AR039695A1 - Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit) - Google Patents

Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit)

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Publication number
AR039695A1
AR039695A1 ARP030102149A ARP030102149A AR039695A1 AR 039695 A1 AR039695 A1 AR 039695A1 AR P030102149 A ARP030102149 A AR P030102149A AR P030102149 A ARP030102149 A AR P030102149A AR 039695 A1 AR039695 A1 AR 039695A1
Authority
AR
Argentina
Prior art keywords
replaced
groups
hal
atoms
independently
Prior art date
Application number
ARP030102149A
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English (en)
Inventor
Eggenweiler Hans-Michael Dr
Wolf Michael Dr
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Merck Patent Gmbh
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR039695A1 publication Critical patent/AR039695A1/es

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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Abstract

Estos derivados de fórmula (1), actúan como inhibidores de la fosfodiesterasa IV y pueden emplearse para el tratamiento de osteoporosis, tumores, caquexia, aterosclerosis, artritis reumatoidea, esclerosis múltiple, diabetes mellitus, procesos inflamatorios, alergias, asma, enfermedades, autoinmunes, enfermedades miocárdicas y SIDA. Reivindicación 1: Compuestos de la fórmula (1) donde: R1, R2 son en cada caso, independientemente entre sí, H, OH, OR8, -SR8, -SOR8, -SO2R8, o Hal; R1 y R2 también son juntos -OCH2O- u -OCH2CH2O-; R3, R3' son en cada caso, independientemente entre sí, H, A"R7, COA"R7, COOA"R7, CONH2, CONHA''R7, CON(A"R7)(A"')R7, CONR10Het, NH2, NHA"R7, N(A"R7)(A"'R7), NCOA''R7 o NCOOA''R7; V, W son oxígeno, o sustituyentes de hidrógeno, con la condición de que, cuando V significa O, W es H, H, y viceversa; B es un radical isocíclico o heterocíclico aromático, que esta insustituido o que puede estar mono, di o trisustituido por R4, R5 y/o R6; X es N o CR3, R4, R5, R6 son en cada caso, independientemente entre sí, H, A''R7, OH, OA''R7, NO2, NH2, NHA''R7, N(A''R7)(A'''R7), NHCOA''R7, NHCOOA''R7, NHCONH2, NHCONHA''R7, NHCON(A''R7)(A'''R7), Hal, COOH, COOA''R7, CONH2, CONHA''R7, CON(A''R7)(A'''R7); o un resto del grupo de fórmulas (2); R7 es H, COOH, COOA, CONH2, CONHA, CONAA', NH2, NHA, NAA', NCOA, NCOOA, OH u OA; R8 es A, cicloalquilo C3-7, alquilencicloalquilo C4-8 o alquenilo C2-8; R9 es alquilo C1-10, cicloalquilo C3-7, alquilencicloalquilo C4-8 o alquenilo C2-8, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe, NEt y/o por grupos -CH=CH- y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; Y es alquileno C1-10 o alquenileno C2-8, donde uno, dos o tres grupos CH2 pueden estar reemplazado por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; A, A' son en cada caso, independientemente entre sí, alquilo C1-10 o alquenilo C2-8, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl, o arilo o Het; A y A' también son juntos una cadena de alquileno C2-7, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9, NCOR9 o NCOOR9; A'', A''' en cada caso, independientemente entre sí, están ausentes, son alquileno C1-10, alquenileno C2-8 o cicloalquileno C3-7, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; A'' y A''' también son juntos una cadena de alquileno C2-7, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9, NCOR9 o NCOOR9; arilo es fenilo, naftilo, fluorenilo, o bifenilo insustituido o mono, di o trisustituido por Hal, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2A, COR10, SO2N(R10)2, S(O)mR11, R10 es H o alquilo C1-6; R11 es alquilo C1-6; Het es un heterociclo mono o bicíclico saturado, no saturado o aromático con 1 ó 2 átomos de N, O y/o S, que está insustituido o mono o disustituido por el oxígeno del carbonilo, Hal, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2R11, COR10, SO2NR10 y/o S(O)mR11; Hal es F, Cl, Br o I; m es 0, 1 ó 2; así como los derivados, solvatos y estereoisómeros de los mismos de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones.
ARP030102149A 2002-06-19 2003-06-18 Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit) AR039695A1 (es)

Applications Claiming Priority (1)

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DE10227269A DE10227269A1 (de) 2002-06-19 2002-06-19 Thiazolderivate

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AR039695A1 true AR039695A1 (es) 2005-03-09

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ARP030102149A AR039695A1 (es) 2002-06-19 2003-06-18 Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit)

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US (1) US7790723B2 (es)
EP (1) EP1513837B1 (es)
JP (1) JP4555076B2 (es)
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Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10227269A1 (de) * 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
GB0401334D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
CN1984901B (zh) 2004-05-18 2011-02-09 先灵公司 用作pde4抑制剂的取代的2-喹啉基-*唑
GB0411056D0 (en) 2004-05-18 2004-06-23 Novartis Ag Organic compounds
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
GB0424284D0 (en) 2004-11-02 2004-12-01 Novartis Ag Organic compounds
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EP2532677A1 (en) 2005-10-21 2012-12-12 Novartis AG Human antibodies against il13 and therapeutic uses
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
GB0601951D0 (en) 2006-01-31 2006-03-15 Novartis Ag Organic compounds
PL2322525T3 (pl) 2006-04-21 2014-03-31 Novartis Ag Pochodne puryny do zastosowania jako agoniści receptora adenozyny A<sub>2A</sub>
BRPI0717564A2 (pt) 2006-09-29 2013-10-22 Novartis Ag Pirazolopirimidinas como inibidores de pi3k lipídeo cinase
CA2667962A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
RS51644B (en) 2007-01-10 2011-10-31 Irm Llc. UNITS AND PREPARATIONS AS CHANNEL INHIBITORS ACTIVATING PROSTHESES
PL2155721T3 (pl) 2007-05-07 2011-07-29 Novartis Ag Związki organiczne
PT2444120T (pt) 2007-12-10 2018-01-03 Novartis Ag Análogos da amilorida espirocíclicos como bloqueadores de enac
KR20100113557A (ko) 2008-01-11 2010-10-21 노파르티스 아게 키나제 억제제로서의 피리미딘
AU2009256645A1 (en) 2008-06-10 2009-12-17 Novartis Ag Pyrazine derivatives as epithelial sodium channel blockers
JP6071198B2 (ja) 2008-07-15 2017-02-01 テラコス，インコーポレーテッド 重水素化ベンジルベンゼン誘導体及び使用方法
ES2396023T3 (es) 2009-01-29 2013-02-18 Novartis Ag Bencimidazoles sustituidos para el tratamiento de astrocitomas
SI2443089T1 (sl) * 2009-06-18 2014-07-31 Concert Pharmaceuticals, Inc. Devterirani derivati izoindolin-1,3-diona kot inhibitorji pde4 in tnf-alfa
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
JP5781510B2 (ja) 2009-08-12 2015-09-24 ノバルティス アーゲー ヘテロ環式ヒドラゾン化合物および癌および炎症の処置のためのそれらの使用
JP5819831B2 (ja) 2009-08-17 2015-11-24 インテリカイン， エルエルシー 複素環式化合物およびそれらの使用
WO2011020861A1 (en) 2009-08-20 2011-02-24 Novartis Ag Heterocyclic oxime compounds
EP2813227A1 (en) 2009-10-22 2014-12-17 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
JP2014505088A (ja) 2011-02-10 2014-02-27 ノバルティス アーゲー Ｃ−ＭＥＴチロシンキナーゼ阻害剤としての［１，２，４］トリアゾロ［４，３−ｂ］ピリダジン化合物
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
US9102671B2 (en) 2011-02-25 2015-08-11 Novartis Ag Compounds and compositions as TRK inhibitors
US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
JP5957526B2 (ja) 2011-09-15 2016-07-27 ノバルティス アーゲー チロシンキナーゼとしての６−置換３−（キノリン−６−イルチオ）−［１，２，４］トリアゾロ［４，３−ａ］ピラジン
WO2013038378A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
WO2013038373A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
EP2755652B1 (en) 2011-09-16 2021-06-02 Novartis AG N-substituted heterocyclyl carboxamides
ES2558457T3 (es) 2011-09-16 2016-02-04 Novartis Ag Compuestos heterocíclicos para el tratamiento de fibrosis quística
EP2793893A4 (en) 2011-11-23 2015-07-08 Intellikine Llc IMPROVED TREATMENT REGIMES USING MTOR INHIBITORS
EA021233B1 (ru) * 2012-03-14 2015-05-29 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, обладающий сосудосуживающим, антиконгестивным, противовоспалительным действием (варианты)
US8809340B2 (en) 2012-03-19 2014-08-19 Novartis Ag Crystalline form
EP3964513A1 (en) 2012-04-03 2022-03-09 Novartis AG Combination products with tyrosine kinase inhibitors and their use
WO2013161933A1 (ja) * 2012-04-26 2013-10-31 富山化学工業株式会社 重水素化含窒素複素環カルボキサミド誘導体
CN104718201A (zh) 2012-06-12 2015-06-17 艾伯维公司 吡啶酮和哒嗪酮衍生物
US9446131B2 (en) 2013-01-31 2016-09-20 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US9433680B2 (en) 2013-01-31 2016-09-06 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US8778365B1 (en) 2013-01-31 2014-07-15 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US9452173B2 (en) 2013-01-31 2016-09-27 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
CN105246482A (zh) 2013-03-15 2016-01-13 因特利凯有限责任公司 激酶抑制剂的组合及其用途
TW201605450A (zh) 2013-12-03 2016-02-16 諾華公司 Ｍｄｍ２抑制劑與ＢＲＡＦ抑制劑之組合及其用途
JP6474963B2 (ja) * 2014-03-04 2019-02-27 持田製薬株式会社 洗浄用組成物
KR20160141856A (ko) 2014-04-24 2016-12-09 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 피라진 유도체
PT3134396T (pt) 2014-04-24 2019-12-16 Novartis Ag Derivados de amino piridina como inibidores da fosfatidilinositol 3-quinase
CN106458979B (zh) 2014-04-24 2020-03-27 诺华股份有限公司 作为磷脂酰肌醇3-激酶抑制剂的氨基吡嗪衍生物
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
US10195208B2 (en) 2014-07-31 2019-02-05 Novartis Ag Combination therapy
US11395820B2 (en) 2016-03-16 2022-07-26 H. Lee Moffitt Cancer Center And Research Institute, Inc. Small molecules against cereblon to enhance effector t cell function
US10782276B2 (en) 2018-06-14 2020-09-22 Manufacturing Resources International, Inc. System and method for detecting gas recirculation or airway occlusion
WO2020014489A2 (en) 2018-07-11 2020-01-16 H. Lee Moffitt Cancer Center And Research Institute, Inc. Dimeric immuno-modulatory compounds against cereblon-based mechanisms
WO2020250116A1 (en) 2019-06-10 2020-12-17 Novartis Ag Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis
JOP20220044A1 (ar) 2019-08-28 2023-01-30 Novartis Ag مشتقات 1، 3- فينيل أريل غير متجانسة بها استبدال واستخدامها في معالجة مرض
TW202140550A (zh) 2020-01-29 2021-11-01 瑞士商諾華公司 使用抗ｔｓｌｐ抗體治療炎性或阻塞性氣道疾病之方法
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19533975A1 (de) * 1995-09-14 1997-03-20 Merck Patent Gmbh Arylalkyl-diazinone
DE19632549A1 (de) * 1996-08-13 1998-02-19 Merck Patent Gmbh Arylalkanoylpyridazine
DE10227269A1 (de) * 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate

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