CA3163105A1 - Substituted aminoquinolones as dgkalpha inhibitors for immune activation - Google Patents

Substituted aminoquinolones as dgkalpha inhibitors for immune activation

Info

Publication number
CA3163105A1
CA3163105A1 CA3163105A CA3163105A CA3163105A1 CA 3163105 A1 CA3163105 A1 CA 3163105A1 CA 3163105 A CA3163105 A CA 3163105A CA 3163105 A CA3163105 A CA 3163105A CA 3163105 A1 CA3163105 A1 CA 3163105A1
Authority
CA
Canada
Prior art keywords
methy1
oxo
dihydroquinoline
group
carbonitrile
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3163105A
Other languages
English (en)
French (fr)
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
Benjamin Bader
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer AG
Bayer Pharma AG
Original Assignee
Bayer AG
Bayer Pharma AG
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 Bayer AG, Bayer Pharma AG filed Critical Bayer AG
Publication of CA3163105A1 publication Critical patent/CA3163105A1/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—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
    • A61K31/4545—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen 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
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA3163105A 2019-11-28 2020-11-24 Substituted aminoquinolones as dgkalpha inhibitors for immune activation Pending CA3163105A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP19212252.1 2019-11-28
EP19212252 2019-11-28
EP20181065.2 2020-06-19
EP20181065 2020-06-19
PCT/EP2020/083198 WO2021105117A1 (en) 2019-11-28 2020-11-24 Substituted aminoquinolones as dgkalpha inhibitors for immune activation

Publications (1)

Publication Number Publication Date
CA3163105A1 true CA3163105A1 (en) 2021-06-03

Family

ID=73476184

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3163105A Pending CA3163105A1 (en) 2019-11-28 2020-11-24 Substituted aminoquinolones as dgkalpha inhibitors for immune activation

Country Status (22)

Country Link
US (2) US12478621B2 (https=)
EP (1) EP4065574A1 (https=)
JP (2) JP7523542B2 (https=)
KR (1) KR20220122637A (https=)
CN (4) CN115003665B (https=)
AU (1) AU2020393384A1 (https=)
BR (1) BR112022010112A2 (https=)
CA (1) CA3163105A1 (https=)
CL (1) CL2022001406A1 (https=)
CO (1) CO2022007005A2 (https=)
CR (1) CR20220236A (https=)
DO (1) DOP2022000110A (https=)
EC (1) ECSP22041839A (https=)
GE (2) GEP20247646B (https=)
IL (1) IL293213A (https=)
JO (1) JOP20220131A1 (https=)
MX (1) MX2022006466A (https=)
PE (1) PE20231098A1 (https=)
PH (1) PH12022551260A1 (https=)
SA (1) SA522432734B1 (https=)
TW (1) TWI894183B (https=)
WO (1) WO2021105117A1 (https=)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20220236A (es) 2019-11-28 2022-10-03 Bayer Pharma AG Aminoquinolonas sustituidas como inhibidores de dgk alfa para la activación inmune
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
CA3162979A1 (en) 2019-12-23 2021-07-01 Upender Velaparthi Substituted piperazine derivatives useful as t cell activators
BR112022012179A2 (pt) 2019-12-23 2022-09-06 Bristol Myers Squibb Co Compostos de quinazolina substituída úteis como ativadores de célula t
IL294032A (en) 2019-12-24 2022-08-01 Carna Biosciences Inc Compounds that regulate diacylglycerol kinase
AU2022299051B2 (en) * 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
MX2023014762A (es) * 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
JP7686091B2 (ja) 2021-06-23 2025-05-30 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
JP7651018B2 (ja) * 2021-06-23 2025-03-25 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
WO2023011456A1 (en) * 2021-08-03 2023-02-09 Beigene, Ltd. Pyrazolopyridinone compounds
EP4486741A4 (en) * 2022-03-01 2026-04-08 Insilico Medicine Ip Ltd Diacylglycerol Kinase (DGK) Alpha Inhibitors and Their Uses
CN117088874A (zh) * 2022-05-19 2023-11-21 轩竹生物科技股份有限公司 二酰甘油激酶抑制剂及其用途
US12600723B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US12600722B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
JP2025163312A (ja) * 2022-09-06 2025-10-29 小野薬品工業株式会社 ジアシルグリセロールキナーゼαおよび／またはζ阻害活性を有する化合物およびその医薬用途
CN116283803A (zh) * 2022-12-05 2023-06-23 上海旭东海普药业有限公司 一种氟马西尼中间体的制备方法
EP4661869A1 (en) 2023-02-06 2025-12-17 Bayer Aktiengesellschaft Combinations of dgk (diacylglycerol kinase) inhibitors and immune checkpoint inhibitors and modulators
WO2025030002A2 (en) * 2023-08-02 2025-02-06 Arvinas Operations, Inc. Dgk targeting compounds and uses thereof
WO2025051110A1 (en) * 2023-09-04 2025-03-13 Insilico Medicine Ip Limited Combinations treatments of diacylglycerol kinase (dgk) alpha inhibitors and other therapies
CN119143671B (zh) * 2024-11-21 2025-05-16 九洲药业(杭州)有限公司 一种插羰反应一锅法简便合成喹啉酮衍生物的方法

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4435479A1 (de) 1994-10-04 1996-04-11 Bayer Ag Chinolon- und Naphthyridoncarbonsäure-Derivate
ATE255575T1 (de) 1998-09-29 2003-12-15 Wyeth Corp Substituierte 3-cyanochinoline als protein tyrosine kinase inhibitoren
SE0002320D0 (sv) * 1999-10-25 2000-06-21 Active Biotech Ab Malignant tumors
WO2003091247A2 (en) 2002-04-25 2003-11-06 Pharmacia Corporation Piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
TWI331034B (en) 2002-07-08 2010-10-01 Piramal Life Sciences Ltd Inhibitors of cyclin-dependent kinases and their use
US7884127B2 (en) * 2002-07-08 2011-02-08 Pirimal Life Sciences Ltd. Inhibitors of cyclin dependent kinases and their use
JP2005170792A (ja) 2002-11-22 2005-06-30 Mitsubishi Pharma Corp Ｌ−プロリン誘導体およびその医薬としての用途。
TW200418829A (en) 2003-02-14 2004-10-01 Avanir Pharmaceutics Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
DE10337191A1 (de) * 2003-08-13 2005-03-17 Bayer Healthcare Ag Neue Verwendung von Chinolon-Antibiotika
JP2007528402A (ja) 2004-03-09 2007-10-11 エラン ファーマシューティカルズ，インコーポレイテッド 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬
US20060019975A1 (en) 2004-07-23 2006-01-26 Pfizer Inc Novel piperidyl derivatives of quinazoline and isoquinoline
EP1807074B1 (en) 2004-11-03 2013-10-23 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
TW200800999A (en) 2005-09-06 2008-01-01 Astrazeneca Ab Novel compounds
GB0605689D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic compounds
WO2010042867A2 (en) 2008-10-09 2010-04-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
FR2953834B1 (fr) 2009-12-10 2012-01-13 Galderma Res & Dev Nouveaux composes 4-(azacycloalkyl)-benzene-1,3-diol comme inhibiteurs de la tyrosinase, leur procede de preparation et leur utilisation en medecine humaine ainsi qu'en cosmetique
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
US9050334B2 (en) 2010-07-16 2015-06-09 Innov88 Llc MIF inhibitors and their uses
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2012142498A2 (en) 2011-04-13 2012-10-18 Innovimmune Biotherapeutics, Inc. Mif inhibitors and their uses
MX2014002542A (es) 2011-08-29 2014-07-09 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
EP2892534B8 (en) 2012-09-06 2021-09-15 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN110627770A (zh) 2013-11-18 2019-12-31 福马疗法公司 作为bet溴域抑制剂的四氢喹啉组成物
US9273067B2 (en) 2014-02-19 2016-03-01 Bristol-Myers Squibb Company Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
HK1246593A1 (zh) 2015-06-04 2018-09-14 Kura Oncology, Inc. 用於抑制menin蛋白与mll蛋白的相互作用的方法及组合物
JPWO2017014170A1 (ja) 2015-07-17 2018-04-26 武田薬品工業株式会社 複素環化合物
US10376504B2 (en) 2015-07-29 2019-08-13 Merck, Sharp & Dohme Corp. Substituted quinolinones as PDE9 inhibitors
CN108699055B (zh) 2015-12-13 2020-10-23 杭州英创医药科技有限公司 用作抗癌药物的杂环化合物
PT3889145T (pt) 2015-12-17 2024-04-02 Merck Patent Gmbh 8-ciano-5-piperidino-quinolinas como antagonistas de tlr7/8 e suas utilizações para tratamento de distúrbios imunitários
WO2017158619A1 (en) 2016-03-15 2017-09-21 Natco Pharma Limited A modified process for the preparation of ceritinib and amorphous form of ceritinib
AU2018340475B2 (en) 2017-09-28 2023-01-19 Transthera Sciences (Nanjing), Inc. PDE9 inhibitor and use thereof
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
CN111511729A (zh) 2017-12-19 2020-08-07 默克专利股份公司 Tlr7/8拮抗剂及其用途
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CN112585139B (zh) 2018-06-27 2023-12-01 百时美施贵宝公司 用作t细胞激活剂的萘啶酮化合物
KR102767739B1 (ko) 2018-06-27 2025-02-12 브리스톨-마이어스 스큅 컴퍼니 T 세포 활성화제로서 유용한 치환된 나프티리디논 화합물
CA3108099A1 (en) 2018-07-31 2020-02-06 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
CN111410659B (zh) 2019-01-08 2023-08-15 药捷安康(南京)科技股份有限公司 Pde9抑制剂及其用途
CN111471059B (zh) 2019-01-23 2022-12-02 药捷安康(南京)科技股份有限公司 Pde9抑制剂及其用途
EP3919483A4 (en) 2019-01-29 2022-02-09 Brightgene Bio-medical Technology Co., Ltd. HETEROCYCLIC BENZOPYRIDONE COMPOUND AND USE THEREOF
WO2020182076A1 (zh) 2019-03-08 2020-09-17 南京药捷安康生物科技有限公司 磷酸二酯酶抑制剂的用途
SG11202110401WA (en) 2019-04-09 2021-10-28 Hoffmann La Roche Hexahydro-1h-pyrazino[1,2-a]pyrazine compounds for the treatment of autoimmune disease
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
CR20220236A (es) 2019-11-28 2022-10-03 Bayer Pharma AG Aminoquinolonas sustituidas como inhibidores de dgk alfa para la activación inmune
US20230062100A1 (en) 2019-11-28 2023-03-02 Bayer Aktiengesellschaft Substituted aminoquinolones as dgkalpha inhibitors for immune activation
US20230064809A1 (en) 2019-11-28 2023-03-02 Bayer Aktiengesellschaft Substituted aminoquinolones as dgkalpha inhibitors for immune activation

Also Published As

Publication number Publication date
US11998539B2 (en) 2024-06-04
KR20220122637A (ko) 2022-09-02
IL293213A (en) 2022-07-01
CN119523983A (zh) 2025-02-28
JP7523542B2 (ja) 2024-07-26
EP4065574A1 (en) 2022-10-05
SA522432734B1 (ar) 2025-05-22
TW202134230A (zh) 2021-09-16
CN115003665B (zh) 2024-11-08
BR112022010112A2 (pt) 2022-09-06
JOP20220131A1 (ar) 2023-01-30
AU2020393384A1 (en) 2022-06-09
CO2022007005A2 (es) 2022-06-10
US12478621B2 (en) 2025-11-25
CL2022001406A1 (es) 2023-03-10
MX2022006466A (es) 2022-08-17
US20230201186A1 (en) 2023-06-29
CN119564686A (zh) 2025-03-07
GEP20247646B (en) 2024-07-25
PE20231098A1 (es) 2023-07-18
GEAP202415986A (en) 2024-02-12
CN115003665A (zh) 2022-09-02
JP7802850B2 (ja) 2026-01-20
TWI894183B (zh) 2025-08-21
WO2021105117A1 (en) 2021-06-03
CN119424429A (zh) 2025-02-14
JP2024099684A (ja) 2024-07-25
DOP2022000110A (es) 2022-06-30
US20230148194A1 (en) 2023-05-11
CR20220236A (es) 2022-10-03
JP2023504249A (ja) 2023-02-02
ECSP22041839A (es) 2022-06-30
PH12022551260A1 (en) 2024-06-03

Similar Documents

Publication Publication Date Title
JP7802850B2 (ja) 免疫活性化のためのｄｇｋアルファ阻害剤としての置換アミノキノロン類
US20230062100A1 (en) Substituted aminoquinolones as dgkalpha inhibitors for immune activation
CA3163107A1 (en) Substituted aminoquinolones as dgkalpha inhibitors for immune activation
CA2956992C (en) 2-(MORPHOLIN-4-YL)-1,7-NAPHTHYRIDINES
EP4214204A1 (en) Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors
EP3532474A2 (en) 4,5-annulated 1,2,4-triazolones
AU2022258751A1 (en) Phosphorus derivatives as novel sos1 inhibitors
CA3070013A1 (en) Substituted pyrrolopyridine-derivatives
EP3390387A1 (en) Heteroarylbenzimidazole compounds
WO2022167627A1 (en) Map4k1 inhibitors
EA050445B1 (ru) Замещенные аминохинолоны в качестве ингибиторов dgkalpha для иммунной активации
EA048866B1 (ru) ЗАМЕЩЕННЫЕ АМИНОХИНОЛОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ DGKα ДЛЯ ИММУННОЙ АКТИВАЦИИ
HK40072887B (zh) 作为免疫活化的DGKα抑制剂的取代的氨基喹诺酮
HK40072887A (en) Substituted aminoquinolones as dgkalpha inhibitors for immune activation
WO2020048831A1 (en) 5-aryl-3,9-diazaspiro[5.5]undecan-2-one compounds

Legal Events

Date Code Title Description
D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D11-D117 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION RECEIVED

Effective date: 20241118

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241118

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D118 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20241223

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20250425

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D11-D155 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: ALL REQUIREMENTS FOR EXAMINATION DETERMINED COMPLIANT

Effective date: 20250429

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 5TH ANNIV.) - STANDARD

Year of fee payment: 5

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20251023

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20251023

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20251204

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20260326

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20260409

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20260409

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20260409