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AR075396A1 - Derivados de quinazolinas y composiciones farmaceuticas - Google Patents

Derivados de quinazolinas y composiciones farmaceuticas

Info

Publication number
AR075396A1
AR075396A1 ARP100100376A ARP100100376A AR075396A1 AR 075396 A1 AR075396 A1 AR 075396A1 AR P100100376 A ARP100100376 A AR P100100376A AR P100100376 A ARP100100376 A AR P100100376A AR 075396 A1 AR075396 A1 AR 075396A1
Authority
AR
Argentina
Prior art keywords
hal
atoms
atom
replaced
group
Prior art date
Application number
ARP100100376A
Other languages
English (en)
Inventor
Thomas E Richardson
Ruoxi Lan
Frank Stieber
Amanda E Sulton
David Perrey
Harold George Vandeveer
Andreas Goutopoulos
Xiaoling Chen
Lesley Liu-Bujalski
Srinivasa R Karra
Bayard R Huck
Yufang Xiao
Brian L Hodous
Hui Qiu
Reinaldo C Jones
Brian Heasley
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=42199208&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR075396(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 AR075396A1 publication Critical patent/AR075396A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/06Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos de amino carboxamida azaheterocíclica sustituida, su fabricacion y su uso para el tratamiento de enfermedades hiperproIiferativas como el cáncer. Reivindicacion 1: Un compuesto caracterizado porque responde a la Formula (1) y sales aceptables farmacéuticamente, solvatos o prodrogas del mismo, donde: X es N o C-R3, Y es NH, O se encuentra ausente, R1 es L1-R4-L2-R5-L3-R6, L1-R4-L2-R5 o L1-R4, R2', R2'' cada uno, en forma independiente entre si, son H, A Hal, OH, OA, SH, CN, NH2, NO2, NHA, NH-L1-Ar, NHCOA, NHCO-L1-Ar, NHSO2A, NHSO2-L1-Ar, NHCONHA o NHCONH-L1-Ar, L1-Ar, O-L1-Ar, L1-R4, L1, L3 cada uno, en forma independiente entre si son una union simple, alquileno no ramificado o ramificado con 1, 2, 3, 4 o 5 átomos de C el cual puede estar no sustituido, o estar mono- o disustituido con Hal, OH, CN, NH2, NH(LA), N(LA)2, NO2, COOH, N3, etenilo o etinilo, y/o monosustituidos con R4, y en el cual uno o dos grupos CH2 se pueden reemplazar con un átomo de O o S o con un grupo -NH-, -N(LA)-, -CONH-, -N(LA)COO-, -SO2- o -NHCO-, R3 es H, A, Hal, OH, COOH, SH, NH2, NO2 o CN, R4, R5, R6 cada uno, en forma independiente entre si, son Ar, o alquilo monocíclico con 3, 4, 5, 6 o 7 átomos del anillo, en el cual uno o dos grupos CH2 se pueden reemplazar con un átomo de O o S y/o con un grupo -NH-, -NA-, -CHA-, -CO-, CH=N o -CH=CH-, y/o en el cual el grupo conector CH se puede reemplazar con un átomo de N, y el cual puede estar mono o di-sustituido con Hal o LA, L2 es -NHCO-, -NHCOO-, -NHCONH-, -NHCONA-, -NHCOA-, -O-, -S-.,-NH-, -NHSO2-, -SO2NH-, -CONH-, -CONHCONH-, -NHCONHCO-, o -A-, Ar es un homo- o heterociclo aromático mono- o bicíclico con 0, 1, 2, 3 o 4 átomos de N, O y/o S y 5, 6, 7, 8, 9, o 10 átomos del esqueleto, que pueden estar no sustituidos o, en forma independiente entre si estar mono- di- o tri-sustituidos con Hal A, OH, SH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONHA, NHCONH2, NHSO2A, CHO, COA, SO2NH2, SO2A y/o SO2Hal, y en el cual un átomo de N del anillo puede estar sustituido con un átomo de O para formar un grupo N-oxido, y en el cual en el caso de un anillo aromático bicíclico uno de los dos anillos puede estar parcialmente saturado. A es alquilo lineal o cíclico no ramificado o ramificado con 1, 2, 3, 4, 5, 6, 7 o 8 átomos de C en el cual uno o dos grupos CH2 se pueden reemplazar con un átomo de O o S y/o con un grupo -NH-, -CO-, -NHCOO-, -NHCONH-, -N(LA)-, -CONH-, -NHCO- o -CH=CH-, y en el cual 1-3 átomos de H se pueden reemplazar con Hal, y en el cual uno o dos grupos CH3 se pueden reemplazar con OH, SH, NH2, NH(LA), N(LA)2, NHCOOH, NHCONH2 o CN, LA es alquilo lineal no ramificado o ramificado con 1, 2, 3 o 4 átomos de C, Hal es F, Cl, Br o I.
ARP100100376A 2009-02-11 2010-02-11 Derivados de quinazolinas y composiciones farmaceuticas AR075396A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20735409P 2009-02-11 2009-02-11

Publications (1)

Publication Number Publication Date
AR075396A1 true AR075396A1 (es) 2011-03-30

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Family Applications (1)

Application Number Title Priority Date Filing Date
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Country Status (26)

Country Link
US (2) US8637532B2 (es)
EP (1) EP2396307B1 (es)
JP (1) JP5642714B2 (es)
KR (1) KR101699991B1 (es)
CN (1) CN102317269B (es)
AR (1) AR075396A1 (es)
AU (1) AU2010214095B2 (es)
BR (1) BRPI1008325A2 (es)
CA (1) CA2751886C (es)
CL (1) CL2011001967A1 (es)
DK (1) DK2396307T3 (es)
EA (1) EA020731B1 (es)
ES (1) ES2527940T3 (es)
HK (1) HK1166070A1 (es)
HR (1) HRP20141239T1 (es)
IL (1) IL214412A0 (es)
MX (1) MX338354B (es)
MY (1) MY160468A (es)
NZ (1) NZ595087A (es)
PL (1) PL2396307T3 (es)
PT (1) PT2396307E (es)
SG (1) SG173473A1 (es)
SI (1) SI2396307T1 (es)
UA (1) UA107188C2 (es)
WO (1) WO2010093419A1 (es)
ZA (1) ZA201106624B (es)

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CN109369634B (zh) * 2018-12-19 2021-07-27 陕西国际商贸学院 具有抗肿瘤活性的2-甲氧基烟酰胺衍生物制备方法及用途
RU2723481C1 (ru) * 2019-10-03 2020-06-11 ФЕДЕРАЛЬНОЕ ГОСУДАРСТВЕННОЕ УНИТАРНОЕ ПРЕДПРИЯТИЕ "ИНСТИТУТ ХИМИЧЕСКИХ РЕАКТИВОВ И ОСОБО ЧИСТЫХ ХИМИЧЕСКИХ ВЕЩЕСТВ НАЦИОНАЛЬНОГО ИССЛЕДОВАТЕЛЬСКОГО ЦЕНТРА "КУРЧАТОВСКИЙ ИНСТИТУТ" (НИЦ "Курчатовский институт - ИРЕА) 4-[метил 4-(аминометил)циклогексанкарбоксилат]хиназолин и способ его получения
EP4051673A1 (en) 2019-11-01 2022-09-07 Syngenta Crop Protection AG Pesticidally active fused bicyclic heteroaromatic compounds
CN112778217B (zh) * 2019-11-08 2024-01-26 沈阳化工研究院有限公司 一种喹唑啉类化合物及其应用
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