US 2014/0005100 A1Published application

Novel cyclosporin derivatives for the treatment and prevention of a viral infection

AssigneeS&T Global Inc.

InventorsZhuang Su, Zhengyu Long, Zhennian Huang, Suizhou Yang

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Abstract

The present invention relates to a compound of the formula (I), (II), (III), (IV), (V), or (VI) or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection using the same.

Claims44

Dependent claims

A compound of the formulae (I), (II), (III), (IV), (V) or (VI):

or pharmaceutically acceptable salt thereof, wherein the symbols have the following meanings and are, for each occurrence, independently selected:
R1 is n-butyl or (E)-but-2-enyl;
R2 is ethyl, 1-hydroxyethyl, isopropyl or n-propyl;
W is O, or S;
each occurrence of R3 and R5 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, or aryl or substituted aryl;
each occurrence Ra and Rb is independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, phenyl or substituted phenyl, or Ra and Rb, together with the nitrogen atom to which they are attached, form a heterocycle or substituted heterocycle;
and
n is an integer of 1, 2, 3, 4, 5, or 6.

5 more elements

A compound selected from:

[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Thiomorpholino)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-methylamino)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Pyrrolidinyl)Butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Piperidinyl)Butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Morpholino)Butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Thiomorpholino)Butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N,N-Dimethylamino)butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N,N-Diethylamino)butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propylamino)butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propyl-N-methylamino)butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propyl-N-ethylamino)butylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-(4-Methyl)pentylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-(5-Methyl)hexylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-2-Methoxypropylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(2-Methoxypropyloxy)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Thiomorpholino)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-(4-Methyl)pentylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-(5-Methyl)hexylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-2-Methoxypropylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-2-(2-Methoxypropyloxy)propylthio-Sar]-3-[(γ-methylthio)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-(4-Methyl)pentylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-(5-Methyl)hexylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-2-Methoxypropylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-2-(2-Methoxypropyloxy)propylthio-Sar]-3-[(γ-methyloxy)methoxy-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Thiomorpholino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-iso-Propylamino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-iso-Propyl-N-methylamino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Thiomorpholino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-4-Methylpiperazinyl)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-methylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Pyrrolidinyl)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Piperidinyl)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Morpholino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Thiomorpholino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-4-Methylpiperazinyl)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N,N-Dimethylamino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N,N-Diethylamino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propylamino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propyl-N-methylamino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propyl-N-ethylamino)butylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-n-Pentylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-(4-Methyl)pentylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-(5-Methyl)hexylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-Methoxypropylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(2-Methoxypropyloxy)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Pyrrolidinyl)ethylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Piperidinyl)ethylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Morpholino)ethylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Thiomorpholino)ethylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-iso-Propyl-N-ethylamino)ethylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Thiomorpholino)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-4-Methylpiperazinyl)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propylamino)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-methylamino)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Pyrrolidinyl)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Piperidinyl)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Morpholino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-Thiomorpholino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N,N-Dimethylamino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N,N-Diethylamino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propylamino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propyl-N-methylamino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-4-(N-iso-Propyl-N-ethylamino)butylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-n-Pentylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-(4-Methyl)pentylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-(5-Methyl)hexylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-2-Methoxypropylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(2-Methoxypropyloxy)propylthio-Sar]-3-[(γ-allyloxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-iso-propoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-iso-propoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-iso-propoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-iso-propoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-iso-propoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-iso-propoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-iso-butoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-iso-butoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-iso-butoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-iso-butoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-iso-butoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-iso-butoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-2-ethylbutoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-2-ethylbutoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-2-ethylbutoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-2-ethylbutoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-2-ethylbutoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-2-ethylbutoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-(2-methoxyethoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[β-(2-methoxyethoxy)-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[β-[2-(2-methoxyethoxy)ethoxy]-NMeSer]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[β-[2-(2-methoxyethoxy)ethoxy]-NMeSer]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-iso-propylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-iso-propylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino) propylthio-Sar]-3-[(β-iso-propylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-iso-propylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-iso-propylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-iso-propylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-iso-butylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-iso-butylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-iso-butylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-iso-butylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-iso-butylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-iso-butylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(β-2-ethylbutylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(β-2-ethylbutylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(β-2-ethylbutylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(β-2-ethylbutylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(β-2-ethylbutylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-2-ethylbutylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[β-(2-methoxyethylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[(β-(2-methoxyethylthio)-NMeCys]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[β-[2-(2-methoxyethoxy)ethylthio]-NMeCys]-4-cyclosporin;
[(R)-3-(N-Morpholino)propylthio-Sar]-3-[β-[2-(2-methoxyethoxy)ethylthio]-NMeCys]-4-cyclosporin:
[(β-Methoxy)-NMeSer]-4-cyclosporin;
[(β-iso-Propoxy)-NMeSer]-4-cyclosporin;
[(β-Pentan-3-yloxy)-NMeSer]-4-cyclosporin;
[(β-iso-Butoxy)-NMeSer]-4-cyclosporin;
[(β-2-Ethylbutoxy)-NMeSer]-4-cyclosporin;
[(β-2-(N,N-Diethylamino)ethoxy)-NMeSer]-4-cyclosporin;
[β-(2-Methoxyethoxy)-NMeSer]-4-cyclosporin;
[β-[2-(2-Methoxyethoxy)ethoxy]-NMeSer]-4-cyclosporin;
[(β-Methylthio)-NMeCys]-4-cyclosporin;
[(β-iso-Propylthio)-NMeCys]-4-cyclosporin;
[(β-Pentan-3-ylthio)-NMeCys]-4-cyclosporin;
[(β-iso-Butylthio)-NMeCys]-4-cyclosporin;
[(β-2-Ethylbutylthio)-NMeCys]-4-cyclosporin;
[(β-2-(N,N-Diethylamino)ethylthio)-NMeCys]-4-cyclosporin;
[β-(2-Methoxyethylthio)-NMeCys]-4-cyclosporin;
and
[β-[2-(2-Methoxyethoxy)ethylthio]-NMeCys]-4-cyclosporin, or a pharmaceutically acceptable salt thereof.

158 more elements

A compound selected from:

[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Morphlino)propylthio-Sar]-3-[(γ-hydroxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Dimethylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N,N-Diethylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-methylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-iso-Propyl-N-ethylamino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Pyrrolidinyl)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Piperidinyl)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Morphlino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-Thiomorpholino)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-3-(N-4-Methylpiperazinyl)propylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N,N-Diethylamino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-iso-Propylamino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-iso-Propyl-N-methylamino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-iso-Propyl-N-ethylamino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Pyrrolidinyl)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Piperidinyl)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Morpholino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
[(R)-2-(N-Thiomorpholino)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
and
[(R)-2-(N-4-Methylpiperazinyl)ethylthio-Sar]-3-[(γ-methoxy)-NMeLeu]-4-cyclosporin;
or a pharmaceutically acceptable salts thereof.

23 more elements

Dependencies are inferred from the claim text.

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Abstract