Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.

Abstract: Optoelectronic devices include triplet blocking compounds of formula I wherein R1 is, independently at each occurrence, C1-20 hydrocarbyl and at least one of R1 is R3; R2 is independently at each occurrence C1-20 hydrocarbyl, C1-20 hydrocarbyloxy, C1-20 thioether, C1-20 hydrocarbylcarbonyloxy or cyano; R3 is —R4XR5; R4 is a direct bond, C1-20 aryl, C1-20 arylalkyl, C1-20 alkylaryl, C1-20 substituted aryl, C1-20 substituted arylalkyl, or C1-20 substituted alkylaryl; R5 is C1-20 hydrocarbyl or C1-20 hydrocarbyl containing at least one S, N, O or P atom between carbon atoms; R6 is C1-20 alkyl or C1-20 substituted alkyl; X is —O—, —S—, —COO—, —OOC—, —CSS—, —SSC—, NR6 or PR6; a is independently at each occurrence 0, 1 or 2; and n is 0 or 1.

Abstract: A novel process for the production of Fmoc (9H-fluoren-9-ylmethoxycarbonyl)-based compounds is provided, wherein a protecting group for the 9-hydroxymethyl group of the fluorene ring system is utilized. These compounds are useful for the modification of protein and peptide drugs.

Abstract: A compound of formula (I) or of formula (II) wherein X is oxygen or sulfur, and Y is a residue of pipecolic acid or a residue of an amino acid, preferably a naturally occurring amino acid.

Abstract: Norbornene monomers with fluorene group and polymer material thereof are disclosed. The norbornene monomers with fluorene group are prepared by Diels-Alder reation. The Norbornene monomers containing fluorene groups are highly active for ring-opening-metathesis polymerization (ROMP), and the molecular weight and PDI value of the obtained polymers are controllable.

Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).

Abstract: A novel process for the production of Fmoc (9H-fluoren-9-ylmethoxycarbonyl)-based compounds is provided, wherein a protecting group for the 9-hydroxymethyl group of the fluorene ring system is utilized. These compounds are useful for the modification of protein and peptide drugs.

Abstract: The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.

Abstract: The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulphonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.

Abstract: Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.

Abstract: An imide compound represented by the formula (I): wherein R1 represents a C1-C20 aliphatic hydrocarbon group etc., W1 represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., and A represents a group represented by the formula (I-1): wherein A1 represents —CH2—CH2— etc., and a chemically amplified resist composition containing the same.

Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.

Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.

Abstract: Disclosed are several different processes that can be utilized to prepare endohedral metallofullerenes with specific characteristics. Processes can be utilized to prepare monoadducts including cycloaddition of functional groups to the [6,6] double bond of a pyrene-type site of the fullerene. Also disclosed are simple, economical methods for separating fullerene isomers based upon the different oxidation potentials of the isomers.

Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.

Abstract: Compounds for utilization as anti-tumor agents against cancer and certain inflammatory and arthritic conditions designed with multiple active sites to cause inhibition and cell death synthesized from the starting compound 1,4,5,8-tetrachloroanthraquinone. Included are anti-tumor compounds of the class 1,4,5,8-tetrakis-alkylaminoalkyl, 1,4,5,8-tetrakis-hydroxyalkylaminoalkyl, 1,4,5,8-tetrakis-chloroethylamino, 1,2-bischloroethylamino-1,4,5,8-tetrakis-aminoethylamino derivatives of Anthraquinone. Also includes mixtures of groupings such as 1-aminoalkylamino-4,5,8-tris-(1,2-dimethyl)aminoalkylamino anthraquinone, 1,2-dichloroethyl 1-aminoalkyl amino-4,5,8-tris-aminoethylamino anthraquinone, bis-1,4aminoalkylamino bis-5,8-alkylaminoanthraquinone, 1,4-bis-chloroalkylamino-5,8-bisaminoalkylamino anthraquinone and others.

Abstract: In accordance with one aspect, the present invention provides a compound of general formula (I), its stereoisomers thereof and/or its pharmaceutically acceptable salts thereof, which have antibacterial activity; with methods of treating infectious diseases in warm blooded animals employing these new compounds. wherein R1 is selected from optionally substituted alkyl.

Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.

Abstract: A novel process for the production of Fmoc (9H-fluoren-9-ylmethoxycarbonyl)-based compounds is provided, wherein a protecting group for the 9-hydroxymethyl group of the fluorene ring system is utilized. These compounds are useful for the modification of protein and peptide drugs.

Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-8)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.

Abstract: The present invention relates to novel salt forms of vildagliptin (LAF237), i.e. salt forms of(S)-1-[(3-hydroxy-1-adamantyl)amino]acetyl-2-cyano-pyrrolidine.

Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

Abstract: The present invention relates to a process for preparing vildagliptin of formula (I) with high chemical and enantiomeric purity and compositions comprising vildagliptin. In addition, the present invention relates to (2S,2?S)-1,1?-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)imino]bis(1-oxo-2,1-ethanediyl)]di(2-pyrrolidinecarbonitrile) of formula (II), processes for preparing, and compositions comprising a compound for formula (II). Furthermore, the invention relates to processes for determining the purity of vildagliptin using a compound of formula (II).

Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-

Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.

Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives.

Abstract: The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulphonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.

Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.

Abstract: The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula VIII wherein R12 and R13 are as defined herein.

Abstract: A novel fluorene compound is provided which has at least one fluorene group represented by the following general formula [III] or [IV]:

Abstract: The present invention relates to aromatic amine derivatives having a specific structure; and organic electroluminescent devices comprising a cathode, an anode and one or plural organic thin film layers including at least a light emitting layer which are sandwiched between the cathode and the anode wherein at least one of the organic thin film layers contains the above aromatic amine derivatives in the form of a single substance or a component of a mixture. There are provided the organic electroluminescent devices exhibiting a long life and a high efficiency of light emission which are capable of emitting a blue light having a high color purity, as well as the aromatic amine derivatives capable of realizing such organic electroluminescent devices.

Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

Abstract: The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and R3 represents a carboxyl group and the like.

Abstract: A carbamate compound is disclosed.

Abstract: A compound of formula (I) wherein R and R2 together with the nitrogen atom to which they are attached form pyrrolidinyl or piperidinyl, R1 is a group of formula (II) R3 and R?3 are hydrogen, deuterium or halogen, R4, R5 and R10 are independently of each other hydrogen or alkyl, R6, R7 and R8 are hydrogen or deuterium; R9 is amino, alkyl, aryl, heterocyclyl or mercapto; and, if X is oxygen, R9 is additionally hydrogen; R?10 is alkyl, X is sulphur, oxygen, NR10, or N+(R?10)2; Y is sulphur or oxygen, and m is 0, 1 or 2; with the proviso that, when R and R2 together with the nitrogen atom to which they are attached form piperidinyl, m is O, Y is S and Y is attached in position 3 of said piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S) -configuration which is e.g. useful as antimicrobial, antibacterial.

Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.

Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is S— or —HC?CH—; and Y is O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen

Abstract: An adamantanetricarboxylic acid derivative is represented by following Formula (1): wherein X is a hydrogen atom or a hydrocarbon group; and R1, R2 and R3 may be the same as or different from one another and are each a carboxyl group which may be protected by a protecting group, or a carbonyl halide group, wherein at least one of R1, R2 and R3 is a carboxyl group which is protected by a protecting group, or a carbonyl halide group.

Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula X-Z-X? where X and X? are, each independently, a (9-fluorenylidene)malononitrile group, and Z is a linking group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.

Abstract: An organic electroluminescence device comprises a cathode, an anode and a layer of an organic thin film comprising one or a plurality of layers and disposed between the cathode and the anode, wherein at least one of the layers in the layer of an organic thin film comprises a laminate of a layer comprising a metal complex having an energy gap of 2.8 eV or greater and a layer of a host material. The organic electroluminescence device exhibits a higher efficiency of light emission and has a longer life than conventional devices while the emitted light has a high luminance.

Abstract: This invention relates to a novel organophotoreceptor that includes: (a) a charge transport material comprising a fluorenone hydrazone having a) least two fluorenone alkylsulfonylphenylhydrazone groups, b) at least two fluorenone pyrrolylhydrazone groups, c) at least two fluorenone benzotriazolylhydrazone groups, d) at least two fluorenone sulfolanylhydrazone groups, e) at least two fluorenone pyrazolylhydrazone groups, f) at least two fluorenone naphthylhydrazone groups, g) at least two fluorenone tetrazolylhydrazone groups, h) at least two fluorenone stilbenylhydrazone groups, or i) at least two fluorenone (9H-fluoren-9-ylidene)benzylhydrazone groups. Some of these fluoreneones may be represented by the formula where n is an integer between 2 and 6, inclusive; R1 is hydrogen, alkyl, or aryl; R2 is alkylsulfonylphenyl or one of its derivatives; X is a linking group having the formula —(CH2)m—, branched or linear.

Abstract: Process for the preparation of stable activated derivatives of carbamic acid, comprising at least one protected amino group and an activated carbamic acid function, from an amino acid derivative in which the amino group is protected. The process includes: a) a step of transformation of the —COOH group of the amino acid derivative into a —CON3 group to obtain an acyl azide; b) a step of transformation of the —CON3 group of the acyl azide into a —NCO group to obtain an isocyanate; c) a step of treating the isocyanate to obtain a stable derivative of carbamic acid.

Abstract: An alizarin-based chromogenic substrate, a composition containing the substrate, and its use to detect the presence of an enzymatic activity are disclosed. The substrate is particularly applicable in the field of biological diagnosis.

Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where the formula is described in the especification; and ?(b) a charge generating compound.

Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula ?where n is an integer between 2 and 6, inclusive; R1 and R2 are, independently, H, halogen, carboxyl, hydroxyl, thiol, cyano, nitro, aldehyde group, ketone group, an ether group, an ester group, a carbonyl group, an alkyl group, an alkaryl group, or an aryl group; X is a linking group having the formula —(CH2)m—, branched or linear, where m is an integer between 0 and 20, inclusive, and one or more of the methylene groups can be optionally replaced by O, S, C?O, O?S?O, a heterocyclic group, an aromatic group, urethane, urea, an ester group, a NR3 group, a CHR4 group, or a CR5R6 group where R3, R4, R5, and R6 are, independently, H, an alkyl group, an alkaryl group, a heterocyclic group, or an aryl group; Y comprises a bond, C, N, O, S, a branched or linear —(CH2)p— gr

Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.