62 results about "Ketolide" patented technology

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.

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.

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; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

The invention relates to an antibiotic streptomyces, fermentation product of which can inhibit broad spectrum fungus and protozoan, and field experiment can control crop fungus plant disease and root-knot nematode. The antibiotic streptomyces has good effect, no pollution nuisance and no residue. The antifungal agent has extremely low hazardness for the people and good performance and development prospect for medical and agricultural use. The invention is named as SIM001 antibiotic streptomyces which is Streptomyces antibioticus subspecies xi an, and is preserved as patent in the depositary institution appointed by patent office of state intellectual property office; the preservation data is April 14th, 2005, the name of the depositary institution is CGMCC, and the number of preservation is CGMCC No.1349. The whole cell hydrolysate of the antibiotic streptomyces contains L, L-DAP (Diaminopimelic acid) and no characteristic glucide; the cytoderm belongs to I type and glucide type C; one of the main antibacterial materials is polyene macrocyclic ketolide which belongs to the broad spectrum antifungal substance.

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.

A method for treatment for conditions in human beings associated with either or both reactive arthritis or bursitis comprising administering a combination of a member of the family of synthetic purine nucleoside analog antiviral drugs, a member of the tetracycline family, and a member of the nitroimidazole family, or alternatively, administering a combination of a member of the family of synthetic purine nucleoside analog antiviral drugs, a member of the beta-lactam family, and a member of the nitroimidazole family, or alternatively, administering a combination of a member of the family of synthetic purine nucleoside analog antiviral drugs, a member of the macrolide antimicrobial family, and a member of the nitroimidazole family, or alternatively, administering a combination of a member of the family of synthetic purine nucleoside analog antiviral drugs, a member of the ketolide antimicrobial family, and a member of the nitroimidazole family.

Provided herein are ketolide derivatives, which can be used as antibacterial agents. 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, Corynebacterium, Bacillus, Enterobactericeae, Propionibacterium acnes or any combination thereof. Also provided are processes for preparation of compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.

Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macro-cyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.

The invention provides compounds with a general formula (I) or (II), and acceptable salts or esters prepared from the compounds and inorganic acid or organic acid. In the general formula (I) or (II), Ar refers to aromatic heterocyclic hydrocarbyl or substituted aromatic heterocyclic hydrocarbyl; and X refers to hydrogen or fluorine. The compounds have a novel structure; 9-oxime hydroxyl of ketolide is connected with an aromatic heterocyclic hydrocarbon through a propargyl side chain; and the compounds are easy and convenient to synthesize and are suitable for industrial production. Moreover, the compounds have outstanding antibacterial activity on clinically common sensitive bacteria and drugfast bacteria, such as staphylococcus aureus, streptococcus pneumonia, streptococcus pyogenes, staphylococcus epidermidis and the like, can be independently used or serve as one of active ingredients to be mixed with other medicines to treat bacterial infection and the like in various formulations or medication ways. Correspondingly, the invention also provides a preparation method for the compounds, use of the compounds as anti-infective agents and corresponding medicinal compositions.

The present invention includes compounds of the formula wherein: X is hydrogen or halide; R<2> is hydrogen, acyl, or a hydroxy protecting group; R<6> is hydrogen, hydroxyl, or -OR wherein R is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R<13> is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

6-0-carbamoyl ketolide antibacterials of the formula: wherein R<1>, R<2>, R<3>, R<4>, R<5>, R6, X, X', Y, and Y' are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

The invention discloses a series of erythromycin A ketolide antibiotic derivatives containing quinoline substituent group, represented by a formula I. The invention also provides preparation methods and applications of the derivatives, and side-chain intermediates of the compounds and synthesis methods thereof. The key point of the invention is that the compounds represented by the formula I have the efficacy of broad-spectrum antibiotics, and have outstanding antibacterial activity and anti-resistance activity in inhibiting Gram-positive bacteria and Gram-negative bacteria. The compounds provided by the invention can be used as broad-spectrum antibiotics, and also have antibacterial and antiviral activities in inhibiting Gram-positive bacteria and Gram-negative bacteria.

The invention relates to a novel purity method for 3-hydroxy clarithromycin, and belongs to the synthesis field of pharmaceutical intermediate. The 3-hydroxy clarithromycin can be gained by adopting clarithromycin as the raw material through acid hydrolysis. Through the analysis and the comparison to the physico-chemical properties of the principal product and the by product, the 3-hydroxy clarithromycin is purified by respectively adopting a one-time sedimentation method, a two-time sedimentation method, and a purge method. The invention has the advantages that a synthetic route of clarithromycin with simple operation, high productivity, and low cost is provided, the reaction time of the synthetic route is short, the product productivity is high, the subsequent process is simple and easy to be operated, and the productive efficiency of ketolide antibiotics can be greatly improved.

15-fluoroketolides of the formula

having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.

In one aspect, the present invention relates to a process for the preparation of 6-O-substituted erythromycin derivatives comprising, in the presence of a palladium catalyst and a phosphine, 2′-substituted and optionally 4″-substituted 9- Reaction of oxime erythromycin derivatives with an alkylating agent. On the other hand, the present invention relates to a method for preparing 6-O-substituted erythromycin ketolide by using palladium-catalyzed alkylation reaction.

6-O-Acyl ketolide antibacterials of the formula (I), wherein R1, R2, R3, R4, W, X, X', Y, and Y' are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

The present invention relates to novel 2-halogenated-6-O-substituted ketolide derivatives of formula (I) or (II) with antibacterial activity and pharmaceutically acceptable salts and esters thereof, containing a therapeutically effective amount of the compound of the present invention Compositions with pharmaceutically acceptable carriers combined therewith, methods for treating bacterial infections by administering to mammals a pharmaceutical composition containing a therapeutically effective amount of the compound of the present invention, and methods for their preparation.

The present invention provides pharmaceutical compositions and solid formulations comprising EP-013420 of form I, form II, form Ia, amorphous form and monohydrate and the methods of formulation preparations. The present invention provides methods of treating bacterial infections by administering the pharmaceutical compositions to a subject in need of such treatment.

The invention provides a novel acylide derivative which has a general formula I or a general formula II or which is an acceptable salt or ester composed of a compound having the general formula I or the general formula II and an inorganic acid or organic acid. The novel acylide derivative according to the embodiment has a novel structure and has excellent antibacterial activity on clinically common sensitive bacteria and drug resistant bacteria, and part of compounds of the novel acylide derivative are as good as or better than telithromycin in inhibitory and bactericidal activity. The existing knowledge about the structure-activity relation of acylides is broken through, the novel acylide derivative having bactericidal activity is provided and is as good as the telithromycin in the market in activity, and the novel acylide derivative is easy to industrially produce. Researches show that targets of the acylides acting on bacterial ribosomes are different from those of ketolides. In total, compared with the prior ketolides having defects, the novel acylide derivative has better market prospect in resisting drug resistant bacteria.

An efficient process for producing an 11,12-cyclic carbamate 6-O-substituted ketolide derivatives having the natural stereochemistry at the 10-position.