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31. 发明公开

EP0365149A3 Leukotriene antagonist prodrugs 失效
标题翻译：白三烯拮抗剂前体药物
公开(公告)号：EP0365149A3
公开(公告)日：1990-07-25
申请号：EP89309643.8
申请日：1989-09-21
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： Gleason, John Gerald , Newton, John Frederick , Smallheer, Joanne , Hall, Ralph Floyd , Phipps, Kathleen A.
IPC分类号： C07C323/56 , C07C323/60 , C07C323/66 , C07C323/67 , C07D233/84 , C07D257/04 , A61K31/19
CPC分类号： C07D257/04 , A61K31/19 , C07C45/298 , C07C45/44 , C07C45/56 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C47/575 , C07C255/33 , C07C323/56 , C07C323/60 , C07C323/66 , C07C323/67 , C07D233/84 , C07D233/90 , C07D303/40 , C07D303/48 , C07D307/38 , C07D307/54 , C07D309/30
摘要： A compound represented by the following structural formula (I):
wherein (a) R₁ is C₈ to C₁₃ alkyl, C₇ to C₁₂ alkoxy, C₇ to C₁₂ alkylthio, C₁₀ to C₁₂ 1-alkynyl, 10-undecynyloxy, 11-dodecynyl, phenyl-C₄ to C₁₀ alkyl, phenyl-C₃ to C₉ alkoxy, phenylthio-C₃ to C₉ alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, alkoxy, methylthio or trifluoromethylthio, thienyl-C₄ to C₁₀ alkyl furyl-C₄ to C₁₀ alkyl,trifluoromethyl-C₇ to C₁₂ alkyl or cycloheyl-C₄ to C₁₀ alkyl; and
R₂ is hydrogen, bromo, chloro, methyl, trifluoromethyl, hydroxy, alkoxy or nitro; (b) or R₁ is hydrogen and R₂ is C₈ to C₁₃ alkyl, C₇ to C₁₂ alkoxy, C₇ to C₁₂ alkylthio, C₁₀ to C₁₂ 1-alkynyl, 10-undecynyloxy, 11-dodecynyl, phenyl-C₄ to C₁₀ alkyl, phenyl-C₃ to C₉ alkoxy, phenylthio-C₃ to C₉ alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, alkoxy, methylthio or trifluoromethylthio, furyl-C₄ to C₁₀ alkyl, trifluoromethyl-C₇ to C₁₂ alkyl or cyclohexyl-C₄ to C₁₀ alkyl;
q is 0, 1, or 2;
Y is COR₃, CH(R₄)(CH₂) m COR₃ or CH(R₄)(CH₂) m -tetrazol-5-yl the tetrazol-5-yl being unsubstituted or substituted with A; R₁₆ and R₁₇ are independently hydrogen or C₁₋₄ alkyl;
j is 0 to 6; R₁₈ is hydrogen, alkyl, COR₃, SO₃H, SO₂NH₂, COCH₂OH or CHOHCH₂OH;
R₃ is amino, (CH₂) n CO₂CH₂CONR₁₆R₁₇, or OR₁₄;
R₁₄ is hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, alkylaryl, alkylarylalkyl, alkyl substituted amino or alkylamino, - OCH₂CONR₇R₈, indanyl, pivaloyloxymethyl, acetoxymethyl, propionyloxymethyl, glycyloxymethyl, phenylglycyloxymethyl, or thienylglycyloxymethyl;
R₄ is hydrogen, methyl, alkoxy, fluoro or hydroxy;
m is 0, or 1;
R is (CH₂) n COR₆, CH(CO₂H)CH₂COR₆, (CH₂) n CO₂CH₂CONR₁₆,R₁₇, or an imidazole of the formula n is 0 to 6;
R₅ is hydrogen, amino, or NHCOCH₂CH₂CH(NH₂)CO₂H;
R₆ is amino, NH(CH₂) n CO₂H, SO₃H, SO₂NH₂, CN, tetrazol-5-yl unsubstituted or substituted with A as defined above, or OR₁₅;
R₇ is hydrogen, alkyl or alkenyl;
R₈ is hydrogen, alkyl, carboxyl or carboxamido, or,
when R₇ and R₉ are hydrogen or alkyl, (CH₂) m COOR₁₅;
R₉ is hydrogen, alkyl or (CH₂) m COOR₁₅;
R₁₅ is hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, alkylaryl, alkylarylalkyl, allayl substituted amino or alkylamino, -OCH₂CONR₇R₈, indanyl, pivaloyloxymethyl, acetoxymethyl, propionyloxymethyl, glycyloxymethyl, phenylglycyloxymethyl, or thienylglycyloxymethyl;
provided that 1) when n is 0, R₅ is hydrogen, 2) R₇, R₈ and R₉ are not all hydrogen, 3) any of R₁and R₂ above are not alkylthio or phenylthioalkyl when q is 1 or 2, 4) R₃ and R₆ are not both hydroxy, 5) OR₁₄ and OR₁₅ are not simultaneously hydroxy; 6) if R₄ is hydroxy and m is 0, R₁₄ is hydrogen; or
a pharmaceutically acceptable salt thereof.
摘要翻译：由下列结构式（Ⅰ）表示的化合物：其中（a）R 1是C 8 -C 13烷基，C 8 -C 12烷氧基，C 8 -C 12烷硫基，C 10 -C 12 1-炔基，苯基-C3-C8烷氧基，苯基硫基-C3-C8烷基，其中苯基任选地被溴，氯，三氟甲基，烷氧基，甲硫基或三氟甲硫基取代，噻吩基-C4-C10烷基呋喃基-C4-C10烷基，三氟甲基-C 8至C 12烷基或环
己基-C 4至C 10烷基; 和R 2是氢，溴，氯，甲基，三氟甲基，羟基，烷氧基或硝基; （b）或R 1是氢和R 2是C 8 -C 13烷基，C 8 -C 12烷氧基，C 8 -C 12烷硫基，C 10 -C 12 1-炔基，10-十一碳炔氧基，11-十二炔基，苯基-C 4 -C 10烷基，任选地被溴，氯，三氟甲基，烷氧基，甲硫基或三氟甲硫基，呋喃基-C 4至C 10烷基，三氟甲基-C 8至C 12烷基或环己基-C 4至C 10烷基取代的苯基;苯基硫基-C 3至C 8烷基; q是0,1或2; Y是COR 3，CH（R 4）（CH 2）mCOR 3或CH（R 4）（CH 2）m-四唑-5-基，四唑-5-基未被取代或被A取代; R 16和R 18独立地是氢或C 1-4烷基; j是0至6; R 17是氢，烷基，COR 3，SO 3 H，SO 2 NH 2，COCH 2 OH或CHOHCH 2 OH; R 3是氨基，（CH 2）n CO 2 CH 2 CONR 16 R 17或OR 14; 烷基，烷基芳基，烷基芳基烷基，烷基取代的氨基或烷基氨基，-OCH 2 CONR 8 R 9，茚满基，新戊酰氧基甲基，乙酰氧基甲基，丙酰氧基甲基，甘氨酰氧甲基，苯基甘氨酰氧甲基或噻吩基甘氨酰氧甲基; R 4是氢，甲基，烷氧基，氟或羟基; m是0或1; R是（CH 2）n COR 6，CH（CO 2 H）CH 2 COR 6，（CH 2）n CO 2 CH 2 CONR 16，R 17或式n的咪唑是0-6; R 5是氢，氨基或NHCOCH 2 CH 2 CH（NH 2）CO 2 H; R 6为氨基，NH（CH 2）n CO 2 H，SO 3 H，SO 2 NH 2，CN，未被取代或被上述定义的A取代的四唑-5-基或OR 15; R 7是氢，烷基或链烯基; R 7是氢，烷基，羧基或甲酰氨基，或当R 7和R 7是氢或烷基时，（CH 2）m COOR 15; R 8是氢，烷基或（CH 2）m COOR 15; 烷基，环烷基，芳基，芳基烷基，烷基芳基，烷基芳基烷基，烯丙基取代的氨基或烷基氨基，-OCH 2 CONR 8 R 9，茚满基，新戊酰氧基甲基，乙酰氧基甲基，丙酰氧基甲基，条件是1）当n是0时，R 5是氢，2）R 6，R 7和R 7不全是氢，3）当q是1或2,4时，上述R 1和R 2中的任何一个都不是烷硫基或苯硫基烷基，R 3和R 6是不是两个羟基，5）OR 14和OR 15不同时是羟基; 6）如果R 4是羟基并且m是0，R 14是氢; 或其药学上可接受的盐。

32. 发明公开

EP0094727A3 Substituted heterocyclyl phenylformamidines, processes for their preparation and their pharmaceutical use 失效
标题翻译：取代的杂环基苯甲酰胺，其制备方法及其药物用途
公开(公告)号：EP0094727A3
公开(公告)日：1985-01-09
申请号：EP83200690
申请日：1983-05-16
申请人： ISTITUTO DE ANGELI S.p.A.
发明人： Cereda, Enzo , Bietti, Giuseppe , Donetti, Arturo , Del Soldato, Piero , Giachetti, Antonio , Pagani, Ferdinando
IPC分类号： C07D213/38 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/84 , C07D233/95 , C07D239/26 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/28
CPC分类号： C07D213/40 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/84 , C07D233/95 , C07D239/26 , C07D239/36 , C07D249/08 , C07D263/32 , C07D271/06 , C07D271/07 , C07D277/28 , C07D277/40 , C07D277/42 , C07D307/38 , C07D307/52 , C07D333/12 , C07D333/16 , C07D333/20 , C07D405/12
摘要： Object of the present invention are new pharmacologically active substituted heterocyclylphenylformamidines of formula
in which A represents a hydrogen atom, an amino group which may be substituted by one or two alkyl groups having 1 to 3 carbon atoms or a saturated heterocyclic ring, R represents a hydrogen atom or a methyl group, R 1 represents a linear or branched alkyl group which may contain 1 or 2 heteroatoms such as a sulfur, an oxygen or nitrogen atom or may form a substituted or an unsubstituted cyclic ring, an alkenyl group, an alkynyl group, a cycloalkyl group or a phenyl group, R 2 and R 3 which may be the same or different, represent a hydrogen atom, an alkyl or alkoxy group having 1 to 3 carbon atom or a halogen atom, m and n represent 0 or 1, Het represents a substituted or unsubstituted heterocyclic ring containing from 1 to 3 heteroatoms (except the imidazole ring when R 1 is a linear or branched alkyl group not containing heteroatoms and R 2 and R 3 are both hydrogen atoms), tautomers thereof and acid addition salts of the aforesaid compounds. Processes for preparation of the compounds of formula (I) and their intermediates as well as pharmaceutical compositions containing them are also object of this invention. The new compounds are H 2 -receptor blocking agents, inhibit gastric acid secretion, and are useful antiulcer agents.

33. 发明公开

EP0087274A2 Pyrimidone derivatives 失效
标题翻译： Pyrimidonderivate。
公开(公告)号：EP0087274A2
公开(公告)日：1983-08-31
申请号：EP83300822.0
申请日：1983-02-17
申请人： SMITH KLINE & FRENCH LABORATORIES LIMITED
发明人： Brown, Thomas Henry
IPC分类号： C07D417/14 , C07D405/14 , C07D401/14 , C07D401/06 , A61K31/505 , A61K31/425
CPC分类号： C07D213/64 , C07D213/38 , C07D213/61 , C07D233/64 , C07D239/36 , C07D277/48 , C07D295/096 , C07D307/38 , C07D307/52 , C07D403/06 , C07D403/14 , C07D417/14
摘要： The invention provides histamine H 2 -antaponist compounds of formula (1):-
and pharmaceutically acceptable salts thereof, where

W is a 2-furanyl or 2-thienyl group optionally substituted in the 5-position with a group R 1 R 2 N(CH 2 ) a -; a 2-pyridyl group optionally substituted in the 4- or 6-position with a group R 1 R 2 N(CH 2 ) a -; a phenyl group substituted in the 3-or 4-position with a group R 1 R 2 N(CH 2 ) a -; a 4-imidazolyl group optionally substituted in the 5-position with methyl or bromine; a 2-pyridyl group optionally substituted in the 3-position with C 1-4 alkyl, C 1-4 , alkoxy, halogen, amino or hydroxy; a 2-thiazolyl group or a 2-guanidino-4-thiazolyl group;
X is (CH 2 ) b in which b is from 3 to 6, or (CH 2 ) d S(CH 2 ) e in which dand e are the same or different and are from 1 to 3 or, when W is substituted phenyl or 2-pyridyl substituted in the 4- or 6- position with a group R 1 R 2 N(CH 2 ) a -, O(CH 2 ) t in which f is from 2 to 5;
Z is hydrogen or C 1-4 alkyl;
A is C 1 -C 5 alkylene or (CH 2 ) p A 1 (CH 2 ) q - where A' is oxygen or sulphur and p and q are such that their sum is from 1 to 4;
B is an optionally substituted pyridyl, where the optional substituent is one or more C 1-4 alkyl, or C 1-4 alkoxy or hydroxy groups or halogen atoms or an N-oxo group or a phenyl group optionally substituted with one or more C 1-4 alkyl or C 1-4 alkoxy groups or halogen atoms or B is a 6-(2,3-dihydro-1,4-benzodioxinyl) or a 5-(1,3-benzodioxolyl) group or B is a 2-furanyl or 2-thienyl group optionally substituted in the 5-position with a group R 1 R 2 N(CH 2 ) a -; a phenyl group substituted in the 3- of 4-position with a group R 1 R 2 N(CH 2 ) a - or a 3-pyridyl group substituted in the 5- or 6-position or a 4-pyridyl group substituted in the 2-position by a group R 1 R 2 N(CH 2 ) a -;
R' and R 2 can be the same or different and are hydrogen or C 1-4 alkyl or together form a 1,4-butanediyl, 1,5-pentanediyl, 1,6-hexanediyl or 1,7-heptanediyl group; and a is 1 to 4.
摘要翻译：本发明提供了式（I）的组胺H2拮抗剂化合物：其... ...其药学上可接受的盐，其中W是在5-位上任选被一个R基团取代的2-呋喃基或2-噻吩基 <1> [R <2> N（CH 2）A-; 任选在4-或6-位被R 1 R 2 N（CH 2）a - 取代的2-吡啶基; 在3-或4-位被R 1 R 2 N（CH 2）a - 取代的苯基; 任选在5-位被甲基或溴取代的4-咪唑基; 任选在3-位被C 1-4烷基，C 1-4烷氧基，卤素，氨基或羟基取代的2-吡啶基; 2-噻唑基或2-胍基-4-噻唑基; X为（CH 2）b，其中b为3至6，或（CH 2）d S（CH 2）e，其中d和e为相同或不同且为1至3，或当W为4-或6-位取代的苯基或2-吡啶基时，R 1，R 2，N（CH 2）a - ，O（CH 2）其中f为2至5; Z为氢或C1-4烷基; A为C1-C5亚烷基或（CH2）pA 1（CH2）q-，其中A 1为氧或硫，p为和q是它们的总和为1至4; ... B是任选取代的吡啶基，其中任选的取代基是一个或多个C 1-4烷基。或C 1-4烷氧基或羟基或卤素原子或任选被一个或多个C 1-4烷基或C 1-4烷氧基或卤素原子取代的N-氧代基或苯基，或B是6-（2,3 - 二氢-1,4-苯并二恶英基）或5-（1,3-苯并多恶唑基）基团，或B是任选在5位被R 1 R 2取代的2-呋喃基或2-噻吩基 > N（CH 2）A-; 在3-位的4-位上被基团R 1，R 2，N（CH 2）a - 取代的苯基或在5-或6-位取代的3-吡啶基或4-吡啶基在2位被基团取代R 1 R 2 N（CH 2）a - ; ... R 1和R 2可以相同或不同，为氢或C 1-4烷基或一起形成1,4-丁二基，1,5-戊二基，1,6-己二基或1,7-庚二基; a是1到4。

34. 发明公开

EP3180296A4 METHODS OF PRODUCING ALKYLFURANS 审中-公开
公开(公告)号：EP3180296A4
公开(公告)日：2018-01-24
申请号：EP15832265
申请日：2015-08-14
申请人： MICROMIDAS INC
发明人： HUCUL DENNIS A , HIRSCH-WEIL DIMITRI A , MASUNO MAKOTO NATHANAEL , BISSELL JOHN ALBERT II , WOOD ALEX B , ARAIZA ROBERT JOSEPH , HENTON DANIEL R , BROWNING SHAWN M , SMITH RYAN L
IPC分类号： C07D307/36 , C07B31/00 , C07D307/38 , C07D307/44 , C07D307/48
CPC分类号： C07D307/36 , C07C2/865 , C07D307/38 , C07D307/44 , C07D307/48
摘要： Provided herein are methods of producing dialkylfurans, such as 2,5-dimethylfuran, and other alkyl furans, such as 2-methylfuran. For example, 2,5-dimethylfuran may be produced by hydrogenation of (5-methylfuran-2-yl) methanol or 2-(chloromethyl)-5-methylfuran in the presence of a solid supported metal catalyst having an excess of either basic or acidic sites (as determined by chemisorption of CO2 or NH3). The process could further include a urea reagent (TMU, DMPU, TMI) and an alkyl benzene.

35. 发明公开

EP3233794A1 INDENYL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND MEDICAL USES THEREOF 无效转让
标题翻译：茚基化合物，药物组合物及其医学用途
公开(公告)号：EP3233794A1
公开(公告)日：2017-10-25
申请号：EP15823453.4
申请日：2015-12-16
申请人： ADT Pharmaceuticals, Inc.
发明人： PIAZZA, Gary A. , CHEN, Xi , KEETON, Adam B. , BOYD, Michael R.
IPC分类号： C07D207/14 , C07D213/24 , C07D235/30 , C07D307/38 , C07D307/52 , C07D405/12 , C07C43/205 , C07C233/58 , A61K31/075 , A61K31/166 , A61K31/443 , A61K31/506 , A61K31/341 , A61K31/44 , A61K31/505 , A61K31/40 , A61P35/00
CPC分类号： C07D317/64 , A61K31/341 , A61K31/36 , A61K31/40 , A61K31/401 , A61K31/44 , A61K31/445 , A61K45/06 , A61K2300/00 , C07C233/58 , C07C235/32 , C07C237/20 , C07C2601/02 , C07C2602/08 , C07D207/14 , C07D207/337 , C07D211/56 , C07D213/24 , C07D213/75 , C07D235/30 , C07D307/38 , C07D307/52 , C07D307/54 , C07D405/12
摘要： Disclosed are compounds, for example, compounds of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.
摘要翻译：公开了化合物，例如其中R，R 0，R 1 -R 8，n，X，Y，Y'和E如本文所述的式（I）化合物，含有这样的化合物以及治疗或预防疾病或病症例如癌症的方法。

36. 发明公开

EP3180296A1 METHODS OF PRODUCING ALKYLFURANS 审中-公开
标题翻译：生产烷基呋喃的方法
公开(公告)号：EP3180296A1
公开(公告)日：2017-06-21
申请号：EP15832265.1
申请日：2015-08-14
申请人： Micromidas, Inc.
发明人： HUCUL, Dennis A. , HIRSCH-WEIL, Dimitri A. , MASUNO, Makoto Nathanael , BISSELL, John Albert II , WOOD, Alex B. , ARAIZA, Robert Joseph , HENTON, Daniel R. , BROWNING, Shawn M. , SMITH, Ryan L.
IPC分类号： C07B31/00
CPC分类号： C07D307/36 , C07C2/865 , C07D307/38 , C07D307/44 , C07D307/48
摘要： Provided herein are methods of producing dialkylfurans, such as 2,5-dimethylfuran, and other alkyl furans, such as 2-methylfuran. For example, 2,5-dimethylfuran may be produced by hydrogenation of (5-methylfuran-2-yl) methanol or 2-(chloromethyl)-5-methylfuran in the presence of a solid supported metal catalyst having an excess of either basic or acidic sites (as determined by chemisorption of CO2 or NH3). The process could further include a urea reagent (TMU, DMPU, TMI) and an alkyl benzene.
摘要翻译：本文提供生产二烷基呋喃如2,5-二甲基呋喃和其他烷基呋喃如2-甲基呋喃的方法。例如，2,5-二甲基呋喃可通过（5-甲基呋喃-2-基）甲醇或2-（氯甲基）在具有过量的固体负载型金属催化剂的存在下-5-甲基呋喃的氢化来生产碱性或酸性部位（如通过化学吸附CO 2或NH 3所确定的）。该方法可以进一步包括尿素试剂（TMU，DMPU，TMI）和烷基苯。

37. 发明授权

EP2303825B1 CHEMICAL TRANSFORMATION OF LIGNOCELLULOSIC BIOMASS INTO FUELS AND CHEMICALS 有权
标题翻译：化学转化木质纤维素生物质燃料和化学品
公开(公告)号：EP2303825B1
公开(公告)日：2016-11-09
申请号：EP09767606.8
申请日：2009-06-16
申请人： Wisconsin Alumni Research Foundation
发明人： BINDER, Joseph, Bartholomew , RAINES, Ronald, Thaddeus
IPC分类号： C07D307/28 , C07D307/36 , C07D307/38 , C07D307/44 , C07D307/48 , C07D307/50
CPC分类号： C07H3/02 , C07D307/28 , C07D307/36 , C07D307/38 , C07D307/44 , C07D307/48 , C07D307/50

38. 发明公开

EP2969202A1 METALLORGANOCATALYSIS FOR ASYMMETRIC TRANSFORMATIONS 审中-公开
标题翻译：不对称变换的金属结构分析
公开(公告)号：EP2969202A1
公开(公告)日：2016-01-20
申请号：EP14779902.7
申请日：2014-03-11
申请人： Rutgers, the State University of New Jersey
发明人： ZHANG, Xumu
IPC分类号： B01J31/00
CPC分类号： B01J31/2409 , B01J31/2414 , B01J2231/643 , B01J2231/645 , B01J2531/0205 , B01J2531/0263 , B01J2531/16 , B01J2531/17 , B01J2531/18 , B01J2531/26 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/84 , B01J2531/842 , B01J2540/22 , B01J2540/225 , B01J2540/66 , B01J2540/68 , C07B53/00 , C07C201/12 , C07C209/52 , C07C213/02 , C07D307/38 , C07F17/00 , C07F17/02 , C07C205/04 , C07C205/09 , C07C205/32 , C07C211/30 , C07C211/29 , C07C211/27 , C07C217/58
摘要： A ligand having the structure or its enantiomer; (I) wherein: each one of R
a , R
b , R
c and R
d is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH
2 NH; *CH(CH
3 )NH (C*,
R ); and the organocatalyst is an organic molecule catalyst covalently bound to the bridge group. Also, a catalyst having the structure or its enantiomer: (II) wherein: each one of R
a , R
b , R
c and R
d is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH
2 NH; *CH(CH
3 )NH (C*,
R ); and *CH(CH
3 )NH (C*,
S ); the organocatalyst is an organic molecule catalyst covalently bound to the bridge group; and M is selected from the group consisting of Rh, Pd, Cu, Ru, Ir, Ag, Au, Zn, Ni, Co, and Fe.
摘要翻译：具有该结构或其对映体的配体; （I）其中：R a，R b，R c和R d中的每一个选自烷基，环烷基和芳基; 桥基选自CH 2 NH; * CH（CH 3）NH（C *，R）; 有机催化剂是与桥基共价结合的有机分子催化剂。此外，具有以下结构或其对映异构体的催化剂：（II）其中：R a，R b，R c和R d中的每一个选自烷基，环烷基和芳基; 桥组选自CH 2 NH; * CH（CH 3）NH（C *，R）; 和* CH（CH 3）NH（C *，S）; 有机催化剂是与桥基共价结合的有机分子催化剂; M选自Rh，Pd，Cu，Ru，Ir，Ag，Au，Zn，Ni，Co和Fe。

39. 发明授权

EP2528914B1 FURO[3,2-B]PYRANE DERIVATIVES USEFUL IN THE SYNTHESIS OF HALICHONDRIN B ANALOGS 有权
标题翻译： FURO [3,2-B]吡咯烷基合成缬氨酸
公开(公告)号：EP2528914B1
公开(公告)日：2014-06-11
申请号：EP11702900.9
申请日：2011-01-26
申请人： Eisai R&D Management Co., Ltd.
发明人： ENDO, Atsushi , CHASE, Charles,E. , FANG, Francis, G.
IPC分类号： C07D405/06 , C07D405/12 , C07D493/04
CPC分类号： C07F7/1864 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55

40. 发明授权

EP1673356B1 SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES 失效
标题翻译：取代BENZYLAMINOALKYLENHETEROCYCLEN
公开(公告)号：EP1673356B1
公开(公告)日：2012-04-11
申请号：EP04790126.9
申请日：2004-10-05
申请人： Newron Pharmaceuticals S.p.A.
发明人： SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania, Nikem
IPC分类号： C07D261/02 , C07D307/14 , C07D307/38 , C07D319/12 , C07D213/38 , C07D233/54 , C07D249/02 , C07D277/10 , C07D327/04 , C07D333/20 , C07D307/81 , C07D235/14 , A61K31/341 , A61K31/422 , A61K31/426
CPC分类号： C07D261/02 , A61K31/341 , A61K31/422 , A61K31/426 , C07D213/38 , C07D233/64 , C07D235/14 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/28 , C07D307/14 , C07D307/38 , C07D307/52 , C07D307/81 , C07D309/04 , C07D319/12 , C07D333/20
摘要： This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

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