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Nabriva Therapeutics

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Novak R.,Nabriva Therapeutics
Annals of the New York Academy of Sciences | Year: 2011

In 1951, the first reference to the antibacterial substance pleuromutilin was made in a paper published in theProceedings of the National Academy of Sciences. Researchers had identified several species of the mold genusPleurotusthat inhibited the growth ofStaphylococcus aureus. The elucidation of the structure in 1962 led to the initiation of a development program at Sandoz, which was followed by the approval of tiamulin in 1979 for use in veterinary medicine. Although in 2007 retapamulin became the first pleuromutilin approved for topical use in humans, it was not until 2011, exactly 60 years after the first mention of the class, that a pleuromutilin antibiotic, BC-3781, could be tested successfully in a clinical phase II trial for systemic use in patients. This review will discuss key aspects of this antibacterial class and provide some insight into the question of why it took half a century to develop a systemic pleuromutilin for human use. © 2011 New York Academy of Sciences.


Patent
Nabriva Therapeutics | Date: 2012-10-26

A process for the preparation of 14-O[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl)acetyl]mutilins of formula feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.


A compound of formula (I)n is 0 to 4;m is 0 or 1 with the proviso that the sulphur atom and R_(3) are in vicinal position (if m = 0 then R_(3) is in position 2, and if m = 1 then R_(3) is on position 1);R is ethyl or vinyl;R_(1) is hydrogen or (C_(1-6))alkyl,R_(2) is hydrogen or- (C_(3)-_(6))cycloalkyl, or- unsubstituted (C_(1)-_(6))alkyl, or- (C_(1)-_(6))alkyl substituted by one or more of- hydroxy; preferably one or two,- methoxy,- halogen,- (C_(3)-_(6))cycloalkyl, orR_(1) and R_(2) 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, orR_(1) is hydroxy and R_(2) is formyl;R_(3) is OH, OR_(4), a halogen atom, or- with the proviso that R_(3) is bound to 2 R_(3) represents -O-(CH_(2))_(p)-O- with p is 2 or 3;R_(4) is unsubstituted (C_(1)-_(6))alkyl or (C_(3)-_(6))cycloalkyl.


Patent
Nabriva Therapeutics | Date: 2015-01-21

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 formula processes for the preparation of such compounds and their use as pharmaceuticals.


Patent
Nabriva Therapeutics | Date: 2011-01-12

A process for the preparation of 14-O-[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl) acetyl]mutilins of formula


Patent
Nabriva Therapeutics | Date: 2011-05-23

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.


Patent
Nabriva Therapeutics | Date: 2011-11-30

A compound of formula


Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C_(0-4))alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C_(0-4))alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C_(0-4))alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C_(0-4))alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C_(0-4))alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C_(0-4))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.


Compounds selected from the group ofN-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C_(0-4))alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C_(0-4))alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C_(0-4))alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C_(0-4))alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C_(0-4))alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C_(0-4))alkyt-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.


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

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