CN119317625A - 喹唑啉衍生物的结晶形式、其制备、组合物和用途 - Google Patents

喹唑啉衍生物的结晶形式、其制备、组合物和用途 Download PDF

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Publication number
CN119317625A
CN119317625A CN202280070755.1A CN202280070755A CN119317625A CN 119317625 A CN119317625 A CN 119317625A CN 202280070755 A CN202280070755 A CN 202280070755A CN 119317625 A CN119317625 A CN 119317625A
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CN
China
Prior art keywords
crystalline form
free base
powder diffraction
ray powder
diffraction pattern
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.)
Pending
Application number
CN202280070755.1A
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English (en)
Chinese (zh)
Inventor
王铮
周鼎
程子强
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.)
F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Priority to CN202510509201.2A priority Critical patent/CN120309620A/zh
Priority to CN202510509243.6A priority patent/CN120309621A/zh
Priority to CN202510508208.2A priority patent/CN120623183A/zh
Publication of CN119317625A publication Critical patent/CN119317625A/zh
Pending legal-status Critical Current

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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/14—Adipic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/185—Saturated compounds having only one carboxyl group and containing keto groups
    • C07C59/225—Saturated compounds having only one carboxyl group and containing keto groups containing —CHO groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202280070755.1A 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途 Pending CN119317625A (zh)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN202510509201.2A CN120309620A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510509243.6A CN120309621A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510508208.2A CN120623183A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2021125016 2021-10-20
CNPCT/CN2021/125016 2021-10-20
PCT/CN2022/126169 WO2023066296A1 (en) 2021-10-20 2022-10-19 Crystalline forms of quinazoline derivatives, preparation, composition and use thereof

Related Child Applications (3)

Application Number Title Priority Date Filing Date
CN202510508208.2A Division CN120623183A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510509201.2A Division CN120309620A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510509243.6A Division CN120309621A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途

Publications (1)

Publication Number Publication Date
CN119317625A true CN119317625A (zh) 2025-01-14

Family

ID=86057927

Family Applications (4)

Application Number Title Priority Date Filing Date
CN202280070755.1A Pending CN119317625A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510509201.2A Pending CN120309620A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510509243.6A Pending CN120309621A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510508208.2A Pending CN120623183A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途

Family Applications After (3)

Application Number Title Priority Date Filing Date
CN202510509201.2A Pending CN120309620A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510509243.6A Pending CN120309621A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN202510508208.2A Pending CN120623183A (zh) 2021-10-20 2022-10-19 喹唑啉衍生物的结晶形式、其制备、组合物和用途

Country Status (25)

Country Link
US (1) US20240417403A1 (https=)
EP (2) EP4399207B1 (https=)
JP (2) JP2024539212A (https=)
KR (1) KR20240090181A (https=)
CN (4) CN119317625A (https=)
AU (1) AU2022371540A1 (https=)
CA (1) CA3232101A1 (https=)
CL (1) CL2024001231A1 (https=)
CO (1) CO2024004745A2 (https=)
CR (1) CR20240163A (https=)
DK (1) DK4399207T3 (https=)
ES (1) ES3059167T3 (https=)
FI (1) FI4399207T3 (https=)
HR (1) HRP20260049T1 (https=)
IL (1) IL312004A (https=)
LT (1) LT4399207T (https=)
MA (1) MA66471B1 (https=)
MX (1) MX2024004738A (https=)
PE (1) PE20242106A1 (https=)
PL (1) PL4399207T3 (https=)
PT (1) PT4399207T (https=)
RS (1) RS67641B1 (https=)
SI (1) SI4399207T1 (https=)
SM (1) SMT202600023T1 (https=)
WO (1) WO2023066296A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
WO2025195333A1 (en) 2024-03-19 2025-09-25 F. Hoffmann-La Roche Ag Pharmaceutical formulation of erbb2 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101356171A (zh) * 2005-11-15 2009-01-28 阿雷生物药品公司 作为erbbi型受体酪氨酸激酶抑制剂用于治疗增殖性疾病的n4-苯基-喹唑啉-4-胺衍生物和相关化合物
WO2017148391A1 (zh) * 2016-03-01 2017-09-08 上海医药集团股份有限公司 一种含氮杂环化合物、制备方法、中间体、组合物和应用
WO2018055023A1 (en) * 2016-09-22 2018-03-29 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of lung cancer
WO2019214634A1 (en) * 2018-05-08 2019-11-14 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Erbb receptor inhibitors
CN112654612A (zh) * 2018-09-18 2021-04-13 苏州赞荣医药科技有限公司 作为抗肿瘤剂的喹唑啉衍生物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE69720965T2 (de) 1996-02-13 2004-02-05 Astrazeneca Ab Chinazolinderivate und deren verwendung als vegf hemmer
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101356171A (zh) * 2005-11-15 2009-01-28 阿雷生物药品公司 作为erbbi型受体酪氨酸激酶抑制剂用于治疗增殖性疾病的n4-苯基-喹唑啉-4-胺衍生物和相关化合物
WO2017148391A1 (zh) * 2016-03-01 2017-09-08 上海医药集团股份有限公司 一种含氮杂环化合物、制备方法、中间体、组合物和应用
WO2018055023A1 (en) * 2016-09-22 2018-03-29 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of lung cancer
WO2019214634A1 (en) * 2018-05-08 2019-11-14 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Erbb receptor inhibitors
CN112654612A (zh) * 2018-09-18 2021-04-13 苏州赞荣医药科技有限公司 作为抗肿瘤剂的喹唑啉衍生物

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Publication number Publication date
ES3059167T3 (en) 2026-03-19
PT4399207T (pt) 2026-01-16
SMT202600023T1 (it) 2026-03-09
JP2026027273A (ja) 2026-02-18
KR20240090181A (ko) 2024-06-21
FI4399207T3 (fi) 2026-01-28
CN120309620A (zh) 2025-07-15
CA3232101A1 (en) 2023-04-27
CN120309621A (zh) 2025-07-15
CO2024004745A2 (es) 2024-04-29
SI4399207T1 (sl) 2026-04-30
RS67641B1 (sr) 2026-02-27
JP2024539212A (ja) 2024-10-28
EP4399207A4 (en) 2025-03-19
LT4399207T (lt) 2026-02-10
HRP20260049T1 (hr) 2026-02-27
AU2022371540A1 (en) 2024-03-21
DK4399207T3 (da) 2026-02-02
MX2024004738A (es) 2024-05-14
PE20242106A1 (es) 2024-10-28
IL312004A (en) 2024-06-01
CN120623183A (zh) 2025-09-12
CR20240163A (es) 2024-06-12
MA66471B1 (fr) 2026-02-27
WO2023066296A1 (en) 2023-04-27
EP4399207A1 (en) 2024-07-17
US20240417403A1 (en) 2024-12-19
EP4399207B1 (en) 2025-11-26
PL4399207T3 (pl) 2026-03-23
CL2024001231A1 (es) 2024-08-09
EP4717689A2 (en) 2026-04-01

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