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1. 发明公开

EP2308851A1 Imidazolone and imidazolidinone derivatives as 11B-HSD1 inhibitors for the treatment of diabetes 审中-公开
标题翻译：咪唑啉和咪唑啉酮衍生物11B-HSD1抑制剂
公开(公告)号：EP2308851A1
公开(公告)日：2011-04-13
申请号：EP10175995.9
申请日：2007-10-09
申请人： F. Hoffmann-La Roche AG
发明人： Ackermann, Jean , Amrein, Kurt , Hunziker, Daniel , Kuhn, Bernd , Mayweg,, Alexander V. , Neidhart, Werner , Takahashi, Tadakatsu
IPC分类号： C07D233/02 , C07D233/06 , C07D233/10 , C07D233/28 , C07D471/10 , A61P3/10 , A61K31/4166
CPC分类号： C07D233/02 , A61K9/2054 , A61K9/4866 , C07D233/06 , C07D233/10 , C07D233/28 , C07D471/06 , C07D471/10
摘要： Compounds of formula

as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
摘要翻译：式1化合物及其药学上可接受的盐和酯，其中R 1至R 6具有权利要求1中给出的含义，可以以药物组合物的形式使用。

2. 发明公开

EP2158186A1 IONISCHE N-HALTIGE VERBINDUNGEN 审中-公开
标题翻译：离子的含N化合物
公开(公告)号：EP2158186A1
公开(公告)日：2010-03-03
申请号：EP08773394.5
申请日：2008-06-12
申请人： Cognis IP Management GmbH
发明人： BUSCH, Stefan , BIRNBRICH, Paul , MEYER, Joachim , KLAGGE, Ronald
IPC分类号： C07D233/10 , B01F17/32
CPC分类号： C07D233/10 , B01F17/0042 , C08F2/28
摘要： Ionic N-containing compounds of the general formula (I), wherein the index n is the number 0 or 1 and the radicals R1 to R5 independently from each other are hydrogen or alkyl, cycloalkyl or aryl radicals with 1 to 25 carbon atoms, wherein the alkyl radicals can be saturated or olefinically unsaturated, straight-chained or branched, and the cycloalkyl radicals can be saturated or olefinically unsaturated, with the following stipulations: (1) if n = 1, at least one of the radials R1 to R5 must contain up to 25 carbon atoms, (2) if n = 0, at least one of the radicals R1, R2, R3 or R5 must contain 8 to 25 carbon atoms, (3) the carbon atoms carrying the radicals R2 and R3 are linked via a C-C-single bond or a C=C-double bond, (4) in the radicals R1 to R5 - if they are alkyl or cycloalkyl radicals - a hydrogen atom linked to a carbon atom can be substituted with an -OH or NH2 group, or an -O-, -COO- or -NH- group can be inserted between two neighboring carbon atoms linked via a C-C single bond, (5) in the radicals R1 to R5 - if they are aryl radicals - a hydrogen atom linked to a carbon atom can be optionally substituted with an alkyl or cycloalkyl group having 1 to 12 carbon atoms, with the stipulation that the following applies to said alkyl or cycloalkyl group: optionally a hydrogen atom linked to a carbon atom can be substituted with an -OH or NH2 group or an -O-, -COO- or -NH- group can be inserted between two neighboring carbon atoms linked via a C-C-single bond, said compounds being suitable as temporary surfactants, particularly for the production of aqueous emulsions or dispersions.

3. 发明授权

EP1268440B1 IMIDAZOLE CARBENES 有权
标题翻译： IMIDAZOLCARBENE
公开(公告)号：EP1268440B1
公开(公告)日：2005-12-07
申请号：EP01917276.6
申请日：2001-04-05
申请人： The Queen's University of Belfast
发明人： EARLE, Martyn, John , SEDDON, Kenneth, Richard "Tara"
IPC分类号： C07D233/06 , C07D233/10
CPC分类号： C07D231/12 , C07D233/06 , C07D233/10 , C07D233/56 , C07D249/08
摘要： A process for the preparation of imidazolium carbenes of formula (I) wherein R1 and R2 which can be the same or different, are hydrogen or linear or branched hydrocarbyl groups comprising heating an imidazolium halide with a strong base under reduced pressure and separating the resultant products is described. Also described is a process for the preparation of salts of these imidazolium carbenes, and their use as ionic liquids.

4. 发明公开

EP1383748A2 NOVEL COMPOUNDS AND COMPOSITIONS AS CATHEPSIN INHIBITORS 审中-公开
标题翻译：新化合物和组合物作为抑制剂CATHEPSIN
公开(公告)号：EP1383748A2
公开(公告)日：2004-01-28
申请号：EP01988420.4
申请日：2001-12-24
申请人： AXYS PHARMACEUTICALS, INC. , Halley, Frank , Aventis Pharmaceuticals Inc.
发明人： GRAUPE, Michael , PATTERSON, John , PICKETT, Stephen, D. , LINK, John , LI, Jiayao , ALDOUS, David , THURAIRATNAM, Sukanthini , TIMM, Andreas , HALLEY, Frank , LAI, Justine
IPC分类号： C07D263/56 , C07D277/64 , C07D295/18 , C07C317/44 , C07D271/06 , C07C323/60 , C07D205/08 , C07D277/26 , C07C317/50 , C07D207/26 , C07D233/10 , C07D498/04 , C07D271/10 , C07D413/04 , C07D223/12 , A61K31/16 , A61P29/00
CPC分类号： C07D207/273 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/40 , C07D223/10 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12 , Y02A50/411
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

5. 发明公开

EP1204644A1 SYNTHESIS OF SUBSTITUTED AMIDINES 审中-公开
标题翻译：合成取代的脒
公开(公告)号：EP1204644A1
公开(公告)日：2002-05-15
申请号：EP00941119.0
申请日：2000-06-19
申请人： ELI LILLY AND COMPANY
发明人： CHOUEIRY, Daniele , GIRAUD, Daniel, Lionel , SCHOTTEN, Theo
IPC分类号： C07D233/06 , C07D233/08 , C07D233/10 , C07D239/06 , C07D243/04 , C07D401/06 , C07D405/04 , C07D401/04
CPC分类号： C07D239/06 , C07D233/06 , C07D235/18 , C07D243/04 , C07D405/04 , C07D451/02 , C40B40/00
摘要： The present invention provides a process for preparing amidines starting from carboxylic acid derivatives, in which the carboxylic acid containing moiety is attached to a sp3-, or sp?2- or sp1¿-hybridized carbon atom. The sp2-hybridized carbon atom, to which the carboxylic acid containing moiety is attached to may be part of an aromatic or heteroaromatic or olefinic system.

6. 发明公开

EP1104407A1 COMPOUNDS AS SELECTIVE AGONISTS AT ALPHA 2B OR 2B/2C ADRENERGIC RECEPTORS 有权
标题翻译：化合物ALPHA 2B或作为选择性激动剂2B / 2C肾上腺素能受体
公开(公告)号：EP1104407A1
公开(公告)日：2001-06-06
申请号：EP00939699.5
申请日：2000-06-08
申请人： Allergan Sales, Inc.
发明人： CHOW, Ken , GIL, Daniel, W. , BURKE, James, A. , HARCOURT, Dale, A. , GARST, Michael, E. , WHEELER, Larry, A. , MUNK, Stephen, A.
IPC分类号： C07D233/54 , A61K31/33 , A61P43/00 , C07D409/06 , C07D263/28 , C07D413/12 , C07D233/84 , C07D233/10 , C07D405/06 , C07D401/06 , C07D403/06 , C07D495/04
CPC分类号： C07D233/56 , C07D233/10 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Compounds having adrenergic activity which are a selective agonists for one or both of the α2B and α2C adrenoceptor receptor subtypes in prefrence to the α2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds; R is H or lower alkyl; X is S or C(H)R1, wherein R1 is H or lower alkyl, Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y1CH2-, wherein Y1 is O, N or S.

7. 发明授权

EP0622357B1 Process for the production of cyclic amidine 失效
标题翻译：一种制备环脒过程
公开(公告)号：EP0622357B1
公开(公告)日：1996-11-06
申请号：EP94300455.6
申请日：1994-01-21
申请人： LION AKZO COMPANY LIMITED
发明人： Noda, Seiji , Tsuji, Takeshi
IPC分类号： C07D233/06 , C07D233/10 , C07D239/06 , C07D243/04 , C07D245/02
CPC分类号： C07D239/26 , C07D233/06 , C07D233/10 , C07D243/04 , C07D245/02

8. 发明授权

EP0002943B1 Process for the manufacture of imidazolines 失效
标题翻译：咪唑啉的制备方法
公开(公告)号：EP0002943B1
公开(公告)日：1982-01-13
申请号：EP78300886.5
申请日：1978-12-21
申请人： Albright & Wilson Limited
发明人： Phillips, Brinley Morris , Lace, Robert Briscoe , Lambie, Alan James
IPC分类号： C07D233/10 , C07D233/14 , C07D233/16
CPC分类号： C07D233/10 , C07D233/14

10. 发明公开

EP3177144A4 COMPOSITIONS AND METHODS FOR SELECTIVELY DEPLETING SENESCENT CELLS 无效
公开(公告)号：EP3177144A4
公开(公告)日：2018-01-24
申请号：EP15824181
申请日：2015-07-22
申请人： BIOVENTURES LLC
发明人： ZHENG GUANGRONG , ZHOU DAOHONG , LIU XINGUI , WANG YINGYING , CHANG JIANHUI , FENG WEI , SHAO LIJIAN , LUO YI
IPC分类号： C07D233/10 , A61K31/55 , A61K31/635 , A61P35/00 , C07D207/38 , C07D401/06 , C07D405/06
CPC分类号： A61K31/45 , A23L33/10 , A23V2002/00 , A61K31/4015 , A61K31/4412 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/55 , A61K31/635 , C07D207/38 , C07D211/76 , C07D211/88 , C07D211/96 , C07D223/10 , C07D401/06 , C07D405/06 , A61K2300/00 , A23V2200/302
摘要： The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises piperlongumine (PL) or derivative thereof. The selective killing of senescent cells may delay aging and/or treat age-related disorders.

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