CR20180372A - Derivados de pirazolo [1,5-a] pirazin-4-ilo - Google Patents

Derivados de pirazolo [1,5-a] pirazin-4-ilo

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Publication number
CR20180372A
CR20180372A CR20180372A CR20180372A CR20180372A CR 20180372 A CR20180372 A CR 20180372A CR 20180372 A CR20180372 A CR 20180372A CR 20180372 A CR20180372 A CR 20180372A CR 20180372 A CR20180372 A CR 20180372A
Authority
CR
Costa Rica
Prior art keywords
alkyl
hydroxy
independently
cycloalkyl
halo
Prior art date
Application number
CR20180372A
Other languages
English (en)
Inventor
Alpay; Dermenci
Dafydd Rhys; Owen
Stephen Wayne; Wright
Matthew Frank; Brown
Andrew; Fensome
Xiaojing; Yang
Li Huang; Xing
Matthew Merrill; Hayward
Brian Stephen; Gerstenberger
Original Assignee
Pfizer
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.)
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of CR20180372A publication Critical patent/CR20180372A/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto que tiene la siguiente estructura o una sal de este aceptable desde el punto de vista farmacéutico, o un solvato aceptable desde el punto de vista farmacéutico de un compuesto o una sal aceptable desde el punto de vista farmacéutico, en donde A, A¿ y A¿¿ son independientemente O, C=O, C-R¿ o N-R¿¿, en donde R¿ y R¿¿ pueden ser independientemente H, amino, -NR7COR6, COR6, -CONR7R8, C1-C6 alquilo o hidroxi(C1-C6 alquilo), y R¿¿ puede estar presente o ausente, y está presente donde las reglas de valencia lo permiten, y en donde no más de uno de A, A¿ y A¿¿ es O o C=O; R0 y R son independientemente H, Br, Cl, F o C1-C6 alquilo; R1 es H, C1-C6 alquilo o hidroxi(C1-C6 alquilo); R2 se selecciona del grupo que consiste en H, C1-C6 alquilo, C1-C6 alcoxi, hidroxi(C1-C6 alquilo), fenil(C1-C6 alquilo), formilo, heteroarilo, heterocíclico, -COR6, -OCOR6, -COOR6, -NR7COR6, -CONR7R8 y -(CH2)n-W, en donde W es ciano, hidroxi, C3-C8 cicloalquilo, -SO2NR7R8 y -SO2-R9, en donde R9 es C1-C6 alquilo, C3-C8 cicloalquilo, heteroarilo o heterocíclico; en donde cada uno de alquilo, cicloalquilo, heterocíclico o heteroarilo puede ser no sustituido o sustituido por halo, ciano, hidroxi o C1-C6 alquilo; X es C-R3 o N, en donde R3 puede ser H o C1-C6 alquilo; R4 y R5 son independientemente H, amino, C1-C6 alquilo o hidroxi(C1-C6 alquilo); R6, R7 y R8 son, cada uno independientemente, H, C1-C6 alquilo, C1-C4 alcoxi(C1-C6 alquilo) o C3-C8 cicloalquilo, dicho C1-C6 alquilo se sustituye opcionalmente con halo, CN o hidroxi; o R7 y R8, junto con el átomo unido a estos, forman un anillo de 5 o 6 miembros, en donde el anillo se sustituye opcionalmente con halo, hidroxi, CN o C1-C6 alquilo; y n es 0, 1, 2 o 3. También se proporcionan métodos de tratamiento tales como inhibidores de quinasas Janus y composiciones farmacéuticas que contienen los compuestos de la invención y combinaciones de estos con otros agentes terapéuticos.
CR20180372A 2016-02-24 2017-02-10 Derivados de pirazolo [1,5-a] pirazin-4-ilo CR20180372A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662299130P 2016-02-24 2016-02-24
PCT/IB2017/050748 WO2017144995A1 (en) 2016-02-24 2017-02-10 Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors

Publications (1)

Publication Number Publication Date
CR20180372A true CR20180372A (es) 2018-09-19

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CR20180372A CR20180372A (es) 2016-02-24 2017-02-10 Derivados de pirazolo [1,5-a] pirazin-4-ilo

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US (3) US10144738B2 (es)
EP (2) EP3712153B1 (es)
JP (1) JP6505956B2 (es)
KR (1) KR102128671B1 (es)
CN (1) CN109071546B (es)
AR (1) AR107714A1 (es)
AU (1) AU2017222417B2 (es)
CA (1) CA2958490C (es)
CL (1) CL2018002358A1 (es)
CO (1) CO2018008799A2 (es)
CR (1) CR20180372A (es)
CU (1) CU24511B1 (es)
CY (1) CY1122949T1 (es)
DK (1) DK3419978T3 (es)
DO (1) DOP2018000187A (es)
EA (1) EA035036B1 (es)
EC (1) ECSP18072109A (es)
ES (1) ES2794779T3 (es)
GE (1) GEP20217242B (es)
HK (1) HK1258157A1 (es)
HR (1) HRP20200781T1 (es)
HU (1) HUE049305T2 (es)
IL (1) IL260923B (es)
LT (1) LT3419978T (es)
MA (2) MA52987A (es)
MD (1) MD3419978T2 (es)
ME (1) ME03743B (es)
MX (1) MX2018010236A (es)
MY (1) MY189118A (es)
NI (1) NI201800080A (es)
NZ (1) NZ744349A (es)
PH (1) PH12018501788A1 (es)
PL (1) PL3419978T3 (es)
PT (1) PT3419978T (es)
RS (1) RS60261B1 (es)
RU (1) RU2718902C2 (es)
SG (1) SG11201806307YA (es)
SI (1) SI3419978T1 (es)
SV (1) SV2018005726A (es)
TN (1) TN2018000295A1 (es)
TW (1) TWI665201B (es)
UA (1) UA119835C2 (es)
UY (1) UY37133A (es)
WO (1) WO2017144995A1 (es)
ZA (1) ZA201804972B (es)

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CA2958490C (en) 2024-02-27
PH12018501788A1 (en) 2019-06-17
TWI665201B (zh) 2019-07-11
TW201741313A (zh) 2017-12-01
HRP20200781T1 (hr) 2020-07-24
NZ744349A (en) 2023-06-30
MD3419978T2 (ro) 2020-07-31
CL2018002358A1 (es) 2018-11-30
CA2958490A1 (en) 2017-08-24
CO2018008799A2 (es) 2018-09-20
HK1258157A1 (zh) 2019-11-08
IL260923B (en) 2022-01-01
UY37133A (es) 2017-09-29
US20190071448A1 (en) 2019-03-07
AU2017222417B2 (en) 2020-07-09
MY189118A (en) 2022-01-26
ECSP18072109A (es) 2018-10-31
EP3712153A1 (en) 2020-09-23
CU20180078A7 (es) 2019-02-04
ES2794779T3 (es) 2020-11-19
PL3419978T3 (pl) 2020-11-30
AR107714A1 (es) 2018-05-23
RS60261B1 (sr) 2020-06-30
MA43668B1 (fr) 2020-05-29
MA52987A (fr) 2021-04-28
KR102128671B1 (ko) 2020-06-30
US10822341B2 (en) 2020-11-03
SI3419978T1 (sl) 2020-08-31
WO2017144995A1 (en) 2017-08-31
AU2017222417A1 (en) 2018-08-02
RU2718902C2 (ru) 2020-04-15
DOP2018000187A (es) 2019-01-31
SG11201806307YA (en) 2018-09-27
EP3419978B1 (en) 2020-04-15
HUE049305T2 (hu) 2020-09-28
CU24511B1 (es) 2021-05-12
KR20180103158A (ko) 2018-09-18
CY1122949T1 (el) 2021-10-29
CN109071546A (zh) 2018-12-21
UA119835C2 (uk) 2019-08-12
RU2018130547A (ru) 2020-03-25
RU2018130547A3 (es) 2020-03-25
JP6505956B2 (ja) 2019-04-24
EA035036B1 (ru) 2020-04-20
PT3419978T (pt) 2020-06-01
CN109071546B (zh) 2021-03-02
US20200399281A1 (en) 2020-12-24
EA201891463A1 (ru) 2019-03-29
TN2018000295A1 (en) 2020-01-16
DK3419978T3 (da) 2020-06-02
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