SG11201700785UA - Method for the preparation of (4s)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1-6-naphthyridine-3-carbox-amide and the purification thereof for use as an active pharmaceutical ingredient - Google Patents

Method for the preparation of (4s)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1-6-naphthyridine-3-carbox-amide and the purification thereof for use as an active pharmaceutical ingredient

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Publication number
SG11201700785UA
SG11201700785UA SG11201700785UA SG11201700785UA SG11201700785UA SG 11201700785U A SG11201700785U A SG 11201700785UA SG 11201700785U A SG11201700785U A SG 11201700785UA SG 11201700785U A SG11201700785U A SG 11201700785UA SG 11201700785U A SG11201700785U A SG 11201700785UA
Authority
SG
Singapore
Prior art keywords
carbox
naphthyridine
methoxyphenyl
dihydro
ethoxy
Prior art date
Application number
SG11201700785UA
Other languages
English (en)
Inventor
Johannes Platzek
Gunnar Garke
Alfons Grunenberg
Original Assignee
Bayer Pharma AG
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51260727&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG11201700785U(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of SG11201700785UA publication Critical patent/SG11201700785UA/en

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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
    • A61K31/435—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
SG11201700785UA 2014-08-01 2015-07-29 Method for the preparation of (4s)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1-6-naphthyridine-3-carbox-amide and the purification thereof for use as an active pharmaceutical ingredient SG11201700785UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14179544 2014-08-01
PCT/EP2015/067340 WO2016016287A1 (fr) 2014-08-01 2015-07-29 Procédé pour fabriquer du (4s)-4-(4-cyano-2-méthoxyphényl)-5-éthoxy-2,8-diméthyl-1,4-dihydro-1,6-naphthyridin-3-carboxamide et le purifier en vue de l'utiliser en tant que principe actif pharmaceutique

Publications (1)

Publication Number Publication Date
SG11201700785UA true SG11201700785UA (en) 2017-02-27

Family

ID=51260727

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201700785UA SG11201700785UA (en) 2014-08-01 2015-07-29 Method for the preparation of (4s)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1-6-naphthyridine-3-carbox-amide and the purification thereof for use as an active pharmaceutical ingredient

Country Status (30)

Country Link
US (4) USRE49575E1 (fr)
EP (2) EP3660015A1 (fr)
JP (1) JP6818674B2 (fr)
KR (2) KR20230066477A (fr)
CN (4) CN106795155B (fr)
AR (1) AR101403A1 (fr)
AU (1) AU2015295376C1 (fr)
BR (1) BR112017001678B1 (fr)
CA (2) CA2956529A1 (fr)
CL (1) CL2017000263A1 (fr)
CO (1) CO2017000886A2 (fr)
DK (1) DK3174875T3 (fr)
ES (1) ES2828704T3 (fr)
HR (1) HRP20201800T1 (fr)
HU (1) HUE051350T2 (fr)
IL (1) IL250239B (fr)
JO (1) JO3648B1 (fr)
LT (1) LT3174875T (fr)
MX (1) MX369467B (fr)
MY (1) MY198066A (fr)
PE (1) PE20170141A1 (fr)
PL (1) PL3174875T3 (fr)
PT (1) PT3174875T (fr)
RS (1) RS60921B1 (fr)
RU (1) RU2729998C9 (fr)
SG (1) SG11201700785UA (fr)
SI (1) SI3174875T1 (fr)
TW (1) TWI684593B (fr)
UY (1) UY36251A (fr)
WO (1) WO2016016287A1 (fr)

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CN106795155B (zh) * 2014-08-01 2023-06-16 拜耳医药股份有限公司 一种化合物的制备方法及其纯化以用作活性药物成分
LT3337800T (lt) 2015-08-21 2019-08-12 Bayer Pharma Aktiengesellschaft (4s)-4-(4-ciano-2-metoksifenil)-5-etoksi-2,8-dimetil-1,4-dihidro-1,6-naftiridin-3-karboksamido, skirto naudoti kaip veikliojo farmacinio ingrediento, gamybos būdas ir gryninimas
EP3560922A1 (fr) 2018-04-24 2019-10-30 Bayer Aktiengesellschaft Procédé de preparation de (4s) - 4- (4-cyano-2-methoxyphenyl) -5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide par résolution racémique par esters d'acide tartrique
JP2022523986A (ja) 2019-03-05 2022-04-27 バイエル アクチェンゲゼルシャフト 中間体化合物２－クロロ－５－メチル－４－ピリジナミンを使用した、２－クロロ－５－メチル－４－ニトロ－ピリジン－１－オキシドからの４－アミノ－５－メチル－１ｈ－ピリジン－２（１ｈ）－オン（ｍｒアンタゴニストフィネレノンを合成するための中間体化合物）の合成
JP2022523984A (ja) 2019-03-05 2022-04-27 バイエル アクチェンゲゼルシャフト ４－アミノ－５－メチルピリドンを調製する方法
KR20220084103A (ko) * 2019-10-17 2022-06-21 바이엘 악티엔게젤샤프트 부분입체이성질체 타르타르산 에스테르를 사용한 라세미체 분해에 의한 2-시아노에틸 (4s)-4-(4-시아노-2-메톡시페닐)-5-에톡시-2,8-디메틸-1,4-디히드로-1,6-나프티리딘-3-카르복실레이트의 제조 방법
EP4045499A1 (fr) * 2019-10-17 2022-08-24 Bayer Aktiengesellschaft Procédé de préparation de (2-cyanoéthyl (4s)-4-(4-cyano-2-méthoxy-phényl)-5-hydroxy-2,8-diméthyl-1,4-dihydro-1,6-naphtyridin-3-carboxylate par séparation racémique au moyen d'esters d'acide tartrique diastéréoisomères
EP4045502A1 (fr) * 2019-10-17 2022-08-24 Bayer Aktiengesellschaft Procédé photochimique pour la préparation de (4r, 4s)-4-(4-cyano-2-méthoxyphényl)-5-éthoxy-2,8-diméthyl-1,4-dihydro-1,6-naphtyridine-3-carbox-amide
WO2021074077A1 (fr) * 2019-10-17 2021-04-22 Bayer Aktiengesellschaft Procédé de production des esters acyloxyméthyles d'acide (4s)-(4-cyano-2-méthoxyphényl)-5-éthoxy-2,8-diméthyl-1,4-dihydro-1,6-naphtyridin-3-carboxylique
EP3900722A1 (fr) 2020-04-22 2021-10-27 Bayer AG Association de finerenone et de pecavaptan pour le traitement et / ou la prevention des maladies cardiovasculaires et / ou renales
CN115916197A (zh) 2020-04-22 2023-04-04 拜耳公司 用于治疗和/或预防心血管和/或肾脏疾病的非奈利酮和sglt2抑制剂的组合
TW202214624A (zh) 2020-06-16 2022-04-16 德商拜耳廠股份有限公司 藉由催化不對稱漢斯（ｈａｎｔｚｓｃｈ）酯還原法進行之製備（４ｓ）－４－（４－氰基－２－甲氧基苯基）－５－乙氧基－２，８－二甲基－１，４－二氫－１，６－㖠啶－３－羧醯胺的方法
CN112237573B (zh) * 2020-10-29 2023-12-22 瑞阳制药股份有限公司 含finerenone的片剂及其制备方法
WO2022214206A1 (fr) 2021-04-08 2022-10-13 Bayer Aktiengesellschaft Combinaison de finérénone et de pecavaptan pour le traitement et/ou la prévention de maladies cardiovasculaires et/ou rénales
CN114149427A (zh) * 2021-12-18 2022-03-08 上海鼎雅药物化学科技有限公司 非奈利酮及其中间体的合成方法
CN115340540A (zh) * 2022-01-20 2022-11-15 奥锐特药业股份有限公司 制备非奈利酮及其中间体的方法
CN114524812A (zh) * 2022-03-18 2022-05-24 湖南凯铂生物药业有限公司 1,4-二氢-1,6-萘啶化合物的晶型制备以及合成方法
WO2023205164A1 (fr) 2022-04-18 2023-10-26 Teva Pharmaceuticals International Gmbh Procédés de préparation de finérénone
EP4286368A1 (fr) 2022-05-31 2023-12-06 Bayer Aktiengesellschaft Procédé de production de 4-formyl-3-méthoxybenzonitrile
WO2024075139A1 (fr) * 2022-10-06 2024-04-11 Maithri Drugs Private Limited Procédé de préparation de finérénone et de ses intermédiaires
WO2024110523A1 (fr) 2022-11-23 2024-05-30 Bayer Aktiengesellschaft Traitement d'une maladie rénale chronique chez un patient atteint de diabète sucré de type i

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