CU20150118A7 - Compuestos de biaril-amida como inhibidores de cinasa - Google Patents

Compuestos de biaril-amida como inhibidores de cinasa

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Publication number
CU20150118A7
CU20150118A7 CUP2015000118A CU20150118A CU20150118A7 CU 20150118 A7 CU20150118 A7 CU 20150118A7 CU P2015000118 A CUP2015000118 A CU P2015000118A CU 20150118 A CU20150118 A CU 20150118A CU 20150118 A7 CU20150118 A7 CU 20150118A7
Authority
CU
Cuba
Prior art keywords
compounds
biaril
cinasa
inhibitors
amida
Prior art date
Application number
CUP2015000118A
Other languages
English (en)
Other versions
CU24351B1 (es
Inventor
Robert Aversa
Paul A Barsanti
Mathew Burger
Michael Patrick Dillon
Alan Dipesa
Cheng Hu
Yan Lou
Gisele Nishiguchi
Yue Pan
Valery Polyakov
Savithri Ramurthy
Alice C Rico
Lina Setti
Aaron Smith
Sharadha Subramanian
Benjamin Taft
Huw Tanner
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 CU20150118A7 publication Critical patent/CU20150118A7/es
Publication of CU24351B1 publication Critical patent/CU24351B1/es

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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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
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    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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Abstract

La presente invención proporciona compuestos de la fórmula (I) como se describen en la presente y las sales de los mismos y los usos terapéuticos de estos compuestos para el tratamiento de los trastornos asociados con la actividad de cinasa Raf. La invención proporciona además composiciones farmacéuticas que comprenden estos compuestos y composiciones que comprenden estos compuestos y un co-agente terapéutico
CUP2015000118A 2013-03-14 2014-03-13 Compuestos de biaril-amida como inhibidores de cinasa CU24351B1 (es)

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Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014110466A1 (en) * 2013-01-12 2014-07-17 Dawei Zhang Pyridine compounds used as pi3 kinase inhibitors
JO3773B1 (ar) 2013-03-14 2021-01-31 Janssen Pharmaceutica Nv معدلات p2x7
EP3112366B1 (en) 2013-03-14 2018-02-28 Janssen Pharmaceutica NV P2x7 modulators
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 Ｐ２ｘ７調控劑
AU2014230814B2 (en) 2013-03-14 2017-12-21 Boehringer Ingelheim International Gmbh Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
ES2689526T3 (es) 2013-03-14 2018-11-14 Janssen Pharmaceutica Nv Moduladores de P2X7
US9242969B2 (en) * 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
HRP20200341T1 (hr) 2013-10-18 2020-06-12 Celgene Quanticel Research, Inc. Bromodomenski (bet) inhibitori
MX2016009135A (es) * 2014-01-14 2016-10-05 Millennium Pharm Inc Heteroarilos y usos de estos.
US10202373B2 (en) 2014-01-14 2019-02-12 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
EP3660050A1 (en) 2014-03-14 2020-06-03 Novartis AG Antibody molecules to lag-3 and uses thereof
UY36294A (es) * 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EP3191478B1 (en) * 2014-09-12 2019-05-08 Novartis AG Compounds and compositions as raf kinase inhibitors
WO2016039977A1 (en) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv P2x7 modulators
KR102510588B1 (ko) 2014-09-12 2023-03-17 베링거 인겔하임 인터내셔날 게엠베하 카텝신 c의 스피로사이클릭 억제제
EA201790600A1 (ru) 2014-09-12 2017-07-31 Янссен Фармацевтика Нв Модулирующие p2x7 n-ацил-триазолопиразины
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
CN114920840A (zh) 2014-10-14 2022-08-19 诺华股份有限公司 针对pd-l1的抗体分子及其用途
US20170340733A1 (en) 2014-12-19 2017-11-30 Novartis Ag Combination therapies
JO3746B1 (ar) 2015-03-10 2021-01-31 Aduro Biotech Inc تركيبات وطرق لتنشيط الإشارات المعتمدة على "منبه أو تحفيز جين انترفيرون"
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
PL3317301T3 (pl) 2015-07-29 2021-11-15 Novartis Ag Terapie skojarzone zawierające cząsteczki przeciwciał przeciw lag-3
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
EP3316902A1 (en) 2015-07-29 2018-05-09 Novartis AG Combination therapies comprising antibody molecules to 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
CA3002560A1 (en) 2015-10-23 2017-04-27 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
MY198562A (en) 2015-11-03 2023-09-05 Janssen Biotech Inc Antibodies specifically binding pd-1 and their uses
JP2019503349A (ja) 2015-12-17 2019-02-07 ノバルティス アーゲー Ｐｄ−１に対する抗体分子およびその使用
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
HRP20201400T1 (hr) 2016-02-19 2020-11-27 Sprint Bioscience Ab Spojevi 6-aril-4-(morfolin-4-il)-1h-piridin-2-ona korisni za liječenje karcinoma i dijabetesa
CN108884067B (zh) * 2016-02-19 2021-01-08 思普瑞特生物科学公司 可用于治疗癌症和糖尿病的6-杂环基-4-吗啉-4-基吡啶-2-酮化合物
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
MX2018015353A (es) * 2016-06-10 2019-09-09 Novartis Ag Usos terapeuticos de un inhibidor de c-raf.
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS 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
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
WO2018049191A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer
IL292977A (en) 2016-09-09 2022-07-01 Incyte Corp Pyrazolopyridine derivatives as modulators of hpk1 and their use in cancer therapy
AR109595A1 (es) 2016-09-09 2018-12-26 Incyte Corp Compuestos de pirazolopirimidina y usos de estos como inhibidores de hpk1
KR102341660B1 (ko) * 2016-09-19 2021-12-23 노파르티스 아게 Raf 억제제 및 erk 억제제를 포함하는 치료적 조합
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
WO2018152220A1 (en) 2017-02-15 2018-08-23 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
EP3615083A4 (en) * 2017-04-28 2021-05-19 Zamboni Chem Solutions Inc. RAF DEGRADATION CONJUGATES
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
CN110494166B (zh) 2017-05-02 2022-11-08 诺华股份有限公司 组合疗法
EP3642240A1 (en) 2017-06-22 2020-04-29 Novartis AG Antibody molecules to cd73 and uses thereof
JOP20200014A1 (ar) 2017-08-03 2022-10-30 Novartis Ag توليفة علاجية لمثبط كيناز تيروزين egfr من الجيل الثالث ومثبط 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
EP3679159A1 (en) 2017-09-08 2020-07-15 H. Hoffnabb-La Roche Ag Diagnostic and therapeutic methods for cancer
MX2020006438A (es) 2017-12-21 2020-09-17 Boehringer Ingelheim Int Nuevas piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1.
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
LT3755703T (lt) 2018-02-20 2022-10-10 Incyte Corporation N-(fenil)-2-(fenil)pirimidin-4-karboksamido dariniai ir susiję junginiai, kaip hpk1 inhibitoriai, skirti vėžio gydymui
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
US10752635B2 (en) 2018-02-20 2020-08-25 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
MA53726A (fr) 2018-09-25 2022-05-11 Incyte Corp Composés pyrazolo[4,3-d]pyrimidine en tant que modulateurs des alk2 et/ou fgfr
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
WO2020065613A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
MA53722A (fr) 2018-09-28 2022-03-30 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycérol lipase
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
AU2019407159A1 (en) 2018-12-20 2021-07-15 Novartis Ag Combination therapy with a Raf inhibitor and a CKD4/6 inhibitor for use in the treatment of cancer
CA3133812A1 (en) * 2019-03-22 2020-10-01 Kinnate Biopharma Inc. Inhibitors of raf kinases
AU2020268814A1 (en) 2019-05-03 2021-12-16 Kinnate Biopharma Inc. Inhibitors of RAF kinases
BR112021022335A2 (pt) 2019-05-13 2021-12-28 Novartis Ag Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin-4-il)-4-metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf para o tratamento de câncer
EP4010338A1 (en) 2019-08-06 2022-06-15 Incyte Corporation Solid forms of an hpk1 inhibitor
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
CN114555596B (zh) 2019-09-30 2025-02-25 詹森药业有限公司 放射性标记的mgl pet配体
AU2020371727A1 (en) 2019-10-24 2022-05-26 Pierre Fabre Medicament Inhibitors of RAF kinases
EP4071146A4 (en) * 2019-12-06 2023-01-04 Medshine Discovery Inc. BIARYL COMPOUND AS PAN-RAF KINASE INHIBITOR
EP4106756A1 (en) 2020-02-18 2022-12-28 Novartis AG Therapeutic combinations comprising a raf inhibitor for use in treating braf mutant nsclc
EP4110341A2 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a raf inhibitor
US11891387B2 (en) 2020-03-26 2024-02-06 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
US20240000789A1 (en) 2020-05-12 2024-01-04 Novartis Ag Therapeutic combinations comprising a craf inhibitor
AU2021285032A1 (en) 2020-06-02 2022-12-08 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
WO2022043955A1 (en) 2020-08-31 2022-03-03 Novartis Ag Combination therapy of a raf inhibitor and a mek inhibitor for the treatment of sarcoma
WO2022060996A1 (en) * 2020-09-18 2022-03-24 Kinnate Biopharma Inc. Inhibitors of raf kinases
US11377431B2 (en) 2020-10-12 2022-07-05 Kinnate Biopharma Inc. Inhibitors of RAF kinases
JP2023550591A (ja) 2020-11-02 2023-12-04 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 ＥＧＦＲ阻害薬としての置換１Ｈ－ピラゾロ［４，３－ｃ］及び誘導体
US12414955B2 (en) 2020-11-25 2025-09-16 Deciphera Pharmaceuticals, Llc Anti-viral activity of VPS34 inhibitors
AR124449A1 (es) 2020-12-22 2023-03-29 Qilu Regor Therapeutics Inc Inhibidores de sos1 y usos de los mismos
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
MX2023012521A (es) * 2021-04-23 2023-12-15 Kinnate Biopharma Inc Formas en estado solido de (s)-n-(3-(2-((r)-1-hidroxipropano-2-il) amino)-6-morfolinopiridin-4-il)-4-metilfenil)-3-(2,2,2-trifluoroe til)pirrolidin-1-carboxamida y sales de las mismas.
AU2022261117A1 (en) 2021-04-23 2023-11-23 Pierre Fabre Medicament Treatment of cancer with a raf inhibitor
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
CN117425650A (zh) * 2021-06-04 2024-01-19 齐鲁制药有限公司 一种raf激酶抑制剂的晶型及其制备方法
CN118201922A (zh) * 2021-11-12 2024-06-14 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
WO2023099592A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
EP4441054A1 (en) 2021-12-01 2024-10-09 Boehringer Ingelheim International GmbH Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
MX2024006681A (es) 2021-12-01 2024-08-26 Boehringer Ingelheim Int Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del 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
CN118591540A (zh) 2021-12-01 2024-09-03 勃林格殷格翰国际有限公司 包含环状2-氨基-3-氰基噻吩的kras降解化合物
CN118613485A (zh) 2021-12-01 2024-09-06 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
EP4444429A1 (en) 2021-12-09 2024-10-16 Deciphera Pharmaceuticals, LLC Raf kinase inhibitors and methods of use thereof
EP4452975A1 (en) 2021-12-23 2024-10-30 Boehringer Ingelheim International GmbH 8-aza quinazolines as brain-penetrant sos1-inhibitors
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
US20250179584A1 (en) 2022-03-02 2025-06-05 Novartis Ag Precision therapy for the treatment of cancer
IL316768A (en) 2022-05-25 2025-01-01 Ikena Oncology Inc MEK inhibitors and their uses
IL318900A (en) 2022-08-10 2025-04-01 Novartis Ag Amorphous solid dispersions containing naproxen
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
KR20250093392A (ko) 2022-10-26 2025-06-24 베링거 인겔하임 인터내셔날 게엠베하 Sting을 활성화시킬 수 있는 헤테로사이클릭 화합물
WO2024088991A1 (en) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
US20240174641A1 (en) 2022-10-26 2024-05-30 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating 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
AU2024311847A1 (en) * 2023-06-13 2025-11-27 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2024258917A1 (en) * 2023-06-13 2024-12-19 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
AU2024304207A1 (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 (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
US20250206729A1 (en) * 2023-12-22 2025-06-26 Deciphera Pharmaceuticals, Llc Dual raf and tubulin inhibitors and methods of use thereof
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
US20250313560A1 (en) 2024-04-03 2025-10-09 Boehringer Ingelheim International Gmbh Novel bicyclic benzylamido pyridine derivatives as SOS1 inhibitors

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
DE3486009T2 (de) 1983-09-09 1993-04-15 Takeda Chemical Industries Ltd 5-pyridyl-1,3-thiazol-derivate, ihre herstellung und anwendung.
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
JP4713698B2 (ja) 1997-03-05 2011-06-29 スージェン， インク． 疎水性薬剤の処方
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
DE60001229T2 (de) 1999-04-09 2003-10-30 Smithkline Beecham Corp., Philadelphia Triarylimidazole
CN1348370A (zh) 1999-04-15 2002-05-08 布里斯托尔-迈尔斯斯奎布公司 环状蛋白酪氨酸激酶抑制剂
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
MXPA02005106A (es) 1999-11-22 2002-11-07 Smithkline Beecham Plc Compuestos novedosos.
EP1251848B1 (en) 2000-01-18 2004-06-23 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
WO2001052846A1 (en) 2000-01-18 2001-07-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
US7235658B2 (en) 2000-03-06 2007-06-26 Smithkline Beecham P.L.C. Imidazol derivatives as Raf kinase inhibitors
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 (en) 2000-03-30 2001-10-11 Takeda Chemical Industries, Ltd. Substituted 1,3-thiazole compounds, their production and use
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
KR100904011B1 (ko) 2000-06-12 2009-06-22 에자이 알앤드디 매니지먼트 가부시키가이샤 1,2-디하이드로피리딘 화합물 및 그의 제조 방법
CA2428191A1 (en) 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
WO2002039954A2 (en) 2000-11-20 2002-05-23 Smithkline Beecham Corporation Novel compounds
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
WO2002064136A2 (en) 2001-01-26 2002-08-22 Chugai Seiyaku Kabushiki Kaisha Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
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
DK1499311T3 (da) 2002-03-29 2010-03-08 Novartis Vaccines & Diagnostic Substituerede benzaboler og anvendelse deraf som RAF-kinaseinhibitorer
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
AU2003263404A1 (en) 2002-09-18 2004-04-08 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tgf) inhibitors
DE60327443D1 (de) 2002-09-18 2009-06-10 Pfizer Prod Inc Neue oxazolverbindungen als inhibitoren des transforming growth factor (tgf)
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
CA2542105C (en) 2003-10-08 2011-08-02 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1682126B1 (en) 2003-10-16 2009-07-01 Novartis Vaccines and Diagnostics, Inc. Substituted benzazoles and use thereof as inhibitors of raf kinase
DK1692113T3 (en) 2003-11-14 2018-01-08 Lorus Therapeutics Inc ARYLIMIDAZOLES AND USE THEREOF AS ANTICANCES
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
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation 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
WO2005123696A1 (en) * 2004-06-15 2005-12-29 Astrazeneca Ab Substituted quinazolones as anti-cancer agents
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415367D0 (en) * 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
EP1786802A1 (en) 2004-08-31 2007-05-23 Biogen Idec MA, Inc. 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
WO2007109093A2 (en) * 2006-03-17 2007-09-27 Wyeth Pyrazolo[1,5-a]pyrimidine derivatives and methods of use thereof
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
DK2050749T3 (en) 2006-08-08 2018-01-08 Chugai Pharmaceutical Co Ltd PYRIMIDINE DERIVATIVES AS PI3K INHIBITOR AND USE THEREOF
WO2008071605A2 (en) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
CN101842361B (zh) 2007-06-27 2013-06-05 阿斯利康(瑞典)有限公司 吡嗪酮衍生物及其在治疗肺病中的用途
CA2694284A1 (en) 2007-06-29 2009-01-08 Jennifer Cossrow 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.
EP2176249A2 (en) * 2007-07-02 2010-04-21 Boehringer Ingelheim International GmbH New chemical compounds
JP2010533159A (ja) * 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物９４７
SG183036A1 (en) 2007-07-17 2012-08-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2693967A1 (en) 2007-07-19 2009-01-29 Schering Corporation Heterocyclic amide compounds as protein kinase inhibitors
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
WO2009030952A2 (en) 2007-09-05 2009-03-12 Astrazeneca Ab Phenylcarboxamide derivatives as inhibitors and effectors of the hedgehog pathway
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
KR101408517B1 (ko) 2008-03-21 2014-06-17 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
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
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
EP2300466B1 (en) * 2008-06-20 2014-08-06 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
HRP20120577T1 (hr) 2008-07-24 2012-08-31 Nerviano Medical Sciences S.R.L. 3,4-diarilpirazoli kao inhibitori proteinskih kinaza
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
EP2473499A1 (en) 2009-09-04 2012-07-11 Novartis AG Bipyridines useful for the treatment of proliferative diseases
WO2011059610A1 (en) 2009-11-10 2011-05-19 Glaxosmithkline Llc Benzene sulfonamide thiazole and oxazole compounds
AU2010339271B2 (en) 2009-12-28 2015-09-03 General Incorporated Association Pharma Valley Project Supporting Organization 1,3,4-oxadiazole-2-carboxamide compound
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
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
JP5941069B2 (ja) 2011-02-07 2016-06-29 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節のための化合物および方法、ならびにそれに対する適応症
US20140221374A1 (en) * 2011-03-17 2014-08-07 Ruga Corporation Raf kinase inhibitors
EP2739143B1 (en) 2011-08-05 2018-07-11 Gary A. Flynn 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
JP5995975B2 (ja) 2011-09-21 2016-09-21 セルゾーム リミテッド Ｍｔｏｒ阻害剤としてのモルホリノ置換尿素またはカルバメート誘導体
CA2871270A1 (en) 2012-05-02 2013-11-07 Lupin Limited Substituted pyridine compounds as crac modulators
BR112014027181A2 (pt) 2012-05-15 2017-06-27 Novartis Ag derivados de benzamida para a inibição da atividade de abl1, abl2 e 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
US9586948B2 (en) 2012-10-08 2017-03-07 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
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
CN107001329B (zh) 2014-09-12 2020-09-01 诺华股份有限公司 作为激酶抑制剂的化合物和组合物

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