JP7663603B2 - 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類 - Google Patents

免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類 Download PDF

Info

Publication number
JP7663603B2
JP7663603B2 JP2022564007A JP2022564007A JP7663603B2 JP 7663603 B2 JP7663603 B2 JP 7663603B2 JP 2022564007 A JP2022564007 A JP 2022564007A JP 2022564007 A JP2022564007 A JP 2022564007A JP 7663603 B2 JP7663603 B2 JP 7663603B2
Authority
JP
Japan
Prior art keywords
group
alkyl
phenyl
atom
compound
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.)
Active
Application number
JP2022564007A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023522250A5 (https=
JP2023522250A (ja
Inventor
シュミース,ノルバート
レーン,ウルリケ
キルヒホフ,デニス
ぺーターセン,キルスティン
グェン,ティ・タン・イエン
グリーズ,マライケ
ヴェルベック,ニコラス
ベマー,ウルフ
バデル,ベンジャミン
ストッキヒト,デトレフ
コセムンド,ディルク
オフリンガ,リエンク
リンク,コリナ
ノヴァク‐レッペル,カトリン
ローゼンペーター,ウルリッヒ
Original Assignee
バイエル・アクチエンゲゼルシヤフト
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 バイエル・アクチエンゲゼルシヤフト filed Critical バイエル・アクチエンゲゼルシヤフト
Publication of JP2023522250A publication Critical patent/JP2023522250A/ja
Publication of JP2023522250A5 publication Critical patent/JP2023522250A5/ja
Priority to JP2025062751A priority Critical patent/JP2025120943A/ja
Application granted granted Critical
Publication of JP7663603B2 publication Critical patent/JP7663603B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/454Non 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/695Silicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/10Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2827Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
JP2022564007A 2020-04-24 2021-04-20 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類 Active JP7663603B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025062751A JP2025120943A (ja) 2020-04-24 2025-04-04 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20171280 2020-04-24
EP20171280.9 2020-04-24
PCT/EP2021/060167 WO2021214019A1 (en) 2020-04-24 2021-04-20 Substituted aminothiazoles as dgkzeta inhibitors for immune activation

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2025062751A Division JP2025120943A (ja) 2020-04-24 2025-04-04 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類

Publications (3)

Publication Number Publication Date
JP2023522250A JP2023522250A (ja) 2023-05-29
JP2023522250A5 JP2023522250A5 (https=) 2025-02-25
JP7663603B2 true JP7663603B2 (ja) 2025-04-16

Family

ID=70464845

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2022564007A Active JP7663603B2 (ja) 2020-04-24 2021-04-20 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類
JP2022564009A Pending JP2023522251A (ja) 2020-04-24 2021-04-20 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類
JP2025062751A Pending JP2025120943A (ja) 2020-04-24 2025-04-04 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2022564009A Pending JP2023522251A (ja) 2020-04-24 2021-04-20 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類
JP2025062751A Pending JP2025120943A (ja) 2020-04-24 2025-04-04 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類

Country Status (32)

Country Link
US (3) US20230167103A1 (https=)
EP (2) EP4139286B1 (https=)
JP (3) JP7663603B2 (https=)
KR (1) KR20230005247A (https=)
CN (6) CN115697980B (https=)
AR (1) AR121929A1 (https=)
AU (1) AU2021261524A1 (https=)
CA (2) CA3180670A1 (https=)
CL (1) CL2022002919A1 (https=)
CO (1) CO2022014876A2 (https=)
CR (1) CR20220536A (https=)
DK (1) DK4139286T3 (https=)
DO (1) DOP2022000223A (https=)
EC (1) ECSP22080829A (https=)
ES (1) ES3029140T3 (https=)
FI (1) FI4139286T3 (https=)
GE (2) GEAP202416095A (https=)
HR (1) HRP20250519T1 (https=)
HU (1) HUE071024T2 (https=)
IL (1) IL297499A (https=)
JO (1) JOP20220267A1 (https=)
LT (1) LT4139286T (https=)
MA (1) MA59379B1 (https=)
MX (1) MX2022013388A (https=)
PE (1) PE20230322A1 (https=)
PH (1) PH12022552828A1 (https=)
PL (1) PL4139286T3 (https=)
PT (1) PT4139286T (https=)
RS (1) RS66889B1 (https=)
SI (1) SI4139286T1 (https=)
TW (1) TWI894261B (https=)
WO (2) WO2021214019A1 (https=)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL294032A (en) 2019-12-24 2022-08-01 Carna Biosciences Inc Compounds that regulate diacylglycerol kinase
AR120896A1 (es) 2019-12-25 2022-03-30 Astellas Pharma Inc COMPUESTO DE PIRIDAZINIL-TIAZOLCARBOXAMIDA COMO INHIBIDORES DE DGKz
CN115697980B (zh) 2020-04-24 2025-03-21 拜耳公司 作为dgkzeta抑制剂用于免疫活化的取代的氨基噻唑
CR20230415A (es) 2020-11-30 2023-09-08 Kotobuki Pharmaceutical Co Ltd Compuesto de heteroarilcarboxamida
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
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
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CN119654312A (zh) * 2022-08-08 2025-03-18 百时美施贵宝公司 用作t细胞活化剂的取代的四唑基化合物
EP4661869A1 (en) 2023-02-06 2025-12-17 Bayer Aktiengesellschaft Combinations of dgk (diacylglycerol kinase) inhibitors and immune checkpoint inhibitors and modulators
WO2024200410A1 (en) 2023-03-31 2024-10-03 Bayer Aktiengesellschaft Microcrystalline forms of (r)-2-(n-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoroanilino)propanamide and processes for their preparation
CN120826393A (zh) * 2023-04-06 2025-10-21 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的噻唑类化合物
WO2024235203A1 (zh) * 2023-05-15 2024-11-21 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的化合物
WO2025061020A1 (zh) * 2023-09-21 2025-03-27 楚浦创制(武汉)医药科技有限公司 苯并五元杂环衍生物及其制备方法与应用、药物组合物
WO2025067360A1 (zh) * 2023-09-27 2025-04-03 海思科医药集团股份有限公司 一种DGKzeta拮抗剂及其在医药上的应用
WO2025082274A1 (zh) * 2023-10-17 2025-04-24 楚浦创制(武汉)医药科技有限公司 硫代羰基化合物及其应用
WO2025082460A1 (zh) * 2023-10-20 2025-04-24 上海先祥医药科技有限公司 二酰基甘油激酶抑制剂化合物及其应用
WO2025167814A1 (zh) * 2024-02-06 2025-08-14 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的化合物
WO2026068294A1 (en) * 2024-09-24 2026-04-02 Bayer Aktiengesellschaft Improved nanoseeding process

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018089902A1 (en) 2016-11-13 2018-05-17 Apogee Biotechnology Corporation Diaminothiazole compounds, compositions and methods of use
WO2019133445A1 (en) 2017-12-28 2019-07-04 Inception Ibd, Inc. Aminothiazoles as inhibitors of vanin-1
WO2020006016A1 (en) 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Naphthyridinone compounds useful as t cell activators
WO2020006018A1 (en) 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001230026A1 (en) * 2000-02-04 2001-08-14 Novo-Nordisk A/S 2,4-diaminothiazole derivatives
RU2324685C2 (ru) 2002-08-07 2008-05-20 Ф.Хоффманн-Ля Рош Аг Производные тиазола, способ их получения и применение, фармацевтическая композиция, обладающая свойствами антагонистов рецепторов npy
US20050137239A1 (en) 2003-12-17 2005-06-23 Hines Michelle D. Thiazole derivatives
US20080146585A1 (en) 2004-04-20 2008-06-19 Ab Science Use Of C-Kit Inhibitors For Treating Inflammatory Muscle Disorders Including Myositis And Muscular Dystrophy
WO2005102318A1 (en) 2004-04-20 2005-11-03 Ab Science Use of c-kit inhibitors for treating hiv related diseases
AU2005236055B2 (en) 2004-04-20 2011-10-06 Transtech Pharma, Llc Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
WO2005102346A2 (en) 2004-04-23 2005-11-03 Ab Science Use of c-kit inhibitors for treating fibrosis
JP2007533731A (ja) 2004-04-23 2007-11-22 アブ サイエンス マラリア原虫関連の疾病を処置するためのc−kit阻害剤の使用法
WO2005102326A2 (en) 2004-04-23 2005-11-03 Ab Science Use of c-kit inhibitors for treating renal diseases
EP1742627A4 (en) 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
JP2007538064A (ja) 2004-05-18 2007-12-27 アブ サイエンス 化学または生物兵器に曝露された患者を処置するための肥満細胞阻害剤の使用法
WO2005115385A1 (en) 2004-05-24 2005-12-08 Ab Science Use of c-kit inhibitors for treating acne
WO2005115304A2 (en) 2004-05-24 2005-12-08 Ab Science Use of c-kit inhibitors for treating fibrodysplasia
UA92746C2 (en) 2005-05-09 2010-12-10 Акилайон Фармасьютикалз, Инк. Thiazole compounds and methods of use
CA2618646A1 (en) 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
WO2007022415A2 (en) 2005-08-18 2007-02-22 Pharmacopeia, Inc. Substituted 2-aminothiazoles for treating neurodegenerative diseases
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
KR100903974B1 (ko) 2007-09-27 2009-06-25 한국화학연구원 2,4,5-삼중치환-1,3-티아졸 유도체 및 약제학적으로 허용가능한 그의 염, 그의 제조방법 및 그를 유효성분으로함유하는 spc 수용체 활성으로 유발되는 염증관련 질환치료제
US9315449B2 (en) 2008-05-15 2016-04-19 Duke University Substituted pyrazoles as heat shock transcription factor activators
AP2010005480A0 (en) 2008-06-03 2010-12-31 Siga Technologies Inc Small molecule inhibitors for the treatment or prevention of denque virus infection.
JP5322296B2 (ja) 2008-08-20 2013-10-23 日本曹達株式会社 テトラゾイルオキシム誘導体を含む植物病害防除剤の使用方法
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2013033037A2 (en) 2011-08-26 2013-03-07 The Regents Of The University Of California Novel antiprion compounds
CN103058949A (zh) 2011-10-18 2013-04-24 华东理工大学 做为dhodh抑制剂的噻唑衍生物及其应用
CN103159695B (zh) 2011-12-08 2015-08-12 首都师范大学 可抑制hiv复制并对耐药hiv病毒株有效的噻唑类化合物及其制备方法和用途
GB201307233D0 (en) 2013-04-22 2013-05-29 Vib Vzw Compounds and uses thereof
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
WO2015046193A1 (ja) 2013-09-25 2015-04-02 塩野義製薬株式会社 Trpv4阻害活性を有する芳香族複素環式アミン誘導体
WO2015199206A1 (ja) 2014-06-27 2015-12-30 塩野義製薬株式会社 Trpv4阻害活性を有する6員環誘導体
CN106109467B (zh) 2016-06-20 2020-04-17 中国药科大学 三类羧基取代芳香化合物在耐吡嗪酰胺结核病及结核病治疗中的医药用途
WO2021028382A1 (en) 2019-08-12 2021-02-18 Bayer Aktiengesellschaft [1,2,4]triazolo[1,5-c]quinazolin-5-amines
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
JP2022547882A (ja) 2019-09-06 2022-11-16 インフレイゾーム リミテッド Nlrp3阻害剤
WO2021091885A2 (en) 2019-11-04 2021-05-14 Alector Llc Siglec-9 ecd fusion molecules and methods of use thereof
AR120896A1 (es) 2019-12-25 2022-03-30 Astellas Pharma Inc COMPUESTO DE PIRIDAZINIL-TIAZOLCARBOXAMIDA COMO INHIBIDORES DE DGKz
KR20230005289A (ko) 2020-04-24 2023-01-09 베링거 인겔하임 인터내셔날 게엠베하 지방 간 질환 및 지방간염의 치료에서 장시간-작용성 glp-1/글루카곤 수용체 작용제로서 글루카곤 유사체
CN115697980B (zh) 2020-04-24 2025-03-21 拜耳公司 作为dgkzeta抑制剂用于免疫活化的取代的氨基噻唑

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018089902A1 (en) 2016-11-13 2018-05-17 Apogee Biotechnology Corporation Diaminothiazole compounds, compositions and methods of use
WO2019133445A1 (en) 2017-12-28 2019-07-04 Inception Ibd, Inc. Aminothiazoles as inhibitors of vanin-1
WO2020006016A1 (en) 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Naphthyridinone compounds useful as t cell activators
WO2020006018A1 (en) 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators

Also Published As

Publication number Publication date
CN120093739A (zh) 2025-06-06
EP4139287B1 (en) 2025-02-26
CA3180819A1 (en) 2021-10-28
DOP2022000223A (es) 2022-11-15
TW202200552A (zh) 2022-01-01
EP4139287C0 (en) 2025-02-26
TWI894261B (zh) 2025-08-21
WO2021214019A1 (en) 2021-10-28
CO2022014876A2 (es) 2023-03-17
CR20220536A (es) 2023-01-17
JOP20220267A1 (ar) 2022-10-24
JP2023522251A (ja) 2023-05-29
CN120093742A (zh) 2025-06-06
MA59379B1 (fr) 2025-04-30
CN120093740A (zh) 2025-06-06
PH12022552828A1 (en) 2023-11-20
PT4139286T (pt) 2025-05-21
ES3029140T3 (en) 2025-06-23
JP2025120943A (ja) 2025-08-18
CL2022002919A1 (es) 2023-03-31
AR121929A1 (es) 2022-07-27
LT4139286T (lt) 2025-05-12
SI4139286T1 (sl) 2025-06-30
EP4139286A1 (en) 2023-03-01
CN115697980A (zh) 2023-02-03
US20230167078A1 (en) 2023-06-01
CA3180670A1 (en) 2021-10-28
RS66889B1 (sr) 2025-07-31
ECSP22080829A (es) 2022-11-30
EP4139287A1 (en) 2023-03-01
US11964953B2 (en) 2024-04-23
WO2021214020A1 (en) 2021-10-28
BR112022019057A2 (pt) 2022-11-08
HRP20250519T1 (hr) 2025-06-20
FI4139286T3 (fi) 2025-05-07
US20230139936A1 (en) 2023-05-04
KR20230005247A (ko) 2023-01-09
DK4139286T3 (da) 2025-05-05
EP4139286B1 (en) 2025-02-26
HUE071024T2 (hu) 2025-07-28
PL4139286T3 (pl) 2025-08-11
CN115697979A (zh) 2023-02-03
GEP20257731B (en) 2025-02-10
CN115697980B (zh) 2025-03-21
MX2022013388A (es) 2022-11-30
CN115697979B (zh) 2025-06-24
US20230167103A1 (en) 2023-06-01
GEAP202416095A (en) 2024-08-26
PE20230322A1 (es) 2023-02-22
CN120093741A (zh) 2025-06-06
JP2023522250A (ja) 2023-05-29
IL297499A (en) 2022-12-01
AU2021261524A1 (en) 2022-11-24

Similar Documents

Publication Publication Date Title
JP7663603B2 (ja) 免疫活性化のためのdgkzeta阻害剤としての置換アミノチアゾール類
US11787797B2 (en) 4,5-annulated 1,2,4-triazolones
US20230064809A1 (en) Substituted aminoquinolones as dgkalpha inhibitors for immune activation
US20230062100A1 (en) Substituted aminoquinolones as dgkalpha inhibitors for immune activation
EP3774769A1 (en) 4-(3-amino-6-fluoro-1h-indazol-5-yl)-1,2,6-trimethyl-1,4-dihydropyridine-3,5-dic arbonitrile compounds for treating hyperproliferative disorders
EP3645531A1 (en) Thiazole compounds useful as prmt5 inhibitors
WO2017207534A1 (en) Substituted heteroarylbenzimidazole compounds
BR112022019057B1 (pt) Aminotiazóis substituídos como inibidores de dgkzeta para ativação imune, seus usos, composição e combinação farmacêuticas, e kit
HK40081016A (en) Substituted aminothiazoles as dgkzeta inhibitors for immune activation
HK40081016B (zh) 作为dgkzeta抑制剂用於免疫活化的取代的氨基噻唑
EA048085B1 (ru) Замещенные аминотиазолы в качестве ингибиторов dgkzeta для иммунной активации
WO2025021997A1 (en) New map4k1 inhibitors

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20240417

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20241216

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20241216

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250124

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250207

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20250207

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20250124

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20250220

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20250311

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250404

R150 Certificate of patent or registration of utility model

Ref document number: 7663603

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150