CO6491081A2 - Compuestosy metodos inhibidores de jak de pirazolopirimidina - Google Patents

Compuestosy metodos inhibidores de jak de pirazolopirimidina

Info

Publication number
CO6491081A2
CO6491081A2 CO12011326A CO12011326A CO6491081A2 CO 6491081 A2 CO6491081 A2 CO 6491081A2 CO 12011326 A CO12011326 A CO 12011326A CO 12011326 A CO12011326 A CO 12011326A CO 6491081 A2 CO6491081 A2 CO 6491081A2
Authority
CO
Colombia
Prior art keywords
pirazolopirimidina
jak
compounds
compound
methods
Prior art date
Application number
CO12011326A
Other languages
English (en)
Inventor
Paul A Gibbons
Emily Hanan
Wendy Liu
P Lyssikatos Joseph
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 CO6491081A2 publication Critical patent/CO6491081A2/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, enantiámeros, diasteriomeros, 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.
CO12011326A 2009-07-02 2012-01-25 Compuestosy metodos inhibidores de jak de pirazolopirimidina CO6491081A2 (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
CO6491081A2 true CO6491081A2 (es) 2012-07-31

Family

ID=43411778

Family Applications (1)

Application Number Title Priority Date Filing Date
CO12011326A CO6491081A2 (es) 2009-07-02 2012-01-25 Compuestosy metodos inhibidores de jak de pirazolopirimidina

Country Status (35)

Country Link
US (6) US8999998B2 (es)
EP (3) EP3333169B1 (es)
JP (4) JP5769261B2 (es)
KR (3) KR101825754B1 (es)
CN (2) CN104910161B (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) NZ622283A (es)
PE (2) PE20120575A1 (es)
PH (1) PH12015500666A1 (es)
PL (1) PL2448941T3 (es)
PT (1) PT2448941T (es)
RS (1) RS56671B1 (es)
RU (2) RU2567238C2 (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 (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS54181B9 (sr) 2005-12-13 2020-01-31 Incyte Holdings Corp Heteroaril supstituisani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
MY154969A (en) 2007-06-13 2015-08-28 Incyte Corp Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CA2740792C (en) 2008-10-31 2016-06-21 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
MX2011012262A (es) 2009-05-22 2012-01-25 Incyte Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il] octano-o heptano-nitrilo como inhibidores de cinasas janus (jak).
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
KR102283091B1 (ko) 2010-03-10 2021-07-30 인사이트 홀딩스 코포레이션 Ｊａｋ１ 저해제로서의 피페리딘­４­일 아제티딘 유도체
MA34234B1 (fr) 2010-04-07 2013-05-02 Hoffmann La Roche Composes pyrazol-4-yl-heterocyclyle-carboxamide et leurs procedes d'utilisation
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Ｊａｋ抑制劑的局部製劑
CN105367577B (zh) * 2010-07-13 2019-04-23 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
MA34804B1 (fr) 2010-11-03 2014-01-02 Dow Agrosciences Llc Compositions pesticides et procedes apparentes
WO2012067822A1 (en) * 2010-11-16 2012-05-24 Abbott Laboratories Pyrazolo [1, 5 -a] pyrimidin potassium channel modulators
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
WO2012158399A1 (en) 2011-05-13 2012-11-22 Abbott Laboratories Condensed 2 - carbamoylpyridazinones as potassium channel modulators
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
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
SG2014012579A (en) 2011-09-27 2014-04-28 Hoffmann La Roche Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
AU2012314376B2 (en) 2011-09-30 2017-04-06 Oncodesign S.A. Macrocyclic FLT3 kinase inhibitors
CN104010505B (zh) 2011-10-26 2017-03-15 陶氏益农公司 杀虫组合物和与其相关的方法
EP2788332A1 (en) 2011-12-07 2014-10-15 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
MA37572B1 (fr) 2012-04-27 2017-10-31 Dow Agrosciences Llc Compositions pesticides et procédés correspondants
US9282739B2 (en) 2012-04-27 2016-03-15 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
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
WO2014064134A1 (en) * 2012-10-26 2014-05-01 F. Hoffmann-La Roche Ag 3,4-disubstituted 1 h-pyrazole and 4,5-disubstituted thiazole inhibitors of syk
KR20210037012A (ko) 2012-11-15 2021-04-05 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
NZ731337A (en) 2012-12-07 2019-02-22 Vertex Pharma 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
NZ711976A (en) 2013-03-06 2019-01-25 Incyte Holdings Corp 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
JP2016512815A (ja) * 2013-03-15 2016-05-09 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縮合ピラゾロピリミジン誘導体
SG10201801069QA (en) * 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
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
JP6487426B2 (ja) 2013-10-17 2019-03-20 ダウ アグロサイエンシィズ エルエルシー 有害生物防除化合物の調製法
JP2016535008A (ja) 2013-10-17 2016-11-10 ダウ アグロサイエンシィズ エルエルシー 有害生物防除化合物の調製法
CA2925954A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
KR20160072155A (ko) 2013-10-17 2016-06-22 다우 아그로사이언시즈 엘엘씨 살충성 화합물의 제조 방법
WO2015058020A1 (en) 2013-10-17 2015-04-23 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
JP2016539092A (ja) 2013-10-17 2016-12-15 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
AU2014340424B2 (en) 2013-10-22 2017-06-29 Dow Agrosciences Llc Pesticidal compositions and related methods
WO2015061170A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
JP2016536307A (ja) 2013-10-22 2016-11-24 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
WO2015061151A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Pesticidal compositions and related methods
AU2014340430B2 (en) 2013-10-22 2017-05-25 Dow Agrosciences Llc Pesticidal compositions and related methods
RU2016119368A (ru) 2013-10-22 2017-11-28 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи Синергетические пестицидные композиции и связанные с ними способы
WO2015061145A1 (en) 2013-10-22 2015-04-30 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
MX2016005319A (es) 2013-10-22 2016-08-12 Dow Agrosciences Llc Composiciones pesticidas y metodos relacionados.
US9149040B2 (en) 2013-10-22 2015-10-06 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
TW201517797A (zh) 2013-10-22 2015-05-16 Dow Agrosciences Llc 協同性殺蟲組成物及相關方法（十一）
MX2016005310A (es) 2013-10-22 2016-08-08 Dow Agrosciences Llc Composiciones pesticidas sinergicas y metodos relacionados.
RU2016119566A (ru) 2013-10-22 2017-11-28 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи Синергетические пестицидные композиции и относящиеся к ним способы
MX2016005324A (es) 2013-10-22 2016-08-12 Dow Agrosciences Llc Composiciones pesticidas y metodos relacionados.
US9801383B2 (en) 2013-10-22 2017-10-31 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
JP2016534086A (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
US9801376B2 (en) 2013-10-22 2017-10-31 Dow Agrosciences Llc Synergistic pesticidal compositions and related methods
CA2929316C (en) * 2013-11-08 2021-12-28 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
WO2015084384A1 (en) * 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
KR102153886B1 (ko) * 2013-12-06 2020-09-09 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제 억제제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물, 이의 제조 방법, 이의 상이한 고체형 및 방사성표지된 유도체
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
CN106456628A (zh) 2014-03-19 2017-02-22 无限药品股份有限公司 用于治疗PI3K‑γ介导的障碍的杂环化合物
US9493439B1 (en) 2014-04-07 2016-11-15 University Of Kentucky Research Foundation Proteasome inhibitors
EA201692011A1 (ru) * 2014-04-08 2017-01-30 Инсайт Корпорейшн Лечение b-клеточных злокачественных новообразований с применением комбинации ингибиторов jak и pi3k
JP2017516850A (ja) * 2014-05-23 2017-06-22 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｊａｋ阻害剤である５−クロロ−２−ジフルオロメトキシフェニルピラゾロピリミジン化合物
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
CN110590787A (zh) 2014-06-05 2019-12-20 沃泰克斯药物股份有限公司 Atr激酶抑制剂的制备方法及其不同的固体形式
RS59054B1 (sr) 2014-06-17 2019-08-30 Vertex Pharma Postupak za lečenje raka korišćenjem kombinacije chk1 i atr inhibitora
US9029556B1 (en) 2014-07-31 2015-05-12 Dow Argosciences Llc Process for the preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine
US9029555B1 (en) 2014-07-31 2015-05-12 Dow Agrosciences Llc Process for the preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine
WO2016018444A1 (en) 2014-07-31 2016-02-04 Dow Agrosciences Llc Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine
WO2016028328A1 (en) 2014-08-19 2016-02-25 Dow Agrosciences Llc Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine
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
US11464774B2 (en) 2015-09-30 2022-10-11 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
CA3004506A1 (en) 2015-11-06 2017-05-11 Samumed, Llc Use of n-(5-(3-(7-(3- fluorophenyl)-3h-imidazo[4,5-c]pyridin-2-yl)-1h-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide in the 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
CN108473501B (zh) * 2016-02-18 2021-07-16 豪夫迈·罗氏有限公司 治疗化合物、其组合物及使用方法
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
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
JP6900491B2 (ja) * 2016-12-29 2021-07-07 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾロピリミジン化合物及びその使用方法
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
JP2020503336A (ja) 2016-12-29 2020-01-30 ダウ アグロサイエンシィズ エルエルシー 殺有害生物化合物の調製方法
ES2938648T3 (es) * 2017-01-17 2023-04-13 Astrazeneca Ab Inhibidores selectivos de JAK1
CN110494434B (zh) * 2017-03-14 2022-05-24 豪夫迈·罗氏有限公司 吡唑并氯苯基化合物、其组合物及其使用方法
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
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
KR20200010390A (ko) * 2017-05-22 2020-01-30 에프. 호프만-라 로슈 아게 치료 화합물 및 조성물, 및 이의 사용 방법
CN110678467B (zh) * 2017-05-22 2023-06-13 豪夫迈·罗氏有限公司 治疗化合物和组合物及其使用方法
BR112020000964A2 (pt) 2017-07-18 2020-07-14 Bayer Cropscience Aktiengesellschaft 3-heteroariloxi-1h-pirazóis substituídos e sais dos mesmos e seu uso como substâncias ativas herbicidas
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
CN111587250A (zh) * 2018-01-15 2020-08-25 豪夫迈·罗氏有限公司 作为jak抑制剂的吡唑并嘧啶化合物
CN111868063B (zh) * 2018-01-17 2023-08-01 葛兰素史克知识产权开发有限公司 PI4KIIIβ抑制剂
EP3746429B1 (en) 2018-01-30 2022-03-09 Incyte Corporation Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
WO2019172243A1 (ja) 2018-03-07 2019-09-12 三菱ケミカル株式会社 透明樹脂組成物、樹脂成形体、ランプカバー、車両用ランプカバー、コンビネーションランプカバー及び車両
EA202092343A1 (ru) 2018-03-30 2021-01-20 Инсайт Корпорейшн Лечение гнойного гидраденита с использованием ингибиторов jak
AU2019252259A1 (en) * 2018-04-13 2020-12-03 Incyte Corporation Biomarkers for graft-versus-host disease
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
EP3911317A2 (en) * 2019-01-17 2021-11-24 BioSplice Therapeutics, Inc. Methods of treating cartilage disorders through inhibition of clk and dyrk
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
EP3986899A1 (en) * 2019-06-18 2022-04-27 F. Hoffmann-La Roche AG Pyrazolopyrimidine aryl ether inhibitors of jak kinases and uses thereof
CN114026096A (zh) * 2019-06-18 2022-02-08 豪夫迈·罗氏有限公司 四唑取代的吡唑并嘧啶类jak激酶抑制剂及其用途
AU2020297415A1 (en) 2019-06-18 2022-01-06 F. Hoffmann-La Roche Ag Pyrazolopyrimidine sulfone inhibitors of JAK kinases and uses thereof
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) 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
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
CN115466227A (zh) * 2022-06-30 2022-12-13 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-***盐酸盐的制备方法

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
CA2376835C (en) 1999-07-02 2009-09-15 Eisai Co., Ltd. Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
PT1382339E (pt) * 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
KR20040097375A (ko) 2002-04-23 2004-11-17 시오노기 앤드 컴파니, 리미티드 피라졸로[1, 5-에이]피리미딘 유도체 및 이를 함유한엔에이디(피)에이취 산화효소 저해제
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7161003B1 (en) 2002-09-04 2007-01-09 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
US7199119B2 (en) 2002-10-31 2007-04-03 Amgen Inc. Antiinflammation agents
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
EP1615697A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S New pyrazolo[1,5-a] pyrimidine 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
US7393873B2 (en) * 2003-07-02 2008-07-01 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
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
US7507826B2 (en) * 2004-03-30 2009-03-24 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
CA2563305A1 (en) 2004-04-09 2005-11-24 University Of South Florida Combination therapies for cancer and proliferative angiopathies
CA2565037A1 (en) 2004-04-28 2005-11-10 Cv Therapeutics, Inc. Purine derivatives as a1 adenosine receptor antagonists
JP2008504294A (ja) 2004-06-25 2008-02-14 アムジエン・インコーポレーテツド サイトカイン介在疾患および他の疾患の治療において有用な縮合トリアゾールおよびインダゾール
PT1812440E (pt) 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases
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
AR057979A1 (es) 2005-10-06 2008-01-09 Schering Corp PIRAZOLPIRIMIDINAS COMO INHIBIDORAS DE PROTEíNA QUINASA. COMPOSICIONES FARMACEUTICAS.
KR20080063806A (ko) * 2005-10-06 2008-07-07 쉐링 코포레이션 단백질 키나제 억제제로서의 피라졸로피리미딘
ATE517874T1 (de) 2005-10-21 2011-08-15 Exelixis Inc Pyrimidinone als modulatoren von caseinkinase ii (ck2)
BRPI0619517A2 (pt) 2005-12-08 2011-10-04 Novartis Ag ácidos pirazolo[1,5-a]piridina-3-carboxìlicos como inibidores de ephb e vegfr2 cinase
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
WO2007117494A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
RU2440980C2 (ru) 2006-06-02 2012-01-27 Ниппон Синяку Ко., Лтд. 9,10-секопрегнановое производное и фармацевтические средства
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
CN101522682A (zh) 2006-10-30 2009-09-02 诺瓦提斯公司 作为抗炎剂的杂环化合物
US20080176870A1 (en) 2006-11-20 2008-07-24 Bert Nolte Heterobicyclic metalloprotease inhibitors
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
BRPI0818543A2 (pt) 2007-10-12 2018-10-23 Ingenium Pharmaceuticals Gmbh inibidores de proteína cinase
ES2610190T3 (es) 2007-11-28 2017-04-26 Dana-Farber Cancer Institute, Inc. Inhibidores de miristato de moléculas pequeñas de Bcr-abl y métodos de uso
AU2008345225A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2010019762A1 (en) 2008-08-13 2010-02-18 Jenrin Discovery Purine compounds as cannabinoid receptor blockers
CA2740792C (en) * 2008-10-31 2016-06-21 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
BRPI1008473A2 (pt) 2009-02-06 2019-04-02 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. compostos heterocíclicos bicíclicos substituídos como moduladores de gama secretase
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
CA2793024A1 (en) 2010-03-17 2011-09-22 F. Hoffmann-La Roche Ag Imidazopyridine compounds, compositions and methods of use
WO2011134831A1 (en) 2010-04-30 2011-11-03 Cellzome Limited Pyrazole compounds as jak inhibitors

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