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1. 发明授权

US11565996B2 Compounds for use as inhibitors of alternative oxidase or cytochrome bc1 complex 有权
公开(公告)号：US11565996B2
公开(公告)日：2023-01-31
申请号：US17060013
申请日：2020-09-30
申请人： AlternOx Scientific Limited
发明人： Anthony Lennox Moore , Mary Susan Albury , Luke Edward Young , Catherine Elliott
IPC分类号： C07C255/53 , C07C235/60 , A61K31/11 , C07C39/373 , C07C47/565 , C07C49/835 , A01N49/00 , C07C69/63 , C07C65/28 , C07C69/84 , C07C69/18 , C07C69/157 , C07C39/24 , A01N31/16 , A01N35/04 , A01N37/24 , A01N37/40 , A01N37/44 , C07C43/178 , A01N63/50 , A01N37/02 , A01N37/34 , A61K31/055 , A61K31/085 , A61K31/12 , A61K31/166 , A61K31/222 , A61K31/277 , C07C43/23 , C07C69/21
摘要： The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.

2. 发明授权

US09447019B2 Fluorinated CBD compounds, compositions and uses thereof 有权
标题翻译：氟化CBD化合物，组合物及其用途
公开(公告)号：US09447019B2
公开(公告)日：2016-09-20
申请号：US14759689
申请日：2014-01-08
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD , UNIVERSIDADE DE SAO PAULO-USP , UNIVERSIDADE FEDERAL DO RIO GRANDE DO SUL-UFRGS
发明人： Raphael Mechoulam , Antonio Waldo Zuardi , Flavio Pereira Kapczinski , Jaime Eduardo Cecilio Hallak , Francisco Silveira Guimaraes , Jose Alexandre de Souza Crippa , Aviva Breuer
IPC分类号： A61K31/055 , C07C39/42 , C07C69/63 , C07C69/16 , C07C39/373
CPC分类号： A61K31/055 , C07C39/373 , C07C39/42 , C07C69/16 , C07C69/63 , C07C2601/16
摘要： The present invention relates to fluorine substituted CBD compounds, compositions thereof and uses thereof for the preparation of medicaments.
摘要翻译：本发明涉及氟取代的CBD化合物及其组合物及其用于制备药物的用途。

3. 发明申请

US20150203445A1 COMPOUNDS FOR USE AS INHIBITORS OF ALTERNATIVE OXIDASE OR CYTOCHROME BC1 COMPLEX 审中-公开
标题翻译：用作替代性氧化酶或细胞色素BC1复合物的化合物
公开(公告)号：US20150203445A1
公开(公告)日：2015-07-23
申请号：US14397164
申请日：2013-04-24
申请人： The University of Sussex
发明人： Anthony Lennox Moore , Mary Susan Albury , Luke Edward Young , Catherine Elliott
IPC分类号： C07C255/53 , A61K31/277 , A01N31/16 , C07C39/373 , A61K31/055 , A01N37/24 , C07C235/60 , A61K31/166 , A01N35/04 , C07C49/835 , A61K31/12 , C07C43/23 , A61K31/085 , A01N37/02 , C07C69/21 , A61K31/222 , C07C47/565 , A61K31/11 , A01N37/34
CPC分类号： C07C255/53 , A01N31/16 , A01N35/04 , A01N37/02 , A01N37/24 , A01N37/34 , A01N37/40 , A01N37/44 , A01N49/00 , A01N63/04 , A61K31/055 , A61K31/085 , A61K31/11 , A61K31/12 , A61K31/166 , A61K31/222 , A61K31/277 , C07C39/245 , C07C39/373 , C07C43/1787 , C07C43/23 , C07C47/565 , C07C49/835 , C07C65/28 , C07C69/157 , C07C69/18 , C07C69/21 , C07C69/63 , C07C69/84 , C07C235/60 , Y02A50/409
摘要： The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.
摘要翻译：本发明提供了用于抑制微生物替代氧化酶（AOX）和/或细胞色素bc1复合物的化合物。本发明延伸到这样的抑制剂在农业化学品和药物中的用途，用于治疗微生物感染，包括真菌感染。

4. 发明申请

US20130331460A1 CHRYSOPHAENTIN ANALOGS THAT INHIBIT FTSZ PROTEIN 有权
标题翻译：抑制FTSZ蛋白的CHRYSOPHAENTIN模拟物
公开(公告)号：US20130331460A1
公开(公告)日：2013-12-12
申请号：US14000761
申请日：2012-02-24
申请人： Carole A. Bewley , Peter Wipf
发明人： Carole A. Bewley , Peter Wipf
IPC分类号： C07C39/373 , A61K45/06 , C07C37/14 , A61K31/055
CPC分类号： C07C37/14 , A61K31/055 , A61K31/085 , A61K45/06 , C07C39/373 , C07C43/23 , C07D321/00 , Y02A50/473
摘要： Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, methods for using the chrysophaentin compounds, and methods for synthesizing the chrysophaentin compounds are disclosed. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.
摘要翻译：公开了抗微生物菌素化合物的实施方案，包括辣椒素化合物的药物组合物，使用辣椒素化合物的方法，以及合成辣椒素化合物的方法。辣椒素化合物的某些实施方案抑制FtsZ蛋白，从而抑制临床相关细菌（包括耐药菌株）的生长。

5. 发明授权

US5817890A Process for preparation of halogenated or pseudohalogenated cyclic organic compounds 失效
标题翻译：制备卤化或假卤代环状有机化合物的方法
公开(公告)号：US5817890A
公开(公告)日：1998-10-06
申请号：US401254
申请日：1995-03-09
申请人： Lucette Duhamel , Pierre Duhamel , Bertrand Leblond , Jean-Marie Poirier
发明人： Lucette Duhamel , Pierre Duhamel , Bertrand Leblond , Jean-Marie Poirier
IPC分类号： C07D301/26 , C07C29/10 , C07C29/124 , C07C29/64 , C07C35/48 , C07C37/06 , C07C39/24 , C07C39/26 , C07C39/28 , C07C39/373 , C07C45/51 , C07C45/58 , C07C49/463 , C07C49/687 , C07D303/08
CPC分类号： C07C45/512 , C07C35/48 , C07C45/58 , C07C49/463 , C07C49/687 , C07D303/08
摘要： The present invention relates to new fluorinated hexane compounds corresponding to the following general formula (II): ##STR1## in which X'.sub.2, X'.sub.3, and X'.sub.4 are the same or different, and denote a halogen or a pseudohalogen, preferably a halogen, more preferably chlorine and fluorine, with the condition that, when R.sub.1 is hydroxyl, cyano, amido, imido, ethoxy, benzyloxy, cyclohexyloxy and tert-butoxy, not all the halogens can simultaneously be chlorine and R.sub.4, R.sub.3 and R.sub.5 are simultaneously equal to H; R.sub.1 denotes a hydrogen, a hydrocarbon chain such as an alkyl chain, alkoxy, cycloalkyl ether, an aromatic group, aromatic ether or an alkoxy, carbonyl, carboxyl or acyloxy, cyano, amido, imido or hydroxyl group; R.sub.4 denotes a hydrogen, a fluorine atom, a hydrocarbon chain such as, for example, an alkyl chain, an aromatic group or a carbonyl, carboxyl or carboxamide group or else a radical joined to the hexane ring by a chalcogen or by an element of Group V, preferably of the first Period, such as an amido, alkoxy or acyloxy group; in which the radicals R.sub.3 and R.sub.5, which are different or preferably the same, denote a fluorine, or preferably hydrogen, atom or also a hydrocarbon chain as defined above in the case of R.sub.4.
摘要翻译：本发明涉及对应于以下通式（II）的新的氟化己烷化合物：其中X'2，X'3和X'4相同或不同，表示卤素或假卤素，优选卤素，更优选氯和氟，条件是当R1是羟基，氰基，酰氨基，亚氨基，乙氧基，苄氧基，环己氧基和叔丁氧基时，不是所有的卤素都可以同时为氯，R4，R3和R5 同时等于H; R 1表示氢，烃链如烷基链，烷氧基，环烷基醚，芳族基团，芳族醚或烷氧基，羰基，羧基或酰氧基，氰基，酰胺基，亚氨基或羟基; R4表示氢，氟原子，烃链，例如烷基链，芳族基团或羰基，羧基或羧酰胺基团，或者由硫属化合物连接到己烷环上的基团，或者由优选第一阶段的V族如酰氨基，烷氧基或酰氧基; 其中不同或优选相同的基团R3和R5表示在R4的情况下如上所定义的氟或优选氢原子或烃链。

6. 发明授权

US5243110A Dehydrochlorination of 1,1-bis(R-phenyl)-2,2,2-trichloroethanes 失效
标题翻译： 1,1-BIS（R-PHENYL）-2,2,2-三氯乙烯的脱氯
公开(公告)号：US5243110A
公开(公告)日：1993-09-07
申请号：US901072
申请日：1992-06-19
申请人： Jaume Castella Sola , Jaime Palencia Adrubau
发明人： Jaume Castella Sola , Jaime Palencia Adrubau
IPC分类号： B01J31/02 , C07B61/00 , C07C17/25 , C07C22/04 , C07C25/24 , C07C29/58 , C07C39/373 , C07C41/24 , C07C43/225 , C07C201/12 , C07C205/11
CPC分类号： C07C17/25
摘要： 1,1-Bis(R-phenyl)-2,2,2-trichloroethanes are dehydrochlorinated in high yields, e.g., into 1,1-bis(chlorophenyl)-2,2-dichloroethylenes, by reacting same with an aqueous solution of an alkali metal hydroxide, in liquid state in the presence of a phase transfer agent, e.g., a quaternary ammonium compound, but in the absence of any reaction solvent.
摘要翻译：将1,1-双（R-苯基）-2,2,2-三氯乙烷以高产率脱氯化氢，例如，通过使其与水溶液反应，形成1,1-双（氯苯基）-2,2-二氯乙烯在相转移剂（例如季铵化合物）的存在下，在不存在任何反应溶剂的情况下为液态的碱金属氢氧化物。

7. 发明授权

US5072025A Process for the production of 3,5-disubstituted-4-acetoxystyrene 失效
标题翻译：制备3,5-二取代-4-乙酰氧基苯乙烯的方法
公开(公告)号：US5072025A
公开(公告)日：1991-12-10
申请号：US559759
申请日：1990-07-26
申请人： Richard Vicari , Mohammad Aslam , Wilson B. Ray , Kenneth G. Davenport , Ralph Dammel , Juergen Lingnau , Karl-Friedrich Doessel
发明人： Richard Vicari , Mohammad Aslam , Wilson B. Ray , Kenneth G. Davenport , Ralph Dammel , Juergen Lingnau , Karl-Friedrich Doessel
IPC分类号： C07C39/373 , C07C45/54 , C07C45/63 , C07C49/825 , G03F7/038
CPC分类号： G03F7/038 , C07C39/373 , C07C45/54 , C07C45/63 , C07C49/825
摘要： 3-substituted-4-hydroxy- and 4-acetoxystyrene compounds, especially 3,5-di(methyl, bromo or chloro)-4-acetoxystyrene as well as a process for its preparation. 2,6-dimethylphenol is acylated with acetic anhydride and HF catalyzed to produce 3,5-dimethyl-4-hydroxy-acetophenone. After subsequent esterification with acetic anhydride and catalyzed hydrogenation to form 1-(3',5'-dimethyl-4'-acetoxyphenyl)ethanol, this intermediate is then dehydrated with an acid and a polymerization inhibitor to produce 3,5-dimethyl-4-acetoxystyrene.
摘要翻译： 3-取代-4-羟基 - 和4-乙酰氧基苯乙烯化合物，特别是3,5-二（甲基，溴或氯）-4-乙酰氧基苯乙烯以及其制备方法。 2,6-二甲基苯酚用乙酸酐进行酰化，HF催化反应生成3,5-二甲基-4-羟基苯乙酮。在用乙酸酐进行酯化和催化氢化后，形成1-（3'，5'-二甲基-4'-乙酰氧基苯基）乙醇，然后将该中间体用酸和阻聚剂脱水，得到3,5-二甲基-4 乙酰氧基苯乙烯

8. 发明授权

US4996225A Tri-phenyl alkane derivatives and their oestrogenic, anti-oestrogenic and progestanic uses 失效
标题翻译：三苯基烷烃衍生物及其雌激素，抗雌激素和孕激素的用途
公开(公告)号：US4996225A
公开(公告)日：1991-02-26
申请号：US420437
申请日：1989-10-12
申请人： Reijo J. Toivola , Arto J. Karjalainen , Kauko O. A. Kurkela , Marja-Liisa Soderwall , Lauri V. M. Kangas , Guillermo L. Blanco , Hannu K. Sundquist
发明人： Reijo J. Toivola , Arto J. Karjalainen , Kauko O. A. Kurkela , Marja-Liisa Soderwall , Lauri V. M. Kangas , Guillermo L. Blanco , Hannu K. Sundquist
IPC分类号： A61K31/045 , A61K31/135 , A61K31/165 , C07C29/09 , C07C29/10 , C07C29/128 , C07C33/18 , C07C33/26 , C07C33/28 , C07C37/00 , C07C37/055 , C07C39/12 , C07C39/21 , C07C39/215 , C07C39/367 , C07C39/373 , C07C43/178 , C07C43/225 , C07C43/23 , C07D207/08 , C07D295/08 , C07D295/092 , C07D307/06 , C07D307/12 , C07D307/14 , C07D309/04 , C07D309/10 , C07D309/12
CPC分类号： C07D295/088 , C07C29/095 , C07C29/10 , C07C29/1285 , C07C309/00 , C07C33/26 , C07C33/28 , C07C37/001 , C07C37/055 , C07C39/12 , C07C39/21 , C07C39/367 , C07C39/373 , C07C43/1782 , C07C43/225 , C07C43/23 , C07D307/06 , C07D307/12 , C07D307/14 , C07D309/04 , C07D309/12
摘要： ##STR1## wherein n is 0 to 4, R
1 and R
2 , which can be the same or different, are H or OH; R
3 is --O--(CH
2 )
m --CH
2 --NR
6 R
7 wherein m is 1 or 2, R
6 and R
7 , which can be the same or different, are H or an alkyl group of 1 to 4 carbon atoms, or --NR
6 R
7 can form a pyrrolidinyl group; and R
4 is halogen, and their non-toxic pharmaceutically acceptable salts and phenolic esters of aliphatic or aromatic carboxylic acids, acid anhydrides or acid chlorides thereof are disclosed. These compounds exhibit valuable pharmacological properties as estrogenic, anti-estrogenic, and progestanic agents. They show activity against oestrogen-dependent tumors.

9. 发明授权

US4963590A Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same 失效
标题翻译：药理活性化合物，其制备方法和含有它们的组合物
公开(公告)号：US4963590A
公开(公告)日：1990-10-16
申请号：US126911
申请日：1987-11-27
申请人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka T. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
发明人： Reijo J. Backstrom , Kalevi E. Heinola , Erkki J. Honkanen , Seppo K. Kaakkola , Pekka J. Kairisalo , Inge-Britt Y. Linden , Pekka T. Mannisto , Erkki A. O. Nissinen , Pentti Pohto , Aino K. Pippuri , Jarmo J. Pystynen
IPC分类号： C07C27/00 , A61K31/00 , A61K31/04 , A61K31/045 , A61K31/047 , A61K31/05 , A61K31/06 , A61K31/075 , A61K31/085 , A61K31/11 , A61K31/12 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/33 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/47 , A61K31/495 , A61P9/12 , A61P25/00 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07C20060101 , C07C39/08 , C07C39/24 , C07C39/26 , C07C39/373 , C07C43/20 , C07C43/23 , C07C45/00 , C07C45/56 , C07C45/67 , C07C45/74 , C07C47/52 , C07C47/565 , C07C47/575 , C07C49/20 , C07C49/245 , C07C49/747 , C07C49/76 , C07C49/83 , C07C49/835 , C07C49/84 , C07C59/40 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/68 , C07C59/90 , C07C65/00 , C07C65/03 , C07C65/21 , C07C67/00 , C07C69/017 , C07C69/035 , C07C69/73 , C07C69/76 , C07C205/20 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07C213/00 , C07C231/00 , C07C233/00 , C07C233/12 , C07C235/44 , C07C235/54 , C07C235/66 , C07C239/00 , C07C253/00 , C07C255/37 , C07C255/53 , C07C301/00 , C07C309/65 , C07C311/15 , C07C317/22 , C07D207/32 , C07D207/325 , C07D207/333 , C07D211/14 , C07D211/22 , C07D211/30 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/08 , C07D295/13 , C07D295/18 , C07D295/185 , C07D317/52 , C07D317/62 , C07D319/24 , C07D405/04 , C07D405/06
CPC分类号： C07D207/333 , C07C205/22 , C07C205/23 , C07C205/26 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/56 , C07C205/57 , C07C255/00 , C07C317/00 , C07C323/00 , C07C43/23 , C07C45/565 , C07C45/673 , C07C45/74 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07C59/56 , C07C59/64 , C07C59/68 , C07D211/32 , C07D211/58 , C07D213/30 , C07D215/14 , C07D295/13 , C07D295/185 , C07D317/62 , C07D319/24 , C07D405/04
摘要： Pharmacologically active catechol derivatives of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently comprise hydrogen, alkyl, acyl, optionally substituted aroyl, lower alkylsulfonyl or alkylcabamoyl or taken together form a lower alkylidene or cycloalkylidene, X comprises an electronegative substituent such as halogen, nitro, cyano, lower alkylsulfonyl, sulfonamido, aldehyde, caboxyl or trifluoromethyl and R.sub.3 comprises hydrogen, halogen, hydroxy alkyl, amino, nitro, cyano, trifluoromethyl, lower alkylsulfonyl, sulfonamide, aldehyde, alkyl carbonyl, aralkylidene carbonyl or carboxyl or a group selected from ##STR2## wherein R.sub.4 comprises hydrogen, alkyl, cyano, carboxyl or acyl and R.sub.5 comprises hydrogen, cyano, carboxyl, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, optionally substituted aroyl or heteroaroyl, hydroxyalkyl or carboxyalkyl or R.sub.4 and R.sub.5 together form a five to seven membered substituted cycloalkanone ring;--(CO).sub.n (CH.sub.2).sub.m --CORwherein n is 0-1 and m is 0-7 and R comprises hydroxy, alkyl, carboxyalkyl, optionally substituted alkene, alkoxy or optionally substituted amino; ##STR3## wherein R.sub.8 and R.sub.9 independently comprise hydrogen or one of the following optionally substituted groups; alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, or together form an optionally substituted piperidyl group;--NH--CO--R.sub.10wherein R.sub.10 comprises a substituted alkyl group.
摘要翻译：式I的药理活性儿茶酚衍生物其中R 1和R 2独立地包括氢，烷基，酰基，任选取代的芳酰基，低级烷基磺酰基或烷基氨基甲酰基，或一起形成低级亚烷基或环烷叉基，X包括电负性取代基如卤素，硝基，氰基，低级烷基磺酰基，亚磺酰氨基，醛，呋喃甲酰基或三氟甲基，R3包括氢，卤素，羟基烷基，氨基，硝基，氰基，三氟甲基，低级烷基磺酰基，磺酰胺，醛，烷基羰基，亚烷基羰基或羧基或选自其中R 4包括氢，烷基，氰基，羧基或酰基，R 5包括氢，氰基，羧基，烷氧基羰基，羧基烯基，硝基，酰基，任选取代的芳酰基或杂芳酰基，羟基烷基或羧基烷基或R4和R5一起形成五至七元取代的环烷酮环; - （CO）n（CH 2）m -COR其中n为0-1，m为0-7，R为羟基，烷基，羧基烷基，任选取代的烯烃，烷氧基或任选取代的氨基; 其中R8和R9独立地包含氢或以下任选取代的基团之一; 烷基，烯基，炔基，环烷基，芳烷基，或一起形成任选取代的哌啶基; -NH-CO-R 10，其中R 10包含取代的烷基。

10. 发明授权

US4801616A Diphenylmethanone compounds and anti-inflammatory use thereof 失效
标题翻译：二苯甲酮化合物及其抗炎用途
公开(公告)号：US4801616A
公开(公告)日：1989-01-31
申请号：US843907
申请日：1986-03-25
申请人： D. Mark Gapinski
发明人： D. Mark Gapinski
IPC分类号： A61K31/047 , A61K31/05 , A61K31/085 , A61K31/12 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/235 , A61K31/275 , A61K31/34 , A61K31/343 , A61K31/41 , A61P29/00 , A61P43/00 , C07C27/00 , C07C39/373 , C07C41/00 , C07C43/20 , C07C45/46 , C07C45/62 , C07C45/67 , C07C45/71 , C07C49/82 , C07C49/83 , C07C49/835 , C07C49/84 , C07C59/215 , C07C59/90 , C07C65/105 , C07C65/21 , C07C65/24 , C07C65/28 , C07C65/34 , C07C67/00 , C07C69/035 , C07C69/16 , C07C69/94 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/42 , C07C235/84 , C07C253/00 , C07C255/54 , C07D257/04 , C07D307/79 , C07D307/86 , C07C121/76 , C07D257/02
CPC分类号： C07D257/04 , C07C255/00 , C07C45/46 , C07C45/62 , C07C45/67 , C07C45/673 , C07C45/71 , C07C49/83 , C07C49/84 , C07C59/90
摘要： This invention provides certain diphenylmethane derivatives, their pharmaceutical formulations, and their use in treating inflammation and arthritis in mammals.
摘要翻译：本发明提供某些二苯基甲烷衍生物，其药物制剂及其在治疗哺乳动物炎症和关节炎中的用途。

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