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11. 发明授权

US5955495A Method of treating diseases of the CNS 失效
标题翻译：治疗CNS疾病的方法
公开(公告)号：US5955495A
公开(公告)日：1999-09-21
申请号：US837140
申请日：1997-04-14
申请人： Michael Bos , Heinz Stadler , Jurgen Wichmann
发明人： Michael Bos , Heinz Stadler , Jurgen Wichmann
IPC分类号： A61K31/34 , A61K31/343 , A61P25/00 , A61P25/20 , A61P25/28 , C07D307/85 , C07D307/86
CPC分类号： C07D307/85 , A61K31/343 , C07D307/86
摘要： The invention is concerned with the use of compounds of the general formula ##STR1## wherein R.sup.1 -R.sup.4 signify hydrogen, halogen, lower-alkyl, lower-alkoxy, aryl, benzyloxy, lower-alkoxy-lower-alkyl, lower-alkyl-sulphanyl, lower-alkyl-sulphanyl-lower-alkyl or R.sup.1 and R.sup.2 together signify the group --O--(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 --O-- andR.sup.5 signifies hydrogen or hydroxy,as well as their pharmaceutically acceptable salts in the control or prevention of illnesses or disorders of the central nervous system such as migraine, schizophrenia, anxiety states, sleep disorders, anorexia, Alzheimer's disease, addictions (alcohol, nicotine, benzodiazepine, cocaine, etc.), as well as disorders which result from damage to the head/brain or to the spinal column/bone marrow and, respectively, for the production of corresponding medicaments.
摘要翻译：本发明涉及以下通式的化合物的用途：其中R 1 -R 4表示氢，卤素，低级烷基，低级烷氧基，芳基，苄氧基，低级烷氧基 - 低级烷基，低级烷基 - 硫基，烷基 - 硫基 - 低级 - 烷基或R 1和R 2一起表示基团-O-（CH 2）2 - 或 - （CH 2）2 -O-，并且R 5表示氢或羟基，以及它们在对照中的药学上可接受的盐，预防偏头痛，精神分裂症，焦虑症，睡眠障碍，厌食症，阿尔茨海默病，成瘾症（酒精，尼古丁，苯二氮卓，可卡因等）的中枢神经系统疾病或病症，以及由于损伤引起的疾病头/脑或脊柱/骨髓，分别用于生产相应的药物。

12. 发明授权

US4577173A Electromagnetic relay and method for manufacturing such relay 失效
标题翻译：电磁继电器及其制造方法
公开(公告)号：US4577173A
公开(公告)日：1986-03-18
申请号：US659894
申请日：1984-10-11
申请人： Helmut Schedele , Josef Schweiger , Heinz Stadler
发明人： Helmut Schedele , Josef Schweiger , Heinz Stadler
IPC分类号： H01H49/00 , H01H50/02 , H01H50/04 , H01H50/18 , H01H50/44 , H01H51/22 , H01H51/24
CPC分类号： H01H49/00 , H01H50/023 , H01H51/2254 , H01H2009/0285 , H01H2050/446 , Y10T29/4902
摘要： A relay having a coil body 1 with a tongue-shaped armature mounted on the inside of the coil body and the armature is secured at one end 6a to a first coil flange 4 and its free end moveable between two pole plates 8 which are in the vicinity of the second coil flange 5. At the end where the armature 6 is fastened the coil flange 4 comprises a rim bead which together with the retaining webs 21 of the armature 6 form a planar seating surface for a sealing film 12 and at the other end of the coil flange 5 the two pole plates 8 together with spacing members of the coil body form a planar seating surface for a sealing film 9 and a good seal of the relay is obtained due to such simple structure while maintaining good magnetic coupling.
摘要翻译：具有线圈主体1的继电器，其具有安装在线圈体内部的舌状电枢和电枢，其一端6a固定到第一线圈凸缘4，并且其自由端可在两个极板8之间移动，在电枢6被紧固的端部处，线圈凸缘4包括边缘凸缘，其与电枢6的保持腹板21一起形成用于密封薄膜12的平面安置表面，并且在另一个线圈法兰5的端部，两个极板8与线圈体的间隔构件一起形成用于密封膜9的平坦的就座表面，并且由于这种简单的结构而获得良好的继电器密封，同时保持良好的磁耦合。

13. 发明授权

US4539540A Electromagnetic rotating armature relay 失效
标题翻译：电磁旋转电枢继电器
公开(公告)号：US4539540A
公开(公告)日：1985-09-03
申请号：US495648
申请日：1983-05-18
申请人： Rolf-Dieter Kimpel , Heinz Stadler , Alfred Heinzl
发明人： Rolf-Dieter Kimpel , Heinz Stadler , Alfred Heinzl
IPC分类号： H01H50/18 , H01H50/54 , H01H50/58
CPC分类号： H01H50/548
摘要： The rotating armature relay exhibits one or two ferromagnetic bars which are provided with an insulating covering in their central area. Contact springs are secured in the insulation covering, the contacting, free ends of said contact springs respectively interacting with cooperating contact elements anchored in a base body. As a result, a slide-free and, thus, low-friction actuation derives as, however, does relatively high friction at the contact locations, whereby contact impacts are suppressed and foreign layers are abraded from the contact surfaces.
摘要翻译：旋转电枢继电器显示一个或两个铁磁条，它们在其中心区域设有绝缘覆盖物。接触弹簧固定在绝缘覆盖层中，所述接触弹簧的接触自由端分别与锚定在基体中的协作接触元件相互作用。因此，无滑动且因此低摩擦力的致动来源于接触位置处的相对较高的摩擦力，从而抑制接触冲击并且从接触表面磨蚀外来层。

14. 发明授权

US4363426A Device for conveying and dispensing liquid media 失效
标题翻译：用于输送和分配液体介质的装置
公开(公告)号：US4363426A
公开(公告)日：1982-12-14
申请号：US194335
申请日：1980-10-06
申请人： Alfred Heinzl , Heinz Stadler
发明人： Alfred Heinzl , Heinz Stadler
IPC分类号： F04B13/00 , B01F15/04 , B29B7/60 , B67D7/64 , F04B13/02 , F04B53/12 , G01F11/04 , B67D5/46 , B67D5/52
CPC分类号： G01F11/04 , B01F15/0237 , B01F15/0462 , B29B7/603 , F04B13/02 , F04B53/129
摘要： A device for conveying and dispensing liquid media such as casting resin has at least one piston pump having a cylinder chamber which forms a seal for a piston therein which is connected via an input opening to a feed container for receiving a supply of liquid therefrom. The cylinder chamber has an output opening and the piston is tubular in form having wall perforations in the region of the input opening for admitting the liquid to the interior of the piston and has a valve at a discharging end thereof for exit of the liquid from the piston. A seal is thus formed by which the piston operates entirely surrounded by the liquid medium to be dispensed and external seals between the piston and the atmosphere are eliminated.
摘要翻译：用于输送和分配诸如铸塑树脂的液体介质的装置具有至少一个活塞泵，其具有气缸室，该气缸室形成用于其中的活塞的密封件，其经由输入开口连接到用于从其接收液体供应的进料容器。气缸室具有输出开口，并且活塞为管状形式，在输入开口的区域具有壁穿孔，用于将液体引入活塞的内部，并且在其排出端具有阀，用于将液体从活塞。因此形成密封件，通过该密封件，活塞完全由要分配的液体介质包围，并且消除了活塞和大气之间的外部密封。

15. 发明授权

US08487102B2 Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists 有权
标题翻译：吡唑并吡啶化合物作为双重NK1 / NK3受体拮抗剂
公开(公告)号：US08487102B2
公开(公告)日：2013-07-16
申请号：US13083636
申请日：2011-04-11
申请人： Philippe Jablonski , Matthias Nettekoven , Angelique Patiny-Adam , Hasane Ratni , Heinz Stadler
发明人： Philippe Jablonski , Matthias Nettekoven , Angelique Patiny-Adam , Hasane Ratni , Heinz Stadler
IPC分类号： C07D471/04
CPC分类号： C07D487/04
摘要： The present invention relates to a compound of formula I wherein R1, R2, R3, Ar, and n are as defined herein or to a pharmaceutically active acid addition salt. Compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
摘要翻译：本发明涉及其中R 1，R 2，R 3，Ar和n如本文所定义或与药学活性的酸加成盐的式I化合物。式I的化合物对NK1和NK3受体（双重NK1 / NK3受体拮抗剂）同时显示出高亲和力，可用于治疗精神分裂症。

16. 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）。

17. 发明申请

US20110178055A1 DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：双NK1 / NK3受体拮抗剂
公开(公告)号：US20110178055A1
公开(公告)日：2011-07-21
申请号：US13076891
申请日：2011-03-31
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/551 , A61K31/5377 , A61P25/18
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译：本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。本发明还提供具有式I的新化合物和制备本发明化合物的方法。

18. 发明申请

US20110152257A1 ETHYNYL COMPOUNDS USEFUL FOR TREATMENT OF CNS DISORDERS 有权
标题翻译：乙炔化合物可用于治疗中枢神经系统疾病
公开(公告)号：US20110152257A1
公开(公告)日：2011-06-23
申请号：US12964785
申请日：2010-12-10
申请人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindermann , Heinz Stadler , Eric Vieira
发明人： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindermann , Heinz Stadler , Eric Vieira
IPC分类号： A61K31/519 , C07D487/04 , C07D471/04 , A61K31/437 , A61K31/5377 , A61P25/18 , A61P25/16 , A61P25/00 , A61P25/24 , A61P25/04 , A61P25/30
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or 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) and they are therefore useful for the treatment of diseases related to this receptor.
摘要翻译：本发明涉及下式的乙炔基化合物，其中X，Y，Z和R 4如本文所定义，或其药学上可接受的盐或酸加成盐，涉及外消旋混合物或其相应的对映异构体和/或旋光异构体和/ 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）的正变构调节剂（PAM），因此它们可用于治疗与该受体有关的疾病。

19. 发明申请

US20100075954A1 SUBSTITUTED IMIDAZO[1,5-A][1,2,4]TRIAZOLO[1,5-D][1,4]BENZODIAZEPINE DERIVATIVES 失效
标题翻译：取代的咪唑并[1,5-A] [1,2,4]三唑并[1,5-D] [1,4]苯并恶嗪衍生物
公开(公告)号：US20100075954A1
公开(公告)日：2010-03-25
申请号：US12618802
申请日：2009-11-16
申请人： Henner Knust , Heinz Stadler , Andrew William Thomas
发明人： Henner Knust , Heinz Stadler , Andrew William Thomas
IPC分类号： A61K31/551 , C07D243/10 , A61P25/28
CPC分类号： A61K31/5517 , C07D487/14
摘要： The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.
摘要翻译：本发明涉及通过施用治疗有效量的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂治疗阿尔茨海默病的方法其中R 1，R 2和R 3如本文所定义，并且其药学上可接受的酸加成盐。本发明还提供新颖的式I-A化合物和含有它们的药物组合物。

20. 发明申请

US20090137806A1 DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：双NK1 / NK3受体拮抗剂
公开(公告)号：US20090137806A1
公开(公告)日：2009-05-28
申请号：US12361569
申请日：2009-01-29
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： C07D401/04 , C07D497/10
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译：本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。本发明还提供具有式I的新化合物和制备本发明化合物的方法。

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