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1. 发明申请

WO2011095607A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：具有CXCR7调节活性的模板固定化肽
公开(公告)号：WO2011095607A1
公开(公告)日：2011-08-11
申请号：PCT/EP2011/051686
申请日：2011-02-04
申请人： POLYPHOR AG , GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
发明人： GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
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）的新型模板固定的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。

2. 发明申请

WO2013182240A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2013182240A1
公开(公告)日：2013-12-12
申请号：PCT/EP2012/060766
申请日：2012-06-06
申请人： POLYPHOR AG , GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
发明人： GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
IPC分类号： C07K7/64
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr 1 -His 2 -Xaa 3 -Cys 4 -Ser 5 -Xaa 6 -DPro 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 -Tyr 12 -Xaa 13 -Xaa 14 -Xaa 15 -Pro 16 -), disulfide bond between Cys 4 and Cys 11 , and pharmaceutically acceptable salts thereof, with Xaa 3 , Xaa 6 , Xaa 8 , Xaa 13 , Xaa 14 and Xaa 15 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.
摘要翻译：通式为（-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-）的β-发夹肽模拟物，Cys4和 Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa3，Xaa6，Xaa8，Xaa13，Xaa14和Xaa15具有有利的药理学性质并可用于预防HIV感染健康个体或减慢和停止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员调节组织修复的试剂。这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法来制造。

3. 发明申请

WO2012168336A1 BETA - HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS 审中-公开
标题翻译：作为CXC4拮抗剂的BETA - HAIRPIN PEPTIDOMIMITICS
公开(公告)号：WO2012168336A1
公开(公告)日：2012-12-13
申请号：PCT/EP2012/060763
申请日：2012-06-06
申请人： POLYPHOR AG , OBRECHT, Daniel , GOMBERT, Frank, Otto , ZIMMERMANN, Johann
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , ZIMMERMANN, Johann
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , A61K38/00 , C07K1/047 , C07K7/64
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr 1 -His 2 -Xaa 3 -Cys 4 -Ser 5 - Ala 6 -Xaa 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 -Tyr 12 -Xaa 13 -Xaa 14-D Pro 15 -Pro 16 -), disulfide bond between Cys 4 and Cys 11 , and pharmaceutically acceptable salts thereof, with Xaa 3 , Xaa 7 , Xaa 8 , Xaa 13 and Xaa 14 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.
摘要翻译： ß-通式为环（-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-）的发夹肽模拟物，Cys4和 Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa3，Xaa7，Xaa8，Xaa13和Xaa14具有有利的药理学性质并且可用于预防健康个体中的HIV感染或用于减缓和停止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员调节组织修复的试剂。这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。

4. 发明申请

WO2011095218A1 TEMPLATE-FIXED PEP TIDOMIME TICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：模板固定PEP TIDOMIME TICS与CXCR7调节活动
公开(公告)号：WO2011095218A1
公开(公告)日：2011-08-11
申请号：PCT/EP2010/051417
申请日：2010-02-05
申请人： POLYPHOR AG , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , LÖWE, Ralf , ZIMMERMANN, Johann
发明人： GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , LÖWE, Ralf , ZIMMERMANN, Johann
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是从连接的羰基（C = O）连接到下一个元素的氮（N）连接的α-氨基酸残基顺时针方向，并且其中所述元件取决于它们在链中的位置在说明书中定义，并且权利要求书具有作用于受体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。

5. 发明申请

WO2008028472A1 THERMISCHER RUSSFILTER 审中-公开
标题翻译：热油烟过滤器
公开(公告)号：WO2008028472A1
公开(公告)日：2008-03-13
申请号：PCT/DE2007/001570
申请日：2007-09-05
申请人： ZIMMERMANN, Johann
发明人： ZIMMERMANN, Johann
IPC分类号： F02B19/10 , F02B19/16
CPC分类号： F01N3/021 , F01N3/0235 , F02B3/06 , F23J15/025 , F23J2215/10
摘要： Der „Thermische Rußfilter" gehört als Einrichtung, als Komponente zu den Dieseleinspritzsystemen, angeordnet an den heißesten Stellen in der Nähe der Einspritzdüse, um NO 2 , an der Oberfläche von erzeugten Rußpartikeln in HONO beziehungsweise NO aufzuspalten. Die Rußpartikel werden dabei vollständig aufgebraucht, weil ein Steuergerät über einen Rußsensor die richtigen Werte nach dort einprogrammierten Kennlinien/ Kennfeldern, nach der Stellung des Rußfilters zur Einspritzdüse vergleicht und ihn beim Einspritzvorgang über die Temperaturveränderung der Stellglieder (9/9') auf den richtigen „Rußspalt" (R+/ R_) zum „Injektor" einstellt (V_/V+). Dies ist mit Hilfe von Bimaterial -Elementen (9/9') in sehr kurzer Zeit möglich, da das Steuergerät drahtlos und in Echtzeit die Kraftstoffeinspritzung verändern kann. Durch die Auskleidung des Rohres (10) mit langfaseriger, offenporiger und oberflächenrauer keramischer Substanz (zum Beispiel mit Zirkoniumoxid), erhält man eine strömungsgünstige, da turbulente Strömung für eine Gasströmungsgeschwindigkeit bis zur höchsten Schallgeschwindigkeit, die günstig für den Ablauf der Verbrennung im Zylinder eines Tauchkolbenmotors ist.
摘要翻译：该“热烟尘过滤器”属于作为设备，作为位于在喷射喷嘴附近的最热位置处的柴油喷射系统中的组件，以在HONO或分割NO _{2 ，生成的烟灰粒子的表面上NO。烟灰粒子从而完全用尽，因为经由烟灰传感器控制单元，用于编程的有特征/特性映射进行比较正确的值，以烟尘过滤器与所述注射喷嘴并在致动器（9/9“）的温度变化的注射过程中的位置，以正确的他” Rußspalt “（R + / R_）为” 注射器“集（V_ / V +）。这是可能的，在很短的时间双材料-elements（9/9“）的帮助，因为该控制器可以改变喷油无线和实时。通过管（10）的陶瓷材料（例如，氧化锆）的长纤维，开放多孔性和粗糙表面的衬里，以获得有利的流动，因为对于一个气体流速声音的最高速度，筒状活塞发动机的气缸中的低燃烧的过程紊流是。}

6. 发明申请

WO2009106586A1 QUINOLINES AS INHIBITORS OF FARNESYL PYROPHOSPHATE SYNTHASE 审中-公开
标题翻译：作为呋喃糖磷酸酯合成酶抑制剂的喹啉
公开(公告)号：WO2009106586A1
公开(公告)日：2009-09-03
申请号：PCT/EP2009/052314
申请日：2009-02-26
申请人： NOVARTIS AG , AMSTUTZ, René , BOLD, Guido , COTESTA, Simona , JAHNKE, Wolfgang , MARZINZIK, Andreas , MUELLER-HARTWIEG, Constanze , OFNER, Silvio , STAUFFER, Frédéric , ZIMMERMANN, Johann
发明人： AMSTUTZ, René , BOLD, Guido , COTESTA, Simona , JAHNKE, Wolfgang , MARZINZIK, Andreas , MUELLER-HARTWIEG, Constanze , OFNER, Silvio , STAUFFER, Frédéric , ZIMMERMANN, Johann
IPC分类号： C07D215/48 , C07D401/04 , C07F9/60 , C07D215/18 , C07D409/04 , C07D409/14 , C07D417/12 , A61K31/675 , A61P35/04
CPC分类号： C07D215/48 , C07D215/18 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/12 , C07F9/60 , C07F9/65583 , C07F9/65586
摘要： The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.
摘要翻译：本发明涉及式（I）化合物，其中取代基如本说明书所述，其可用作法呢基焦磷酸合酶调节剂，例如，在增殖性疾病的治疗中，涉及制造这些化合物的方法及其中间体。

7. 发明申请

WO2005014006A1 COMBINATIONS OF A CATHEPSIN K INHIBITOR AND A BISPHOPHONATE IN THE TREATMENT OF BONE METASTASIS, TUMOR GROWTH AND TUMOR-INDUCED BONE LOSS 审中-公开
标题翻译：骨钙素抑制剂和双膦酸盐治疗骨质疏松，肿瘤生长和肿瘤诱发骨丢失的组合
公开(公告)号：WO2005014006A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008107
申请日：2004-07-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ZIMMERMANN, Johann , GOESSL, Carsten
发明人： ZIMMERMANN, Johann , GOESSL, Carsten
IPC分类号： A61K31/663
CPC分类号： A61K31/505 , A61K31/451 , A61K31/495 , A61K31/506 , A61K31/66 , A61K31/663 , A61K31/675 , A61K2300/00
摘要： This invention relates to pharmaceutical preparations comprising certain types of bisphosphonates and certain types of Cathepsin K inhibitors, in particular in the prevention and treatment of bone metastases, tumor-induced hypercalcemia, tumor growth, tumor-induced bone loss and bone loss diseases such as osteoporosis or cancer-therapy-induced bone loss.
摘要翻译：本发明涉及包含某些类型的双膦酸盐和某些类型的组织蛋白酶K抑制剂的药物制剂，特别是在预防和治疗骨转移，肿瘤诱导的高钙血症，肿瘤生长，肿瘤诱导的骨丢失和骨丢失疾病如骨质疏松症或癌症治疗引起的骨丢失。

8. 发明申请

WO2017207118A1 BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FORMS THEREOF 审中-公开
标题翻译：具有弹性蛋白酶抑制活性和气溶胶剂型的β-HAIRPIN肽制剂
公开(公告)号：WO2017207118A1
公开(公告)日：2017-12-07
申请号：PCT/EP2017/025157
申请日：2017-05-31
申请人： POLYPHOR AG
发明人： BRUIJNZEEL, Piet , ZIMMERMANN, Johann , BARTH, Philip , CHEVALIER, Eric , LUDIN, Christian , KELLER, Manfred
IPC分类号： A61K8/64 , A61K38/12 , A61K9/00 , A61P11/00 , C07K7/64
摘要： The present invention relates to pharmaceutical aerosols comprising a β-hairpin peptidomimetic of formula cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro-Gln-Lys-Tyr- D Pro-Pro-), or a pharmaceutically acceptable salt thereof, having inhibitory activity against human neutrophil elastase. It further relates to solid or liquid pharmaceutical compositions and kits for preparing and administering such aerosols. The invention can be used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fibrosis (CF), non-cystic fibrosis bronchiactasis (NCFB), or chronic obstructive pulmonary disease (COPD), or infections, or diseases, or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further relates to a pharmaceutical composition or a pharmaceutical aerosol comprising the active compound cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro-Gln-Lys-Tyr- D Pro-Pro-), or any pharmaceutically acceptable salt thereof, for use in a method for the prevention, management or treatment of diseases or conditions of the lungs being mediated by or resulting from human neutrophil elastase activity in a subject.
摘要翻译：本发明涉及药物气雾剂，其包含式环（-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-）的β-发夹肽模拟物 Pro-Pro-）或其药学上可接受的盐，其对人嗜中性粒细胞弹性蛋白酶具有抑制活性。它还涉及用于制备和施用这种气雾剂的固体或液体药物组合物和试剂盒。本发明可用于预防，治疗或治疗肺部疾病，如α-1抗胰蛋白酶缺乏症（AATD），囊性纤维化（CF），非囊性纤维化支气管扩张症（NCFB）或慢性阻塞性肺病（COPD），或由人嗜中性粒细胞弹性蛋白酶活性介导或由其产生的感染，或肺的疾病或病症。因此，本发明进一步涉及包含活性化合物环（-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-D-D）的药物组合物或药用气雾剂。 Pro-Pro-）或其任何药学上可接受的盐，用于预防，管理或治疗受试者中由人嗜中性粒细胞弹性蛋白酶活性介导或由其产生的肺疾病或病症的方法。

9. 发明申请

WO2013050346A1 TEMPLATE -FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 审中-公开
标题翻译：作为FPR1的抑制剂的模板化混合肽
公开(公告)号：WO2013050346A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069412
申请日：2012-10-02
申请人： POLYPHOR AG
发明人： JUNG, Françoise , OBRECHT, Daniel , LÖWE, Ralf , ZIMMERMANN, Johann , LEMERCIER, Guillaume , CHEVALIER, Eric
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I): cyclo[P 1 -P 2 -P 3 -P 4 -P 5 -P 6 -P 7 -P 8 -P 9 -P 10 -P 11 -P 12 -P 13 -P 14 -T 1 -T 2 ] wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions,immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：通式（I）：环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2]的新型模板固定β-发夹肽模拟物其中单个元件T或P是沿任一方向连接的α-氨基酸残基，根据其在链中的位置如说明书和权利要求及其盐中所定义，其具有拮抗生物效应的性质受体FPR1。它们可以用作治疗或预防炎性疾病，过敏性疾病，免疫学障碍，神经炎症，神经障碍，阻塞性气道疾病，传染病，缺血再灌注损伤和增殖性疾病如疾病或疾病的疾病或病症的药物。癌症。这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。

10. 发明申请

WO2009027095A4 AEROSOLS FOR SINUNASAL DRUG DELIVERY 审中-公开
公开(公告)号：WO2009027095A4
公开(公告)日：2009-03-05
申请号：PCT/EP2008/007090
申请日：2008-08-29
申请人： PARI PHARMA GMBH , KELLER, Manfred , SCHUSCHNIG, Uwe , ZIMMERMANN, Johann , LUBER, Martin , BÖHM, Andreas
发明人： KELLER, Manfred , SCHUSCHNIG, Uwe , ZIMMERMANN, Johann , LUBER, Martin , BÖHM, Andreas
IPC分类号： A61K9/00 , A61M11/00 , A61M15/00 , B05B3/00 , B05C11/02
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.

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