PL2272517T5 - Orto-skondensowane pochodne pirydynowe i pirymidynowe (np. puryny) jako inhibitory kinaz białkowych - Google Patents

Orto-skondensowane pochodne pirydynowe i pirymidynowe (np. puryny) jako inhibitory kinaz białkowych

Info

Publication number
PL2272517T5
PL2272517T5 PL10184485T PL10184485T PL2272517T5 PL 2272517 T5 PL2272517 T5 PL 2272517T5 PL 10184485 T PL10184485 T PL 10184485T PL 10184485 T PL10184485 T PL 10184485T PL 2272517 T5 PL2272517 T5 PL 2272517T5
Authority
PL
Poland
Prior art keywords
purines
ortho
protein kinases
pyrimidine derivatives
kinases inhibitors
Prior art date
Application number
PL10184485T
Other languages
English (en)
Other versions
PL2272517T3 (pl
Inventor
Valerio Berdini
Robert George Boyle
Gordon Saxty
David Winter Walker
Steven John Woodhead
Paul Graham Wyatt
John Caldwell
Ian Collins
Tatiana Faria Da Fonseca
Alastair Donald
Original Assignee
Astex Therapeutics Ltd
Cancer Research Tech Ltd
The Institute Of Cancer Res Royal Cancer Hospital
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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35715573&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PL2272517(T5) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0423655A external-priority patent/GB0423655D0/en
Application filed by Astex Therapeutics Ltd, Cancer Research Tech Ltd, The Institute Of Cancer Res Royal Cancer Hospital filed Critical Astex Therapeutics Ltd
Publication of PL2272517T3 publication Critical patent/PL2272517T3/pl
Publication of PL2272517T5 publication Critical patent/PL2272517T5/pl

Links

Classifications

    • 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • 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
    • 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
    • A61K31/52Purines, e.g. adenine
    • 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
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
PL10184485T 2004-10-25 2005-10-25 Orto-skondensowane pochodne pirydynowe i pirymidynowe (np. puryny) jako inhibitory kinaz białkowych PL2272517T5 (pl)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US62182104P 2004-10-25 2004-10-25
GB0423655A GB0423655D0 (en) 2004-10-25 2004-10-25 Pharmaceutical compounds
US68411905P 2005-05-24 2005-05-24
EP20050797685 EP1812004B1 (en) 2004-10-25 2005-10-25 Ortho- condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors
EP10184485.0A EP2272517B2 (en) 2004-10-25 2005-10-25 Ortho -condensed pyridine and pyrimidine derivatives (e.g. purines) as protein kinases inhibitors

Publications (2)

Publication Number Publication Date
PL2272517T3 PL2272517T3 (pl) 2015-04-30
PL2272517T5 true PL2272517T5 (pl) 2018-04-30

Family

ID=35715573

Family Applications (1)

Application Number Title Priority Date Filing Date
PL10184485T PL2272517T5 (pl) 2004-10-25 2005-10-25 Orto-skondensowane pochodne pirydynowe i pirymidynowe (np. puryny) jako inhibitory kinaz białkowych

Country Status (14)

Country Link
US (3) US8546407B2 (pl)
EP (2) EP2272517B2 (pl)
JP (1) JP5128284B2 (pl)
AR (1) AR051342A1 (pl)
AT (1) ATE513549T1 (pl)
CY (1) CY1115946T1 (pl)
DK (1) DK2272517T4 (pl)
ES (1) ES2523266T5 (pl)
MY (1) MY179032A (pl)
PL (1) PL2272517T5 (pl)
PT (1) PT2272517E (pl)
SI (1) SI2272517T2 (pl)
UY (1) UY29176A1 (pl)
WO (1) WO2006046024A1 (pl)

Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
NZ564065A (en) * 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
KR20080026654A (ko) 2005-07-14 2008-03-25 아스텔라스세이야쿠 가부시키가이샤 헤테로시클릭 야누스 키나제 3 억제제
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
DE102005037733A1 (de) * 2005-08-10 2007-02-15 Merck Patent Gmbh Adeninderivate
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
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
US20070208053A1 (en) * 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
EP2029592A1 (en) * 2006-04-25 2009-03-04 Astex Therapeutics Limited Pharmaceutical compounds
US20090082370A1 (en) * 2006-04-25 2009-03-26 Neil Thomas Thompson Pharmaceutical Combinations of PK Inhibitors and Other Active Agents
WO2007125321A2 (en) * 2006-04-25 2007-11-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
WO2008012635A2 (en) * 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
US8227603B2 (en) 2006-08-01 2012-07-24 Cytokinetics, Inc. Modulating skeletal muscle
US8299248B2 (en) 2006-08-02 2012-10-30 Cytokinetics, Incorporated Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols and methods for their use
EP2666777A1 (en) 2006-08-02 2013-11-27 Cytokinetics, Inc. Certain chemical entities having an imidazo<4,5-b>pyrazin-2(3H)-one core, compositions and methods
US20090318476A1 (en) * 2006-08-09 2009-12-24 Merck Frosst Canada Ltd. Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
AR064415A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de pirrolo-piperidinas y purinas,composiciones farmaceuticas que los contienen y usos en trastornos y/o enfermedades mediadas por pka y pkb.
AR064416A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
EP2139478A4 (en) * 2007-03-30 2010-05-05 Cytokinetics Inc CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
JP2010527915A (ja) * 2007-04-26 2010-08-19 アバロン ファーマシューティカルズ,インコーポレイテッド 多重環化合物及びその用途
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
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
CN104119336B (zh) * 2007-10-05 2016-08-24 维拉斯通股份有限公司 嘧啶取代的嘌呤衍生物
AU2008309383B2 (en) 2007-10-11 2012-04-19 Astrazeneca Ab Pyrrolo [2, 3 -D] pyrimidin derivatives as protein kinase B inhibitors
PL2288610T3 (pl) 2008-03-11 2017-12-29 Incyte Holdings Corporation Azetydynowe i cyklobutanowe pochodne jako inhibitory jak
US8193202B2 (en) 2008-04-21 2012-06-05 Lexicon Pharmaceuticals, Inc. LIMK2 inhibitors, compositions comprising them, and methods of their use
AR074072A1 (es) 2008-11-11 2010-12-22 Lilly Co Eli Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme
KR20110075015A (ko) 2008-11-11 2011-07-05 일라이 릴리 앤드 캄파니 P70 s6 키나제 억제제 및 egfr 억제제 조합 요법
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
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
EA020151B1 (ru) 2009-10-23 2014-09-30 Эли Лилли Энд Компани Ингибиторы akt и фармацевтические составы, их содержащие
PT2496567T (pt) 2009-11-05 2017-11-15 Rhizen Pharmaceuticals S A Novos moduladores de quinase benzopiran
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
US8946433B2 (en) 2010-09-17 2015-02-03 Mallinckrodt Llc Process for the preparation of sufentanil base and related compounds
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
JP5927201B2 (ja) 2010-12-16 2016-06-01 カルチャン リミテッド Ask1阻害ピロロピリミジン誘導体
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
BR112013025410A2 (pt) 2011-04-01 2016-12-20 Astrazeneca Ab tratamento terapêutico
RS58326B1 (sr) 2011-05-04 2019-03-29 Rhizen Pharmaceuticals S A Nova jedinjenja kao modulatori proteinskih kinaza
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
WO2013010015A2 (en) 2011-07-13 2013-01-17 Cytokinetics, Inc. Combination als therapy
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
CA2856646C (en) 2011-11-30 2020-01-14 Astrazeneca Ab Combination treatment of cancer
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
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
KR101988079B1 (ko) 2012-07-04 2019-06-11 리젠 파마슈티컬스 소시에떼 아노님 선택적 pi3k 델타 억제제
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
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
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
CN108289867A (zh) 2015-07-02 2018-07-17 地平线孤儿病有限责任公司 Ado-抗性的半胱胺类似物和其用途
TW201726140A (zh) 2015-09-17 2017-08-01 瑞典商阿斯特捷利康公司 治療癌症之新型生物標記及方法
US12430543B2 (en) 2017-04-04 2025-09-30 Hailo Technologies Ltd. Structured sparsity guided training in an artificial neural network
US10387298B2 (en) 2017-04-04 2019-08-20 Hailo Technologies Ltd Artificial neural network incorporating emphasis and focus techniques
US11238334B2 (en) 2017-04-04 2022-02-01 Hailo Technologies Ltd. System and method of input alignment for efficient vector operations in an artificial neural network
US11544545B2 (en) 2017-04-04 2023-01-03 Hailo Technologies Ltd. Structured activation based sparsity in an artificial neural network
US11551028B2 (en) 2017-04-04 2023-01-10 Hailo Technologies Ltd. Structured weight based sparsity in an artificial neural network
US11615297B2 (en) 2017-04-04 2023-03-28 Hailo Technologies Ltd. Structured weight based sparsity in an artificial neural network compiler
EP3697786B1 (en) 2017-10-18 2022-08-31 Blueprint Medicines Corporation Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase
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)
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
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
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL297170A (pl) 1963-04-04 1900-01-01
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
IT1252567B (it) 1991-12-20 1995-06-19 Italfarmaco Spa Derivati di 5-isochinolinsolfonammidi inibitori delle protein-chinasi
GB9312853D0 (en) 1993-06-22 1993-08-04 Euro Celtique Sa Chemical compounds
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
US6140317A (en) * 1996-01-23 2000-10-31 Novartis Ag Pyrrolopyrimidines and processes for their preparation
EP0944388A4 (en) 1996-04-03 2001-08-16 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
CA2744096C (en) 1996-07-31 2013-07-30 Laboratory Corporation Of America Holdings Biomarkers and targets for diagnosis, prognosis and management of prostate disease
US6432947B1 (en) * 1997-02-19 2002-08-13 Berlex Laboratories, Inc. N-heterocyclic derivatives as NOS inhibitors
US6187778B1 (en) 1997-08-05 2001-02-13 Pfizer Inc. 4-aminopyrrole (3, 2-D) pyrimidines as neuropeptide Y receptor antagonists
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
NZ508314A (en) 1998-06-02 2004-03-26 Osi Pharm Inc Pyrrolo[2,3d]pyrimidine compositions and their use
IL139811A0 (en) 1998-06-04 2002-02-10 Abbott Lab Cell adhesion-inhibiting antinflammatory compounds
TW505646B (en) 1998-06-19 2002-10-11 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
US6262066B1 (en) 1998-07-27 2001-07-17 Schering Corporation High affinity ligands for nociceptin receptor ORL-1
HK1045306A1 (zh) 1999-06-03 2002-11-22 Abbott Laboratories 抑制细胞黏附的抗炎化合物
US7160890B2 (en) * 1999-12-02 2007-01-09 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
AU2728201A (en) 1999-12-21 2001-07-03 Sugen, Inc. 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors
IL136458A0 (en) 2000-05-30 2001-06-14 Peptor Ltd Protein kinase inhibitors
ES2251512T3 (es) 2000-08-31 2006-05-01 F. Hoffmann-La Roche Ag Derivados de quinazolina como antagonista adrenergicos alfa-1.
EP1347980A4 (en) 2000-12-01 2005-02-09 Osi Pharm Inc RECEPTOR SPECIFIC COMPOUNDS OF ADENOSINE-A1, -A2A, AND-A3 AND USES THEREOF
US6673802B2 (en) 2000-12-01 2004-01-06 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6680324B2 (en) * 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
NZ555911A (en) 2002-01-07 2008-07-31 Eisai R&D Man Co Ltd Deazapurines and uses thereof
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
EP2508204B1 (en) * 2002-06-26 2014-09-24 Ono Pharmaceutical Co., Ltd. Remedies for diseases caused by vascular contraction or dilation
US20040138238A1 (en) 2002-08-08 2004-07-15 Dhanoa Dale S. Substituted aminopyrimidine compounds as neurokinin antagonists
US20030139427A1 (en) * 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
AU2003290673B2 (en) 2002-11-08 2011-01-06 Massachusetts Institute Of Technology Small technetium-99m and rhenium labeled agents and methods for imaging tissues, organs and tumors
BR0316991A (pt) 2002-12-04 2005-10-25 Eisai Co Ltd Compostos de anel de 1,3-diidro-imidazol fundido
EP1444982A1 (de) * 2003-02-06 2004-08-11 Merckle Gmbh Verwendung von Purinderivaten als selektive Kinase-Inhibitoren
SE0300457D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
EP1601357A4 (en) 2003-03-10 2007-10-03 Schering Corp HETEROCYCLIC KINASE INHIBITORS: METHOD OF USE AND SYNTHESIS
US20060128956A1 (en) 2003-04-21 2006-06-15 Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky (Purin-6-yl) amino acid and production method thereof
FR2856685B1 (fr) 2003-06-25 2005-09-23 Merck Sante Sas Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
CA2536954C (en) 2003-08-29 2012-11-27 Exelixis, Inc. C-kit modulators and methods of use
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
TW200526626A (en) 2003-09-13 2005-08-16 Astrazeneca Ab Chemical compounds
EP1684694A2 (en) * 2003-11-21 2006-08-02 Array Biopharma, Inc. Akt protein kinase inhibitors
EP2308562B1 (en) * 2003-12-25 2015-02-25 Ono Pharmaceutical Co., Ltd. Azetidine ring compounds and drugs comprising the same
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス, インコーポレイテッド キナーゼ調節因子および使用方法
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
JP5274842B2 (ja) 2004-12-28 2013-08-28 エグゼリクシス, インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター(p70S6K、Akt−1およびAkt−2)としての[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジンまたは[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジン化合物
FR2880540B1 (fr) 2005-01-13 2008-07-11 Aventis Pharma Sa Utilisation de derives de la purine comme inhibiteurs de la proteine hsp90
FR2880626B1 (fr) 2005-01-13 2008-04-18 Aventis Pharma Sa Derives de la purine, compositions les contenant et utilisation
WO2006091450A1 (en) 2005-02-18 2006-08-31 Lexicon Genetics Incorporated 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds
US20060281768A1 (en) 2005-06-10 2006-12-14 Gaul Michael D Thienopyrimidine and thienopyridine kinase modulators
KR20080026654A (ko) 2005-07-14 2008-03-25 아스텔라스세이야쿠 가부시키가이샤 헤테로시클릭 야누스 키나제 3 억제제
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
US20070208053A1 (en) 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
WO2007125321A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
US20090082370A1 (en) 2006-04-25 2009-03-26 Neil Thomas Thompson Pharmaceutical Combinations of PK Inhibitors and Other Active Agents
WO2007125315A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
JP2009534454A (ja) 2006-04-25 2009-09-24 アステックス、セラピューティックス、リミテッド 医薬化合物
EP2029592A1 (en) 2006-04-25 2009-03-04 Astex Therapeutics Limited Pharmaceutical compounds
AR064416A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
AR064415A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de pirrolo-piperidinas y purinas,composiciones farmaceuticas que los contienen y usos en trastornos y/o enfermedades mediadas por pka y pkb.
AU2008309383B2 (en) 2007-10-11 2012-04-19 Astrazeneca Ab Pyrrolo [2, 3 -D] pyrimidin derivatives as protein kinase B inhibitors

Also Published As

Publication number Publication date
SI2272517T2 (sl) 2017-12-29
CY1115946T1 (el) 2017-01-25
US9006430B2 (en) 2015-04-14
EP1812004A1 (en) 2007-08-01
ATE513549T1 (de) 2011-07-15
AR051342A1 (es) 2007-01-03
JP2008517984A (ja) 2008-05-29
EP1812004B1 (en) 2011-06-22
UY29176A1 (es) 2006-05-31
EP2272517A1 (en) 2011-01-12
PL2272517T3 (pl) 2015-04-30
EP2272517B1 (en) 2014-10-01
US20140107137A1 (en) 2014-04-17
ES2523266T3 (es) 2014-11-24
DK2272517T4 (da) 2017-11-27
US20140303177A1 (en) 2014-10-09
MY179032A (en) 2020-10-26
JP5128284B2 (ja) 2013-01-23
ES2523266T5 (es) 2017-12-29
DK2272517T3 (da) 2014-10-27
SI2272517T1 (sl) 2015-01-30
US8546407B2 (en) 2013-10-01
HK1110503A1 (en) 2008-07-18
US20090247538A1 (en) 2009-10-01
EP2272517B2 (en) 2017-09-20
WO2006046024A1 (en) 2006-05-04
PT2272517E (pt) 2014-12-04
US8809336B2 (en) 2014-08-19

Similar Documents

Publication Publication Date Title
PL2272517T5 (pl) Orto-skondensowane pochodne pirydynowe i pirymidynowe (np. puryny) jako inhibitory kinaz białkowych
SG153875A1 (en) Pyrimidine urea derivatives as kinase inhibitors
DK2348023T3 (da) Heteroaryl-substituerede pyrrolo[2,3-b]pyridiner og pyrrolo[2,3-b]pyrimidiner som Janus-kinase-inhibitorer
SI2395004T1 (sl) Derivati piro (2,3-b) piridina kot inhibitorji proteinske kinaze
EP1796467A4 (en) INHIBITORS IMIDAZO {4,5-B} PYRAZINONE PROTEIN KINASES
ZA200710343B (en) Bicyclic derivatives as p38 kinase inhibitors
AP2326A (en) Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors.
GB0415364D0 (en) Pyrimidine derivatives
IL188027A0 (en) Bicyclic derivatives as p38 kinase inhibitors
PL1763517T3 (pl) Pochodne pirymidyny jako inhibitory 11BETA-HSD1
HK1110502A (en) Ortho-condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors
ZA200709919B (en) Pyrrol (2,3-B) pyridine derivatives protein kinase inhibitors
ZA200609510B (en) Pyrimidine urea derivatives as kinase inhibitors
HK1121740A (en) Pyrazole-isoquinoline urea derivatives as p38 kinase inhibitors
HK1116786A (en) Pyrazolo(1, 5a) pyrimidines as protein kinase inhibitors
ZA200803288B (en) Pyrazole-isoquinoline urea derivatives as p38 kinase inhibitors