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2. 发明公开

EP3559006A1 COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES 审中-公开
公开(公告)号：EP3559006A1
公开(公告)日：2019-10-30
申请号：EP17882731.7
申请日：2017-12-13
申请人： Arvinas Operations, Inc. , Yale University
发明人： CREW, Andrew, P. , HORNBERGER, Keith, R. , CREWS, Craig, M. , BURSLEM, George
IPC分类号： C07D495/04 , C07D513/14 , C07D209/32 , A61K31/519

3. 发明公开

EP3101019A1 SULFONAMIDE DERIVATIVES AS BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES 审中-公开
标题翻译：苏氨酸衍生物ALS BCL-2-SELEKTIVE APOPTOSEINDUKTOREN ZUR BEHANDLUNG VON KREBS SOWIE VON IMMUNERKRANKUNGEN
公开(公告)号：EP3101019A1
公开(公告)日：2016-12-07
申请号：EP16169764.4
申请日：2009-12-04
申请人： AbbVie Inc.
发明人： BRUNCKO, Milan , DING, Hong , DOHERTY, George, A. , ELMORE, Steven, W. , HASVOLD, Lisa , HEXAMER, Laura , KUNZER, Aaron, R. , MANTEI, Robert, A. , MCCLELLAN, William, J. , PARK, Chang, H. , PARK, Cheol-min , PETROS, Andrew, M. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , TAO, Zhi-fu , WANG, Gary, T. , WANG, Le , WANG, Xilu , WENDT, Michael, D.
IPC分类号： C07D405/12 , A61K31/404 , A61P35/00 , C07D209/32 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D235/26 , C07D249/04 , C07D295/14 , C07D309/14 , C07D401/12 , C07D295/125
CPC分类号： C07D405/12 , C07D209/32 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D231/56 , C07D235/26 , C07D249/04 , C07D295/125 , C07D295/14 , C07D309/14 , C07D401/12 , C07D417/12
摘要： Disclosed are compounds of formula (I) which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
摘要翻译：公开了抑制抗凋亡Bcl-2或Bcl-xL蛋白活性的式（I）化合物，含有该化合物的组合物和治疗其中表达抗凋亡Bcl-2蛋白的疾病的方法。

4. 发明公开

EP2170826A1 PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES 有权
标题翻译： NSAIDs的前体药物具有很高的皮肤和膜的普及率及新医疗用途
公开(公告)号：EP2170826A1
公开(公告)日：2010-04-07
申请号：EP07825791.2
申请日：2007-06-04
申请人： Techfields Inc , Yu, Chongxi
发明人： YU, Chongxi , XU, Lina
IPC分类号： C07D209/32 , C07D231/12 , C07D471/08 , C07D487/08 , C07D213/74 , C07D215/10 , C07D217/12 , A61K31/44 , A61P29/00 , A61P3/00
CPC分类号： C07D513/04 , C07D205/04 , C07D211/22 , C07D295/088 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/052
摘要： The novel positively charged pro-drugs of NSAIAs in the general formulas (1, 2a, 2b, 2c, or 2d) 'Structure 1, 2a, 2b, 2c, or 2d' were designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) 'Structure 1, 2a, 2b, 2c, or 2d' indicated above can be prepared from metal salts, organic base salts, or immobilized base salts of NSAIAs with suitable halide compounds. The positively charged amino groups in the pro-drugs in this invention largely increase the solubility of the drugs in water and will bond to the negative charge on the phosphate head group of membrane. Thus, the local concentration of the outside of the membrane or skin will be very high and will facilitate the passage of these pro-drugs from a region of high concentration to a region of low concentration. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the pro-drug. When the molecules of membrane move, the membrane may 'crack' a little bit due to the bonding of the pro-drug. This will let the pro- drug insert into the membrane. At pH 7.4, only about 99% of the amino group is protonated. W hen the amino group is not protonated, the bonding between the amino group of the pro-drug and the phosphate head group of the membrane will disassociate, and the pro-drug will enter the membrane completely. When the amino group of the pro-drug flips to the other side of the membrane and thus becomes protonated, then the pro-drug is pulled into the cytosol, a semi- liquid concentrated aqueous solution or suspension. These pro-drugs can be used for treating and preventing diabetes (type I or/and type II), abnormal blood glucose and lipid levels, stroke, heart attack, and other heart and vascular diseases Alzheimer's diseases, Parkinson's diseases and other neurodegenerative diseases, psoriasis, discoid lupus erythematosus, systemic lupus erythematosus (SLE), autoimmune hepatitis, multiple sclerosis (MS), and other autoimmune diseases, amyotrophic lateral sclerosis (ALS), oculopharyngeal muscular dystrophy ( OPMD), and other muscle disorders, inflamed hemorrhoids, cryptitis, other inflammatory conditions of the anorectum, and pruritus ani, prostatitis, prostatocystitis, varicose veins, autoimmune liver inflammation, autoimmune kidney inflammation, vein inflammation and other inflammations, skin cancers, breast cancer, colon-rectum cancer, oral cancer, and other cancers, scars, abnormal vascular skin lesions, birthmarks, moles (nevi), skin tags, aging spots (liver spots), and other skin disorders. These pro-drugs can be administered transdermally without the help of skin penetration enhancers.

5. 发明公开

EP2114879A1 PPAR ACTIVE COMPOUNDS 审中-公开
标题翻译： PPAR活性化合物
公开(公告)号：EP2114879A1
公开(公告)日：2009-11-11
申请号：EP08731467.0
申请日：2008-03-05
申请人： PLEXXIKON, INC.
发明人： LIN, Jack , LEE, Byunghun , SHI, Shenghua , ZHANG, Chao , ARTIS, Dean , IBRAHIM, Prabha , WANG, Weiru , ZUCKERMAN, Rebecca
IPC分类号： C07D209/18 , C07D209/30 , C07D209/32 , C07D401/12 , C07D403/12 , A61K31/405 , A61P3/00
CPC分类号： C07D401/12 , C07D209/18 , C07D403/12
摘要： Compounds as shown below are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ.
摘要翻译：描述了对PPARα，PPARδ和PPARγ中的至少一种有活性的如下所示的化合物，其可用于涉及调节PPARα，PPARδ和PPARγ中的至少一种的治疗和/或预防方法。

6. 发明公开

EP1960355A1 3-AMINO-1-ARYLPROPYL INDOLES AND AZA-SUBSTITUTED INDOLES 审中-公开
标题翻译： 3-AMINO-1-ARYLPROPYL INDOLES和AZA-SUBSTITUTED INDOLES
公开(公告)号：EP1960355A1
公开(公告)日：2008-08-27
申请号：EP06819600.5
申请日：2006-11-20
申请人： F.HOFFMANN-LA ROCHE AG
发明人： IYER, Pravin , LUCAS, Matthew C , SCHOENFELD, Ryan Craig , VILLA, Marzia , WEIKERT, Robert James
IPC分类号： C07D209/14 , C07D231/56 , C07D409/06 , C07D209/30 , C07D307/79 , C07D413/06 , C07D209/32 , C07D333/52 , C07D471/04 , C07D209/40 , C07D401/06 , A61K31/44 , C07D209/42 , C07D403/06 , A61P25/00
CPC分类号： C07D209/12 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/32 , C07D209/40 , C07D209/42 , C07D231/56 , C07D235/06 , C07D235/24 , C07D235/26 , C07D307/79 , C07D311/04 , C07D333/52 , C07D333/58 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/06 , C07D413/06 , C07D417/10 , C07D471/04
摘要： The present invention provides compounds of the formula: (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译：本发明提供了式（I）化合物或其药学上可接受的盐，溶剂化物或前药，其中p，Ar，R 1，R 2，R 3，R a，R b，R c，R d和R e如本文所定义。还提供了药物组合物，使用方法和制备该化合物的方法。

7. 发明授权

EP0993442B1 HYDRAZINE DERIVATIVES 失效
标题翻译： HYDRAZINDERIVATE
公开(公告)号：EP0993442B1
公开(公告)日：2003-04-23
申请号：EP98937498.8
申请日：1998-06-18
申请人： F. HOFFMANN-LA ROCHE AG
发明人： BROADHURST, Michael John , JOHNSON, William, Henry , WALTER, Daryl, Simon
IPC分类号： C07C311/49 , A61K31/18 , C07C259/06 , C07C281/02 , C07C281/06 , C07D209/32 , C07D209/48 , C07D211/58 , C07D211/98 , C07D213/42 , C07D213/56
CPC分类号： C07D207/325 , C07C243/28 , C07C243/32 , C07C259/06 , C07C311/49 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/14 , C07D209/48 , C07D211/38 , C07D211/58 , C07D213/42 , C07D213/56 , C07D213/77 , C07D215/38 , C07D231/12 , C07D233/56 , C07D233/76 , C07D239/26 , C07D239/42 , C07D249/08 , C07D263/22 , C07D275/02 , C07D277/30 , C07D277/56 , C07D277/82 , C07D279/02 , C07D305/06 , C07D307/52 , C07D307/68 , C07D307/81 , C07D309/06 , C07D309/14 , C07D309/30 , C07D317/28 , C07D333/34 , C07D333/38 , C07D335/02 , Y10S514/837 , Y10S514/861 , Y10S514/863 , Y10S514/885 , Y10S514/903
摘要： Hydrazine derivatives of formula (I) wherein Y signifies CO or SO2; R1 signifies lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 signifies lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y signifies SO¿2? and signifies lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR?5R6¿ when Y signifies CO; and R3 signifies hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonly, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl- lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R?2 and R3¿ together form the residue of a 5-, 6- or 7- membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 signifies lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkly-lower alkyl or a grouping of the formula X-aryl, X-heteroaryl or -(CH¿2?)1-2-CH=CR?7R8¿; X signifies a spacer group; R?5 and R6¿ each individually signify hydrogen, lower alkyl or aryl-lower alkyl; and R?7 and R8¿ together represent a lower alkylene group in which one methylene group is optionally replaced by a hetero atom; and their pharmaceutically acceptable salts inhibit not only the release of tumour necrosis factor (TNF-α) and transforming growth factor (TGF-α) from cells, but also keratinocyte proliferation. They are useful as medicaments, especially for the treatment of inflammation, fever, haemorrhage, sepsis, rheumatoid arthritis, osteoarthritis, multiple sclerosis or psoriasis.
摘要翻译：甲酰亚胺Y的肼衍生物是CO或SO 2; R1是低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基或芳基 - 低级烷基; 当Y为SO2时，R2为低级烷基，卤代低级烷基，芳基 - 低级烷基，芳基 - 低级烯基或芳基，为低级烷基，卤代低级烷基，低级烷氧基，低级烷氧基羰基，酰基，低级环烷基，芳基，当Y为CO时，低级烷基，芳基 - 低级烷氧基或NR5R6; 低级烯基，低级炔基，低级环烷基，低级环烷基 - 低级烷基，芳基 - 低级烷基，芳基 - 低级烯基，芳基 - 低级烷基，低级烷氧基，低级烷氧基，低级烷氧基，，芳基或杂环基; 或R 2和R 3一起形成5-，6-或7-元环酰胺，环状酰亚胺，环状磺酰胺或环状氨基甲酸酯基团的残基; R4是低级烷基，羟基 - 低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基或式X-基，X-杂芳基或 - （CH2）1-2-CH = CR7R8基团; X是间隔基; R5和R6各自独立地为氢，低级烷基或芳基 - 低级烷基; 并且R 7和R 8一起代表一个亚甲基任选被杂原子取代的低级亚烷基; 并且其药学上可接受的盐不仅抑制肿瘤坏死因子（TNF-α）和转化生长因子（TGF-α）从细胞的释放，而且抑制角质形成细胞增殖。它们可用作药物，特别是用于治疗炎症，发烧，出血，败血症，类风湿性关节炎，骨关节炎，多发性硬化或牛皮癣。

8. 发明公开

EP1119549A4 PROCESS FOR PREPARING 4-SUBSTITUTED-1H-INDOLE-3-GLYOXAMIDES 审中-公开
标题翻译：过程用于在4位取代的1H-吲哚-3- GLYOXAMIDEN
公开(公告)号：EP1119549A4
公开(公告)日：2003-01-29
申请号：EP99917552
申请日：1999-04-15
申请人： LILLY CO ELI
发明人： ANDERSON BENJAMIN ALAN , HARN NANCY KAY , MILLER RICHARD DUANE , PLOCHARCZYK EDWARD FRANCIS
IPC分类号： C07D209/22 , C07D209/12 , C07D209/32 , C07D209/34
CPC分类号： C07D209/22 , Y02P20/55

9. 发明公开

EP1071663A4 PROCESS FOR PREPARING 4-SUBSTITUTED-1H-INDOLE-3-GLYOXAMIDES 审中-公开
标题翻译：用于生产4-取代的1H-吲哚-3-乙醛酰胺
公开(公告)号：EP1071663A4
公开(公告)日：2002-06-19
申请号：EP99917556
申请日：1999-04-15
申请人： LILLY CO ELI
发明人： ANDERSON BENJAMIN ALAN , HARN NANCY KAY
IPC分类号： C07D209/12 , C07D209/22 , C07D209/30 , C07D209/32 , C07D209/34 , C07D209/16
CPC分类号： C07D209/30 , C07D209/22 , Y02P20/55

10. 发明授权

EP0865421B1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS 失效
标题翻译： ARYLETHANOLAMINDERIVATE及其用途非典型β-肾上腺能受体激动剂
公开(公告)号：EP0865421B1
公开(公告)日：2002-03-27
申请号：EP96943050.3
申请日：1996-12-06
申请人： GLAXO GROUP LIMITED
发明人： GREEN, Richard, Howard-Glaxo Wellcome plc
IPC分类号： C07C229/42 , C07C217/84 , A61K31/19 , A61K31/40 , C07D209/24 , C07D209/32
CPC分类号： C07D209/08 , C07C217/84 , C07C229/42 , C07D215/04

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