BR112019008295A2 - composto inibidor de multiquinase, e forma cristalina e utilização do mesmo - Google Patents

composto inibidor de multiquinase, e forma cristalina e utilização do mesmo

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Publication number
BR112019008295A2
BR112019008295A2 BR112019008295A BR112019008295A BR112019008295A2 BR 112019008295 A2 BR112019008295 A2 BR 112019008295A2 BR 112019008295 A BR112019008295 A BR 112019008295A BR 112019008295 A BR112019008295 A BR 112019008295A BR 112019008295 A2 BR112019008295 A2 BR 112019008295A2
Authority
BR
Brazil
Prior art keywords
crystalline form
inhibitor compound
compound
multikinase inhibitor
formula
Prior art date
Application number
BR112019008295A
Other languages
English (en)
Other versions
BR112019008295B1 (pt
Inventor
Wu Frank
Original Assignee
Nanjing Transthera Biosciences Co Ltd
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 Nanjing Transthera Biosciences Co Ltd filed Critical Nanjing Transthera Biosciences Co Ltd
Publication of BR112019008295A2 publication Critical patent/BR112019008295A2/pt
Publication of BR112019008295B1 publication Critical patent/BR112019008295B1/pt

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Classifications

    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

a presente invenção refere-se a um composto conforme representado por fórmula (i) (i) ou um sal farmaceuticamente aceitável e estereoisômero do mesmo, em que r1, r2, x, y, p, w e ar são como definidos na descrição. o composto de fórmula (i) da presente invenção pode ser utilizado na preparação de um fármaco para tratamento de cânceres mediados por anormalidade de multiquinases. também proporcionado é uma forma cristalina i de um composto 4-(5-(2-clorofenil)-3-metil-2,10-diidropirazol [4,3-b]pirido[4,3-e][1,4]diazepin-8-il)morfolina, em que em um padrão de difração de raio x do pó de forma cristalina i, apresenta picos característicos em 7,4 ± 0,2o, 17,9 ± 0,2o, 18,9 ± 0,2o, 19,4 ± 0,2o, 21,5 ± 0,2o e 23,7 ± 0,2o.
BR112019008295-6A 2016-12-13 2017-12-12 Composto inibidor de multiquinase, forma cristalina do composto de fórmula iii, formulação/composição farmacêutica, seus usos, métodos para a preparação da forma cristalina e do composto de fórmula iii e intermediário para a preparação do composto de fórmula iii BR112019008295B1 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201611174146.3 2016-12-13
CN201611174146 2016-12-13
CN201710426594.6 2017-06-08
CN201710426594 2017-06-08
CN201710593933 2017-07-20
CN201710593933.X 2017-07-20
PCT/CN2017/115698 WO2018108079A1 (zh) 2016-12-13 2017-12-12 多激酶抑制剂化合物、其晶型及用途

Publications (2)

Publication Number Publication Date
BR112019008295A2 true BR112019008295A2 (pt) 2019-07-09
BR112019008295B1 BR112019008295B1 (pt) 2024-03-12

Family

ID=62557952

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112019008295-6A BR112019008295B1 (pt) 2016-12-13 2017-12-12 Composto inibidor de multiquinase, forma cristalina do composto de fórmula iii, formulação/composição farmacêutica, seus usos, métodos para a preparação da forma cristalina e do composto de fórmula iii e intermediário para a preparação do composto de fórmula iii

Country Status (10)

Country Link
US (3) US10208042B1 (pt)
EP (1) EP3447056A4 (pt)
JP (1) JP6594571B2 (pt)
KR (1) KR102373577B1 (pt)
CN (1) CN108218868B (pt)
AU (1) AU2017376353B2 (pt)
BR (1) BR112019008295B1 (pt)
CA (1) CA3041155C (pt)
RU (1) RU2723985C9 (pt)
WO (1) WO2018108079A1 (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108218868B (zh) 2016-12-13 2019-02-19 南京药捷安康生物科技有限公司 多激酶抑制剂化合物、其晶型及用途
JP2023515549A (ja) * 2020-02-24 2023-04-13 薬捷安康（南京）科技股▲分▼有限公司 マルチキナーゼ阻害剤の新規用途
US20230212167A1 (en) * 2020-05-08 2023-07-06 Transthera Sciences (Nanjing), Inc. Method for synthesizing anti-tumor compound and intermediates thereof
WO2022197104A1 (ko) * 2021-03-16 2022-09-22 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물의 결정형
KR20230163440A (ko) * 2021-03-29 2023-11-30 트랜스테라 사이언시즈 (난징), 인크. 멀티 키나제 억제제의 병용 응용
CN115322196A (zh) * 2021-05-10 2022-11-11 药捷安康(南京)科技股份有限公司 多激酶抑制剂的药物组合物及其用途
TW202320760A (zh) * 2021-11-27 2023-06-01 大陸商藥捷安康(南京)科技股份有限公司 激酶抑制劑的新用途
WO2023104074A1 (zh) * 2021-12-07 2023-06-15 药捷安康(南京)科技股份有限公司 激酶抑制剂的新用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6350786B1 (en) * 1998-09-22 2002-02-26 Hoffmann-La Roche Inc. Stable complexes of poorly soluble compounds in ionic polymers
US6440959B1 (en) 1999-04-21 2002-08-27 Hoffman-La Roche Inc. Pyrazolobenzodiazepines
CN101899049A (zh) * 2004-10-13 2010-12-01 霍夫曼-拉罗奇有限公司 二取代吡唑并苯并二氮杂*类
CN102603743B (zh) * 2012-02-24 2014-05-28 南京天易生物科技有限公司 抗肿瘤的氮杂苯并[f]薁衍生物其制备方法及其用途
CN108218868B (zh) 2016-12-13 2019-02-19 南京药捷安康生物科技有限公司 多激酶抑制剂化合物、其晶型及用途

Also Published As

Publication number Publication date
CA3041155C (en) 2021-12-14
US10889586B2 (en) 2021-01-12
US20190040064A1 (en) 2019-02-07
EP3447056A4 (en) 2019-09-18
AU2017376353B2 (en) 2020-02-06
WO2018108079A1 (zh) 2018-06-21
AU2017376353A1 (en) 2019-05-16
JP6594571B2 (ja) 2019-10-23
US20190152972A1 (en) 2019-05-23
KR20190068626A (ko) 2019-06-18
EP3447056A1 (en) 2019-02-27
CN108218868A (zh) 2018-06-29
BR112019008295B1 (pt) 2024-03-12
US11718620B2 (en) 2023-08-08
US10208042B1 (en) 2019-02-19
CN108218868B (zh) 2019-02-19
US20210130354A1 (en) 2021-05-06
JP2019518784A (ja) 2019-07-04
RU2723985C9 (ru) 2020-09-21
RU2723985C1 (ru) 2020-06-18
AU2017376353A2 (en) 2019-06-27
KR102373577B1 (ko) 2022-03-10
CA3041155A1 (en) 2018-06-21

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B25D Requested change of name of applicant approved

Owner name: TRANSTHERA SCIENCES (NANJING), INC. (CN)

B25G Requested change of headquarter approved

Owner name: TRANSTHERA SCIENCES (NANJING), INC. (CN)

B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 12/12/2017, OBSERVADAS AS CONDICOES LEGAIS