LT2733142T - Metil-{4,6-diamino-2-[1-(2-fluorbenzil)-1h-pirazol[3,4-b]piridin-3-il]pirimidin-5-il}metilkarbamato, skirto naudoti kaip farmaciškai veiksmingo ingrediento, gamybos būdas - Google Patents
Metil-{4,6-diamino-2-[1-(2-fluorbenzil)-1h-pirazol[3,4-b]piridin-3-il]pirimidin-5-il}metilkarbamato, skirto naudoti kaip farmaciškai veiksmingo ingrediento, gamybos būdasInfo
- Publication number
- LT2733142T LT2733142T LTEP14154762.0T LT14154762T LT2733142T LT 2733142 T LT2733142 T LT 2733142T LT 14154762 T LT14154762 T LT 14154762T LT 2733142 T LT2733142 T LT 2733142T
- Authority
- LT
- Lithuania
- Prior art keywords
- methylcarbamate
- fluorobenzyl
- pyrazolo
- pyrimidin
- diamino
- Prior art date
Links
- 239000004480 active ingredient Substances 0.000 title 1
- WXXSNCNJFUAIDG-UHFFFAOYSA-N riociguat Chemical compound N1=C(N)C(N(C)C(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F WXXSNCNJFUAIDG-UHFFFAOYSA-N 0.000 title 1
Classifications
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C325/00—Thioaldehydes; Thioketones; Thioquinones; Oxides thereof
- C07C325/02—Thioketones; Oxides thereof
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- 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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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
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- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
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- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Diabetes (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09177371 | 2009-11-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| LT2733142T true LT2733142T (lt) | 2018-10-10 |
Family
ID=43536603
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LTEP18178602.1T LT3415515T (lt) | 2009-11-27 | 2010-11-22 | Metil-{4,6-diamino-2-[1-(2-fluorbenzil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}metilkarbamato gamybos būdas |
| LTEP14154762.0T LT2733142T (lt) | 2009-11-27 | 2010-11-22 | Metil-{4,6-diamino-2-[1-(2-fluorbenzil)-1h-pirazol[3,4-b]piridin-3-il]pirimidin-5-il}metilkarbamato, skirto naudoti kaip farmaciškai veiksmingo ingrediento, gamybos būdas |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LTEP18178602.1T LT3415515T (lt) | 2009-11-27 | 2010-11-22 | Metil-{4,6-diamino-2-[1-(2-fluorbenzil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}metilkarbamato gamybos būdas |
Country Status (43)
Families Citing this family (27)
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| CN102791707B (zh) * | 2009-11-27 | 2014-10-29 | 拜耳知识产权有限责任公司 | {4,6-二氨基-2-[1-(2-氟苄基)-1h-吡唑并[3,4-b]吡啶-3-基]嘧啶-5-基}甲基氨基甲酸甲酯的制备方法以及为了将其用作药用活性成分的纯化方法 |
| WO2011066352A1 (en) | 2009-11-27 | 2011-06-03 | Genzyme Corporation | An amorphous and a crystalline form of genz 112638 hemitartrat as inhibitor of glucosylceramide synthase |
| DE102010021637A1 (de) | 2010-05-26 | 2011-12-01 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
| DE102010043380A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Benzyl-substituierte Carbamate und ihre Verwendung |
| DE102010043379A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung |
| UA111754C2 (uk) | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| KR102026059B1 (ko) | 2011-11-25 | 2019-09-26 | 아드베리오 파마 게엠베하 | 치환된 5-플루오로-1h-피라졸로피리딘의 제조 방법 |
| KR20150119871A (ko) * | 2013-02-21 | 2015-10-26 | 아드베리오 파마 게엠베하 | 메틸 ｛4,6-디아미노-2-[1-(2-플루오로벤질)-1H-피라졸로[3,4-b]피리디노-3-일]피리미디노-5-일｝메틸 카르바메이트의 형태 |
| CN104327107A (zh) | 2013-10-17 | 2015-02-04 | 广东东阳光药业有限公司 | 一种氟喹诺酮类抗菌药物的制备方法 |
| TN2017000092A1 (en) | 2014-09-19 | 2018-07-04 | Bayer Pharma AG | Benzyl substituted indazoles as bub1 inhibitors. |
| WO2016113415A1 (en) | 2015-01-16 | 2016-07-21 | Sandoz Ag | Process for the preparation of riociguat essentially free from genotoxic impurities |
| CN105367568B (zh) * | 2015-11-18 | 2019-08-20 | 浙江京新药业股份有限公司 | 一种制备利奥西呱的方法 |
| 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 |
| MX2018007152A (es) | 2015-12-14 | 2018-08-15 | Ironwood Pharmaceuticals Inc | Uso de estimuladores de guanilato ciclasa soluble (sgc) para el tratamiento de la disfuncion del esfinter gastrointestinal. |
| WO2017103760A1 (en) * | 2015-12-15 | 2017-06-22 | Alembic Pharmaceuticals Limited | Novel polymorph of riociguat and its process for the preparation |
| CN108069960A (zh) * | 2016-11-15 | 2018-05-25 | 江苏豪森药业集团有限公司 | 利奥西呱中间体的制备方法 |
| 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 |
| EP3554488A2 (en) | 2016-12-13 | 2019-10-23 | Cyclerion Therapeutics, Inc. | Use of sgc stimulators for the treatment of esophageal motility disorders |
| 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 |
| 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 |
| 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 |
| CN111689961A (zh) * | 2020-06-01 | 2020-09-22 | 江苏华阳制药有限公司 | 一种利奧西呱的新晶型及其制备方法 |
| 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 |
| CN112316932B (zh) * | 2020-11-13 | 2022-03-01 | 中国石油大学(北京) | 一种粗对苯二甲酸加氢精制催化剂及其制备方法和应用 |
| CN112316968B (zh) * | 2020-11-13 | 2022-03-01 | 中国石油大学(北京) | 一种粗对苯二甲酸加氢精制催化剂及其制备方法和应用 |
| CN117229282A (zh) * | 2023-09-11 | 2023-12-15 | 安徽美诺华药物化学有限公司 | 一种利奥西呱的合成工艺 |
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| DE10057751A1 (de) * | 2000-11-22 | 2002-05-23 | Bayer Ag | Neue Carbamat-substituierte Pyrazolopyridinderivate |
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| DE10132416A1 (de) * | 2001-07-04 | 2003-01-16 | Bayer Ag | Neue Morpholin-überbrückte Pyrazolopyridinderivate |
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| DE10222550A1 (de) * | 2002-05-17 | 2003-11-27 | Bayer Ag | Substituierte Benzyl-pyrazolopyridine |
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| KR200342343Y1 (ko) | 2003-11-17 | 2004-02-18 | 김강철 | 탄성체 유희용구 |
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| DE102006043443A1 (de) * | 2006-09-15 | 2008-03-27 | Bayer Healthcare Ag | Neue aza-bicyclische Verbindungen und ihre Verwendung |
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| CN102791707B (zh) * | 2009-11-27 | 2014-10-29 | 拜耳知识产权有限责任公司 | {4,6-二氨基-2-[1-(2-氟苄基)-1h-吡唑并[3,4-b]吡啶-3-基]嘧啶-5-基}甲基氨基甲酸甲酯的制备方法以及为了将其用作药用活性成分的纯化方法 |
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| DE102010043380A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Benzyl-substituierte Carbamate und ihre Verwendung |
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| DE102012200360A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte Triazine und ihre Verwendung |
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