PE20130038A1 - Derivados de piperidin-4-il azetidina como inhibidores de jak1 - Google Patents

Derivados de piperidin-4-il azetidina como inhibidores de jak1

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Publication number
PE20130038A1
PE20130038A1 PE2012001467A PE2012001467A PE20130038A1 PE 20130038 A1 PE20130038 A1 PE 20130038A1 PE 2012001467 A PE2012001467 A PE 2012001467A PE 2012001467 A PE2012001467 A PE 2012001467A PE 20130038 A1 PE20130038 A1 PE 20130038A1
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PE
Peru
Prior art keywords
piperidin
alkyl
azethydine
pyrimidin
acetonitrile
Prior art date
Application number
PE2012001467A
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English (en)
Inventor
Taisheng Huang
Chu-Biao Xue
Anlai Wang
Ling Kong
Hai Fen Ye
Wenqing Yao
James D Rodgers
Stacey Shepard
Haisheng Wang
Lixin Shao
Hui-Yin Li
Qun Li
Original Assignee
Incyte Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44065466&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130038(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of PE20130038A1 publication Critical patent/PE20130038A1/es

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    • 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
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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  • Pharmacology & Pharmacy (AREA)
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  • Transplantation (AREA)
  • Pain & Pain Management (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)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIPERIDIN-4-IL AZETIDINA DE FORMULA (I) DONDE X ES N O CR2, EN DONDE R2 ES H, HALO, CN, ALQUILO(C1-C4), ENTRE OTROS; Y ES N O CR3, EN DONDE R3 ES H, CN, NITRO, ALQUENILO(C2-C6), ENTRE OTROS; Z ES H, CN, HALO, ALQUILO(C1-C3), ENTRE OTROS; L ES C(=O), S(=O)2, C(=O)O, ENTRE OTROS; A ES ALQUILO(C1-C6), CICLOALQUILO(C3-C14), ARILO(C6-C14), ENTRE OTROS; R1 ES ALQUILO(C1-C4), HIDROXILO, ALCOXI(C1-C4), F, ENTRE OTROS; n ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: {1-{1-[3-FLUORO-2-(TRIFLUOROMETIL)ISONICOTINOIL]PIPERIDIN-4-IL}-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO; {1-[1-(3-FLUORO-4-QUINOLIN-6-ILBENZOIL)PIPERIDIN-4-IL]-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO; {3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]-1-[1-(3,4,5-TRIFLUOROBENZOIL)PIPERIDIN-4-IL]AZETIDIN-3-IL}ACETONITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA ACTIVIDAD DE JANUS QUINASA (JAK1) SIENDO UTILES EN EL TRATAMIENTO DE ARTRITIS REUMATOIDE, LUPUS, DERMATITIS ATOPICA
PE2012001467A 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de jak1 PE20130038A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31258810P 2010-03-10 2010-03-10
US41560210P 2010-11-19 2010-11-19

Publications (1)

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PE20130038A1 true PE20130038A1 (es) 2013-01-28

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ID=44065466

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PE2012001467A PE20130038A1 (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de jak1

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US (6) US8765734B2 (es)
EP (5) EP4036088B1 (es)
JP (6) JP5858484B2 (es)
KR (7) KR102354472B1 (es)
CN (1) CN102985417B (es)
AR (1) AR081315A1 (es)
AU (1) AU2011224484A1 (es)
BR (1) BR112012022513A2 (es)
CA (1) CA2792508C (es)
CL (1) CL2012002501A1 (es)
CO (1) CO6602158A2 (es)
CR (1) CR20120510A (es)
CY (2) CY1120154T1 (es)
DK (3) DK3354652T3 (es)
EA (1) EA030376B1 (es)
EC (1) ECSP12012218A (es)
ES (4) ES2662588T3 (es)
HK (2) HK1177741A1 (es)
HR (3) HRP20160326T1 (es)
HU (3) HUE028723T2 (es)
IL (1) IL221823A (es)
LT (2) LT3354652T (es)
ME (2) ME02386B (es)
MX (5) MX354212B (es)
MY (2) MY175156A (es)
NO (1) NO3050882T3 (es)
NZ (1) NZ602313A (es)
PE (1) PE20130038A1 (es)
PH (1) PH12015502575B1 (es)
PL (3) PL3050882T3 (es)
PT (2) PT3050882T (es)
RS (3) RS57219B1 (es)
SG (1) SG183551A1 (es)
SI (3) SI3354652T1 (es)
SM (1) SMT201600085B (es)
TW (6) TWI766281B (es)
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