BR112022019057A2 - Aminotiazóis substituídos como inibidores de dgkzeta para ativação imune - Google Patents

Aminotiazóis substituídos como inibidores de dgkzeta para ativação imune

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Publication number
BR112022019057A2
BR112022019057A2 BR112022019057A BR112022019057A BR112022019057A2 BR 112022019057 A2 BR112022019057 A2 BR 112022019057A2 BR 112022019057 A BR112022019057 A BR 112022019057A BR 112022019057 A BR112022019057 A BR 112022019057A BR 112022019057 A2 BR112022019057 A2 BR 112022019057A2
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BR
Brazil
Prior art keywords
compounds
dgkzeta
inhibitors
immune activation
substituted aminothiazoles
Prior art date
Application number
BR112022019057A
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English (en)
Inventor
Schmees Norbert
Röhn Ulrike
Kirchhoff Dennis
Petersen Kirstin
Thanh Uyen Nguyen Thi
GREES Mareike
Werbeck Nicolas
Boemer Ulf
Bader Benjamin
Stoeckigt Detlef
Kosemund Dirk
Offringa Rienk
Link Corinna
Nowak-Reppel Katrin
Original Assignee
Bayer Ag
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Publication date
Application filed by Bayer Ag filed Critical Bayer Ag
Publication of BR112022019057A2 publication Critical patent/BR112022019057A2/pt

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
    • C07D277/38—Nitrogen atoms
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    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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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
    • A61K31/425—Thiazoles
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    • 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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    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

AMINOTIAZÓIS SUBSTITUÍDOS COMO INIBIDORES DE DGKZETA PARA ATIVAÇÃO IMUNE. A presente invenção refere-se a compostos de aminotiazol da fórmula geral (I): (I), em que R1, R2, R3 e R4 são conforme definido no presente documento, métodos de preparo dos referidos compostos, compostos intermediários úteis para a preparação de compostos referidos, composições farmacêuticas e combinações que incluam os referidos compostos e o uso dos referidos para o fabrico de composições farmacêuticas para o tratamento e/ou profilaxia de doenças, em particular de distúrbios regulamentadas por diacilglicerol quinase zeta ( DGKZeta ), como agente único ou em combinação com outros ingredientes ativos.
BR112022019057A 2020-04-24 2021-04-20 Aminotiazóis substituídos como inibidores de dgkzeta para ativação imune BR112022019057A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20171280 2020-04-24
PCT/EP2021/060167 WO2021214019A1 (en) 2020-04-24 2021-04-20 Substituted aminothiazoles as dgkzeta inhibitors for immune activation

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BR112022019057A2 true BR112022019057A2 (pt) 2022-11-08

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US (3) US20230167078A1 (pt)
EP (2) EP4139287A1 (pt)
JP (2) JP2023522250A (pt)
KR (1) KR20230005247A (pt)
CN (2) CN115697979A (pt)
AR (1) AR121929A1 (pt)
AU (1) AU2021261524A1 (pt)
BR (1) BR112022019057A2 (pt)
CA (2) CA3180670A1 (pt)
CL (1) CL2022002919A1 (pt)
CO (1) CO2022014876A2 (pt)
CR (1) CR20220536A (pt)
DO (1) DOP2022000223A (pt)
EC (1) ECSP22080829A (pt)
IL (1) IL297499A (pt)
MX (1) MX2022013388A (pt)
PE (1) PE20230322A1 (pt)
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WO2021130638A1 (en) 2019-12-24 2021-07-01 Carna Biosciences, Inc. Diacylglycerol kinase modulating compounds
PE20230322A1 (es) 2020-04-24 2023-02-22 Bayer Ag Aminotiazoles sustituidos como inhibidores de dgkzeta para la activacion inmune
KR20230116838A (ko) 2020-11-30 2023-08-04 아스테라스 세이야쿠 가부시키가이샤 헤테로아릴카르복시아미드 화합물
KR20240023629A (ko) 2021-06-23 2024-02-22 길리애드 사이언시즈, 인코포레이티드 디아실글리세롤 키나제 조절 화합물
MX2023014762A (es) 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
CN117396478A (zh) 2021-06-23 2024-01-12 吉利德科学公司 二酰基甘油激酶调节化合物
CN117377671A (zh) 2021-06-23 2024-01-09 吉利德科学公司 二酰基甘油激酶调节化合物
WO2024036100A1 (en) * 2022-08-08 2024-02-15 Bristol-Myers Squibb Company Substituted tetrazolyl compounds useful as t cell activators
WO2024165469A1 (en) 2023-02-06 2024-08-15 Bayer Aktiengesellschaft Combinations of dgk (diacylglycerol kinase) inhibitors and immune checkpoint inhibitors and modulators

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