PE20131197A1 - Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen - Google Patents

Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen

Info

Publication number
PE20131197A1
PE20131197A1 PE2013000399A PE2013000399A PE20131197A1 PE 20131197 A1 PE20131197 A1 PE 20131197A1 PE 2013000399 A PE2013000399 A PE 2013000399A PE 2013000399 A PE2013000399 A PE 2013000399A PE 20131197 A1 PE20131197 A1 PE 20131197A1
Authority
PE
Peru
Prior art keywords
pharmaceutical compositions
compositions containing
alkenyl
jak inhibitors
pyrazolopyrimidine compounds
Prior art date
Application number
PE2013000399A
Other languages
English (en)
Inventor
Jeffrey Blaney
Paul A Gibbons
Emily Hanan
Joseph P Lyssikatos
Steven R Magnuson
Richard Pastor
Thomas E Rawson
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42129330&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20131197(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of PE20131197A1 publication Critical patent/PE20131197A1/es

Links

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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRAZOLOPIRIMIDINA DE FORMULA Ia DONDE: R1 ES H; R2 ES -OR4, -NR3R4, -NR3S(O)R4, ENTRE OTROS, EN DONDE R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R4 ES H, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R3 Y R4 SE TOMAN JUNTOS CON EL NITROGENO AL CUAL ESTAN UNIDOS PARA FORMAR UN HETEROCICLILO OPCIONALMENTE SUSTITUIDO; Z ES -OR6 O -NR5R6, EN DONDE R5 ES H O ALQUILO C1-C3; R6 ES H, ALQUENILO C2-C10, ENTRE OTROS OPCIONALMENTE SUSTITUIDOS; R7 ES H O HALOGENO. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE JAK QUINASAS SIENDO UTILES PARA EL TRATAMIENTO DE PSORIASIS, DIABETES, ATEROESCLEROSIS, TRASTORNOS NEUROLOGICOS
PE2013000399A 2008-10-31 2009-11-02 Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen PE20131197A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11049708P 2008-10-31 2008-10-31

Publications (1)

Publication Number Publication Date
PE20131197A1 true PE20131197A1 (es) 2013-11-06

Family

ID=42129330

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2013000399A PE20131197A1 (es) 2008-10-31 2009-11-02 Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen
PE2011000946A PE20110828A1 (es) 2008-10-31 2009-11-02 Compuestos de pirazolopirimidina como inhibidores de jak

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2011000946A PE20110828A1 (es) 2008-10-31 2009-11-02 Compuestos de pirazolopirimidina como inhibidores de jak

Country Status (20)

Country Link
US (3) US8637526B2 (es)
EP (2) EP2962566A1 (es)
JP (1) JP5769199B2 (es)
KR (1) KR101686685B1 (es)
CN (1) CN102271515B (es)
AU (1) AU2009308675A1 (es)
BR (1) BRPI0914404A2 (es)
CA (1) CA2740792C (es)
CL (1) CL2011000973A1 (es)
CO (1) CO6361856A2 (es)
CR (1) CR20110224A (es)
EC (1) ECSP11011014A (es)
ES (1) ES2545541T3 (es)
HK (1) HK1161529A1 (es)
IL (1) IL212085A0 (es)
MX (1) MX2011004494A (es)
PE (2) PE20131197A1 (es)
RU (1) RU2539568C2 (es)
SG (1) SG194397A1 (es)
WO (1) WO2010051549A1 (es)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
EP3372605B1 (en) 2008-10-22 2021-11-03 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors
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
EP2475659B1 (en) 2009-09-08 2015-10-28 F.Hoffmann-La Roche Ag 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
RU2594742C2 (ru) 2010-05-20 2016-08-20 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
MX358682B (es) * 2010-07-13 2018-08-31 Hoffmann La Roche Derivados de pirazolo [1,5a]pirimidina y de tieno[3,2b] pirimidina como moduladores de la cinasa asociada al receptor de la interleucina 4 (irak4).
BR112013002212A2 (pt) 2010-07-29 2017-09-26 Merck Patent Gmbh carboxamidas aza-heterocíclicas de aminas cíclicas
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
PT3808749T (pt) 2012-12-07 2023-06-07 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis como inibidores da quinase atr para o tratamento de doenças de cancro
US20160123982A1 (en) 2013-02-04 2016-05-05 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
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
WO2014143241A1 (en) * 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2980089B1 (en) * 2013-03-28 2017-12-20 Takeda Pharmaceutical Company Limited Heterocyclic compound
HUE031980T2 (en) 2013-04-25 2017-08-28 Beigene Ltd Condensed heterocyclic compounds as protein kinase inhibitors
HUE049281T2 (hu) 2013-09-13 2020-09-28 Beigene Switzerland Gmbh Anti-PD1 antitestek, valamint terapeutikumként és diagnosztikumként történõ alkalmazásuk
CN103539753B (zh) * 2013-10-22 2017-06-23 上海药明康德新药开发有限公司 一种3‑取代‑4‑异恶唑羧酸的合成方法
WO2015073267A1 (en) * 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
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
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
CA2936079C (en) 2014-01-24 2022-07-19 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
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
NZ764151A (en) 2014-06-05 2023-12-22 Vertex Pharma 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
RU2736219C2 (ru) 2014-06-17 2020-11-12 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации ингибиторов снк1 и atr
WO2016000619A1 (en) 2014-07-03 2016-01-07 Beigene, Ltd. Anti-pd-l1 antibodies and their use as therapeutics and diagnostics
GB201414730D0 (en) 2014-08-19 2014-10-01 Tpp Global Dev Ltd Pharmaceutical compound
CA2966581A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
CN115925711A (zh) * 2014-11-06 2023-04-07 Bial研发投资股份有限公司 取代的吡唑并[1,5-a]嘧啶以及它们在治疗医学障碍中的用途
LT3699181T (lt) 2014-11-16 2023-05-10 Array Biopharma, Inc. Kristalinė (s)-n-(5-((r)-2-(2,5-difluorfenil)-pirolidin-1-il)-pirazolo[1,5-a] pirimidin-3-il)-3 -hidroksipirolidino-1-karboksamido vandenilio sulfato forma
US10329294B2 (en) 2015-03-12 2019-06-25 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of IRAK4 activity
EP3268367B8 (en) * 2015-03-12 2022-11-16 Merck Sharp & Dohme LLC Carboxamide inhibitors of irak4 activity
WO2017004342A1 (en) 2015-07-02 2017-01-05 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
JP6917974B2 (ja) 2015-07-06 2021-08-11 ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． ジアリール大環状多形
DK3325488T3 (da) 2015-07-21 2020-09-14 Turning Point Therapeutics Inc Chiral diaryl-makrocyklus og anvendelse deraf til behandling af cancer
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
EP3156405A1 (en) * 2015-10-13 2017-04-19 Boehringer Ingelheim International GmbH Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
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
CN105503730B (zh) * 2015-12-25 2018-06-22 山东大学 吡唑类衍生物及其制备方法与应用
MA44610A (fr) 2016-04-04 2019-02-13 Loxo Oncology Inc Formulations liquides de (s)-n-(5-((r)-2-(2,5-difluorophényl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CN109311887B (zh) 2016-04-06 2022-09-13 Bial研发投资股份有限公司 吡唑并[1,5-a]嘧啶基甲酰胺化合物以及它们在治疗医学病症中的用途
MX2018012208A (es) 2016-04-06 2019-03-28 Lysosomal Therapeutics Inc Compuestos a base de imidazo [1,5-a] pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos.
WO2017176962A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics, Inc. Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
EP3452045A1 (en) * 2016-05-04 2019-03-13 Lysosomal Therapeutics Inc. Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds
EP3452481A4 (en) 2016-05-05 2020-02-26 Lysosomal Therapeutics Inc. IMIDAZO [1,2-B] SUBSTITUTED PYRIDAZINES, IMIDAZO [1,5-B] SUBSTITUTED PYRIDAZINES, RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL CONDITIONS
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders
HUE053643T2 (hu) 2016-05-18 2021-07-28 Loxo Oncology Inc (S)-N-(5 -((R)-2-(2,5-difluor-fenil)-pirrolidin-1-il)-pirazolo[1,5-A] pirimidin-3-il)-3-hidroxi-pirrolidin-1-karboxamid elõkészítése
EP3481393B1 (en) 2016-07-05 2021-04-14 Beigene, Ltd. Combination of a pd-1 antagonist and a raf inhibitor for treating cancer
BR112019001607A2 (pt) 2016-07-28 2019-04-30 Tp Therapeutics, Inc. inibidores macrocíclicos de quinases
TW202233628A (zh) 2016-08-16 2022-09-01 英屬開曼群島商百濟神州有限公司 (s)-7-(1-丙烯醯基六氫吡啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑並[1,5-a]嘧啶-3-甲醯胺的晶型、其製備和用途
FI3500299T3 (fi) 2016-08-19 2024-02-14 Beigene Switzerland Gmbh Tsanubrutinibin yhdistelmä cd20-tai pd-1-vasta-aineen kanssa käytettäväksi syövän hoidossa
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
US11555038B2 (en) 2017-01-25 2023-01-17 Beigene, Ltd. Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
WO2018166993A2 (en) * 2017-03-14 2018-09-20 F. Hoffmann-La Roche Ag Pyrazolochlorophenyl compounds, compositions and methods of use thereof
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
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
BR112019024322A2 (pt) * 2017-05-22 2020-06-16 F. Hoffmann-La Roche Ag Compostos e composições terapêuticos e métodos de uso dos mesmos
WO2018215390A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
US11597768B2 (en) 2017-06-26 2023-03-07 Beigene, Ltd. Immunotherapy for hepatocellular carcinoma
UA126158C2 (uk) 2017-07-28 2022-08-25 Тьорнінґ Поінт Терапьютикс, Інк. Макроциклічні сполуки і їх використання
WO2019023468A1 (en) 2017-07-28 2019-01-31 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
EA202091475A1 (ru) 2017-12-15 2020-09-09 Пирамид Байосайенсиз, Инк. ПРОИЗВОДНЫЕ 5-(2-(2,5-ДИФТОРФЕНИЛ)ПИРРОЛИДИН-1-ИЛ)-3-(1H-ПИРАЗОЛ-1-ИЛ)ПИРАЗОЛО[1,5-а]ПИРИМИДИНА И РОДСТВЕННЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Trk КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ РАКА
JOP20200152A1 (ar) 2017-12-19 2022-10-30 Turning Point Therapeutics Inc مركبات حلقية كبرى لعلاج مرض
ES2938751T3 (es) 2018-09-10 2023-04-14 Lilly Co Eli Derivados de pirazol[1,5-a]pirimidina-3-carboxamida útiles en el tratamiento de la psoriasis y el lupus eritematoso sistémico
CA3115088A1 (en) 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN109251205A (zh) * 2018-10-22 2019-01-22 上海凌凯医药科技有限公司 一种高效合成5-氯吡唑并[1,5-a]嘧啶的方法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
CN111217816B (zh) * 2018-11-27 2022-08-16 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
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
JP2022537354A (ja) 2019-06-18 2022-08-25 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
MA56518A (fr) * 2019-06-18 2022-04-27 Hoffmann La Roche Inhibiteurs de sulfone pyrazolopyrimidine de jak kinases et leurs utilisations
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TWI810520B (zh) 2020-02-12 2023-08-01 美商美國禮來大藥廠 7-(甲基胺基)吡唑并[1,5-a]嘧啶-3-甲醯胺化合物
CN113387831A (zh) * 2020-03-11 2021-09-14 苏州大学 酰胺类化合物及其在制备神经炎症抑制剂中的应用
CN113549073B (zh) * 2020-04-24 2022-07-12 成都先导药物开发股份有限公司 作为JAK抑制剂的吡唑并[1,5-a]嘧啶衍生物
WO2023057394A1 (en) * 2021-10-04 2023-04-13 Forx Therapeutics Ag N,n-dimethyl-4-(7-(n-(1-methylcyclopropyl)sulfamoyl)-imidazo[1,5-a]pyridin-5-yl)piperazine-1-carboxamide derivatives and the corresponding pyrazolo[1,5-a]pyridine derivatives as parg inhibitors for the treatment of cancer
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4187099A (en) 1977-11-16 1980-02-05 Monsanto Company 3-Aryl-4-isothiazolecarboxylic acid and 3-aryl-4-isoxazolecarboxylic acid derivatives and their use as herbicides
ES517193A0 (es) 1981-11-10 1983-12-01 Wellcome Found Un procedimiento para la preparacion de nuevos derivados de imidazo (4,5-c)piridina.
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
US6841549B1 (en) 1999-07-02 2005-01-11 Eisai Co., Ltd. Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
NZ518884A (en) 1999-12-10 2004-02-27 Pfizer Prod Inc Pyrrolo[2,3-d]pyrimidine compounds
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
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
WO2004041285A1 (en) 2002-10-31 2004-05-21 Amgen Inc. Antiinflammation agents
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And 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
EP1615697A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof
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
US20060030536A1 (en) 2004-04-09 2006-02-09 University Of South Florida Combination therapies for cancer and proliferative angiopathies
US7517888B2 (en) 2004-04-28 2009-04-14 Cv Therapeutics, Inc. A1 adenosine receptor antagonists
NZ551660A (en) * 2004-06-21 2009-08-28 Hoffmann La Roche Pyrrazolo-pyrimidine derivatives and their use in diseases or conditions where mGluR2 activation plays a role
US20050288502A1 (en) 2004-06-25 2005-12-29 Andersen Denise L Substituted heterocyclic compounds and methods of use
US7528138B2 (en) * 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
US20100216798A1 (en) * 2005-07-29 2010-08-26 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
JP5152922B2 (ja) * 2005-10-06 2013-02-27 メルク・シャープ・アンド・ドーム・コーポレーション プロテインキナーゼを阻害するためのピラゾロ［１，５−ａ］ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法
US7645762B2 (en) 2005-10-06 2010-01-12 Schering Corporation Substituted pyrazolo[1,5-a] pyrimidines as protein kinase inhibitors
JP5376950B2 (ja) 2005-10-21 2013-12-25 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リミジオン類
EP1963316A2 (en) 2005-12-08 2008-09-03 Novartis AG Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
US7274215B2 (en) * 2006-01-17 2007-09-25 M2000 Sa. Reconfigurable integrated circuits with scalable architecture including one or more adders
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
TW201345908A (zh) * 2006-07-05 2013-11-16 Mitsubishi Tanabe Pharma Corp 吡唑并〔１，５-ａ〕嘧啶化合物
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
RU2009120389A (ru) 2006-10-30 2010-12-10 Новартис АГ (CH) Гетероциклические соединения в качестве противовоспалительных агентов
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
CN101889004B (zh) 2007-10-12 2014-09-10 阿斯利康公司 蛋白激酶抑制剂
AU2008331867B2 (en) 2007-11-28 2014-05-22 Dana-Farber Cancer Institute, Inc. Small molecule myristate inhibitors of Bcr-abl and methods of use
US8642660B2 (en) 2007-12-21 2014-02-04 The 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
WO2010063487A1 (en) * 2008-12-05 2010-06-10 Merz Pharma Gmbh & Co. Kgaa Pyrazolopyrimidines, a process for their preparation and their use as medicine
AP2011005779A0 (en) 2009-02-06 2011-08-31 Ortho Mcneil Janssen Pharm Novel susbstituted bicyclic heterocyclic compoundsas 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
DE102009012264A1 (de) * 2009-03-11 2010-09-16 Uhde Gmbh Vorrichtung und Verfahren zur Dosierung oder Absperrung primärer Verbrennungsluft in den Primärheizraum von horizontalen Koksofenkammern
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
EP2491039A1 (en) 2009-10-20 2012-08-29 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors
MX2012010265A (es) 2010-03-17 2012-10-01 Hoffmann La Roche Compuestos de imidazopiridina, composiciones y metodos de uso.
KR20130094693A (ko) 2010-04-30 2013-08-26 셀좀 리미티드 Ｊａｋ 저해제로서의 피라졸 화합물

Also Published As

Publication number Publication date
RU2011121876A (ru) 2012-12-20
IL212085A0 (en) 2011-06-30
EP2348860A4 (en) 2012-10-24
MX2011004494A (es) 2011-05-24
ECSP11011014A (es) 2011-05-31
KR20110079887A (ko) 2011-07-11
JP2012507569A (ja) 2012-03-29
RU2539568C2 (ru) 2015-01-20
CN102271515A (zh) 2011-12-07
US8637526B2 (en) 2014-01-28
SG194397A1 (en) 2013-11-29
US20120022043A1 (en) 2012-01-26
CO6361856A2 (es) 2012-01-20
EP2962566A1 (en) 2016-01-06
CA2740792C (en) 2016-06-21
CL2011000973A1 (es) 2012-07-20
KR101686685B1 (ko) 2016-12-14
HK1161529A1 (en) 2012-07-27
US20140107099A1 (en) 2014-04-17
CA2740792A1 (en) 2010-05-06
WO2010051549A1 (en) 2010-05-06
JP5769199B2 (ja) 2015-08-26
CR20110224A (es) 2011-06-09
CN102271515B (zh) 2014-07-02
PE20110828A1 (es) 2011-11-22
AU2009308675A1 (en) 2010-05-06
BRPI0914404A2 (pt) 2019-03-06
EP2348860A1 (en) 2011-08-03
EP2348860B1 (en) 2015-05-27
ES2545541T3 (es) 2015-09-11
US20160244456A1 (en) 2016-08-25

Similar Documents

Publication Publication Date Title
PE20131197A1 (es) Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen
ECSP11010830A (es) Derivados de heteroarilo como inhibidores de dgat1
NI201000198A (es) Compuestos triazina como inhibidores mtor y quinasa p13.
ECSP11010885A (es) Heteroarilos sustituidos
CR20110028A (es) Derivados de pirimidina como inhibidores de cinasa
AR070221A1 (es) Derivados de ftalazinona inhibidores de polimerasas, composiciones farmaceuticas que los contienen y usos de los mismos para prevenir y/o tratar tumores cancerigenos,lesiones isquemicas y otras enfermedades asociadas.
PE20121048A1 (es) Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17
PE20121159A1 (es) DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTOR
PE20141203A1 (es) Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
PE20140975A1 (es) Derivados de imidazopirazina como inhibidores de syk
PE20091734A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
UY37440A (es) Compuestos inhibidores de la prostaglandina d sintasa hematopoyética (h-pgds)
CU20110030A7 (es) Compuestos orgánicos
AR072016A1 (es) Derivados de isoxazol que funcionan como potenciadores de los receptores de glutamato
PE20170333A1 (es) Compuestos de isoindolinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados
NI201000011A (es) Derivados de pirimidina 934.
PE20080068A1 (es) Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
PE20091419A1 (es) Derivados acidos de carboxicicloalquilamino como moduladores de los receptores de esfingosina-1-fosfato (s1p)
PE20151748A1 (es) Inhibidores de bace1
PE20170083A1 (es) Nuevos compuestos
CO6430428A2 (es) Composiciones, síntesis, y métodos de utilización de derivados de arilopiperazina
CO6362013A2 (es) Derivados de rifamicina
AR072198A1 (es) Derivados de isoquinolinona como antagonistas de nk3 y composiciones farmaceuticas que los contienen
DK1723140T3 (da) Fremgangsmåde til fremstilling af tryptase-inhibitorer

Legal Events

Date Code Title Description
FD Application declared void or lapsed