EA201070012A1 - МЕТАБОЛИТЫ (R)-3-(4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА, ИНГИБИТОРА JANUS КИНАЗ - Google Patents

МЕТАБОЛИТЫ (R)-3-(4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА, ИНГИБИТОРА JANUS КИНАЗ

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Publication number
EA201070012A1
EA201070012A1 EA201070012A EA201070012A EA201070012A1 EA 201070012 A1 EA201070012 A1 EA 201070012A1 EA 201070012 A EA201070012 A EA 201070012A EA 201070012 A EA201070012 A EA 201070012A EA 201070012 A1 EA201070012 A1 EA 201070012A1
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EA
Eurasian Patent Office
Prior art keywords
pyrrolo
pyrazol
pyrimidin
janus
metabolites
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EA201070012A
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English (en)
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EA017790B1 (ru
Inventor
Джеймс Д. Роджерс
Аргириос Г. Арванитис
Джек Гуоен Ши
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Инсайт Корпорейшн
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Publication of EA201070012A1 publication Critical patent/EA201070012A1/ru
Publication of EA017790B1 publication Critical patent/EA017790B1/ru

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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

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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)
  • Genetics & Genomics (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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

Данное изобретение предлагает активные метаболиты 3-(4-(7Н-пирроло[2,3-d]пиримидин-4-ил)-1Н-пиразол-1-ил)-3-циклопентилпропаннитрила, которые модулируют активность Janus киназ и которые используют для лечения заболеваний, связанных с активностью Janus киназ, включая, например, связанные с иммунной системой болезни, кожные заболевания, миелоидные пролиферативные нарушения, рак и другие болезни.
EA201070012A 2007-06-13 2008-06-12 МЕТАБОЛИТЫ (R)-3-(4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА, ИНГИБИТОРА JANUS КИНАЗ EA017790B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US94369507P 2007-06-13 2007-06-13
PCT/US2008/066658 WO2008157207A2 (en) 2007-06-13 2008-06-12 Metabolites of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3- cyclopentylpropanenitrile

Publications (2)

Publication Number Publication Date
EA201070012A1 true EA201070012A1 (ru) 2010-06-30
EA017790B1 EA017790B1 (ru) 2013-03-29

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EA201070012A EA017790B1 (ru) 2007-06-13 2008-06-12 МЕТАБОЛИТЫ (R)-3-(4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА, ИНГИБИТОРА JANUS КИНАЗ

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US (5) US7834022B2 (ru)
EP (1) EP2173751B1 (ru)
JP (1) JP5479331B2 (ru)
KR (1) KR20100049008A (ru)
CN (1) CN101815717B (ru)
AR (1) AR067024A1 (ru)
AU (1) AU2008266182B8 (ru)
BR (1) BRPI0812563A2 (ru)
CA (1) CA2689158C (ru)
CL (1) CL2008001709A1 (ru)
CO (1) CO6251255A2 (ru)
CR (1) CR11149A (ru)
EA (1) EA017790B1 (ru)
EC (1) ECSP099821A (ru)
ES (1) ES2448868T3 (ru)
GE (1) GEP20125534B (ru)
HK (1) HK1141020A1 (ru)
IL (1) IL202429A0 (ru)
MX (2) MX339139B (ru)
NZ (1) NZ581801A (ru)
PL (1) PL2173751T3 (ru)
PT (1) PT2173751E (ru)
TW (1) TWI426911B (ru)
UA (1) UA99465C2 (ru)
WO (1) WO2008157207A2 (ru)
ZA (1) ZA200908820B (ru)

Families Citing this family (78)

* 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
ES2612196T3 (es) 2005-12-13 2017-05-12 Incyte Holdings Corporation Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus
EP2121692B1 (en) * 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
MX342814B (es) 2007-06-13 2016-10-13 Incyte Holdings Corp Sales de inhibidor de janus cinasa (r)-3-(4-7h-pirrolo[2,3-d]pirim idin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
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.
CN101910152B (zh) * 2007-11-16 2014-08-06 因塞特公司 作为janus激酶抑制剂的4-吡唑基-n-芳基嘧啶-2-胺和4-吡唑基-n-杂芳基嘧啶-2-胺
BRPI0908433A2 (pt) 2008-02-06 2019-09-24 Novartis Ag pirrolo[2,3-d]piridinas e empregos destas como inibidores tirosina cinase
MX2010010012A (es) 2008-03-11 2010-10-20 Incyte Corp Derivados de azetidina y ciclobutano como inhibidores de 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.
JOP20190230A1 (ar) * 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
PT2401267E (pt) * 2009-02-27 2014-04-10 Ambit Biosciences Corp Derivados de quinazolina moduladores de quinase jak e sua utilização em métodos
KR20120030447A (ko) 2009-05-22 2012-03-28 인사이트 코포레이션 Ｊａｋ 저해물질로서 ３-［４-（７ｈ-피롤로［２,３-ｄ］피리미딘-４-일）-１ｈ-피라졸-１-일］옥탄- 또는 헵탄-니트릴
CA2762174C (en) * 2009-05-22 2018-02-20 Incyte 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
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
US20120034226A1 (en) * 2009-09-16 2012-02-09 Riken Diagnostic method of skin inflammatory disease
EA021478B1 (ru) * 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
WO2011103423A1 (en) 2010-02-18 2011-08-25 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
RS60680B1 (sr) 2010-03-10 2020-09-30 Incyte Holdings Corp Piperidin-4-il azetidin derivati kao inhibitori jak1
WO2011130146A1 (en) * 2010-04-14 2011-10-20 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
KR20130102060A (ko) 2010-09-01 2013-09-16 암비트 바이오사이언시즈 코포레이션 퀴나졸린 화합물 및 이의 사용 방법
KR102027394B1 (ko) * 2010-11-02 2019-10-01 더 트러스티스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 탈모 질환의 치료 방법
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
MX357939B (es) 2011-02-18 2018-07-31 Novartis Pharma Ag Terapia de combinacion de inhibidor de objetivo de rapamicina en mamifero/janus cinasa (mtor/jak).
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 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
BR112014013224B1 (pt) * 2011-11-30 2023-03-07 Emory University Inibidores de jak antivirais úteis no tratamento ou prevenção de infecções retrovirais e outras infecções virais
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
IN2014DN10670A (ru) 2012-06-15 2015-08-28 Concert Pharmaceuticals Inc
US20150197525A1 (en) 2012-06-15 2015-07-16 Concert Pharmaceuticals, Inc. Deuterated derivatives of 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
US9181271B2 (en) 2012-11-01 2015-11-10 Incyte Holdings Corporation Tricyclic fused thiophene derivatives as JAK inhibitors
RS62329B1 (sr) 2012-11-15 2021-10-29 Incyte Holdings Corp Dozni oblici ruksolitiniba sa produženim vremenom oslobađanja
ES2900492T3 (es) 2013-03-06 2022-03-17 Incyte Holdings Corp Procesos y productos intermedios para elaborar un inhibidor de JAK
PT3231801T (pt) 2013-05-17 2019-05-24 Incyte Corp Sal de bipirazole como inibidor da jak
EA201690357A1 (ru) 2013-08-07 2016-07-29 Инсайт Корпорейшн Лекарственные формы с замедленным высвобождением для ингибитора jak1
AU2014309017A1 (en) 2013-08-20 2016-03-10 Incyte Corporation Survival benefit in patients with solid tumors with elevated C-reactive protein levels
CA2945151C (en) 2014-04-08 2022-08-02 Incyte Corporation Treatment of b-cell malignancies by a combination jak and pi3k inhibitors
EP3137471A1 (en) 2014-04-30 2017-03-08 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 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
WO2016024232A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
HRP20220738T1 (hr) 2014-08-11 2022-08-19 Acerta Pharma B.V. Terapijske kombinacije inhibitora btk, inhibitora pd-1 i/ili inhibitora pd-l1
UA119835C2 (uk) 2016-02-24 2019-08-12 Пфайзер Інк. ПОХІДНІ ПІРАЗОЛО[1,5-а]ПІРАЗИН-4-ІЛУ ЯК JAK-ІНГІБІТОРИ
EP3452039B1 (en) 2016-05-04 2024-07-03 Sun Pharmaceutical Industries, Inc. Treatment of hair loss disorders with deuterated jak inhibitors
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
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
IL311485A (en) 2018-02-16 2024-05-01 Incyte Corp JAK1 pathway inhibitors for the treatment of cytokine-related disorders
JP2021519772A (ja) 2018-03-30 2021-08-12 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ 炎症性皮膚疾患のバイオマーカー
DK3773593T3 (da) 2018-03-30 2024-05-27 Incyte Corp Behandling af hidradenitis suppurativa under anvendelse af JAK-inhibitorer
CA3097025A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
CA3224985A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
MX2021004946A (es) 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
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
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
CN113924301A (zh) * 2019-04-12 2022-01-11 北京普祺医药科技有限公司 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
AU2020378630A1 (en) 2019-11-08 2022-05-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CR20220280A (es) 2019-11-22 2022-09-02 Incyte Corp Terapia de combinación que comprende un inhibidor de alk2 y un inhibidor de jak2
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115836065A (zh) 2020-06-02 2023-03-21 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
US20230322787A1 (en) 2020-08-12 2023-10-12 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
CA3192055A1 (en) 2020-08-18 2022-02-24 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
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems 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
MX9800215A (es) 1995-07-06 1998-03-31 Novartis Ag Pirrolopirimidas y procesos para su preparacion.
PL345906A1 (en) 1998-06-04 2002-01-14 Abbott Lab Cell adhesion-inhibiting antinflammatory compounds
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
EP1087970B1 (en) 1998-06-19 2004-04-28 Pfizer Products Inc. PYRROLO 2,3-d]PYRIMIDINE COMPOUNDS
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
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
EP1382339B1 (en) * 1999-12-10 2007-12-05 Pfizer Products Inc. Compositions containing pyrrolo ¬2,3-d pyrimidine derivatives
EP1263759B1 (en) * 1999-12-24 2010-09-08 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
US6930115B2 (en) * 2000-06-23 2005-08-16 Mitsubishi Pharma Corporation Antitumor effect potentiators
CN100351253C (zh) * 2000-06-26 2007-11-28 辉瑞产品公司 作为免疫抑制剂的吡咯并[2,3－d]嘧啶化合物
CA2413330A1 (en) 2000-06-28 2002-01-03 Smithkline Beecham P.L.C. Wet milling process
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
CA2436487A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd. Methods of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
EP1414443B1 (en) 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
JP4456365B2 (ja) 2001-09-19 2010-04-28 アベンティス・ファーマ・ソシエテ・アノニム 化合物
WO2003037347A1 (en) 2001-10-30 2003-05-08 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea 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
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
JP2006509000A (ja) 2002-11-26 2006-03-16 ファイザー・プロダクツ・インク 移植片拒絶反応の処置の方法
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
JP2006518381A (ja) 2003-02-07 2006-08-10 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
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
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
JP2007512316A (ja) 2003-11-25 2007-05-17 ファイザー・プロダクツ・インク アテローム性動脈硬化症の治療方法
CN1893952A (zh) 2003-12-17 2007-01-10 辉瑞产品公司 用于治疗移植排斥的吡咯并[2,3－d]嘧啶化合物
US20050165029A1 (en) * 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
EP1730146B1 (en) 2004-03-30 2011-05-04 Vertex Pharmaceuticals Incorporated 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
BRPI0510627A (pt) 2004-05-03 2007-10-30 Novartis Ag combinações que compreendem um agonista do receptor s1p e um inibidor da jak3 quinase
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
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
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
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
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.
CN101142218B (zh) * 2005-02-03 2013-02-06 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并嘧啶
ATE540948T1 (de) 2005-05-20 2012-01-15 Vertex Pharma Pyrrolopyridine als proteinkinasehemmer
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
US8580802B2 (en) 2005-09-30 2013-11-12 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-D]pyrimidines as inhibitors of Janus kinases
ES2612196T3 (es) 2005-12-13 2017-05-12 Incyte Holdings Corporation Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus
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
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
CA2636189A1 (en) 2006-01-17 2007-07-26 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of janus kinases
EP2001884A1 (en) 2006-04-05 2008-12-17 Vertex Pharmaceuticals, Inc. Deazapurines useful as inhibitors of janus kinases
EP2121692B1 (en) * 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
MX342814B (es) 2007-06-13 2016-10-13 Incyte Holdings Corp Sales de inhibidor de janus cinasa (r)-3-(4-7h-pirrolo[2,3-d]pirim idin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
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.
CN101910152B (zh) 2007-11-16 2014-08-06 因塞特公司 作为janus激酶抑制剂的4-吡唑基-n-芳基嘧啶-2-胺和4-吡唑基-n-杂芳基嘧啶-2-胺
MX2010010012A (es) 2008-03-11 2010-10-20 Incyte Corp Derivados de azetidina y ciclobutano como inhibidores de 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.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
KR20120030447A (ko) 2009-05-22 2012-03-28 인사이트 코포레이션 Ｊａｋ 저해물질로서 ３-［４-（７ｈ-피롤로［２,３-ｄ］피리미딘-４-일）-１ｈ-피라졸-１-일］옥탄- 또는 헵탄-니트릴
CA2762174C (en) 2009-05-22 2018-02-20 Incyte 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
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
WO2011103423A1 (en) 2010-02-18 2011-08-25 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
RS60680B1 (sr) 2010-03-10 2020-09-30 Incyte Holdings Corp Piperidin-4-il azetidin derivati kao inhibitori jak1
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
MX357939B (es) 2011-02-18 2018-07-31 Novartis Pharma Ag Terapia de combinacion de inhibidor de objetivo de rapamicina en mamifero/janus cinasa (mtor/jak).
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 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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