Abstract: The present invention discloses compounds of formula I, II, III, or IV, or a racemate, enantiomer, regioisomer, salt, ester or prodrug 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 invention relates to novel semi-synthetic macrolides of formula (I) having antibacterial activity.

Abstract: The present invention relates to an improved, cost effective and easy process for the preparation of azithromycin monohydrate isopropanol clathrate. The process provides a one-step method of preparing azithromycin monohydrate isopropanol clathrate directly from 9-deoxo-9a-aza-9a-homoerythromycin A. The process comprises at least partial dissolution and/or suspension of 9-deoxo-9a-aza-9a homoerythromycin A in isopropanol to form a mixture, adding methylating solution to the said mixture, refluxing or heating said mixture to form a reaction mixture, adding alkaline solution to the reaction mixture to adjust pH from about 10 to about 11 and isolating pure azithromycin monohydrate isopropanol clathrate. The process helps in reducing the total time of preparation, total utility cost for the production and also helps to avoid handling loss.

Abstract: Disclosed herein are compositions and methods used to modulate a NH2-terminal Jun Kinase activity. These compositions and methods can be employed to regulate metabolic disorders associated with, for example, insulin such as diabetes. The reduction in NH2-terminal Jun Kinase activity can lead to the reduction in weight and improve insulin sensitivity.

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: Azithromycin is prepared in a high yield by a simple process using a crystalline 9-deoxo-9a-aza-9a-homoerythromycin A hydrate.

Abstract: A clathrate of azithromycin hydrate with 1,2-propyleneglycol is much less hygroscopic than azithromycin hydrate or crystals known in the art, therefore, it can be useful for the preparation of a medicine for treating various microbial infections.

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

Abstract: The present invention discloses, inter alia, a compound of the following formula, 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 aforementioned compounds. The invention further includes processes by which to make the compounds of the present invention.

Abstract: Antimicrobial ketolide compounds are provided having the formula (A): as well as pharmaceutically acceptable salts, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds, methods of treating bacterial infections by the administration of such compounds, and processes for the preparation of the compounds.

Abstract: The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents an anti-inflammatory steroid or nonsteroid subunit, or an antineoplastic or antiviral subunit and L represents a linking group covalently linking M and V; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory/neoplastic/viral diseases and conditions in humans and animals.

Abstract: The invention features a method of delivering a drug to a diseased cell by linking the drug to a rifamycin derivative, compositions that include drug-rifamycin conjugates of the invention, and methods for treating disease using those compositions.

Abstract: A subject of the invention is a process for the preparation of the compounds of formula (I): Wherein the substituents are defined as in the application. The compounds of this invention exhibit antibiotic properties.

Abstract: The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, D represents a nonsteroidal subunit (nonsteroidal moiety) derived from nonsteroid drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linking group covalently linking M and D; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals.

Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.

Abstract: The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals. Such compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-?. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.

Abstract: This invention relates to compounds of the formula wherein a, R1, R2, R3, R4, R5, R6 and X are each as defined above, and to pharmaceutically acceptable salts thereof, useful as potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating bacterial and protozoal infections by administering the compounds of formula I.

Abstract: The present invention relates to a dry blend, used for forming azithromycin tablets by direct compression, comprising non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. This invention also relates to an azithromycin tablet comprising non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. Preferably, the azithromycin tablet is formed by directly compressing the dry blend, of the present invention, to form said azithromycin tablet. Preferably, the azithromycin tablet, of the present invention, contains a dosage of 250 mgA, 500 mgA or 600 mgA of azithromycin. This invention further relates to an azithromycin tablet which is produced by forming a dry blend of a non-granulated azithromycin form A and at least one pharmaceutically acceptable excipient. The azithromycin tablet is then formed by directly compressing the dry blend.

Abstract: The invention relates to a pharmaceutical composition for preventing and/or treating eye infections, which is to be used by local application. It is in particular directed towards such a composition which is in the form of an eye lotion which can be distributed by drops, in which an antibiotic of the macrolide class, such as azithromycin, is in solution in an oily vehicle. This vehicle is, in particular, of the type of product essentially consisting of medium-chain triglycerides in which the alcohol functions of the glycerol are entirely esterified by carboxylic acids made from saturated hydrocarbons, the molecule of which comprises from 5 to 12 carbon atoms. They are preferably linear-chain fatty acids comprising from 8 to 10 carbon atoms, such as caprylic acid or capric acid. The composition is advantageously prepared by dissolving the active agent in the oily vehicle at a temperature not exceeding 70° C.

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 invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.

Abstract: Novel 6,11-4-carbon bridged ketolides, pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.

Abstract: The present invention relates to processes and intermediates for the preparation of 6–11 bicyclic erythromycin derivatives.

Abstract: Antibacterial compounds having formula (I) and formula (II) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates employed in the processes, compositions containing the compounds, and methods for prophylaxis or treatment of bacterial infections in a fish or a mammal using the compounds are disclosed.

Abstract: The invention provides new macrolides antibiotics of formula I with improved biological properties and having the formula wherein R1, R2 and R3 are as herein described.

Abstract: Antibacterial compounds having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods for prophylaxis or treatment of bacterial infections using the compounds are disclosed.

Abstract: The invention relates to crystal forms of azithromycin, an antibiotic useful in the treatment of infections.

Abstract: Azithromycin in the form of a monohydrate comprising from 4.0% to 6.5% of water, a process for its preparation and its use in pharmaceutical compositions.

Abstract: The invention relates to novel methods for using macrolide anti-infective agents. The macrolide anti-infective agents demonstrate antibacterial activity against multi-drug resistant strains of bacteria and, in particular, methicillin-resistant Staphylococcus aureus (MRSA). Methods for inhibiting the activity of multi-drug resistant bacterial organisms and methods for treating a bacterial infection caused by such organisms are described herein.

Abstract: Various macrolide compounds such as those having the following formulas are provided where the variables have the values provided herein.

Abstract: The invention relates to a method of preparing compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.

Abstract: Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I: wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P212121, with average unit cell parameters a=8.2 to 9.7 ?, b=11.5 to 13.5 ?, c=44.5 to 47.0 ?, ?=?=?=90°, wherein a, b and c represent the crystal axes lengths and ?, ? and ? represent the angles between the crystal axes.

Abstract: Antibacterial compounds having formula (I) and formula (II) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods for prophylaxis or treatment of bacterial infections using the compounds are disclosed.

Abstract: 11,12 ? lactone ketolides of the following formula: and pharmaceutically acceptable salts and solvates thereof, wherein R, R1, R2, and R3 are as described herein. The disclosure also relates to processes for the preparation of such compounds, to compositions containing them, and to their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

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 invention relates to halo derivatives of 9a-N-(N?-arylcarbamoyl)- and 9a-N-(N?-arylthiocarbamoyl)-9-deoxo-9a-aza-9a-homoerythromycin A of the general formula (I) wherein R has the meaning of a substituted aryl group of the formula (II) wherein substituents a, b, c, d and e are the same or different and at least one of them has the meaning of halo, a (C1-C6)haloalkyl or a (C1-C6)haloalkoxy group, whereas the remaining ones have the meaning of hydrogen, halo, a (C1-C6)alkyl or a (C1-C6)alkoxy group, and X has the meaning of oxygen or sulfur, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to a process for their preparation, to a process for the preparation of pharmaceutical compositions comprising them and to the use of these pharmaceutical compositions for the treatment or prevention of bacterial infections.

Abstract: The invention features methods and compositions for treating ocular infections. The method comprises topically administering to an eye of an animal in need of such treatment an ocular infection-treating amount of azithromycin.

Abstract: This invention relates to a powder for oral suspension, and an oral suspension made therefrom, which comprises a n-propanol solvate of non-dihydrate azithromycin and an azithromycin conversion stabilizing excipient, wherein said excipient reduces the conversion of the form of azithromycin, when placed in suspension, to another form of azithromycin. This invention also relates to an oral suspension which comprises a n-propanol solvate of non-dihydrate azithromycin and an aqueous vehicle.

Abstract: This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-o-methyl-4-C-[(propylamino)methyl]-?-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-?-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.

Abstract: The invention relates to a process for making Azithromycin crystals using a number of process steps that avoids the use of cumbersome and/or inefficient extraction and/or isolation procedures.

Abstract: 9a-N-[N?-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A and of 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A and their pharmaceutically acceptable addition salts with inorganic or organic acids are provided, along with a process for their preparation, pharmaceutical compositons, and use in treating bacterial infections.

Abstract: A macrolide antibiotic of the formula wherein the variables are defined as described herein.

Abstract: Novel 6,11-4-carbon bridged ketolides, pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.

Abstract: A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate) has been obtained. Preparation of the novel form of azithromycin comprises the steps of dissolving azithromycin in isopropanol, followed by the slow addition of water to the organic solution.

Abstract: An oral dosage form of azithromycin which does not exhibit an adverse food effect; Specific azithromycin oral dosage forms including tablets, powders for oral suspensions and unit dose packets; Methods of treating microbial infections with the dosage forms; And therapeutic packages containing the dosage forms.

Abstract: A procedure for preparing 6-O-alkyl erythromycin compounds having the formula: wherein R1 is a loweralkyl group, R2 and R3 an independently hydrogen or a hydroxy-protecting group, except that R2 and R3 may not both be hydrogen simultaneously; Y is oxygen or a specifically substituted oxime; and Z is hydrogen, hydroxy or protected-hydroxy; by reaction of the compound wherein R1 is hydrogen with an alkylating reagent, is the presence of a strong alkali metal base and also in the presence of a weak organic amino base, in a suitable stirred or agitated polar aprotic solvent, or a mixture of such polar aprotic solvents maintained at a reaction temperature and for a period of time sufficient to effect alkyation.

Abstract: Disclosed are 9-hydrazone erythromycin and 9-azine erythromycin derivatives and the processes for making the same. The compounds are useful intermediates for conversion into 6-O-alkyl erythromycin. Also disclosed are the processes for converting the compounds into 6-O-alkyl erythromycin.

Abstract: Antimicrobial compounds having the formula as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: Novel compounds of the formula wherein the substituents are defined as in the application having antibiotic properties.