CA3123360A1 - 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 - Google Patents

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 Download PDF

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Publication number
CA3123360A1
CA3123360A1 CA3123360A CA3123360A CA3123360A1 CA 3123360 A1 CA3123360 A1 CA 3123360A1 CA 3123360 A CA3123360 A CA 3123360A CA 3123360 A CA3123360 A CA 3123360A CA 3123360 A1 CA3123360 A1 CA 3123360A1
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CA
Canada
Prior art keywords
active compound
wetting agent
formula
water
compound product
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
CA3123360A
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English (en)
French (fr)
Inventor
Peter Fey
Michal SOWA
Joerg BROCKOB
Markus Longerich
Guido Becker
Heike Neumann
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.)
Adverio Pharma GmbH
Original Assignee
Adverio Pharma GmbH
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 Adverio Pharma GmbH filed Critical Adverio Pharma GmbH
Publication of CA3123360A1 publication Critical patent/CA3123360A1/en
Pending legal-status Critical Current

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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)
CA3123360A 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 Pending CA3123360A1 (en)

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 (1)

Publication Number Publication Date
CA3123360A1 true CA3123360A1 (en) 2020-06-25

Family

ID=64744472

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3123360A Pending CA3123360A1 (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

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

Also Published As

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
KR102872983B1 (ko) 2025-10-17
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
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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