SI3050882T1 - Derivati piperidin-4-il azetidina, kot inhibitorji JAK1 - Google Patents

Derivati piperidin-4-il azetidina, kot inhibitorji JAK1 Download PDF

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Publication number
SI3050882T1
SI3050882T1 SI201131432T SI201131432T SI3050882T1 SI 3050882 T1 SI3050882 T1 SI 3050882T1 SI 201131432 T SI201131432 T SI 201131432T SI 201131432 T SI201131432 T SI 201131432T SI 3050882 T1 SI3050882 T1 SI 3050882T1
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disease
piperidin
salt
use according
compound
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SI201131432T
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English (en)
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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
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Incyte Holdings Corporation
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Application filed by Incyte Holdings Corporation filed Critical Incyte Holdings Corporation
Publication of SI3050882T1 publication Critical patent/SI3050882T1/sl

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    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
    • A61K31/435—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • 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
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
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    • A—HUMAN NECESSITIES
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    • C07D401/14—Heterocyclic 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Claims (8)

  1. Derivati piperidin-4-il azetidina, kot inhibitorji JAKI Patentni zahtevki
    1. Spojina, kije {l-{l-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il{-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1 H-pirazol-1 -il]azetidin-3-il}acetonitril ali njena farmacevtsko sprejemljiva sol, za uporabo v zdravljenju bolezni izbrane izmed zavrnitve vsadka in bolezni presadka proti gostitelju.
  2. 2. Spojina ali sol za uporabo po zahtevku 1, kjer je sol, sol {1 - {1 -[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il} -3 - [4-(7H-pirolo [2,3 -d]pirimidin-4-il)-lH-pirazol-l-il]azetidin-3-il}acetonitril adipinske kisline.
  3. 3. Spojina ali sol za uporabo po zahtevku 1 ali 2, kjer je bolezen zavrnitev vsadka.
  4. 4. Spojina ali sol za uporabo po zahtevku 1 ali 2, kjer je bolezen, bolezen presadka proti gostitelju.
  5. 5. Uporaba spoj ine, ki j e {1 - {1 - [3 -fluoro-2-(trifluorometil)izonikotinoil]piperidin-4- il} -3 - [4-(7H-pirolo[2,3 -d]pirimidin-4-il)-1 H-pirazol-1 -il] azetidin-3 -il} acetonitril, ali njene farmacevtsko sprejemljive soli, za pripravo zdravila za zdravljenje bolezni izbrane izmed zavrnitve vsadka in bolezni presadka proti gostitelju.
  6. 6. Uporaba po zahtevku 5, kjer je sol, sol {l-{l-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il} -3 - [4-(7H-pirolo [2,3-d]pirimidin-4-il)-1 H-pirazol-Ι-il]azetidin-3-il}acetonitril adipinske kisline.
  7. 7. Uporaba po zahtevku 5 ali 6, kjer je bolezen zavrnitev vsadka.
  8. 8. Uporaba po zahtevku 5 ali 6, kjer je bolezen, bolezen presadka proti gostitelju.
SI201131432T 2010-03-10 2011-03-09 Derivati piperidin-4-il azetidina, kot inhibitorji JAK1 SI3050882T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31258810P 2010-03-10 2010-03-10
US41560210P 2010-11-19 2010-11-19
EP15195698.4A EP3050882B1 (en) 2010-03-10 2011-03-09 Piperidin-4-yl azetidine derivatives as jak1 inhibitors

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SI3050882T1 true SI3050882T1 (sl) 2018-06-29

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SI201131892T SI3354652T1 (sl) 2010-03-10 2011-03-09 Derivati piperidin-4-il azetidina kot inhibitorji JAK1
SI201131432T SI3050882T1 (sl) 2010-03-10 2011-03-09 Derivati piperidin-4-il azetidina, kot inhibitorji JAK1
SI201130747A SI2545045T1 (sl) 2010-03-10 2011-03-09 Derivati piperidin-4-ila kot zaviralci JAK1

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US (6) US8765734B2 (sl)
EP (5) EP3354652B1 (sl)
JP (6) JP5858484B2 (sl)
KR (7) KR20220015492A (sl)
CN (1) CN102985417B (sl)
AR (1) AR081315A1 (sl)
AU (1) AU2011224484A1 (sl)
BR (1) BR112012022513A2 (sl)
CA (1) CA2792508C (sl)
CL (1) CL2012002501A1 (sl)
CO (1) CO6602158A2 (sl)
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CY (2) CY1120154T1 (sl)
DK (3) DK2545045T3 (sl)
EA (1) EA030376B1 (sl)
EC (1) ECSP12012218A (sl)
ES (4) ES2662588T3 (sl)
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IL (1) IL221823A (sl)
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MX (5) MX347851B (sl)
MY (2) MY175156A (sl)
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PE (1) PE20130038A1 (sl)
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PL (3) PL3354652T3 (sl)
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SG (1) SG183551A1 (sl)
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