AR113852A1 - Procedimiento para la preparación de (3s)-3-(4-cloro-3-{[(2s,3r)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico y su forma cristalina para uso como principio activo farmacéutico - Google Patents

Procedimiento para la preparación de (3s)-3-(4-cloro-3-{[(2s,3r)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico y su forma cristalina para uso como principio activo farmacéutico

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Publication number
AR113852A1
AR113852A1 ARP180103492A ARP180103492A AR113852A1 AR 113852 A1 AR113852 A1 AR 113852A1 AR P180103492 A ARP180103492 A AR P180103492A AR P180103492 A ARP180103492 A AR P180103492A AR 113852 A1 AR113852 A1 AR 113852A1
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AR
Argentina
Prior art keywords
formula
methylbutanoyl
chlorophenyl
chloro
phenyl
Prior art date
Application number
ARP180103492A
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English (en)
Inventor
Spindler Felix Dr
Julia Ksel
Olenik Britta Dr
Lovis Kai Dr
Rubenbauer Philipp Dr
Fey Peter Dr
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Bayer Pharma AG
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Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of AR113852A1 publication Critical patent/AR113852A1/es

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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/88—Carboxylic acid amides having nitrogen atoms of carboxamide groups bound to an acyclic carbon atom and to a carbon atom of a six-membered aromatic ring wherein at least one ortho-hydrogen atom has been replaced
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    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
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    • C07C233/53—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/54—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
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    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/53—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/55—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
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    • C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
    • C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
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Abstract

La presente se refiere a un procedimiento para la preparación de (3S)-3-(4-cloro-3-{[(2S,3R)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico de la fórmula (1), el compuesto de la fórmula (1) en la forma cristalina y su uso para el tratamiento y/o la prevención de enfermedades, en particular para el tratamiento y/o la prevención de enfermedades cardiovasculares, cardiopulmonares y cardiorrenales. Reivindicación 1: Procedimiento para la preparación de (3S)-3-(4-cloro-3-{[(2S,3R)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico de fórmula (1) en la modificación cristalina 1 de fórmula (2), caracterizada porque el compuesto de la fórmula (1) se agita en un disolvente inerte seleccionado de una lista que contiene heptano, 2-metoxi-2-metil-propano, etanol, etanoato de etilo o mezclas de estos disolventes, a una temperatura de 20ºC a 120ºC y opcionalmente se aísla después de enfriar el compuesto de fórmula (2). Reivindicación 11: (3S)-3-(4-cloro-3-{[(2S,3R)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico en la modificación cristalina 1 de fórmula (2), caracterizada porque el Espectro IR del compuesto muestra máximos de banda a 1709, 1660, 1534, 1491, 1263, 1167, 1131, 1093, 1016 cm⁻¹.
ARP180103492A 2017-12-01 2018-11-28 Procedimiento para la preparación de (3s)-3-(4-cloro-3-{[(2s,3r)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico y su forma cristalina para uso como principio activo farmacéutico AR113852A1 (es)

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US (2) US11332435B2 (es)
EP (1) EP3717480A1 (es)
JP (1) JP2021504396A (es)
KR (1) KR20200094762A (es)
CN (1) CN111433204A (es)
AR (1) AR113852A1 (es)
AU (1) AU2018374452A1 (es)
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CA (1) CA3083986A1 (es)
CL (1) CL2020001420A1 (es)
CO (1) CO2020006789A2 (es)
IL (1) IL274715A (es)
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MX (2) MX2020005646A (es)
PE (1) PE20211391A1 (es)
RU (1) RU2020121714A (es)
SG (1) SG11202004577VA (es)
TW (1) TW201936568A (es)
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DE102011007272A1 (de) 2011-04-13 2012-10-18 Bayer Pharma Aktiengesellschaft Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung
MA53368A (fr) 2018-07-24 2021-06-02 Bayer Ag Formes galéniques pharmaceutiques à libération modifiée à administrer par voie orale
CN112998965B (zh) * 2021-02-22 2022-02-08 杭州可靠护理用品股份有限公司 具有粪便提示功能的婴儿纸尿裤
WO2024099361A1 (zh) * 2022-11-08 2024-05-16 南京明德新药研发有限公司 一种烷基羧酸类化合物的晶型及其应用

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DE102011007272A1 (de) 2011-04-13 2012-10-18 Bayer Pharma Aktiengesellschaft Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung

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CN111433204A (zh) 2020-07-17
US20220234996A1 (en) 2022-07-28
US11332435B2 (en) 2022-05-17
JP2021504396A (ja) 2021-02-15
BR112020010837A2 (pt) 2020-11-10
CA3083986A1 (en) 2019-06-06
AU2018374452A1 (en) 2020-06-04
WO2019105881A1 (de) 2019-06-06
JOP20200133A1 (ar) 2020-05-31
CL2020001420A1 (es) 2020-10-23
CO2020006789A2 (es) 2020-08-31
EP3717480A1 (de) 2020-10-07
SG11202004577VA (en) 2020-06-29
TW201936568A (zh) 2019-09-16
US20210179541A1 (en) 2021-06-17
UY37987A (es) 2019-06-28
KR20200094762A (ko) 2020-08-07
RU2020121714A (ru) 2022-01-04
PE20211391A1 (es) 2021-07-27
MX2022012998A (es) 2022-11-08
MX2020005646A (es) 2020-08-20
IL274715A (en) 2020-07-30

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