公开(公告)号：EP1175435B1

公开(公告)日：2005-04-20

申请号：EP00936703.8

申请日：2000-04-29

申请人： Aventis Pharma Deutschland GmbH

发明人： VERTESY, Laszlo ,  KURZ, Michael ,  SCHIELL, Matthias ,  HOFMANN, Joachim

IPC分类号： C07K7/08 ,  A61K38/10 ,  A61P31/00 ,  C12P21/02

CPC分类号： C07K7/08 ,  A61K38/00

摘要： The invention relates to compounds of general formula (I) AcPhe-Aib-Aib-Aib-x-w-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-R, wherein R represents Phe-ol or Phe-al and w, x, y and z have the following meaning a) w represents Gly or Ala; x represents Aib and y and z represent Iva; b) w represents Gly; x, y and z represent Iva; c) w represents Gly; x and z represent Aib and y represents Iva; d) w represents Gly; x, y and z represent Aib; or e) w represents Gly; x and y represent Aib and z represents Iva. The invention also relates to compounds of general formula (II) AcPhe-Iva-Gln-Aib-Ile-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Ser, wherein x represents Hyp or Pro synthesized from Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium. The invention further relates to a method for isolating cephaibols from the culture medium and to the purification thereof. The invention additionally relates to the utilization of cephaibols as pharmaceutically active substances, especially for controlling parasites.

公开(公告)号：EP1175435A1

公开(公告)日：2002-01-30

申请号：EP00936703.8

申请日：2000-04-29

申请人： Aventis Pharma Deutschland GmbH

发明人： VERTESY, Laszlo ,  KURZ, Michael ,  SCHIELL, Matthias ,  HOFMANN, Joachim

IPC分类号： C07K7/08 ,  A61K38/10 ,  A61P31/00 ,  C12P21/02

CPC分类号： C07K7/08 ,  A61K38/00

摘要： The invention relates to compounds of general formula (I) AcPhe-Aib-Aib-Aib-x-w-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-R, wherein R represents Phe-ol or Phe-al and w, x, y and z have the following meaning a) w represents Gly or Ala; x represents Aib and y and z represent Iva; b) w represents Gly; x, y and z represent Iva; c) w represents Gly; x and z represent Aib and y represents Iva; d) w represents Gly; x, y and z represent Aib; or e) w represents Gly; x and y represent Aib and z represents Iva. The invention also relates to compounds of general formula (II) AcPhe-Iva-Gln-Aib-Ile-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Ser, wherein x represents Hyp or Pro synthesized from Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium. The invention further relates to a method for isolating cephaibols from the culture medium and to the purification thereof. The invention additionally relates to the utilization of cephaibols as pharmaceutically active substances, especially for controlling parasites.

公开(公告)号：EP1140042A1

公开(公告)日：2001-10-10

申请号：EP99958170.5

申请日：1999-12-07

申请人： Aventis Pharma Deutschland GmbH

发明人： GERLACH, Uwe ,  HOFMANN, Joachim ,  LANG, Hans, Jochen ,  WEI, AguanWashington Uni. School of Medicine

IPC分类号： A61K31/00 ,  A61K31/353 ,  A61K31/18 ,  A61K31/4433 ,  A61K31/352 ,  A01N43/16 ,  A61P33/10 ,  A61P33/14

CPC分类号： A61K31/4433 ,  A61K31/00 ,  A61K31/18 ,  A61K31/352 ,  A61K31/353

摘要： The invention relates to the utilization of inhibitors of the KQT1 channel in order produce a medicament for treating diseases which are caused by parasitic helminths and ectoparasites. According to the invention, inhibitors of the KQT1 channel depict a novel lethal fundamental constituent for parasitic helminths and ectoparasites. Blockers of the cellular KQT1 channel, said channel occurring in the parasitic helminths and ectoparasites, are therefore used to produce a medicament for treating vertebrates and humans which are afflicted with the parasitic helminths or ectoparasites. These KQT1 blockers are used alone as medicaments or in combination with other medicaments and therapeutic measures. Inhibitors of the KQT1 channel also depict a novel working mechanism for plant pests such as insects, spiders, mollusks and nematoda, and are consequently used in order to produce a plant protective agent.