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1. 发明申请

US20180118706A1 Synthetic Route To Anhydroryanodol, Ryanodol And Structural Analogues 审中-公开
公开(公告)号：US20180118706A1
公开(公告)日：2018-05-03
申请号：US15848686
申请日：2017-12-20
申请人： California Institute of Technology
发明人： Sarah Reisman , Kangway V. Chuang , Chen Xu
IPC分类号： C07D309/30 , C07C49/753 , C07D309/32 , C07C43/23 , C07C49/743 , C07C49/577 , C07C43/315
CPC分类号： C07D309/30 , C07C43/23 , C07C43/315 , C07C49/577 , C07C49/743 , C07C49/753 , C07D309/32
摘要： This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogues thereof and novel compounds prepared thereby.

2. 发明申请

US20130123367A1 VINYLOGOUS CHALCONE DERIVATIVES AND THEIR MEDICAL USE 审中-公开
标题翻译：乙酰胆碱衍生物及其医学用途
公开(公告)号：US20130123367A1
公开(公告)日：2013-05-16
申请号：US13811739
申请日：2011-07-27
申请人： Thomas Erker , Gerda Brunhofer , Ulrich Jäger , Katrina Vanura , Verena Dirsch , Elke Heiss
发明人： Thomas Erker , Gerda Brunhofer , Ulrich Jäger , Katrina Vanura , Verena Dirsch , Elke Heiss
IPC分类号： C07C49/255 , C07C49/577 , C07C323/22
CPC分类号： C07C49/255 , A61K31/121 , A61K45/06 , C07C49/577 , C07C49/755 , C07C49/84 , C07C323/22 , C07C2602/08 , C07F17/02 , A61K2300/00
摘要： The present invention relates to vinylogous chalcone derivatives, in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these compounds, and their medical use, including their use in the treatment or prevention of cancer, in particular malignant hematological diseases/disorders.
摘要翻译：本发明涉及野生型查耳酮衍生物，特别是本文所述和定义的式（I）化合物，包含这些化合物的药物组合物及其医学用途，包括其在治疗或预防癌症中的用途，特别是恶性血液学疾病/病症。

3. 发明申请

US20100034766A1 Malodor Counteracting Compositions 审中-公开
标题翻译：恶臭反应组合
公开(公告)号：US20100034766A1
公开(公告)日：2010-02-11
申请号：US12444752
申请日：2007-10-22
申请人： Thomas McGee , Felix Flachsmann , Markus Gautschi , Philip Kraft , Richard P. Sgaramella , Kumar Venkateswara Vedantam
发明人： Thomas McGee , Felix Flachsmann , Markus Gautschi , Philip Kraft , Richard P. Sgaramella , Kumar Venkateswara Vedantam
IPC分类号： A61L9/01 , C07C69/74 , C07C49/00
CPC分类号： C07C69/716 , A61L9/01 , C07C49/175 , C07C49/255 , C07C49/35 , C07C49/577 , C07C69/34 , C07C69/40 , C07C69/708 , C07C233/05 , C07C2601/14 , C11B9/0019 , C11B9/0034 , C11B9/0061
摘要： A malodor counteracting composition comprising at least one compound of formula (A) and at least one compound of formula (B) wherein n, X, Y and R1 to R4 are as defined in the description.
摘要翻译：包含至少一种式（A）化合物和至少一种式（B）化合物的恶臭反作用组合物，其中n，X，Y和R 1至R 4如说明书中所定义。

4. 发明授权

US06864264B1 1-adamantyl chalcones for the treatment of proliferative disorders 失效
标题翻译： 1-金刚烷基查尔酮用于治疗增殖性疾病
公开(公告)号：US06864264B1
公开(公告)日：2005-03-08
申请号：US10224723
申请日：2002-08-20
申请人： Gloria L. Anderson , Tawfeq Abdul-Raheem Kaimari
发明人： Gloria L. Anderson , Tawfeq Abdul-Raheem Kaimari
IPC分类号： A61K31/44 , A61K31/47 , A61K45/06 , C07D213/00 , C07D215/00
CPC分类号： C07D215/14 , A61K31/44 , A61K31/47 , A61K45/06 , C07C45/46 , C07C45/74 , C07C49/567 , C07C49/577 , C07C49/653 , C07C49/83 , C07C49/84 , C07C205/45 , C07C225/22 , C07C255/56 , C07C2603/74 , A61K2300/00 , C07C49/563
摘要： The present invention relates to the compounds of the general formula (I), a composition for and a method of treating breast cancer or other proliferative disorders in a subject using a compound of general formula [I], wherein the substituents are as defined in the specification.
摘要翻译：本发明涉及通式（I）的化合物，使用通式[I]化合物治疗受试者的乳腺癌或其他增殖性病症的组合物和方法，其中取代基如规范。

5. 发明申请

US20020169170A1 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US20020169170A1
公开(公告)日：2002-11-14
申请号：US10022045
申请日：2001-12-18
发明人： Alexander Glenn Godfrey , Daniel Timothy Kohlman , John Cunningham O' Toole , Yao-Chang Xu , Tony Yantao Zhang
IPC分类号： A61K031/495 , A61K031/496
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： A method for potentiating the action of a serotonin reuptake inhibitor in increasing the availability of serotonin, norepinephrin and dopamine in the brain, comprising administering to a patient in need of such treatment a serotonin reuptake inhibitor in combination with an effective amount of a compound of the formula 1 wherein Arnull is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkyl halo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkyl halo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is null(CnullO)null, nullCHOHnull or nullCH2null; or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof.
摘要翻译：一种用于增强5-羟色胺再摄取抑制剂在增加脑中5-羟色胺，去甲肾上腺素和多巴胺的可利用性的作用的方法，包括向需要这种治疗的患者施用5-羟色胺再摄取抑制剂与有效量的其中Ar'是被一至三个选自氢，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6）烷基， -C 6）烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R1是氢，（C1-C6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基; R2是被一个或两个选自氢（C1-C6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基，（C2-C6）烷基）取代基取代的苯基，萘基或（C3-C12））烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R 3选自氢（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6）烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤素，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; X是 - （C = O） - ， - CHOH-或-CH 2 - ; 或其药学上可接受的盐，外消旋物，旋光异构体或溶剂合物

6. 发明授权

US06239135B1 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US06239135B1
公开(公告)日：2001-05-29
申请号：US09208553
申请日：1998-12-09
申请人： Daniel Timothy Kohlman , Yao-Chang Xu
发明人： Daniel Timothy Kohlman , Yao-Chang Xu
IPC分类号： A61K31495
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： A series of aryl piperazine compounds of the formula: or the pharmaceutically acceptable salts thereof, are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.
摘要翻译：一系列下式的芳基哌嗪化合物或其药学上可接受的盐是用于治疗与5-羟色胺1A受体相关或受其影响的病症的有效药物; 该化合物在该受体上是特别有效的拮抗剂，特别可用于缓解尼古丁和烟草戒断症状。

7. 发明授权

US5292771A Substituted .beta.-diketones and their use 失效
标题翻译：取代的β-二酮及其用途
公开(公告)号：US5292771A
公开(公告)日：1994-03-08
申请号：US958487
申请日：1992-10-08
申请人： Reijo J. Backstrom , Erkki J. Honkanen , Jarmo J. Pystynen , Anne M. Luiro , Paivi A. Aho , Inge-Britt Y. Linden , Erkki A. O. Nissinen , Pentti Pohto
发明人： Reijo J. Backstrom , Erkki J. Honkanen , Jarmo J. Pystynen , Anne M. Luiro , Paivi A. Aho , Inge-Britt Y. Linden , Erkki A. O. Nissinen , Pentti Pohto
IPC分类号： A61K31/00 , A61K31/06 , A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/258 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C205/45 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , A61K31/38 , A61K31/44 , A61K31/47
CPC分类号： C07C205/45 , A61K31/00 , A61K31/06 , A61K31/12 , A61K31/165 , A61K31/275 , A61K31/345 , C07C233/31 , C07C235/84 , C07C255/56 , C07C317/24 , C07C49/217 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/258 , C07C49/567 , C07C49/577 , C07C65/36 , C07C65/40 , C07C2101/02
摘要： Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.
摘要翻译：式（Ⅰ）化合物其中n为0或1，R 1和R 2独立地为甲基，乙基或环丙基，R为任选取代的苯基或杂芳基或其盐或酯可用于治疗炎症性肠病。

8. 发明授权

US5086074A 1-aminomethyl-1,2,3,4-tetrahydronaphthalenes 失效
标题翻译： 1-氨基甲基-1,2,3,4-四氢萘
公开(公告)号：US5086074A
公开(公告)日：1992-02-04
申请号：US499232
申请日：1990-03-26
申请人： John F. DeBernardis , Robert E. Zelle , Fatima Z. Basha
发明人： John F. DeBernardis , Robert E. Zelle , Fatima Z. Basha
IPC分类号： C07C45/00 , C07C45/46 , C07C45/63 , C07C45/71 , C07C49/577 , C07C49/697 , C07C49/747 , C07C49/753 , C07C62/32 , C07C62/34 , C07C211/30 , C07C215/50 , C07C217/74 , C07C229/50 , C07C233/18 , C07C255/47 , C07C259/08 , C07C323/22 , C07D207/06 , C07D207/08 , C07D207/32 , C07D207/335 , C07D213/38 , C07D307/52 , C07D317/70 , C07D319/20 , C07D319/22 , C07D333/20 , C07D333/24 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14
CPC分类号： C07D207/08 , C07C211/30 , C07C215/50 , C07C217/74 , C07C229/50 , C07C233/18 , C07C255/47 , C07C259/08 , C07C323/22 , C07C45/004 , C07C45/46 , C07C45/63 , C07C45/71 , C07C49/577 , C07C49/697 , C07C49/747 , C07C49/753 , C07C62/32 , C07C62/34 , C07D207/06 , C07D207/335 , C07D213/38 , C07D307/52 , C07D317/70 , C07D319/20 , C07D319/22 , C07D333/20 , C07D333/24 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07C2101/08 , C07C2102/10
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sup.2 is selected from hydroxy and lower alkoxy, R.sup.5 is lower alkyl, and R.sup.11 and R.sup.12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective .alpha..sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.
摘要翻译：下式化合物及其药学上可接受的盐，其中R2选自羟基和低级烷氧基，R5是低级烷基，R11和R12独立地选自氢，卤素，羟基，甲氧基和低级烷基，是选择性的可用于治疗青光眼的α2肾上腺素能受体拮抗剂。

9. 发明授权

US4829091A Process for the preparation of ketones and novel insecticides produced therefrom 失效
标题翻译：用于制备由其制备的酮和新型杀虫剂的方法
公开(公告)号：US4829091A
公开(公告)日：1989-05-09
申请号：US55265
申请日：1987-05-27
申请人： Frank D. Mills , Richard T. Brown , Giles D. Mills, Jr
发明人： Frank D. Mills , Richard T. Brown , Giles D. Mills, Jr
IPC分类号： A01N35/02 , A01N43/08 , C07C45/67 , C07C49/577 , C07D307/42
CPC分类号： C07C45/676 , A01N35/02 , A01N43/08 , C07C49/577 , C07D307/42
摘要： An improved method for the decarbalkoxylation of alkylated .beta.-keto esters to obtain high yields of ketones. In accordane with the method, decarbalkoxylation of alkylated .beta.-keto esters is accomplished by heating the esters in the presence of dilute aqueous alkali and an effective amount of a phase-transfer agent. The method produces commercially practical yields of ketone in a manner which is facile, economical and environmentally safe. Novel methylene-linked pyrethroid ketones produced from the improved method exhibit insecticidal activity against various agricultural pests.
摘要翻译：烷基化β-酮酯的脱烷基氧化的改进方法，以获得高产率的酮。根据该方法，烷基化β-酮酯的脱烷基氧化通过在稀碱水溶液和有效量的相转移剂的存在下加热酯来实现。该方法以便利，经济和环境安全的方式产生商业上实用的酮产率。由改进的方法生产的新型亚甲基联结的拟除虫菊酯对各种农业害虫具有杀虫活性。

10. 发明授权

US4182729A Arylvinyl cyclopropyl ketones 失效
标题翻译：芳基乙烯基环丙基酮
公开(公告)号：US4182729A
公开(公告)日：1980-01-08
申请号：US885575
申请日：1978-03-13
申请人： Joseph C. Collins
发明人： Joseph C. Collins
IPC分类号： C07C33/34 , C07C33/50 , C07C45/68 , C07C45/74 , C07C49/213 , C07C49/215 , C07C49/217 , C07C49/223 , C07C49/233 , C07C49/235 , C07C49/245 , C07C49/255 , C07C49/567 , C07C49/573 , C07C49/577 , C07D317/54 , C07D317/60 , C07C49/84 , C07D317/06
CPC分类号： C07D317/60 , C07C33/34 , C07C33/50 , C07C45/74 , C07C49/567 , C07C49/573 , C07C49/577 , C07D317/54
摘要： Aryl substituted diketones and keto-esters, useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester. The intermediate iodides are prepared by condensing a methyl cyclopropyl ketone with an aromatic aldehyde to give an arylvinyl cyclopropyl ketone, reducing the latter to an arylethyl cyclopropyl carbinol or arylvinyl cyclopropyl carbinol, treating the carbinol with phosphorus tribromide and then with zinc bromide to give an arylalkyl or arylalkenyl bromide, and then replacing the bromine atom by iodine.
摘要翻译：通过使芳基烷基或芳基烯基碘与适当的二酮或酮酯的金属盐反应来制备用作抗病毒剂和杀虫剂的芳基取代的二酮和酮酯。中间体碘化物通过将甲基环丙基酮与芳族醛缩合得到芳基乙烯基环丙基酮，将其还原成环丙基甲醇或芳基乙烯基环丙基甲醇的芳基乙基酯，然后用溴化三溴化硼处理甲醇，得到芳基烷基或芳基烯基溴，然后用碘代替溴原子。

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