专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US08957213B2 Ethynyl compounds 有权
公开(公告)号：US08957213B2
公开(公告)日：2015-02-17
申请号：US13452973
申请日：2012-04-23
申请人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Heinz Stadler , Eric Vieira
发明人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Heinz Stadler , Eric Vieira
IPC分类号： C07D401/04 , C07D401/14 , A61K31/4439 , A61K31/444 , C07D403/04
CPC分类号： C07D403/04 , A61K31/506 , C07D401/04 , C07D401/14 , Y02T10/7011
摘要： The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3′, R4, R4′, R5, R6, R6′, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.

42. 发明授权

US08772300B2 Phenyl or pyridinyl-ethynyl derivatives 有权
标题翻译：苯基或吡啶基 - 乙炔基衍生物
公开(公告)号：US08772300B2
公开(公告)日：2014-07-08
申请号：US13443911
申请日：2012-04-11
申请人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
发明人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D213/56 , C07D213/57 , C07D239/28 , C07D401/06 , C07D403/06 , C07D407/12 , C07D413/06
摘要： The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2′ are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′ together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4′ are each independently hydrogen or lower alkyl, or R4 and R4′ together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式I的乙炔基衍生物，其中Y是N或C-R3; R3是氢，甲基，卤素或腈; R1是苯基或吡啶基，其各自任选被卤素，低级烷基或低级烷氧基取代; R2 / R2'各自独立地为氢，被卤素取代的低级烷基或低级烷基，或R2和R2'与它们所连接的N-原子一起形成吗啉环，哌啶环或氮杂环丁烷环，其中每个未取代或取代的一个或多个选自低级烷氧基，卤素，羟基和甲基的取代基; R 4 / R 4'各自独立地为氢或低级烷基，或者R 4和R 4'一起形成C 3-5环烷基，四氢呋喃或氧杂环丁烷环; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。

43. 发明授权

US08648088B2 Ethynyl nitrogen containing heteroaryl pyrazolidin-3-one derivatives 有权
标题翻译：含炔基氮杂芳基吡唑烷-3-酮衍生物
公开(公告)号：US08648088B2
公开(公告)日：2014-02-11
申请号：US13454167
申请日：2012-04-24
申请人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
发明人： Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC分类号： C07D401/04 , A61K31/506 , C07D403/04 , A61K31/4439
CPC分类号： C07D401/04 , C07D403/04 , C07D487/04
摘要： The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3′, R4, and R4′ are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式I的乙炔基衍生物，其中G，X，R 1，R 2，R 3，R 3'，R 4和R 4'如本文所定义，或其药学上可接受的酸加成盐，涉及外消旋混合物或其相应的对映体和/或其光学异构体和/或立体异构体。式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。

44. 发明授权

US08420661B2 Arylethynyl derivatives 有权
标题翻译：甲基乙炔基衍生物
公开(公告)号：US08420661B2
公开(公告)日：2013-04-16
申请号：US13066044
申请日：2011-04-05
申请人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
发明人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC分类号： C07D211/00 , C07D213/00 , C07D215/00 , C07D217/00 , C07D219/00 , C07D221/00 , C07D211/68 , C07D211/80 , C07D213/02 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , A61K31/44 , A61K31/70
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D491/107 , C07D498/04
摘要： The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2′, R3, R3′, R4, R4′, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
摘要翻译：本发明涉及式I的乙炔基化合物，其中R 1，R 2，R 2'，R 3，R 3'，R 4，R 4'，U，V，W，Y，m和n如本文所定义，加成盐，与外消旋混合物或其相应的对映体和/或光学异构体和/或其立体异构体。式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。

45. 发明授权

US08389536B2 Positive allosteric modulators (PAM) 有权
标题翻译：正变构调节剂（PAM）
公开(公告)号：US08389536B2
公开(公告)日：2013-03-05
申请号：US12908014
申请日：2010-10-20
申请人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
发明人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC分类号： A61K31/506
CPC分类号： C07D213/74 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/505 , A61K31/506 , C07D213/64 , C07D239/34 , C07D239/42 , C07D401/06 , C07D405/12 , C07D413/06 , C07D493/08
摘要： The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4′, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
摘要翻译：本发明涉及式I的苯基乙炔基化合物，其中R 1，R 2，X，L，R 3，R 4，R 4'，R c和n如说明书和权利要求中所定义，并且与药学上可接受的酸加成盐相关，混合物或其相应的对映异构体和/或其光学异构体和/或立体异构体。式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。它们可用于治疗精神分裂症或认知疾病。

46. 发明申请

US20110015202A1 IMIDAZOLES 有权
公开(公告)号：US20110015202A1
公开(公告)日：2011-01-20
申请号：US12833017
申请日：2010-07-09
申请人： Georg Jaeschke , Lothar Lindemann , Eric Vieira , Juergen Wichmann
发明人： Georg Jaeschke , Lothar Lindemann , Eric Vieira , Juergen Wichmann
IPC分类号： A61K31/501 , C07D401/04 , A61K31/4439 , C07D401/14 , A61K31/444 , C07D403/04 , A61K31/497 , C07D403/14 , A61K31/506 , A61P25/28 , A61P29/00 , A61P25/18 , A61P25/08 , A61P25/24 , A61P25/14 , A61P25/30
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
摘要翻译：本发明涉及以下通式的咪唑衍生物：其中R 1，R 2，R 3和R 4如说明书中所定义及其药学上可接受的盐。式I化合物是代谢型谷氨酸受体拮抗剂。它们可用于治疗或预防mGluR5受体介导的疾病。

47. 发明授权

US08334287B2 Imidazoles 有权
标题翻译：咪唑
公开(公告)号：US08334287B2
公开(公告)日：2012-12-18
申请号：US12833017
申请日：2010-07-09
申请人： Georg Jaeschke , Lothar Lindemann , Eric Vieira , Juergen Wichmann
发明人： Georg Jaeschke , Lothar Lindemann , Eric Vieira , Juergen Wichmann
IPC分类号： A61K31/4965 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
摘要翻译：本发明涉及以下通式的咪唑衍生物：其中R 1，R 2，R 3和R 4如说明书中所定义及其药学上可接受的盐。式I化合物是代谢型谷氨酸受体拮抗剂。它们可用于治疗或预防mGluR5受体介导的疾病。

48. 发明授权

US07951824B2 4-aryl-pyridine-2-carboxyamide derivatives 有权
标题翻译： 4-芳基 - 吡啶-2-甲酰胺衍生物
公开(公告)号：US07951824B2
公开(公告)日：2011-05-31
申请号：US11699786
申请日：2007-01-30
申请人： Georg Jaeschke , Will Spooren , Eric Vieira
发明人： Georg Jaeschke , Will Spooren , Eric Vieira
IPC分类号： C07D401/12 , C07D213/81 , A61K31/443
CPC分类号： C07D417/12 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/14
摘要： The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in the specification herein.
摘要翻译：本发明涉及用作代谢型谷氨酸受体拮抗剂的式（I）的新型吡啶-2-甲酰胺衍生物：其中Y，Z，R 1，R 2和R 3如本说明书中所定义。

49. 发明申请

US20110098313A1 POSITIVE ALLOSTERIC MODULATORS (PAM) 有权
标题翻译：积极的独立调制器（PAM）
公开(公告)号：US20110098313A1
公开(公告)日：2011-04-28
申请号：US12908014
申请日：2010-10-20
申请人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
发明人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC分类号： A61K31/506 , C07D239/42 , A61K31/505 , C07D213/72 , A61K31/44 , A61K31/4433 , C07D405/12 , C07D239/04 , A61P25/00
CPC分类号： C07D213/74 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/505 , A61K31/506 , C07D213/64 , C07D239/34 , C07D239/42 , C07D401/06 , C07D405/12 , C07D413/06 , C07D493/08
摘要： The present invention relates to phenylethynyl compounds of formula I whereinR1, R2, X, L, R3, R4, R4′, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
摘要翻译：本发明涉及式I的苯基乙炔基化合物，其中R 1，R 2，X，L，R 3，R 4，R 4'，R c和n如说明书和权利要求中所定义，并且与药学上可接受的酸加成盐相关，混合物或其相应的对映异构体和/或其光学异构体和/或立体异构体。式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。它们可用于治疗精神分裂症或认知疾病。

50. 发明授权

US06462198B1 Carbamic acid derivatives 失效
公开(公告)号：US06462198B1
公开(公告)日：2002-10-08
申请号：US09545622
申请日：2000-04-10
申请人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
发明人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D41312
CPC分类号： C07D213/30 , C07C233/91 , C07C271/64 , C07C333/10 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/61 , C07D263/48 , C07D271/07 , C07D271/113 , C07D295/088 , C07D311/84 , C07D333/16 , C07D335/14 , C07D413/12
摘要： The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulas wherein R4 and R5 signifies hydrogen, lower alkyl, lower alkoxy, cyclohexyl, lower alkyl-cyclohexyl or trifluoromethyl, with the proviso that at least one of R4 or R5 has to be hydrogen; as well as to their pharmaceutically acceptable salts. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式