CO2022018232A2 - Proceso para preparar carbamato de metil {4,6–diamino–2–[5–fluoro–1–(2–fluorobencil)–1h–pirazolo[3,4–b]piridin–3–il]pirimidin–5–il} - Google Patents

Proceso para preparar carbamato de metil {4,6–diamino–2–[5–fluoro–1–(2–fluorobencil)–1h–pirazolo[3,4–b]piridin–3–il]pirimidin–5–il}

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Publication number
CO2022018232A2
CO2022018232A2 CONC2022/0018232A CO2022018232A CO2022018232A2 CO 2022018232 A2 CO2022018232 A2 CO 2022018232A2 CO 2022018232 A CO2022018232 A CO 2022018232A CO 2022018232 A2 CO2022018232 A2 CO 2022018232A2
Authority
CO
Colombia
Prior art keywords
fluorobenzyl
pyrazolo
pyrimidin
diamino
pyridin
Prior art date
Application number
CONC2022/0018232A
Other languages
English (en)
Inventor
Guido Becker
Michal Sowa
Peter Fey
Markus Longerich
Joerg Brockob
Heike Neumann
Nadine Bremeyer
Thomas Frenzel
Helene Faber
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 CO2022018232A2 publication Critical patent/CO2022018232A2/es

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Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/067—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents attached to the same carbon chain, which is not interrupted by carbocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

La presente solicitud se refiere a un proceso novedoso y eficiente para preparar carbamato de metil {4,6–diamino–2–[5–fluoro–1–(2–fluorobencil)–1H–pirazolo[3,4–b]piridin–3–il]pirimidin–5–il} de la fórmula (I) (I) en la forma cristalina de la modificación I, donde el difractograma de rayos X del compuesto de la fórmula (I) en la modificación I exhibe máximos pico del ángulo 2 theta en 5.9, 6.9, 22.7, de pureza muy alta, resultando significativamente más rentable que el proceso conocido en la técnica y pudiéndose obtener con equipamientos piloto y en plantas de producción tradicionales (depósitos de agitación/dispositivos para aislamiento).
CONC2022/0018232A 2020-06-16 2022-12-15 Proceso para preparar carbamato de metil {4,6–diamino–2–[5–fluoro–1–(2–fluorobencil)–1h–pirazolo[3,4–b]piridin–3–il]pirimidin–5–il} CO2022018232A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20180229.5A EP3925953A1 (en) 2020-06-16 2020-06-16 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
PCT/EP2021/066019 WO2021254981A1 (en) 2020-06-16 2021-06-15 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

Publications (1)

Publication Number Publication Date
CO2022018232A2 true CO2022018232A2 (es) 2022-12-20

Family

ID=71103286

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0018232A CO2022018232A2 (es) 2020-06-16 2022-12-15 Proceso para preparar carbamato de metil {4,6–diamino–2–[5–fluoro–1–(2–fluorobencil)–1h–pirazolo[3,4–b]piridin–3–il]pirimidin–5–il}

Country Status (17)

Country Link
US (1) US20230219952A1 (es)
EP (2) EP3925953A1 (es)
JP (1) JP2023530142A (es)
KR (1) KR20230025862A (es)
CN (1) CN115697978A (es)
AR (1) AR122635A1 (es)
AU (1) AU2021294233A1 (es)
BR (1) BR112022023035A2 (es)
CA (1) CA3187147A1 (es)
CL (1) CL2022003600A1 (es)
CO (1) CO2022018232A2 (es)
CR (1) CR20220647A (es)
IL (1) IL298913A (es)
MX (1) MX2022015952A (es)
PE (1) PE20231553A1 (es)
TW (1) TW202214625A (es)
WO (1) WO2021254981A1 (es)

Families Citing this family (3)

* 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
ES2956054A1 (es) * 2022-05-03 2023-12-12 Moehs Iberica Sl 2-(5-FLUORO-1-(2-FLUOROBENCIL)-1H-PIRAZOLO[3,4-b]PIRIDIN-3-IL)-5-NITROSOPIRIMIDIN-4,6-DIAMINA O UNA SAL DE LA MISMA, PROCEDIMIENTO PARA SU PREPARACION Y SU USO EN LA SINTESIS DE VERICIGUAT
CN115043835B (zh) * 2022-06-17 2023-05-09 常州制药厂有限公司 一种维立西呱的精制纯化方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
RS54433B1 (en) * 2009-11-27 2016-04-28 Adverio Pharma Gmbh PROCEDURE FOR THE PRODUCTION OF METHYL- {4,6-DIAMINO-2- [1- (2-FLUOROBENZYL) -1H-PYRAZOLO [3,4-B] PYRIDIN-3-IL] PYRIMIDIN-5-IL} METHYLCARBAMATE AND ITS Purification thereof ITS USE AS A PHARMACEUTICAL AGENCY
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
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
CN103038232B (zh) * 2010-05-26 2016-01-20 阿德弗里奥药品有限责任公司 单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途
DE102010040233A1 (de) * 2010-09-03 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Bicyclische Aza-Heterocyclen und ihre Verwendung
PE20141582A1 (es) * 2011-09-02 2014-11-06 Bayer Ip Gmbh Pirimidinas anilladas sustituidas y uso de las mismas
HUE041592T2 (hu) * 2011-11-25 2019-05-28 Adverio Pharma Gmbh Eljárás szubsztituált 5-fluor-1H-pirazolopiridinek elõállítására
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

Also Published As

Publication number Publication date
EP3925953A1 (en) 2021-12-22
JP2023530142A (ja) 2023-07-13
CR20220647A (es) 2023-03-03
AU2021294233A1 (en) 2022-12-22
CA3187147A1 (en) 2021-12-23
TW202214625A (zh) 2022-04-16
KR20230025862A (ko) 2023-02-23
CL2022003600A1 (es) 2023-04-28
PE20231553A1 (es) 2023-10-03
CN115697978A (zh) 2023-02-03
AR122635A1 (es) 2022-09-28
US20230219952A1 (en) 2023-07-13
BR112022023035A2 (pt) 2022-12-27
IL298913A (en) 2023-02-01
EP4165028A1 (en) 2023-04-19
MX2022015952A (es) 2023-01-24
WO2021254981A1 (en) 2021-12-23

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