BR112015016327A8 - inibidores da atividade de pirazol quinase substituídos por policíclicos e seu uso - Google Patents

inibidores da atividade de pirazol quinase substituídos por policíclicos e seu uso

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Publication number
BR112015016327A8
BR112015016327A8 BR112015016327A BR112015016327A BR112015016327A8 BR 112015016327 A8 BR112015016327 A8 BR 112015016327A8 BR 112015016327 A BR112015016327 A BR 112015016327A BR 112015016327 A BR112015016327 A BR 112015016327A BR 112015016327 A8 BR112015016327 A8 BR 112015016327A8
Authority
BR
Brazil
Prior art keywords
polycyclic
kinase activity
substituted pyrazole
substituted
activity inhibitors
Prior art date
Application number
BR112015016327A
Other languages
English (en)
Other versions
BR112015016327A2 (pt
Inventor
Lin Guowu
Zhao Li
Jin Qiaomei
Guo Qinglong
Lu Tao
Yang Taotao
Chen Yadong
Lu Yi
Wang Yue
Wang Zhanwei
Original Assignee
Univ China Pharma
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 Univ China Pharma filed Critical Univ China Pharma
Publication of BR112015016327A2 publication Critical patent/BR112015016327A2/pt
Publication of BR112015016327A8 publication Critical patent/BR112015016327A8/pt

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Classifications

    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Agronomy & Crop Science (AREA)
  • Endocrinology (AREA)
  • Pest Control & Pesticides (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Plant Pathology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)

Abstract

abstract: the present invention relates to the field of medicinal chemistry, and in particular relates to 4-(five-membered heterocyclic pyrimidine/pyridine substituted) amino-1h-3-pyrazolecarboxamide derivatives, the preparation method thereof, pharmaceutical compositions containing these compounds and the medicinal use thereof, especially as protein kinase inhibitors for anti-tumour use. tradução do resumo resumo patente de invenção: "inibidores da atividade de pirazol cinase substituídos por policíclicos e seu uso". a presente invenção refere-se ao campo de química medicinal, e em particular refere-se aos derivados de 4-(pirimidina/piridina heterocíclica de cinco membros substituída) amino-1h-3-pirazolcarboxamida, ao seu método de preparação, às composições farmacêuticas contendo estes compostos e ao seu uso medicinal, especialmente como inibidores da proteína cinase para uso anti-tumoral.
BR112015016327A 2013-01-08 2014-01-07 inibidores da atividade de pirazol quinase substituídos por policíclicos e seu uso BR112015016327A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2013100052586A CN103012428A (zh) 2013-01-08 2013-01-08 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途
PCT/CN2014/070195 WO2014108053A1 (zh) 2013-01-08 2014-01-07 含多环取代的吡唑类激酶活性抑制剂及其用途

Publications (2)

Publication Number Publication Date
BR112015016327A2 BR112015016327A2 (pt) 2017-07-11
BR112015016327A8 true BR112015016327A8 (pt) 2018-01-23

Family

ID=47961580

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015016327A BR112015016327A8 (pt) 2013-01-08 2014-01-07 inibidores da atividade de pirazol quinase substituídos por policíclicos e seu uso

Country Status (13)

Country Link
US (1) US9550792B2 (pt)
EP (1) EP2955185B1 (pt)
JP (1) JP6322848B2 (pt)
KR (1) KR102136628B1 (pt)
CN (3) CN103012428A (pt)
AU (1) AU2014204633B2 (pt)
BR (1) BR112015016327A8 (pt)
CA (1) CA2897366C (pt)
DK (1) DK2955185T3 (pt)
ES (1) ES2863175T3 (pt)
PT (1) PT2955185T (pt)
RU (1) RU2655921C2 (pt)
WO (1) WO2014108053A1 (pt)

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CN103435606A (zh) * 2013-08-22 2013-12-11 中国药科大学 CDK2与GSK3β双重抑制剂及用途
CN104592251B (zh) * 2015-01-23 2019-10-01 上海复星医药产业发展有限公司 4-(稠杂环取代氨基)-1h-吡唑-3-甲酰胺类化合物及其用途
CN107235906B (zh) * 2017-06-28 2020-05-01 郑州大学第一附属医院 一组吡唑酰胺类衍生物及其应用
CN107245073B (zh) * 2017-07-11 2020-04-17 中国药科大学 4-(芳杂环取代)氨基-1h-3-吡唑甲酰胺类flt3抑制剂及其用途
CN111148743B (zh) 2017-10-06 2023-12-15 福马治疗有限公司 抑制泛素特异性肽酶30
CN109970717B (zh) * 2017-12-28 2022-10-18 中国药科大学 4-(脂肪环并嘧啶/吡啶取代)氨基-1h-3-吡唑甲酰胺类flt3抑制剂及其用途
CN110835334B (zh) * 2018-08-16 2022-10-18 中国药科大学 吲哚取代唑类化合物及其用途
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CN113677341A (zh) * 2019-02-01 2021-11-19 南卡罗莱纳大学 双环吡啶组合物及其用于癌症治疗的方法
KR20200100429A (ko) * 2019-02-18 2020-08-26 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
CN110183464B (zh) * 2019-05-31 2021-08-31 淮阴工学院 一种抗癌化合物艾斯替尼及其合成方法和应用
CN112794855B (zh) * 2019-11-13 2023-07-28 中国药科大学 N-芳基嘧啶-4-胺类衍生物的制备方法与应用
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CN114685371A (zh) * 2022-03-08 2022-07-01 四川大学 吡唑甲酰胺衍生物及其制备方法和用途
CN115746002B (zh) * 2022-11-13 2023-12-08 药康众拓(江苏)医药科技有限公司 一种氘代氮杂吲哚氨基-吡唑甲酰胺类化合物及其用途

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CN105189517A (zh) 2015-12-23
CA2897366A1 (en) 2014-07-17
US9550792B2 (en) 2017-01-24
PT2955185T (pt) 2021-02-23
EP2955185A1 (en) 2015-12-16
KR20150120966A (ko) 2015-10-28
AU2014204633A1 (en) 2015-08-27
DK2955185T3 (da) 2021-03-29
JP2016504395A (ja) 2016-02-12
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