ES2527770T3 - Derivados de tetrahidroindolona y tetrahidroindazolona - Google Patents

Derivados de tetrahidroindolona y tetrahidroindazolona Download PDF

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ES2527770T3
ES2527770T3 ES06736330.9T ES06736330T ES2527770T3 ES 2527770 T3 ES2527770 T3 ES 2527770T3 ES 06736330 T ES06736330 T ES 06736330T ES 2527770 T3 ES2527770 T3 ES 2527770T3
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alkyl
aryl
saturated
group
independently
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Kenneth He Huang
Jeron Eaves
James Veal
Thomas Barta
Lifeng Geng
Lindsay Hinkley
Gunnar Hanson
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Serenex Inc
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Serenex Inc
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
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  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Un compuesto de fórmula XXV, **Fórmula** o una de sus sales farmacéuticamente aceptable, en donde R3 y R4 son independientemente (a) H, (b) halo o (c) un grupo alquilo C1-C15 en donde hasta seis de los átomos de carbono en dicho grupo alquilo están opcionalmente reemplazados independientemente por R22, carbonilo, etenilo, etinilo o un resto seleccionado entre N, O, S, SO2 o SO, con la condición de que dos átomos de O, dos átomos de S, o un átomo de O y S 10 no sean inmediatamente adyacentes entre sí, en donde R22 es (i) heteroarilo, (ii) arilo, (iii) cicloalquilo C3-C10 saturado o insaturado, o (iv) heterocicloalquilo C2-C10 saturado o insaturado, en donde cada arilo, heteroarilo, cicloalquil saturado o insaturado, o heterocicloalquilo saturado o insaturado, independientemente, está opcionalmente sustituido con al menos un grupo, que es independientemente hidroxi, halo, amino, ciano, carboxi, carboxamido, nitro, oxo, -S-alquilo (C1-C6), -SO2-alquilo (C1-C6), -SO2-arilo, -SO-alquilo (C1-C6), -SO-arilo, -SO2NH2, -SO2NH-alquilo (C1-C6), -SO2NH-arilo, alcoxi (C1-C6) o mono- o di-alquilamino (C1-C10); y cada R22 está opcionalmente condensado con un grupo arilo C6-C10, grupo cíclico C5-C8 saturado o un grupo heterocicloalquilo C5-C10; en donde cada (c) está opcionalmente sustituido en cualquier posición disponible con alquil C1-C10, haloalquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, hidroxi, carboxi, carboxamido, oxo, halo, amino, ciano, nitro, -SH, -S-alquilo (C1-C6), -SO2-alquilo (C1-C6), -SO2NH2, -SO2NH-alquilo (C1-C6), -SO2NH-arilo, -SO2-arilo, - SO-alquilo (C1-C6), -SO2-arilo, alcoxi C1-C6, alqueniloxi C2-C10, alquiniloxi C2-C10, mono o di-alquilamino (C1-C10), -Oalquil C1-C10-Z o R23, en donde Z es OR0 o -N(R30)2, en donde cada R30 es independientemente -H o alquilo C1-C6, o N(R30)2 representa pirrolidinilo, piperidinilo, piperazinilo, 30 azepanilo, 1,3- o 1,4-diazepanilo, o morfolinilo, cada uno de los cuales está opcionalmente sustituido con hidroxi, amino, aminoalquilo, alquilo C1-C6, mono- o di-alquilamino (C1-C6), alcoxi C1-C6 o halógeno; R0 es -H, -alquilo C1-C10, -alquenilo C2-C10, -alquinilo C2-C10, arilo, heteroarilo o -acilo C1-C6; R23 es (1) heteroarilo, (2) arilo.
ES06736330.9T 2005-02-25 2006-02-27 Derivados de tetrahidroindolona y tetrahidroindazolona Active ES2527770T3 (es)

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Application Number Priority Date Filing Date Title
US65623005P 2005-02-25 2005-02-25
US656230P 2005-02-25
US70571505P 2005-08-04 2005-08-04
US705715P 2005-08-04
US72796505P 2005-10-18 2005-10-18
US727965P 2005-10-18
PCT/US2006/006988 WO2006091963A1 (en) 2005-02-25 2006-02-27 Tetrahydroindolone and tetrahydroindazolone derivatives

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Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
AU2005294404A1 (en) * 2004-10-04 2006-04-20 Myriad Genetics, Inc. Compounds for Alzheimer's disease
ES2527770T3 (es) * 2005-02-25 2015-01-29 Serenex, Inc. Derivados de tetrahidroindolona y tetrahidroindazolona
US7728008B2 (en) * 2005-06-27 2010-06-01 Bristol-Myers Squibb Company N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US20070207984A1 (en) * 2006-02-27 2007-09-06 Huang Kenneth H Cyclohexylamino Benzene, Pyridine, and Pyridazine Derivatives
CA2648216C (en) * 2006-04-13 2016-06-07 Michael Gutschow Tetrahalogenated compounds useful as inhibitors of angiogenesis
NZ572600A (en) 2006-05-12 2011-08-26 Myrexis Inc 6-Amino-purine derivatives for the treatment of cancer and fibrogenetic disorders
DK2018380T3 (da) * 2006-05-19 2012-01-23 Abbott Lab CNS-aktiverede kondenserede bi-heterocyklisk-substituerede azabicykliske alkanderivater
US10336757B2 (en) * 2006-06-30 2019-07-02 Sloan-Kettering Institute For Cancer Research Treatment of neurodegenerative diseases through inhibition of HSP90
US7678803B2 (en) 2006-08-24 2010-03-16 Serenex, Inc. Quinazoline derivatives for the treatment of cancer
WO2008024970A2 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
WO2008024963A1 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Benzene, pyridine, and pyridazine derivatives
US20080119457A1 (en) * 2006-08-24 2008-05-22 Serenex, Inc. Benzene, Pyridine, and Pyridazine Derivatives
US20080070933A1 (en) * 2006-08-24 2008-03-20 Huang Kenneth H Purine, Pyrimidine, and Azaindole Derivatives
WO2008024961A1 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Dihydropyridazine, tetrahydropyridine, chromanone, and dihydronaphthalenone derivatives as heat-shock protein 90 inhibitors
WO2008024980A2 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives
FR2907453B1 (fr) 2006-10-24 2008-12-26 Sanofi Aventis Sa Nouveaux derives du fluorene,compositions les contenant et utilisation
US20100280032A1 (en) * 2006-10-26 2010-11-04 Synta Pharmaceuticals Corp. Method for treating inflammatory disorders
CN101273991B (zh) * 2007-03-28 2010-05-26 广东同德药业有限公司 四氢吲哚酮/四氢吲唑酮/四氢咔唑衍生物及其盐在制备抗病毒药物中的应用
EP2146967A2 (en) * 2007-04-16 2010-01-27 Serenex, Inc. Tetrahydroindole and tetrahydroindazole derivatives
EP1997805A1 (en) * 2007-06-01 2008-12-03 Commissariat à l'Energie Atomique Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
JP5374377B2 (ja) * 2007-10-18 2013-12-25 武田薬品工業株式会社 複素環化合物
FR2955323B1 (fr) * 2010-01-19 2015-01-16 Sanofi Aventis Nouveaux derives d'indazole inhibiteurs d'hsp90, compositions les contenant et utilisation
FR2943341B1 (fr) * 2009-03-19 2011-03-11 Sanofi Aventis Nouveaux derives d'indazole inhibiteurs d'hsp90,compositions les contenant et utilisation
BRPI1009375A2 (pt) * 2009-03-19 2016-03-15 Sanofi Aventis derivados inibidores de hsp90, composições que os contém e utilização
EP3578664B1 (en) * 2009-03-30 2024-10-30 Nordic Bioscience A/S Collagen iv neo-epitope fibrosis assay
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
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
US9205086B2 (en) 2010-04-19 2015-12-08 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a Hsp90 inhibitory compounds and a EGFR inhibitor
CN101872359B (zh) * 2010-06-11 2013-08-14 北京邮电大学 实现演变点发现的社会网络演化分析方法及系统
GB201009853D0 (en) 2010-06-11 2010-07-21 Chroma Therapeutics Ltd HSP90 inhibitors
CN102311389A (zh) * 2010-06-29 2012-01-11 王小龙 一种氮芳香取代吡唑衍生物、及其合成和抗癌应用
CN101955461B (zh) * 2010-10-08 2012-11-21 广州暨南生物医药研究开发基地有限公司 一种Hsp90抑制剂Xbj-B11及其制备方法与应用
CN101967125B (zh) 2010-10-08 2012-07-04 广州暨南生物医药研究开发基地有限公司 一种Hsp90抑制剂Xbj-B16-1及其制备方法与应用
CA2830195A1 (en) 2011-03-15 2012-09-20 Martin E. Gleave Combination of anti-clusterin oligonucleotide with hsp90 inhibitor for the treatment of prostate cancer
CN102675288B (zh) * 2011-03-18 2014-01-01 北京师范大学 2-((2-(双(2-吡啶甲基)氨基)乙基)氨基)-4-(3，6，6-三甲基-4-氧-4，5，6，7-四氢吲唑基)苯甲酰胺及制备、应用
US9439899B2 (en) 2011-11-02 2016-09-13 Synta Pharmaceuticals Corp. Cancer therapy using a combination of HSP90 inhibitors with topoisomerase I inhibitors
CA2853806C (en) 2011-11-02 2020-07-14 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with platinum-containing agents
JP2014533299A (ja) 2011-11-14 2014-12-11 シンタ ファーマシューティカルズ コーポレーション Ｂｒａｆ阻害剤とｈｓｐ９０阻害剤の組合せ療法
WO2014025395A1 (en) 2012-08-06 2014-02-13 Duke University Compounds and methods for targeting hsp90
CN103467356B (zh) * 2013-08-12 2015-04-01 绍兴文理学院 一种四氢吲哚化合物及其制备方法与应用
NZ729137A (en) 2014-08-04 2022-07-29 Nuevolution As Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
WO2016040809A1 (en) * 2014-09-11 2016-03-17 Esanex, Inc. Indazolyl- and indolyl-benzamide derivatives
US20160143884A1 (en) * 2014-11-26 2016-05-26 Esanex, Inc. Use of tetrahydroindazolylbenzamide and tetrahydroindolylbenzamide derivatives for the treatment of human immunodeficiency virus (hiv) and acquired immune deficiency syndrome (aids)
CN104592203A (zh) * 2015-01-30 2015-05-06 广州暨南生物医药研究开发基地有限公司 一种2-氨基-4-四氢吲唑取代的苯甲酰胺化合物及其在制备抗肿瘤药物中的应用
CN104592230B (zh) * 2015-01-30 2017-02-01 广州暨南生物医药研究开发基地有限公司 一种2‑（石榴皮烷‑3‑氨基）‑4‑四氢吲唑取代的苯甲酰胺化合物及其应用
WO2016191412A1 (en) * 2015-05-26 2016-12-01 University Of South Florida Antimicrobial compositions, methods of use, and methods of treatment of infections
WO2017059434A1 (en) 2015-10-02 2017-04-06 Esanex, Inc. Use of tetrahydroindazolylbenzamide and tetrahydroindolylbenzamide derivatives for the treatment of cancer
RU2721119C2 (ru) * 2015-10-13 2020-05-15 Нихон Нохияку Ко., Лтд. Содержащее оксимную группу конденсированное гетероциклическое соединение или его соль, сельскохозяйственный и садовый инсектицид, содержащий данное соединение, и способ применения данного инсектицида
US11261187B2 (en) 2016-04-22 2022-03-01 Duke University Compounds and methods for targeting HSP90
WO2017201226A1 (en) * 2016-05-18 2017-11-23 Esanex, Inc. Combination therapies using indazolylbenzamide derivatives for the treatment of cancer
EP3515436A1 (en) 2016-09-23 2019-07-31 Esanex, Inc. Combination therapies using indazolylbenzamide derivatives for the treatment of cancer
SMT201900517T1 (it) 2017-03-20 2019-11-13 Forma Therapeutics Inc Composizioni di pirrolopirrolo come attivatori di piruvato chinasi (pkr)
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
CN113226356B (zh) 2018-09-19 2025-03-04 诺沃挪第克健康护理股份公司 活化丙酮酸激酶r
CN114615977B (zh) 2019-09-19 2025-01-14 诺沃挪第克健康护理股份公司 丙酮酸激酶r(pkr)活化组合物
JP7746259B2 (ja) 2019-12-20 2025-09-30 ヌエヴォリューション・アクティーゼルスカブ 核内受容体に対して活性の化合物
JP2021098692A (ja) 2019-12-20 2021-07-01 ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ 核内受容体に対して活性の化合物
US11780843B2 (en) 2020-03-31 2023-10-10 Nuevolution A/S Compounds active towards nuclear receptors
US11613532B2 (en) 2020-03-31 2023-03-28 Nuevolution A/S Compounds active towards nuclear receptors
US20230219890A1 (en) * 2020-06-11 2023-07-13 Betta Pharmaceuticals Co.,Ltd Bicyclic compounds and use thereof
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
CN114213332B (zh) * 2022-02-21 2022-05-17 深圳市人民医院 一种四氢吲唑类化合物及其制备方法和应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4024862A1 (de) * 1990-08-04 1992-02-13 Hoechst Ag 4,5,6,7-tetrahydro-3-aryl-indazole, verfahren zu ihrer herstellung und ihre verwendung als herbizide
GB9812038D0 (en) 1998-06-04 1998-07-29 Merck Sharp & Dohme Therapeutic compound
GB9900222D0 (en) * 1999-01-06 1999-02-24 Merck Sharp & Dohme Therapeutic compounds
GB9911053D0 (en) * 1999-05-12 1999-07-14 Pharmacia & Upjohn Spa 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents
US6743817B2 (en) 2000-09-06 2004-06-01 Neurogen Corporation Substituted fused pyrroleimines and pyrazoleimines
WO2003016254A1 (en) 2001-08-09 2003-02-27 Ono Pharmaceutical Co., Ltd. Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient
DE10148618B4 (de) * 2001-09-25 2007-05-03 Schering Ag Substituierte N-(1,4,5,6-Tetrahydro-cyclopentapyrazol-3-yl)-Derivate, deren Herstellung und Verwendung als Arzneimittel
WO2003073999A2 (en) * 2002-03-01 2003-09-12 Pintex Pharmaceuticals, Inc. Pini-modulating compounds and methods of use thereof
WO2004052862A1 (ja) 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
ES2527770T3 (es) * 2005-02-25 2015-01-29 Serenex, Inc. Derivados de tetrahidroindolona y tetrahidroindazolona
JPWO2006109846A1 (ja) 2005-04-06 2008-11-20 武田薬品工業株式会社 トリアゾール誘導体およびその用途
EP2146967A2 (en) * 2007-04-16 2010-01-27 Serenex, Inc. Tetrahydroindole and tetrahydroindazole derivatives

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