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1. 发明专利

AU2004281536B2 Novel alanyl-amino peptidase inhibitors for functionally influencing different cells and treating immunological, inflammatory, neuronal, and other diseases 未知
公开(公告)号：AU2004281536B2
公开(公告)日：2009-07-09
申请号：AU2004281536
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK PHARMACEUTICALS AG
发明人： ANSORGE SIEGFRIED , NORDHOFF KARSTEN , TAGER MICHAEL , STRIGGOW FRANK , BANK UTE
IPC分类号： C07C259/06 , A61K31/00 , A61K31/4015 , 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
摘要： The invention relates to substances which specifically inhibit peptidases splitting ala-p-nitroanilide for use in medicine. The invention further relates to the use of at least one such substance or of a pharmaceutical or cosmetic composition containing at least one such substance for the prophylaxis and therapy of diseases, in particular the prophylaxis and therapy of diseases with an overshooting immune response (autoimmune diseases, allergies and transplant rejections), of other chronic inflammatory diseases, neuronal diseases and brain damages, skin diseases (acne and psoriasis, among others), tumor diseases and special virus infections (including SARS).

2. 发明专利

AU2004281959B9 Novel dipeptidyl peptidase IV inhibitors used for functionally influencing different cells and treating immunological, inflammatory, neuronal, and other diseases 未知
公开(公告)号：AU2004281959B9
公开(公告)日：2009-11-26
申请号：AU2004281959
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK PHARMACEUTICALS AG
发明人： TAGER MICHAEL , BANK UTE , STRIGGOW FRANK , NORDHOFF KARSTEN , ANSORGE SIEGFRIED
IPC分类号： C07D205/08 , 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 , C07D213/82 , C07D225/02 , C07D401/12 , C07D405/12 , C07D417/12 , C07F9/6506
摘要： The present invention relates to substances capable of specifically inhibiting Gly-Pro-p-nitroanilide cleaving peptidases, for a use in the medical field. Furthermore, the invention relates to the use of at least one of such substances or of at least one pharmaceutical or cosmetic composition containing at least one such substance for a prophylaxis or a therapy of diseases, particularly for a prophylaxis and a therapy of diseases accompanied by an excessive immune response (autoimmune diseases, allergies, transplant rejections), of other chronic-inflammatory diseases, of neuronal diseases and cerebral damage, of skin diseases (inter alia acne, psoriasis), of tumor diseases and of specific virus infections (inter alia SARS).

3. 发明专利

AU2004281536B9 Novel alanyl-amino peptidase inhibitors for functionally influencing different cells and treating immunological, inflammatory, neuronal, and other diseases 未知
公开(公告)号：AU2004281536B9
公开(公告)日：2009-10-08
申请号：AU2004281536
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK PHARMACEUTICALS AG
发明人： ANSORGE SIEGFRIED , NORDHOFF KARSTEN , TAGER MICHAEL , STRIGGOW FRANK , BANK UTE
IPC分类号： C07C259/06 , A61K31/00 , A61K31/4015 , 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
摘要： The invention relates to substances which specifically inhibit peptidases splitting ala-p-nitroanilide for use in medicine. The invention further relates to the use of at least one such substance or of a pharmaceutical or cosmetic composition containing at least one such substance for the prophylaxis and therapy of diseases, in particular the prophylaxis and therapy of diseases with an overshooting immune response (autoimmune diseases, allergies and transplant rejections), of other chronic inflammatory diseases, neuronal diseases and brain damages, skin diseases (acne and psoriasis, among others), tumor diseases and special virus infections (including SARS).

4. 发明专利

AU2004280090B2 Dual alanyl aminopeptidase and dipeptidyl peptidase IV inhibitors for functionally influencing different cells and for treating immunological, inflammatory, neuronal and other diseases 未知
公开(公告)号：AU2004280090B2
公开(公告)日：2009-08-13
申请号：AU2004280090
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK PHARMACEUTICALS AG
发明人： STRIGGOW FRANK , NORDHOFF KARSTEN , TAGER MICHAEL , BANK UTE , ANSORGE SIEGFRIED
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
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.

5. 发明专利

AU2004281959B2 Novel dipeptidyl peptidase IV inhibitors used for functionally influencing different cells and treating immunological, inflammatory, neuronal, and other diseases 未知
公开(公告)号：AU2004281959B2
公开(公告)日：2009-07-23
申请号：AU2004281959
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK PHARMACEUTICALS AG
发明人： TAGER MICHAEL , BANK UTE , STRIGGOW FRANK , NORDHOFF KARSTEN , ANSORGE SIEGFRIED
IPC分类号： C07D205/08 , 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 , C07D213/82 , C07D225/02 , C07D401/12 , C07D405/12 , C07D417/12 , C07F9/6506
摘要： The present invention relates to substances capable of specifically inhibiting Gly-Pro-p-nitroanilide cleaving peptidases, for a use in the medical field. Furthermore, the invention relates to the use of at least one of such substances or of at least one pharmaceutical or cosmetic composition containing at least one such substance for a prophylaxis or a therapy of diseases, particularly for a prophylaxis and a therapy of diseases accompanied by an excessive immune response (autoimmune diseases, allergies, transplant rejections), of other chronic-inflammatory diseases, of neuronal diseases and cerebral damage, of skin diseases (inter alia acne, psoriasis), of tumor diseases and of specific virus infections (inter alia SARS).

6. 发明专利

AU2004280090A1 Dual alanyl aminopeptidase and dipeptidyl peptidase IV inhibitors for functionally influencing different cells and for treating immunological, inflammatory, neuronal and other diseases 未知
公开(公告)号：AU2004280090A1
公开(公告)日：2005-04-21
申请号：AU2004280090
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG
发明人： STRIGGOW FRANK , NORDHOFF KARSTEN , TAGER MICHAEL , BANK UTE , ANSORGE SIEGFRIED
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
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.

7. 发明专利

AU2008290827A1 Method for activating regulatory t-cells 未知
公开(公告)号：AU2008290827A1
公开(公告)日：2009-02-26
申请号：AU2008290827
申请日：2008-08-21
申请人： IMTM GMBH
发明人： WOLKE CARMEN , TAGER MICHAEL , TADJE JANINE , BANK UTE , LENDECKEL UWE , ANSORGE SIEGFRIED
IPC分类号： A61K31/165 , A61K31/40 , A61K31/513 , A61P35/00

8. 发明专利

AU2006314813A1 Novel dual-use peptidase inhibitors as prodrugs for a therapy of inflammatory and other diseases 未知
公开(公告)号：AU2006314813A1
公开(公告)日：2007-05-24
申请号：AU2006314813
申请日：2006-11-10
申请人： IMTM GMBH
发明人： REICHSTEIN IRENE , BANK UTE , FUCHS PETRA , TAGER MICHAEL , NEUBERT KLAUS , ANSORGE SIEGFRIED , FAUST JURGEN , 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.

9. 发明专利

AU2004281959A1 Novel dipeptidyl peptidase IV inhibitors used for functionally influencing different cells and treating immunological, inflammatory, neuronal, and other diseases 未知
公开(公告)号：AU2004281959A1
公开(公告)日：2005-04-28
申请号：AU2004281959
申请日：2004-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG
发明人： TAGER MICHAEL , BANK UTE , STRIGGOW FRANK , NORDHOFF KARSTEN , ANSORGE SIEGFRIED
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
摘要： The present invention relates to substances capable of specifically inhibiting Gly-Pro-p-nitroanilide cleaving peptidases, for a use in the medical field. Furthermore, the invention relates to the use of at least one of such substances or of at least one pharmaceutical or cosmetic composition containing at least one such substance for a prophylaxis or a therapy of diseases, particularly for a prophylaxis and a therapy of diseases accompanied by an excessive immune response (autoimmune diseases, allergies, transplant rejections), of other chronic-inflammatory diseases, of neuronal diseases and cerebral damage, of skin diseases (inter alia acne, psoriasis), of tumor diseases and of specific virus infections (inter alia SARS).

10. 发明专利

AU2002344178A1 Medicament containing an effector of the glutathione metabolism together with $g(a)-lipoic acid for treating diabetes mellitus 未知
公开(公告)号：AU2002344178A1
公开(公告)日：2002-12-09
申请号：AU2002344178
申请日：2002-05-27
申请人： ESPARMA GMBH , IMTM GMBH
发明人： ANSORGE SIEGFRIED , KOEGST DIETER , TAGER MICHAEL , FRIES GERHARD
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

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