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DK3421470T3 - Substituerede 5-fluor-1h-pyrazolopyridiner i krytallinsk form - Google Patents

Substituerede 5-fluor-1h-pyrazolopyridiner i krytallinsk form Download PDF

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Publication number
DK3421470T3
DK3421470T3 DK18178621.1T DK18178621T DK3421470T3 DK 3421470 T3 DK3421470 T3 DK 3421470T3 DK 18178621 T DK18178621 T DK 18178621T DK 3421470 T3 DK3421470 T3 DK 3421470T3
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DK
Denmark
Prior art keywords
crythallic
pyrazolopyridines
fluoro
substituted
crythallic form
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DK18178621.1T
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English (en)
Inventor
Peter Fey
Alfons Grunenberg
Donald Bierer
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Adverio Pharma Gmbh
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Publication of DK3421470T3 publication Critical patent/DK3421470T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/10Heterocyclic 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 doubly bound oxygen or sulphur atoms
    • C07D295/104Heterocyclic 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 doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/02Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms
    • C07C317/04Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/02Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/023Preparation; Separation; Stabilisation; Use of additives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/02Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/02Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/037Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements with quaternary ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/06Heterocyclic 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
    • C07D295/067Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Cardiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Plant Substances (AREA)
DK18178621.1T 2011-11-25 2012-11-21 Substituerede 5-fluor-1h-pyrazolopyridiner i krytallinsk form DK3421470T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11190789 2011-11-25
EP11192301 2011-12-07
EP12790891.1A EP2782914B1 (de) 2011-11-25 2012-11-21 Verfahren zur herstellung von substituierten 5-fluor-1h-pyrazolopyridinen

Publications (1)

Publication Number Publication Date
DK3421470T3 true DK3421470T3 (da) 2021-04-06

Family

ID=47222101

Family Applications (3)

Application Number Title Priority Date Filing Date
DK15151593.9T DK2896617T3 (da) 2011-11-25 2012-11-21 Fremgangsmåde til fremstilling af substituerede (z)-alpha-fluoro-beta-amino-acrylaldehyder
DK12790891.1T DK2782914T3 (da) 2011-11-25 2012-11-21 Fremgangsmåde til fremstilling af substituerede 5-fluor-1h-pyrazolopyridiner
DK18178621.1T DK3421470T3 (da) 2011-11-25 2012-11-21 Substituerede 5-fluor-1h-pyrazolopyridiner i krytallinsk form

Family Applications Before (2)

Application Number Title Priority Date Filing Date
DK15151593.9T DK2896617T3 (da) 2011-11-25 2012-11-21 Fremgangsmåde til fremstilling af substituerede (z)-alpha-fluoro-beta-amino-acrylaldehyder
DK12790891.1T DK2782914T3 (da) 2011-11-25 2012-11-21 Fremgangsmåde til fremstilling af substituerede 5-fluor-1h-pyrazolopyridiner

Country Status (41)

Country Link
US (7) US8802847B2 (da)
EP (3) EP3421470B8 (da)
JP (4) JP6189315B2 (da)
KR (3) KR101993022B1 (da)
CN (3) CN105503867B (da)
AP (2) AP2014007705A0 (da)
AR (1) AR088983A1 (da)
AU (3) AU2012342547C1 (da)
BR (2) BR112014012414B1 (da)
CA (2) CA3040720C (da)
CL (2) CL2014001339A1 (da)
CO (1) CO6960555A2 (da)
CR (3) CR20210072A (da)
CU (3) CU24354B1 (da)
CY (1) CY1124000T1 (da)
DK (3) DK2896617T3 (da)
DO (3) DOP2014000112A (da)
EA (4) EA030018B1 (da)
EC (1) ECSP14001627A (da)
ES (3) ES2864009T3 (da)
GT (1) GT201400101A (da)
HR (3) HRP20181818T1 (da)
HU (3) HUE031029T2 (da)
IL (3) IL232585A0 (da)
JO (3) JOP20120351B1 (da)
LT (3) LT2782914T (da)
MX (2) MX357481B (da)
MY (3) MY168412A (da)
PE (3) PE20190180A1 (da)
PH (2) PH12014501160B1 (da)
PL (3) PL3421470T3 (da)
PT (3) PT2782914T (da)
RS (3) RS61609B1 (da)
SG (3) SG11201402111QA (da)
SI (3) SI3421470T1 (da)
TR (1) TR201816203T4 (da)
TW (5) TWI631123B (da)
UA (3) UA120278C2 (da)
UY (2) UY34467A (da)
WO (1) WO2013076168A1 (da)
ZA (2) ZA201403613B (da)

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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
US20230067593A1 (en) * 2020-02-03 2023-03-02 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
EP4396185A1 (en) 2021-08-31 2024-07-10 Teva Pharmaceuticals International GmbH Solid state forms of vericiguat and process for preparation thereof
ES2956054B2 (es) 2022-05-03 2024-07-01 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
WO2024038398A1 (en) * 2022-08-18 2024-02-22 Torrent Pharmaceuticals Limited Novel salt of substituted 5-fluoro-1h-pyrazolopyridines and its uses
WO2025114276A1 (en) 2023-12-01 2025-06-05 Krka, D.D., Novo Mesto Solid oral composition comprising vericiguat
US20250205235A1 (en) 2023-12-20 2025-06-26 Adverio Pharma Gmbh Dose regimen for vericiguat
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