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31. 发明公开

EP3853202A1 COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS 审中-公开
公开(公告)号：EP3853202A1
公开(公告)日：2021-07-28
申请号：EP19779734.3
申请日：2019-09-19
申请人： ModernaTX, Inc.
发明人： BENENATO, Kerry E. , CORNEBISE, Mark , HENNESSY, Edward
IPC分类号： C07C229/16 , C07C233/36 , C07C251/38 , C07C255/24 , C07C259/06 , C07C279/28 , C07C279/36 , C07C311/05 , C07C311/51 , C07C311/64 , C07C335/08 , A61K47/28 , A61K47/14 , A61K47/24 , C07C323/25 , C07C275/14

32. 发明公开

EP3341358A1 PREPARATION OF SULFONAMIDE-CONTAINING ANTIMICROBIALS AND SUBSTRATE TREATING COMPOSITIONS OF SULFONAMIDE-CONTAINING ANTIMICROBIALS 有权
公开(公告)号：EP3341358A1
公开(公告)日：2018-07-04
申请号：EP16838177.0
申请日：2016-08-26
申请人： Nano Safe Coatings Incorporated (a Florida Corporation 3 P 14000024914)
发明人： FOUCHER, Daniel , WOLFAARDT, Gideon , CASCHERA, Alexander Gabriel , KHAN, Aman Ullah , MISTRY, Kamlesh , RONAN, Evan Lindsay Gilmore , POROSA, Lukasz
IPC分类号： C07C311/18 , A01N41/06 , A01N55/10 , A01N57/22 , A01P1/00 , A61L2/16 , A61L31/08 , A61L31/16 , C07C303/40 , C07C307/06 , C07C311/05 , C07F7/18 , C07F9/40
CPC分类号： A01N57/22 , A01N41/06 , A01N55/00 , B05D3/065 , C07C307/06 , C07C311/05 , C07C311/18 , C07C2602/42 , C07F7/1804 , C07F9/4006
摘要： A quaternary ammonium sulfonamide compound of formula (I): wherein R = (II), C1-C3 linear or branched alkyl, R1 and R2 are the same or different and selected from C1 to C18 linear or branched alkyl, R3 and R4 are the same or different and selected from C1 to C4 linear or branched alkyl, CF3, OR5 where R5 is C1 to C8 linear or branched alkyl or polyethylene oxide, l is 1, 2, 3, 4, 5, 6, 7 or 8, m is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 or 17, n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 or 18, wherein the aryl groups of R may be substituted or unsubstituted, X = halogen, and Y = (III) wherein R6, R7, R8, R9 and R10 are the same or different and selected from C1 to C6 linear or branched alkyl and the benzophenone is selected from the group consisting of substituted benzophenone and unsubstituted benzophenone, processes for preparing the compound and antimicrobial surface coating compositions of the compound.

34. 发明授权

EP2096106B1 NOVEL POLYAMINE DERIVATIVES 有权
标题翻译：新多胺
公开(公告)号：EP2096106B1
公开(公告)日：2014-06-18
申请号：EP07831667.6
申请日：2007-11-12
申请人： Nihon University
发明人： MIYAKE, Muneharu , KUSAMA, Tadashi , MASUKO, Takashi
IPC分类号： C07C311/05 , C07C311/18 , A61K31/18 , A61P25/16 , A61P25/28 , A61P43/00
CPC分类号： C07C311/18 , C07C311/05

35. 发明公开

EP2408557A2 PROCESS FOR HYDROGENATING KETONES IN THE PRESENCE OF RU (II) CATALYSTS 有权
标题翻译：一种用于制造的Ru（II）催化剂的方法
公开(公告)号：EP2408557A2
公开(公告)日：2012-01-25
申请号：EP10710411.9
申请日：2010-03-17
申请人： Johnson Matthey Public Limited Company
发明人： DYKE, Alan , GRAINGER, Damian, Mark , MEDLOCK, Jonathan, Alan , NEDDEN, Hans, Guenter , LE PAIH, Jacques, Jean, Marie , ROSEBLADE, Stephen, James , SEGER, Andreas , SIVAKUMAR, Vilvanathan , ZANOTTI-GEROSA, Antonio
IPC分类号： B01J23/46 , C07C29/145 , C07C311/05 , C07C311/18 , C07C33/20
CPC分类号： B01J31/1805 , B01J31/2295 , B01J2231/643 , B01J2531/0238 , B01J2531/821 , C07C29/145 , C07C311/05 , C07C311/07 , C07C311/18 , C07C311/20 , C07C2523/70 , C07C2531/18 , C07C2601/14 , C07C2601/16 , C07F15/0046 , C07F15/0053 , C07C33/22
摘要： The present invention relates to a process for hydrogenating a substrate comprising a carbon- heteroatom double bond, the process comprising the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I): R
1-10 , A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.

36. 发明公开

EP1736467A1 NOVEL SULFONAMIDE DERIVATIVE 审中-公开
标题翻译：新型磺酰胺衍生物
公开(公告)号：EP1736467A1
公开(公告)日：2006-12-27
申请号：EP05728832.6
申请日：2005-04-04
申请人： Dainippon Sumitomo Pharma Co., Ltd.
发明人： BAN, Hitoshi , ASANO, Shigehiro
IPC分类号： C07C307/02 , A61K31/255 , A61K31/44 , A61K31/454 , A61K31/506 , A61K31/55 , A61K31/664 , A61P3/06 , A61P9/10 , A61P43/00 , C07C307/06 , C07C311/05 , C07C311/18 , C07C317/32 , C07D211/64 , C07D213/06 , C07D223/06 , C07D401/04 , C07D413/04 , C07D417/04 , C07F9/59
CPC分类号： C07D211/60 , A61K31/255 , A61K31/44 , A61K31/454 , A61K31/506 , A61K31/55 , A61K31/664 , C07C307/02 , C07C307/06 , C07C311/18 , C07C311/37 , C07C2601/14 , C07D211/28 , C07D211/34 , C07D211/58 , C07D211/64 , C07D211/70 , C07D211/72 , C07D401/04 , C07D417/04 , C07D451/02 , C07F9/598
摘要： A compound of the formula (1):

wherein
m, n and p is independently an integer of 0 to 4 with the proviso that 3 ≦ m + n ≦ 8; X is the formula: NR 4 , etc.; R 1 , R 3 and R 4 are a substituted or unsubstituted aryl group, etc.; R 2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: -SO 2 -, etc.; and Z is an oxygen atom, etc.;
or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.
摘要翻译：式（1）的化合物：其中m，n和p独立地为0至4的整数，条件是3≤m+n≤8; X为式：NR4等; R1，R3和R4是取代或未取代的芳基等; R2是氢原子等; a，b，c，d，e和f是氢原子或取代或未取代的烷基等; Y是式：-SO2-等; Z是氧原子等; 或其前药或其药学上可接受的盐具有增强低密度脂蛋白受体表达的活性，因此可用作治疗高脂血症或动脉硬化的药剂。

37. 发明公开

EP1379493A2 NON-IMIDAZOLE ARYL ALKYLAMINES COMPOUNDS AS HISTAMINE H3 RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES 审中-公开
标题翻译：非咪唑阿魏酸亚苄基维生素ALS组胺素H3抗抑郁药，HERSTELLUNG UND PHARMAZEUTISCHE VERWENDUNGEN
公开(公告)号：EP1379493A2
公开(公告)日：2004-01-14
申请号：EP02723329.5
申请日：2002-03-21
申请人： Eli Lilly and Company
发明人： BEAVERS, Lisa, Selsam , GADSKI, Robert, Alan , HIPSKIND, Philip, Arthur , LINDSLEY, Craig, William , LOBB, Karen, Lynn , NIXON, James, Arthur , PICKARD, Richard, Todd , SCHAUS, John, Mehnert , TAKAKUWA, Takako , WATSON, Brian, Morgan
IPC分类号： C07C217/58 , A61K31/395 , A61K31/131 , A61P3/00 , A61P25/00 , C07D295/08 , C07D295/12 , C07C217/20 , C07C311/05 , C07C311/13 , C07C311/18 , C07C237/08 , C07D295/14 , C07C217/74 , C07C271/34 , C07C323/62 , C07C271/24 , C07C233/73 , C07C237/32 , C07C311/17 , C07C409/12
CPC分类号： C07D207/27 , C07B2200/07 , C07C217/20 , C07C217/58 , C07C217/74 , C07C233/73 , C07C237/08 , C07C237/32 , C07C271/24 , C07C271/34 , C07C311/05 , C07C311/09 , C07C311/11 , C07C311/18 , C07C2601/02 , C07C2601/14 , C07C2602/10 , C07D207/09 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/26 , C07D213/38 , C07D215/20 , C07D217/06 , C07D217/08 , C07D217/24 , C07D231/04 , C07D231/12 , C07D233/36 , C07D233/56 , C07D235/14 , C07D241/44 , C07D243/08 , C07D249/08 , C07D295/088 , C07D295/096 , C07D295/13 , C07D295/15 , C07D307/12 , C07D307/14 , C07D307/46 , C07D333/34 , C07D401/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D487/04
摘要： The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereofwhich have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor -related diseases.
摘要翻译：本发明公开了具有选择性组胺-H 3受体拮抗剂活性的式（I）的新型取代芳基烷基胺化合物或其药学上可接受的盐以及其制备方法。在另一个实施方案中，本发明公开了包含这种环胺的药物组合物以及使用它们治疗肥胖症和其他组胺H3受体相关疾病的方法。

38. 发明公开

EP1296944A1 SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：EP1296944A1
公开(公告)日：2003-04-02
申请号：EP01937173.1
申请日：2001-05-04
申请人： ELI LILLY AND COMPANY
发明人： AIKINS, James, Abraham , FRAY, Andrew, Hendley , MILLER, William, David , ORNSTEIN, Paul, Leslie , ZARRINMAYEH, Hamideh , ZIMMERMAN, Dennis, Michael
IPC分类号： C07C311/05 , A61K31/18
CPC分类号： C07C311/05
摘要： The present invention relates to a compound of formula (Ia) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.
摘要翻译：本发明涉及式（Ia）化合物或其药学上可接受的盐，其可用于治疗与谷氨酸功能低下相关的病症，例如精神病和神经疾病。

40. 发明公开

EP1183232A2 MONOFLUOROALKYL DERIVATIVES 有权
标题翻译：单氟衍生物
公开(公告)号：EP1183232A2
公开(公告)日：2002-03-06
申请号：EP00923110.1
申请日：2000-04-17
申请人： ELI LILLY AND COMPANY
发明人： BENDER, David, Michael , CANTRELL, Buddy, Eugene , FRAY, Andrew, Hendley , JONES, Winton, Dennis , MILLER, William, David , MITCHELL, David , SIMON, Richard, Lee , ZARRINMAYEH, Hamideh , ZIMMERMAN, Dennis, Michael
IPC分类号： C07C311/03 , C07C311/04 , C07C311/06 , C07C311/05 , C07C311/08 , C07D333/20 , C07D213/81 , C07D213/82 , C07C311/37 , A61K31/18 , A61K31/44 , A61K31/38
CPC分类号： C07D213/81 , C07C307/06 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/08 , C07C311/39 , C07D209/34 , C07D213/38 , C07D213/61 , C07D213/82 , C07D261/18 , C07D295/192 , C07D333/20 , C07D333/38
摘要： The present invention provides monofluoroalkyl derivatives of the formula (I) wherein: A represents SO2, CO2 or CONH; Ra represents (1-6C)alkyl, (2-6C)alkenyl, -(1-4C)alkyl(3-8C)cycloalkyl, or (1-4C)alkylaromatic; Rb represents H, (1-6C)alkyl, (2-6C)alkenyl, -(1-4C)alkyl(3-8C)cycloalkyl, or (1-4C)alkylaromatic; or R?a and Rb¿ together with the carbon atoms to which they are attached form a (3-8C) saturated carbocyclic ring, a (3-8C) saturated carbocyclic ring containing a heteroatom selected from the group consisting of sulfur or oxygen, or a (5-8C) carbocyclic ring containing one double bond; R1 represents an unsubstituted or substituted aromatic group, an unsubstituted or substituted heteroaromatic group, or an unsubstituted or substituted (5-8C)cycloalkyl group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or when A represents SO¿2?, a group of formula R?3R4¿N in which R?3 and R4¿ each independently represents (1-4C)alkyl or , together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; or a pharmaceutically acceptable salt thereof, useful for potentiating glutamate receptor function in a mammal and thereof, useful for treating a wide variety of condutions, such as psychiatric and neurological disorder.
摘要翻译：本发明提供了式（I）的单氟烷基衍生物，其中：A代表SO 2，CO 2或CONH; Ra代表（1-6C）烷基，（2-6C）链烯基， - （1-4C）烷基（3-8C）环烷基或（1-4C）烷基芳香族基团; Rb代表H，（1-6C）烷基，（2-6C）烯基， - （1-4C）烷基（3-8C）环烷基或（1-4C）烷基芳族; 或R'a和Rb'与它们所连接的碳原子一起形成（3-8C）饱和碳环，含有选自硫或氧的杂原子的（3-8C）饱和碳环，或含有一个双键的（5-8C）碳环; R1表示未取代或取代的芳族基团，未取代或取代的杂芳族基团或未取代或取代的（5-8C）环烷基; （1-6C）烷基，（3-6C）环烷基，（1-6C）氟烷基，（1-6C）氯烷基，（2-6C）烯基，（1-4C）烷氧基（1-4C）烷基，（1-4C）烷基或（1-4C）烷氧基取代的苯基，或当A代表SO 2 2时，式R 3 R 4 N的基团，其中R 3和R 4各自是（1-4C）烷基或与它们所连接的氮原子一起形成氮杂环丁烷基，吡咯烷基，哌啶基，吗啉代，哌嗪基，六氢氮杂基或八氢吖辛因基; 或其药学上可接受的盐，用于增强哺乳动物及其哺乳动物中的谷氨酸受体功能，可用于治疗多种途径，如精神病和神经紊乱。

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