[go: up one dir, main page]

PE20171102A1 - Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados - Google Patents

Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados

Info

Publication number
PE20171102A1
PE20171102A1 PE2017000602A PE2017000602A PE20171102A1 PE 20171102 A1 PE20171102 A1 PE 20171102A1 PE 2017000602 A PE2017000602 A PE 2017000602A PE 2017000602 A PE2017000602 A PE 2017000602A PE 20171102 A1 PE20171102 A1 PE 20171102A1
Authority
PE
Peru
Prior art keywords
processes
jak inhibitors
intermediary compounds
preparing
pyrrolo
Prior art date
Application number
PE2017000602A
Other languages
English (en)
Inventor
Jiacheng Zhou
Pingli Liu
Qiyan Lin
Brian W Metcalf
David Meloni
Yongchun Pan
Michael Xia
Mei Li
Tai-Yuen Yue
James D Rodgers
Haisheng Wang
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42026219&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20171102(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of PE20171102A1 publication Critical patent/PE20171102A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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
    • C07D231/16—Halogen atoms or nitro radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/30—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/0825—Preparations of compounds not comprising Si-Si or Si-cyano linkages
    • C07F7/083—Syntheses without formation of a Si-C bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design 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)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Se refiere a un proceso para preparar sal de fosfato de (3R)-ciclopentil-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)pirazol-1-il]propionitrilo que comprende hacer reaccionar el compuesto (3R)-ciclopentil-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)pirazol-1-il]propionitrilo con acido fosforico en presencia de 2-propanol y diclorometano. Tambien se refiere a un metodo de purificacion de dicha sal que comprende recristalizar la sal de fosfato de (3R)-ciclopentil-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)pirazol-1-il]propionitrilo a partir de una mezcla de solventes que comprende metanol, 2-propanol y n-heptano.
PE2017000602A 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados PE20171102A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20171102A1 true PE20171102A1 (es) 2017-08-07

Family

ID=42026219

Family Applications (4)

Application Number Title Priority Date Filing Date
PE2011001347A PE20110858A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados
PE2017000602A PE20171102A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados
PE2016000575A PE20160788A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados
PE2021000139A PE20211639A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2011001347A PE20110858A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados

Family Applications After (2)

Application Number Title Priority Date Filing Date
PE2016000575A PE20160788A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados
PE2021000139A PE20211639A1 (es) 2009-01-15 2010-01-14 Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado

Country Status (29)

Country Link
US (10) US8410265B2 (es)
EP (3) EP3272738B1 (es)
JP (6) JP5650662B2 (es)
KR (7) KR102422043B1 (es)
CN (5) CN108395433B (es)
AR (2) AR082747A1 (es)
AU (5) AU2010204772B2 (es)
BR (3) BRPI1006794B1 (es)
CA (2) CA3121743A1 (es)
CL (3) CL2011001668A1 (es)
CO (1) CO6400137A2 (es)
EA (3) EA020643B1 (es)
EC (1) ECSP11011268A (es)
ES (2) ES2641761T3 (es)
IL (7) IL214061A (es)
JO (3) JOP20190230A1 (es)
MA (1) MA33038B1 (es)
MX (5) MX357874B (es)
MY (3) MY186533A (es)
NZ (5) NZ594057A (es)
PE (4) PE20110858A1 (es)
PH (1) PH12016502060B1 (es)
PL (2) PL2398774T3 (es)
PT (2) PT3272738T (es)
SG (3) SG172468A1 (es)
TN (1) TN2011000329A1 (es)
TW (7) TWI720517B (es)
WO (1) WO2010083283A2 (es)
ZA (1) ZA201104909B (es)

Families Citing this family (150)

* 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
EP3838903B1 (en) 2005-12-13 2023-11-22 Incyte Holdings Corporation Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor
CN101932582B (zh) 2007-06-13 2013-09-25 因塞特公司 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐
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.
KR101580482B1 (ko) * 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 ４－피라졸릴－ｎ－아릴피리미딘－２－아민 및 ４－피라졸릴－ｎ－헤테로아릴피리미딘－２－아민
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
RS59632B1 (sr) 2009-05-22 2020-01-31 Incyte Holdings Corp 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori
US8716303B2 (en) * 2009-05-22 2014-05-06 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2011044481A1 (en) * 2009-10-09 2011-04-14 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
MX2012009541A (es) * 2010-02-18 2012-10-01 Incyte Corp Derivados de ciclobutano y metilciclobutano como inhibidores de janus cinasa.
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
CA2796388A1 (en) 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
NZ603686A (en) 2010-05-21 2014-11-28 Incyte Corp Topical formulation for a jak inhibitor
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ 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
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
MX357939B (es) 2011-02-18 2018-07-31 Novartis Pharma Ag Terapia de combinacion de inhibidor de objetivo de rapamicina en mamifero/janus cinasa (mtor/jak).
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
KR20140040819A (ko) 2011-06-20 2014-04-03 인사이트 코포레이션 Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체
CA2844507A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag Jak pi3k/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
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
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
RS67061B1 (sr) 2012-06-15 2025-08-29 Sun Pharmaceutical Industries Inc Deuterisani derivati ruksolitiniba
WO2014011540A1 (en) 2012-07-09 2014-01-16 Emory University Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014028756A1 (en) 2012-08-17 2014-02-20 Concert Pharmaceuticals, Inc. Deuterated baricitinib
WO2014060381A1 (de) 2012-10-18 2014-04-24 Bayer Cropscience Ag Heterocyclische verbindungen als schädlingsbekämpfungsmittel
BR112015009751A2 (pt) 2012-10-31 2017-07-11 Bayer Cropscience Ag novos compostos heterocíclicos como pesticidas
SG11201503141TA (en) 2012-11-01 2015-06-29 Incyte Corp Tricyclic fused thiophene derivatives as jak inhibitors
US10166191B2 (en) 2012-11-15 2019-01-01 Incyte Corporation Sustained-release dosage forms of ruxolitinib
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
DK2964650T3 (en) 2013-03-06 2019-02-11 Incyte Holdings Corp PROCEDURES AND INTERMEDIATES FOR THE MANUFACTURE OF A JAK INHIBITOR
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
MX385187B (es) 2013-05-17 2025-03-14 Incyte Holdings Corp Derivados del bipirazol como inhibidores de janus cinasa (jak)
SI3030227T1 (sl) 2013-08-07 2020-08-31 Incyte Corporation Dozirne oblike s podaljšanim sproščanjem za inhibitor 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
HRP20171846T1 (hr) 2013-12-05 2018-01-12 Pfizer Inc. PIROLO[2,3-d]PIRIMIDINIL-, PIROLO[2,3-b]PIRAZINIL- I PIROLO[2,3-d]PIRIDINILAKRILAMIDI
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
EA202191009A1 (ru) 2014-04-08 2021-08-31 Инсайт Корпорейшн Лечение b-клеточных злокачественных новообразований с применением комбинации ингибиторов jak и pi3k
BR112016025427A2 (pt) 2014-04-30 2017-08-15 Incyte Corp processos de preparação de um inibidor de jak1 e formas do mesmo
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
PT3179991T (pt) 2014-08-11 2021-11-26 Acerta Pharma Bv Combinações terapêuticas de um inibidor de btk e um inibidor de bcl-2
HUE059131T2 (hu) 2014-08-11 2022-10-28 Acerta Pharma Bv BTK-inhibitor, PD-1-inhibitor és/vagy PD-L1-inhibitor terápiás kombinációja
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
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
WO2016088094A1 (en) * 2014-12-05 2016-06-09 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
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
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
CN108699063B (zh) * 2015-12-31 2020-06-26 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺
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
ES2877200T3 (es) * 2016-01-26 2021-11-16 Hangzhou Bangshun Pharmaceutical Co Ltd Derivado azacíclico de cinco miembros de pirrolopirimidina y aplicación del mismo
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
LT3452039T (lt) 2016-05-04 2024-10-25 Sun Pharmaceutical Industries, Inc. Plaukų slinkimo sutrikimo gydymas deuterintais jak inhibitoriais
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
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
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
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
US10596161B2 (en) 2017-12-08 2020-03-24 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
LT3746429T (lt) 2018-01-30 2022-05-10 Incyte Corporation (1-(3-fluor-2-(trifluormetil)izonikotinil)piperidin-4-ono) gamybos būdai
BR112020016628A2 (pt) 2018-02-16 2020-12-15 Incyte Corporation Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
MY206999A (en) 2018-03-30 2025-01-23 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
MA52208A (fr) 2018-04-13 2021-02-17 Incyte Corp Biomarqueurs pour une maladie du greffon contre l'hôte
PE20210919A1 (es) 2018-05-04 2021-05-19 Incyte Corp Sales de un inhibidor de fgfr
CN119241541A (zh) 2018-05-04 2025-01-03 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
KR102884803B1 (ko) 2018-06-01 2025-11-12 인사이트 코포레이션 Pi3k 관련 장애의 치료를 위한 투여 요법
WO2020028258A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide
KR20210056382A (ko) * 2018-09-04 2021-05-18 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 억제제 및 이의 중간체를 제조하는 방법
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
SG11202104321PA (en) 2018-10-31 2021-05-28 Incyte Corp Combination therapy for treatment of hematological diseases
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
AU2020219797B2 (en) * 2019-02-06 2025-10-16 Sun Pharmaceutical Industries, Inc. Process for preparing enantiomerically enriched jak inhibitors
WO2020185532A1 (en) 2019-03-08 2020-09-17 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
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 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
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
PE20230251A1 (es) 2019-11-22 2023-02-07 Incyte Corp Terapia de combinacion que comprende un inhibidor de alk2 y un inhibidor de jak2
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
IL293001A (en) 2019-12-04 2022-07-01 Incyte Corp Derivatives of fgfr repressors
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
PL4157831T3 (pl) 2020-06-02 2025-03-03 Incyte Corporation Sposoby wytwarzania inhibitora jak1
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
US20230322787A1 (en) * 2020-08-12 2023-10-12 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
CN116761792A (zh) * 2020-08-18 2023-09-15 因赛特公司 用于制备jak抑制剂的方法和中间体
WO2022040172A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
AU2021329303A1 (en) 2020-08-18 2023-04-06 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
CA3196551A1 (en) 2020-10-28 2022-05-05 Sun Pharmaceutical Industries, Inc. Regimens for the treatment of hair loss disorders with deuterated jak inhibitors
MX2023006542A (es) 2020-12-08 2023-08-25 Incyte Corp Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del 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
CN114853760B (zh) * 2021-02-03 2025-12-05 南京正大天晴制药有限公司 一种芦可替尼中间体的制备方法
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
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
FI4333840T3 (fi) 2021-05-03 2025-12-12 Incyte Corp Jak1-reitin estäjiä kyhmykutinan hoitoon
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
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
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
AU2022313345B2 (en) * 2021-07-20 2025-12-18 Coval Biopharma (Shanghai) Co., Ltd. Anti-inflammatory coupling compound drug, and preparation method therefor and use thereof
AU2022328272A1 (en) 2021-08-11 2024-02-22 Sun Pharmaceutical Industries, Inc. Treatment of hair loss disorders with deuterated jak inhibitors
AU2022328282A1 (en) 2021-08-12 2024-02-22 Sun Pharmaceutical Industries, Inc. Treatment of jak-inhibition-responsive disorders with prodrugs of jak inhibitors
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
IL316549A (en) 2022-05-04 2024-12-01 Sun Pharmaceutical Ind Inc Dosing regimens for treatment with dual JAK inhibitors
US20250215005A1 (en) * 2022-05-19 2025-07-03 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
CN119032095A (zh) * 2022-08-22 2024-11-26 印度颗粒有限公司 制备鲁索利替尼的改进方法
WO2024099396A1 (zh) * 2022-11-11 2024-05-16 浙江奥翔药业股份有限公司 芦可替尼晶体及其药物组合物
CN118255768A (zh) * 2022-12-26 2024-06-28 上海科胜药物研发有限公司 一种jak抑制剂及其中间体的制备方法
CN116082382B (zh) * 2023-02-13 2025-11-21 上海瀚合瑞医药科技有限公司 芦可替尼关键中间体的制备方法
CN118852013B (zh) * 2023-04-28 2025-09-26 武汉人福创新药物研发中心有限公司 一种芦可替尼及其中间体的制备方法
WO2025052191A1 (en) 2023-09-04 2025-03-13 Granules India Limited Improved process for the preparation of ruxolitinib and novel crystalline form thereof
US12364699B2 (en) 2023-10-10 2025-07-22 Sun Pharmaceuticals Industries, Inc. Method of treating hair loss disorders
CN117946120A (zh) * 2024-01-30 2024-04-30 正大制药（青岛）有限公司 一种磷酸芦可替尼有关物质a的制备方法
CN118047782A (zh) * 2024-02-06 2024-05-17 南京道尔医药研究院有限公司 制备芦可替尼中间体的方法
US12247034B1 (en) * 2024-04-19 2025-03-11 Sun Pharmaceutical Industries, Inc. Crystalline form of deuruxolitinib phosphate
CN118994172A (zh) * 2024-09-12 2024-11-22 广州科锐特生物科技有限公司 一种磷酸芦可替尼的制备方法
CN119528911B (zh) * 2024-10-21 2025-11-28 南通常佑药业科技有限公司 一种芦可替尼的制备方法

Family Cites Families (68)

* 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
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
ATE380031T1 (de) 1999-12-10 2007-12-15 Pfizer Prod Inc Pyrrolo 2,3-d pyrimidinderivate enthaltende zusammensetzungen
AR034854A1 (es) 2000-11-17 2004-03-24 Takeda Chemical Industries Ltd Compuesto de imidazol condensado, prodroga del mismo, composición farmaceutica y agente para reducir androgenos que lo contienen ,metodo para producirlo, sal diastereomerica de dicho compuesto y metodo para producir un compuesto opticamente activo del compuesto
KR20050004214A (ko) 2002-05-31 2005-01-12 에자이 가부시키가이샤 피라졸 화합물 및 이것을 포함하여 이루어지는 의약 조성물
WO2004013141A1 (en) 2002-08-06 2004-02-12 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (tek) activity
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
ES2373639T3 (es) * 2002-12-19 2012-02-07 The Scripps Research Institute Composiciones y usos para estabilizar la transtiretina e inhibir el plegamiento anómalo de la transtiretina.
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
US7709645B2 (en) 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1781654A1 (en) * 2004-07-27 2007-05-09 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.
US20060281764A1 (en) 2005-06-10 2006-12-14 Gaul Michael D Aminopyrimidines as kinase modulators
US20060281755A1 (en) 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using aminopyrimidines kinase modulators
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
US7867949B2 (en) 2005-10-14 2011-01-11 Sumitomo Chemical Company, Limited Hydrazide compound and pesticidal use of the same
EP3838903B1 (en) * 2005-12-13 2023-11-22 Incyte Holdings Corporation Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor
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
SG170828A1 (en) 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us 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
EP3443958A1 (en) 2006-11-22 2019-02-20 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
JP2010524858A (ja) * 2007-04-10 2010-07-22 エスジーエックス ファーマシューティカルズ、インコーポレイテッド 縮合環複素環キナーゼ調節因子
CN101932582B (zh) 2007-06-13 2013-09-25 因塞特公司 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐
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.
AR067354A1 (es) * 2007-06-29 2009-10-07 Sunesis Pharmaceuticals Inc Compuestos utiles como inhibidores de la raf quinasa
KR101580482B1 (ko) 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 ４－피라졸릴－ｎ－아릴피리미딘－２－아민 및 ４－피라졸릴－ｎ－헤테로아릴피리미딘－２－아민
UA101493C2 (ru) 2008-03-11 2013-04-10 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы jak
CN102056846A (zh) * 2008-03-19 2011-05-11 比亚尔-坡特拉有限公司 催化不对称氢化
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
RS59632B1 (sr) 2009-05-22 2020-01-31 Incyte Holdings Corp 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori
US8716303B2 (en) 2009-05-22 2014-05-06 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2011044481A1 (en) 2009-10-09 2011-04-14 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
MX2012009541A (es) 2010-02-18 2012-10-01 Incyte Corp Derivados de ciclobutano y metilciclobutano como inhibidores de janus cinasa.
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
NZ603686A (en) 2010-05-21 2014-11-28 Incyte Corp Topical formulation for a jak inhibitor
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ 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
MX357939B (es) 2011-02-18 2018-07-31 Novartis Pharma Ag Terapia de combinacion de inhibidor de objetivo de rapamicina en mamifero/janus cinasa (mtor/jak).
KR20140040819A (ko) 2011-06-20 2014-04-03 인사이트 코포레이션 Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체
CA2844507A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag Jak pi3k/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
BR122020005540B8 (pt) 2021-07-27
BRPI1006794A2 (pt) 2015-08-25
IL242752A (en) 2017-06-29
US8883806B2 (en) 2014-11-11
US20130253191A1 (en) 2013-09-26
US20180237442A1 (en) 2018-08-23
EP2398774B1 (en) 2017-07-05
TWI710562B (zh) 2020-11-21
US9908888B2 (en) 2018-03-06
AU2020201709B2 (en) 2021-12-09
JOP20190231A1 (ar) 2017-06-16
IL274422A (en) 2020-06-30
EA020643B1 (ru) 2014-12-30
TWI720517B (zh) 2021-03-01
EP4501410A3 (en) 2025-08-06
MX383742B (es) 2025-03-14
CL2016000346A1 (es) 2016-11-25
US20250340559A1 (en) 2025-11-06
CN108395433A (zh) 2018-08-14
JP2019048835A (ja) 2019-03-28
MX349632B (es) 2017-08-07
US8410265B2 (en) 2013-04-02
ES3001142T3 (es) 2025-03-04
AU2020201709A1 (en) 2020-03-26
EP4501410A2 (en) 2025-02-05
KR20210130846A (ko) 2021-11-01
JP2012515212A (ja) 2012-07-05
EP3272738B1 (en) 2024-11-13
IL267122A (en) 2019-08-29
JO3441B1 (ar) 2019-10-20
US10364248B2 (en) 2019-07-30
NZ594057A (en) 2013-11-29
TW201718591A (zh) 2017-06-01
JP6430464B2 (ja) 2018-11-28
TW202003521A (zh) 2020-01-16
EA201400575A1 (ru) 2015-02-27
TWI740775B (zh) 2021-09-21
KR20180011887A (ko) 2018-02-02
PE20160788A1 (es) 2016-09-04
PL2398774T3 (pl) 2017-11-30
US20210253584A1 (en) 2021-08-19
ECSP11011268A (es) 2011-12-30
JP6843955B2 (ja) 2021-03-17
CN119306753A (zh) 2025-01-14
CO6400137A2 (es) 2012-03-15
KR20190083010A (ko) 2019-07-10
US9290506B2 (en) 2016-03-22
JP2017081934A (ja) 2017-05-18
EP3272738A3 (en) 2018-04-04
US8993582B2 (en) 2015-03-31
MX357874B (es) 2018-07-27
US20130253193A1 (en) 2013-09-26
US20200002341A1 (en) 2020-01-02
ES2641761T3 (es) 2017-11-13
EA034207B1 (ru) 2020-01-16
EA201991779A2 (ru) 2019-12-30
PH12016502060A1 (en) 2017-09-18
CL2013002617A1 (es) 2014-03-28
KR102138485B1 (ko) 2020-07-27
BR122020005528B1 (pt) 2022-05-17
MY182004A (en) 2021-01-18
CA3121743A1 (en) 2010-07-22
NZ617077A (en) 2015-05-29
SG10201913261QA (en) 2020-03-30
JP5650662B2 (ja) 2015-01-07
KR101824742B1 (ko) 2018-02-01
IL242751B (en) 2018-03-29
JP2020073491A (ja) 2020-05-14
US20130253190A1 (en) 2013-09-26
EA201170935A1 (ru) 2012-02-28
TWI665200B (zh) 2019-07-11
IL214061A (en) 2017-06-29
NZ739757A (en) 2019-01-25
JP2021100930A (ja) 2021-07-08
NZ706894A (en) 2016-11-25
CN105669676A (zh) 2016-06-15
JP2015091805A (ja) 2015-05-14
MX363976B (es) 2019-04-10
MY186533A (en) 2021-07-25
US20160257687A1 (en) 2016-09-08
TW201524982A (zh) 2015-07-01
AU2022201630B2 (en) 2024-04-18
MX2011007102A (es) 2011-09-15
KR101999933B1 (ko) 2019-07-12
CN102348693A (zh) 2012-02-08
CN105669676B (zh) 2018-04-24
MA33038B1 (fr) 2012-02-01
KR102422043B1 (ko) 2022-07-18
KR102318359B1 (ko) 2021-10-27
AU2016216537B2 (en) 2018-05-10
IL274422B (en) 2021-06-30
JP6630802B2 (ja) 2020-01-15
CN102348693B (zh) 2016-03-16
CN105669675A (zh) 2016-06-15
SG10201705183SA (en) 2017-07-28
KR20110104119A (ko) 2011-09-21
TWI644915B (zh) 2018-12-21
AU2010204772A1 (en) 2011-08-04
AR082747A1 (es) 2013-01-09
SG172468A1 (en) 2011-08-29
CA2749483A1 (en) 2010-07-22
TWI462924B (zh) 2014-12-01
US20100190981A1 (en) 2010-07-29
EP2398774A2 (en) 2011-12-28
MY163540A (en) 2017-09-15
KR20200095568A (ko) 2020-08-10
IL283038A (en) 2021-06-30
CN108395433B (zh) 2024-10-22
AU2018202625B2 (en) 2019-12-12
CA2749483C (en) 2021-07-27
PH12016502060B1 (en) 2017-09-18
AU2016216537A1 (en) 2016-09-01
AU2022201630A1 (en) 2022-03-31
IL267122B (en) 2020-05-31
KR102220482B1 (ko) 2021-02-25
ZA201104909B (en) 2018-11-28
BR122020005540B1 (pt) 2021-03-02
WO2010083283A2 (en) 2010-07-22
EP3272738A2 (en) 2018-01-24
TW201038575A (en) 2010-11-01
IL214061A0 (en) 2011-08-31
KR20220104280A (ko) 2022-07-26
US20150218174A1 (en) 2015-08-06
PE20211639A1 (es) 2021-08-24
MX2019003989A (es) 2019-08-12
PT3272738T (pt) 2025-01-24
WO2010083283A3 (en) 2010-10-14
NZ725585A (en) 2018-05-25
PE20110858A1 (es) 2011-12-04
TN2011000329A1 (en) 2013-03-27
TWI814080B (zh) 2023-09-01
BRPI1006794B1 (pt) 2022-05-17
AU2010204772B2 (en) 2016-05-26
PL3272738T3 (pl) 2025-03-17
IL242750B (en) 2019-06-30
JOP20190230A1 (ar) 2017-06-16
AU2018202625A1 (en) 2018-05-10
EA201991779A3 (ru) 2020-04-30
TW202146417A (zh) 2021-12-16
US10975085B2 (en) 2021-04-13
PT2398774T (pt) 2017-09-29
US9000161B2 (en) 2015-04-07
CL2011001668A1 (es) 2012-02-03
TW201936608A (zh) 2019-09-16
TW202118766A (zh) 2021-05-16
BRPI1006794A8 (pt) 2017-07-11
US12247030B2 (en) 2025-03-11
KR20210022770A (ko) 2021-03-03
JP6054355B2 (ja) 2016-12-27
AR127757A2 (es) 2024-02-28

Similar Documents

Publication Publication Date Title
PE20171102A1 (es) Procesos para preparar inhibidores de jak y compuestos intermediarios relacionados
AR067355A1 (es) Procesos para la preparacion de pirazoles
CL2014000441A1 (es) Una entidad quimica que comprende el compuesto sulfamato de {(1s,2s,4r)-4-[(6-{[(1r,2s)-5-cloro-2-metoxi-2,3-dihidro-1h-inden-1-il]amino}pirimidin-4-il)oxi]-2-hidroxiciclopentil}metilo; inhibidor de la activacion de la enzima nedd-8; forma cristalina i; profarmaco del compuesto; composicion farmaceutica; un metodo para tratar el cancer.
IN2014KN00929A (es)
MY160785A (en) Manufacturing process for pyrimidine derivatives
CL2012000560A1 (es) Procedimiento de preparacion del compuesto intermediario acido 3-oxo-tetrahidrotiofeno-2-carboxilico, utiles en la preparacion de dihidrotienopirimidinas (divisional de la solicitud 3095-08).
EA200900690A1 (ru) Способ получения силденафила
TW200801027A (en) Processes for production of 4-(biphenylyl)azetidin-2-one phosphonic acids
PE20180504A1 (es) PROCESOS E INTERMEDIARIOS PARA LA PREPARACION DE {1-(ETILSULFONIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO
PH12012501438A1 (en) Method for preparing tetrazole methanesulfonic acid salts, and novel compound used in same
CL2011000296A1 (es) Proceso de preparación del ester metílico del ácido 4-oxo-octahidro-indol-1-carboxílico y compuestos intermediarios utilizados.
TN2009000401A1 (en) New methods
UA101835C2 (uk) Спосіб отримання похідних 1-(2-галогенбіфеніл-4-іл)-циклопропанкарбонової кислоти
MX2010001229A (es) Procedimiento para la resolucion de zopiclona y compuestos intermedios.
MY164880A (en) Process for the preparation of isoxazolyl-methoxy-nicotinic acids
BR112012013582A2 (pt) processo para síntese de intermediários úteis para a produção de compostos de indazol e azaindazol substituídos
WO2011102640A3 (en) Method for preparing sitagliptin and amine salt intermediates used therein
BRPI0808570B8 (pt) processo para a preparação de inibidores de glyt-1
MX2010009876A (es) Nuevo proceso para la preparacion de derivados de acido ciclohexanocarboxilico por medio del derivado de ciclohexanocarboxamida correspondiente.
WO2012111027A3 (en) Process for pemetrexed disodium
BR112012007145A2 (pt) processo para a preparação de compostos imidazol bifenílicos
TW200635905A (en) Processes for producing 4-aminoquinazolines
UA85701C2 (ru) Способ получения ингибиторов триптазы
BRPI0515259A (pt) método para produção de compostos de imidazol enantioméricos
UA106595C2 (uk) Спосіб одержання празугрелю