公开(公告)号：US5247076A

公开(公告)日：1993-09-21

申请号：US921181

申请日：1992-08-04

申请人： Mark Goulet ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

发明人： Mark Goulet ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

IPC分类号： C07H19/01 ,  A61K20060101 ,  A61K31/395 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/435 ,  A61K31/436 ,  A61K31/70 ,  A61K31/7056 ,  A61P37/06 ,  C07D20060101 ,  C07D498/12 ,  C07D498/18 ,  C07H7/06 ,  C07H15/04 ,  C07H19/02

CPC分类号： C07H19/01

摘要： Imidazolidyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

公开(公告)号：US5057499A

公开(公告)日：1991-10-15

申请号：US360621

申请日：1989-06-02

申请人： Helmut Mrozik ,  Peter J. Sinclair

发明人： Helmut Mrozik ,  Peter J. Sinclair

IPC分类号： C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC分类号： C07H19/01 ,  A01N43/90

摘要： There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the perhydrooxepine derivatives. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US4978656A

公开(公告)日：1990-12-18

申请号：US231318

申请日：1988-08-12

申请人： Timothy A. Blizzard ,  Helmut Mrozik ,  Gaye Marino ,  Peter J. Sinclair

发明人： Timothy A. Blizzard ,  Helmut Mrozik ,  Gaye Marino ,  Peter J. Sinclair

IPC分类号： H04N5/222 ,  A01N43/90 ,  A61K31/435 ,  A61K31/495 ,  A61P33/10 ,  C07D471/18 ,  C07D471/22 ,  C07D491/22 ,  C07D498/22 ,  C07F7/18 ,  C07F9/6561 ,  G06T7/00 ,  H04N5/232 ,  H04N5/33 ,  H04N5/365 ,  H04N17/00

CPC分类号： C07D491/22 ,  A01N43/90 ,  C07D498/22 ,  C07F7/1856 ,  C07F9/6561

摘要： There are disclosed synthetic derivatives of the natural product paraherquamide. The synthetic derivatives are prepared by reactions at the parahequamide A, B, E, F and G rings, that is at carbon atoms 14 to 16, the lactam ring and carbon atoms 24 to 26 as well as carbon atoms 5 and 12. The compounds are active antiparasitic agents and compositions for that use are also disclosed.

公开(公告)号：US4897383A

公开(公告)日：1990-01-30

申请号：US309569

申请日：1989-02-13

申请人： Peter J. Sinclair

发明人： Peter J. Sinclair

IPC分类号： C07H17/08 ,  A01N43/90 ,  A01N47/34 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC分类号： C07H19/01 ,  A01N43/90

摘要： There are disclosed novel avermectin derivatives wherein the 3"- or 3'-methoxy group and/or the 4"- or 4'-hydroxyl group are replaced by hydrogen. The 3"- or 3'-desmethoxy-avermectins can further be derivatized at the 4"- or 4'-positions as the amino, semicarbazone or oxime analogs. The 3"- or 3'-desmethoxy-avermectins are prepared by the reaction of Samarium iodide on the corresponding 4"- or 4'-oxo-avermectins. The 4"- or 4'-deoxo-avermectins are prepared by radical deoxygenation of the corresponding hydroxy-avermectins. Di-deoxygenated avermectin derivatives are obtained by combination of these two methods or by treating avermectin aglycone or avermectin monosaccharide with a dihydropyran. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.