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1. 发明专利

JP2012031170A Novel compounds for medical use as peptidase effectors 审中-公开
标题翻译：用于医学用途的新型化合物作为肽类效应物
公开(公告)号：JP2012031170A
公开(公告)日：2012-02-16
申请号：JP2011162967
申请日：2011-07-26
申请人： Imtm Gmbh , イーエムテーエムゲーエムベーハー
发明人： ANSORGE SIEGFRIED , BANK UTE , HEIMBURG ANTJE , JULIUS HEIKO , NORDHOFF CARSTEN , TAEGER MICHAEL
IPC分类号： C07C237/10 , A61K8/42 , A61K8/44 , A61K8/46 , A61K8/49 , A61K8/58 , A61K31/165 , A61K31/167 , A61K31/18 , A61K31/221 , A61K31/27 , A61K31/405 , A61K31/4245 , A61K31/425 , A61K31/427 , A61K31/4418 , A61K31/505 , A61K31/52 , A61K31/695 , A61K45/00 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P19/02 , A61P21/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P33/06 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , A61Q19/00 , C07C271/20 , C07C311/32 , C07C311/35 , C07C311/41 , C07D209/08 , C07D209/20 , C07D213/30 , C07D213/56 , C07D239/26 , C07D271/12 , C07D277/04 , C07D417/12 , C07D473/00 , C07F7/18
CPC分类号： C07D473/00 , C07C237/20 , C07C237/22 , C07C237/34 , C07C271/22 , C07C311/47 , C07D209/08 , C07D209/20 , C07D213/55 , C07D213/56 , C07D239/20 , C07D239/26 , C07D271/12 , C07D277/04 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a novel compound which can concertedly inhibit ectoenzymes dipeptidyl peptidase IV (DPIV) and alanyl aminopeptidase (APN) cooperatively.SOLUTION: The compound is a compound of formula (I) or an acid addition salt with an organic acid and/or inorganic acid. (In the formula, residues R1, R2, R3 and R4 may be the same or different, -H, >C(=O), -C(=O)O- and the like; E represents -O-, -S-, -NH- and the like; Y represents -O-, -NH- and the like; B represents an alkyl substituted group or an alkoxy substituted group having an aryl group or a heterocyclic ring; and C represents a substitution group having amide bond or sulfonamide bond).
摘要翻译：要解决的问题：提供一种能够协同抑制二肽基肽酶IV（DPIV）和丙氨酰氨基肽酶（APN）的新型化合物。化合物是式（I）的化合物或与有机酸和/或无机酸的酸加成盐。（式中，残基R1，R2，R3和R4可以相同或不同，-H，> C（= O），-C（= O）O-等; E表示-O - ， - S - ，-NH-等; Y表示-O-，-NH-等; B表示烷基取代基或具有芳基或杂环的烷氧基取代基; C表示具有酰胺的取代基键或磺酰胺键）。版权所有（C）2012，JPO＆INPIT

2. 发明申请

WO02096398A3 MEDICAMENT CONTAINING AN EFFECTOR OF THE GLUTATHIONE METABOLISM TOGETHER WITH DOLLAR G(A)-LIPOIC ACID FOR TREATING DIABETES MELLITUS 审中-公开
标题翻译： DRUGS含有DOLLAR G（A）硫辛酸谷胱甘肽ZUSSAMMEN的效应糖尿病的治疗下
公开(公告)号：WO02096398A3
公开(公告)日：2003-02-27
申请号：PCT/EP0205811
申请日：2002-05-27
申请人： ESPARMA GMBH , IMTM GMBH , TAEGER MICHAEL , ANSORGE SIEGFRIED , FRIES GERHARD , KOEGST DIETER
发明人： TAEGER MICHAEL , ANSORGE SIEGFRIED , FRIES GERHARD , KOEGST DIETER
IPC分类号： C07D207/16 , A61K31/136 , A61K31/137 , A61K31/36 , A61K31/385 , A61K31/401 , A61K31/403 , A61K38/55 , A61K45/00 , A61P3/10 , A61P43/00 , A61K31/40 , A61K31/135
CPC分类号： A61K31/385 , A61K31/136 , A61K31/36 , A61K31/401 , A61K31/403 , A61K2300/00
摘要： The invention relates to a medicament containing an effector of the glutathione metabolism together with alpha -lipoic acid for treating diabetes mellitus. This medicament enables disturbances of the thiol-disulfide status or those that occur, for example, in diabetes mellitus to be treated simultaneously, separately or in a temporally graduated manner.
摘要翻译：本发明涉及包含谷胱甘肽代谢的效应与在糖尿病的治疗中的上下文α-硫辛酸一起药物。该药物的糖尿病的干扰可以同时发生，被单独处理或在时间上交错。

3. 发明申请

WO2005037257A3 NOVEL ALANYL-AMINO PEPTIDASE INHIBITORS FOR FUNCTIONALLY INFLUENCING DIFFERENT CELLS AND TREATING IMMUNOLOGICAL, INFLAMMATORY, NEURONAL, AND OTHER DISEASES 审中-公开
标题翻译：新丙氨酰氨酶抑制剂对不同细胞分泌功能的影响和治疗免疫性炎症，神经和其他疾病
公开(公告)号：WO2005037257A3
公开(公告)日：2006-09-14
申请号：PCT/EP2004011643
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG , ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL , STRIGGOW FRANK
发明人： ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL , STRIGGOW FRANK
IPC分类号： A61K31/00 , A61K31/4015 , C07C259/06 , C07C317/44 , C07C325/02 , C07C327/48 , C07D207/46 , C07D221/14 , C07D233/90 , C07D241/52 , C07D253/06 , C07D257/04 , C07D261/20 , C07D307/46 , C07D323/00 , C07D333/36 , C07D339/08 , C07D405/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D487/04 , C07D513/04 , C07F9/53
CPC分类号： C07C327/48 , C07C259/06 , C07C317/44 , C07C325/02 , C07C2601/10 , C07C2601/14 , C07D207/46 , C07D221/14 , C07D233/90 , C07D241/52 , C07D253/06 , C07D257/04 , C07D261/20 , C07D307/46 , C07D323/00 , C07D333/36 , C07D339/08 , C07D405/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D487/04 , C07D513/04 , C07F9/5333
摘要： The invention relates to medicinally used substances which specifically inhibit peptidases splitting ala-p-nitroanilide. The invention further relates to the use of at least one such substance or at least one pharmaceutical or cosmetic composition containing such a substance for preventing and treating diseases, especially diseases with an overshooting immune response (autoimmune diseases, allergies, and transplant rejections), other chronic inflammatory diseases, neuronal diseases, brain damages, skin diseases (acne and psoriasis, among others), tumor diseases, and special viral infections (including SARS).
摘要翻译：本发明涉及特异性抑制丙氨酸 - 对硝基苯胺裂解肽酶，用于药物中的物质。此外，本发明涉及使用在这样的物质或至少一个的至少至少一个这样的药物或化妆品组合物用于治疗疾病的预防和治疗，特别是用于治疗疾病与过冲从其他的免疫应答（自身免疫性疾病，变态反应和移植排斥），慢性预防和治疗物质容纳 -entzündlichen疾病，神经疾病和脑损伤，皮肤疾病（特别是痤疮和牛皮癣），肿瘤疾病和特定的病毒感染（包括SARS）。

4. 发明申请

WO2005034940A8 Dual alanyl Aminopeptidase and dipeptidyl peptidase IV inhibitors for functionally influencing different cells and for treating immunological, inflammatory, neuronal and other disease 审中-公开
标题翻译：双丙氨酰基氨肽酶和二肽基肽酶IV抑制剂为不同的小区的功能性的影响力和免疫学的治疗中，entz} ndlicher，神经元和其他疾病
公开(公告)号：WO2005034940A8
公开(公告)日：2006-06-01
申请号：PCT/EP2004011644
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG , ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL , STRIGGOW FRANK
发明人： ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL , STRIGGOW FRANK
IPC分类号： A61K31/404 , A61K31/4045 , C07C233/83 , C07C243/28 , C07C251/86 , C07C327/48 , C07D207/327 , C07D295/15 , C07D307/52 , C07D317/58 , C07D403/06 , C07D405/06 , C07D513/04
CPC分类号： C07C327/48 , C07C233/83 , C07C251/86 , C07D317/60 , C07D401/14 , C07D403/06 , C07D409/14 , C07D413/06 , C07D413/14
摘要： The invention relates to substances, which specifically inhibit both Ala-p-nitroanilide-cleaving peptidases as well as Gly-Pro-p-nitroanilide-cleaving peptidases, for use in the field of medicine. The invention also relates to the use of at least one substance of this type or of at least one pharmaceutical or cosmetic composition, which contains at least one of the aforementioned substances, for preventing and treating diseases, particularly for preventing and treating diseases with an overshooting immune response (autoimmune disease, allergies and transplant rejections), other chronic inflammatory diseases, neuronal diseases and cerebral damages, skin diseases (inter alia, acne and psoriasis), tumor diseases and special viral infections (inter alia, SARS).
摘要翻译：本发明涉及特异性抑制两者丙氨酸 - 对硝基苯胺裂解肽酶以及甘氨酸 - 脯氨酸 - 对硝基苯胺裂解肽酶，用于药物中的物质。此外，本发明涉及使用在这样的物质或至少一个的至少至少一个这样的药物或化妆品组合物用于治疗疾病的预防和治疗，尤其是用于预防和伴随着的过度免疫应答疾病（自身免疫性疾病，变态反应和移植排斥）的治疗，与其他慢性物质容纳 -entzündlichen疾病，神经疾病和脑损伤，皮肤疾病（特别是痤疮和牛皮癣），肿瘤疾病和特定的病毒感染（包括SARS）。

5. 发明申请

WO2005063234A3 USE OF AT LEAST ONE EFFECTOR OF GLUTATHIONE METABOLISM, TOGETHER WITH ALPHA-LIPONIC ACID FOR THE TREATMENT OF LUNG DISEASES 审中-公开
标题翻译：使用具有α-硫辛酸的谷胱甘肽的效应用于治疗肺疾病
公开(公告)号：WO2005063234A3
公开(公告)日：2005-09-22
申请号：PCT/EP2004014687
申请日：2004-12-23
申请人： ESPARMA GMBH , IMTM GMBH , ANSORGE SIEGFRIED , KOEGST DIETER , TAEGER MICHAEL , FRIES GERHARD
发明人： ANSORGE SIEGFRIED , KOEGST DIETER , TAEGER MICHAEL , FRIES GERHARD
IPC分类号： A61K31/137 , A61K31/20 , A61K31/366 , A61K45/06
CPC分类号： A61K45/06 , A61K31/137 , A61K31/20 , A61K31/366 , A61K2300/00
摘要： The invention relates to the use of at least one effector of glutathione metabolism, together alpha liponic acid, the salts and/or prodrugs thereof for simultaneous or timed cytoprotective treatment of chronically obstructive lung diseases.
摘要翻译：本发明涉及使用谷胱甘肽代谢中的至少一种效应连同α-硫辛酸，其为慢性阻塞性肺部疾病的同时，单独或顺序治疗的细胞保护的盐和/或前药。

6. 发明申请

WO2005034940A2 DUAL ALANYL AMINOPEPTIDASE AND DIPEPTIDYL PEPTIDASE IV INHIBITORS FOR FUNCTIONALLY INFLUENCING DIFFERENT CELLS AND FOR TREATING IMMUNOLOGICAL, INFLAMMATORY, NEURONAL AND OTHER DISEASES 审中-公开
标题翻译：双丙氨酰氨肽和二肽基肽酶IV抑制剂对不同细胞分泌功能的影响和治疗免疫性炎症，神经和其他疾病
公开(公告)号：WO2005034940A2
公开(公告)日：2005-04-21
申请号：PCT/EP2004011644
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG
发明人： ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL , STRIGGOW FRANK
IPC分类号： A61K31/404 , A61K31/4045 , C07C233/83 , C07C243/28 , C07C251/86 , C07C327/48 , C07D207/327 , C07D295/15 , C07D307/52 , C07D317/58 , C07D403/06 , C07D405/06 , C07D513/04 , C07D207/32
CPC分类号： C07C327/48 , C07C233/83 , C07C251/86 , C07D317/60 , C07D401/14 , C07D403/06 , C07D409/14 , C07D413/06 , C07D413/14
摘要： The invention relates to substances, which specifically inhibit both Ala-p-nitroanilide-cleaving peptidases as well as Gly-Pro-p-nitroanilide-cleaving peptidases, for use in the field of medicine. The invention also relates to the use of at least one substance of this type or of at least one pharmaceutical or cosmetic composition, which contains at least one of the aforementioned substances, for preventing and treating diseases, particularly for preventing and treating diseases with an overshooting immune response (autoimmune disease, allergies and transplant rejections), other chronic inflammatory diseases, neuronal diseases and cerebral damages, skin diseases (inter alia, acne and psoriasis), tumor diseases and special viral infections (inter alia, SARS).
摘要翻译：本发明涉及特异性抑制两者丙氨酸 - 对硝基苯胺裂解肽酶以及甘氨酸 - 脯氨酸 - 对硝基苯胺裂解肽酶，用于药物中的物质。此外，本发明涉及使用在这样的物质或至少一个的至少至少一个这样的药物或化妆品组合物用于治疗疾病的预防和治疗，尤其是用于预防和伴随着的过度免疫应答疾病（自身免疫性疾病，变态反应和移植排斥）的治疗，与其他慢性物质容纳 -entzündlichen疾病，神经疾病和脑损伤，皮肤疾病（特别是痤疮和牛皮癣），肿瘤疾病和特定的病毒感染（包括SARS）。

7. 发明申请

WO2011113895A3 CHARACTERIZATION AND VALIDATION OF INHIBITORS AND LIGANDS OF DIPEPTIDYL AMINOPEPTIDASE IV (DP IV) 审中-公开
标题翻译：抑制剂和胰蛋白酶抑制剂IV的配体的特征和鉴定（DP IV）
公开(公告)号：WO2011113895A3
公开(公告)日：2011-12-08
申请号：PCT/EP2011054040
申请日：2011-03-17
申请人： IMTM GMBH , ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL
发明人： ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL
IPC分类号： A61K31/496 , A61K31/00 , A61P29/00 , A61P37/00 , C12Q1/37 , G01N33/50
CPC分类号： A61K31/496 , A61K31/00 , A61K45/06 , C12Q1/37 , G01N2500/02 , A61K2300/00
摘要： The invention relates to a method for characterization and validation of inhibitors or ligands of DPIV, DP8 or DP9 by their interaction with specific binding sites in silico and in vitro. It describes the use of special binding properties at the binding site of the DPIV in the central pore of DPIV, which is distant from the catalytic domain by at least 10 Angström (1 nm) which is essential for the steric inhibition of this peptidase and related enzymes like DP8 and DP9 by DPIV ligands or steric inhibitors for the use of these compounds to suppress DNA synthesis of lymphocytes, dermal cells and other cells. This finding is also important in that this technique can be used to predict unwanted side effects of DPIV related drugs and exclude effects of DPIV inhibitors developed for the treatment of Diabetes mellitus type II on immune functions and vice versa.
摘要翻译：本发明涉及通过其与电子学和体外特异性结合位点的相互作用来表征和验证DPIV，DP8或DP9的抑制剂或配体的方法。它描述了在DPIV的中心孔的DPIV的结合位点处使用特殊的结合性质，DPIV的中心孔远离催化结构域至少10埃（1nm），其对于该肽酶的空间抑制和相关的必需通过DPIV配体的DP8和DP9的酶或空间抑制剂来使用这些化合物来抑制淋巴细胞，真皮细胞和其它细胞的DNA合成。这一发现也很重要，因为该技术可用于预测DPIV相关药物的不良副作用，并排除了为治疗II型糖尿病而开发的DPIV抑制剂对免疫功能的影响，反之亦然。

8. 发明专利

AU2011203290B2 Novel Compounds For Medical Use As Peptidase Effectors 未知
公开(公告)号：AU2011203290B2
公开(公告)日：2012-05-17
申请号：AU2011203290
申请日：2011-07-05
申请人： IMTM GMBH
发明人： ANSORGE SIEGFRIED , BANK UTE , HEIMBURG ANKE , JULIUS HEIKO , NORDHOFF KARSTEN , TAEGER MICHAEL
IPC分类号： C07C237/00 , A61K31/165 , A61K31/167 , A61K31/403 , A61K31/44 , A61K31/52 , A61P1/00 , A61P3/10 , A61P9/00 , A61P11/00 , A61P17/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/00 , C07D213/50
摘要： Abstract Novel compounds for medical use as peptidase effectors The invention relates to compounds of the general formula (1) N,. Y R3' R4 or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. The invention also relates to pharmaceutically effective compositions comprising at least one compound of the general formula (1), optionally together with one or more pharmaceutically acceptable carrier(s), auxiliary substance(s) and/or adjuvant(s) or cosmetically effective compositions comprising at least one compound of the general formula (1), optionally in combination with one or more cosmetically acceptable carrier(s), auxiliary substance(s) and/or adjuvant(s).

9. 发明专利

AT549326T 未知
公开(公告)号：AT549326T
公开(公告)日：2012-03-15
申请号：AT06829004
申请日：2006-11-10
申请人： IMTM GMBH
发明人： ANSORGE SIEGFRIED , NEUBERT KLAUS , BANK UTE , REICHSTEIN IRENE , FAUST JUERGEN , TAEGER MICHAEL , FUCHS PETRA , SENNS BIANCA
IPC分类号： C07D277/06 , A61K31/427 , A61P25/00 , C07D295/18 , C07D417/12
摘要： Compounds of the general formulae (1) and (2) A-B-D-B'-A'(1) and A-B-D-E(2) in which A and A' may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B' may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is -S-S- or -Se-Se-; and E is the group -CH2-CH(NH2)-R9 or -CH2-*CH(NH2)-R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residue, heterocycloalkyl residue, heteroarylalkyl residue, arylamidoalkyl residue, heteroarylamidoalkyl residue, unsubstituted or mono- or poly-substituted aryl residue or heteroaryl residue having one or more five-, six- or seven-membered ring(s) and * designates a chiral carbon atom preferably in the S- or L-configuration; or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formulae (1) and (2) in medicine.

10. 发明专利

AU2011203290A1 Novel Compounds For Medical Use As Peptidase Effectors 未知
公开(公告)号：AU2011203290A1
公开(公告)日：2012-02-16
申请号：AU2011203290
申请日：2011-07-05
申请人： IMTM GMBH
发明人： ANSORGE SIEGFRIED , BANK UTE , HEIMBURG ANKE , JULIUS HEIKO , NORDHOFF KARSTEN , TAEGER MICHAEL
IPC分类号： A61K31/165 , A61K31/167 , A61K31/403 , A61K31/44 , A61K31/52 , A61P1/00 , A61P3/10 , A61P9/00 , A61P11/00 , A61P17/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/00 , C07C237/00
摘要： Abstract Novel compounds for medical use as peptidase effectors The invention relates to compounds of the general formula (1) N,. Y R3' R4 or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. The invention also relates to pharmaceutically effective compositions comprising at least one compound of the general formula (1), optionally together with one or more pharmaceutically acceptable carrier(s), auxiliary substance(s) and/or adjuvant(s) or cosmetically effective compositions comprising at least one compound of the general formula (1), optionally in combination with one or more cosmetically acceptable carrier(s), auxiliary substance(s) and/or adjuvant(s).

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