Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: Avermectin and avermectin monosaccharaide compounds, derivatives, and compositions thereof are provided as well as processes for preparing such compounds, derivatives, and compositions. Intermediates in the preparation of avermectin and avermectin monosaccharaide derivatives and methods of controlling pests are also provided. The avermectin and avermectin monosaccharaide derivatives are demonstrated as useful in controlling pests, in particular pests that are harmful to crop plants and to its propagation materials, such as representatives of the class insecta, the order Acarina and the class nematede.

Abstract: Spinetoram is selectively produced in excellent yields by hydrogenating a mixture of 3?-O-ethyl spinosyn J and 3?-O-ethyl spinosyn L in a water miscible organic solvent using hydrogen gas and a heterogeneous catalyst.

Abstract: A compound of formula wherein X? is an anion; n is 1, 2, 3 or 4; R1 is C1-C12alkyl, C3-C8cycloalkyl; or C2-C12alkenyl; R2 is hydrogen, unsubstituted or substituted C1-C12alkyl or C2-C12alkenyl; R3 is hydrogen, unsubstituted or substituted C1-C12alkyl, C3-C12cycloalkyl, C2-C12alkenyl; or C2-C12alkynyl; or R2 and R3 together are an alkylene or alkenylene bridge; and, where applicable, E/Z isomers, E/Z isomeric mixtures and/or tautomers; with the proviso that R1 is not sec-butyl or isopropyl when R2 is H and R3 is methyl; and, where applicable, their possible tautomers; a process for the preparation of those compounds and their tautomers and the use thereof; pesticidal compositions in which the active ingredient has been selected from those compounds and their tautomers; and a process for the preparation of those compositions and the use thereof; intermediates, in free form or in salt form, for the preparation of those compounds and, where applicable, their tautomers, in free form or in salt form, are descr

Abstract: What is described are a compound of the formula (I) Wherein U is —N(R2)OR3 or —N+(O?)?C(RE)RZ); n is 0 or 1; X—Y is —CH?CH— or —CH2—CH2—; R1 is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 and R3 are, for example; independently from each other, —Q, —C(?O)—Z—Q or —CN; RZ and RE are, independently from each other, —Q, —C(?O)—Z—Q or —CN; or RZ and RE together are a three- to seven membered alkylene or alkenylene bridge, which is unsubstituted or mono- to tri-substituted; Z is a bond, O or —NR4—; Q is H, C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, C3-C12-Cycloalkyl, C5-C12-cycloalkenyl, aryl, or heterocyclyl, which are unsubstituted or mono- to pentasubstituted; R4 is for example H, C1-C8alkyl, hydroxy-C1-C8alkyl, C3-C8cycloalkyl or C2-C8alkenyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof; a process for preparing these compounds, their isomers and tautomers and the use of these compounds, their isomers and tautomers; pesticidal compositions whose active compound is selected

Abstract: This invention relates to a novel class of antibiotic agents, more specifically to macrolides comprising an oxazolidinone structure, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them.

Abstract: The present invention provides a method for stabilizing a macrolide compound, and an efficient method for producing the compound. Specifically, it provides a method for stabilizing a macrolide compound, in which a 12-membered ring macrolide compound, such as a compound expressed by the formula (1) and a cyclodextrin are both present, and a method for producing a macrolide compound, in which a cyclodextrin is made to be present in a culture broth of actinomycetes having an ability of producing the macrolide compound.

Abstract: The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.

Abstract: The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The compounds have the following structure: wherein T is the macrocyclic part.

Abstract: Methods for the purification of the macrolide moxidectin result in higher purity levels than can often otherwise be obtained. The crystalline moxidectin is then used in a wide variety of pharmaceutical and veterinary applications, including the prevention, treatment and control of parasites in plants, animals and humans.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: This invention provides a crystalline azithromycin L-malate monohydrate for treating various microbial infections, which has high thermostability, solubility and non-hygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.

Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: A compound of formula (I); that has the S-configuration at the 4?-position and wherein the bond between carbon atoms 22 and 23 is a single or a double bond; R1 is C1-C12alkyl, C3-C8cycloalkyl; or C2-C12alkenyl; R2 is H, or, for example, unsubstituted or mono- to penta-substituted C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl or C1-C6alkoxy-C1-C6alkyl; R3 is H or, for example, C1-C12alkyl; X is a bond, O, NR4 or S; and Z is C?O, C?S or S02; and, where applicable, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in salt form; a process for the preparation of and the use of those compounds and their isomers and tautomers; starting materials for the preparation of the compounds of formula (I); pesticidal compositions in which the active ingredient has been selected from those compounds and their tautomers; and a method of controlling pests using those compositions are described.

Abstract: Compounds of the avermectin family or derivatives thereof, notably emamectins are formulated into pharmaceutical compositions useful for the treatment of dermatological conditions in humans, in particular rosacea.

Abstract: The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-? lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.

Abstract: Provided is a method of predicting risk of lung cancer recurrence in a lung cancer patient or after a patient has lung cancer treatment, the method including: obtaining a biological sample from a lung cancer patient; measuring an expression level of at least one marker gene from the biological sample, the marker gene being selected from the group consisting of marker genes of Table 1, 2 or 3, to obtain data for the expression level of the marker gene; and determining whether the expression level of the marker gene corresponds to an expression level of a recurrence group or an expression level of a non-recurrence group.

Abstract: This invention features a compound of the following formula: T-(-L-C)m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.

Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, having antimicrobial activity, processes for their preparation, compositions containing them and to their use in medicine.

Abstract: The present invention provides ketolide derivatives, which can be used as anti-bacterial agents. Compounds disclosed herein can be used for the treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods of treating bacterial infections.

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: Compounds of Formula (I), and pharmaceutically acceptable salts, esters, and prodrugs thereof: (I) are disclosed, wherein A, B, D, L, X, Y, Z and R2?, are described herein. The compounds exhibit antibacterial properties. The compounds of Formula (I) can be employed to treat or prevent bacterial infections as compounds per se or in the form of pharmaceutically acceptable salts, esters, or prodrugs. The compounds and their salts, esters, and prodrugs can also be employed as ingredients in pharmaceutical compositions, optionally in combination with other antibacterial agents, for the treatment of bacterial infections. Processes for making the compounds are also disclosed.

Abstract: A compound of formula (I) compositions comprising same, processes for their preparation and use of said compounds, particularly in the treatment of microbial infections.

Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.

Abstract: A compound of formula (I) wherein the bond between carbon atoms 22 and 23 may be a single or a double bond; R1 is C1-C12alkyl, C3-C8cycloalkyl, or C2-C12alkenyl; R2 and R3 are, for example, independently of each other hydrogen, C1-C12alkyl, C3-C12cycloalkyl, C2-C12alkenyl, C2-C12alkynyl, aryl or heteroaryl; and, where applicable, to E/Z isomers, mixtures of E/Z isomers, diastereomers and/or tautomers, in each case in free form or in salt form; pesticidal compositions in which the active ingredient has been selected from those compounds and their tautomers; and a method of controlling pests using those compositions are described.

Abstract: Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: the present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.

Abstract: A compound of the formula (I) wherein the bond between carbon atoms 22 and 23 indicated with a broken line is a single or double bond, n is 0, 1 or 2, R1 represents, for instance, a C1-C12alkyl group, R2 represents, for instance, R15 group, R3 represents, for instance, R2 group, R4 represents, for instance, a chemical constituent, R5 represents, for instance, hydrogen, and R6 represents, for instance, R16 group; wherein R15 represents, for instance, unsubstituted or mono- to pentasubstituted C1-C6alkyl group, and R16 represent, for instance, hydrogen, or R15; and if appropriate, an E/Z isomer and/or diastereoisomer and/or tautomer of the compound of formula (I), in each case in free form or in salt form. Such compounds have been found to have pesticidal properties.

Abstract: A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd?N—.

Abstract: The present invention provides ketolide derivatives, which can be used as antibacterial agents. In particular, compounds described herein can be used for treating or preventing conditions caused by or contributed to by Gram-positive, Gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp. Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebaclerium, Bacillus or Enterobactericeae. Also provided are processes for preparing such ketolide derivatives, pharmaceutical compositions thereof, and methods of treating bacterial infections.

Abstract: The present invention provides a chromoprotein produced by Actinomadura sp. 21G792, as well as amino acid and nucleic acid sequences of the apoprotein component of the chromoprotein and of components of the biosynthetic pathway for the chromophore. The present invention is useful for developing pharmaceutical and treating diseases such as cancer or bacterial infections.

Abstract: The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specifically C. difficile infections.

Abstract: The present invention relates to 14- or 15-membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

Abstract: Spinetoram is selectively produced in excellent yields by hydrogenating a mixture of 3?-O-ethyl spinosyn J and 3?-O-ethyl spinosyn L in a water miscible organic solvent using hydrogen gas and a heterogeneous catalyst.

Abstract: Compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof, effective in the prevention and/or treatment of infections with microbes: (1) (a) wherein R1 is hydrogen or straight-chain C1-6 alkylcarbonyl; R2 is hydrogen or C1-6 alkylcarbonyl; R3 is hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkenyl, C2-6 alkenylcarbonyl, C2-6 alkynyl, or an Ar—B— group (wherein Ar is aryl or a heterocyclic group; and B is C1-6 alkyl, C1-6 alkylcarbonyl, C2-6 alkenyl, C2-6 alkenylcarbonyl, or C2-6 alkynyl); R5, R6, R7 and R8 are each hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or an Ar—B?— group (wherein B? is C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl); X is oxygen or —NR4— (wherein R4 is hydrogen, C1-6 alkyl or C1-6 alkyl which may be substituted with Ar); and R4? is hydrogen or a group represented by the general formula (a) (wherein R3? and R4? are each hydrogen or straight-chain or branched C1-6 alkylcarbonyl)

Abstract: The present inventors intended to search for substances that can regulate the expression of a molecular chaperone, GRP78, using the expression of GRP78 as an indicator. As a result, a novel tetronic acid derivative, versipelostatin compound (also known as JL68) shown in formula (I) having the activity of suppressing GRP78 expression was isolated from the metabolite of Streptomyces versipellis strain 4083-SVS6.

Abstract: Methods for the purification of the macrolide moxidectin result in higher purity levels than can often otherwise be obtained. The crystalline moxidectin is then used in a wide variety of pharmaceutical and veterinary applications, including the prevention, treatment and control of parasites in plants, animals and humans.

Abstract: The present invention relates to derivatives of 9-keto spinosyns, which are substituted by a ?N—(O, NH or NRx)—Ry moiety in the C-9 position, to methods for their manufacture, and to their use for controlling animal pests.

Abstract: A pharmaceutical compound comprising a compound of formula I and a pharmaceutically acceptable 2-amino-1,3-propanediol beside one or more pharmaceutically acceptable excipient(s).

Abstract: A compound represented by the general formula (I) or a salt thereof: wherein represents —CH?CH—, —CH2—CH2— or the like, between R1 and the carbon atom at 4?-position represents a single bond or a double bond, between R2 and the carbon atom at 5-position represents a single bond or a double bond, and for example, 1) when represents —CH?CH— or —CH2—CH2—, and between R1 and the carbon atom at 4?-position represents a double bond, R1 represents ?C(R11)(R12) (wherein R11 represents a lower alkyl group or the like and R12 represents a hydrogen atom or the like) or the like, and R2 represents a hydroxyl group or the like, or R2 may be combined together with the carbon atom at 5-position to form a carbonyl group, and 2) when represents —CH?CH— or —CH2—CH2—, and between R1 and the carbon atom at 4?-position represents a single bond, R1 represents —OCH(R1a)(R1b) (wherein R1a represents a lower alkyl or the like and R1b represents a hydrogen atom or the like) or the like, and R2 re

Abstract: Sixteen membered macrolide anti-infective agents having a structure according to formula I where R1, R2, R3, R4, R5, and R6 are as defined herein, and related compounds are disclosed.

Abstract: This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.

Abstract: Provided is a compound represented by the general formula (I) or a salt thereof: wherein, —XY— represents —CH?CH— and the like, between R2 and the carbon atom at 5-position represents a single bond or a double bond, R1 represents a lower alkyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group (wherein a lower alkyl moiety of said lower alkoxycarbonyl group may be substituted with a heterocyclic group) and the like, and R1a represents a hydrogen atom, provided when R1 represents a lower alkoxycarbonyl group and the like, R1a may further represents a lower alkoxycarbonyl group and the like, when between R2 and the carbon atom at 5-position is a single bond, R2 represents a hydroxyl group and the like, and when between R2 and the carbon atom at the 5-position is a double bound, R2 combines with the carbon atom at 5-position to form a hydroxime group (—C(?NOH)) and the like, and R3 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The present invention relates to methods for producing novel spinosyn derivatives which are substituted with a 1-hydroxy-ethyl radical in the C-21 position and to novel spinosyn derivatives of this type per se and to their use for producing novel spinosyns.

Abstract: A polyketide or glycosylated polyketide which has the formula: wherein R* is methyl or ethyl; each of R1-R6 is methyl; X1 is OH or H; and/or X2 is=O, OH or H; X3 is OH or H; X4 is OH or H; a pi bond is present at positions 10-11, 8-9, 4-5 and/or 2-3; and wherein at least one of the following characteristics is present: X1 is H; X2 is OH or H; X3 is H; X4 is H; or a pi bond is present at positions 10-11, 8-9, 4-5 and/or 2-3.