AR082414A1 - Carboxamidas azaheterociclicas biciclicas utiles para tratar enfermedades hiperproliferativas e inflamatorias, composiciones farmaceuticas que las contienen y procedimiento para prepararlas - Google Patents

Carboxamidas azaheterociclicas biciclicas utiles para tratar enfermedades hiperproliferativas e inflamatorias, composiciones farmaceuticas que las contienen y procedimiento para prepararlas

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Publication number
AR082414A1
AR082414A1 ARP110102741A ARP110102741A AR082414A1 AR 082414 A1 AR082414 A1 AR 082414A1 AR P110102741 A ARP110102741 A AR P110102741A AR P110102741 A ARP110102741 A AR P110102741A AR 082414 A1 AR082414 A1 AR 082414A1
Authority
AR
Argentina
Prior art keywords
hal
atoms
replaced
nhco
mono
Prior art date
Application number
ARP110102741A
Other languages
English (en)
Inventor
Thomas E Richardson
Bayard R Huck
Constantin Neagu
Yufang Xiao
Srinivasa Karra
Ruoxi Lan
Igor Mochalkin
Amanda E Sutton
Lizbeth Celeste Dselm
Reinaldo Jones
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR082414A1 publication Critical patent/AR082414A1/es

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    • 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
    • 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
    • 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
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • 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

Landscapes

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

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) y sus sales, solvatos, solvatos de sales o profármacos farmacéuticamente aceptables, en donde X es N o C-R3; Y es NH, O ó está ausente; R1 es L1-R4-L2-R5 o L1-R4; R2 es A, Hal, OH, OA, SH, CN, NH2, NO2, NHA, NH-L1-Ar, NHCOA, NHCO-L1-Ar, NHSO2A, NHSO2-L1-Ar, NHCONHA, NHCONH-L1-Ar, L1-Ar, O-L1-Ar, L1-R4; L1 es un enlace simple, metileno o metileno sustituido con metilo, en donde el metileno o el grupo metilo del metileno sustituido con metilo puede no estar sustituido o puede estar mono- o disustituido con Hal, OH, CN, NH2, NH(LA), N(LA)2, NO2, COOH, N3, etenilo o etinilo, y/o monosustituido con R4 y en donde uno o dos grupos CH2 pueden estar reemplazados por un átomo de O ó de S o por 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 son cada uno, de modo independiente entre sí, Ar o A cíclico que puede estar mono- o disustituido 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 que tiene 0, 1, 2, 3 ó 4 átomos de N, O y/o S y 5, 6, 7, 8, 9 ó 10 átomos del esqueleto, que puede no estar sustituido o, de modo independiente entre sí, puede estar mono-, di- o trisustituido 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 donde un átomo de N del anillo puede estar sustituido con un átomo de O para formar un grupo N-óxido, y en donde en el caso de un ciclo aromático bicíclico en dos de los anillos puede estar parcialmente saturado; A es un alquilo lineal o cíclico no ramificado o ramificado que tiene 1, 2, 3, 4, 5, 6, 7 u 8 átomos de C, en donde uno o dos grupos CH2 pueden estar reemplazados por un átomo de O ó de S y/o por un grupo -NH-, -CO-, -NHCOO-, - NHCONH-, -N(LA)-, -CONH-, -NHCO- o -CH=CH- y en donde 1 - 3 átomos de H pueden estar reemplazados por Hal y en donde uno o dos grupos CH3 pueden estar reemplazados por OH, SH, NH2, NH(LA), N(LA)2, NHCOOH, NHCONH2 o CN; LA es un alquilo no ramificado o ramificado, lineal que tiene 1, 2, 3 ó 4 átomos de C, en donde 1, 2 ó 3 átomos de H pueden estar reemplazados por Hal; Hal es F, Cl, Br o I.
ARP110102741A 2010-07-29 2011-07-29 Carboxamidas azaheterociclicas biciclicas utiles para tratar enfermedades hiperproliferativas e inflamatorias, composiciones farmaceuticas que las contienen y procedimiento para prepararlas AR082414A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US36896410P 2010-07-29 2010-07-29

Publications (1)

Publication Number Publication Date
AR082414A1 true AR082414A1 (es) 2012-12-05

Family

ID=44532723

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Application Number Title Priority Date Filing Date
ARP110102741A AR082414A1 (es) 2010-07-29 2011-07-29 Carboxamidas azaheterociclicas biciclicas utiles para tratar enfermedades hiperproliferativas e inflamatorias, composiciones farmaceuticas que las contienen y procedimiento para prepararlas

Country Status (19)

Country Link
US (1) US8710044B2 (es)
EP (1) EP2598492B1 (es)
JP (1) JP5894157B2 (es)
KR (1) KR101852644B1 (es)
CN (1) CN103003250B (es)
AR (1) AR082414A1 (es)
AU (1) AU2011285247B2 (es)
BR (1) BR112013002090A2 (es)
CA (1) CA2806610C (es)
CL (1) CL2013000263A1 (es)
EA (1) EA023132B1 (es)
ES (1) ES2557383T3 (es)
HK (1) HK1183302A1 (es)
IL (1) IL224072A (es)
MX (1) MX2013001054A (es)
NZ (1) NZ604379A (es)
SG (1) SG187166A1 (es)
UA (1) UA110113C2 (es)
WO (1) WO2012013282A1 (es)

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Also Published As

Publication number Publication date
US20130137677A1 (en) 2013-05-30
MX2013001054A (es) 2013-02-21
BR112013002090A2 (pt) 2016-05-24
AU2011285247A1 (en) 2013-03-14
EP2598492B1 (en) 2015-10-28
CA2806610C (en) 2018-08-28
CN103003250A (zh) 2013-03-27
NZ604379A (en) 2015-01-30
JP2013532668A (ja) 2013-08-19
KR101852644B1 (ko) 2018-04-26
CL2013000263A1 (es) 2013-09-06
SG187166A1 (en) 2013-02-28
EA201300186A1 (ru) 2013-12-30
KR20130096714A (ko) 2013-08-30
US8710044B2 (en) 2014-04-29
EA023132B1 (ru) 2016-04-29
CA2806610A1 (en) 2012-02-02
HK1183302A1 (zh) 2013-12-20
IL224072A0 (en) 2013-03-05
IL224072A (en) 2016-02-29
AU2011285247B2 (en) 2016-08-04
ES2557383T3 (es) 2016-01-25
WO2012013282A1 (en) 2012-02-02
WO2012013282A8 (en) 2012-03-29
JP5894157B2 (ja) 2016-03-23
CN103003250B (zh) 2016-02-17
UA110113C2 (xx) 2015-11-25
EP2598492A1 (en) 2013-06-05

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