The present application provides crystal forms A and B of a free base of a compound represented by formula (I), and relates to a use of the crystal forms A and B.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61P 31/06 - Antibacterial agents for tuberculosis
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
Provided in the present application is a method for preventing or treating acute bacterial skin and skin structure infections (ABSSSI), or alleviating ABSSSI-related conditions. The method comprises administering a therapeutic agent by intravenous infusion to a patient in need thereof for up to 7 consecutive days, wherein the therapeutic agent for each intravenous infusion comprises about 10 mg to about 500 mg of a compound as shown in formula (I) and/or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, metabolite or deuterated substance thereof.
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
Provided in the present application is a method of preventing or treating diabetic foot infection (DFI) or alleviating a DFI-related disorder. The method comprises administering a topical therapeutic agent to a patient in need thereof, wherein the topical therapeutic agent contains a compound as shown in formula (I) and/or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, metabolite or deuterated compound thereof, and the DFI is caused by Gram-positive bacterial infection.
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present application provides a method for preventing or treating a prosthetic joint infection (PJI), or for alleviating PJI-related symptoms. The method comprises: administering a therapeutic agent to a joint cavity of a patient in need thereof, the therapeutic agent comprising a compound represented by formula (I) and/or a pharmaceutically acceptable salt, a hydrate, a solvate, a prodrug, a metabolite, or a deuterated substance thereof.
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
Provided in the present application is a method for treating a prosthetic joint infection (PJI), which method comprises: a therapeutic agent is infused intravenously at least once into a patient in need, wherein the therapeutic agent contains about 100 mg to about 500 mg of a compound as represented by formula (I) and/or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, metabolite, or deuterated compound thereof.
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present application provides a method for preventing prosthetic joint infection (PJI). The method comprises administering at least one intravenous infusion of a therapeutic agent to a subject in need, wherein the therapeutic agent comprises about 100 mg to about 500 mg of a compound represented by formula (I) and/or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, metabolite or deuterated compound thereof, and a single intravenous infusion lasts for about 20 minutes to about 3 hours.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
Provided in the present application are salts of compounds, or hydrates, solvates, prodrugs, metabolites or deuterated compounds thereof, the salts being triphenylacetate salts of compounds of formula (I), L being a bond, an alkyl group or any alkoxy group in which a central carbon atom is substituted by an aryl group, and G being hydrogen, an alkyl group, a haloalkyl group, an alkenyl group, an alkynyl group, an optionally substituted cycloalkyl group or an optionally substituted heterocyclyl group. Further provided in the present application are a plurality of crystal forms of the salts, a preparation method therefor and the use thereof.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
The present invention provides use of a rifamycin-nitroimidazole coupled molecule, or a deuterated substance thereof, a metabolite thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof in the preparation of a drug for the treatment or prevention of a disease caused by mycobacterium tuberculosis infection. The rifamycin-nitroimidazole coupled molecule has a structure represented by formula I. The rifamycin-nitroimidazole coupled molecule or the deuterated substance thereof, the metabolite thereof, the pharmaceutically acceptable salt thereof, or the prodrug thereof in the present invention can inhibit mycobacterium tuberculosis comprising multi-drug-resistant (MDR) and extensive drug-resistant mycobacterium tuberculosis (XDR-TB), and then is used for treating or preventing infection and a disease caused by mycobacterium tuberculosis.
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 31/06 - Antibacterial agents for tuberculosis
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present disclosure provides methods, drug combinations and kits for treating, ameliorating, reversing and/or preventing a Helicobacter pylori (H. pylori) infection in a subject in need thereof.
Provided is a rifamycin-quinolizinone coupled molecule ointment. Raw material components of the rifamycin-quinolizinone coupled molecule ointment comprise, based on the total mass percentage of 100%, rifamycin-quinolizinone coupled molecules in an amount of 0.05%-0.7%, polyethylene glycol 400 in an amount of 55%-65%, polyethylene glycol 3350 in an amount of 25%-35%, propylene glycol in an amount of 8%-12%, a solubilizer in an amount of 0.1%-1%, and an antioxidant in an amount of 0.3%-1%. The rifamycin-quinolizinone coupled molecule ointment can improve the medicament content of the preparation and the stability of the medicament components, thereby improving the medication effect and user experience.
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
The present application relates to a pharmaceutical composition comprising sulbactam or a pharmaceutically acceptable salt thereof, avibactam or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, wherein unit dose ratio of said sulbactam or the pharmaceutically acceptable salt thereof and said avibactam or the pharmaceutically acceptable salt thereof is about 8:1 to about 4:1, unit dose of said sulbactam or the pharmaceutically acceptable salt thereof is about 1 g-4 g, and unit dose of said avibactam or the pharmaceutically acceptable salt thereof is about 0.125 g-1 g. The present application also relates to methods of treating bacterial infections using said pharmaceutical composition.
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
The present application relates to a pharmaceutical composition, comprising: sulbactam or a pharmaceutically acceptable salt thereof, and avibactam or a pharmaceutically acceptable salt thereof, the unit dose ratio of the sulbactam or the pharmaceutically acceptable salt thereof to the avibactam or the pharmaceutically acceptable salt thereof being about 8:1 to about 4:1, the unit dose of the sulbactam or the pharmaceutically acceptable salt thereof being about 1-4 g, and the unit dose of the avibactam or the pharmaceutically acceptable salt thereof being about 0.125-1 g; and optionally a pharmaceutically acceptable carrier. The present application also relates to a method for treating a bacterial infection using the pharmaceutical composition.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 13/00 - Drugs for disorders of the urinary system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
14.
PENAM DERIVATIVES FOR TREATING BACTERIAL INFECTIONS
Novel iron chelating group conjugated penam derivatives described herein show antibacterial activity, and could be used as antibacterial agents or beta-lactamase inhibitors (BLIs) which are of value for application in combination with other antibacterial agents. (Formula I)
C07D 499/00 - Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula: , e.g. penicillins, penemsSuch ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
A61K 31/431 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems containing further heterocyclic ring systems, e.g. ticarcillin, azlocillin, oxacillin
Novel iron chelating group conjugated penam derivatives described herein show antibacterial activity, and could be used as antibacterial agents or beta-lactamase inhibitors (BLIs) which are of value for application in combination with other antibacterial agents.
C07D 499/87 - Compounds being unsubstituted in position 3 or with substituents other than only two methyl radicals attached in position 3, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/431 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems containing further heterocyclic ring systems, e.g. ticarcillin, azlocillin, oxacillin
C07D 519/06 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or containing at least one condensed beta-lactam ring system, provided for by groups , or , e.g. a penem or a cepham system
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
16.
ANTI-MICROBIAL COMPOSITION FOR TREATING GRAM-NEGATIVE BACTERIAL INFECTION
The present invention discloses an anti-microbial composition for treating Gram-negative bacterial infection. The composition comprises: TNP-2092 and a cell membrane penetrating agent. The cell membrane penetrating agent is polymyxin B or polymyxin E. The anti-microbial pharmaceutical composition for treating Gram-negative bacterial infection uses a joint application of TNP-2092 and the cell membrane penetrating agent to treat Gram-negative bacterial infection. The invention provides better anti-microbial activity when compared to using only TNP-2092 or the cell membrane penetrating agent. The invention achieves synergy in anti-microbial activity, and can be used to treat Gram-negative bacterial infections, including an infection of a drug resistant bacteria.
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
18.
BICYCLIC NITROIMIDAZOLES COVALENTLY LINKED TO SUBSTITUTED PHENYL OXAZOLIDINONES
The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bi-cyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild- type and resistant strains of pathogens, and are there-fore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.
Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
21.
(R/S) RIFAMYCIN DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS
Rifamycin derivatives having the following structure of general formula (I) (both hydroquinone and corresponding quinone (C1-C4) forms): or its salts, hydrates or prodrugs thereof; wherein a preferred R1 comprises hydrogen or acetyl and a prefered R2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.
4) forms):
wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG. 1, provided L is not
1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.
4) forms):
2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.
Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to a series of novel spiro rifamycin derivatives which have demonstrated potent antimicrobial activity.
C07D 225/04 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely designed in that they have a rifamycin moiety covalently linked to a linker group through the C-3 carbon of the rifamycin moiety and the linker is, in turn covalently linked to a therapeutic moiety or antibacterial agent/pharmacophore. The therapeutic moiety can be a quinolone, an oxazolidinone, a macrolide, an aminoglycoside, a tetracycline core or a structure/pharmacophore associated with an antibacterial agent.
Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to C-25 carbamate derivatives of rifamycin having another functional group or pharmacophore covalently attached to this position through a carbamate linkage. The resulting compounds exert their antimicrobial activity through a dual-function mechanism and therefore exhibit reduced frequency of resistance.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed rifamycin derivative has a rifamycin moiety covalently linked to a linker through an iminomethylenyl (—CH═N—) group at the C-3 carbon of the rifamycin moiety and the linker is, in turn, covalently linked to a quinolone structure or its pharmacophore within the DNA gyrase and topoisomerase IV inhibitor family. The inventive rifamycins are novel and exhibit activity against both rifampin and ciprofloxacin-resistant microorganisms.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
patents
