HK1178899A1 - Method for producing methyl-4,6-diamino-2-[1-(2-fluorobenzyl)-1h- pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-ylmethyl carbamate and its purification for use thereof as pharmaceutical substance 46--2-[1-(2-)-1h-[34-b]-3-]-5- - Google Patents

Method for producing methyl-4,6-diamino-2-[1-(2-fluorobenzyl)-1h- pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-ylmethyl carbamate and its purification for use thereof as pharmaceutical substance 46--2-[1-(2-)-1h-[34-b]-3-]-5-

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Publication number
HK1178899A1
HK1178899A1 HK13105844.2A HK13105844A HK1178899A1 HK 1178899 A1 HK1178899 A1 HK 1178899A1 HK 13105844 A HK13105844 A HK 13105844A HK 1178899 A1 HK1178899 A1 HK 1178899A1
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HK
Hong Kong
Prior art keywords
pyrimidino
pyridino
fluorobenzyl
pyrazolo
diamino
Prior art date
Application number
HK13105844.2A
Other languages
English (en)
Chinese (zh)
Inventor
Franz-Josef Mais
Joachim Rehse
Winfried Joentgen
Konrad Siegel
Original Assignee
Adverio Pharma Gmbh
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Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43536603&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1178899(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Adverio Pharma Gmbh filed Critical Adverio Pharma Gmbh
Publication of HK1178899A1 publication Critical patent/HK1178899A1/xx

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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
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    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C325/00—Thioaldehydes; Thioketones; Thioquinones; Oxides thereof
    • C07C325/02—Thioketones; Oxides thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
HK13105844.2A 2009-11-27 2013-05-16 Method for producing methyl-4,6-diamino-2-[1-(2-fluorobenzyl)-1h- pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-ylmethyl carbamate and its purification for use thereof as pharmaceutical substance 46--2-[1-(2-)-1h-[34-b]-3-]-5- HK1178899A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09177371 2009-11-27
PCT/EP2010/067949 WO2011064171A2 (de) 2009-11-27 2010-11-22 Verfahren zur herstellung von methyl-{4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamat und dessen aufreinigung für die verwendung als pharmazeutischer wirkstoff

Publications (1)

Publication Number Publication Date
HK1178899A1 true HK1178899A1 (en) 2013-09-19

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ID=43536603

Family Applications (2)

Application Number Title Priority Date Filing Date
HK13105844.2A HK1178899A1 (en) 2009-11-27 2013-05-16 Method for producing methyl-4,6-diamino-2-[1-(2-fluorobenzyl)-1h- pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-ylmethyl carbamate and its purification for use thereof as pharmaceutical substance 46--2-[1-(2-)-1h-[34-b]-3-]-5-
HK15102784.9A HK1202292A1 (en) 2009-11-27 2015-03-18 Process for preparing methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1h- pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-ylmethylcarbamate and its purification for use as pharmaceutically active compound 46--2-[1-(2-)-1h-[34-b]-3-]-5-

Family Applications After (1)

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HK15102784.9A HK1202292A1 (en) 2009-11-27 2015-03-18 Process for preparing methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1h- pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-ylmethylcarbamate and its purification for use as pharmaceutically active compound 46--2-[1-(2-)-1h-[34-b]-3-]-5-

Country Status (43)

Country Link
US (5) US8492544B2 (hu)
EP (5) EP2504334B1 (hu)
JP (4) JP5859451B2 (hu)
KR (2) KR101766931B1 (hu)
CN (2) CN104059064B (hu)
AR (1) AR079134A1 (hu)
AU (3) AU2010323227B2 (hu)
BR (3) BR112012012617B8 (hu)
CA (2) CA2781799C (hu)
CL (1) CL2012001329A1 (hu)
CO (1) CO6551708A2 (hu)
CR (1) CR20120280A (hu)
CU (1) CU24084B1 (hu)
CY (1) CY1115861T1 (hu)
DK (4) DK2733142T3 (hu)
DO (2) DOP2012000144A (hu)
EA (3) EA031632B1 (hu)
EC (2) ECSP12011921A (hu)
ES (4) ES2775902T3 (hu)
GT (1) GT201200158A (hu)
HK (2) HK1178899A1 (hu)
HR (4) HRP20141073T1 (hu)
HU (2) HUE040328T2 (hu)
IL (4) IL219683A (hu)
JO (3) JO3107B1 (hu)
LT (2) LT2733142T (hu)
MA (1) MA33783B1 (hu)
MX (1) MX2012005938A (hu)
MY (2) MY180184A (hu)
NZ (3) NZ600199A (hu)
PE (2) PE20180203A1 (hu)
PL (4) PL2733142T3 (hu)
PT (4) PT2604608E (hu)
RS (4) RS53585B1 (hu)
SI (4) SI2733142T1 (hu)
SM (1) SMT201400164B (hu)
TN (1) TN2012000257A1 (hu)
TR (1) TR201816146T4 (hu)
TW (1) TWI496781B (hu)
UA (1) UA110779C2 (hu)
UY (1) UY33048A (hu)
WO (1) WO2011064171A2 (hu)
ZA (1) ZA201204610B (hu)

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CN105294686B (zh) * 2015-11-30 2017-03-22 郑州大明药物科技有限公司 一种利奥西呱的制备方法
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WO2018096550A1 (en) * 2016-11-28 2018-05-31 Msn Laboratories Private Limited, R&D Center Process for the preparation of methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate and its polymorphs thereof
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WO2018130226A1 (zh) * 2017-01-16 2018-07-19 苏州科睿思制药有限公司 利奥西呱的新晶型及其制备方法和用途
BR112021000358A2 (pt) 2018-07-11 2021-04-06 Cyclerion Therapeutics, Inc. Uso de estimulantes de sgc para o tratamento de distúrbios mitocondriais
EP4099987A1 (en) * 2020-02-03 2022-12-14 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
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