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21. 发明专利

DE10125882B4 未知
公开(公告)号：DE10125882B4
公开(公告)日：2007-03-29
申请号：DE10125882
申请日：2001-05-28
申请人： ESPARMA GMBH , IMTM GMBH
发明人： TAEGER MICHAEL , ANSORGE SIEGFRIED , FRIES GERHARD , KOEGST DIETER
IPC分类号： A61K31/381 , C07D207/16 , A61K31/136 , A61K31/137 , A61K31/36 , A61K31/385 , A61K31/401 , A61K31/403 , A61K38/55 , A61K45/00 , A61P3/10 , A61P43/00

22. 发明专利

DE10348023A1 未知
公开(公告)号：DE10348023A1
公开(公告)日：2005-05-19
申请号：DE10348023
申请日：2003-10-15
申请人： IMTM GMBH , KEYNEUROTEK AG
发明人： ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , TAEGER MICHAEL , STRIGGOW FRANK
IPC分类号： A61K31/00 , 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 , C07D307/52 , C07D403/12 , C07D405/14 , C07D407/12 , C07D417/14 , C07C235/32 , A61K31/34
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).

23. 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.

24. 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).

25. 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.

26. 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).

27. 发明专利

CA2772975A1 NOVEL MULTIFUNCTIONAL PEPTIDASE INHIBITORS, ESPECIALLY FOR MEDICAL USE 未知
公开(公告)号：CA2772975A1
公开(公告)日：2011-03-10
申请号：CA2772975
申请日：2010-08-26
申请人： IMTM GMBH
发明人： ANSORGE SIEGFRIED , BANK UTE , NORDHOFF KARSTEN , ROEHNERT PETER , STEFIN SOFIA , STRIGGOW FRANK , TAEGER MICHAEL
IPC分类号： C07C237/20 , A61K31/164 , A61K31/165 , A61P3/10 , A61P17/00 , A61P29/00 , A61P37/00 , C07C237/22 , C07C271/20 , C07D213/56 , C07D239/26 , C07D263/24 , C07D277/06 , C07D295/185 , C07D333/24
摘要： The invention relates to compounds of the general formula (1) 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 medicine.

30. 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).

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