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1. 发明申请

WO2019195063A1 AZA-BENZOTHIOPHENE COMPOUNDS AS STING AGONISTS 审中-公开
公开(公告)号：WO2019195063A1
公开(公告)日：2019-10-10
申请号：PCT/US2019/024455
申请日：2019-03-28
申请人： MERCK SHARP & DOHME CORP. , ALTMAN, Michael, D. , CASH, Brandon, D. , CUMMING, Jared, N. , DEMONG, Duane, E. , HAIDLE, Andrew, M. , JEWELL, James, P. , LARSEN, Matthew, A. , LU, Min , OTTE, Ryan, D. , TAOKA, Brandon, M. , TROTTER, Benjamin Wesley , TRUONG, Quang, T.
发明人： ALTMAN, Michael, D. , CASH, Brandon, D. , CUMMING, Jared, N. , DEMONG, Duane, E. , HAIDLE, Andrew, M. , JEWELL, James, P. , LARSEN, Matthew, A. , LU, Min , OTTE, Ryan, D. , TAOKA, Brandon, M. , TROTTER, Benjamin Wesley , TRUONG, Quang, T.
IPC分类号： C07D333/64 , C07D409/06 , C07D409/12
摘要： Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 5 , R 6 , R 8 , R 9 , A, X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.

2. 发明申请

WO2016165007A1 INHIBITORS OF ESTROGEN RECEPTOR ALPHA AND THEIR USE AS THERAPEUTICS FOR CANCER 审中-公开
标题翻译：雌激素受体抑制剂及其作为癌症治疗的用途
公开(公告)号：WO2016165007A1
公开(公告)日：2016-10-20
申请号：PCT/CA2016/000117
申请日：2016-04-18
申请人： THE UNIVERSITY OF BRITISH COLUMBIA
发明人： TCHERKASSOV, Artem , RENNIE, Paul, S. , SINGH, Kriti , MUNUGANTI, Ravi Shashi Nayana
IPC分类号： C07D411/06 , A61K31/166 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/404 , A61K31/4152 , A61K31/4155 , A61P35/00 , C07D333/64 , C07D409/06
CPC分类号： A61K31/166 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/404 , A61K31/4152 , A61K31/4155 , C07D231/30 , C07D317/68 , C07D319/18 , C07D333/64 , C07D333/66 , C07D333/74 , C07D403/06 , C07D409/06
摘要： This invention provides of compounds having structures of Formula A, uses of these compounds for treatment of various indications, including breast cancer, as well as methods of treatment involving these compounds.
摘要翻译：本发明提供了具有式A结构的化合物，这些化合物用于治疗各种适应症（包括乳腺癌）的用途，以及涉及这些化合物的治疗方法。

3. 发明申请

WO2010087306A1 抗神経変性疾患剤审中-公开
标题翻译：抗神经病变药物
公开(公告)号：WO2010087306A1
公开(公告)日：2010-08-05
申请号：PCT/JP2010/050903
申请日：2010-01-25
申请人：株式会社林原生物化学研究所 , 太田人水 , 穐田研志 , 太田恒孝 , 河田敏雄 , 福田恵温
发明人：太田　人水 , 穐田　研志 , 太田　恒孝 , 河田　敏雄 , 福田　恵温
IPC分类号： A61K31/4709 , A61K31/352 , A61K31/381 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/41 , A61K31/4152 , A61K31/4155 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/423 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/47 , A61K31/4706 , A61K31/501 , A61P11/00 , A61P21/02 , A61P21/04 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , C07D209/14 , C07D209/60 , C07D213/34 , C07D215/12 , C07D231/22 , C07D235/20 , C07D261/12 , C07D263/32 , C07D263/56 , C07D277/20 , C07D277/30 , C07D277/36 , C07D277/64 , C07D277/84 , C07D311/74 , C07D333/32 , C07D333/64 , C07D405/06 , C07D413/06 , C07D417/06
CPC分类号： C07D277/22 , C07D209/14 , C07D213/74 , C07D215/06 , C07D215/12 , C07D231/22 , C07D235/20 , C07D261/12 , C07D263/56 , C07D277/28 , C07D277/64 , C07D277/84 , C07D311/74 , C07D333/32 , C07D333/64 , C07D405/06 , C07D413/06 , C07D417/06
摘要：　新規の抗神経変性疾患剤を提供することを課題とし、下記一般式１で表される化合物を有効成分とする抗神経変性疾患剤を提供することにより解決する。【化１】　一般式１におけるＲ１乃至Ｒ３は、それぞれ独立に、水素原子又は適宜の置換基を表し、Ｚ１は複素環を、また、Ｚ２はＺ１と同じか異なる複素環又は芳香環を表し、それらの複素環及び芳香環は置換基を有していてもよい。ｏは０又は１、２のいずれかである整数を表し、ｐは、０又は１のいずれかである整数を表し、ｏが０又は２のとき、ｐは１であり、ｏが１のとき、ｐは０である。ｏが０の場合、Ｒ１、Ｒ２は存在せず、ｐが０の場合、Ｒ３は存在せず、Ｒ２が結合する炭素とＺ２とは一重結合となる。Ｘｌ－は適宜の対アニオンを表し、ｑは１又は２のいずれかである整数を表す。
摘要翻译：公开了一种新型的抗神经变性疾病剂。抗神经变性疾病剂包含由通式（1）表示的化合物作为活性成分。在通式（1）中，R 1至R 3独立地表示氢原子或适当的取代基; Z1表示杂环，Z2表示与由Z1表示的杂环相同或不同的杂环或芳香环，其中杂环和芳环各自可具有取代基; o表示0,1或2的整数，p表示0或1的整数，其中当o为0时p为1，当o为1时p为0，当o为0时，不存在R1和R2 并且当p为0时，R 3不存在，R 2结合的碳原子和Z 2通过单键彼此结合; X1 - 表示适当的抗衡阴离子; q表示1或2的整数。

4. 发明申请

WO2005081960A3 INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B 审中-公开
标题翻译：蛋白酪氨酸磷酸化酶1B的抑制剂
公开(公告)号：WO2005081960A3
公开(公告)日：2006-03-30
申请号：PCT/US2005005722
申请日：2005-02-23
申请人： WYETH CORP , LEE JINBO , KIRINCICH STEVE J , SMITH MICHAEL J , WILSON DOUGLAS P , FOLLOWS BRUCE C , WAN ZHAO-KUI , JOSEPH-MCCARTHY DIANE M , ERBE DAVID V , ZHANG YAN-LING , XU WEIXIN , TAM STEVE Y
发明人： LEE JINBO , KIRINCICH STEVE J , SMITH MICHAEL J , WILSON DOUGLAS P , FOLLOWS BRUCE C , WAN ZHAO-KUI , JOSEPH-MCCARTHY DIANE M , ERBE DAVID V , ZHANG YAN-LING , XU WEIXIN , TAM STEVE Y
IPC分类号： C07D333/52 , A61K31/381 , A61K31/407 , A61K31/4743 , A61K31/55 , C07D333/54 , C07D333/56 , C07D333/58 , C07D333/60 , C07D333/62 , C07D333/64 , C07D333/70 , C07D333/72 , C07D495/04 , C07D498/02
CPC分类号： C07D495/04 , C07D333/70
摘要： Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
摘要翻译：蛋白酪氨酸磷酸酶（PTPase）如PTP1B可以在调节各种细胞反应（如胰岛素信号）方面发挥作用。取代的双环稠合噻吩化合物可以抑制PTP1B，从而诱导更大的胰岛素敏感性。因此，PTP1B抑制可以为PTPase介导的病症例如糖尿病提供替代治疗。

5. 发明申请

WO2005108355A3 DIHYDROBENZOTHIOPHENES 审中-公开
标题翻译：二氢苯并噻
公开(公告)号：WO2005108355A3
公开(公告)日：2006-03-23
申请号：PCT/EP2005004554
申请日：2005-04-28
申请人： MERCK PATENT GMBH , FINSINGER DIRK , ANZALI SOHEILA , FRECH MATTHIAS , GLEITZ JOHANNES , HEISS NINA , HOCK BJOERN , SCHIEMANN KAI , ZENKE FRANK
发明人： FINSINGER DIRK , ANZALI SOHEILA , FRECH MATTHIAS , GLEITZ JOHANNES , HEISS NINA , HOCK BJOERN , SCHIEMANN KAI , ZENKE FRANK
IPC分类号： C07D333/56 , A61K31/381 , A61K31/4535 , A61P35/00 , C07D333/52 , C07D333/54 , C07D333/58 , C07D333/60 , C07D333/64 , C07D409/04
CPC分类号： C07D333/54 , C07D333/56 , C07D333/58 , C07D333/60 , C07D333/64 , C07D409/04
摘要： The invention relates to compounds of formula (I), in which W, R
摘要翻译：式（I）化合物的总结，其中W，R

6. 发明申请

WO2004087061A2 TUBULIN BINDING AGENTS AND CORREPONDING PRODRUG CONSTRUCTS 审中-公开
标题翻译：管IN ING ING ING。。。。。。。。。。。。
公开(公告)号：WO2004087061A2
公开(公告)日：2004-10-14
申请号：PCT/US2004009417
申请日：2004-03-26
申请人： OXIGENE INC , UNIV BAYLOR , PINNEY KEVIN G , MOCHARLA VANI P , CHEN ZHI , GARNER CHARLES M , GHATAK ANJAN , HADIMANI MALLINATH , KESSLER JIMMY , DORSEY JAMES M , EDVARDSON KLAUS , CHAPLIN DAVID J , PREZIOSO JOSEPH , JELINEK CHRISTOPHER
发明人： PINNEY KEVIN G , MOCHARLA VANI P , CHEN ZHI , GARNER CHARLES M , GHATAK ANJAN , HADIMANI MALLINATH , KESSLER JIMMY , DORSEY JAMES M , EDVARDSON KLAUS , CHAPLIN DAVID J , PREZIOSO JOSEPH , JELINEK CHRISTOPHER
IPC分类号： A61K20060101 , A61K31/075 , C07C41/00 , C07C43/215 , C07C43/23 , C07C45/51 , C07C45/64 , C07C49/84 , C07C205/45 , C07C217/84 , C07C217/94 , C07C225/22 , C07D233/54 , C07D307/80 , C07D307/81 , C07D333/56 , C07D333/64 , C07F9/12 , C07F9/18 , C07F9/24 , C07F9/655 , C07F9/6553 , A61K
CPC分类号： C07C43/23 , A61K31/075 , A61K31/66 , C07C43/215 , C07C45/512 , C07C45/64 , C07C45/673 , C07C49/755 , C07C49/84 , C07C205/37 , C07C205/45 , C07C217/84 , C07C217/94 , C07C223/06 , C07C225/22 , C07C237/08 , C07C2602/08 , C07C2602/10 , C07D307/80 , C07D307/81 , C07D333/56 , C07D333/64 , C07F9/12 , C07F9/18 , C07F9/247 , C07F9/65517 , C07F9/655354
摘要： A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.
摘要翻译：已经发现了一组不同的微管蛋白结合剂，其在结构上通常通过能够维持适于分子识别微管蛋白的芳基 - 芳基，伪pi堆叠距离的半刚性分子框架来表征。在酚类或氨基形式中，这些配体可进一步官能化以制备能够显示肿瘤细胞脉管系统的选择性靶向和破坏的磷酸酯，磷酸盐，氨基磷酸酯和其它前体药物。

7. 发明申请

WO0242289A2 PROCESS FOR PREPARING 3-ARYL-BENZO[B]THIOPHENES 审中-公开
标题翻译：制备3-芳基苯并[B]噻吩的方法
公开(公告)号：WO0242289A2
公开(公告)日：2002-05-30
申请号：PCT/US0142940
申请日：2001-11-14
申请人： LILLY CO ELI , LUKE WAYNE DOUGLAS , SANDERSON HEIDI ANN , ZHENG HUA
发明人： LUKE WAYNE DOUGLAS , SANDERSON HEIDI ANN , ZHENG HUA
IPC分类号： C07D333/52 , C07D333/56 , C07D333/64 , C07D409/00 , C07D333/00
CPC分类号： C07D333/64 , C07D333/56
摘要： The present invention relates to a process for preparing a compound of formula (I): which includes cyclodehydrating a compound of formula (II): in the presence of an acid activated clay or acid activated zeolite catalyst and in the presence of a suitable solvent.
摘要翻译：制备式（I）化合物的方法本发明涉及制备式（I）化合物的方法：其包括在酸活化的粘土或酸活化的沸石催化剂存在下并在合适的溶剂存在下将式（II）化合物环化脱水：

8. 发明申请

WO02028815A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO02028815A1
公开(公告)日：2002-04-11
申请号：PCT/US2001/027725
申请日：2001-09-21
IPC分类号： C07D295/02 , A61K31/131 , A61K31/255 , A61K31/277 , A61K31/343 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/426 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/5375 , A61K31/695 , A61P25/00 , A61P25/28 , C07C211/30 , C07C215/42 , C07C217/74 , C07C225/18 , C07C323/32 , C07D205/04 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/22 , C07D215/12 , C07D217/14 , C07D277/64 , C07D295/03 , C07D295/096 , C07D295/10 , C07D295/20 , C07D307/79 , C07D307/80 , C07D307/81 , C07D333/54 , C07D333/56 , C07D333/58 , C07D333/62 , C07D333/64 , C07D333/68 , A61K31/135 , A61K31/46 , C07C217/56
CPC分类号： C07D295/03 , C07C211/30 , C07C215/42 , C07C217/74 , C07C323/32 , C07C2602/42 , C07D215/12 , C07D217/14 , C07D277/64 , C07D295/096 , C07D307/79 , C07D307/80 , C07D307/81 , C07D333/54 , C07D333/56 , C07D333/58
摘要： A compound of the formula in which R and R are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.
摘要翻译：下式的化合物其中R 1和R 2各自为氢或C 1-4烷基，或者R 1和R 2与它们所连接的氮原子一起形成氮杂环丁烷基，吡咯烷基，哌啶基，哌嗪基或吗啉代所述基团任选被1至3个选自C 1-4烷基，羟甲基，C 1-4烷氧基甲基和酰胺基的取代基取代，R 3是萘基，吲哚基，苯并噻吩基，苯并呋喃基，苯并噻唑基，喹啉基或异喹啉基，所述基团任选被取代，并且n是1或2; m为0或1，条件是当m为1时，n为1; 或其盐或酯。

9. 发明申请

WO99015016A1 METHODS FOR REGULATING TRKA EXPRESSION 审中-公开
标题翻译：调节TRKA表达的方法
公开(公告)号：WO99015016A1
公开(公告)日：1999-04-01
申请号：PCT/US1998/019558
申请日：1998-09-18
IPC分类号： C07D333/64 , A61K31/38 , A61K31/4025 , A61K31/445 , A61K31/4535 , A61K31/55 , A61P5/32 , A61P15/12 , A61P25/00 , A61P25/28 , A01N43/12
CPC分类号： A61K31/38 , A61K31/4025 , A61K31/445 , A61K31/4535
摘要： The current invention provides methods for the upregulation of trkA in a mammal, including humans, comprising the administration of an effective amount of a compound of formula (I), wherein R and R are, independently, -H, -CH3, -CO(C1-C6 alkyl), or -COAr, where Ar is optionally substituted phenyl; R is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof. In addition, the current invention provides method to increase the effect of NGF (Nerve Growth Factor), whether the NGF is from endogenous of exogenous sources. Further, the current invention provides methods for maintaining the homeostasis and health of the hippocampus, hypothalamus, and cortex, thus maintaining their biological functions.
摘要翻译：本发明提供了哺乳动物（包括人）中trkA上调的方法，包括施用有效量的式（I）化合物，其中R 1和R 3独立地是-H， -CH 3，-CO（C 1 -C 6烷基）或-COAr，其中Ar是任选取代的苯基; R 2选自吡咯烷，哌啶和六亚甲基亚氨基; 或其药学上可接受的盐或溶剂合物。此外，本发明提供增加NGF（神经生长因子）的作用的方法，NGF是否来自外来源的内源性。此外，本发明提供了维持海马，下丘脑和皮质的稳态和健康的方法，从而保持其生物学功能。

10. 发明申请

WO1997023476A1 HETEROCYCLYL-CONDENSED BENZOYLGUANIDINES, THEIR PRODUCTION AND USE AS INHIBITORS OF THE CELLULAR Na+/H+-ANTIPORTER 审中-公开
标题翻译： HETEROCYCLYLKONDENSIERTE benzoylguanidines，生产及其作为细胞Na + / H +反向转运蛋白的抑制剂
公开(公告)号：WO1997023476A1
公开(公告)日：1997-07-03
申请号：PCT/EP1996005645
申请日：1996-12-16
申请人： MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG , BAUMGARTH, Manfred , GERICKE, Rolf , MINCK, Klaus-Otto , BEIER, Norbert
发明人： MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
IPC分类号： C07D333/64
CPC分类号： C07D333/54 , C07D333/62 , C07D333/64 , C07D333/66 , C07D333/68
摘要： Cyclic sulphones of formula (I) are disclosed, in which: R and R each independently of one another stand for H, A, CF3, CH2F, CHF2, C2F5, Hal, OH, OA, NH2, NHA, NA2, NO2 or CN; X stands for CR R , C=Z, O, S, NH, NA or NR ; Y stands for CR R , C=Z, O, NH, NA, or NR ; Z stands for O, S, NH, NA, NOH, NOA, CH2, CHA or CA2; R , R , R and R each independently of one another stand for H, A, R , Hal, OH, OA, SH, SA, NH2, NHA or NA2, or alternatively, R and R or R and R can together represent a bond, only one such bond being present in each molecule; R and R together can also stand for O-(CH2)2-O or O-(CH2)3-O; R and R each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R stands for phenyl or benzyl which is unsubstituted or single-, double- or triple-substituted by A, OA, NH2, NHA, NA2, F, Cl, Br and/or CF3; and n is 0 or 1. Also disclosed are the physiologically tolerable salts of these compounds. These compounds and their salts have anti-arrhythmic properties and act as inhibitors of the cellular Na+/H+-antiporter.
摘要翻译：式（I）其中，R <1>和R <2>各自独立地是H，A，CF 3，CH 2 F，CHF 2，C 2 F 5，哈尔，OH，OA，NH 2，NHA，NA2，NO 2或CN，X的环状砜 CR <4> - [R <5>，C = Z，O，S，NH，NA或NR <3>中，Y为CR <6> - [R <7>，C = Z，O，NH，NA或NR <3> 中，Z是O，S，NH，NA，NOH，NOA，CH 2，CHA或CA2，R <4>，R <5> - [R <6>和R <7>各自独立地是H，A，R <3>，哈尔，OH，OA，SH，SA，NH 2，NHA或NA2或者R <5>和R <6>或R <7>和R <8>在每一种情况下一起键，在每个分子中，最多只有一个这样的结合可以发生，R <4>和R <5>一起是可替代地-O-（CH 2）2 O或O-（CH2）3-O-，R <8>和R <9>各自独立为H或A，A 碳原子数1〜6的烷基中，Hal是F，Cl，Br或I和R <3>是未取代的或单 - ，二 - 或A，OA，NH 2，NHA，NA2，F，氯，溴三取代的和/或 CF 3 - 取代的苯基或苄基，n是0或1，以及它们的生理学可接受的盐表现出抗心率失常特性，并作为细胞的抑制剂 ARY的Na + / H +反向转运蛋白。

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