ECSP12011645A - Compuestos y métodos inhibidores de jak de pirazolopirimidina - Google Patents

Compuestos y métodos inhibidores de jak de pirazolopirimidina

Info

Publication number
ECSP12011645A
ECSP12011645A ECSP12011645A ECSP12011645A EC SP12011645 A ECSP12011645 A EC SP12011645A EC SP12011645 A ECSP12011645 A EC SP12011645A EC SP12011645 A ECSP12011645 A EC SP12011645A
Authority
EC
Ecuador
Prior art keywords
methods
pirazolopirimidina
jak
inhibiting compounds
compound
Prior art date
Application number
Other languages
English (en)
Inventor
Paul Gibbons
Emily Hanan
Joseph P Lyssikatos
Steven R Magnuson
Rohan Mendonca
Richard Pastor
Thomas E Rawson
Michael Siu
Mark E Zak
Aihe Zhou
Bing-Yan Zhu
Original Assignee
Genentech Inc
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 Genentech Inc filed Critical Genentech Inc
Publication of ECSP12011645A publication Critical patent/ECSP12011645A/es

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Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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

Landscapes

  • 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)

Abstract

Un compuesto de la Fórmula I, enantiómeros, diasteriomeross, tautómeros o sales farmaceúticamente aceptables de los mismos, en donde R1, R2 y R3 son definidos en la presente, son útiles como inhibidores de uno o más quinasas Janus. Se describe una composición farmacéutica que incluye un compuesto de la Fórmula I y un portador, adyuvante o vehículo farmacéuticamente aceptable, y métodos para tratar o reducir la severidad de una enfermedad o condición en respuesta a la inhibición de una actividad de quinasas Janus en un paciente.
ECSP12011645 2009-07-02 2012-02-02 Compuestos y métodos inhibidores de jak de pirazolopirimidina ECSP12011645A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22291809P 2009-07-02 2009-07-02

Publications (1)

Publication Number Publication Date
ECSP12011645A true ECSP12011645A (es) 2012-03-30

Family

ID=43411778

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP12011645 ECSP12011645A (es) 2009-07-02 2012-02-02 Compuestos y métodos inhibidores de jak de pirazolopirimidina

Country Status (35)

Country Link
US (6) US8999998B2 (es)
EP (3) EP3670514A1 (es)
JP (4) JP5769261B2 (es)
KR (3) KR101903305B1 (es)
CN (2) CN102482284B (es)
AU (1) AU2010266188B2 (es)
BR (1) BRPI1010197A2 (es)
CA (1) CA2767097A1 (es)
CL (1) CL2012000001A1 (es)
CO (1) CO6491081A2 (es)
CR (2) CR20170115A (es)
DK (1) DK2448941T3 (es)
EC (1) ECSP12011645A (es)
ES (1) ES2657839T3 (es)
HR (1) HRP20180157T1 (es)
HU (1) HUE035537T2 (es)
IL (3) IL217224B (es)
IN (1) IN2012DN00755A (es)
LT (1) LT2448941T (es)
MA (1) MA33502B1 (es)
MX (1) MX2012000169A (es)
MY (1) MY160156A (es)
NO (1) NO2448941T3 (es)
NZ (4) NZ738778A (es)
PE (2) PE20151249A1 (es)
PH (1) PH12015500666A1 (es)
PL (1) PL2448941T3 (es)
PT (1) PT2448941T (es)
RS (1) RS56671B1 (es)
RU (2) RU2675857C2 (es)
SG (2) SG10201509607XA (es)
SI (1) SI2448941T1 (es)
UA (1) UA110324C2 (es)
WO (1) WO2011003065A2 (es)
ZA (2) ZA201200490B (es)

Families Citing this family (128)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI630207B (zh) 2005-12-13 2018-07-21 英塞特控股公司 作為傑納斯激酶（ＪＡＮＵＳ ＫＩＮＡＳＥ）抑制劑之經雜芳基取代之吡咯并〔２，３-ｂ〕吡啶及吡咯并〔２，３-ｂ〕嘧啶
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
RU2539568C2 (ru) 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
EP3050882B1 (en) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
SG184475A1 (en) 2010-04-07 2012-11-29 Hoffmann La Roche Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
KR101995013B1 (ko) 2010-07-13 2019-07-02 에프. 호프만-라 로슈 아게 Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체
CN105360131A (zh) 2010-11-03 2016-03-02 陶氏益农公司 杀虫组合物和与其相关的方法
US8609669B2 (en) 2010-11-16 2013-12-17 Abbvie Inc. Potassium channel modulators
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
EP2688872A4 (en) * 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED KINASES
WO2012158399A1 (en) 2011-05-13 2012-11-22 Abbott Laboratories Condensed 2 - carbamoylpyridazinones as potassium channel modulators
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US8614206B2 (en) 2011-09-27 2013-12-24 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
CA2852688C (en) 2011-10-26 2021-06-29 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
WO2013086229A1 (en) 2011-12-07 2013-06-13 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
US9708288B2 (en) 2012-04-27 2017-07-18 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
US9282739B2 (en) 2012-04-27 2016-03-15 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
JP2015528435A (ja) * 2012-08-10 2015-09-28 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾールカルボキサミド化合物、組成物及び使用方法
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
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
WO2014089379A1 (en) 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2014118388A1 (en) 2013-02-04 2014-08-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
CN105189509B (zh) 2013-03-06 2017-12-19 因赛特公司 用于制备jak抑制剂的方法及中间体
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2970288A1 (en) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2970289A1 (en) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
MX389256B (es) 2013-10-04 2025-03-20 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
MX2016004942A (es) 2013-10-17 2016-06-28 Dow Agrosciences Llc Procesos para la preparacion de compuestos plaguicidas.
CA2925952A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
KR20160074540A (ko) 2013-10-17 2016-06-28 다우 아그로사이언시즈 엘엘씨 살충성 화합물의 제조 방법
CN105636445B (zh) 2013-10-17 2018-12-07 美国陶氏益农公司 制备杀虫化合物的方法
CA2925873A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
JP2016536295A (ja) 2013-10-17 2016-11-24 ダウ アグロサイエンシィズ エルエルシー 有害生物防除性化合物の製造方法
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
JP2016534076A (ja) 2013-10-22 2016-11-04 ダウ アグロサイエンシィズ エルエルシー 相乗的有害生物防除組成物および関連する方法
WO2015061146A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
KR102275655B1 (ko) 2013-10-22 2021-07-09 코르테바 애그리사이언스 엘엘씨 살충 조성물 및 관련 방법
CA2927220A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
NZ719776A (en) 2013-10-22 2017-06-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
CA2926433A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Pesticidal compositions and related methods
WO2015061163A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Pesticidal compositions and related methods
MX2016005310A (es) 2013-10-22 2016-08-08 Dow Agrosciences Llc Composiciones pesticidas sinergicas y metodos relacionados.
AR098091A1 (es) 2013-10-22 2016-05-04 Dow Agrosciences Llc Composiciones pesticidas sinérgicas y métodos relacionados
AU2014340416B2 (en) 2013-10-22 2017-09-07 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
KR102286233B1 (ko) 2013-10-22 2021-08-06 코르테바 애그리사이언스 엘엘씨 살충 조성물 및 관련 방법
AR098097A1 (es) 2013-10-22 2016-05-04 Dow Agrosciences Llc Composiciones plaguicidas sinérgicas y métodos relacionados
WO2015061165A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Pesticidal compositions and related methods
CN105828612A (zh) 2013-10-22 2016-08-03 美国陶氏益农公司 协同杀虫组合物和相关方法
US9549560B2 (en) 2013-10-22 2017-01-24 Dow Agrosciences Llc Pesticidal compositions and related methods
WO2015061148A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
CA2926345A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
EP3066094B1 (en) * 2013-11-08 2020-01-08 Takeda Pharmaceutical Company Limited Pyrazole for the treatment autoimmune disorders
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
WO2015083028A1 (en) 2013-12-05 2015-06-11 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
JP2016540773A (ja) * 2013-12-06 2016-12-28 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な化合物
WO2015085132A1 (en) * 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
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
EP4066834A1 (en) 2014-03-19 2022-10-05 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
KR20240153401A (ko) * 2014-04-08 2024-10-22 인사이트 홀딩스 코포레이션 Ｊａｋ 및 ｐｉ3ｋ 억제제 조합에 의한 ｂ-세포 악성종양의 치료
PE20211782A1 (es) 2014-05-23 2021-09-08 Hoffmann La Roche Compuestos de 5-cloro-2-difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
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
HRP20200186T1 (hr) 2014-06-05 2020-05-29 Vertex Pharmaceuticals Inc. Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici
JP6936007B2 (ja) 2014-06-17 2021-09-15 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｃｈｋ１阻害剤とａｔｒ阻害剤との組み合わせを使用してがんを処置する方法
EP3186229A4 (en) 2014-07-31 2018-01-10 Dow AgroSciences LLC Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine
AR098108A1 (es) 2014-07-31 2016-05-04 Dow Agrosciences Llc Proceso para la preparación de 3-(3-cloro-1h-pirazol-1-il)piridina
JP2017523163A (ja) 2014-07-31 2017-08-17 ダウ アグロサイエンシィズ エルエルシー ３−（３−クロロ−１ｈ−ピラゾール−１−イル）ピリジンの製造方法
CN107074774A (zh) 2014-08-19 2017-08-18 美国陶氏益农公司 制备3‑(3‑氯‑1h‑吡唑‑1‑基)吡啶的方法
WO2016039781A1 (en) 2014-09-12 2016-03-17 Dow Agrosciences Llc Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2016202898A1 (en) * 2015-06-19 2016-12-22 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
CN108349985A (zh) 2015-09-14 2018-07-31 无限药品股份有限公司 异喹啉酮的固体形式、其制备方法、包含其的组合物及其使用方法
EP3355926B1 (en) 2015-09-30 2025-12-24 Vertex Pharmaceuticals Inc. Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using
NZ742200A (en) 2015-11-06 2023-01-27 Samumed Llc Treatment of osteoarthritis
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
EP3416967B1 (en) * 2016-02-18 2022-02-09 F. Hoffmann-La Roche AG Therapeutic compounds, compositions and methods of use thereof
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
SI3464285T1 (sl) 2016-06-01 2023-02-28 Biosplice Therapeutics, Inc. Postopek za pripravo N-(5-(3-(7-(3-fluorofenil)-3H-imidazo(4,5-C)piridin-2-il)-1H-indazol-5- il)piridin-3-il)-3-metilbutanamida
WO2017214269A1 (en) 2016-06-08 2017-12-14 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
CR20190310A (es) * 2016-12-29 2019-08-21 Hoffmann La Roche Compuestos de pirazolopirimidina y métodos de uso de los mismos
CN110139853B (zh) 2016-12-29 2023-06-16 美国陶氏益农公司 用于制备杀有害生物化合物的方法
CN110325036B (zh) 2016-12-29 2021-10-26 美国陶氏益农公司 用于制备杀虫化合物的方法
SMT202300051T1 (it) * 2017-01-17 2023-03-17 Astrazeneca Ab Inibitori selettivi di jak1
JP2020510061A (ja) * 2017-03-14 2020-04-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾロクロロフェニル化合物、組成物及びその使用方法
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
EP3610264A1 (en) 2017-04-13 2020-02-19 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
RU2769696C2 (ru) * 2017-05-22 2022-04-05 Ф. Хоффманн-Ля Рош Аг Терапевтические соединения и композиции и способы их применения
EP3630767A1 (en) * 2017-05-22 2020-04-08 H. Hoffnabb-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
CA3070010A1 (en) 2017-07-18 2019-01-24 Bayer Cropscience Aktiengesellschaft Substituted 3-heteroaryloxy-1h-pyrazoles and salts thereof and their use as herbicidal active substances
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
EP3740488A1 (en) * 2018-01-15 2020-11-25 F. Hoffmann-La Roche AG Pyrazolopyrimidine compounds as jak inhibitors
SG11202006453SA (en) * 2018-01-17 2020-08-28 Glaxosmithkline Ip Dev Ltd Pi4kiiibeta inhibitors
EP3746429B1 (en) 2018-01-30 2022-03-09 Incyte Corporation Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-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
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
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
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
CN114008050B (zh) * 2019-06-18 2024-12-31 豪夫迈·罗氏有限公司 Jak激酶的吡唑并嘧啶芳基醚抑制剂及其用途
PE20220577A1 (es) 2019-06-18 2022-04-20 Hoffmann La Roche Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos
TW202115069A (zh) 2019-06-18 2021-04-16 瑞士商赫孚孟拉羅股份公司 Ｊａｋ激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
JP2022551649A (ja) 2019-10-10 2022-12-12 インサイト・コーポレイション 移植片対宿主病のバイオマーカー
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
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
CA3177830A1 (en) 2020-05-13 2021-11-18 Maria BECONI Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
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

Family Cites Families (60)

* 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
NZ516260A (en) 1999-07-02 2004-08-27 Eisai Co Ltd Fused imidazole compounds and remedies for diabetes mellitus
PT1382339E (pt) * 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
US7662826B2 (en) 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
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
JP2006512313A (ja) 2002-10-31 2006-04-13 アムジェン インコーポレイテッド 抗炎症剤
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
US20070270408A1 (en) 2003-04-11 2007-11-22 Novo Nordisk A/S Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
WO2004089471A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
SE0301372D0 (sv) * 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
EP1643960A2 (en) * 2003-07-02 2006-04-12 Merck & Co., Inc. Arylsulfonamide derivatives
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
NZ584499A (en) * 2004-03-30 2011-08-26 Vertex Pharma Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
WO2005110477A2 (en) 2004-04-09 2005-11-24 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
US20050288502A1 (en) 2004-06-25 2005-12-29 Andersen Denise L Substituted heterocyclic compounds and methods of use
EP1812440B1 (en) 2004-11-04 2010-09-22 Vertex Pharmaceuticals, Inc. Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
EP1910369A1 (en) 2005-07-29 2008-04-16 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
AR057979A1 (es) 2005-10-06 2008-01-09 Schering Corp PIRAZOLPIRIMIDINAS COMO INHIBIDORAS DE PROTEíNA QUINASA. COMPOSICIONES FARMACEUTICAS.
US7776865B2 (en) * 2005-10-06 2010-08-17 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
JP5119157B2 (ja) 2005-10-21 2013-01-16 エクセリクシス， インク． カゼインキナーゼｉｉ（ｃｋ２）モジュレーターとしてのピラゾロ−ピリミジン類
AU2006322187A1 (en) 2005-12-08 2007-06-14 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
CN101460499A (zh) * 2006-04-05 2009-06-17 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的去氮杂嘌呤
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
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
JP2010508315A (ja) 2006-10-30 2010-03-18 ノバルティス アーゲー 抗炎症剤としてのヘテロ環式化合物
CA2670083A1 (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
CA2702008A1 (en) * 2007-10-12 2009-04-16 Ingenium Pharmaceuticals Gmbh Inhibitors of protein kinases
MX2010005671A (es) 2007-11-28 2010-06-25 Dana Farber Cancer Inst Inc Inhibidores de miristato de moleculas pequeñas contra bcr-abl y metodos de uso.
US8642660B2 (en) * 2007-12-21 2014-02-04 The 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
RU2539568C2 (ru) * 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
WO2010063487A1 (en) 2008-12-05 2010-06-10 Merz Pharma Gmbh & Co. Kgaa Pyrazolopyrimidines, a process for their preparation and their use as medicine
WO2010089292A1 (en) 2009-02-06 2010-08-12 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators
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
AU2010309882B2 (en) 2009-10-20 2016-01-28 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors
US20130096104A1 (en) 2010-03-17 2013-04-18 Genentech, Inc. Imidazopyridine compounds, compositions and methods of use
EP2566867A1 (en) 2010-04-30 2013-03-13 Cellzome Limited Pyrazole compounds as jak inhibitors

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