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AR046748A1 - Derivados de amina que inhiben,regulan,y/o modulan tirosinaquinasas,composiciones farmaceuticas que los contienen,procedimientos de preparacion y compuestos intermediarios - Google Patents

Derivados de amina que inhiben,regulan,y/o modulan tirosinaquinasas,composiciones farmaceuticas que los contienen,procedimientos de preparacion y compuestos intermediarios

Info

Publication number
AR046748A1
AR046748A1 ARP040104503A ARP040104503A AR046748A1 AR 046748 A1 AR046748 A1 AR 046748A1 AR P040104503 A ARP040104503 A AR P040104503A AR P040104503 A ARP040104503 A AR P040104503A AR 046748 A1 AR046748 A1 AR 046748A1
Authority
AR
Argentina
Prior art keywords
mono
unsubstituted
hal
atoms
cooh
Prior art date
Application number
ARP040104503A
Other languages
English (en)
Inventor
Guenter Dr Hoelzemann
Kai Dr Schiemann
Wilfried Dr Rautenberg
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 AR046748A1 publication Critical patent/AR046748A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos de la fórmula (1), en donde: X es C o N; B es N, CH o C-CN; R1 es H, A, OH, NH2, -(CH2)m-Ar o -(CH2)m-Het2; R2 cuando X = N, está ausente o cuando X = C, es H, A, Hal, CN, -(CH2)p-Ar, -(CH2)p-COOH, -(CH2)p-COOA, -(CH2)p-Het3, -(CH2)p- NH2, SO2A, CHO o COA; R3 es H, A, -S-A, -(CH2)p-Ar, -(CH2)p-Het, NH-(CH2)p-Ar, NH-(CH2)p-Het, NH2, NHA, NA2, NH-alquilen-NH2, NH-alquilen-NHA, NH-alquilen-NA2 o NA-alquilen-NA2; R4 es -(CH2)s-(Ar1)n-Y-R6; R5 es H o CH3; R4 y R5 también son juntos Het4-N-(CH2-CH2-)2; R6 es Het4, -(CH2)r-NH2, -(CH2)r-NHA o -(CH2)rNA2; Y es O, S, (CH2)q o NH; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OH, OA, NH2, NO2, CN, COOH, COOA, CONH2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2, SO2A, -CH2-COOH u -OCH2-COOH; Ar1 es fenileno o piperazin-diílo; Het es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, NHA, NA2, OA, COOA, CN, -(CH2)p-Ar, -(CH2)t-OH, -(CH2)p-Het1 o el oxígeno del carbonilo (=O); Het1 es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono o disustituido con A o el oxígeno del carbonilo (=O); Het2 es un heterociclo monocíclico aromático con 1 a 3 átomos de N, O y/o S, que puede estar insustituido o mono o disustituido con A; Het3 es un heterociclo monocíclico saturado o aromático con 1 a 3 átomos de N, O y/o S, que puede estar insustituido o mono o disustituido con A; Het4 es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, CONH2, CONHA, CONA2 o Ar2; Ar2 es fenilo insustituido o mono, di o trisustituido con Hal, A, OH, OA, NH2, NO2, CN, COOH, COOA, CONH2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 o SO2A; R7, R8, R9, R10 son cada uno, de modo independiente entre sí, H, A o - (CH2)p-Ar; A es alquilo C1-10, en donde también 1-7 átomos de H pueden estar reemplazados por F y/o cloro; m es 0, 1, 2, 3 ó 4; n es 0 ó 1; p es 0, 1, 2, 3 ó 4; q es 0, 1, 2, 3 ó 4; r es 0, 1, 2, 3 ó 4; s es 0, 1, 2, 3 ó 4; Hal es F, Cl, Br o I; y cuando X = C; R1 y R2 también pueden ser juntos -(CH2)4- o R2 y R3 también pueden ser juntos -(CHR7-NR8-CHR9-CHR10)-, y, cuando Ar1 es piperazin-diílo, R6 también puede ser H o alquilo C1-6; así como sus derivados, solvatos, tautómeros, sales y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de las tirosina quinasas, en especial de la TIE-2, y de las Raf-quinasas, y se pueden utilizar, entre otras cosas, para el tratamiento de tumores.
ARP040104503A 2003-12-04 2004-12-03 Derivados de amina que inhiben,regulan,y/o modulan tirosinaquinasas,composiciones farmaceuticas que los contienen,procedimientos de preparacion y compuestos intermediarios AR046748A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10356579A DE10356579A1 (de) 2003-12-04 2003-12-04 Aminderivate

Publications (1)

Publication Number Publication Date
AR046748A1 true AR046748A1 (es) 2005-12-21

Family

ID=34638319

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ARP040104503A AR046748A1 (es) 2003-12-04 2004-12-03 Derivados de amina que inhiben,regulan,y/o modulan tirosinaquinasas,composiciones farmaceuticas que los contienen,procedimientos de preparacion y compuestos intermediarios

Country Status (10)

Country Link
US (1) US7816365B2 (es)
EP (1) EP1727820B1 (es)
JP (1) JP4829123B2 (es)
AR (1) AR046748A1 (es)
AT (1) ATE524474T1 (es)
AU (1) AU2004295032B2 (es)
CA (1) CA2548156C (es)
DE (1) DE10356579A1 (es)
ES (1) ES2373661T3 (es)
WO (1) WO2005054246A2 (es)

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Also Published As

Publication number Publication date
WO2005054246A3 (de) 2005-07-28
EP1727820A2 (de) 2006-12-06
WO2005054246A2 (de) 2005-06-16
ATE524474T1 (de) 2011-09-15
US20070112006A1 (en) 2007-05-17
DE10356579A1 (de) 2005-07-07
CA2548156C (en) 2012-10-30
US7816365B2 (en) 2010-10-19
EP1727820B1 (de) 2011-09-14
JP2007513099A (ja) 2007-05-24
JP4829123B2 (ja) 2011-12-07
CA2548156A1 (en) 2005-06-16
ES2373661T3 (es) 2012-02-07
AU2004295032B2 (en) 2010-11-25
AU2004295032A1 (en) 2005-06-16

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