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51. 发明授权

US08293730B2 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]苯并二氮杂衍生物
公开(公告)号：US08293730B2
公开(公告)日：2012-10-23
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： A61P25/00 , A61K31/55 , C07D487/14
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。

52. 发明申请

US20110257402A1 PYRRAZOLOPYRIDINE COMPOUNDS AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：吡咯啉吡啶化合物作为NK1 / NK3受体拮抗剂
公开(公告)号：US20110257402A1
公开(公告)日：2011-10-20
申请号：US13083636
申请日：2011-04-11
申请人： Philippe Jablonski , Matthias Nettekoven , Angëlique Patiny-Adam , Hasane Ratni , Heinz Stadler
发明人： Philippe Jablonski , Matthias Nettekoven , Angëlique 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。

53. 发明授权

US06552088B2 Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US06552088B2
公开(公告)日：2003-04-22
申请号：US09886669
申请日：2001-06-21
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07C23300
CPC分类号： C07D295/155 , C07C217/54 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42
摘要： Biphenyl substituted amides with activity as antagonists of the neurokinin 1 (NK-1, substance P) receptor.
摘要翻译：具有作为神经激肽1（NK-1，物质P）受体的拮抗剂的活性的联苯取代的酰胺。

54. 发明授权

US06274588B1 4-phenyl-pyrimidine derivatives 失效
标题翻译： 4-苯基 - 嘧啶衍生物
公开(公告)号：US06274588B1
公开(公告)日：2001-08-14
申请号：US09575382
申请日：2000-05-22
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07D23924
CPC分类号： C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/48 , C07D401/04
摘要： The invention provides compounds of the formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be —CH═CH—CH═CH—, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′ are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; and n is 0-2; X is —C(O)N(R4″)— or —N(R4″)C(O)—; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.
摘要翻译：本发明提供的化合物，其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 1和R 2一起可以是-CH = CH-CH = CH-，其中R 1和R 2与两个碳环它们所连接的原子形成稠环; R3是卤素，三氟甲基，低级烷基或低级烷氧基; R4 / R4'各自独立地是氢或低级烷基; R5是低级烷基，低级烷氧基，氨基，苯基，羟基 - 低级烷基，氰基 - 低级烷基，氨基甲酰基 - 低级烷基，吡啶基，嘧啶基， - （CH2）n-哌嗪基，其任选被一个或两个低级烷基或羟基 - 低级烷基取代， - （CH 2） - （CH 2）n - 哌啶基， - （CH 2）n + 1-咪唑基，低级烷基 - 硫烷基，低级烷基磺酰基，苄基氨基，-NH-（CH 2）n + n + 1N（R4“）2，-O-（CH2）n + 1-吗啉基，-O-（CH2）n + 1-哌啶基或-O-（CH2）n + 1N（R4” 其中R4“是氢或低级烷基; 和n为0-2; X为-C（O）N（R4“） - 或-N（R4”）C（O） - ;以及其药学上可接受的酸加成盐。对NK-1受体具有良好的亲和性，因此可用于治疗与该受体有关的疾病。

55. 发明授权

US5732968A Apparatus for the longitudinal adjustment 失效
标题翻译：纵向调整装置
公开(公告)号：US5732968A
公开(公告)日：1998-03-31
申请号：US581535
申请日：1996-01-11
申请人： Helmut Wladar , Johann Zotter , Andreas Janisch , Karl Stritzl , Hubert Wuerthner , Franz Luschnig , Reinhold Wawra , Alois Himmetsberger , Heinz Stadler , Henry Freisinger
发明人： Helmut Wladar , Johann Zotter , Andreas Janisch , Karl Stritzl , Hubert Wuerthner , Franz Luschnig , Reinhold Wawra , Alois Himmetsberger , Heinz Stadler , Henry Freisinger
IPC分类号： A63C9/00 , A63C9/081
CPC分类号： A63C9/005
摘要： A longitudinal-adjusting device (1) for a ski-binding part (7) consists of a guide rail (2) fastened on a ski (3), on which an adjusting plate (5) is guided movably and lockably, which adjusting plate carries the ski-binding part (7). A locking part (10) is supported movably transversely with respect to the longitudinal direction of the ski in the adjusting plate (5), which locking part has locking teeth (12) on the underside, which teeth engage locking teeth (13) on the upper side of the guide rail (2). The locking part (10) is loaded by a spring (15) and has an operating member (18) with two surfaces (22, 23), which rest on a lateral section (21) of the adjusting plate (5).
摘要翻译： PCT No.PCT / EP95 / 01660 Sec。 371日期1996年1月11日 102（e）日期1996年1月11日PCT 1995年5月2日PCT PCT。 WO95 / 30459 PCT公开号日期：1995年11月16日用于滑雪装订部分（7）的纵向调节装置（1）由固定在滑雪板（3）上的导轨（2）组成，调节板（5）可在其上移动，可调节地，该调节板承载滑雪板结合部分（7）。锁定部分（10）在调节板（5）中相对于滑雪板的纵向可横向移动，该锁定部分在下侧具有锁定齿（12），该齿与锁定齿（13）接合导轨（2）的上侧。锁定部分（10）由弹簧（15）装载，并具有一个具有两个表面（22,23）的操作件（18），该表面搁置在调节板（5）的一个横向部分（21）上。

56. 发明授权

US5688946A Amino acid derivatives having renin inhibiting activity 失效
标题翻译：具有肾素抑制活性的氨基酸衍生物
公开(公告)号：US5688946A
公开(公告)日：1997-11-18
申请号：US277111
申请日：1994-07-19
申请人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
发明人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
IPC分类号： C12N9/99 , A61K31/195 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/435 , A61K31/54 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07D207/34 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D277/20 , C07D277/30 , C07D277/68 , C07D333/24 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D453/02 , C07F9/6512 , C07K1/113 , C07K5/06 , C07K5/065 , C07K14/81 , C07D295/12 , C07D295/22 , A61K31/95 , A61K37/00
CPC分类号： C07K5/06078 , A61K38/00
摘要： The compounds of the formula ##STR1## in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：光学纯非对映异构体，非对映异构体，非对映异构体外消旋体的混合物或非对映异构体外消旋物的混合物及其药学上可用的盐形式的式I化合物抑制天然酶肾素的活性，因此可用于用于控制或预防高血压和心脏功能不全的药物制剂形式。

57. 发明授权

US5665718A Imidazodiazepines 失效
标题翻译：咪唑并二氮杂
公开(公告)号：US5665718A
公开(公告)日：1997-09-09
申请号：US586439
申请日：1996-01-16
申请人： Thierry Godel , Walter Hunkeler , Heinz Stadler , Ulrich Widmer
发明人： Thierry Godel , Walter Hunkeler , Heinz Stadler , Ulrich Widmer
IPC分类号： A61K31/41 , A61K31/55 , A61K31/5517 , A61P21/02 , A61P25/08 , A61P25/20 , A61P43/00 , C07D487/02 , C07D487/04 , C07D495/12 , C07D495/14 , C07D498/14 , A61K31/555 , C07D521/000
CPC分类号： C07D487/04 , C07D495/14
摘要： The invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR2## Q is one of the residues ##STR3## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered membered heterocycle optionally containing a further hetero atom or a fused benzene ring,R.sup.3 is hydrogen and R.sup.4 is lower alkyl or R.sup.3 and R.sup.4 together are dimethylene or trimethylene andR.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,the compounds of formula I having the (S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.3 and R.sup.4 together are dimethylene or trimethylene,and pharmaceutically acceptable acid addition salts thereof. These compounds and salts have pronounced anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties.
摘要翻译：本发明涉及下式化合物：其中A与由α和β表示的两个碳原子一起是残基“（A1）”（A2）和（IMA）>（A3）Q （Q1）＆lt; IMAGE＆gt;（Q2）和＆lt; IMAGE＆gt;（Q3）中的一个R 1和R 2各自独立地为氢，低级烷基，低级烯基，低级炔基，低级羟烷基，低级烷氧基 - 低级烷基，（C 3 -C 6） - 环烷基，（C 3 -C 6） - 环烷基 - 低级烷基，氨基 - 低级烷基，低级烷基氨基 - 低级烷基，二低级烷基氨基 - 低级烷基或芳基 - 低级烷基或与氮原子一起为任选含有另外的杂原子或稠合苯环的5-至8-元元杂环，R 3为氢，R 4为低级烷基或R 3和R 4一起为二亚甲基或三亚甲基，R 5和R 6各自独立地为氢，卤素，三氟甲基，低级烷氧基或硝基，当R 3表示具有（S）构型的式I化合物时，相对于由γ表示的碳原子和R4一起是二亚甲基或三亚甲基，及其药学上可接受的酸加成盐。这些化合物和盐具有明显的抗焦虑，抗惊厥，肌肉松弛剂和镇静催眠特性。

58. 发明授权

US5134123A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5134123A
公开(公告)日：1992-07-28
申请号：US318576
申请日：1989-03-03
申请人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
发明人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
IPC分类号： A61K31/16 , A61K31/41 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K38/00 , A61P9/04 , A61P9/12 , C07C215/26 , C07C231/02 , C07C237/00 , C07C237/22 , C07C317/44 , C07C323/60 , C07D231/12 , C07D233/54 , C07D233/64 , C07D263/04 , C07D263/06 , C07D263/24 , C07D277/20 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/06 , C07D417/12 , C07F9/6506 , C07K5/06 , C07K14/81
CPC分类号： C07D233/64 , C07C215/26 , C07C237/00 , C07C317/44 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12 , Y02P20/55
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：其中A，R 1，R 2，R 3，R 4，R 5和R 6如上所述的式Ⅺ化合物被描述。式I的化合物对天然酶肾素具有抑制活性，因此可以以用于控制或预防高血压和心脏功能不全的药物制剂的形式使用。

59. 发明授权

US5065663A Electropneumatic or electrohydraulic linear drive mechanism 失效
标题翻译：电动气动或电动液压线性驱动机构
公开(公告)号：US5065663A
公开(公告)日：1991-11-19
申请号：US623166
申请日：1990-11-06
申请人： Heinz Stadler , Alfred Heinzl , Wilhelm Krakowetz
发明人： Heinz Stadler , Alfred Heinzl , Wilhelm Krakowetz
IPC分类号： F15B15/24 , F15B15/28
CPC分类号： F15B15/2815 , F15B15/24
摘要： A linear drive mechanism has a combination of a drive cylinder, a drive rod stroke-limiting element, position sensors, a solenoid, and a terminal strip, together with internal wirings and hose connections. The drive mechanism can be arbitrarily arranged quickly and simply at a processing apparatus or assembly structure as a unit, and only a cable having the external signal and control lines as well as a supply line for the pressure agent need be connected thereto. No disturbing and involved wirings and position sensing elements therefore need be arranged in the actual tool region.
摘要翻译：线性驱动机构具有驱动气缸，驱动杆行程限制元件，位置传感器，螺线管和端子排以及内部配线和软管连接的组合。驱动机构可以在作为一个单元的处理装置或组装结构中快速和简单地任意布置，并且只有具有外部信号和控制线的电缆以及用于压力试剂的供应管线需要连接到其上。因此，不需要在实际的工具区域中布置布线和位置感测元件。

60. 发明授权

US4684910A Armature retaining spring and coil flange contact chamber for an electromagnetic relay 失效
标题翻译：用于电磁继电器的电枢保持弹簧和线圈法兰接触室
公开(公告)号：US4684910A
公开(公告)日：1987-08-04
申请号：US894825
申请日：1986-08-08
申请人： Michael Dittmann , Heinz Stadler
发明人： Michael Dittmann , Heinz Stadler
IPC分类号： H01H50/28 , H01F7/13
CPC分类号： H01H50/28
摘要： An electromagnetic relay includes a coil having a winding between two coil flanges wherein one of the coil flanges forms a pocket-shaped contact chamber. An angled yoke is provided for the coil on which is seated a flat armature that is secured by an armature retaining spring. Male retaining members extending from the angled yoke mount the retaining spring and can be bent to set the armature restoring force. Separation of the moving parts of the relay at an end face of one coil flange from the winding enables casting compound to fill the winding space and seal the contact chamber.
摘要翻译：一种电磁继电器包括具有两个线圈凸缘之间的绕组的线圈，其中一个线圈凸缘形成一个袋形接触腔。为线圈提供了一个倾斜的轭架，线圈座位于通过电枢保持弹簧固定的扁平电枢上。从倾斜的轭延伸的公保持构件安装保持弹簧并且可以弯曲以设定电枢恢复力。在一个线圈凸缘的端面处的继电器的运动部分与绕组的分离使得铸造复合物能够填充绕组空间并密封接触室。

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