PE20191613A1 - Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret - Google Patents

Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret

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Publication number
PE20191613A1
PE20191613A1 PE2019000791A PE2019000791A PE20191613A1 PE 20191613 A1 PE20191613 A1 PE 20191613A1 PE 2019000791 A PE2019000791 A PE 2019000791A PE 2019000791 A PE2019000791 A PE 2019000791A PE 20191613 A1 PE20191613 A1 PE 20191613A1
Authority
PE
Peru
Prior art keywords
pyridin
alkyl
compounds
ret kinase
inhibitors
Prior art date
Application number
PE2019000791A
Other languages
English (en)
Inventor
Steven W Andrews
Sean Aronow
James F Blake
Barbara J Brandhuber
James Collier
Adam Cook
Julia Haas
Yutong Jiang
Gabrielle R Kolakowski
Elizabeth A Mcfaddin
Megan L Mckenney
Oren T Mcnulty
Andrew T Metcalf
David A Moreno
Ginelle A Ramann
Tony P Tang
Li Ren
Shane M Walls
Original Assignee
Array Biopharma 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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of PE20191613A1 publication Critical patent/PE20191613A1/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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/495—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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • 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
    • 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
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • 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

Abstract

Se refiere a compuestos de pirazolo[1,5-a]piridina sustituidos de formula I, donde X1, X2, X3 y X4 son independientemente CH, CCH3, CF o N; A es H, CN, CI, metilo, etilo o ciclopropilo; B es H, alquilo de C1-C6 opcionalmente sustituido con 1-3 fluoros, entre otros; D es un anillo heterociclico de 4-7 miembros monociclicos saturado que tiene un Nitrogeno; Ra es C1-C6 alquilo, hidroxi C1-C6 alquilo o C1-C6 alquil-; y Rb es un hidroxi o hetCicbCH2-. Tiene como compuestos preferidos: 1 -(5-(3-ciano-6-metoxipirazolo[1,5-a]piridin-4-il) piridin-2-il)-4-etil-N-isopropilpiperidin-4-carboxamida; (S)-(1-(5-(3-ciano-6-etoxipirazolo[1,5-a]piridin-4-il)piridin-2-il)piperidin-3-il)carbamato; entre otros. Estos compuestos son inhibidores de la quinasa RET y son utiles para el tratamiento de enfermedades proliferativas como diversos tipos de cancer. Ademas, se incluyen composiciones que contienen dichos compuestos.
PE2019000791A 2016-10-10 2017-10-10 Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret PE20191613A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662406275P 2016-10-10 2016-10-10
US201762447849P 2017-01-18 2017-01-18
US201762491180P 2017-04-27 2017-04-27
US201762531690P 2017-07-12 2017-07-12
US201762566030P 2017-09-29 2017-09-29
PCT/US2017/055993 WO2018071454A1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

Publications (1)

Publication Number Publication Date
PE20191613A1 true PE20191613A1 (es) 2019-11-05

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Country Status (34)

Country Link
US (5) US10144734B2 (es)
EP (2) EP4144735A1 (es)
JP (1) JP7075399B2 (es)
KR (1) KR102287752B1 (es)
CN (1) CN110177786B (es)
AU (1) AU2017342027B2 (es)
BR (1) BR112019007143A2 (es)
CA (1) CA3039912A1 (es)
CL (1) CL2019000942A1 (es)
CO (1) CO2019004649A2 (es)
CR (1) CR20190224A (es)
DK (1) DK3523302T3 (es)
DO (1) DOP2019000091A (es)
EC (1) ECSP19033052A (es)
ES (1) ES2926136T3 (es)
HR (1) HRP20221154T1 (es)
HU (1) HUE060089T2 (es)
IL (1) IL265918B (es)
JO (1) JOP20190077A1 (es)
LT (1) LT3523302T (es)
MD (1) MD3523302T2 (es)
MX (1) MX2019004204A (es)
PE (1) PE20191613A1 (es)
PH (1) PH12019500776A1 (es)
PL (1) PL3523302T3 (es)
PT (1) PT3523302T (es)
RS (1) RS63510B1 (es)
SA (1) SA519401544B1 (es)
SG (1) SG11201903187WA (es)
SI (1) SI3523302T1 (es)
TN (1) TN2019000107A1 (es)
TW (1) TWI752098B (es)
UA (1) UA125032C2 (es)
WO (1) WO2018071454A1 (es)

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