AR067082A1 - Derivados de indazolamida, proceso de preparacion, medicamentos que los contienen y usos de los mismos, fundamentalmente, como agentes antitumorales y/o antivirales. - Google Patents
Derivados de indazolamida, proceso de preparacion, medicamentos que los contienen y usos de los mismos, fundamentalmente, como agentes antitumorales y/o antivirales.Info
- Publication number
- AR067082A1 AR067082A1 ARP080102635A ARP080102635A AR067082A1 AR 067082 A1 AR067082 A1 AR 067082A1 AR P080102635 A ARP080102635 A AR P080102635A AR P080102635 A ARP080102635 A AR P080102635A AR 067082 A1 AR067082 A1 AR 067082A1
- Authority
- AR
- Argentina
- Prior art keywords
- nar
- nhet
- hal
- atoms
- replaced
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 2
- 230000000259 anti-tumor effect Effects 0.000 title 1
- 239000003443 antiviral agent Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 101710113864 Heat shock protein 90 Proteins 0.000 abstract 2
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 abstract 2
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 abstract 2
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical class C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000000565 sulfonamide group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 230000033228 biological regulation Effects 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000003453 indazolyl group Chemical class N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- -1 p-methoxybenzyloxy Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- A—HUMAN NECESSITIES
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- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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Abstract
Derivados de indazol de la formula 1 en donde R1 es H, OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-metoxibenciloxi, SH, S(O)mCH3, SO2NH2, Hal, CF3 o CH3, R2 es heterociclo mono- o bicíclico saturado o insaturado no sustituido mono-, di- o trisustituido con R4 y/o R5 con 1 a 4 átomos de N, y/o S, que al menos contiene un átomo de N y en donde el átomo de está unido directamente con el grupo carbonilo adyacente, R3 es H, Hal, A, OA, AlkOH, COOA, COA, COHet, CONH2, CONHA, CONAA', CONHAr, CONH(AlkAr), CONAAr, CONA(AlkAr), CONHHet, CONH(AlkHet), CONA-Het, CONA(AlkHet), AlkCOOA, AlkCONHA, AlkCONAA', AlkNHCONH2, AlkNHCONHA, AlkNHCONAA', AlkNHCOA, AlkNHCOAr, AlkNHSO2A, AlkNH-SO2Ar, AlkNASO2Ar, AlkNHSO2CH2Ar, AlkNASO2CH2Ar, AlkAr, AlkHet, NHAr, NHA, NAA', NAAr, NAHet o NHHet, R4 es H, A, Ar, (CH2)nHet, Hal, CN, NO2, NH2, OH, OA, OAr, OAlkAr, OAlkHet, OAHet, SH, SA, SAr, SAlkAr, SHet, SAlkHet, COA, COAr, COHet, S(O)mA, S(O)mAr, S(O)mAAr, S(O)mHet, S(O)mAHet, NHA, NHAr, NHHet, NAA', NAAr, NAHet, COOH, COOA, CONH2, CONHA, CONAA', CONH(CH2)nAr, CONA(CH2)nAr, CONH(CH2)nHet, CONA(CH2)nHet, SO2NH2, SO2NHA, SO2NAA',SO2NH(CH2)nAr, SO2NA(CH2)nAr, SO2NH(CH2)nHet, SO2NA(CH2)nHet, NHCOA, NACOA', NHCO(CH2)nAr, NACO(CH2)nAr, NHCO(CH2)nHet, NACO(CH2)nHet, NHSO2A, NASO2A', NHSO2(CH2)nAr, NASO2(CH2)nAr, NHSO2(CH2)nHet, NASO2(CH2)nHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCONHAr, NHCONHHet, =O (oxígeno del carbonilo), AlkNH2, OAlkNHA, OAlkNAA', OAlkOHOAlkOA, OAlkCN, CONHAlkNH2, CONHAlkNHA, CONHAlkNAA', COAlkNH2COAlkNHA o COAlkNAA', R5 es H, A, Ar, Het, AlkAr, AlkHet, COA, CO(CH2)nAr, CO(CH2)nHet, SO2A, SO2(CH2)nAr, SO2(CH2)nHet, COOA, COOAr, COOHet, CONHA, CONHAr o CONHHet, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetrapentasustituido con A, OA, OH, SH, S(O)mA, Hal, NO2, CN, COA, COOH, COOA, CONR6R7, SO2NR6R7, NR6R7, OCONR6R7, NR6COR7, NR6SO2R7, NR6CONR6R7, (CH2)nNHSO2A, O(CH2)pCN, SO2Het1, O(CH2)pNR6R7 y/o (CH2)mHet1, A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde 1-3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe o NEt y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl, Alk1 alquilo cíclico C3-8, Alk1 es alquenilo o alquinilo C2-6, Alk es alquileno no ramificado o, ramificado C1-8, en donde 1-7 átomos de H pueden estar reemplazados por OH, F, Cl y/o Br, y/o en donde uno o dos grupos CH2 pueden estar reemplazados por O, Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar no sustituido o que puede estar mono-, di- o trisustituido con A, OA, OH, SH, S(O)mA, Hal, NO2, CN, COA, COOA, CONR6R7, SO2NR6R7, NR6R7, OCONR6R7, NR6COR7, NR6SO2R7, NR6CONR6R7, =S, =NH, =NA y/u =O (oxígeno del carbonilo), Het1 es un heterociclo saturado monocíclico con 1 a 3 átomos de N y/u O, que puede estar no sustituido o que puede estar mono-, di- o trisustituido con A, OA, OH y/u =O (oxígeno del carbonilo), R6, R7 es cada uno, de modo independiente entre sí, H o alquilo C1-6, en donde 1-3 grupos CH2 pueden estar reemplazados po O, S, SO, SO2, NH, NMe, o NEt y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl, Hal es F, Cl, Br o I, m es 0, 1 o 2, n es 0, 1, 2, 3 o 4, p es 1, 2, 3 o 4, así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempena un papel importante.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102007028521A DE102007028521A1 (de) | 2007-06-21 | 2007-06-21 | Indazolamidderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR067082A1 true AR067082A1 (es) | 2009-09-30 |
Family
ID=39772843
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080102635A AR067082A1 (es) | 2007-06-21 | 2008-06-20 | Derivados de indazolamida, proceso de preparacion, medicamentos que los contienen y usos de los mismos, fundamentalmente, como agentes antitumorales y/o antivirales. |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20100256137A1 (es) |
| EP (1) | EP2155690B1 (es) |
| JP (1) | JP5426539B2 (es) |
| KR (1) | KR20100038206A (es) |
| CN (1) | CN101687808A (es) |
| AR (1) | AR067082A1 (es) |
| AT (1) | ATE518837T1 (es) |
| AU (1) | AU2008266585B2 (es) |
| BR (1) | BRPI0812518A2 (es) |
| CA (1) | CA2691019C (es) |
| DE (1) | DE102007028521A1 (es) |
| EA (1) | EA201000007A1 (es) |
| ES (1) | ES2375114T3 (es) |
| IL (1) | IL202830A (es) |
| MX (1) | MX2009013129A (es) |
| WO (1) | WO2008155001A1 (es) |
| ZA (1) | ZA201000431B (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102006030479A1 (de) * | 2006-07-01 | 2008-03-20 | Merck Patent Gmbh | Indazolderivate |
| WO2009039248A2 (en) | 2007-09-18 | 2009-03-26 | Stanford University | Methods of treating a flaviviridae family viral infection and compositions for treating a flaviviridae family viral infection |
| US9101628B2 (en) | 2007-09-18 | 2015-08-11 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and composition of treating a flaviviridae family viral infection |
| US8940730B2 (en) | 2007-09-18 | 2015-01-27 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and compositions of treating a Flaviviridae family viral infection |
| US9149463B2 (en) | 2007-09-18 | 2015-10-06 | The Board Of Trustees Of The Leland Standford Junior University | Methods and compositions of treating a Flaviviridae family viral infection |
| JP2012520884A (ja) | 2009-03-18 | 2012-09-10 | ザ ボード オブ トラスティーズ オブ ザ リランド スタンフォード ジュニア ユニバーシティー | フラビウイルス科ウイルス感染症を治療する方法および組成物 |
| EP2408448A4 (en) * | 2009-03-18 | 2012-09-19 | Univ Leland Stanford Junior | METHOD AND COMPOSITIONS FOR TREATING FLAVIVIRIDAE VIRUS INFECTIONS |
| AR078411A1 (es) | 2009-05-07 | 2011-11-09 | Lilly Co Eli | Compuesto de vinil imidazolilo y composicion farmaceutica que lo comprende |
| AR077405A1 (es) | 2009-07-10 | 2011-08-24 | Sanofi Aventis | Derivados del indol inhibidores de hsp90, composiciones que los contienen y utilizacion de los mismos para el tratamiento del cancer |
| CN101991572B (zh) * | 2009-08-21 | 2012-07-04 | 华东理工大学 | 一种二肽基肽酶ⅳ新抑制剂 |
| FR2949467B1 (fr) | 2009-09-03 | 2011-11-25 | Sanofi Aventis | Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation |
| DE102010046837A1 (de) * | 2010-09-29 | 2012-03-29 | Merck Patent Gmbh | Phenylchinazolinderivate |
| US9487506B2 (en) | 2011-04-13 | 2016-11-08 | Merck Sharp & Dohme Corp. | Mineralocorticoid receptor antagonists |
| CN105218625A (zh) * | 2014-06-10 | 2016-01-06 | 首都医科大学 | 异喹啉类衍生物,其制备,纳米结构,活性和应用 |
| CR20170005A (es) * | 2014-07-08 | 2017-05-08 | Viiv Healthcare Uk Ltd | Derivados de insoindolina |
| CN104098513B (zh) * | 2014-07-30 | 2016-08-24 | 天津市斯芬克司药物研发有限公司 | 一种吲唑化合物衍生物及其制备方法 |
| CN104840459B (zh) * | 2015-03-31 | 2017-12-22 | 中国医学科学院基础医学研究所 | 17‑丙烯胺‑17‑去甲氧格尔德霉素在制备治疗癫痫的药物中的用途 |
| US11046670B2 (en) | 2015-10-19 | 2021-06-29 | Board Of Regents, The University Of Texas System | Piperazinyl norbenzomorphan compounds and methods for using the same |
| CA3022512A1 (en) * | 2016-04-29 | 2017-11-02 | Board Of Regents, The University Of Texas System | Sigma receptor binders |
| EP3568128B1 (en) | 2017-01-12 | 2022-07-06 | The University of Kansas | Hsp90b n-terminal isoform-selective inhibitors |
| CN107311986B (zh) * | 2017-07-07 | 2020-05-01 | 山东大学 | 四氢异喹琳-3-羧酸类热休克蛋白90抑制剂及其应用 |
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| US5968921A (en) | 1997-10-24 | 1999-10-19 | Orgegon Health Sciences University | Compositions and methods for promoting nerve regeneration |
| AU3378599A (en) | 1998-04-03 | 1999-10-25 | University Of Pittsburgh | Benzoquinoid ansamycins for the treatment of cardiac arrest and stroke |
| AU776652B2 (en) | 1999-03-12 | 2004-09-16 | United States Of America, Represented By The Secretary, Department Of Health And Human Services, The | Method of inhibiting a chaperone protein |
| WO2001072779A1 (en) | 2000-03-24 | 2001-10-04 | Duke University | Characterization of grp94-ligand interactions and purification, screening, and therapeutic methods relating thereto |
| WO2002002123A1 (en) | 2000-06-29 | 2002-01-10 | Trustees Of Boston University | Use of geldanamycin and related compounds for prophylaxis or treatment of fibrogenic disorders |
| EP1322325A4 (en) | 2000-07-20 | 2004-09-15 | Merck & Co Inc | INHIBITION OF PROCESSING AND REPLICATION OF HEPATITIS C VIRUS |
| US6946456B2 (en) | 2000-07-28 | 2005-09-20 | Sloan-Kettering Institute For Cancer Research | Methods for treating cell proliferative disorders and viral infections |
| US6897231B2 (en) * | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| US6982274B2 (en) | 2001-04-16 | 2006-01-03 | Eisai Co., Ltd. | 1H-indazole compound |
| JPWO2002100833A1 (ja) * | 2001-06-12 | 2004-09-24 | 住友製薬株式会社 | Ｒｈｏキナーゼ阻害剤 |
| EP1450784A4 (en) | 2001-11-09 | 2005-02-09 | Conforma Therapeutics Corp | HSP90-INHIBITABLE ZEARALANOL COMPOUNDS AND METHOD FOR THEIR PREPARATION AND USE |
| NZ539193A (en) * | 2002-09-05 | 2008-04-30 | Aventis Pharma Sa | Novel aminoindazole derivatives as medicines and pharmaceutical compositions containing same |
| AU2004268820B2 (en) * | 2003-08-29 | 2011-07-21 | Cancer Research Technology Ltd | Pyrimidothiophene compounds |
| EA010160B1 (ru) * | 2003-09-18 | 2008-06-30 | Конформа Терапьютикс Корпорейшн | Новые гетероциклические соединения - ингибиторы hsp90 и способы их получения |
| CN101027053A (zh) | 2004-07-27 | 2007-08-29 | 诺瓦提斯公司 | Hsp90抑制剂 |
| ME02051B (me) * | 2005-04-13 | 2015-05-20 | Astex Therapeutics Ltd | Derivati hidroksibenzamida i njihova primena kao inhibitora hsp90 |
| DE102006030479A1 (de) * | 2006-07-01 | 2008-03-20 | Merck Patent Gmbh | Indazolderivate |
| EA200900613A1 (ru) * | 2006-11-29 | 2009-10-30 | Пфайзер Продактс Инк. | Спирокетоновые ингибиторы ацетил-коа-карбоксилаз |
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2007
- 2007-06-21 DE DE102007028521A patent/DE102007028521A1/de not_active Withdrawn
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2008
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- 2008-05-23 ES ES08758745T patent/ES2375114T3/es active Active
- 2008-05-23 KR KR1020107001391A patent/KR20100038206A/ko not_active Application Discontinuation
- 2008-05-23 JP JP2010512545A patent/JP5426539B2/ja not_active Expired - Fee Related
- 2008-05-23 US US12/665,445 patent/US20100256137A1/en not_active Abandoned
- 2008-05-23 CN CN200880021101A patent/CN101687808A/zh active Pending
- 2008-05-23 WO PCT/EP2008/004154 patent/WO2008155001A1/de active Application Filing
- 2008-05-23 EA EA201000007A patent/EA201000007A1/ru unknown
- 2008-05-23 AT AT08758745T patent/ATE518837T1/de active
- 2008-05-23 MX MX2009013129A patent/MX2009013129A/es not_active Application Discontinuation
- 2008-05-23 EP EP08758745A patent/EP2155690B1/de not_active Not-in-force
- 2008-05-23 AU AU2008266585A patent/AU2008266585B2/en not_active Ceased
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- 2008-06-20 AR ARP080102635A patent/AR067082A1/es unknown
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2009
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Also Published As
| Publication number | Publication date |
|---|---|
| JP2010530377A (ja) | 2010-09-09 |
| EA201000007A1 (ru) | 2010-06-30 |
| ATE518837T1 (de) | 2011-08-15 |
| KR20100038206A (ko) | 2010-04-13 |
| IL202830A0 (en) | 2010-06-30 |
| WO2008155001A1 (de) | 2008-12-24 |
| CN101687808A (zh) | 2010-03-31 |
| US20100256137A1 (en) | 2010-10-07 |
| MX2009013129A (es) | 2010-01-15 |
| EP2155690A1 (de) | 2010-02-24 |
| ES2375114T3 (es) | 2012-02-24 |
| BRPI0812518A2 (pt) | 2015-03-31 |
| CA2691019C (en) | 2015-06-30 |
| JP5426539B2 (ja) | 2014-02-26 |
| IL202830A (en) | 2015-08-31 |
| DE102007028521A1 (de) | 2008-12-24 |
| CA2691019A1 (en) | 2008-12-24 |
| EP2155690B1 (de) | 2011-08-03 |
| ZA201000431B (en) | 2011-12-28 |
| AU2008266585B2 (en) | 2013-02-14 |
| AU2008266585A1 (en) | 2008-12-24 |
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