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1. 发明申请

WO02053170A3 COMBINED USE OF ENZYME INHIBITORS AND PHARMACEUTICAL PREPARATIONS THEREOF FOR THE TREATMENT AND PROPHYLAXIS OF ARTERIOSCLEROSIS, FOR THE TREATMENT AND PREVENTION OF ALLERGIC REACTIONS OF TYPE I ACCORDING TO THE GELL AND COOMBS CLASSIFICATION, AND FOR THE TREATMENT AND PREVENTION OF DERMATOLOGICAL DISEASES ASSOCIATED WITH FO 审中-公开
标题翻译：酶抑制剂和药物制剂及其用于治疗和动脉粥样硬化的预防结合使用，用于治疗和预防过敏性反应来I型和盖尔和库姆斯治疗和预防皮肤病滤泡及表皮HYPERKERATOS
公开(公告)号：WO02053170A3
公开(公告)日：2003-02-20
申请号：PCT/EP0115199
申请日：2001-12-21
申请人： INST MEDIZINTECHNOLOGIE MAGDEB , ANSORGE SIEGFRIED , LENDECKEL UWE , NEUBERT KLAUS , REINHOLD DIRK , VETTER ROBERT , GOLLNICK HARALD
发明人： ANSORGE SIEGFRIED , LENDECKEL UWE , NEUBERT KLAUS , REINHOLD DIRK , VETTER ROBERT , GOLLNICK HARALD
IPC分类号： C12N9/99 , A61K38/55 , A61K45/00 , A61P9/10 , A61P17/00 , A61P17/06 , A61P35/00 , A61P37/06 , A61P37/08 , A61K45/06
CPC分类号： A61K38/55 , A61K38/05 , A61K38/06 , A61K38/556 , A61K45/06 , A61K2300/00
摘要： The invention relates to the use of inhibitors of dipeptidyl peptidase IV (DP IV) and enzymes having the same specific nature of substrate (DP IV enzyme activity), combined with inhibitors of alanyl aminopeptidase (aminopeptidase N, APN), or enzymes having the same specific nature of substrate (APN enzyme activity), for the additive to superadditive inhibition of the activation and proliferation (DNS synthesis) of human T lymphocytes or mononuclear cells and of the production of TH2 cytokines for the treatment and prevention of allergic reactions of type I according to the Gell and Coombs classification, for the additive to superadditive inhibition of the activation and proliferation (DNS synthesis) of human epidermal and follicular keratinocytes and those of the transitional region between the skin and the mucosa, and for the treatment and prevention of dermatological diseases associated with follicular and epidermal hyperkeratosis and reinforced keratinocyte proliferation. The invention also relates to the use of inhibitors of dipeptidyl peptidase IV (DP IV) and enzymes having the same specific nature of substrate (DP IV enzyme activity), combined with inhibitors of alanyl aminopeptidase (aminopeptidase N, APN), or enzymes having the same specific nature of substrate (APN enzyme activity), inhibitors of X-pro-aminopeptidase (aminopeptidase P, APP), inhibitors of the angiotensin-converting enzyme (ACE) and/or of prolyoligopeptidase (POP, prolylendopeptidase, PEP) for the additive to superadditive inhibition of the activation, DNS synthesis and proliferation of human T lymphocytes or mononuclear cells for the treatment and prophylaxis of arteriosclerosis. The invention further relates to pharmaceutical preparations comprising a plurality of inhibitors of enzymes of the above-mentioned groups.
摘要翻译：本发明涉及使用二肽基肽酶IV抑制剂（DP IV）以及具有组合相同的底物特异性（DP IV-类似酶活性）用具有相似的底物特异性丙氨酰基氨肽酶的抑制剂（氨肽酶N，APN）或酶的酶（APN-类似的根据盖尔和库姆斯和添加剂以超加和抑制的酶活性）的添加剂，以超加和抑制人T淋巴细胞或单核细胞和生产Th2细胞因子的活化和增殖（DNA合成）的，用于治疗和预防I型的过敏性反应的活化，增殖（DNA合成）的人表皮和毛囊角化细胞以及那些皮肤粘膜的过渡区以及用于治疗和预防皮肤疾病与表皮角化过度和滤泡和增加角化细胞增殖的。本发明还涉及使用二肽基肽酶IV（DP IV）的抑制剂，以及作为具有组合相同的底物特异性（DP IV-类似酶的活性）与丙氨酰基氨肽酶的抑制剂（氨肽酶N，APN）或酶（DP IV的底物特异性相同的酶为添加剂的超加和抑制活化的-Analogue酶活性），X-脯氨肽酶的（氨肽酶P，APP）中，“血管紧张素转化酶”的（ACE）和/或所述Prolyoligopeptidase（POP，脯氨酰内肽酶，PEP），DNA 合成和人T Lymphozaten或单核细胞用于治疗和预防动脉硬化的增殖。本发明还涉及一种包括多个上述基团的酶的抑制剂的药物制剂。

2. 发明申请

WO2005004906A3 USE OF DP IV AND APN INHIBITORS FOR THE TREATMENT OF DERMATOLOGICAL DISEASES INVOLVING THE HYPERPROLIFERATION AND MODIFIED DIFFERENTIATION CONDITIONS OF FIBROBLASTS 审中-公开
标题翻译：使用和DP IV抑制剂APN用于治疗与HYPER增殖和皮肤病成纤维细胞的改进差分状态
公开(公告)号：WO2005004906A3
公开(公告)日：2005-06-09
申请号：PCT/EP2004007377
申请日：2004-07-06
申请人： INST MEDIZINTECHNOLOGIE MAGDEB , ANSORGE SIEGFRIED , GOLLNICK HARALD , LENDECKEL UWE , NEUBERT KLAUS , REINHOLD DIRK , VETTER ROBERT , SCHRAVEN BURKHART , THIELITZ ANJA , FAUST JUERGEN
发明人： ANSORGE SIEGFRIED , GOLLNICK HARALD , LENDECKEL UWE , NEUBERT KLAUS , REINHOLD DIRK , VETTER ROBERT , SCHRAVEN BURKHART , THIELITZ ANJA , FAUST JUERGEN
IPC分类号： A61K45/06 , A61P17/00 , A61K38/55
CPC分类号： A61K45/06
摘要： The invention relates to a method for inhibiting the DNA synthesis of human fibroblasts that is necessary for proliferation, by the individual or combined action of inhibitors of alanyl-aminopeptidase (APN) and dipeptidylpeptidase IV (DP IV) that is expressed by said cells. The DNA synthesis (proliferation) of human fibroblasts is inhibited by a dosage-dependent administration of the APN and/or the DP IV. According to the invention, the application of inhibitors of the aforementioned enzyme or of preparations and administrable forms containing said inhibitors is eminently suitable for the treatment and prevention of dermatological diseases involving fibroblastic hyperproliferation and modified differentiation conditions of fibroblasts.
摘要翻译：本发明涉及一种通过由这些细胞丙氨酰氨肽（APN），和二肽基肽酶IV（DP IV）表示的蛋白的抑制剂的唯一或组合作用用于抑制人成纤维细胞的DNA合成所必需的增殖的方法。人成纤维细胞的DNA合成（增殖）是剂量依赖性通过APN和/或DP IV抑制剂给药抑制。我们的发明显示，上述酶的抑制剂或含有制剂和药物形式的这些抑制剂的施用它们适用于治疗和预防与过度增殖fibroblastar皮肤病学病症和分化成纤维细胞的修饰的状态。

3. 发明专利

DE10155093A1 Inhibiting DNA synthesis in T-lymphocytes, keratinocytes and TH2 cytokine production, comprises combined administration of dipeptidyl peptidase and alanyl-aminopeptidase inhibitors 未知
公开(公告)号：DE10155093A1
公开(公告)日：2003-06-12
申请号：DE10155093
申请日：2001-11-09
申请人： INST MEDIZINTECHNOLOGIE MAGDEB , ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS
发明人： ANSORGE SIEGFRIED , GOLLNICK HARALD , LENDECKEL UWE , NEUBERT KLAUS , REINHOLD DIRK , VETTER ROBERT
IPC分类号： A61K38/55 , A61K38/05
摘要： Inhibiting the activation and proliferation (DNA synthesis) of human T-lymphocytes or mononuclear cells and the production of TH2 cytokines comprises combined administration of dipeptidyl peptidase IV (DP IV) inhibitors and alanyl-aminopeptidase (aminopeptidase N, APN) inhibitors. The DP IV and APN inhibitors may be replaced by enzymes with the same substrate specificity. Independent claims are also included for the following: (1) the combined use of DP IV and APN inhibitors for the (super-)additive inhibition of the activation and proliferation (DNA synthesis) of human epidermal and follicular keratinocytes and those in the transition region between the skin and mucosa; (2) the combined use of DP IV and APN inhibitors, X-Pro-aminopeptidase (APP) inhibitors, ACE inhibitors and/or prolyloligopeptidase (POP) inhibitors for the (super-)additive inhibition of the activation and proliferation (DNA synthesis) of human T-lymphocytes or mononuclear cells; and (3) pharmaceutical preparations containing DP IV and APN inhibitors (or enzymes with the same substrate specificity) and optionally APP, ACE and/or POP inhibitors.

4. 发明专利

AT482715T 未知
公开(公告)号：AT482715T
公开(公告)日：2010-10-15
申请号：AT03709761
申请日：2003-03-07
申请人： IMTM GMBH , ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C
发明人： ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C , FAUST JUERGEN , LENDECKEL UWE , REINHOLD DIRK , VETTER ROBERT
IPC分类号： A61K38/05 , C12N9/99 , A61K31/195 , A61K31/40 , A61K31/426 , A61K31/4453 , A61K38/55 , A61K45/00 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00
摘要： The invention relates to a process for the-inhibition of the DNA synthesis necessary for the proliferation of human sebaceous cells (sebocytes) by the isolated or joint effect of inhibitors of alanyl aminopeptidase (APN) and dipetidyl peptidase IV (DP IV) expressed by these cells. The DNA synthesis (proliferation) of human sebaceous cells is inhibited by the administration of the inhibitors of APN and/or of DP IV depending on the dose. Our invention shows that, for a therapy and for a prevention of dermatological diseases with sebaceous hyperproliferation and modified conditions of differentiation, the application of inhibitors of the above-mentioned enzymes and of corresponding pharmaceutical preparations and dosage forms thereof is suitable.

5. 发明专利

AU2003214105A2 Use of enzyme inhibitors with aminopeptidase N and/or dipeptidylpeptidase IV activities and pharmaceutical preparations produced therefrom for the therapy and prevention of dermatological diseases with seborrhoeic hyperproliferation and altered differentiation states 未知
公开(公告)号：AU2003214105A2
公开(公告)日：2003-09-29
申请号：AU2003214105
申请日：2003-03-07
申请人： IMTM INST FUR MEDIZINTECHNOLOG , ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , CHRISTOS ZOUBOULIS
发明人： ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C , FAUST JURGEN , LENDECKEL UWE , REINHOLD DIRK , VETTER ROBERT
IPC分类号： C12N9/99 , A61K31/195 , A61K31/40 , A61K31/426 , A61K31/4453 , A61K38/55 , A61K45/00 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , A61K38/05
摘要： The invention relates to a process for the-inhibition of the DNA synthesis necessary for the proliferation of human sebaceous cells (sebocytes) by the isolated or joint effect of inhibitors of alanyl aminopeptidase (APN) and dipetidyl peptidase IV (DP IV) expressed by these cells. The DNA synthesis (proliferation) of human sebaceous cells is inhibited by the administration of the inhibitors of APN and/or of DP IV depending on the dose. Our invention shows that, for a therapy and for a prevention of dermatological diseases with sebaceous hyperproliferation and modified conditions of differentiation, the application of inhibitors of the above-mentioned enzymes and of corresponding pharmaceutical preparations and dosage forms thereof is suitable.

6. 发明专利

DE19826972A1 Inhibiting keratinocyte activation and proliferation, for treatment of dermatological disorders such as psoriasis or actinic precancerous states 未知
公开(公告)号：DE19826972A1
公开(公告)日：1999-12-23
申请号：DE19826972
申请日：1998-06-18
申请人： UNIV MAGDEBURG TECH , UNIV HALLE WITTENBERG , ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS
发明人： ANSORGE SIEGFRIED , BORN ILONA , BUEHLING FRANK , FAUST JUERGEN , GOLLNICK HARALD , LENDECKEL UWE , NEUBERT KLAUS , REINHOLD DIRK , VETTER ROBERT
IPC分类号： A61K38/07 , A61K38/05
摘要： The use of inhibitors (I) of dipeptidyl peptidase IV (DP IV) or analogous enzymes is claimed for inhibiting the activation and proliferation of keratinocytes (including malignantly transformed keratinocytes) and tumor cells derived from keratinocytes.- DETAILED DESCRIPTION - An INDEPENDENT CLAIM is included for (I)-containing pharmaceutical preparations for use as above.- ACTIVITY - Antiinflammatory; dermatological; antipsoriatic; cytostatic.- MECHANISM OF ACTION - Dipeptidyl peptidase IV inhibitor; DNA synthesis inhibitor.- Inhibition of DP IV in keratinocytes suppresses activation and DNA synthesis in these cells and thus suppresses proliferation. Addition of N( epsilon )-4-nitrobenzyloxycarbonyl-L-lysine-thiazolidide (Ia) at 2 mu M reduced DNA synthesis (measured after 72 hours) in cultured NHEK Ad human keratinocytes by ca. 50 %

7. 发明专利

AU2003214105B2 Use of enzyme inhibitors with aminopeptidase N and/or dipeptidylpeptidase IV activities and pharmaceutical preparations produced therefrom for the therapy and prevention of dermatological diseases with seborrhoeic hyperproliferation and altered differentiation states 未知
公开(公告)号：AU2003214105B2
公开(公告)日：2008-11-13
申请号：AU2003214105
申请日：2003-03-07
申请人： ANSORGE SIEGFRIED , GOLLNICK HARALD , IMTM GMBH , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C
发明人： NEUBERT KLAUS , VETTER ROBERT , ANSORGE SIEGFRIED , REINHOLD DIRK , ZOUBOULIS CHRISTOS C , LENDECKEL UWE , GOLLNICK HARALD , FAUST JURGEN
IPC分类号： C12N9/99 , A61K31/195 , A61K31/40 , A61K31/426 , A61K31/4453 , A61K38/55 , A61K45/00 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00
摘要： The invention relates to a process for the-inhibition of the DNA synthesis necessary for the proliferation of human sebaceous cells (sebocytes) by the isolated or joint effect of inhibitors of alanyl aminopeptidase (APN) and dipetidyl peptidase IV (DP IV) expressed by these cells. The DNA synthesis (proliferation) of human sebaceous cells is inhibited by the administration of the inhibitors of APN and/or of DP IV depending on the dose. Our invention shows that, for a therapy and for a prevention of dermatological diseases with sebaceous hyperproliferation and modified conditions of differentiation, the application of inhibitors of the above-mentioned enzymes and of corresponding pharmaceutical preparations and dosage forms thereof is suitable.

8. 发明专利

EA008745B1 ПРИМЕНЕНИЕ ИНГИБИТОРОВ ФЕРМЕНТОВ С АКТИВНОСТЬЮ АМИНОПЕПТИДАЗЫ N И/ИЛИ ДИПЕПТИДИЛПЕПТИДАЗЫ IV И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ ДЛЯ ЛЕЧЕНИЯ И ПРОФИЛАКТИКИ ДЕРМАТОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ С СЕБОЦИТАРНОЙ ГИПЕРПРОЛИФЕРАЦИЕЙ И ИЗМЕНЕННЫМИ ДИФФЕРЕНЦИРОВАННЫМИ СОСТОЯНИЯМИ 未知
公开(公告)号：EA008745B1
公开(公告)日：2007-08-31
申请号：EA200401212
申请日：2003-03-07
申请人： IMTM GMBH , ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C
发明人： ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C , FAUST JURGEN , LENDECKEL UWE , REINHOLD DIRK , VETTER ROBERT
IPC分类号： A61K38/05 , C12N9/99 , A61K31/195 , A61K31/40 , A61K31/426 , A61K31/4453 , A61K38/55 , A61K45/00 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00
摘要： ИзобретениекасаетсяспособаподавлениясинтезаДНКсебоцитовчеловека, необходимогодляпролиферации, посредствомотдельногоилисовместногодействияингибитороваланиламинопептидазы (APN) идипептидилпептидазы IV (DP IV), экспрессированныхв этихклетках. СинтезДНК (пролиферация) себоцитовчеловекаподавляетсяпутемвведенияингибиторов APN или/и DP IV взависимостиотдозы. Данноеизобретениепредлагаетдлялеченияи профилактикидерматологическихзаболеванийс себоцитарнойпролиферациейи измененнымидифференцированнымисостояниямиприменениеингибитороввышеназванныхферментовилисоответствующихкомпозицийи препаративныхготовыхформнаихоснове.

9. 发明专利

AU2003214105A1 USE OF ENZYME INHIBITORS WITH AMINOPEPTIDASE N AND/OR DIPEPTIDYLPEPTIDASE IV ACTIVITIES AND PHARMACEUTICAL PREPARATIONS PRODUCED THEREFROM FOR THE THERAPY AND PREVENTION OF DERMATOLOGICAL DISEASES WITH SEBORRHOEIC HYPERPROLIFERATION AND ALTERED DIFFERENTIATION STATES 未知
公开(公告)号：AU2003214105A1
公开(公告)日：2003-09-29
申请号：AU2003214105
申请日：2003-03-07
申请人： IMTM INST FUR MEDIZINTECHNOLOG , ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C
发明人： ANSORGE SIEGFRIED , GOLLNICK HARALD , NEUBERT KLAUS , ZOUBOULIS CHRISTOS C , FAUST JURGEN , LENDECKEL UWE , REINHOLD DIRK , VETTER ROBERT
IPC分类号： C12N9/99 , A61K31/195 , A61K31/40 , A61K31/426 , A61K31/4453 , A61K38/55 , A61K45/00 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , A61K38/05
摘要： The invention relates to a process for the-inhibition of the DNA synthesis necessary for the proliferation of human sebaceous cells (sebocytes) by the isolated or joint effect of inhibitors of alanyl aminopeptidase (APN) and dipetidyl peptidase IV (DP IV) expressed by these cells. The DNA synthesis (proliferation) of human sebaceous cells is inhibited by the administration of the inhibitors of APN and/or of DP IV depending on the dose. Our invention shows that, for a therapy and for a prevention of dermatological diseases with sebaceous hyperproliferation and modified conditions of differentiation, the application of inhibitors of the above-mentioned enzymes and of corresponding pharmaceutical preparations and dosage forms thereof is suitable.

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