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7384922 |
6-11 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...
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7384921 |
Polymorphic 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...
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7365174 |
Azalide 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 R 1 is...
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7365056 |
Substituted 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...
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7351696 |
Compounds
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...
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7342000 |
Semisynthetic 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...
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7335753 |
Bifunctional 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...
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7332476 |
Pyridyl 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...
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RE40040 |
Process 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...
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7312201 |
Tetracyclic 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...
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7309782 |
Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.
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7297682 |
Diphosphate 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...
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7291602 |
11,12-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...
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7276487 |
9a, 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...
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7273853 |
6-11 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...
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7271155 |
9A, 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...
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RE39836 |
Macrolide antinfective agents
Compounds of the formula
wherein
R a is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C);...
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7265094 |
9N-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...
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7262172 |
Macrolides
The invention relates to novel semi-synthetic macrolides of formula (I) having antibacterial activity. More particularly this invention relates to derivatives of 8a-aza-8a-homoerythromycin A, to...
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RE39743 |
2-halogenated derivatives of 5-0 desosaminyl-erythronolide a, their preparation process and their antibiotic use
Novel compounds of the formula
wherein the substituents are defined as in the application having antibiotic properties.
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7235646 |
Process for the preparation of azithromycin monohydrate isopropanol clathrate
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...
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7232897 |
Compositions and methods for modulating NH2-terminal Jun Kinase activity
Disclosed herein are compositions and methods used to modulate a NH 2 -terminal Jun Kinase activity. These compositions and methods can be employed to regulate metabolic disorders associated with,...
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7229972 |
3,6-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...
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RE39591 |
6-O-substituted ketolides having antibacterial activity
Antimicrobial compounds having the formula
as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating...
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7205395 |
Process of preparing azithromycin and crystalline 9-deoxo-9a-aza-9a-homoerythromycin A hydrate used therein
Azithromycin is prepared in a high yield by a simple process using a crystalline 9-deoxo-9a-aza-9a-homoerythromycin A hydrate.
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7205394 |
Clathrate of azithromycin hydrate with 1,2-propyleneglycol, method for the manufacture thereof and pharmaceutical composition comprising same
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...
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RE39560 |
Erythromycin A derivatives and method for preparing same
Erythromycin A derivatives represented by the general formula
wherein R 1 is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3...
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RE39531 |
9-hydrazone and 9-azine erythromycin derivatives and a process for making the same
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....
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7189704 |
6-11 bicyclic ketolide derivatives
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...
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7163924 |
Ketolide derivatives
Antimicrobial ketolide compounds are provided having the formula (A):
as well as pharmaceutically acceptable salts, esters or prodrugs thereof, pharmaceutical compositions comprising such...
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7157433 |
Compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules
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...
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RE39383 |
Process for 6-O-alkylation of erythromycin derivatives
A procedure for preparing 6-O-alkyl erythromycin compounds having the formula:
wherein R 1 is a loweralkyl group, R 2 and R 3 an independently hydrogen or a hydroxy-protecting group, except...
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7122525 |
Targeted therapeutics and uses thereof
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...
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7119180 |
2-halogenated derivatives of 5-O-desosaminyl-erythronolide A, their preparation process and their antibiotic use
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...
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7109176 |
Nonsteroidal anti-inflammatory substances, compositions and methods for their use
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...
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7105179 |
Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.
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7091187 |
Compounds, compositions and methods for treatment of inflammatory diseases and conditions
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...
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7081525 |
Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.
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7071170 |
Macrolide antibiotics
This invention relates to compounds of the formula
wherein a, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and X are each as defined above, and to pharmaceutically acceptable salts thereof, useful as...
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7070811 |
Directly compressible formulations of azithromycin
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...
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RE39149 |
Method of administering azithromycin
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;...
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7064110 |
6-11 bicycle 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...
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7064109 |
Pharmaceutical composition based on macrolides for topical application in ophthalmology
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...
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7053192 |
Crystal forms of azithromycin
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.
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7049417 |
6,11-4-Carbon bridged ketolides
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...
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7022679 |
Processes for the preparation of 6-11 bicyclic erythromycin derivatives
The present invention relates to processes and intermediates for the preparation of 6–11 bicyclic erythromycin derivatives. In particular, the present invention relates to processes and...
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6998390 |
Oxolide antibacterials
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...
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6995143 |
Macrolides with antibacterial activity
The invention provides new macrolides antibiotics of formula I with improved biological properties and having the formula
wherein R 1 , R 2 and R 3 are as herein described.
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6992069 |
Tricyclic macrolide antibacterial compounds
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...
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6949519 |
Macrolide solvates
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.
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