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1. 发明申请

WO2007131764A3 NEW HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE THEREOF 审中-公开
标题翻译：用于抑制整合及其使用的新型杂环化合物
公开(公告)号：WO2007131764A3
公开(公告)日：2008-01-10
申请号：PCT/EP2007004283
申请日：2007-05-14
申请人： JERINI AG , ZISCHINSKY GUNTHER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CHRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
发明人： ZISCHINSKY GUNTHER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CHRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
IPC分类号： C07D401/12 , A61K31/44 , A61P29/00 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D405/12 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, 0 and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.
摘要翻译：本发明涉及式（I）化合物，其中：A是选自芳族杂环5元环系的基团; Ar是选自包含任选取代的5元和6元芳环体系的基团，其中环系统含有0,1,2或3个选自N，O和S的杂原子; Z是一个连接子？是式（II）的基团及其用于抑制整联蛋白的用途。

2. 发明专利

BRPI0706800A2 未知
公开(公告)号：BRPI0706800A2
公开(公告)日：2011-04-05
申请号：BRPI0706800
申请日：2007-01-31
申请人： JERINI AG
发明人： ZISCHINSKY GUNTER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
IPC分类号： C07D401/12 , A61K31/4545 , A61P35/00 , C07D471/04
摘要： The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

3. 发明专利

BRPI0711659A2 未知
公开(公告)号：BRPI0711659A2
公开(公告)日：2012-01-17
申请号：BRPI0711659
申请日：2007-05-14
申请人： JERINI AG
发明人： ZOSCHINSKY GUNTHER , STRAGIES ROLAND , OSTERKAMP FRANK , SCHARN DIRK , HUMMEL GERD , KALKHOF HOLGER , ZAHN GRIT , VOSSMEYER DOERTE , CHRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH
IPC分类号： C07D401/12 , A61K31/44 , A61P29/00 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and Ψ is a radical of formula (II) and their use for the inhibition of integrin.

4. 发明专利

CA2635403A1 COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE THEREOF 未知
公开(公告)号：CA2635403A1
公开(公告)日：2007-08-09
申请号：CA2635403
申请日：2007-01-31
申请人： JERINI AG
发明人： REINEKE ULRICH , SCHARN DIRK , ZISCHINSKY GUNTHER , STRAGIES ROLAND , OSTERKAMP FRANK , CHRISTNER-ALBRECHT CLAUDIA , HUMMEL GERD , VOSSMEYER DOERTE , KALKHOF HOLGER , ZAHN GRIT
IPC分类号： C07D401/12 , A61K31/4545 , A61P35/00 , C07D471/04
摘要： The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

5. 发明专利

AU2007211620A1 Compounds for the inhibition of integrins and use thereof 未知
公开(公告)号：AU2007211620A1
公开(公告)日：2007-08-09
申请号：AU2007211620
申请日：2007-01-31
申请人： JERINI AG
发明人： CHRISTNER-ALBRECHT CLAUDIA , HUMMEL GERD , STRAGIES ROLAND , KALKHOF HOLGER , OSTERKAMP FRANK , REINEKE ULRICH , VOSSMEYER DORTE , SCHARN DIRK , ZISCHINSKY GUNTHER , ZAHN GRIT
IPC分类号： C07D401/12 , A61K31/4545 , A61P35/00 , C07D471/04
摘要： The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

6. 发明专利

MX2008014345A NUEVOS COMPUESTOS HETEROCICLICOS PARA LA INHIBICION DE INTEGRINAS Y SU USO. 未知
公开(公告)号：MX2008014345A
公开(公告)日：2008-11-27
申请号：MX2008014345
申请日：2007-05-14
申请人： JERINI AG
发明人： HUMMEL GERD , STRAGIES ROLAND , ZAHN GRIT , OSTERKAMP FRANK , ZISCHINSKY GUNTHER , REINEKE ULRICH , SCHARN DIRK , KALKHOF HOLGER , VOSSMEYER DORTE , CHRISTNER-ALBRECHT CLAUDIA
IPC分类号： C07D401/12 , A61K31/44 , A61P29/00 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： La presente invención se refiere a un compuesto de fórmula G-Z-A-Ar-? en donde A es un radical seleccionado del grupo que comprende sistemas anulares aromáticos, heterocíclicos, de 5 miembros; Ar es un radical seleccionado del grupo que comprende sistemas anulares aromáticos de 5 y 6 miembros sustituidos en forma opcional, por el cual el sistema anular contiene 0, 1, 2 ó 3 heteroátomos seleccionados del grupo que comprende N, O y S; Z es un radical seleccionado en forma individual e independiente del grupo que comprende (CH2)n-E-(CH2)m-L-(CH2)k y (CH2)m-L-(CH2)k, en donde E es un radical que está o bien ausente o bien presente, por lo cual si E está presente, E se selecciona del grupo que comprende O, S, NH, NRa, CO, SO, SO2, acetileno y etileno sustituido; L es un radical que está o bien ausente o bien presente, por lo cual si L está presente, L se selecciona en forma individual e independiente del grupo que comprende O, S, NH, NRb, CO, SO, SO2, etileno sustituido y acetileno; y k, m y n son en forma individual e independiente 0, 1, 2 ó 3; ? es un radical de fórmula (II) (ver fórmula (II)) en donde Q es un radical seleccionado del grupo que comprende un enlace directo, alquilo de 1 a 4 átomos de carbono, C=O, C=S, O, S, CRaRb, NRa-NRb, N=N, CRa=N, N=CRa, (C=O)-O, O-(C=O), SO2, NRa, (C=O)-NRa, NRa-(C=O)-NRb, NRc-(C=O), O-(C=O)-NRc, NRc-(C=O)-O, NRc-(C=S), (C=S)-NRc, NRc-(C=S)-NRd, NRc-SO2 y SO2-NRc. R1, Ra, Rb, Rc, y Rd son radicales que se seleccionan en forma individual e independiente del grupo que comprende H, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, heterociclilo, heterociclilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, arilalquilo, arilalquilo sustituido heteroarilalquilo, heteroarilalquilo sustituido, cicloalquilalquilo, cicloalquilalquilo sustituido, heterociclilalquilo, heterociclilalquilo sustituido, alcoloxi, alquiloxialquilo, alquiloxialquilo sustituido, alquiloxicicloalquilo, alquiloxicicloalquilo sustituido, alquiloxiheterociclilo, alquiloxiheterociclilo sustituido, alquiloxiarilo, alquiloxiarilo sustituido, alquiloxiheteroarilo, alquiloxiheteroarilo sustituido, alquiltioalquilo, alquiltioalquilo sustituido, alquiltiocicloalquilo y alquiltiocicloalquilo sustituido, hidroxi, hidroxi sustituido, oxo, tio, tio sustituido, aminocarbonilo, aminocarbonilo sustituido, formilo, formilo sustituido, tioformilo, tioformilo sustituido, amino, amino sustituido, hidroxilo, hidroxilo sustituido, mercapto, mercapto sustituido, hidrazino, hidrazino sustituido, diazeno, diazeno sustituido, imino, imino sustituido, amidino, amidino sustituido, iminometilamino, iminometilamino sustituido, ureido, ureido sustituido, formilamino, formilamino sustituido, aminocarboniloxi, aminocarboniloxi sustituido, hidroxicarbonilamino, hidroxicarbonilamino sustituido, hidroxicarbonilo, hidroxicarbonilo sustituido, formiloxi, formiloxi sustituido, tioformilamino, tioformilamino sustituido, aminotiocarbonilo, aminotiocarbonilo sustituido, tioureido, tioureido sustituido, sufonilo, sulfonilo sustituido, sulfonamino, sulfonamino sustituido, aminosulfonilo, sustituido aminosulfonilo, ciano y halógeno; R2 es un resto hidrofóbico; R3 es un radical seleccionado del grupo que comprende OH, alquiloxi de 1 a 8 átomos de carbono y arilalquiloxi de 0 a 6 átomos de carbono; R4 es un radical seleccionado del grupo que comprende hidrógeno, halógeno y alquilo de 1 a 4 átomos de carbono; y G es un radical que contiene un resto básico.

7. 发明专利

MX2008008866A COMPUESTOS PARA INHIBICION DE INTEGRINAS Y SU USO. 未知
公开(公告)号：MX2008008866A
公开(公告)日：2008-10-23
申请号：MX2008008866
申请日：2007-01-31
申请人： JERINI AG
发明人： HUMMEL GERD , STRAGIES ROLAND , ZAHN GRIT , OSTERKAMP FRANK , REINEKE ULRICH , ZISCHINSKY GUNTHER , SCHARN DIRK , KALKHOF HOLGER , VOSSMEYER DORTE , CHRISTNER-ALBRECHT CLAUDIA
IPC分类号： C07D401/12 , A61K31/4545 , A61P35/00 , C07D471/04
摘要： La presente invención se refiere a un compuesto de fórmula (I), en donde A es un anillo heterocíclico no aromático, Ar está ausente o es fenileno; ( es un radical de fórmula (II), R2 es una porción hidrofóbica; y G es un radical que contiene una o más porciones seleccionadas del grupo que consiste de NH, OH y una porción básica. Los compuestos son inhibidores de integrinas, especialmente antagonistas del receptor alfa5beta1 de fibronectina, útiles como agentes anti-angiogénicos.

8. 发明专利

CA2652101A1 NEW HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE THEREOF 未知
公开(公告)号：CA2652101A1
公开(公告)日：2007-11-22
申请号：CA2652101
申请日：2007-05-14
申请人： JERINI AG
发明人： CHRISTNER-ALBRECHT CLAUDIA , REINEKE ULRICH , STRAGIES ROLAND , ZISCHINSKY GUNTHER , OSTERKAMP FRANK , VOSSMEYER DORTE , ZAHN GRIT , KALKHOF HOLGER , HUMMEL GERD , SCHARN DIRK
IPC分类号： C07D401/12 , A61K31/44 , A61P29/00 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring syste m contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, 0 and S; Z is a linker and .PSI. is a radical of formula (II) and their use fo r the inhibition of integrin.

9. 发明专利

AU2007251756A1 New heterocyclic compounds for the inhibition of integrins and use thereof 未知
公开(公告)号：AU2007251756A1
公开(公告)日：2007-11-22
申请号：AU2007251756
申请日：2007-05-14
申请人： JERINI AG
发明人： REINEKE ULRICH , ZISCHINSKY GUNTHER , STRAGIES ROLAND , SCHARN DIRK , VOSSMEYER DORTE , KALKHOF HOLGER , HUMMEL GERD , CHRISTNER-ALBRECHT CLAUDIA , ZAHN GRIT , OSTERKAMP FRANK
IPC分类号： C07D401/12 , A61K31/44 , A61P29/00 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and Ψ is a radical of formula (II) and their use for the inhibition of integrin.

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