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81. 发明专利

CA2598360A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH PROTEASE INHIBITORY ACTIVITY 未知
公开(公告)号：CA2598360A1
公开(公告)日：2006-08-24
申请号：CA2598360
申请日：2005-02-17
申请人： POLYPHOR LTD , UNIV ZUERICH
发明人： GOMBERT FRANK , MOEHLE KERSTIN , LUDIN CHRISTIAN , HENZE HEIKO , SELLIER ODILE , DEMARCO STEVEN J , JUNG FRANCOISE , OBRECHT DANIEL
IPC分类号： C07K7/06 , A61K38/04 , C07K7/08 , C07K7/64
摘要： wherein Z is a chain of 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

82. 发明专利

AU2005327825A1 Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity 未知
公开(公告)号：AU2005327825A1
公开(公告)日：2006-08-24
申请号：AU2005327825
申请日：2005-02-17
申请人： UNIV ZUERICH , POLYPHOR LTD
发明人： OBRECHT DANIEL , JUNG FRANCOISE , MOEHLE KERSTIN , HENZE HEIKO , LUDIN CHRISTIAN , GOMBERT FRANK , SELLIER ODILE , DEMARCO STEVEN J
IPC分类号： C07K7/06 , A61K38/04 , C07K7/08 , C07K7/64
摘要： wherein Z is a chain of 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

83. 发明专利

BR0215855A 未知
公开(公告)号：BR0215855A
公开(公告)日：2005-07-12
申请号：BR0215855
申请日：2002-08-20
申请人： UNIVERSITOT ZUERICH , POLYPHOR LTD
发明人： VRIJBLOED JAN WIM , OBRECHT DANIEL , ROBINSON JOHN ANTHONY , SELLIER ODILE , KESSLER MARC
IPC分类号： A61K38/00 , A61P31/04 , C07K1/04 , C07K5/078 , C07K7/64 , C07K7/08 , A61K38/12
摘要： Template-fixed &bgr;-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 α-amino acid residues which, depend on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa and Acinetobacter. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. In a specific embodiment, the template is based on the D-Pro-L-Pro dipeptides. These &bgr;-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid—and solution phase synthetic strategy.

84. 发明专利

CA2496215A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIBACTERIAL ACTIVITY 未知
公开(公告)号：CA2496215A1
公开(公告)日：2004-03-04
申请号：CA2496215
申请日：2002-08-20
申请人： POLYPHOR LTD , UNIV ZUERICH
发明人： ROBINSON JOHN ANTHONY , SELLIER ODILE , KESSLER MARC , OBRECHT DANIEL , VRIJBLOED JAN WIM
IPC分类号： A61K38/00 , A61P31/04 , C07K1/04 , C07K5/078 , C07K7/64 , C07K7/08 , A61K38/12
摘要： Template-fixed .beta.-hairpin peptidomimetics of the general formula (I), wherein Z is a template-fixed chain of 12 .alpha.-amino acid residues which, depending on their positions in the chain (counted starting from the N- terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and t he claims, and salts thereof, have the property to selectively inhibit the grow th of or to kill microorganisms such as Pseudomonas aeruginosa and Acinetobacte r. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. In a specific embodiment, the template is based on the D-Pro-L-P ro dipeptide. These .beta.-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

85. 发明专利

BRPI0721259C1 composto, composição farmacêutica, uso de composto, e, processo para a fabricação de composto 未知
公开(公告)号：BRPI0721259C1
公开(公告)日：2021-05-25
申请号：BRPI0721259
申请日：2007-02-28
申请人： POLYPHOR LTD , UNIV ZUERICH
发明人： BARBARA ROMAGNOLI , CHRISTIAN LUDIN , DANIEL OBRECHT , FRANK GOMBERT , HEIKO HENZE , JAN WIM VRIJBLOED , JOHN ANTHONY ROBINSON , KERSTIN MOEHLE , RESHMI MUKHERJEE , STEVEN J DEMARCO
IPC分类号： A61K38/12 , C07K7/56
摘要： composto, composição farmacêutica, uso de composto, e, processo para a fabricação de composto. os peptidomiméticos tipo grampo de cabelo (beta) fixados sobre matriz ciclo(-tyr-his-x-cys-ser-ala-dpro-dab-arg-tyr-cys-tyr-gln-lys- pro-pro), ligação de dissulfeto entre cys4 e gys11, e sais farmaceuticamente aceitáveis destes, com x sendo ala ou tyr, têm propriedades antagonizadoras cxcr4 e podem ser usados para prevenir infecções por hiv em indivíduos saudáveis ou para diminuir e parar a progressão viral em pacientes infectados; ou onde o câncer é mediado ou resultante da atividade receptora de cxcr4; ou onde as doenças imunológicas são mediadas ou resultantes da atividade receptora de cxcr4; ou para tratar a imunossupressão; ou, em particular, para a mobilização das células tronco das células tronco do sistema periférico e/ou célula tronco mesenquimal (msc) e/ou outras células tronco cuja retenção depende do receptor de cxcr4. estes peptidomiméticos tipo grampo de cabelo (beta) podem ser fabricados através de um processo que é fundamentado em um estratégia sintética de fase sólida e de solução, usando métodos que são bem, conhecidos àqueles adequadamente habilitados na química peptídica.

86. 发明专利

NO342041B1 Templatfikserte β-hårnålspeptidomimetika, sammensetning innholdende disse, anvendelse derav samt fremgangsmåter for fremstilling derav. 未知
公开(公告)号：NO342041B1
公开(公告)日：2018-03-12
申请号：NO20074674
申请日：2007-09-13
申请人： POLYPHOR LTD , UNIV ZUERICH
发明人： GOMBERT FRANK , DEMARCO STEVEN J , MOEHLE KERSTIN , HENZE HEIKO , OBRECHT DANIEL , SELLIER ODILE , JUNG FRANÇOISE , LUDIN CHRISTIAN
IPC分类号： C07K1/06 , A61K38/04 , A61K38/08 , A61K38/10 , C07K7/06 , C07K7/08 , C07K7/64
摘要： Templatfikserte ?-hårnålspeptidomimetika av generell formel (I), hvori Z er en kjede av 11??-aminosyrerester som, avhengig av deres stilling i kjeden, (telling starter fra den N-terminale aminosyren) er Gly eller Pro eller Pro(4NHCOPhe), eller er av visse typer som, som de gjenværende symbolene i formelen over, er definert i beskrivelsen og kravene, og salter av disse, som har den egenskapen å hemme proteaser, særlig serinproteaser, særlig katepsin G, elastase eller tryptase. Disse hårnålspeptidomimetika kan bli fremstilt ved fremgangsmåter som er basert på en blanding av fast- og løsningsfase syntesestrategi.

87. 发明专利

CY1111282T1 ΠΕΠΤΙΔΟΜΙΜΗΤΕΣ ΣΤΑΘΕΡΟΥ ΕΚΜΑΓΕΙΟΥ 未知
公开(公告)号：CY1111282T1
公开(公告)日：2015-08-05
申请号：CY101100950
申请日：2010-10-22
申请人： POLYPHOR LTD
发明人： DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , OBRECHT DANIEL , GOMBERT FRANK , LUDIN CHRISTIAN , VRIJBLOED JAN WIM
IPC分类号： C07K7/56 , A61K38/12
摘要： Οισταθερού-εκμαγείουβ-φουρκέταςπεπτιδομιμητές Kυκλo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), δισουλφιδικούδεσμούμεταξύ Cys4 και Cys11, καιφαρμακευτικώςαποδεκτάάλατααυτών, μετοΧ ναείναι Ala ή Tyr, έχουν CXCR4 ανταγωνιστικέςιδιότητεςκαιμπορείναχρησιμοποιηθούνγιαπρόληψη HIV μολύνσεωνσευγιήάτομαή γιαεπιβράδυνσηκαιδιακοπήτηςιικήςεξέλιξηςσεμολυσμένουςασθενείς˙ή όπουΚαρκίνοςδιαμεσολαβείταιή προκύπτειαπόδραστικότητα CXCR4 υποδοχέα˙ή όπουανοσολογικέςνόσοιδιαμεσολαβούνταιή προκύπτουναπόδραστικότητα CXCR4 υποδοχέα- ήγιααντιμετώπισηανοσοκαταστολής- ή, συγκεκριμένα, γιακινητοποίησηβλαστικώνκυττάρωνπεριφερειακούαίματοςβλαστικώνκυττάρωνκαι/ήμεσεγχυματικώνβλαστικώνκυττάρων (MSC), και/ήάλλωνβλαστικώνκυττάρωντωνοποίωνη διατήρησηεξαρτάταιαπότον CXCR4 υποδοχέα. Αυτοίοιβ-φουρκέταςπεπτιδομιμητέςμπορείναπαρασκευαστούνμεμιαδιαδικασίαη οποίαβασίζεταισεμιαμεικτήστερεής- καιδιαλυμένης-φάσηςσυνθετικήστρατηγική, χρησιμοποιώνταςμεθόδουςοιοποίεςείναιπολύγνωστέςστουςεπαρκώςειδικευμένουςστηνπεπτιδικήχημεία.

88. 发明专利

ES2491166T3 Miméticos de lazo de horquilla beta fijados a patrón y su utilización en exposición en fagos 未知
公开(公告)号：ES2491166T3
公开(公告)日：2014-09-05
申请号：ES03779935
申请日：2003-11-15
申请人： POLYPHOR LTD , UNIVERSITÄT ZÜRICH
发明人： VRIJBLOED JAN WIM , OBRECHT DANIEL , LOCURIO SERGIO , GOMBERT FRANK OTTO , LUDIN CHRISTIAN , JUNG FRANÇOISE
IPC分类号： C12N15/10 , C07K1/04 , C07K7/04 , C40B40/02
摘要： Compuesto de la fórmula R1-Cys-Z-Cys-R2 (I), en el cual cada uno de los Cys es un residuo L-cisteína, los dos grupos -SH de los dos residuos L-cisteína se sustituyen por un grupo -S-S-, R1 y R2 son Glu-Thr y Thr-Lys; o Lys-Thr y Thr-Glu; o Thr-Glu y Lys-Thr; o Thr-Lys y Glu-Thr; o Leu- Glu y Lys-Val; o Val-Lys y Glu-Leu; o Glu-Leu y Val-Lys; o Lys-Leu y Val-Glu; o Glu-Leu-Lys y Glu-Val-Lys; o Lys- Val-Glu y Lys-Leu-Glu; o Leu-Glu-Lys y Glu-Lys-Val; o Val-Lys-Glu y Lys-Glu-Leu; o Glu-Lys-Leu y Val-Glu-Lys; o Lys-Glu-Val y Leu-Lys-Glu; o Lys-Glu-Leu y Val-Lys-Glu; o Glu-Lys-Val y Leu-Glu-Lys, y Z es una cadena de 6 hasta 20 residuos aminoacídicos, siendo cada uno de estos residuos, independientemente, el residuo de un aminoácido L10 alfa de origen natural, con la condición, de que Z contenga una de las fracciones -Lys-Trp- Phe-Ser-Asn-His-Tyr-Gln- [SEQ ID NO:23]; y -Phe-Leu-Ala-His-Tyr-Ala- [SEQ ID NO:24].

89. 发明专利

SI1856140T1 Matrično fiksirani beta-lasnični peptidomimetiki z inhibitorno aktivnostjo za proteaze 未知
公开(公告)号：SI1856140T1
公开(公告)日：2014-04-30
申请号：SI200531837
申请日：2005-02-17
申请人： UNIV ZUERICH , POLYPHOR LTD
发明人： DE MARCO STEVEN J , MOEHLE KERSTIN , HENZE HEIKO , SELLIER ODILE , JUNG FRANCOISE , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K7/00 , A61K38/00

90. 发明专利

PT1856140E PEPTIDOMIMÉTICOS EM GANCHO DE CABELO BETA, FIXADOS EM MATRIZ, TENDO ACTIVIDADE INIBIDORA DE PROTEASES 未知
公开(公告)号：PT1856140E
公开(公告)日：2014-03-27
申请号：PT05707463
申请日：2005-02-17
申请人： POLYPHOR LTD , UNIVERSITÄT ZÜRICH
发明人： GOMBERT FRANK , HENZE HEIKO , OBRECHT DANIEL , LUDIN CHRISTIAN , MARCO STEVEN J DE , MOEHLE KERSTIN , SELLIER ODILE , JUNG FRANÇOISE
IPC分类号： C07K7/06 , A61K38/04 , C07K7/08 , C07K7/64

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