AU2010266188B2 - Pyrazolopyrimidine JAK inhibitor compounds and methods - Google Patents

Pyrazolopyrimidine JAK inhibitor compounds and methods Download PDF

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Publication number
AU2010266188B2
AU2010266188B2 AU2010266188A AU2010266188A AU2010266188B2 AU 2010266188 B2 AU2010266188 B2 AU 2010266188B2 AU 2010266188 A AU2010266188 A AU 2010266188A AU 2010266188 A AU2010266188 A AU 2010266188A AU 2010266188 B2 AU2010266188 B2 AU 2010266188B2
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Australia
Prior art keywords
pyrazolo
alkyl
pyrimidine
carboxamide
pyrazol
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Ceased
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AU2010266188A
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AU2010266188A1 (en
Inventor
Paul Gibbons
Emily Hanan
Wendy Liu
Joseph P. Lyssikatos
Steven R. Magnuson
Rohan Mendonca
Richard Pastor
Thomas E. Rawson
Michael Siu
Mark E. Zak
Aihe Zhou
Bing-Yan Zhu
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Genentech Inc
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Genentech Inc
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Priority to AU2015255320A priority Critical patent/AU2015255320B2/en
Application granted granted Critical
Publication of AU2010266188B2 publication Critical patent/AU2010266188B2/en
Priority to AU2017228672A priority patent/AU2017228672A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2010266188A 2009-07-02 2010-07-02 Pyrazolopyrimidine JAK inhibitor compounds and methods Ceased AU2010266188B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2015255320A AU2015255320B2 (en) 2009-07-02 2015-11-13 Pyrazolopyrimidine JAK inhibitor compounds and methods
AU2017228672A AU2017228672A1 (en) 2009-07-02 2017-09-14 Pyrazolopyrimidine JAK inhibitor compounds and methods

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22291809P 2009-07-02 2009-07-02
US61/222,918 2009-07-02
PCT/US2010/040906 WO2011003065A2 (en) 2009-07-02 2010-07-02 Pyrazolopyrimidine jak inhibitor compounds and methods

Related Child Applications (1)

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AU2015255320A Division AU2015255320B2 (en) 2009-07-02 2015-11-13 Pyrazolopyrimidine JAK inhibitor compounds and methods

Publications (2)

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AU2010266188A1 AU2010266188A1 (en) 2012-02-02
AU2010266188B2 true AU2010266188B2 (en) 2015-11-26

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AU2010266188A Ceased AU2010266188B2 (en) 2009-07-02 2010-07-02 Pyrazolopyrimidine JAK inhibitor compounds and methods

Country Status (35)

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US (6) US8999998B2 (OSRAM)
EP (3) EP3333169B1 (OSRAM)
JP (4) JP5769261B2 (OSRAM)
KR (3) KR20180108858A (OSRAM)
CN (2) CN102482284B (OSRAM)
AU (1) AU2010266188B2 (OSRAM)
BR (1) BRPI1010197A2 (OSRAM)
CA (1) CA2767097A1 (OSRAM)
CL (1) CL2012000001A1 (OSRAM)
CO (1) CO6491081A2 (OSRAM)
CR (2) CR20170115A (OSRAM)
DK (1) DK2448941T3 (OSRAM)
EC (1) ECSP12011645A (OSRAM)
ES (1) ES2657839T3 (OSRAM)
HR (1) HRP20180157T1 (OSRAM)
HU (1) HUE035537T2 (OSRAM)
IL (3) IL217224B (OSRAM)
IN (1) IN2012DN00755A (OSRAM)
LT (1) LT2448941T (OSRAM)
MA (1) MA33502B1 (OSRAM)
MX (1) MX2012000169A (OSRAM)
MY (1) MY160156A (OSRAM)
NO (1) NO2448941T3 (OSRAM)
NZ (4) NZ738778A (OSRAM)
PE (2) PE20151249A1 (OSRAM)
PH (1) PH12015500666A1 (OSRAM)
PL (1) PL2448941T3 (OSRAM)
PT (1) PT2448941T (OSRAM)
RS (1) RS56671B1 (OSRAM)
RU (2) RU2675857C2 (OSRAM)
SG (2) SG177454A1 (OSRAM)
SI (1) SI2448941T1 (OSRAM)
UA (1) UA110324C2 (OSRAM)
WO (1) WO2011003065A2 (OSRAM)
ZA (2) ZA201200490B (OSRAM)

Families Citing this family (128)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ME01312B (me) 2005-12-13 2013-12-20 Incyte Corp Heteroaril supstituirani pirol0[2,3-b]piridini i pirol0 [ 2,3-b]pirimidini kao inhibitori janus kinaze
PL2173752T5 (pl) 2007-06-13 2022-12-05 Incyte Holdings Corporation Sole (r)-3-(4-(7h-pirolo(2,3-d)pirymidyn-4-ylo)-1h-pirazol-1-ilo)-3-cyklopentylopropanonitrylu inhibitora kinazy janusowej
AU2009308675A1 (en) 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods
SMT201900698T1 (it) 2009-05-22 2020-01-14 Incyte Holdings Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]ottano- o eptano-nitrile come inibitori di jak
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
KR101857680B1 (ko) 2010-03-10 2018-05-14 인사이트 홀딩스 코포레이션 Jak1 저해제로서의 피페리딘­4­일 아제티딘 유도체
KR101464060B1 (ko) 2010-04-07 2014-11-20 에프. 호프만-라 로슈 아게 피라졸-4-일-헤테로사이클릴-카복사마이드 화합물 및 사용 방법
CA2799928C (en) 2010-05-21 2020-03-31 Incyte Corporation Topical formulation for a jak inhibitor
CN110003219A (zh) 2010-07-13 2019-07-12 弗·哈夫曼-拉罗切有限公司 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物
CA2816076C (en) 2010-11-03 2020-07-14 Dow Agrosciences Llc Pyridyl-pyrazolyl molecules
US8609669B2 (en) * 2010-11-16 2013-12-17 Abbvie Inc. Potassium channel modulators
AR083933A1 (es) 2010-11-19 2013-04-10 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
EP2688872A4 (en) * 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED KINASES
US8859549B2 (en) 2011-05-13 2014-10-14 Abbvie, Inc. Potassium channel modulators
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
JP2014517079A (ja) 2011-06-22 2014-07-17 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 Atrキナーゼ阻害剤として有用な化合物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013045461A1 (en) 2011-09-27 2013-04-04 F. Hoffmann-La Roche Ag Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
DK2760867T3 (en) 2011-09-30 2016-04-11 Oncodesign Sa Macrocyclic FLT3 kinase inhibitors
UA114611C2 (uk) 2011-10-26 2017-07-10 Дау Аґросаєнсиз Елелсі Пестицидні композиції і способи, що їх стосуються
US9012443B2 (en) 2011-12-07 2015-04-21 Amgen Inc. Bicyclic aryl and heteroaryl sodium channel inhibitors
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9282739B2 (en) 2012-04-27 2016-03-15 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
NZ700595A (en) 2012-04-27 2016-04-29 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
US9708288B2 (en) 2012-04-27 2017-07-18 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
EP2882718A4 (en) * 2012-08-10 2015-12-23 Hoffmann La Roche PYRAZOL CARBOXAMIDE COMPOUNDS AND COMPOSITIONS AND METHOD OF USE THEREOF
CN103073549A (zh) * 2012-09-07 2013-05-01 苏州康润医药有限公司 3-溴吡唑啉[1,5-α]吡嘧啶-2-甲酸的合成工艺
CN104640850A (zh) * 2012-10-26 2015-05-20 霍夫曼-拉罗奇有限公司 3,4-二取代的1h-吡唑和4,5-二取代的噻唑的syk抑制剂
PE20200175A1 (es) 2012-11-15 2020-01-24 Incyte Holdings Corp Formas de dosificacion de ruxolitinib de liberacion sostenida
EP4190786B1 (en) 2012-12-07 2025-02-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2951590A1 (en) 2013-02-04 2015-12-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
WO2014138168A1 (en) 2013-03-06 2014-09-12 Incyte Corporation Processes and intermediates for making a jak inhibitor
WO2014143242A1 (en) * 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8957078B2 (en) 2013-03-15 2015-02-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
TWI730935B (zh) * 2013-08-07 2021-06-21 美商英塞特公司 Jak1抑制劑之持續釋放劑型
DK3052485T3 (da) 2013-10-04 2021-10-11 Infinity Pharmaceuticals Inc Heterocykliske forbindelser og anvendelser deraf
CA2926095A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
EP3057430A4 (en) 2013-10-17 2017-09-13 Dow AgroSciences LLC Processes for the preparation of pesticidal compounds
CN105636442B (zh) 2013-10-17 2018-04-27 美国陶氏益农公司 制备杀虫化合物的方法
BR112016008070B8 (pt) 2013-10-17 2022-08-23 Dow Agrosciences Llc Compostos pesticidas, e seus processos de preparação
CA2925952A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
WO2015058026A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
CN105636440A (zh) 2013-10-17 2016-06-01 美国陶氏益农公司 制备杀虫化合物的方法
JP6509209B2 (ja) 2013-10-22 2019-05-08 ダウ アグロサイエンシィズ エルエルシー 農薬組成物および関連する方法
NZ719541A (en) 2013-10-22 2017-11-24 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
TW201519776A (zh) 2013-10-22 2015-06-01 Dow Agrosciences Llc 協同性殺蟲組成物及相關方法(八)
TW201519777A (zh) 2013-10-22 2015-06-01 Dow Agrosciences Llc 協同性殺蟲組成物及相關方法(九)
TW201519782A (zh) 2013-10-22 2015-06-01 Dow Agrosciences Llc 殺蟲組成物及相關方法(五)
RU2016119360A (ru) 2013-10-22 2017-11-28 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи Синергетические пестицидные композиции и связанные с ними способы
KR20160074581A (ko) 2013-10-22 2016-06-28 다우 아그로사이언시즈 엘엘씨 상승작용적 살충 조성물 및 관련 방법
RU2656391C2 (ru) 2013-10-22 2018-06-05 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи Пестицидные композиции и связанные с ними способы
CN105792650A (zh) 2013-10-22 2016-07-20 美国陶氏益农公司 协同杀虫组合物和相关方法
RU2016119566A (ru) 2013-10-22 2017-11-28 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи Синергетические пестицидные композиции и относящиеся к ним способы
US9549560B2 (en) 2013-10-22 2017-01-24 Dow Agrosciences Llc Pesticidal compositions and related methods
US9445597B2 (en) 2013-10-22 2016-09-20 Dow Agrosciences Llc Pesticidal compositions and related methods
AU2014340424B2 (en) 2013-10-22 2017-06-29 Dow Agrosciences Llc Pesticidal compositions and related methods
TW201519775A (zh) 2013-10-22 2015-06-01 Dow Agrosciences Llc 協同性殺蟲組成物及相關方法(七)
MX2016005325A (es) 2013-10-22 2016-08-08 Dow Agrosciences Llc Composiciones pesticidas sinergicas y metodos relacionados.
WO2015061149A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
WO2015061142A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
UY35821A (es) * 2013-11-08 2015-06-30 Takeda Pharmaceutical Compuesto heterocíclico
CN104650092B (zh) * 2013-11-16 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
EA030472B1 (ru) 2013-12-05 2018-08-31 Пфайзер Инк. ПИРРОЛО[2,3-d]ПИРИМИДИНИЛ-, ПИРРОЛО[2,3-b]ПИРАЗИНИЛ- И ПИРРОЛО[2,3-d]ПИРИДИНИЛАКРИЛАМИДЫ
US10160760B2 (en) 2013-12-06 2018-12-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP3077393A1 (en) * 2013-12-06 2016-10-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
TW201620911A (zh) * 2014-03-17 2016-06-16 雷西肯製藥股份有限公司 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法
WO2015143012A1 (en) 2014-03-19 2015-09-24 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
US9493439B1 (en) 2014-04-07 2016-11-15 University Of Kentucky Research Foundation Proteasome inhibitors
EP3795152A1 (en) * 2014-04-08 2021-03-24 Incyte Corporation Treatment of b-cell malignancies by a combination jak and pi3k inhibitor
SI3145929T1 (sl) * 2014-05-23 2021-10-29 Hoffmann La Roche 5-kloro-2-difluorometoksifenil pirazolopirimidinove spojine, ki so zaviralci janusove kinaze
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
AU2015271030B2 (en) * 2014-06-05 2019-05-16 Vertex Pharmaceuticals Incorporated Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof
SI3157566T1 (sl) 2014-06-17 2019-08-30 Vertex Pharmaceuticals Incorporated Postopek za zdravljenje raka z uporabo kombinacije inhibitorjev CHK1 in ATR
AR098107A1 (es) 2014-07-31 2016-05-04 Dow Agrosciences Llc Proceso para la preparación de 3-(3-cloro-1h-pirazol-1-il)piridina
BR112017000418A2 (pt) 2014-07-31 2017-11-07 Dow Agrosciences Llc processo para a preparação de 3-(3-cloro-1h-pirazol-1-il)piridina
KR20170039121A (ko) 2014-07-31 2017-04-10 다우 아그로사이언시즈 엘엘씨 3-(3-클로로-1h-피라졸-1-일)피리딘의 제조 방법
US9024031B1 (en) 2014-08-19 2015-05-05 Dow Agrosciences Llc Process for the preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine
AR098113A1 (es) 2014-09-12 2016-05-04 Dow Agrosciences Llc Proceso para la preparación de 3-(3-cloro-1h-pirazol-1-il)piridina
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
WO2016202898A1 (en) * 2015-06-19 2016-12-22 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
NZ740616A (en) * 2015-09-14 2023-05-26 Infinity Pharmaceuticals Inc Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
RU2768621C1 (ru) 2015-09-30 2022-03-24 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr
EP3371187A4 (en) 2015-11-06 2019-09-04 Samumed, LLC 2- (1H-INDAZOLE-3-YL) -3H-IMIDAZO [4,5-C] PYRIDINE AND ITS USE AS AN INHIBITOR OF INHIBITOR
TW201720828A (zh) * 2015-11-23 2017-06-16 赫孚孟拉羅股份公司 治療性化合物及組合物以及其使用方法
JP6936236B2 (ja) 2016-02-18 2021-09-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 治療化合物、組成物及びその方法の使用
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
MX390577B (es) 2016-06-01 2025-03-20 Samumed Llc Proceso de preparación de n-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida.
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN106008525B (zh) * 2016-06-16 2018-08-07 南京工业大学 一种小分子有机纳米肿瘤光热治疗试剂及其制备方法
BR112019013287A2 (pt) * 2016-12-29 2019-12-24 Hoffmann La Roche compostos de pirazolopirimidina e métodos de uso dos mesmos
BR112019008372B1 (pt) 2016-12-29 2021-11-09 Dow Agrosciences Llc Processo para preparação de compostos pesticidas
US10233155B2 (en) 2016-12-29 2019-03-19 Dow Agrosciences Llc Processes for the preparation of pesticide compounds
WO2018134213A1 (en) 2017-01-17 2018-07-26 Astrazeneca Ab Jak1 selective inhibitors
EP3596072B1 (en) 2017-03-14 2022-06-22 F. Hoffmann-La Roche AG Pyrazolochlorophenyl compounds, compositions and methods of use thereof
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
US20200088732A1 (en) 2017-04-13 2020-03-19 INSERM (Institut National de la Santé et de la Recherche Mèdicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
PL233595B1 (pl) * 2017-05-12 2019-11-29 Celon Pharma Spolka Akcyjna Pochodne pirazolo[1,5-a]pirymidyny jako inhibitory kinazy JAK
MA48942A (fr) * 2017-05-22 2020-04-08 Hoffmann La Roche Composés thérapeutiques, compositions et procédés d'utilisation associés
TW201900648A (zh) 2017-05-22 2019-01-01 瑞士商赫孚孟拉羅股份公司 治療性化合物及組成物以及其使用方法
RU2020107152A (ru) 2017-07-18 2021-08-27 Байер Кропсайенс Акциенгезельшафт Замещенные 3-гетероарилокси-1н-пиразолы и их соли, а также применение в качестве гербицидных активных веществ
CN107686456B (zh) * 2017-07-25 2018-10-23 杭州师范大学 一种喹喏酮关键中间体乙酯胺化物及其制备方法和应用
CN109422751B (zh) * 2017-09-03 2022-04-22 上海美志医药科技有限公司 一类具有降解酪氨酸蛋白激酶jak3活性的化合物
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
WO2019139714A1 (en) 2018-01-15 2019-07-18 Genentech, Inc. Pyrazolopyrimidine compounds as jak inhibitors
WO2019141694A1 (en) * 2018-01-17 2019-07-25 Glaxosmithkline Intellectual Property Development Limited Pi4kiiibeta inhibitors
MA51771B1 (fr) 2018-01-30 2022-03-31 Incyte Corp Procédés de préparation de (1-(3-fluoro-2-(trifluorométhyl)isonicotinyl)pipéridine-4-one)
CN110476009A (zh) 2018-03-07 2019-11-19 三菱化学株式会社 透明树脂组合物、树脂成型体、灯罩、车辆用灯罩、组合灯罩和车辆
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
SG11202010092XA (en) 2018-04-13 2020-11-27 Incyte Corp Biomarkers for graft-versus-host disease
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
WO2020150552A2 (en) * 2019-01-17 2020-07-23 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220024405A (ko) 2019-06-18 2022-03-03 에프. 호프만-라 로슈 아게 Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용
EP3986900A1 (en) 2019-06-18 2022-04-27 F. Hoffmann-La Roche AG Tetrazole-substituted pyrazolopyrimidine inhibitors of jak kinases and uses thereof
JP7716993B2 (ja) 2019-06-18 2025-08-01 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト Jakキナーゼのピラゾロピリミジンアリールエーテル阻害剤及びその使用
AU2020356575A1 (en) 2019-09-27 2022-04-14 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
CA3157499A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
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
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115003667B (zh) * 2020-02-26 2025-04-15 百济神州有限公司 Tyk-2抑制剂
MX2022014254A (es) 2020-05-13 2023-02-16 Disc Medicine Inc Anticuerpos anti-hemojuvelina (hjv) para tratar mielofibrosis.
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022256358A1 (en) 2021-06-03 2022-12-08 Genentech, Inc. Process for preparing medicaments
CN115466227B (zh) * 2022-06-30 2024-07-19 杭州国瑞生物科技有限公司 一种3-(氯甲基)-1-甲基-1h-1,2,4-三唑盐酸盐的制备方法
WO2024262911A1 (ko) * 2023-06-19 2024-12-26 주식회사 에이조스바이오 신규 피라졸로 피리미딘계 화합물 및 이의 용도

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005002552A2 (en) * 2003-07-03 2005-01-13 Astex Therapeutics Limited Benzimidazole derivatives and their use as protein kinases inhibitors

Family Cites Families (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES8401486A1 (es) 1981-11-10 1983-12-01 Wellcome Found Un procedimiento para la preparacion de nuevos derivados de imidazo (4,5-c)piridina.
US4602035A (en) 1983-12-07 1986-07-22 Hoechst-Roussel Pharmaceuticals Inc. Antidepressant (3-aryl-2,3-dihydrobenzofuran-3-yl)alkylamines
US4847256A (en) 1986-10-16 1989-07-11 American Cyanamid Company 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
US6136595A (en) 1993-07-29 2000-10-24 St. Jude Children's Research Hospital Jak kinases and regulations of cytokine signal transduction
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
US5705625A (en) 1994-12-15 1998-01-06 The Johns Hopkins University School Of Medicine Nucleic Acid Encoding novel protein tyrosine kinase
US7070972B1 (en) 1995-01-13 2006-07-04 The United States Of America As Represented By The Department Of Health And Human Services Janus family kinases and identification of immune modulators
US7091020B1 (en) 1995-12-05 2006-08-15 Incyte Corporation Human Jak2 kinase
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
US6235741B1 (en) 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
FR2791562B1 (fr) 1999-03-29 2004-03-05 Oreal Composition tinctoriale contenant une pyrazolo-[1,5-a]- pyrimidine et une polyaminopyrimidine monocyclique a titre de bases d'oxydation et un coupleur, et procedes de teinture
AU778450B2 (en) 1999-07-02 2004-12-09 Eisai R&D Management Co., Ltd. Fused imidazole compounds and remedies for diabetes mellitus
UA72290C2 (uk) * 1999-12-10 2005-02-15 Пфайзер Продактс Інк. СПОЛУКИ ПІРОЛО[2.3-d]ПІРИМІДИНУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ (ВАРІАНТИ), СПОСІБ ІНГІБУВАННЯ ПРОТЕЇНКІНАЗ АБО JANUS КІНАЗИ 3 (ВАРІАНТИ)
CN100343255C (zh) 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5-a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
US7161003B1 (en) 2002-09-04 2007-01-09 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
AU2003270701B2 (en) 2002-10-31 2009-11-12 Amgen Inc. Antiinflammation agents
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2004089471A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
US20070270408A1 (en) 2003-04-11 2007-11-22 Novo Nordisk A/S Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
SE0301372D0 (sv) * 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
WO2005004810A2 (en) * 2003-07-02 2005-01-20 Merck & Co., Inc. Arylsulfonamide derivatives
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
PT1730146E (pt) * 2004-03-30 2011-07-11 Vertex Pharma Azaindoles úteis como inibidores de jak e outras proteínas quinases
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
US20060030536A1 (en) 2004-04-09 2006-02-09 University Of South Florida Combination therapies for cancer and proliferative angiopathies
JP2007535560A (ja) 2004-04-28 2007-12-06 シーブイ・セラピューティクス・インコーポレイテッド A1アデノシンレセプターアンタゴニスト
EP1765825A1 (en) 2004-06-25 2007-03-28 Amgen Inc. Condensed triazoles and indazoles useful in treating citokines mediated diseases and other diseases
ES2354824T3 (es) 2004-11-04 2011-03-18 Vertex Pharmaceuticals, Inc. Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas.
WO2007013673A1 (en) 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
WO2007039797A1 (en) 2005-10-03 2007-04-12 Pfizer Products Inc. Use of cannabinoid receptor-1 antagonist for treating inflammation and arthritis
CA2624500A1 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
CA2624882C (en) * 2005-10-06 2014-05-20 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
US8372851B2 (en) 2005-10-21 2013-02-12 Exelixis, Inc. Pyrazolo pyrimidines as casein kinase II (CK2) modulators
EP1963316A2 (en) 2005-12-08 2008-09-03 Novartis AG Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
US8541406B2 (en) * 2006-02-07 2013-09-24 Nv Remynd Thiadiazole derivatives for the treatment of neurodegenerative diseases
TW200800997A (en) 2006-03-22 2008-01-01 Astrazeneca Ab Chemical compounds
KR20090018895A (ko) * 2006-04-05 2009-02-24 버텍스 파마슈티칼스 인코포레이티드 야누스 키나제의 억제제로서 유용한 데아자푸린
KR20150140872A (ko) 2006-06-02 2015-12-16 니뽄 신야쿠 가부시키가이샤 9,10-세코프레그난 유도체 및 의약
AR061793A1 (es) 2006-07-05 2008-09-24 Mitsubishi Tanabe Pharma Corp Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
RU2009120389A (ru) 2006-10-30 2010-12-10 Новартис АГ (CH) Гетероциклические соединения в качестве противовоспалительных агентов
WO2008063671A2 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
CN101889004B (zh) * 2007-10-12 2014-09-10 阿斯利康公司 蛋白激酶抑制剂
CN101917849B (zh) 2007-11-28 2014-11-05 达那-法伯癌症研究所 Bcr-abl的小分子豆蔻酸酯抑制剂及其使用方法
WO2009086303A2 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
US8252791B2 (en) 2008-08-13 2012-08-28 Jenrin Discovery, Inc. Purine compounds as cannabinoid receptor blockers
AU2009308675A1 (en) * 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods
WO2010063487A1 (en) 2008-12-05 2010-06-10 Merz Pharma Gmbh & Co. Kgaa Pyrazolopyrimidines, a process for their preparation and their use as medicine
ES2481715T3 (es) 2009-02-06 2014-07-31 Janssen Pharmaceuticals, Inc. Compuestos heterocíclicos bicíclicos sustituidos novedosos como moduladores de gamma-secretasa
TWI461425B (zh) 2009-02-19 2014-11-21 Janssen Pharmaceuticals Inc 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
MX2012004020A (es) 2009-10-20 2012-05-08 Cellzome Ltd Analogos de heterociclilo pirazolopirimidina como inhibidores de jak.
EP2547338A2 (en) 2010-03-17 2013-01-23 F. Hoffmann-La Roche AG Imidazopyridine compounds, compositions and methods of use
KR20130094693A (ko) 2010-04-30 2013-08-26 셀좀 리미티드 Jak 저해제로서의 피라졸 화합물

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005002552A2 (en) * 2003-07-03 2005-01-13 Astex Therapeutics Limited Benzimidazole derivatives and their use as protein kinases inhibitors

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