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11. 发明授权

US4252810A 9,10-Dihydro-4H-benzo[4,5]cyclohepta [1,2-b]thiophen-4,9-imines 失效
标题翻译： 9,10-二氢-4H-苯并[4,5]环庚并[1,2-b]噻吩-4,9-亚胺
公开(公告)号：US4252810A
公开(公告)日：1981-02-24
申请号：US960811
申请日：1978-11-15
申请人： Paul S. Anderson , Ben E. Evans
发明人： Paul S. Anderson , Ben E. Evans
IPC分类号： A61K31/435 , A61P21/02 , A61P25/20 , A61P43/00 , C07D333/80 , C07D495/18 , A61K31/38 , A61K31/44 , C07D495/12
CPC分类号： C07D333/80
摘要： 9,10-Dihydro-4H-benzo[4,5]cyclohepta [1,2-b]thiophen-4,9-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease.
摘要翻译： 9,10-二氢-4H-苯并[4,5]环庚并[1,2-b]噻吩-4,9-亚胺，其衍生物和药学上可接受的盐可用作抗焦虑剂，作为肌肉松弛剂和用于治疗锥体外系疾病如帕金森病。

12. 发明授权

US3755357A 2,3 - dihydro - 5-trifluoromethyl-1h-di-benzo(2,3:6,7)thiepino(4,5-c)pyrroles as cns-depressants 失效
标题翻译： 2,3-二氢-5-三氟甲基-1H-二苯并（2,3：6,7）噻吩并（4,5-C）吡啶作为CNS-抑制剂
公开(公告)号：US3755357A
公开(公告)日：1973-08-28
申请号：US3755357D
申请日：1971-05-19
申请人： CIBA GEIGY CORP
发明人： SCHINDLER W , GYSIN L
IPC分类号： C07D513/04 , A61K31/38 , A61K31/40 , C07D337/14 , C07D495/04 , C07D495/12 , C07D27/36
CPC分类号： C07D495/04 , A61K31/38 , A61K31/40 , C07C323/00 , C07D337/14 , Y10S514/966
摘要： COMPOUNDS OF THE CLASS 2,3-DIHYDRO-5-(TRIFLUOROMETHYL)-1H-DIBENZO(2,3:6,7)THIEPINO(4,5-C)PYRROLE AND ITS 2-ALKYL-DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS HAVE A DEPRESSANT EFFECT ON THE CENTRAL NERVOUS SYSTEM, THEY CAN BE PREPARED FROM 10,11-BIS(BROMOMETHYL)-2-(TRIFLUOROMETHYL)-DIBENZO(B,F)THIEPIN AND A PRIMARY AMINE; THE COMPOUNDS ARE ACTIVE INGREDIENTS OF PHARMACEUTICAL COMPOSITIONS.

13. 发明申请

US20180237454A1 COMPOSITIONS AND METHODS FOR TREATING NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS 审中-公开
公开(公告)号：US20180237454A1
公开(公告)日：2018-08-23
申请号：US15886559
申请日：2018-02-01
申请人： Dana-Farber Cancer Institute, Inc.
发明人： James Elliott Bradner , Jun Qi
IPC分类号： C07D495/14 , C07D495/12 , C07D487/04 , A61K31/5517 , A61K31/551 , C07D519/00
CPC分类号： C07D495/14 , A61K31/551 , A61K31/5517 , A61P35/00 , C07D487/04 , C07D495/12 , C07D519/00 , Y02A50/411
摘要： The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

14. 发明授权

US09908895B2 Tricyclic fused thiophene derivatives as JAK inhibitors 有权
公开(公告)号：US09908895B2
公开(公告)日：2018-03-06
申请号：US14873078
申请日：2015-10-01
申请人： Incyte Corporation , Incyte Holdings Corporation
发明人： Yun-Long Li , Wenyu Zhu , Song Mei , Joseph Glenn
IPC分类号： C07D495/12 , C07D495/14 , A61K31/437
CPC分类号： C07D495/14 , A61K31/437 , C07D495/12
摘要： The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

15. 发明授权

US09533996B2 Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6h)-ones 有权
标题翻译：治疗噻吩 - ，呋喃和吡啶稠合的偶氮嘧啶-5-（6h） - 酮
公开(公告)号：US09533996B2
公开(公告)日：2017-01-03
申请号：US14853856
申请日：2015-09-14
申请人： Dart Neuroscience (Cayman) Ltd.
发明人： Bryan Branstetter , James Breitenbucher , Brian Dyck , Laurent Gomez , Andrew Richard Hudson , Tami Jo Marrone , Marco Peters , Troy Vickers , Michael Weinhouse
IPC分类号： C07D495/14 , C07D495/22 , C07D471/14 , C07D471/22 , C07D487/14 , C07D487/22 , C07D491/22 , C07D498/08 , C07D491/147 , C07D491/107 , C07D519/00 , C07D495/12
CPC分类号： A61K31/553 , A61K31/519 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/55 , A61K31/551 , C07D471/14 , C07D487/14 , C07D491/107 , C07D491/147 , C07D491/22 , C07D495/12 , C07D495/14 , C07D495/22 , C07D498/08 , C07D519/00
摘要： Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
摘要翻译：本文描述了式I和式II的化合物，其合成方法，包含该化合物的组合物，以及该化合物和组合物在治疗众多疾病和病症（包括与CNS疾病和病症相关的认知缺陷）中的用途。

16. 发明授权

US08586764B2 Organic dyes and preparation method thereof and dye-sensitized solar cells 失效
标题翻译：有机染料及其制备方法和染料敏化太阳能电池
公开(公告)号：US08586764B2
公开(公告)日：2013-11-19
申请号：US13383308
申请日：2010-07-09
申请人： Peng Wang , Yupeng Wang , Ning Cai , Wangdong Zeng , Mingfei Xu , Jingyuan Liu
发明人： Peng Wang , Yupeng Wang , Ning Cai , Wangdong Zeng , Mingfei Xu , Jingyuan Liu
IPC分类号： C07F7/02 , C07D491/12 , C07D495/12 , C07D409/14 , C07D411/14
CPC分类号： C09B57/008 , H01G9/2031 , H01G9/2059 , H01L51/0061 , H01L51/0074 , H01L51/0094 , Y02E10/542 , Y02E10/549
摘要： An organic dye and preparation method thereof and dye-sensitized solar cells using this organic dye are provided. The structure of the organic dye molecule is donor-conjugated unit(s)-acceptor. The organic dye with broad spectrum response and high molar-absorption coefficient is obtained by modifying the structure by using various conjugated unit(s) in combination with donor and acceptor. The conditions of preparation of the organic dye are mild and the yield is high, and the organic dye can be used for highly effective dye-sensitized solar cells.
摘要翻译：提供有机染料及其制备方法和使用该有机染料的染料敏化太阳能电池。有机染料分子的结构是供体共轭单位 - 受体。具有广谱响应和高摩尔吸光系数的有机染料通过使用各种共轭单元与供体和受体结合来改变结构而获得。有机染料的制备条件温和，产率高，有机染料可用于高效染料敏化太阳能电池。

17. 发明申请

US20070232799A1 PROCESS FOR PREPARING 6-ARYL-4H-S-TRIAZOLO[3,4-c]-THIENO[2,3-e]-1,4-DIAZEPINES 审中-公开
标题翻译：制备6-氨基-4H-哒嗪并[3,4-c] - 噻吩并[2,3-e] -1,4-二氮杂的方法
公开(公告)号：US20070232799A1
公开(公告)日：2007-10-04
申请号：US11749971
申请日：2007-05-17
申请人： Werner Belzer , Ralf Lock
发明人： Werner Belzer , Ralf Lock
IPC分类号： C07D495/12
CPC分类号： C07D495/04 , C07D495/14
摘要： An improved process for preparing 6-aryl-4H-s-triazolo[3,4-c]-thieno[2,3-e]-1,4-diazepines of formula I, wherein: R1 is a hydrogen or halogen atom or a C1-C6 alkyl group, R2 is a hydrogen or halogen atom or a C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C6 cycloalkyl group or a 5- or 6-membered oxygen-, sulphur- or nitrogen-containing heterocyclic group which may optionally be substituted at the nitrogen atom by a C1-C3 alkyl group, and R3 is a hydrogen or halogen atom.
摘要翻译：用于制备式I的6-芳基-4H-三唑并[3,4-c]噻吩并[2,3-e] -1,4-二氮杂的改进方法，其中：R 1 >是氢或卤素原子或C 1 -C 6烷基，R 2是氢或卤素原子或C 1 -C 6烷基， C 1 -C 6烷基，C 1 -C 6羟烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6 - C 6环烷基或可以任选地在氮原子上被C 1〜N取代的5-或6-元的含氧，含硫或含氮杂环基团， -C 3烷基，R 3是氢或卤素原子。

18. 发明授权

US6110914A Spiroazabicyclic heterocyclic compounds 有权
标题翻译：螺环双环杂环化合物
公开(公告)号：US6110914A
公开(公告)日：2000-08-29
申请号：US171983
申请日：1998-10-29
申请人： Eifion Phillips , Robert Mack , John Macor , Simon Semus
发明人： Eifion Phillips , Robert Mack , John Macor , Simon Semus
IPC分类号： C07D491/22 , A61K20060101 , A61K31/395 , A61K31/435 , A61K31/4353 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/438 , A61K31/439 , A61K31/44 , A61K31/444 , A61K31/4738 , A61K31/4745 , A61K31/496 , A61K31/5377 , A61K31/695 , A61P20060101 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P43/00 , C07D20060101 , C07D491/12 , C07D491/20 , C07D495/12 , C07D499/21 , C07F5/02 , C07F7/18 , C07P499/21
CPC分类号： C07D491/22
摘要： A compound of formula ##STR1## wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H.sub.2 or F.sub.2 ;A is N or C(R.sup.2); G is N or C(R.sup.3); D is N or C(R.sup.4);with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;R.sup.1 is hydrogen or C.sub.1 to C.sub.4 alkyl;R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 ; R.sup.5 and R.sup.6 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, C(O)R.sup.7, C(O)NHR.sup.8, C(O)OR.sup.9, SO.sub.2 R.sup.10 or may together be (CH.sub.2).sub.j Q(CH.sub.2).sub.k where Q is O, S, NR.sup.11, or a bond; j is 2 to 7, k is 0 to 2; R.sup.7, R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are independently C.sub.1 -C.sub.4 alkyl, aryl, or heteroaryl, or an enantiomer thereof,and the pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
摘要翻译： PCT No.PCT / SE98 / 01364 Sec。 371日期：1998年10月29日第 102（e）1998年10月29日PCT PCT 1998年7月10日PCT公布。公开号WO99 / 03859 日期1999年1月28日其中n为0或1的下式化合物： m为0或1; p为0或1; X是氧或硫; Y是CH，N或NO; W是氧，H2或F2; A为N或C（R2）; G为N或C（R3）; D是N或C（R4）; 条件是A，G和D中不超过一个为氮，但Y，A，G和D中的至少一个为氮或NO; R1是氢或C1-C4烷基; R2，R3和R4独立地是氢，卤素，C1-C4烷基，C2-C4烯基，C2-C4炔基，芳基，杂芳基，OH，OC1-C4烷基，CO2R1，-CN，-NO2，-NR5R6， CF 3，-OSO 2 CF 3或R 2，R 3或R 3和R 4分别可以一起形成分别含有0和2个氮原子之间的分别为A和G或G和D的六元芳族或杂芳族环，并被一个 C 1 -C 4烷基，C 2 -C 4烯基，C 2 -C 4炔基，芳基，杂芳基，OH，OC 1 -C 4烷基，CO 2 R 1，-CN，-NO 2，-NR 5 R 6 - CF 3，-OSO 2 CF 3; R 5和R 6独立地是氢，C 1 -C 4烷基，C（O）R 7，C（O）NHR 8，C（O）OR 9，SO 2 R 10或可以一起为（CH 2）j Q（CH 2） NR11，或债券; j为2〜7，k为0〜2; R 7，R 8，R 9，R 10和R 11独立地为C 1 -C 4烷基，芳基或杂芳基，或其对映异构体及其药学上可接受的盐，其制备方法，含有它们的组合物及其在治疗中的用途，在治疗或预防精神病和智力障碍。

19. 发明授权

US5935969A Pyrido-thiopyrandoinazoles with antitumor activity 失效
标题翻译：具有抗肿瘤活性的吡啶 - 硫代吡咯烷酮
公开(公告)号：US5935969A
公开(公告)日：1999-08-10
申请号：US973865
申请日：1998-01-05
申请人： A. Paul Krapcho
发明人： A. Paul Krapcho
IPC分类号： C07D495/16 , A61K31/435 , C07D495/12
CPC分类号： C07D495/16
摘要： This invention is directed to compounds of formula (I) wherein one of X, Y, Z or T is nitrogen (.dbd.N--) and the others are .dbd.CH--; these compounds have been shown to have antitumor activity. ##STR1##
摘要翻译： PCT No.PCT / US96 / 10966 Sec。 371日期：1998年1月5日 102（e）日期1998年1月5日PCT提交1996年7月3日PCT公布。出版物WO97 / 02267 日本1997年1月23日本发明涉及式（I）的化合物，其中X，Y，Z或T中的一个为氮（= N-），其余为= CH-; 这些化合物已被证明具有抗肿瘤活性。

20. 发明授权

US5623080A Fluorone and pyronin Y derivatives 失效
标题翻译：氟和pyronin Y衍生物
公开(公告)号：US5623080A
公开(公告)日：1997-04-22
申请号：US388802
申请日：1995-02-15
申请人： Douglas C. Neckers , Jianmin Shi
发明人： Douglas C. Neckers , Jianmin Shi
IPC分类号： C07D311/78 , C07D311/82 , C07D311/84 , C07D498/06 , C08F2/50 , C08G59/68 , G03F7/028 , G03F7/029 , G03F7/031 , G03F7/038 , G03F7/075 , A01N43/02 , C07D495/12
CPC分类号： C08F2/50 , C07D311/78 , C07D311/82 , C07D311/84 , C08G59/68 , G03F7/028 , G03F7/029 , G03F7/031 , G03F7/038 , G03F7/0755 , Y10S430/115 , Y10S430/122 , Y10S430/124 , Y10S430/126
摘要： A compound of the formula (I) or (II): ##STR1## where R.sup.1, R.sup.2, R.sup.5 and R.sup.6 are the same or different and represent a hydrogen atom or a halogen atom and R.sup.1 and R.sup.2 may combine to form a ring; R.sup.3, and R.sup.4 are the same or different and represent a hydrogen atom, a halogen atom, a benzoyl group, a group of the formula --L(CH.sub.2).sub.n R.sup.8 where n is 1 to 8, R.sup.8 is a hydrogen, hydroxy, amino, dialkylamino, --COR.sup.16 or --COOR.sup.14 where R.sup.16 is a hydrogen, chlorine, COCl, C.sub.1 -C.sub.8 alkyl, --NR.sub.2 or aryl and R.sup.14 is a hydrogen, C.sub.1 -C.sub.8 alkyl, aryl, COR, 2,4-dinitrophenyl, N-imido or --NR.sub.2 and L is a direct bond or C.dbd.O; W is .dbd.O; W.sup.1 is hydrogen or --OR.sup.9, where R.sup.9 is hydrogen, C.sub.1 -C.sub.8 alkyl, acyl or a group of the formula --(CH.sub.2).sub.n R.sup.10 where n is 1 to 8 and R.sup.10 is amino, dialkylamino, hydroxy, acryloyl or methacryloyl; Y is oxygen, sulfur, selenium, tellurium, C.dbd.O, or >N--R.sup.13 is where R.sup.13 is 4-methylphenyl, and A is hydrogen, alkenyl, dichlorotriazinylamino, or an electron withdrawing group selected from the group consisting of COOR.sup.11, C(O)OCOR.sup.11, CONR.sub.2, CN, NO.sub.2, NCS, NCO, SO.sub.2 R.sup.12, SO.sub.3, R.sup.12, SO.sub.3 R.sup.11, SO.sub.2 NR.sub.2 and CX.sub.3.sup.2 where X.sup.2 is the same or different and is a halogen atom and R.sup.11 is hydrogen, alkyl, aryl, or aralkyl, and R.sup.12 is hydrogen, alkyl, aryl, or aralkyl; provided that when R.sup.1 -R.sup.6 are all hydrogen, A is not hydrogen.
摘要翻译：式（I）或（II）的化合物：其中R 1，R 2，R 5和R 6相同或不同，表示氢原子或卤原子，并且R 1和R 2可以组合形成戒指 R 3和R 4相同或不同，表示氢原子，卤素原子，苯甲酰基，式-L（CH 2）n R 8的基团，其中n为1至8，R 8为氢，羟基，氨基，二烷基氨基，-COR 16或-COOR 14，其中R 16是氢，氯，COCl，C 1 -C 8烷基，-NR 2或芳基，R 14是氢，C 1 -C 8烷基，芳基，COR，2,4-二硝基苯基，或-NR2和L是直接键或C = O; W = 0; W1是氢或-OR9，其中R9是氢，C1-C8烷基，酰基或式 - （CH2）nR10的基团，其中n是1-8，R10是氨基，二烷基氨基，羟基，丙烯酰基或甲基丙烯酰基; Y是氧，硫，硒，碲，C = O或> N-R13，其中R13是4-甲基苯基，A是氢，烯基，二氯三嗪基氨基或选自COOR11，C （O）OCOR11，CONR2，CN，NO2，NCS，NCO，SO2R12，SO3，R12，SO3R11，SO2NR2和CX32，其中X2相同或不同，为卤素原子，R11为氢，烷基，芳基或芳烷基，和R 12是氢，烷基，芳基或芳烷基; 条件是当R 1 -R 6都是氢时，A不是氢。

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