PE20231098A1 - Aminoquinolonas sustituidas como inhibidores de dgk alfa para la activacion inmune - Google Patents

Aminoquinolonas sustituidas como inhibidores de dgk alfa para la activacion inmune

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Publication number
PE20231098A1
PE20231098A1 PE2022000967A PE2022000967A PE20231098A1 PE 20231098 A1 PE20231098 A1 PE 20231098A1 PE 2022000967 A PE2022000967 A PE 2022000967A PE 2022000967 A PE2022000967 A PE 2022000967A PE 20231098 A1 PE20231098 A1 PE 20231098A1
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Peru
Prior art keywords
alkyl
alkoxy
cycloalkyl
substituted
oxo
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PE2022000967A
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English (en)
Inventor
Norbert Schmees
Lars Wortmann
Dennis Kirchhoff
Thi Thanh Uyen Nguyen
Nicolas Werbeck
Ulf Bomer
Kirstin Petersen
Christina Kober
Detlef Stockigt
Christian Lechner
Robin Michael Meier
Simon Anthony Herbert
Isabel Patrizia Kerschgens
Dirk Kosemund
Rienk Offringa
Mareike Grees
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Bayer Ag
Bayer Pharma AG
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Publication of PE20231098A1 publication Critical patent/PE20231098A1/es

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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/47Quinolines; Isoquinolines
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    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
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    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/4965Non-condensed pyrazines
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    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • 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
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Abstract

Refiere a compuestos de aminoquinolona de la formula general (I), en donde R1 es -C(=O)N(H)C2H5, -C(=O)N(CH3)2, entre otros; R2 se selecciona entre fenilo, naftilo y heteroarilo de 5 a 10 miembros, el cual se sustituye 1-4 veces con hidroxialquilo C1-C6, haloalcoxi C1-C6, entre otros; R3, R4 y R5 se seleccionan de (C1-C2-alcoxi)-(alquilo C1-C6)-, (alcoxi C1-C2)-(alcoxi C1-C6)-, cicloalquiloxi C3-C6, entre otros; R6 y R7 se seleccionan de alquilo C1-C4, alcoxi C1-C4, hidroxi, entre otros; R8 se selecciona de metilo y etilo; R9 y R10 junto al atomo de nitrogeno al que estan unidos representan un grupo heterocicloalquilo de 4 a 7 miembros sustituido con alquilo C1-C4, cicloalquilo C3-C4, hidroxi y oxo; R12 y R15 son H o alquilo C1-C4; R11, R13 y R14 se seleccionan de fenilo y heteroarilo de 5-6 miembros, el cual se sustituye con haloalquilo C1-C2, cicloalquilo C3-C4, -N(R9)(R10), entre otros; R16 se selecciona de alquilo C1-C4, cicloalquilo C3-C4 y haloalquilo C2-C4; R17 representa un grupo heterocicloalquilo de 4 a 7 miembros sustituido 1-3 veces con alquilo C1-C4, cicloalquilo C3-C4, alcoxi C1-C4, hidroxi y oxo; R18 y R19 son H, metilo o etilo, R20 es un grupo (heterocicloalquilo de 4 a 7 miembros)-(alquilo C1-C4) ; y m y n son 1, 2 o 3. Dichos compuestos son 4-{4-[5-(metanosulfonil)-1,3-benzoxazol-2-il]-4-metilpiperidin-1-il}-1-metil-2-oxo-1,2-dihidroquinolina-3-carbonitrilo, entre otros. Ademas, la presente refiere a su metodo de preparacion con compuestos intermedios de formulas (II) y (III) y a una composicion farmaceutica que los compone junto a un inhibidor de DGK? para el tratamiento o profilaxis de cancer, o una afeccion con una respuesta inmune desregulada, o un trastorno asociado con la senalizacion aberrante de DGK?.
PE2022000967A 2019-11-28 2020-11-24 Aminoquinolonas sustituidas como inhibidores de dgk alfa para la activacion inmune PE20231098A1 (es)

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EP19212252 2019-11-28
EP20181065 2020-06-19
PCT/EP2020/083198 WO2021105117A1 (en) 2019-11-28 2020-11-24 Substituted aminoquinolones as dgkalpha inhibitors for immune activation

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US (1) US20230148194A1 (es)
EP (1) EP4065574A1 (es)
JP (1) JP2023504249A (es)
KR (1) KR20220122637A (es)
CN (1) CN115003665A (es)
AU (1) AU2020393384A1 (es)
BR (1) BR112022010112A2 (es)
CA (1) CA3163105A1 (es)
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JO (1) JOP20220131A1 (es)
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PE (1) PE20231098A1 (es)
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