AR079015A1 - Acidos 3-fenilpropionicos sustituidos, metodo de preparacion y uso de los mismos - Google Patents
Acidos 3-fenilpropionicos sustituidos, metodo de preparacion y uso de los mismosInfo
- Publication number
- AR079015A1 AR079015A1 ARP100103934A ARP100103934A AR079015A1 AR 079015 A1 AR079015 A1 AR 079015A1 AR P100103934 A ARP100103934 A AR P100103934A AR P100103934 A ARP100103934 A AR P100103934A AR 079015 A1 AR079015 A1 AR 079015A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- formula
- represents hydrogen
- trifluoromethyl
- fluorine
- Prior art date
Links
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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- A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
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- C07C205/35—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
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- C07C205/38—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton to carbon atoms of the same non-condensed six-membered aromatic ring or to carbon atoms of six-membered aromatic rings being part of the same condensed ring system the oxygen atom of at least one of the etherified hydroxy groups being further bound to a carbon atom of a six-membered aromatic ring, e.g. nitrodiphenyl ethers
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- 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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Abstract
Reivindicacion 1: Compuesto de formula (1) en la que R1A representa hidrogeno, fluor, metilo, trifluorometilo, etilo, 1,1-difluoroetilo, 2,2,2-trifluoroetilo, n-propilo, ciclopropilo o ciclobutilo, R1B representa hidrogeno o metilo, R2A representa hidrogeno, metilo, trifluorometilo, etilo, 1,1-difluoroetilo, 2,2,2-trifluoroetilo o n-propilo, R2B representa hidrogeno o metilo, o R1A y R2A están enlazados entre sí y forman, junto con los átomos de carbono a los que están unidos, un anillo de ciclopropilo de formula (2) en la que R1B y R2B tienen los significados anteriormente dados, o R2A y R2B están enlazados entre sí y forman, junto con el átomo de carbono al que están unidos, un grupo cíclico de formulas (3) en las que n significa el numero 1, 2 o 3, R3 representa hidrogeno, fluor, metilo o trifluorometilo, R4 representa hidrogeno, fluor, cloro, ciano, metilo, trifluorometilo o etilo, R5A representa metilo, trifluorometilo o etilo, R5B representa trifluorometilo, o R5A y R5B están enlazados entre sí y forman, junto con el átomo de carbono al que están unidos, un anillo de cicloalquilo sustituido con difluor de formulas (4), R6 representa hidrogeno, fluor, cloro, bromo, ciano, alquilo C1-4, alquenilo C2-4, ciclopropilo o ciclobutilo, en los que alquilo C1-C4 y alquenilo C2-4 pueden estar sustituidos hasta tres veces con fluor y ciclopropilo y ciclobutilo hasta dos veces con fluor, y R7 representa hidrogeno, fluor, cloro, ciano, metilo, trifluorometilo, etilo, metoxilo o trifluorometoxilo, así como sus sales, solvatos y solvatos de las sales. Reivindicacion 4: Procedimiento para la preparacion de un compuesto de formula (1) como se define en las reivindicaciones 1 a 3, caracterizado porque se acopla un ácido carboxílico de formula (5) en la que R5A, R5B, R6 y R7 tienen los significados dados en las reivindicaciones 1 a 3, en un disolvente inerte con ayuda de un agente de condensacion o a través de la etapa intermedia del correspondiente cloruro de ácido carboxílico en presencia de una base con una amina de formula (6) en la que R1A, R1B, R2A, R2B, R3 y R4 tienen los significados dados en las reivindicaciones 1 a 3, T1 representa alquilo C1-4 o bencilo, hasta una amida de ácido carboxílico de formula (7) en la que R1A, R1B, R2A, R2B, R3, R4, R5A, R5B, R6, R7 y T1 tienen los significados anteriormente dados, y a continuacion se escinde el resto éster T1 mediante solvolisis básica o ácida o, en el caso de que T1 represente bencilo, también mediante hidrogenolisis con obtencion del ácido carboxílico de formula (1) y eventualmente los compuestos de formula (1) se separan segun procedimientos conocidos por el experto en sus enantiomeros y/o diastereomeros y/o se hacen reaccionar con los correspondientes (i) disolventes y/o (ii) bases hasta sus solvatos, sales y/o solvatos de las sales. Reivindicacion 7: Uso de un compuesto como se define en una de las reivindicaciones 1 a 3, para la preparacion de un medicamento para el tratamiento y/o la prevencion de insuficiencia cardíaca, angina de pecho, hipertension, hipertension pulmonar, isquemias, enfermedades vasculares, alteraciones de la microcirculacion, enfermedades tromboembolicas y arteriosclerosis.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102009046115A DE102009046115A1 (de) | 2009-10-28 | 2009-10-28 | Substituierte 3-Phenylpropansäuren und ihre Verwendung |
Publications (1)
Publication Number | Publication Date |
---|---|
AR079015A1 true AR079015A1 (es) | 2011-12-21 |
Family
ID=43232960
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100103934A AR079015A1 (es) | 2009-10-28 | 2010-10-26 | Acidos 3-fenilpropionicos sustituidos, metodo de preparacion y uso de los mismos |
Country Status (23)
Country | Link |
---|---|
US (2) | US20110130445A1 (es) |
EP (1) | EP2493845B1 (es) |
JP (1) | JP5801312B2 (es) |
KR (1) | KR20120101411A (es) |
CN (1) | CN102712577B (es) |
AR (1) | AR079015A1 (es) |
AU (1) | AU2010311678B2 (es) |
BR (1) | BR112012010057A2 (es) |
CA (1) | CA2777152C (es) |
DE (1) | DE102009046115A1 (es) |
DK (1) | DK2493845T3 (es) |
ES (1) | ES2446970T3 (es) |
HK (1) | HK1177195A1 (es) |
HR (1) | HRP20140270T1 (es) |
IL (1) | IL218989A (es) |
MX (1) | MX2012004951A (es) |
PL (1) | PL2493845T3 (es) |
PT (1) | PT2493845E (es) |
RU (1) | RU2553263C2 (es) |
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DE102009046115A1 (de) | 2009-10-28 | 2011-09-08 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 3-Phenylpropansäuren und ihre Verwendung |
EP2549875B1 (en) | 2010-03-25 | 2015-05-13 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
WO2011149921A1 (en) | 2010-05-27 | 2011-12-01 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
EP2632551B1 (en) | 2010-10-28 | 2016-07-06 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
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DE102011007272A1 (de) * | 2011-04-13 | 2012-10-18 | Bayer Pharma Aktiengesellschaft | Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung |
EP2820005A1 (en) * | 2012-02-28 | 2015-01-07 | Piramal Enterprises Limited | Phenyl alkanoic acid derivatives as gpr agonists |
DE102012208530A1 (de) | 2012-05-22 | 2013-11-28 | Bayer Pharma AG | Substituierte Piperidinoacetamide und ihre Verwendung |
TWI594975B (zh) | 2013-04-24 | 2017-08-11 | 第一三共股份有限公司 | 二羧酸化合物 |
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US20170327457A1 (en) * | 2014-09-09 | 2017-11-16 | Bristol-Myers Squibb Company | Phenyl-(aza)cycloalkyl carboxylic acid gpr120 modulators |
CA2962724C (en) | 2014-09-26 | 2019-11-19 | Daiichi Sankyo Company, Limited | Salt of dicarboxylic acid compound |
PL3207023T3 (pl) | 2014-10-14 | 2020-01-31 | Syngenta Participations Ag | Sposób wytwarzania halo-podstawionych benzenów |
MY182134A (en) * | 2014-12-18 | 2021-01-18 | Bayer Pharma AG | Substituted pyridyl-cycloalkyl-carboxylic acids, compositions containing them and uses thereof |
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SI3325013T2 (sl) | 2015-07-23 | 2023-11-30 | Bayer Pharma Aktiengesellschaft | Stimulatorji/aktivatorji topne gvanilat ciklaze v kombinaciji z zaviralcem NEP in/ali antagonistom angiotenzina II in njihova uporaba |
CN109890379A (zh) | 2016-10-11 | 2019-06-14 | 拜耳制药股份公司 | 包含sGC活化剂和盐皮质激素受体拮抗剂的组合产品 |
CN106565637A (zh) * | 2016-11-04 | 2017-04-19 | 天津雅奥科技发展有限公司 | 一种3‑氧杂环丁烷乙酸的合成方法 |
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MX2020005646A (es) * | 2017-12-01 | 2020-08-20 | Bayer Pharma AG | Procedimiento para la preparacion de (3s)-3-(4-cloro-3-{[(2s,3r)-2 -(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-aci do ciclo-propilpropanoico y su forma cristalina para uso como principio activo farmaceutico. |
EP3498298A1 (en) | 2017-12-15 | 2019-06-19 | Bayer AG | The use of sgc stimulators and sgc activators alone or in combination with pde5 inhibitors for the treatment of bone disorders including osteogenesis imperfecta (oi) |
CN112055584A (zh) | 2018-04-30 | 2020-12-08 | 拜耳公司 | sGC活化剂和sGC刺激剂用于治疗认知障碍的用途 |
SG11202011018PA (en) | 2018-05-15 | 2020-12-30 | Bayer Ag | 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization |
EP3574905A1 (en) | 2018-05-30 | 2019-12-04 | Adverio Pharma GmbH | Method of identifying a subgroup of patients suffering from dcssc which benefits from a treatment with sgc stimulators and sgc activators in a higher degree than a control group |
US10905667B2 (en) | 2018-07-24 | 2021-02-02 | Bayer Pharma Aktiengesellschaft | Orally administrable modified-release pharmaceutical dosage form |
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WO2020164008A1 (en) | 2019-02-13 | 2020-08-20 | Bayer Aktiengesellschaft | Process for the preparation of porous microparticles |
CN117337278A (zh) * | 2021-05-14 | 2024-01-02 | 南京明德新药研发有限公司 | 烷基羧酸化合物及其应用 |
TW202342420A (zh) * | 2022-02-18 | 2023-11-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 羧酸類化合物、其製備方法及其在醫藥上的應用 |
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CN115850102A (zh) * | 2022-12-29 | 2023-03-28 | 浙江工业大学 | 一种奥司他韦的制备方法 |
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- 2010-10-21 MX MX2012004951A patent/MX2012004951A/es active IP Right Grant
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US9018414B2 (en) | 2015-04-28 |
JP5801312B2 (ja) | 2015-10-28 |
MX2012004951A (es) | 2012-06-13 |
HRP20140270T1 (hr) | 2014-04-25 |
US20140142069A1 (en) | 2014-05-22 |
UY32970A (es) | 2011-05-31 |
CN102712577A (zh) | 2012-10-03 |
KR20120101411A (ko) | 2012-09-13 |
ES2446970T3 (es) | 2014-03-11 |
BR112012010057A2 (pt) | 2019-09-24 |
IL218989A (en) | 2015-10-29 |
TW201127373A (en) | 2011-08-16 |
US20110130445A1 (en) | 2011-06-02 |
AU2010311678B2 (en) | 2015-09-03 |
CA2777152A1 (en) | 2011-05-05 |
RU2012121577A (ru) | 2013-12-10 |
ZA201202465B (en) | 2013-08-28 |
WO2011051165A1 (de) | 2011-05-05 |
RU2553263C2 (ru) | 2015-06-10 |
HK1177195A1 (en) | 2013-08-16 |
PT2493845E (pt) | 2014-02-24 |
EP2493845A1 (de) | 2012-09-05 |
JP2013509369A (ja) | 2013-03-14 |
TWI487519B (zh) | 2015-06-11 |
CA2777152C (en) | 2017-09-19 |
IL218989A0 (en) | 2012-06-28 |
AU2010311678A1 (en) | 2012-05-17 |
CN102712577B (zh) | 2014-10-15 |
EP2493845B1 (de) | 2013-12-25 |
DK2493845T3 (en) | 2014-03-24 |
DE102009046115A1 (de) | 2011-09-08 |
PL2493845T3 (pl) | 2014-05-30 |
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