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US 5,344,925 AGranted
Imidazolidyl macrolides having immunosuppressive activity
AssigneeMerck & Co., Inc.
InventorsMark Goulet, Peter J. Sinclair, Frederick Wong, Matthew J. Wyvratt
Life of this patent
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Abstract
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.
Claims7
A compound which is selected from the group consisting of:
- 17-ethyl-1,14-dihydroxy-12-[2'-(4"-(4"'-(meta-phenoxy-tert-butyl acetate)-2"'-imidazolylmethyloxy)-3"-methoxycyclohexyl)-1'-methyl-vinyl]-2 3,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.s up.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1,14-dihydroxy-12-[2'-(4"-(4"'-(meta-phenoxyacetic acid)-2"'-imidazolylmethyloxy)-3"-methoxycyclohexyl)-1'-methylvinyl]-23,25 -dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4azatricyclo[22.3.1.0.sup.4, 9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-14-(N,N-dimethylaminoacetoxy)-12-[2'-(4"-(4"'-(3"",5""-d imethoxyphenyl)-2"'-imidazolylmethyloxy)-3"-methoxycyclohexyl)-1'-methylvin yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3. 1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-14-(3""'-(N,N-diethylamino)-propanoyloxy)-12-[2'-(4"-(4" '-(3"",5""-dimethoxyphenyl)-2"'-imidazolylmethyloxy)-3"-methoxycyclohexyl)- 1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetra-methyl-11,28-dioxa-4-azat ricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-14-(3""'-aminopropanoyloxy)-12-[2'-(4"-(4"'-(3"",5""-dim ethoxyphenyl) -2"'-imidazolylmethyloxy) -3"-methoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,2 1,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-14-(2""',6""'-diaminohexanoyloxy)-12-[2'-(4"-(4"'-(3"",5 ""-dimethoxyphenyl)-2"'-imidazolylmethyloxy)-3"-methoxycyclohexyl)-1'-methy lvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[2 2.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- or a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.