WO2011039735A3 - Composés ayant une activité inhibitrice et utilisations de ceux-ci - Google Patents

Composés ayant une activité inhibitrice et utilisations de ceux-ci Download PDF

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Publication number
WO2011039735A3
WO2011039735A3 PCT/IB2010/054475 IB2010054475W WO2011039735A3 WO 2011039735 A3 WO2011039735 A3 WO 2011039735A3 IB 2010054475 W IB2010054475 W IB 2010054475W WO 2011039735 A3 WO2011039735 A3 WO 2011039735A3
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WO
WIPO (PCT)
Prior art keywords
compounds
inhibitory activity
ddx3
ddx3 inhibitory
compound
Prior art date
Application number
PCT/IB2010/054475
Other languages
English (en)
Other versions
WO2011039735A2 (fr
Inventor
Marco Radi
Maurizio Botta
Federico Falchi
Giovanni Maga
Fausto Baldanti
Stefania Paolucci
Original Assignee
Consiglio Nazionale Delle Ricerche
Università Degli Studi Di Siena
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Consiglio Nazionale Delle Ricerche, Università Degli Studi Di Siena filed Critical Consiglio Nazionale Delle Ricerche
Priority to US13/499,547 priority Critical patent/US20120202814A1/en
Publication of WO2011039735A2 publication Critical patent/WO2011039735A2/fr
Publication of WO2011039735A3 publication Critical patent/WO2011039735A3/fr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/36Sulfur atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/17Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40Nitrogen atoms
    • C07D251/54Three nitrogen atoms
    • C07D251/66Derivatives of melamine in which a hetero atom is directly attached to a nitrogen atom of melamine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links

Abstract

La présente invention concerne l'utilisation médicale du composé de formule 1, 2, 3 ou 4 :
PCT/IB2010/054475 2009-10-02 2010-10-04 Composés ayant une activité inhibitrice et utilisations de ceux-ci WO2011039735A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US13/499,547 US20120202814A1 (en) 2009-10-02 2010-10-04 Compounds with ddx3 inhibitory activity and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24803009P 2009-10-02 2009-10-02
US61/248,030 2009-10-02

Publications (2)

Publication Number Publication Date
WO2011039735A2 WO2011039735A2 (fr) 2011-04-07
WO2011039735A3 true WO2011039735A3 (fr) 2011-06-16

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2010/054475 WO2011039735A2 (fr) 2009-10-02 2010-10-04 Composés ayant une activité inhibitrice et utilisations de ceux-ci

Country Status (2)

Country Link
US (1) US20120202814A1 (fr)
WO (1) WO2011039735A2 (fr)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2595965B1 (fr) * 2010-07-20 2016-06-22 Vestaron Corporation Triazines et pyrimidines insecticides
US8697739B2 (en) 2010-07-29 2014-04-15 Novartis Ag Bicyclic acetyl-CoA carboxylase inhibitors and uses thereof
AU2013313974A1 (en) 2012-09-04 2015-03-12 Niigata University Cancer diagnostic and therapeutic method targeting molecules expressed in cancer stem cells
GB201300435D0 (en) 2013-01-10 2013-02-27 Medical Res Council Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases
JP6120311B2 (ja) * 2013-02-12 2017-04-26 学校法人銀杏学園 ポリフェノール化合物
GB201404372D0 (en) * 2014-03-12 2014-04-23 Univ Warwick Assay and treatment
CN104739838B (zh) * 2014-09-30 2017-07-14 三峡大学 小分子抑制剂及在抑制鸟氨酸脱羧酶(odc)上的应用
EP3256461B1 (fr) 2015-02-13 2023-09-13 Azienda Ospedaliera Universitaria Senese Dérivés d'urée et de sulfonamide utilisés en tant qu'inhibiteurs d'hélicase ddx3 humaine utiles dans le traitement de maladies virales
CN104974142A (zh) * 2015-06-12 2015-10-14 中国人民解放军第二军医大学 取代三氨基三嗪类分泌型天冬氨酸蛋白酶抑制剂及其制备方法
WO2017066428A1 (fr) 2015-10-13 2017-04-20 H. Lee Moffitt Cancer Center & Research Institute, Inc. Inhibiteurs de brd4-kinase à utiliser en tant qu'agents thérapeutiques anticancéreux
ITUA20161994A1 (it) * 2016-03-24 2017-09-24 Azienda Ospedaliera Univ Senese Uso degli inibitori ddx3 come agenti anti-iperproliferativi
CN111466338B (zh) * 2019-01-23 2022-03-22 中国科学院广州生物医药与健康研究院 Ddx5基因缺失的生精障碍小鼠模型及其构建方法
BR112022000325A2 (pt) 2019-07-11 2022-03-15 Escape Bio Inc Indazois e azaindazois como inibidores de lrrk2
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Alk﹘5抑制劑和彼之用途
CN113893254B (zh) * 2021-09-07 2023-03-21 南开大学 一种去乙酰化酶sirt1变构激动剂及其应用

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US20050101518A1 (en) * 2002-01-18 2005-05-12 David Solow-Cordero Methods of treating conditions associated with an EDG-2 receptor
US20060199804A1 (en) * 2005-02-25 2006-09-07 Kudos Pharmaceuticals Ltd Compounds
WO2007071199A1 (fr) * 2005-12-22 2007-06-28 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Composes de 2,4-disubstituee amido-6-substituee-[1,3,5]triazine ou de 1,3-pyrimidine, leurs procedes d'elaboration, et preparations pharmaceutiques les contenant et leurs utilisations
CN101058573A (zh) * 2006-04-18 2007-10-24 上海医药工业研究院 2-腙代三嗪类化合物,其制备方法和以该化合物为活性成分的药物组合物及其用途
WO2008094319A2 (fr) * 2007-02-01 2008-08-07 The Board Of Regents Of The University Of Texas Sytem Procédés et compositions d'agonistes/activateurs du récepteur de mort trail
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US20090088420A1 (en) * 2007-04-12 2009-04-02 University Of Southern California Compounds with hiv-1 integrase inhibitory activity and use thereof as anti-hiv/aids therapeutics

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US20050101518A1 (en) * 2002-01-18 2005-05-12 David Solow-Cordero Methods of treating conditions associated with an EDG-2 receptor
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WO2007071199A1 (fr) * 2005-12-22 2007-06-28 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Composes de 2,4-disubstituee amido-6-substituee-[1,3,5]triazine ou de 1,3-pyrimidine, leurs procedes d'elaboration, et preparations pharmaceutiques les contenant et leurs utilisations
CN101058573A (zh) * 2006-04-18 2007-10-24 上海医药工业研究院 2-腙代三嗪类化合物,其制备方法和以该化合物为活性成分的药物组合物及其用途
WO2008094319A2 (fr) * 2007-02-01 2008-08-07 The Board Of Regents Of The University Of Texas Sytem Procédés et compositions d'agonistes/activateurs du récepteur de mort trail
US20090088420A1 (en) * 2007-04-12 2009-04-02 University Of Southern California Compounds with hiv-1 integrase inhibitory activity and use thereof as anti-hiv/aids therapeutics
WO2009023558A1 (fr) * 2007-08-10 2009-02-19 Vm Discovery Inc. Compositions et procédés pour modulateurs d'apoptose

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DENG J ET AL: "Discovery of structurally diverse HIV-1 integrase inhibitors based on a chalcone pharmacophore", BIOORGANIC & MEDICINAL CHEMISTRY, PERGAMON, GB, vol. 15, no. 14, 15 July 2007 (2007-07-15), pages 4985 - 5002, XP026265763, ISSN: 0968-0896, [retrieved on 20070715], DOI: DOI:10.1016/J.BMC.2007.04.041 *
MAGA GIOVANNI ET AL: "Pharmacophore Modeling and Molecular Docking Led to the Discovery of Inhibitors of Human Immunodeficiency Virus-1 Replication Targeting the Human Cellular Aspartic Acid-Glutamic Acid-Alanine-Aspartic Acid Box Polypeptide 3", JOURNAL OF MEDICINAL CHEMISTRY, vol. 51, no. 21, November 2008 (2008-11-01), pages 6635 - 6638, XP002616029, ISSN: 0022-2623 *
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WO2011039735A2 (fr) 2011-04-07
US20120202814A1 (en) 2012-08-09

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