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PE20160126A1 - Derivados del bipirazol como inhibidores jak - Google Patents

Derivados del bipirazol como inhibidores jak

Info

Publication number
PE20160126A1
PE20160126A1 PE2015002406A PE2015002406A PE20160126A1 PE 20160126 A1 PE20160126 A1 PE 20160126A1 PE 2015002406 A PE2015002406 A PE 2015002406A PE 2015002406 A PE2015002406 A PE 2015002406A PE 20160126 A1 PE20160126 A1 PE 20160126A1
Authority
PE
Peru
Prior art keywords
bipirazole
derivatives
jak
acetidin
bipyrazol
Prior art date
Application number
PE2015002406A
Other languages
English (en)
Inventor
Ganfeng Cao
Zhongjiang Jia
Qun Li
Jincong Zhuo
Song Mei
Yongchun Pan
Ding-Quan Qian
Yun-Long Li
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of PE20160126A1 publication Critical patent/PE20160126A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Biotechnology (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La presente invencion proporciona compuestos de la formula (I): o sales farmaceuticamente aceptables de este, asi como sus composiciones y metodos de uso, que inhiben la actividad de la Janus quinasa (JAK) y son utiles en el tratamiento de enfermedades relacionadas con la actividad de JAK, que incluyen, por ejemplo, trastornos inflamatorios, trastornos autoinmunitarios, cancer, y otras enfermedades. Donde Cy1 es fenilo, piridilo, etc. Y es N o CH, R1 es alquilo C1-6, etc. R2 es hidrogeno, etc. R7 es H, F, CL, etc. R8 es H, F, CL, etc. R9 es H, F, CL, etc. R10 es H, F, CL, etc. compuestos preferidos son: 5-[3-(cianometil)-3-(3'-metilo-1H, 1'H-4,4'-bipirazol-1-il) acetidin-1-il]-N-[(1S)-2, 2, 2-trifluoro-1-metiletil] pirazina-2-carboxamida; 5-[3-(cianometil)-3-(3'-metilo-1H, 1'H-4,4'-bipirazol-1-il) acetidin-1-il]-N-isopropilpirazina-2-carboxamida
PE2015002406A 2013-05-17 2014-05-16 Derivados del bipirazol como inhibidores jak PE20160126A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361824683P 2013-05-17 2013-05-17

Publications (1)

Publication Number Publication Date
PE20160126A1 true PE20160126A1 (es) 2016-02-24

Family

ID=50983151

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2015002406A PE20160126A1 (es) 2013-05-17 2014-05-16 Derivados del bipirazol como inhibidores jak
PE2020000001A PE20200527A1 (es) 2013-05-17 2014-05-16 Derivados del bipirazol como inhibidores jak

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2020000001A PE20200527A1 (es) 2013-05-17 2014-05-16 Derivados del bipirazol como inhibidores jak

Country Status (36)

Country Link
US (8) US9382231B2 (es)
EP (6) EP3786162B1 (es)
JP (5) JP6415543B2 (es)
KR (4) KR102663357B1 (es)
CN (2) CN105452239B (es)
AR (2) AR096330A1 (es)
AU (5) AU2014265279B2 (es)
BR (1) BR112015028501B8 (es)
CA (1) CA2911536C (es)
CL (1) CL2015003355A1 (es)
CR (2) CR20190156A (es)
CY (3) CY1119105T1 (es)
DK (4) DK3786162T3 (es)
EA (2) EA036448B1 (es)
ES (5) ES2960731T3 (es)
FI (2) FI4275756T3 (es)
HK (1) HK1245769B (es)
HR (5) HRP20231048T1 (es)
HU (4) HUE043573T2 (es)
IL (4) IL242453B (es)
LT (5) LT2997023T (es)
ME (2) ME03355B (es)
MX (2) MX373238B (es)
MY (1) MY174788A (es)
PE (2) PE20160126A1 (es)
PH (2) PH12015502563B1 (es)
PL (4) PL2997023T3 (es)
PT (5) PT3527263T (es)
RS (5) RS58743B1 (es)
SG (2) SG11201509180WA (es)
SI (5) SI3527263T1 (es)
SM (5) SMT202300352T1 (es)
TR (1) TR201905814T4 (es)
TW (4) TWI885650B (es)
UA (1) UA117830C2 (es)
WO (1) WO2014186706A1 (es)

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