KR102872983B1 - 개선된 특성을 갖는 메틸 ｛4,6-디아미노-2-[5-플루오로-1-(2-플루오로벤질)-1H-피라졸로[3,4-b]피리딘-3-일]피리미딘-5-일}카르바메이트 활성 화합물 생성물, 및 그의 제조법 및 제형 - Google Patents

개선된 특성을 갖는 메틸 ｛4,6-디아미노-2-[5-플루오로-1-(2-플루오로벤질)-1H-피라졸로[3,4-b]피리딘-3-일]피리미딘-5-일}카르바메이트 활성 화합물 생성물, 및 그의 제조법 및 제형

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KR102872983B1
KR102872983B1 KR1020217018155A KR20217018155A KR102872983B1 KR 102872983 B1 KR102872983 B1 KR 102872983B1 KR 1020217018155 A KR1020217018155 A KR 1020217018155A KR 20217018155 A KR20217018155 A KR 20217018155A KR 102872983 B1 KR102872983 B1 KR 102872983B1
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active compound
formula
water
compound product
compound
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KR20210104703A (ko
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페터 파이
미할 조바
외르크 브로코프
마르쿠스 롱게리히
구이도 베커
하이케 노이만
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아드베리오 파마 게엠베하
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    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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)
  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020217018155A 2018-12-17 2019-12-16 개선된 특성을 갖는 메틸 ｛4,6-디아미노-2-[5-플루오로-1-(2-플루오로벤질)-1H-피라졸로[3,4-b]피리딘-3-일]피리미딘-5-일}카르바메이트 활성 화합물 생성물, 및 그의 제조법 및 제형 Active KR102872983B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18213115 2018-12-17
EP18213115.1 2018-12-17
PCT/EP2019/085255 WO2020126983A1 (en) 2018-12-17 2019-12-16 Methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate active compound product having improved properties, production and formulation thereof

Publications (2)

Publication Number Publication Date
KR20210104703A KR20210104703A (ko) 2021-08-25
KR102872983B1 true KR102872983B1 (ko) 2025-10-17

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KR1020217018155A Active KR102872983B1 (ko) 2018-12-17 2019-12-16 개선된 특성을 갖는 메틸 ｛4,6-디아미노-2-[5-플루오로-1-(2-플루오로벤질)-1H-피라졸로[3,4-b]피리딘-3-일]피리미딘-5-일}카르바메이트 활성 화합물 생성물, 및 그의 제조법 및 제형

Country Status (19)

Country Link
US (1) US12172996B2 (https=)
EP (1) EP3898624A1 (https=)
JP (1) JP7529667B2 (https=)
KR (1) KR102872983B1 (https=)
CN (1) CN113207290B (https=)
AR (1) AR116912A1 (https=)
AU (1) AU2019409269B2 (https=)
BR (1) BR112021009122A2 (https=)
CA (1) CA3123360A1 (https=)
CL (1) CL2021001580A1 (https=)
CO (1) CO2021007668A2 (https=)
IL (1) IL283976B2 (https=)
JO (1) JOP20210155B1 (https=)
MX (1) MX2021007090A (https=)
PE (1) PE20211593A1 (https=)
SG (1) SG11202104953VA (https=)
TW (1) TWI830835B (https=)
UA (1) UA129677C2 (https=)
WO (1) WO2020126983A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI830835B (zh) 2018-12-17 2024-02-01 德商亞德維瑞醫藥有限公司 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物
EP4099987B1 (en) 2020-02-03 2025-03-12 Adverio Pharma GmbH Nanoformulations of methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
EP3925953A1 (en) 2020-06-16 2021-12-22 Adverio Pharma GmbH Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
WO2025114276A1 (en) 2023-12-01 2025-06-05 Krka, D.D., Novo Mesto Solid oral composition comprising vericiguat

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2745813B1 (fr) 1996-03-07 1998-05-07 Rhone Poulenc Chimie Agglomerats spheriques d'acide 10-phenothiazinylpropanoique et leur procede de preparation
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
UY33041A (es) 2009-11-27 2011-06-30 Bayer Schering Pharma Aktienegesellschaft Procedimiento para la preparaciòn de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificaciòn para el uso como principio activo farmacèutico
PL2604608T3 (pl) 2009-11-27 2016-02-29 Adverio Pharma Gmbh Sposób wytwarzania {4,6-diamino-2-[1-(2-fluorobenzylo)-1H-pirazolo[3,4-b]pirydyn-3-ylo]pirymidyn-5-ylo}metylokarbaminianu metylu
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
ES2603028T3 (es) * 2011-11-25 2017-02-23 Adverio Pharma Gmbh Procedimiento para la preparación de (Z)-alfa-fluoro-beta-amino-acrilaldehídos sustituidos
MX2015010725A (es) * 2013-02-21 2016-05-31 Adverio Pharma Gmbh Formas de metil {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b] piridino-3-il] pirimidino-5-il} metil carbamato.
PL2792682T3 (pl) 2013-04-19 2017-04-28 Zach System Sposób wytwarzania stałej postaci octanu abirateronu
WO2016113415A1 (en) * 2015-01-16 2016-07-21 Sandoz Ag Process for the preparation of riociguat essentially free from genotoxic impurities
WO2017025981A1 (en) * 2015-08-13 2017-02-16 Msn Laboratories Private Limited Process for the preparation of methyl 4,6-diamino-2-[l-(2-fhiorobenzvr)-lh-pyrazolo i3,4-blpvridin-3-vn-5-pyrimidinyl(methvl)carbamate and its polymorphs thereof
TWI830835B (zh) 2018-12-17 2024-02-01 德商亞德維瑞醫藥有限公司 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物
CN113272286B (zh) 2019-01-22 2024-04-16 阿德弗里奥药品有限责任公司 制备4-(2,2,3,3-四氟丙基)吗啉的方法
EP4099987B1 (en) * 2020-02-03 2025-03-12 Adverio Pharma GmbH Nanoformulations of methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
EP3925953A1 (en) * 2020-06-16 2021-12-22 Adverio Pharma GmbH Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate

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Publication number Publication date
MX2021007090A (es) 2021-08-11
PE20211593A1 (es) 2021-08-18
CL2021001580A1 (es) 2021-12-03
SG11202104953VA (en) 2021-06-29
JOP20210155B1 (ar) 2025-10-01
AU2019409269A1 (en) 2021-06-03
JP7529667B2 (ja) 2024-08-06
IL283976B1 (en) 2024-12-01
TW202039488A (zh) 2020-11-01
IL283976B2 (en) 2025-04-01
CN113207290A (zh) 2021-08-03
JOP20210155A1 (ar) 2023-01-30
EP3898624A1 (en) 2021-10-27
BR112021009122A2 (pt) 2021-08-10
US20220048907A1 (en) 2022-02-17
UA129677C2 (uk) 2025-07-02
WO2020126983A1 (en) 2020-06-25
IL283976A (en) 2021-07-29
CA3123360A1 (en) 2020-06-25
JP2022515376A (ja) 2022-02-18
AR116912A1 (es) 2021-06-23
AU2019409269B2 (en) 2025-04-03
TWI830835B (zh) 2024-02-01
CO2021007668A2 (es) 2021-07-19
CN113207290B (zh) 2024-04-09
KR20210104703A (ko) 2021-08-25
US12172996B2 (en) 2024-12-24

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