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BR112015027951A2 - arilquinazolinas - Google Patents

arilquinazolinas

Info

Publication number
BR112015027951A2
BR112015027951A2 BR112015027951A BR112015027951A BR112015027951A2 BR 112015027951 A2 BR112015027951 A2 BR 112015027951A2 BR 112015027951 A BR112015027951 A BR 112015027951A BR 112015027951 A BR112015027951 A BR 112015027951A BR 112015027951 A2 BR112015027951 A2 BR 112015027951A2
Authority
BR
Brazil
Prior art keywords
arylquinazolines
threonine
formula
cancer cells
well
Prior art date
Application number
BR112015027951A
Other languages
English (en)
Other versions
BR112015027951B1 (pt
BR112015027951A8 (pt
Inventor
Buchstaller Hans-Peter
Fuchss Thomas
Emde Ulrich
Mederski Werner
Original Assignee
Merck Patent Gmbh
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=50729442&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112015027951(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of BR112015027951A2 publication Critical patent/BR112015027951A2/pt
Publication of BR112015027951A8 publication Critical patent/BR112015027951A8/pt
Publication of BR112015027951B1 publication Critical patent/BR112015027951B1/pt

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    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • C07C25/02Monocyclic aromatic halogenated hydrocarbons
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    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
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    • C07D401/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
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    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
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    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Closures For Containers (AREA)

Abstract

resumo patente de invenção: "arilquinazolinas". a presente invenção refere-se a novos compostos da fórmula (i), que podem ser usados para inibição de quinase de serina, treonina, proteína, bem como para sensibilização de células cancerígenas em relação a agentes anticancerígenos e/ou à radiação ionizante.
BR112015027951-1A 2013-05-11 2014-05-08 Arilquinazolinas, seu uso e seu processo de produção, e composição farmacêutica BR112015027951B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102013008118.1 2013-05-11
DE102013008118.1A DE102013008118A1 (de) 2013-05-11 2013-05-11 Arylchinazoline
PCT/EP2014/001236 WO2014183850A1 (de) 2013-05-11 2014-05-08 Arylchinazoline

Publications (3)

Publication Number Publication Date
BR112015027951A2 true BR112015027951A2 (pt) 2017-07-25
BR112015027951A8 BR112015027951A8 (pt) 2019-12-24
BR112015027951B1 BR112015027951B1 (pt) 2022-05-31

Family

ID=50729442

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015027951-1A BR112015027951B1 (pt) 2013-05-11 2014-05-08 Arilquinazolinas, seu uso e seu processo de produção, e composição farmacêutica

Country Status (32)

Country Link
US (6) US9732094B2 (pt)
EP (1) EP2994467B1 (pt)
JP (1) JP6562903B2 (pt)
KR (1) KR102292811B1 (pt)
CN (1) CN105358552B (pt)
AR (2) AR096235A1 (pt)
AU (1) AU2014267723B2 (pt)
BR (1) BR112015027951B1 (pt)
CA (1) CA2911668C (pt)
CL (1) CL2015003285A1 (pt)
DE (1) DE102013008118A1 (pt)
DK (1) DK2994467T3 (pt)
ES (1) ES2693774T3 (pt)
HK (1) HK1221719A1 (pt)
HR (1) HRP20181775T1 (pt)
HU (1) HUE041397T2 (pt)
IL (2) IL242348B (pt)
LT (1) LT2994467T (pt)
MX (1) MX362183B (pt)
MY (1) MY173126A (pt)
NZ (1) NZ713362A (pt)
PE (1) PE20152001A1 (pt)
PH (1) PH12015502339A1 (pt)
PL (1) PL2994467T3 (pt)
PT (1) PT2994467T (pt)
RS (1) RS57838B1 (pt)
RU (1) RU2701193C2 (pt)
SG (1) SG11201509268YA (pt)
SI (1) SI2994467T1 (pt)
TR (1) TR201816069T4 (pt)
UA (1) UA116020C2 (pt)
WO (1) WO2014183850A1 (pt)

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DE102013008118A1 (de) 2013-05-11 2014-11-13 Merck Patent Gmbh Arylchinazoline
CN112263677A (zh) 2015-02-26 2021-01-26 默克专利股份公司 用于治疗癌症的pd-1/pd-l1抑制剂
AU2016280003B2 (en) 2015-06-16 2021-09-16 Merck Patent Gmbh PD-L1 antagonist combination treatments
WO2017166104A1 (en) * 2016-03-30 2017-10-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
WO2018065938A1 (en) 2016-10-06 2018-04-12 Pfizer Inc. Dosing regimen of avelumab for the treatment of cancer
JP7113826B2 (ja) * 2016-12-19 2022-08-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング プロテインキナーゼ阻害剤および追加的化学療法剤の組み合わせ
WO2018178134A1 (en) * 2017-03-30 2018-10-04 Merck Patent Gmbh Pharmaceutical formulation
WO2018178129A1 (en) 2017-03-30 2018-10-04 Merck Patent Gmbh Crystalline form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol
AU2018241774B2 (en) * 2017-03-30 2024-06-27 Merck Patent Gmbh Combination of an anti-PD-L1 antibody and a DNA-PK inhibitor for the treatment of cancer
IL269667B2 (en) * 2017-03-30 2024-09-01 Merck Patent Gmbh Solid forms of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol, their preparation and medicinal preparations containing them
CA3088792A1 (en) 2018-01-17 2019-07-25 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
KR20200109358A (ko) 2018-01-17 2020-09-22 버텍스 파마슈티칼스 인코포레이티드 Dna-pk 억제제
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