JP5876146B2 - Jak阻害剤としてのアゼチジニルフェニル、ピリジル、またはピラジニルカルボキサミド誘導体 - Google Patents

Jak阻害剤としてのアゼチジニルフェニル、ピリジル、またはピラジニルカルボキサミド誘導体 Download PDF

Info

Publication number
JP5876146B2
JP5876146B2 JP2014517080A JP2014517080A JP5876146B2 JP 5876146 B2 JP5876146 B2 JP 5876146B2 JP 2014517080 A JP2014517080 A JP 2014517080A JP 2014517080 A JP2014517080 A JP 2014517080A JP 5876146 B2 JP5876146 B2 JP 5876146B2
Authority
JP
Japan
Prior art keywords
alkyl
pyrrolo
azetidin
pyrazol
cyanomethyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2014517080A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014520146A5 (enExample
JP2014520146A (ja
Inventor
ウェンチン・ヤオ
デイビッド・エム・バーンズ
ジンコン・ジュオ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Incyte Holdings Corp
Original Assignee
Incyte Holdings 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.)
Filing date
Publication date
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of JP2014520146A publication Critical patent/JP2014520146A/ja
Publication of JP2014520146A5 publication Critical patent/JP2014520146A5/ja
Application granted granted Critical
Publication of JP5876146B2 publication Critical patent/JP5876146B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P3/08Drugs 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2014517080A 2011-06-20 2012-06-19 Jak阻害剤としてのアゼチジニルフェニル、ピリジル、またはピラジニルカルボキサミド誘導体 Active JP5876146B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161498942P 2011-06-20 2011-06-20
US61/498,942 2011-06-20
US201261591094P 2012-01-26 2012-01-26
US61/591,094 2012-01-26
PCT/US2012/043099 WO2012177606A1 (en) 2011-06-20 2012-06-19 Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors

Publications (3)

Publication Number Publication Date
JP2014520146A JP2014520146A (ja) 2014-08-21
JP2014520146A5 JP2014520146A5 (enExample) 2015-08-06
JP5876146B2 true JP5876146B2 (ja) 2016-03-02

Family

ID=46513833

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014517080A Active JP5876146B2 (ja) 2011-06-20 2012-06-19 Jak阻害剤としてのアゼチジニルフェニル、ピリジル、またはピラジニルカルボキサミド誘導体

Country Status (22)

Country Link
US (5) US8691807B2 (enExample)
EP (1) EP2721028B1 (enExample)
JP (1) JP5876146B2 (enExample)
KR (1) KR20140040819A (enExample)
CN (1) CN103797010B (enExample)
AR (1) AR086983A1 (enExample)
AU (1) AU2012273164B2 (enExample)
BR (1) BR112013032720A2 (enExample)
CA (1) CA2839767A1 (enExample)
CL (1) CL2013003647A1 (enExample)
CO (1) CO6821966A2 (enExample)
CR (1) CR20130668A (enExample)
EA (1) EA201490042A1 (enExample)
EC (1) ECSP14013148A (enExample)
ES (1) ES2560611T3 (enExample)
IL (1) IL230008A (enExample)
MX (1) MX344479B (enExample)
MY (1) MY165963A (enExample)
PE (1) PE20140832A1 (enExample)
PH (1) PH12013502612A1 (enExample)
TW (1) TWI577676B (enExample)
WO (1) WO2012177606A1 (enExample)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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.
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
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k 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
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
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
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K 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
PL3409278T3 (pl) 2011-07-21 2021-02-22 Sumitomo Pharma Oncology, Inc. Heterocykliczne inhibitory kinazy białkowej
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
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Pi3k 억제제로서 헤테로시클릴아민
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
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
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
CA2897200C (en) 2013-01-14 2021-07-06 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
PE20191245A1 (es) 2013-01-15 2019-09-18 Incyte Holdings Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
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
CN105658653A (zh) 2013-08-23 2016-06-08 因赛特公司 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9493450B2 (en) 2014-02-13 2016-11-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PE20161573A1 (es) 2014-02-13 2017-01-19 Incyte Corp Ciclopropilamina como inhibidor de la lsd1
CA2940659C (en) * 2014-02-28 2023-01-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
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
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
PE20180455A1 (es) 2015-04-03 2018-03-05 Incyte Corp Compuestos heterociclicos como inhibidores de lsd1
ES2734048T3 (es) * 2015-04-29 2019-12-04 Wuxi Fortune Pharmaceutical Co Ltd Inhibidores de Janus cinasas (JAK)
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
WO2017027717A1 (en) 2015-08-12 2017-02-16 Incyte Corporation Bicyclic fused pyrimidine compounds as tam inhibitors
SG10202001219UA (en) 2015-08-12 2020-03-30 Incyte Corp Salts of an lsd1 inhibitor
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
CN111606893B (zh) * 2015-09-25 2021-05-04 迪哲(江苏)医药股份有限公司 用于抑制jak的化合物和方法
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
EP4086259A1 (en) 2015-11-06 2022-11-09 Incyte Corporation Heterocyclic compounds as pi3k-gamma inhibitors
EP3360878B9 (en) 2015-12-11 2021-05-05 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Azetidine derivative, preparation method therefor, and use thereof
TW201726623A (zh) 2015-12-17 2017-08-01 英塞特公司 作為免疫調節劑之雜環化合物
WO2017120194A1 (en) 2016-01-05 2017-07-13 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
AU2017241524B2 (en) 2016-03-28 2021-07-08 Incyte Corporation Pyrrolotriazine compounds as TAM inhibitors
CN109414410B (zh) 2016-04-22 2022-08-12 因赛特公司 Lsd1抑制剂的制剂
WO2017223414A1 (en) 2016-06-24 2017-12-28 Incyte Corporation HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS
EP3558963B1 (en) 2016-12-22 2022-03-23 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
ES2929193T3 (es) * 2016-12-22 2022-11-25 Incyte Corp Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de la internalización de PD-L1
TWI821200B (zh) 2017-09-27 2023-11-11 美商英塞特公司 Tam抑制劑之鹽
IL295978B2 (en) 2017-10-18 2024-01-01 Incyte Corp Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma inhibitors
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
CN109867676B (zh) * 2017-12-01 2020-10-30 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
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
CN117959303A (zh) 2018-04-13 2024-05-03 住友制药肿瘤公司 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂
SG11202010092XA (en) 2018-04-13 2020-11-27 Incyte Corp Biomarkers for graft-versus-host disease
CN108484468A (zh) * 2018-05-11 2018-09-04 南京大学 芳基氮杂环丁烷类化合物的制备方法
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
EP3805219A4 (en) 2018-06-06 2022-03-23 Gengle Therapeutics, Inc. PYRAZOLOPYRIMIDI DERIVATIVE, ITS USE AND PHARMACEUTICAL COMPOSITION
US11241438B2 (en) 2018-06-29 2022-02-08 Incyte Corporation Formulations of an AXL/MER inhibitor
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
IL282643B2 (en) 2018-10-31 2025-08-01 Incyte Corp A selective jak1 inhibitor for use in a method of treating hematological disease
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
PH12021551455A1 (en) 2018-12-19 2022-04-18 Incyte Corp Jak1 pathway inhibitors for the treatment of gastrointestinal disease
NZ778055A (en) 2019-02-12 2025-11-28 Sumitomo Pharma America Inc Formulations comprising heterocyclic protein kinase inhibitors
IL285999B2 (en) 2019-03-05 2026-01-01 Incyte Corp JAK1 inhibitor pathway for the treatment of chronic lung allograft dysfunction
US11624751B2 (en) 2019-03-19 2023-04-11 Incyte Corporation Biomarkers for vitiligo
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
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
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
JP7518900B2 (ja) 2019-10-16 2024-07-18 インサイト・コーポレイション 皮膚エリテマトーデス及び扁平苔癬(lp)の治療のためのjak1阻害剤の使用
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
EP4114401A1 (en) 2020-03-06 2023-01-11 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
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
WO2022040180A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak inhibitor
US11897889B2 (en) 2020-08-18 2024-02-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
EP4240739A1 (en) 2020-11-06 2023-09-13 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof
TW202237125A (zh) 2020-12-04 2022-10-01 美商英塞特公司 用於治療皮膚疾病之jak抑制劑與維生素d類似物
AU2021396231A1 (en) 2020-12-08 2023-06-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
MX2023008141A (es) 2021-01-11 2023-10-20 Incyte Corp Terapia combinada que comprende el inhibidor de la vía de proteínas tirosina cinasas de janus cinasas (jak) y el inhibidor de la proteína cinasa asociada a rho (rock).
SI4333840T1 (sl) 2021-05-03 2026-01-30 Incyte Corporation Zaviralci poti jak1 za zdravljenje pruriga nodularisa
US20240309095A1 (en) 2021-07-07 2024-09-19 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
MX2024006954A (es) 2021-12-08 2024-06-21 Incyte Corp Anticuerpos anti calreticulina (calr) mutante y usos de estos.
CN114149437A (zh) * 2021-12-24 2022-03-08 安徽大学 一种吡咯并嘧啶五元氮杂环衍生物及其制备方法和用途
EP4565229A1 (en) 2022-08-05 2025-06-11 Incyte Corporation Treatment of urticaria using jak inhibitors
EP4611753A1 (en) 2022-10-31 2025-09-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
TW202438061A (zh) 2023-03-16 2024-10-01 美商英塞特公司 用於治療氣喘之jak1路徑抑制劑
WO2025096716A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Anti-mutant calreticulin (calr) antibody-drug conjugates and uses thereof
WO2025226637A1 (en) 2024-04-22 2025-10-30 Incyte Corporation Combination therapy with an anti-colony stimulating factor 1 receptor antibody and a jak inhibitor

Family Cites Families (307)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
US3632836A (en) 1968-10-25 1972-01-04 Dow Chemical Co Solid curable polyepoxides modified with hydrolyzed liquid polyepoxides
US3832460A (en) 1971-03-19 1974-08-27 C Kosti Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue
US4140755A (en) 1976-02-13 1979-02-20 Hoffmann-La Roche Inc. Sustained release tablet formulations
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
DE3220113A1 (de) 1982-05-28 1983-12-01 Basf Ag, 6700 Ludwigshafen Difluormethoxiphenylthiophosphorsaeureester
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4404335A (en) 1982-08-16 1983-09-13 The Dow Chemical Company Hydrolyzing epoxy resins in absence of solvent and in presence of oxalic acid and a phosphonium compound
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
US4921947A (en) 1986-03-31 1990-05-01 Eli Lilly And Company Process for preparing macrolide derivatives
ATE139232T1 (de) 1989-10-11 1996-06-15 Teijin Ltd Bizyklische pyrimidinderivate, verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammensetzung
US5403593A (en) 1991-03-04 1995-04-04 Sandoz Ltd. Melt granulated compositions for preparing sustained release dosage forms
IT1258781B (it) 1992-01-16 1996-02-29 Zambon Spa Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (fr) 1992-08-27 1994-11-10 Sanofi Elf Dérivés d'acide thiényl ou pyrrolyl carboxyliques, leur préparation et médicaments les contenant.
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
JPH0710876A (ja) 1993-06-24 1995-01-13 Teijin Ltd 4位に環状アミノ基を有するピロロ[2,3―d]ピリミジン
USH1439H (en) 1993-10-18 1995-05-02 The Dow Chemical Company Method to increase the level of α-glycol in liquid epoxy resin
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
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
US5630943A (en) 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9604361D0 (en) 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
CA2250232A1 (en) 1996-04-03 1997-10-09 Allen I. Oliff A method of treating cancer
JP2000513711A (ja) 1996-04-18 2000-10-17 メルク エンド カンパニー インコーポレーテッド 癌の治療法
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
WO1997045412A1 (en) 1996-05-30 1997-12-04 Merck & Co., Inc. A method of treating cancer
US6624138B1 (en) 2001-09-27 2003-09-23 Gp Medical Drug-loaded biological material chemically treated with genipin
CA2286239A1 (en) 1997-04-07 1998-10-15 Merck & Co., Inc. A method of treating cancer
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
US5919779A (en) 1997-08-11 1999-07-06 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-Heteroaryl-dipyrido(2,3-B:3', 2'-F) azepines and their use in the prevention or treatment of HIV infection
US7153845B2 (en) 1998-08-25 2006-12-26 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
US6025366A (en) 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
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
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd 1h―イミダゾピリジン誘導体
WO2000015195A1 (en) 1998-09-10 2000-03-23 Nycomed Danmark A/S Quick release pharmaceutical compositions of drug substances
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
JP2002538121A (ja) 1999-03-03 2002-11-12 メルク エンド カムパニー インコーポレーテッド プレニルタンパク質トランスフェラーゼの阻害剤
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6217895B1 (en) 1999-03-22 2001-04-17 Control Delivery Systems Method for treating and/or preventing retinal diseases with sustained release corticosteroids
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
AU3565999A (en) 1999-04-16 2000-11-02 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
WO2001027104A1 (en) 1999-10-13 2001-04-19 Banyu Pharmaceutical Co., Ltd. Substituted imidazolidinone derivatives
US7235258B1 (en) 1999-10-19 2007-06-26 Nps Pharmaceuticals, Inc. Sustained-release formulations for treating CNS-mediated disorders
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
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
ATE250924T1 (de) 2000-04-07 2003-10-15 Medidom Lab Cyklosporin, hyaluronsäure und polysorbate enthaltenes augenarzneimittel
WO2001081345A1 (en) 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
MXPA02010618A (es) 2000-04-25 2004-05-05 Icos Corp Inhibidores de fosfatidilinositol 3-quinasa delta.
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
IL153115A0 (en) 2000-06-16 2003-06-24 Curis Inc Angiogenesis-modulating compositions and uses
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
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
ATE407132T1 (de) 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
US20040077654A1 (en) 2001-01-15 2004-04-22 Bouillot Anne Marie Jeanne Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
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
JP4316893B2 (ja) 2001-05-16 2009-08-19 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 Srcおよび他のプロテインキナーゼのインヒビター
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
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.
US6429231B1 (en) 2001-09-24 2002-08-06 Bradley Pharmaceuticals, Inc. Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
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
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
US6949668B2 (en) 2001-11-30 2005-09-27 Teijin Limited Process for producing 5-(3-cyanophenyl)-3-formylbenzoic acid compound
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
JP5466346B2 (ja) 2002-04-15 2014-04-09 レキット ベンキーザー エルエルシー グアイフェネシン組合せ剤の徐放
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
DE60318198T2 (de) 2002-05-02 2008-12-04 Merck & Co., Inc. Tyrosinkinase-hemmer
MXPA04011004A (es) 2002-05-07 2005-01-25 Control Delivery Sys Inc Procesos para formar un dispositivo de administracion de farmaco.
NZ537155A (en) 2002-05-23 2006-09-29 Cytopia Pty Ltd Protein kinase inhibitors
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
EP1535934A4 (en) 2002-06-26 2005-11-02 Idemitsu Kosan Co HYDROGENATED COPOLYMER, METHOD FOR THE PRODUCTION THEREOF AND THIS CONTAINING HOTMELT ADHESIVE COMPOSITION
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
EP1541563A4 (en) 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
JP2006502183A (ja) 2002-09-20 2006-01-19 アルコン,インコーポレイテッド ドライアイ障害の処置のためのサイトカイン合成インヒビターの使用
US20040204404A1 (en) 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
WO2004041814A1 (en) 2002-11-04 2004-05-21 Vertex Pharmaceuticals Incorporated Heteroaryl-pyramidine derivatives as jak inhibitors
US8034831B2 (en) 2002-11-06 2011-10-11 Celgene Corporation Methods for the treatment and management of myeloproliferative diseases using 4-(amino)-2-(2,6-Dioxo(3-piperidyl)-isoindoline-1,3-dione in combination with other therapies
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
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
UY28126A1 (es) 2002-12-24 2004-06-30 Alcon Inc Uso de glucocorticoides selectivos para la superficie ocular en el tratamiento de la sequedad ocular
TW200418806A (en) 2003-01-13 2004-10-01 Fujisawa Pharmaceutical Co HDAC inhibitor
US7444183B2 (en) 2003-02-03 2008-10-28 Enteromedics, Inc. Intraluminal electrode apparatus and method
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
US7547794B2 (en) 2003-04-03 2009-06-16 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
FR2857454B1 (fr) 2003-07-08 2006-08-11 Aventis Pasteur Dosage des acides techoiques des bacteries gram+
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
CA2536954C (en) 2003-08-29 2012-11-27 Exelixis, Inc. C-kit modulators and methods of use
EP1678147B1 (en) 2003-09-15 2012-08-08 Lead Discovery Center GmbH Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
DE602004030470D1 (de) 2003-10-24 2011-01-20 Santen Pharmaceutical Co Ltd Therapeutisches mittel für keratokonjunktive erkrankungen
US7387793B2 (en) 2003-11-14 2008-06-17 Eurand, Inc. Modified release dosage forms of skeletal muscle relaxants
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
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
JP4939229B2 (ja) 2003-12-19 2012-05-23 シェーリング コーポレイション Cxc−ケモカインレセプターリガンドおよびcc−ケモカインレセプターリガンドとしてのチアジアゾール
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
PL1706385T3 (pl) 2003-12-23 2011-03-31 Astex Therapeutics Ltd Pochodne pirazolu jako modulatory kinazy białkowej
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
US20050277629A1 (en) 2004-03-18 2005-12-15 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies (Lansbury)
NZ584499A (en) 2004-03-30 2011-08-26 Vertex Pharma Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases
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
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
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
CN1960988B (zh) 2004-06-10 2012-01-25 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
EP1765819B1 (en) 2004-06-30 2014-03-12 Vertex Pharmaceuticals Inc. Azaindoles useful as inhibitors of protein kinases
US7138423B2 (en) 2004-07-20 2006-11-21 Bristol-Myers Squibb Company Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
FR2873691B1 (fr) 2004-07-29 2006-10-06 Sanofi Synthelabo Derives d'amino-piperidine, leur preparation et leur application en therapeutique
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
WO2006022459A1 (en) 2004-08-23 2006-03-02 Mogam Biotechnology Institute Primer and probe for detection of sars coronavirus, kit comprising the primer and/or the probe, and detection method thereof
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
RU2394826C2 (ru) 2004-10-13 2010-07-20 Ф.Хоффманн-Ля Рош Аг Дизамещенные пиразолобензодиазепины, используемые в качестве ингибиторов cdk2 и ангиогенеза, а также для лечения злокачественных новообразований молочной железы, толстого кишечника, легкого и предстательной железы
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
EP1812440B1 (en) 2004-11-04 2010-09-22 Vertex Pharmaceuticals, Inc. Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
BRPI0517887A (pt) 2004-11-24 2008-10-21 Novartis Ag combinações de inibidores de jaks
US7517870B2 (en) 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
US20060128803A1 (en) 2004-12-14 2006-06-15 Alcon, Inc. Method of treating dry eye disorders using 13(S)-HODE and its analogs
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.
TW200635899A (en) 2004-12-22 2006-10-16 Astrazeneca Ab Chemical compounds
EP1844037A1 (en) 2005-01-20 2007-10-17 Pfizer Limited Chemical compounds
RU2434871C2 (ru) 2005-02-03 2011-11-27 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы
WO2007044050A2 (en) 2005-02-04 2007-04-19 Bristol-Myers Squibb Company 1h-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
MX2007011316A (es) 2005-03-15 2007-11-12 Irm Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
KR20080013886A (ko) 2005-04-05 2008-02-13 파마코페이아, 인코포레이티드 면역억제용 퓨린 및 이미다조피리딘 유도체
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
NZ564065A (en) 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
AU2006254840B2 (en) 2005-06-08 2012-08-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
PL2395004T3 (pl) 2005-06-22 2016-08-31 Plexxikon Inc Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej
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
FR2889662B1 (fr) 2005-08-11 2011-01-14 Galderma Res & Dev Emulsion de type huile-dans-eau pour application topique en dermatologie
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
US20070128633A1 (en) 2005-10-11 2007-06-07 Chembridge Research Laboratories, Inc. Cell-free protein expression systems and methods of use thereof
DK1937664T3 (da) 2005-10-14 2011-07-18 Sumitomo Chemical Co Hydrazidforbindelse og pesticid anvendelse af den samme
DK1945631T3 (da) 2005-10-28 2012-10-22 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidinderivater til anvendelse som tyrosinkinaseinhibitorer til behandling af cancer
NZ567851A (en) 2005-11-01 2011-09-30 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
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
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
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
MX2008008320A (es) 2005-12-23 2008-09-03 Smithkline Beecham Corp Inhibidores de azaindol de aurora cinasas.
JP4643455B2 (ja) 2006-01-12 2011-03-02 株式会社ユニバーサルエンターテインメント 遊技システム
AR060316A1 (es) 2006-01-17 2008-06-11 Vertex Pharma Azaindoles de utilidad como inhibidores de janus quinasas
US20070208053A1 (en) 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
JP2009525350A (ja) 2006-02-01 2009-07-09 スミスクライン ビーチャム コーポレーション Rafキナーゼ阻害薬として有用なピロロ[2,3,b]ピリジン誘導体
US7745477B2 (en) 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
RU2008136766A (ru) 2006-02-24 2010-03-27 Тева Фармасьютикл Индастриес Лтд. (Il) Таблетки метопролола сукцината пролонгированного действия и способы их приготовления
JPWO2007105637A1 (ja) 2006-03-10 2009-07-30 小野薬品工業株式会社 含窒素複素環誘導体およびそれらを有効成分とする薬剤
TWI382984B (zh) 2006-04-03 2013-01-21 Astellas Pharma Inc 雜環化合物
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
WO2007116313A2 (en) 2006-04-12 2007-10-18 Pfizer Limited Pyrrolidine derivatives as modulators of chemokine ccr5 receptors
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
EP2040704A2 (en) 2006-05-18 2009-04-01 Bayer Healthcare Ag Pharmaceutical compositions comprising implitapide and methods of using same
US7691811B2 (en) 2006-05-25 2010-04-06 Bodor Nicholas S Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
NZ573174A (en) 2006-06-01 2012-01-12 Msd Consumer Care Inc Sustained release pharmaceutical dosage form containing phenylephrine
WO2008011557A2 (en) 2006-07-20 2008-01-24 Borchardt Allen J Heteroaryl inhibitors of rho kinase
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
ATE517868T1 (de) 2006-08-16 2011-08-15 Boehringer Ingelheim Int Pyrazinverbindungen, ihre verwendung und herstellungsverfahren
AU2007293653B2 (en) 2006-09-08 2011-02-17 Novartis Ag N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
WO2008035376A2 (en) 2006-09-19 2008-03-27 Council Of Scientific & Industrial Research A novel bio-erodible insert for ophthalmic applications and a process for the preparation thereof
AR063141A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2- ( benzimidazolil ) purina 8- sustituida para inmunosupresion
TW200831104A (en) 2006-10-04 2008-08-01 Pharmacopeia Inc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
WO2008058126A2 (en) 2006-11-06 2008-05-15 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
US20080119496A1 (en) 2006-11-16 2008-05-22 Pharmacopeia Drug Discovery, Inc. 7-Substituted Purine Derivatives for Immunosuppression
KR101532256B1 (ko) 2006-11-22 2015-06-29 인사이트 코포레이션 키나제 억제제로서의 이미다조트리아진 및 이미다조피리미딘
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
CN101562977A (zh) 2006-12-15 2009-10-21 艾博特公司 新的二唑化合物
EP2125781A2 (en) 2006-12-20 2009-12-02 Amgen Inc. Substituted heterocycles and methods of use
US8338455B2 (en) 2006-12-20 2012-12-25 Amgen Inc. Compounds and methods of use
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
US8389014B2 (en) 2006-12-22 2013-03-05 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Gel useful for the delivery of ophthalmic drugs
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
ES2431163T3 (es) 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
WO2008124323A1 (en) 2007-04-03 2008-10-16 Array Biopharma Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
US8188178B2 (en) 2007-05-07 2012-05-29 3M Innovative Properties Company Cold shrinkable article including an epichlorohydrin composition
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
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.
WO2009007839A1 (en) 2007-07-11 2009-01-15 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
CN101815712A (zh) 2007-08-01 2010-08-25 辉瑞有限公司 吡唑化合物及其作为raf抑制剂的用途
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
EP2217235A4 (en) 2007-11-15 2011-01-12 Musc Found For Res Dev INHIBITORS OF PIM PROTEIN KINASES, COMPOSITIONS AND METHOD FOR THE TREATMENT OF CANCER
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
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
PL3133080T3 (pl) 2008-01-18 2018-12-31 Inst Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Nowe cytostatyczne nukleozydy 7-deazapurynowe
CN101959404B (zh) 2008-02-04 2015-12-02 墨丘瑞医疗有限公司 单磷酸腺苷活化蛋白激酶调节剂
UY31679A1 (es) 2008-03-03 2009-09-30 Inhibidores de cinasa pim y metodos para su uso
PL2288610T3 (pl) 2008-03-11 2017-12-29 Incyte Holdings Corporation Azetydynowe i cyklobutanowe pochodne jako inhibitory jak
EA201001456A1 (ru) 2008-03-21 2011-06-30 Новартис Аг Новые гетероциклические соединения и их применение
US8344144B2 (en) 2008-06-18 2013-01-01 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
US20110212157A1 (en) 2008-06-26 2011-09-01 Anterios, Inc. Dermal delivery
UY31952A (es) 2008-07-02 2010-01-29 Astrazeneca Ab 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim
FR2933409B1 (fr) 2008-07-03 2010-08-27 Centre Nat Rech Scient NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
EP2384326B1 (en) 2008-08-20 2014-04-23 Zoetis LLC Pyrrolo[2,3-d]pyrimidine compounds
CN104311480A (zh) 2008-09-02 2015-01-28 诺华股份有限公司 作为激酶抑制剂的吡啶甲酰胺衍生物
CA2735782A1 (en) 2008-09-02 2010-03-11 Novartis Ag Heterocyclic pim-kinase inhibitors
BRPI0918496A2 (pt) 2008-09-02 2019-09-24 Novartis Ag composto inibidor bicíclico de quinase, uso do mesmo, composição farmacêutica e método para inibir a atividade da quinase pim em uma célula
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.
EP2350054A4 (en) * 2008-10-17 2012-03-28 Merck Canada Inc AZETIDINE DERIVATIVES AS INHIBITORS OF THE STEAROYL COENZYME A DELTA 9 DESATURASE
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
EP2210890A1 (en) 2009-01-19 2010-07-28 Almirall, S.A. Oxadiazole derivatives as S1P1 receptor agonists
US8263601B2 (en) 2009-02-27 2012-09-11 Concert Pharmaceuticals, Inc. Deuterium substituted xanthine derivatives
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
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
EP2451813B1 (en) 2009-07-08 2014-10-01 Leo Pharma A/S Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme JAK INHIBITION FOR BLOCKING TOXICITY ASSOCIATED WITH RNA INTERFERENCE
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase 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
SG10201405568UA (en) 2009-09-08 2014-11-27 Hoffmann La Roche 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
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
AU2010309882B2 (en) 2009-10-20 2016-01-28 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors
US8671402B2 (en) 2009-11-09 2014-03-11 Bank Of America Corporation Network-enhanced control of software updates received via removable computer-readable medium
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
CN102740888B (zh) 2009-11-24 2016-10-12 奥尔德生物制药公司 Il-6抗体及其用途
EP2506852A4 (en) 2009-12-04 2013-06-19 Univ Texas INTERFERONTHERAPIES IN COMBINATION WITH BLOCKING OF STAT3 ACTIVATION
WO2011075334A1 (en) 2009-12-18 2011-06-23 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
US8461328B2 (en) 2010-01-12 2013-06-11 Genentech, Inc. Tricyclic heterocyclic compounds, compositions and methods of use thereof
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
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
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
US8637529B2 (en) 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
WO2012045020A1 (en) 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine
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
CA2819560A1 (en) 2010-12-03 2012-06-07 Ym Biosciences Australia Pty Ltd Treatment of jak2-mediated conditions
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
CN102247368B (zh) 2011-05-19 2013-05-29 安徽永生堂药业有限责任公司 一种复方阿伐斯汀缓释片及其制备方法
CN102218042A (zh) 2011-05-26 2011-10-19 青岛黄海制药有限责任公司 富马酸喹硫平组合物的缓释片剂及其制备方法
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
WO2013007768A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
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
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
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
ES2867048T3 (es) 2012-06-15 2021-10-20 Concert Pharmaceuticals Inc Derivados deuterados de ruxolitinib
CA2879603A1 (en) 2012-07-27 2014-01-30 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
CN102772384A (zh) 2012-08-07 2012-11-14 四川百利药业有限责任公司 一种盐酸米诺环素缓释片及其制备方法
US9573958B2 (en) 2012-08-31 2017-02-21 Principia Biopharma, Inc. Benzimidazole derivatives as ITK inhibitors
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
CA2940659C (en) * 2014-02-28 2023-01-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
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
US10363260B2 (en) 2014-05-28 2019-07-30 Oncotracker, Inc. Anti-cancer effects of JAK2 inhibitors in combination with thalidomide derivatives and glucocorticoids
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
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
CN113906032A (zh) 2019-02-06 2022-01-07 康塞特医药品有限公司 用于制备对映异构体富集的jak抑制剂的方法

Also Published As

Publication number Publication date
AR086983A1 (es) 2014-02-05
NZ618982A (en) 2015-08-28
CN103797010A (zh) 2014-05-14
ES2560611T3 (es) 2016-02-22
EP2721028A1 (en) 2014-04-23
AU2012273164B2 (en) 2015-05-28
CR20130668A (es) 2014-03-31
EP2721028B1 (en) 2015-11-04
US20170253598A1 (en) 2017-09-07
TWI577676B (zh) 2017-04-11
US10513522B2 (en) 2019-12-24
MY165963A (en) 2018-05-18
HK1197056A1 (zh) 2015-01-02
BR112013032720A2 (pt) 2016-09-13
CA2839767A1 (en) 2012-12-27
MX344479B (es) 2016-12-16
US20140171409A1 (en) 2014-06-19
US8691807B2 (en) 2014-04-08
TW201311686A (zh) 2013-03-16
PE20140832A1 (es) 2014-07-14
US11214573B2 (en) 2022-01-04
JP2014520146A (ja) 2014-08-21
US20130018034A1 (en) 2013-01-17
US9611269B2 (en) 2017-04-04
ECSP14013148A (es) 2015-03-31
CL2013003647A1 (es) 2014-07-04
US9023840B2 (en) 2015-05-05
US20200079783A1 (en) 2020-03-12
AU2012273164A1 (en) 2013-05-02
CN103797010B (zh) 2016-02-24
EA201490042A1 (ru) 2014-10-30
CO6821966A2 (es) 2013-12-31
MX2013015087A (es) 2014-02-11
KR20140040819A (ko) 2014-04-03
PH12013502612A1 (en) 2014-04-28
WO2012177606A1 (en) 2012-12-27
IL230008A (en) 2016-10-31
US20150225411A1 (en) 2015-08-13

Similar Documents

Publication Publication Date Title
JP5876146B2 (ja) Jak阻害剤としてのアゼチジニルフェニル、ピリジル、またはピラジニルカルボキサミド誘導体
JP5917544B2 (ja) Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
JP6318291B2 (ja) Jak1阻害剤としてのピペリジン−4−イルアゼチジン誘導体
US9359358B2 (en) Cyclohexyl azetidine derivatives as JAK inhibitors
TWI840646B (zh) 作為jak抑制劑之聯吡唑衍生物
US9249145B2 (en) Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
KR20140019300A (ko) Jak 억제제로서 사이클로부틸 치환된 피롤로피리딘 및 피롤로피리미딘 유도체
HK1197056B (en) Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
NZ618982B2 (en) Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
HK1189877B (en) Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors

Legal Events

Date Code Title Description
RD01 Notification of change of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7426

Effective date: 20150227

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20150227

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150618

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150618

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20151113

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20151222

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20151224

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160120

R150 Certificate of patent or registration of utility model

Ref document number: 5876146

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250