Abstract

The invention relates to novel rufomycin analogs targeting C1pC1 protease. The compounds of the invention have antibacterial activity, for example, with anti-tuberculosis properties, and are useful for the treatment of, for example, tuberculosis.

IPC Classes  ?

• C07K 7/54 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
• A61K 38/12 - Cyclic peptides

Abstract

The present invention relates to compounds of formula (IA): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

IPC Classes  ?

• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings

Abstract

The present invention relates to pretomanid in amorphous form. The invention also relates to method of using the same, such as in a method of treating a mycobacterial infection.

IPC Classes  ?

• C07D 498/04 - Ortho-condensed systems
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/10 - DispersionsEmulsions
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• 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

Abstract

The present invention relates to therapeutic combinations of anti-bacterial agents linezolid, bedaquiline and pretomanid, and optionally with pyrazinamide, in a short-course oral dosage regimen for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 31/4965 - Non-condensed pyrazines
• 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
• C07D 498/04 - Ortho-condensed systems
• C07D 263/20 - Oxygen atoms attached in position 2
• C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
• C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61P 31/04 - Antibacterial agents

Abstract

Provided are methods of preparing a homogeneous mixture from a solid dosage form in settings including a point of care setting. The methods include obtaining a solid dosage form comprising a drug product, adding the solid dosage form to a container having at least one flexible section, adding a liquid to the container, mixing the solid dosage form with the liquid to disperse, disintegrate, suspend, and/or dissolve the solid dosage form thereby creating a homogeneous mixture. Also provided are containers and devices for use in such methods.

IPC Classes  ?

• A61J 1/20 - Arrangements for transferring fluids, e.g. from vial to syringe
• B01F 31/55 - Mixers with shaking, oscillating, or vibrating mechanisms the materials to be mixed being contained in a flexible bag submitted to periodical deformation
• B01F 35/513 - Flexible receptacles, e.g. bags supported by rigid containers
• B01F 23/50 - Mixing liquids with solids
• B01F 21/00 - Dissolving

Abstract

Provided herein are compounds of Formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis. Provided herein are compounds of Formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/695 - Silicon compounds
• C07F 7/08 - Compounds having one or more C—Si linkages
• A61P 31/06 - Antibacterial agents for tuberculosis
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• 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
• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
• A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
• A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• A61K 31/42 - Oxazoles
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings

Abstract

Provided herein are compounds of Formula (I) and Formula (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis. Provided herein are compounds of Formula (I) and Formula (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07F 7/08 - Compounds having one or more C—Si linkages
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Provided herein are compounds of Formula (I) and Formula (II) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis. Provided herein are compounds of Formula (I) and Formula (II) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
• C07F 7/08 - Compounds having one or more C—Si linkages
• A61K 31/695 - Silicon compounds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

The present invention relates to pretomanid in amorphous form. The invention also relates to method of using the same, such as in a method of treating a mycobacterial infection.

IPC Classes  ?

• C07D 498/04 - Ortho-condensed systems
• A61P 31/04 - Antibacterial agents
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

The present invention relates to pretomanid in amorphous form. The invention also relates to method of using the same, such as in a method of treating a mycobacterial infection.

IPC Classes  ?

• C07D 498/04 - Ortho-condensed systems
• A61P 31/06 - Antibacterial agents for 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
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 31/04 - Antibacterial agents

Abstract

Provided are methods of preparing a homogeneous mixture from a solid dosage form in settings including a point of care setting. The methods include obtaining a solid dosage form comprising a drug product, adding the solid dosage form to a container having at least one flexible section, adding a liquid to the container, mixing the solid dosage form with the liquid to disperse, disintegrate, suspend, and/or dissolve the solid dosage form thereby creating a homogeneous mixture. Also provided are containers and devices for use in such methods.

IPC Classes  ?

• B01F 13/02 - Mixers with gas agitation, e.g. with air supply tubes
• B01F 5/10 - Circulation mixers
• B01F 3/18 - Mixing, e.g. dispersing, emulsifying, according to the phases to be mixed solid with solids

Abstract

Provided are methods of preparing a homogeneous mixture from a solid dosage form in settings including a point of care setting. The methods include obtaining a solid dosage form comprising a drug product, adding the solid dosage form to a container having at least one flexible section, adding a liquid to the container, mixing the solid dosage form with the liquid to disperse, disintegrate, suspend, and/or dissolve the solid dosage form thereby creating a homogeneous mixture. Also provided are containers and devices for use in such methods.

IPC Classes  ?

• B01F 35/513 - Flexible receptacles, e.g. bags supported by rigid containers
• B01F 21/00 - Dissolving
• B01F 23/50 - Mixing liquids with solids
• B01F 31/00 - Mixers with shaking, oscillating, or vibrating mechanisms
• B01F 33/00 - Other mixersMixing plantsCombinations of mixers
• A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
• A61K 9/08 - Solutions
• A61K 9/10 - DispersionsEmulsions

Abstract

Fixed-dose pharmaceutical dosage form are described that may be useful in methods for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
• A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
• A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like

Abstract

Fixed-dose pharmaceutical dosage form are described that may be useful in methods for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/47 - QuinolinesIsoquinolines
• A61K 31/4965 - Non-condensed pyrazines
• 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

Goods & Services

Pharmaceuticals dispensing device used to dissolve solid dosage forms in liquid form.

Goods & Services

Pharmaceuticals dispensing device used to dissolve solid dosage forms in liquid form.

Goods & Services

Pharmaceuticals dispensing device used to dissolve solid dosage forms in liquid form.

Goods & Services

pharmaceuticals dispensing device used to dissolve solid dosage forms in liquid form

Goods & Services

pharmaceuticals dispensing device used to dissolve solid dosage forms in liquid form

Goods & Services

pharmaceuticals dispensing device used to dissolve solid dosage forms in liquid form

Abstract

Provided herein are compounds of Formula (I) and Formula (II) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• C07D 513/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
• C07D 513/04 - Ortho-condensed systems

Abstract

Provided herein are compounds of Formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen
• A61K 31/695 - Silicon compounds
• A61P 31/04 - Antibacterial agents

Abstract

Provided herein are compounds of Formula (I) and Formula (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

Provided herein are compounds of Formula (I) and Formula (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

Provided herein are compounds of Formula (I) and Formula (II) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/425 - Thiazoles
• A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
• C07D 277/00 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
• C07D 513/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
• C07D 513/04 - Ortho-condensed systems

Abstract

Provided herein are compounds of Formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/695 - Silicon compounds
• A61P 31/04 - Antibacterial agents
• C07D 209/02 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
• C07D 209/04 - IndolesHydrogenated indoles

Abstract

Described is an oral pharmaceutical composition including a granulate including a pharmaceutically effective amount of pretomanid or pharmaceutically acceptable solvate thereof. Such granulate may have a bulk density in a range of about 0.3 to 0.8 g/mL and/or a particle size distribution such that no more than about 30 wt.% of the granulate is retained on an ASTM #60 (250µm) sieve. In particular, the composition may provide that at least 40 wt.% of the pretomanid (e.g., at least 60 wt.%) is dissolved within 20 minutes as measured in a USP-II Apparatus at 37± 2° C in 0.5% hexadecyltrimethylammonium bromide (HDTMA) in 0.1N HCl.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam

Abstract

Described is an oral pharmaceutical composition including a granulate including a pharmaceutically effective amount of pretomanid or pharmaceutically acceptable solvate thereof. Such granulate may have a bulk density in a range of about 0.3 to 0.8 g/mL and/or a particle size distribution such that no more than about 30 wt.% of the granulate is retained on an ASTM #60 (250µm) sieve. In particular, the composition may provide that at least 40 wt.% of the pretomanid (e.g., at least 60 wt.%) is dissolved within 20 minutes as measured in a USP-II Apparatus at 37± 2° C in 0.5% hexadecyltrimethylammonium bromide (HDTMA) in 0.1N HCl.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam

Abstract

Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61K 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 31/06 - Antibacterial agents for tuberculosis
• C07D 263/20 - Oxygen atoms attached in position 2
• C07D 263/24 - Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
• C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 491/08 - Bridged systems
• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• C07D 495/08 - Bridged systems
• C07D 495/10 - Spiro-condensed systems
• C07D 498/08 - Bridged systems
• C07D 513/08 - Bridged systems

Abstract

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

IPC Classes  ?

• C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• C07F 5/02 - Boron compounds
• A61P 31/06 - Antibacterial agents for tuberculosis
• A61K 31/69 - Boron compounds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/4965 - Non-condensed pyrazines

Abstract

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

IPC Classes  ?

• C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

The present invention relates to therapeutic combinations of anti-bacterial agents linezolid, bedaquiline and pretomanid, and optionally with pyrazinamide, in a short-course oral dosage regimen for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/47 - QuinolinesIsoquinolines
• 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 31/4965 - Non-condensed pyrazines
• A61P 31/04 - Antibacterial agents

Abstract

Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.

IPC Classes  ?

• C07D 263/20 - Oxygen atoms attached in position 2
• C07D 263/24 - Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• C07D 495/10 - Spiro-condensed systems
• C07D 498/08 - Bridged systems
• A61P 31/06 - Antibacterial agents for tuberculosis
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 491/08 - Bridged systems
• C07D 495/08 - Bridged systems

Abstract

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/69 - Boron compounds
• C07F 5/02 - Boron compounds

Abstract

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

IPC Classes  ?

• A01N 55/08 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur containing boron
• A61K 31/69 - Boron compounds
• C07F 5/02 - Boron compounds

Abstract

The present invention relates to compounds of formula (I): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

IPC Classes  ?

• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 31/06 - Antibacterial agents for tuberculosis
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

IPC Classes  ?

• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 31/06 - Antibacterial agents for tuberculosis
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

Abstract

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to therapeutic combinations of anti-bacterial agents linezolid, bedaquiline and pretomanid, and optionally with pyrazinamide, in a short-course oral dosage regimen for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/47 - QuinolinesIsoquinolines
• 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
• C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
• C07D 263/20 - Oxygen atoms attached in position 2
• C07D 413/02 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
• C07D 498/04 - Ortho-condensed systems

Abstract

The present invention relates to therapeutic combinations of anti-bacterial agents linezolid, bedaquiline and pretomanid, and optionally with pyrazinamide, in a short-course oral dosage regimen for the treatment of tuberculosis.

IPC Classes  ?

• A61K 31/47 - QuinolinesIsoquinolines
• 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
• C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
• C07D 263/20 - Oxygen atoms attached in position 2
• C07D 413/02 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
• C07D 498/04 - Ortho-condensed systems

Abstract

The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.

IPC Classes  ?

• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.

IPC Classes  ?

• C07D 495/10 - Spiro-condensed systems
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61P 31/04 - Antibacterial agents
• C07D 417/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Abstract

Described herein are compounds and compositions for treating drug resistant and persistent tuberculosis. Also described herein is a method of screening for identifiying biofilm formation inhibitors.

IPC Classes  ?

• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom