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Class 536/7.4 - Additional nitrogen containing


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain at least one nitrogen other than
No. of patents: 347
Last issue date: 01/17/2012


1                  
NumberTitleIssue Date
809770810a-Azalide compound
[Object]: To provide a compound having a novel structure effective against Hemophilus influenzae and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. ...
01/17/2012
7989600Macrolide compounds containing biotin and photo-affinity group for macrolide target identification
The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to t...
08/02/2011
7872109Motilide polymorphs
The invention provides polymorphs of a motilide having a structure represented by formula Ia ...
01/18/2011
7767797Macrocyclic compounds and methods of use thereof
The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds. ...
08/03/2010
7683162Process of preparing a crystalline azithromycin monohydrate
The present invention provides a process of preparing a crystalline azithromycin monohydrate. The process involves dissolving azithromycin in a solution containing ethanol, adding the dissolved azithromycin into water to precipitate the crystals, isolating and dryin...
03/23/2010
7563877Processes for the preparation of -(2-aminobenzo[]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182
The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a). In particular, the present invention relates to processes and intermediates for the preparation of O-(2-aminobenzo[d]ox...
07/21/2009
7488811Macrolide compounds endowed with antiinflammatory activity
Macrolide compounds lacking cladinose in position 3 having antiinflammatory activity and substantially free of antibiotic properties, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them as active ingredient. ...
02/10/2009
7468428Lyophilized azithromycin formulation
The invention provides among other things a stable, sterile pharmaceutical formulation comprising lyophilized azithromycin and ethanol. The invention also provides a method of producing a stable, sterile pharmaceutical product comprising lyophilized azithromycin. Th...
12/23/2008
7438924Dry granulated formulations of azithromycin
This invention relates to a pharmaceutical formulation, in the form of a tablet, sachet or powder for suspension dosage form, which comprises dry granulated particles of a non-dihydrate form of azithromycin and, optionally, one or more pharmaceutically acceptable ex...
10/21/2008
7435805O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and...
10/14/2008
74199623,6-bicyclolides
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 com...
09/02/2008
74199619a-azalides with anti-inflammatory activity
Macrolides with anti-inflammatory activity are described. Particularly described are 9a-azalides and their anti-inflammatory activity without cladinose in position 3, the pharmaceutically acceptable salts thereof and the pharmaceutical composition that contain them ...
09/02/2008
7414114Process for preparation of anhydrous azithromycin
The present invention provides a stable form of azithromycin derivatives that act as antibiotics. These compounds are in anhydrous form and have increased stability over the hydrated forms. ...
08/19/2008
74140306-11 Bicyclic erythromycin derivatives
The present invention discloses compounds of formulaes I, II, III, or IV, or a racemate, enantiomer, regioisomer, salt, ester or prodrug thereof: which exhibit antibacterial properties. The present invention further relates...
08/19/2008
7410952Derivatives of azithromycin
The invention relates to derivatives of azithromycin, processes for the manufacture thereof and pharmaceutical compositions thereof preferably together with azithromycin. ...
08/12/2008
74079423,6-bridged 9,12-oxolides
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 com...
08/05/2008
7402568Bicyclic 9a-azalide derivatives
The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceuti...
07/22/2008
7384921Polymorphic forms of 6-11 bicyclic ketolide derivatives
The present invention includes EP-13420 polymorphic crystalline forms: Form I, Form II, Form Ia, and monohydrate and amorphous EP-13420 which posses distinct physical properties. In another embodiment of the present invention, there are provided methods of producing...
06/10/2008
73849226-11 bridged oxime erythromycin derivatives
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 comp...
06/10/2008
7368297Method for forming catalytic sites at the surface of a support
A method for forming catalytic sites at the surface of a support, which includes: depositing on the surface a liquid film (3) containing elements (4) of a living matter, capable of moving when subjected to an electric and/or magnetic field and designed...
05/06/2008
7365056Substituted 9a-N-(N′-(sulfonyl)phenylcarbamoyl)derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithomycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9-a-aza-9a-homoerithronolide A
The invention relates to substituted 9a-N-{N′-[4-(sulfonyl)phenyl]carbamoyl} derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-di-hydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalid...
04/29/2008
7365174Azalide and azalactam derivatives and method for producing the same
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; R...
04/29/2008
7351696Compounds
The present invention relates to compounds 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 infe...
04/01/2008
7342000Semisynthetic macrolide antibiotics of the azalide series
The invention relates to N″-substituted 9a-N-(N′-carbamoyl-γ-aminopropyl), 9a-N-(N′-thiocarbamoyl-γ-aminopropyl), 9a-N-[N′-β-cyanoethyl)-N′-carbamoyl-γ-aminopropyl] and 9a-N-[N′-β-cyanoethyl)-N′-thiocarbamoyl-γ-am inopropyl] derivatives of 9-deox...
03/11/2008
7335753Bifunctional heterocyclic compounds and methods of making and using same
The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using...
02/26/2008
7332476Pyridyl substituted ketolide antibiotics
Antimicrobial macrolide and ketolide compounds are provided having formulas XII: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; me...
02/19/2008
RE40040Process of use in converting the 4″(S)-OH functional group of the cladinose unit of an azamacrolide to 4″(R)-NH2
The subject-matter of the invention is a process for the stereoselective preparation of a compound of general formula I by stereoselective displacement by a nitrogenous nucleophilic compound of the activated alcohol functional gr...
01/29/2008
7312201Tetracyclic bicyclolides
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 pharmace...
12/25/2007
7309782Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections. ...
12/18/2007
7307156Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections. ...
12/11/2007
7297682Diphosphate salt of a 4″—substituted-9-deoxo-9 A—AZA—homoerythromycin derivatives and its pharmaceutical composition
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]-α-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideo...
11/20/2007
729160211,12-lactone bicyclolides
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 pharmace...
11/06/2007
7282221Antiviral product, use and formulation thereof
An antiviral product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antiviral product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosag...
10/16/2007
7282486Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections. ...
10/16/2007
72764879a, 11-3C-bicyclic 9a-azalide derivatives
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 pharmace...
10/02/2007
72738536-11 bicyclic ketolide derivatives
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 pharmace...
09/25/2007
7271154Antibiotic conjugates
This invention features a compound of the following formula: wherein T is a transportophore, L is a bond or linker, and C is an antibiotic therapeutic agent, the transportophore is covalently bonded to the antibi...
09/18/2007
72711559A, 11-2C-bicyclic 9a-azalide derivatives
The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to ...
09/18/2007
RE39836Macrolide antinfective agents
Compounds of the formula wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); subst...
09/11/2007
72650949-substituted 6-11 bicyclic erythromycin derivatives
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 furthe...
09/04/2007
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