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1. 发明专利

CA2455246A1 DRUG PREPARATION COMPRISING A-LIPOIC ACID, AMBROXOL AND/OR INHIBITORS OF THE ANGIOTENSIN-CONVERTING ENZYME (ACE) AND ITS USE FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 未知
公开(公告)号：CA2455246A1
公开(公告)日：2004-07-28
申请号：CA2455246
申请日：2004-01-16
申请人： KEYNEUROTEK AG , IMTM GMBH INST FUER MEDIZINTEC
发明人： ROEHNERT PETER , ANSORGE SIEGFRIED , REYMANN KLAUS , STRIGGOW FRANK , TAEGER MICHAEL , SCHROEDER ULRICH
IPC分类号： A61K45/00 , A61K31/137 , A61K31/385 , A61K31/401 , A61K38/55 , A61K45/06 , A61P7/04 , A61P9/10 , A61P21/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , A61K31/19 , A61K31/403 , A61K31/407 , A61K31/4166 , A61K31/472
摘要： The present invention concerns the use of a drug composition for the prevention and the therapy of neurodegenerative diseases (for example ischemic or hemorrhagic stroke, focal and global ischemia, amyotrophic lateral slerosis (ALS), Alzheimer's disease , Parkinson's disease, Hunntington's disease, multiple sclerosis). The combination of effective agents comprises at least two of the following substances: .alpha.-lipoic acid; ambroxol and one or several inhibitors) of the angiotensin-converting enzyme (ACE). It could surprisingly be found in the experiments on which the invention is based that neuronal cells which are particularly sensitive to degenerative insults, have less free constitutiona l thiol groups than have other cells of the central nervous system (CNS). It was demonstrated th at this reduced content of free thiol groups is causally connected to the damaging of those cells after a degenerative event. By using the combination of .alpha.-lipoic acid, ambroxo l and/or an ACE inhibitor, the damage after a neurodegenerative insult could be reduced by 4 0 to 45 %.

2. 发明专利

JP2004307467A Drug preparations comprising alpha-lipoic acid, ambroxol and/or angiotensin-converting enzyme (ace) inhibitor, and its use for treatment of neurodegenerative disorder 审中-公开
公开(公告)号：JP2004307467A
公开(公告)日：2004-11-04
申请号：JP2004018916
申请日：2004-01-27
申请人： Inst Fuer Medizintechnologie Magdeburg Gmbh Imtm , Keyneurotek Ag , インスティテュートヒューアメディツィンテクノロギーマグデブルクゲーエムベーハーイーエムテーエム , キーニューロテックアーゲー
发明人： ROEHNERT PETER , STRIGGOW FRANK , REYMANN KLAUS , ANSORGE SIEGFRIED , TAEGER MICHAEL , SCHROEDER ULRICH
IPC分类号： A61K45/00 , A61K31/137 , A61K31/385 , A61K31/401 , A61K38/55 , A61K45/06 , A61P7/04 , A61P9/10 , A61P21/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00
CPC分类号： A61K45/06
摘要： PROBLEM TO BE SOLVED: To provide a drug composition for the prevention and treatment of neurodegenerative disorders (for example, ischemic or hemorrhagic stroke, focal and global ischemia, amyotropic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, Huntington's disease and multiple sclerosis).
SOLUTION: This drug composition comprises at least two substances selected from the group consisting of α-lipoic acid, its salt and isomer, ambroxol, its salt and prodrug, the angiotensin-converting enzyme (ACE) inhibitor, and optionally contains a pharmaceutically acceptable normal carrier, an additive and an adjuvant.
COPYRIGHT: (C)2005,JPO&NCIPI

3. 发明申请

WO2005037779A3 NOVEL DIPEPTIDYL PEPTIDASE IV INHIBITORS USED FOR FUNCTIONALLY INFLUENCING DIFFERENT CELLS AND TREATING IMMUNOLOGICAL, INFLAMMATORY, NEURONAL, AND OTHER DISEASES 审中-公开
标题翻译：新的二肽基肽酶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：WO2005037779A3
公开(公告)日：2005-07-07
申请号：PCT/EP2004011645
申请日：2004-10-15
申请人： INST MEDIZINTECHNOLOGIE MAGDEB , 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： A61K31/55 , C07C229/34 , C07C235/56 , C07C243/28 , C07C251/80 , C07C251/86 , C07C255/61 , C07C259/14 , C07C271/28 , C07C311/08 , C07C311/19 , C07C311/29 , C07C323/60 , C07C327/48 , C07D205/08 , C07D213/82 , C07D225/02 , C07D401/12 , C07D405/12 , C07D417/12 , C07F9/6506
CPC分类号： C07C235/56 , C04B35/632 , C07C229/34 , C07C243/28 , C07C251/80 , C07C251/86 , C07C255/61 , C07C259/14 , C07C271/28 , C07C311/08 , C07C311/19 , C07C311/29 , C07C323/60 , C07C327/48 , C07C2601/10 , C07C2603/74 , C07D205/08 , C07D213/82 , C07D225/02 , C07D401/12 , C07D405/12 , C07D417/12 , C07F9/65061
摘要： The invention relates to medicinally used substances which specifically inhibit peptidases splitting Gly-Pro-p-nitroanilide. The invention further relates to the use of at least one such substance or at least one pharmaceutical or cosmetic composition containing at least one such substance for preventing and treating diseases, particularly 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，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

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）。

5. 发明申请

WO02053169A2 USE OF ENZYME INHIBITORS OF THE DIPEPTIDYPEPTIDASE IV (EC 3.3.14.5) IN ADDITION TO THE AMINOPEPTIDASE N (EC 3.4.11.2), INDIVIDUALLY OR IN A COMBINATION THEREOF, AND PHARMACEUTICAL PREPARATIONS THEREOF FOR THE PREVENTION AND/OR THERAPY OF ISCHAEMIA-CAUSED ACUTE AND CHRONIC NEURODEGENERATIVE PROCESS AND ILLNESSES, FOR EXAMPLE 审中-公开
标题翻译：二肽基肽酶IV的酶抑制剂（EC 3.4.14.5）和氨肽酶N（EC3.4.11.2），单独或组合，和药物制剂THEREOF用于预防和/或治疗缺血相关的急性和慢性神经变性过程和疾病中的用途
公开(公告)号：WO02053169A2
公开(公告)日：2002-07-11
申请号：PCT/EP0115196
申请日：2001-12-21
申请人： KEYNEUROTEK AG I G , ANSORGE SIEGFRIED , LENDECKEL UWE , STRIGGOW FRANK , NEUBERT KLAUS , REYMANN KLAUS , KAEHNE THILO
发明人： ANSORGE SIEGFRIED , LENDECKEL UWE , STRIGGOW FRANK , NEUBERT KLAUS , REYMANN KLAUS , KAEHNE THILO
IPC分类号： A61K31/00 , A61K38/03 , A61P9/10 , A61P25/00 , A61K38/00
CPC分类号： A61K31/00 , A61K38/03 , A61K2300/00
摘要： The invention relates to a method which reduces or prevents lesions to cerebral tissues after ischaemia or brain/cerebral traumas, involving the separate or combined administration and effect of enzyme inhibitors of alanyl-aminopeptidase (APN) and dipeptidylpeptidase IV (DP IV) or enzymes having the same similar substrate specificity. The invention demonstrates that in order to prevent or treat the above-mentioned indications, the separate or combined application of inhibitors of the above-mentioned enzymes or corresponding preparations and forms of administration are suitable.
摘要翻译：本发明包括一种方法，其中通过分开或联合施用和丙氨酰 - 氨基肽酶的Enzyminihibitoren（APN）的效果和二肽基肽酶IV（DP IV）或相同的酶或类似底物特异性，脑组织由于缺血或损伤 vermnidern颅骨/脑外伤或可预防。我们的发明显示，用于上述适应症的预防和治疗中，上述酶或相应的制剂和给药形式的抑制剂的单独或联合施用是其适合的。

6. 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）。

7. 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）。

8. 发明申请

WO2004082699A3 USE OF INCENSE OR HYDROGENATION PRODUCTS FOR PREVENTING AND/OR TREATING A CEREBRAL ISCHEMIA AND/OR CEREBRAL TRAUMATIC LESION 审中-公开
标题翻译：使用焚香或其加氢预防和/或治疗脑缺血和/或颅骨/脑外伤的
公开(公告)号：WO2004082699A3
公开(公告)日：2005-02-10
申请号：PCT/EP2004002839
申请日：2004-03-18
申请人： KEYNEUROTEK AG , STRIGGOW FRANK , SCHMIDT WERNER , MACK TILL
发明人： STRIGGOW FRANK , SCHMIDT WERNER , MACK TILL
IPC分类号： A61K31/19 , A61K36/00 , A61K36/324 , A61K35/78
CPC分类号： A61K31/19 , A61K36/324
摘要： The invention relates to the use of incense hydrogenation products (olibanum), the hydrogenated components thereof, the derivatives thereof, the physiologically tolerable salts thereof and hydrated incense extracts for producing a drug used for preventing and/or treating a cerebral ischemia, cerebral traumatic lesion and/or the Alzheimer's disease. Said invention also relates to the use of the incense, the extracts thereof, the substances contained therein, the physiologically tolerable salts thereof, the derivatives thereof and the physiologically tolerable salts of said derivatives, pure boswellic acids, tirucallic acids and other triterpenes, the physiologically tolerable salts thereof, the derivatives thereof and the physiologically tolerable salts of said derivatives for producing a drug for preventing and/or treating a cerebral ischemia and/or cerebral traumatic lesion.
摘要翻译：本发明涉及使用香（乳香），及其氢化成分和生理上可接受的盐和它们的衍生物的氢化的和氢化香提取物在制备用于治疗脑缺血，颅/脑外伤和/或老年痴呆症的预防和/或治疗性治疗疾病。根据本发明进一步是使用香，香提取物，包含在香物质，它们的生理学上可接受的盐，它们的衍生物和它们的生理盐，纯乳香酸，tirucallic酸或其它三萜烯，用于制备药物用于预防性及其生理学上可接受的盐，衍生物或它们的盐提供和/或脑缺血和/或可用的颅/脑外伤的治疗性治疗。

9. 发明申请

WO02053169A8 USE OF DIPEPTYLPEPTIDASE IV AND AMINOPEPTIDASE-N INHIBITORS IN THE TREATMENT OF ISCHAEMIA-INDUCED NEURO-DEGENERATION 审中-公开
标题翻译：作者二肽基肽酶IV和氨肽酶N INHIBOTOREN FOR缺血诱导的神经变性的治疗中的用途
公开(公告)号：WO02053169A8
公开(公告)日：2003-04-10
申请号：PCT/EP0115196
申请日：2001-12-21
申请人： KEYNEUROTEK AG I G , ANSORGE SIEGFRIED , LENDECKEL UWE , STRIGGOW FRANK , NEUBERT KLAUS , REYMANN KLAUS , KAEHNE THILO
发明人： ANSORGE SIEGFRIED , LENDECKEL UWE , STRIGGOW FRANK , NEUBERT KLAUS , REYMANN KLAUS , KAEHNE THILO
IPC分类号： A61K31/00 , A61K38/03 , A61P9/10 , A61P25/00 , A61K38/00
CPC分类号： A61K31/00 , A61K38/03 , A61K2300/00
摘要： The invention relates to a method which reduces or prevents lesions to cerebral tissues after ischaemia or brain/cerebral traumas, involving the separate or combined administration and effect of enzyme inhibitors of alanyl-aminopeptidase (APN) and dipeptidylpeptidase IV (DP IV) or enzymes having the same similar substrate specificity. The invention demonstrates that in order to prevent or treat the above-mentioned indications, the separate or combined application of inhibitors of the above-mentioned enzymes or corresponding preparations and forms of administration are suitable.
摘要翻译：本发明包括一种方法，其中通过分开或联合施用和丙氨酰 - 氨基肽酶的Enzyminihibitoren（APN）的效果和二肽基肽酶IV（DP IV）或相同的酶或类似底物特异性，脑组织由于缺血或损伤 vermnidern颅骨/脑外伤或可预防。我们的发明显示，用于上述适应症的预防和治疗中，上述酶或相应的制剂和给药形式的抑制剂的单独或联合施用是其适合的。

10. 发明专利

DE10348044A1 未知
公开(公告)号：DE10348044A1
公开(公告)日：2005-05-19
申请号：DE10348044
申请日：2003-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG
发明人： ANSORGE SIEGFRIED , BANK UTE , NORFHOFF 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 , C07D307/38 , C07C229/02 , A61K31/198 , A61K31/34
摘要： Acrylic acid derivatives (C1), hydrazones (C2), imines (C3), bicyclic compounds (C4), hydrazine or azo compounds (C5), hexafluoropropane derivatives (C6), amino acids (C7), heterocyclic compounds (C8), alkenyl cyclic compounds (C9), bicyclic compounds (C10), pyridine, pyrimidine, pyridazine or triazine derivatives (C11), cyclic imides (C12), carbonate-type compounds (C13), sulfone-type compounds (C14), heterocyclic compounds (C15) and thiazolidinone derivatives (C16) are used in medicine. [Image] Definitions for C1-C3: X', Z' : OH, SH, 1-12C alkoxy, 1-12C alkylthio, optionally substituted (hetero)aryl or (hetero)cycloalkyl, NH 2, NHR 2> or NR 2>R 3>; Y' : O, S or NR4; R 1>-R 4>Q'; Q' : H; optionally substituted 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl; OH, SH, 1-12C alkoxy or 1-12C alkylthio; or optionally substituted (hetero)aryl, (hetero)cycloalkyl, amino, carbonyl, thiocarbonyl or imino. Definitions for C4: X 1>-X 4>CH or CR 3>; Y 1>-Y 3>optionally substituted C, N, O or P; R 1>1-4 of Q'; R 2>1-6 of Q'; R 3> is not defined. Definitions for C5: Y' : O, S, NH or NR5; R 1>-R 5>Q'. Definitions for C6: Y' : O, S, NH or NR 1>; X', Z' : OH, SH, 1-8C alkoxy, 1-8C alkylthio, optionally substituted (hetero)aryl or (hetero)cycloalkyl, NH 2, NHR 2> or NR 2>R 3>; R 1>-R 3>Q'. Definitions for C7: Y' : O, S, NH or NR 4>; X', Z' : OH, SH, 1-8C alkoxy, 1-8C alkylthio, optionally substituted (hetero)aryl or (hetero)cycloalkyl, NH 2, NHR 5> or NR 5>R 6>; R 1>-R 6>Q'. Definitions for C8: X' : an N, O, S or P heteroatom or a functional group containing this heteroatom as a ring atom; R 1>1-10 of Q'; the 6-membered ring can contain 1-3 further heteroatoms and 0-3 double bonds. Definitions for C9: X 1>CH 2, CHR 3>, CR 3>R 4>, NH, NR 4>, O or S; X 2>-X 4>CH, CR 5> or N; R 1>-R 5>Q'. Definitions for C10: X', Z' : CH, CR 1> or N, at least one being N; R 1>Q'; the rings are optionally substituted, optionally fused, contain 0-3 double bonds and can contain further N atoms. Definitions for C11: R 1>1-5 of Q'. Definitions for C12: Y1', Y2' : O, S, NH or NR 6>; R 1>-R 6>Q'. Definitions for C13: X', Z' : OH, SH, 1-8C alkoxy, 1-8C alkylthio, optionally substituted (hetero)aryl or (hetero)cycloalkyl, NH 2, NHR 1> or NR 1>R 2>; Y' : O, S, NH or NR 3>; R 1>-R 3>Q'. Definitions for C14: Y 1>, Y 2>O, S, NH or NR 3>; R 1>-R 3>Q'. Definitions for C15: X' : O, S, NH or NR 9>; R 1>-R 9>Q'. Definitions for C16: R 1>-R 5>H, Me, CH 2R 6>, CHR 6>R 7>, CR 6>R 7>R 8>, OH, OR 6>, NH 2, NHR 6>, NR 6>R 7>, COR 6>, C(NH)R 6>, C(NR 7>)R 6>, CSR 6>, PH 2, PHR 6>, PR 6>R 7>, PO(OH) 2, PO(OH)(OR 6>), PO(OR 6>)(OR 7>) or CN; A', Y', Z' : CH 2, CHR 9>, CR 9>R 10>, CO, CS, C(NH), C(NR 9>), NH, NR 9>, NOH, NOR 9>, O, S, SO 2, PH, PR 9>, P(O)OH, P(O)OR 9>, P(OH) 3, P(OH) 2OR 9>, P(OH)(OR 9>)(OR 10>), P(OR 9>)(OR 10>)(OR 11>); X' : N, CH, CR 12>, P, PO, P(OH) 2, P(OH)(OR 12>) or P(OR 12>)(OR 13>); R 6>-R 13>Q'. ACTIVITY : Immunosuppressive; Antiinflammatory; Neuroprotective; Antiulcer; Antiarthritic; Antidiabetic; Antiallergic; Antiasthmatic; Dermatological; Antipsoriatic; Antiseborrheic; Nootropic; Antiparkinsonian; Anticonvulsant; Antibacterial; Antiarteriosclerotic; Vasotropic. MECHANISM OF ACTION : Alanyl aminopeptidase (APN) inhibitor; Dipeptidyl peptidase IV (DPIV) inhibitor. N-(1-(4-methyl-1-piperidinylcarbonyl)-2-(2-furyl)vinyl)-4-chlorobenzamide had an IC50 of 18.5 mu M against DPIV and 6.2 mu M against APN.

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