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1. 发明公开

EP3939664A1 COMPOUNDS FOR USE IN THE TREATMENT OF VIRAL INFECTIONS BY VIRUS OF THE FAMILY CORONAVIRIDAE 审中-公开
公开(公告)号：EP3939664A1
公开(公告)日：2022-01-19
申请号：EP20382647.4
申请日：2020-07-17
申请人： Consejo Superior De Investigaciones Científicas
发明人： GUTIÉRREZ RODRÍGUEZ, Marta , IZQUIERDO GARCÍA, Carolina , GASTAMINZA LANDART, Pablo , GARAIGORTA DE DIOS, Urtzi
IPC分类号： A61P31/14 , A61K31/47 , C07D215/52
摘要： The present invention relates to new derivatives of 2-phenyl-quinoline-4-carboxylic acid or pharmaceutically acceptable salt thereof and to combination of said compounds with other active ingredients, for use in the treatment and/or prevention of viral infections by virus from the family Coronaviridae, to the use of said compound or its combinations in the manufacture of a medicament for the treatment or prevention of said diseases and to a method of treating and/or preventing said diseases by administration of said compound or its combinations.

2. 发明公开

EP3728192A1 NOVEL QUINOLINE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS DISEASE 审中-公开
公开(公告)号：EP3728192A1
公开(公告)日：2020-10-28
申请号：EP18826249.7
申请日：2018-12-14
申请人： F. Hoffmann-La Roche AG
发明人： FENG, Song , QIU, Zongxing , WU, Guolong , CHEN, Dongdong , LI, Chao
IPC分类号： C07D215/18 , C07D215/233 , C07D215/52 , A61P31/12 , A61K31/47

3. 发明公开

EP3191452A1 SUBSTITUIERTE N,2-DIARYLCHINOLIN-4-CARBOXAMIDE UND IHRE ANTI-INFLAMMATORISCHE VERWENDUNG 审中-公开
标题翻译： SUBSTITUIERTE N，2-DIARYLCHINOLIN-4-CARBOXAMIDE和IHRE抗炎药物 - 维生素E
公开(公告)号：EP3191452A1
公开(公告)日：2017-07-19
申请号：EP15757299.1
申请日：2015-09-07
申请人： Bayer Pharma Aktiengesellschaft
发明人： BECK, Hartmut , THALER, Tobias , KAST, Raimund , MEIBOM, Daniel , MEININGHAUS, Mark , TERJUNG, Carsten , DELBECK, Martina , LUSTIG, Klemens , MUENSTER, Uwe , OLENIK, Britta
IPC分类号： C07D215/52 , C07D215/60 , C07D401/12 , A61K31/47 , A61P11/00 , A61P37/00
CPC分类号： C07D215/52 , C07D215/60 , C07D401/04 , C07D401/12
摘要： The invention relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to methods for producing the same, to the use thereof either alone or in combination in the treatment and/or prevention of diseases and to their use for producing drugs for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of fibrotic and inflammatory diseases.
摘要翻译：本发明涉及新的取代的N，2-二芳基喹啉-4-甲酰胺衍生物，其制备方法，其单独或组合用于治疗和/或预防疾病及其用于制备用于治疗和/或预防疾病，特别是用于治疗和/或预防纤维化和炎性疾病。

4. 发明授权

EP1968944B1 ALKYLSULPHONAMIDE QUINOLINES 有权
标题翻译：烷基磺酰胺喹啉
公开(公告)号：EP1968944B1
公开(公告)日：2016-04-20
申请号：EP06835833.2
申请日：2006-12-11
申请人： AstraZeneca AB
发明人： SIMPSON, Thomas , KANG, James , ALBERT, Jeffrey , ALHAMBRA, Cristobal , KOETHER, Gerard , WOODS, James , LI, Yan
IPC分类号： C07D215/52 , A61K31/47 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P3/04 , A61P35/00
CPC分类号： C07D215/38 , C07D215/14 , C07D215/52

5. 发明授权

EP1928835B1 ALKYL SULFOXIDE QUINOLINES AS NK-3 RECEPTOR LIGANDS 有权
标题翻译： ALKYLSULFOXIDCHINOLINE AS NK-3受体配体
公开(公告)号：EP1928835B1
公开(公告)日：2011-04-20
申请号：EP06784189.0
申请日：2006-09-19
申请人： AstraZeneca AB
发明人： ALBERT, Jeffrey, S. , KOETHER, Gerard, M. , ALHAMBRA, Cristobal , KANG, James , SIMPSON, Thomas, R. , WOODS, James , LI, Yan
IPC分类号： C07D215/52 , A61K31/47 , A61K31/4709 , A61P11/00 , A61P25/00 , C07D401/12
CPC分类号： C07D215/52 , C07D401/12
摘要： Compounds of Formula (I) wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

6. 发明公开

EP1968968A1 COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS 审中-公开
标题翻译：组合物和方法进行调制控制的离子通道
公开(公告)号：EP1968968A1
公开(公告)日：2008-09-17
申请号：EP06840532.3
申请日：2006-12-21
申请人： PainCeptor Pharma Corp.
发明人： VOHRA, Rahul , BABINSKI, Kazimierz , BROCHU, Jean-Louis , NTIRAMPEBURA, Deogratias , WEI, Chang-Qing , ZAMBONI, Robert, Joseph , REAYI, Ayub, A.
IPC分类号： C07D401/12 , A61K31/47 , A61K31/496 , A61K31/517 , A61K31/551 , A61P25/00 , A61P29/00 , C07D215/52 , C07D239/74 , C07D239/88 , C07D239/91 , C07D239/94 , C07D401/04 , C07D401/06 , C07D401/14
CPC分类号： C07D239/91 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/551 , C07D215/233 , C07D215/44 , C07D215/46 , C07D215/52 , C07D239/94 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Disclosed are quinoline and quinazoline compounds which modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include quinoline or quinazoline derivatives substituted at the 4- position via N(H), C(O) or O moieties.

7. 发明公开

EP1812398A1 COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：和作业LINKS AT NK3受体及其应用在医学
公开(公告)号：EP1812398A1
公开(公告)日：2007-08-01
申请号：EP05807869.2
申请日：2005-11-10
申请人： SmithKline Beecham Corporation
发明人： SMITH, Paul William, GlaxoSmithKline , WYMAN, Paul Adrian, GlaxoSmithKline
IPC分类号： C07D215/52 , A61K31/47 , A61P25/18 , A61P25/22 , A61P25/24
CPC分类号： C07D401/12 , C07D215/52 , C07D409/14
摘要： The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R2 is C1-6alkyl, C3-6cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R3 is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxyC1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-6alkyl; R5 is hydrogen; or R5 and R3, together with the nterconnecting atoms, form a 4, 5 or 6 membered ring; R6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and heir use as medicaments particularly in treating disorders of the Central Nervous System (CNS).

8. 发明公开

EP1809606A1 COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：在NK3受体上具有活性的化合物及其在医学上的用途
公开(公告)号：EP1809606A1
公开(公告)日：2007-07-25
申请号：EP05802078.5
申请日：2005-11-10
申请人： SmithKline Beecham Corporation
发明人： BRADLEY, Daniel Marcus, GlaxoSmithKline , PORTER, Roderick Alan, GlaxoSmithKline , SMITH, Paul William, GlaxoSmithKline , STEAD, Rachel Elizabeth Anne, GlaxoSmithKline , VONG, Antonio Kuok Keong, GlaxoSmithKline
IPC分类号： C07D215/52 , A61K31/47 , A61P25/18 , A61P25/24
CPC分类号： C07D409/04 , C07D215/52
摘要： The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R2 is C1-6alkyl or C3-6cycloalkyl; n is 1 or 2; R3 is hydrogen, C1-6alkyl or C3-6cycloalkyl; X is -(C=O)- or -SO2-; R4 is C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6haloalkoxy, amino, monoC1-6alkylamino or diC1-6alkylamino, or R4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C1-6alkyl, C1-6haloalkyl, C1-6alkoxy or C1-6haloalkoxy; R5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK3 receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明还涉及式（I）化合物，其药学上可接受的盐，溶剂合物或前药：其中R 1为苯基或环己基，其任一个任选被1,2或3个卤原子取代，所述卤原子可以相同或不同; R2是C1-6烷基或C3-6环烷基; n是1或2; R3是氢，C1-6烷基或C3-6环烷基; X是 - （C = O） - 或-SO 2 - ; R 4是C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6卤代烷氧基，氨基，单C 1-6烷基氨基或二C 1-6烷基氨基，或者R 4是杂环基或碳环基，或更多卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或C 1-6卤代烷氧基; R5为苯基或噻吩基，其任一个任选被1,2或3个卤素原子取代; y是0,1或2; 其中当y是1或2时，Y是卤素原子，并且其中当y是2时，卤素原子可以相同或不同。还公开了所述化合物在治疗由NK3受体活化介导的疾病和病症中的用途，含有所述衍生物的组合物及其制备方法。

9. 发明授权

EP1131294B1 QUINOLINE DERIVATIVES AS NK-2 AND NK-3 RECEPTOR LIGANDS 有权
标题翻译：喹啉，NK-2和NK-3受体配体
公开(公告)号：EP1131294B1
公开(公告)日：2006-12-20
申请号：EP99959340.3
申请日：1999-11-22
申请人： GlaxoSmithKline S.p.A. , Laboratoire Glaxosmithkline S.A.S.
发明人： FARINA, Carlo SmithKline Beecham S.p.A. , GIARDINA, Giuseppe SmithKline Beecham S.p.A. , GRUGNI, Mario SmithKline Beecham S.p.A. , NADLER, Guy M. M. G. SmithKline Beecham Lab. Phar. , RAVEGLIA, Luca Francesco SmithKline Beecham S.p.A.
IPC分类号： C07D215/52 , A61K31/4725 , C07D401/06 , A61K31/4709 , A61P25/00 , A61P11/00 , A61K31/47
CPC分类号： C07D401/06 , C07D215/52 , C07D401/14
摘要： A compound, or a solvate or a salt thereof, of formula (I), wherein R is linear or branched alkyl; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety -(CH2)n-NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 or Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or alkyl or R4 and R together with the carbon atom to which they are attached form an optionally substituted C3-12 cycloalkyl group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds as NK-2 or NK-3 receptor ligands.

10. 发明授权

EP0940391B1 Quinoline derivatives as tachykinin NK3 receptor antagonists 失效
标题翻译：喹啉衍生物作为速激肽NK 3受体拮抗剂
公开(公告)号：EP0940391B1
公开(公告)日：2004-08-18
申请号：EP98204483.6
申请日：1995-05-23
申请人： GlaxoSmithKline S.p.A.
发明人： Farina, Carlo , Giardina, Giuseppe Arnaldo Maria , Grugni, Mario , Raveglia, Luca Francesco
IPC分类号： C07D215/52 , A61K31/47 , C07D409/04 , C07D405/04 , C07D401/04 , C07D409/12 , C07D221/18 , C07D417/04 , C07D401/12 , C07D405/12
CPC分类号： C04B35/632 , A61K31/00 , A61K31/4709 , C07D215/52 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D417/04

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