AR079668A1 - Compuestos carboxamida y su uso como inhibidores de calpaina - Google Patents
Compuestos carboxamida y su uso como inhibidores de calpainaInfo
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- AR079668A1 AR079668A1 ARP100104834A ARP100104834A AR079668A1 AR 079668 A1 AR079668 A1 AR 079668A1 AR P100104834 A ARP100104834 A AR P100104834A AR P100104834 A ARP100104834 A AR P100104834A AR 079668 A1 AR079668 A1 AR 079668A1
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Abstract
Compuestos carboxamida y su uso para la elaboracion de un medicamento. Los compuestos carboxamida son inhibidores de calpaína (cisteína proteasas dependientes del calcio). Por lo tanto, también se refiere al uso de dichos compuestos carboxamida para tratar un trastorno asociado con una actividad elevada de calpaína. Reivindicacion 1: Un compuesto carboxamida caracterizado porque es de la formula (1) en donde R1 es alquilo C1-10, alquenilo C2-10, alquinilo C2-10, donde los ultimos 3 radicales mencionados pueden estar parcial o totalmente halogenados y/o tener 1, 2 o 3 sustituyentes R1a, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, donde un grupo CH2 en la porcion cicloalquilo de los ultimos dos radicales mencionados puede reemplazarse por O, NH, o S, o dos átomos de C adyacentes pueden formar una union doble, donde la porcion cicloalquilo puede tener además 1, 2, 3 o 4 radicales R1b, arilo, hetarilo, aril-C1-6-alquilo, aril-C2-6-alquenilo, hetaril-C1-4-alquilo o hetaril-C2-6-alquenilo, donde arilo y hetarilo en los ultimos 6 radicales mencionados puede no estar sustituido o tener 1, 2, 3 o 4 radicales idénticos o diferentes R1c; donde R1a se selecciona en forma independiente entre sí entre OH, SH, COOH, CN, OCH2COOH, alcoxi C1-6, haloalcoxi C1-6, cicloalquiloxi C3-7, alquiltio C1-6, haloalquiltio C1-6, COORa1, CONRa2Ra3, SO2NRa2Ra3, NRa2-SO2-Ra4, NRa2-CO-Ra5, SO2-Ra4 y NRa6Ra7, R1b se selecciona en forma independiente entre sí entre OH, SH, COOH, CN, OCH2COOH, halogeno, fenilo que opcionalmente tiene 1, 2 o 3 sustituyentes R1d, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, donde las porciones alquilo en los ultimos 3 sustituyentes mencionados pueden estar parcial o totalmente halogenadas y/o tener 1, 2 o 3 sustituyentes R1a, COORb1, CONRb2Rb3, SO2NRb2Rb3, NRb2-SO2-Rb4, NRb2-CO-Rb5, SO2-Rb4 y NRb6Rb7, además dos radicales R1b pueden formar juntos un grupo alquileno C1-4, o 2 radicales R1b unidos a átomos de C adyacentes de cicloalquilo pueden formar también junto con los átomos de carbono a los cuales están unidos un anillo benceno, R1c se selecciona en forma independiente entre sí entre OH, SH, halogeno, NO2, NH2, CN, COOH, OCH2COOH, alquilo C1-6, alcoxi C1-6, alcoxi C1-6-alquilo C1-4, alquiltio C1-6, donde las porciones alquilo en los ultimos 4 sustituyentes mencionados pueden estar parcial o totalmente halogenadas y/o tener 1, 2 o 3 sustituyentes R1a, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, cicloalquiloxi C3-7, donde la porcion cicloalquilo de los ultimos tres radicales mencionados puede tener 1, 2, 3 o 4 radicales R1b, arilo, hetarilo, O-arilo, O-CH2-arilo, donde los ultimos tres radicales mencionados no están sustituidos en la porcion arilo o pueden tener 1, 2, 3 o 4 radicales R1d, COORc1, CONRc2Rc3, SO2NRc2Rc3, NRc2-SO2-Rc4 NRc2-CO-Rc5, SO2-Rc4, -(CH2)pNRc6Rc7 con p = 0, 1, 2, 3, 4, 5 o 6 y O-(CH2)qNRc6Rc7 con q = 2, 3, 4, 5 o 6; donde Ra1, Rb1 y Rc1 son en forma independiente entre sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-C1-4-alquilo, hetarilo o hetaril-C1-4-alquilo, donde arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, Ra2, Rb2 y Rc2 son en forma independiente entre si H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-C1-4-alquilo, hetarilo o hetaril-C1-4-alquilo, donde arilo y hetarilo en tos ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, y Ra3, Rb3 y Rc3 son en forma independiente entre si H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-C1-4-alquilo, hetarilo o hetaril-C1-4-alquilo, donde arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1 2 o 3 sustituyentes R1d, o los dos radicales Ra2 y Ra3, o Rb2 y Rb3 o Rc2 y Rc3 forman junto con el átomo de N un heterociclo con nitrogeno de entre 3 y 7 miembros opcionalmente sustituido que puede tener opcionalmente 1, 2 o 3 heteroátomos adicionales idénticos o diferentes del grupo de O, N, S como miembros del anillo, Ra4, Rb4 y Rc4 son en forma independiente entre sí alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, arilo, aril-C1-4-alquilo, hetarilo o hetaril-C1-4-alquilo, donde arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, Ra5, Rb5 y Rc5 tienen en forma independiente entre sí uno de los significados mencionados para Ra1, Rb1 y Rc1; Ra6, Rb6 y Rc6 son en forma independiente entre sí H, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-4, CO-alquilo C1-6, CO-O-alquilo C1-6, SO2-alquilo C1-6, arilo, hetarilo, O-arilo, OCH2-arilo, aril-C1-4-alquilo, hetaril-C1-4-alquilo, CO-arilo, CO-hetarilo, CO-(aril-C1-4-alquilo), CO-(hetaril-C1-4-alquilo), CO-Oarilo, CO-O-hetarilo, CO-O-(aril-C1-4-alquilo), CO-O(hetaril-C1-4-alquilo), SO2-arilo, SO2-hetarilo, SO2-(aril-C1-4-alquilo) o SO2-(hetaril-C1-4-alquilo), donde arilo y hetarilo en los ultimos 18 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, Ra7, Rb7 y Rc7 son en forma independiente entre sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes R1a, o alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquil C3-7-alquilo C1-4, alcoxi C1-6-alquilo C1-6, arilo, aril-C1-4-alquilo, hetarilo o hetaril-C1-4-alquilo, donde arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, o los dos radicales Ra6 y Ra7, o Rb6 y Rb7 o Rc6 y Rc7 forman junto con el átomo de N un heterociclo con nitrogeno de entre 3 y 7 miembros opcionalmente sustituido que puede tener opcionalmente 1, 2 o 3 heteroátomos adicionales idénticos o diferentes del grupo de O, N y S como miembros del anillo, o dos radicales R1b o dos radicales R1c unidos a átomos de C adyacentes forman junto con los átomos de C a los cuales están unidos un carbociclo de 4, 5, 6 o 7 miembros opcionalmente sustituido o un heterociclo opcionalmente sustituido que tiene 1, 2 o 3 heteroátomos idénticos o diferentes del grupo de O, N y S como miembros del anillo; R1d se selecciona entre halogeno, OH, SH, NO2, COOH, C(O)NH2, CHO, CN, NH2, OCH2COOH, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquiltio C1-6, haloalquiltio C1-6, CO-alquilo C1-6, CO-O-alquilo C1-6, NH-alquilo C1-6, NHCHO, NH-C(O)alquilo C1-6, y SO2-alquilo C1-6; R2 es cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, donde un grupo CH2 en la porcion cicloalquilo de los ultimos dos radicales mencionados puede reemplazarse por O, NH, o S, o dos átomos de C adyacentes pueden formar una union doble, donde la porcion cicloalquilo puede tener adicionalmente 1, 2, 3 o 4 radicales R2b; arilo, O-arilo, O-CH2-arilo, hetarilo, aril-C1-6-alquilo, aril-C2-6-alquenilo, hetaril-C1-4-alquilo o hetaril-C2-6-alquenilo, donde arilo y hetarilo en los ultimos 8 radicales mencionados pueden no estar sustituidos o tener 1, 2, 3 o 4 radicales R2c idénticos o diferentes; donde R2b tiene uno de los significados indicados para R1b, y R2c tiene uno de los significados indicados para R1c; R3 es haloalquilo C1-4 o alquilo C1-6, alquenilo C3-6, alquinilo C3-6, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-2, heterocicloalquil C3-6-alquilo C1-2, alcoxi C1-4-alquilo C1-2, donde alquilo, alquenilo, alcoxi, alquinilo, cicloalquilo, heterocicloalquilo en los ultimos 7 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes Rxa, arilo, aril-C1-4-alquilo, hetarilo o hetaril-C1-4-alquilo, donde arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes Rxd, donde Rxa tiene uno de los significados indicados para R1a, y Rxd tiene uno de los significados indicados para R1d; R4 y R5 se seleccionan en forma independiente entre si entre halogeno, NH2, CN, CF3, CHF2, CH2F, O-CF3, O-CHF2, O-CH2F, COOH, OCH2COOH, alquilo C1-2, alcoxi C1-2, alcoxi C1-2-alquilo C1-2, alquiltio C1-2, CH2NRR', donde R y R' se seleccionan en forma independiente entre sí entre hidrogeno y alquilo C1-4; m es 0,1 o 2; n es 0,1 o 2; y los tautomeros del mismo, los hidratos del mismo, las prodrogas del mismo y las sales farmacéuticamente adecuadas del mismo.
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SG11201406345XA (en) | 2012-04-03 | 2014-11-27 | Abbvie Deutschland | Carboxamide compounds and their use as calpain inhibitors v |
JP6256771B2 (ja) | 2012-12-06 | 2018-01-10 | セルジーン クオンティセル リサーチ,インク. | ヒストンデメチラーゼ阻害剤 |
US10471038B2 (en) | 2015-10-08 | 2019-11-12 | Productive Aging Laboratory, Co., Ltd. | Inhibitor of muscle damage or muscle fatigue |
WO2017156071A1 (en) | 2016-03-09 | 2017-09-14 | Blade Therapeutics, Inc. | Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof |
EP3481835A4 (en) | 2016-07-05 | 2020-02-26 | Blade Therapeutics, Inc. | CALPAIN MODULATORS AND THEIR THERAPEUTIC USES |
KR20190063473A (ko) | 2016-09-28 | 2019-06-07 | 블레이드 테라퓨틱스, 인크. | 칼페인 조정자 및 그 치료학적 용도 |
RU2020130022A (ru) * | 2018-03-28 | 2022-05-04 | Блэйд Терапьютикс, Инк. | Модуляторы кальпаина и их терапевтическое применение |
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US4826835A (en) | 1985-10-23 | 1989-05-02 | Rorer Pharmaceutical Corporation | Pyridyl-pyridazinone and pyridyl-pyrazolinone compounds and their use in the treatment of congestive heart failure |
US4743608A (en) | 1986-07-15 | 1988-05-10 | Rorer Pharmaceutical Corporation | Pyridone-pyridyl-imidazolyl and triazolyl compounds and their use as cardiotonic agents |
PT708085E (pt) * | 1994-10-19 | 2002-11-29 | Novartis Ag | Eteres antivirais de isosteros de substrato de aspartato protease |
DE19642591A1 (de) | 1996-10-15 | 1998-04-16 | Basf Ag | Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung |
DE19650975A1 (de) | 1996-12-09 | 1998-06-10 | Basf Ag | Neue heterocyclisch substituierte Benzamide und deren Anwendung |
CN1245486A (zh) | 1996-12-11 | 2000-02-23 | Basf公司 | 用作钙蛋白酶抑制剂的酮苯甲酰胺 |
US6083944A (en) | 1997-10-07 | 2000-07-04 | Cephalon, Inc. | Quinoline-containing α-ketoamide cysteine and serine protease inhibitors |
SK13932000A3 (sk) | 1998-04-20 | 2001-05-10 | Basf Aktiengesellschaft | Heterocyklicky substituované amidy, ich príprava a použitie |
DE19818614A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue substituierte Amide, deren Herstellung und Anwendung |
CA2328720A1 (en) | 1998-04-20 | 1999-10-28 | Basf Aktiengesellschaft | Novel heterocyclically substituted amides with cysteine protease-inhibiting effect |
CA2328396C (en) | 1998-04-20 | 2009-02-10 | Basf Aktiengesellschaft | New substituted amides, their production and their use |
DE19817459A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue heterozyklische substituierte Amide, Herstellung und Anwendung |
US6482832B1 (en) | 1998-05-25 | 2002-11-19 | Abbott Laboratories | Heterocyclically substituted amides, their production and their use |
DE10114762A1 (de) | 2001-03-26 | 2002-10-02 | Knoll Gmbh | Verwendung von Cysteinprotease-Inhibitoren |
DK1482924T3 (da) * | 2002-03-05 | 2008-09-29 | Merck Frosst Canada Ltd | Cathepsin-cystein-protease-inhibotorer |
AU2006275413B2 (en) | 2005-08-02 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
KR20150090282A (ko) | 2006-12-29 | 2015-08-05 | 아비에 도이치란트 게엠베하 운트 콤파니 카게 | 카복스아미드 화합물 및 칼페인 억제제로서의 이의 용도 |
WO2008106130A2 (en) | 2007-02-26 | 2008-09-04 | Achillion Pharmaceuticals, Inc. | Tertiary amine substituted peptides useful as inhibitors of hcv replication |
TWI519530B (zh) | 2009-02-20 | 2016-02-01 | 艾伯維德國有限及兩合公司 | 羰醯胺化合物及其作為鈣蛋白酶(calpain)抑制劑之用途 |
US8236798B2 (en) | 2009-05-07 | 2012-08-07 | Abbott Gmbh & Co. Kg | Carboxamide compounds and their use as calpain inhibitors |
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EP2516393A1 (en) | 2012-10-31 |
ZA201204496B (en) | 2013-02-27 |
US20150252017A1 (en) | 2015-09-10 |
JP2013515039A (ja) | 2013-05-02 |
US9051304B2 (en) | 2015-06-09 |
CN102933548A (zh) | 2013-02-13 |
CN102933548B (zh) | 2015-03-11 |
ES2525149T3 (es) | 2014-12-18 |
US20110152265A1 (en) | 2011-06-23 |
WO2011076811A1 (en) | 2011-06-30 |
AU2010334915B2 (en) | 2014-11-06 |
BR112012015659A2 (pt) | 2016-05-24 |
UY33150A (es) | 2011-06-30 |
RU2012131276A (ru) | 2014-01-27 |
AU2010334915A1 (en) | 2012-06-21 |
SG181915A1 (en) | 2012-07-30 |
RU2567392C2 (ru) | 2015-11-10 |
JP5726207B2 (ja) | 2015-05-27 |
HK1176066A1 (en) | 2013-07-19 |
MX2012007323A (es) | 2012-11-06 |
EP2516393B1 (en) | 2014-10-29 |
NZ600342A (en) | 2013-12-20 |
TW201138771A (en) | 2011-11-16 |
KR20120102132A (ko) | 2012-09-17 |
IL220586A (en) | 2015-10-29 |
CA2783704A1 (en) | 2011-06-30 |
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