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51. 发明授权

US08362009B2 Substituted diazepan orexin receptor antagonists 有权
标题翻译：取代的二氮杂菜素食欲肽受体拮抗剂
公开(公告)号：US08362009B2
公开(公告)日：2013-01-29
申请号：US12739304
申请日：2008-10-27
申请人： Jeffrey M. Bergman , Paul J. Coleman , Christopher D. Cox , Anthony J. Roecker
发明人： Jeffrey M. Bergman , Paul J. Coleman , Christopher D. Cox , Anthony J. Roecker
IPC分类号： A61P43/00 , A61K31/551 , C07D243/06
CPC分类号： C07D403/14 , C07D403/04 , C07D413/14 , C07D417/14
摘要： The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的二氮杂环庚烷化合物，其可用于治疗神经性和精神疾病以及食欲素受体参与的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗其中涉及食欲素受体的疾病中的用途。

52. 发明申请

US20090124604A1 4-OXOQUINAZOLIN-3-YL BENZAMIDE DERIVATIVES FOR THE TREATMENT OF CYTOKINE DISEASES 失效
标题翻译：用于治疗细胞因子疾病的4-OXOQUINAZOLIN-3-YL BENZAMIDE DERIVATIVES
公开(公告)号：US20090124604A1
公开(公告)日：2009-05-14
申请号：US11817137
申请日：2006-02-23
申请人： Ian Alun Nash , Jonathan Erle Finlayson , Caroline Rachel Thompson
发明人： Ian Alun Nash , Jonathan Erle Finlayson , Caroline Rachel Thompson
IPC分类号： A61K31/551 , C07D403/14 , A61K31/496 , C07D413/14 , A61P1/00 , A61P11/06 , A61P31/18 , A61P37/02 , A61P17/06 , A61P9/00 , A61K31/5377 , A61K31/517 , C07D243/06
CPC分类号： C07D413/14 , C07D239/91 , C07D413/12
摘要： The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
摘要翻译：本发明涉及式（I）的化合物，其中m为1-2，并且每个R 1为诸如氰基，卤代，三氟甲基杂环基和杂环氧基的基团; R2是三氟甲基或（1-6C）烷基; R3是氢或卤素; R4是异恶唑基; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其用于治疗由细胞因子介导的疾病或医学病症的用途。

53. 发明申请

US20080188465A1 Process of Preparation of Olanzapine Form I 审中-公开
标题翻译：奥氮平制备方法Ⅰ
公开(公告)号：US20080188465A1
公开(公告)日：2008-08-07
申请号：US11928791
申请日：2007-10-30
申请人： Hiren V. Patel , Anup K. Ray , Pramod B. Patel , Mahendra R. Patel
发明人： Hiren V. Patel , Anup K. Ray , Pramod B. Patel , Mahendra R. Patel
IPC分类号： A61K31/551 , C07D243/06 , A61P25/18 , A61P25/22
CPC分类号： C07D495/04
摘要： A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2.3-b][1,5]benzodiazepine, or olanzapine.
摘要翻译：制备2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂或奥氮平的多晶型I的方法。

54. 发明授权

US07056921B2 Substituted chroman derivatives 失效
标题翻译：取代的色原衍生物
公开(公告)号：US07056921B2
公开(公告)日：2006-06-06
申请号：US10714577
申请日：2003-11-13
申请人： Stefan Berg , Martin Nylöf , Svante Ross , Seth-Olov Thorberg
发明人： Stefan Berg , Martin Nylöf , Svante Ross , Seth-Olov Thorberg
IPC分类号： A61K31/497 , C07D403/02 , C07D243/06
CPC分类号： C07D405/12 , C07D311/58 , C07D407/12
摘要： The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1–C6 alkyl; R1 is H, C1–C6 alkyl or C3–C6 cycloalkyl; R3 is C1–C6 alkyl, C3–C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0–4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
摘要翻译：本发明涉及新的具有式（I）的哌啶基或哌嗪基取代的二氢-2H-1-苯并吡喃衍生物化合物，其中X是N或CH; Y是NR 2 CH 2，CH 2 NR 2，NR 2 CO， CONR 2，NR 2 SO 2或NR 2 CONR 2其中R 1，R 2，R 2，R 2， 2是H或C 1 -C 6烷基; R 1是H，C 1 -C 6烷基或C 3 -C 6烷基或C 3 -C 6烷基， SUB>环烷基; R 3是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，环烷基或（CH 2 CH 2）n - 芳基，其中芳基是苯基或含有一个或两个选自N，O和S的杂原子的杂芳环，并且其可以是单 - 或被R 4和/或R 5二取代的二价基团。 n为0-4; 作为（R） - 对映异构体，（S） - 对映异构体或游离碱或其药学上可接受的盐或溶剂合物形式的外消旋体，其制备方法，含有所述治疗活性化合物的药物组合物和所述活性化合物。

55. 发明授权

US5712274A Thienotriazolodiazepine compounds and their pharmaceutical use 失效
标题翻译：噻吩并三唑并噻嗪类化合物及其药物用途
公开(公告)号：US5712274A
公开(公告)日：1998-01-27
申请号：US413444
申请日：1995-03-30
申请人： Hiroyuki Sueoka , Shuji Ehara , Haruhito Kobayashi , Takeshi Arichi , Hirotsugu Komatsu
发明人： Hiroyuki Sueoka , Shuji Ehara , Haruhito Kobayashi , Takeshi Arichi , Hirotsugu Komatsu
IPC分类号： C07D495/14 , A61K31/55 , C07D243/06
CPC分类号： C07D495/14
摘要： Thienotriazolodiazepine compounds of the formula (1) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof, and pharmaceutical use thereof. The compounds of the present invention are useful as preventive and therapeutic drugs for inflammatory diseases and allergic diseases, in which cell adhesion is involved.
摘要翻译：式（1）的噻吩并三唑并噻嗪类化合物其中每个符号如说明书中所定义，其药学上可接受的盐及其药物用途。本发明的化合物可用作涉及细胞粘附的炎性疾病和过敏性疾病的预防和治疗药物。

56. 发明授权

US3917629A Certain 2-oxy-5-phenyl-6-aza-7-chloro-1,2-dihydro-3H-1,4-benzodiazepines 失效
标题翻译：某些2-氧基-5-苯基-6-氮杂-7-氯-1,2-二氢-3H-1,4-苯并二氮杂
公开(公告)号：US3917629A
公开(公告)日：1975-11-04
申请号：US46312974
申请日：1974-04-22
申请人： DEGUSSA
发明人： VON BEBENBURG WALTER , OFFERMANNS HERIBERT
IPC分类号： A61K31/55 , A61P25/20 , A61P29/00 , C07D471/04 , C07D243/06
CPC分类号： C07D471/04 , Y10S514/916
摘要： There are produced 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula:

wherein: R1 is hydrogen, a lower alkyl group, a lower alkenyl group, a cycloalkyl group, a hydroxy lower alkyl group a lower alkoxy lower alkyl group, an amino-alkyl group, mono or dialkyl aminoalkyl or a 5 to 7 membered heterocyclic ring having 1 to 2 nitrogen atoms or 1 nitrogen atom and 1 oxygen atom in the ring attached to alkyl; R2 is hydrogen, lower alkyl or lower alkoxy lower alkyl; R3 is hydrogen, lower alkyl or lower alkoxy; and R4 is hydrogen or halogen and pharmaceutically acceptable salts thereof. The compounds have pharmacodynamic properties including psychosedative and especially anxiolytic properties as well as spasmolytic and antiphlogistic action.
摘要翻译：产生下式的6-氮杂-1,2-二氢-3H-1,4-苯并二氮杂：R1OR2 || N-CH角度CH-R3 I Cl | C = N | | R4其中：

57. 发明申请

US20200223845A1 NOVEL VIRAL REPLICATION INHIBITORS 审中-公开
公开(公告)号：US20200223845A1
公开(公告)日：2020-07-16
申请号：US16798859
申请日：2020-02-24
申请人： Katholieke Universiteit Leuven
发明人： Dorothée Bardiot , Gunter Carlens , Kai Dallmeier , Suzanne Kaptein , Mohamed Koukni , Arnaud Marchand , Johan Neyts , Wim Smets
IPC分类号： C07D471/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D223/04 , C07D231/12 , C07D333/22 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D261/08 , C07D207/06 , C07D265/30 , C07D267/10 , C07D275/02 , C07D498/04 , C07D279/12 , A61K31/415 , C07D409/12 , A61K31/34 , A61K31/381 , A61K31/40 , C07D207/323 , C07D403/06 , C07D405/12 , C07D407/06 , C07D271/04 , C07D285/06 , A61K31/4439 , C07D403/12 , C07D243/06 , A61K31/437 , C07D211/06 , A61K45/06 , C07D513/04 , C07D407/04 , C07D307/46 , C07D207/335 , C07D211/16 , C07D241/04 , C07D243/08 , C07D263/32 , C07D271/08 , C07D277/28 , C07D285/10 , C07D307/52 , C07D413/12 , C07D487/04
摘要： The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.

58. 发明授权

US08835421B2 Benzimidazole linked pyrrolo[2,1-c[1,4] benzodiazepine hybrids as potential antitumour agents and process for the preparation thereof 有权
标题翻译：苯并咪唑连接的吡咯并[2,1-c [1,4]苯并二氮杂作为潜在的抗肿瘤剂及其制备方法
公开(公告)号：US08835421B2
公开(公告)日：2014-09-16
申请号：US12921594
申请日：2008-10-31
申请人： Ahmen Kamal , Pogula Praveen Kumar , Bobburi Naga Seshadri , Kokkonda Sreekanth
发明人： Ahmen Kamal , Pogula Praveen Kumar , Bobburi Naga Seshadri , Kokkonda Sreekanth
IPC分类号： A61K31/5517 , C07D243/06 , C07D403/12
CPC分类号： C07D403/12 , A61K31/5517 , C07D243/06
摘要： The present invention provides a compounds of general formula (8), (11) and (14), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula (8), (11) and (14).
摘要翻译：本发明提供通式（8），（11）和（14）的化合物，其可用作抗人肿瘤细胞系的潜在抗肿瘤剂。本发明还提供了制备通式（8），（11）和（14）的吡咯并[2,1-c] [1,4]苯并二氮杂杂化物的方法。

59. 发明申请

US20090253685A1 Product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent 审中-公开
标题翻译：包含至少一种Cdc25磷酸酶抑制剂与至少一种其它抗癌剂组合的产品
公开(公告)号：US20090253685A1
公开(公告)日：2009-10-08
申请号：US12154319
申请日：2008-05-22
申请人： Gregoire Provost , Marie-Christine Brezak Pannetier , Christian Diolez
发明人： Gregoire Provost , Marie-Christine Brezak Pannetier , Christian Diolez
IPC分类号： A61K31/551 , C07D243/06 , A61P35/00
CPC分类号： A61K45/06 , C07D519/00
摘要： A subject of the invention is a product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent for a therapeutic use which is simultaneous, separate or spread over time in the treatment of cancer.According to the invention, the other anti-cancer agent is preferably chosen from: analogues of DNA bases such as 5-fluorouracil; Type I and/or II topoisomerase inhibitors such as for example camptothecin and its analogues, doxorubicin or armsacrine; compounds interacting with the cell spindle such as for example paclitaxel (Taxol); compounds acting on the cytoskeleton such as vinblastine; inhibitors of the transduction of the signal passing through the heterotrimeric G proteins; prenyltransferase inhibitors, and in particular farnesyltransferase inhibitors; cyclin-dependent kinase (CDKs) inhibitors; alkylating agents such as cisplatin; antagonists of folic acid such as methotrexate; and inhibitors of the synthesis of DNA and cell division cell such as mitomycin C. A further subject of the invention is (1R)-1-[({(2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine, or a pharmaceutically acceptable salt thereof, useful as an anticancer agent.
摘要翻译：本发明的主题是包含至少一种Cdc25磷酸酶抑制剂与用于治疗用途的至少一种其他用于治疗用途的抗癌剂的产品，其在治疗癌症中随时间同时，分离或扩散。根据本发明，其它抗癌剂优选选自：DNA碱基的类似物，例如5-氟尿嘧啶; I型和/或II型拓扑异构酶抑制剂，例如喜树碱及其类似物，多柔比星或武arms嗪; 与细胞纺锤体相互作用的化合物，例如紫杉醇（紫杉醇）; 作用于细胞骨架的化合物如长春花碱; 通过异源三聚体G蛋白的信号转导的抑制剂; 异戊烯转移酶抑制剂，特别是法呢基转移酶抑制剂; 细胞周期蛋白依赖性激酶（CDKs）抑制剂; 烷化剂如顺铂; 叶酸拮抗剂如甲氨蝶呤; 以及合成DNA和细胞分裂细胞例如丝裂霉素C的抑制剂。本发明的另一个主题是（1R）-1 - [（{（2R）-2-氨基-3 - [（8S）-8-（环己基甲基）-2-苯基-5,6-二氢咪唑并[1,2-a]吡嗪-7（8H） - 基] -3-氧代丙基}二硫代）甲基] -2 - [（8S） -2-苯基-5,6-二氢咪唑并[1,2-a]吡嗪-7（8H） - 基] -2-氧代乙基胺或其药学上可接受的盐，可用作抗癌剂。

60. 发明申请

US20070287697A1 Cgrp Receptor Antagonists 有权
标题翻译： Cgrp受体拮抗剂
公开(公告)号：US20070287697A1
公开(公告)日：2007-12-13
申请号：US11665520
申请日：2005-10-12
申请人： Daniel Paone , Anthony Shaw , Craig Potteiger
发明人： Daniel Paone , Anthony Shaw , Craig Potteiger
IPC分类号： A61K31/55 , A61K31/44 , A61K31/445 , A61K31/551 , A61P43/00 , C07D213/00 , C07D237/26 , C07D241/36 , C07D267/02 , C07D243/06 , C07D239/70 , C07D223/02 , C07D211/00 , A61K31/553 , A61K31/4985 , A61K31/519
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译：式（I）和式（II）化合物（其中R 1，R 2，R 4，A，B，W， X，Y和Z如本文所定义）可用作CGRP受体的拮抗剂，可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

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