JP5775070B2 - ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 - Google Patents

ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 Download PDF

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JP5775070B2
JP5775070B2 JP2012512060A JP2012512060A JP5775070B2 JP 5775070 B2 JP5775070 B2 JP 5775070B2 JP 2012512060 A JP2012512060 A JP 2012512060A JP 2012512060 A JP2012512060 A JP 2012512060A JP 5775070 B2 JP5775070 B2 JP 5775070B2
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pyrimidin
pyrrolo
pyridin
pyrrolidin
pyrazol
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Expired - Fee Related
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JP2012527483A (ja
JP2012527483A5 (https=
Inventor
ジェイムズ・ディ・ロジャース
ステイシー・シェパード
アーギリオス・ジー・アーバニティス
ハイシェン・ワン
ルイス・ストレース
ビバリー・フォルマー
リシン・シャオ
チュ・ウェンユ
ジョゼフ・ピー・グレン
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Incyte Corp
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Incyte Corp
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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
    • A61K31/505—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
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    • 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
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    • A61P17/04—Antipruritics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
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    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
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    • C—CHEMISTRY; METALLURGY
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
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    • C07D—HETEROCYCLIC COMPOUNDS
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  • Chemical & Material Sciences (AREA)
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  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2012512060A 2009-05-22 2010-05-21 ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 Expired - Fee Related JP5775070B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US18062209P 2009-05-22 2009-05-22
US61/180,622 2009-05-22
US22509209P 2009-07-13 2009-07-13
US61/225,092 2009-07-13
PCT/US2010/035783 WO2010135650A1 (en) 2009-05-22 2010-05-21 N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS

Publications (3)

Publication Number Publication Date
JP2012527483A JP2012527483A (ja) 2012-11-08
JP2012527483A5 JP2012527483A5 (https=) 2013-07-04
JP5775070B2 true JP5775070B2 (ja) 2015-09-09

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JP2012512060A Expired - Fee Related JP5775070B2 (ja) 2009-05-22 2010-05-21 ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体

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US (2) US8716303B2 (https=)
EP (1) EP2432555B1 (https=)
JP (1) JP5775070B2 (https=)
KR (1) KR101771401B1 (https=)
CN (1) CN102458581B (https=)
AR (1) AR076794A1 (https=)
AU (1) AU2010249380B2 (https=)
BR (1) BRPI1012159B1 (https=)
CA (1) CA2762174C (https=)
CL (1) CL2011002956A1 (https=)
CO (1) CO6440524A2 (https=)
CR (1) CR20110620A (https=)
EA (1) EA025520B1 (https=)
ES (1) ES2487542T3 (https=)
IL (1) IL216463A (https=)
MX (1) MX2011012353A (https=)
MY (1) MY156727A (https=)
NZ (1) NZ596479A (https=)
SG (1) SG176130A1 (https=)
TW (1) TW201100429A (https=)
WO (1) WO2010135650A1 (https=)
ZA (1) ZA201108544B (https=)

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JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
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WO2010135650A1 (en) 2010-11-25
EP2432555A1 (en) 2012-03-28
CR20110620A (es) 2012-02-02
AU2010249380B2 (en) 2015-08-20
ZA201108544B (en) 2013-04-24
IL216463A0 (en) 2012-02-29
ES2487542T3 (es) 2014-08-21
SG176130A1 (en) 2011-12-29
EP2432555B1 (en) 2014-04-30
EA201171454A1 (ru) 2012-06-29
CO6440524A2 (es) 2012-05-15
CN102458581A (zh) 2012-05-16
MY156727A (en) 2016-03-15
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NZ596479A (en) 2014-01-31
US8716303B2 (en) 2014-05-06
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EA025520B1 (ru) 2017-01-30
US20100298334A1 (en) 2010-11-25
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BRPI1012159B1 (pt) 2022-01-25
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US9334274B2 (en) 2016-05-10
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