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    • 3. 发明授权
    • Benzylamine analogues
    • 苄胺类似物
    • US07514475B2
    • 2009-04-07
    • US11583499
    • 2006-10-19
    • Kazuo KoyamaShinji MarumotoNarihiro TodaHiroshi KogenKeiko Suzuki
    • Kazuo KoyamaShinji MarumotoNarihiro TodaHiroshi KogenKeiko Suzuki
    • A61K31/137C07C205/04
    • C07C219/30C07C271/44C07C323/20C07C323/25C07C333/04C07D213/64C07D213/68C07D215/20C07D317/58C07D333/38
    • A compound of the formula (I): wherein R1 is a C1-C6 alkyl, an amino, a (C1-C6 alkyl)amino, a di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and are a hydrogen or a C1-C6 alkyl; Arom is an unsubstituted or substituted aryl or an unsubstituted or substituted heteroaryl; wherein the substituted aryl is substituted at 1 to 5 positions and the substituted heteroaryl is substituted at 1 to 3 positions; wherein the heteroaryl is furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; and wherein the substituents of the substituted aryl and of the substituted heteroaryl are independently halogen, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro or carboxyl; A is an ethylene or propylene; Ra is a hydrogen, a C1-C6 alkyl or a C2-C6 alkenyl; E is a single bond, an oxygen, a sulfur or —NR4—, wherein R4 is a hydrogen or a C1-C7 alkanoyl; X1 and X2 are the same or different and are an oxygen or a sulfur, or a pharmacologically acceptable salt or ester thereof.
    • 式(I)的化合物:其中R1是C1-C6烷基,氨基,(C1-C6烷基)氨基,二(C1-C6烷基)氨基或含氮饱和杂环; R2和R3相同或不同,为氢或C1-C6烷基; Arom是未取代或取代的芳基或未取代或取代的杂芳基; 其中取代的芳基在1至5个位置被取代,并且取代的杂芳基在1至3个位置被取代; 吡唑基,咪唑基,恶唑基,异恶唑基,噻唑基,异噻唑基,1,2,3-恶二唑基,吡喃基,吡啶基,哒嗪基,嘧啶基,吡嗪基或喹啉基;其中杂芳基为呋喃基,噻吩基,吡咯基, 并且其中取代的芳基和取代的杂芳基的取代基独立地为卤素,C 1 -C 6烷基,卤代C 1 -C 6烷基,C 1 -C 6烷氧基,C 1 -C 6烷硫基,C 1 -C 3亚烷基二氧基,C 1 -C 7烷酰基, C7烷氧基羰基,氨基,C1-C7烷酰基氨基,羟基,巯基,氰基,硝基或羧基; A是乙烯或丙烯; R a是氢,C 1 -C 6烷基或C 2 -C 6烯基; E是单键,氧,硫或-NR4-,其中R4是氢或C1-C7烷酰基; X1和X2相同或不同,为氧或硫,或其药理学上可接受的盐或酯。
    • 5. 发明授权
    • Amino acid derivatives
    • 氨基酸衍生物
    • US06018020A
    • 2000-01-25
    • US96570
    • 1998-06-12
    • Michael Richard AttwoodDavid Nigel HurstPhilip Stephen JonesPaul Brittain KayTony Michael RaynhamFrancis Xavier Wilson
    • Michael Richard AttwoodDavid Nigel HurstPhilip Stephen JonesPaul Brittain KayTony Michael RaynhamFrancis Xavier Wilson
    • C12N15/09A01N43/34A01N43/36A61K38/00A61P31/12A61P31/14C07C205/04C07C205/45C07C271/18C07D207/12C07D207/20C07D211/70C07D223/04C07D227/04C07D405/10C07D407/10C07D409/10C07K7/06A61K38/08
    • C07K7/06A61K38/00
    • The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.7 represent lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl;R.sup.8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; andR.sup.9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower alkoxycarbonyl,and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.
    • 本发明提供下式的氨基酸衍生物,其中E代表CHO或B(OH)2; R 1表示低级烷基(任选被卤素,氰基,低级烷硫基,芳基 - 低级烷硫基,芳基或杂芳基取代),低级烯基或低级炔基; R 2表示任选被羟基,羧基,芳基,氨基羰基或低级环烷基取代的低级烷基; 并且R 3表示氢或低级烷基; 或R 2和R 3一起表示任选被羟基取代的二 - 或三亚甲基; R4代表低级烷基(任选被羟基,低级环烷基,羧基,芳基,低级烷硫基,氰基 - 低级烷硫基或芳基 - 低级烷硫基取代),低级烯基,芳基或低级环烷基; R5代表低级烷基(任选被羟基,低级烷硫基,芳基,芳基 - 低级烷硫基或氰基 - 低级烷硫基取代)或低级环烷基; R6代表氢或低级烷基; R7代表低级烷基(任选被羟基,羧基,芳基或低级环烷基取代)或低级环烷基; R8代表任选被羟基,羧基或芳基取代的低级烷基; 并且R 9表示低级烷基羰基,羧基 - 低级烷基羰基,芳基羰基,低级烷基磺酰基,芳基磺酰基,低级烷氧基羰基或芳基 - 低级烷氧基羰基,以及式I酸性化合物与碱的碱,其为用作抗病毒剂的病毒蛋白酶抑制剂, 治疗或预防丙型肝炎,丙型肝炎和人类GB病毒引起的感染。
    • 6. 发明授权
    • Process for the acylation of aromatic ethers
    • 芳香醚酰化的方法
    • US6013840A
    • 2000-01-11
    • US765533
    • 1997-01-09
    • Michel SpagnolLaurent GilbertEric BenazziChristian Marcilly
    • Michel SpagnolLaurent GilbertEric BenazziChristian Marcilly
    • B01J29/08C07C45/46C07C49/84C07C205/04C07C211/09C07C231/12C07C235/32C07C253/30C07C255/40C07C45/00
    • B01J29/084C07C45/46
    • The present invention concerns a process for the acylation of an aromatic ether.Preferably the invention relates to a process for the acylation of a substituted aromatic ether, in particular veratrol.The acylation process of the invention consists of reacting the ether with an acylation agent in the presence of a zeolitic catalyst, and is characterized in that the acylation reaction is carried out in the presence of an effective quantity of a catalyst comprising a faujasite type zeolite or a Y zeolite with the following physico-chemical characteristics:an atomic ratio denoted "global Si/Me.sup.1 " between the number of atoms of the element silicon and the number of atoms of every trivalent element Me.sup.1 contained in the zeolite in the range 2.4 to 90, preferably in the range 2.4 to 75, and more preferably in the range 2.4 to 60;an Me.sup.2 alkali metal content such that the atomic ratio Me.sup.2 /Me.sup.1(IV) between the number of atoms of alkali metal Me.sup.2 and the number of atoms of every trivalent element Me.sup.1(IV) included in the zeolitic network is less than 0.2, preferably less than 0.1, and more preferably less than 0.05.
    • PCT No.PCT / FR96 / 00716 Sec。 371日期1997年1月9日 102(e)日期1997年1月9日PCT提交1996年5月10日PCT公布。 出版物WO96 / 35655 日期:1996年11月14日本发明涉及一种酰化芳族醚的方法。 优选地,本发明涉及酰化取代的芳族醚,特别是藜芦醇的方法。 本发明的酰化方法包括在沸石催化剂存在下使醚与酰化剂反应,其特征在于酰化反应在有效量的含有八面沸石型沸石的催化剂或 具有以下物理化学特性的Y沸石:在元素硅的原子数与沸石中所含的每个三价元素Me1的原子数在2.4至90之间的原子比表示为“全局Si / Me1” ,优选在2.4至75范围内,更优选在2.4至60范围内; Me2碱金属含量使得碱金属Me2的原子数与沸石网络中包含的每个三价元素Me1(IV)的原子数之间的原子比Me2 / Me1(IV)小于0.2,优选较少 小于0.1,更优选小于0.05。