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1. 发明授权

US10414745B2 Phenol derivatives to treat cancer 有权
公开(公告)号：US10414745B2
公开(公告)日：2019-09-17
申请号：US15570348
申请日：2016-04-29
申请人： FUNDACIÓN MEDINA. CENTRO DE EXCELENCIA EN INVESTIGACIÓN DE MEDICAMENTOS INNOVADORES EN ANDALUCÍA
发明人： Nuria De Pedro Montejo , Victor Gonzalez Menendez , Gloria Crespo Sueiro , Ignacio Perez-Victoria Moreno De Barreda , Bastien Cautain , Maria Francisca Vicente Perez , Jose Fernando Reyes Benitez , Olga Genilloud Rodriguez , Carmen Grinan Lison , Juan Antonio Marchal Corrales
IPC分类号： A61P35/00 , C12P7/24 , C12P7/26 , C12P17/06 , C07D311/02 , C07D311/04 , C07D311/22 , C07D311/58 , C07D311/82 , C07D311/86 , C07C49/86 , C12R1/645 , C07C49/248 , C07C49/255
摘要： The present invention relates to compounds of general formula (I) wherein R1-R8 take various meanings, pharmaceutical compositions containing them and their use in medicine, particularly for the treatment and/or prophylaxis of cancer.

2. 发明申请

US20170320810A1 NOVEL ASPIRIN DERIVATIVES AND USES THEREOF 有权
公开(公告)号：US20170320810A1
公开(公告)日：2017-11-09
申请号：US15660032
申请日：2017-07-26
申请人： North Carolina Agricultural and Technical State University
发明人： Shengmin Sang
IPC分类号： C07C69/78 , C07C69/86 , C07C49/835 , C07C49/86 , A61K31/616
CPC分类号： C07C69/78 , A61K31/616 , C07C49/835 , C07C49/86 , C07C69/86
摘要： The present invention provides novel aspirin derivatives useful for preventing and/or treating cancer. The novel compounds of this invention may be particularly useful for the prevention and/or treatment of cancers affecting the gastrointestinal system, such as colorectal cancer.

3. 发明申请

US20150148259A1 NOVEL PHENYL GLYOXAL PROBES 有权
标题翻译：新款PHYYL GLYOXAL PROBES
公开(公告)号：US20150148259A1
公开(公告)日：2015-05-28
申请号：US14405467
申请日：2013-06-04
申请人： The Scripps Research Institute
发明人： Paul R. Thompson , Kevin L. Bicker , Venkataraman Subramanian
IPC分类号： G01N33/68 , C07D311/90 , G01N33/92 , C07D495/04 , C07C45/61 , G01N33/58 , C07C49/86 , C07D311/86
CPC分类号： G01N33/581 , C07B59/00 , C07B2200/05 , C07C45/61 , C07C49/86 , C07C247/04 , C07D311/86 , C07D311/90 , C07D493/10 , C07D495/04 , C12Q1/34 , G01N33/532 , G01N33/582 , G01N33/583 , G01N33/68 , G01N33/6803 , G01N33/6893 , G01N33/92 , G01N2333/775 , G01N2333/978 , G01N2440/18 , G01N2458/15 , G01N2500/00 , G01N2570/00
摘要： Novel phenyl-glyoxal based anti-citrulline probes and methods of synthesis are provided. Methods of use, such as, the development of methods for monitoring substrate citrullination over time; for identifying citrullinated proteins from cells are described.
摘要翻译：提供了新的苯基乙二醛基抗瓜氨酸探针和合成方法。使用方法，例如开发用于随时间监测底物瓜氨酸化的方法; 用于鉴定来自细胞的瓜氨酸化蛋白质。

4. 发明授权

US5324859A Deuterated benzaldehydes 失效
标题翻译：氘化苯甲醛
公开(公告)号：US5324859A
公开(公告)日：1994-06-28
申请号：US5978
申请日：1993-01-19
申请人： Erik O. Pettersen , Rolf O. Larsen , John M. Dornish , Bernt Borretzen , Reidar Oftebro , Thomas Ramdahl
发明人： Erik O. Pettersen , Rolf O. Larsen , John M. Dornish , Bernt Borretzen , Reidar Oftebro , Thomas Ramdahl
IPC分类号： A61K31/12 , A61K9/22 , A61K31/165 , A61K31/19 , A61K31/235 , A61K31/275 , A61K31/335 , A61K31/357 , A61K31/385 , A61K31/425 , A61K31/426 , A61P35/00 , C07B59/00 , C07C47/52 , C07C47/544 , C07C49/86 , C07C67/32 , C07C69/76 , C07C69/92 , C07C233/65 , C07C235/46 , C07C235/84 , C07C237/30 , C07C253/30 , C07C255/54 , C07C255/56 , C07C255/57 , C07C255/58 , C07D263/18 , C07D277/04 , C07D317/14 , C07D339/08 , C07D407/04 , C07C47/54 , C07C47/542
CPC分类号： C07D407/04 , C07B59/001 , C07C235/84 , C07C255/56 , C07C47/544 , C07C69/76
摘要： New compounds of formula I: ##STR1## wherein Y may be CN or ##STR2## wherein A may be H, D, alkyl with 1-4 carbon atoms, OR wherein R is H or alkyl with 1-4 carbon atoms, or --NR.sub.1 R.sub.2 or --CR.sub.1 R.sub.2 R.sub.3 wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and are H or alkyl with 1-4 carbon atoms;Z is H, D, Y or alkyl with 1-4 C-atoms, halogen, nitro, amino, monoalkyl amino or dialkyl amino wherein the alkyl groups have 1-4 C atoms, or --OR wherein R may be H or alkyl with 1-4 C-atoms or --CR.sub.4, R.sub.5 R.sub.6 wherein R.sub.4, R.sub.5 and R.sub.6 may be the same or different and may be H or F;and pharmaceutically acceptable salts thereof,are useful as anti-cancer agents or as intermediates for preparing anti-cancer agents.
摘要翻译：式I的新化合物：其中Y可以是CN或其中A可以是H，D，具有1-4个碳原子的烷基，或其中R是H或具有1-4个碳原子的烷基或-NR 1 R 2或-CR 1 R 2 R 3，其中R 1，R 2和R 3相同或不同，为H或具有1-4个碳原子的烷基; Z是H，D，Y或具有1-4个C原子的卤素，硝基，氨基，一烷基氨基或二烷基氨基，其中烷基具有1-4个C原子，或-OR，其中R可以是H或具有 1-4个C原子或-CR 4，R 5 R 6，其中R 4，R 5和R 6可以相同或不同，并且可以是H或F; 和其药学上可接受的盐可用作抗癌剂或用作制备抗癌剂的中间体。

5. 发明授权

US4892940A Aromatic naphthyl compounds, a process for their preparation and their use in human and veterinary medicine and in cosmetic compositions 失效
标题翻译：芳香族萘基化合物，其制备方法及其在人和兽医学和化妆品组合物中的应用
公开(公告)号：US4892940A
公开(公告)日：1990-01-09
申请号：US52930
申请日：1987-05-22
申请人： Jean Maignan , Gerard Lang , Gerard Malle , Serge Restle , Braham Shroot
发明人： Jean Maignan , Gerard Lang , Gerard Malle , Serge Restle , Braham Shroot
IPC分类号： C07C41/00 , A61K8/00 , A61K8/30 , A61K8/34 , A61K8/35 , A61K8/36 , A61K8/368 , A61K8/37 , A61K8/41 , A61K8/42 , A61K8/49 , A61K31/045 , A61K31/085 , A61K31/12 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/215 , A61P17/00 , A61P29/00 , A61P37/08 , C07C29/143 , C07C33/18 , C07C33/26 , C07C33/28 , C07C33/32 , C07C33/46 , C07C41/18 , C07C43/14 , C07C43/164 , C07C43/20 , C07C43/23 , C07C45/30 , C07C45/46 , C07C47/546 , C07C49/215 , C07C49/76 , C07C49/86 , C07C51/347 , C07C57/44 , C07C59/48 , C07C59/64 , C07C59/84 , C07C59/90 , C07C63/36 , C07C65/24 , C07C65/34 , C07C65/40 , C07C67/00 , C07C69/618 , C07C69/738 , C07C69/76 , C07C231/00 , C07C231/02 , C07C233/11 , C07C233/65 , C07C235/34 , C07C235/66 , C07C235/84 , C07C239/00
CPC分类号： C07C65/40 , C07C43/23 , C07C45/305 , C07C49/86 , C07C59/90 , C07C65/24 , C07C65/34 , Y10S514/844 , Y10S514/859 , Y10S514/88
摘要： An aromatic naphthyl compound of the formula ##STR1## wherein n is 0 or 1,R' is hydrogen, OH, acyloxy, alkoxy or NH.sub.2,R" is hydrogen or lower alkoxy, or R' and R" taken together form an oxo, methano or hydroxy-imino radical,R is --CH.sub.2 OH or --COR.sub.8,R.sub.8 is hydrogen, --OR.sub.9 or ##STR2## R.sub.9 is hydrogen, alkyl having 1-20 carbon atoms, mono or polyhydroxyalkyl, aryl, aralkyl, the residue of a sugar or ##STR3##is 1, 2 or 3,r' and r" each independently represent hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, benzyl, the residue of amino acid or the residue of aminated sugar, or r' and r" together form a heterocycle,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen, lower alkyl, alkoxy having 1-4 carbon atoms, fluoroalkoxy, CF.sub.3, cycloalkyl, lower acyl, halogen, OH, amino, acylamino or alkoxy carbonyl,R.sub.5, R.sub.6 and R.sub.7 represent hydrogen or methyl or when n=1, R.sub.5 and R.sub.7 taken together can form with the benzene ring a naphthalene ring, and the salts of the compound of formula I or their geometric or optical isomers.These compounds are useful in human and veterinary medicine and in cosmetic compositions.
摘要翻译：式（I）的芳香族萘基化合物，其中n为0或1，R'为氢，OH，酰氧基，烷氧基或NH 2，R“为氢或低级烷氧基，或R'和R”为一起形成氧代，甲醇或羟基亚氨基，R为-CH 2 OH或-COR 8，R 8为氢，-OR 9或R 9为氢，具有1-20个碳原子的烷基，单或多羟基烷基，芳基，芳烷基，糖或“IMAGE”的残基为1,2或3，r'和r“各自独立地表示氢，烷基，单羟基烷基，多羟基烷基，芳基，苄基，氨基酸的残基或胺化糖的残基，或 r'和r“一起形成杂环，R 1，R 2，R 3和R 4表示氢，低级烷基，具有1-4个碳原子的烷氧基，氟烷氧基，CF 3，环烷基，低级酰基，卤素，OH，氨基，酰氨基或烷氧基羰基，R 5，R 6和R 7表示氢或甲基，或当n = 1时，R 5和R 7一起可以与苯环形成萘环，式I化合物或其几何形式的盐 c或光学异构体。这些化合物可用于人和兽医学和化妆品组合物。

6. 发明授权

US4806141A Herbicidal compounds and compositions 失效
标题翻译：除草剂及组合物
公开(公告)号：US4806141A
公开(公告)日：1989-02-21
申请号：US937467
申请日：1986-12-02
申请人： Keith G. Watson , Lynette A. Garson , Graham J. Bird , Graeme J. Farquharson
发明人： Keith G. Watson , Lynette A. Garson , Graham J. Bird , Graeme J. Farquharson
IPC分类号： A01N47/04 , A01N33/24 , A01N35/06 , A01N35/10 , A01N37/00 , A01N37/02 , A01N37/10 , A01N37/22 , A01N37/34 , A01N37/48 , A01N41/04 , A01N41/06 , A01N41/10 , C07C45/00 , C07C45/45 , C07C45/51 , C07C45/67 , C07C45/71 , C07C45/74 , C07C47/542 , C07C47/55 , C07C47/565 , C07C47/575 , C07C49/255 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C49/86 , C07C67/00 , C07C239/00 , C07C251/42 , C07C251/44 , C07C251/50 , C07C301/00 , C07C303/28 , C07C309/63 , C07C309/73 , C07C313/00 , C07C323/21 , A01N33/00
CPC分类号： C07C255/00 , A01N35/10 , A01N37/00 , A01N37/02 , A01N37/10 , A01N37/22 , A01N37/48 , A01N41/04 , A01N41/06 , A01N41/10 , C07C323/00 , C07C45/455 , C07C45/513 , C07C45/673 , C07C45/71 , C07C45/74 , C07C47/542 , C07C47/55 , C07C47/565 , C07C47/575 , C07C49/255 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C49/86
摘要： The invention concerns novel compounds of the formula I ##STR1## wherein Z is selected from hydrogen, halogen, C.sub.1 to C.sub.6 alkyl, and C.sub.1 to C.sub.6 alkoxy;Y is selected from halogen, C.sub.1 to C.sub.6 alkyl and C.sub.1 to C.sub.6 alkoxy;X is selected from halogen, C.sub.1 to C.sub.6 alkyl and C.sub.1 to C.sub.6 alkoxy and if Y is methyl and Z is hydrogen or methyl then at least one of X is not methyl;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl and phenyl; andm is an integer chosen from 1 to 3.The compounds are cereal selective herbicides and in further embodiments the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of compounds of formula I, herbicidal compositions containing as active ingredient a compound of formula I, and processes for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I.
摘要翻译：本发明涉及式I的新型化合物其中Z选自氢，卤素，C 1至C 6烷基和C 1至C 6烷氧基; Y选自卤素，C 1至C 6烷基和C 1至C 6烷氧基; X选自卤素，C 1至C 6烷基和C 1至C 6烷氧基，如果Y是甲基，Z是氢或甲基，那么X中的至少一个不是甲基; R 1选自氢，烷基，烯基，炔基，取代的烷基，烷基磺酰基，芳基磺酰基，酰基和无机或有机阳离子; R2选自烷基，取代的烷基，烯基，卤代烯基，炔基和卤代炔基; R3选自烷基，氟烷基，烯基，炔基和苯基; 并且m是选自1至3的整数。化合物是谷物选择性除草剂，并且在进一步的实施方案中，本发明提供了制备式I化合物的方法，可用于制备式I化合物的中间体，含有活性的除草组合物成分为式I化合物，以及通过向植物或植物的生长培养基施用有效量的式I化合物来严重损害或杀死有害植物的方法。

7. 发明授权

US4536344A Process for formylating aryl halides 失效
标题翻译：甲酰化芳基卤化物的方法
公开(公告)号：US4536344A
公开(公告)日：1985-08-20
申请号：US549339
申请日：1983-11-04
申请人： Paul Fiedler , Rudolf Braden
发明人： Paul Fiedler , Rudolf Braden
IPC分类号： C07C67/36 , C07C45/00 , C07C45/49 , C07C45/68 , C07C47/54 , C07C47/542 , C07C47/548 , C07C47/55 , C07C47/575 , C07C49/86 , C07C67/00 , C07C69/035 , C07C69/78 , C07C253/00 , C07C255/56
CPC分类号： C07C45/49
摘要： Aryl halides are formylated with carbon monoxide and hydrogen in the presence of a noble metal catalyst, tertiary organic nitrogen compounds and phosphanes or phosphites.
摘要翻译：在贵金属催化剂，叔有机氮化合物和磷烷或亚磷酸盐的存在下，芳基卤化物用一氧化碳和氢气甲酰化。

8. 发明授权

US4478849A Secondary amines, their preparation and use in pharmaceutical compositions 失效
标题翻译：仲胺，它们的制备和在药物组合物中的应用
公开(公告)号：US4478849A
公开(公告)日：1984-10-23
申请号：US474199
申请日：1983-03-10
申请人： Anthony T. Ainsworth , David G. Smith
发明人： Anthony T. Ainsworth , David G. Smith
IPC分类号： A61K31/195 , A61K31/205 , A61K31/24 , A61K31/34 , C07C45/28 , C07C49/86 , C07C65/32 , C07C233/00 , C07C233/12 , C07C275/34
CPC分类号： C07C275/34 , C07C205/45 , C07C205/54 , C07C45/28 , C07C49/86 , C07C65/32 , Y10S514/884 , Y10S514/909
摘要： The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or antihyperglycaemic activity.
摘要翻译：式（II）的化合物：其中R 1为氢，氟或氯原子或羟基，羟甲基，甲基，甲氧基，氨基，甲酰氨基，乙酰氨基，甲基磺酰氨基，硝基，苄氧基，甲基磺酰基甲基，脲基，三氟甲基或对甲氧基苄基氨基; R2是氢，氟或氯原子或羟基; R3是氢或氯原子或羟基; R4是羧酸基团或其盐，酯或酰胺; R5是氢，氯或氟原子或甲基，甲氧基或羟基或羧酸基团或其盐，酯或酰胺; R6是氢原子或甲基或丙基; X是氧原子或键; 并且Y是至多6个碳原子的亚烷基，或已经发现具有抗肥胖和/或抗高血糖活性的键。

9. 发明授权

US4464391A Pesticides 失效
标题翻译：农药
公开(公告)号：US4464391A
公开(公告)日：1984-08-07
申请号：US172943
申请日：1980-07-28
申请人： Michael Elliott , Norman F. Janes , David A. Pulman
发明人： Michael Elliott , Norman F. Janes , David A. Pulman
IPC分类号： A01N37/10 , A01N37/36 , A01N53/00 , A01N53/02 , C07C45/29 , C07C45/43 , C07C45/63 , C07C45/67 , C07C49/86 , C07C69/743 , C07C255/53 , C07C121/75
CPC分类号： C07C255/00 , A01N37/10 , A01N37/36 , A01N53/00 , C07C45/292 , C07C45/43 , C07C45/63 , C07C45/673 , C07C49/86
摘要： New insecticides are of formula: ##STR1## wherein R.sup.1 represents hydrogen or a methyl group; R.sup.2 represents hydrogen or a halogeno or lower alkyl group; R.sup.3 represents hydrogen or a halogeno or carbo(lower alkoxy) group which contains at least 2 carbon atoms in the lower alkoxy residue when R.sup.2 represents methyl; with the proviso that (a) R.sup.2 and R.sup.3 each represent hydrogen only when R.sup.1 represents methyl, (b) when R.sup.1 and R.sup.3 each represent hydrogen and R.sup.2 represents alkyl, that alkyl group contains at least 2 carbon atoms and (c) when R.sup.3 represents halogeno, R.sup.2 represents hydrogen or halogeno; and R represents a group which forms insecticidal esters with chrysanthemic acid e.g. 5-benzyl-3-furylmethyl, 3-phenoxybenzyl, .alpha.-cyano-3-phenoxybenzyl. The esters are prepared by forming the ester linkage conventionally or by a Wittig reaction using a 3-formyl- or 3-acetyl-2,2-dimethyl cyclopropane carboxylic acid esterified with the desired residue or by an alkyl group which is subsequently converted to the desired residue.
摘要翻译：新的杀虫剂具有下式：其中R 1表示氢或甲基; R2表示氢或卤代或低级烷基; 当R 2表示甲基时，R 3表示氢或低级烷氧基残基中含有至少2个碳原子的卤代或碳（低级烷氧基）基团; 条件是（a）R 2和R 3各自表示氢，当R 1表示甲基时，（b）当R 1和R 3各自表示氢且R 2表示烷基时，该烷基含有至少2个碳原子，和（c）当R 3表示卤代，R 2表示氢或卤素; R表示与菊酸形成杀虫剂的基团，例如， 5-苄基-3-呋喃基甲基，3-苯氧基苄基，α-氰基-3-苯氧基苄基。酯通过常规形成酯键或通过Wittig反应制备，使用用所需残基酯化的3-甲酰基或3-乙酰基-2,2-二甲基环丙烷羧酸或通过烷基将其转化为所需残留物。

10. 发明授权

US4438117A 2-Substituted thio-4,5-diarylpyrimidines 失效
标题翻译： 2-取代的硫代-4,5-二芳基嘧啶
公开(公告)号：US4438117A
公开(公告)日：1984-03-20
申请号：US183336
申请日：1980-09-03
申请人： Saul C. Cherkofsky
发明人： Saul C. Cherkofsky
IPC分类号： C07C45/00 , C07C49/86 , C07D239/40 , A61K31/505 , C07D239/22
CPC分类号： C07D239/40 , C07C45/00 , C07C49/86 , Y10S514/825
摘要： 2-Substitutedthio-4,5-diarylpyrimidines, such as 2-(1,1,2,2-tetrafluoroethylthio)-4,5-bis(4-methoxy-phenyl)pyrimidine useful for treating arthritis and/or alleviating pain.
摘要翻译： 2-取代的硫代-4,5-二芳基嘧啶，例如可用于治疗关节炎和/或缓解疼痛的2-（1,1,2,2-四氟乙硫基）-4,5-双（4-甲氧基 - 苯基）嘧啶。

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