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1. 发明专利

CA2847490C TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 未知
公开(公告)号：CA2847490C
公开(公告)日：2015-11-17
申请号：CA2847490
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ZUMBRUNN JURG , DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , A61K38/19 , A61P31/18 , C07K1/04 , C07K1/06 , C07K7/08 , C07K14/715 , C40B40/10
摘要： Template-fixed .beta.-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 .alpha.-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These .beta.-hairpin peptidornimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

2. 发明专利

ES2550241T3 Peptidomiméticos en horquilla beta fijados sobre una plantilla, con actividad antagonista con respecto a CXCR4 未知
公开(公告)号：ES2550241T3
公开(公告)日：2015-11-05
申请号：ES04730251
申请日：2004-04-29
申请人： POLYPHOR AG , UNIVERSITÄT ZÜRICH
发明人： ZUMBRUNN JÜRG , DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , C07K1/04
摘要： Compuesto de fórmula general**Fórmula** en la que**Fórmula** es DPro-LPro; y Z es una cadena de 14 residuos de a aminoácidos, contándose las posiciones de dichos residuos de aminoácidos empezando desde el aminoácido terminal N, de manera que estos residuos de aminoácidos son, dependiendo de su posición en la cadena**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** formando Cys en P4 y P11 un puente de bisulfuro; o bien**Tabla** Cys en P4 y P11 forman un puente de bisulfuro; y sales farmacéuticamente aceptables del mismo.

3. 发明专利

EA010163B1 СВЯЗАННЫЕ С МАТРИЦЕЙ ПЕПТИДОМИМЕТИКИ β-ШПИЛЕЧНОЙ СТРУКТУРЫ С АКТИВНОСТЬЮ АНТАГОНИСТОВ CXCR4 未知
公开(公告)号：EA010163B1
公开(公告)日：2008-06-30
申请号：EA200501550
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ZUMBRUNN JURG , DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , A61P31/18 , C07K1/04
摘要： Связанныес матрицейβ-шпилечныепептидомиметикиобщейформулы (I)где Z представляетсобойсвязаннуюс матрицейцепочкуиз 12, 14 или 18 α-аминокислотныхостатков, которые, взависимостиотположенияв цепи (считая, начинаяс N-концевойаминокислоты), представляютсобой Gly, NMeGly, Pro, или Pip, илиостаткиопределенныхтипов, которые, каки остальныесимволыв приведеннойвышеформуле, определеныв описаниии формулеизобретения, исолиэтихсоединений, которыеобладаютсвойствамиантагонистов CXCR4 имогутприменятьсядляпредотвращенияВИЧ-инфекцийу здоровыхлюдейилидлязамедленияилиостановкиразвитиявирусау инфицированныхпациентов; илив случае, еслиракопосредованиливызванактивностьюрецептора CXCR4; илив случае, еслииммунологическиезаболеванияопосредованыиливызваныактивностьюрецептора CXCR4; илидлялеченияиммуносупрессии; илиприаферезномсборестволовыхклетокпериферическойкрови. Этиβ-шпилечныепептидомиметикиможнополучатьприпомощиспособа, основанногонасмешаннойстратегиитвердофазногосинтезаи синтезав растворе.

4. 发明专利

BRPI0409928A 未知
公开(公告)号：BRPI0409928A
公开(公告)日：2006-04-25
申请号：BRPI0409928
申请日：2004-04-29
申请人： POLYPHOR AG , UNIVERSITOT ZUERICH
发明人： ZUMBRUNN JUERG , DEMARCO STEVEN J , MUKHERJEE RESHMI , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： A61K38/00 , A61K38/12 , C07K1/04 , C07K7/64
摘要： Template-fixed ²-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 18 ±-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These ²-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

5. 发明专利

CA2524253A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 未知
公开(公告)号：CA2524253A1
公开(公告)日：2004-11-11
申请号：CA2524253
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： LOCIURO SERGIO , DEMARCO STEVEN J , OBRECHT DANIEL , ZUMBRUNN JUERG , LUDIN CHRISTIAN , VRIJBLOED JAN WIM , GOMBERT FRANK , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , ROMAGNOLI BARBARA , MUKHERJEE RESHMI , HENZE HEIKO
IPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , C07K1/04
摘要： Template-fixed .beta.-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 .alpha.-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in t he description and the claims, and salts thereof, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patient s; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collection s of peripheral blood stem cells. These .beta.-hairpin peptidornimetics can be manufactured by a process which is based on a mixed solid- and solution phas e synthetic strategy.

6. 发明专利

CA2524253C TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 未知
公开(公告)号：CA2524253C
公开(公告)日：2016-03-29
申请号：CA2524253
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ZUMBRUNN JUERG , DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , C07K1/04 , C07K1/06 , C07K7/08
摘要： Template-fixed .beta.-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 .alpha.-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These .beta.-hairpin peptidornimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

7. 发明专利

CA2847486C TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 未知
公开(公告)号：CA2847486C
公开(公告)日：2016-03-15
申请号：CA2847486
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ZUMBRUNN JURG , DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K14/00 , A61K38/00 , A61K38/12 , A61K38/19 , A61P31/18 , C07K1/04 , C07K1/06 , C07K7/64 , C07K14/715 , C40B40/10
摘要： Template-fixed .beta.-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 .alpha.-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These .beta.-hairpin peptidornimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

8. 发明专利

AU2004234062B2 Template- fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 未知
公开(公告)号：AU2004234062B2
公开(公告)日：2010-07-15
申请号：AU2004234062
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： MUKHERJEE RESHMI , ROMAGNOLI BARBARA , DEMARCO STEVEN J , VRIJBLOED JAN WIM , GOMBERT FRANK , ZUMBRUNN JURG , HENZE HEIKO , ROBINSON JOHN ANTHONY , LOCIURO SERGIO , OBRECHT DANIEL , MOEHLE KERSTIN , LUDIN CHRISTIAN
IPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , C07K1/04
摘要： Template-fixed ²-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 18 ±-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These ²-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

9. 发明专利

ES2306924T3 PEPTIDOMIMETICOS FIJADOS A UNA MATRIZ COMO MEDICAMENTOS CONTRA EL VIH Y EL CANCER. 未知
公开(公告)号：ES2306924T3
公开(公告)日：2008-11-16
申请号：ES03816774
申请日：2003-05-02
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ZUMBRUNN JURG , DEMARCO J STEVEN , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , MUKHERJEE RESHMI
IPC分类号： C07K7/06 , C07K7/08 , C07K14/00
摘要： Compuestos de fórmula general: (Ver fórmula) en los que (Ver fórmula) es un grupo que presenta una de las fórmulas D Pro-L Pro y L Pro-D Pro R 20 es H; alquilo; alquenilo; o aril-alquilo inferior; R 32 es H; alquilo inferior; o aril-alquilo inferior; R 33 es H; alquilo, alquenilo; -(CH2)m(CHR 61 )sOR 55 ; -(CH2)m(CHR 61 )sNR 34 R 63 ; -(CH2)m(CHR 61 )sOCONR 75 R 82 ; -(CH2)m(CHR 61 )sNR 20 CONR 78 R 82 ; -(CH2)O(CHR 61 )s,COR 64 ; -(CH2)O(CHR 61 )s -CONR 58 R 59 , -(CH2)O(CHR 61 )sPO (OR 60 )2; -(CH2)o(CHR 61 )sSO2R 62 ; o -(CH2)o(CHR 61 )sC6H4R 8 ; R 34 es H; alquilo inferior; arilo, o aril-alquilo inferior; R 33 y R 34 conjuntamente pueden formar: -(CH2)2 - 6-; -(CH2)2O(CH2)2-; -(CH2)2S(CH2)2-; o -(CH2)2NR 57 (CH2)2-; R 37 es H; F; Br; Cl; NO2; CF3; alquilo inferior; -(CH2)p(CHR 61 )sOR 55 ; -(CH2)p(CHR 61 )sNR 33 R 34 ; -(CH2)p(CHR 61 )s OCONR 33 R 75 ; -(CH2)p(CHR 61 )sNR 20 CONR 33 R 12 ; -(CH2)o(CHR 61 )sCOOR 17 ; -(CH2)o(CHR 61 )sCONR 58 R 59 ; -(CH2)o (CHR 61 )sPO(OR 60 )2; -(CH2)o(CHR 61 )sSO2R 62 ; o -(CH2)o(CHR 61 )sC6H4R 8 ; R 50 es H; alquilo inferior; o aril-alquilo inferior; R 55 es H; alquilo inferior; alquenilo inferior; aril-alquilo inferior; -(CH2)m(CHR 61 )sOR 57 ; -(CH2)m(CHR 61 )s NR 34 R 63 ; -(CH2)m(CHR 61 )sOCONR 75 R 82 ; -(CH2)m(CHR 61 )sNR 20 CONR 78 R 82 ; -(CH2)O(CHR 61 )s -COR 64 ; -(CH2)O (CHR 61 )COOR 57 ; o -(CH2)O(CHR 61 )sCONR 58 R 59 ; R 56 es H; alquilo inferior; alquenilo inferior; aril-alquilo inferior; -(CH2)m(CHR 61 )sOR 57 ; -(CH2)m(CHR 61 )s NR 34 R 63 ; -(CH2)m(CHR 61 )sOCONR 75 R 82 ; -(CH2)m(CHR 61 )sNR 20 CONR 78 R 82 ; -(CH2)o(CHR 61 )s -COR 64 ; o -(CH2)o (CHR 61 )sCONR 58 R 59 ; R 57 es H; alquilo inferior; alquenilo inferior; arilo alquilo inferior; o heteroarilo alquilo inferior; R 58 es H; alquilo inferior; alquenilo inferior; arilo; heteroarilo; aril-alquilo inferior; o heteroaril-alquilo inferior; R 59 es...

10. 发明专利

AU2003232254A1 TEMPLATE-FIXED PEPTIDOMIMETICS AS MEDICAMENTS AGAINST HIV AND CANCER 未知
公开(公告)号：AU2003232254A1
公开(公告)日：2004-11-23
申请号：AU2003232254
申请日：2003-05-02
申请人： POLYPHOR AG
发明人： ROBINSON JOHN ANTHONY , ROMAGNOLI BARBARA , ZUMBRUNN JURG , DEMARCO J STEVEN , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , MUKHERJEE RESHMI , MOEHLE KERSTIN , OBRECHT DANIEL
IPC分类号： C07K7/06 , C07K7/08 , C07K14/00
摘要： Template-fixed &bgr;-hairpin peptidomimetics of the General Formula (I); wherein Z1 and Z2 are template-fixed chains of 4 and 6 or 5 and 7 α-amino acid residues and salts thereof. They have CXCR4-antagonizing properties and can be used as medicaments. These &bgr;-sheet peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

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