EA028194B1 - Соединения биариламида в качестве ингибиторов киназы - Google Patents

Соединения биариламида в качестве ингибиторов киназы Download PDF

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EA028194B1
EA028194B1 EA201591727A EA201591727A EA028194B1 EA 028194 B1 EA028194 B1 EA 028194B1 EA 201591727 A EA201591727 A EA 201591727A EA 201591727 A EA201591727 A EA 201591727A EA 028194 B1 EA028194 B1 EA 028194B1
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room temperature
ring
alkyl
methyl
equiv
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EA201591727A
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Russian (ru)
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EA201591727A1 (ru
Inventor
Роберт Аверса
Пол А. Барсанти
Мэттью Бургер
Майкл Патрик Диллон
Алан Дипеса
Чэн Ху
Ян Лоу
Жизель Нисигути
Юэ Пань
Валерий Поляков
Савитхри Рамуртхи
Элис Рико
Лина Сетти
Аарон Смит
Шарадха Субраманиан
Бенджамин Тафт
Хью Таннер
Лифын Вань
Наим Юсуфф
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Новартис Аг
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Publication of EA201591727A1 publication Critical patent/EA201591727A1/ru
Publication of EA028194B1 publication Critical patent/EA028194B1/ru

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    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
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Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105050602B (zh) * 2013-01-12 2018-05-25 张大为 作为pi3激酶抑制剂的吡啶化合物
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TWI644671B (zh) 2013-03-14 2018-12-21 比利時商健生藥品公司 Ｐ２ｘ７調節劑
WO2014152537A1 (en) 2013-03-14 2014-09-25 Janssen Pharmaceutica Nv P2x7 modulators
WO2014140075A1 (en) 2013-03-14 2014-09-18 Boehringer Ingelheim International Gmbh Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c
ES2666155T3 (es) 2013-03-14 2018-05-03 Janssen Pharmaceutica Nv Moduladores de P2X7
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
EA035727B1 (ru) * 2013-10-18 2020-07-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы бромодомена
TN2016000270A1 (en) 2014-01-14 2017-10-06 Millennium Pharm Inc Heteroaryls and uses thereof.
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
KR20240110004A (ko) 2014-03-14 2024-07-12 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
AU2015315693B2 (en) 2014-09-12 2020-01-16 Janssen Pharmaceutica Nv P2X7 modulating n-acyl-triazolopyrazines
EP3191478B1 (en) * 2014-09-12 2019-05-08 Novartis AG Compounds and compositions as raf kinase inhibitors
CA2960968A1 (en) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv P2x7 modulators
CN108047240B (zh) 2014-09-12 2020-08-04 勃林格殷格翰国际有限公司 组织蛋白酶c的螺环化合物抑制剂
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
US9988452B2 (en) 2014-10-14 2018-06-05 Novartis Ag Antibody molecules to PD-L1 and uses thereof
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
JP6692826B2 (ja) 2015-03-10 2020-05-13 アドゥロ バイオテック，インク． 「インターフェロン遺伝子刺激因子」依存性シグナル伝達の活性化のための組成物及び方法
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CN108025051B (zh) 2015-07-29 2021-12-24 诺华股份有限公司 包含抗pd-1抗体分子的联合疗法
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
WO2017019894A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to lag-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
HRP20220436T1 (hr) 2015-11-03 2022-05-27 Janssen Biotech, Inc. Protutijela koja se specifično vežu na pd-1 i njihove uporabe
CA3007671A1 (en) 2015-12-17 2017-06-22 Novartis Ag Antibody molecules to pd-1 and uses thereof
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
RS60900B1 (sr) * 2016-02-19 2020-11-30 Sprint Bioscience Ab Jedinjenja 6-heterociklil-4-morfolin-4-ilpiridin-2-ona korisna za lečenje kancera i dijabetesa
RU2754664C2 (ru) * 2016-02-19 2021-09-06 Спринт Биосайенс Аб 6-арил-4-морфолин-1-илпиридоны, пригодные для лечения рака или диабета
KR20180134347A (ko) 2016-04-15 2018-12-18 제넨테크, 인크. 암의 진단 및 치료 방법
JP2019517549A (ja) 2016-06-10 2019-06-24 ノバルティス アーゲー Ｃ−ｒａｆ阻害薬の治療的使用
US11098077B2 (en) 2016-07-05 2021-08-24 Chinook Therapeutics, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
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
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
KR20230038807A (ko) 2016-09-09 2023-03-21 인사이트 코포레이션 Hpk1 조절제로서의 피라졸로피리딘 유도체 및 암의 치료를 위한 이의 용도
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
KR102341660B1 (ko) * 2016-09-19 2021-12-23 노파르티스 아게 Raf 억제제 및 erk 억제제를 포함하는 치료적 조합
EP3878850A1 (en) 2016-12-22 2021-09-15 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
US20180228786A1 (en) 2017-02-15 2018-08-16 Incyte Corporation Pyrazolopyridine compounds and uses thereof
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
JP2020518660A (ja) * 2017-04-28 2020-06-25 クォーツ セラピューティクス，インコーポレイティド Ｒａｆ分解性結合体化合物
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
ES2952265T3 (es) * 2017-05-02 2023-10-30 Novartis Ag Terapia combinada que comprende un inhibidor de Raf y trametinib
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag Antibody molecules to cd73 and uses thereof
MX2020001254A (es) 2017-08-03 2020-03-20 Novartis Ag Combinacion terapeutica de un inhibidor tirosina quinasa del egfr de tercera generacion y un inhibidor raf.
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
US11859252B2 (en) 2017-09-08 2024-01-02 Genentech, Inc. Diagnostic and therapeutic methods for cancer
LT3728254T (lt) 2017-12-21 2023-05-10 Boehringer Ingelheim International Gmbh Naujieji benzilaminu pakeistieji piridopirimidinonai ir jų dariniai kaip sos1 inhibitoriai
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
HUE059624T2 (hu) 2018-02-20 2022-11-28 Incyte Corp N-(fenil)-2-(fenil)pirimidin-4-karboxamid származékok és rokon vegyületek HPK1-inhibitorokként rák kezelésére
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
EP3797109A4 (en) * 2018-05-22 2022-02-23 JS Innomed Holdings Ltd. HETEROCYCLIC COMPOUNDS USED AS KINASE INHIBITORS, COMPOSITIONS COMPRISING THE HETEROCYCLIC COMPOUND, AND METHODS OF USE THEREOF
AR126019A1 (es) 2018-05-30 2023-09-06 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
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 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
CN110950868B (zh) * 2018-09-27 2022-05-13 苏州锐明新药研发有限公司 吡唑并嘧啶化合物及制备方法与制备抗癌症药物的应用
MA53722A (fr) 2018-09-28 2022-03-30 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycérol lipase
WO2020065613A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
MX2021007477A (es) 2018-12-20 2021-08-05 Novartis Ag Terapia de combinacion con un inhibidor de raf y un inhibidor de cdk4/6 para utilizar en el tratamiento del cancer.
CA3133812A1 (en) * 2019-03-22 2020-10-01 Kinnate Biopharma Inc. Inhibitors of raf kinases
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 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
PH12022550271A1 (en) 2019-08-06 2023-06-26 Incyte Corp Solid forms of an hpk1 inhibitor
WO2021027943A1 (zh) * 2019-08-14 2021-02-18 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
EP4031578A1 (en) 2019-09-18 2022-07-27 Novartis AG Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
EP4038070B1 (en) 2019-09-30 2025-07-09 Janssen Pharmaceutica NV Radiolabelled mgl pet ligands
CA3158530A1 (en) * 2019-10-24 2021-04-29 Stephen W. Kaldor Inhibitors of raf kinases
CN114746417B (zh) * 2019-12-06 2023-12-08 齐鲁制药有限公司 Pan-RAF激酶抑制剂的联芳基化合物
US20230226030A1 (en) 2020-02-18 2023-07-20 Novartis Ag Therapeutic combinations comprising a raf inhibitor for use in treating braf mutant nsclc
AU2021225491A1 (en) 2020-02-28 2022-10-20 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, an Erk inhibitor and a RAF inhibitor
EP4126860A1 (en) 2020-03-26 2023-02-08 Janssen Pharmaceutica NV Monoacylglycerol lipase modulators
US20240000789A1 (en) 2020-05-12 2024-01-04 Novartis Ag Therapeutic combinations comprising a craf inhibitor
US20230212164A1 (en) 2020-06-02 2023-07-06 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
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
EP4203963A1 (en) 2020-08-31 2023-07-05 Novartis AG Combination therapy of a raf inhibitor and a mek inhibitor for the treatment of sarcoma
US11407737B2 (en) * 2020-09-18 2022-08-09 Kinnate Biopharma Inc. Inhibitors of RAF kinases
WO2022081469A1 (en) * 2020-10-12 2022-04-21 Kinnate Biopharma Inc. Inhibitors of raf kinases
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 (en) 2020-11-25 2022-06-02 Deciphera Pharmaceuticals, Llc Morpholino derivatives as vsp34 inhibitors for use in the treatment of a viral infection
WO2022140427A1 (en) 2020-12-22 2022-06-30 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
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
JP2024516972A (ja) * 2021-04-23 2024-04-18 キネート バイオファーマ インク． Ｒａｆ阻害薬による癌の処置
CA3216258A1 (en) * 2021-04-23 2022-10-27 Stephen W. Kaldor Solid state forms of (s)-n-(3-(2-(((r)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-methylphenyl)-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and salts thereof
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
TWI812259B (zh) * 2021-06-04 2023-08-11 大陸商齊魯製藥有限公司 Raf激酶抑制劑的晶型及其製備方法
WO2023083330A1 (zh) * 2021-11-12 2023-05-19 百极优棠(广东)医药科技有限公司 Drak2抑制剂及其制备方法和应用
CN118647620A (zh) 2021-12-01 2024-09-13 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-氰基噻吩及其衍生物
JP2024543975A (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
KR20240128852A (ko) 2021-12-01 2024-08-27 베링거 인겔하임 인터내셔날 게엠베하 암 치료를 위한 고리형 2-아미노-3-시아노 티오펜 및 유도체
US20250145608A1 (en) 2021-12-01 2025-05-08 Boehringer Ingelheim Int'l GmbH Corp. Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
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
US20250129095A1 (en) 2021-12-01 2025-04-24 Boehringer Ingelheim Int'l GmbH Corp. Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
TW202337455A (zh) 2021-12-09 2023-10-01 美商迪賽孚爾製藥有限公司 Ｒａｆ激酶抑制劑及其使用方法
CN118434735A (zh) 2021-12-23 2024-08-02 勃林格殷格翰国际有限公司 8-氮杂喹唑啉作为脑渗透sos1抑制剂
CN118974036A (zh) * 2022-02-03 2024-11-15 皮埃尔法布雷医药公司 Raf激酶的抑制剂
CN115947691B (zh) * 2022-03-01 2024-08-16 四川大学 哒嗪砜类衍生物及其用途
TW202342766A (zh) 2022-03-02 2023-11-01 瑞士商諾華公司 用於癌症治療之精準療法
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
JP2025526729A (ja) 2022-08-10 2025-08-15 ノバルティス アーゲー ナポラフェニブを含む非晶質固体分散体
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
KR20250092268A (ko) 2022-10-26 2025-06-23 베링거 인겔하임 인터내셔날 게엠베하 Sting을 활성화시킬 수 있는 헤테로사이클릭 화합물
US20240174642A1 (en) 2022-10-26 2024-05-30 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
CR20250088A (es) 2022-10-26 2025-05-21 Boehringer Ingelheim Int Compuestos heterocíclicos con capacidad para activar el receptor sting
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 (en) 2023-04-17 2024-10-24 Ikena Oncology, Inc. Tead inhibitors and uses thereof in the treatment of proliferative disorders
WO2024246099A1 (en) 2023-05-30 2024-12-05 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
AU2024302328A1 (en) * 2023-06-13 2025-11-27 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2024258919A1 (en) * 2023-06-13 2024-12-19 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2024263460A1 (en) * 2023-06-13 2024-12-26 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 (en) * 2023-08-09 2025-02-13 Pierre Fabre Medicament Indazole compounds and azaindazole compounds as inhibitors of raf kinases
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
US20250206729A1 (en) * 2023-12-22 2025-06-26 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
WO2025210041A1 (en) 2024-04-03 2025-10-09 Boehringer Ingelheim International Gmbh Bicyclic benzylamido pyridine derivatives as sos1 inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006005918A1 (en) * 2004-07-09 2006-01-19 Astrazeneca Ab 2, 4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer

Family Cites Families (109)

* 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 (en) 1983-09-09 1992-12-16 Takeda Chemical Industries, Ltd. 5-pyridyl-1,3-thiazole derivatives, their production and use
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
AU4618497A (en) 1996-08-27 1998-03-19 Novartis Ag Herbicidal s-substituted 1,2,4,6-thiatriazines
ATE554750T1 (de) 1997-03-05 2012-05-15 Sugen Inc Hydrophobe pharmazeutische wirkstoffe enthaltende zubereitungen
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 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
ES2187473T3 (es) 1999-04-09 2003-06-16 Smithkline Beecham Corp Triarylimidazoles.
EP2308833A3 (en) 1999-04-15 2011-09-28 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
JP2000302680A (ja) 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
WO2001021598A1 (en) 1999-09-23 2001-03-29 Astrazeneca Ab Therapeutic quinazoline compounds
IL149150A0 (en) 1999-11-22 2002-12-01 Smithkline Beecham Plc 2-(4-(6-methoxy-naphthalene-2-yl)-5-pyridin-4-yl-1h-imidazole-2-yl)-2-methyl-derivatives, pharmaceutical compositions comprising them and use thereof as tie2 receptor kinase inhibitors
WO2001052845A1 (en) 2000-01-18 2001-07-26 Vertex Pharmaceuticals Incorpoated Gyrase inhibitors and uses thereof
AU2001232809A1 (en) 2000-01-18 2001-07-31 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR029803A1 (es) 2000-02-21 2003-07-16 Smithkline Beecham Plc Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
AU2001235838A1 (en) 2000-03-06 2001-09-17 Smithkline Beecham Plc Imidazol derivatives as raf kinase inhibitors
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
US7495018B2 (en) 2000-03-30 2009-02-24 Takeda Pharmaceutical Company Limited Substituted 1,3-thiazole compounds, their production and use
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.
US6642252B2 (en) 2000-11-07 2003-11-04 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
EP1343779B1 (en) 2000-11-20 2007-06-27 Smithkline Beecham Corporation Novel compounds
AU2002232439A1 (en) 2000-11-29 2002-06-11 Glaxo Group Limited Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors
JP4267920B2 (ja) 2001-01-26 2009-05-27 中外製薬株式会社 代謝調節剤として有用なマロニル−ＣｏＡ脱炭酸酵素阻害剤
US7199124B2 (en) 2001-02-02 2007-04-03 Takeda Pharmaceutical Company Limited JNK inhibitor
WO2002076960A1 (en) 2001-03-22 2002-10-03 Abbott Gmbh & Co. Kg 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
EA007987B1 (ru) 2002-03-29 2007-02-27 Чирон Корпорейшн Замещённые бензазолы и их применение в качестве ингибиторов киназы raf
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
PL375975A1 (en) 2002-09-18 2005-12-12 Pfizer Products Inc. Novel oxazole and thiazole compounds as transforming growth factor (tgf) inhibitors
CA2498047C (en) 2002-09-18 2009-05-19 Pfizer Products Inc. Novel imidazole 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
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
CN1863774B (zh) 2003-10-08 2010-12-15 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
KR20060118472A (ko) 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 ｒａｆ 키나아제의 저해제로서 그것의 사용
WO2005047266A1 (en) 2003-11-14 2005-05-26 Lorus Therapeutics Inc. Aryl imidazoles and their use as anti-cancer agents
WO2005085241A1 (ja) 2004-03-05 2005-09-15 Taisho Pharmaceutical Co., Ltd. チアゾール誘導体
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
KR20070028536A (ko) * 2004-06-15 2007-03-12 아스트라제네카 아베 항암제로서의 치환된 퀴나졸론
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
CA2578630A1 (en) 2004-08-31 2006-03-09 Wen-Cherng Lee Pyrimidinylimidazoles as tgf-beta inhibitors
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
WO2006044509A2 (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
CN101405289A (zh) * 2006-03-17 2009-04-08 惠氏公司 吡唑并[1,5-a]嘧啶衍生物和其使用方法
CA2682189C (en) 2006-04-07 2015-12-08 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
ES2657635T3 (es) 2006-08-08 2018-03-06 Chugai Seiyaku Kabushiki Kaisha Derivado de pirimidina como inhibidor de PI3K y uso del mismo
WO2008071605A2 (en) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
HRP20141174T1 (hr) 2007-06-27 2015-02-13 Astrazeneca Ab Derivati pirazinona i njihova uporaba za lijeäśenje bolesti pluä†a
TWI444379B (zh) 2007-06-29 2014-07-11 Sunesis Pharmaceuticals Inc 有用於作為Ｒａｆ激酶抑制劑之化合物
NZ582349A (en) 2007-06-29 2012-06-29 Sunesis Pharmaceuticals Inc Heterocyclic compounds useful as raf kinase inhibitors
EP2176249A2 (en) 2007-07-02 2010-04-21 Boehringer Ingelheim International GmbH New chemical compounds
EP2178866A2 (en) * 2007-07-09 2010-04-28 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
EP2170830B1 (en) 2007-07-17 2014-10-15 Plexxikon, Inc. 2-FLUORO-BENZENESULFONAMIDE COMPOUNDS AS Raf KINASE MODULATORS
KR101552742B1 (ko) 2007-07-19 2015-09-11 머크 샤프 앤드 돔 코포레이션 단백질 키나제 억제제로서의 헤테로사이클릭 아미드 화합물
JP2010538003A (ja) 2007-08-29 2010-12-09 グラクソスミスクライン エルエルシー チアゾールおよびオキサゾールキナーゼ阻害薬
TW200916458A (en) 2007-09-05 2009-04-16 Astrazeneca Ab Heterocyclic compounds and methods of use thereof
WO2009047163A1 (en) 2007-10-10 2009-04-16 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
CN102015686B (zh) 2008-03-21 2014-07-02 诺华股份有限公司 杂环化合物及其用途
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
WO2009152356A2 (en) 2008-06-11 2009-12-17 Irm Llc Compounds and compositions useful for the treatment of malaria
EP2300466B1 (en) * 2008-06-20 2014-08-06 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
JP5385382B2 (ja) 2008-07-24 2014-01-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ プロテインキナーゼ阻害剤としての３，４−ジアリールピラゾール
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
EP2376485B1 (en) 2008-12-19 2017-12-06 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
US20110130380A1 (en) 2009-09-04 2011-06-02 Barsanti Paul A Heteroaryl Kinase Inhibitors
EP2498608A4 (en) 2009-11-10 2013-04-24 Glaxosmithkline Llc BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
CA2785679C (en) 2009-12-28 2017-12-12 General Incorporated Association Pharma Valley Project Supporting Organization 1,3,4-oxadiazole-2-carboxamide compound
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
KR20130048293A (ko) 2010-06-25 2013-05-09 노파르티스 아게 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물
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
WO2012109075A1 (en) 2011-02-07 2012-08-16 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2012125981A2 (en) * 2011-03-17 2012-09-20 Selexagen Therapeutics, Inc. Raf kinase inhibitors
WO2013022766A1 (en) 2011-08-05 2013-02-14 Flynn Gary A Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors
BR112014004560A2 (pt) 2011-09-01 2017-04-04 Irm Llc compostos e composições como inibidores de c-kit quinase
KR20140070616A (ko) 2011-09-21 2014-06-10 셀좀 리미티드 Mtor 저해제로서의 모르폴리노 치환된 우레아 또는 카바메이트 유도체
EP2844655A1 (en) 2012-05-02 2015-03-11 Lupin Limited Substituted pyridine compounds as crac modulators
ES2670667T3 (es) 2012-05-15 2018-05-31 Novartis Ag Derivados de benzamida para inhibir la actividad de ABL1, ABL2 y BCR-ABL1
TW201414704A (zh) 2012-07-02 2014-04-16 Biogen Idec Inc 作爲ＲＯＲ－γ受體之反向促效劑之含聯芳化合物
WO2014058691A1 (en) 2012-10-08 2014-04-17 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
EP3191478B1 (en) 2014-09-12 2019-05-08 Novartis AG Compounds and compositions as raf kinase inhibitors
JP6646044B2 (ja) 2014-09-12 2020-02-14 ノバルティス アーゲー キナーゼ阻害剤としての化合物および組成物
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006005918A1 (en) * 2004-07-09 2006-01-19 Astrazeneca Ab 2, 4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
N. BABCHIA, A. CALIPEL, F. MOURIAUX, A.-M. FAUSSAT, F. MASCARELLI: "The PI3K/Akt and mTOR/P70S6K Signaling Pathways in Human Uveal Melanoma Cells: Interaction with B-Raf/ERK", INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE, ¬ASSOCIATION FOR RESEARCH IN VISION AND OPHTHALMOLOGY, ETC.|, vol. 51, no. 1, 1 January 2010 (2010-01-01), pages 421 - 429, XP055046622, ISSN: 01460404, DOI: 10.1167/iovs.09-3974 *

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