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11. 发明申请

US20120122903A1 1-H-QUINAZOLINE-2, 4-DIONES FOR USE IN THE TREATMENT OF NEURONAL CEROID LIPOFUSCINOSIS 审中-公开
标题翻译： 1-H-Quinazoline-2，4-DIONES用于治疗神经性白蛋白LIPOFUSCUSOSIS
公开(公告)号：US20120122903A1
公开(公告)日：2012-05-17
申请号：US13384280
申请日：2010-07-23
申请人： Hans O Kalkman , Henri Mattes
发明人： Hans O Kalkman , Henri Mattes
IPC分类号： A61K31/517 , C07D403/10 , A61P25/28 , C07D239/96
CPC分类号： A61K31/517
摘要： The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of neuronal ceroid lipofuscinosis.
摘要翻译：本发明涉及竞争性AMPA受体拮抗剂用于治疗，预防或延迟神经元类蜡状脂褐斑病的进展。

12. 发明授权

US5510353A Certain aminoguanidine compounds, pharmaceutical compositions containing them and their use in treating gastrointestinal motility disorders and disorders associated with cephalic pain 失效
标题翻译：某些氨基胍化合物，含有它们的药物组合物及其用于治疗胃肠蠕动障碍和与头痛有关的疾病
公开(公告)号：US5510353A
公开(公告)日：1996-04-23
申请号：US370038
申请日：1995-01-09
申请人： Rudolf K. A. Giger , Henri Mattes
发明人： Rudolf K. A. Giger , Henri Mattes
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61P1/00 , A61P1/04 , C07C9/08 , C07D209/10 , C07D209/14 , C07D241/16 , C07D333/58 , C07D403/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/08 , C07F9/572 , A61K31/425
CPC分类号： C07D403/12 , C07D209/14 , C07D333/58 , C07D409/12 , C07D417/12 , C07D471/04 , C07F7/0814 , C07F9/5728
摘要： Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.
摘要翻译：式AX-Y-NH-B的化合物，其中A衍生自任选取代的苯并噻吩，吲哚，4-氮杂 - 和7-氮杂 - 苯并噻吩或 - 吲哚，A在5位氢，卤素，任选取代的烷基，羟基硝基，氨基，烷基氨基，酰氨基，烷氧基羰基，氨磺酰基，氰基，三甲基甲硅烷基，羧基，氨基甲酰基，磷酸酯，氧基氨基甲酰基，杂环基或醚或酯基，XY是-CR8 = N-或CH（R8）-NH-其中R8 是-H或烷基并连接在A的3位，B是杂环基或残基，环烷基，芳基，金刚烷基，酰基或氨基甲酰基，X 2是烷硫基或NR 3 R 10，其中R 3是H或烷基或R 3和R 10 与它们所连接的氮原子一起形成游离形式或盐形式的杂环基，具有药理活性，例如，用于治疗胃肠道疾病。

13. 发明授权

US06265219B1 Transponder tagging of constituents used in compound synthesis 失效
标题翻译：复合合成中使用的成分的应答器标签
公开(公告)号：US06265219B1
公开(公告)日：2001-07-24
申请号：US08739843
申请日：1996-10-30
申请人： Rudolf Karl Andreas Giger , Henri Mattes , Andrew Malcolm Bray , Nobuyoshi Joe Maeji
发明人： Rudolf Karl Andreas Giger , Henri Mattes , Andrew Malcolm Bray , Nobuyoshi Joe Maeji
IPC分类号： G01N33532
CPC分类号： G06K19/04 , B01J19/0046 , B01J2219/00463 , B01J2219/00504 , B01J2219/00506 , B01J2219/00545 , B01J2219/00547 , B01J2219/00567 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00689 , C40B70/00 , Y10T436/13
摘要： A synthesis member preferably comprises two elements: a crown and a stem. The stem includes a tag, such as a transponder, that is used to identify the synthesis member and/or the synthetic history of the synthesis member when used in the automated synthesis of compound libraries containing large numbers (e.g. 1000 or more) compounds. The crown provides the location at which compounds are synthesized. The combination of a crown for use with compound synthesis and stem allows the tracking of individual synthesis members from a library containing thousands of such synthesis members. Because each synthesis member is individually tracked and can be logged into a database and/or process flow control system, the synthesis of several thousand individual compounds in conventional containers, such as round bottom flasks is made possible using only traditional compound synthesis approaches.
摘要翻译：合成构件优选地包括两个元件：冠和杆。当用于自动合成含有大量（例如1000个或更多个）化合物的化合物文库时，该茎包括标签，例如应答器，其用于鉴定合成成员和/或合成成员的合成历史。表冠提供合成化合物的位置。用于化合物合成和茎的冠的组合允许从包含数千种这样的合成成员的文库中追踪个体合成成员。由于每个合成成分都被单独追踪并可以被记录到数据库和/或工艺流程控制系统中，所以使用传统的复合合成方法可以在常规容器（如圆底烧瓶）中合成几千个单独的化合物。

14. 发明授权

US06589950B1 Purine derivatives inhibitors of tyrosine protein kinase SYK 有权
标题翻译：嘌呤衍生物酪氨酸蛋白激酶SYK抑制剂
公开(公告)号：US06589950B1
公开(公告)日：2003-07-08
申请号：US10048577
申请日：2002-03-19
申请人： Stephen Paul Collingwood , Judy Hayler , Darren Mark Le Grand , Henri Mattes , Keith Allan Menear , Clive Victor Walker , Xiao-Ling Cockcroft
发明人： Stephen Paul Collingwood , Judy Hayler , Darren Mark Le Grand , Henri Mattes , Keith Allan Menear , Clive Victor Walker , Xiao-Ling Cockcroft
IPC分类号： C07D47316
CPC分类号： C07D473/24 , A61K31/52 , C07D473/16 , C07D473/18
摘要： Disclosed are compounds of the formula in free or salt form, wherein X, R1, R2, R3, and R4 are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
摘要翻译：公开的是无游离或盐形式的化合物，其中X，R 1，R 2，R 3和R 4如本说明书中所定义，其制备及其作为药物的用途，特别是用于治疗炎性或阻塞性气道疾病。

15. 发明授权

US06177520B1 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US06177520B1
公开(公告)日：2001-01-23
申请号：US08984640
申请日：1997-12-03
申请人： Henri Mattes
发明人： Henri Mattes
IPC分类号： C08F800
CPC分类号： C07C271/16 , C07B2200/11
摘要： Use of a compound of formula I wherein R1 is a C1-4 alkoxy or thioalkoxy group, and R2 is a group of formula SR10 or OR10 wherein R10 is a C1-4 carboxylic or thiocarboxylic acid residue in salt, ester, free acid or activated form, or an activated form thereof, as a linker in solid phase synthesis of organic compounds, preferably of carbamates and secondary amines, and in addition are provided processes, solid phase systems and intermediates based on the compound of formula I.
摘要翻译：使用式I的化合物，其中R1是C1-4烷氧基或硫代烷氧基，R2是式SR10或OR10的基团，其中R10是盐，酯，游离酸或活化形式的C1-4羧酸或硫代羧酸残基，或作为固相合成有机化合物，优选氨基甲酸酯和仲胺的接头，另外还提供了基于式I化合物的方法，固相体系和中间体。

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