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公开(公告)号：US20180105485A1
公开(公告)日：2018-04-19
申请号：US15842032
申请日：2017-12-14
发明人： Ming-Ming ZHOU , Michael OHLMEYER , Adam VINCEK , Nilesh ZAWARE
IPC分类号： C07C225/20 , C07C237/40 , A61K31/5375 , A61K31/517 , A61K31/498 , A61K31/4965 , C07C229/68 , C07C229/48 , A61K31/4468 , A61K31/4409 , A61K31/4406 , A61K31/277 , C07C255/58 , A61K31/18 , C07C311/38 , A61K31/196 , C07C229/56 , C07C237/30 , A61K31/245 , C07C229/60 , C07D249/04 , C07D295/16 , C07D235/26 , C07D209/08 , C07D239/74 , C07D241/42 , C07D217/02 , C07D215/06 , C07D241/20 , C07D211/58 , C07D213/74 , C07D295/21 , C07D209/40 , C07D249/06 , C07D215/38 , C07D213/76 , C07D213/75 , A61K31/47 , A61K31/4402 , A61K31/44 , A61K31/4192 , A61K31/4184 , A61K31/404 , A61K31/195 , A61K31/166 , A61K31/136 , A61K45/06
CPC分类号： C07C225/20 , A61K31/136 , A61K31/166 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/245 , A61K31/277 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4468 , A61K31/47 , A61K31/4965 , A61K31/498 , A61K31/517 , A61K31/5375 , A61K45/06 , C07C229/48 , C07C229/56 , C07C229/60 , C07C229/68 , C07C237/30 , C07C237/40 , C07C255/58 , C07C311/38 , C07D209/08 , C07D209/40 , C07D211/58 , C07D213/74 , C07D213/75 , C07D213/76 , C07D215/06 , C07D215/38 , C07D217/02 , C07D235/26 , C07D239/74 , C07D241/20 , C07D241/42 , C07D249/04 , C07D249/06 , C07D295/16 , C07D295/21 , A61K2300/00
摘要： Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.
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公开(公告)号：US06949567B2
公开(公告)日：2005-09-27
申请号：US10083008
申请日：2002-02-26
申请人： Andrea Aschenbrenner , Katharina Aulinger Fuchs , Matthias Dormeyer , Gabriel Garcia , Bernd Kramer , Jürgen Kraus , Rolf Krauss , Johan Leban , Stefano Pegoraro , Wael Saeb , Kristina Wolf
发明人： Andrea Aschenbrenner , Katharina Aulinger Fuchs , Matthias Dormeyer , Gabriel Garcia , Bernd Kramer , Jürgen Kraus , Rolf Krauss , Johan Leban , Stefano Pegoraro , Wael Saeb , Kristina Wolf
IPC分类号： A61P33/02 , A61P35/00 , C07C275/40 , C07C275/42 , C07C311/21 , C07C311/37 , C07C311/38 , C07C311/46 , C07C311/47 , C07C317/50 , C07C323/44 , C07C335/22 , C07D209/48 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/24 , C07D261/18 , C07D277/82 , C07D295/13 , C07D307/14 , C07D333/38 , C07D333/54 , C07D413/12 , A61K31/17 , C07C275/28 , C07C275/30
CPC分类号： C07D209/48 , C07C275/40 , C07C275/42 , C07C311/21 , C07C311/37 , C07C311/38 , C07C311/46 , C07C311/47 , C07C317/50 , C07C323/44 , C07C335/22 , C07C2603/74 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/24 , C07D261/18 , C07D277/82 , C07D295/13 , C07D307/14 , C07D333/38 , C07D333/54
摘要： The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C═O, C═S, C═NH, (C═O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.
摘要翻译： 本发明涉及具有式（I）的新的二苯脲或其盐，其中Y是C-O，C-S，C-NH，（C-O）2或SO 2。 以及这些化合物的制备方法及其在治疗原生动物疾病中的用途以及细胞内蛋白质降解途径的抑制是有益的疾病。
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公开(公告)号：US6143747A
公开(公告)日：2000-11-07
申请号：US875025
申请日：1998-02-26
IPC分类号： C07D295/08 , A61K31/18 , A61K31/185 , A61K31/195 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61P31/12 , A61P43/00 , C07C311/29 , C07C311/38 , C07D213/38 , C07D233/54 , C07D233/61 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D263/54 , C07D277/66 , C07D277/82 , C07D295/12 , C07D295/22 , C07D295/26 , C07D303/36 , C07D307/14 , C07D307/79 , C07D317/62 , C07D319/18 , C07D333/34 , C07D405/12 , C07D417/12 , C07D401/12
CPC分类号： C07C311/29 , C07D235/26 , C07D235/32 , C07D277/82 , C07D295/26 , C07D307/79 , C07D317/62 , C07D319/18 , C07D405/12
摘要： Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
摘要翻译： PCT No.PCT / US96 / 00607 Sec。 371日期1998年2月26日 102（e）1998年2月26日PCT PCT 1996年1月18日PCT公布。 第WO96 / 22287号公报 日期1996年7月25日双磺酰氨基羟乙基氨基化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及下式的逆转录病毒蛋白酶抑制化合物：或其药学上可接受的盐，前药或酯，其中变量如本文所定义。
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公开(公告)号：US5998665A
公开(公告)日：1999-12-07
申请号：US089706
申请日：1998-06-03
申请人： Michael Bos , Claus Riemer , Andrew Sleight
发明人： Michael Bos , Claus Riemer , Andrew Sleight
IPC分类号： A61K31/63 , A61K31/18 , A61K31/325 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/505 , A61P25/00 , C07C311/21 , C07C311/38 , C07C311/44 , C07D209/08 , C07D213/76 , C07D239/48 , C07D239/50 , C07D239/69 , C07D403/04
CPC分类号： C07D213/76 , C07C311/21 , C07C311/44 , C07D209/08 , C07D239/48 , C07D239/50 , C07D239/69 , C07D403/04
摘要： The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.
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公开(公告)号：US5869531A
公开(公告)日：1999-02-09
申请号：US525095
申请日：1995-09-08
申请人： Andreas Weichert , Heinz-Werner Kleemann , Hans-Jochen Lang , Jan-Robert Schwark , Udo Albus , Wolfgang Scholz
发明人： Andreas Weichert , Heinz-Werner Kleemann , Hans-Jochen Lang , Jan-Robert Schwark , Udo Albus , Wolfgang Scholz
IPC分类号： A61K31/165 , A61K31/155 , A61K31/18 , A61K31/275 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/02 , A61P35/00 , A61P41/00 , A61P43/00 , C07C22/00 , C07C277/08 , C07C279/22 , C07C311/29 , C07C311/38 , C07C317/44 , C07C323/62 , C07C233/64 , C07C279/02
CPC分类号： C07C317/44 , C07C279/22
摘要： Disclosed are 4-(2'-trifluoromethylethyl)benzoylguanidine and 3-methylsulfonyl-4-(2'-trifluoromethylethyl)benzoylguanidine. Also disclosed are pharmaceutical compositions and the use of the compounds in the treatment of disorders induced by ischemia.
摘要翻译： 公开了4-（2'-三氟甲基乙基）苯甲酰基胍和3-甲基磺酰基-4-（2'-三氟甲基乙基）苯甲酰基胍。 还公开了药物组合物和该化合物在治疗由局部缺血诱导的病症中的用途。
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公开(公告)号：US5138039A
公开(公告)日：1992-08-11
申请号：US745393
申请日：1991-08-15
申请人： Shigemi Seri , Hirohiko Yamauchi , Makoto Azuma , Yoji Arata
发明人： Shigemi Seri , Hirohiko Yamauchi , Makoto Azuma , Yoji Arata
IPC分类号： A61K51/00 , A61B5/055 , A61K49/00 , A61K49/06 , A61K51/04 , A61P1/16 , A61P43/00 , C07B59/00 , C07C237/06 , C07C237/10 , C07C311/18 , C07C311/38 , C07C311/41 , C07F5/00
CPC分类号： C07C311/41 , A61K49/06 , A61K51/0478 , A61K51/048 , A61K51/0497 , C07C237/06 , C07C237/10 , A61K2123/00
摘要： A chelating compound of the formula:(R--NHOC--CH.sub.2).sub.n --A--(CH.sub.2 COOH).sub.m (I)wherein R is an aromatic ring-containing organic group, A is a residue of an aminopolyacetic acid excluding acetic acid groups (--CH.sub.2 COOH) therefrom, m is an integer of at least two and n is an integer of 1 or 2, or its salt, which has a specificity to a hepatobiliary system so that a complex formed between said chelating compound and a metallic element through a coordinate bond is useful and a diagnostic or therapeutic agent for hepatobiliary organs and tissues.
摘要翻译： 一种下式的螯合化合物：（R-NHOC-CH 2）nA-（CH 2 COOH）m（I）其中R是含芳环的有机基团，A是除乙酸基团（-CH 2 COOH）之外的氨基多乙酸的残基， 由此，m为至少2的整数，n为1或2的整数，或其盐，其对肝胆系统具有特异性，使得通过配位键形成在所述螯合化合物与金属元素之间的络合物为 有用的和用于肝胆器官和组织的诊断或治疗剂。
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公开(公告)号：US20190233369A1
公开(公告)日：2019-08-01
申请号：US16378823
申请日：2019-04-09
发明人： Erwin HACKER , Georg BONFIG-PICARD , Stefan LEHR , Udo BICKERS , Martin HESS , Klaus TRABOLD , Mathias SCHMIDT , Frank ZIEMER , Juan Pedro RUIZ-SANTAELLA MORENO
IPC分类号： C07C311/38 , A01N43/653 , C07D405/06 , A01N25/00 , A01N39/04 , A01N41/06
CPC分类号： C07C311/38 , A01N25/00 , A01N39/04 , A01N41/06 , A01N43/653 , C07D405/06 , Y02A40/143 , A01N37/50 , A01N2300/00
摘要： Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, wherein the symbols are defined as in claim 1, preferably cyprosulfamide [Compound (A1)].
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公开(公告)号：US20160200666A1
公开(公告)日：2016-07-14
申请号：US14914672
申请日：2014-08-29
发明人： Ming-Ming ZHOU , Michael OHLMEYER , Adam VINCEK , Nilesh ZAWARE
IPC分类号： C07C225/20 , A61K31/245 , C07C237/30 , A61K31/166 , C07C229/56 , A61K31/196 , C07C311/38 , A61K31/18 , C07C255/58 , A61K31/277 , A61K31/136 , C07D213/74 , A61K31/4402 , A61K31/4406 , A61K31/4409 , C07D213/75 , C07D211/58 , A61K31/4468 , C07C229/48 , C07C229/68 , C07D241/20 , A61K31/4965 , C07D215/06 , A61K31/47 , C07D217/02 , C07D241/42 , A61K31/498 , C07D239/74 , A61K31/517 , C07D209/08 , A61K31/404 , C07D235/26 , A61K31/4184 , C07D295/16 , A61K31/5375 , C07C237/40 , C07D249/04 , A61K31/4192 , C07C229/60
CPC分类号： C07C225/20 , A61K31/136 , A61K31/166 , A61K31/18 , A61K31/195 , A61K31/196 , A61K31/245 , A61K31/277 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4468 , A61K31/47 , A61K31/4965 , A61K31/498 , A61K31/517 , A61K31/5375 , A61K45/06 , C07C229/48 , C07C229/56 , C07C229/60 , C07C229/68 , C07C237/30 , C07C237/40 , C07C255/58 , C07C311/38 , C07D209/08 , C07D209/40 , C07D211/58 , C07D213/74 , C07D213/75 , C07D213/76 , C07D215/06 , C07D215/38 , C07D217/02 , C07D235/26 , C07D239/74 , C07D241/20 , C07D241/42 , C07D249/04 , C07D249/06 , C07D295/16 , C07D295/21 , A61K2300/00
摘要： Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.
摘要翻译： 公开了式I的环状野生型酰胺。该化合物可用于治疗由含有乙酰赖氨酸的蛋白质的不适当活性引起的疾病。 所述组合物包含作为溴结构域抑制剂的环状野生型酰胺属。
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公开(公告)号：US20040028612A1
公开(公告)日：2004-02-12
申请号：US10456895
申请日：2003-06-05
IPC分类号： A61K049/00 , C07D471/02 , C07D41/02 , C07C311/38
CPC分类号： G01N33/52
摘要： The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
摘要翻译： 本发明涉及一种改进的光学方法和光学感测装置，用于确定水性介质中体外和/或体内多羟基取代的有机分子的水平。 特别地，在哺乳动物中实施感官设计以确定糖水平。 具体地说，在糖如果糖或葡萄糖的存在下，将染料与共轭含氮杂环芳族硼酸取代的双鎓化合物组合。 紫罗兰是优选的芳族共轭含氮硼酸取代的化合物。 该方法对于测定人的糖含量是有用的。
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公开(公告)号：US20020022659A1
公开(公告)日：2002-02-21
申请号：US09908430
申请日：2001-07-18
发明人： Gregory D. Harris , Stephen R. Anderson , Sridhar Desikan , Paul A. Meenan , Benjamin R. Stone , Pascal H. Toma , Subodh Shrinivas Deshmukh
IPC分类号： C07C311/38 , A61K031/18
CPC分类号： C07K5/06026 , A61K38/00 , C07C311/41 , C07K5/06191
摘要： This invention relates generally to crystalline and salt forms of compounds of formula I: 1 that are useful as HIV protease inhibitors, pharmaceutical compositions comprising the same, and methods of using the same for treating viral infection.
摘要翻译： 本发明一般涉及式I化合物的结晶和盐形式：其可用作HIV蛋白酶抑制剂，含有该蛋白酶抑制剂的药物组合物，及其用于治疗病毒感染的方法。
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