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1. 发明申请

US20110251169A1 Arylethynyl derivatives 有权
标题翻译：甲基乙炔基衍生物
公开(公告)号：US20110251169A1
公开(公告)日：2011-10-13
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： A61K31/397 , A61K31/501 , C07D417/04 , A61K31/541 , C07D413/04 , A61P25/28 , A61K31/5355 , A61K31/506 , C07D401/04 , A61K31/4439 , C07D401/14 , A61K31/444 , C07D403/04 , A61K31/5377
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。

2. 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。

3. 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。

4. 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。

5. 发明申请

US20120277243A1 PYRAZOLIDIN-3-ONE DERIVATIVES 有权
标题翻译：吡唑啉-3-酮衍生物
公开(公告)号：US20120277243A1
公开(公告)日：2012-11-01
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： A61K31/4439 , A61P25/00 , A61P25/28 , C07D401/04 , A61K31/501 , A61K31/506 , C07D487/04 , C07D401/14 , A61K31/444 , A61P25/18 , C07D403/04
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）。

6. 发明申请

US20120270852A1 PHENYL OR PYRIDINYL-ETHYNYL DERIVATIVES 有权
标题翻译：苯基或吡啶基乙炔衍生物
公开(公告)号：US20120270852A1
公开(公告)日：2012-10-25
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： A61K31/506 , A61K31/44 , C07D401/06 , A61K31/444 , C07D239/28 , A61K31/505 , C07D405/12 , A61K31/4427 , C07D413/06 , A61K31/5377 , A61K31/4545 , C07D403/06 , C07D213/85 , A61P25/00 , A61P25/18 , A61P35/00 , C07D213/81
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）。

7. 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）。

8. 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）。

9. 发明授权

US5420018A Device for the preservation and analysis of samples, in particular for bacteriological examinations, isolation of micro-organisms and development of isolation colonies, and a method for seeding the samples onto a culture medium in said device 失效
标题翻译：用于保存和分析样品的装置，特别是用于细菌检查，分离微生物和分离菌落的开发，以及将样品接种到所述装置中的培养基上的方法
公开(公告)号：US5420018A
公开(公告)日：1995-05-30
申请号：US85195
申请日：1993-06-29
申请人： Antonio Ricci
发明人： Antonio Ricci
IPC分类号： C12M1/24 , C12M1/28 , C12M1/30 , C12M1/34 , C12Q1/04 , C12Q1/24
CPC分类号： C12M23/44 , C12M23/22 , C12M23/38
摘要： A device for the preservation and analysis of samples, comprising a first container (1) and a second container (5) for containing a sample and a maintaining or culture liquid; said first container comprises at least two mutually communicating chambers (2, 3), of which a first chamber (2) comprises an element (7) carrying a culture medium and a distributor member (19), and the second chamber (3) comprises on its base (13) at least one element (14) projecting into the chamber itself and able to break at least one weakened portion (26) of the base (SA) of said second container (5), this latter being insertable into said second chamber (3).The method for seeding onto the face of the element (7) comprises distribution along paths extending substantially in mutually perpendicular directions which are preferably parallel and, respectively, orthogonal to the axis of the element (7).
摘要翻译：一种用于保存和分析样品的装置，包括用于容纳样品和维持或培养液体的第一容器（1）和第二容器（5）; 所述第一容器包括至少两个相互连通的腔室（2,3），其中第一腔室（2）包括承载培养基的元件（7）和分配器构件（19），并且所述第二腔室（3）包括在其底部（13）上突出到腔室本身中的至少一个元件（14）能够破坏所述第二容器（5）的底座（SA）的至少一个弱化部分（26），后者可插入所述第二室（3）。用于接种在元件（7）的表面上的方法包括基本上沿彼此垂直的方向延伸的路径的分布，其优选地平行并且分别地垂直于元件（7）的轴线。

10. 发明授权

US4148609A Method for measuring antistreptolysin concentration in blood 失效
标题翻译：血液中抗血浆溶血素浓度的测定方法
公开(公告)号：US4148609A
公开(公告)日：1979-04-10
申请号：US747048
申请日：1976-12-02
申请人： Antonio Ricci
发明人： Antonio Ricci
IPC分类号： G01N33/555 , G01N33/569 , G01N33/16
CPC分类号： G01N33/56944 , G01N33/555 , Y10S436/815
摘要： A method for measuring the antistreptolysin concentration in a human blood sample by adding a solution of oxidized 0-streptolysin to the blood sample (diluted), incubating, reacting with a reducing solution, incubating and relating the resulting hemolysis to the antistreptolysin concentration.
摘要翻译：通过向血液样品中添加氧化的O-链球菌溶血素溶液（稀释），温育，与还原溶液反应，孵育并使所得溶血与抗溶血素溶解浓度相关联，来测量人血液样品中的抗溶血素浓度的方法。

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