 2015-03-25 2017-08-17 Novartis Ag Formylated N-heterocyclic derivatives as FGFR4 inhibitors

Also Published As

Publication number Publication date
JP2019529444A (ja) 2019-10-17
JP6906811B2 (ja) 2021-07-21
SG10202102822RA (en) 2021-05-28
MX2019003143A (es) 2019-06-17
EP3517535A4 (en) 2020-02-26
KR102783517B1 (ko) 2025-03-19
AU2017327954A1 (en) 2019-05-02
US20200339541A1 (en) 2020-10-29
CN109843873B (zh) 2022-06-17
RU2729069C1 (ru) 2020-08-04
CA3036594C (en) 2024-02-13
US11059805B2 (en) 2021-07-13
CN109843873A (zh) 2019-06-04
CA3036594A1 (en) 2018-03-22
AU2017327954B2 (en) 2022-02-03
EP3517535B1 (en) 2022-06-29
CN107840842A (zh) 2018-03-27
US10710981B2 (en) 2020-07-14
WO2018049781A1 (zh) 2018-03-22
US20210332027A1 (en) 2021-10-28
US11572353B2 (en) 2023-02-07
KR20190052113A (ko) 2019-05-15
US20190210997A1 (en) 2019-07-11
EP3517535A1 (en) 2019-07-31
MX390747B (es) 2025-03-21

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