Abstract: Pleuromutilin derivative compounds of the following formula (I), and uses thereof for the treatment of diseases mediated by microbes, are disclosed

Abstract: Pleuromutilin derivative compounds of the following formula (I), and uses thereof for the treatment of diseases mediated by microbes, are disclosed

Abstract: The present invention relates to purification methods of pleuromutilin (I) by means of crystallisation and/or recrystallisation. The process according to the present invention is carried out in the presence of i-propylacetate.

Abstract: Pleuromutilin derivative compounds of the following formula (I), and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: The present invention relates to purification methods of pleuromutilin (I) by means of crystallisation and/or recrystallisation. The process according to the present invention is carried out in the presence of i-propylacetate.

Abstract: A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2?, and if m=1 then R3 is on position 1?); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl; R2 is hydrogen or —(C3-6)cycloalkyl, or —unsubstituted (C1-6)alkyl, or —(C1-6)alkyl substituted by one or more of —hydroxy; preferably one or two, —methoxy, —halogen, —(C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatome e.g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or —with the proviso that R3 is bound to 2? R3 represents —O—(CH2)P—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl.

Abstract: Pleuromutilin derivative compounds of the following formula (I), and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) said formulation being buffered to a pharmaceutically acceptable pH-value, especially a pH-value of from 2 to 6, in particular a pH value of from 3 to 5.5, preferred a pH-value of about 4 to 5, particularly preferred about 5.

Abstract: Pleuromutilin derivative compounds of the following formula (I), and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2?, and if m=1 then R3 is on position 1?); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl; R2 is hydrogen or—(C3-6)cycloalkyl, or—unsubstituted (C1-6)alkyl, or—(C1-6)alkyl substituted by one or more of—hydroxy; preferably one or two,—methoxy,—halogen,—(C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatome e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or—with the proviso that R3 is bound to 2? R3 represents —O—(CH2)P—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl.

Abstract: A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of

Abstract: A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of

Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.

Abstract: Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.

Abstract: A compound of formula (I) wherein Y is oxygen or sulfur, and X1, X2 and X3 are independently of each other hydrogen, halogen, hydroxy or linear or branched (C1-6)-alkoxy, or hydroxy-(C1-6)alkyl or (C1-6)alkoxy-(C1-6)alkyl, mono- or dihalogenated (C1-6)-alkyl, amino(C1-6)-alkyl, hydroxy(C1-6)-alkyl, with one of the two provisos that: (1) at least of X1, X2 and X3 is other than hydrogen, and (2) X2 is other than hydroxy, when X1 and X3 are hydrogen.

Abstract: A compound of formula wherein PROT is an amine protecting group and PROT? is hydrogen; or PROT and PROT? together with the nitrogen atom to which they are attached form a heterocyclic ring as an amine protecting group, and PROT? is a thiol protecting group, processes for its production, intermediates in their production and production of intermediates in stereoisomerically pure form, and their use for the production of pharmaceutically active compounds.

Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.

Abstract: Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.

Abstract: A compound of formula wherein PROT is an amine protecting group and PROT? is hydrogen; or PROT and PROT? together with the nitrogen atom to which they are attached form a heterocyclic ring as an amine protecting group, and PROT? is a thiol protecting group, processes for its production, intermediates in their production and production of intermediates in stereoisomerically pure form, and their use for the production of pharmaceutically active compounds.