A61K31/545

SYRINGE FOR RECONSTITUTING AND INJECTING A PHARMACEUTICAL SOLUTION
20210386937 · 2021-12-16 ·

A prefilled syringe includes a tubular containment body extending along an axis between a front end element and a rear end element, a fixed plug and two sliding plugs. A bypass channel in the initial position of the syringe is between the first two plugs which form, together with a third plug at the end of the syringe plunger, a first containment chamber containing a first liquid substance and a second containment chamber containing a second solid or liquid substance. The fixed plug is in contact with the front end element and is provided with a non-through cavity offset with respect to the axis and facing towards the front end element.

SYRINGE FOR RECONSTITUTING AND INJECTING A PHARMACEUTICAL SOLUTION
20210386937 · 2021-12-16 ·

A prefilled syringe includes a tubular containment body extending along an axis between a front end element and a rear end element, a fixed plug and two sliding plugs. A bypass channel in the initial position of the syringe is between the first two plugs which form, together with a third plug at the end of the syringe plunger, a first containment chamber containing a first liquid substance and a second containment chamber containing a second solid or liquid substance. The fixed plug is in contact with the front end element and is provided with a non-through cavity offset with respect to the axis and facing towards the front end element.

PROCESSES FOR PREPARING A DIAZABICYCLOOCTANE COMPOUND

A process for preparing a diazabicyclooctane compound represented by the following formula (I):

##STR00001##

wherein A represents RcO—; B represents NH or NC.sub.1-6 alkyl; C represents a benzyl group; Rc represents a C.sub.1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):

##STR00002##

wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.

PROCESSES FOR PREPARING A DIAZABICYCLOOCTANE COMPOUND

A process for preparing a diazabicyclooctane compound represented by the following formula (I):

##STR00001##

wherein A represents RcO—; B represents NH or NC.sub.1-6 alkyl; C represents a benzyl group; Rc represents a C.sub.1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):

##STR00002##

wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.

PROCESSES FOR PREPARING A DIAZABICYCLOOCTANE COMPOUND

A process for preparing a diazabicyclooctane compound represented by the following formula (I):

##STR00001##

wherein A represents RcO—; B represents NH or NC.sub.1-6 alkyl; C represents a benzyl group; Rc represents a C.sub.1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):

##STR00002##

wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.

SOLID FORMS OF AN ORALLY-DELIVERED BETA-LACTAMASE INHIBITOR AND USES THEREOF

Disclosed herein are crystalline forms of ((2-Ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate. Also disclosed herein are methods of treating a bacterial with a crystalline form of ((2-Ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate.

SOLID FORMS OF AN ORALLY-DELIVERED BETA-LACTAMASE INHIBITOR AND USES THEREOF

Disclosed herein are crystalline forms of ((2-Ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate. Also disclosed herein are methods of treating a bacterial with a crystalline form of ((2-Ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate.

MULTICOMPONENT CRYSTAL FORMULATIONS
20220168312 · 2022-06-02 ·

A multicomponent crystal (or co-crystal) comprising a first active pharmaceutical ingredient and a second active pharmaceutical ingredient. The multicomponent crystal is formed/sustained by non-covalent interactions between the nitrogen-containing heterocycle alpha-substituted with an amino group of the first active pharmaceutical ingredient and a carboxylic acid group of the second active pharmaceutical ingredient, suitably as well as other further non-covalent interactions with other H-bond forming groups. The multicomponent crystal may provide an improved multidrug dosage form comprising lamotrigine and valproic acid as the first and second active pharmaceutical ingredients, respectively. A pharmaceutical composition comprising a therapeutically effective amount of the multicomponent crystal and a pharmaceutically acceptable excipient, and a method of forming the multicomponent crystal, are also provided.

MULTICOMPONENT CRYSTAL FORMULATIONS
20220168312 · 2022-06-02 ·

A multicomponent crystal (or co-crystal) comprising a first active pharmaceutical ingredient and a second active pharmaceutical ingredient. The multicomponent crystal is formed/sustained by non-covalent interactions between the nitrogen-containing heterocycle alpha-substituted with an amino group of the first active pharmaceutical ingredient and a carboxylic acid group of the second active pharmaceutical ingredient, suitably as well as other further non-covalent interactions with other H-bond forming groups. The multicomponent crystal may provide an improved multidrug dosage form comprising lamotrigine and valproic acid as the first and second active pharmaceutical ingredients, respectively. A pharmaceutical composition comprising a therapeutically effective amount of the multicomponent crystal and a pharmaceutically acceptable excipient, and a method of forming the multicomponent crystal, are also provided.

Processes for preparing a diazabicyclooctane compound

A process for preparing a diazabicyclooctane compound represented by the following formula (I): ##STR00001##
wherein A represents RcO—; B represents NH or NC.sub.1-6 alkyl; C represents a benzyl group; Rc represents a C.sub.1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): ##STR00002##
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.