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1. 发明申请

WO2022171782A1 MACROCYCLIC 1,3-BRIDGED 6-CHLORO-7-PYRAZOL-4-YL-1H-INDOLE-2-CARBOXYLATE AND 6-CHLORO-7-PYRIMIDIN-5-YL-1H-INDOLE-2-CARBOXYLATE DERIVATIVES AS MCL-1 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2022171782A1
公开(公告)日：2022-08-18
申请号：PCT/EP2022/053340
申请日：2022-02-11
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE BOECK, Benoît, Christian, Albert, Ghislain , ROMBOUTS, Frederik, Jan, Rita , JERHAOUI, Soufyan
IPC分类号： C07D515/18 , C07D403/14 , A61K31/407 , A61K31/4162 , A61K31/506 , A61P35/00 , A61P35/02
摘要： The present invention relates to compounds of formula (I) wherein XI is as myeloid cell leukemia-1 (MCL-1) inhibitors for the treatment of cancer, such as e.g. prostate, lung, pancreatic, breast, ovarian, and cervical cancer, melanoma, B-cell chronic lymphocytic leukemia (CLL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL). An exemplary compound is e.g. compound 1

2. 发明申请

WO2013139697A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：一致的约束，全合成的大环化合物
公开(公告)号：WO2013139697A1
公开(公告)日：2013-09-26
申请号：PCT/EP2013/055368
申请日：2013-03-15
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , ERMERT, Philipp , OUMOUCH, Said , PIETTRE, Arnaud , GOSALBES, Jean-François , THOMMEN, Marc
IPC分类号： C07D273/02 , C07D498/04 , C07D498/18 , C07D515/06 , C07D515/18 , C07D515/22 , C07D291/08 , A61K31/395 , A61P31/04
CPC分类号： C07D273/02 , C07D291/08 , C07D498/04 , C07D498/08 , C07D498/18 , C07D515/06 , C07D515/08 , C07D515/18 , C07D515/22
摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1 ) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
摘要翻译：式（I）的构象限制的空间定义的大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.由该环系统I描述的大环通过平行合成或组合化学在溶液中容易地制备或固相。它们被设计为与各种特异性生物靶标类型相互作用，例如对G-蛋白偶联受体（GPCR）具有激动作用或拮抗活性，对酶或抗微生物活性的抑制活性。特别地，这些大环化合物显示对亚型1（ECE-1）和/或半胱氨酸蛋白酶组织蛋白酶S（CatS）的内皮素转化酶的抑制活性，和/或作为催产素（OT）受体的拮抗剂，促甲状腺激素释放激素（TRH）受体和/或白三烯B4（LTB4）受体和/或作为铃蟾肽3（BB3）受体的激动剂，和/或显示针对至少一种细菌菌株的抗微生物活性。因此，它们作为各种疾病的药物具有巨大的潜力。

3. 发明申请

WO2022253713A1 TARGETED PROTEIN DEGRADATION USING BIFUNCTIONAL COMPOUNDS THAT BIND UBIQUITIN LIGASE AND TARGET MCL-1 PROTEIN 审中-公开
公开(公告)号：WO2022253713A1
公开(公告)日：2022-12-08
申请号：PCT/EP2022/064481
申请日：2022-05-27
申请人： CAPTOR THERAPEUTICS S.A.
发明人： COTTENS, Sylvain , DREWNIAK-SWITALSKA, Magda , KACZANOWSKA, Katarzyna , TOMCZYK, Tomasz , TRACZ, Andrzej , WALCZAK, Michal , WOJCIK, Karolina
IPC分类号： C07D401/14 , C07D401/04 , C07D471/04 , C07D513/04 , C07D515/18 , A61P35/00 , A61K31/4439
摘要： A compound of formula (I); [MCL-1 ligand moiety] - [linker] - [ligase ligand moiety] (I); or a salt, solvate, hydrate, isomer or prodrug thereof, wherein [MCL-1 ligand moiety] is a compound of Formula (A), Formula (B) or Formula (C), and its use in the treatment of cancer.

4. 发明申请

WO2021032591A1 MACROCYCLIC SULFONYLUREA DERIVATIVES USEFUL AS NLRP3 INHIBITORS 审中-公开
公开(公告)号：WO2021032591A1
公开(公告)日：2021-02-25
申请号：PCT/EP2020/072759
申请日：2020-08-13
申请人： INFLAZOME LIMITED
发明人： COOPER, Matthew , MILLER, David , MACLEOD, Angus , ALANINE, Thomas , THOM, Stephen , SHANNON, Jonathan , CARRILLO ARREGUI, Jokin , ST-GALLAY, Stephen
IPC分类号： C07D515/08 , C07D515/18 , C07D515/22 , A61P29/00 , A61K31/439
摘要： The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyl ureas. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP 3 inhibition.

5. 发明申请

WO2014092100A1 複素環化合物审中-公开
标题翻译：杂环化合物
公开(公告)号：WO2014092100A1
公开(公告)日：2014-06-19
申请号：PCT/JP2013/083140
申请日：2013-12-10
申请人：武田薬品工業株式会社
发明人：小池　竜樹 , 梶田　雄一 , 吉川　真人 , 池田　周平 , 木村　英司 , 蓮井　智章 , 西　俊哉 , 福田　広美
IPC分类号： C07D213/74 , A61K31/444 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/02 , C07D451/04 , C07D487/10 , C07D487/18 , C07D491/18 , C07D515/18 , C12N9/99 , C12N15/09
CPC分类号： C07D498/08 , A61K9/2018 , A61K9/4858 , C07D213/12 , C07D213/72 , C07D213/74 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/02 , C07D451/04 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , C07D487/18 , C07D491/08 , C07D491/18 , C12N9/99
摘要：　本発明は、癲癇、神経変性疾患などの予防または治療剤として有用な化合物またはその塩を提供することを課題とする。本発明は、式：(I)［式中、各記号は本明細書中で定義した通りである。］で表される化合物またはその塩に関する。
摘要翻译：本发明的目的是提供可用作预防或治疗癫痫，神经变性疾病等的药剂的化合物或其盐。本发明涉及由式（I）表示的化合物（在该式中，每个符号如说明书中所定义）或其盐。

6. 发明申请

WO2011045330A1 MACROCYCLIC INTEGRASE INHIBITORS 审中-公开
标题翻译：大环集成抑制剂
公开(公告)号：WO2011045330A1
公开(公告)日：2011-04-21
申请号：PCT/EP2010/065300
申请日：2010-10-13
申请人： Tibotec Pharmaceuticals , THURING, Johannes Wilhelmus J. , BONFANTI, Jean-François , FORTIN, Jérôme Michel Claude
发明人： THURING, Johannes Wilhelmus J. , BONFANTI, Jean-François , FORTIN, Jérôme Michel Claude
IPC分类号： C07D471/18 , C07D498/18 , C07D513/18 , C07D515/18 , A61K31/547 , A61P31/18 , C07D498/22
CPC分类号： C07D513/18 , C07D471/18 , C07D498/18 , C07D498/22 , C07D515/18
摘要： Compound having formula (I), wherein - W is NH-, -N(CH 3 )- or piperazine, - X is a bond, -C(=O)- or S(=O) 2 -, - Y is C 3-7 alkylene, and - Z is NH-C(=O)- or -O-, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.
摘要翻译：具有式（I）的化合物，其中-W是NH-，-N（CH 3） - 或哌嗪，-X是键，-C（= O） - 或S（= O）2 - ， - Y是C 3- 7亚烷基和-Z是NH-C（= O） - 或-O-，及其药学上可接受的盐，其药物制剂和用作HIV抑制剂。

7. 发明申请

WO2008140420A3 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2008140420A3
公开(公告)日：2009-04-30
申请号：PCT/SG2008000179
申请日：2008-05-14
申请人： S BIO PTE LTD , WANG HAISHAN
发明人： WANG HAISHAN
IPC分类号： C07D498/18 , A61K31/529 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D515/18
CPC分类号： C07D498/18 , C07D498/08 , C07D515/18
摘要： The present invention relates to pyrimidine compounds that are useful as agents for the treatment of kinase related disorders such as proliferative disorders. More particularly, the present invention relates to substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of kinase related disorders such as proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
摘要翻译：本发明涉及可用作治疗激酶相关疾病如增殖性疾病的药剂的嘧啶化合物。更具体地，本发明涉及取代的嘧啶化合物，其制备方法，含有这些化合物的药物组合物和这些化合物在治疗增殖性疾病中的用途。这些化合物可用作治疗许多激酶相关病症的药物，例如增殖性疾病，包括肿瘤和癌症以及与激酶相关或与激酶相关的其它病症或病症。

8. 发明申请

WO01051128A1 INHIBITORS OF PRENYL-PROTEIN TRANSFERASE 审中-公开
标题翻译： PRENYL TRANSFERASE抑制剂
公开(公告)号：WO01051128A1
公开(公告)日：2001-07-19
申请号：PCT/US2001/000635
申请日：2001-01-09
IPC分类号： A61P35/00 , C07D498/18 , C07D515/18 , A61K31/4375 , C07D498/14
CPC分类号： C07D498/18 , C07D515/18
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制异戊烯转移酶和致癌Ras蛋白异戊二烯化的拟肽大环化合物。本发明还涉及包含本发明化合物的化学治疗组合物，以及用于抑制异戊烯基蛋白转移酶和致癌Ras蛋白异戊烯化的方法。

9. 发明申请

WO2022076622A2 MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 审中-公开
公开(公告)号：WO2022076622A2
公开(公告)日：2022-04-14
申请号：PCT/US2021/053858
申请日：2021-10-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： MCCARTNEY, Jason , ABELA, Alexander Russell , ABRAHAM, Sunny , ANDERSON, Corey Don , ARUMUGAM, Vijayalaksmi , CHAU, Jaclyn , CLEMENS, Jeremy , CLEVELAND, Thomas , COON, Timothy Richard , DWIGHT, Timothy A. , FANNING, Lev Tyler Dewey , FRIEMAN, Bryan A. , GULEVICH, Anton V. , HADIDA RUAH, Sara Sabina , ISHIHARA, Yoshihiro , KHATUYA, Haripada , KRENITSKY, Paul , MELILLO, Vito , MILLER, Mark Thomas , PARASELLI, Prasuna , PIERRE, Fabrice , SILINA, Alina , TRAN, Joe A. , UY, Johnny , VALDEZ, Lino , VICKERS, Troy , ZHOU, Jinglan
IPC分类号： C07D515/08 , C07D519/00 , C07D515/18 , A61P11/00 , A61K31/529
摘要： This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having core structure (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of CFTR mediated diseases, including cystic fibrosis, using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and combination therapies employing those modulators, and processes and intermediates for making such modulators.

10. 发明申请

WO2014152275A1 DEUTERIUM MODIFIED DERIVATIVES OF THE NS5B POLYMERASE INHIBITOR TMC647055 审中-公开
标题翻译： NS5B聚合酶抑制剂TMC647055的DEUTERIUM改性衍生物
公开(公告)号：WO2014152275A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/027151
申请日：2014-03-14
申请人： CONCERT PHARMACEUTICALS, INC.
发明人： MORGAN, Adam
IPC分类号： C07D515/18 , C07B59/00 , A61K31/55 , A61P31/14
CPC分类号： C07D515/18
摘要： This invention relates to novel NS5B polymerase inhibitors and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of HCV.
摘要翻译：本发明涉及新型NS5B聚合酶抑制剂及其药学上可接受的盐。本发明还提供包含本发明化合物的组合物以及这些组合物在治疗通过施用HCV抑制剂有益治疗的疾病和病症的方法中的用途。

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