AR118043A1 - DERIVADOS DE INDAZOLIL-ISOXAZOL COMO INHIBIDORES DE c-KIT QUINASA - Google Patents

DERIVADOS DE INDAZOLIL-ISOXAZOL COMO INHIBIDORES DE c-KIT QUINASA

Info

Publication number
AR118043A1
AR118043A1 ARP200100351A ARP200100351A AR118043A1 AR 118043 A1 AR118043 A1 AR 118043A1 AR P200100351 A ARP200100351 A AR P200100351A AR P200100351 A ARP200100351 A AR P200100351A AR 118043 A1 AR118043 A1 AR 118043A1
Authority
AR
Argentina
Prior art keywords
denotes
hal
atoms
unsubstituted
substituted
Prior art date
Application number
ARP200100351A
Other languages
English (en)
Inventor
Blum Andreas Dr
Dorsch Dieter Dr
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 AR118043A1 publication Critical patent/AR118043A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/05—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/48—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
    • C07C311/49—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/575—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/10—Spiro-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
    • 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • 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
    • C07D491/08—Bridged systems
    • 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Compuestos derivados de indazolil-isoxazol con actividad inhibidora de c-KIT quinasa, un proceso para su preparación, intermediarios utilizados en dicho proceso, medicamentos y un kit que los comprenden y el uso de los mismos para el tratamiento del cáncer. Reivindicación 1: Los compuestos de la fórmula (1) caracterizados porque R¹ denota Hal, CF₃, OA, Het¹, COOR³ o CON(R³)₂, R² denota H, Hal o CN, R³ denota H o A, X denota fenileno, piridin-diilo, 1,3-tiazol-diilo o pirazol-diilo, cada uno de los cuales está sin sustituir o sustituido una, dos o tres veces con Hal y/o A, Y está ausente o denota CO, O[C(R³)₂]ₙ, NR³CO, CONR³, CONR³[C(R³)₂]ₙ, CONHCH₂C(CH₃)₂, SO₂, SO₂N(R³), -N= o S(=O, =NR³), Z denota H, A, Hal, OA, [C(R³)₂]ₙHet² o N=S(=O)A₂, A denota alquilo ramificado o no ramificado con 1 - 10 átomos de C, donde uno o dos grupos CH y/o CH₂ no adyacentes pueden ser reemplazados con átomos de O y donde 1 - 7 átomos de H pueden ser reemplazados con R⁵, o denota (CH₂)ₙCyc, Cyc denota alquilo cíclico que tiene de 3 - 7 átomos de C, R⁵ denota F, Cl, OH, SO₂A o N(R³)₂, Het¹ denota pirazolilo el cual puede estar sustituido una o dos veces con A, Het² denota un heterociclo saturado o insaturado, aromático, monocíclico, de 4 a 7 miembros que tiene de 1 a 4 átomos de N, O y/o S, el cual puede estar sin sustituir o sustituido una, dos o tres veces con A, Hal, CN, OR³, [C(R³)₂]ₙN(R³)₂, [C(R³)₂]ₙSO₂A, [C(R³)₂]ₙNR³SO₂A, Het³, =NR³ y/o =O, o denota un heterociclo saturado o insaturado, aromático, bicíclico, de 7 a 10 miembros que tiene de 1 a 4 átomos de N, O y/o S, el cual puede estar sin sustituir o sustituido una, dos o tres veces con A, Hal, CN, OR³, [C(R³)₂]ₙN(R³)₂, [C(R³)₂]ₙSO₂A, [C(R³)₂]ₙNR³SO₂A, Het³, =NR³ y/o =O, Het³ denota un heterociclo saturado o insaturado, aromático, monocíclico, de 4 a 7 miembros que tiene de 1 a 4 átomos de N, O y/o S, el cual puede estar sin sustituir o puede estar sustituido una o dos veces con A, Hal, OR³, oxetanilo y/o =O, o denota un heterociclo saturado o insaturado, aromático, bicíclico, de 7 a 10 miembros que tiene de 1 a 4 átomos de N, O y/o S, el cual puede estar sin sustituir o puede estar sustituido una o dos veces con A, Hal, OR³, oxetanilo y/o =O, Hal denota F, Cl, Br o I, n denota 0, 1, 2 ó 3, y sus solvatos, sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo las mezclas de los mismos en todas las proporciones.
ARP200100351A 2019-02-11 2020-02-10 DERIVADOS DE INDAZOLIL-ISOXAZOL COMO INHIBIDORES DE c-KIT QUINASA AR118043A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP19156318 2019-02-11

Publications (1)

Publication Number Publication Date
AR118043A1 true AR118043A1 (es) 2021-09-15

Family

ID=65408901

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP200100351A AR118043A1 (es) 2019-02-11 2020-02-10 DERIVADOS DE INDAZOLIL-ISOXAZOL COMO INHIBIDORES DE c-KIT QUINASA

Country Status (24)

Country Link
US (2) US12486260B2 (es)
EP (2) EP4520326A3 (es)
JP (3) JP7630433B2 (es)
KR (1) KR20210129674A (es)
CN (2) CN113474334B (es)
AR (1) AR118043A1 (es)
AU (2) AU2020220333B2 (es)
BR (1) BR112021014466A2 (es)
CA (1) CA3129601A1 (es)
DK (1) DK3924340T3 (es)
ES (1) ES3015269T3 (es)
FI (1) FI3924340T3 (es)
HR (1) HRP20250227T1 (es)
HU (1) HUE070387T2 (es)
IL (2) IL285421B2 (es)
LT (1) LT3924340T (es)
MX (1) MX2021009426A (es)
NZ (1) NZ779815A (es)
PL (1) PL3924340T3 (es)
PT (1) PT3924340T (es)
RS (1) RS66498B1 (es)
SG (1) SG11202108636SA (es)
SI (1) SI3924340T1 (es)
WO (1) WO2020165062A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3746070A4 (en) 2018-01-29 2021-09-01 Capulus Therapeutics, LLC SREBP INHIBITORS WITH A 6-LINKED CENTER RING
CN114945365A (zh) * 2019-11-13 2022-08-26 卡普勒斯疗法有限责任公司 包括噻吩中心环的srebp抑制剂
CN114000167B (zh) * 2021-11-25 2024-02-06 南京先进生物材料与过程装备研究院有限公司 一种电化学合成吡唑类化合物的方法
EP4593822A2 (en) * 2022-09-28 2025-08-06 The Trustees Of Columbia University In The City Of New York Novel gpx4 inhibitors and uses thereof

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
CA2658190C (en) 2006-07-20 2013-01-29 Amgen Inc. Di-amino-substituted heterocyclic compounds and methods of use
UA107360C2 (en) 2009-08-05 2014-12-25 Biogen Idec Inc Bicyclic aryl sphingosine 1-phosphate analogs
UY32922A (es) 2009-10-06 2011-04-29 Bayer Schering Pharma Ag Derivados de 3, 5-diciano-4-(1h-indazol-5-il)-2,6-dimetil-1,4-dihidropiridina fluoro-sustituidos y procedimientos de uso de los mismos
BR112013015460B1 (pt) * 2010-12-20 2022-01-25 Merck Serono S.A. Derivados de indazolil triazol, kit, e composição farmacêutica
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
KR101731624B1 (ko) 2014-07-01 2017-05-04 광주과학기술원 세포 리프로그래밍 유도용 조성물
MX382436B (es) * 2016-01-11 2025-03-13 Merck Patent Gmbh Derivados de quinolin-2-ona.
US10722495B2 (en) * 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof

Also Published As

Publication number Publication date
US12486260B2 (en) 2025-12-02
US20260042753A1 (en) 2026-02-12
HUE070387T2 (hu) 2025-06-28
IL285421A (en) 2021-09-30
JP2022520374A (ja) 2022-03-30
MX2021009426A (es) 2021-09-10
AU2025287415A1 (en) 2026-01-22
JP7744540B2 (ja) 2025-09-25
EP3924340B1 (en) 2025-01-29
CN118955486A (zh) 2024-11-15
JP2025084757A (ja) 2025-06-03
EP4520326A3 (en) 2025-06-11
SG11202108636SA (en) 2021-09-29
DK3924340T3 (da) 2025-02-24
EP3924340A1 (en) 2021-12-22
PL3924340T3 (pl) 2025-03-31
RS66498B1 (sr) 2025-03-31
CA3129601A1 (en) 2020-08-20
IL285421B2 (en) 2026-02-01
JP2026015711A (ja) 2026-01-30
AU2020220333A1 (en) 2021-09-30
AU2020220333B2 (en) 2025-10-16
HRP20250227T1 (hr) 2025-04-11
IL323370A (en) 2025-11-01
CN113474334A (zh) 2021-10-01
CN113474334B (zh) 2024-08-06
IL285421B1 (en) 2025-10-01
LT3924340T (lt) 2025-03-10
US20220127254A1 (en) 2022-04-28
PT3924340T (pt) 2025-02-21
JP7630433B2 (ja) 2025-02-17
BR112021014466A2 (pt) 2021-09-21
SI3924340T1 (sl) 2025-04-30
FI3924340T3 (fi) 2025-03-03
KR20210129674A (ko) 2021-10-28
ES3015269T3 (en) 2025-04-30
NZ779815A (en) 2026-03-27
WO2020165062A1 (en) 2020-08-20
EP4520326A2 (en) 2025-03-12

Similar Documents

Publication Publication Date Title
AR118043A1 (es) DERIVADOS DE INDAZOLIL-ISOXAZOL COMO INHIBIDORES DE c-KIT QUINASA
PY2054376A (es) Degradadores bifuncionales de brd9 y sus métodos de uso
CL2022001111A1 (es) Degradadores de moléculas pequeñas de helios y procedimientos de uso
AR112797A1 (es) Inhibidores de kras g12c y métodos para utilizarlos
AR111314A1 (es) Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
AR111878A1 (es) Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
AR110753A1 (es) Inhibidores selectivos de jak1
UY33501A (es) Derivados de acil sulfonamida y sus sales farmacéuticamente aceptables para uso en medicina
UY33500A (es) Derivados de acil sulfonamida y sus sales farmacéuticamente aceptables para uso en medicina
AR092959A1 (es) Derivados de nucleosidos 2-metil sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales
AR089944A1 (es) Derivados de tetrahidro-quinazolinona
AR111233A1 (es) Inhibidores de tyk2, usos y métodos para la producción de los mismos
AR111820A1 (es) Derivados de indolina sustituidos como inhibidores de la replicación de virus del dengue
AR104963A1 (es) Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak
AR111315A1 (es) Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
AR097087A1 (es) Derivados de oxoquinazolinil-butanamida
AR090587A1 (es) Compuestos triciclicos sustituidos con actividad hacia los receptores ep1
UY38096A (es) Inhibidores de arginasa y sus métodos de uso
AR107927A1 (es) Compuestos de pirrolidina, sal farmacéuticamente aceptable del mismo, composición farmacéutica que lo comprende y su uso para la fabricación de un medicamento
AR090103A1 (es) Derivados ciclicos de diaminopirimidina
AR093035A1 (es) Derivados de pirrolotriazinona como inhibidores de pi3k
AR125122A1 (es) Actividad antiviral de inhibidores de vps34
AR125117A1 (es) Actividad antiviral de inhibidores de vps34
CO6640204A2 (es) Derivados de (metilsulfonil) etilbenceno isoindolina y sus usos terapéuticos
AR098723A1 (es) Derivados de pirazolopirimidin-2-ilo como inhibidores de jak