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
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- 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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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 |
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DE102009046115A DE102009046115A1 (de) | 2009-10-28 | 2009-10-28 | Substituierte 3-Phenylpropansäuren und ihre Verwendung |
Publications (1)
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ARP100103934A AR079015A1 (es) | 2009-10-28 | 2010-10-26 | Acidos 3-fenilpropionicos sustituidos, metodo de preparacion y uso de los mismos |
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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) |
TW (1) | TWI487519B (es) |
UY (1) | UY32970A (es) |
WO (1) | WO2011051165A1 (es) |
ZA (1) | ZA201202465B (es) |
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DE102009046115A1 (de) | 2009-10-28 | 2011-09-08 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 3-Phenylpropansäuren und ihre Verwendung |
WO2011119518A1 (en) | 2010-03-25 | 2011-09-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
EP2575473B1 (en) | 2010-05-27 | 2016-01-20 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
WO2012058132A1 (en) | 2010-10-28 | 2012-05-03 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
AU2011340721A1 (en) | 2010-12-07 | 2013-06-20 | Bayer Intellectual Property Gmbh | Substituted 1-benzylcycloalkylcarboxlic acids and use thereof |
DE102011007272A1 (de) | 2011-04-13 | 2012-10-18 | Bayer Pharma Aktiengesellschaft | Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung |
NZ631569A (en) * | 2012-02-28 | 2016-10-28 | Piramal Entpr Ltd | 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 |
TW201625584A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
TW201625601A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 噻吩-2-基-吡啶-2-基-1h-吡唑-4-羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
TW201625586A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 環己烯-1-基-吡啶-2-基-1h-吡唑-4-羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
US9938228B2 (en) * | 2014-09-09 | 2018-04-10 | Boehringer Ingelheim International Gmbh | Process for the preparation of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione |
US20170327457A1 (en) | 2014-09-09 | 2017-11-16 | Bristol-Myers Squibb Company | Phenyl-(aza)cycloalkyl carboxylic acid gpr120 modulators |
BR112017005694A2 (pt) | 2014-09-26 | 2017-12-12 | Daiichi Sankyo Co Ltd | cristais de um sal, ou hidrato do mesmo, cristais de um trihidrato de sal dissódico, composição farmacêutica, uso dos cristais, e, método para prevenção ou tratamento de hiperfosfatemia. |
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AU2015367540B2 (en) * | 2014-12-18 | 2019-09-05 | Bayer Pharma Aktiengesellschaft | Substituted Pyridyl-cycloalkyl-carboxylic acids, compositions containing them and medical uses thereof |
EA201792346A1 (ru) | 2015-05-06 | 2018-05-31 | Байер Фарма Акциенгезельшафт | ПРИМЕНЕНИЕ sGC СТИМУЛЯТОРОВ, sGC АКТИВАТОРОВ, ОТДЕЛЬНО И В КОМБИНАЦИЯХ С PDE5 ИНГИБИТОРАМИ, ДЛЯ ЛЕЧЕНИЯ ПАЛЬЦЕВИДНЫХ ЯЗВ (DU), СОПУТСТВУЮЩИХ СИСТЕМНОМУ СКЛЕРОЗУ (SSc) |
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JP7237823B2 (ja) | 2016-10-11 | 2023-03-13 | バイエル ファーマ アクチエンゲゼルシャフト | Sgcアクチベーターとミネラルコルチコイド受容体アンタゴニストとを含む組合せ |
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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. |
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BR112020022340A2 (pt) | 2018-05-15 | 2021-02-02 | Bayer Aktiengesellschaft | benzamidas substituídas por 1,3-tiazol-2-il para o tratamento de doenças associadas com sensibilização de fibras nervosas |
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2009
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2010
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- 2010-10-21 MX MX2012004951A patent/MX2012004951A/es active IP Right Grant
- 2010-10-21 JP JP2012535750A patent/JP5801312B2/ja not_active Expired - Fee Related
- 2010-10-21 BR BR112012010057A patent/BR112012010057A2/pt not_active IP Right Cessation
- 2010-10-21 EP EP10768933.3A patent/EP2493845B1/de not_active Not-in-force
- 2010-10-21 PL PL10768933T patent/PL2493845T3/pl unknown
- 2010-10-21 KR KR1020127013589A patent/KR20120101411A/ko not_active Application Discontinuation
- 2010-10-21 AU AU2010311678A patent/AU2010311678B2/en not_active Ceased
- 2010-10-21 RU RU2012121577/04A patent/RU2553263C2/ru not_active IP Right Cessation
- 2010-10-21 CN CN201080059787.9A patent/CN102712577B/zh not_active Expired - Fee Related
- 2010-10-21 PT PT107689333T patent/PT2493845E/pt unknown
- 2010-10-21 DK DK10768933.3T patent/DK2493845T3/en active
- 2010-10-21 WO PCT/EP2010/065910 patent/WO2011051165A1/de active Application Filing
- 2010-10-21 CA CA2777152A patent/CA2777152C/en not_active Expired - Fee Related
- 2010-10-25 UY UY0001032970A patent/UY32970A/es not_active Application Discontinuation
- 2010-10-26 AR ARP100103934A patent/AR079015A1/es unknown
- 2010-10-27 TW TW099136615A patent/TWI487519B/zh not_active IP Right Cessation
- 2010-10-28 US US12/914,101 patent/US20110130445A1/en not_active Abandoned
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2012
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- 2012-04-04 ZA ZA2012/02465A patent/ZA201202465B/en unknown
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2013
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- 2013-10-03 US US14/045,630 patent/US9018414B2/en active Active
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2014
- 2014-03-21 HR HRP20140270AT patent/HRP20140270T1/hr unknown
Also Published As
Publication number | Publication date |
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AU2010311678A1 (en) | 2012-05-17 |
DE102009046115A1 (de) | 2011-09-08 |
RU2012121577A (ru) | 2013-12-10 |
US20140142069A1 (en) | 2014-05-22 |
ZA201202465B (en) | 2013-08-28 |
WO2011051165A1 (de) | 2011-05-05 |
IL218989A (en) | 2015-10-29 |
PT2493845E (pt) | 2014-02-24 |
HK1177195A1 (en) | 2013-08-16 |
US20110130445A1 (en) | 2011-06-02 |
RU2553263C2 (ru) | 2015-06-10 |
TWI487519B (zh) | 2015-06-11 |
EP2493845B1 (de) | 2013-12-25 |
AU2010311678B2 (en) | 2015-09-03 |
CN102712577B (zh) | 2014-10-15 |
KR20120101411A (ko) | 2012-09-13 |
BR112012010057A2 (pt) | 2019-09-24 |
IL218989A0 (en) | 2012-06-28 |
TW201127373A (en) | 2011-08-16 |
MX2012004951A (es) | 2012-06-13 |
EP2493845A1 (de) | 2012-09-05 |
CN102712577A (zh) | 2012-10-03 |
PL2493845T3 (pl) | 2014-05-30 |
CA2777152A1 (en) | 2011-05-05 |
ES2446970T3 (es) | 2014-03-11 |
HRP20140270T1 (hr) | 2014-04-25 |
US9018414B2 (en) | 2015-04-28 |
JP2013509369A (ja) | 2013-03-14 |
JP5801312B2 (ja) | 2015-10-28 |
CA2777152C (en) | 2017-09-19 |
DK2493845T3 (en) | 2014-03-24 |
UY32970A (es) | 2011-05-31 |
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