CY1119707T1 - Ενωσεις διαρυλικου αμιδιου ως αναστολεις της κινασης - Google Patents

Ενωσεις διαρυλικου αμιδιου ως αναστολεις της κινασης

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Publication number
CY1119707T1
CY1119707T1 CY20171101348T CY171101348T CY1119707T1 CY 1119707 T1 CY1119707 T1 CY 1119707T1 CY 20171101348 T CY20171101348 T CY 20171101348T CY 171101348 T CY171101348 T CY 171101348T CY 1119707 T1 CY1119707 T1 CY 1119707T1
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CY
Cyprus
Prior art keywords
compounds
diablic
amid
models
care units
Prior art date
Application number
CY20171101348T
Other languages
English (en)
Inventor
Robert AVERSA
Paul A. Barsanti
Matthew Burger
Michael Patrick Dillon
Alan Dipesa
Cheng Hu
Yan Lou
Gisele Nishiguchi
Yue Pan
Valery Polyakov
Savithri Ramurthy
Alice Rico
Lina Setti
Aaron Smith
Sharadha Subramanian
Benjamin TAFT
Huw Tanner
Lifeng Wan
Naeem Yusuff
Original Assignee
Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CY1119707T1 publication Critical patent/CY1119707T1/el

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    • 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
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    • 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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    • A61K31/541Non-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

Η παρούσα εφεύρεση παρέχει ενώσεις με τον Τύπο (I) όπως περιγράφεται στο παρόν, και άλατα των ενώσεων αυτών, και θεραπευτικές χρήσεις των ενώσεων αυτών για τη θεραπευτική αντιμετώπιση διαταραχών οι οποίες σχετίζονται με τη δραστηριότητα των κινασών Raf. Η εφεύρεση παρέχει περαιτέρω φαρμακευτικές συνθέσεις οι οποίες περιέχουν τις ενώσεις αυτές, και συνθέσεις οι οποίες περιέχουν τις ενώσεις αυτές και ένα θεραπευτικό συν-παράγοντα.
CY20171101348T 2013-03-14 2017-12-22 Ενωσεις διαρυλικου αμιδιου ως αναστολεις της κινασης CY1119707T1 (el)

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Families Citing this family (112)

* 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
US9040534B2 (en) 2013-03-14 2015-05-26 Janssen Pharmaceutica Nv [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
JO3773B1 (ar) 2013-03-14 2021-01-31 Janssen Pharmaceutica Nv معدلات p2x7
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
PE20151727A1 (es) 2013-03-14 2015-12-17 Boehringer Ingelheim Int Acido 2-aza-biciclo[2.2.1]heptano-3-carboxilico (bencil-ciano-metil)-amidas sustituidas inhibidores de catepsina c
WO2014152589A1 (en) 2013-03-14 2014-09-25 Janssen Pharmaceutica Nv P2x7 modulators
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CN108558889B (zh) * 2013-10-18 2021-11-05 赛尔基因昆蒂赛尔研究公司 布罗莫结构域抑制剂
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9802960B2 (en) * 2014-01-14 2017-10-31 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
AU2015229103C9 (en) 2014-03-14 2020-11-26 Immutep S.A.S 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
ES2714048T3 (es) 2014-09-12 2019-05-24 Janssen Pharmaceutica Nv Moduladores de P2X7
AU2015314355B2 (en) 2014-09-12 2019-06-20 Boehringer Ingelheim International Gmbh Spirocyclic inhibitors of Cathepsin C
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
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
MA40035A (fr) 2014-10-14 2016-04-21 Dana Farber Cancer Inst Inc Molécules d'anticorps de pd-l1 et leurs utilisations
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
US10449211B2 (en) 2015-03-10 2019-10-22 Aduro Biotech, Inc. Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
EP3964528A1 (en) 2015-07-29 2022-03-09 Novartis AG Combination therapies comprising antibody molecules to lag-3
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
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
AU2016341445B2 (en) 2015-10-23 2020-08-27 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
BR112018008867A8 (pt) 2015-11-03 2019-02-26 Janssen Biotech Inc anticorpos que se ligam especificamente a pd-1 e seus usos
AU2016369537B2 (en) 2015-12-17 2024-03-14 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
CN113845472A (zh) * 2016-02-19 2021-12-28 思普瑞特生物科学公司 可用于治疗癌症和糖尿病的6-芳基-4-吗啉-1-基吡啶酮化合物
EP3416957B1 (en) * 2016-02-19 2020-07-01 Sprint Bioscience AB 6-heterocyclyl-4-morpholin-4-ylpyridin-2-one compounds useful for the treatment of cancer and diabetes
CN109072311A (zh) 2016-04-15 2018-12-21 豪夫迈·罗氏有限公司 用于癌症的诊断和治疗方法
CA3026876A1 (en) * 2016-06-10 2017-12-14 Novartis Ag Therapeutic uses of a c-raf inhibitor
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, 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
TW201811799A (zh) 2016-09-09 2018-04-01 美商英塞特公司 吡唑并嘧啶化合物及其用途
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
EP3510032B1 (en) 2016-09-09 2022-07-06 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
MX2019003095A (es) 2016-09-19 2019-07-04 Novartis Ag Combinaciones terapeuticas que comprenden un inhibidor de raf y un inhibidor de erk.
JP7219218B2 (ja) 2016-12-22 2023-02-07 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 新規のベンジルアミノ置換キナゾリンおよびsos1阻害剤としての誘導体
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
US10787443B2 (en) * 2017-04-28 2020-09-29 Zamboni Chem Solutions Inc. RAF-degrading conjugate compounds
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
JP7309614B2 (ja) * 2017-05-02 2023-07-18 ノバルティス アーゲー 組み合わせ療法
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES
CA3069564A1 (en) * 2017-08-03 2019-02-07 Novartis Ag Therapeutic combination of a third-generation egfr tyrosine kinase inhibitor and a raf inhibitor
CN111373055B (zh) 2017-09-08 2024-07-23 豪夫迈·罗氏有限公司 用于癌症的诊断和治疗方法
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
PL3728254T3 (pl) 2017-12-21 2023-06-12 Boehringer Ingelheim International Gmbh Benzyloaminopodstawione pirydopirymidynony i pochodne jako inhibitory sos1
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
HRP20220833T1 (hr) 2018-02-20 2022-10-28 Incyte Corporation Derivati n-(fenil)-2-(fenil)pirimidin-4-karboksamida i odgovarajući spojevi kao inhibitori hpk1 za liječenje raka
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
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
UY38247A (es) 2018-05-30 2019-12-31 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
US11111247B2 (en) 2018-09-25 2021-09-07 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
WO2020063636A1 (zh) * 2018-09-27 2020-04-02 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
CA3111309A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
WO2020065613A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
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.
CN113874381A (zh) * 2019-03-22 2021-12-31 金耐特生物制药公司 Raf激酶的抑制剂
CN114072148A (zh) 2019-05-03 2022-02-18 金耐特生物制药公司 Raf激酶的抑制剂
KR20220008273A (ko) * 2019-05-13 2022-01-20 노파르티스 아게 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태
JP2022543155A (ja) 2019-08-06 2022-10-07 インサイト・コーポレイション Hpk1阻害剤の固体形態
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
JP2022548881A (ja) 2019-09-18 2022-11-22 ノバルティス アーゲー Entpd2抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv MGL PET RADIOLABE LIGANDS
CA3158530A1 (en) 2019-10-24 2021-04-29 Stephen W. Kaldor Inhibitors of raf kinases
US20230046018A1 (en) * 2019-12-06 2023-02-16 Medshine Discovery Inc. Biaryl compound as pan-raf kinase inhibitor
TW202140029A (zh) 2020-02-18 2021-11-01 瑞士商諾華公司 用於治療braf突變型nsclc的包含raf抑制劑之治療組合
EP4110341A2 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a raf inhibitor
KR20220157999A (ko) 2020-03-26 2022-11-29 얀센 파마슈티카 엔.브이. 모노아실글리세롤 리파아제 조절제
WO2021229439A1 (en) 2020-05-12 2021-11-18 Novartis Ag Therapeutic combinations comprising a craf inhibitor
PE20240493A1 (es) 2020-06-02 2024-03-15 Boehringer Ingelheim Int 2-amino-3-cianotiofenos anulados y derivados para el tratamiento del 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
WO2022090481A1 (en) 2020-11-02 2022-05-05 Boehringer Ingelheim International Gmbh Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors
JP2024501280A (ja) 2020-12-22 2024-01-11 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
CN117561057A (zh) * 2021-04-23 2024-02-13 金耐特生物制药公司 用raf抑制剂治疗癌症
BR112023021916A2 (pt) * 2021-04-23 2023-12-19 Kinnate Biopharma Inc Formas em estado sólido de (s)-n-(3-(2-(((r)-1- hidroxipropan-2-il)amino)-6-morfolinopiridin-4-il)-4- metilfenil)-3-(2,2,2-trifluoretil)pirrolidina-1-carboxamida e sais desta
US12065427B2 (en) 2021-04-29 2024-08-20 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating STING
WO2022253334A1 (zh) * 2021-06-04 2022-12-08 南京明德新药研发有限公司 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
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
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
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
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
IL312905A (en) 2021-12-01 2024-07-01 Boehringer Ingelheim Int 2-amino-3-cyano ring thiophenes and history for cancer therapy
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
WO2023108108A1 (en) * 2021-12-09 2023-06-15 Deciphera Pharmaceuticals, Llc Raf kinase inhibitors and methods of use thereof
WO2023118250A1 (en) 2021-12-23 2023-06-29 Boehringer Ingelheim International Gmbh 8-aza quinazolines as brain-penetrant sos1-inhibitors
US11814384B2 (en) 2022-02-03 2023-11-14 Kinnate Biopharma Inc. Inhibtors of 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
TW202404581A (zh) 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Mek抑制劑及其用途
WO2024033703A1 (en) 2022-08-10 2024-02-15 Novartis Ag Amorphous solid dispersions comprising naporafenib
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
US20240166629A1 (en) 2022-10-26 2024-05-23 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
US20240174642A1 (en) 2022-10-26 2024-05-30 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
WO2024089006A1 (en) 2022-10-26 2024-05-02 Boehringer Ingelheim International Gmbh Heterocyclic compounds capable of activating sting
WO2024166131A1 (en) 2023-02-09 2024-08-15 Satyarx Pharma Innovations Private Limited Heteroaryl compounds as pkmyt1 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
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
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
WO2000042012A1 (en) 1999-01-13 2000-07-20 Bayer Corporation φ-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
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
DE60030741T2 (de) 1999-09-23 2007-09-06 Astrazeneca Ab Chinazoline verbindungen als heilmittel
ES2228629T3 (es) 1999-11-22 2005-04-16 Smithkline Beecham Plc Derivados de imidazol y su uso como inhibidores de raf-quinasa.
WO2001052846A1 (en) 2000-01-18 2001-07-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AU782883B2 (en) 2000-01-18 2005-09-08 Vertex Pharmaceuticals Incorpoated Gyrase inhibitors and uses thereof
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
ES2218391T3 (es) 2000-03-06 2004-11-16 Smithkline Beecham Plc Derivados de imidazol como inhibidores de raf-cinasa.
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
DE60137426D1 (de) 2000-06-12 2009-03-05 Eisai R&D Man Co Ltd 1,2-dihydropyridinverbindungen, verfahren zu deren herstellung und deren verwendung
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
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
EP1377290B1 (en) 2001-01-26 2006-10-04 Chugai Seiyaku Kabushiki Kaisha Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
CA2437248A1 (en) 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. 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
AU2003226211B2 (en) 2002-03-29 2008-05-29 Novartis Vaccines And Diagnostics, Inc. Substituted benzazoles and use thereof as RAF kinase inhibitors
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
OA12926A (en) 2002-09-18 2006-10-13 Pfizer Prod Inc Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors.
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
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
EP1673343A4 (en) 2003-10-08 2008-09-10 Irm Llc COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
CA2542653A1 (en) 2003-10-16 2005-04-28 Chiron Corporation Substituted benzazoles and use thereof as inhibitors of raf kinase
CA2545942C (en) 2003-11-14 2012-07-10 Lorus Therapeutics Inc. Aryl imidazoles and their use as anti-cancer agents
MY146532A (en) 2004-03-05 2012-08-15 Taisho Pharmaceutical Co Ltd Thiazole derivative
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
JP2008502666A (ja) * 2004-06-15 2008-01-31 アストラゼネカ アクチボラグ 抗癌剤としての置換キナゾロン類
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
JP2008511631A (ja) 2004-08-31 2008-04-17 バイオジェン・アイデック・エムエイ・インコーポレイテッド TGF−βインヒビターとしてのピリミジニルイミダゾール
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
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
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
AU2007282535B9 (en) 2006-08-08 2013-06-20 Chugai Seiyaku Kabushiki Kaisha Pyrimidine derivative as PI3K inhibitor and use thereof
WO2008071605A2 (en) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
RU2479580C2 (ru) 2007-06-27 2013-04-20 Астразенека Аб Производные пиразинона и их применение для лечения легочных заболеваний
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
US7968536B2 (en) 2007-06-29 2011-06-28 Millennium Pharmaceuticals, Inc. Heterocyclic compounds useful as RAF kinase inhibitors
WO2009003998A2 (en) 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Antiproliferative compounds based on 5-membered heterocycles
US20100261723A1 (en) * 2007-07-09 2010-10-14 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
CA2693967A1 (en) 2007-07-19 2009-01-29 Schering Corporation Heterocyclic amide compounds as protein kinase inhibitors
US20110190280A1 (en) 2007-08-29 2011-08-04 George Adjabeng Thiazole And Oxazole Kinase Inhibitors
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
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
JP5384611B2 (ja) 2008-03-21 2014-01-08 ノバルティス アーゲー 新規ヘテロ環式化合物およびそれらの使用
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
JP2011525183A (ja) * 2008-06-20 2011-09-15 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なイミダゾピリジンおよびイミダゾピラジン化合物
WO2010010154A1 (en) 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
EP3354650B1 (en) 2008-12-19 2022-02-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
AU2010291206A1 (en) 2009-09-04 2012-02-23 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
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
JP5794922B2 (ja) 2009-12-28 2015-10-14 一般社団法人ファルマバレープロジェクト支援機構 1,3,4−オキサジアゾール−2−カルボキサミド化合物
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
US20130096149A1 (en) 2010-06-25 2013-04-18 Novartis Ag Heteroaryl compounds and compositions as protein kinase inhibitors
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
SG192686A1 (en) 2011-02-07 2013-09-30 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
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
KR101962495B1 (ko) 2011-09-01 2019-03-26 노파르티스 아게 C-kit 키나제 억제제로서의 화합물 및 조성물
AU2012311458B2 (en) 2011-09-21 2016-02-04 Cellzome Limited Morpholino substituted urea or carbamate derivatives as mTOR inhibitors
CA2871270A1 (en) 2012-05-02 2013-11-07 Lupin Limited Substituted pyridine compounds as crac modulators
MX2014013373A (es) 2012-05-15 2015-08-14 Novartis Ag Derivados de benzamida para inhibir la actividad de abl1, abl2 y bcr-abl1.
AR091654A1 (es) 2012-07-02 2015-02-18 Biogen Idec Inc COMPUESTOS QUE CONTIENEN BIARILO COMO AGONISTAS INVERSOS DE RECEPTORES ROR-g
EP2903613B1 (en) 2012-10-08 2017-11-22 Merck Sharp & Dohme Corp. Pyrazole derivatives useful as inhibitors of irak4 activity
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 (en) 2014-09-12 2020-10-21 Novartis AG Compounds and compositions as kinase inhibitors
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa

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