AR036875A1 - Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa - Google Patents
Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfaInfo
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- AR036875A1 AR036875A1 ARP020103499A ARP020103499A AR036875A1 AR 036875 A1 AR036875 A1 AR 036875A1 AR P020103499 A ARP020103499 A AR P020103499A AR P020103499 A ARP020103499 A AR P020103499A AR 036875 A1 AR036875 A1 AR 036875A1
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Abstract
Compuestos que son útiles como inhibidores de las metaloproteinasas de matriz (MMP), enzima que convierte el TNF-a TACE, agrecanasa o una combinación de los mismos, composiciones farmacéuticas que contienen el mismo y métodos para usar el mismo. Reivindicación 1: Un compuesto de la fórmula (1) o un estereoisómero o una forma de sal farmacéuticamente aceptable del mismo; en donde el anillo B es un anillo heterocíclico o carbocíclico no aromático de 4-7 miembros que comprende: átomos de carbono, 0-3 grupos carbonilo, 0-3 enlaces dobles, y 0-2 heteroátomos de anillo seleccionados de O, N, NR1, y S(O)p, con la condición de que el anillo B contiene otros enlaces diferentes a S-S, O-O, ó S-O; R1 se selecciona de Q, alquileno C1-6-Q, alquenileno C2-6-Q, alquinileno C2-6-Q, (CRaRa1)qO(CRaRa1)s-Q, (CRaRa1)qNRa(CRaRa1)s-Q, (CRaRa1)rC(O)(CRaRa1)s-Q, (CRaRa1)rC(O)-alquenileno C2-6-Q, (CRaRa1)rC(O)O(CRaRa1)s-Q, (CRaRa1)rOC(O)O(CRaRa1)s-Q, (CRaRa1)rOC(O)NRa(CRaRa1)s-Q, (CRaRa1)rC(O)NRaRa1, (CRaRa1)rC(O)NRa(CRaRa1)s-Q, (CRaRa1)qNRaC(O)(CRaRa1)s-Q, (CRaRa1)qNRaC(O)O(CRaRa1)s-Q, (CRaRa1)qNRaC(O)NRa(CRaRa1)s-Q, (CRaRa1)rS(O)p(CRaRa1)s-Q, (CRaRa1)rNRaSO2(CRaRa1)s-Q, y (CRaRa1)rSO2NRa(CRaRa1)s-Q; R2 se selecciona de Q, alquileno C1-6-Q, alquenileno C2-6-Q, alquinileno C2-6-Q, (CRaRa1)rO (CRaRa1)s-Q, (CRaRa1)rNRa(CRaRa1)s-Q, (CRaRa1)rC(O)(CRaRa1)s-Q, (CRaRa1)rC(O)-alquenileno C2-6-Q, (CRaRa1)rC(O)O(CRaRa1)s-Q, (CRaRa1)rC(O)NRaRa1, (CRaRa1)rC(O)NRa(CRaRa1)s-Q, (CRaRa1)rNRaC(O)(CRaRa1)s-Q, (CRaRa1)rNRaC(O)O(CRaRa1)s-Q, (CRaRa1)rNRaC(O)NRa(CRaRa1)s-Q, (CRaRa1)rS(O)p(CRaRa1)s-Q, y (CRaRa1)rSO2NRa(CRaRa1)s-Q; Q se selecciona de H, un carbociclo C3-6 sustituido con 0-3 Rd, y un heterociclo de 5-10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituidos con 0-3 Rd; R3 se selecciona de Q1, Cl, F, alquileno C1-6-Q1, alquenileno C2-6-Q1, alquinileno C2-6-Q1, (CRaRa1)rO(CRaRa1)s-Q1, (CRaRa1)rNRa(CRaRa1)s-Q1, (CRaRa1)rNRaC(O)(CRaRa1)s-Q1, (CRaRa1)rC(O)NRa(CRaRa1)s-Q1, (CRaRa1)rC(O)(CRaRa1)s-Q1, (CRaRa1)rC(O)O(CRaRa1)s-Q1, (CRaRa12)rS(O)p(CRaRa1)s-Q1, y (CRaRa1)rSO2NRa(CRaRa1)s-Q1; Q1 se selecciona de H, fenilo sustituido con 0-3 Rd, naftilo sustituido con 0-3 Rd y un heterociclo de 5-10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-3 Rd; Za se selecciona de del grupo de fórmulas (2); X es S, SO, SO2, O, ó NR14; Y es N ó CR17; R11 y R12, cada vez que se presentan, se seleccionan independientemente de H, Rc, alquilo C1-6 sustituido con 0-3 Rc1, carbociclo C3-10 sustituido con 0-3 Rc1, y heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y sustituido con 0-3 Rc1 ; R13 y R13a cada vez que se presentan, se seleccionan independientemente de H, Rc, alquilo C1-6 sustituido con 0-3 Rc1, carbociclo C3-10 sustituido con 0-3 Rc1, y un heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-3 Rc1; alternativamente, cuando R13 y R13a se enlazan a átomos de carbono adyacentes, junto con los átomos de carbono a los cuales se enlazan, forman un anillo de 5-7 miembros que consiste de: átomos de carbono, 0-2 grupos carbonilo, 0-3 dobles enlaces, y 0-2 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-2 Rc1; R14, cada vez que se presenta, se selecciona independientemente de H, alquilo C1-4, fenilo, y bencilo; R15 y R16, cada vez que se presentan, se seleccionan independientemente de H, Rc1, alquilo C1-6 sustituido con 0-3 Rc1, carbociclo C3-10 sustituido con 0-3 Rc1, y un heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-3 Rc1; alternativamente, cuando R15 y R16 se enlazan a los átomos de carbono adyacentes, junto con los átomos de carbono a los cuales se enlazan, forman un anillo de 5-7 miembros, que consiste de: átomos de carbono, 0-2 grupos carbonilo, 0-3 dobles enlaces, 0-2 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p; este anillo está sustituido con 0-2 Rc1; alternativamente, cuando R15 y R16 se enlazan al mismo átomo de carbono, junto con el átomo de carbono al cual están enlazados, forman un anillo de 3-7 miembros que consiste de: átomos de carbono, 0-2 grupos carbonilo, 0-3 dobles enlaces, y 0-2 heteroátomos seleccionados de N, O, y S(O)p; este anillo está sustituido con 0-2 Rc1; R17 se selecciona de H, Cl, F, y alquilo C1-4; Ra, cada vez que se presenta, se selecciona independientemente de H, alquilo C1-4, fenilo, y bencilo; Ra1, cada vez que se presenta, se selecciona independientemente de H y alquilo C1-4; Ra2, cada vez que se presenta, se selecciona independientemente de alquilo C1-4, fenilo, y bencilo; Rc, cada vez que se presenta, se selecciona independientemente de alquilo C1-6, ORa, Cl, F, Br, I, -CN, NO2, NRaRa1, C(O)Ra, C(O)ORa, C(O)NRaRa1, RaNC(O)NRaRa1, OC(O)NRaRa1, RaNC(O)ORa, S(O)2NRaRa1, NRaS(O)2Ra2, NRaS(O)2NRaRa1, OS(O)2NRaRa1, NRaS(O)2Ra2, S(O)pRa2, CF3, OCF3, CF2CF3, CH2F, y CHF2; Rc1, cada vez que se presenta, se selecciona independientemente de alquilo C1-6, ORa, Cl, F, Br, I, =O, -CN, NO2, NRaRa1, C(O)Ra, C(O)ORa, C(O)NRaRa1, RaNC(O)NRaRa1, OC(O)NRaRa1, RaNC(O)ORa, S(O)2NRaRa1, NRaS(O)2Ra2, NRaS(O)2NRaRa1, OS(O)2NRaRa1, NRaS(O)2Ra2, S(O)pRa2, CF3, OCF3, CF2CF3, CH2F, y CHF2; Rd, cada vez que se presenta, se selecciona independientemente de alquilo C1-6, ORa, Cl, F, Br, I, =O, -CN, NO2, NRaRa1, C(O)Ra, C(O)ORa, C(O)NRaRa1, RaNC(O)NRaRa1, OC(O)NRaRa1, RaNC(O)O, S(O)2NRaRa1, NRaS(O)2Ra2, NRaS(O)2NRaRa1, OS(O)2NRaRa1, NRaS(O)2Ra2, S(O)pRa2, CF3, OCF3, CF2CF3, carbociclo C3-10, y un heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p; p, cada vez que se presenta, se selecciona de 0, 1, y 2; q, cada vez que se presenta, se selecciona de 1, 2, 3, y 4; r, cada vez que se presenta, se selecciona de 0, 1, 2, 3, y 4; y, s, cada vez que se presenta, se selecciona de 0, 1, 2, 3, y 4.
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US32263001P | 2001-09-17 | 2001-09-17 |
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AR036875A1 true AR036875A1 (es) | 2004-10-13 |
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ARP020103499A AR036875A1 (es) | 2001-09-17 | 2002-09-17 | Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa |
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US (1) | US6740649B2 (es) |
EP (1) | EP1427408A4 (es) |
AR (1) | AR036875A1 (es) |
AU (1) | AU2002341715A1 (es) |
WO (1) | WO2003024899A2 (es) |
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GB0505969D0 (en) | 2005-03-23 | 2005-04-27 | Novartis Ag | Organic compounds |
JP5463034B2 (ja) * | 2005-05-20 | 2014-04-09 | アラントス・フアーマシユーテイカルズ・ホールデイング・インコーポレイテツド | ピリミジン若しくはトリアジン縮合二環式メタロプロテアーゼ阻害薬 |
US20070155738A1 (en) * | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
WO2007016597A2 (en) * | 2005-07-29 | 2007-02-08 | The Regents Of The University Of California | Targeting tnf-alpha converting enzyme (tace)-dependent growth factor shedding in cancer therapy |
PE20070335A1 (es) | 2005-08-30 | 2007-04-21 | Novartis Ag | Benzimidazoles sustituidos y metodos para su preparacion |
US8067415B2 (en) | 2005-11-01 | 2011-11-29 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of CCR2 |
US8067457B2 (en) * | 2005-11-01 | 2011-11-29 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of CCR2 |
US20100016289A1 (en) * | 2005-11-01 | 2010-01-21 | Kevin Sprott | Compounds Useful as Antagonists of CCR2 |
ES2430139T3 (es) | 2005-12-30 | 2013-11-19 | Novartis Ag | Compuestos de piperidina 3,5-sustituido como inhibidores de renina |
MX2008013238A (es) * | 2006-04-12 | 2008-10-21 | Merck & Co Inc | Antagonistas de los canales de calcio de tipo t de piridil amida. |
ES2541107T3 (es) | 2007-06-25 | 2015-07-16 | Novartis Ag | Derivados de N5-(2-etoxietil)-N3-(2-piridinil)-3,5-piperidindicarboxamida para su uso como inhibidores de renina |
ATE494926T1 (de) | 2008-03-25 | 2011-01-15 | Affectis Pharmaceuticals Ag | Neuartige p2x7r-antagonisten und ihre verwendung |
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WO2011054433A1 (en) * | 2009-11-07 | 2011-05-12 | Merck Patent Gmbh | Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors |
JPWO2012102297A1 (ja) * | 2011-01-26 | 2014-06-30 | 杏林製薬株式会社 | ピラゾロピリジン誘導体、またはその薬理学的に許容される塩 |
WO2012110190A1 (en) | 2011-02-17 | 2012-08-23 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
WO2012163792A1 (en) | 2011-05-27 | 2012-12-06 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
WO2012163456A1 (en) | 2011-05-27 | 2012-12-06 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
RS57919B1 (sr) * | 2011-12-16 | 2019-01-31 | Poseida Therapeutics Inc | Trpc4 modulatori za primenu u lečenju ili prevenciji bola |
RU2685234C1 (ru) * | 2013-12-09 | 2019-04-17 | Юсб Байофарма Спрл | Конденсированные бициклические гетероароматические производные в качестве модуляторов активности tnf |
GB201321739D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
BR112018001960A2 (pt) * | 2015-08-03 | 2018-09-18 | Bristol-Myers Squibb Company | compostos heterocíclicos úteis como moduladores de tnf alfa |
KR101772440B1 (ko) | 2015-08-31 | 2017-08-30 | 한국식품연구원 | 4-(4-하이드록시-4-메틸펜틸)-3-사이클로-헥센-1-카복스알데하이드를 포함하는 신생혈관형성 촉진용 조성물 |
DK3860998T3 (da) | 2018-10-05 | 2024-03-25 | Annapurna Bio Inc | Forbindelser og sammensætninger til behandlinger af tilstande, der er forbundet med APJ-receptoraktivitet |
CN109439606B (zh) * | 2018-11-14 | 2022-06-28 | 中国科学院青岛生物能源与过程研究所 | 一种提高间苯三酚产量的基因工程菌及其构建方法与应用 |
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US5210079A (en) | 1988-01-07 | 1993-05-11 | E. I. Du Pont De Nemours And Company | Treatment of chronic renal failure with imidazole angiotensin-II receptor antagonists |
DE4036706A1 (de) * | 1990-11-17 | 1992-05-21 | Hoechst Ag | Verfahren zur behandlung der cardialen sowie der vasculaeren hypertrophie und hyperplasie |
WO1995026188A1 (en) * | 1994-03-29 | 1995-10-05 | Merck & Co., Inc. | Treatment of atherosclerosis with angiotensin ii receptor blocking imidazoles |
GB9929979D0 (en) * | 1999-12-17 | 2000-02-09 | Darwin Discovery Ltd | Hydroxamic acid derivatives |
BR0109467A (pt) | 2000-03-17 | 2003-06-03 | Bristol Myers Squibb Pharma Co | Composto derivados de (beta)-aminoácidos cìclicos, composição farmacêutica, método de tratamento de condições ou doenças mediadas por mps, tnf, aggrecanase ou uma combinação destes em mamìferos e uso de composto |
EP1373199A4 (en) * | 2001-03-15 | 2004-04-07 | Bristol Myers Squibb Pharma Co | SPIROCYCLIC BETA-AMINOACID DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES AND THE CONVERSION ENZYME OF TNF-ALPHA (TAGE) |
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- 2002-09-16 WO PCT/US2002/029685 patent/WO2003024899A2/en not_active Application Discontinuation
- 2002-09-16 US US10/244,626 patent/US6740649B2/en not_active Expired - Lifetime
- 2002-09-16 AU AU2002341715A patent/AU2002341715A1/en not_active Abandoned
- 2002-09-16 EP EP02775865A patent/EP1427408A4/en not_active Withdrawn
- 2002-09-17 AR ARP020103499A patent/AR036875A1/es not_active Application Discontinuation
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US20030139388A1 (en) | 2003-07-24 |
EP1427408A2 (en) | 2004-06-16 |
EP1427408A4 (en) | 2005-10-26 |
AU2002341715A1 (en) | 2003-04-01 |
WO2003024899A3 (en) | 2003-11-27 |
US6740649B2 (en) | 2004-05-25 |
WO2003024899A2 (en) | 2003-03-27 |
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