AR095312A1 - Compuestos de biarilamida como inhibidores de cinasa - Google Patents

Compuestos de biarilamida como inhibidores de cinasa

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Publication number
AR095312A1
AR095312A1 ARP140101014A ARP140101014A AR095312A1 AR 095312 A1 AR095312 A1 AR 095312A1 AR P140101014 A ARP140101014 A AR P140101014A AR P140101014 A ARP140101014 A AR P140101014A AR 095312 A1 AR095312 A1 AR 095312A1
Authority
AR
Argentina
Prior art keywords
alkyl
ring
halogen
alkoxy
independently
Prior art date
Application number
ARP140101014A
Other languages
English (en)
Inventor
Rico Alice
Subramanian Sharadha
Taft Benjamin
Patrick Dillon Michael
Dipesa Alan
Hu Cheng
Nishiguchi Gisele
Pan Yue
Wan Lifeng
A Barsanti Paul
Lou Yan
Ramurthy Savithri
Burger Matthew
Polyakov Valery
Yusuff Naeem
Setti Lina
Smith Aaron
Aversa Robert
Tanner Huw
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR095312A1 publication Critical patent/AR095312A1/es

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    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D213/72—Nitrogen atoms
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Abstract

Compuestos para el tratamiento de trastornos asociados con la actividad de la cinasa Raf; composiciones farmacéuticas que comprenden estos compuestos, y composiciones que comprenden estos compuestos y un co-agente terapéutico. Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: Z¹ es O, S, S(=O) o SO₂; Z² es N, S o CRᵃ, donde Rᵃ es H, halógeno, alquilo C₁₋₄ o haloalquilo C₁₋₄; R¹ es CN, halógeno, OH, alcoxilo C₁₋₄, o alquilo C₁₋₄ que está opcionalmente sustituido con uno a tres grupos seleccionados de halógeno, alcoxilo C₁₋₄, CN, e hidroxilo; el Anillo B se selecciona a partir de fenilo, piridina, pirimidina, pirazina, piridazina, piridona, pirimidona, pirazinona, piridazinona, y tiazol, cada uno de los cuales está opcionalmente sustituido con hasta dos grupos seleccionados entre halógeno, OH, CN, alquilo C₁₋₄, alquenilo C₂₋₄, -O-alquilo C₁₋₄, NH₂, NH-alquilo C₁₋₄, -N(alquilo C₁₋₄)₂, -SO₂R², NHSO₂R², NHC(O)R², NHCO₂R², cicloalquilo C₃₋₆, heteroarilo de 5 - 6 miembros, -O-cicloalquilo C₃₋₆, -O-(heteroarilo de 5 - 6 miembros), heterocicloalquilo C₄₋₈, y -O-(heterocicloalquilo de 4 - 8 miembros), donde cada heterocicloalquilo y heteroarilo contiene hasta tres heteroátomos seleccionados entre N, O y S como miembros del anillo, donde cada alquilo C₁₋₄, alquenilo C₂₋₄, cicloalquilo C₃₋₆, heteroarilo de 5 - 6 miembros, y heterocicloalquilo de 4 - 8 miembros está opcionalmente sustituido con hasta tres grupos seleccionados de oxo, hidroxilo, halógeno, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxilo C₁₋₄, y -(CH₂)₁₋₂Q, donde Q es OH, alcoxilo C₁₋₄, -CN, NH₂, -NHR³, -N(R³)₂, -SO₂R³, NHSO₂R³, NHC(O)OR³, o NHC(O)R³; cada R² y R³ es independientemente alquilo C₁₋₄; y el Anillo B está opcionalmente condensado a un anillo aromático o no aromático de 5 - 6 miembros que contiene hasta dos heteroátomos seleccionados entre N, O y S, donde el anillo de 5 - 6 miembros que puede estar sustituido con halógeno, alquilo C₁₋₄, haloalquilo C₁₋₄, o alcoxilo C₁₋₄, y si el anillo fusionado es no aromático las opciones sustituyentes pueden incluir además oxo; cada Y se selecciona independientemente entre alquilo C₁₋₄, alcoxilo C₁₋₄, CN, halógeno, oxo, -(CH₂)ₚOR⁴, -(CH₂)ₚN(R⁴)₂, -(CH₂)ₚNHC(O)R⁴, -(CH₂)ₚNHCOO(alquilo C₁₋₄), e imidazol, o dos grupos Y en el anillo A opcionalmente se toman juntos para formar un anillo fusionado o anillo puenteado A, donde dicho anillo condensado o puenteado opcionalmente contiene un heteroátomo seleccionado a partir de N, O y S como miembro del anillo, y está opcionalmente sustituido con hasta a dos grupos seleccionados entre alquilo C₁₋₄, alcoxilo C₁₋₄, CN, halógeno, oxo, -(CH₂)ₚOR⁴, -(CH₂)ₚN(R⁴)₂, -(CH₂)ₚNHC(O)R⁴, y -(CH₂)ₚNHCOO(alquilo C₁₋₄); cada R⁴ es independientemente H o alquilo C₁₋₄; cada p es independientemente 0, 1, ó 2; q es 0, 1, ó 2; Z³, Z⁴, y Z⁵ se seleccionan independientemente entre CH y N y opcionalmente NO; L es -C(=O)-NR⁴-[CY] o -NR⁴-C(=O)-[CY], donde [CY] indica cual átomo de L está enlazado a CY; y CY es un anillo aromático seleccionado entre fenilo, piridina, pirimidina, pirazina, piridazina, piridona, tiazol, isotiazol, oxazol, pirazol, y isoxazol, en el que el anillo está opcionalmente fusionado a un tiofeno, imidazol, oxazolona, o anillo de pirrol; y CY es sustituido con hasta dos grupos seleccionados de halógeno, CN, R⁵, OR⁵, SO₂R⁵, -S(=NH)(=O)R⁵, OH, NH₂, NHR⁵, y -N(R⁵)₂, en donde cada R⁵ es independientemente alquilo C₁₋₄, alquenilo C₂₋₄, heterociclilo C₄₋₆, heteroarilo de 5 miembros que contiene hasta tres heteroátomos seleccionados a partir de N, O y S como miembros del anillo, o cicloalquilo C₃₋₈, y R⁵ es opcionalmente sustituido con hasta cuatro grupos seleccionados de oxo, halógeno, CN, R⁶, OH, OR⁶, SO₂R⁶, NH₂, NHR⁶, N(R⁶)₂, NHSO₂R⁶, NHCOOR⁶, NHC(=O)R⁶, CH₂OR⁷, -CH₂N(R⁷)₂, en el que cada R⁶ es independientemente alquilo C₁₋₄, y cada R⁷ es independientemente H o alquilo C₁₋₄; y dos R⁴, R⁵, R⁶, o R⁷ en el mismo átomo de nitrógeno se pueden juntar para formar un anillo heterocíclico de 5 - 6 miembros que contiene opcionalmente un N, O ó S adicional como miembro del anillo y opcionalmente sustituido con hasta dos grupos seleccionados entre alquilo C₁₋₄, oxo, halógeno, OH, y alcoxilo C₁₋₄.
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