JP6849614B2 - 増殖性、自己免疫性または炎症性疾患の処置に有用な１−［（シクロペンチルまたは２−ピロリジニル）カルボニルアミノメチル］−４−（１，３−チアゾール−５−イル）ベンゼンの誘導体 - Google Patents

増殖性、自己免疫性または炎症性疾患の処置に有用な１−［（シクロペンチルまたは２−ピロリジニル）カルボニルアミノメチル］−４−（１，３−チアゾール−５−イル）ベンゼンの誘導体 Download PDF

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JP6849614B2
JP6849614B2 JP2017566216A JP2017566216A JP6849614B2 JP 6849614 B2 JP6849614 B2 JP 6849614B2 JP 2017566216 A JP2017566216 A JP 2017566216A JP 2017566216 A JP2017566216 A JP 2017566216A JP 6849614 B2 JP6849614 B2 JP 6849614B2
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JP2018509468A (ja
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シウリ アレッシオ
シウリ アレッシオ
ゼンジャール マイケル
ゼンジャール マイケル
ホ チャン クウォク
ホ チャン クウォク
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University of Dundee
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JP2017566216A 2015-03-13 2016-03-14 増殖性、自己免疫性または炎症性疾患の処置に有用な１−［（シクロペンチルまたは２−ピロリジニル）カルボニルアミノメチル］−４−（１，３−チアゾール−５−イル）ベンゼンの誘導体 Active JP6849614B2 (ja)

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GB201504314A GB201504314D0 (en) 2015-03-13 2015-03-13 Small molecules
GB1504314.4 2015-03-13
GB1521858.9 2015-12-11
GBGB1521858.9A GB201521858D0 (en) 2015-03-13 2015-12-11 Small molecules
PCT/GB2016/050691 WO2016146985A1 (en) 2015-03-13 2016-03-14 Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl)carbonylaminomethyl]-4-(1,3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or inflammatory diseases

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Families Citing this family (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
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
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
JP6817962B2 (ja) 2015-01-20 2021-01-20 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． ターゲティングされたアンドロゲン受容体分解のための化合物および方法
AU2016232705C1 (en) * 2015-03-18 2021-06-17 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
EP3319944A4 (en) 2015-07-10 2019-04-24 Arvinas, Inc. MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS
EP3337476A4 (en) * 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
CA3014644A1 (en) 2016-02-15 2017-08-24 The Regents Of The University Of Michigan Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
CN121974842A (zh) 2016-05-10 2026-05-05 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
CN110087680B (zh) 2016-08-19 2024-03-19 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
CA3036834A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
GB2554071A (en) * 2016-09-14 2018-03-28 Univ Dundee Small molecules
EP3512842B1 (en) 2016-09-15 2024-01-17 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
SI3526202T1 (sl) 2016-10-11 2025-04-30 Arvinas Operations, Inc. Spojine in postopki za ciljno razgradnjo androgenskih receptorjev
WO2018075908A1 (en) * 2016-10-21 2018-04-26 University Of Miami Materials and methods for treating ophthalmic inflammation
MX2019005007A (es) * 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
CN110753693A (zh) 2016-12-23 2020-02-04 阿尔维纳斯运营股份有限公司 Egfr蛋白水解靶向嵌合分子和相关使用方法
IL325835A (en) * 2016-12-23 2026-03-01 Univ Yale Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
IL319363A (en) 2017-01-31 2025-05-01 Arvinas Operations Inc Cervalon ligands and bifunctional compounds containing them
CN110573507B (zh) * 2017-04-14 2023-11-14 邓迪大学 小分子
EP3391907B8 (en) 2017-04-20 2020-03-04 iOmx Therapeutics AG Intracellular kinase sik3 associated with resistance against anti-tumour immune responses, and uses thereof
EP4717317A3 (en) 2017-06-20 2026-06-03 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
US11267822B2 (en) 2017-09-13 2022-03-08 The Regents Of The University Of Michigan BET bromodomain protein degraders with cleavable linkers
KR102129367B1 (ko) * 2017-10-20 2020-07-03 한국화학연구원 세레브론 단백질의 분해 유도 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
WO2019084026A1 (en) * 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
US10519152B2 (en) 2017-12-21 2019-12-31 Astrazeneca Ab Compounds and their use in treating cancer
EP3508499A1 (en) 2018-01-08 2019-07-10 iOmx Therapeutics AG Antibodies targeting, and other modulators of, an immunoglobulin gene associated with resistance against anti-tumour immune responses, and uses thereof
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
CN111902141A (zh) 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
BR112020020307A2 (pt) 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
CN111741769B (zh) * 2018-04-20 2022-09-16 四川科伦博泰生物医药股份有限公司 一种多功能化合物、其制备方法及其在医药上的应用
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
CA3103205A1 (en) 2018-06-13 2019-12-19 Amphista Therapeutics Ltd Bifunctional molecules for targeting uchl5
WO2019238886A1 (en) 2018-06-13 2019-12-19 University Of Dundee Bifunctional molecules for targeting usp14
CA3103185A1 (en) * 2018-06-13 2019-12-19 Amphista Therapeutics Ltd Bifunctional molecules for targeting rpn11
US11542273B2 (en) 2018-07-04 2023-01-03 Mitsubishi Tanabe Pharma Corporation Amide compound having bet proteolysis-inducing action and medicinal application thereof
WO2020027225A1 (ja) 2018-07-31 2020-02-06 ファイメクス株式会社 複素環化合物
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
MX2021001957A (es) 2018-08-22 2021-07-15 Cullgen Shanghai Inc Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk).
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
CN119219628A (zh) * 2018-09-07 2024-12-31 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的多环化合物和方法
CN112996800B (zh) * 2018-10-16 2024-06-25 勃林格殷格翰国际有限公司 作为smarca2和/或smarca4的降解剂的新型蛋白水解靶向嵌合体（protac）及其衍生物
AU2019365238A1 (en) * 2018-10-24 2021-05-13 F. Hoffmann-La Roche Ag Conjugated chemical inducers of degradation and methods of use
EP3873608A1 (en) 2018-10-31 2021-09-08 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
EP4371987B9 (en) 2018-10-31 2025-11-26 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds as hpk1 inhibitors
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Process for preparing extracellular vesicles
KR20210141554A (ko) 2019-03-21 2021-11-23 코디악 바이오사이언시즈, 인크. 세포외 소포 접합체 및 이의 용도
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
CA3146023A1 (en) 2019-07-05 2021-01-14 Iomx Therapeutics Ag Antibodies binding igc2 of igsf11 (vsig3) and uses thereof
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CN112390852B (zh) * 2019-08-14 2022-10-18 上海济煜医药科技有限公司 作为蛋白降解剂的化合物及其制备方法和应用
WO2021041348A1 (en) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
CN112457365B (zh) * 2019-09-09 2023-06-09 中国医学科学院药物研究所 一类靶向蛋白质水解通路的功能分子及其制备和应用
MX2022004526A (es) 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
WO2021127443A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US20230117831A1 (en) * 2020-01-08 2023-04-20 The Broad Institute, Inc. Multi-functional chimeric molecules
PT116050B (pt) * 2020-01-09 2022-06-15 Hovione Farm S A Conjugados fármaco-ligando e inibidores das proteínas da família bromodomínio e domínio extraterminal -(bet) modificados
CA3169810A1 (en) * 2020-02-03 2021-08-12 Design Therapeutics, Inc. Methods and compounds for the treatment of genetic disease
BR112022016901A2 (pt) 2020-02-26 2022-12-06 Cullgen Shanghai Inc Compostos de degradação do receptor de tropomiosina quinase (trk) e métodos de uso
CN115996918A (zh) 2020-05-09 2023-04-21 阿尔维纳斯运营股份有限公司 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
EP4175668A1 (en) 2020-07-06 2023-05-10 iOmx Therapeutics AG Antibodies binding igv of igsf11 (vsig3) and uses thereof
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
TW202221000A (zh) 2020-09-30 2022-06-01 英屬開曼群島商百濟神州有限公司 用於降解ｅｇｆｒ之雙功能化合物及相關使用方法
GB202017717D0 (en) 2020-11-10 2020-12-23 Univ Dundee Improved small molecules
CA3204523A1 (en) * 2021-01-08 2022-07-14 Aseem Ansari Methods and compounds for treating friedreich's ataxia
CN116802180B (zh) * 2021-01-22 2024-05-28 泰比棣医药科技(石家庄)有限公司 一种降解脱氧核糖核酸(dna)聚合酶的化合物及其用途
CN116847848A (zh) 2021-02-10 2023-10-03 百济神州有限公司 Egfr降解剂和使用方法
CN113171467B (zh) * 2021-03-09 2023-04-07 中国科学院化学研究所 一种基于nqo1调控的嵌合体分子及其应用
CN115154419B (zh) * 2021-04-02 2023-11-28 中国科学院上海药物研究所 一种纳米胶束前体和纳米胶束，其制备方法及应用
CN118388454A (zh) 2021-04-16 2024-07-26 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
EP4330251A4 (en) 2021-04-30 2025-03-05 BeiGene Switzerland GmbH EGFR DEGRADING AGENTS AND METHODS OF USE THEREOF
US20240299558A1 (en) * 2021-06-18 2024-09-12 University Of Maryland, Baltimore Proteolysis targeting chimeras and polypharmacological agents targeting bcl-2, and methods of use thereof
CN113636931B (zh) * 2021-08-05 2024-02-13 康龙化成(宁波)科技发展有限公司 基因编码化合物库起始头片段化合物及其在基因编码化合物库合成上的应用
CA3240051A1 (en) 2021-12-30 2023-07-06 Beigene Switzerland Gmbh Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
EP4511128A1 (en) 2022-04-20 2025-02-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
PE20260006A1 (es) 2023-01-26 2026-01-06 Arvinas Operations Inc Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2024246838A1 (en) 2023-05-31 2024-12-05 Beigene Switzerland Gmbh Compounds for the degradation of egfr kinase
EP4735451A1 (en) 2023-06-30 2026-05-06 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
TW202530189A (zh) 2023-09-29 2025-08-01 日商第一三共股份有限公司 ３－苯基丙基胺衍生物
CN122228262A (zh) 2023-11-02 2026-06-16 金橘生物科技公司 降解剂及其用途
AU2024392985A1 (en) 2023-12-08 2026-06-04 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy
CN122270449A (zh) 2023-12-13 2026-06-23 百济神州(苏州)生物科技有限公司 通过将irak4抑制剂与e3连接酶配体缀合来降解irak4以及使用方法
WO2026016710A1 (zh) * 2024-07-16 2026-01-22 北京大学深圳研究生院 用于靶向蛋白降解的基于pamam-peg的纳米颗粒
US20260092058A1 (en) * 2024-09-30 2026-04-02 St. Jude Children's Research Hospital, Inc. Small Molecule Degraders and Fluorescent Probes of PXR
CN120865239B (zh) * 2025-09-25 2025-12-12 深圳大学 基于苯并咪唑融合共价弹头的降解剂及其制备方法与应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001295041A1 (en) 2000-09-08 2002-03-22 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
WO2013106646A2 (en) * 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
GB201311910D0 (en) * 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
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
US12312316B2 (en) * 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
JP6817962B2 (ja) 2015-01-20 2021-01-20 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． ターゲティングされたアンドロゲン受容体分解のための化合物および方法
EP3337476A4 (en) * 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins

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