CN116655627A - 一种化合物的制备方法及其纯化以用作活性药物成分 - Google Patents

一种化合物的制备方法及其纯化以用作活性药物成分 Download PDF

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Publication number
CN116655627A
CN116655627A CN202310616268.7A CN202310616268A CN116655627A CN 116655627 A CN116655627 A CN 116655627A CN 202310616268 A CN202310616268 A CN 202310616268A CN 116655627 A CN116655627 A CN 116655627A
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compound
formula
compounds
mixture
water
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J·普拉策克
G·加尔克
A·格鲁嫩贝格
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Bayer Pharma AG
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Bayer Pharma AG
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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
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    • A61P13/00—Drugs for disorders of the urinary system
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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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  • Organic Chemistry (AREA)
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  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • 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)
CN202310616268.7A 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分 Pending CN116655627A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP14179544 2014-08-01
EP14179544.3 2014-08-01
PCT/EP2015/067340 WO2016016287A1 (de) 2014-08-01 2015-07-29 Verfahren zur herstellung von (4s)- 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carbox-amid und dessen aufreinigung für die verwendung als pharmazeutischer wirkstoff
CN201580053456.7A CN106795155B (zh) 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分

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CN201580053456.7A Active CN106795155B (zh) 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分
CN202310619597.7A Pending CN116655629A (zh) 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分
CN202310620718.XA Active CN116655630B (zh) 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分

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CN202310619597.7A Pending CN116655629A (zh) 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分
CN202310620718.XA Active CN116655630B (zh) 2014-08-01 2015-07-29 一种化合物的制备方法及其纯化以用作活性药物成分

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JP (1) JP6818674B2 (enExample)
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CN (4) CN116655627A (enExample)
AR (1) AR101403A1 (enExample)
AU (1) AU2015295376C1 (enExample)
BR (1) BR112017001678B1 (enExample)
CA (2) CA3146285C (enExample)
CL (1) CL2017000263A1 (enExample)
CO (1) CO2017000886A2 (enExample)
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PE (1) PE20170141A1 (enExample)
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RU (1) RU2729998C9 (enExample)
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116655629A (zh) * 2014-08-01 2023-08-29 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
WO2025112640A1 (zh) * 2023-12-01 2025-06-05 山东诚创蓝海医药科技有限公司 一种非奈利酮-马来酸共晶及其制备方法

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PT3337800T (pt) 2015-08-21 2019-08-05 Bayer Pharma AG Método para a preparação de (4s)-4-(4-ciano-2-metoxi fenil)-5-etoxi-2,8-dimetil-1,4-di-hidro-1-6-naftiridina-3- carboxamida e purificação do mesmo para a utilização como ingrediente farmacêutico ativo
EP3560922A1 (de) 2018-04-24 2019-10-30 Bayer Aktiengesellschaft Verfahren zur herstellung von (4s)- 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carbox-amid durch racemat-spaltung mittels diastereomerer weinsäureester
MX2021010612A (es) 2019-03-05 2021-09-28 Bayer Ag Sintesis de 4-amino-5-metil-1h-piridin-2(1h)-on (compuesto intermediario para la sintesis del antagonista mr finerenona) a partir de 2-cloro-5-metil-4-nitro-piridina-1-oxido usando el compuesto intermediario 2-cloro-5-metil-4-piridinamina.
CN113412255B (zh) 2019-03-05 2024-07-02 拜耳公司 制备4-氨基-5-甲基吡啶酮的方法
MX2022004480A (es) * 2019-10-17 2022-05-06 Bayer Ag Procedimiento para preparar esteres aciloximetilicos del acido (4s)-(4-ciano-2-metoxifenil)-5-etoxi-2,8-dimetil-1,4-dihidro-1,6- naftiridin-3-carboxilico.
WO2021074072A1 (de) * 2019-10-17 2021-04-22 Bayer Aktiengesellschaft Verfahren zur herstellung von 2-cyanoethyl (4s)-4-(4-cyano-2-methoxy-phenyl)-5-hydroxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxylat durch racemat-spaltung mittels diastereomerer weinsäureester
MX2022004467A (es) * 2019-10-17 2022-05-03 Bayer Ag Procedimiento para preparar (4s)-4-(4-ciano-2-metoxi-fenil)-5-etox i-2,8-dimetil-1,4-dihidro-1,6-naftiridin-3-carboxilato de 2-cianoetilo mediante separacion de racematos utilizando esteres diastereomericos de acido tartarico.
BR112022005899A2 (pt) 2019-10-17 2022-06-28 Bayer Ag Método fotoquímico para preparar (4r,4s)-4-(ciano-2-metoxifenil)-5-etoxi-2,8-dietil-1,4-dihidro-1,6-naftidirina-1,6-carboxamida
EP3900722A1 (en) 2020-04-22 2021-10-27 Bayer AG Combination of finerenone and pecavaptan for the treatment and/or prevention of cardiovascular and/or renal diseases
US20230201174A1 (en) 2020-04-22 2023-06-29 Bayer Aktiengesellschaft Combination of finerenone and a sglt2 inhibitor for the treatment and/or prevention of cardiovascular and/or renal diseases
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 (en) 2021-04-08 2022-10-13 Bayer Aktiengesellschaft Combination of finerenone and pecavaptan for the treatment and/or prevention of cardiovascular and/or renal diseases
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
CN115340539B (zh) 2022-01-19 2024-02-27 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
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
US20250270184A1 (en) 2022-04-18 2025-08-28 Teva Pharmaceuticals International Gmbh Processes for the preparation of finerenone
EP4286368A1 (de) 2022-05-31 2023-12-06 Bayer Aktiengesellschaft Verfahren zur herstellung von 4-formyl-3-methoxybenzonitril
WO2024075139A1 (en) * 2022-10-06 2024-04-11 Maithri Drugs Private Limited A process for preparation of finerenone and intermediates thereof
WO2024094181A1 (zh) 2022-11-04 2024-05-10 南京威凯尔生物医药科技有限公司 通过非对映酒石酸酯拆分外消旋体制备非奈利酮的方法
EP4622646A1 (en) * 2022-11-23 2025-10-01 Bayer Aktiengesellschaft Treatment of chronic kidney disease in type i diabetes mellitus
WO2024126694A1 (en) 2022-12-16 2024-06-20 Bayer Aktiengesellschaft Sequential one-pot synthesis for preparing 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
WO2024147053A1 (en) * 2023-01-03 2024-07-11 Optimus Drugs Pvt Ltd Improved process for the preparation of finerenone
CN120731206A (zh) * 2023-03-17 2025-09-30 江苏恒瑞医药股份有限公司 一种1,4-二氢-1,6-萘啶酰胺化合物的可药用盐、晶型及其制备方法
WO2025104752A1 (en) * 2023-11-18 2025-05-22 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of (4s)4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
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