CO2017001049A2 - Compuestos derivados de 3-amino-n-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(piridinil/pirimidinil)pirazin-2-carboxamida activos como inhibidores de proteina quinasa c - Google Patents

Compuestos derivados de 3-amino-n-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(piridinil/pirimidinil)pirazin-2-carboxamida activos como inhibidores de proteina quinasa c

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Publication number
CO2017001049A2
CO2017001049A2 CONC2017/0001049A CO2017001049A CO2017001049A2 CO 2017001049 A2 CO2017001049 A2 CO 2017001049A2 CO 2017001049 A CO2017001049 A CO 2017001049A CO 2017001049 A2 CO2017001049 A2 CO 2017001049A2
Authority
CO
Colombia
Prior art keywords
inhibitors
aminopiperidin
pyrazine
pyridinyl
pyrimidinyl
Prior art date
Application number
CONC2017/0001049A
Other languages
English (en)
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=CO2017001049(A2) "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 CO2017001049A2 publication Critical patent/CO2017001049A2/es

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    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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

Se divulgan inhibidores de la PKC. Los inhibidores de la PKC son útiles para el tratamiento de enfermedades asociadas con PKC, incluyendo algunos tipos de cáncer. Los inhibidores de la PKC tienen eficacia mejorada en cantidades de dosis más bajas para lograr la regresión del tumor, potencia mejorada, perfil PK, absorción, tolerancia gastrointestinal y selectividad de quinasa
CONC2017/0001049A 2014-08-06 2017-02-03 Compuestos derivados de 3-amino-n-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(piridinil/pirimidinil)pirazin-2-carboxamida activos como inhibidores de proteina quinasa c CO2017001049A2 (es)

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 (1)

Publication Number Publication Date
CO2017001049A2 true CO2017001049A2 (es) 2017-05-31

Family

ID=53836145

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0001049A CO2017001049A2 (es) 2014-08-06 2017-02-03 Compuestos derivados de 3-amino-n-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(piridinil/pirimidinil)pirazin-2-carboxamida activos como inhibidores de proteina quinasa c

Country Status (42)

Country Link
US (6) US9452998B2 (es)
EP (2) EP3514151A1 (es)
JP (1) JP6644765B2 (es)
KR (2) KR102605181B1 (es)
CN (2) CN113214246A (es)
AP (1) AP2017009729A0 (es)
AR (1) AR101456A1 (es)
AU (1) AU2015298364B2 (es)
BR (1) BR112017002263B1 (es)
CA (1) CA2956996C (es)
CL (1) CL2017000290A1 (es)
CO (1) CO2017001049A2 (es)
CR (1) CR20170036A (es)
CU (1) CU24465B1 (es)
CY (1) CY1122407T1 (es)
DK (1) DK3177608T3 (es)
DO (1) DOP2017000035A (es)
EA (1) EA033361B1 (es)
EC (1) ECSP17013903A (es)
ES (1) ES2754248T3 (es)
GT (1) GT201700025A (es)
HR (1) HRP20192224T1 (es)
HU (1) HUE047862T2 (es)
IL (1) IL250318B (es)
JO (1) JO3589B1 (es)
LT (1) LT3177608T (es)
MX (1) MX2017001640A (es)
MY (1) MY195488A (es)
NI (1) NI201700012A (es)
PE (1) PE20170241A1 (es)
PH (1) PH12017500215A1 (es)
PL (1) PL3177608T3 (es)
PT (1) PT3177608T (es)
RS (1) RS59692B1 (es)
SG (1) SG11201700664UA (es)
SI (1) SI3177608T1 (es)
SV (1) SV2017005373A (es)
TN (1) TN2017000032A1 (es)
TW (1) TWI680968B (es)
UY (1) UY36258A (es)
WO (1) WO2016020864A1 (es)
ZA (1) ZA201700786B (es)

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CA2991276A1 (en) * 2015-08-14 2017-02-23 Novartis Ag Pharmaceutical combinations and their use
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WO2019053595A1 (en) * 2017-09-12 2019-03-21 Novartis Ag INHIBITORS OF PROTEIN KINASE C FOR THE TREATMENT OF CHOROIDAL MELLANOMA
MA54133B1 (fr) 2018-03-08 2022-01-31 Incyte Corp Composés d'aminopyrazine diol utilisés comme inhibiteurs de pi3k-y
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
US11046658B2 (en) 2018-07-02 2021-06-29 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
CN111440142B (zh) * 2019-01-16 2021-06-18 上海璎黎药业有限公司 吗啉基喹唑啉化合物的制备方法及其中间体
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
WO2021102004A1 (en) * 2019-11-18 2021-05-27 Ideaya Biosciences, Inc. Dosing regimens for a protein kinase c inhibitor
JP2023527792A (ja) 2020-05-27 2023-06-30 アキシャル セラピューティクス，インク． Ｔｌｒ２調節剤化合物、医薬組成物、及びそれらの使用
PL243663B1 (pl) * 2020-06-29 2023-09-25 Univ Medyczny Im Piastow Slaskich We Wroclawiu Zastosowanie wanikozydów
JP2023541011A (ja) * 2020-09-08 2023-09-27 イデアヤ、バイオサイエンシズ、インコーポレイテッド 医薬組み合わせおよび腫瘍治療
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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