AR062468A1 - Compuestos de azabenzofuranil y metodos de uso - Google Patents

Compuestos de azabenzofuranil y metodos de uso

Info

Publication number
AR062468A1
AR062468A1 ARP070103712A ARP070103712A AR062468A1 AR 062468 A1 AR062468 A1 AR 062468A1 AR P070103712 A ARP070103712 A AR P070103712A AR P070103712 A ARP070103712 A AR P070103712A AR 062468 A1 AR062468 A1 AR 062468A1
Authority
AR
Argentina
Prior art keywords
alkyl
cr19r20
cr14r15
nhc
noc
Prior art date
Application number
ARP070103712A
Other languages
English (en)
Original Assignee
Genentech Inc
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 Genentech Inc filed Critical Genentech Inc
Publication of AR062468A1 publication Critical patent/AR062468A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se hace referencia a los compuestos de azabenzofuranil de la formula 1 con actividad antineoplásica y/o antiinflamatoria y, más específicamente, a los compuestos de azabenzofuranil que inhiben la actividad de la quinasa MEK. También proporciona composiciones y métodos utiles para la inhibicion del crecimiento celular anomalo o el tratamiento de un trastorno hiperproliferativo, o el tratamiento de una enfermedad inflamatoria en un mamífero, y hace referencia a métodos de uso de los compuestos para diagnostico o tratamiento de células de mamíferos, o procesos patologicos relacionados, in vitro, in situ e in vivo. Reivindicacion 1: Un compuesto seleccionado a partir de la formula (1) y solvatos y sales del mismo, donde Z1 es CR1 o N; Z2 es CR2 o N; Z3 es CR3 o N, Z4 es CR4 o N; donde uno o dos de Z1, Z2, Z3 y Z4 son N; R1, R2, R3 y R4 se seleccionan, independientemente uno de otro entre H, halo, CN, CF3, -OCF3, -NO2, -(CR14R15)nC(=Y)R11, -(CR14R15)nC(=Y)OR11, - (CR14R15)nC(=Y)NR11R12, -(CR14R15)nNR11R12, -(CR14R15)nOR11, -(CR14R15)nSR11, -(CR14R15)nNR12C(=Y)R11, -(CR14R15)nNR12C(=Y)OR11, -(CR14R15)nNR13C(=Y)NR11R12, -(CR14R15)nNR12SO2R11, -(CR14R15)nOC(=Y)R11, -(CR14R15)nOC(=Y)OR11, - (CR14R15)nOC(=Y)NR11R12, -(CR14R15)nOS(O)2(OR11), -(CR14R15)nOP(=Y)(OR11)(OR12), -(CR14R15)nOP(OR11)(OR12), -(CR14R15)nS(O)R11, -(CR14R15)nS(O)2R11, -(CR14R15)nS(O)2NR11R12; -(CR14R15)nS(O)(OR11), -(CR14R15)nS(O)2(OR11), -(CR14R15)nSC(=Y)R11, - (CR14R15)nSC(=Y)OR11, -(CR14R15)nSC(=Y)NR11R12, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo y heteroarilo; W es como en formulas (2); R5 y R6 se seleccionan independientemente uno de otro entre H o alquilo C1- 12; X1 se selecciona entre R11, -OR11, -NR11R12, -S(O)R11 y -S(O)2R11; donde X1 es R11 o -OR11, R11 o -OR11 de X1 y -R5 se unen opcionalmente al átomo de N al que están ligados para formar un anillo de 4 a 7 subunidades saturado o insaturado con 0 a 2 heteroátomos adicionales seleccionados entre O, S, y N, donde este anillo se sustituye opcionalmente por uno o más grupos seleccionados entre halo, CN, CF3, -OCF3, -NO2, oxo, Si(alquil C1-6), -(CR19R20)nC(=Y')R16, -(CR19R20)nC(=Y')OR16, - (CR19R20)nC(=Y')NR16R17, -(CR19R20)nNR16R17, -(CR19R20)nOR16, -(CR19R20)n-SR16, -(CR19R20)nNR16C(=Y')R17, -(CR19R20)nNR16C(=Y')OR17, -(CR19R20)nNR18C(=Y')NR16R17, -(CR19R20)nNR17SO2R16, -(CR19R20)nOC(=Y')R16, -(CR19R20)nOC(=Y')OR16, - (CR19R20)nOC(=Y')NR16R17, -(CR19R20)nOS(O)2(OR16), -(CR19R20)nOP(=Y')(OR16)(OR17), -(CR19R20)nOP(OR16)(OR17), -(CR19R20)nS(O)R16, -(CR19R20)nS(O)2R16, -(CR19R20)nS(O)2NR16R17; -(CR19R20)nS(O)(OR16), -(CR19R20)nS(O)2(OR16), -(CR19R20)nSC(=Y')R16, - (CR19R20)nSC(=Y')OR16, -(CR19R20)nSC(=Y')NR16R17, y R21; X2 se selecciona entre carbociclilo, heterociclilo, arilo y heteroarilo; R11, R12 y R13 son, independientemente uno de otro, H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo o heteroarilo, o R11 y R12 junto con el nitrogeno al que están unidos forman un anillo saturado, insaturado o aromático de 3 a 8 subunidades con 0 a 2 heteroátomos seleccionado entre O, S y N, donde dicho anillo se sustituye opcionalmente por uno o más grupos seleccionados entre halo, CN, CF3, -OCF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), -C(O)NH2, - C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, -OC(O)NH(alquilo C1-6), - OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)NH(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)NH(alquilo C1-6)2, -NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); R14 y R15 se seleccionan, independientemente uno de otro, entre H, alquilo C1-12, arilo, carbociclilo, heterociclilo y heteroarilo; m y n se seleccionan independientemente uno de otro entre 0, 1, 2, 3, 4, 5 o 6; Y es independientemente O, NR11 o S; donde cada uno de esos alquilos, alquenilos, alquinilos, carbociclilos, heterociclilos, arilos y heteroarilos de R1, R2, R3, R4, R5, R6, X1, X2, R11, R12, R13, R14 y R15 se sustituye de forma opcional e independientemente uno de otro, por uno o más grupos seleccionados independientemente uno de otro entre halo, CN, CF3, -OCF3, -NO2, oxo, Si(alquilo C1-6), -(CR19R20)nC(=Y')R16, -(CR19R20)nC(=Y')OR16, -(CR19R20)nC(=Y')NR16R17, -(CR19R20)nNR16R17, - (CR19R20)nOR16, -(CR19R20)n-SR16, -(CR19R20)nNR16C(=Y')R17, -(CR19R20)nNR16C(=Y')OR17, -(CR19R20)nNR18C(=Y')NR16R17, -(CR19R20)nNR17SO2R16, -(CR19R20)nOC(=Y')R16, -(CR19R20)nOC(=Y')OR16, -(CR19R20)nOC(=Y')NR16R17, -(CR19R20)nOS(O)2(OR16), - (CR19R20)nOP(=Y')(OR16)(OR17), -(CR19R20)nOP(OR16)(OR17), -(CR19R20)nS(O)R16, -(CR19R20)nS(O)2R16, -(CR19R20)nS(O)2NR16R17; -(CR19R20)nS(O)(OR16), -(CR19R20)nS(O)2(OR16), -(CR19R20)nSC(=Y')R16, -(CR19R20)nSC(=Y')OR16, -(CR19R20)nSC(=Y')NR16R17, y R21; cada R16, R17 y R18 es independientemente H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo o heteroarilo, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo o heteroarilo, se sustituye opcionalmente por uno o más grupos seleccionados entre halo, CN, -OCF3, CF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), - C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, - OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)N(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, - NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); o R16 y R17 junto con el nitrogeno al que están unidos forman un anillo saturado, insaturado o aromático de 3 a 8 subunidades con 0 a 2 heteroátomos seleccionado entre O, S y N, donde dicho anillo se sustituye opcionalmente por uno o más grupos seleccionados entre halo, CN, -OCF3, CF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, - CO2(alquilo C1-6), -C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, - OC(O)NH2, -OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)N(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); R19 y R20 se seleccionan independientemente entre H, alquilo C1-12, -(CH2)n-arilo, -(CH2)n-carbociclilo, (CH2)n-heterociclilo y -(CH2)n-heteroarilo; R21 es alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo o heteroarilo, donde cada subunidad de R21 se sustituye opcionalmente por uno o más grupos seleccionados entre halo oxo, CN, -OCF3, CF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1- 6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), -C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, -OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1- 6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)N(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); cada Y' es independientemente O, NR22 o S; y R22 es H o alquilo C1-12.
ARP070103712A 2006-08-21 2007-08-21 Compuestos de azabenzofuranil y metodos de uso AR062468A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US83916106P 2006-08-21 2006-08-21
US87159106P 2006-12-22 2006-12-22
US91762307P 2007-05-11 2007-05-11
US94474107P 2007-06-18 2007-06-18

Publications (1)

Publication Number Publication Date
AR062468A1 true AR062468A1 (es) 2008-11-12

Family

ID=38925647

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070103712A AR062468A1 (es) 2006-08-21 2007-08-21 Compuestos de azabenzofuranil y metodos de uso

Country Status (16)

Country Link
US (1) US20080085886A1 (es)
EP (1) EP2069354B1 (es)
JP (1) JP5448818B2 (es)
KR (1) KR101428116B1 (es)
AR (1) AR062468A1 (es)
AT (1) ATE531720T1 (es)
AU (1) AU2007286808B2 (es)
BR (1) BRPI0714635A2 (es)
CA (1) CA2660546A1 (es)
ES (1) ES2376771T3 (es)
IL (1) IL196956A (es)
MX (1) MX2009001878A (es)
NO (1) NO20091197L (es)
PE (1) PE20080611A1 (es)
TW (1) TWI411614B (es)
WO (1) WO2008024725A1 (es)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008024724A1 (en) * 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
CA2932121A1 (en) 2007-11-30 2009-06-11 Newlink Genetics Corporation Ido inhibitors
EP2085390A1 (en) * 2008-01-31 2009-08-05 Institut National De La Sante Et De La Recherche Medicale (Inserm) Labelled analogues of halobenzamides as multimodal radiopharmaceuticals and their precursors
JP5651125B2 (ja) 2008-12-10 2015-01-07 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｍｅｋ阻害剤に対する耐性を付与するｍｅｋ突然変異
CA2757729A1 (en) 2009-04-14 2010-10-21 Masanori Kai Haloalkylsulfonanilide derivative
CN102134218A (zh) * 2009-06-15 2011-07-27 凯美隆(北京)药业技术有限公司 6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂
MX340392B (es) 2010-02-25 2016-07-06 Dana Farber Cancer Inst Inc Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.
BR112012022801B8 (pt) 2010-03-09 2019-10-29 Dana Farber Cancer Inst Inc método de identificar um indivíduo que tem câncer que é provável beneficiar-se do tratamento com uma terapia de combinação com um inibidor de raf e um segundo inibidor e uso de um inibidor de raf e um segundo inibidor para a fabricação de um medicamento para tratar câncer
WO2012071458A1 (en) 2010-11-22 2012-05-31 Array Biopharma Inc. Heterocyclic inhibitors of beta - secretase for the treatment of neurodegenerative diseases
SG194544A1 (en) 2011-05-27 2013-12-30 Bayer Ip Gmbh Chiral synthesis of n-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides
PE20190262A1 (es) 2011-08-01 2019-02-25 Genentech Inc Metodos para tratar el cancer por el uso de antagonistas de union al eje pd-1 e inhibidores de mek
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
EP2916859B1 (en) 2012-11-02 2017-06-28 The U.S.A. as represented by the Secretary, Department of Health and Human Services Method of reducing adverse effects in a cancer patient undergoing treatment with a mek inhibitor
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
CU24481B1 (es) 2014-03-14 2020-03-04 Immutep Sas Moléculas de anticuerpo que se unen a lag-3
WO2016011160A1 (en) 2014-07-15 2016-01-21 Genentech, Inc. Compositions for treating cancer using pd-1 axis binding antagonists and mek inhibitors
JP6681905B2 (ja) 2014-09-13 2020-04-15 ノバルティス アーゲー Ａｌｋ阻害剤の併用療法
AU2015327868A1 (en) 2014-10-03 2017-04-20 Novartis Ag Combination therapies
CR20170143A (es) 2014-10-14 2017-06-19 Dana Farber Cancer Inst Inc Moléculas de anticuerpo que se unen a pd-l1 y usos de las mismas
WO2016100882A1 (en) 2014-12-19 2016-06-23 Novartis Ag Combination therapies
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
WO2017019896A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to pd-1
PT3317301T (pt) 2015-07-29 2021-07-09 Novartis Ag Terapias de associação compreendendo moléculas de anticorpo contra lag-3
SG11201803520PA (en) 2015-11-03 2018-05-30 Janssen Biotech Inc Antibodies specifically binding pd-1 and their uses
CN106883270B (zh) 2015-11-26 2019-03-26 财团法人工业技术研究院 有机金属化合物、包含其的有机发光装置
AU2016369537B2 (en) 2015-12-17 2024-03-14 Novartis Ag Antibody molecules to PD-1 and uses thereof
MX2018012471A (es) 2016-04-15 2019-02-21 Genentech Inc Metodos de diagnostico y terapeuticos para el cancer.
WO2018213810A1 (en) 2017-05-19 2018-11-22 Nflection Therapeutics, Inc. Pyrrolopyridine-aniline compounds for treatment of dermal disorders
CA3063535A1 (en) 2017-05-19 2018-11-22 Nflection Therapeutics, Inc. Fused heteroaromatic-aniline compounds for treatment of dermal disorders
KR20200041387A (ko) 2017-09-08 2020-04-21 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
CN111655288A (zh) 2017-11-16 2020-09-11 诺华股份有限公司 组合疗法
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
JP7361727B2 (ja) 2018-05-24 2023-10-16 ヤンセン バイオテツク，インコーポレーテツド Ｐｓｍａ結合剤及びその使用
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
US11572344B2 (en) 2018-11-20 2023-02-07 Nflection Therapeutics, Inc. Cyanoaryl-aniline compounds for treatment of dermal disorders
KR20210106437A (ko) 2018-12-20 2021-08-30 노파르티스 아게 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물
CN113490528A (zh) 2019-02-15 2021-10-08 诺华股份有限公司 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
EP3924055B1 (en) 2019-02-15 2024-04-03 Novartis AG Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
JP2022529985A (ja) 2019-04-19 2022-06-27 ヤンセン バイオテツク，インコーポレーテツド 抗ｐｓｍａ／ｃｄ３抗体で前立腺癌を治療する方法
MX2022007759A (es) 2019-12-20 2022-07-19 Novartis Ag Combinacion del anticuerpo anti tim-3 mbg453 y anticuerpo anti tgf-beta nis793, con o sin decitabina o el anticuerpo anti pd-1 spartalizumab, para el tratamiento de mielofibrosis y sindrome mielodisplasico.
CN115916199A (zh) 2020-06-23 2023-04-04 诺华股份有限公司 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案
MX2023008909A (es) 2021-01-28 2023-10-23 Janssen Biotech Inc Proteínas de unión a psma y usos de estas.
CN117794929A (zh) 2021-02-02 2024-03-29 法国施维雅药厂 选择性bcl-xl protac化合物及使用方法
WO2022195551A1 (en) 2021-03-18 2022-09-22 Novartis Ag Biomarkers for cancer and methods of use thereof
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
WO2023225320A1 (en) 2022-05-20 2023-11-23 Novartis Ag Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
AR129382A1 (es) 2022-05-20 2024-08-21 Novartis Ag Conjugados de anticuerpo-fármaco inhibidores de bcl-xl y met y sus métodos de uso
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
WO2024189481A1 (en) 2023-03-10 2024-09-19 Novartis Ag Panras inhibitor antibody-drug conjugates and methods of use thereof

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5328920A (en) * 1991-04-17 1994-07-12 Hoechst-Roussel Pharmaceuticals Incorporated Substituted (pyridinylamino)-indoles
US5214204A (en) * 1991-07-19 1993-05-25 Abbott Laboratories Arylamidoalkyl-n-hydroxyurea compounds having lipoxygenase inhibitory activity
EP0530537B1 (en) * 1991-08-12 1997-01-08 Takeda Chemical Industries, Ltd. Condensed pyrimidine derivatives, their production and use as antitumor agents
CA2083891A1 (en) * 1991-12-03 1993-06-04 Angus Murray Macleod Heterocyclic compounds, compositions containing them and their use in therapy
JPH05345780A (ja) * 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
US5852046A (en) * 1993-08-03 1998-12-22 Hoechst Aktiengesellschaft Benzo-fused heterocyclic compounds having a 5-membered ring processes for their preparation their use as medicaments their use as diagnostic agents and medicaments containing them
US5350748A (en) * 1993-08-18 1994-09-27 Warner-Lambert Company 3-thio or amino substituted-benzo[b]thiophene-2-carboxamides and 3-oxygen, thio, or amino substituted-benzofuran-2-carboxamides as inhibitors of cell adhesion
DE4425609A1 (de) * 1994-07-20 1996-01-25 Bayer Ag Benzofuranyl- und Benzothienyloxazolidinone
FR2777886B1 (fr) * 1998-04-27 2002-05-31 Adir Nouveaux derives benzothiopheniques, benzofuraniques et indoliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6410562B1 (en) * 1998-12-18 2002-06-25 Eli Lilly And Company Hypoglycemic imidazoline compounds
EP1144385B1 (en) * 1999-01-13 2005-08-17 Warner-Lambert Company Llc Benzoheterocycles and their use as mek inhibitors
JP2000204079A (ja) * 1999-01-13 2000-07-25 Warner Lambert Co ジアリ―ルアミン
FR2799756B1 (fr) * 1999-10-15 2001-12-14 Adir Nouveaux derives benzothiopheniques, benzofuraniques et indoliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
ES2461854T3 (es) * 2000-07-19 2014-05-21 Warner-Lambert Company Llc Ésteres oxigenados de ácidos 4-yodofenilamino-benzhidroxámicos
DE10110750A1 (de) * 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
US6653346B1 (en) * 2002-02-07 2003-11-25 Galileo Pharmaceuticals, Inc. Cytoprotective benzofuran derivatives
CN1652792A (zh) * 2002-03-13 2005-08-10 阵列生物制药公司 作为mek抑制剂的n3烷基化苯并咪唑衍生物
SI2130537T1 (sl) * 2002-03-13 2013-01-31 Array Biopharma, Inc. N3-alkilirani derivati benzimidazola kot inhibitorji mek
US20040009976A1 (en) * 2002-04-30 2004-01-15 Kumiko Takeuchi Hypoglycemic imidazoline compounds
CL2003002287A1 (es) * 2002-11-25 2005-01-14 Wyeth Corp COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS
JP2005104838A (ja) * 2003-01-09 2005-04-21 Tanabe Seiyaku Co Ltd 縮合フラン化合物
US7144907B2 (en) * 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
DE10351436A1 (de) * 2003-11-04 2005-06-09 Merck Patent Gmbh Verwendung von Thienopyrimidinen
CA2545821C (en) * 2003-12-22 2010-09-21 Basilea Pharmaceutica Ag Aroylfuranes and aroylthiophenes
CA2601983A1 (en) * 2005-04-06 2006-10-12 Astrazeneca Ab Substituted heterocycles and their use as chk1, pdk1 and pak inhibitors
WO2007027855A2 (en) * 2005-09-01 2007-03-08 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
WO2008024724A1 (en) * 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
TWI389895B (zh) * 2006-08-21 2013-03-21 Infinity Discovery Inc 抑制ｂｃｌ蛋白質與結合夥伴間之交互作用的化合物及方法
CA2662348A1 (en) * 2006-09-21 2008-03-27 Wyeth Indolylalkylpyridin-2-amines for the inhibition of .beta.-secretase

Also Published As

Publication number Publication date
EP2069354B1 (en) 2011-11-02
KR20090042332A (ko) 2009-04-29
ES2376771T3 (es) 2012-03-16
JP5448818B2 (ja) 2014-03-19
JP2010501585A (ja) 2010-01-21
NO20091197L (no) 2009-05-20
EP2069354A1 (en) 2009-06-17
BRPI0714635A2 (pt) 2013-06-18
AU2007286808B2 (en) 2012-12-06
ATE531720T1 (de) 2011-11-15
CA2660546A1 (en) 2008-02-28
KR101428116B1 (ko) 2014-08-07
IL196956A0 (en) 2009-11-18
TWI411614B (zh) 2013-10-11
US20080085886A1 (en) 2008-04-10
IL196956A (en) 2014-04-30
MX2009001878A (es) 2009-03-03
TW200817415A (en) 2008-04-16
AU2007286808A1 (en) 2008-02-28
WO2008024725A1 (en) 2008-02-28
PE20080611A1 (es) 2008-07-21

Similar Documents

Publication Publication Date Title
AR062468A1 (es) Compuestos de azabenzofuranil y metodos de uso
AR064031A1 (es) Compuestos de azaindolilo y metodos de uso
AR062469A1 (es) Compuestos de azabenzotiofeno y azabenzofurano como inhibidores de la quinasa mek, una composicion farmaceutica que los comprende y el uso de estos en el tratamiento de trastornos inflamatorios e hiperproliferativos.
AR069803A1 (es) 5- anilinoimiazopiridinas y metodos de uso
AR072092A1 (es) Diazacarbazoles y metodos de uso
RU2011103454A (ru) Бициклические гетероциклы в качестве ингибиторов киназы мек
AR060054A1 (es) Inhibidores de c-met protein quinasas. composiciones farmaceuticas.
RU2011103434A (ru) Изоиндолоны и способы их применения
CY1124357T1 (el) Προσδιορισμος ανισορροπιας αλληλουχιας νουκλεϊκων οξεων
AR041250A1 (es) Derivados de sulfonamida como inhibidores de enzimas convertidoras de tnf-alfa
AR058542A1 (es) Compuestos herbicidas derivados de isoxazolina, procesos de preparacon, composiciones que los comprenden y uso en el control o inhibicion de plantas.
AR064155A1 (es) Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso
ES2571028T3 (es) Compuestos inhibidores de fosfoinositida 3-cinasa y métodos de uso
CO6220878A2 (es) Composicion herbicida que comprende un derivado de isoxazolina o una sal del mismo
AR050793A1 (es) Derivados de isoxazolina, procedimientos para su preparacion y su uso como herbicidas
ES2566482T3 (es) Derivados de oxazol sustituidos, composición farmacéutica que contiene los derivados, y método para tratar la enfermedad de Parkinson utilizando los mismos
AR069637A1 (es) Derivados de pirazinas
CO6150178A2 (es) Derivados de pirazol como inhibidores de la citocromooxidasa p450
CO6241117A2 (es) Derivados de n-(fenil) -n-morfolin-4-il-piridin -2-il) - -pirimidina-2, 4-diamina como inhibidores del ephb4 quinasa para el tratamiento de condiciones proliferativas
AR054625A1 (es) Compuestos de oxazolidinona,procedimiento para prepararlos,composiciones farmaceuticas que los contienen,y uso como agentes antimicrobianos.
AR070127A1 (es) Pirrolo - pirimidinas y pirrolo -piridinas
EA201101089A1 (ru) Производные оксадиазола в качестве агонистов рецептора s1p1
PE20071022A1 (es) Compuestos derivados de dibencilamina como inhibidores de la proteina de transferencia del colesteril ester (cept)
AR067116A1 (es) Compuestos derivados de piperazina utiles como agentes herbicidas y procedimiento para combatir el crecimiento indeseado de plantas.
PE20070359A1 (es) Inhibidores de pirimidinilpirazol de aurora quinasas

Legal Events

Date Code Title Description
FB Suspension of granting procedure