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1. 发明授权

US09828362B2 1,4-disubstituted imidazole derivative 有权
公开(公告)号：US09828362B2
公开(公告)日：2017-11-28
申请号：US15443892
申请日：2017-02-27
申请人： Sumitomo Dainippon Pharma Co., Ltd.
发明人： Hitoshi Ban , Manabu Kusagi , Shingo Tojo , Futoshi Hasegawa , Miki Hashizume
IPC分类号： C07D401/12
CPC分类号： C07C233/88 , A61P35/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a 1,4-disubstituted imidazole derivative of formula (1′) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6 alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

2. 发明授权

US08686044B2 Amide derivative, pest control agent containing the amide derivative, and use of the amide derivative 有权
标题翻译：酰胺衍生物，含有酰胺衍生物的害虫控制剂，以及酰胺衍生物的用途
公开(公告)号：US08686044B2
公开(公告)日：2014-04-01
申请号：US13016604
申请日：2011-01-28
申请人： Yumi Kobayashi , Hidenori Daido , Hiroyuki Katsuta , Michikazu Nomura , Hidetaka Tsukada , Atsushi Hirabayashi , Yusuke Takahashi , Yoji Aoki , Atsuko Kawahara , Yasuaki Fukazawa , Mai Hirose
发明人： Yumi Kobayashi , Hidenori Daido , Hiroyuki Katsuta , Michikazu Nomura , Hidetaka Tsukada , Atsushi Hirabayashi , Yusuke Takahashi , Yoji Aoki , Atsuko Kawahara , Yasuaki Fukazawa , Mai Hirose
IPC分类号： A01N37/18 , A61K31/16 , A61K31/165
CPC分类号： A01N37/22 , A01N37/46 , A01N43/40 , A01N43/78 , A61K31/167 , C07C233/88 , C07C237/42 , C07C255/57 , C07C255/60 , C07D213/82
摘要： An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action.In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclie. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R1 and R2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G1)-Q1 or —C(=G1)-G2Q2, and G1 to G3 each represent oxygen atoms or the like. Q1 and Q2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y1 and Y5 each represent a halogen atom or the like, Y2 and Y4 each represent a hydrogen atom or the like, and Y3 represents a C2-C5 haloalkyl group.
摘要翻译：提供由下式（1）表示的酰胺衍生物作为酰胺衍生物，其对害虫防治作用显示出显着优异的效果。在下式（1）中，A表示碳原子，氮原子等，K表示形成来自苯或杂环的环状连接基所需的非金属原子团。 X表示卤素原子等; n表示0〜4的整数.R 1，R 2表示氢原子，烷基等。 T表示-C（= G1）-Q1或-C（= G1）-G2Q2，并且G1至G3各自表示氧原子等。 Q1和Q2各自表示氢原子，烷基，芳基等。 Y 1和Y 5各自表示卤素原子等，Y 2和Y 4各自表示氢原子等，Y 3表示C 2〜C 5卤代烷基。

3. 发明授权

US08067648B2 Method for synthesizing radioactive ligand having 18F-labeled fluorobenzene ring 有权
标题翻译：合成具有18 F标记氟苯环的放射性配体的方法
公开(公告)号：US08067648B2
公开(公告)日：2011-11-29
申请号：US12161974
申请日：2006-11-29
申请人： Kazutoshi Suzuki , Ming-Rong Zhang , Katsushi Kumata
发明人： Kazutoshi Suzuki , Ming-Rong Zhang , Katsushi Kumata
IPC分类号： C07B59/00 , C07C231/12 , C07C233/25 , C07C303/26 , C07C309/73
CPC分类号： C07B59/001 , C07B2200/05 , C07C233/88 , C07C309/00 , Y10T436/196666
摘要： A phenyl tin compound is synthesized by using a derivative having various functional groups and a bromo- or iodo-benzene ring as a labeling material of a radioactive ligand. On the other hand, a novel hydroxytosyl iodobenzene compound having an electron-donating group is obtained by oxidizing iodobenzene having one or more electron-donating groups and reacting it with tosylic acid. Then, a diphenyliodonium salt which is a labeling precursor is synthesized by reacting the resulting compound with various phenyl tin compounds. Finally, a 18F-labeled ligand having various functional groups and a [18F] fluorobenzene ring is synthesized by reacting the resulting diphenyliodonium salt with [18F]F−.
摘要翻译：通过使用具有各种官能团的衍生物和溴或碘 - 苯环作为放射性配体的标记材料来合成苯基锡化合物。另一方面，通过氧化具有一个或多个给电子基团的碘苯并将其与甲苯磺酸反应得到具有给电子基团的新的羟基苯基碘苯化合物。然后，通过使所得化合物与各种苯基锡化合物反应来合成作为标记前体的二苯基碘鎓盐。最后，通过使得到的二苯基碘鎓盐与[18 F] F- - 反应合成具有各种官能团和[18 F]氟苯环的18 F标记的配体。

4. 发明申请

US20090234162A1 Radioactive Halogen-Labeled Phenyloxyaniline Derivatives 审中-公开
标题翻译：放射性卤素标记苯氧基苯胺衍生物
公开(公告)号：US20090234162A1
公开(公告)日：2009-09-17
申请号：US11884763
申请日：2005-12-28
申请人： Kazutoshi Suzuki , Tetsuya Suhara , Christer Halldin , Ming-Rong Zhang , Atsuro Nakazato
发明人： Kazutoshi Suzuki , Tetsuya Suhara , Christer Halldin , Ming-Rong Zhang , Atsuro Nakazato
IPC分类号： C07C233/25
CPC分类号： A61K51/04 , C07B59/001 , C07B2200/05 , C07C233/88
摘要： A radioactive halogen-labeled phenyoxyaniline derivative represented by the following formula: wherein R1 represents a group such as an alkyl group; X1, X2, X3 and X4 represent each a hydrogen atom, an alkyl group, an alkoxy group, an alkoxy group carrying 11C introduced thereinto or a radioactive halogen atom, provided that at least one of X1, X2, X3 and X4 represents an alkoxy group carrying 11C introduced thereinto or a radioactive halogen atom; which is a compound useful as a PBR ligand having a high affinity and a high selectivity. In in vitro measurement of PBR, a PBR ligand having a high affinity and a high selectivity is labeled with a radioactive halogen nuclear species so as to enable the measurement of PBR in vivo with the use of means including not only PET but also SPECT. Thus, a compound which is useful in early diagnosing, preventing and treating diseases such as Alzheimer type dementia can be obtained.
摘要翻译：由下式表示的放射性卤素标记的苯氧基苯胺衍生物：其中R1表示烷基等基团; X 1，X 2，X 3和X 4各自表示氢原子，烷基，烷氧基，带有11C的烷氧基或放射性卤素原子，条件是X 1，X 2，X 3和X 4中的至少一个表示烷氧基携带11C的基团或放射性卤素原子; 其是可用作具有高亲和力和高选择性的PBR配体的化合物。在PBR的体外测量中，具有高亲和力和高选择性的PBR配体用放射性卤素核物种进行标记，以便能够使用不仅包括PET而且还包括SPECT的方法在体内测量PBR。因此，可以获得可用于早期诊断，预防和治疗诸如阿尔茨海默氏型痴呆症的疾病的化合物。

5. 发明申请

US20080249180A1 MALONAMIDES AS OREXIN ANTAGONISTS 失效
标题翻译：马洛康作为OREXIN拮抗剂
公开(公告)号：US20080249180A1
公开(公告)日：2008-10-09
申请号：US12044002
申请日：2008-03-07
申请人： Luca Gobbi , Henner Knust , Parichehr Malherbe , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
发明人： Luca Gobbi , Henner Knust , Parichehr Malherbe , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
IPC分类号： A61K31/165 , C07C233/01
CPC分类号： C07C233/29 , C07C233/15 , C07C233/32 , C07C233/88 , C07C2601/02 , C07C2601/08 , C07D211/16 , C07D211/46 , C07D213/40 , C07D213/75 , C07D295/185 , C07D309/14
摘要： The present invention relates to compounds of formula I wherein Ar1, Ar2, R, R1, R2, R3 and n are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译：本发明涉及式I化合物，其中Ar 1，Ar 2，R 1，R 1，R 2， >，R 3和n如本文所定义，或其药学上合适的酸加成盐，光学纯对映异构体，外消旋体或非对映体混合物。式I化合物是食欲素受体拮抗剂，可用于治疗其中食欲素途径如睡眠障碍的疾病。

6. 发明授权

US06479548B2 Substituted stilbenes as glucose uptake enhancers 失效
标题翻译：取代的二苯乙烯作为葡萄糖摄取增强剂
公开(公告)号：US06479548B2
公开(公告)日：2002-11-12
申请号：US09872763
申请日：2001-05-31
申请人： John Patterson , Sophia Park , Robert T. Lum , Wayne R. Spevak
发明人： John Patterson , Sophia Park , Robert T. Lum , Wayne R. Spevak
IPC分类号： A61K31195
CPC分类号： C07C233/81 , C07C233/88 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C237/42 , C07C309/51 , C07C309/61 , C07D317/60
摘要： Compound of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mammalian hosts, and processes for their preparation, are also described.
摘要翻译：配方化合物使胰岛素受体激酶活化。还描述了包含该化合物的药物组合物，以及通过将哺乳动物宿主施用这些化合物及其制备方法来治疗高血糖症和涉及葡萄糖水平不平衡的其它疾病，特别是用于治疗II型糖尿病的方法。

7. 发明授权

US6124455A Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity 失效
标题翻译：在芳族或杂芳族部分具有吸电子取代基的四氢萘，苯并二氢吡喃，二氢苯并噻喃和1,2,3,4-四氢喹啉羧酸的芳基或杂芳基酰胺具有类视黄醇样生物活性
公开(公告)号：US6124455A
公开(公告)日：2000-09-26
申请号：US491176
申请日：2000-01-25
申请人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
发明人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： C07D311/66 , A61K31/00 , A61K31/16 , A61K31/164 , A61K31/195 , A61K31/196 , A61K31/24 , A61K31/353 , A61K31/38 , A61K31/382 , A61K31/44 , A61P17/00 , A61P35/00 , A61P43/00 , C07C233/81 , C07C233/88 , C07C235/66 , C07C327/48 , C07D215/40 , C07D311/58 , C07D335/06 , C07D237/02 , C07D239/02 , C07D241/02 , C07D275/02 , C07D277/02
CPC分类号： C07C235/66 , C07C233/81 , C07C233/88 , C07C327/48 , C07D215/40 , C07D311/58 , C07D335/06 , C07C2102/10
摘要： Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.
摘要翻译：下式的化合物其中符号具有本说明书中定义的含义具有类视黄醇样生物活性。

8. 发明授权

US5886225A Process for the hydrogenation of imines 失效
标题翻译：亚胺氢化方法
公开(公告)号：US5886225A
公开(公告)日：1999-03-23
申请号：US973575
申请日：1997-12-05
申请人： Hans-Peter Jalett , Felix Spindler , Reinhard Georg Hanreich
发明人： Hans-Peter Jalett , Felix Spindler , Reinhard Georg Hanreich
IPC分类号： B01J31/02 , C07B61/00 , C07C209/52 , C07C213/02 , C07C217/08 , C07C233/88 , C07D333/36 , C07C209/38
CPC分类号： C07C209/52 , C07C217/08 , C07C233/88 , C07D333/36
摘要： A process for the hydrogenation of imines with hydrogen under elevated pressure in the presence of iridium catalysts and with or without an inert solvent, wherein the reaction mixture contains hydrogen iodide.
摘要翻译： PCT No.PCT / EP96 / 02419 Sec。 371 1997年12月5日第 102（e）日期1997年12月5日PCT Filted 1996年6月4日PCT公布。公开号WO96 / 41793 日期：1996年12月27日在惰性溶剂存在下，在高压下用氢气氢化亚胺的方法，其中反应混合物含有碘化氢。

9. 发明授权

US5856490A Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity 失效
标题翻译：在芳族或杂芳族部分具有吸电子取代基的四氢萘，苯并二氢吡喃，二氢苯并噻喃和1,2,3,4-四氢喹啉羧酸的芳基或杂芳基酰胺具有类视黄醇样生物活性
公开(公告)号：US5856490A
公开(公告)日：1999-01-05
申请号：US923864
申请日：1997-09-04
申请人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
发明人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： C07D311/66 , A61K31/00 , A61K31/16 , A61K31/164 , A61K31/195 , A61K31/196 , A61K31/24 , A61K31/353 , A61K31/38 , A61K31/382 , A61K31/44 , A61P17/00 , A61P35/00 , A61P43/00 , C07C233/81 , C07C233/88 , C07C235/66 , C07C327/48 , C07D215/40 , C07D311/58 , C07D335/06 , C07D405/12
CPC分类号： C07C235/66 , C07C233/81 , C07C233/88 , C07C327/48 , C07D215/40 , C07D311/58 , C07D335/06 , C07C2102/10
摘要： Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
摘要翻译：符号具有本说明书中定义的含义的式“IMAGE”的化合物具有类视黄醇样生物活性。

10. 发明授权

US5675024A Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity 失效
标题翻译：在芳族或杂芳族部分具有吸电子取代基的四氢萘，苯并二氢吡喃，二氢苯并噻喃和1,2,3,4-四氢喹啉羧酸的芳基或杂芳基酰胺具有类视黄醇样生物活性
公开(公告)号：US5675024A
公开(公告)日：1997-10-07
申请号：US562000
申请日：1995-11-22
申请人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
发明人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： C07D311/66 , A61K31/00 , A61K31/16 , A61K31/164 , A61K31/195 , A61K31/196 , A61K31/24 , A61K31/353 , A61K31/38 , A61K31/382 , A61K31/44 , A61P17/00 , A61P35/00 , A61P43/00 , C07C233/81 , C07C233/88 , C07C235/66 , C07C327/48 , C07D215/40 , C07D311/58 , C07D335/06 , C07D405/12
CPC分类号： C07C235/66 , C07C233/81 , C07C233/88 , C07C327/48 , C07D215/40 , C07D311/58 , C07D335/06 , C07C2102/10
摘要： Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
摘要翻译：符号具有本说明书中定义的含义的式“IMAGE”的化合物具有类视黄醇样生物活性。

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