TWI830835B - 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 - Google Patents

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 Download PDF

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Publication number
TWI830835B
TWI830835B TW108145683A TW108145683A TWI830835B TW I830835 B TWI830835 B TW I830835B TW 108145683 A TW108145683 A TW 108145683A TW 108145683 A TW108145683 A TW 108145683A TW I830835 B TWI830835 B TW I830835B
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Taiwan
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active compound
formula
wetting agent
water
compound product
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TW108145683A
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English (en)
Chinese (zh)
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TW202039488A (zh
Inventor
彼得 費伊
米哈爾 索瓦
約爾格 布羅克布
馬庫斯 朗格里奇
古伊多 貝克爾
海克 紐曼
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德商亞德維瑞醫藥有限公司
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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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Cardiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
TW108145683A 2018-12-17 2019-12-13 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 TWI830835B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18213115.1 2018-12-17
EP18213115 2018-12-17

Publications (2)

Publication Number Publication Date
TW202039488A TW202039488A (zh) 2020-11-01
TWI830835B true TWI830835B (zh) 2024-02-01

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TW108145683A TWI830835B (zh) 2018-12-17 2019-12-13 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

Country Status (19)

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US (1) US12172996B2 (enExample)
EP (1) EP3898624A1 (enExample)
JP (1) JP7529667B2 (enExample)
KR (1) KR102872983B1 (enExample)
CN (1) CN113207290B (enExample)
AR (1) AR116912A1 (enExample)
AU (1) AU2019409269B2 (enExample)
BR (1) BR112021009122A2 (enExample)
CL (1) CL2021001580A1 (enExample)
CO (1) CO2021007668A2 (enExample)
IL (1) IL283976B2 (enExample)
JO (1) JOP20210155B1 (enExample)
MX (1) MX2021007090A (enExample)
PE (1) PE20211593A1 (enExample)
SG (1) SG11202104953VA (enExample)
TW (1) TWI830835B (enExample)
UA (1) UA129677C2 (enExample)
WO (1) WO2020126983A1 (enExample)
ZA (1) ZA202105021B (enExample)

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
WO2021156223A1 (en) 2020-02-03 2021-08-12 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130143900A1 (en) * 2011-11-25 2013-06-06 Bayer Intellectual Property Gmbh Process for preparing substituted 5-fluoro-1H-pyrazolopyridines

Family Cites Families (13)

* 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
DK3415515T3 (da) 2009-11-27 2020-03-16 Adverio Pharma Gmbh Fremgangsmåde til fremstilling af methyl-{4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamat
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
CA2901636A1 (en) * 2013-02-21 2014-08-28 Adverio Pharma Gmbh Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate
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
EP3914588A1 (en) 2019-01-22 2021-12-01 Adverio Pharma GmbH Process for manufacturing 4-(2,2,3,3-tetrafluoropropyl)morpholine
WO2021156223A1 (en) * 2020-02-03 2021-08-12 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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130143900A1 (en) * 2011-11-25 2013-06-06 Bayer Intellectual Property Gmbh Process for preparing substituted 5-fluoro-1H-pyrazolopyridines

Also Published As

Publication number Publication date
AU2019409269B2 (en) 2025-04-03
CO2021007668A2 (es) 2021-07-19
ZA202105021B (en) 2026-05-27
BR112021009122A2 (pt) 2021-08-10
CN113207290B (zh) 2024-04-09
US20220048907A1 (en) 2022-02-17
TW202039488A (zh) 2020-11-01
US12172996B2 (en) 2024-12-24
PE20211593A1 (es) 2021-08-18
KR20210104703A (ko) 2021-08-25
EP3898624A1 (en) 2021-10-27
MX2021007090A (es) 2021-08-11
AU2019409269A1 (en) 2021-06-03
IL283976B2 (en) 2025-04-01
UA129677C2 (uk) 2025-07-02
SG11202104953VA (en) 2021-06-29
JOP20210155A1 (ar) 2023-01-30
WO2020126983A1 (en) 2020-06-25
CN113207290A (zh) 2021-08-03
CA3123360A1 (en) 2020-06-25
JOP20210155B1 (ar) 2025-10-01
CL2021001580A1 (es) 2021-12-03
KR102872983B1 (ko) 2025-10-17
JP2022515376A (ja) 2022-02-18
JP7529667B2 (ja) 2024-08-06
AR116912A1 (es) 2021-06-23
IL283976A (en) 2021-07-29
IL283976B1 (en) 2024-12-01

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