EA019504B1 - ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ - Google Patents

ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ Download PDF

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Publication number
EA019504B1
EA019504B1 EA200870048A EA200870048A EA019504B1 EA 019504 B1 EA019504 B1 EA 019504B1 EA 200870048 A EA200870048 A EA 200870048A EA 200870048 A EA200870048 A EA 200870048A EA 019504 B1 EA019504 B1 EA 019504B1
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EA
Eurasian Patent Office
Prior art keywords
pyrrolo
pyrazol
pyrimidin
propannitrile
phenyl
Prior art date
Application number
EA200870048A
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English (en)
Russian (ru)
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EA200870048A1 (ru
Inventor
Джеймс Д. Роджерс
Стейси Шепард
Томас П. Мадускуи
Хайшэн Ван
Нику Фалахатпишех
Мария Рафальски
Аргириос Г. Арванитис
Льюис Сторейс
Рави Кумар Джаллури
Джордан С. Фридман
Кришна Вадди
Original Assignee
Инсайт Корпорейшн
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Application filed by Инсайт Корпорейшн filed Critical Инсайт Корпорейшн
Publication of EA200870048A1 publication Critical patent/EA200870048A1/ru
Publication of EA019504B1 publication Critical patent/EA019504B1/ru

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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EA200870048A 2005-12-13 2006-12-12 ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ EA019504B1 (ru)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US74990505P 2005-12-13 2005-12-13
US81023106P 2006-06-02 2006-06-02
US85062506P 2006-10-10 2006-10-10
US85687206P 2006-11-03 2006-11-03
US85940406P 2006-11-16 2006-11-16
PCT/US2006/047369 WO2007070514A1 (en) 2005-12-13 2006-12-12 Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
EA200870048A1 EA200870048A1 (ru) 2009-02-27
EA019504B1 true EA019504B1 (ru) 2014-04-30

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ID=37903501

Family Applications (3)

Application Number Title Priority Date Filing Date
EA200870048A EA019504B1 (ru) 2005-12-13 2006-12-12 ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
EA201691294A EA036785B1 (ru) 2005-12-13 2006-12-12 ГЕТЕРОАРИЛ-ЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
EA201200132A EA035795B1 (ru) 2005-12-13 2006-12-12 Гетероарилзамещенные пирроло[2,3-b]пиридины в качестве ингибиторов янус-киназы

Family Applications After (2)

Application Number Title Priority Date Filing Date
EA201691294A EA036785B1 (ru) 2005-12-13 2006-12-12 ГЕТЕРОАРИЛ-ЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
EA201200132A EA035795B1 (ru) 2005-12-13 2006-12-12 Гетероарилзамещенные пирроло[2,3-b]пиридины в качестве ингибиторов янус-киназы

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US (16) US7598257B2 (OSRAM)
EP (10) EP2348023B9 (OSRAM)
JP (4) JP5017278B2 (OSRAM)
KR (4) KR101391900B1 (OSRAM)
CN (4) CN103214484B (OSRAM)
AR (1) AR057995A1 (OSRAM)
AT (1) ATE525374T1 (OSRAM)
AU (1) AU2006326548B2 (OSRAM)
BE (1) BE2013C014I2 (OSRAM)
BR (1) BRPI0619817B8 (OSRAM)
CA (1) CA2632466C (OSRAM)
CR (2) CR10065A (OSRAM)
CY (8) CY1112762T1 (OSRAM)
DK (7) DK2474545T3 (OSRAM)
EA (3) EA019504B1 (OSRAM)
EC (2) ECSP088540A (OSRAM)
ES (10) ES2612196T3 (OSRAM)
FR (2) FR13C0007I2 (OSRAM)
HR (7) HRP20110903T1 (OSRAM)
HU (7) HUE041382T2 (OSRAM)
IL (3) IL192019A (OSRAM)
LT (6) LT2474545T (OSRAM)
LU (1) LU92137I2 (OSRAM)
ME (1) ME01312B (OSRAM)
MX (1) MX346183B (OSRAM)
MY (2) MY159449A (OSRAM)
NZ (2) NZ569015A (OSRAM)
PL (7) PL2455382T3 (OSRAM)
PT (7) PT2474545T (OSRAM)
RS (7) RS54181B9 (OSRAM)
SG (3) SG10201506912RA (OSRAM)
SI (7) SI1966202T1 (OSRAM)
TW (6) TWI553008B (OSRAM)
UA (2) UA116187C2 (OSRAM)
WO (1) WO2007070514A1 (OSRAM)
ZA (1) ZA200805165B (OSRAM)

Cited By (3)

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WO2017082759A1 (ru) * 2015-11-13 2017-05-18 Акционерное Общество "Р-Фарм" (Ао "Р-Фарм") {3-[(7н-пирролo[2,3-d]пиримидин-4-ил)-азолил]азетидин-3-ил}-ацетонитрилы в качестве ингибиторов янус киназ
RU2644155C1 (ru) * 2016-12-12 2018-02-08 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") 2-(3-(4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1H-пиразол-1-ил)-1-(этилсульфонил)азетидин-3-ил)ацетонитрила геминафтилдисульфонат в качестве ингибитора Янус киназ
RU2701206C2 (ru) * 2014-12-16 2019-09-25 Центаурус Биофарма Ко., Лтд. Пирролопиримидиновое соединение

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EP1928874A1 (en) * 2005-09-16 2008-06-11 AstraZeneca AB Heterobicyclic compounds as glucokinase activators
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
KR101467723B1 (ko) * 2005-11-01 2014-12-03 탈자진 인코포레이티드 키나제의 비-아릴 메타-피리미딘 억제제
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
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JP5140600B2 (ja) * 2005-12-23 2013-02-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー オーロラキナーゼのアザインドール阻害薬
JP5099005B2 (ja) * 2006-04-03 2012-12-12 アステラス製薬株式会社 ヘテロ化合物
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CA2668652C (en) 2006-11-20 2018-06-12 President And Fellows Of Harvard College Inhibitors of voltage-gated ion channels for use in treating pain and pruritis
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CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
EP4606378A3 (en) * 2007-06-13 2025-11-05 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-( 4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3- cyclopentylprop anenitrile
EP2176249A2 (en) * 2007-07-02 2010-04-21 Boehringer Ingelheim International GmbH New chemical compounds
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WO2009049028A1 (en) * 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
JP2011500806A (ja) * 2007-10-25 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
JP5480813B2 (ja) * 2007-11-16 2014-04-23 インサイト・コーポレイション Janusキナーゼ阻害剤としての置換複素環
BRPI0908433A2 (pt) * 2008-02-06 2019-09-24 Novartis Ag pirrolo[2,3-d]piridinas e empregos destas como inibidores tirosina cinase
US20110105436A1 (en) * 2008-03-10 2011-05-05 Auckland Uniservices Limited Heteroaryl compounds, compositions, and methods of use in cancer treatment
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AR071717A1 (es) 2008-05-13 2010-07-07 Array Biopharma Inc Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer.
JP2011525892A (ja) * 2008-06-18 2011-09-29 メルク・シャープ・エンド・ドーム・コーポレイション Janusキナーゼの阻害剤
BRPI0909945A2 (pt) * 2008-06-20 2015-07-28 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
BRPI0910021A2 (pt) * 2008-06-20 2015-09-01 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinas em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
AT507187B1 (de) 2008-10-23 2010-03-15 Helmut Dr Buchberger Inhalator
JOP20190230A1 (ar) * 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
US8765727B2 (en) * 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
AU2010249380B2 (en) * 2009-05-22 2015-08-20 Incyte Holdings Corporation 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
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