EA033361B1 - Ингибиторы протеинкиназы c и способы их применения - Google Patents

Ингибиторы протеинкиназы c и способы их применения

Info

Publication number
EA033361B1
EA033361B1 EA201790323A EA201790323A EA033361B1 EA 033361 B1 EA033361 B1 EA 033361B1 EA 201790323 A EA201790323 A EA 201790323A EA 201790323 A EA201790323 A EA 201790323A EA 033361 B1 EA033361 B1 EA 033361B1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
methods
protein kinase
pkc
pkc inhibitors
Prior art date
Application number
EA201790323A
Other languages
English (en)
Other versions
EA201790323A1 (ru
Inventor
Michael Scott Visser
Julien Papillon
Michael Joseph Luzzio
Original Assignee
Novartis 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53836145&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA033361(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of EA201790323A1 publication Critical patent/EA201790323A1/ru
Publication of EA033361B1 publication Critical patent/EA033361B1/ru

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Classifications

    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pulmonology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Раскрыты ингибиторы протеинкиназы C (PKC). Ингибиторы PKC являются полезными для лечения PKC-ассоциированных заболеваний, включая некоторые типы рака. Ингибиторы PKC имеют большую эффективность при более низких дозах для достижения регрессии опухоли, улучшенную активность, PK профиль, абсорбцию, желудочно-кишечную переносимость и селективность в отношении киназ.
EA201790323A 2014-08-06 2015-08-05 Ингибиторы протеинкиназы c и способы их применения EA033361B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462033679P 2014-08-06 2014-08-06
PCT/IB2015/055951 WO2016020864A1 (en) 2014-08-06 2015-08-05 Protein kinase c inhibitors and methods of their use

Publications (2)

Publication Number Publication Date
EA201790323A1 EA201790323A1 (ru) 2017-06-30
EA033361B1 true EA033361B1 (ru) 2019-10-31

Family

ID=53836145

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201790323A EA033361B1 (ru) 2014-08-06 2015-08-05 Ингибиторы протеинкиназы c и способы их применения

Country Status (42)

Country Link
US (7) US9452998B2 (ru)
EP (2) EP3514151A1 (ru)
JP (1) JP6644765B2 (ru)
KR (2) KR102605181B1 (ru)
CN (2) CN113214246A (ru)
AP (1) AP2017009729A0 (ru)
AR (1) AR101456A1 (ru)
AU (1) AU2015298364B2 (ru)
BR (1) BR112017002263B1 (ru)
CA (1) CA2956996C (ru)
CL (1) CL2017000290A1 (ru)
CO (1) CO2017001049A2 (ru)
CR (1) CR20170036A (ru)
CU (1) CU24465B1 (ru)
CY (1) CY1122407T1 (ru)
DK (1) DK3177608T3 (ru)
DO (1) DOP2017000035A (ru)
EA (1) EA033361B1 (ru)
EC (1) ECSP17013903A (ru)
ES (1) ES2754248T3 (ru)
GT (1) GT201700025A (ru)
HR (1) HRP20192224T1 (ru)
HU (1) HUE047862T2 (ru)
IL (1) IL250318B (ru)
JO (1) JO3589B1 (ru)
LT (1) LT3177608T (ru)
MX (1) MX2017001640A (ru)
MY (1) MY195488A (ru)
NI (1) NI201700012A (ru)
PE (1) PE20170241A1 (ru)
PH (1) PH12017500215A1 (ru)
PL (1) PL3177608T3 (ru)
PT (1) PT3177608T (ru)
RS (1) RS59692B1 (ru)
SG (1) SG11201700664UA (ru)
SI (1) SI3177608T1 (ru)
SV (1) SV2017005373A (ru)
TN (1) TN2017000032A1 (ru)
TW (1) TWI680968B (ru)
UY (1) UY36258A (ru)
WO (1) WO2016020864A1 (ru)
ZA (1) ZA201700786B (ru)

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JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
RU2018108804A (ru) * 2015-08-14 2019-09-16 Новартис Аг Фармацевтические комбинации и их применение
SG11201900090TA (en) 2016-07-14 2019-02-27 Mingsight Pharmaceuticals Inc Treatment of cancer
US11413284B2 (en) * 2017-09-12 2022-08-16 Novartis Ag Protein kinase C inhibitors for treatment of uveal melanoma
LT3762368T (lt) 2018-03-08 2022-06-10 Incyte Corporation Aminopirazindiolio junginiai, kaip pi3k-γ inhibitoriai
CN110496223B (zh) * 2018-05-17 2021-09-10 复旦大学附属肿瘤医院 一种治疗非霍奇金氏淋巴瘤的药物组合物
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
WO2020092924A1 (en) * 2018-11-02 2020-05-07 Board Of Regents, The University Of Texas System Combination therapy for the treatment of egfr tyrosine kinase inhibitor resistant cancer
EP3908282A1 (en) * 2019-01-07 2021-11-17 Ideaya Biosciences, Inc. Treatment of cancer having gnaq or gna11 genetic mutations with protein kinase c inhibitors
KR102405055B1 (ko) * 2019-01-16 2022-06-07 상하이 잉리 파마슈티컬 컴퍼니 리미티드 모르폴리노퀴나졸린 화합물의 제조방법 및 이의 중간체
WO2020198469A1 (en) * 2019-03-27 2020-10-01 Ideaya Biosciences Inc. Method for treating epidermal growth factor receptor-driven cancers with protein kinase c inhibitors in combination with an egfr-tyrosine kinase inhibitor
US20220401440A1 (en) * 2019-11-18 2022-12-22 Ideaya Biosciences, Inc. Dosing regimens for a protein kinase c inhibitor
BR112022024071A2 (pt) 2020-05-27 2022-12-20 Axial Therapeutics Inc Compostos moduladores de tlr2, composições farmacêuticas e usos dos mesmos
PL243663B1 (pl) * 2020-06-29 2023-09-25 Univ Medyczny Im Piastow Slaskich We Wroclawiu Zastosowanie wanikozydów
IL300952A (en) * 2020-09-08 2023-04-01 Ideaya Biosciences Inc Drug combination and tumor treatment
WO2024125543A1 (zh) * 2022-12-16 2024-06-20 苏州科睿思制药有限公司 达洛色替的晶型及其制备方法和用途

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