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61. 发明公开

EP0896531A1 IL-8 RECEPTOR ANTAGONISTS 失效
标题翻译： IL-8受体拮抗剂
公开(公告)号：EP0896531A1
公开(公告)日：1999-02-17
申请号：EP96929723.0
申请日：1996-08-21
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： WIDDOWSON, Katherine, Louisa , VEBER, Daniel, Frank , JUREWICZ, Anthony, Joseph , RUTLEDGE, Melvin, Clarence, Jr. , HERTZBERG, Robert, Philip
IPC分类号： A61K31 , A61P29 , A61P37 , C07C253 , C07C255 , C07C275 , C07C307 , C07C309 , C07C311 , C07C317 , C07C323 , C07C335 , C07D213 , C07D215 , C07D217 , C07D277 , C07D317 , C07D333 , C07D409
CPC分类号： C07D213/30 , A61K31/17 , A61K31/18 , A61K31/223 , A61K31/275 , A61K31/277 , A61K31/36 , A61K31/381 , A61K31/426 , A61K31/47 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C307/10 , C07C309/15 , C07C311/10 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/42 , C07C323/44 , C07C335/18 , C07C2602/08 , C07C2603/18 , C07D213/71 , C07D215/36 , C07D217/02 , C07D277/36 , C07D277/46 , C07D317/66 , C07D333/28 , C07D333/34 , C07D333/36 , C07D409/04 , Y02A50/411
摘要： This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要翻译：本发明涉及新型化合物和苯基脲在治疗由趋化因子白细胞介素-8（IL-8）介导的疾病状态中的新用途。

62. 发明公开

EP0592439A1 AMINOSULFONYL CARBAMATES 失效
标题翻译：氨基磺酰氨基甲酸酯
公开(公告)号：EP0592439A1
公开(公告)日：1994-04-20
申请号：EP91920248.0
申请日：1991-11-05
申请人： WARNER-LAMBERT COMPANY
发明人： PICARD, Joseph, Armand , SLISKOVIC, Drago, Robert
IPC分类号： A61K31 , A61P3 , A61P9 , A61P43 , C07C307 , C07D209 , C07D213 , C07D235 , C07D295 , C07D307
CPC分类号： C07D213/42 , C07C307/06 , C07C307/08 , C07C307/10 , C07C2601/14 , C07D235/30 , C07D295/26 , C07D307/14
摘要： Composé de la formule générale (I) utile dans le traitement de l'hypercholestérolémie et de l'athéroschlérose, dans laquelle X représente oxygène ou soufre; R représente hydrogène, alkyle contenant 1 à 8 atomes de carbone ou benzyle; R1 représente phényle, phényle substitué, naphtyle, naphtyle substitué, un groupe aralkyl, un groupe hétérocyclique ou une chaîne d'hydrocarbures contenant 1 à 20 atomes de carbone, laquelle est saturée ou contient une à trois doubles liaisons, R2 et R3 sont chacun sélectionnés parmi l'hydrogène, à condition qu'il ne représente pas l'un et l'autre de l'hydrogène, un groupe aralkyle, une chaîne d'hydrocarbures contenant 1 à 20 atomes de carbone, laquelle est saturée ou contient 1 à 3 doubles liaisons, alkyle C1-6 à substitution w, un groupe hétérocyclique, phényle, phényle substitué ou NR2R3 pris ensemble forment un groupe hétérocyclique monocyclique.
摘要翻译：通式（I）中的高胆固醇血症和athéroschlérose，其中X表示氧或硫的治疗中有用的化合物， R为氢，含有1至8个碳原子的烷基或苄基; R 1是苯基，取代的苯基，萘基，取代的萘基，芳烷基，杂环基或含有碳原子数为1〜20的烃链，其是饱和的或含有一个至三个双键，R2和R3每个所选择的选自氢，条件是它不表示氢或者，芳烷基，碳原子数1〜20的烃链，其是饱和的或含有1至3个双键，取代的C 1-6烷基，杂环，苯基，取代的苯基或NR 2 R 3一起形成单环杂环基。

63. 发明公开

EP3416948A1 SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME 审中-公开
公开(公告)号：EP3416948A1
公开(公告)日：2018-12-26
申请号：EP17705416.0
申请日：2017-02-16
申请人： The University Of Queensland , The Provost, Fellows, Foundation Scholars, and the other members of Board, of the College of the Holy & Undiv. Trinity of Queen Elizabeth near Dublin
发明人： O'NEILL, Luke , COLL, Rebecca , COOPER, Matthew , ROBERTSON, Avril , SCHRODER, Kate , MACLEOD, Angus Murray , MILLER, David John
IPC分类号： C07D231/18 , C07C307/06 , C07C307/08 , C07C307/10 , C07D295/26 , A61P29/00
CPC分类号： C07D295/26 , C07C307/06 , C07C307/10 , C07C2601/14 , C07C2602/08 , C07C2603/10 , C07D231/18
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: Formula (I) wherein Q is selected from O, S and Se; J is S or Se; W1 and W2, when present, are independently selected from N and C; R1 and R2 are independently selected from the group consisting of hydrogen, C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W1 and W2 is present and is a nitrogen atom and when R1 and R2 are cyclic then the respective W1 or W2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

64. 发明公开

EP3229793A4 COMPOSITIONS AND METHODS RELATING TO THE TREATMENT OF CANCER, AUTOIMMUNE DISEASE, AND NEURODEGENERATIVE DISEASE 审中-公开
公开(公告)号：EP3229793A4
公开(公告)日：2018-08-01
申请号：EP15866774
申请日：2015-12-14
申请人： THE JACKSON LABORATORY
发明人： MILLS KEVIN DAVID , HASHAM MUNEER GULAMHUSEIN
IPC分类号： A61K31/145 , C07C307/10 , C07C311/08 , C07C311/39 , C07C311/47 , C07C335/16 , C07C335/20 , C07C335/22 , C07D205/04 , C07D295/26 , C07F9/12 , C07F9/38
CPC分类号： C07C335/20 , C07C307/10 , C07C311/08 , C07C311/39 , C07C311/47 , C07C335/16 , C07C335/22 , C07D205/04 , C07D295/26 , C07F9/12 , C07F9/3873
摘要： Described herein are methods and compositions relating to the treatment of e.g., cancer, autoimmune disease, immune deficiency, and/or neurodegenerative disease. In some embodiments, the methods of treatment relate to administering a compound as described herein. In some embodiments, the subject treated according to the methods described herein is a subject determined to have an increased level of DNA damage.

65. 发明公开

EP3275861A1 TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：四环素化合物
公开(公告)号：EP3275861A1
公开(公告)日：2018-01-31
申请号：EP17183980.6
申请日：2010-08-27
申请人： Tetraphase Pharmaceuticals, Inc.
发明人： Deng,, Yonghong , Plamondon,, Louis , Sun,, Cuixiang , Xiao,, Xiao-Yi , Zhou,, Jingye , Sutcliffe,, Joyce, A. , Ronn,, Magnus, P.
IPC分类号： C07C237/26 , C07C311/21 , C07D207/04 , C07D211/54 , C07D213/82 , C07D233/60 , C07D307/10 , C07D295/088 , A61P31/04 , A61K31/165 , A61K31/18 , A61K31/401 , A61K31/397 , A61K31/4453 , A61K31/4164 , A61K31/4406 , A61K31/415 , A61K31/4402
CPC分类号： C07C311/08 , C07C237/26 , C07C307/10 , C07C311/09 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2603/40 , C07C2603/44 , C07C2603/46 , C07D205/04 , C07D207/12 , C07D207/16 , C07D209/44 , C07D209/52 , C07D211/54 , C07D211/60 , C07D213/70 , C07D213/74 , C07D213/82 , C07D223/06 , C07D231/18 , C07D233/60 , C07D233/84 , C07D295/15 , C07D307/64
摘要： The present invention is directed to a compound represented by Structural Formula (I):

or a pharmaceutically acceptable salt thereof. X in formula (I) is selected from -OCF 3 and -OCH 3 . The other variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
摘要翻译：本发明涉及由结构式（I）表示的化合物：或其药学上可接受的盐。式（I）中的X选自-OCF 3和-OCH 3。结构式（I）的其他变量在本文中定义。还描述了包含结构式（I）的化合物及其治疗用途的药物组合物。

66. 发明公开

EP3154537A4 ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF 有权
公开(公告)号：EP3154537A4
公开(公告)日：2017-12-27
申请号：EP15806506
申请日：2015-06-11
申请人： MERCK SHARP & DOHME
发明人： LEAVITT KENNETH , CROWLEY BRENDAN , BELL IAN M , HARVEY ANDREW , AVERY THOMAS , PAUL DHARAM , RIPPER JUSTIN , HUFF BELINDA , SINGH RAJINDER , SCHAEFFER LAURENT , JOSEPH CHRISTOPHE , MORICE CHRISTOPHE , GIETHLEN BRUNO , BAZZINI PATRICK , FROMEYER AURELIE
IPC分类号： C07C311/08 , A61K31/18 , A61P25/28 , C07C311/37 , C07D213/64 , C07D213/69 , C07D239/34
CPC分类号： C07C311/29 , C07C307/10 , C07C311/08 , C07C323/67 , C07C2601/02 , C07C2602/50 , C07D213/64 , C07D213/65 , C07D213/69 , C07D239/34
摘要： Disclosed are compounds of Formula (IVA), or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof: Formula (IVA), wherein "RIa", "RIb", "RIc", "RId", "RIe", are defined herein above, which compounds are believed suitable for use in positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR) receptors, for example, those found in the cerebral cortex and the hippocampus. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Alzheimer's disease (AD), schizophrenia, and Parkinson's disease (PD), or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

67. 发明公开

EP2990403A1 ANTHRANILAMIDES, SULFONAMIDES AND NITRO ANALOGUES DERIVED THEREFROM AS ANTHELMINTICS 审中-公开
标题翻译： ANTHRANILAMIDE SOWIE ABGELEITETE SULFONAMIDE UND NITRO ANALOGE ALS ANTHELMINTISCHE VERBINDUNGEN
公开(公告)号：EP2990403A1
公开(公告)日：2016-03-02
申请号：EP14182960.6
申请日：2014-08-29
申请人： Novartis Tiergesundheit AG
发明人： The designation of the inventor has not yet been filed
IPC分类号： C07D213/61 , C07C205/11 , C07C311/08 , C07C311/20 , A61P33/10 , A61K31/18
CPC分类号： C07D213/61 , C07C235/56 , C07C307/10 , C07C311/08 , C07C311/09 , C07C311/10 , C07C311/14 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/40 , C07C2602/42 , C07D213/26 , C07D213/64 , C07D213/65 , C07D213/84 , C07D231/12 , C07D231/20 , C07D231/56 , C07D239/26 , C07D239/30 , C07D239/34 , C07D249/12 , C07D277/30 , C07D277/62 , C07D277/64 , C07D279/12 , C07D295/155 , C07D295/185 , C07D295/26 , C07D333/24 , C07D333/28 , C07F5/025 , C07F7/0818
摘要： The present invention relates to a new compound of formula

wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasites, in and on vertebrates.
摘要翻译：本发明涉及一种新的式化合物，其中变量具有如权利要求中所示的含义; 或其对映异构体或其盐。式（I）化合物可用于控制寄生虫，特别是脊椎动物内和寄生虫的寄生虫。

68. 发明公开

EP2740723A4 SULPHAMIDE DERIVATIVE HAVING AN ADAMANTYL GROUP AND A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 有权
标题翻译：亚硝胺类药物艾滋病毒抗体药物联合药物化学制剂ZULÄSSIGENSALZ DAVON
公开(公告)号：EP2740723A4
公开(公告)日：2015-01-07
申请号：EP12763010
申请日：2012-03-30
申请人： KOREA RES INST CHEM TECH
发明人： KIM KI YOUNG , AHN JIN HEE , KANG SEUNG KYU , BAE MYUNG AE , AHN SUNG HOON , KIM HEE YOUN , JUNG WON HOON , KANG NAM SOOK , RHEE SANG DAL
IPC分类号： C07C307/10 , A61K31/18 , A61P3/10
CPC分类号： C07D417/04 , A61K31/18 , C07C307/10 , C07C2603/74 , C07D285/10 , C07D285/14 , C07D285/15 , C07D285/16 , C07D285/36 , C07D417/10 , C07D417/12

69. 发明公开

EP2628727A2 Biaryl PDE4 inhibitors for treating pulmonary and cardiovascular disorders 审中-公开
标题翻译： Biaryl-PDE4-Inhibitoren zur Behandlung von Lungen- und Herz-Kreislauferkrankungen
公开(公告)号：EP2628727A2
公开(公告)日：2013-08-21
申请号：EP13000709.9
申请日：2008-11-20
申请人： Decode Genetics EHF
发明人： Singh, Jasbir , Gurney, Mark , Burgin, Alex , Kiselyov, Alexander , Rao, Munagala , Hagen, Timothy
IPC分类号： C07D207/16 , C07D213/64 , C07D213/79 , C07D231/12 , C07D239/42 , C07D401/06 , C07D471/04 , C07D473/18 , C07D473/40 , C07D285/135 , C07D213/06 , C07D213/74 , C07D213/75 , C07D213/84 , C07D401/04 , C07D233/90 , C07D275/06
CPC分类号： C07C217/84 , A61K31/136 , A61K31/397 , A61K31/41 , A61K31/426 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C65/40 , C07C69/94 , C07C275/32 , C07C275/62 , C07C305/24 , C07C307/10 , C07D205/04 , C07D207/16 , C07D213/38 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D233/90 , C07D239/42 , C07D257/04 , C07D275/06 , C07D277/42 , C07D285/12 , C07D285/135 , C07D401/04 , C07D401/06 , C07D403/04 , C07D471/04 , C07D473/18 , C07D473/40
摘要： The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula Ia, Ib, Ic or Id:

or salt thereof, in particular a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及含有至少一个其它环的联芳基化合物的属。该化合物是可用于治疗和预防中风，心肌梗死和心血管炎性疾病和病症的PDE4抑制剂。化合物具有通式Ia，Ib，Ic或Id：或其盐，特别是其药学上可接受的盐。

70. 发明公开

EP2496556A1 ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： ACYLAMINSUBSTITUIERTE CYCLISCHE CARBOXYLSAUREDERIVATE UND IHRE VERWENDUNG ALS ARZNEIMITTEL
公开(公告)号：EP2496556A1
公开(公告)日：2012-09-12
申请号：EP10776045.6
申请日：2010-11-02
申请人： SANOFI
发明人： PERNERSTORFER, Josef , KLEEMANN, Heinz-Werner , SCHAEFER, Matthias , SAFAROVA, Alena , PATEK, Marcel
IPC分类号： C07D213/16 , C07D305/04 , C07D309/08 , C07D335/14 , C07D317/06 , C07C235/54 , A61K31/085
CPC分类号： C07C235/54 , C07C231/00 , C07C231/02 , C07C235/42 , C07C235/84 , C07C255/50 , C07C255/54 , C07C255/57 , C07C307/10 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/22 , C07C2602/50 , C07D213/16 , C07D213/64 , C07D213/69 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/18 , C07D305/04 , C07D305/06 , C07D305/08 , C07D309/04 , C07D309/08 , C07D309/14 , C07D313/04 , C07D317/06 , C07D317/68 , C07D317/72 , C07D333/16 , C07D333/32 , C07D335/02 , C07D335/14 , C07D335/18 , C07D493/10
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are pharmaceutically active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 20至R 22和R 50具有权利要求中所述的含义，其为药学活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

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