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1. 发明申请

US20230044112A1 HEPATITIS B CORE PROTEIN MODULATORS 有权
公开(公告)号：US20230044112A1
公开(公告)日：2023-02-09
申请号：US17140800
申请日：2021-01-04
申请人： Assembly Biosciences, Inc. , INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
发明人： William W. Turner, JR. , Lee D. Arnold , Hans Maag , Leping Li , Mark G. Bures , Simon Nicolas Haydar , Samson Francis
IPC分类号： C07D417/12 , C07D403/12 , A61K45/06 , C07D401/12 , C07D413/12 , C07D417/14 , C07D453/02 , C07D471/04 , A61P31/20 , C07D243/38 , C07D267/20 , C07D281/16
摘要： The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

2. 发明申请

US20210101872A1 C-ABL TYROSINE KINASE INHIBITORY COMPOUND EMBODIMENTS AND METHODS OF MAKING AND USING THE SAME 有权
公开(公告)号：US20210101872A1
公开(公告)日：2021-04-08
申请号：US16976012
申请日：2019-03-08
申请人： The USA, as represented by the Secretary, Dept. of Health and Human Services , Pontificia Universidad Católica de Chile
发明人： Juan J. Marugan , Marc Ferrer , Noel T. Southall , Andres E. Dulcey , Xin Hu , Christopher R. Dextras , Daniel C. Talley , Alejandra Alvarez , Silvana Zanlungo , Rommy M. Von Bernhardi
IPC分类号： C07D243/38 , C07D267/20 , C07F7/08 , C07D281/16 , C07D267/18 , C07C227/22 , C07C201/12 , C07C319/14 , C07D401/04 , C07D403/04 , C07D413/10 , C07F5/02 , C07D413/04 , C07D471/04 , C07D487/04 , C07D413/14 , C07D417/04 , A61P33/06 , A61P25/28 , A61P25/08 , A61P35/02 , A61K31/554 , A61K31/5513 , A61K31/553
摘要： Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

3. 发明授权

US10377748B2 Hepatitis B core protein modulators 有权
公开(公告)号：US10377748B2
公开(公告)日：2019-08-13
申请号：US15760284
申请日：2016-09-15
申请人： Assembly Biosciences, Inc. , INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
发明人： William Turner , Lee Daniel Arnold , Hans Maag , Leping Li , Mark Bures , Simon Haydar , Samson Francis
IPC分类号： C07D417/12 , A61P31/20 , C07D403/12 , A61K45/06 , C07D401/12 , C07D413/12 , C07D417/14 , C07D453/02 , C07D471/04 , C07D243/38 , C07D267/20 , C07D281/16
摘要： The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

4. 发明申请

US20180362543A1 HIV REPLICATION INHIBITOR 审中-公开
公开(公告)号：US20180362543A1
公开(公告)日：2018-12-20
申请号：US16110697
申请日：2018-08-23
申请人： Shionogi & Co., Ltd.
发明人： Kenji TOMITA , Yoshiyuki TAODA , Tsutomu IWAKI , Takashi KAWASUJI , Toshiyuki AKIYAMA , Shuichi SUGIYAMA , Yoshinori TAMURA , Masafumi IWATSU
IPC分类号： C07D498/06 , C07D285/36 , C07D405/14 , C07D243/04 , C07D491/06 , C07D221/18 , C07D291/08 , C07D225/08 , C07D279/02 , C07D209/80 , C07D243/12 , C07D405/04 , C07D237/36 , C07D513/06 , C07D243/38 , C07D267/20 , C07D223/18 , C07D335/10 , C07D471/10 , C07D498/04 , C07D413/04 , C07D241/44 , C07D409/04 , C07D221/12 , C07D471/04 , C07D281/02 , C07D265/34 , C07D275/06 , C07D491/056 , C07D273/01 , C07D495/14 , C07D495/04 , C07D487/04 , C07D513/04 , C07D401/04 , C07D471/06 , C07D311/80
摘要： The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R1 is substituted or unsubstituted alkyl etc.; R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R4 is a hydrogen atom etc.; R6 is substituted or unsubstituted alkyl etc.

5. 发明授权

US09193749B2 Dibenzo[b,f][1,4]oxazepin-11-yl-N-hydroxybenzamides as HDAC inhibitors 有权
标题翻译：二苯并[b，f] [1,4]氧氮杂-11-基-N-羟基苯甲酰胺作为HDAC抑制剂
公开(公告)号：US09193749B2
公开(公告)日：2015-11-24
申请号：US13767478
申请日：2013-02-14
申请人： Forum Pharmaceuticals, Inc. , MethylGene, Inc.
发明人： Robert Deziel , Silvana Leit , Patrick Beaulieu , Yves Andre Chantigny , John Mancuso , Pierre Tessier , Gideon Shapiro , Richard Chesworth , David Smil
IPC分类号： C07D491/00 , C07H13/10 , C07D209/02 , C07D209/08 , C07D209/52 , C07D209/94 , C07D221/12 , C07D223/16 , C07D223/20 , C07D223/22 , C07D223/26 , C07D223/28 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/24 , C07D243/38 , C07D265/38 , C07D267/14 , C07D267/18 , C07D267/20 , C07D279/22 , C07D279/26 , C07D285/36 , C07D291/08 , C07D313/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/06 , C07D413/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D487/14 , C07D491/08 , C07D495/04 , C07D498/04 , C07D513/04 , C07D281/16 , C07D295/155
CPC分类号： C07D498/04 , C07C259/06 , C07C259/10 , C07D209/02 , C07D209/08 , C07D209/52 , C07D209/94 , C07D221/12 , C07D223/16 , C07D223/20 , C07D223/22 , C07D223/24 , C07D223/26 , C07D223/28 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/24 , C07D243/38 , C07D265/38 , C07D267/14 , C07D267/18 , C07D267/20 , C07D279/22 , C07D279/26 , C07D281/16 , C07D285/36 , C07D291/08 , C07D295/155 , C07D313/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/06 , C07D413/12 , C07D471/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D487/08 , C07D487/14 , C07D491/08 , C07D495/04 , C07D513/04 , C07H13/10
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地说，本发明提供式（I）化合物，其中Q，J，L和Z如说明书中所定义。

6. 发明授权

US5869483A Tricyclic benzazepine vasopressin antagonists 失效
标题翻译：三环苯并氮平加压素拮抗剂
公开(公告)号：US5869483A
公开(公告)日：1999-02-09
申请号：US639014
申请日：1996-04-24
申请人： Jay Donald Albright , Fuk-Wah Sum
发明人： Jay Donald Albright , Fuk-Wah Sum
IPC分类号： C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/55 , C07D223/16
CPC分类号： C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
摘要翻译：在V1和/或V2受体上表现出拮抗剂活性并表现出体内血管加压素拮抗剂活性的通式I的三环化合物：本文定义的式I化合物，其用于治疗特征在于过量肾脏重吸收水的疾病的方法，以及这些化合物的制备方法。

7. 发明授权

US5846969A Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives 失效
标题翻译：三环杂环磺酰胺和磺酸酯衍生物
公开(公告)号：US5846969A
公开(公告)日：1998-12-08
申请号：US873033
申请日：1997-06-11
申请人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
IPC分类号： C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D498/04 , C07D513/04 , C07F7/18 , A61K31/55 , A61K31/505 , C07D487/00 , C07D471/00
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).
摘要翻译：（I）表示的磺酰胺衍生物或磺酸酯衍生物：（I）{G表示芳香族5-或6-元环; L表示O或-N（R 1） - （R 1表示氢或低级烷基）; （D）环A和B各自表示不饱和的5-或6-元环; Y表示O，S（O）n，C（R3）（R4），C（O），N（R5），CH（R6）CH（R7），C（R8）= C（R9））C（O），N = C（R 11），OCH（R 12），S（O）n CH（R 13）或N（R 14）CH（R 15）。

8. 发明授权

US5846968A N-substituted azaheterocyclic carboxylic acids and esters 失效
标题翻译： N-取代的氮杂环状羧酸和酯
公开(公告)号：US5846968A
公开(公告)日：1998-12-08
申请号：US863746
申请日：1997-05-27
申请人： Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Henrik Sune Andersen , Rolf Hohlweg , Peter Madsen , Uffe Bang Olsen
发明人： Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Henrik Sune Andersen , Rolf Hohlweg , Peter Madsen , Uffe Bang Olsen
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/55 , A61P3/08 , A61P3/10 , A61P3/14 , A61P25/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07D211/60 , C07D401/06 , C07D413/06 , C07D267/20 , C07D281/16
CPC分类号： C07D401/06 , C07D211/60 , C07D413/06
摘要： The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
摘要翻译：本发明涉及新的N-取代的氮杂杂环羧酸及其酯，其中取代的烷基链形成N-取代基或其盐的一部分，其制备方法，含有它们的组合物及其用于临床的用途治疗C型纤维通过引起神经源性疼痛或炎症而发挥病理生理作用的疼痛，痛觉过敏和/或炎性病症。

9. 发明授权

US5686445A Pyridobenzoxazepine and pyridobenzothiazepine vasopressin antagonists 失效
标题翻译：吡啶并苯并西泮和吡啶并苯并硫氮平加压素拮抗剂
公开(公告)号：US5686445A
公开(公告)日：1997-11-11
申请号：US637908
申请日：1996-04-25
申请人： Jay Donald Albright , Xuemei Du
发明人： Jay Donald Albright , Xuemei Du
IPC分类号： C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/55
CPC分类号： C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
摘要翻译：在V1和/或V2受体上表现出拮抗剂活性并表现出体内血管加压素拮抗剂活性的通式I的三环化合物：本文定义的式I化合物，其用于治疗特征在于过量肾脏重吸收水的疾病的方法，以及这些化合物的制备方法。

10. 发明授权

US5602121A Alkyl-substituted compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的烷基取代的化合物
公开(公告)号：US5602121A
公开(公告)日：1997-02-11
申请号：US354793
申请日：1994-12-12
申请人： Jian-Min Fu
发明人： Jian-Min Fu
IPC分类号： C07D267/20 , A61K31/55 , C07D413/04 , C07D417/04
CPC分类号： C07D267/20
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 . . . is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2。。。选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; Y选自N和CH; R 1表示C 1-4烷基; n为0,1或2; q为1或2; 并且Z是任选地被OH，卤素，C 1-4烷基或C 1-4烷氧基取代并任选地引入选自O，N和S的杂原子的C 5-10-10烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

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