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AR076755A1 - Compuestos carboxamida y su uso como inhibidores de calpaina - Google Patents

Compuestos carboxamida y su uso como inhibidores de calpaina

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Publication number
AR076755A1
AR076755A1 ARP100101566A AR076755A1 AR 076755 A1 AR076755 A1 AR 076755A1 AR P100101566 A ARP100101566 A AR P100101566A AR 076755 A1 AR076755 A1 AR 076755A1
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AR
Argentina
Prior art keywords
alkyl
aryl
cycloalkyl
radicals
substituents
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English (en)
Inventor
Andreas Kling
Helmut Mack
Moeller
Jantos
Wilfried Hornberger
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Abbott Gmbh & Co Kg
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42470549&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR076755(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbott Gmbh & Co Kg filed Critical Abbott Gmbh & Co Kg
Publication of AR076755A1 publication Critical patent/AR076755A1/es

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Abstract

Su uso para la fabricacion de un medicamento. Los compuestos carboxamida son inhibidores de calpaína (cisteína proteasas dependientes del calcio). Por lo tanto, la presente también se refiere al uso de dichos compuestos carboxamida para tratar un trastorno asociado con una alta actividad de calpaína. Reivindicacion 1: Un compuesto de carboxamida caracterizado porque es de la formula (1) en donde - - - - - indica una union simple o, si R4 se encuentra ausente, indica una union doble; R1 es hidrogeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, donde los ultimos 3 radiales 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 además puede tener 1, 2, 3 o 4 radicales R1b, arilo, hetarilo, aril-alquilo C1-6, aril-alquenilo C2-6, hetaril-alquilo C1-4 o hetaril-alquenilo C2-6, donde los grupos arilo y hetarilo en los ultimos 6 radicales mencionados pueden no estar sustituidos o llevar 1, 2, 3 o 4 radicales R1c idénticos o diferentes; 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, -NRa2SO2Ra4, NRa2-CO-Ra5, SO2-Ra4 y NRa6Ra7; R1b se selecciona en forma independiente entre si entre OH, SH, COOH, CN, OCH2COOH, halogeno, fenilo que tiene opcionalmente 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 los radicales R1b pueden formar juntos un grupo alquileno C1-4, o 2 radicales R1b unidos a átomos de C de cicloalquilo adyacentes también pueden formar 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, y donde 1 o 2 grupos CH2 en la porcion cicloalquilo pueden reemplazarse por O, NH o S, arilo, hetarilo, O-arilo, O-CH2-arilo, donde los ultimos tres radicales mencionados no están sustituidos en la porcion arilo o pueden llevar 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)q-NRc6Rc7 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-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos 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 sí H, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyente 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-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los 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 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-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos 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 opcionalmente sustituido de entre 3 y 7 miembros que puede tener opcionalmente 1, 2 o 3 heteroátomos adicionales iguales o diferentes seleccionados entre 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-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, y 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-alquilo C1-4, hetaril-alquilo C1-4, CO-arilo, CO-hetarilo, CO-(aril-alquilo C1-4), CO-(hetaril-alquilo C1-4), CO-O-arilo, CO-O-hetarilo, CO-O-(aril-alquilo C1-4), CO-O-(hetaril-alquilo C1-4), SO2-arilo, SO2-hetarilo, SO2-(aril-alquilo C1-4) o SO2-(hetaril-alquilo C1-4), donde los grupos arilo y hetarilo en los ultimos 18 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes R1d, y 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 C1-4, arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos 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 opcionalmente sustituido de entre 3 y 7 miembros que puede tener opcionalmente 1, 2 o 3 heteroátomos adicionales iguales o diferentes seleccionados entre O, N y S como miembros del anillo, o dos radicales R1b o R1c unidos a átomos de C adyacentes forman junto con los átomos de C a los cuales están unidos un carbociclo opcionalmente sustituido de 4, 5, 6 o 7 miembros o un heterociclo opcionalmente sustituido que tiene 1, 2 o 3 heteroátomos iguales o diferentes seleccionados entre 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 o dos radicales R1d unidos a átomos de carbono adyacentes pueden formar juntos una porcion -O-Alk''-O-, donde Alk'' es alcandiilo C1-2 lineal, que no está sustituido o donde 1 o 2 átomos de hidrogeno pueden reemplazarse por fluor, cloro o metilo; R2 es cicloalquilo C3-7, donde un grupo CH2 en la porcion cicloalquilo 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 Ra2, arilo, o hetarilo, donde los grupos arilo y hetarilo pueden no estar sustituidos o llevar 1, 2, 3 o 4 radicales R2b iguales o diferentes, donde R2a tiene uno de los significados indicados para R1b, y R2b tiene uno de los significados indicados para R1c; R3a y R3b son en forma independiente entre sí hidroxi o alcoxi C1-4, o junto con el átomo de carbono al cual están unidos son C=O o C=NR3; o R3a y R3b juntos forman una porcion S-Alk-S, O-Alk-S o O-Alk-O, donde Alk es alcandiilo C2-5 lineal, que puede no estar sustituido o estar sustituido con 1, 2, 3 o 4 radicales seleccionados entre alquilo C1-4 o halogeno; R3 es H, alquilo C1-6, alcoxi C1-6, alquenilo C2-6, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-4, alqueniloxi C2-6, cicloalquiloxi C3-6 o cicloalquil C3-6-alquiloxi C1-4; R4 se encuentra ausente o indica hidrogeno; A es C=O, S(=O) o S(=O)2; Q es una union simple o una porcion Alk'-Z, donde Z está unido a R2 y se selecciona entre una union simple, O, S, S(=O), S(=O)2 y NRq, donde Rq se selecciona entre hidrogeno, alquilo C1-4 y haloalquilo C1-4; Alk' es alcandiilo C1-3 lineal, donde 1, 2 o 3 átomos de hidrogeno pueden reemplazarse por alquilo C1-4, haloalquilo C1-4 o halogeno; X es hidrogeno o un radical de las formulas C(=O)-O-Rx1, C(=O)-NRx2Rx3, C(=O)-N(Rx4)-alquilen C1-6-NRx2Rx3 o C(=O)N(Rx4)NRx2Rx3, en donde Rx1 es hidrogeno, alquilo C1-6, haloalquilo C1-6, alquilo C1-6 que tiene 1, 2 o 3 sustituyentes Rxa, 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, donde los grupos alquilo, alquenilo, alcoxi, alquinilo, cicloalquilo, heterocicloalquilo en los ultimos 6 radicales mencionados no están sustituidos o tienen 1, 2 o 3 sustituyentes Rxa, o arilo, aril-alquilo C1-4, hetarilo o hetaril-alquilo C1-4, donde los grupos arilo y hetarilo en los ultimos 4 radicales mencionados no
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Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9051304B2 (en) * 2009-12-22 2015-06-09 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors V
CN103748070B (zh) 2011-05-31 2015-06-24 施万生物制药研发Ip有限责任公司 脑啡肽酶抑制剂
ES2653215T3 (es) 2011-05-31 2018-02-06 Theravance Biopharma R&D Ip, Llc Inhibidores de neprilisina
WO2012166390A1 (en) * 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
ITMI20121668A1 (it) * 2012-10-05 2014-04-06 Dipharma Francis Srl Sintesi di un intermedio di un composto antivirale
CN104458709A (zh) * 2013-09-12 2015-03-25 中国药科大学 一种筛选钙激活中性蛋白酶-1抑制剂高通量筛选方法
DE102014110782A1 (de) * 2014-07-30 2016-02-04 Eberhard Karls Universität Tübingen Medizinische Fakultät Herstellung von Pyrrolidinderivaten
US10590084B2 (en) 2016-03-09 2020-03-17 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
WO2018050631A1 (en) * 2016-09-13 2018-03-22 Haplogen Gmbh Antiviral compounds
CA3038331A1 (en) 2016-09-28 2018-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
JP2025507472A (ja) * 2022-03-01 2025-03-21 ウエストバック バイオファーマ カンパニー リミテッド ケトアミド系誘導体及びその製薬における使用

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL9001562A (nl) 1990-07-09 1992-02-03 Keystone Int Meet- en regelafsluiter.
US5444042A (en) 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
MY115155A (en) 1993-09-09 2003-04-30 Upjohn Co Substituted oxazine and thiazine oxazolidinone antimicrobials.
WO1996041638A1 (en) 1995-06-13 1996-12-27 Sanofi Winthrop, Inc. Calpain inhibitors for the treatment of neurodegenerative diseases
AU6964096A (en) 1995-09-15 1997-04-01 Pharmacia & Upjohn Company Aminoaryl oxazolidinone n-oxides
DE69628050T2 (de) 1995-10-25 2004-04-01 Senju Pharmaceutical Co., Ltd. Angiogenese Hemmer
DE19642591A1 (de) * 1996-10-15 1998-04-16 Basf Ag Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung
WO1998021186A1 (en) * 1996-11-13 1998-05-22 Cephalon, Inc. Benzothiazo and related heterocyclic group-containing cysteine and serine protease inhibitors
DE19650975A1 (de) 1996-12-09 1998-06-10 Basf Ag Neue heterocyclisch substituierte Benzamide und deren Anwendung
TR199901305T2 (xx) 1996-12-11 1999-08-23 Basf Aktiengesellschaft Calpain-�nleyicileri olarak ketonbenzamidler
US6083944A (en) 1997-10-07 2000-07-04 Cephalon, Inc. Quinoline-containing α-ketoamide cysteine and serine protease inhibitors
US20030220234A1 (en) 1998-11-02 2003-11-27 Selvaraj Naicker Deuterated cyclosporine analogs and their use as immunodulating agents
HRP20000788A2 (en) 1998-04-20 2001-06-30 Basf Ag Novel heterocyclically substituted amides with cysteine protease-inhibiting effect
DE19818614A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Amide, deren Herstellung und Anwendung
BR9909774A (pt) 1998-04-20 2000-12-19 Basf Ag Amida, uso de amidas, e, preparação farmacêutica para uso oral, parenteral ou intraperitoneal
DE19817459A1 (de) * 1998-04-20 1999-10-21 Basf Ag Neue heterozyklische substituierte Amide, Herstellung und Anwendung
EP1082308B1 (de) 1998-04-20 2009-04-01 Abbott GmbH & Co. KG Heterocyclisch substituierte amide als calpainhemmer
ATE524440T1 (de) 1998-05-25 2011-09-15 Abbott Gmbh & Co Kg Heterocyclische substituierte amide, deren herstellung und anwendung
GB9918037D0 (en) 1999-07-30 1999-09-29 Biochemie Gmbh Organic compounds
JP2004509083A (ja) * 2000-09-01 2004-03-25 スミスクライン・ビーチャム・コーポレイション 治療方法
DE10114762A1 (de) 2001-03-26 2002-10-02 Knoll Gmbh Verwendung von Cysteinprotease-Inhibitoren
ES2294494T3 (es) 2004-04-19 2008-04-01 Symed Labs Limited Un nuevo procedimiento para la preparacion de linezolid y compuestos relacionados.
ES2243131B1 (es) 2004-05-07 2007-02-01 Consejo Sup. Investig. Cientificas Tiamidas derivadas de bifenilo como inhibidores de calpaina.
DE602004020812D1 (de) 2004-07-20 2009-06-04 Symed Labs Ltd Neue zwischenprodukte für linezolid und verwandte verbindungen
EP1804823A4 (en) 2004-09-29 2010-06-09 Amr Technology Inc NEW CYCLOSPORIN ANALOGUE AND ITS PHARMACEUTICAL APPLICATIONS
TW200716636A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
WO2007018589A2 (en) 2005-07-28 2007-02-15 Bio-Rad Laboratories, Inc. Separation of proteins based on isoelectric point using solid-phase buffers
RU2441020C2 (ru) 2005-08-02 2012-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серинпротеазы
US7514068B2 (en) 2005-09-14 2009-04-07 Concert Pharmaceuticals Inc. Biphenyl-pyrazolecarboxamide compounds
EP1798232A1 (en) 2005-12-08 2007-06-20 Hybrigenics S.A. Inhibitors of cysteine proteases, the pharmaceutical compositions thereof and their therapeutic applications
US20090062302A1 (en) 2006-01-24 2009-03-05 Buser-Doepner Carolyn A Jak2 Tyrosine Kinase Inhibition
US20080015933A1 (en) 2006-07-14 2008-01-17 Vulano Group, Inc. System for creating dynamically personalized media
US8796267B2 (en) 2006-10-23 2014-08-05 Concert Pharmaceuticals, Inc. Oxazolidinone derivatives and methods of use
CN101616908B (zh) 2006-12-29 2014-09-10 Abbvie德国有限责任两合公司 羧酰胺化合物及它们作为钙蛋白酶抑制剂的用途
KR101222412B1 (ko) 2007-02-15 2013-01-15 에프. 호프만-라 로슈 아게 Ｔａａｒ1 리간드로서의 2-아미노옥사졸린
EP2125113A2 (en) 2007-02-26 2009-12-02 Achillion Pharmaceuticals, Inc. Tertiary amine substituted peptides useful as inhibitors of hcv replication
AU2008242703B2 (en) 2007-04-19 2011-08-18 Concert Pharmaceuticals Inc. Deuterated morpholinyl compounds
US7531685B2 (en) 2007-06-01 2009-05-12 Protia, Llc Deuterium-enriched oxybutynin
US20090131485A1 (en) 2007-09-10 2009-05-21 Concert Pharmaceuticals, Inc. Deuterated pirfenidone
US20090118238A1 (en) 2007-09-17 2009-05-07 Protia, Llc Deuterium-enriched alendronate
US20090082471A1 (en) 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched fingolimod
US20090088416A1 (en) 2007-09-26 2009-04-02 Protia, Llc Deuterium-enriched lapaquistat
JP2010540635A (ja) 2007-10-02 2010-12-24 コンサート ファーマシューティカルズ インコーポレイテッド ピリミジンジオン誘導体
WO2009051782A1 (en) 2007-10-18 2009-04-23 Concert Pharmaceuticals Inc. Deuterated etravirine
US20090105338A1 (en) 2007-10-18 2009-04-23 Protia, Llc Deuterium-enriched gabexate mesylate
US20090131363A1 (en) 2007-10-26 2009-05-21 Harbeson Scott L Deuterated darunavir
US8598211B2 (en) * 2009-12-22 2013-12-03 Abbvie Inc. Carboxamide compounds and their use as calpain inhibitors IV

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WO2010128102A1 (en) 2010-11-11

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