CN104254533B - 用作激酶抑制剂的噻唑或噻二唑取代的吡啶基化合物 - Google Patents

用作激酶抑制剂的噻唑或噻二唑取代的吡啶基化合物 Download PDF

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CN104254533B
CN104254533B CN201380013584.XA CN201380013584A CN104254533B CN 104254533 B CN104254533 B CN 104254533B CN 201380013584 A CN201380013584 A CN 201380013584A CN 104254533 B CN104254533 B CN 104254533B
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acn
isopropylamino
thiazole
bases
solvent
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CN104254533A (zh
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V.R.佩蒂
S.R.库马
S.K.奈尔
A.巴纳吉
R.西斯特拉
W.J.皮茨
J.海因斯
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Bristol Myers Squibb Co
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CN201380013584.XA 2012-01-13 2013-01-11 用作激酶抑制剂的噻唑或噻二唑取代的吡啶基化合物 Active CN104254533B (zh)

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US201261586148P 2012-01-13 2012-01-13
US61/586,148 2012-01-13
PCT/US2013/021134 WO2013106641A1 (en) 2012-01-13 2013-01-11 Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors

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CN104254533A CN104254533A (zh) 2014-12-31
CN104254533B true CN104254533B (zh) 2017-09-08

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US (3) US9242976B2 (enExample)
EP (1) EP2802579B1 (enExample)
JP (1) JP6096219B2 (enExample)
CN (1) CN104254533B (enExample)
ES (1) ES2575604T3 (enExample)
WO (1) WO2013106641A1 (enExample)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6109195B2 (ja) 2012-01-13 2017-04-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ キナーゼ阻害剤として有用な複素環置換されたピリジル化合物
EP2903617B1 (en) * 2012-10-08 2019-01-30 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
PE20150953A1 (es) 2012-11-08 2015-06-20 Bristol Myers Squibb Co Compuestos de piridilo sustituidos con heteroarilo utiles como moduladores de cinasa
WO2014074657A1 (en) 2012-11-08 2014-05-15 Bristol-Myers Squibb Company Bicyclic heterocycle substituted pyridyl compounds useful as kinase modulators
TW201524952A (zh) * 2013-03-15 2015-07-01 Araxes Pharma Llc Ｋｒａｓ ｇ１２ｃ之共價抑制劑
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
UY35935A (es) 2014-01-03 2015-06-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos de nicotinamida sustituida con heteroarilo como inhibidores de quinasa y moduladores de irak-4
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法
KR102641263B1 (ko) 2015-06-24 2024-02-26 브리스톨-마이어스 스큅 컴퍼니 헤테로아릴 치환된 아미노피리딘 화합물
CN108026099B (zh) * 2015-06-24 2020-07-10 百时美施贵宝公司 经杂芳基取代的氨基吡啶化合物
EP3313840B1 (en) 2015-06-24 2019-07-24 Bristol-Myers Squibb Company Heteroaryl substituted aminopyridine compounds
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EA038635B9 (ru) 2015-11-16 2021-10-26 Араксис Фарма Ллк 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
US20180073208A1 (en) * 2016-09-14 2018-03-15 Caterpillar Inc. Automated Method to Determine Haul Road Repair Need
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
TWI825663B (zh) * 2016-10-14 2023-12-11 美商林伯士拉克許米公司 Tyk2抑制劑及其用途
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
TW201900640A (zh) 2017-05-11 2019-01-01 美商必治妥美雅史谷比公司 作為irak4抑制劑之噻吩并吡啶及苯并噻吩
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CA3063440A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Covalent inhibitors of kras
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
EP3684365A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND USES OF SUCH
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES OF THE LATEST
WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
JP7569688B2 (ja) 2017-12-22 2024-10-18 ハイバーセル，インコーポレイテッド ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2020010177A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
EP3817822A4 (en) 2018-07-06 2022-07-27 Kymera Therapeutics, Inc. PROTEIN DEGRADANTS AND USES THEREOF
TWI898556B (zh) 2018-07-13 2025-09-21 美商基利科學股份有限公司 吡咯并[1,2-b]嗒衍生物
CA3224985A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
EP3829580A1 (en) 2018-08-01 2021-06-09 Araxes Pharma LLC Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
TWI727392B (zh) * 2018-08-13 2021-05-11 美商基利科學股份有限公司 噻二唑irak4抑制劑
SG11202105424PA (en) 2018-11-30 2021-06-29 Kymera Therapeutics Inc Irak degraders and uses thereof
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
KR20220035447A (ko) 2019-07-18 2022-03-22 브리스톨-마이어스 스큅 컴퍼니 IRAK4 억제제로서 유용한 피라졸로[3,4-d]피롤로[1,2-b]피리다지닐 화합물
WO2021011724A1 (en) 2019-07-18 2021-01-21 Bristol-Myers Squibb Company Tricyclic heteroaryl compounds useful as irak4 inhibitors
JP7573596B2 (ja) 2019-07-23 2024-10-25 ブリストル－マイヤーズ スクイブ カンパニー Ｉｒａｋ４阻害剤として有用なチエノピリジニルおよびチアゾロピリジニル化合物
CN112279845B (zh) * 2019-07-24 2023-07-28 中国医学科学院药物研究所 芳基或杂芳基取代的噻二唑类化合物及其抗菌用途
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
MX2022007576A (es) 2019-12-17 2022-09-23 Kymera Therapeutics Inc Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos.
WO2021158495A1 (en) 2020-02-03 2021-08-12 Bristol-Myers Squibb Company Benzo[5,6][1,4]dioxino[2,3-b]pyridine compounds useful as irak4 inhibitors
JP7682191B2 (ja) 2020-02-03 2025-05-23 ブリストル－マイヤーズ スクイブ カンパニー Ｉｒａｋ４阻害剤として有用な三環ヘテロアリール化合物
US20230142629A1 (en) * 2020-02-19 2023-05-11 Nurix Therapeutics, Inc. Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US20240076285A1 (en) * 2020-12-16 2024-03-07 Shankar Venkatraman Compounds and compositions for treating conditions associated with sting activity
AU2021413371A1 (en) 2020-12-30 2023-07-13 Kymera Therapeutics, Inc. Irak degraders and uses thereof
AU2022220043A1 (en) 2021-02-15 2023-08-31 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
CN118302168A (zh) 2021-10-29 2024-07-05 凯麦拉医疗公司 Irak4降解剂和其制备
EP4472967A2 (en) 2022-01-31 2024-12-11 Kymera Therapeutics, Inc. Irak degraders and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004065378A1 (en) * 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
WO2010117425A1 (en) * 2009-03-31 2010-10-14 Biogen Idec Ma Inc. Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
CN102264731A (zh) * 2008-12-26 2011-11-30 奥米罗有限公司 1,2,4-*二唑衍生物及其治疗用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
AUPR688101A0 (en) 2001-08-08 2001-08-30 Luminis Pty Limited Protein domains and their ligands
GB0211019D0 (en) 2002-05-14 2002-06-26 Syngenta Ltd Novel compounds
ATE530530T1 (de) 2002-06-28 2011-11-15 Astellas Pharma Inc Diaminopyrimidincarbonsäureamidderivat
CN1820001A (zh) 2003-07-10 2006-08-16 神经能质公司 经取代的杂环二芳基胺类似物
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
FR2896503B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives soufres d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
KR20100020454A (ko) 2007-06-08 2010-02-22 바이엘 크롭사이언스 소시에떼아노님 살진균제 헤테로사이클릴-피리미디닐-아미노 유도체
WO2009046416A1 (en) 2007-10-05 2009-04-09 Targegen Inc. Anilinopyrimidines as jak kinase inhibitors
GB0719644D0 (en) 2007-10-05 2007-11-14 Cancer Rec Tech Ltd Therapeutic compounds and their use
CN102458402B (zh) 2009-06-12 2013-10-02 百时美施贵宝公司 用作激酶调节剂的烟酰胺化合物
JP2012254939A (ja) * 2009-10-07 2012-12-27 Astellas Pharma Inc オキサゾール化合物
JP5770198B2 (ja) 2009-10-30 2015-08-26 ヤンセン ファーマシューティカ エヌ．ベー． オピオイド受容体調節因子としてのフェノキシ置換ピリミジン
US20190192510A1 (en) 2010-02-01 2019-06-27 Nippon Chemiphar Co., Ltd. Gpr119 agonist
JP2014515029A (ja) 2011-04-29 2014-06-26 アイカーン・スクール・オブ・メディシン・アト・マウント・シナイ キナーゼ阻害剤
WO2013106614A1 (en) * 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Triazolyl-substituted pyridyl compounds useful as kinase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004065378A1 (en) * 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
CN102264731A (zh) * 2008-12-26 2011-11-30 奥米罗有限公司 1,2,4-*二唑衍生物及其治疗用途
WO2010117425A1 (en) * 2009-03-31 2010-10-14 Biogen Idec Ma Inc. Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use

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