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11. 发明申请

WO03002593A3 PEPTIDE STRUCTURES USEFUL FOR COMPETITIVE MODULATION OF DIPEPTIDYL PEPTIDASE IV CATALYSIS 审中-公开
标题翻译：磷酸二酯酶IV竞争性调节有用的肽结构
公开(公告)号：WO03002593A3
公开(公告)日：2003-09-04
申请号：PCT/EP0207128
申请日：2002-06-27
申请人： PROBIODRUG AG , DEMUTH HANS ULRICH , HOFFMANN TORSTEN , MANHART SUSANNE , HOFFMANN MATTHIAS , HEINS JOCHEN
发明人： DEMUTH HANS ULRICH , HOFFMANN TORSTEN , MANHART SUSANNE , HOFFMANN MATTHIAS , HEINS JOCHEN
IPC分类号： A61K38/00 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , A61P3/00 , A61P3/10 , A61P43/00 , C07K5/00 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/10 , C07K7/06
CPC分类号： C07K7/06 , A61K38/04 , A61K38/06 , A61K38/07 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The present invention refers to a compound represented by the general formula (I): and pharmaceutically acceptable salts thereof. The compounds can be used for the preparation of a medicament for the prophylaxis or treatment of a condition mediated by modulation of the dipeptidyl peptidase IV activity, wherein the condition preferably is selected from impaired glucose tolerance, diabetes mellitus, glucosuria and metabolic acidosis.
摘要翻译：本发明涉及由通式（I）表示的化合物及其药学上可接受的盐。所述化合物可用于制备用于预防或治疗通过调节二肽基肽酶IV活性介导的病症的药物，其中所述病症优选选自葡萄糖耐量异常，糖尿病，糖尿病和代谢性酸中毒。

12. 发明申请

WO03002595A2 NEW DIPEPTIDYL PEPTIDASE IV INHIBITORS AND THEIR USES AS ANTI-CANCER AGENTS 审中-公开
标题翻译：新型肽酶IV抑制剂及其作为抗癌剂的用途
公开(公告)号：WO03002595A2
公开(公告)日：2003-01-09
申请号：PCT/EP0207129
申请日：2002-06-27
申请人： PROBIODRUG AG , DEMUTH HANS-ULRICH , HOFFMANN TORSTEN , VON HOERSTEN STEPHAN
发明人： DEMUTH HANS-ULRICH , HOFFMANN TORSTEN , VON HOERSTEN STEPHAN
IPC分类号： C07D295/18 , A61K31/13 , A61K31/40 , A61K31/426 , A61K35/00 , A61K38/00 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , A61K45/00 , A61P3/04 , A61P3/10 , A61P9/10 , A61P17/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/28 , A61P35/00 , A61P35/04 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/04 , C07D207/06 , C07D277/04 , C07K5/062 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/10 , C07K7/06 , C07K7/08
CPC分类号： C07D295/185 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D277/04 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K7/06
摘要： The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.
摘要翻译：本发明提供本发明的DPIV-抑制剂及其相应的药学上可接受的酸加成盐形式的新用途，用于治疗由DPIV或DPIV样酶如癌和肿瘤介导的病症。在更优选的实施方案中，本发明的化合物可用于治疗转移和肿瘤定植。

13. 发明申请

WO2013024043A3 IN VIVO SCREENING MODELS FOR TREATMENT OF QC-RELATED DISORDERS 审中-公开
标题翻译：用于治疗与QC有关的疾病的生殖器筛查模型
公开(公告)号：WO2013024043A3
公开(公告)日：2013-06-06
申请号：PCT/EP2012065724
申请日：2012-08-10
申请人： PROBIODRUG AG , GRAUBNER SIGRID , JAGLA WOLFGANG , SCHILLING STEPHAN , CYNIS HOLGER , HOFFMANN TORSTEN , WERMANN MICHAEL , SCHULZ KATRIN , BAEUSCHER CHRISTOPH , KOHLMANN STEFANIE , DEMUTH HANS-ULRICH
发明人： GRAUBNER SIGRID , JAGLA WOLFGANG , SCHILLING STEPHAN , CYNIS HOLGER , HOFFMANN TORSTEN , WERMANN MICHAEL , SCHULZ KATRIN , BAEUSCHER CHRISTOPH , KOHLMANN STEFANIE , DEMUTH HANS-ULRICH
IPC分类号： C07K14/47 , A01K67/027 , C12N9/10
CPC分类号： A01K67/0278 , A01K2217/052 , A01K2217/15 , A01K2217/206 , A01K2227/105 , A01K2267/0312 , C07K14/4711 , C12N9/104
摘要： The present invention provides a double transgenic non-human animal, in particular a transgenic mouse encoding Qpct proteins, which have been implicated in Qpct-related diseases, and Amyloid Precursor Protein (APP). The present invention additionally provides cells and cell lines comprising transgenes encoding for Qpct and APP. The present invention further provides methods and compositions for evaluating agents that affect Qpct, for use in compositions for the treatment of Qpct-related diseases.
摘要翻译：本发明提供双重转基因非人动物，特别是编码Qpct蛋白的转基因小鼠，其涉及Qpct相关疾病和淀粉样蛋白前体蛋白（APP）。本发明另外提供了包含编码Qpct和APP的转基因的细胞和细胞系。本发明还提供了用于评估影响Qpct的药剂的方法和组合物，用于治疗Qpct相关疾病的组合物。

14. 发明申请

WO0234242A3 METHOD FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHOLOGICAL DISORDERS 审中-公开
标题翻译：治疗神经病学和神经病学疾病的方法
公开(公告)号：WO0234242A3
公开(公告)日：2003-01-30
申请号：PCT/EP0112478
申请日：2001-10-29
申请人： PROBIODRUG AG , VON HOERSTEN STEPHAN , HOFFMANN TORSTEN , DEMUTH HANS-ULRICH , KUEHN-WACHE KERSTIN , FRIEDRICH DANIEL
发明人： VON HOERSTEN STEPHAN , HOFFMANN TORSTEN , DEMUTH HANS-ULRICH , KUEHN-WACHE KERSTIN , FRIEDRICH DANIEL
IPC分类号： A61K45/00 , A61K31/00 , A61K31/17 , A61K31/40 , A61K31/426 , A61K38/00 , A61K38/17 , A61P1/14 , A61P9/12 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , A61P29/02 , A61P43/00 , C07D277/04 , A61K31/425
CPC分类号： A61K31/17 , A61K31/00 , A61K31/40 , A61K31/426 , A61K38/17 , A61K2300/00
摘要： The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable attractin inhibitor causes the reduction of activity in the enzyme attraction or in isoforms thereof in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY(1-36), NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects.
摘要翻译：本发明公开了一种治疗性处理动物（包括人）用于心身，抑郁和神经精神疾病如焦虑，抑郁，失眠，精神分裂症，癫痫，痉挛和慢性疼痛的方法。施用合适的吸引蛋白抑制剂导致哺乳动物脑中的酶吸引力或其同种型的活性降低，并导致神经肽Y（NPY）和类似底物的降解降低的因果结果。这种治疗将导致功能活跃的神经元NPY（1-36）的浓度降低或延迟。由于产生的内源性NPY（1-36）的稳定性增加，NPY活性延长，从而导致其它功能活性的NPY Y1受体活性，从而促进抗抑郁，抗焦虑，镇痛，抗高血压和其他神经功能。

15. 发明申请

WO2005074983A3 TREATMENT OF RHINITIS WITH ANTICHOLINERGICS ALONE IN COMBINATION WITH ANTIHISTAMINES PHOSPHODIESTERASE 4 INHIBITORS, OR CORTICOSTEROIDS 审中-公开
标题翻译：与抗生素相关的抗病毒药物与抗生素抑制剂4抑制剂或角质素化合物的治疗
公开(公告)号：WO2005074983A3
公开(公告)日：2006-04-13
申请号：PCT/EP2005000653
申请日：2005-01-24
申请人： SOFOTEC GMBH & CO KG , MAUS JOACHIM , PETZOLD URSULA , SZELENYI ISTVAN , HOFFMANN TORSTEN , WEINGART MARIO
发明人： MAUS JOACHIM , PETZOLD URSULA , SZELENYI ISTVAN , HOFFMANN TORSTEN , WEINGART MARIO
IPC分类号： A61K31/401 , A61K31/519 , A61K31/55 , A61K31/573 , A61K39/00 , A61K45/06 , A61P11/00
CPC分类号： A61K45/06 , A61K31/401 , A61K31/519 , A61K31/55 , A61K31/573 , A61K2300/00
摘要： The present invention provides novel combinations comprising a topical anticholinergic drug alone or in combination with topically administered antihistamines, topically or orally administered phosphodiesterase 4 inhibitors or topical corticosteroids for the treatment of rhinitis of various origins. It further comprises presentation of these combinations in locally applied formulations and includes various pharmaceutical formulations suitable for topical application, e.g. nasal sprays, nasal drops, emulsions, pastes, creams and gels.
摘要翻译：本发明提供新颖的组合，其包括单独的局部抗胆碱能药物或局部施用的抗组胺剂，局部或口服给予的磷酸二酯酶4抑制剂或局部皮质类固醇用于治疗各种原因的鼻炎。其还包括在局部施用的制剂中呈现这些组合，并且包括适用于局部应用的各种药物制剂，例如。鼻喷雾剂，滴鼻剂，乳剂，糊剂，霜剂和凝胶剂。

16. 发明申请

WO2013127539A3 PHARMACEUTICAL FORMULATION CONTAINING FLUPIRTIN 审中-公开
标题翻译：药物制剂含氟吡汀
公开(公告)号：WO2013127539A3
公开(公告)日：2013-12-19
申请号：PCT/EP2013000615
申请日：2013-03-01
申请人： MEDA PHARMA GMBH & CO KG , MOSCHNER KATRIN , HOFFMANN TORSTEN , WEINGART MARIO , HILDEBRAND-CYRENER ANNEGRET
发明人： MOSCHNER KATRIN , HOFFMANN TORSTEN , WEINGART MARIO , HILDEBRAND-CYRENER ANNEGRET
IPC分类号： A61K9/28 , A61K9/20 , A61K9/50 , A61K31/44
CPC分类号： A61K9/2866 , A61K9/2072 , A61K9/2813 , A61K9/2846 , A61K9/2853 , A61K31/135 , A61K31/44 , A61K45/06 , A61K2300/00
摘要： The invention relates to drug preparations with controlled active ingredient released in the form of microtablets which contain, as active ingredient, flupirtin or one of its physiologically compatible salts, and to processes for their production.
摘要翻译：本发明涉及一种具有在包含作为活性成分的氟吡汀或其生理学上可接受的盐和它们的制造过程中的一个微型片剂的形式的活性成分的受控释放的药物组合物。

17. 发明申请

WO2006089658A3 NK1 ANTAGONISTS 审中-公开
标题翻译： NK1拮抗剂
公开(公告)号：WO2006089658A3
公开(公告)日：2006-12-21
申请号：PCT/EP2006001310
申请日：2006-02-14
申请人： HOFFMANN LA ROCHE , HOFFMANN TORSTEN , SCHNIDER PATRICK
发明人： HOFFMANN TORSTEN , SCHNIDER PATRICK
IPC分类号： C07D213/75 , A61K31/44 , A61P25/18 , C07D213/82
CPC分类号： C07D213/75 , C07D213/82
摘要： The present invention relates to compounds of the formula (I), wherein R 1 /R 1' are hydrogen or methyl; X is -C(O)N(CH 3 )- or -N(CH 3 )C(O)-; and to pharmaceutically acceptable acid addition salts thereof for the treatment of numerous inflammatory conditions, migraine, rheumatoid arthritis, asthma, inflammatory bowel disease, mediation of the emetic reflex, Parkinson's disease, anxiety, depression, psychosis, motion sickness, induced vomiting, pain, headache, migraine, Alzheimer's disease, multiple sclerosis, attenuation of morphine withdrawal, cardiovascular changes, oedema, such as oedema caused by thermal injury, chronic inflammatory diseases such as rheumatoid arthritis, asthma/bronchial hyperreactivity and other respiratory diseases including allergic rhinitis, inflammatory diseases of the gut including ulcerative colitis and Crohn's disease, ocular injury and ocular inflammatory diseases, traumatic brain injury, motion sickness, emesis and psychoimmunologic or psychosomatic disorders.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 1，R 1'是氢或甲基; X是-C（O）N（CH 3） - 或-N（CH 3）C（O） - ; 及其药学上可接受的酸加成盐用于治疗许多炎性疾病，偏头痛，类风湿性关节炎，哮喘，炎性肠病，催吐反射介导，帕金森病，焦虑症，抑郁症，精神病，晕动病，诱发的呕吐，疼痛，头痛，偏头痛，阿尔茨海默病，多发性硬化症，吗啡戒断减弱，心血管改变，水肿如热损伤引起的水肿，慢性炎性疾病如类风湿性关节炎，哮喘/支气管高反应性和其他呼吸系统疾病，包括过敏性鼻炎，炎性疾病包括溃疡性结肠炎和克罗恩病，眼部损伤和眼部炎性疾病，创伤性脑损伤，晕动病，呕吐和精神免疫或心身疾病。

18. 发明申请

WO2012092373A3 IN VIVO POLYNUCLEOTIDE DELIVERY CONJUGATES HAVING ENZYME SENSITIVE LINKAGES 审中-公开
标题翻译：具有酶敏感性连接的生物多核苷酸转运途径
公开(公告)号：WO2012092373A3
公开(公告)日：2013-10-24
申请号：PCT/US2011067588
申请日：2011-12-28
申请人： ARROWHEAD RES CORP , ROZEMA DAVID B , LEWIS DAVID L , WAKEFIELD DARREN H , KITAS ERIC A , HADWIGER PHILIPP , WOLFF JON A , ROEHL INGO , MOHR PETER , HOFFMANN TORSTEN , JAHN-HOFMANN KERSTIN , MUELLER HANS MARTIN , OTT GUENTHER , BLOKHIN ANDREI V , CARLSON JEFFREY C , BENSON JONATHAN D
发明人： ROZEMA DAVID B , LEWIS DAVID L , WAKEFIELD DARREN H , KITAS ERIC A , HADWIGER PHILIPP , WOLFF JON A , ROEHL INGO , MOHR PETER , HOFFMANN TORSTEN , JAHN-HOFMANN KERSTIN , MUELLER HANS MARTIN , OTT GUENTHER , BLOKHIN ANDREI V , CARLSON JEFFREY C , BENSON JONATHAN D
IPC分类号： A61K48/00 , A61K31/675
CPC分类号： C07K5/06034 , A61K47/58 , A61K47/60 , C07K5/06078 , C07K5/06104 , C07K5/06113 , C12N15/111 , C12N15/87 , C12N2310/14 , C12N2310/3513 , C12N2320/32 , C12N2800/95 , C12N2810/10
摘要： The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.
摘要翻译：本发明涉及用于将RNA干扰（RNAi）多核苷酸递送至细胞体内的组合物。组合物包含用酶切割二肽 - 氨基苄基 - 碳酸酯掩蔽剂可逆地修饰的两亲膜活性多胺。改性掩盖聚合物的膜活性，而可逆性提供生理反应性。可逆修饰的多胺（动态多偶联物或DPC）进一步与RNAi多核苷酸共价连接或与靶向RNAi多核苷酸靶向分子缀合物共同施用。

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