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11. 发明授权

US07368576B2 Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents 失效
标题翻译：二肽基肽酶IV抑制剂及其用途作为抗癌剂
公开(公告)号：US07368576B2
公开(公告)日：2008-05-06
申请号：US11481349
申请日：2006-07-05
申请人： Stephan von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
发明人： Stephan von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
IPC分类号： C07D277/04 , C07D277/16 , C07D277/18 , C07D291/02 , C07D291/04
CPC分类号： A61K31/401 , A61K31/426 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55
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。

12. 发明授权

US07335645B2 Effectors of dipeptidyl peptidase IV for topical use 失效
标题翻译：二肽基肽酶IV用于局部使用的作用
公开(公告)号：US07335645B2
公开(公告)日：2008-02-26
申请号：US11069926
申请日：2005-03-01
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
IPC分类号： A61K38/00 , A61K31/33
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。

13. 发明授权

US07166579B2 Prodrugs of DP IV-inhibitors 有权
标题翻译： DP IV抑制剂的前药
公开(公告)号：US07166579B2
公开(公告)日：2007-01-23
申请号：US10735582
申请日：2003-12-11
申请人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
发明人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
IPC分类号： A61K38/05 , A61K38/04
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06173 , C07K5/0806 , C07K5/0808 , C07K5/0823
摘要： Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
摘要翻译：丝氨酸肽酶二肽基肽酶IV的不稳定抑制剂的前药化合物用于治疗各种疾病，特别是代谢紊乱。前药化合物可用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病。

14. 发明授权

US07060719B2 Glutaminyl based DPIV inhibitors 有权
标题翻译：基于谷氨酰胺基的DPIV抑制剂
公开(公告)号：US07060719B2
公开(公告)日：2006-06-13
申请号：US10779158
申请日：2004-02-13
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
IPC分类号： A61K31/425 , A61K31/40 , C07D277/04 , C07D207/00
CPC分类号： C07D277/04 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D295/185 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K7/06
摘要： The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
摘要翻译：本发明提供下式的化合物：其中X = CH 2或S或其药学上可接受的盐可用于治疗由DPIV或DPIV样酶如关节炎，肥胖，免疫和自身免疫介导的病症疾病，同种异体移植，癌症，神经元疾病和皮肤疾病。

15. 发明申请

US20060100253A1 Novel compounds for the treatment of neurological disorders 失效
标题翻译：用于治疗神经障碍的新型化合物
公开(公告)号：US20060100253A1
公开(公告)日：2006-05-11
申请号：US11290735
申请日：2005-11-30
申请人： Andre Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
IPC分类号： A61K31/427 , C07D417/14
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention relates to novel inhibitors of prolyl endopeptidase of formula 1 W—KCONH—X—CON—Y—CO—Z (1) wherein K, W, X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer's disease, Down Syndrome, Parkinson disease and Chorea Huntington.
摘要翻译：本发明涉及式1的脯氨酰内肽酶的新型抑制剂<？in-line-formula description =“In-line Formulas”end =“lead”→> W-KCONH-X-CON-Y-CO-Z ）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中K，W，X，Y和Z在说明书中规定。该化合物可用于治疗诸如轻度认知障碍（MCI），阿尔茨海默病，唐氏综合症，帕金森病和霍乱金淋巴瘤等疾病。

16. 发明申请

US20050233978A1 Novel inhibitors of dipeptidyl peptidase I 失效
公开(公告)号：US20050233978A1
公开(公告)日：2005-10-20
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： C07K5/06 , A61K38/04 , C07K5/04
CPC分类号： C07K5/06026 , C07K5/06
摘要： The present invention relates to new compounds that act as specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I). Those compounds are represented by the general formula and the pharmaceutical salts thereof, in which R is an acyl-residue including urethane and 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 may be optionally substituted, or is H, 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 my be optionally substituted, or is H.

17. 发明申请

US20050222221A1 Method for the improvement of islet signaling in diabetes mellitus and for its prevention 审中-公开
公开(公告)号：US20050222221A1
公开(公告)日：2005-10-06
申请号：US10676832
申请日：2003-10-01
申请人： Hans-Ulrich Demuth , Konrad Glund
发明人： Hans-Ulrich Demuth , Konrad Glund
IPC分类号： C07D277/04 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/425 , A61K31/426 , A61K38/00 , A61K45/00 , A61K45/06 , A61P3/10 , A61P5/50 , A61P19/02 , A61P29/00 , A61P31/18 , A61P37/06 , A61P43/00
CPC分类号： A61K45/06 , A61K31/00 , A61K31/40 , A61K31/426 , Y10S514/866
摘要： The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic β-cells and to cause differentiation of pancreatic epithelial cells into insulin producing β-cells. Oral administration a DP IV inhibitor causes the active form of GLP-1 to be preserved longer under physiological conditions. The extended presence of GLP-1, in particular in the pancreatic tissue facilitates differentiation and regeneration of the β-cells already present that are in need of repair. These repaired insulin producing cells can contribute to the correction and maintenance of normal physiological glycemic levels.

18. 发明授权

US06890905B2 Methods for improving islet signaling in diabetes mellitus and for its prevention 失效
标题翻译：改善糖尿病胰岛信号的方法及其预防
公开(公告)号：US06890905B2
公开(公告)日：2005-05-10
申请号：US10216349
申请日：2002-08-09
申请人： Hans-Ulrich Demuth , Konrad Glund , Andrew J. Pospisilik , Kerstin Kuehn-Wache
发明人： Hans-Ulrich Demuth , Konrad Glund , Andrew J. Pospisilik , Kerstin Kuehn-Wache
IPC分类号： A61K31/40 , A61K31/426 , A61K38/00 , A61K31/425 , A61K31/70
CPC分类号： A61K31/40 , A61K31/426
摘要： The present invention discloses methods for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic β-cells, to cause differentiation of pancreatic epithelial cells into insulin producing β-cells, to improve muscle sensitivity to insulin and other weight control efforts by the chronic oral administration of a DP IV-inhibitor. The administration causes the active form of GLP-1 and other non-nutrient stimulated growth hormones to remain biologically active longer under physiological conditions. The extended presence of such hormones, in particular in the pancreatic tissue can also facilitate differentiation and regeneration of the β-cells already present that are in need of repair.
摘要翻译：本发明公开了用于治疗性治疗哺乳动物（包括但不限于人）的方法，以增加内源性胰腺β-细胞的相对胰岛素产生性能，使胰腺上皮细胞分化为产生胰岛素的β细胞，以改善肌肉对胰岛素和其他体重控制努力通过慢性口服给予DP IV抑制剂。在生理条件下，给药导致GLP-1和其他非营养刺激生长激素的活性形式在生物活性更长的时间内保持生物活性。这种激素，特别是胰腺组织的延长存在也可促进已经存在的需要修复的β细胞的分化和再生。

19. 发明申请

US20050014946A1 Substituted amino ketone compounds 审中-公开
标题翻译：取代的氨基酮化合物
公开(公告)号：US20050014946A1
公开(公告)日：2005-01-20
申请号：US10914261
申请日：2004-08-09
申请人： Hans-Ulrich Demuth , Ulrich Heiser , Torsten Hoffmann , Andre Niestroj
发明人： Hans-Ulrich Demuth , Ulrich Heiser , Torsten Hoffmann , Andre Niestroj
IPC分类号： A61K31/4439 , A61K31/4709 , A61K31/675 , C07D211/82 , C07D217/12 , C07F9/28
CPC分类号： A61K31/4439 , A61K31/4709 , A61K31/675 , C07D211/82 , C07D217/12 , C07F9/28
摘要： The present invention relates to compounds of the general formula I B—(CH—R1)n—C(═X2)-D (I) and pharmaceutically acceptable salts thereof including stereoisomers, to the use of the compounds for the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidosis, diabetes mellitus, diabetic neuropathy and nephropathy and of sequelae caused by diabetes mellitus in mammals.
摘要翻译：本发明涉及通式I B-（CH-R 1）n C（= X 2）-D（I）的化合物及其药学上可接受的盐，包括立体异构体，用于治疗糖耐量异常，糖尿病，高脂血症，代谢性酸中毒，糖尿病，糖尿病性神经病变和肾病以及哺乳动物糖尿病引起的后遗症。

20. 发明授权

US06725586B2 Self-cleaning iron 失效
标题翻译：自清铁
公开(公告)号：US06725586B2
公开(公告)日：2004-04-27
申请号：US10380268
申请日：2003-03-12
申请人： Roger Horcher , Klaus Maier , Ulrich Demuth
发明人： Roger Horcher , Klaus Maier , Ulrich Demuth
IPC分类号： D06F7518
CPC分类号： D06F75/18
摘要： The invention concerns a flash iron comprising a water reservoir (2), a flash chamber (32) and a drip device having an axially mobile rod (4) whereof the total stroke comprises a first travel enabling the steam to flow towards the orifice (520) of a module (5) and a second travel moving the module (5) by opening a wider orifice (220) for water passing from the reservoir (2) to the flash chamber (32). The invention is characterised in that the tightness between the reservoir (2), the module (5) and the flash chamber (32) is provided by a first compressed seal, and the tightness between the rod and the module is provided by a second compressed seal, the two seals being parts of one and the same elastomeric component (52) borne by the module (5).
摘要翻译：本发明涉及一种闪蒸铁，其包括储水器（2），闪蒸室（32）和具有轴向活动杆（4）的滴水装置，其中总行程包括使蒸汽能够朝向孔口流动的第一行程（520 ）和通过打开用于水从储存器（2）流到闪蒸室（32）的水的更宽的孔口（220）来移动模块（5）的第二行程。本发明的特征在于，储存器（2），模块（5）和闪蒸室（32）之间的紧密性由第一压缩密封件提供，并且杆和模块之间的紧密度由第二压缩两个密封件是由模块（5）承载的同一弹性体部件（52）的部件。

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