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1. 发明申请

WO2007039219A1 QUINOLINE COMPOUNDS CAPABLE OF BINDING THE CB2 AND/OR THE 5-HT6 RECEPTOR 审中-公开
标题翻译：可结合CB2和/或5-HT6受体的喹啉化合物
公开(公告)号：WO2007039219A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009416
申请日：2006-09-26
申请人： GLAXO GROUP LIMITED , AHMED, Mahmood , GIBLIN, Gerard, Martin, Paul , JOHNSON, Christopher, Norbert , LIVERMORE, David, George, Hubert , MILLER, Neil, Derek , MOSS, Stephen, Frederick , WITTY, David, R
发明人： AHMED, Mahmood , GIBLIN, Gerard, Martin, Paul , JOHNSON, Christopher, Norbert , LIVERMORE, David, George, Hubert , MILLER, Neil, Derek , MOSS, Stephen, Frederick , WITTY, David, R
IPC分类号： C07D401/06 , C07D215/36 , C07D491/10 , A61K31/4709 , A61P25/00
CPC分类号： C07D491/10 , C07D215/36 , C07D401/06
摘要： The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT 6 receptor and/or are capable of selectively modulating the cannabinoid 2 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.
摘要翻译：本发明涉及新颖的喹啉衍生物，例如式（I）化合物，其具有5-HT 6受体的拮抗剂效能和/或能够选择性调节大麻素2受体和使用的这些化合物或其药物组合物用于治疗CNS障碍。

2. 发明申请

WO2007039220A1 NOVEL QUINOLINE COMPOUNDS CAPABLE OF BINDING AT THE CB2 RECEPTOR 审中-公开
标题翻译：可以在CB2受体上结合的新型喹啉化合物
公开(公告)号：WO2007039220A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009417
申请日：2006-09-26
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , LIVERMORE, David, George, Hubert
发明人： GIBLIN, Gerard, Martin, Paul , LIVERMORE, David, George, Hubert
IPC分类号： C07D215/40 , C07D401/12 , C07D405/12 , A61K31/4704 , A61P25/28
CPC分类号： C07D405/12 , C07D215/40 , C07D401/12
摘要： The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess are capable of selectively modulating the cannabinoid 2 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.
摘要翻译：本发明涉及具有能够选择性调节大麻素2受体的式（I）化合物和这些化合物或其药物组合物在治疗CNS障碍中的用途的新型喹啉衍生物。

3. 发明申请

WO2003053443A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2003053443A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014823
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
发明人： BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
IPC分类号： A61K31/495
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I)and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要翻译：一种治疗或预防通过催产素作用介导的疾病或病症的方法，其包括向有需要的哺乳动物施用有效量的式I化合物和/或其生理上可接受的衍生物，其中所述取代基具有给定的含义在说明中。公开了式I的新化合物及其制备方法。

4. 发明申请

WO2008116814A1 PYRROLE AND ISOINDOLE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译： PYRROLE和ISOINDOLE CARBOXAMIDE衍生物作为P2X7调节剂
公开(公告)号：WO2008116814A1
公开(公告)日：2008-10-02
申请号：PCT/EP2008/053343
申请日：2008-03-20
申请人： GLAXO GROUP LIMITED , GLEAVE, Robert, James , LIVERMORE, David, George, Hubert , WALTER, Daryl, Simon
发明人： GLEAVE, Robert, James , LIVERMORE, David, George, Hubert , WALTER, Daryl, Simon
IPC分类号： C07D207/38 , C07D209/46 , A61K31/4015 , A61K31/4035 , A61P29/00 , A61P25/28
CPC分类号： C07D207/38 , C07D209/46
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R 2 represents hydrogen, halogen, C 1-6 alkyl, C 6-10 arylmethyl-, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkylmethyl-; and any of said C 1-6 alkyl, C 6-10 arylmethyl-, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R 3 represents hydrogen, fluorine or methyl; or R 2 and R 3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl and C 2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation or neurodegeneration.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：其中：R 2表示氢，卤素，C 1-6烷基，C 1〜 C 3-6亚芳基甲基 - ，C 2-6亚烯基，C 2-6亚炔基或C 3-6环烷基甲基 - ; 和任何所述C 1-6烷基，C 6-10-10芳基甲基 - ，C 2-6 - 烯基，C 2 - 6个炔基或C 3-6环烷基甲基 - 任选被1,2或3个卤素原子取代; R 3表示氢，氟或甲基; 或R 2和R 3与它们所连接的碳原子一起形成任选被1,2或3个取代基取代的苯环，其可以相同或不同的，选自C 1-6烷基，C 2-6亚烯基和C 2-6亚炔基。化合物或盐调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。本发明还提供了这些化合物或其盐或其药物组合物在治疗由P2X7受体介导的病症中的用途，例如疼痛，炎症或神经变性。

5. 发明授权

EP1928833B1 NOVEL QUINOLINE COMPOUNDS CAPABLE OF BINDING AT THE CB2 RECEPTOR 有权
标题翻译： NEW喹啉化合物要能够约束被CB 2受体结合
公开(公告)号：EP1928833B1
公开(公告)日：2009-02-18
申请号：EP06792301.1
申请日：2006-09-26
申请人： GLAXO GROUP LIMITED
发明人： GIBLIN, Gerard, Martin, Paul , LIVERMORE, David, George, Hubert
IPC分类号： C07D215/40 , C07D401/12 , C07D405/12 , A61K31/4704 , A61P25/28
CPC分类号： C07D405/12 , C07D215/40 , C07D401/12
摘要： The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess are capable of selectively modulating the cannabinoid 2 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.

6. 发明授权

EP1458393B1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 有权
标题翻译：取代，如哌嗪催产素拮抗剂
公开(公告)号：EP1458393B1
公开(公告)日：2008-06-25
申请号：EP02799077.9
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED
发明人： BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
IPC分类号： A61K31/495 , C07D241/08 , A61P15/06 , C07D401/08 , C07D401/12 , C07D417/12 , C07D403/12 , C07D403/08 , C07D405/14 , C07D417/08 , C07D403/06 , C07D405/06 , C07D417/06 , C07D413/06 , C07D409/06 , C07D401/06 , A61K31/496
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I)and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.

7. 发明公开

EP1458393A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 有权
标题翻译：取代，如哌嗪催产素拮抗剂
公开(公告)号：EP1458393A1
公开(公告)日：2004-09-22
申请号：EP02799077.9
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED
发明人： BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
IPC分类号： A61K31/495 , C07D241/08 , A61P15/06 , C07D401/08 , C07D401/12 , C07D417/12 , C07D403/12 , C07D403/08 , C07D405/14 , C07D417/08 , C07D403/06 , C07D405/06 , C07D417/06 , C07D413/06 , C07D409/06 , C07D401/06 , A61K31/496
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I)and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.

8. 发明公开

EP0639194A1 CYCLIC KETAL DERIVATIVES 失效
标题翻译：循环缩酮。
公开(公告)号：EP0639194A1
公开(公告)日：1995-02-22
申请号：EP92901579.0
申请日：1992-01-05
申请人： GLAXO GROUP LIMITED
发明人： SIDEBOTTOM, Philip, James , LESTER, Michael, George , PROCOPIOU, Panayiotis, Alexandrou , WATSON, Nigel, Stephen , BIONDI, Stefano , RAMSAY, Michael, Vincent, John , LIVERMORE, David, George, Hubert , ROSS, Barry, Clive Glaxo Group Research Limited
IPC分类号： A61K31 , A61P3 , C07D493
CPC分类号： C07D493/08
摘要： Compounds are described of formula (Ia), (Ib), wherein R1 represents a hydrogen atom, a hydroxyl group or a group selected from -OCOCH=CHCH(CH¿3?)(CH2)3CH3, -OCOCH=CHC(CH3)=CHCH(CH3)CH2CH3 or -OCO-X-CH2CH(CH3)CH2CH3 [where X is -CH=CHCH(CH3)-, -CH2CH(OH)CH(CH3)-, -CH=CHC(OH)(CH3)-, -CH2CH(OH)CH2- or -CH2CH2CH(CH3)-]; R?2¿ represents a hydroxyl group, a group -OCOR7 or a group -OCO¿2R?7 (where R7 is a group selected from C¿1-8?alkyl, aryl, arylC1-4alkyl and C3-8cycloalkyl); R?3¿ represents a group selected from (a) (where R8 is a hydrogen atom or an acetyl group), -C(CH¿3?)=CHCH(CH2R?9)CH¿2Ph (where R9 is a hydrogen or a hydroxyl group), -C(CH¿2?OH)=CHCH(CH3)CH2Ph, -C(=CH2)CH(OH)CH(CH2OH)CH2Ph, -C(=CH2)CH(NHCOCH3)CH(CH3)CH2Ph, -C(CH2NHCOCH3)=CHCH(CH3)CH2Ph and (b); R?4, R5 and R6¿ may each independently represent a hydrogen atom or a methyl group; and salts thereof. These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

9. 发明公开

EP2142502A1 PYRROLE AND ISOINDOLE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的吡咯和异吲哚羧酰胺衍生物
公开(公告)号：EP2142502A1
公开(公告)日：2010-01-13
申请号：EP08718063.4
申请日：2008-03-20
申请人： Glaxo Group Limited
发明人： GLEAVE, Robert, James , LIVERMORE, David, George, Hubert , WALTER, Daryl, Simon
IPC分类号： C07D207/38 , C07D209/46 , A61K31/4015 , A61K31/4035 , A61P29/00 , A61P25/28
CPC分类号： C07D207/38 , C07D209/46
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl-; and any of said C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R3 represents hydrogen, fluorine or methyl; or R2 and R3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation or neurodegeneration.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：其中：R 2表示氢，卤素，C 1-6烷基，C 6-10芳基甲基 - ，C 2-6烯基，C 2-6炔基或C 3-6 - 6环烷基甲基 - ; 并且所述C 1-6烷基，C 6-10芳基甲基 - ，C 2-6烯基，C 2-6炔基或C 3-6环烷基甲基 - 中的任一个任选地被1,2或3个卤素原子取代; 和R3代表氢，氟或甲基; 或者R 2和R 3与它们所连接的碳原子一起形成任选被1,2或3个取代基取代的苯环，所述取代基可以相同或不同，选自C 1-6烷基，C 2-6 烯基和C 2-6炔基。这些化合物或盐调节P2X7受体功能，并且能够拮抗ATP在P2X7受体上的作用。本发明还提供了这些化合物或盐或其药物组合物在治疗由P2X 7受体介导的病症例如疼痛，炎症或神经变性中的用途。

10. 发明公开

EP1928856A1 QUINOLINE COMPOUNDS CAPABLE OF BINDING THE CB2 AND/OR THE 5-HT6 RECEPTOR 审中-公开
标题翻译：喹啉化合物要能够约束被CB 2和/或5-HT6受体结合
公开(公告)号：EP1928856A1
公开(公告)日：2008-06-11
申请号：EP06792300.3
申请日：2006-09-26
申请人： GLAXO GROUP LIMITED
发明人： AHMED, Mahmood , GIBLIN, Gerard, Martin, Paul , JOHNSON, Christopher, Norbert , LIVERMORE, David, George, Hubert , MILLER, Neil, Derek , MOSS, Stephen, Frederick , WITTY, David, R
IPC分类号： C07D401/06 , C07D215/36 , C07D491/10 , A61K31/4709 , A61P25/00
CPC分类号： C07D491/10 , C07D215/36 , C07D401/06
摘要： The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT6 receptor and/or are capable of selectively modulating the cannabinoid 2 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.

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