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81. 发明申请

US20110092501A1 NOVEL INHIBITORS 有权
标题翻译：新型抑制剂
公开(公告)号：US20110092501A1
公开(公告)日：2011-04-21
申请号：US12880369
申请日：2010-09-13
申请人： Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
发明人： Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
IPC分类号： A61K31/535 , C07D403/02 , A61K31/4184 , A61K31/454 , C07D401/02 , C07D413/14 , C07D471/04 , A61K31/437 , A61P35/00 , A61P29/00 , A61P25/00 , A61P35/04 , A61P3/00 , A61P5/00
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K45/06 , C07D235/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
摘要翻译：本发明涉及式（I）的新型吡咯烷衍生物：其中R1，R2和R3如本文所定义，作为谷氨酰胺酰环化酶抑制剂（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。

82. 发明授权

US07897633B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US07897633B2
公开(公告)日：2011-03-01
申请号：US11923307
申请日：2007-10-24
申请人： Stephan Schilling , Mirko Buchholz , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
发明人： Stephan Schilling , Mirko Buchholz , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
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。

83. 发明授权

US07816325B2 Secondary binding site of dipeptidyl peptidase IV (DP IV) 有权
标题翻译：二肽基肽酶IV（DP IV）的二级结合位点
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。

84. 发明申请

US20100159032A1 COMBINATIONS USEFUL FOR THE TREATMENT OF NEURONAL DISORDERS 审中-公开
标题翻译：用于治疗神经疾病的组合
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。

85. 发明申请

US20100119475A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20100119475A1
公开(公告)日：2010-05-13
申请号：US12554611
申请日：2009-09-04
申请人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
发明人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
IPC分类号： A61K31/4184 , C07D417/14 , C07D403/10 , C07D405/14 , C07D471/04 , A61K31/433 , A61K31/4439 , A61K39/395 , A61K38/20 , A61K38/21 , A61P35/00 , A61P3/00 , A61P25/00
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.
摘要翻译：通式（I）的化合物：其中R1，R2，R3，R4，X和Y如本文所定义，是谷氨酰胺酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰胺酰环化酶活性治疗的病症。

86. 发明申请

US20080293618A1 CYCLOPROPYL-FUSED PYRROLIDINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE IV INHIBITORS 失效
标题翻译：作为DIPEPTIDYL PEPTIDASE IV抑制剂的环丙基 - 氟化吡咯烷衍生物
公开(公告)号：US20080293618A1
公开(公告)日：2008-11-27
申请号：US12120595
申请日：2008-05-14
申请人： Ulrich Heiser , Andre J. Niestroj , Ulf-Torsten Gaertner , Hans-Ulrich Demuth
发明人： Ulrich Heiser , Andre J. Niestroj , Ulf-Torsten Gaertner , Hans-Ulrich Demuth
IPC分类号： A61K31/403 , C07D209/52 , A61K31/69 , A61K31/7088 , A61P3/00 , A61P35/00 , A61K38/28 , C07F5/02
CPC分类号： C07F5/025
摘要： The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.
摘要翻译：本发明涉及用于治疗和/或预防包括癌症和肿瘤在内的哺乳动物疾病，转移和肿瘤定植的式（1）的DP IV抑制剂; 和代谢疾病。

87. 发明授权

US07381537B2 Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease 有权
标题翻译：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
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre J. Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre J. Niestroj , Stephan Schilling , Ulrich Heiser
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。

88. 发明授权

US07368421B2 Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis 失效
标题翻译：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
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Konrad Glund , Ulrich Heiser , Stephan von Hoersten
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Konrad Glund , Ulrich Heiser , Stephan von Hoersten
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。

89. 发明授权

US07144856B2 Inhibitors of dipeptidyl peptidase I 失效
公开(公告)号：US07144856B2
公开(公告)日：2006-12-05
申请号：US10997821
申请日：2004-11-24
申请人： Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
IPC分类号： A61K38/05 , C07K5/06
CPC分类号： C07K5/06026 , C07K5/06
摘要： The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I)which can be used in the treatment of malignant cell degeneration, immune diseases impaired wound healing and metabolic diseases of humans and are represented by the general formula and the pharmaceutical salts thereof, in which R is a peptide or a branched or unbranched C1–C9 alkyl chain, a branched or unbranched C2–C9 alkenyl chain, a branched or unbranched C2–C9 alkynyl chain, a C3–C9 cycloalkyl, C4–C9 carbocyclic, C5–C14 aryl, C3–C9 heteroaryl, C3–C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R′ is a branched or unbranched C1–C9 alkyl chain, a branched or unbranched C2–C9 alkenyl chain, a branched or unbranched C2–C9 alkynyl chain, a C3–C9 cycloalkyl, C4–C9 cycloalkenyl, C2–C9 heterocycloalkyl, C3–C9 heterocycloalkenyl, C5–C14 aryl, C3–C9 heteroaryl, C3–C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues may be optionally substituted, or is H.

90. 发明申请

US20060178315A1 Irreversible cysteine protease inhibitors of legumain 失效
标题翻译：不可逆的半胱氨酸蛋白酶抑制剂
公开(公告)号：US20060178315A1
公开(公告)日：2006-08-10
申请号：US10485723
申请日：2002-07-23
申请人： Andre Niestroj , Ulrich Heiser , Bernd Gerhartz , Matthias Hoffmann , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Bernd Gerhartz , Matthias Hoffmann , Hans-Ulrich Demuth
IPC分类号： A61K38/04 , C07K5/04 , C07D403/02
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0806
摘要： Presented are compounds represented by the following general formulas (I) and (II), for inhibiting cysteine protease legumain for modulating associated disease states in subjects.
摘要翻译：提出了由以下通式（I）和（II）表示的化合物，其用于抑制半胱氨酸蛋白酶调节因子用于调节受试者中的相关疾病状态。

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