CN115364061A - C-met抑制剂的片剂制剂 - Google Patents

C-met抑制剂的片剂制剂 Download PDF

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Publication number
CN115364061A
CN115364061A CN202210949714.1A CN202210949714A CN115364061A CN 115364061 A CN115364061 A CN 115364061A CN 202210949714 A CN202210949714 A CN 202210949714A CN 115364061 A CN115364061 A CN 115364061A
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CN
China
Prior art keywords
tablet
triazin
quinolin
imidazo
ylmethyl
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Pending
Application number
CN202210949714.1A
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English (en)
Chinese (zh)
Inventor
E·贡萨尔维斯
C·陶赫曼
S-F·严
S·维帕古塔
Z·宗
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Novartis AG
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Novartis AG
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53762251&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN115364061(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN115364061A publication Critical patent/CN115364061A/zh
Pending legal-status Critical Current

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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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61JCONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/10Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495Heterocyclic 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61JCONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/06Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of pills, lozenges or dragees
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN202210949714.1A 2014-07-25 2015-07-22 C-met抑制剂的片剂制剂 Pending CN115364061A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201462028865P 2014-07-25 2014-07-25
US62/028,865 2014-07-25
PCT/IB2015/055561 WO2016012963A1 (en) 2014-07-25 2015-07-22 Tablet formulation of 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
CN201580052264.4A CN106714784A (zh) 2014-07-25 2015-07-22 2‑氟‑N‑甲基‑4‑[7‑(喹啉‑6‑基甲基)咪唑并[1,2‑b][1,2,4]三嗪‑2‑基]苯甲酰胺的片剂制剂

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201580052264.4A Division CN106714784A (zh) 2014-07-25 2015-07-22 2‑氟‑N‑甲基‑4‑[7‑(喹啉‑6‑基甲基)咪唑并[1,2‑b][1,2,4]三嗪‑2‑基]苯甲酰胺的片剂制剂

Publications (1)

Publication Number Publication Date
CN115364061A true CN115364061A (zh) 2022-11-22

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Application Number Title Priority Date Filing Date
CN202210949714.1A Pending CN115364061A (zh) 2014-07-25 2015-07-22 C-met抑制剂的片剂制剂
CN201580052264.4A Pending CN106714784A (zh) 2014-07-25 2015-07-22 2‑氟‑N‑甲基‑4‑[7‑(喹啉‑6‑基甲基)咪唑并[1,2‑b][1,2,4]三嗪‑2‑基]苯甲酰胺的片剂制剂

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CN201580052264.4A Pending CN106714784A (zh) 2014-07-25 2015-07-22 2‑氟‑N‑甲基‑4‑[7‑(喹啉‑6‑基甲基)咪唑并[1,2‑b][1,2,4]三嗪‑2‑基]苯甲酰胺的片剂制剂

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US (5) US10085993B2 (enExample)
EP (2) EP3172209B1 (enExample)
JP (3) JP6770946B2 (enExample)
KR (2) KR102581121B1 (enExample)
CN (2) CN115364061A (enExample)
AR (1) AR101286A1 (enExample)
AU (4) AU2015293539A1 (enExample)
CA (1) CA2954840A1 (enExample)
CL (1) CL2017000180A1 (enExample)
CO (1) CO2017000586A2 (enExample)
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PE (1) PE20170523A1 (enExample)
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PL (1) PL3172209T3 (enExample)
PT (1) PT3172209T (enExample)
SG (2) SG10201900648SA (enExample)
SI (1) SI3172209T1 (enExample)
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KR102581121B1 (ko) 2014-07-25 2023-09-21 노파르티스 아게 2-플루오로-n-메틸-4-[7-(퀴놀린-6-일메틸)이미다조[1,2-b][1,2,4]트리아진-2-일]벤즈아미드의 정제 제제
IL305639B1 (en) 2016-08-10 2025-10-01 Hoffmann La Roche Medicinal products containing Akt protein kinase inhibitors
TWI853027B (zh) 2019-05-16 2024-08-21 瑞士商諾華公司 N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羥基吡咯啶-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲醯胺之結晶形狀
US20220378790A1 (en) * 2019-10-24 2022-12-01 Hanmi Pharm Co., Ltd. Pharmaceutical preparation comprising an amide derivative inhibiting the growth of cancer cell and a pharmaceutical product containing the same
WO2022007752A1 (zh) * 2020-07-06 2022-01-13 苏州晶云药物科技股份有限公司 苯甲酰胺类化合物及其二盐酸盐的新晶型及其制备方法
CN114853762A (zh) * 2021-02-03 2022-08-05 四川科伦药物研究院有限公司 一种咪唑并三嗪类化合物的固体形式及其制备方法和用途
WO2023138492A1 (zh) * 2022-01-19 2023-07-27 南京明德新药研发有限公司 一种包含嘧啶基团的三并环类化合物的组合物及其制备方法和应用
WO2023249994A1 (en) * 2022-06-22 2023-12-28 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
CA3264627A1 (en) 2022-08-19 2024-02-22 Mirati Therapeutics, Inc. SOLID PHARMACEUTICAL COMPOSITIONS OF ADAGRASIB
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
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CN102724970A (zh) * 2009-11-09 2012-10-10 惠氏有限责任公司 来那替尼马来酸盐的片剂制剂

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SG11201700147SA (en) 2017-02-27
ES2857523T3 (es) 2021-09-29
US20170231997A1 (en) 2017-08-17
SG10201900648SA (en) 2019-02-27
AR101286A1 (es) 2016-12-07
EA039220B1 (ru) 2021-12-20
DK3172209T3 (da) 2021-02-22
PT3172209T (pt) 2021-02-11
JP2022046659A (ja) 2022-03-23
US20190015418A1 (en) 2019-01-17
KR20230136693A (ko) 2023-09-26
EA202191301A1 (ru) 2021-11-30
EP3172209B1 (en) 2020-12-02
US20210113569A1 (en) 2021-04-22
US12208101B2 (en) 2025-01-28
CO2017000586A2 (es) 2017-06-20
EP3848376A1 (en) 2021-07-14
JP6770946B2 (ja) 2020-10-21
AU2021202500A1 (en) 2021-05-20
MX379279B (es) 2025-03-11
PL3172209T3 (pl) 2021-06-14
SI3172209T1 (sl) 2021-03-31
AU2020200912B2 (en) 2021-01-28
CN106714784A (zh) 2017-05-24
AU2018207947A1 (en) 2018-08-09
AU2015293539A1 (en) 2017-02-02
JP2017521469A (ja) 2017-08-03
KR20170039211A (ko) 2017-04-10
MX2021000595A (es) 2021-04-13
JP2020114852A (ja) 2020-07-30
US20220249498A1 (en) 2022-08-11
US20250339440A1 (en) 2025-11-06
BR112017000953A2 (pt) 2017-11-14
HUE053346T2 (hu) 2021-06-28
US10085993B2 (en) 2018-10-02
FR22C1058I2 (fr) 2023-11-17
JP7002587B2 (ja) 2022-01-20
MY187276A (en) 2021-09-17
EP3172209A1 (en) 2017-05-31
ECSP17011672A (es) 2018-03-31
WO2016012963A1 (en) 2016-01-28
GT201700007A (es) 2018-12-18
FR22C1058I1 (fr) 2023-01-06
US10596178B2 (en) 2020-03-24
MX2017001177A (es) 2017-05-01
IL250166A0 (en) 2017-03-30
IL250166B (en) 2021-01-31
CA2954840A1 (en) 2016-01-28
TW202200148A (zh) 2022-01-01
KR102581121B1 (ko) 2023-09-21
PE20170523A1 (es) 2017-05-17
NL301208I2 (nl) 2025-03-20
NZ728089A (en) 2024-01-26
HUS2200054I1 (hu) 2023-01-28
NO2022058I1 (no) 2022-12-16
TWI724993B (zh) 2021-04-21
TW201613595A (en) 2016-04-16
CL2017000180A1 (es) 2017-09-15
EA201790259A1 (ru) 2017-06-30
PH12017500121A1 (en) 2017-05-29
AU2020200912A1 (en) 2020-02-27
JO3618B1 (ar) 2020-08-27

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