CR11149A - METABOLITOS DEL INHIBIDOR DE JANUS QUINASA (R)-3-(4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL)-3-CICLOPENTILPROPANONITRILO - Google Patents

METABOLITOS DEL INHIBIDOR DE JANUS QUINASA (R)-3-(4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL)-3-CICLOPENTILPROPANONITRILO

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Publication number
CR11149A
CR11149A CR11149A CR11149A CR11149A CR 11149 A CR11149 A CR 11149A CR 11149 A CR11149 A CR 11149A CR 11149 A CR11149 A CR 11149A CR 11149 A CR11149 A CR 11149A
Authority
CR
Costa Rica
Prior art keywords
janus
metabolites
cyclopentilpropanonitrile
quinasa
pirimidin
Prior art date
Application number
CR11149A
Other languages
English (en)
Inventor
James D Rodgers
Argyrios G Arvanitis
Jack Guoen Shi
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.)
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Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of CR11149A publication Critical patent/CR11149A/es

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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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Transplantation (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)

Abstract

La presente invencion provee metabolitos activos de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo que modulan la actividad de janus quinasas y son utiles para tratamiento de enfermedades relacionadas con la actividad de janus quinasas que incluyen, por ejemplo, enfermedades relacionadas con el sistema inmune, trastornos cutaneos, trastornos proliferativos mieloides, cancer y otras enfermedades.
CR11149A 2007-06-13 2009-12-07 METABOLITOS DEL INHIBIDOR DE JANUS QUINASA (R)-3-(4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL)-3-CICLOPENTILPROPANONITRILO CR11149A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94369507P 2007-06-13 2007-06-13

Publications (1)

Publication Number Publication Date
CR11149A true CR11149A (es) 2010-02-04

Family

ID=40029276

Family Applications (1)

Application Number Title Priority Date Filing Date
CR11149A CR11149A (es) 2007-06-13 2009-12-07 METABOLITOS DEL INHIBIDOR DE JANUS QUINASA (R)-3-(4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL)-3-CICLOPENTILPROPANONITRILO

Country Status (25)

Country Link
US (5) US7834022B2 (es)
EP (1) EP2173751B1 (es)
JP (1) JP5479331B2 (es)
KR (1) KR20100049008A (es)
CN (1) CN101815717B (es)
AR (1) AR067024A1 (es)
AU (1) AU2008266182B8 (es)
BR (1) BRPI0812563A2 (es)
CA (1) CA2689158C (es)
CL (1) CL2008001709A1 (es)
CO (1) CO6251255A2 (es)
CR (1) CR11149A (es)
EA (1) EA017790B1 (es)
EC (1) ECSP099821A (es)
ES (1) ES2448868T3 (es)
GE (1) GEP20125534B (es)
IL (1) IL202429A0 (es)
MX (2) MX2009013403A (es)
NZ (1) NZ581801A (es)
PL (1) PL2173751T3 (es)
PT (1) PT2173751E (es)
TW (1) TWI426911B (es)
UA (1) UA99465C2 (es)
WO (1) WO2008157207A2 (es)
ZA (1) ZA200908820B (es)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
TWI630207B (zh) 2005-12-13 2018-07-21 英塞特控股公司 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
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.
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
ES2569528T3 (es) * 2007-11-16 2016-05-11 Incyte Holdings Corporation 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
CN101981036B (zh) 2008-02-06 2013-09-04 诺瓦提斯公司 吡咯并[2,3-d]嘧啶及其作为酪氨酸激酶抑制剂的用途
PL2288610T3 (pl) 2008-03-11 2017-12-29 Incyte Holdings Corporation Azetydynowe i cyklobutanowe pochodne jako inhibitory jak
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.
TWI665200B (zh) 2009-01-15 2019-07-11 英塞特公司 製造jak抑制劑之方法及相關中間化合物
PL2401267T3 (pl) 2009-02-27 2014-06-30 Ambit Biosciences Corp Pochodne chinazoliny modulujące kinazę JAK i ich zastosowanie w metodach
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
JP2011083279A (ja) * 2009-09-16 2011-04-28 Institute Of Physical & Chemical Research 皮膚炎症性疾患の診断方法
CN105541847B (zh) * 2009-10-09 2019-08-16 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
CN102844317B (zh) 2010-02-18 2015-06-03 因西特公司 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物
EP3050882B1 (en) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
PH12012502046A1 (en) * 2010-04-14 2017-07-26 Array Biopharma Inc 5,7-substituted~imidazo[1,2-c]pyrimidines as inhibitors of jak kinases
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
CN103298805A (zh) 2010-09-01 2013-09-11 埃姆比特生物科学公司 喹唑啉化合物及其使用方法
PL2635299T3 (pl) * 2010-11-02 2020-03-31 The Trustees Of Columbia University In The City Of New York Sposoby leczenia zaburzeń utraty włosów
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
HK1198579A1 (en) 2011-08-10 2015-04-30 Novartis Pharma Ag Jak p13k/mtor combination therapy
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AU2012323399A1 (en) * 2011-10-12 2014-05-29 Array Biopharma Inc. 5,7-substituted-imidazo[1,2-c]pyrimidines
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
CN104185420B (zh) * 2011-11-30 2017-06-09 埃默里大学 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
ES2867048T3 (es) 2012-06-15 2021-10-20 Concert Pharmaceuticals Inc Derivados deuterados de ruxolitinib
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
CA2879603A1 (en) 2012-07-27 2014-01-30 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
AU2013337824B2 (en) 2012-11-01 2018-03-08 Incyte Holdings Corporation Tricyclic fused thiophene derivatives as JAK inhibitors
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
CN105189509B (zh) 2013-03-06 2017-12-19 因赛特公司 用于制备jak抑制剂的方法及中间体
SMT202100040T1 (it) 2013-05-17 2021-03-15 Incyte Corp Derivati di bipirazolo come inibitori di jak
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
EP3035966A1 (en) 2013-08-20 2016-06-29 Incyte Corporation Survival benefit in patients with solid tumors with elevated c-reactive protein levels
KR20240153401A (ko) 2014-04-08 2024-10-22 인사이트 홀딩스 코포레이션 Jak 및 pi3k 억제제 조합에 의한 b-세포 악성종양의 치료
JP2017514832A (ja) 2014-04-30 2017-06-08 インサイト・コーポレイションIncyte Corporation Jak1抑制剤を調製する方法及びその新しい形態
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
EP3179991B1 (en) 2014-08-11 2021-10-06 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor and a bcl-2 inhibitor
SI3179992T1 (sl) 2014-08-11 2022-09-30 Acerta Pharma B.V. Terapevtske kombinacije zaviralca BTK, zaviralca PD-1 in/ali zaviralca PD-L1
AR101504A1 (es) 2014-08-11 2016-12-21 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6
RS60261B1 (sr) 2016-02-24 2020-06-30 Pfizer Pirazolo[1,5-a]pirazin-4-il derivativi kao jak-inhibitori
HRP20241345T1 (hr) 2016-05-04 2024-12-20 Sun Pharmaceutical Industries, Inc. Liječenje poremećaja gubitka kose deuteriranim inhibitorima jak
CN107513067A (zh) 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
EP3746429B1 (en) 2018-01-30 2022-03-09 Incyte Corporation Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
KR102830476B1 (ko) 2018-02-16 2025-07-08 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
EP3775284A1 (en) 2018-03-30 2021-02-17 Incyte Corporation Biomarkers for inflammatory skin disease
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
SG11202010092XA (en) 2018-04-13 2020-11-27 Incyte Corp Biomarkers for graft-versus-host disease
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案
JP7286755B2 (ja) 2018-07-31 2023-06-05 ロクソ オンコロジー, インコーポレイテッド (s)-5-アミノ-3-(4-((5-フルオロ-2-メトキシベンズアミド)メチル)フェニル)-1-(1,1,1-トリフルオロプロパン-2-イル)-1h-ピラゾール-4-カルボキサミドの噴霧乾燥分散体および製剤
IL282643B2 (en) 2018-10-31 2025-08-01 Incyte Corp A selective jak1 inhibitor for use in a method of treating hematological disease
KR102645439B1 (ko) 2018-11-09 2024-03-11 (주)아모레퍼시픽 아우레오바시디움 풀루란스 균주의 배양물 또는 추출물을 포함하는 저자극 피부 재생 또는 피부 진정용 조성물
JP2022515198A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド FGFRチロシンキナーゼの阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3,5-二甲氧基苯基)氨基)喹喔啉衍生物
KR20210116488A (ko) 2018-12-20 2021-09-27 인사이트 코포레이션 액티빈 수용체-유사 키나제-2의 억제제로서의 이미다조피리다진 및 이미다조피리딘 화합물
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
WO2020201362A2 (en) 2019-04-02 2020-10-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
BR112021020339A2 (pt) * 2019-04-12 2021-12-07 Primegene Beijing Co Ltd Compostos derivados de pirazolopirazina, composição farmacêutica, e uso dos mesmos
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
JP2022551649A (ja) 2019-10-10 2022-12-12 インサイト・コーポレイション 移植片対宿主病のバイオマーカー
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
JP7717065B2 (ja) 2019-11-22 2025-08-01 インサイト コーポレーション Alk2阻害剤及びjak2阻害剤を含む併用療法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CA3177830A1 (en) 2020-05-13 2021-11-18 Maria BECONI Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
CN115836065B (zh) 2020-06-02 2025-07-01 因赛特公司 制备jak1抑制剂的方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022036030A1 (en) 2020-08-12 2022-02-17 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
US11897889B2 (en) 2020-08-18 2024-02-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
WO2022040180A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak inhibitor
AU2021396231A1 (en) 2020-12-08 2023-06-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
SI4333840T1 (sl) 2021-05-03 2026-01-30 Incyte Corporation Zaviralci poti jak1 za zdravljenje pruriga nodularisa
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
AU2022328272A1 (en) 2021-08-11 2024-02-22 Sun Pharmaceutical Industries, Inc. Treatment of hair loss disorders with deuterated jak inhibitors
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation

Family Cites Families (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
EP0836602B1 (en) 1995-07-05 2002-01-30 E.I. Du Pont De Nemours And Company Fungicidal pyrimidinones
ATE212993T1 (de) 1995-07-06 2002-02-15 Novartis Erfind Verwalt Gmbh Pyrolopyrimidine und verfahren zu ihrer herstellung
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
IL139811A0 (en) 1998-06-04 2002-02-10 Abbott Lab Cell adhesion-inhibiting antinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
TW505646B (en) 1998-06-19 2002-10-11 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds
WO2000009495A1 (en) 1998-08-11 2000-02-24 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
PT1382339E (pt) * 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
WO2001047922A2 (en) * 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
ATE465756T1 (de) * 2000-06-23 2010-05-15 Mitsubishi Tanabe Pharma Corp Antitumoreffekt-verstärker
PL359563A1 (pl) 2000-06-26 2004-08-23 Pfizer Products Inc. Związki pirolo [2,3-d] pirymidynowe jako środki immunosupresyjne
DE60105023T2 (de) 2000-06-28 2005-08-18 Smithkline Beecham P.L.C., Brentford Nassvermahlungsverfahren
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
JP2004528295A (ja) 2001-01-30 2004-09-16 サイトピア ピーティワイ リミテッド キナーゼ阻害方法
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
CA2455181C (en) 2001-08-01 2010-04-06 Merck & Co., Inc. Benzimidazo[4,5-f]isoquinolinone derivatives
MXPA04002243A (es) 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.
CN101703509A (zh) 2001-10-30 2010-05-12 诺瓦提斯公司 作为flt3受体酪氨酸激酶活性抑制剂的星形孢菌素衍生物
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
WO2004041814A1 (en) 2002-11-04 2004-05-21 Vertex Pharmaceuticals Incorporated Heteroaryl-pyramidine derivatives as jak inhibitors
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
WO2004047843A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2515132C (en) 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
CA2545192A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
CA2549485A1 (en) 2003-12-17 2005-07-07 Pfizer Products Inc. Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
US20050239806A1 (en) * 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
NZ584499A (en) 2004-03-30 2011-08-26 Vertex Pharma Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
KR20070006889A (ko) 2004-05-03 2007-01-11 노파르티스 아게 S1p 수용체 작용제 및 jak3 키나제 억제제를 포함하는조합물
WO2005110410A2 (en) 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
BRPI0517887A (pt) 2004-11-24 2008-10-21 Novartis Ag combinações de inibidores de jaks
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
RU2434871C2 (ru) * 2005-02-03 2011-11-27 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы
NZ564065A (en) 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
JP5119154B2 (ja) * 2005-09-22 2013-01-16 インサイト・コーポレイション Janusキナーゼの四環系阻害剤
EP2532667A1 (en) 2005-09-30 2012-12-12 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
US20130137681A1 (en) 2005-12-13 2013-05-30 Incyte Corporation HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
TWI630207B (zh) 2005-12-13 2018-07-21 英塞特控股公司 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
AR060316A1 (es) 2006-01-17 2008-06-11 Vertex Pharma Azaindoles de utilidad como inhibidores de janus quinasas
CN101460499A (zh) 2006-04-05 2009-06-17 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的去氮杂嘌呤
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
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.
ES2569528T3 (es) 2007-11-16 2016-05-11 Incyte Holdings Corporation 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
PL2288610T3 (pl) 2008-03-11 2017-12-29 Incyte Holdings Corporation Azetydynowe i cyklobutanowe pochodne jako inhibitory jak
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.
TWI665200B (zh) 2009-01-15 2019-07-11 英塞特公司 製造jak抑制劑之方法及相關中間化合物
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
CN105541847B (zh) 2009-10-09 2019-08-16 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
CN102844317B (zh) 2010-02-18 2015-06-03 因西特公司 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物
EP3050882B1 (en) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
HK1198579A1 (en) 2011-08-10 2015-04-30 Novartis Pharma Ag Jak p13k/mtor combination therapy
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak

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