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1. 发明公开

EP4186888A1 COMPOUND AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS 审中-公开
公开(公告)号：EP4186888A1
公开(公告)日：2023-05-31
申请号：EP22204047.9
申请日：2018-03-15
申请人： ModernaTX, Inc.
发明人： BENENATO, Kerry E. , KUMARASINGHE, Ellalahewage Sathyajith , CORNEBISE, Mark
IPC分类号： C07C229/16 , C07D233/61 , C07C275/14 , C07C311/05 , C07C335/08 , C07C233/36 , C07D295/13 , C07C279/28 , C07D239/46 , C07D473/00 , A61K47/14 , A61K47/24 , A61K47/28 , A61K9/127 , A61K9/51 , C07D249/04 , C07C259/06 , C07C307/06 , C07C219/06 , C07C229/08 , C07C229/12
摘要： The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

3. 发明公开

EP1736467A4 NOVEL SULFONAMIDE DERIVATIVE 审中-公开
标题翻译： NEUESSULFONSÄÜAMIDDERIVAT
公开(公告)号：EP1736467A4
公开(公告)日：2009-07-01
申请号：EP05728832
申请日：2005-04-04
申请人： DAINIPPON SUMITOMO PHARMA CO
发明人： BAN HITOSHI , ASANO SHIGEHIRO
IPC分类号： A61K31/255 , A61K31/44 , A61K31/454 , A61K31/506 , A61K31/55 , A61K31/664 , A61P3/06 , A61P9/10 , A61P43/00 , C07C307/02 , C07C307/06 , C07C311/05 , C07C311/18 , C07C311/37 , C07C317/32 , C07D211/28 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/64 , C07D211/70 , C07D211/72 , C07D213/06 , C07D223/06 , C07D401/04 , C07D413/04 , C07D417/04 , C07D451/02 , 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： Disclosed are a compound represented by the formula (1) below, a prodrug thereof, and their pharmaceutically acceptable salts which have an effect of increasing LDL receptor expression and are useful as drugs for treating hyperlipemia, arteriosclerosis and the like. (1) (In the formula, m, n and p independently represent an integer of 0-4 and 3 ≤ m + n ≤ 8; X represents a group expressed as NR4 or the like; R1, R3 and R4 represent a substituted or unsubstituted aryl group or the like; R2 represents a hydrogen atom or the like; a, b, c, d, e and f respectively represent a hydrogen atom, a substituted or unsubstituted alkyl group or the like; Y represents -SO2- or the like; and Z represents an oxygen atom or the like.)
摘要翻译：公开了由下式（1）表示的化合物，其前药和它们的药学上可接受的盐，其具有增加LDL受体表达的作用并且可用作治疗高脂血症，动脉硬化等的药物。（1）（式中，m，n和p分别独立地表示0〜4的整数，且3≤m+n≤8; X表示以NR 4等表示的基团; R 1，R 3和R 4表示取代或未取代的芳基等; R 2表示氢原子等; a，b，c，d，e和f分别表示氢原子，取代或未取代的烷基等; Y表示-SO 2 - 或类似;并且Z表示氧原子等。）

4. 发明公开

EP1241159A4 AROMATIC DIAMIDE DERIVATIVES, CHEMICALS FOR AGRICULTURAL OR HORTICULTURAL USE AND USAGE THEREOF 审中-公开
标题翻译：芳香酰胺中的用途农业和园艺业及其使用衍生工具，化学品
公开(公告)号：EP1241159A4
公开(公告)日：2006-03-01
申请号：EP00985836
申请日：2000-12-22
申请人： NIHON NOHYAKU CO LTD
发明人： TOHNISHI MASANORI , KOHNO EIJI , NAKAO HAYAMI , NISHIDA TATEKI , FURUYA TAKASHI , SHIMIZU TOSHIAKI , SEO AKIRA , SAKATA KAZUYUKI , FUJIOKA SHINSUKE
IPC分类号： A01N37/30 , A01N41/06 , A01N43/16 , A01N43/28 , A01N43/40 , A01N47/12 , A01N47/28 , A01N57/14 , C07C233/66 , C07C233/69 , C07C233/75 , C07C233/78 , C07C239/16 , C07C271/12 , C07C271/20 , C07C271/28 , C07C275/14 , C07C307/06 , C07C311/05 , C07C311/18 , C07C323/12 , C07C323/43 , C07C335/08 , C07D295/205 , C07F9/24
CPC分类号： C07D295/205 , A01N37/30 , A01N41/06 , A01N43/16 , A01N43/28 , A01N43/40 , A01N47/12 , A01N47/28 , A01N57/14 , C07C233/66 , C07C233/69 , C07C233/75 , C07C233/78 , C07C239/16 , C07C271/12 , C07C271/20 , C07C271/28 , C07C275/14 , C07C307/06 , C07C311/05 , C07C311/18 , C07C323/12 , C07C323/43 , C07C335/08 , C07C2601/02 , C07F9/2458
摘要： Aromatic diamide derivatives of general formula (I) or salts thereof; chemicals for agricultural or horticultural use; and usage thereof [wherein A1 is optionally substituted C¿1-8? alkylene, C3-8 alkenylene, or the like; B is O- or -N(R?4¿)- (wherein R4 is H, C¿1-6? alkyl, halo C1-6 alkyl, or the like); R?1¿ is H, C¿1-6? alkyl, optionally substituted phenyl, an optionally substituted heterocyclic group, or the like; R?2 and R3¿ are each H, C¿3-6? cycloalkyl, or -A?2-R8¿ (wherein A2 is C(=O)-, -C(=S)-, or -C(=NR9)-; and R?8 and R9¿ are each H, C¿1-6? alkyl, or the like); Q?1 to Q5¿ are each carbon or nitrogen; X and Y are each halogeno, cyano, nitro, C¿3-6? cycloalkyl, optionally substituted phenyl, an optionally substituted heterocyclic group, or the like; n is 0 to 4; m is 1 to 5; and Z?1 and Z2¿ are each O or S]. The above chemicals exhibit remarkable controlling effects against various agricultural, forest and horticultural insect pests and stored grain insect pests which injure paddy rice, fruit trees, vegetables, other crop plants, flowers, ornamental plants, or the like.
摘要翻译：本发明涉及由通式（I）表示的芳族二酰胺衍生物： AEA <1>任选substituiertem（C1-C8），亚烷基，（C3-C8）烯基或类似的，B是 - O-或-N（R <4>） - （其中R <4>为H，（C1-C6）烷基，卤代（C1-C6）烷基等），R <1>为H，（C 1 -C C6）烷基，任选取代的苯基，任选取代的杂环基团，或类似物，R <2>和R <3>各自为H，（C3-C6）环烷基或-A <2> -R <8>（ A <2>是-C（= O） - ， - C（= S） - 或-C（= NR <9>） - ，R <8>和R <9>各自为H，（C1-C6）烷基等），Q <1>至Q <5>各自为碳或氮，X和Y各自是卤素，氰基，硝基，（C3-C6）环烷基，任选取代的苯基，任选取代的杂环基团，或像中，n是0至4，m是1至5，和Z <1>和Z <2>各为0或SRS或其盐，在农业和园艺化学的，和化学的使用。本发明的农业和园艺化学品表现出对各种害虫显着的防治效果：如农业，林业和园艺害虫和储粮害虫等，这些伤害水稻，果树，蔬菜，其它作物，花卉和观赏植物等。

5. 发明公开

EP1435936A1 5'-CARBAMOYL-1,1-BIPHENYL-CARBOXAMIDE DERIVATIVES AND THEIR USE AS P38 KINASE INHIBITORS 审中-公开
标题翻译： 5'-CARBAMOYL-1,1-BIPHENYL-CARBONSAUREAMID-DERIVATE UND IHRE VERWENDUNG ALS P38-KINASE-HEMMER
公开(公告)号：EP1435936A1
公开(公告)日：2004-07-14
申请号：EP02801339.9
申请日：2002-10-16
申请人： GLAXO GROUP LIMITED
发明人： ANGELL, Richard, Martync/o GlaxoSmithKline , ASTON, Nicola, MaryGlaxoSmithKline , BAMBOROUGH, PaulGlaxoSmithKline , BAMFORD, Mark, JamesGlaxoSmithKline , COCKERILL, George, Stuartc/o GlaxoSmithKline , MERRICK, Suzanne, JoyGlaxoSmithKline , SMITH, Kathryn, JaneGlaxoSmithKline , WALKER, Ann, LouiseGlaxoSmithKline
IPC分类号： A61K31/166 , A61K31/167 , C07C233/65 , C07C233/66 , C07C233/69 , C07C237/22 , C07C311/05 , C07D213/40 , C07D215/12 , C07D231/40 , C07D277/46 , C07D285/12 , C07D417/04
CPC分类号： C07D213/40 , C07C233/65 , C07C233/69 , C07C233/78 , C07C237/22 , C07C237/42 , C07C311/05 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D215/12 , C07D231/40 , C07D277/46 , C07D285/135 , C07D417/04
摘要： Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, -SO2NR4R5, -CONR4R5 and -COOR4; and when m is 2 to 4 R1 is additionally selected from C1-6alkoxy, hydroxy, NR4R5, -NR4SO2R5, -NR4SOR5, -NR4COR5, and -NR4CONR4R5; R2 is selected from hydrogen, C1-6alkyl and -(CH2)n-C3-7cycloalkyl; R3 is the group -CO-NH-(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1-6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
摘要翻译：式（I）化合物：其中当m为0至4时R 1选自C 1-6烷基，C 3-7环烷基，C 2-6烯基，-SO 2 NR 4 R 5，-CONR 4 R 5和-COOR 4; 当m为2至4时，R1另外选自C1-6烷氧基，羟基，NR4R5，-NR4SO2R5，-NR4SOR5，-NR4COR5和-NR4CONR4R5; R2选自氢，C1-6烷基和 - （CH2）n-C3-7环烷基; R3是-CO-NH-（CH2）p-R6基团; U选自甲基和卤素; W选自甲基和氯; V和Y各自独立地选自氢，甲基和卤素; m选自0,1,2,3和4，其中所得碳链的每个碳原子可以任选被一个或两个独立地选自C 1-6烷基的基团取代; n选自0,1,2和3; p和r独立地选自0,1和2; s选自0,1和2; 或其药学上可接受的盐或溶剂合物，以及它们作为药物的用途，特别是作为p38激酶抑制剂

6. 发明公开

EP0980864A3 Sulphonamide derivatives 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：EP0980864A3
公开(公告)日：2003-07-09
申请号：EP99306006.0
申请日：1999-07-28
申请人： ELI LILLY AND COMPANY
发明人： Arnold, Macklin Brian , Bender, David Michael , Jones, Winton Dennis , Ornstein, Paul Leslie , Simon, Richard Lee , Zarrinmayeh, Hamideh , Zimmerman, Dennis Michael , Fray, Andrew Hendley
IPC分类号： C07C311/04 , C07C311/09 , C07D333/20 , C07C311/03 , C07C311/05 , C07D213/53 , C07D213/81 , C07D213/82 , A61K31/18 , A61K31/38 , A61K31/44
CPC分类号： C07D213/42 , C07C311/03 , C07C311/04 , C07D213/26 , C07D213/81 , C07D333/16 , C07D333/20
摘要： The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

7. 发明公开

EP1311474A1 SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：EP1311474A1
公开(公告)日：2003-05-21
申请号：EP01932536.4
申请日：2001-05-04
申请人： ELI LILLY AND COMPANY
发明人： ARNOLD, Macklin, Brian , BLEISCH, Thomas, John , CUFF, George, William , ORNSTEIN, Paul, Leslie , 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 (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.

8. 发明公开

EP1268396A1 DIPHENYL ETHER COMPOUNDS USEFUL IN THERAPY 有权
标题翻译：二苯基醚化合物可用于治疗
公开(公告)号：EP1268396A1
公开(公告)日：2003-01-02
申请号：EP01917347.5
申请日：2001-03-19
申请人： Pfizer Limited , Pfizer Inc.
发明人： ANDREWS, Mark, David , HEPWORTH, David , MIDDLETON, Donald, Stuart , STOBIE, Alan
IPC分类号： C07C217/58 , C07C229/38 , C07C237/28 , C07C255/43 , C07C255/59 , C07C311/05 , C07C311/08 , C07C311/37 , C07C317/32 , C07C323/20 , C07C323/32 , C07C323/67 , C07D207/12 , C07D231/38 , C07D233/61 , C07D249/06 , C07D249/08 , C07D295/08 , C07D295/18 , A61K31/137
CPC分类号： H04L12/14 , 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 , C07D231/38 , C07D233/56 , C07D249/06 , C07D249/08 , C07D295/096 , C07D295/192 , G06F11/2038 , G06F11/2097 , H04L12/1403
摘要： A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein R3 is independ ently CF¿3?, OCF3, C1-C4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and the other variables are as defined in the claims. These compounds inhibit monoamine re-uptake and in particular exhibit activity as selective serotonin re-uptake inhibitors. They are useful in disorders such as depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder, substance abuse disorders and sexual dysfunction including premature ejaculation.
摘要翻译：通式（I）的化合物或其药学上可接受的盐，溶剂合物或多晶型物; 其中R3独立地为CF 3，OCF 3，C 1 -C 4烷硫基或C 1 -C 4烷氧基; n是1,2或3; 而其他变量如权利要求中所定义。这些化合物抑制单胺再摄取，特别是显示出作为选择性5-羟色胺再摄取抑制剂的活性。它们可用于抑郁症，注意力缺陷多动障碍，强迫症，创伤后应激障碍，药物滥用障碍和包括早泄在内的性功能障碍等疾病。

9. 发明授权

EP0864615B1 Azofarbstoffmischungen 失效
公开(公告)号：EP0864615B1
公开(公告)日：2002-11-27
申请号：EP98810109.3
申请日：1998-02-12
申请人： Ciba Specialty Chemicals Holding Inc.
发明人： Herzig, Paul , Clément, Antoine , Dreier, Romeo , Arquint, Alfons
IPC分类号： C09B67/22 , C07C229/16 , C07C233/43 , C07C271/28 , C07C275/40 , C07C311/05
CPC分类号： C09B67/0051 , C07C229/16 , C07C233/43 , Y10S8/922 , Y10S534/01

10. 发明公开

EP0864615A1 Azofarbstoffmischungen 失效
公开(公告)号：EP0864615A1
公开(公告)日：1998-09-16
申请号：EP98810109.3
申请日：1998-02-12
申请人： Ciba Specialty Chemicals Holding Inc.
发明人： Herzig, Paul , Clément, Antoine , Dreier, Romeo , Arquint, Alfons
IPC分类号： C09B67/22 , C07C229/16 , C07C233/43 , C07C271/28 , C07C275/40 , C07C311/05
CPC分类号： C09B67/0051 , C07C229/16 , C07C233/43 , Y10S8/922 , Y10S534/01
摘要： Farbstoffmischung enthaltend
als Komponente (A) einen Farbstoff der Formel
als Komponente (B) einen Farbstoff der Formel
und/oder
als Komponente (C) einen Farbstoff der Formel
worin D je den Rest einer Diazokomponente der Benzol-, Naphthalin-, Diphenyl-, Azobenzol-, Thiophen-, Benzthiazol-, Benzisothiazol-, Thiazol-, Thiadiazol-, Indazol-, Benztriazol-, Pyrazol-, Anthrachinon-, Naphtholsäureimid-, Chromon oder Diphenylenoxidreihe ist, X je Wasserstoff, Halogen, CF 3 , R 3 , OR 3 , NH-CO-R 7 , NH-CO-OR 8 , NH-SO 2 -R 7 oder NHCO-NR 4 R 5 , wobei R 3 C 1 -C 6 -Alkyl, R 4 und R 5 unabhängig voneinander je Wasserstoff, C 1 -C 4 -Al-kyl oder C 1 -C 4 -Alkoxy-C 2 -C 4 -alkyl, R 7 Wasserstoff, C 1 -C 6 -Alkyl, C 1 -C 4 -Alkoxy-C 1 -C 4 -alkyl oder Phenyl und R 8 C 1 -C 6 -Alkyl oder C 1 -C 4 -Alkoxy-C 2 -C 4 -alkyl bedeuten, und Y je Wasserstoff, Halogen, Methoxy, Ethoxy oder O(CH 2 ) n -OR 9 bedeutet, worin R 9 Wasserstoff, Methyl oder CH 2 CH 2 CN und n eine ganze Zahl von 1 bis 6 ist.
Die Farbstoffe eignen sich insbesondere zum Färben von Textilmaterial aus Polyesterfasern.
摘要翻译：一种染料混合物，其包含作为组分（A）下式的染料作为（B）成分的式和/或作为组分（C）下式的染料，其中d是每个基团的苯重氮组分，萘，联苯，偶氮苯的染料 - ，噻吩，苯并噻唑，苯并异噻唑，噻唑，噻二唑，吲唑，苯并三唑，吡唑，蒽醌，Naphtholsäureimid-，色酮或Diphenylenoxidreihe，X是氢，卤素，CF 3，R 3，OR 3，NH -CO-R 7，-NHCO-OR 8，NH-SO2-R7或NHCO-NR4R5，其中R3的C1-C6烷基，R4和R5各自独立为氢，C1-C4烷基或C1-C4烷氧基 -C 2 -C 4 - 烷基，R7是氢，C1-C6烷基，C1-C4烷氧基C1-C4烷基或苯基，和R 8的C 1 -C 6烷基或C 1 -C 4烷氧基-C 2 -C 4 - 烷基，和Y各自为氢，卤素，甲氧基，乙氧基或O（CH 2）N-OR 9是其中R 9是氢，甲基或CH 2 CH 2，n是从1到6的整数。这些染料特别适用于从聚酯纤维染色纺织材料。

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