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PE20152001A1 - Arilquinazolinas - Google Patents

Arilquinazolinas

Info

Publication number
PE20152001A1
PE20152001A1 PE2015002381A PE2015002381A PE20152001A1 PE 20152001 A1 PE20152001 A1 PE 20152001A1 PE 2015002381 A PE2015002381 A PE 2015002381A PE 2015002381 A PE2015002381 A PE 2015002381A PE 20152001 A1 PE20152001 A1 PE 20152001A1
Authority
PE
Peru
Prior art keywords
phenyl
pyridazin
morpholin
halo
methanol
Prior art date
Application number
PE2015002381A
Other languages
English (en)
Inventor
Hans-Peter Buchstaller
Werner Mederski
Thomas Fuchss
Ulrich Emde
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=PE20152001(A1) "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 PE20152001A1 publication Critical patent/PE20152001A1/es

Links

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
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
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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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    • C07D239/72Quinazolines; Hydrogenated quinazolines
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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
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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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)
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  • Pharmacology & Pharmacy (AREA)
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  • 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)
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Abstract

La invencion se refiere a nuevos compuestos de la formula (I), que se pueden usar para la inhibicion de serina treonina proteina quinasas, asi como para la sensibilizacion de celulas cancerosas ante agentes anticancer y/o radiacion ionizante. Donde X es CH, CF, S o N, Y es CH, S o N, Z es C o N, --- Forma, cuando Z=C, junto con el enlace simple un enlace doble. Esta ausente cuando Z=N. n ES 1 o 2 en donde cuando N=1, X=S. y cuando n=2, ambos son X=CH, etc. R1, R2, R3, R4 son H, halo, etc. R5 es H, halo, etc. C y C es fenilo no sustituido o mono sustituido o disustituido por R6, etc. R6 es halo, etc. Compuestos preferidos son: [2-cloro-4-fluoro-5-(7-morfolin-4-il-quinazolin-4-il)-fenil]-(5-metoxi-piridazin-3-il)-metanol, [4-fluoro-3-(7-morfolin-4-il-quinazolin-4-il)-fenil]-(5-metoxi-piridazin-3-il)-metanol, [2,4-difluoro-5-[7-morfolin-4-il-quinazol-4-il)-fenil]-imidazol[1,2-b]piridazin-6-il-metanol
PE2015002381A 2013-05-11 2014-05-08 Arilquinazolinas PE20152001A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102013008118.1A DE102013008118A1 (de) 2013-05-11 2013-05-11 Arylchinazoline

Publications (1)

Publication Number Publication Date
PE20152001A1 true PE20152001A1 (es) 2016-01-13

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ID=50729442

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015002381A PE20152001A1 (es) 2013-05-11 2014-05-08 Arilquinazolinas

Country Status (31)

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US (6) US9732094B2 (es)
EP (1) EP2994467B1 (es)
JP (1) JP6562903B2 (es)
KR (1) KR102292811B1 (es)
CN (1) CN105358552B (es)
AR (2) AR096235A1 (es)
AU (1) AU2014267723B2 (es)
BR (1) BR112015027951B1 (es)
CA (1) CA2911668C (es)
CL (1) CL2015003285A1 (es)
DE (1) DE102013008118A1 (es)
DK (1) DK2994467T3 (es)
ES (1) ES2693774T3 (es)
HR (1) HRP20181775T1 (es)
HU (1) HUE041397T2 (es)
IL (2) IL242348B (es)
LT (1) LT2994467T (es)
MX (1) MX362183B (es)
MY (1) MY173126A (es)
NZ (1) NZ713362A (es)
PE (1) PE20152001A1 (es)
PH (1) PH12015502339B1 (es)
PL (1) PL2994467T3 (es)
PT (1) PT2994467T (es)
RS (1) RS57838B1 (es)
RU (1) RU2701193C2 (es)
SG (1) SG11201509268YA (es)
SI (1) SI2994467T1 (es)
TR (1) TR201816069T4 (es)
UA (1) UA116020C2 (es)
WO (1) WO2014183850A1 (es)

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DE102013008118A1 (de) 2013-05-11 2014-11-13 Merck Patent Gmbh Arylchinazoline
RU2714233C2 (ru) 2015-02-26 2020-02-13 Мерк Патент Гмбх Ингибиторы pd-1 / pd-l1 для лечения рака
MX390878B (es) 2015-06-16 2025-03-21 Merck Patent Gmbh Usos medicos de antagonista de ligando 1 de muerte programada (pd-l1).
WO2017166104A1 (en) * 2016-03-30 2017-10-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
IL265762B2 (en) 2016-10-06 2024-04-01 Merck Patent Gmbh 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
SG11201909062WA (en) * 2017-03-30 2019-10-30 Merck Patent Gmbh Pharmaceutical formulation
DK3601265T3 (da) * 2017-03-30 2023-09-18 Merck Patent Gmbh Fast form af (s)-[2-chlor-4-fluor-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol
ES2926628T3 (es) * 2017-03-30 2022-10-27 Merck Patent Gmbh Forma cristalina de (S)-[2-cloro-4-fluoro-5-(7-morfolin-4-ilquinazolin-4-il)fenil]-(6-metoxi-piridazin-3-il)-metanol
CN110494161A (zh) * 2017-03-30 2019-11-22 默克专利股份有限公司 用于治疗癌症的抗pd-l1抗体和dna-pk抑制剂的组合
ES2980444T3 (es) * 2018-01-17 2024-10-01 Vertex Pharma Inhibidores de ADN-PK
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