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PE20180929A1 - Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5 - Google Patents

Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5

Info

Publication number
PE20180929A1
PE20180929A1 PE2018000306A PE2018000306A PE20180929A1 PE 20180929 A1 PE20180929 A1 PE 20180929A1 PE 2018000306 A PE2018000306 A PE 2018000306A PE 2018000306 A PE2018000306 A PE 2018000306A PE 20180929 A1 PE20180929 A1 PE 20180929A1
Authority
PE
Peru
Prior art keywords
bicyclic aromatic
aromatic ring
novel analogs
prmt5 inhibitors
compounds
Prior art date
Application number
PE2018000306A
Other languages
English (en)
Inventor
Tongfei Wu
Dirk Brehmer
Lijs Beke
An Boeckx
Gaston Stanislas Marcella Diels
Ronaldus Arnodus Hendrika Joseph Gilissen
Edward Charles Lawson
Vineet Pande
Marcus Cornelis Bernardus Catharina Parade
Wim Bert Griet Schepens
Johannes Wilhelmus John F Thuring
Marcel Viellevoye
Weime Sun
Lieven Meerpoel
Original Assignee
Janssen Pharmaceutica Nv
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.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20180929A1 publication Critical patent/PE20180929A1/es

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Abstract

SE REFIERE A COMPUESTOS ANALOGOS DE NUCLEOSIDOS SUSTITUIDOS EN EL ANILLO AROMATICO BICICLICO 6-6 DE FORMULA (I) DONDE R1 Y R2 SON CADA UNO H O -C-(=O)-(ALQUILO C1-C4); Y ES -O-, -CH2- O -CF2-; Z ES -CH2-, ETINILO, ENTRE OTROS; Ar ES UN SISTEMA ANULAR AROMATICO BICICLICO DE 10 MIEMBROS CONSTITUIDO POR DOS ANILLOS DE 6 MIEMBROS CONDENSADOS; Het ES UN SISTEMA ANULAR HETEROCICLICO AROMATICO BICICLICO. SON COMPUESTOS PREFERIDOS LOS DE FORMULA (i), (ii), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA METILTRANSFERASA PRMT5 SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS AUTOINMUNITARIOS, CANCER, ENFERMEDAD NEURODEGENERATIVA
PE2018000306A 2015-08-26 2016-08-25 Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5 PE20180929A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562209941P 2015-08-26 2015-08-26
EP15184011 2015-09-07
US201662306233P 2016-03-10 2016-03-10

Publications (1)

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PE20180929A1 true PE20180929A1 (es) 2018-06-08

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PE2022000450A PE20221629A1 (es) 2015-08-26 2016-08-25 Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5
PE2018000306A PE20180929A1 (es) 2015-08-26 2016-08-25 Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5

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Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI791251B (zh) * 2015-08-26 2023-02-01 比利時商健生藥品公司 使用作為ｐｒｍｔ５抑制劑之新穎經６-６雙環芳香環取代之核苷類似物
US10898504B2 (en) * 2016-03-10 2021-01-26 Janssen Pharmaceutica Nv Substituted nucleoside analogues for use as PRMT5 inhibitors
CA2969295A1 (en) * 2016-06-06 2017-12-06 Pfizer Inc. Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor
LT3512857T (lt) 2016-09-14 2021-04-12 Janssen Pharmaceutica Nv Menin-mll sąveikos spirobicikliniai inhibitoriai
US10611778B2 (en) 2016-09-14 2020-04-07 Janssen Pharmaceutica Nv Fused bicyclic inhibitors of menin-MLL interaction
US12084462B2 (en) 2016-09-14 2024-09-10 Janssen Pharmaceutica Nv Spiro bicyclic inhibitors of menin-MLL interaction
WO2018065365A1 (en) 2016-10-03 2018-04-12 Janssen Pharmaceutica Nv Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
EP3519413A1 (en) * 2016-10-03 2019-08-07 Janssen Pharmaceutica NV Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
MX391405B (es) 2016-12-15 2025-03-21 Janssen Pharmaceutica Nv Inhibidores de azepano de la interacción menina-mll.
GB201700526D0 (en) * 2017-01-12 2017-03-01 Univ Of Hull Therapeutic use
PE20191359A1 (es) 2017-02-27 2019-10-01 Janssen Pharmaceutica Nv Uso de biomarcadores en la identificacion de pacientes con cancer que seran sensibles al tratamiento con un inhibidor de prmt5
BR112020002736A2 (pt) 2017-08-09 2020-07-28 Prelude Therapeutics, Incorporated inibidores seletivos da proteína arginina metiltransferase 5 (prmt5)
CA3079545A1 (en) * 2017-10-26 2019-05-02 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
CA3084253A1 (en) * 2017-12-05 2019-06-13 Angex Pharmaceutical, Inc. Heterocyclic compounds as prmt5 inhibitors
MX2020005944A (es) 2017-12-08 2020-08-24 Janssen Pharmaceutica Nv Analogos espirobiciclicos novedosos.
EP3724190B1 (en) * 2017-12-13 2022-07-06 Lupin Limited Substituted bicyclic heterocyclic compounds as prmt5 inhibitors
US11396517B1 (en) 2017-12-20 2022-07-26 Janssen Pharmaceutica Nv Exo-aza spiro inhibitors of menin-MLL interaction
US10711007B2 (en) 2018-03-14 2020-07-14 Prelude Therapeutics Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
DK3765461T3 (da) 2018-03-14 2023-11-20 Prelude Therapeutics Inc Selektive protein argininmethyltransferase 5 (prmt5)-hæmmere
WO2020033285A1 (en) * 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
MA53287A (fr) * 2018-08-07 2022-05-11 Merck Sharp & Dohme Inhibiteurs de prmt5
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3897667A4 (en) 2018-12-21 2023-04-19 Memorial Sloan Kettering Cancer Center SALICYL-ADENOSINE MONOSULFAMATE ANALOGS AND THEIR USES
CN109400545B (zh) * 2018-12-24 2022-03-25 济南大学 一种精氨酸甲基转移酶5抑制剂及其应用
CN109369507A (zh) * 2018-12-26 2019-02-22 重庆市碚圣医药科技股份有限公司 一种n-(2,2-二乙氧基乙基)邻苯二甲酰亚胺的提纯方法
WO2020168125A1 (en) * 2019-02-13 2020-08-20 Prelude Therapeutics, Incorporated Selective inhibitor of protein arginine methyltransferase 5 (prmt5)
WO2020190073A1 (ko) * 2019-03-20 2020-09-24 한국화학연구원 신규한 아졸로피리미딘 헤테로고리 화합물을 유효 성분으로 함유하는 약제학적 조성물
BR112021019125A2 (pt) * 2019-03-25 2021-11-30 1200 Pharma Llc Inibidores de prmt5 e usos dos mesmos
WO2020205867A1 (en) 2019-04-02 2020-10-08 Aligos Therapeutics, Inc. Compounds targeting prmt5
JP2022527556A (ja) * 2019-04-05 2022-06-02 プレリュード・セラピューティクス・インコーポレイテッド プロテインアルギニンメチルトランスフェラーゼ５の選択的阻害剤
US12440506B2 (en) 2019-04-05 2025-10-14 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
CA3141855A1 (en) * 2019-05-30 2020-12-03 Angex Pharmaceutical, Inc. Heterocyclic compounds as prmt5 inhibitors
TW202112375A (zh) 2019-06-06 2021-04-01 比利時商健生藥品公司 使用ｐｒｍｔ５抑制劑治療癌症之方法
ES2967457T3 (es) 2019-06-10 2024-04-30 Lupin Ltd Inhibidores de PRMT5
JOP20210327A1 (ar) 2019-06-12 2023-01-30 Janssen Pharmaceutica Nv مركبات وسيطة سبيرو ثنائية الحلقة جديدة
EP4031555A1 (en) 2019-09-18 2022-07-27 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
JP2022553077A (ja) * 2019-10-21 2022-12-21 アクセント・セラピューティクス・インコーポレイテッド Ｍｅｔｔｌ３モジュレーター
US12447152B2 (en) * 2019-10-22 2025-10-21 Lupin Limited Pharmaceutical combination of PRMT5 inhibitors
GB201915447D0 (en) * 2019-10-24 2019-12-11 Johnson Matthey Plc Polymorphs of avapritinib and methods of preparing the polymorphs
EP4069698A1 (en) * 2019-12-03 2022-10-12 Lupin Limited Substituted nucleoside analogs as prmt5 inhibitors
US12441730B2 (en) 2019-12-17 2025-10-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
UA129208C2 (uk) 2019-12-19 2025-02-05 Янссен Фармацевтика Нв Заміщені спіропохідні з прямим ланцюгом
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
CN115135383B (zh) 2020-02-18 2024-06-11 吉利德科学公司 抗病毒化合物
CN111233869B (zh) * 2020-03-12 2022-09-16 杭州新博思生物医药有限公司 用于制备瑞德西韦关键中间体的新化合物及其制备方法
US20220112194A1 (en) * 2020-04-01 2022-04-14 Aligos Therapeutics, Inc. Compounds targeting prmt5
US20240101589A1 (en) * 2020-10-08 2024-03-28 Strom Therapeutics Limited Inhibitors of mettl3
CN112645875A (zh) * 2020-12-09 2021-04-13 深圳海王医药科技研究院有限公司 一种盐酸丙卡特罗杂质的制备方法
JP7688152B2 (ja) 2021-04-16 2025-06-03 ギリアード サイエンシーズ， インコーポレイテッド アミドを使用してカルバヌクレオシドを調製する方法
CN113234079B (zh) * 2021-04-30 2022-02-01 上海湃隆生物科技有限公司 用作prmt5抑制剂的核苷类似物
CN117157297A (zh) * 2021-07-20 2023-12-01 上海齐鲁制药研究中心有限公司 Prmt5抑制剂
CN115703796A (zh) * 2021-08-09 2023-02-17 苏州恩泰新材料科技有限公司 一种瑞德西韦重要中间体制备方法
KR20240049311A (ko) 2021-08-18 2024-04-16 길리애드 사이언시즈, 인코포레이티드 인지질 화합물 및 이의 제조 및 사용 방법
GB202117230D0 (en) 2021-11-29 2022-01-12 Argonaut Therapeutics Ltd Peptide vaccine
GB202203588D0 (en) 2022-03-15 2022-04-27 Argonaut Therapeutics Ltd Cancer diagnostic
CN116655638B (zh) * 2022-05-12 2024-01-26 上海齐鲁制药研究中心有限公司 氘代prmt5抑制剂
CN116003339B (zh) * 2022-12-01 2024-06-28 南京师范大学 一种巨噬细胞迁移抑制因子mif双光子荧光探针及其制备方法和应用
WO2024170488A1 (en) 2023-02-13 2024-08-22 Astrazeneca Ab Prmt5 inhibitor for use in cancer therapy
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
EP4553080A1 (en) 2023-11-07 2025-05-14 Ustav Organicke Chemie a Biochemie AV CR, v.v.i. Nucleoside derivatives as antiviral agents against coronaviruses
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4224438A (en) 1970-07-14 1980-09-23 Boehringer Mannheim Gmbh Adenosine-5'-carboxylic acid amides
US6143749A (en) 1995-06-07 2000-11-07 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
AU2002351077A1 (en) 2001-11-05 2003-05-19 Exiqon A/S Oligonucleotides modified with novel alpha-l-rna analogues
US7034147B2 (en) 2001-11-29 2006-04-25 Irm Llc Nucleoside analog libraries
RU2317994C2 (ru) * 2002-02-19 2008-02-27 Си Ви Терапьютикс, Инк. Частичные и полные агонисты аденозиновых рецепторов а1
US20040043959A1 (en) 2002-03-04 2004-03-04 Bloom Laura A. Combination therapies for treating methylthioadenosine phosphorylase deficient cells
US7144674B2 (en) * 2002-03-20 2006-12-05 Sumitomo Chemical Company, Limited Positive resist composition
AU2002951247A0 (en) * 2002-09-06 2002-09-19 Alchemia Limited Compounds that interact with kinases
US20060167241A1 (en) 2003-07-15 2006-07-27 Mitsui Chemicals, Inc. Method for synthesizing cyclic bisdinucleoside
EP1694642A4 (en) 2003-12-19 2010-10-06 Koronis Pharmaceuticals Inc MUTAGENIC HETEROCYCLES
EP1844062A2 (en) 2005-01-21 2007-10-17 Methylgene, Inc. Inhibitors of dna methyltransferase
WO2008001101A2 (en) 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
US20080132525A1 (en) 2006-12-04 2008-06-05 Methylgene Inc. Inhibitors of DNA Methyltransferase
AU2009298802A1 (en) 2008-09-23 2010-04-08 Alnylam Pharmaceuticals, Inc. Chemical modifications of monomers and oligonucleotides with cycloaddition
WO2011075665A2 (en) 2009-12-18 2011-06-23 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
US9029343B2 (en) 2010-12-03 2015-05-12 Epizyme, Inc. Modulators of histone methyltransferase, and methods of use thereof
BR112013013668A2 (pt) * 2010-12-03 2016-09-06 Epizyme Inc moduladores 7-deazapurina de histona metiltransferase, e métodos de uso dos mesmos
CN103354808B (zh) 2010-12-16 2016-08-10 Abbvie公司 抗病毒化合物
WO2012138530A1 (en) 2011-04-04 2012-10-11 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services 2'-o-aminooxymethyl nucleoside derivatives for use in the synthesis and modification of nucleosides, nucleotides and oligonucleotides
WO2013062943A1 (en) 2011-10-24 2013-05-02 Glaxosmithkline Intellectual Property Development Limited New compounds
WO2013151975A1 (en) 2012-04-02 2013-10-10 Northeastern University Compositions and methods for the inhibition of methyltransferases
WO2014035140A2 (en) 2012-08-30 2014-03-06 Kainos Medicine, Inc. Compounds and compositions for modulating histone methyltransferase activity
US20140100184A1 (en) 2012-08-31 2014-04-10 Baylor College Of Medicine Selective inhibitors of histone methyltransferase dot1l
CA2899363A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP2935243B1 (en) 2012-12-21 2018-03-14 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
SI2935222T1 (sl) 2012-12-21 2019-02-28 Epizyme Inc. Inhibitorji PRMT5 in njihove uporabe
US8906900B2 (en) 2012-12-21 2014-12-09 Epizyme, Inc. PRMT5 inhibitors and uses thereof
EP2975938A4 (en) 2013-03-15 2017-02-15 Ohio State Innovation Foundation Inhibitors of prmt5 and methods of their use
WO2015106025A1 (en) 2014-01-09 2015-07-16 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
EP3160477A4 (en) 2014-06-25 2018-07-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
PT3164130T (pt) 2014-07-01 2019-11-18 Millennium Pharm Inc Compostos de heteroaril úteis como inibidores de enzima ativadora de sumo
SG11201706050WA (en) 2015-02-24 2017-09-28 Pfizer Substituted nucleoside derivatives useful as anticancer agents
TWI791251B (zh) 2015-08-26 2023-02-01 比利時商健生藥品公司 使用作為ｐｒｍｔ５抑制劑之新穎經６-６雙環芳香環取代之核苷類似物
WO2017153186A1 (en) 2016-03-10 2017-09-14 Janssen Pharmaceutica Nv Substituted nucleoside analogues for use as prmt5 inhibitors
WO2018065365A1 (en) 2016-10-03 2018-04-12 Janssen Pharmaceutica Nv Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
EP3519413A1 (en) * 2016-10-03 2019-08-07 Janssen Pharmaceutica NV Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
PE20191359A1 (es) 2017-02-27 2019-10-01 Janssen Pharmaceutica Nv Uso de biomarcadores en la identificacion de pacientes con cancer que seran sensibles al tratamiento con un inhibidor de prmt5
MX2020005944A (es) 2017-12-08 2020-08-24 Janssen Pharmaceutica Nv Analogos espirobiciclicos novedosos.

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