专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明授权

US5585468A Substituted thioureas as bifunctional chelators 失效
标题翻译：取代硫脲作为双功能螯合剂
公开(公告)号：US5585468A
公开(公告)日：1996-12-17
申请号：US204197
申请日：1994-06-27
申请人： Daniel J. Coughlin , Benjamin A. Belinka, Jr.
发明人： Daniel J. Coughlin , Benjamin A. Belinka, Jr.
IPC分类号： G01N33/58 , A61K39/44 , A61K47/48 , A61K51/00 , A61K51/08 , A61K51/10 , C07C335/06 , C07C335/14 , C07C335/16 , C07C335/22 , C07C337/06 , C07D207/44 , C07D207/452 , C07D213/34 , C07D213/71 , C09K3/00
CPC分类号： C07D207/452 , A61K47/48 , A61K51/082 , A61K51/088 , A61K51/1093 , C07C335/22 , C07C337/06 , C07D213/71 , A61K2121/00 , A61K2123/00
摘要： This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.
摘要翻译： PCT No.PCT / US93 / 03208 Sec。 371日期1994年6月27日第 102（e）日期1994年6月27日PCT提交1993年4月8日PCT公布。出版物WO93 / 21151 日期：1993年10月28日本发明涉及用于将金属离子与生物活性分子偶联的螯合剂。特别地，提供了用于螯合金属例如锝的大量硫脲，其可以与靶向分子例如抗体，肽或蛋白质缀合。

22. 发明授权

US5527885A Bifunctional isothiocyanate derived thiocarbonyls as ligands for metal binding 失效
标题翻译：双官能异硫氰酸酯衍生的硫代羰基作为金属结合的配体
公开(公告)号：US5527885A
公开(公告)日：1996-06-18
申请号：US268445
申请日：1994-06-30
申请人： Daniel J. Coughlin , Benjamin A. Belinka, Jr.
发明人： Daniel J. Coughlin , Benjamin A. Belinka, Jr.
IPC分类号： G01N33/58 , A61K39/44 , A61K47/48 , A61K51/00 , A61K51/08 , A61K51/10 , C07C335/06 , C07C335/14 , C07C335/16 , C07C335/22 , C07C337/06 , C07D207/44 , C07D207/452 , C07D213/34 , C07D213/71 , C09K3/00 , A61K35/14
CPC分类号： C07D207/452 , A61K47/48 , A61K51/082 , A61K51/088 , A61K51/1093 , C07C335/22 , C07C337/06 , C07D213/71 , A61K2121/00 , A61K2123/00
摘要： This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.
摘要翻译：本发明涉及用于将金属离子与生物活性分子偶联的螯合剂。特别地，提供了用于螯合金属例如锝的异硫氰酸酯衍生的硫代羰基，其可以与靶向分子例如抗体，肽或蛋白质缀合。

23. 发明授权

US4968829A Novel substituted aromatic compounds 失效
标题翻译：新型取代芳香族化合物
公开(公告)号：US4968829A
公开(公告)日：1990-11-06
申请号：US368465
申请日：1989-06-19
申请人： Clive A. Henrick
发明人： Clive A. Henrick
IPC分类号： A01N47/06 , A01N47/12 , A01N47/14 , A01N47/22 , A01N47/28 , A01N47/32 , A01N49/00 , C07C271/10 , C07C271/12 , C07C271/16 , C07C333/04 , C07C335/06 , C07D303/24
CPC分类号： C07C323/00 , A01N47/06 , A01N47/12 , A01N47/14 , A01N47/22 , A01N47/28 , A01N47/32 , A01N49/00 , C07C271/12 , C07C271/16 , C07C335/06 , C07D303/24
摘要： Substituted phenoxy, phenylthio and anilino compounds, intermediates therefor, synthesis thereof, and their use for the control of pests.
摘要翻译：取代的苯氧基，苯硫基和苯胺基化合物，其中间体，其合成及其用于防治害虫的用途。

24. 发明授权

US2994710A Novel polyhalogenopolycycloalkene derivatives as foliage fungicides 失效
标题翻译：新型多卤素多环烯烃衍生物作为叶面杀真菌剂
公开(公告)号：US2994710A
公开(公告)日：1961-08-01
申请号：US70550457
申请日：1957-12-27
申请人： SHELL OIL CO
发明人： GABRIEL MORALES JUAN
IPC分类号： C07C275/18 , C07C275/22 , C07C335/06 , C07C335/08 , C07C335/14
CPC分类号： C07C335/08 , C07C275/18 , C07C275/22 , C07C335/06 , C07C335/14 , C07C2602/42 , C07C2603/90

25. 发明授权

US6086864A Pharmaceutical formulations comprising polythiourea and methods of use thereof 失效
标题翻译：包含聚硫脲的药物制剂及其使用方法
公开(公告)号：US6086864A
公开(公告)日：2000-07-11
申请号：US979031
申请日：1997-11-26
申请人： Michael J. Mullins , William A. Fordyce , William J. Kruper , Norton P. Peet , Alan D. Cardin
发明人： Michael J. Mullins , William A. Fordyce , William J. Kruper , Norton P. Peet , Alan D. Cardin
IPC分类号： A61K31/795 , A61F6/04 , A61P31/12 , A61P31/18 , C07C335/06 , C07C335/16 , C07C335/20 , C07F9/09 , C07F9/24 , C08G18/32 , C08G18/38 , C08G18/71 , C08G18/00
CPC分类号： C07C335/16 , C07C335/20
摘要： The oligomers of the present invention are polythioureas having 3 to 50 recurring units derived from aromatic diamines substituted with anionic groups, and having a number average molecular weight of less than 10,000. These oligomers are water-soluble, preferably have a rigid backbone, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of AIDS.
摘要翻译：本发明的低聚物是具有3至50个由阴离子基团取代的芳族二胺衍生的重复单元，数均分子量小于10,000的聚硫脲。这些低聚物是水溶性的，优选具有刚性主链，并且是药学上可接受的。寡聚物可用于治疗和/或诊断艾滋病。

26. 发明授权

US5817836A 2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的2,4-戊二烯酸衍生物
公开(公告)号：US5817836A
公开(公告)日：1998-10-06
申请号：US854868
申请日：1997-05-12
申请人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： A61K31/35 , A61K31/20 , A61K31/23 , A61K31/38 , A61K31/47 , A61P17/00 , A61P43/00 , C07C57/50 , C07C69/618 , C07C215/02 , C07C215/18 , C07C311/58 , C07C335/06 , C07C403/00 , C07D277/22 , C07D311/58 , C07D333/54 , C07D335/06 , C07D335/04 , C07D207/00 , C07D311/04 , C07D401/00
CPC分类号： C07D333/54 , A61K31/20 , A61K31/23 , C07C57/50 , C07C69/618 , C07D311/58 , C07D335/06
摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.
摘要翻译：式1的化合物其中Z选自由式2和式3所示的基团组成的组。式3 Y是3至8个碳的环烷基或环烯基，任选地被一个或两个R 4基取代，或Y选自苯基，吡啶基，噻吩基，呋喃基，吡咯基，哒嗪基，嘧啶基，吡嗪基，噻唑基，恶唑基和咪唑基，所述基团任选被一个或两个R 4基团取代，二价 Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是S，O或NR5; n为1或2; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，低级烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R 5是H或低级烷基，B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

27. 发明授权

US5776699A Method of identifying negative hormone and/or antagonist activities 失效
标题翻译：鉴定负荷激素和/或拮抗剂活性的方法
公开(公告)号：US5776699A
公开(公告)日：1998-07-07
申请号：US613863
申请日：1996-03-11
申请人： Elliott S. Klein , Sunil Nagpal , Roshantha A. Chandraratna
发明人： Elliott S. Klein , Sunil Nagpal , Roshantha A. Chandraratna
IPC分类号： C07D317/26 , A61K31/15 , A61K31/192 , A61K31/215 , A61K31/216 , A61K31/341 , A61K31/352 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/382 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/47 , A61K38/09 , A61P5/00 , A61P39/02 , C07C20060101 , C07C57/50 , C07C63/33 , C07C63/331 , C07C63/49 , C07C63/66 , C07C63/72 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C69/48 , C07C69/618 , C07C69/76 , C07C69/773 , C07C69/90 , C07C69/94 , C07C233/81 , C07C245/10 , C07C327/48 , C07C335/06 , C07C403/20 , C07D20060101 , C07D213/55 , C07D215/12 , C07D277/20 , C07D277/30 , C07D307/54 , C07D311/58 , C07D333/24 , C07D335/06 , C07F7/08 , G01N33/567
CPC分类号： C07D335/06 , C07C233/81 , C07C245/10 , C07C327/48 , C07C57/50 , C07C63/33 , C07C63/49 , C07C63/66 , C07C63/72 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C69/618 , C07C69/76 , C07C69/90 , C07C69/94 , C07D213/55 , C07D277/30 , C07D307/54 , C07D333/24 , C07F7/0818 , C07C2102/10
摘要： Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
摘要翻译：芳基取代的和芳基和（3-氧代-1-丙烯基）取代的苯并吡喃，苯并噻喃，1,2-二氢喹啉和5,6-二氢萘衍生物具有类视黄醇阴性激素和/或拮抗剂样生物活性。本发明的RAR拮抗剂可以施用于包括人在内的哺乳动物，以预防或减少RAR激动剂在结合受体位点上的作用。具体来说，RAR激动剂与类视黄醇药物一起施用或共同施用以预防或改善由类维生素A或维生素A或维生素A前体引起的毒性或副作用。类视黄醇阴性激素可用于增强其他类维生素A和核受体激动剂的活性。例如，称为AGN 193109的类视黄醇阴性激素有效地增加了体外反式激活测定中其他类维生素A和类固醇激素的有效性。另外，反式激活测定可用于鉴定具有负激素活性的化合物。这些测定是基于负激素下调修饰的具有组成型转录激活子结构域的嵌合维甲酸受体的活性的能力。

28. 发明授权

US5703050A Urea derivatives, their preparation and use 失效
标题翻译：尿素衍生物，其制备和使用
公开(公告)号：US5703050A
公开(公告)日：1997-12-30
申请号：US513815
申请日：1996-01-17
申请人： Otmar Klingler , Gerhard Zoller , Bernd Jablonka , Melitta Just , Gerhard Breipohl , Jochen Knolle , Wolfgang Konig , Hans Ulrich Stilz
发明人： Otmar Klingler , Gerhard Zoller , Bernd Jablonka , Melitta Just , Gerhard Breipohl , Jochen Knolle , Wolfgang Konig , Hans Ulrich Stilz
IPC分类号： C07D215/54 , A61K31/195 , A61K31/197 , A61K31/198 , A61K31/215 , A61K31/445 , A61K31/47 , A61K38/00 , A61P7/02 , A61P35/00 , A61P43/00 , C07C275/40 , C07C275/42 , C07C309/13 , C07C311/31 , C07C335/06 , C07D211/62 , C07D263/32 , C07D453/02 , C07D471/08 , C07K5/06 , C07K5/072 , C07K5/083 , C07K5/097 , C07K5/00
CPC分类号： C07K5/06026 , C07C275/40 , C07D263/32 , C07K5/06113 , C07K5/0806 , C07K5/0821 , A61K38/00
摘要： Urea derivates are disclosed having the formula (I). ##STR1## in which A, B, W, Z, R, R.sup.1, R.sup.2, R.sup.3 and r have the meaning given in the description, as well as a process for preparing the same and their use as inhibitors of thrombocyte aggregation, carcinom cell metastasis and osteoclast binding to bone surface.
摘要翻译： PCT No.PCT / EP94 / 00713 371日期1996年1月17日 102（e）日期1996年1月17日PCT 1994年3月9日PCT公布。 WO94 / 22907 PCT出版物 1994年10月13日公开了具有式（I）的衍生物。其中A，B，W，Z，R，R1，R2，R3和r具有说明书中给出的含义，以及其制备方法及其作为血小板聚集抑制剂的用途，癌细胞转移和破骨细胞结合骨表面。

29. 发明授权

US5663367A 2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的2,4-戊二烯酸衍生物
公开(公告)号：US5663367A
公开(公告)日：1997-09-02
申请号：US656137
申请日：1996-05-31
申请人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： A61K31/35 , A61K31/20 , A61K31/23 , A61K31/38 , A61K31/47 , A61P17/00 , A61P43/00 , C07C57/50 , C07C69/618 , C07C215/02 , C07C215/18 , C07C311/58 , C07C335/06 , C07C403/00 , C07D277/22 , C07D311/58 , C07D333/54 , C07D335/06 , C07D333/12 , C07D307/40 , C07D307/56 , C07D333/22
CPC分类号： C07D333/54 , A61K31/20 , A61K31/23 , C07C57/50 , C07C69/618 , C07D311/58 , C07D335/06
摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.
摘要翻译：式1的化合物其中Z选自由式2和式3所示的基团组成的组。式3 Y是3至8个碳的环烷基或环烯基，任选地被一个或两个R 4基取代，或Y选自苯基，吡啶基，噻吩基，呋喃基，吡咯基，哒嗪基，嘧啶基，吡嗪基，噻唑基，恶唑基和咪唑基，所述基团任选被一个或两个R 4基团取代，二价 Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是S，O或NR5; n为1或2; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，低级烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R 5是H或低级烷基，B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

30. 发明授权

US5385944A Naphthylethylureas and naphthylethylthioureas 失效
标题翻译：萘乙基脲和萘乙基硫脲
公开(公告)号：US5385944A
公开(公告)日：1995-01-31
申请号：US53911
申请日：1993-04-27
申请人： Daniel Lesieur , Said Yous , Patrick Depreux , Gerard Adam , Pierre Renard , Bruno Pfeiffer , Beatrice Guardiola-Lemaitre
发明人： Daniel Lesieur , Said Yous , Patrick Depreux , Gerard Adam , Pierre Renard , Bruno Pfeiffer , Beatrice Guardiola-Lemaitre
IPC分类号： A61K31/17 , A61K8/42 , A61K8/46 , A61P1/00 , A61P17/00 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P35/00 , A61Q7/00 , A61Q17/00 , A61Q19/00 , C07C273/02 , C07C275/24 , C07C335/12 , C07C335/14 , C07C335/06
CPC分类号： C07C335/12 , A61K8/42 , A61K8/46 , A61Q19/00 , C07C275/24 , A61Q17/00 , A61Q7/00 , C07C2101/02 , C07C2101/14 , Y10S514/923
摘要： A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
摘要翻译：选自式（I）的化合物：其中R，R 1，R 2和X的含义在本说明书中定义的式（I）和含有该化合物的药物，其可用于治疗或预防褪黑激素系统紊乱。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式