MD3419978T2 - Derivaţi de pirazolo[1,5-a]pirazin-4-il - Google Patents

Derivaţi de pirazolo[1,5-a]pirazin-4-il

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Publication number
MD3419978T2
MD3419978T2 MDE20190031T MDE20190031T MD3419978T2 MD 3419978 T2 MD3419978 T2 MD 3419978T2 MD E20190031 T MDE20190031 T MD E20190031T MD E20190031 T MDE20190031 T MD E20190031T MD 3419978 T2 MD3419978 T2 MD 3419978T2
Authority
MD
Moldova
Prior art keywords
alkyl
hydroxy
cycloalkyl
independently represent
halo
Prior art date
Application number
MDE20190031T
Other languages
English (en)
Inventor
Matthew Frank Brown
Alpay DERMENCI
Andrew Fensome
Brian Stephen Gerstenberger
Matthew Merrill Hayward
Dafydd Rhys Owen
Stephen Wayne Wright
Li Huang Xing
Xiaojing Yang
Original Assignee
Pfizer
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Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of MD3419978T2 publication Critical patent/MD3419978T2/ro

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    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (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

Se propune un compus având structura (I) sau o sare farmaceutic acceptabilă a acestuia, sau un solvat farmaceutic acceptabil al compusului menţionat sau o sare farmaceutic acceptabilă, în care: A, A' şi A'' independent reprezintă O, C=O, C- R' sau N-R», în care R' şi R» independent pot reprezenta H, amino, -NR7COR6, COR6, -CONR7R8, C1-C6 alchil sau hidroxi(C1-C6 alchil) şi R» poate fi prezent sau absent, şi este prezent acolo unde regulile de valenţă permit şi unde nu mai mult de unul dintre A, A' şi A» reprezintă O sau C=O; Ro şi R independent reprezintă H, Br, CI, F sau C1-C6 alchil; R1 reprezintă H, C1-C6 alchil sau hidroxi(C1-C6 alchil); R2 se selectează din grupa constând din H, C1-C6 alchil, C1-C6 alcoxi, hidroxi(C1-C6 alchil), fenil(C1-C6 alchil), formil, heteroaril, heterociclic, -COR6, -OCOR6, -COOR6, -NR7COR6, -CONR7R8 şi -(CH2)n-W, în care W reprezintă cian, hidroxi, C3-C8 cicloalchil, -SO2NR7R8 şi -SO2-R9, în care R9 reprezintă C1-C6 alchil, C3-C8 cicloalchil, heteroaril sau heterociclic; în care fiecare dintre alchil, cicloalchil, heterociclic sau heteroaril menţionat poate fi substituit sau nesubstituit cu halo, cian, hidroxi sau C1-C6 alchil; X reprezintă C-R3 sau N, în care R3 poate fi H sau C1-C6 alchil; R4 şi R5 independent reprezintă H, amino, C1-C6 alchil sau hidroxi(C1-C6 alchil); R6, R7 şi R8 fiecare independent reprezintă H, C1-C6 alchil, C1-C4 alcoxi(C1-C6 alchil) sau C3-C8 cicloalchil, C1-C6 alchil menţionat este substituit opţional cu halo, CN sau hidroxi; sau R7 şi R8 împreună cu atomul legat de acesta formează un inel cu 5- sau 6- membri, inelul menţionat fiind opţional substituit cu halo, hidroxi, CN sau C1-C6 alchil; şi n este 0, 1, 2 sau 3. Sunt propuse, de asemenea, metode de tratament în calitate de inhibitori ai kinazei Janus şi compoziţii farmaceutice care conţin compuşii invenţiei şi combinaţii ale acestora cu alţi agenţi terapeutici.
MDE20190031T 2016-02-24 2017-02-10 Derivaţi de pirazolo[1,5-a]pirazin-4-il MD3419978T2 (ro)

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
MD3419978T2 true MD3419978T2 (ro) 2020-07-31

Family

ID=58054385

Family Applications (1)

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MDE20190031T MD3419978T2 (ro) 2016-02-24 2017-02-10 Derivaţi de pirazolo[1,5-a]pirazin-4-il

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US (4) US10144738B2 (ro)
EP (2) EP3712153B1 (ro)
JP (1) JP6505956B2 (ro)
KR (1) KR102128671B1 (ro)
CN (1) CN109071546B (ro)
AR (1) AR107714A1 (ro)
AU (1) AU2017222417B2 (ro)
CA (1) CA2958490C (ro)
CL (1) CL2018002358A1 (ro)
CO (1) CO2018008799A2 (ro)
CR (1) CR20180372A (ro)
CU (1) CU24511B1 (ro)
CY (1) CY1122949T1 (ro)
DK (1) DK3419978T3 (ro)
DO (1) DOP2018000187A (ro)
EA (1) EA035036B1 (ro)
EC (1) ECSP18072109A (ro)
ES (1) ES2794779T3 (ro)
GE (1) GEP20217242B (ro)
HK (1) HK1258157A1 (ro)
HR (1) HRP20200781T1 (ro)
HU (1) HUE049305T2 (ro)
IL (1) IL260923B (ro)
LT (1) LT3419978T (ro)
MA (2) MA52987A (ro)
MD (1) MD3419978T2 (ro)
ME (1) ME03743B (ro)
MX (1) MX2018010236A (ro)
MY (1) MY189118A (ro)
NI (1) NI201800080A (ro)
NZ (1) NZ744349A (ro)
PH (1) PH12018501788A1 (ro)
PL (1) PL3419978T3 (ro)
PT (1) PT3419978T (ro)
RS (1) RS60261B1 (ro)
RU (1) RU2718902C2 (ro)
SG (1) SG11201806307YA (ro)
SI (1) SI3419978T1 (ro)
SV (1) SV2018005726A (ro)
TN (1) TN2018000295A1 (ro)
TW (1) TWI665201B (ro)
UA (1) UA119835C2 (ro)
UY (1) UY37133A (ro)
WO (1) WO2017144995A1 (ro)
ZA (1) ZA201804972B (ro)

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HK1258157A1 (zh) 2019-11-08
DK3419978T3 (da) 2020-06-02
MA43668B1 (fr) 2020-05-29
EP3712153A1 (en) 2020-09-23
US20190071448A1 (en) 2019-03-07
HRP20200781T1 (hr) 2020-07-24
CO2018008799A2 (es) 2018-09-20
PT3419978T (pt) 2020-06-01
TN2018000295A1 (en) 2020-01-16
TW201741313A (zh) 2017-12-01
US20230045252A1 (en) 2023-02-09
UY37133A (es) 2017-09-29
UA119835C2 (uk) 2019-08-12
ES2794779T3 (es) 2020-11-19
US10822341B2 (en) 2020-11-03
NZ744349A (en) 2023-06-30
EP3419978B1 (en) 2020-04-15
GEP20217242B (en) 2021-04-12
RU2718902C2 (ru) 2020-04-15
PL3419978T3 (pl) 2020-11-30
EP3419978A1 (en) 2019-01-02
TWI665201B (zh) 2019-07-11
MX2018010236A (es) 2019-01-14
LT3419978T (lt) 2020-06-10
CU24511B1 (es) 2021-05-12
US20200399281A1 (en) 2020-12-24
SG11201806307YA (en) 2018-09-27
HUE049305T2 (hu) 2020-09-28
SV2018005726A (es) 2018-10-24
KR20180103158A (ko) 2018-09-18
ECSP18072109A (es) 2018-10-31
EP3712153B1 (en) 2021-12-01
CA2958490C (en) 2024-02-27
JP6505956B2 (ja) 2019-04-24
KR102128671B1 (ko) 2020-06-30
CY1122949T1 (el) 2021-10-29
RS60261B1 (sr) 2020-06-30
IL260923B (en) 2022-01-01
WO2017144995A1 (en) 2017-08-31
CN109071546A (zh) 2018-12-21
ME03743B (me) 2021-04-20
NI201800080A (es) 2018-11-22
AR107714A1 (es) 2018-05-23
SI3419978T1 (sl) 2020-08-31
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MA52987A (fr) 2021-04-28
JP2019510003A (ja) 2019-04-11
AU2017222417B2 (en) 2020-07-09
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AU2017222417A1 (en) 2018-08-02
RU2018130547A (ru) 2020-03-25
EA201891463A1 (ru) 2019-03-29
US10144738B2 (en) 2018-12-04
CN109071546B (zh) 2021-03-02
EA035036B1 (ru) 2020-04-20
RU2018130547A3 (ro) 2020-03-25
CR20180372A (es) 2018-09-19
BR112018015501A2 (pt) 2018-12-18
US20170240552A1 (en) 2017-08-24
MY189118A (en) 2022-01-26
CL2018002358A1 (es) 2018-11-30
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US11472809B2 (en) 2022-10-18
ZA201804972B (en) 2019-06-26

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