EA202192272A1 - Гранулированный препарат ингибитора parp и способ его получения - Google Patents

Гранулированный препарат ингибитора parp и способ его получения

Info

Publication number
EA202192272A1
EA202192272A1 EA202192272A EA202192272A EA202192272A1 EA 202192272 A1 EA202192272 A1 EA 202192272A1 EA 202192272 A EA202192272 A EA 202192272A EA 202192272 A EA202192272 A EA 202192272A EA 202192272 A1 EA202192272 A1 EA 202192272A1
Authority
EA
Eurasian Patent Office
Prior art keywords
parp inhibitor
granule
protective layer
granulated
production
Prior art date
Application number
EA202192272A
Other languages
English (en)
Inventor
Юаньцзин Го
Ипин ВАН
Вэньюань Фань
Чжэнмин Ду
Ган Цю
Шо Сюй
Хойжу Лв
Original Assignee
Бейджин, Лтд.
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 Бейджин, Лтд. filed Critical Бейджин, Лтд.
Publication of EA202192272A1 publication Critical patent/EA202192272A1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5089—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Настоящее изобретение относится к гранулированной композиции ингибитора PARP и способу ее получения. Гранулированная композиция содержит гранулу и необязательный дополнительный эксципиент, причем указанная гранула содержит (1) ядро гранулы; (2) слой, содержащий лекарственное средство, и (3) необязательный защитный слой, где указанный слой, содержащий лекарственное средство, содержит (a) активный ингредиент и (b) связующее вещество; причем когда композиция содержит защитный слой, указанный защитный слой содержит (c) покрывающий материал; и активный ингредиент представляет собой (R)-2-фтор-10a-метил-7,8,9,10,10a,11-гексагидро-5,6,7a,11-тетраазациклогепта[def]циклопента[a]флуорен-4(5H)-он, его фармацевтически приемлемую соль и гидрат.
EA202192272A 2019-05-31 2020-05-29 Гранулированный препарат ингибитора parp и способ его получения EA202192272A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2019089618 2019-05-31
PCT/CN2020/093438 WO2020239097A1 (zh) 2019-05-31 2020-05-29 一种parp抑制剂微丸制剂及其制备工艺

Publications (1)

Publication Number Publication Date
EA202192272A1 true EA202192272A1 (ru) 2022-03-02

Family

ID=73553507

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202192272A EA202192272A1 (ru) 2019-05-31 2020-05-29 Гранулированный препарат ингибитора parp и способ его получения

Country Status (15)

Country Link
US (1) US20220233550A1 (ru)
EP (1) EP3977984A4 (ru)
JP (1) JP2022534093A (ru)
KR (1) KR20220016028A (ru)
CN (2) CN113438944A (ru)
AU (1) AU2020282478A1 (ru)
BR (1) BR112021018847A2 (ru)
CA (1) CA3141770A1 (ru)
EA (1) EA202192272A1 (ru)
IL (1) IL288467A (ru)
MX (1) MX2021014339A (ru)
SG (1) SG11202112924RA (ru)
TW (1) TW202110455A (ru)
WO (1) WO2020239097A1 (ru)
ZA (1) ZA202109635B (ru)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201401726VA (en) * 2011-12-31 2014-10-30 Beigene Ltd Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors
WO2017032289A1 (en) * 2015-08-25 2017-03-02 Beigene, Ltd. Process for preparing parp inhibitor, crystalline forms, and uses thereof
CN108201536A (zh) * 2016-12-16 2018-06-26 中国科学院上海药物研究所 一种奥拉帕尼口服缓控释药物组合物及其用途
CN106619567A (zh) * 2017-01-02 2017-05-10 佛山市腾瑞医药科技有限公司 一种琥珀酸曲格列汀速释微丸制剂与制备方法
WO2019090141A1 (en) * 2017-11-02 2019-05-09 Vicus Therapeutics, Llc Combination drug therapies for cancer and methods of making and using them

Also Published As

Publication number Publication date
JP2022534093A (ja) 2022-07-27
EP3977984A1 (en) 2022-04-06
IL288467A (en) 2022-01-01
CA3141770A1 (en) 2020-12-03
EP3977984A4 (en) 2023-01-11
AU2020282478A1 (en) 2021-09-16
CN113438944A (zh) 2021-09-24
CN115105484A (zh) 2022-09-27
ZA202109635B (en) 2023-03-29
US20220233550A1 (en) 2022-07-28
MX2021014339A (es) 2022-01-06
BR112021018847A2 (pt) 2021-11-30
TW202110455A (zh) 2021-03-16
SG11202112924RA (en) 2021-12-30
WO2020239097A1 (zh) 2020-12-03
KR20220016028A (ko) 2022-02-08

Similar Documents

Publication Publication Date Title
JOP20220155A1 (ar) مشتقات البيرازول مفيدة كعوامل مضادة للسرطان
FI92904B (fi) Menetelmä suun kautta annettavaksi tarkoitetun, aktiiviyhdistettä kontrolloidusti vapauttavan farmaseuttisen formulaation valmistamiseksi
EP1000615A3 (en) Preparation of pharmaceutically active particles
EA201891463A1 (ru) ПРОИЗВОДНЫЕ ПИРАЗОЛО[1,5-a]ПИРАЗИН-4-ИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ (JAK)
MX2021009854A (es) Compuesto derivado heterociclico novedoso y uso del mismo.
NO20100041L (no) Anvendelse av AT-1 reseptorantagonist eller AT-2 reseptormodulator for behandling av sykdommer assosiert med en okning av AT-1 eller AT-2 reseptorer
MX2007007458A (es) Derivados de quinazolina para inhibir crecimiento de celulas cancerigenas y metodo para la preparacion de los mismos.
WO2011049332A3 (en) 2,7-substituted thieno[3,2-d]pyrimidine compounds as protein kinase inhibitors
WO2011062372A3 (en) 2, 4, 7 -substituted thieno [3, 2 -d] pyrimidine compounds as protein kinase inhibitors
DK0891325T3 (da) Para-substituerede phenylpropansyrederivater som integrinantagonister
WO2007001065A3 (en) Method for the preparation of a wet granulated drug product
WO2011052923A3 (en) Novel 1,6-disubstituted indole compounds as protein kinase inhibitors
WO2001096307A3 (en) Cycloalkyl alkanoic acids as integrin receptor antagonists
WO2020247298A3 (en) 1-pyrazolyl, 5-, 6- disubstituted indazole derivatives as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
CA2360308A1 (en) Glucocorticoid receptor modulators
NZ599762A (en) Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea
EP3620457A4 (en) COMPOUND DERIVED FROM PYRIMIDINE, OPTICAL ISOMER, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION FOR PREVENTING OR TREATING A TYRO 3-RELATED DISEASE, CONSIDERING IT AS AN ACTIVE INGREDIENT
MX2021009755A (es) Combinaciones de compuestos beta-lactámicos y probenecid, y usos de los mismos.
EA202192272A1 (ru) Гранулированный препарат ингибитора parp и способ его получения
ZA202108670B (en) Pharmaceutical preparation and method for producing same
WO2011132901A3 (en) Novel benzamide derivatives
MY194941A (en) C-glycoside derivatives having fused phenyl ring or pharmaceutically acceptable salts thereof, method for preparing the same and pharmaceutical composition comprising the same
CR20200211A (es) Derivados de piridinona y uso como inhibidores selectivos de alk-2
WO2021055797A9 (en) Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
GB0010446D0 (en) Pharmaceutical formulation