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81. 发明申请

US20040199002A1 Process for producing(2-nitrophenyl)acetonitrile derivative and intermediate therefor 审中-公开
标题翻译：制备（2-硝基苯基）乙腈衍生物及其中间体的方法
公开(公告)号：US20040199002A1
公开(公告)日：2004-10-07
申请号：US10490656
申请日：2004-03-25
发明人： Tetsuya Abe , Toshihiro Nagata , Fumiaki Takabe , Kazuto Umezu , Yusuke Hamada
IPC分类号： C07C255/53
CPC分类号： C07C251/40 , C07C201/12 , C07C217/48 , C07C249/08 , C07C253/00 , C07D295/096 , C07C255/37 , C07C255/41 , C07C205/34 , C07C205/44 , C07C205/61
摘要： The present invention lies in a process for producing a compound represented by the following formula nullIVnull, which comprises the following steps (1) to (3), as well as in an intermediate therefor. (1) A step which comprises reacting a compound represented by the following formula nullInull with a compound represented by the following formula nullVInull or with a mixture of a compound represented by the following formula nullVIInull and a compound represented by the following formula nullVIIInull to obtain a compound represented by the following formula nullIXnull, and hydrolyzing the compound represented by the formula nullIXnull under acidic conditions to obtain a compound represented by the following formula nullIInull. (2) A step which comprises reacting the compound represented by the formula nullIInull with hydroxylamine to obtain a compound represented by the following formula nullIIInull. (3) A step which comprises dehydrating the compound represented by the formula nullIIInull to obtain a compound represented by the formula nullIVnull. 1 null(R1)(R2)NnullCH(OR3)(OR4) nullnullnullVInull(CH3)2NnullCH(OCH3)2 nullnullnullVIInull(R1)(R2)NH nullnullnullVIIInull 2
摘要翻译：本发明在于制备由下式（Ⅳ）表示的化合物的方法，该方法包括以下步骤（1）至（3），以及其中间体。（1）使下述式[I]表示的化合物与下述式[Ⅵ]表示的化合物或下式[Ⅶ]表示的化合物的混合物与式得到下述式[Ⅸ]表示的化合物，在酸性条件下水解式[Ⅸ]表示的化合物，得到下述式[Ⅱ]表示的化合物。（2）使式[II]表示的化合物与羟胺反应，得到下式[III]表示的化合物的工序。（3）使式[III]表示的化合物脱水，得到式[IV]表示的化合物的工序。（R1）（R2）N-CH（OR3）（OR4）[VI]（CH3）2N-CH（OCH3）2 [VII]（R1）（R2）NH [

82. 发明申请

US20030060630A1 Method for the manufacture of Anagrelide 有权
标题翻译：阿那格雷制造方法
公开(公告)号：US20030060630A1
公开(公告)日：2003-03-27
申请号：US10134088
申请日：2002-04-25
申请人： Shire US Inc.
发明人： Philip C. Lang , Roxanne P. Spencer , Wen-Lung Yeh , Michael Joseph Roth
IPC分类号： C07D487/14
CPC分类号： C07D487/04 , C07C201/08 , C07C201/12 , C07C227/04 , C07C227/16 , C07C229/16 , C07C205/12 , C07C205/26 , C07C205/44
摘要： Methods are provided for making Anagrelide base from 2,3-dichlorobenzaldehyde. A method is also provided for making an intermediate compound ethyl N-(2,3-dichloro-6-nitrobenzyl)glycine from 2,3-dichlorobenzaldehyde and for reducing the glycine compound using either SnCl2 or a specially defined catalyst. A cyclization method to form Anagrelide base from the corresponding iminoquinazoline compound is further provided.
摘要翻译：提供了从2,3-二氯苯甲醛制备阿那格雷碱的方法。还提供了一种制备中间体化合物N-（2,3-二氯-6-硝基苄基）甘氨酸由2,3-二氯苯甲醛制备的乙腈和用于使用SnCl 2或特别定义的催化剂还原甘氨酸化合物的方法。进一步提供了从相应的亚氨基喹唑啉化合物形成阿那格雷碱的环化方法。

83. 发明申请

US20030055035A1 Pyrano piperidino and thiopyrano compounds and methods of use 失效
标题翻译：吡氯哌啶和噻喃类化合物及其使用方法
公开(公告)号：US20030055035A1
公开(公告)日：2003-03-20
申请号：US09563287
申请日：2000-05-03
发明人： Willilam A. Carroll , Konstantinos A. Agrios , Robert J. Altenbach , Irene Drizin , Michael E. Kort
IPC分类号： C07D471/02 , C07D513/02
CPC分类号： C07D471/04 , C07C45/00 , C07C45/298 , C07C45/41 , C07C45/63 , C07C205/44 , C07D471/14 , C07D491/14 , C07D495/14 , C07C47/565 , C07C47/55
摘要： 1 The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
摘要翻译：本发明提供新的式I化合物，其可用于超极化细胞膜，开放钾通道，松弛平滑肌细胞和抑制膀胱收缩

84. 发明授权

US06448293B1 Diphenyl ether compounds useful in therapy 失效
标题翻译：用于治疗的二苯醚化合物
公开(公告)号：US06448293B1
公开(公告)日：2002-09-10
申请号：US09810378
申请日：2001-03-16
申请人： Mark David Andrews , David Hepworth , Donald Stuart Middleton , Alan Stobie
发明人： Mark David Andrews , David Hepworth , Donald Stuart Middleton , Alan Stobie
IPC分类号： C07C21758
CPC分类号： C07D231/38 , C07C45/71 , C07C47/55 , C07C47/575 , C07C205/44 , C07C217/58 , C07C229/38 , C07C237/28 , C07C255/43 , C07C255/59 , C07C311/05 , C07C311/08 , C07C311/37 , C07C317/32 , C07C323/20 , C07C323/32 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07D231/12 , C07D233/56 , C07D249/06 , C07D249/08 , C07D295/096 , C07D295/192
摘要： A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(O)R6, CO2R9, C(O)NHR6 or SO2NR6R7; R12 is F, OH, CO2H, C3-6cycloalkyl, NH2, CONH2, C1-6alkoxy, C1-6alkoxycarbonyl or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O optionally substituted independently by one or more R13; or R6 and R7, together with the nitrogen to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring optionally substituted independently by one or more R13; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, —NH2, —NH(C1-C6alkyl) or —N(C1-C6alkyl)2; wherein when R1 and R2 are methyl, R4 and R5 are hydrogen and n is 1, R3is not a —SMe group para to the ether linkage linking rings A and B.
摘要翻译：通式（I）的化合物或其药学上可接受的盐，溶剂化物或多晶型物; 其中; R 1和R 2可以相同或不同，为氢，C 1 -C 6烷基，（CH 2）m（C 3 -C 6环烷基），其中m = 0,1,2或3，或R 1和R 2与它们连接形成氮杂环丁烷环; 每个R 3独立地为CF 3，OCF 3，C 1-4烷硫基或C 1 -C 4烷氧基; n为1,2或3; 并且R 4和R 5可以相同或不同，为：A-X，其中A = -CH = CH-或 - （CH 2）p - ，其中p为0,1或2; X是氢，F，Cl，Br，I，CONR6R7，SO2NR6R7，SO2NHC（= O）R6，OH，C1-4烷氧基，NR8SO2R9，NO2，NR6R11，CN，CO2R10，CHO，SR10，S（O）R9或SO2R10 ; R 6，R 7，R 8和R 10可以相同或不同，是氢或被一个或多个R 12独立地取代的C 1-6烷基; R9是任选被一个或多个R 12独立地取代的C 1-6烷基; R 11是氢，任选地被一个或多个R 12，C（O）R 6，CO 2 R 9，C（O）NHR 6或SO 2 NR 6 R 7取代的C 1-6烷基; R 12是F，OH，CO 2 H，C 3-6环烷基，NH 2，CONH 2，C 1-6烷氧基，C

85. 发明申请

US20020042537A1 Method for producing lysine derivative 审中-公开
标题翻译：生产赖氨酸衍生物的方法
公开(公告)号：US20020042537A1
公开(公告)日：2002-04-11
申请号：US09903531
申请日：2001-07-13
申请人： AJINOMOTO CO., INC.
发明人： Masakazu Nakazawa , Daisuke Takahashi , Norimasa Onishi , Masaki Naito , Kunisuke Izawa , Kenzo Yokozeki
IPC分类号： C07C229/04
CPC分类号： C07C229/26 , C07B2200/07 , C07C205/08 , C07C205/15 , C07C205/44 , C07C205/51 , C07C227/04 , C07C227/08 , C07C227/18 , C07C227/32 , C07C229/20 , C07C233/47 , C07C271/22 , C07C309/66 , C07D233/76 , C07D233/96 , C12P13/08 , C12P41/007 , C12P41/009 , Y02P20/55
摘要： The present invention provides a method for industrially producing an optically active lysine derivative useful as a pharmaceutical intermediate. More particularly, the present invention provides a production method including protecting an amino group or an amino group and carboxyl group of optically active 2-amino-6-methyl-6-nitroheptanoic acid with a protecting group, reducing a nitro group to synthesize a 6,6-dimethyl lysine derivative and reacting the 6,6-dimethyl lysine derivative with an acetic acid derivative.
摘要翻译：本发明提供了一种工业生产用作药物中间体的光学活性赖氨酸衍生物的方法。更具体地说，本发明提供一种制备方法，其包括用保护基保护光学活性2-氨基-6-甲基-6-硝基庚酸的氨基或氨基和羧基，还原硝基以合成6 的6-二甲基赖氨酸衍生物，并使6,6-二甲基赖氨酸衍生物与乙酸衍生物反应。

86. 发明申请

US20010025084A1 Photocleavable and acid cleavable linkers for combinatorial chemistry 失效
标题翻译：用于组合化学的可透光和可酸切割接头
公开(公告)号：US20010025084A1
公开(公告)日：2001-09-27
申请号：US09766987
申请日：2001-01-22
发明人： Vinh D. Tran , Vu Van Ma , Ruiyan Liu
IPC分类号： C07C205/00 , C07C309/00 , C07C062/36 , C07C062/32 , C07C062/38 , G01N033/53 , C08L029/02
CPC分类号： C40B80/00 , C07B2200/11 , C07C59/74 , C07C205/37 , C07C205/44 , C07C235/06
摘要： A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is nullNO2 or nullCHO; R2 is nullOCH3, nullCHO or nullH; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and nnull1 or 3-12. 1 A substrate of solid phase synthesis of the formula III is also disclosed. 2
摘要翻译：公开了一种用于固相合成的底物，其包含式I的固相 - 连接体组合。还公开了制备基材和其中有用的化学中间体的方法。其中新型中间体为式II化合物，其中R 1为-NO 2或-CHO; R2是-OCH3，-CHO或-H; R3选自羟基，具有多个氨基的固体支持物的残基和酯的残基，n = 1或3-12。还公开了式III的固相合成的底物。

87. 发明授权

US5705703A Catechol derivatives 失效
标题翻译：儿茶酚衍生物
公开(公告)号：US5705703A
公开(公告)日：1998-01-06
申请号：US784554
申请日：1997-01-21
申请人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose Da Prada , Gerhard Zurcher
发明人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose Da Prada , Gerhard Zurcher
IPC分类号： A61K31/12 , A61K31/195 , A61K31/44 , C07C45/29 , C07C45/30 , C07C45/46 , C07C45/67 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07C205/16 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/49 , C07C255/53 , C07D209/12 , C07D213/02 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04 , C07D498/02 , C07D513/04 , C07C205/20
CPC分类号： C07D513/04 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/00 , C07C255/53 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/46 , C07C45/673 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07D209/12 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04
摘要： Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure. Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.
摘要翻译：式Ia的儿茶酚衍生物其中R a，R b和R c具有本文给出的含义。描述了其在生理条件下可水解的酯和醚衍生物及其药学上可接受的盐，并且具有有价值的药理学性质。特别地，它们抑制了儿茶酚-O-甲基转移酶（COMT），一种可溶性的镁依赖性酶，其催化S-腺苷甲硫氨酸的甲基转移到儿茶酚底物上，由此形成相应的甲基醚。可以通过COMT进行O-甲基化并因此可以失活的合适的底物是例如外源儿茶酚胺和具有儿茶酚结构的外源性治疗活性物质。上述式Ia不仅包括形成本发明一部分的化合物，而且包括已知的化合物：形成本发明一部分的化合物可以根据已知方法制备。

88. 发明授权

US5442070A Derivatives of fluoro-quinoline carboxylic-3-acid and preparation therefor 失效
标题翻译：氟 - 喹啉羧酸-3-酸的衍生物及其制备方法
公开(公告)号：US5442070A
公开(公告)日：1995-08-15
申请号：US211325
申请日：1994-04-07
申请人： Christophe Daubie , Jean-Jacques Legrand , Clive Pemberton
发明人： Christophe Daubie , Jean-Jacques Legrand , Clive Pemberton
IPC分类号： C07D215/28 , A01N43/42 , A61K31/445 , A61K31/4704 , A61K31/4745 , A61P31/00 , A61P31/04 , C07C205/44 , C07D215/54 , C07D471/04 , C07D215/22 , C07D215/18 , C07D215/227
CPC分类号： C07C205/44 , C07D215/54
摘要： This invention relates to new derivatives of fluoro quinoline carboxylic-3 acid having general formula (I), ##STR1## wherein R is a hydrogen atom or an alkyl radical and Hal is a halogen atom, as well as salts thereof, when they exist, preparation thereof and utilization as synthesis intermediary.
摘要翻译： PCT No.PCT / FR92 / 00936 Sec。 371日期1994年4月7日 102（e）日期1994年4月7日PCT提交1992年10月8日PCT公布。公开号WO93 / 07127 本发明涉及具有通式（I），其中R为氢原子或烷基，Hal为卤素原子的通式（I）的氟喹啉羧酸-3的新衍生物，以及它们的盐，当它们存在时，其制备和作为合成中间体的利用。

89. 发明授权

US5237089A Nitro or amino substituted phenylalkyl or phenylalkenyl carboxylic acid derivatives 失效
标题翻译：硝基或氨基取代的苯基烷基或苯基烯基羧酸衍生物
公开(公告)号：US5237089A
公开(公告)日：1993-08-17
申请号：US985534
申请日：1992-12-03
申请人： Peter Plath , Karl Eicken , Norbert Goetz , Jochen Wild , Norbert Meyer , Bruno Wuerzer
发明人： Peter Plath , Karl Eicken , Norbert Goetz , Jochen Wild , Norbert Meyer , Bruno Wuerzer
IPC分类号： A01N37/46 , C07C205/06 , C07C205/34 , C07C205/56 , C07D209/48
CPC分类号： C07D209/48 , A01N37/46 , C07C205/44 , C07C205/56 , C07C255/00
摘要： N-substituted 3,4,5,6-tetrahydrophthalimides and their intermediates of the general formula I ##STR1## where A is --NO.sub.2, --NH.sub.2 or ##STR2## corresponding to the compounds Ia, Ib and Ic, B is --CH.sub.2 --, --CH.sub.2 --CHR.sup.1 --, --CH.sub.2 --CHR.sup.1 --CH.sub.2 --, --CH.dbd., --CH.dbd.CR.sup.1 -- or --CH.dbd.CR.sup.1 --CH.dbd., R.sup.1 being --H, --Cl, --Br or --CH.sub.3, D is ##STR3## or .dbd.C
摘要翻译： B）是N-取代的3,4,5,6-四氢邻苯二甲酰亚胺及其中间体，其中A是与化合物Ia，Ib和Ic相对应的-NO 2，-NH 2或 -CH 2 - ， - CH 2 -CHR 2 - ， - CH =， - CH = CR 1或-CH = CR 1 -CH =，R 1是-H，-Cl，-Br或-CH 3， D为或= C <，取决于末端基团B，X为-H，-Cl或-Br，Y为-H，C 1 -C 7 - 烷基，-Cl，-Br，-CN，-CONH 2 或-CO2R2，其中R2是H，C1-C6-烷基，C5-或C6-环烷基，C1-C4-烷氧基-C2-C4-烷基，C1-C4-烷基巯基-C2-C4-烷基，炔丙基，苄基， α-苯基乙基，α-苯基丙基，被F或Cl单取代或三取代的C 2 -C 4烷基，或CH 3取代或Cl取代的烯丙基，Z是-COOR 2，-CONR 3 R 4，其中R 3和R 4各自为H或C 1 -C 4烷基或一起形成其碳链可被氧原子间隔的5元或6元环脂环。

90. 发明授权

US5236952A Catechol derivatives 失效
标题翻译：儿茶酚衍生物
公开(公告)号：US5236952A
公开(公告)日：1993-08-17
申请号：US686210
申请日：1991-04-16
申请人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose DaPrada , Gerhard Zurcher
发明人： Karl Bernauer , Janos Borgulya , Hans Bruderer , Mose DaPrada , Gerhard Zurcher
IPC分类号： A61K31/12 , A61K31/195 , A61K31/44 , C07C45/29 , C07C45/30 , C07C45/46 , C07C45/67 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07C205/16 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/49 , C07C255/53 , C07D209/12 , C07D213/02 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04 , C07D498/02 , C07D513/04
CPC分类号： C07D513/04 , C07C205/23 , C07C205/37 , C07C205/43 , C07C205/44 , C07C205/45 , C07C205/56 , C07C205/59 , C07C255/00 , C07C255/53 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/46 , C07C45/673 , C07C47/565 , C07C47/575 , C07C49/83 , C07C49/84 , C07C69/017 , C07D209/12 , C07D217/16 , C07D241/44 , C07D253/07 , C07D265/36 , C07D277/24 , C07D277/40 , C07D277/42 , C07D279/16 , C07D285/16 , C07D471/04
摘要： Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
摘要翻译：式Ia的儿茶酚衍生物其中Ra，Rb和Rc具有本文给出的含义，其在生理条件下可水解的酯和醚衍生物及其药学上可接受的盐被描述并且具有有价值的药理学性质。特别地，它们抑制了儿茶酚-O-甲基转移酶（COMT），一种可溶性的镁依赖性酶，其催化S-邻苯二甲酰甲硫氨酸的甲基转移到儿茶酚底物上，由此形成相应的甲基醚。可以通过COMT进行O-甲基化并因此可以失活的合适的底物是例如外来儿茶酚胺和具有儿茶酚结构的非常给予的治疗活性物质。上述式Ia不仅包括形成本发明一部分的化合物，而且包括已知的化合物; 构成本发明一部分的化合物可以根据已知方法制备。

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