AR108223A1 - Derivados de 6-oxo-1,6-dihidro-piridin-3-il - Google Patents

Derivados de 6-oxo-1,6-dihidro-piridin-3-il

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Publication number
AR108223A1
AR108223A1 ARP170100985A ARP170100985A AR108223A1 AR 108223 A1 AR108223 A1 AR 108223A1 AR P170100985 A ARP170100985 A AR P170100985A AR P170100985 A ARP170100985 A AR P170100985A AR 108223 A1 AR108223 A1 AR 108223A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
hydrogen
cycloalkylalkyl
heterocyclylalkyl
Prior art date
Application number
ARP170100985A
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English (en)
Original Assignee
Celgene Quanticel Res Inc
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 Celgene Quanticel Res Inc filed Critical Celgene Quanticel Res Inc
Publication of AR108223A1 publication Critical patent/AR108223A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/08Bridged systems

Abstract

Composiciones que comprenden dichos compuestos, y el uso de dichos compuestos y composiciones para la regulación epigenética por inhibición del reconocimiento mediado por bromodominio de regiones de acetilo lisina de proteínas, tales como histonas. Dichas composiciones y métodos son útiles para el tratamiento de enfermedades mediadas por la señalización celular aberrante, tales como trastornos inflamatorios, cáncer y enfermedades neoplásicas. Reivindicación 1: Un compuesto, o una sal farmacéuticamente aceptable de dicho compuesto, que tiene la estructura de la fórmula (1) en donde, R² es hidrógeno, alquilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; X⁶ es C-H, C-F, C-Cl, C-Br o N; R⁵ es hidrógeno, halógeno, -CN, alquilo, cicloalquilo o alcoxi; R⁶ es hidrógeno, halógeno, -CN, alquilo, cicloalquilo, cicloalquilalquilo, -OR²² o N(R²²)₂; RA es un compuesto de fórmula (2); R¹³ es -Y-Z; Y se selecciona de un enlace, -CH₂- o -CH(alquilo C₁₋₄)-; Z se selecciona de -SO₂R²¹, -N(R²²)SO₂R²¹, -SO₂N(R²²)₂, -N(R²²)SO₂N(R²²)₂, -CON(R²²)₂, -N(R²²)CO₂R²¹, -N(R²²)CON(R²²)₂, -N(R²²)COR²¹, -COR²¹, -OC(O)N(R²²)₂, -OSO₂N(R²²)₂, -OSO₂R²¹, -N(R²²)SO₃R²¹, N(R²²)₂ o -CN; X² es N o C-R¹²; en donde R¹² es hidrógeno, halógeno, -CN, alquilo, cicloalquilo o alcoxi; X⁴ es N o C-R¹⁴; en donde R¹⁴ es hidrógeno, halógeno, -CN, alquilo, cicloalquilo o alcoxi; X es un enlace, -O-, -S-, -N(R⁷)-, -CH₂-, -CF(H)-, CF₂- o -CH(alquilo C₁₋₅)-; R⁷ es H o alquilo C₁₋₆; R¹ es alquilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; cada R²¹ se selecciona independientemente de alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; cada R²² se selecciona independientemente de hidrógeno, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; y con la condición de que el compuesto de fórmula (1) no sea N-[2-(2,4-difluorofenoxi)-6-(1,5-dimetil-6-oxopiridin-3-il)pirimidin-4-il]etansulfinamida.
ARP170100985A 2016-04-18 2017-04-18 Derivados de 6-oxo-1,6-dihidro-piridin-3-il AR108223A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662324279P 2016-04-18 2016-04-18

Publications (1)

Publication Number Publication Date
AR108223A1 true AR108223A1 (es) 2018-08-01

Family

ID=60039979

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170100985A AR108223A1 (es) 2016-04-18 2017-04-18 Derivados de 6-oxo-1,6-dihidro-piridin-3-il

Country Status (7)

Country Link
US (1) US10202360B2 (es)
EP (1) EP3445750A4 (es)
JP (2) JP2019513804A (es)
AR (1) AR108223A1 (es)
AU (1) AU2017252276A1 (es)
TW (1) TW201739744A (es)
WO (1) WO2017184462A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020516672A (ja) 2017-04-18 2020-06-11 セルジーン クオンティセル リサーチ,インク. 治療用化合物
CN110016014B (zh) * 2018-01-08 2023-02-17 中国科学院上海药物研究所 Ezh2抑制剂及其制备和抗肿瘤治疗中的应用
RU2020131507A (ru) 2018-03-29 2022-05-04 Боард Оф Реджентс, Де Юниверсити Оф Техас Систем Имидазопиперазиновые ингибиторы белков-активаторов транскрипции
US10899769B2 (en) 2018-04-06 2021-01-26 Board Of Regents, The University Of Texas System Imidazopiperazinone inhibitors of transcription activating proteins
MX2022000050A (es) 2019-07-02 2022-05-24 Nuvation Bio Inc Compuestos heterocíclicos como inhibidores de bromodominio extraterminal (bet).
US20230174545A1 (en) * 2020-04-29 2023-06-08 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
MX2023000056A (es) 2020-07-02 2023-04-12 Incyte Corp Compuestos tricíclicos de urea como inhibidores de la variante v617f de la cinasa de janus 2 (jak2 v617f).
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
CN112225738B (zh) * 2020-12-18 2021-04-13 北京鑫开元医药科技有限公司 作为tlr8激动剂的化合物、其制备方法、组合物及其用途
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
TW202302589A (zh) 2021-02-25 2023-01-16 美商英塞特公司 作為jak2 v617f抑制劑之螺環內醯胺
CN115703760A (zh) * 2021-08-11 2023-02-17 山东大学 2,4-二取代嘧啶类细胞周期蛋白依赖性激酶酶抑制剂及其制备方法和应用
CA3237199A1 (en) 2021-11-02 2023-05-11 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2011970A1 (en) 1970-03-13 1971-11-18 CH. Boehringer Sohn, 6507 Ingelheim Imidazo-(1, 2-a)- pyrimidines prepn
US3635667A (en) 1970-07-23 1972-01-18 Fmc Corp Drycleaning with hydrogen peroxide
BE786028A (fr) 1971-07-08 1973-01-08 Boehringer Sohn Ingelheim 2,3-dihydro-oxo-imidazo(1,2-a)-pyrimidines, leurs sels d'addition avec des acides et procedes pour les fabriquer
DE2356005A1 (de) 1973-11-09 1975-05-22 Boehringer Sohn Ingelheim Neue 7-amino-imidazo eckige klammer auf 1,2-a eckige klammer zu pyrimidine, diese enthaltende arzneimittel sowie verfahren zu deren herstellung
AU577105B2 (en) 1985-04-02 1988-09-15 T.P.O. :Pharmachim: Acylaminic penicillin derivatives
US6117940A (en) 1997-10-17 2000-09-12 Mjalli; Adnan M. M. Amino-ketone solid support templates
MXPA05002004A (es) 2002-09-26 2005-04-28 Pfizer Derivados de pirazol.
JP2005089352A (ja) 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
JP4718467B2 (ja) 2003-09-23 2011-07-06 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリノンカリウムチャネル阻害剤
KR100703068B1 (ko) 2003-12-30 2007-04-05 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
JP4978192B2 (ja) 2004-04-01 2012-07-18 アステラス製薬株式会社 ピラジン誘導体およびその医薬的使用
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
US7452892B2 (en) 2005-06-17 2008-11-18 Bristol-Myers Squibb Company Triazolopyrimidine cannabinoid receptor 1 antagonists
MX2008000956A (es) 2005-07-26 2008-03-27 Sanofi Aventis Derivados de ciclohexilaminisoquinolona en calidad de inhibidores de rho-quinasa.
PT1910333E (pt) 2005-07-26 2013-08-01 Sanofi Sa Derivados de isoquinolona substituída com piperidinilo como inibidores da rho-cinase
US20070099911A1 (en) 2005-10-28 2007-05-03 Wyeth Pyrroloquinolinone derivatives as 5-hydroxytryptamine-6 ligands
WO2008039882A1 (en) * 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist
MY155009A (en) 2006-12-27 2015-08-28 Sanofi Aventis Cycloalkylamine substituted isoquinolone derivatives
BRPI0720862A2 (pt) 2006-12-27 2014-02-25 Sanofi Aventis Derivados de isoquinolina e isoquinolinona substituídos como inibidores de rho-cinase
PT2102164E (pt) 2006-12-27 2011-01-21 Sanofi Aventis Derivados de isoquinolina e de isoquinolinona substituída com cicloalquilamina
TW200906825A (en) * 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
WO2009029214A1 (en) 2007-08-23 2009-03-05 Amgen Inc. Isoquinolone derivatives as phosphodiesterase 10 inhibitors
CA2712897A1 (en) 2008-01-30 2009-08-06 Pharmacopeia, Inc. Substituted spirocyclic piperidine derivatives as histamine-3 (h3) receptor ligands
WO2009158396A1 (en) 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Diketopiperidine derivatives as hiv attachment inhibitors
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
HUE043536T2 (hu) 2009-10-06 2019-08-28 Millennium Pharm Inc PDK1 inhibitorként alkalmazható heterociklusos vegyületek
ES2792799T3 (es) 2010-06-28 2020-11-12 Merck Patent Gmbh [1,8]naftiridinas 2,4-diaril-sustituidas como inhibidores de quinasas para su uso contra el cáncer
WO2012020786A1 (ja) * 2010-08-11 2012-02-16 日本新薬株式会社 医薬組成物
WO2012101654A2 (en) * 2011-01-25 2012-08-02 Sphaera Pharma Pvt. Ltd Novel triazine compounds
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
BR112014010368A2 (pt) 2011-10-31 2017-04-25 Xenon Pharmaceuticals Inc biaril éter sulfonamidas e seu uso como agentes terapêuticos
CN103183675A (zh) 2011-12-27 2013-07-03 山东轩竹医药科技有限公司 磷酸二酯酶-4抑制剂
KR20150015501A (ko) * 2012-05-30 2015-02-10 니뽄 신야쿠 가부시키가이샤 방향족 복소환 유도체 및 의약
AU2013365926B9 (en) * 2012-12-21 2019-01-17 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
MX2015011984A (es) * 2013-03-12 2015-12-15 Abbvie Inc Inhibidores de bromodominio de dihidro-pirrolopiridinona.
US9670221B2 (en) * 2013-03-14 2017-06-06 Glaxosmithkline Intellectual Property (No. 2) Limited Furopyridines as bromodomain inhibitors
CA2907912A1 (en) * 2013-05-01 2014-11-06 F. Hoffmann-La Roche Ag C-linked heterocycloalkyl substituted pyrimidines and their uses
PL3640241T3 (pl) * 2013-10-18 2022-12-05 Celgene Quanticel Research, Inc. Inhibitory bromodomeny
HUE041546T2 (hu) * 2014-01-09 2019-05-28 Orion Corp Biciklusos heterociklusos származékvegyületek mint bromo doméninhibitorok
SG11201609981RA (en) * 2014-06-04 2016-12-29 Thomas Helledays Stiftelse För Medicinsk Forskning Mth1 inhibitors for treatment of inflammatory and autoimmune conditions
CN110023292B (zh) * 2016-07-18 2022-10-04 北京生命科学研究所 细胞凋亡抑制剂

Also Published As

Publication number Publication date
JP2022064967A (ja) 2022-04-26
WO2017184462A1 (en) 2017-10-26
EP3445750A4 (en) 2019-11-27
US10202360B2 (en) 2019-02-12
EP3445750A1 (en) 2019-02-27
JP2019513804A (ja) 2019-05-30
TW201739744A (zh) 2017-11-16
US20170298040A1 (en) 2017-10-19
AU2017252276A1 (en) 2018-11-15

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