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1. 发明申请

WO1992012158A1 CYCLIC KETAL DERIVATIVES 审中-公开
标题翻译：循环牙膏衍生物
公开(公告)号：WO1992012158A1
公开(公告)日：1992-07-23
申请号：PCT/EP1992000016
申请日：1992-01-05
申请人： GLAXO GROUP LIMITED , 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
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Compounds are described of formula (Ia), (Ib), wherein R represents a hydrogen atom, a hydroxyl group or a group selected from -OCOCH=CHCH(CH3)(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 represents a hydroxyl group, a group -OCOR or a group -OCO2R (where R is a group selected from C1-8alkyl, aryl, arylC1-4alkyl and C3-8cycloalkyl); R represents a group selected from (a) (where R is a hydrogen atom or an acetyl group), -C(CH3)=CHCH(CH2R )CH2Ph (where R is a hydrogen or a hydroxyl group), -C(CH2OH)=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 , R and R 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.
摘要翻译：化合物描述为式（Ia），（Ib），其中R 1表示氢原子，羟基或选自-OCOCH = CHCH（CH 3）（CH 2）3 CH 3，-OCOCH = CHC（CH 3） = CHCH（CH3）CH2CH3或-OCO-X-CH2CH（CH3）CH2CH3 [其中X为-CH = CHCH（CH3） - ， - CH2CH（OH）CH（CH3） - ， - CH = CHC（OH）） - ，-CH 2 CH（OH）CH 2 - 或-CH 2 CH 2 CH（CH 3） - ]; R 2表示羟基，-OCOR 7基团或-OCO 2 R 7基团（其中R 7是选自C 1-8烷基，芳基，芳基C 1-4烷基和C 3-8环烷基的基团）; R 3表示选自（a）（其中R 8为氢原子或乙酰基），-C（CH 3）= CHCH（CH 2 R 9）CH 2 Ph（其中R 9为氢或羟基），-C（CH2OH）= CHCH（CH3）CH2Ph，-C（= CH2）CH（OH）CH（CH2OH）CH2Ph，-C（= CH2）CH（NHCOCH3）CH（CH3），-C（CH 2 NHCOCH 3）= CHCH（CH 3）CH 2 Ph和（b）; R 4，R 5和R 6各自独立地表示氢原子或甲基; 及其盐。这些化合物抑制角鲨烯合成酶和/或用于制备抑制酶角鲨烯合酶的化合物的中间体。本发明的化合物可以配制用于各种病症，其中动物血浆中胆固醇水平的降低将是有益的并且用于抵抗动物中的真菌感染。

2. 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。

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

WO2008138876A1 PYRAZOLE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的吡唑衍生物
公开(公告)号：WO2008138876A1
公开(公告)日：2008-11-20
申请号：PCT/EP2008/055724
申请日：2008-05-08
申请人： GLAXO GROUP LIMITED , BESWICK, Paul John , CHAMBERS, Laura Jane , CHESSELL, Iain Patrick , DAVIES, David John , DEMONT, Emmanuel Hubert , GLEAVE, Robert James , LIVERMORE, David George Hubert , THEOBALD, Pamela Joan , VIMAL, Mythily , WALTER, Daryl Simon
发明人： BESWICK, Paul John , CHAMBERS, Laura Jane , CHESSELL, Iain Patrick , DAVIES, David John , DEMONT, Emmanuel Hubert , GLEAVE, Robert James , LIVERMORE, David George Hubert , THEOBALD, Pamela Joan , VIMAL, Mythily , WALTER, Daryl Simon
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/12 , C07D417/04 , C07D417/06 , C07D471/08
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders / diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：式（I）的吡唑衍生物或其盐调节P2X7受体功能，并且能够拮抗ATP在P2X7受体（P2X7受体）拮抗剂）。本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

5. 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。

6. 发明申请

WO2008020055A1 NOVEL ISOINDOL DERIVATIVES AS EP4 RECEPTOR AGONISTS 审中-公开
标题翻译：新的ISOINDOL衍生物作为EP4受体激动剂
公开(公告)号：WO2008020055A1
公开(公告)日：2008-02-21
申请号：PCT/EP2007/058514
申请日：2007-08-16
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard Martin Paul , HEALY, Mark Patrick , LIVERMORE, David George , PRICE, Helen Susanne , SWARBRICK, Martin Edward
发明人： GIBLIN, Gerard Martin Paul , HEALY, Mark Patrick , LIVERMORE, David George , PRICE, Helen Susanne , SWARBRICK, Martin Edward
IPC分类号： C07D209/46 , C07D209/48 , A61K31/4035 , A61P25/00
CPC分类号： C07D209/46 , C07D209/48
摘要： A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R 1 , R 2 , R 3 , R 4 and R 5 , X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物，其中R 1，R 2，R 3，R 3， 4和R 5，X和Y如说明书中所定义; 制备这种化合物的方法; 包含这些化合物的药物组合物; 并在药物中使用这些化合物。

7. 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。

8. 发明申请

WO2005077926A3 BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES USEFUL FOR THE TREATMENT OF CARDIOVASCULAR DISEASE 审中-公开
公开(公告)号：WO2005077926A3
公开(公告)日：2005-08-25
申请号：PCT/EP2005/001540
申请日：2005-02-10
申请人： SMITHKLINE BEECHAM CORPORATION , HARLING, John, David , LAMBETH, Paul, Francis , LIVERMORE, David, George
发明人： HARLING, John, David , LAMBETH, Paul, Francis , LIVERMORE, David, George
IPC分类号： C07D333/54
摘要： A compound of formula (I) and pharmaceutically acceptable salts and solvates and hydrolysable esters thereof, where X, X 1 , X 2 , X 3 , X 4 and R, R 2 , R 3 , R 4 are defined as in claim 1. These compounds are activators of the hPPAR receptors and are useful for the treatment of cardiovascular disease.

9. 发明申请

WO2005077926A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2005077926A2
公开(公告)日：2005-08-25
申请号：PCT/EP2005001540
申请日：2005-02-10
申请人： SMITHKLINE BEECHAM CORP , HARLING JOHN DAVID , LAMBETH PAUL FRANCIS , LIVERMORE DAVID GEORGE
发明人： HARLING JOHN DAVID , LAMBETH PAUL FRANCIS , LIVERMORE DAVID GEORGE
IPC分类号： C07D307/79 , C07D307/80 , C07D333/54 , C07D333/56 , C07D417/12 , C07D307/00
CPC分类号： C07D307/79 , C07D307/80 , C07D333/54 , C07D333/56 , C07D417/12
摘要： A compound of formula (I) and pharmaceutically acceptable salts and solvates and hydrolysable esters thereof.
摘要翻译：式（I）的化合物及其药学上可接受的盐和溶剂合物及其可水解的酯。

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