-
公开(公告)号：US20050209159A1
公开(公告)日：2005-09-22
申请号：US11069926
申请日：2005-03-01
IPC分类号： A61K9/06 , A61K8/49 , A61K8/72 , A61K9/08 , A61K9/107 , A61K9/12 , A61K9/70 , A61K9/72 , A61K31/765 , A61K38/00 , A61K47/48 , A61P1/02 , A61P3/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07K5/037 , C07K5/06 , C07K5/072 , C07K5/083 , C07K5/113 , C07K7/06 , C07K7/08 , C08G65/329 , A61K38/10 , A61K38/08
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06104 , C07K5/0806 , C07K7/08 , C08G65/329
摘要： The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain; B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.
摘要翻译： 本发明涉及用于局部影响以下通式的二肽基肽酶的活性的化合物：其中A是在侧链中具有至少一个官能团的氨基酸; B是与A的侧链官能团共价结合的化合物，选自（a）链长达20个氨基酸的寡肽，（b）由多达6个氨基酸组成的甘氨酸均聚物 甘氨酸单体，和（c）摩尔质量高达20 000g / mol的聚乙二醇; 和C是选自噻唑烷，吡咯烷，氰基吡咯烷，羟脯氨酸，脱氢脯氨酸或哌啶的酰胺键合的基团。 本发明进一步涉及所述化合物在局部免疫学过程（趋化性，炎性过程，自身免疫性疾病）中的靶向干预的用途，以及与之相关的病理生理和生理过程的有效和靶向治疗（牛皮癣，牙周炎，关节炎，过敏， 炎症），特别是。
-
公开(公告)号：US20050176622A1
公开(公告)日：2005-08-11
申请号：US10667200
申请日：2003-09-18
申请人： Kerstin Kuhn-Wache , Joachim Bar , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
发明人： Kerstin Kuhn-Wache , Joachim Bar , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
IPC分类号： A61K31/155 , A61K31/175 , A61K31/401 , A61K31/455 , A61K31/704 , A61K38/00 , A61K38/08 , A61K38/22 , A61K38/28 , A61P3/00 , C07K7/06 , C12Q1/37
CPC分类号： A61K31/401 , A61K38/00 , C07K7/06 , C12Q1/37 , G01N2500/04
摘要： The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.
摘要翻译： 本申请涉及二肽基肽酶IV的二级结合位点，其与底物之间的关系以及二肽基肽酶IV（DP IV，同义词：DPP IV，CD26，EC 3.4.14.5）的底物特异性的调节。 本申请还涉及结合DP IV的二级结合位点的化合物及其用于调节DP IV的底物特异性的用途; 各种DP IV介导的病症的治疗方法; 以及用于鉴定DP IV和DP IV样酶的二级结合位点的筛选方法。
-
公开(公告)号：US20050171112A1
公开(公告)日：2005-08-04
申请号：US11002169
申请日：2004-12-02
申请人： Ingo Schulz , Stephan Schilling , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth , Steffen Rossner
发明人： Ingo Schulz , Stephan Schilling , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth , Steffen Rossner
IPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04
CPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04 , A61K2300/00
摘要： The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, LiCl, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.
摘要翻译： 本发明提供在哺乳动物例如人中治疗神经元疾病的方法，该方法包括施用有效的，无毒的和药学上可接受量的至少一种QC抑制剂，任选地与至少一种 选自PEP抑制剂，LiCl，DP IV / DP IV类酶的抑制剂，NPY受体配体，NPY激动剂，NPY拮抗剂，ACE抑制剂，PIMT增强剂，β分泌酶抑制剂，抑制剂 γ-分泌酶和中性肽链内切酶抑制剂。
-
54.发明授权公开(公告)号：US08945510B2
公开(公告)日：2015-02-03
申请号：US13479826
申请日：2012-05-24
IPC分类号： A61K51/04 , A61K31/415 , C07D403/10
CPC分类号： A61K51/0453 , C07B59/002
摘要： Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.
摘要翻译： 放射性标记的谷氨酰胺酶（QC）抑制剂作为成像剂，特别地但不排他地作为用于检测神经障碍的医学成像剂; 以及使用放射性标记的抑制剂的用于检测神经系统疾病的药物组合物，方法和试剂盒。
-
公开(公告)号：US20120301398A1
公开(公告)日：2012-11-29
申请号：US13479826
申请日：2012-05-24
IPC分类号： C07D403/10 , G01N33/53 , A61K51/04
CPC分类号： A61K51/0453 , C07B59/002
摘要： Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.
摘要翻译： 放射性标记的谷氨酰胺酶（QC）抑制剂作为成像剂，特别地但不排他地作为用于检测神经障碍的医学成像剂; 以及使用放射性标记的抑制剂的用于检测神经系统疾病的药物组合物，方法和试剂盒。
-
公开(公告)号：US07897633B2
公开(公告)日：2011-03-01
申请号：US11923307
申请日：2007-10-24
IPC分类号： A61K31/417 , A61K31/4164 , C07D233/61
CPC分类号： A61K31/4164 , C07D233/54 , C07D235/06 , C07D403/12 , C07D405/12 , C07D417/12
摘要： The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
摘要翻译： 本发明涉及谷氨酰胺酰基环化酶的新型抑制剂及其组合，用于治疗神经元疾病，特别是阿尔茨海默病，唐氏综合征，帕金森病，霍乱金淋巴瘤，致病精神病，精神分裂症，食物摄入受损，睡眠觉醒，内稳态调节障碍 能量代谢受损，自主神经功能障碍，体内受损的调节，体液，高血压，发热，睡眠失调，厌食，焦虑相关障碍，包括抑郁症，癫痫发作，药物戒断和酒精中毒，神经变性障碍，包括认知功能障碍和痴呆。
-
公开(公告)号：US07816325B2
公开(公告)日：2010-10-19
申请号：US11478217
申请日：2006-06-29
申请人： Kerstin Kühn-Wache , Joachim Bär , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
发明人： Kerstin Kühn-Wache , Joachim Bär , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
IPC分类号： A61K38/08 , A61K39/395
CPC分类号： A61K31/401 , A61K38/00 , C07K7/06 , C12Q1/37 , G01N2500/04
摘要： The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.
摘要翻译： 本申请涉及二肽基肽酶IV的二级结合位点，其与底物之间的关系以及二肽基肽酶IV（DP IV，同义词：DPP IV，CD26，EC 3.4.14.5）的底物特异性的调节。 本申请还涉及结合DP IV的二级结合位点的化合物及其用于调节DP IV的底物特异性的用途; 各种DP IV介导的病症的治疗方法; 以及用于鉴定DP IV和DP IV样酶的二级结合位点的筛选方法。
-
公开(公告)号：US20100159032A1
公开(公告)日：2010-06-24
申请号：US12630760
申请日：2009-12-03
申请人： Ingo Schulz , Stephan Schilling , Hans-Ulrich Demuth , Ulrich Heiser , Andre Johannes Niestroj , Steffen Rossner
发明人： Ingo Schulz , Stephan Schilling , Hans-Ulrich Demuth , Ulrich Heiser , Andre Johannes Niestroj , Steffen Rossner
IPC分类号： A61K33/14 , A61K31/335 , A61K38/05 , A61K31/16 , A61K31/27 , A61P25/28 , A61P25/16 , A61P25/18 , A61P3/04 , A61P25/20 , A61P3/00 , A61P5/00 , A61P9/12 , A61P29/00 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/30 , A61P25/32 , A61K31/4985
CPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04 , A61K2300/00
摘要： The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, LiCl, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.
摘要翻译： 本发明提供在哺乳动物例如人中治疗神经元疾病的方法，该方法包括施用有效的，无毒的和药学上可接受量的至少一种QC抑制剂，任选地与至少一种 选自PEP抑制剂，LiCl，DP IV / DP IV类酶的抑制剂，NPY受体配体，NPY激动剂，NPY拮抗剂，ACE抑制剂，PIMT增强剂，β分泌酶抑制剂，抑制剂 γ-分泌酶和中性肽链内切酶抑制剂。
-
59.发明授权Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease 有权使用谷氨酰胺酰环化酶抑制剂治疗和预防疾病公开(公告)号：US07381537B2
公开(公告)日：2008-06-03
申请号：US10839017
申请日：2004-05-05
IPC分类号： C12Q1/34
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，这种效应物的筛选方法，以及包含这些效果子的这种效应物和药物组合物的用途，用于治疗 可以通过调节QC活性来治疗。 优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。
-
60.发明授权Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis 失效二肽基肽酶IV抑制剂在多发性硬化症的治疗中的应用公开(公告)号：US07368421B2
公开(公告)日：2008-05-06
申请号：US10126374
申请日：2002-04-19
IPC分类号： A61K38/00 , A61K38/02 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , C07K2/00 , C07K7/04 , C07K5/02 , C07K5/08 , C07K5/10
CPC分类号： C07K7/06 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D277/04 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in treating conditions mediated by DP IV or DP IV-like enzymes, such as immune, autoimmune or central nervous system disorder selected from the group consisting of strokes, tumors, ischemia, Parkinson's disease and migraines. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of multiple sclerosis.
摘要翻译： 本发明提供DPIV-抑制剂的新用途。 本发明的化合物及其相应的药学上可接受的酸加成盐形式可用于治疗由DP IV或DP IV样酶介导的病症，例如免疫，自身免疫或中枢神经系统疾病，其选自中风 ，肿瘤，局部缺血，帕金森病和偏头痛。 在更优选的实施方案中，本发明的化合物可用于治疗多发性硬化。
-
-
-
-
-
-
-
-
-
搜索结果
91 条记录 (耗时 0.06 秒)
