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21. 发明授权

US06448293B1 Diphenyl ether compounds useful in therapy 失效
标题翻译：用于治疗的二苯醚化合物
公开(公告)号：US06448293B1
公开(公告)日：2002-09-10
申请号：US09810378
申请日：2001-03-16
申请人： Mark David Andrews , David Hepworth , Donald Stuart Middleton , Alan Stobie
发明人： Mark David Andrews , David Hepworth , Donald Stuart Middleton , Alan Stobie
IPC分类号： C07C21758
CPC分类号： C07D231/38 , C07C45/71 , C07C47/55 , C07C47/575 , C07C205/44 , C07C217/58 , C07C229/38 , C07C237/28 , C07C255/43 , C07C255/59 , C07C311/05 , C07C311/08 , C07C311/37 , C07C317/32 , C07C323/20 , C07C323/32 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07D231/12 , C07D233/56 , C07D249/06 , C07D249/08 , C07D295/096 , C07D295/192
摘要： A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(O)R6, CO2R9, C(O)NHR6 or SO2NR6R7; R12 is F, OH, CO2H, C3-6cycloalkyl, NH2, CONH2, C1-6alkoxy, C1-6alkoxycarbonyl or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O optionally substituted independently by one or more R13; or R6 and R7, together with the nitrogen to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring optionally substituted independently by one or more R13; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, —NH2, —NH(C1-C6alkyl) or —N(C1-C6alkyl)2; wherein when R1 and R2 are methyl, R4 and R5 are hydrogen and n is 1, R3is not a —SMe group para to the ether linkage linking rings A and B.
摘要翻译：通式（I）的化合物或其药学上可接受的盐，溶剂化物或多晶型物; 其中; R 1和R 2可以相同或不同，为氢，C 1 -C 6烷基，（CH 2）m（C 3 -C 6环烷基），其中m = 0,1,2或3，或R 1和R 2与它们连接形成氮杂环丁烷环; 每个R 3独立地为CF 3，OCF 3，C 1-4烷硫基或C 1 -C 4烷氧基; n为1,2或3; 并且R 4和R 5可以相同或不同，为：A-X，其中A = -CH = CH-或 - （CH 2）p - ，其中p为0,1或2; X是氢，F，Cl，Br，I，CONR6R7，SO2NR6R7，SO2NHC（= O）R6，OH，C1-4烷氧基，NR8SO2R9，NO2，NR6R11，CN，CO2R10，CHO，SR10，S（O）R9或SO2R10 ; R 6，R 7，R 8和R 10可以相同或不同，是氢或被一个或多个R 12独立地取代的C 1-6烷基; R9是任选被一个或多个R 12独立地取代的C 1-6烷基; R 11是氢，任选地被一个或多个R 12，C（O）R 6，CO 2 R 9，C（O）NHR 6或SO 2 NR 6 R 7取代的C 1-6烷基; R 12是F，OH，CO 2 H，C 3-6环烷基，NH 2，CONH 2，C 1-6烷氧基，C

22. 发明授权

US06410790B1 3-amin3-arylpropan-1-ol compounds, their preparation and use 失效
标题翻译： 3-氨基-3-芳基丙-1-醇化合物，其制备和用途
公开(公告)号：US06410790B1
公开(公告)日：2002-06-25
申请号：US09545371
申请日：2000-04-07
申请人： Bernd Sundermann , Hagen-Heinrich Hennies , Babette-Yvonne Koegel , Helmut Buschmann
发明人： Bernd Sundermann , Hagen-Heinrich Hennies , Babette-Yvonne Koegel , Helmut Buschmann
IPC分类号： C07C21100
CPC分类号： C07D295/096 , C07C215/28 , C07C215/42 , C07C215/64 , C07C215/70 , C07C217/74 , C07C229/38 , C07C255/59 , C07C323/32 , C07C2601/14 , C07D307/52 , C07D317/58 , C07D333/20
摘要： 3-amino-3-arylpropan-1-ol compounds of formula I: R1 and R2 independently denoting C1-6 alkyl, or together denoting a (CH2)2-6 ring optionally substituted by phenyl, R3 denoting C3-6 alkyl, C3-6 cycloalkyl, aryl optionally containing heteroatoms and optionally substituted by R6 to R8, or a substituted C1-3 alkylphenyl of formula XII: R4 and R5 independently denoting C1-6 alkyl, C3-6 cycloalkyl, phenyl, benzyl, or phenethyl, or together forming a (CH2)3-6 or CH2CH2OCH2CH2 ring, R6 to R8 independently denoting H, F, Cl, Br, CHF2, CF3, OH, OCF3, OR14, NR15R16, SR14, phenyl, SO2CH3, SO2CF3, C1-6 alkyl, CN, COOR14, or CONR15R16, or together forming a OCH2O, OCH2CH2O, CH═CHO, CH═C(CH3)O or (CH2)4 ring, R14 denoting C1-6 alkyl, phenyl, benzyl, or phenethyl, R15 and R16 independently denoting H, C1-6 alkyl, phenyl, benzyl or phenethyl, and A denoting optionally substituted aryl optionally containing heteroatoms, or a diastereomer or enantiomer or pharmaceutically acceptable salt thereof, and their preparation and use in pharmaceutical compositions.
摘要翻译：式I的3-氨基-3-芳基丙-1-醇化合物：R 1和R 2独立地表示C 1-6烷基，或一起表示任选被苯基取代的（CH 2）2-6环，R 3表示C 3-6烷基，C 3 -6环烷基，任选含有杂原子并任选被R 6至R 8取代的芳基或式XII的取代的C 1-3烷基苯基：R 4和R 5独立地表示C 1-6烷基，C 3-6环烷基，苯基，苄基或苯乙基，或一起形成（CH2）3-6或CH2CH2OCH2CH2环，R6至R8独立地表示H，F，Cl，Br，CHF2，CF3，OH，OCF3，OR14，NR15R16，SR14，苯基，SO2CH3，SO2CF3，C1-6烷基，CN，COOR 14或CONR 15 R 16，或一起形成OCH 2 O，OCH 2 CH 2 O，CH = CHO，CH = C（CH 3）O或（CH 2）4环，R 14表示C 1-6烷基，苯基，苄基或苯乙基，R 15和 R16独立地表示H，C 1-6烷基，苯基，苄基或苯乙基，A表示任选地含有杂原子的任选取代的芳基，或其非对映异构体或对映异构体或其药学上可接受的盐，在药物组合物中的应用和用途。

23. 发明授权

US5922763A Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：联苯衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5922763A
公开(公告)日：1999-07-13
申请号：US978739
申请日：1997-11-26
申请人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
发明人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
IPC分类号： C07C211/44 , A61K38/00 , C07C211/48 , C07C211/50 , C07C211/53 , C07C233/65 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/54 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/28 , C07C275/32 , C07C275/38 , C07C275/42 , C07C279/18 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/11 , C07C311/16 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/14 , C07C317/44 , C07C317/46 , C07C321/24 , C07C323/60 , C07C323/62 , C07D207/08 , C07D207/26 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07D257/04 , C07D295/192 , C07F9/40 , C07K5/06 , A61K31/24 , A61K31/19 , C07C229/34 , C07C251/16
CPC分类号： C07D295/192 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/56 , C07C255/57 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/42 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/44 , C07C317/46 , C07C323/60 , C07C323/62 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07K5/06026 , A61K38/00 , C07C2101/14
摘要： The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
摘要翻译：本发明涉及通式的联苯衍生物，其中A至E和X如权利要求1所定义，其立体异构体包括它们的混合物及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，其具有有价值的性质，优选聚集抑制作用，含有这些化合物的药物组合物及其制备方法。

24. 发明授权

US5395957A Separation of enantiomers of cimaterol, (-)-cimaterol and the use thereof in pharmaceutical compositions and animal feeds 失效
标题翻译：西马特罗，（ - ） - 西马特罗的对映异构体的分离及其在药物组合物和动物饲料中的用途
公开(公告)号：US5395957A
公开(公告)日：1995-03-07
申请号：US166584
申请日：1993-12-14
申请人： Wolfgang Resemann , Adolf Durr , Gunther Engelhardt , John F. Quirke
发明人： Wolfgang Resemann , Adolf Durr , Gunther Engelhardt , John F. Quirke
IPC分类号： C07C255/59 , A23K1/16 , A23K1/18 , A61K31/00 , A61K31/275 , A61K31/277 , A61P3/00 , A61P3/04 , A61P11/00 , A61P11/06 , A61P13/02 , A61P15/00 , A61P21/02 , A61P25/04 , A61P29/00 , A61P37/08 , C07B57/00 , C07C253/34 , C07C255/49 , C07C255/00
CPC分类号： A61K31/275 , A23K20/111 , A23K50/30 , A61K31/277 , C07C255/59 , Y10S514/826 , Y10S514/888 , Y10S514/909
摘要： The invention relates to the separation of enantiomers of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.
摘要翻译：本发明涉及分离西马特罗，（ - ） - 西马特罗的对映异构体，其加成盐及其制备方法及其在药物组合物和动物饲料中的应用。

25. 发明授权

US5145870A Aryloxyphenylpropylamines their preparation and use 失效
标题翻译：丙烯酰基丙烯酸酯的制备和使用
公开(公告)号：US5145870A
公开(公告)日：1992-09-08
申请号：US529004
申请日：1990-05-24
申请人： Palle Jakobsen , Jorgen Drejer
发明人： Palle Jakobsen , Jorgen Drejer
IPC分类号： A61K31/135 , A61K31/275 , A61K31/357 , A61K31/36 , A61P9/10 , A61P21/02 , A61P25/04 , A61P25/06 , A61P25/08 , C07C213/02 , C07C217/48 , C07C217/72 , C07C253/30 , C07C255/59 , C07D317/64 , C07D521/00
CPC分类号： C07C217/72 , C07C217/48 , C07C255/59 , C07D317/64 , C07C2101/02 , C07C2102/10
摘要： Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano;R.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.The novel compounds are useful in the treatment of anoxia, migraine, ischemia, epilepsy, traumatic injury and neurodegenerative diseases.

26. 发明授权

US5053427A Guanidino-substituted benzopyrans and their use as pharmaceuticals 失效
标题翻译：甘氨酸取代苯并噻唑及其作为药物的用途
公开(公告)号：US5053427A
公开(公告)日：1991-10-01
申请号：US407227
申请日：1989-09-14
申请人： Geoffrey Stemp , Gordon Burrell , David G. Smith
发明人： Geoffrey Stemp , Gordon Burrell , David G. Smith
IPC分类号： A61K31/155 , A61K31/35 , A61K31/352 , A61K31/435 , A61P1/00 , A61P9/00 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , A61P15/04 , C07C255/59 , C07C255/67 , C07C279/16 , C07C279/28 , C07C335/32 , C07D311/58 , C07D311/68 , C07D405/04 , C07D491/04 , C07D491/052
CPC分类号： C07D405/04 , C07C255/59 , C07C255/67 , C07C279/28 , C07C335/32 , C07D311/68 , C07D491/04 , C07C2102/08
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a and b together form an --O-- or --CH.sub.2 -- linkage or a bond;either Y is N and R.sub.2 is hydrogen; orY is C-R.sub.1whereineither one of R.sub.1 and R.sub.2 is hydrogen and the other is nitro, cyano, halo, CF.sub.3, formyl, aldoxime, CF.sub.3 O, NO.sub.2 --CH.dbd.CH--, NC--CH.dbd.CH--; a group R.sub.x X-- wherein R.sub.x and C.sub.1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, halo, CF.sub.3 and cyano; and X is C.dbd.O, O.C.dbd.O, C.dbd.0.0, CHOH, SO, SO.sub.2, 0.SO, 0.SO.sub.2, CONH, 0.CONH, C.dbd.S, 0.C.dbd.S, C.dbd.S.0, CH.SH, SONH, SO.sub.2 NH, 0.SONH, 0.SO.sub.2 NH, CO--CH.dbd.CH, C.dbd.NHOH, C.dbd.NNH.sub.2 ; or a group R.sub.y R.sub.z NZ-- wherein R.sub.y and R.sub.z are independently hydrogen or C.sub.1-6 alkyl and Z is C.dbd.O, SO or SO.sub.2 ; orR.sub.1 is a C.sub.3-8 cycloalkyl group or a C.sub.1-6 alkyl group optionally substituted by a group which is hydroxy, C.sub.1-6 alkoxy, amino optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-7 alkanoylamino, C.sub.3-8 cycloalkyloxy or C.sub.3-8 cycloalkylamino; and R.sub.2 is hydrogen; orone of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is a different group selected from nitro, cyano, halo, C.sub.1-3 alkylcarbonyl, methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;either one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl; orR.sub.3 and R.sub.4 together are C.sub.2-5 polymethylene;either R.sub.5 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy; andR.sub.6 is hydrogen; orR.sub.5 and R.sub.6 together are a bond;either R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; andR.sub.8 is hydrogen or C.sub.1-6 alkyl; orR.sub.7 and R.sub.8 together are C.sub.2-4 polymethylene;R.sub.9 is CN, NO.sub.2, COR.sub.10 or SO.sub.2 R.sub.10 wherein R.sub.10 is C.sub.1-3 alkyl, NH.sub.2, NH(C.sub.1-3 alkyl), CF.sub.3 or phenyl optionally substituted as defined for R.sub.x ; andthe R.sub.8 N(NR.sub.9)NHR.sub.7 moiety is trans to the R.sub.5 group when R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy;having antihypertensive and/or bronchodilator activity, processes for their preparation and their use as pharmaceuticals.

27. 发明授权

US3996261A Cyanopolyhaloanilines 失效
标题翻译：氨基多卤代苯胺
公开(公告)号：US3996261A
公开(公告)日：1976-12-07
申请号：US629343
申请日：1975-11-06
申请人： Lewis W. Watts, Jr. , Philip H. Moss
发明人： Lewis W. Watts, Jr. , Philip H. Moss
IPC分类号： C07C255/58 , C07C255/59 , C07C121/78 , C07C121/80
CPC分类号： C07C255/58 , C07C255/59
摘要： Novel polyhalo, N-substituted aniline compounds are prepared which have the following structural formula: ##STR1## where R is selected from the group consisting of cyano, nitro, and alkyl sulfone, X is halo and Z represents a radical as follows: ##STR2## where R' and R" are hydrogen or lower alkyl, X is a number ranging from 1 to 5, and Y is 0-3. These compounds are prepared by reacting a polyhalo aromatic compound having the formula ##STR3## where X and R have a significance as just discussed with an appropriate polyamino reactant or aminohydroxy compound which additionally may contain either linkages. These new compounds have biological activity and are also useful as chemical intermediates.
摘要翻译：制备具有以下结构式的新型多卤代，N-取代的苯胺化合物：其中R选自氰基，硝基和烷基砜，X为卤素，Z表示如下基团：IMA图 >其中R'和R“为氢或低级烷基，X为1至5的数，Y为0-3。这些化合物通过使具有式（I）的多卤代芳香族化合物反应来制备，其中X和R具有正如所讨论的适当的聚氨基反应物或氨基羟基化合物的重要性，其另外可以含有两个键。这些新化合物具有生物活性，也可用作化学中间体。

28. 发明授权

US2642436A - substituted - 失效
公开(公告)号：US2642436A
公开(公告)日：1953-06-16
申请号：US2642436D
CPC分类号： C07D295/155 , C07C255/59 , C07D211/14

29. 发明申请

US20190010114A1 DEZOCINE ANALOGUE 审中-公开
公开(公告)号：US20190010114A1
公开(公告)日：2019-01-10
申请号：US16066852
申请日：2017-01-04
申请人： SHANDONG DANHONG PHARMACEUTICAL CO., LTD.
发明人： Yang ZHANG , Wentao WU , Zhixiang LI , Guangwen YANG , Yongbo FANG , Tao ZHANG , Wei GU , Shuhui CHEN , Fei WANG , Jian LI
IPC分类号： C07C215/64 , C07D313/20
CPC分类号： C07C215/64 , C07C217/74 , C07C219/26 , C07C255/59 , C07C2601/02 , C07C2601/14 , C07C2603/80 , C07D313/20
摘要： Disclosed in the present disclosure is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof.

30. 发明申请

US20180327373A1 AMYLOID TARGETING AGENTS AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：US20180327373A1
公开(公告)日：2018-11-15
申请号：US15969328
申请日：2018-05-02
申请人： The Regents of the University of California , Amydis, Inc.
发明人： Jerry Yang , Emmanuel A. Theodorakis , Stella Sarraf
IPC分类号： C07D295/155 , C07D401/14 , C07H19/056 , C07D307/52 , C07D213/57 , C07D295/04 , C07D211/06 , C07C255/42 , C07D265/30 , C07D413/12 , C07D413/10 , C07D241/04 , C07D409/14 , C07D409/10 , C07D409/04 , C07D407/10 , C07D405/10 , C07D405/04 , C07C311/35 , C07D401/04 , C07D333/22 , C07C255/59 , C07C255/58 , C07D213/85
CPC分类号： C07D295/155 , A61B5/0075 , A61B5/4082 , A61B5/4088 , A61P25/28 , C07C255/42 , C07C255/58 , C07C255/59 , C07C311/35 , C07D211/06 , C07D213/57 , C07D213/85 , C07D241/04 , C07D265/30 , C07D295/04 , C07D307/52 , C07D333/22 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/10 , C07D407/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07H13/04 , C07H19/056
摘要： Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.

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