JO3441B1 - طرق لاصلاح مثبطات انزيم jak والمركبات الوسيطة المتعلقة به - Google Patents

طرق لاصلاح مثبطات انزيم jak والمركبات الوسيطة المتعلقة به

Info

Publication number
JO3441B1
JO3441B1 JOP/2010/0010A JOP20100010A JO3441B1 JO 3441 B1 JO3441 B1 JO 3441B1 JO P20100010 A JOP20100010 A JO P20100010A JO 3441 B1 JO3441 B1 JO 3441B1
Authority
JO
Jordan
Prior art keywords
processes
intermediate compounds
jak inhibitors
related intermediate
preparing
Prior art date
Application number
JOP/2010/0010A
Other languages
English (en)
Inventor
Qiyan Lin
Brian W Metcalf
Haisheng Wang
David Meloni
Jiacheng Zhou
Yongchun Pan
Michael Xia
Mei Li
Tai-Yuen Yue
Pingli Liu
James D Rodgers
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Application granted granted Critical
Publication of JO3441B1 publication Critical patent/JO3441B1/ar

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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/00Antineoplastic 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
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/16Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/30Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/0825Preparations of compounds not comprising Si-Si or Si-cyano linkages
    • C07F7/083Syntheses without formation of a Si-C bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/10Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

يتعلق الاكتشاف الحالي بطرق لتحضير بايريمدينات <span dir="LTR">[2,3-<em>d</em>]</span> بايرولو بايرازوليل مستبدلة الجزيئات غير منطبقة مرآويا خاصة بالصيغة <span dir="LTR">III</span> والمركبات الوسيطة التوليفية الصناعية المتعلقة بها. البايريمدينات <span dir="LTR">[2,3-<em>d</em>]</span> بايرولو بايرازوليل مستبدلة الجزيئات غير المنطبقة مرآويا مفيدة كمثبطات لعائلة مستقبِل كاينيز جانوس لبروتين كاينيز تايروزين لمعالجة الامراض الالتهابية واضطرابات التشعب النخاعي العظمي وغير ذلك من الامراض.
JOP/2010/0010A 2009-01-15 2010-01-14 طرق لاصلاح مثبطات انزيم jak والمركبات الوسيطة المتعلقة به JO3441B1 (ar)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14499109P 2009-01-15 2009-01-15

Publications (1)

Publication Number Publication Date
JO3441B1 true JO3441B1 (ar) 2019-10-20

Family

ID=42026219

Family Applications (3)

Application Number Title Priority Date Filing Date
JOP/2019/0230A JOP20190230A1 (ar) 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
JOP/2019/0231A JOP20190231A1 (ar) 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
JOP/2010/0010A JO3441B1 (ar) 2009-01-15 2010-01-14 طرق لاصلاح مثبطات انزيم jak والمركبات الوسيطة المتعلقة به

Family Applications Before (2)

Application Number Title Priority Date Filing Date
JOP/2019/0230A JOP20190230A1 (ar) 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
JOP/2019/0231A JOP20190231A1 (ar) 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به

Country Status (29)

Country Link
US (9) US8410265B2 (ar)
EP (2) EP2398774B1 (ar)
JP (6) JP5650662B2 (ar)
KR (7) KR101824742B1 (ar)
CN (3) CN105669675A (ar)
AR (2) AR082747A1 (ar)
AU (5) AU2010204772B2 (ar)
BR (3) BR122020005540B8 (ar)
CA (2) CA2749483C (ar)
CL (3) CL2011001668A1 (ar)
CO (1) CO6400137A2 (ar)
EA (3) EA020643B1 (ar)
EC (1) ECSP11011268A (ar)
ES (1) ES2641761T3 (ar)
IL (7) IL214061A (ar)
JO (3) JOP20190230A1 (ar)
MA (1) MA33038B1 (ar)
MX (5) MX363976B (ar)
MY (3) MY163540A (ar)
NZ (5) NZ706894A (ar)
PE (4) PE20171102A1 (ar)
PH (1) PH12016502060B1 (ar)
PL (1) PL2398774T3 (ar)
PT (1) PT2398774T (ar)
SG (3) SG10201913261QA (ar)
TN (1) TN2011000329A1 (ar)
TW (7) TWI740775B (ar)
WO (1) WO2010083283A2 (ar)
ZA (1) ZA201104909B (ar)

Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
UA98449C2 (en) 2005-12-13 2012-05-25 Инсайт Корпорейшин Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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.
MY152948A (en) * 2007-11-16 2014-12-15 Incyte Corp 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
LT2432472T (lt) * 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
BRPI1012159B1 (pt) 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
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
JP5946768B2 (ja) * 2009-10-09 2016-07-06 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation 3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
CA2790070C (en) * 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
AU2011240808B2 (en) 2010-04-14 2015-01-22 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of JAK kinases
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
CN102690281A (zh) * 2011-03-22 2012-09-26 上海药明康德新药开发有限公司 1-甲基4-吡唑频哪醇酯的合成方法
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
EP2741747A1 (en) 2011-08-10 2014-06-18 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
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
AU2013274030B2 (en) 2012-06-15 2016-07-07 Sun Pharmaceutical Industries, Inc. Deuterated derivatives of ruxolitinib
WO2014011540A1 (en) 2012-07-09 2014-01-16 Emory University Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
EP2885303B1 (en) 2012-08-17 2018-12-26 CoNCERT Pharmaceuticals, Inc. Deuterated baricitinib
WO2014060381A1 (de) 2012-10-18 2014-04-24 Bayer Cropscience Ag Heterocyclische verbindungen als schädlingsbekämpfungsmittel
JP2016503395A (ja) 2012-10-31 2016-02-04 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 病害生物防除剤としての複素環化合物
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
MY191357A (en) 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
UA120162C2 (uk) 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
JP6449244B2 (ja) 2013-04-19 2019-01-09 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Fgfr抑制剤としての二環式複素環
TWI719401B (zh) 2013-05-17 2021-02-21 美商英塞特公司 作為jak抑制劑之聯吡唑衍生物
PT3030227T (pt) 2013-08-07 2020-06-25 Incyte Corp Formas de dosagem de libertação prolongada para um inibidor de jak1
CN103601749B (zh) * 2013-11-26 2016-04-27 大连联化化学有限公司 一种1-烷基吡唑-4-硼酸频哪醇酯的合成方法
JP6192839B2 (ja) 2013-12-05 2017-09-06 ファイザー・インク ピロロ[2,3−d]ピリミジニル、ピロロ[2,3−b]ピラジニル、およびピロロ[2,3−d]ピリジニルアクリルアミド
CN104860950A (zh) * 2014-02-24 2015-08-26 重庆医药工业研究院有限责任公司 一种制备4-氯吡咯[2,3-d]并嘧啶的方法
PL3129021T3 (pl) 2014-04-08 2021-05-31 Incyte Corporation Leczenie nowotworów złośliwych z komórek b za pomocą skojarzenia inhibitora jak i pi3k
WO2015168246A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
HRP20211813T1 (hr) 2014-08-11 2022-03-04 Acerta Pharma B.V. Terapeutske kombinacije inhibitora btk i inhibitora bcl-2
WO2016024232A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
TW201618775A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Btk抑制劑、pi3k抑制劑、jak-2抑制劑、pd-1抑制劑及/或pd-l1抑制劑之治療組合物
WO2016035014A1 (en) * 2014-09-01 2016-03-10 Sun Pharmaceutical Industries Limited Processes for the preparation of ruxolitinib phosphate
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CZ2014773A3 (cs) 2014-11-10 2016-05-18 Zentiva, K.S. Soli (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu
CN104496904B (zh) * 2014-11-28 2017-01-11 上海北卡医药技术有限公司 一种鲁索利替尼中间体的合成方法
US9873706B2 (en) 2014-12-05 2018-01-23 Sun Pharmaceutical Industries Limited Process for the preparation of baricitinib and an intermediate thereof
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134320A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CZ2015496A3 (cs) 2015-07-14 2017-01-25 Zentiva, K.S. Krystalické formy solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a jejich příprava
CN106397443A (zh) * 2015-07-17 2017-02-15 浙江九洲药业股份有限公司 一种吡咯嘧啶类衍生物中间体的制备方法
HU230805B1 (hu) * 2015-12-23 2018-06-28 Egis Gyógyszergyár Zrt Eljárás és köztitermék baricitinib előállítására
JP6921087B2 (ja) * 2015-12-31 2021-08-18 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. ルキソリチニブの合成プロセス
CZ201629A3 (cs) 2016-01-22 2017-08-02 Zentiva, K.S. Krystalické modifikace solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a způsoby jejich přípravy
WO2017129116A1 (zh) * 2016-01-26 2017-08-03 杭州华东医药集团新药研究院有限公司 吡咯嘧啶五元氮杂环衍生物及其应用
CN107226814A (zh) * 2016-03-23 2017-10-03 罗欣生物科技(上海)有限公司 一种巴瑞克替尼中间体的制备方法
KR20190003711A (ko) 2016-05-04 2019-01-09 콘서트 파마슈티컬즈, 인크. 중수소화된 jak 저해제를 이용한 탈모 장애의 치료
CN107513069A (zh) * 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
CN106188116B (zh) * 2016-07-14 2018-02-06 沧州普瑞东方科技有限公司 一种合成吡唑‑4‑硼酸频那醇酯的方法
CN107722012B (zh) * 2016-08-11 2020-05-29 斯福瑞(南通)制药有限公司 制备4-氯-7H-吡咯并[2,3-d]嘧啶的方法
CN107759623B (zh) * 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
CN107759601B (zh) * 2016-08-23 2020-09-11 苏州旺山旺水生物医药有限公司 一种jak抑制剂及其盐的制备方法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN107501154B (zh) * 2017-09-13 2020-02-11 浙江普洛康裕制药有限公司 (s)-1-(2-氯乙酰基)吡咯烷-2-甲腈的合成方法
CN109651424B (zh) * 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
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
KR20200129099A (ko) 2018-01-30 2020-11-17 인사이트 코포레이션 (1-(3-플루오로-2-(트리플루오로메틸)이소니코티닐)피페리딘-4-온)의 제조 방법
IL276725B2 (en) 2018-02-16 2024-09-01 Incyte Corp JAK1 pathway inhibitors for the treatment of cytokine-related disorders
JP7565798B2 (ja) 2018-03-30 2024-10-11 インサイト・コーポレイション 炎症性皮膚疾患のバイオマーカー
CN112423759A (zh) 2018-03-30 2021-02-26 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
SG11202010092XA (en) 2018-04-13 2020-11-27 Incyte Corp Biomarkers for graft-versus-host disease
DK3788047T3 (da) 2018-05-04 2024-09-16 Incyte Corp Faste former af en FGFR-inhibitor og fremgangsmåder til fremstilling deraf
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
SG11202101785UA (en) * 2018-09-04 2021-03-30 Theravance Biopharma R&D Ip Llc Process for preparing jak inhibitors and intermediates thereof
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
JP7431845B2 (ja) 2018-10-31 2024-02-15 インサイト・コーポレイション 血液疾患の治療のための併用療法
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020163653A1 (en) * 2019-02-06 2020-08-13 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN110538183B (zh) * 2019-10-09 2021-05-04 吉林大学 一种预防和治疗小儿湿疹的组合物及其制备方法
MX2022004513A (es) 2019-10-14 2022-07-19 Incyte Corp Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr).
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021102258A1 (en) 2019-11-22 2021-05-27 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021236139A1 (en) 2020-05-21 2021-11-25 Concert Pharmaceuticals, Inc. Novel deuterated jak inhibitor and uses thereof
US11685731B2 (en) 2020-06-02 2023-06-27 Incyte Corporation Processes of preparing a JAK1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN111790439B (zh) * 2020-07-29 2022-12-27 成都能特科技发展有限公司 一种手性二级胺二苯基膦芳甲酰胺双功能催化剂及其制备方法与应用
CA3194469A1 (en) * 2020-08-12 2022-02-17 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
TW202212341A (zh) 2020-08-18 2022-04-01 美商英塞特公司 製備jak1抑制劑之方法及中間體
MX2023005027A (es) 2020-10-28 2023-07-31 Sun Pharmaceutical Ind Inc Regimenes para el tratamiento de los trastornos de la perdida de cabello con inhibidores de jak deuterados.
EP4259131A1 (en) 2020-12-08 2023-10-18 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
CN112625030A (zh) * 2020-12-25 2021-04-09 杭州澳赛诺生物科技有限公司 一种一锅法合成n-保护3-溴代吡唑的合成方法
CN114907353A (zh) * 2021-02-09 2022-08-16 明慧医药(杭州)有限公司 一种前药化合物及其制备方法和用途
CN112876503B (zh) * 2021-03-18 2022-04-29 中国科学院兰州化学物理研究所 用于癌症硼中子俘获治疗药物的硼酸盐化合物及其制备
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CN113292569A (zh) * 2021-05-25 2021-08-24 常州制药厂有限公司 一种jak抑制剂的制备方法
CN113264936B (zh) * 2021-05-25 2022-08-09 常州制药厂有限公司 一种jak抑制剂关键中间体及其制备方法
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2023288197A1 (en) * 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
CN117355527B (zh) * 2021-07-20 2024-06-07 上海椿安生物医药科技有限公司 一种消炎偶联化合物药物及其制法和应用
AU2022328272A1 (en) 2021-08-11 2024-02-22 Sun Pharmaceutical Industries, Inc. Treatment of hair loss disorders with deuterated jak inhibitors
JP2024532765A (ja) 2021-08-12 2024-09-10 サン ファーマシューティカル インダストリーズ,インコーポレイテッド Jak阻害剤のプロドラッグを用いたjak阻害応答性障害の治療
CA3231996A1 (en) * 2021-09-18 2023-03-23 Satya Srinivas HANUMARA An improved process for the preparation of ruxolitinib phosphate
CN114044777B (zh) * 2022-01-10 2022-04-19 南京佰麦生物技术有限公司 一种磷酸芦可替尼的制备方法
WO2023215520A1 (en) 2022-05-04 2023-11-09 Sun Pharmaceutical Industries, Inc. Dosage regimens for treatment with deuterated jak inhibitors
WO2023223253A1 (en) * 2022-05-19 2023-11-23 Glenmark Life Sciences Limited Process for preparation of ruxolitinib
CN114805368B (zh) * 2022-05-25 2023-12-01 山东诺明康药物研究院有限公司 一种芦克替尼的制备方法
CN115028638A (zh) * 2022-06-09 2022-09-09 安徽大学 一种鲁索替尼中间体的制备方法
CN117384163A (zh) * 2022-07-05 2024-01-12 盛世泰科生物医药技术(苏州)股份有限公司 一种含偕二氟基的化合物及其制备方法和用途
US20240166654A1 (en) * 2022-11-11 2024-05-23 Zhejiang Ausun Pharmaceutical Co., Ltd. Ruxolitinib crystal and pharmaceutical composition thereof

Family Cites Families (65)

* 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
JPS5519438A (en) 1978-07-26 1980-02-12 Mitsubishi Electric Corp Brazing method
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
JP2513001B2 (ja) * 1988-11-01 1996-07-03 山川薬品工業株式会社 光学活性テトラヒドロフラン−2−カルボン酸のラセミ化方法
DE4038356A1 (de) * 1990-12-01 1992-06-04 Bayer Ag Verfahren zur racemisierung von optisch aktiven l-aryl-alkylaminen
JPH04308556A (ja) * 1991-04-05 1992-10-30 Hokuriku Seiyaku Co Ltd 光学活性なベンジルアルコール誘導体のラセミ化方法
JPH06122686A (ja) * 1992-10-12 1994-05-06 Fujisawa Pharmaceut Co Ltd ラセミ体の光学分割法
JPH07247286A (ja) * 1994-01-18 1995-09-26 Sankyo Co Ltd 含窒素環状化合物の光学分割方法
US5630943A (en) 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9602516D0 (en) * 1996-02-08 1996-04-10 Chiroscience Ltd Racemisation
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
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
KR100477818B1 (ko) 1999-12-10 2005-03-22 화이자 프로덕츠 인코포레이티드 피롤로[2,3-d] 피리미딘 화합물
CN1329394C (zh) * 2000-11-17 2007-08-01 武田药品工业株式会社 新咪唑衍生物、其制备方法及其用途
US7429609B2 (en) 2002-05-31 2008-09-30 Eisai R & D Management Co., Ltd. Pyrazole compound and medicinal composition containing the same
KR20050067383A (ko) 2002-08-06 2005-07-01 아스트라제네카 아베 Tie2(tek) 활성을 갖는 축합 피리딘 및 피리미딘
JP2004143053A (ja) * 2002-10-22 2004-05-20 Senju Pharmaceut Co Ltd β−アミノヒドロキサム酸誘導体およびその用途
DK1587821T3 (da) * 2002-12-19 2008-11-10 Scripps Research Inst Sammensætninger og fremgangsmåder til stabilisering af transthyretin og inhibering af transthyretin-fejlfolding
JP2005304368A (ja) * 2004-04-21 2005-11-04 Toyo Kasei Kogyo Co Ltd 光学活性な4−(n−保護アミノ)−1−アルケン−3−オールの製造方法、およびそれを用いた3−ベンザミド−2−ヒドロキシカルボン酸またはその塩の製造方法
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
CA2573362A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
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.
MX2007009429A (es) 2005-02-03 2008-03-18 Vertex Pharma Pirrolopirimidinas utiles como inhibidores de proteinas cinasas.
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
DK1937664T3 (da) 2005-10-14 2011-07-18 Sumitomo Chemical Co Hydrazidforbindelse og pesticid anvendelse af den samme
UA98449C2 (en) 2005-12-13 2012-05-25 Инсайт Корпорейшин Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
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
KR100815432B1 (ko) * 2005-12-29 2008-03-20 엘아이지엔설팅주식회사 사업 재난 관리 시스템, 방법, 및 상기 방법을 실행시키기위한 컴퓨터 판독 가능한 프로그램을 기록한 매체
CA2648250A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
DE102006016426A1 (de) * 2006-04-07 2007-10-11 Merck Patent Gmbh Neuartige Cyclobutyl-Verbindungen als Kinase-Inhibitoren
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
AU2007323725B2 (en) * 2006-11-22 2014-02-20 Incyte Holdings Corporation Imidazotriazines and imidazopyrimidines as kinase inhibitors
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.
US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
GB0704932D0 (en) * 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
EA200901157A1 (ru) * 2007-04-10 2010-04-30 ЭсДжиИкс ФАРМАСЬЮТИКАЛЗ, ИНК. Конденсированные кольцевые гетероциклические модуляторы киназы
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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.
CL2008001933A1 (es) * 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
MY152948A (en) 2007-11-16 2014-12-15 Incyte Corp 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
JP5275371B2 (ja) 2008-03-11 2013-08-28 インサイト・コーポレイション Jak阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
ES2429120T3 (es) * 2008-03-19 2013-11-13 Bial-Portela & Ca, S.A. Hidrogenación catalítica asimétrica
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
IT1393787B1 (it) 2009-03-30 2012-05-08 Cps Color Equipment Spa Dispositivo di erogazione di prodotti fluidi e relativo procedimento di erogazione
BRPI1012159B1 (pt) 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
LT2432472T (lt) 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
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
JP5946768B2 (ja) 2009-10-09 2016-07-06 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation 3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
CA2790070C (en) * 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
EP2741747A1 (en) 2011-08-10 2014-06-18 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

Also Published As

Publication number Publication date
US8883806B2 (en) 2014-11-11
CN105669676B (zh) 2018-04-24
ZA201104909B (en) 2018-11-28
MX363976B (es) 2019-04-10
KR20180011887A (ko) 2018-02-02
CO6400137A2 (es) 2012-03-15
US20130253191A1 (en) 2013-09-26
AU2016216537B2 (en) 2018-05-10
IL274422B (en) 2021-06-30
PL2398774T3 (pl) 2017-11-30
US20210253584A1 (en) 2021-08-19
IL283038A (en) 2021-06-30
MY163540A (en) 2017-09-15
AU2022201630B2 (en) 2024-04-18
ES2641761T3 (es) 2017-11-13
JOP20190231A1 (ar) 2017-06-16
NZ739757A (en) 2019-01-25
JP2015091805A (ja) 2015-05-14
US9000161B2 (en) 2015-04-07
TW202003521A (zh) 2020-01-16
TWI740775B (zh) 2021-09-21
NZ617077A (en) 2015-05-29
EA201991779A2 (ru) 2019-12-30
US20200002341A1 (en) 2020-01-02
TWI814080B (zh) 2023-09-01
JP5650662B2 (ja) 2015-01-07
JP2017081934A (ja) 2017-05-18
KR20200095568A (ko) 2020-08-10
CN105669676A (zh) 2016-06-15
US20130253193A1 (en) 2013-09-26
BRPI1006794A2 (pt) 2015-08-25
JP2021100930A (ja) 2021-07-08
EA201170935A1 (ru) 2012-02-28
SG172468A1 (en) 2011-08-29
WO2010083283A2 (en) 2010-07-22
MX2019003989A (es) 2019-08-12
BRPI1006794A8 (pt) 2017-07-11
US9290506B2 (en) 2016-03-22
PE20160788A1 (es) 2016-09-04
KR20220104280A (ko) 2022-07-26
NZ706894A (en) 2016-11-25
CL2011001668A1 (es) 2012-02-03
TWI720517B (zh) 2021-03-01
US10364248B2 (en) 2019-07-30
US20150218174A1 (en) 2015-08-06
CA2749483A1 (en) 2010-07-22
EA201991779A3 (ru) 2020-04-30
BR122020005528B1 (pt) 2022-05-17
MY186533A (en) 2021-07-25
US20160257687A1 (en) 2016-09-08
AU2022201630A1 (en) 2022-03-31
PT2398774T (pt) 2017-09-29
EA201400575A1 (ru) 2015-02-27
CN105669675A (zh) 2016-06-15
BR122020005540B1 (pt) 2021-03-02
TW201524982A (zh) 2015-07-01
IL242750B (en) 2019-06-30
SG10201705183SA (en) 2017-07-28
AU2018202625B2 (en) 2019-12-12
US8993582B2 (en) 2015-03-31
AR082747A1 (es) 2013-01-09
US20100190981A1 (en) 2010-07-29
KR20210022770A (ko) 2021-03-03
IL267122A (en) 2019-08-29
JP2019048835A (ja) 2019-03-28
AU2020201709B2 (en) 2021-12-09
AU2020201709A1 (en) 2020-03-26
MX349632B (es) 2017-08-07
TWI665200B (zh) 2019-07-11
KR20110104119A (ko) 2011-09-21
JP2020073491A (ja) 2020-05-14
AU2010204772B2 (en) 2016-05-26
CN102348693A (zh) 2012-02-08
TW201038575A (en) 2010-11-01
TW202118766A (zh) 2021-05-16
MX2011007102A (es) 2011-09-15
IL267122B (en) 2020-05-31
JP6430464B2 (ja) 2018-11-28
PE20211639A1 (es) 2021-08-24
MX357874B (es) 2018-07-27
IL242752A (en) 2017-06-29
EA020643B1 (ru) 2014-12-30
NZ725585A (en) 2018-05-25
WO2010083283A3 (en) 2010-10-14
TN2011000329A1 (en) 2013-03-27
CL2013002617A1 (es) 2014-03-28
IL214061A (en) 2017-06-29
CL2016000346A1 (es) 2016-11-25
CN108395433A (zh) 2018-08-14
TW202146417A (zh) 2021-12-16
CN102348693B (zh) 2016-03-16
TWI462924B (zh) 2014-12-01
KR101999933B1 (ko) 2019-07-12
IL242751B (en) 2018-03-29
AU2018202625A1 (en) 2018-05-10
PE20171102A1 (es) 2017-08-07
TW201936608A (zh) 2019-09-16
JOP20190230A1 (ar) 2017-06-16
EP3272738A3 (en) 2018-04-04
SG10201913261QA (en) 2020-03-30
CA2749483C (en) 2021-07-27
MY182004A (en) 2021-01-18
EA034207B1 (ru) 2020-01-16
IL274422A (en) 2020-06-30
KR102220482B1 (ko) 2021-02-25
US8410265B2 (en) 2013-04-02
KR102422043B1 (ko) 2022-07-18
EP2398774B1 (en) 2017-07-05
US9908888B2 (en) 2018-03-06
MA33038B1 (ar) 2012-02-01
ECSP11011268A (es) 2011-12-30
AR127757A2 (es) 2024-02-28
PH12016502060A1 (en) 2017-09-18
US20130253190A1 (en) 2013-09-26
TWI644915B (zh) 2018-12-21
KR20190083010A (ko) 2019-07-10
EP2398774A2 (en) 2011-12-28
PE20110858A1 (es) 2011-12-04
IL214061A0 (en) 2011-08-31
US10975085B2 (en) 2021-04-13
KR102318359B1 (ko) 2021-10-27
AU2016216537A1 (en) 2016-09-01
JP6054355B2 (ja) 2016-12-27
CA3121743A1 (en) 2010-07-22
JP2012515212A (ja) 2012-07-05
NZ594057A (en) 2013-11-29
TWI710562B (zh) 2020-11-21
AU2010204772A1 (en) 2011-08-04
PH12016502060B1 (en) 2017-09-18
JP6630802B2 (ja) 2020-01-15
BR122020005540B8 (pt) 2021-07-27
TW201718591A (zh) 2017-06-01
KR102138485B1 (ko) 2020-07-27
EP3272738A2 (en) 2018-01-24
BRPI1006794B1 (pt) 2022-05-17
JP6843955B2 (ja) 2021-03-17
KR20210130846A (ko) 2021-11-01
KR101824742B1 (ko) 2018-02-01
US20180237442A1 (en) 2018-08-23

Similar Documents

Publication Publication Date Title
PH12016502060A1 (en) Processes for preparing jak inhibitors and related intermediate compounds
MX2011012353A (es) 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 cinasa janus.
MX2011004953A (es) Compuestos utiles como inhibidores de cinasa atr.
MX2011006503A (es) Derivados de pirazina utiles como inhibidores de la cinasa de atr.
MX370390B (es) Compuesto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1, 5-a]pirimidin-3-carboxamida util como inhibidor de cinasa de ataxia telangiectasia mutada (atm) y rad3 relacionados (atr), su preparacion, diferentes formas solidas y sus derivados radiomarcados.
MX2012013081A (es) Compuestos utiles como inhibidores de cinasa atr.
EA201290878A1 (ru) ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-a]ПИРАЗИНА И ИХ ПРИМЕНЕНИЕ ДЛЯ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ, ПСИХИАТРИЧЕСКИХ И МЕТАБОЛИЧЕСКИХ РАССТРОЙСТВ И ЗАБОЛЕВАНИЙ
WO2011143423A3 (en) Compounds useful as inhibitors of atr kinase
EA201290244A1 (ru) ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-b]ПИРИДАЗИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE10
WO2011143425A3 (en) Compounds useful as inhibitors of atr kinase
NZ630721A (en) Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use
MX2010006748A (es) Pirazolo[1,5-a]pirimidinas utiles como inhibidores de jak2.
WO2007136692A3 (en) Crystalline forms of 5-chloro-6- (2, 6-difluoro-4- [3- (methylamino) propoxy] phenyl)-n-((1s)-2, 2, 2,-trifluoro-1-methylethyl] [1,2,4] triazolo [1,5-a] pyrimidin-7-amine salts
WO2009140127A3 (en) SYNTHESIS OF DIHYDROTHIENO[3,2-d]PYRIMIDINE DIOLS AND SIMILAR PYRIMIDINE DIOLS
TH115252A (th) กรรมวิธีสำหรับการเตรียมตัวยับยั้ง jak และสารประกอบตัวกลางที่เกี่ยวข้อง