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1. 发明申请

WO2019046368A1 INDENE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2019046368A1
公开(公告)日：2019-03-07
申请号：PCT/US2018/048449
申请日：2018-08-29
申请人： MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
发明人： DOLLOFF, Nathan G. , ROBINSON, Reeder M. , REITZ, Allen B. , BIAN, Haiyan
IPC分类号： C07C233/23 , C07C233/41 , C07C235/36
摘要： The present invention relates to compounds of formula (I) :, including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of, for example, cancer.

2. 发明申请

WO2017131221A1 INDANE DERIVATIVES AS MGLUR7 MODULATORS 审中-公开
标题翻译：作为MGLUR7调制器的INDANE衍生物
公开(公告)号：WO2017131221A1
公开(公告)日：2017-08-03
申请号：PCT/JP2017/003078
申请日：2017-01-24
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： GOLDBY, Anne , LIWICKI, Gemma , MACK, Stephen , TEALL, Martin , WHITE, Katy
IPC分类号： C07C233/23 , C07D309/08 , C07D309/14 , C07C271/24 , C07D231/12 , C07D231/14 , C07C311/06 , C07D237/14 , C07C317/30 , C07D239/42 , C07D413/12 , C07C233/41 , C07D261/10 , C07C235/36 , C07D205/04
CPC分类号： C07D309/14 , C07B2200/07 , C07C233/23 , C07C233/41 , C07C235/36 , C07C237/20 , C07C271/24 , C07C311/06 , C07C317/30 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D205/04 , C07D213/61 , C07D213/64 , C07D231/12 , C07D231/14 , C07D237/14 , C07D239/42 , C07D261/10 , C07D277/04 , C07D295/027 , C07D295/135 , C07D305/08 , C07D309/08 , C07D413/12
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 a and R4 b are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of formula (I) are mGluR7 modulators.
摘要翻译：本发明提供式（I）的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4和R 5如上所定义，如说明书中所定义的，它们的制备方法，含有它们的药物组合物以及它们在治疗中的用途。式（I）化合物是mGluR7调节剂。

3. 发明申请

WO2015007388A1 SALTS OF (E)-N-((1S,4S)-4-(DIMETHYLAMINO)-1,4-DIPHENYLCYCLOHEXYL)-N-METHYLCINNAMAMIDE 审中-公开
标题翻译：（E）-N - （（1S，4S）-4-（二甲基氨基）-1,4-二苯基甲酰基）-N-甲基吗啉
公开(公告)号：WO2015007388A1
公开(公告)日：2015-01-22
申请号：PCT/EP2014/001941
申请日：2014-07-16
申请人： GRÜNENTHAL GMBH
发明人： GRUSS, Michael
IPC分类号： C07C233/41 , A61K31/165
CPC分类号： C07C233/41 , C07B2200/13 , C07C55/07 , C07C55/10 , C07C57/145 , C07C57/15 , C07C59/245 , C07C59/255
摘要： The invention relates to a salt of (E)-N-((1s,4s)-4-(dimethylamino)-1,4-diphenylcyclohexyl)-N-methylcinnamamide.
摘要翻译：本发明涉及（E）-N - （（1s，4s）-4-（二甲基氨基）-1,4-二苯基环己基）-N-甲基肉桂酰胺的盐。

4. 发明申请

WO2014149819A1 BICYCLIC ANALGESIC COMPOUNDS 审中-公开
标题翻译：双相分解化合物
公开(公告)号：WO2014149819A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/021038
申请日：2014-03-06
申请人： KALYRA PHARMACEUTICALS, INC.
发明人： BUNKER, Kevin, Duane
IPC分类号： C07C233/23 , C07C233/52 , C07C233/06 , C07C233/41 , C07C211/38 , A61K31/16 , A61K31/221 , A61K31/235 , A61K31/13
CPC分类号： A61K31/16 , A61K9/0014 , A61K9/0019 , A61K31/13 , A61K31/133 , A61K31/14 , A61K31/215 , A61K31/216 , A61K31/22 , A61K31/221 , A61K31/235 , A61K31/24 , A61K45/06 , C07C211/62 , C07C217/52 , C07C233/06 , C07C233/23 , C07C233/41 , C07C233/52 , C07C233/63 , C07C235/74 , C07C2602/38
摘要： Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.
摘要翻译：用于治疗疼痛或发热的止痛化合物，其包括与胺连接的双环戊烷部分，化合物与阿片类止痛药的组合，以及通过施用本文所述的化合物治疗疼痛或发热的方法。

5. 发明申请

WO2009065406A3 NOVEL CYCLIC HYDROCARBON COMPOUNDS FOR THE TREATMENT OF DISEASES 审中-公开
标题翻译：新型环状碳氢化合物治疗疾病
公开(公告)号：WO2009065406A3
公开(公告)日：2009-09-11
申请号：PCT/DK2008000410
申请日：2008-11-20
申请人： LEO PHARMA AS , FENSHOLDT JEF , HAVEZ SOPHIE ELISABETH , NOERREMARK BJARNE
发明人： FENSHOLDT JEF , HAVEZ SOPHIE ELISABETH , NOERREMARK BJARNE
IPC分类号： C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14
CPC分类号： C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译：本发明涉及新的环状烃化合物及其衍生物，其制备方法，所述用作药物的化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法并涉及所述化合物在制造药物中的用途。

6. 发明申请

WO2007017670A1 BICYCLO[2.2.]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES 审中-公开
标题翻译： BICYCLO [2.2。] HEPT-7-YLAMINE DERIVATIVES及其用途
公开(公告)号：WO2007017670A1
公开(公告)日：2007-02-15
申请号：PCT/GB2006/002957
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD. , FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , van NEIL, Monique, Bodil , JENNINGS, Andrew, Stephen, Robert
发明人： FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , van NEIL, Monique, Bodil , JENNINGS, Andrew, Stephen, Robert
IPC分类号： C07C271/38 , C07C219/24 , C07C233/41 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/14 , A61K31/27 , A61K31/381 , A61K31/451 , A61K31/221 , A61K31/352 , A61K31/4704 , A61P29/00
CPC分类号： C07C271/38 , C07C219/24 , C07C235/36 , C07C2602/42 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/06 , C07D409/14
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula(I) wherein A is an oxygen atom or group -N(R 12 )-;(i) R 1 is C 1 -C 6 -alkyl or a hydrogen atom; and R 2 is a hydrogen atom or a group -R 5 , -Z-Y-R 5 -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -CO-R 5 ; or -Z-CO 2 H; and R 3 is a lone pair,or C 1 -C 6 -aIkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R 1 and R 3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R 2 is a hydrogen atom; or a group -R 5 , -Z-Y-R 5 , -Z-NR 9 R 10 , -Z-CO-NR 9 R 10 , -Z-NR 9 -CO-R 5 , or -Z-CO 2 H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R 1 and R 2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R 5 , -Z-Y-R 5 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -CO-R 5 ; or -Z-CO 2 H and R 3 is a lone pair, or C 1 -C 6 -alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R 4 is a group of formula (a), (b), (c) or (d); is an C 1 -C 6 -alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1- C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中A是氧原子或基团-N（R 12） - ;（i）R 1是C 1 - C 6 - 烷基或氢原子; R 2是氢原子或基团-R 5，-ZYR 5 -Z-NR 9， [R ^{10 ; -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 -CO-R ^{5 ; 或-Z-CO 2 H; 且R 3是孤对的或C 1 -C 6 - 烷基，在这种情况下，其所连接的氮原子是季氮并带正电荷; 或（ii）R 1和R 3与它们所连接的氮一起形成杂环烷基环，R 2是氢原子; 或基团-R 5，-ZYR 5，-Z-NR 9，R 10，-Z- CO-NR 9 R 10，-Z-NR 9 -CO-R 5，或-Z- CO 2 H，其中附着的氮原子是季氮并带正电荷; 或（iii）R 1和R 2与它们所连接的氮一起形成杂环烷基环，所述环被基团-YR 5 9，-ZYR 5，-Z-NR 9，R 10， -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 -CO-R ^{5 ; 或-Z-CO 2 H和R 3是孤对的或C 1 -C 6 - 烷基，在这种情况下，其所连接的氮原子是季氮并携带正电荷; R 4是式（a），（b），（c）或（d）的基团。是C 1 -C 6 - 烷基，芳基，芳基 - 稠合环烷基，芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C 1〜 C 1 -C 8 - 烷基） - ，杂芳基（C 1 -C 8 - 烷基） - ，环烷基或杂环烷基，剩余的变量如规范中所定义。}}}}}}}}}

7. 发明申请

WO2023077977A1 秋水仙碱衍生物的制备方法及其用途审中-公开
公开(公告)号：WO2023077977A1
公开(公告)日：2023-05-11
申请号：PCT/CN2022/119478
申请日：2022-09-16
申请人：天津市昕晨投资发展有限公司
发明人：姚晨
IPC分类号： C07C237/08 , C07C233/32 , C07C237/22 , C07C233/41 , A61K31/165 , A61K31/27 , A61P29/00 , A61P35/00
摘要：公开了摘要附图所示的化合物或其药学上可接受的盐，其中，R 1和R 2各自独立地选自由H、甲基、乙基、正丙基、和异丙基所组成的组；且R 3选自由H和甲基所组成的组。公开了摘要附图所示的化合物或其药学上可接受的盐的制备方法。公开了摘要附图所示的化合物在治疗疾病和/或症状的药物中的用途。

8. 发明申请

WO2021184123A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF CORONAVIRUS INFECTION AND RESPIRATORY COMPROMISE 审中-公开
公开(公告)号：WO2021184123A1
公开(公告)日：2021-09-23
申请号：PCT/CA2021/050362
申请日：2021-03-18
申请人： SZEWCZUK, Myron R. , ENCYT TECHNOLOGIES, INC.
发明人： HARLESS, William Warren
IPC分类号： A61K31/351 , A61K31/215 , A61K31/14 , C07C233/41 , C07D309/14
摘要： A method of treating a coronavirus infection involves administering an inhibitor of the Neu1 sialidase – G protein-coupled receptor - Matrix metalloproteinase 9 (Neu1-GPCR-MMP9) signaling platform, in particular administering intravenously or by inhalation to a patient infected with COVID-19 and its variants a therapeutically effective amount of oseltamivir phosphate, preferably in conjunction with the oral administration of aspirin, in order to reduce the symptoms of respiratory compromise and/or prevent Acute Respiratory Distress Syndrome (ARDS).

9. 发明申请

WO2018014111A1 CANCER TREATMENT AND METASTASIS INHIBITION USING AN ANTI-CANCER STEM CELL AGENT IN COMBINATION WITH A NEUL SIALIDASE INHIBITOR OR A CYTOKINE INHIBITOR AFTER PRIMARY CANCER TREATMENT 审中-公开
标题翻译：使用抗癌干细胞剂与原发性癌症治疗后的半胱氨酸唾液酸酶抑制剂或细胞因子抑制剂组合的癌症治疗和转移抑制
公开(公告)号：WO2018014111A1
公开(公告)日：2018-01-25
申请号：PCT/CA2017/050768
申请日：2017-06-22
申请人： HARLESS, William Warren , SZEWCZUK, Myron
发明人： HARLESS, William Warren , SZEWCZUK, Myron
IPC分类号： A61K31/616 , A61K31/155 , A61K31/215 , A61K31/635 , A61K31/7068 , A61K33/42 , A61K39/395 , A61K41/00 , A61P35/00 , A61P35/04 , C07C233/41 , C07C279/26 , C07C69/145 , C07D231/12 , C07H15/252 , C07H19/06 , C07K16/24 , C12Q1/68 , G01N33/48
摘要： There is provided methods, compositions and treatment regimens for treating cancer, or for inhibiting metastasis/recurrence of cancer in a patient using 1) a primary cancer treatment such as chemotherapy, and 2) within 12 to 120 hours post-primary treatment: a) a first therapeutic agent effective against cancer stem cells, such as a cytotoxic chemotherapy; and b) a second therapeutic agent that disrupts a downstream effect of a tissue repair signalling cascade induced by the primary treatment, including an inhibitor of neu- 1 sialidase such as oseltamivir phosphate, or an inhibitor of at least one cytokine associated with stem cell enrichment such as HGF, IL-6, TGF-beta, PGE-2 or PDGF-BB. There is also provided a cancer treatment with chemotherapy agent, such as a checkpoint inhibitor, in combination with either a neuraminidase 1 inhibitor such as oseltamivir phosphate, or a COX-2 inhibitor such as celecoxib, or both.
摘要翻译：提供了用于治疗癌症或用于抑制患者中癌症的转移/复发的方法，组合物和治疗方案，其使用1）原发性癌症治疗如化学疗法，以及2）在12至120之内小时后初级治疗：a）有效抗癌症干细胞的第一种治疗剂，如细胞毒性化疗; 和b）破坏由初级治疗诱导的组织修复信号级联反应的下游效应的第二种治疗剂，包括neu-1唾液酸酶抑制剂如磷酸奥司他韦，或与干细胞富集相关的至少一种细胞因子的抑制剂如HGF，IL-6，TGF-β，PGE-2或PDGF-BB。还提供了用诸如检查点抑制剂之类的化疗剂与诸如磷酸奥司他韦之类的神经氨酸酶1抑制剂或诸如塞来考昔之类的COX-2抑制剂或二者组合的癌症治疗。

10. 发明申请

WO2010093706A3 CHEMICALLY PROGRAMMED VACCINATION 审中-公开
标题翻译：化学游泳
公开(公告)号：WO2010093706A3
公开(公告)日：2011-11-10
申请号：PCT/US2010023770
申请日：2010-02-10
申请人： SCRIPPS RESEARCH INST , BARBAS III CARLOS F
发明人： BARBAS III CARLOS F
IPC分类号： A61K31/216 , A61K31/351 , A61K31/397 , A61K31/4192 , A61K31/439 , A61K31/496 , A61K31/499 , A61K39/00 , C07C233/41 , C07C279/16 , C07D205/08 , C07D309/28 , C07D401/12 , C07D405/12 , C07D405/14 , C07D451/04 , C07D471/04 , C07D471/10
CPC分类号： A61K39/39 , A61K31/216 , A61K31/351 , A61K31/397 , A61K31/4192 , A61K31/439 , A61K31/496 , A61K31/499 , A61K39/0011 , A61K2039/6081 , C07C233/52 , C07C279/16 , C07C2601/16 , C07D205/08 , C07D309/28 , C07D405/12 , C07D405/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07K16/2839 , C07K16/44 , C07K2317/732 , C07K2317/734 , C12N2740/16011
摘要： Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
摘要翻译：本文提供了一种化学程序化接种疫苗的方法。方法包括在受试者中诱导共价结合的多克隆抗体应答并用靶向化合物编程多克隆应答。

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