AR124607A2 - Arilquinazolinas - Google Patents

Arilquinazolinas

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Publication number
AR124607A2
AR124607A2 ARP220100052A ARP220100052A AR124607A2 AR 124607 A2 AR124607 A2 AR 124607A2 AR P220100052 A ARP220100052 A AR P220100052A AR P220100052 A ARP220100052 A AR P220100052A AR 124607 A2 AR124607 A2 AR 124607A2
Authority
AR
Argentina
Prior art keywords
hal
formula
attached
pyrimidine ring
compounds
Prior art date
Application number
ARP220100052A
Other languages
English (en)
Inventor
Fuchss Thomas Dr
Emde Ulrich Dr
Buchstaller Hans Dr
- Dr Mederski Werner W K R Peter
Original Assignee
Merck Patent Ges Mit Beschraenkter Haftung
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Family has litigation
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Application filed by Merck Patent Ges Mit Beschraenkter Haftung filed Critical Merck Patent Ges Mit Beschraenkter Haftung
Publication of AR124607A2 publication Critical patent/AR124607A2/es

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    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • 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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    • 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
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Abstract

La invención se refiere a nuevos compuestos de la fórmula (1), que se pueden usar para la inhibición de serina treonina proteína quinasas, así como para la sensibilización de células cancerosas ante agentes anticáncer y/o radiación ionizante. Reivindicación 1: Compuestos de la fórmula (1) en 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, está ausente cuando Z = N, n es 1 ó 2, en donde cuando n = 1, X = S, y cuando n = 2, ambos son X = CH o X unido con el anillo pirimidina es CF y X no unido con el anillo pirimidina es CH o un X es CH y el otro X es N; m es 1 ó 2, en donde cuando m = 1, Y = S, y cuando m = 2, ambos son Y = CH o un Y es CH y el otro Y es N; R¹, R², R³, R⁴ son, de modo independiente entre sí, H, Hal, CN, OH, CONH₂, CONH(LA) o LA; R⁵ es H, Hal, CN o C&
ARP220100052A 2013-05-11 2022-01-12 Arilquinazolinas AR124607A2 (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
AR124607A2 true AR124607A2 (es) 2023-04-12

Family

ID=50729442

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP140101881A AR096235A1 (es) 2013-05-11 2014-05-09 Arilquinazolinas
ARP220100052A AR124607A2 (es) 2013-05-11 2022-01-12 Arilquinazolinas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP140101881A AR096235A1 (es) 2013-05-11 2014-05-09 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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RU2714233C2 (ru) 2015-02-26 2020-02-13 Мерк Патент Гмбх Ингибиторы pd-1 / pd-l1 для лечения рака
AU2016280003B2 (en) 2015-06-16 2021-09-16 Merck Patent Gmbh PD-L1 antagonist combination treatments
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MX2019003755A (es) 2016-10-06 2019-08-12 Pfizer Regimen de dosificacion de avelumab para el tratamiento de cancer.
ES3040063T3 (en) 2016-12-19 2025-10-28 Merck Patent Gmbh Combination of a protein kinase inhibitor and an additional chemotherapeutic agent
JP7166278B2 (ja) 2017-03-30 2022-11-07 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 がんの治療のための抗pd-l1抗体およびdna-pkインヒビターの併用
CN110446706B (zh) * 2017-03-30 2023-05-16 默克专利股份公司 (s)-[2-氯-4-氟-5-(7-吗啉-4-基喹唑啉-4-基)苯基]-(6-甲氧基-哒嗪-3-基)甲醇的晶型
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
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US12121524B2 (en) 2018-01-17 2024-10-22 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
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