Claims for Patent: 6,753,445

Summary for Patent: 6,753,445

Title:	Pleuromutilin derivatives having antibacterial activity
Abstract:	A compound selected from 14--O--[(cycloalkyl-sulfanyl)acetyl]mutilins; 14--O--[(cycloalkyl-alkyl-sulfanyl)acetyl] mutilins; 14--O--[(cycloalkoxy)acetyl] mutilins; and 14--O--[(cycloalkyl-alkoxy)acetyl] mutilins and its use as a pharmaceutical.
Inventor(s):	Ascher; Gerd (Kundl, AT), Berner; Heinz (Vienna, AT)
Assignee:	Biochemie Gesellschaft m.b.H. (Kundl, AT)
Application Number:	10/339,611
Patent Claims:	1. A compound which is a 14--O--[(cycloalkyl-sulfanyl)acetyl]mutilin; 14--O--[(cycloalkyl-alkyl-sulfanyl)acetyl] mutilin; 14--O--[(cycloalkoxy)acetyl] mutilin; or 14--O--[(cycloalkyl-alkoxy)acetyl] mutilin. 2. A compound of formula I ##STR9## wherein R is hydrogen; R.sub.1 is hydrogen or a group of formula ##STR10## wherein X is sulphur, oxygen, or NR.sub.10, wherein R.sub.10 is hydrogen or alkyl; and R.sub.9 is amino, alkyl, aryl, or heterocyclyl; and, if X is oxygen, R.sub.9 is additionally hydrogen; Y is sulphur or oxygen; R.sub.2 is hydrogen or one or more substituents; R.sub.4 is hydrogen or alkyl; R.sub.5 is hydrogen or alkyl; R.sub.3 and R.sub.3 ' are hydrogen, deuterium, or halogen; R.sub.6, R.sub.7, and R.sub.8 are hydrogen or deuterium; m is a number selected from 0 to 4; n is a number selected from 0 to 10; and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. 3. A compound of the formula I.sub.p ##STR11## wherein R.sub.1P is hydrogen or the residue of an amino acid. 4. A compound which is 14--O--[(aminocyclohexan-2-yl-sulfanyl)acetyl]mutilin, 14--O--[(aminocyclohexan-3-yl-sulfanyl)acetyl]mutilin, 14--O--[(N-valyl-aminocyclohexan-2-yl)sulfanyl)-acetyl]-mutilin, or 14--O--[(N-valyl-aminocyclohexan-3-yl)sulfanyl)-acetyl]-mutilin. 5. A compound which is 14--O--[(aminocyclohexan-4-yl-sulfanyl)acetyl]mutilin, or 14--O--[(N-valyl-aminocyclohexan-4-yl)sulfanyl)-acetyl]-mutilin. 6. A compound of claim 1 in the form of a salt. 7. A pharmaceutical composition comprising an effective amount of a compound of claim 1 and at least one pharmaceutical carrier or diluent therefor. 8. A method of treatment of microbial diseases which comprises administering to a subject in need of such treatment an effective amount of a compound of claim 1. 9. A method of claim 8 wherein the subject is a non-human animal.