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1. 发明申请

US20050026994A1 Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors 审中-公开
标题翻译：使用2,4-二氨基-3-羟基羧酸衍生物作为蛋白酶体抑制剂
公开(公告)号：US20050026994A1
公开(公告)日：2005-02-03
申请号：US10035301
申请日：2001-10-25
申请人： Dennis France , Peter Furst , Johann Zimmermann , Carlos Garcia-Echeverria , Dieter Scholz , Pascal Furet , Patricia Imbach
发明人： Dennis France , Peter Furst , Johann Zimmermann , Carlos Garcia-Echeverria , Dieter Scholz , Pascal Furet , Patricia Imbach
IPC分类号： A61K38/00 , A61P17/06 , A61P35/00 , A61P43/00 , C07C237/12 , C07C271/22 , C07K5/00 , A61K31/381 , A61K31/165
CPC分类号： C07C271/22 , Y02P20/55
摘要： The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R1 represents hydrogen; an amino protecting group; or a group of formula R5Y— wherein R5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents —CO—; —NH—CO—; —NH—CS—; —SO2—; —O—CO—; or —O—CS—; R2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g., of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R2 represents arylalkyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R5 represents arylalkyl and Y represents —CO—; or R5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents —O—CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.
摘要翻译：本发明涉及式（I）的2,4-二氨基-3-羟基羧酸的新用途，其中A和B独立地表示键或未取代或取代的氨基酰基部分; R1表示氢; 氨基保护基; 烯基，炔基，芳基，芳基烷基，杂芳基，杂芳基烷基，杂环基或杂环基烷基;或其中R 5表示氢或未取代或取代的烷基，烯基，炔基，芳基， Y表示-CO-; -NH-CO-; -NH-CS-; -SO2-; -O-CO-; 或-O-CS-; R2表示天然氨基酸的侧链; 烷基，芳基烷基，杂芳基烷基或环烷基烷基; 或三甲基甲硅烷基甲基，2-噻吩基甲基或苯乙烯基甲基; R3表示卤素，烷基，烷氧基或羟基烷氧基; 并且R 4表示2（R） - 羟基茚满-1（S） - 基; （S）-2-羟基-1-苯基乙基; 或2-羟基苄基未被取代或在4-位上被甲氧基取代; 在制备用于治疗增殖性疾病例如实体瘤的药物组合物中; 涉及一种治疗温血动物的方法; 和式（I *）的2,4-二氨基-3-羟基羧酸，其中A和B独立地表示未取代或取代的氨基酰基部分; R2代表芳基烷基; R3表示卤素，烷基，烷氧基或羟基烷氧基; R4代表未取代的或在4位被甲氧基取代的2-羟基 - 苄基; R5表示芳基烷基，Y表示-CO-; 或R 5表示被环烷基，萘基，吡啶基或苯基取代的烷基，其中苯基被烷基或氨基取代; Y表示-O-CO; 其药学上可接受的盐; 以及使用这些式（I *）化合物来治疗人或动物体，特别是治疗增殖性疾病。

2. 发明申请

US20060205673A1 2-Amino-3-hydroxy-4-tert-leucyl-amino-5-phenyl-pentanoic acid amide derivatives 审中-公开
标题翻译： 2-氨基-3-羟基-4-叔 - 亮氨酰基 - 氨基-5-苯基 - 戊酸酰胺衍生物
公开(公告)号：US20060205673A1
公开(公告)日：2006-09-14
申请号：US11434398
申请日：2006-05-15
申请人： Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Marc Lang , Johann Zimmermann
发明人： Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Marc Lang , Johann Zimmermann
IPC分类号： A61K38/05 , C07K5/06
CPC分类号： C07K5/0215 , A61K38/00
摘要： The invention relates to compounds of formula I wherein the substituents and symbols are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.
摘要翻译：本发明涉及式I化合物，其中取代基和符号如本说明书所述定义，其制备方法，包含那些化合物的药物及其在制备治疗性治疗药物组合物中的应用温血动物，包括人类。

3. 发明授权

US07700605B2 2-cyano-pyrimidines and-triazines as cysteine protease inhibitors 失效
标题翻译： 2-氰基 - 嘧啶和三嗪作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US07700605B2
公开(公告)日：2010-04-20
申请号：US11995994
申请日：2006-07-17
申请人： Stefanie Flohr , Pascal Furet , Patricia Imbach , Ulrich Hommel , Hans-Ulrich Litshcer , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
发明人： Stefanie Flohr , Pascal Furet , Patricia Imbach , Ulrich Hommel , Hans-Ulrich Litshcer , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
IPC分类号： C07D239/34 , C07D239/42 , C07D239/46 , C07D239/48 , A61K31/505 , A61P35/00 , C07D251/14 , C07D251/42 , C07D251/48 , A61K31/53
CPC分类号： C07D239/34 , C07D239/42
摘要： The invention relates to compounds of the formula I and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
摘要翻译：本发明涉及式I化合物及其盐，其制备方法，用于治疗（特别是半胱氨酸蛋白酶，例如UCH-L3-和/或USP-2依赖性）疾病或用于制备针对这些疾病的药物制剂，治疗温血动物的方法包括向所述动物和药物制剂施用化合物和/或其盐，特别是用于治疗包含所述化合物和/或盐的疾病。

4. 发明申请

US20080214548A1 2-Cyano-Pyrimidines and-Triazines as Cysteine Protease Inhibitors 失效
标题翻译： 2-氰基 - 嘧啶和三嗪作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US20080214548A1
公开(公告)日：2008-09-04
申请号：US11995994
申请日：2006-07-17
申请人： Stefanie Flohr , Pascal Furet , Patricia Imabach , Ulrich Hommel , Hans-Ulrich litscher , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
发明人： Stefanie Flohr , Pascal Furet , Patricia Imabach , Ulrich Hommel , Hans-Ulrich litscher , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
IPC分类号： A61K31/53 , C07D251/14 , A61K31/505 , A61P35/04 , C07D239/28
CPC分类号： C07D239/34 , C07D239/42
摘要： The invention relates to compounds of the formula I and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
摘要翻译：本发明涉及式I化合物及其盐，其制备方法，用于治疗（特别是半胱氨酸蛋白酶，例如UCH-L3-和/或USP-2依赖性）疾病或用于制备针对这些疾病的药物制剂，治疗温血动物的方法包括向所述动物和药物制剂施用化合物和/或其盐，特别是用于治疗包含所述化合物和/或盐的疾病。

5. 发明申请

US20100316576A1 AEROSOLS FOR SINUNASAL DRUG DELIVERY 有权
标题翻译：航空药物交付使用
公开(公告)号：US20100316576A1
公开(公告)日：2010-12-16
申请号：US12675257
申请日：2008-08-29
申请人： Manfred Keller , Uwe Schuschnig , Johann Zimmermann , Martin Luber , Andreas Böhm
发明人： Manfred Keller , Uwe Schuschnig , Johann Zimmermann , Martin Luber , Andreas Böhm
IPC分类号： A61K9/12 , A61P11/06 , A61P11/02 , A61P11/00 , A61M11/00
CPC分类号： A61M11/005 , A61K9/0043 , A61K9/0078 , A61K9/008 , A61K31/7052 , A61M11/00 , A61M15/0085
摘要： A pharmaceutical aerosol is disclosed which is suitable for delivering an active compound to the mucosa of the nose, the osteomeatal complex or a paranasal sinus. The pressure of the aerosol is not constant, but pulsates at a frequency from about 10 to 90 Hz. The aerosol is further characterised in that it exhibits a low effective flow rate of less than about 5 litres per minute. The aerosol is, inter alia, suitable for the prevention, management, or treatment of a disease, symptom, or condition affecting the nose or the paranasal sinuses, such as acute and chronic sinusitis.
摘要翻译：公开了一种适用于将活性化合物递送至鼻粘膜，骨产生复合体或鼻旁窦的药物气溶胶。气溶胶的压力不是恒定的，而是以约10至90Hz的频率脉动。气溶胶的特征还在于它具有小于约5升/分钟的低有效流速。气溶胶尤其适用于预防，治疗或治疗影响鼻子或鼻旁窦的疾病，症状或病症，例如急性和慢性鼻窦炎。

6. 发明申请

US20050246160A1 Information generation system for product formation 审中-公开
标题翻译：产品形成信息生成系统
公开(公告)号：US20050246160A1
公开(公告)日：2005-11-03
申请号：US10519085
申请日：2003-06-13
申请人： Johann Zimmermann
发明人： Johann Zimmermann
IPC分类号： G05B19/418 , G06F17/27
CPC分类号： G05B19/41865 , G05B2219/31395 , Y02P90/20
摘要： A system for the generation and storage of data, each of which represent a component of a technical product or a step in a formation process for the product. The system can generate types of relationships between several data object types and allocate data object types as well as automatically evaluatable specifications for dependencies between data objects to the types of relationships. A classification for data object types in various phases of the formation process is preferably provided. A coupling together of various applications for separate given phases is without the need to generate and maintain an intermediate model or direct interfaces between the applications.
摘要翻译：用于产生和存储数据的系统，每个数据表示技术产品的组成部分或产品形成过程中的步骤。系统可以生成几种数据对象类型之间的关系类型，并分配数据对象类型以及数据对象与关系类型之间的依赖关系的自动可评估规范。优选地提供在形成过程的各个阶段中的数据对象类型的分类。用于单独给定阶段的各种应用的耦合在一起不需要生成和维护应用之间的中间模型或直接接口。

7. 发明授权

US09617308B2 Beta-hairpin peptidomimetics 有权
公开(公告)号：US09617308B2
公开(公告)日：2017-04-11
申请号：US14406108
申请日：2012-06-06
申请人： Frank Otto Gombert , Daniel Obrecht , Alexander Lederer , Johann Zimmermann , Christian Oefner
发明人： Frank Otto Gombert , Daniel Obrecht , Alexander Lederer , Johann Zimmermann , Christian Oefner
IPC分类号： C07K7/54 , C07K7/50 , A61K38/00 , A61K38/12 , A61K38/04 , C07K7/08
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.

8. 发明授权

US08852557B2 Aerosols for sinunasal drug delivery 有权
标题翻译：鼻窦药物输送用气溶胶
公开(公告)号：US08852557B2
公开(公告)日：2014-10-07
申请号：US12675257
申请日：2008-08-29
申请人： Manfred Keller , Uwe Schuschnig , Johann Zimmermann , Martin Luber , Andreas Böhm
发明人： Manfred Keller , Uwe Schuschnig , Johann Zimmermann , Martin Luber , Andreas Böhm
IPC分类号： A01N25/02 , A61K9/12 , B05B17/06 , A61M11/00 , A61K9/00 , A61M15/00
CPC分类号： A61M11/005 , A61K9/0043 , A61K9/0078 , A61K9/008 , A61K31/7052 , A61M11/00 , A61M15/0085
摘要： A pharmaceutical aerosol is disclosed which is suitable for delivering an active compound to the mucosa of the nose, the osteomeatal complex or a paranasal sinus. The pressure of the aerosol is not constant, but pulsates at a frequency from about 10 to 90 Hz. The aerosol is further characterized in that it exhibits a low effective flow rate of less than about 5 liters per minute. The aerosol is, inter alia, suitable for the prevention, management, or treatment of a disease, symptom, or condition affecting the nose or the paranasal sinuses, such as acute and chronic sinusitis.
摘要翻译：公开了一种适用于将活性化合物递送至鼻粘膜，骨产生复合体或鼻旁窦的药物气溶胶。气溶胶的压力不是恒定的，而是以约10至90Hz的频率脉动。气溶胶的特征还在于它具有小于约5升/分钟的低有效流速。气溶胶尤其适用于预防，治疗或治疗影响鼻子或鼻旁窦的疾病，症状或病症，例如急性和慢性鼻窦炎。

9. 发明申请

US20130225506A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 有权
标题翻译：具有CXCR7调节活性的模板固定化肽
公开(公告)号：US20130225506A1
公开(公告)日：2013-08-29
申请号：US13577143
申请日：2011-02-04
申请人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
发明人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.
摘要翻译：通式（I）的新型模板固定β-发夹肽模拟物，其中单个元件T或P是从下述的羰基（C = O）连接点连接到氮（N）的α-氨基酸残基元件，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经系统疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

10. 发明申请

US20080006276A1 Face mask, in particular inhalation mask for use with a therapeutic nebuliser 审中-公开
标题翻译：面罩，特别是与治疗雾化器一起使用的吸入面罩
公开(公告)号：US20080006276A1
公开(公告)日：2008-01-10
申请号：US11825310
申请日：2007-07-05
申请人： Vera Kreutzmann , Sven Rosenbeiger , Johann Zimmermann
发明人： Vera Kreutzmann , Sven Rosenbeiger , Johann Zimmermann
IPC分类号： A61M16/06 , A62B18/02
CPC分类号： A61M16/06 , A61M11/00 , A61M16/0616 , A61M16/0816
摘要： In order to improve the wearing comfort and the sealing in an upper nasal region, the present invention proposes a face mask, in particular an inhalation mask for use with a therapeutic nebuliser, comprising a main mask body that comprises a first circumferential region, which is designed for the application of the mask to a user's face, and a second region for connection to, in particular, a therapeutic nebuliser, wherein a section of the first region is designed for application to an upper nasal region of the face and comprises two sealing lips connected in series. According to the invention, the two sealing lips connected in series are formed by a first inward-facing sealing lip and a second outward-facing sealing lip.
摘要翻译：为了提高上鼻区域的穿着舒适性和密封性，本发明提出了一种面罩，特别是与治疗式雾化器一起使用的吸入面罩，其包括主面罩主体，该主面罩主体包括第一周边区域，设计用于将面罩施加到使用者的脸部，以及第二区域，用于连接到特别是治疗性雾化器，其中第一区域的一部分被设计用于施用于面部的上鼻部区域，并且包括两个密封嘴唇连接在一起。根据本发明，串联连接的两个密封唇由第一向内密封唇和第二向外密封唇形成。

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