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71. 发明授权

US10851123B2 Prodrugs of phenolic TRPV1 agonists 有权
公开(公告)号：US10851123B2
公开(公告)日：2020-12-01
申请号：US16078585
申请日：2017-02-22
申请人： CONCENTRIC ANALGESICS, INC.
发明人： Craig Husfeld , Andrei W. Konradi
IPC分类号： A61P29/00 , C07F9/09 , C07D233/64 , C07D207/16 , C07C259/06 , C07C271/48 , C07C271/54 , C07C275/42 , C07C279/14 , C07C305/10 , C07C307/02 , C07C307/10 , C07C323/12 , C07C323/44 , C07C323/60 , C07C233/20 , C07C233/27 , C07C233/51 , C07F9/12 , C07F9/24 , C07F9/59 , C07D211/26 , C07D213/81 , C07D211/28 , C07D295/185 , C07D207/09
摘要： Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

72. 发明申请

US20170174618A1 EFFICIENT SYNTHESIS OF AMINES AND AMIDES FROM ALCOHOLS AND ALDEHYDES BY USING CASCADE CATALYSIS 审中-公开
公开(公告)号：US20170174618A1
公开(公告)日：2017-06-22
申请号：US15129424
申请日：2015-03-27
申请人： ORGANOFUEL SWEDEN AB
发明人： Armando CÓRDOVA , Per BERGLUND , Mattias ANDERSON , Samson AFEWERKI
IPC分类号： C07C233/27 , C12P13/02 , C12P13/00 , C07C233/25 , C07C231/10
CPC分类号： C07C233/27 , C07C231/02 , C07C231/10 , C07C233/25 , C12P13/001 , C12P13/02 , C07C233/18 , C07C233/20
摘要： The present invention relates generally to an eco-friendly methodology for the conversion of alcohols and aldehydes to amines and amides using an integrated enzyme cascade system with metal- and organocatalysis. More specifically, the present invention relates to synthesis of capsaicinoids starting from vanillin alcohol and using a combination of an enzyme cascade system and catalysts. Furthermore, the method also relates to synthesis of capsaicinoids derivatives starting from vanillin alcohol derivatives and using a combination of an enzyme cascade system and catalysts.

73. 发明申请

US20130023510A1 ARACHIDONIC ACID ANALOGS AND METHODS FOR ANALGESIC TREATMENT USING SAME 有权
标题翻译：芳香酸类似物及其使用方法进行分析治疗
公开(公告)号：US20130023510A1
公开(公告)日：2013-01-24
申请号：US13481333
申请日：2012-05-25
申请人： Lane Brostrom , John R. Falck
发明人： Lane Brostrom , John R. Falck
IPC分类号： A61K31/16 , C07C233/27 , A61K31/167 , C07C275/22 , A61K31/17 , A61P25/04 , C07D203/18 , A61K31/396 , C07C233/20 , C07C231/02 , A61P29/00 , C07C233/10 , C07C233/09
CPC分类号： C07C233/09 , C07C237/22 , C07C275/20 , C07C2601/02 , C07C2601/04 , C07C2601/08
摘要： The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.
摘要翻译：本发明提供花生四烯酸（AA）类似物和含有这些类似物作为止痛治疗活性剂的组合物。提供了制备本发明化合物的各种方法，并描述了药物制剂，包括可注射和口服剂量。某些类似物另外可用作解热组合物和相关的发烧减少治疗。

74. 发明授权

US5760071A Aryl(alkyl)propylamides 失效
公开(公告)号：US5760071A
公开(公告)日：1998-06-02
申请号：US814283
申请日：1997-03-10
申请人： Daniel Lesieur , Veronique Leclerc , Patrick Depreux , Philippe Delagrange , Pierre Renard
发明人： Daniel Lesieur , Veronique Leclerc , Patrick Depreux , Philippe Delagrange , Pierre Renard
IPC分类号： A61K31/16 , A61K31/165 , A61K31/17 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/28 , C07C231/02 , C07C231/12 , C07C233/05 , C07C233/18 , C07C233/19 , C07C233/20 , C07C233/25 , C07C233/27 , C07C233/31 , C07C233/40 , C07C233/60 , C07C235/34 , C07C273/18 , C07C275/24 , C07C309/68 , C07C327/42 , C07C327/46 , C07C335/08 , C07C335/10 , C07C335/12 , C07D209/14 , C07D307/81 , C07D333/58 , A61K31/405
CPC分类号： C07D333/58 , C07C233/05 , C07C233/18 , C07C233/19 , C07C233/20 , C07C233/60 , C07C275/24 , C07D307/81 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2102/10
摘要： The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.

75. 发明授权

US5089628A Fluorine-containing bismaleamic acids and bismaleimides useful for thermosetting resins 失效
标题翻译：含氟的含二硫代酸和二氯甲烷二异氰酸酯用于热固性树脂
公开(公告)号：US5089628A
公开(公告)日：1992-02-18
申请号：US410494
申请日：1989-09-21
申请人： Masamichi Maruta , Akihiro Fukui
发明人： Masamichi Maruta , Akihiro Fukui
IPC分类号： C07C233/27 , C07D207/44 , C07D207/448 , C07D207/456 , C07D209/48 , C08G73/12
CPC分类号： C07D207/448 , C07C233/27 , C07D207/456 , C07D209/48 , C08G73/123
摘要： The invention provides novel fluorine-containing bismaleimides represented by the general formula shown below. The bismaleimides are obtained by dehydrating and cyclizing reaction of corresponding bismaleamic acids which are also novel compounds. For example, maleic anhydride is used for preparing the bismaleamic acids. A mixture of a bismaleimide of the invention and a diamine is useful as a thermosetting resin composition. At 100.degree.-300.degree. C. the resin composition undergoes addition polymerization to turn into a solid resin which are high in moisture resistance and low in dielectric constant. For use in the resin composition it is preferable that both R.sup.1 and R.sup.2 in the general formula of the bismaleimide are --CF.sub.3. ##STR1## wherein A represents a divalent organic group having an ethylenic unsaturated bond; Rf represents fluorine atom or a perfluoroalkyl group; R.sup.1 and R.sup.2 are the same or different and each represent hydrogen atom, methyl group, ethyl group or a halogenated methyl group; and each -N
摘要翻译：本发明提供由以下通式表示的新型含氟双马来酰亚胺。双马来酰亚胺通过相应的双马来酸酸的反应脱水和环化得到，它们也是新型化合物。例如，马来酸酐用于制备双马来酰胺酸。本发明的双马来酰亚胺和二胺的混合物可用作热固性树脂组合物。在100-300℃下，树脂组合物进行加成聚合，变成耐湿性高，介电常数低的固体树脂。为了在树脂组合物中使用，优选双马来酰亚胺的通式中的R 1和R 2均为-CF 3。其中A表示具有烯键式不饱和键的二价有机基团; Rf表示氟原子或全氟烷基; R1和R2相同或不同，分别表示氢原子，甲基，乙基或卤代甲基; 并且每个-N'在相对于芳族醚键-O-的m-或p-位上。

76. 发明授权

US4716175A Saturated fatty acid amides as inhibitors of acyl-CoA:cholesterol acyltransferase 失效
标题翻译：饱和脂肪酸酰胺作为酰基辅酶A的抑制剂：胆固醇酰基转移酶
公开(公告)号：US4716175A
公开(公告)日：1987-12-29
申请号：US17960
申请日：1987-02-24
申请人： Milton L. Hoefle , Ann Holmes , Bruce D. Roth
发明人： Milton L. Hoefle , Ann Holmes , Bruce D. Roth
IPC分类号： C12N9/99 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P3/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/04 , C07C233/05 , C07C233/07 , C07C233/09 , C07C233/12 , C07C233/13 , C07C233/15 , C07C233/16 , C07C233/18 , C07C233/20 , C07C233/22 , C07C233/25 , C07C233/27 , C07C233/29 , C07D213/40 , C07D213/75 , C07D239/42 , C07D239/52 , A61K31/16 , A61K31/165 , C07C103/19 , C07D213/36
CPC分类号： C07D213/40 , C07C233/07 , C07C233/09 , C07D239/52
摘要： Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.

77. 发明授权

US4666943A Fungicidal anilides 失效
标题翻译：杀真菌剂
公开(公告)号：US4666943A
公开(公告)日：1987-05-19
申请号：US514799
申请日：1983-07-19
申请人： Hiroshi Noguchi , Toshiro Kato , Junya Takahashi , Yukio Ishiguri , Shigeo Yamamoto , Naonori Hirata
发明人： Hiroshi Noguchi , Toshiro Kato , Junya Takahashi , Yukio Ishiguri , Shigeo Yamamoto , Naonori Hirata
IPC分类号： A01N37/18 , A01N37/08 , A01N37/22 , A01N37/24 , A01N37/32 , A01N37/34 , A01N37/36 , A01N37/40 , A01N37/46 , A01N39/02 , A01N39/04 , A01N43/24 , A01N47/34 , A01N53/00 , A01N53/04 , A01N53/12 , A01N57/30 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/02 , C07C233/07 , C07C233/08 , C07C233/09 , C07C233/11 , C07C233/12 , C07C233/15 , C07C233/25 , C07C233/27 , C07C233/28 , C07C233/29 , C07C233/43 , C07C233/46 , C07C233/55 , C07C233/58 , C07C233/65 , C07C235/24 , C07C235/56 , C07C237/06 , C07C239/00 , C07C251/48 , C07C253/00 , C07C255/27 , C07C255/44 , C07C255/60
CPC分类号： C07C255/00 , A01N37/22 , A01N37/24 , A01N37/34 , A01N37/40 , A01N39/04 , A01N53/00
摘要： Use of an anilide of the formula: ##STR1## as a fungicidal agent against phytophatogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.
摘要翻译：使用下式的酰苯胺：作为杀真菌剂的植物致病真菌，特别是其对苯并咪唑硫氮菌素杀真菌剂和/或环状酰亚胺杀真菌剂有抗性的菌株。

78. 发明授权

US4647584A Fungicidal aniline derivatives 失效
标题翻译：杀真菌苯胺衍生物
公开(公告)号：US4647584A
公开(公告)日：1987-03-03
申请号：US566427
申请日：1983-12-28
申请人： Junya Takahashi , Toshiro Kato , Hiroshi Noguchi , Yukio Oguri , Shigeo Yamamoto , Katsuzo Kamoshita
发明人： Junya Takahashi , Toshiro Kato , Hiroshi Noguchi , Yukio Oguri , Shigeo Yamamoto , Katsuzo Kamoshita
IPC分类号： A01N47/18 , A01N37/22 , A01N37/24 , A01N37/32 , A01N39/00 , A01N47/20 , A01N47/34 , A01N47/38 , A01N47/40 , A01N53/00 , A01N57/30 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/09 , C07C233/25 , C07C233/27 , C07C233/33 , C07C233/44 , C07C233/60 , C07C233/75 , C07C233/91 , C07C239/00 , C07C255/13 , C07C259/06 , C07C259/08 , C07C259/10 , C07C271/28 , C07C271/38 , C07C313/32 , C07C325/00 , C07C327/22 , C07C327/40 , C07C327/46 , C07C327/50 , C07C333/08 , C07C333/24 , C07D317/28 , C07C125/065
CPC分类号： A01N39/00 , A01N47/20 , A01N47/40 , A01N53/00 , C07D317/28
摘要： A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, and particularly against strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.

79. 发明授权

US4246279A Novel dichloromaleic acid diamide derivatives and their use as fungicides 失效
标题翻译：新型二氯马来酸二酰胺衍生物及其作为杀真菌剂的用途
公开(公告)号：US4246279A
公开(公告)日：1981-01-20
申请号：US8145
申请日：1979-01-31
申请人： Gerhard Bonse , Heinz U. Blank , Wilhelm Brandes , Paul Volker
发明人： Gerhard Bonse , Heinz U. Blank , Wilhelm Brandes , Paul Volker
IPC分类号： A01N37/18 , A01N37/22 , A01N37/30 , A01N43/16 , A01N47/02 , C07C67/00 , C07C233/09 , C07C233/15 , C07C233/20 , C07C233/27 , C07C233/38 , C07C253/00 , C07C255/29 , C07C313/00 , C07C323/41 , C07D307/52 , C07D309/04 , C07D309/20 , C07C103/58 , A01N9/20
CPC分类号： C07D309/04 , A01N37/22 , A01N37/30 , A01N43/16 , A01N47/02 , C07D307/52 , C07D309/20
摘要： Dichloromaleic acid diamides of the formula ##STR1## in which R represents an optionally substituted aliphatic radical with up to 8 carbon atoms, a cycloalkyl radical with 3 to 6 carbon atoms or a substituted phenyl radical,which possess fungicidal properties, are produced by reacting a dichloromaleic halide of the formula ##STR2## in which X is halogen,with an amine of the formulaH.sub.2 N--Rin a diluent and in the presence of an acid-binding agent.
摘要翻译：其中R表示具有至多8个碳原子的任选取代的脂肪族基团，具有3至6个碳原子的环烷基或具有杀真菌性质的取代苯基的式“IMAGE”的二氯苹果酸二酰胺通过使其中X是卤素的式“IMAGE”的二氯马来酰卤与式H2N-R的胺在稀释剂中并在酸结合剂的存在下反应。

80. 发明授权

US4149874A Substituted cyclopropylmethoxy anilides and their use as herbicides 失效
标题翻译：取代的环丙基甲氧基苯胺及其作为除草剂的用途
公开(公告)号：US4149874A
公开(公告)日：1979-04-17
申请号：US807940
申请日：1977-06-21
申请人： Raymond A. Felix
发明人： Raymond A. Felix
IPC分类号： C07C1/02 , A01N37/24 , A01N37/26 , A01N47/20 , A01N47/30 , A01N47/34 , A01N53/00 , C07C17/26 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/25 , C07C233/27 , C07C233/60 , C07C233/91 , C07C235/88 , C07C239/00 , C07C271/12 , C07C271/28 , C07C275/32 , C07C275/34 , C07C275/50 , C07C275/64 , C07C325/00 , C07C333/08 , A01N9/20 , C07C103/127 , C07C103/133 , C07C103/19
CPC分类号： A01N53/00 , A01N37/24 , A01N47/20 , A01N47/30 , C07C17/2635
摘要： Compounds having the formula ##STR1## in which R.sub.1 is alkyl, lower alkenyl, chloro-lower alkyl, lower cycloalkyl, lower alkoxy, thio-lower alkyl, or ##STR2## R.sub.2 is hydrogen, lower alkoxyalkyl or lower alkanoyl; R.sub.3 and R.sub.4 are independently hydrogen, lower alkyl or lower alkoxy; X and Y are independently chloro, fluoro or bromo; Z is hydrogen, methyl, dimethyl, or one methyl and one chloro substituent; and n is 0 or 1. The compounds have utility as herbicides, particularly as post-emergence herbicides.
摘要翻译： {PG，1具有式{r1 {tc，1 {rb {rd，11447799ccff {b1，44 {501 {a，1 {bn，c {sd，5 {sb，26Cl {hd n {a， {bl，bb {bn，55 {sd，11 {s，5 N {M，2 {AB，2 {M，3 {AD，0 O {MR，3 CR {HD 1 {MR，2 { R {HD 2 {A，2 {BN，0 {US，5 {SB，4 OCH {HD 2 {US，5 {LS，4288E {A，3 {BN，D {US，1 {SB， A，3 {BN，2 {US，5 {S，5Y {A，3 {BL，8 {SB，11 {BN，4 {SD，5 {S，5Z {RE {PS {PS，其中R {HD 1 {L是烷基，低级烯基，氯 - 低级烷基，低级环烷基，低级烷氧基，硫代低级烷基或{r1 {tc，1 {rb {ab，4 N {M，1 {AB，2 R {HD 3 {MR，1 {AB，6R {HD 4 {MY，1 {S，10; {RE {PS {PS R {HD 2 {L是氢，低级烷氧基烷基或低级烷酰基; R {HD 3 {L和R {HD 4 {L独立地是氢，低级烷基或低级烷氧基; X和Y独立地是氯，氟或溴; Z是氢，甲基，二甲基或一个甲基和一个氯取代基; 并且n为0或1.该化合物具有除草剂的作用，特别是作为芽后除草剂。

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