MA38398B1 - Composés biaryle amides en tant qu'inhibiteurs de kinase - Google Patents

Composés biaryle amides en tant qu'inhibiteurs de kinase

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Publication number
MA38398B1
MA38398B1 MA38398A MA38398A MA38398B1 MA 38398 B1 MA38398 B1 MA 38398B1 MA 38398 A MA38398 A MA 38398A MA 38398 A MA38398 A MA 38398A MA 38398 B1 MA38398 B1 MA 38398B1
Authority
MA
Morocco
Prior art keywords
compounds
kinase inhibitors
amide compounds
biaryl amide
biaryl
Prior art date
Application number
MA38398A
Other languages
English (en)
Other versions
MA38398A1 (fr
Inventor
Yan Lou
Matthew Burger
Gisele Nishiguchi
Alice Rico
Benjamin Taft
Huw Tanner
Robert Aversa
Paul A Barsanti
Michael Patrick Dillon
Alan Dipesa
Cheng Hu
Yue Pan
Valery Polyakov
Savithri Ramurthy
Lina Setti
Aaron Smith
Sharadha Subramanian
Lifeng Wan
Naeem Yusuff
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of MA38398A1 publication Critical patent/MA38398A1/fr
Publication of MA38398B1 publication Critical patent/MA38398B1/fr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
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    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
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    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

La présente invention concerne des composés de formule (i) tels que décrits ici, et leurs sels, et des utilisations thérapeutiques de ces composés pour le traitement de troubles associés à l'activité raf kinase. L'invention concerne en outre des compositions pharmaceutiques comprenant ces composés, et des compositions comprenant ces composés et un co-agent thérapeutique.
MA38398A 2013-03-14 2014-03-13 Composés biaryle amides en tant qu'inhibiteurs de kinase MA38398B1 (fr)

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Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014110466A1 (fr) * 2013-01-12 2014-07-17 Dawei Zhang Composés pyridine utilisés en tant qu'inhibiteurs de pi3 kinase
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
TWI644671B (zh) 2013-03-14 2018-12-21 比利時商健生藥品公司 P2x7調節劑
US9604982B2 (en) 2013-03-14 2017-03-28 Janssen Pharmaceutica Nv P2X7 modulators
ES2845473T3 (es) 2013-03-14 2021-07-26 Boehringer Ingelheim Int (Bencil-ciano-metil)-amidas sustituidas de ácido 2-aza-biciclo[2.2.1]heptano-3-carboxílico inhibidores de la catepsina- C
US9242969B2 (en) * 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
US9040534B2 (en) 2013-03-14 2015-05-26 Janssen Pharmaceutica Nv [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
SG10201804471PA (en) 2013-10-18 2018-07-30 Celgene Quanticel Research Inc Bromodomain inhibitors
WO2015108881A1 (fr) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Hétéroaryles et utilisations de ceux-ci
WO2015108861A1 (fr) * 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Hétéroaryles et utilisations de ceux-ci
PE20170255A1 (es) 2014-01-24 2017-03-22 Dana Farber Cancer Inst Inc Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas
HUE045065T2 (hu) 2014-01-31 2019-12-30 Novartis Ag TIM-3 antitest molekulák és felhasználásaik
KR102442436B1 (ko) 2014-03-14 2022-09-15 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
CN107074828B (zh) * 2014-09-12 2020-05-19 诺华股份有限公司 用作raf激酶抑制剂的化合物和组合物
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EP3511331A1 (fr) 2014-09-12 2019-07-17 Boehringer Ingelheim International GmbH Inhibiteurs spirocycliques de la cathepsine c
AU2015315693B2 (en) 2014-09-12 2020-01-16 Janssen Pharmaceutica Nv P2X7 modulating n-acyl-triazolopyrazines
WO2016039977A1 (fr) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv Modulateurs de p2x7
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
EP4245376A3 (fr) 2014-10-14 2023-12-13 Novartis AG Molécules d'anticorps de pd-l1 et leurs utilisations
EP3233918A1 (fr) 2014-12-19 2017-10-25 Novartis AG Polythérapies
EA035817B1 (ru) 2015-03-10 2020-08-14 Адуро Байотек, Инк. Композиции и способы для активации сигналинга, зависимого от "гена стимулятора интерферона"
WO2017004133A1 (fr) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Inhibiteurs d'irak et utilisations de ceux-ci
HRP20211058T8 (hr) 2015-07-29 2021-11-26 Novartis Ag Kombinirane terapije koje sadrže molekule antitijela protiv lag-3
EP3328418A1 (fr) 2015-07-29 2018-06-06 Novartis AG Traitements combinés comprenant des molécules d'anticorps qui se lient à pd-1
EP3878465A1 (fr) 2015-07-29 2021-09-15 Novartis AG Polythérapies comprenant des molécules d'anticorps tim-3
CN105153190B (zh) * 2015-08-21 2017-07-21 江西科技师范大学 含联芳基酰胺结构的杂环并嘧啶类化合物及其制备方法和应用
US10208024B2 (en) 2015-10-23 2019-02-19 Array Biopharma Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
PE20181326A1 (es) 2015-11-03 2018-08-20 Janssen Biotech Inc Anticuerpos que se unen especificamente a pd-1 y sus usos
ES2986067T3 (es) 2015-12-17 2024-11-08 Novartis Ag Moléculas de anticuerpos frente a PD-1 y usos de las mismas
CN107021963A (zh) * 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
TWI721104B (zh) * 2016-02-19 2021-03-11 瑞典商斯普林特生物科技公司 6‐芳基或6‐雜芳基‐4‐嗎啉‐4‐芳基‐吡啶‐2‐酮化合物
ES2821400T3 (es) * 2016-02-19 2021-04-26 Sprint Bioscience Ab Compuestos de 6-heterociclil-4-morfolin-4-ilpiridin-2-ona útiles para el tratamiento del cáncer y la diabetes
KR20180134347A (ko) 2016-04-15 2018-12-18 제넨테크, 인크. 암의 진단 및 치료 방법
CA3026876A1 (fr) * 2016-06-10 2017-12-14 Novartis Ag Utilisations therapeutiques d'un inhibiteur de c-raf
EP3507367A4 (fr) 2016-07-05 2020-03-25 Aduro BioTech, Inc. Composés dinucléotidiques cycliques d'acide nucléique bloqué et leurs utilisations
CN106831812B (zh) * 2016-08-09 2019-09-20 江西科技师范大学 含联芳基酰胺结构的杂环并嘧啶或吡嗪类化合物及其应用
WO2018049214A1 (fr) 2016-09-09 2018-03-15 Incyte Corporation Dérivés de pyrazolopyridine comme modulateurs de hpk1 et leurs utilisations pour le traitement du cancer
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
AU2017329090B9 (en) * 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
EP3558979B1 (fr) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Nouvelles quinazolines substituées benzylamino et dérivés en tant qu'inhibiteurs de sos1
WO2018152220A1 (fr) 2017-02-15 2018-08-23 Incyte Corporation Composés de pyrazolopyridine et leurs utilisations
CN106866547B (zh) * 2017-03-15 2020-11-10 江苏省农用激素工程技术研究中心有限公司 2-乙氧基-4,6-二氯嘧啶的合成方法
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
AU2018258581A1 (en) * 2017-04-28 2019-11-07 Quartz Therapeutics, Inc. RAF-degrading conjugate compounds
CA3057969A1 (fr) 2017-05-02 2018-11-08 Novartis Ag Polytherapie
EP3642240A1 (fr) 2017-06-22 2020-04-29 Novartis AG Molécules d'anticorps dirigées contre cd73 et utilisations correspondantes
KR20200036880A (ko) * 2017-08-03 2020-04-07 노파르티스 아게 3세대 EGFR 타이로신 키나아제 억제제 및 Raf 억제제의 치료적 조합물
CN109384782A (zh) * 2017-08-04 2019-02-26 厦门大学 取代五元并六元杂环类化合物、其制备方法、药物组合及其用途
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
HRP20230400T1 (hr) 2017-12-21 2023-06-23 Boehringer Ingelheim International Gmbh Benzilamino supstituirani piridopirimidinoni i derivati kao inhibitori sos1
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
EP3752200A1 (fr) 2018-02-13 2020-12-23 Vib Vzw Ciblage d'une maladie résiduelle minimale dans le cancer avec des antagonistes de rxr
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
EP3755703B1 (fr) 2018-02-20 2022-05-04 Incyte Corporation Dérivés n-(phényl)-2-(phényl)pyrimidine-4-carboxamide et composés similaires en tant qu'inhibiteurs de hpk1 pour le traitemant du cancer
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US12133841B2 (en) * 2018-05-22 2024-11-05 Js Innomed Holdings Ltd. Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
TWI869346B (zh) 2018-05-30 2025-01-11 瑞士商諾華公司 Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法
CN108863884B (zh) * 2018-07-26 2020-07-03 南京富润凯德生物医药有限公司 一种用dast试剂作为消除试剂合成共轭硝基烯取代系列衍生物的方法
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020068729A1 (fr) 2018-09-25 2020-04-02 Incyte Corporation Composés pyrazolo[4,3-d]pyrimidine en tant que modulateurs des alk2 et/ou fgfr
US12054488B2 (en) 2018-09-27 2024-08-06 Suzhou Raymon Pharmaceuticals Company, Ltd. Pyrazolopyrimidine compound and preparation method therefor and use thereof in preparation of anti-cancer drug
KR20210069079A (ko) 2018-09-28 2021-06-10 얀센 파마슈티카 엔.브이. 모노아실글리세롤 리파아제 조절제
MY205440A (en) 2018-09-28 2024-10-21 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
EP3898626A1 (fr) 2018-12-19 2021-10-27 Array Biopharma, Inc. Composés pyrazolo[1,5-a]pyridine substitués servant d'inhibiteurs de tyrosine kinases fgfr
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
CA3123510A1 (fr) 2018-12-20 2020-06-25 Novartis Ag Polytherapie avec un inhibiteur de raf et un inhibiteur de cdk4/6 pour une utilisation dans le traitement du cancer
WO2020198058A1 (fr) * 2019-03-22 2020-10-01 Kinnate Biopharma Inc. Inhibiteurs de kinases raf
TW202106684A (zh) 2019-05-03 2021-02-16 美商奇奈特生物製藥公司 Raf激酶抑制劑
EP3969449B1 (fr) * 2019-05-13 2025-02-12 Novartis AG Nouvelles formes cristallines de n-(3-(2-(2-hydroxyéthoxy)-6-morpholinopyridin-4-yl)-4-méthylphényl)-2(trifluorométhyl)isonicotinamide servant d'inhibiteurs de raf pour le traitement du cancer
BR112022002059A2 (pt) 2019-08-06 2022-06-07 Incyte Corp Formas sólidas de um inibidor de hpk1
CN114174298B (zh) * 2019-08-14 2023-08-01 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
US10702525B1 (en) 2019-09-04 2020-07-07 United Arab Emirates University Pyrimidine derivatives as anti-diabetic agents
CN114502590A (zh) 2019-09-18 2022-05-13 诺华股份有限公司 Entpd2抗体、组合疗法、以及使用这些抗体和组合疗法的方法
JP7697934B2 (ja) 2019-09-30 2025-06-24 ヤンセン ファーマシューティカ エヌ.ベー. 放射線標識されたmgl petリガンド
JP7626910B2 (ja) * 2019-10-24 2025-02-05 ピエール ファーブル メディカモン Rafキナーゼの阻害剤
JP7214925B2 (ja) * 2019-12-06 2023-01-30 メッドシャイン ディスカバリー インコーポレイテッド Pan-RAFキナーゼ阻害剤としてのビアリール化合物
EP4106756A1 (fr) 2020-02-18 2022-12-28 Novartis AG Combinaisons thérapeutiques comprenant un inhibiteur de raf pour une utilisation dans le traitement du cpnpc mutant braf
EP4110341A2 (fr) 2020-02-28 2023-01-04 Novartis AG Combinaison pharmaceutique triple comprenant dabrafenib, un inhibiteur d'erk et un inhibiteur de raf ou un inhibiteur de pd-1
BR112022019077A2 (pt) 2020-03-26 2022-12-27 Janssen Pharmaceutica Nv Moduladores da monoacilglicerol lipase
US20240000789A1 (en) 2020-05-12 2024-01-04 Novartis Ag Therapeutic combinations comprising a craf inhibitor
JP7808058B2 (ja) 2020-06-02 2026-01-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング がんを治療するための縮合環化2-アミノ-3-シアノチオフェン及び誘導体
CN113912591B (zh) * 2020-07-08 2023-10-20 齐鲁制药有限公司 联芳基化合物
CN111995623A (zh) * 2020-08-18 2020-11-27 上海毕得医药科技有限公司 一种7-溴-4-氯-1-甲基-1H-咪唑并[4,5-c]吡啶的合成方法
TW202227088A (zh) 2020-08-31 2022-07-16 瑞士商諾華公司 組合療法
WO2022060996A1 (fr) * 2020-09-18 2022-03-24 Kinnate Biopharma Inc. Inhibiteurs de raf kinases
WO2022081469A1 (fr) * 2020-10-12 2022-04-21 Kinnate Biopharma Inc. Inhibiteurs de kinases raf
US12064421B2 (en) 2020-11-02 2024-08-20 Boehringer Ingelheim International Gmbh Substituted 1H-pyrazolo[4,3-c]pyridines and derivatives as EGFR inhibitors
CA3199999A1 (fr) 2020-11-25 2022-06-02 Deciphera Pharmaceuticals, Llc Derives morpholino utilises en tant qu'inhibiteurs de vps34 dans le traitement d'une infection virale
JP7849366B2 (ja) 2020-12-22 2026-04-21 キル・レガー・セラピューティクス・インコーポレーテッド Sos1阻害剤およびその使用
CN114591324B (zh) * 2021-03-30 2023-05-05 深圳微芯生物科技股份有限公司 一类吡嗪酮衍生物、其制备及其应用
EP4326255A4 (fr) * 2021-04-23 2025-03-12 Pierre Fabre Medicament Formes à l?état solide de (s)-n-(3-(2-(((r)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-méthylphényl)-3-(2,2,2-trifluoroéthyl)pyrrolidine-1-carboxamide et ses sels
BR112023021913A2 (pt) 2021-04-23 2024-01-16 Kinnate Biopharma Inc Tratamento de câncer com inibidor de raf
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
WO2022253334A1 (fr) * 2021-06-04 2022-12-08 南京明德新药研发有限公司 Forme cristalline d'inhibiteur de raf kinase et son procédé de préparation
WO2023083330A1 (fr) * 2021-11-12 2023-05-19 百极优棠(广东)医药科技有限公司 Inhibiteur de drak2, son procédé de préparation et son utilisation
WO2023099624A1 (fr) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh 2-amino-3-cyano thiophènes annelés et leurs dérivés pour le traitement du cancer
CN118574835A (zh) 2021-12-01 2024-08-30 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物
JP2024543976A (ja) 2021-12-01 2024-11-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌の処置のための環化2-アミノ-3-シアノチオフェン及び誘導体
JP2024542692A (ja) 2021-12-01 2024-11-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 環化2-アミノ-3-シアノチオフェンを含むkra分解化合物
TW202340208A (zh) 2021-12-01 2023-10-16 德商百靈佳殷格翰國際股份有限公司 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物
WO2023099608A1 (fr) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh 2-amino-3-cyano thiophènes annelés et leurs dérivés pour le traitement du cancer
CA3240263A1 (fr) 2021-12-09 2023-06-15 Daniel L. Flynn Inhibiteurs de raf kinase et leurs methodes d'utilisation
JP2025501744A (ja) 2021-12-23 2025-01-23 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 脳浸透性sos1阻害剤としての8-アザキナゾリン
EP4472968A1 (fr) * 2022-02-03 2024-12-11 Pierre Fabre Medicament Inhibiteurs de raf kinases
CN115947691B (zh) * 2022-03-01 2024-08-16 四川大学 哒嗪砜类衍生物及其用途
AU2023227427A1 (en) 2022-03-02 2024-09-19 Novartis Ag Precision therapy for the treatment of cancer
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
KR20250041176A (ko) 2022-08-10 2025-03-25 노파르티스 아게 나포라페닙을 포함하는 무정형 고체 분산물
US20260048075A1 (en) 2022-08-10 2026-02-19 Vib Vzw Inhibition of TCF4/ITF2 in the Treatment of Cancer
WO2024089006A1 (fr) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Composés hétérocycliques capables d'activer sting
CA3266173A1 (fr) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Composés hétérocycliques capables d'activer le sting
JP2026512969A (ja) 2022-10-26 2026-04-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Stingを活性化することができる複素環式化合物
TW202440574A (zh) 2023-02-09 2024-10-16 印度商薩蒂亞製藥創新私人有限公司 作為pkmyt1抑制劑的雜芳基化合物
WO2024220470A1 (fr) 2023-04-17 2024-10-24 Ikena Oncology, Inc. Inhibiteurs de tead et leurs utilisations dans le traitement de troubles prolifératifs
WO2024246099A1 (fr) 2023-05-30 2024-12-05 Boehringer Ingelheim International Gmbh 2-amino-3-cyano thiophènes annelés spirocycliques et dérivés pour le traitement du cancer
CN121419963A (zh) * 2023-06-13 2026-01-27 德西费拉制药有限责任公司 双重raf及微管蛋白抑制剂及其使用方法
EP4727922A1 (fr) * 2023-06-13 2026-04-22 Deciphera Pharmaceuticals, LLC Inhibiteurs doubles de raf et de tubuline et leurs procédés d'utilisation
AU2024302328A1 (en) * 2023-06-13 2025-11-27 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
WO2025032214A1 (fr) * 2023-08-09 2025-02-13 Pierre Fabre Medicament Composés indazoles et composés azaindazoles utilisés comme inhibiteurs de kinases raf
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
WO2025083426A1 (fr) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited Nouveaux traitements de la douleur
WO2025137105A1 (fr) * 2023-12-22 2025-06-26 Deciphera Pharmaceuticals, Llc Inhibiteurs doubles de raf et de tubuline et leurs procédés d'utilisation
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
WO2025146548A1 (fr) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Inhibiteurs de sos1 utiles pour traiter la douleur et le cancer
US20250313560A1 (en) 2024-04-03 2025-10-09 Boehringer Ingelheim International Gmbh Novel bicyclic benzylamido pyridine derivatives as SOS1 inhibitors
WO2026015873A1 (fr) * 2024-07-12 2026-01-15 Kymera Therapeutics, Inc. Inhibiteurs de stat6 et leurs utilisations
WO2026037494A1 (fr) * 2024-08-14 2026-02-19 Eracal Therapeutics Ltd. Nouveaux composés et leurs utilisations

Family Cites Families (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
DE3029376A1 (de) 1980-07-31 1982-03-18 Nepera Chemical Co. Inc., Harriman, N.Y. Verfahren zur herstellung von 2,4,5-tris-pyridylimidazolen
EP0149884B1 (fr) 1983-09-09 1992-12-16 Takeda Chemical Industries, Ltd. Dérivés de 5-pyridyle-1,3-thiazole, leur préparation et utilisation
JP2722586B2 (ja) 1989-01-13 1998-03-04 大正製薬株式会社 インドリルイミダゾール誘導体
JP2808460B2 (ja) 1989-11-16 1998-10-08 大正製薬株式会社 イミダゾール誘導体
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
GB2306108A (en) 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
US6268308B1 (en) 1996-08-27 2001-07-31 Syngenta Crop Protection, Inc. Herbicidal S-substituted 1,2,4,6-thiatriazines
AU743024B2 (en) 1997-03-05 2002-01-17 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
GB9711650D0 (en) 1997-06-05 1997-07-30 Pfizer Ltd Compounds useful in therapy
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6211177B1 (en) 1998-11-24 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
EP1140840B1 (fr) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. Diphenylurees a substituants -g(v)-carboxyaryles, inhibitrices de kinase raf
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
DE60001229T2 (de) 1999-04-09 2003-10-30 Smithkline Beecham Corp., Philadelphia Triarylimidazole
EP1169038B9 (fr) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Inhibiteurs cycliques de proteine tyrosine kinase
JP2000302680A (ja) 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
AU7031500A (en) 1999-09-23 2001-04-24 Astrazeneca Ab Therapeutic quinazoline compounds
AU1529901A (en) 1999-11-22 2001-06-04 Smithkline Beecham Plc Compounds
JP2003520233A (ja) 2000-01-18 2003-07-02 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 ジャイレースインヒビターおよびそれらの使用
AU2001232809A1 (en) 2000-01-18 2001-07-31 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
ATE266022T1 (de) 2000-03-06 2004-05-15 Smithkline Beecham Plc Imidazol derivate als raf kinase inhibitoren
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
WO2001074811A2 (fr) 2000-03-30 2001-10-11 Takeda Chemical Industries, Ltd. Composes de 1,3-thiazole substitues, production et utilisation desdits composes
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
ES2320973T3 (es) 2000-06-12 2009-06-01 EISAI R&D MANAGEMENT CO., LTD. Compuestos de 1,2-dihidropiridina, procedimiento para su preparacion y uso de los mismos.
EP1332131A2 (fr) 2000-11-07 2003-08-06 Bristol-Myers Squibb Company Derives d'acide utiles comme inhibiteurs de serines proteases
ATE365730T1 (de) 2000-11-20 2007-07-15 Smithkline Beecham Corp Neuartige verbindungen
JP2004517080A (ja) 2000-11-29 2004-06-10 グラクソ グループ リミテッド Tie−2および/またはvegfr−2の阻害剤として有用なベンゾイミダゾール誘導体
ES2274005T3 (es) 2001-01-26 2007-05-16 Chugai Seiyaku Kabushiki Kaisha Inhibidores de malonyl-coa decarboxilasa usados como moduladores metabolicos.
US7199124B2 (en) 2001-02-02 2007-04-03 Takeda Pharmaceutical Company Limited JNK inhibitor
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
GB0112348D0 (en) 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
WO2003082272A1 (fr) 2002-03-29 2003-10-09 Chiron Corporation Benzazoles substitues et leur utilisation en tant qu'inhibiteurs de la kinase raf
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
MXPA05002981A (es) 2002-09-18 2005-06-22 Pfizer Prod Inc Nuevos compuestos de imidazol como inhibidores del factor de crecimiento transformante (tgf).
AU2003256003A1 (en) 2002-09-18 2004-04-08 Pfizer Products Inc. Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
KR20060118472A (ko) 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 raf 키나아제의 저해제로서 그것의 사용
CA2545942C (fr) 2003-11-14 2012-07-10 Lorus Therapeutics Inc. Imidazoles d'aryle et leur utilisation comme agents anticancereux
RU2367661C2 (ru) 2004-03-05 2009-09-20 Тайсо Фармасьютикал Ко., Лтд. Производные тиазола
KR100749566B1 (ko) 2004-04-21 2007-08-16 이화여자대학교 산학협력단 Alk5 및/또는 alk4 억제제로 유효한 2-피리딜이치환된 이미다졸 유도체
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
PE20060315A1 (es) 2004-05-24 2006-05-15 Irm Llc Compuestos de tiazol como moduladores de ppar
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
MXPA06014696A (es) * 2004-06-15 2007-02-12 Astrazeneca Ab Quinazolonas sustituidas como agentes anticancerosos.
GB0415367D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
AU2005280168A1 (en) 2004-08-31 2006-03-09 Biogen Idec Ma Inc. Pyrimidinylimidazoles as TGF-beta inhibitors
WO2006038734A1 (fr) 2004-10-08 2006-04-13 Astellas Pharma Inc. Dérivés de la pyridazinone inhibiteurs de cytokines
AU2005295734A1 (en) 2004-10-15 2006-04-27 Biogen Idec Ma Inc. Methods of treating vascular injuries
GB0524814D0 (en) * 2005-12-05 2006-01-11 Glaxo Group Ltd Compounds
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
JP2007246520A (ja) 2006-02-15 2007-09-27 Takeda Yuichiro Rage阻害剤
JP2009530296A (ja) * 2006-03-17 2009-08-27 ワイス ピラゾロ[1,5−a]ピリミジン誘導体およびその使用方法
WO2007118149A2 (fr) 2006-04-07 2007-10-18 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical Lollege Thiazole et thiophene analogues et leur utilisation pour traiter des maladies auto-immunes et des cancers
EP2050749B1 (fr) 2006-08-08 2017-11-22 Chugai Seiyaku Kabushiki Kaisha Derive de pyrimidine comme inhibiteur de la pi3k et son utilisation
WO2008071605A2 (fr) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Méthodes de traitement de maladies inflammatoires
JP5140154B2 (ja) 2007-06-27 2013-02-06 アストラゼネカ・アクチエボラーグ ピラジノン誘導体および肺疾患の処置におけるそれらの使用
US7968536B2 (en) 2007-06-29 2011-06-28 Millennium Pharmaceuticals, Inc. Heterocyclic compounds useful as RAF kinase inhibitors
CL2008001933A1 (es) 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
CA2692379A1 (fr) 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Nouveaux composes chimiques
US20100261723A1 (en) * 2007-07-09 2010-10-14 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009012283A1 (fr) 2007-07-17 2009-01-22 Plexxikon Inc. Composés et procédés pour la modulation des kinases et leurs indications
MY150032A (en) 2007-07-19 2013-11-29 Merck Sharp & Dohme Heterocyclic amide compounds as protein kinase inhibitors
WO2009032667A1 (fr) 2007-08-29 2009-03-12 Smithkline Beecham Corporation Inhibiteurs de kinase à base de thiazole et d'oxazole
WO2009030952A2 (fr) 2007-09-05 2009-03-12 Astrazeneca Ab Composés hétérocycliques et leurs procédés d'utilisation
WO2009047163A1 (fr) 2007-10-10 2009-04-16 F. Hoffmann-La Roche Ag Procédés de traitement de maladies inflammatoires
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
WO2009115572A2 (fr) 2008-03-21 2009-09-24 Novartis Ag Nouveaux composés hétérocycliques et leurs utilisations
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
CN102089278A (zh) 2008-06-11 2011-06-08 Irm责任有限公司 用于治疗疟疾的化合物和组合物
CN102131805A (zh) * 2008-06-20 2011-07-20 百时美施贵宝公司 用作激酶抑制剂的咪唑并吡啶和咪唑并吡嗪化合物
PT2324008E (pt) 2008-07-24 2012-06-25 Nerviano Medical Sciences Srl 3,4-diarilpirazoles como inibidores da proteína quinase
WO2010048149A2 (fr) 2008-10-20 2010-04-29 Kalypsys, Inc. Modulateurs hétérocycliques de gpr119 pour le traitement d'une maladie
ES2921576T3 (es) 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
WO2011026911A1 (fr) 2009-09-04 2011-03-10 Novartis Ag Bipyridines utilisées dans le traitement des maladies prolifératives
EP2498608A4 (fr) 2009-11-10 2013-04-24 Glaxosmithkline Llc Composés de benzènesulfonamide-thiazole et oxazole
PL2520575T3 (pl) 2009-12-28 2017-05-31 General Incorporated Association Pharma Valley Project Supporting Organization Związek 1,3,4-oksadiazolo-2-karboksyamidowy
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
JP2013529619A (ja) 2010-06-25 2013-07-22 ノバルティス アーゲー タンパク質キナーゼ阻害剤としてのヘテロアリール化合物および組成物
CN101993415B (zh) 2010-09-15 2013-08-14 北京韩美药品有限公司 作为Hedgehog通路抑制剂的化合物以及包含该化合物的药物组合物及其应用
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20140221374A1 (en) * 2011-03-17 2014-08-07 Ruga Corporation Raf kinase inhibitors
EP2739143B1 (fr) 2011-08-05 2018-07-11 Gary A. Flynn Préparation et procédés d'utilisation d'ortho-aryle hétéroaryle à 5 chaînons -carboxamide contenant des inhibiteurs de kinases multicibles
EP2751104B1 (fr) 2011-09-01 2019-09-25 Novartis AG Composés et compositions en tant qu'inhibiteurs de kinase c-kit
WO2013041652A1 (fr) 2011-09-21 2013-03-28 Cellzome Limited Urée substituée par un groupe morpholino ou dérivés carbamate comme inhibiteurs de mtor
CA2871270A1 (fr) 2012-05-02 2013-11-07 Lupin Limited Composes substitues de pyridine en tant que modulateurs de crac
CN104379574B (zh) 2012-05-15 2017-03-01 诺华股份有限公司 用于抑制abl1、abl2和bcr‑abl1的活性的苯甲酰胺衍生物
AR091654A1 (es) 2012-07-02 2015-02-18 Biogen Idec Inc COMPUESTOS QUE CONTIENEN BIARILO COMO AGONISTAS INVERSOS DE RECEPTORES ROR-g
EP2903613B1 (fr) 2012-10-08 2017-11-22 Merck Sharp & Dohme Corp. Composés pyrazoliques utiles en tant qu'inhibiteurs d'activité d'irak4
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CN107074828B (zh) 2014-09-12 2020-05-19 诺华股份有限公司 用作raf激酶抑制剂的化合物和组合物
EP3191467B1 (fr) 2014-09-12 2020-10-21 Novartis AG Composés et compositions en tant qu'inhibiteurs de kinases
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa

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