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

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

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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
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Argentina
Prior art keywords
denotes
hal
atoms
unsubstituted
substituted
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ARP200100351A
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English (en)
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Blum Andreas Dr
Dorsch Dieter Dr
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Merck Patent Gmbh
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Publication of AR118043A1 publication Critical patent/AR118043A1/es

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    • 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
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    • 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
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    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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

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  • Chemical & Material Sciences (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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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)

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US (2) US12486260B2 (es)
EP (2) EP3924340B1 (es)
JP (3) JP7630433B2 (es)
KR (1) KR102994309B1 (es)
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