MA43668B1 - Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak - Google Patents

Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak

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Publication number
MA43668B1
MA43668B1 MA43668A MA43668A MA43668B1 MA 43668 B1 MA43668 B1 MA 43668B1 MA 43668 A MA43668 A MA 43668A MA 43668 A MA43668 A MA 43668A MA 43668 B1 MA43668 B1 MA 43668B1
Authority
MA
Morocco
Prior art keywords
alkyl
group
hydroxy
independently
cycloalkyl
Prior art date
Application number
MA43668A
Other languages
English (en)
Inventor
Matthew Merrill Hayward
Matthew Frank Brown
Stephen Wayne Wright
Andrew Fensome
Li Huang Xing
Alpay DERMENCI
Brian Stephen Gerstenberger
Dafydd Rhys Owen
Xiaojing Yang
Original Assignee
Pfizer
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of MA43668B1 publication Critical patent/MA43668B1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed 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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (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

La présente invention concerne un composé de structure (i) ou son sel pharmaceutiquement acceptable, ou un solvate pharmaceutiquement acceptable dudit composé ou sel pharmaceutiquement acceptable, a, a' et a'' étant indépendamment o, c=o, c-r' ou n-r'', où r' et r'' peuvent indépendamment être h, un groupe amino, -nr7cor6, cor6, -conr7r8, un groupe alkyle en c1 à c6, ou un groupe hydroxy(alkyle en c1 à c6), et r'' peut être présent ou absent, et est présent où les règles de valence le permettent, et où pas plus d'un de a, a' et a'' est o ou un groupe c=o ; r0 et r sont indépendamment h, br, cl, f, ou un groupe alkyle en c1 à c6 ; r1 est h, un groupe alkyle en c1 à c6, ou un groupe hydroxy(alkyle en c1 à c6) ; r2 est sélectionné dans le groupe constitué de h, du groupe alkyle en c1 à c6, alcoxy en c1 à c6, hydroxy(alkyle en c1 à c6), phényl(alkyle en c1 à c6), formyle, hétéroaryle, hétérocyclique, -cor6, -ocor6, -coor6, -nr7cor6, -conr7r8, et -(ch2)n-w, où w est un groupe cyano, hydroxy, cycloalkyle en c3 à c8, -so2nr7r8, et -so2-r9, où r9 est un groupe alkyle en c1 à c6, cycloalkyle en c3 à c8, hétéroaryle, ou hétérocyclique ; où chacun dudit groupe alkyle, cycloalkyle, hétérocyclique, ou hétéroaryle peut être non substitué ou substitué par un groupe halogéno, cyano, hydroxy, ou alkyle en c1 à c6 ; x est un groupe c-r3 ou n, où r3 peut être h ou un groupe alkyle en c1 à c6 ; r4 et r5 sont indépendamment h, un groupe amino, alkyle en c1 à c6, ou hydroxy(alkyle en c1 à c6) ; r6, r7 et r8 sont chacun indépendamment h, un groupe alkyle en c1 à c6, alcoxy en c1 à c4(alkyle en c1 à c6), ou cycloalkyle en c3 à c8, ledit groupe alkyle en c1 à c6 est éventuellement substitué par un groupe halogéno, cn ou hydroxy ; où, r7 et r8 conjointement à l'atome lié à celui-ci forment un cycle à 5 ou 6 chaînons, ledit cycle étant éventuellement substitué par un groupe halogéno, hydroxy, cn, ou alkyle en c1 à c6 ; et, n à la valeur de 0, 1, 2 ou 3. Sont également décrits des procédés de traitement comme inhibiteurs de janus kinases et des compositions pharmaceutiques contenant les composés de l'invention et leurs combinaisons avec d'autres agents thérapeutiques.
MA43668A 2016-02-24 2017-02-10 Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak MA43668B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662299130P 2016-02-24 2016-02-24
PCT/IB2017/050748 WO2017144995A1 (fr) 2016-02-24 2017-02-10 Dérivés pyrazolo[1,5-a]pyrazin-4-yle comme inhibiteurs jac

Publications (1)

Publication Number Publication Date
MA43668B1 true MA43668B1 (fr) 2020-05-29

Family

ID=58054385

Family Applications (2)

Application Number Title Priority Date Filing Date
MA43668A MA43668B1 (fr) 2016-02-24 2017-02-10 Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak
MA052987A MA52987A (fr) 2016-02-24 2017-02-10 Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak

Family Applications After (1)

Application Number Title Priority Date Filing Date
MA052987A MA52987A (fr) 2016-02-24 2017-02-10 Dérivés de pyrazolo[1,5-a]pyrazin-4-yl en tant qu'inhibiteurs de jak

Country Status (45)

Country Link
US (4) US10144738B2 (fr)
EP (2) EP3712153B1 (fr)
JP (1) JP6505956B2 (fr)
KR (1) KR102128671B1 (fr)
CN (1) CN109071546B (fr)
AR (1) AR107714A1 (fr)
AU (1) AU2017222417B2 (fr)
CA (1) CA2958490C (fr)
CL (1) CL2018002358A1 (fr)
CO (1) CO2018008799A2 (fr)
CR (1) CR20180372A (fr)
CU (1) CU24511B1 (fr)
CY (1) CY1122949T1 (fr)
DK (1) DK3419978T3 (fr)
DO (1) DOP2018000187A (fr)
EA (1) EA035036B1 (fr)
EC (1) ECSP18072109A (fr)
ES (1) ES2794779T3 (fr)
GE (1) GEP20217242B (fr)
HR (1) HRP20200781T1 (fr)
HU (1) HUE049305T2 (fr)
IL (1) IL260923B (fr)
LT (1) LT3419978T (fr)
MA (2) MA43668B1 (fr)
MD (1) MD3419978T2 (fr)
ME (1) ME03743B (fr)
MX (1) MX383747B (fr)
MY (1) MY189118A (fr)
NI (1) NI201800080A (fr)
NZ (1) NZ744349A (fr)
PE (1) PE20181558A1 (fr)
PH (1) PH12018501788A1 (fr)
PL (1) PL3419978T3 (fr)
PT (1) PT3419978T (fr)
RS (1) RS60261B1 (fr)
RU (1) RU2718902C2 (fr)
SG (1) SG11201806307YA (fr)
SI (1) SI3419978T1 (fr)
SV (1) SV2018005726A (fr)
TN (1) TN2018000295A1 (fr)
TW (1) TWI665201B (fr)
UA (1) UA119835C2 (fr)
UY (1) UY37133A (fr)
WO (1) WO2017144995A1 (fr)
ZA (1) ZA201804972B (fr)

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WO2019034973A1 (fr) 2017-08-14 2019-02-21 Pfizer Inc. Pyrazolo[1,5-a]pyrazin-4-yl et dérivés associés

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