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61. 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。

62. 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。

63. 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。

64. 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.

65. 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。

66. 发明授权

US08716296B2 Inhibitors of protein kinases 失效
标题翻译：蛋白激酶抑制剂
公开(公告)号：US08716296B2
公开(公告)日：2014-05-06
申请号：US12226286
申请日：2008-10-13
申请人： Hans Allgeier , Martin Augustin , Anke Müller , Lutz Zeitlmann , Andreas Marquardt , Michael A. Pleiss , Ulrich Heiser , André Johannes Niestroj
发明人： Hans Allgeier , Martin Augustin , Anke Müller , Lutz Zeitlmann , Andreas Marquardt , Michael A. Pleiss , Ulrich Heiser , André Johannes Niestroj
IPC分类号： A01N43/54 , C07D401/00
CPC分类号： C07D403/12 , C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： Compounds of general formula (I): are useful as inhibitors of cyclin dependent kinases such as CDK9.
摘要翻译：通式（I）的化合物：可用作细胞周期依赖性激酶如CDK9的抑制剂。

67. 发明申请

US20120237475A1 Novel Inhibitors 有权
标题翻译：新型抑制剂
公开(公告)号：US20120237475A1
公开(公告)日：2012-09-20
申请号：US13422619
申请日：2012-03-16
申请人： Ulrich Heiser , Daniel Ramsbeck
发明人： Ulrich Heiser , Daniel Ramsbeck
IPC分类号： A61K38/20 , A61K31/4184 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/454 , C07D417/14 , A61K31/541 , C07D405/14 , C07D409/14 , C07D403/14 , A61K31/496 , A61K33/14 , A61K39/395 , A61K38/21 , A61K31/4409 , A61K38/10 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/22 , A61P25/18 , A61P37/02 , A61P37/06 , A61P1/04 , A61P35/00 , A61P31/04 , A61P15/08 , A61P29/00 , A61P35/04 , A61P17/06 , A61P37/00 , A61P3/00 , A61P5/00 , A61P7/00 , A61P25/28 , A61P19/02 , A61P9/10 , A61P1/18 , A61P9/00 , C07D403/10
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
摘要翻译：式（I）的新型杂环衍生物：或其药学上可接受的盐，溶剂化物或多晶型物，包括其所有互变异构体和立体异构体，其中R a，n，R 1和R 2如本文所定义，作为谷氨酰胺酰环化酶抑制剂（QC，EC2.3 .2.5）。

68. 发明申请

US20100273835A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：US20100273835A1
公开(公告)日：2010-10-28
申请号：US12665502
申请日：2008-07-10
申请人： Ulrich Heiser , Andre J. Niestroj , Ingo Schulz
发明人： Ulrich Heiser , Andre J. Niestroj , Ingo Schulz
IPC分类号： A61K31/4402 , C07D277/68 , A61K31/428 , C07D333/38 , A61K31/381 , C07D277/56 , A61K31/427 , C07D213/78 , C07D307/68 , A61K31/341 , C07D403/06 , A61K31/404 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/24 , A61P9/00 , A61P7/02
CPC分类号： C07C271/22 , C07D213/50 , C07D277/24 , C07D277/64 , C07D307/46 , C07D333/22 , C07D333/56 , C07D417/06
摘要： The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims.The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.
摘要翻译：本发明提供了通式（I）的化合物或其药学上可接受的盐，多晶型物或溶剂化物，包括其互变异构体和立体异构体，其中K，W，X; 在整个说明书和权利要求书中描述了Y和Z。本发明的化合物可用作脯氨酰内肽酶（PEP，EC 3.4.21.26）和/或IL-6的抑制剂。

69. 发明申请

US20100099721A1 NOVEL COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗神经疾病的新型化合物
公开(公告)号：US20100099721A1
公开(公告)日：2010-04-22
申请号：US12646111
申请日：2009-12-23
申请人： André J. Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
发明人： André J. Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
IPC分类号： A61K31/428 , A61K31/426 , A61K31/4025 , A61P25/00 , A61P9/10 , A61P7/00
CPC分类号： A61K31/4025 , A61K31/426 , A61K31/428 , A61K45/06 , A61K2300/00
摘要： 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：式1中的脯氨酰内肽酶的抑制剂W-KCONH-X-CON-Y-CO-Z（1）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。

70. 发明授权

US07625939B2 Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase IV inhibitors 失效
标题翻译：环丙基稠合吡咯烷衍生物作为二肽基肽酶IV抑制剂
公开(公告)号：US07625939B2
公开(公告)日：2009-12-01
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： A61K31/40 , C07D209/00
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。

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