The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.
Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.
Described herein are methods for treating transthyretin (TTR) amyloidosis with Compound 1 in a subject comprising certain mutations in the TTR protein (Compound 1). The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.
A61K 31/635 - Composés contenant des groupes para-N-benzènesulfonyl-N-, p. ex. sulfanilamide, p-nitrobenzènesulfonohydrazide contenant un hétérocycle, p. ex. sulfadiazine
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens
4.
PROCESSES FOR PREPARING AG-10, ITS INTERMEDIATES, AND SALTS THEREOF
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib
as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
C07D 231/12 - Composés hétérocycliques contenant des cycles diazole-1, 2 ou diazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant deux ou trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle
C07C 309/04 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone acycliques d'un squelette carboné acyclique saturé contenant un seul groupe sulfo
C07C 309/30 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone de cycles aromatiques à six chaînons d'un squelette carboné de cycles aromatiques à six chaînons non condensés de cycles aromatiques à six chaînons substitués par des groupes alkyle
The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib
as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
C07D 231/12 - Composés hétérocycliques contenant des cycles diazole-1, 2 ou diazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant deux ou trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle
C07C 309/04 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone acycliques d'un squelette carboné acyclique saturé contenant un seul groupe sulfo
C07C 309/30 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone de cycles aromatiques à six chaînons d'un squelette carboné de cycles aromatiques à six chaînons non condensés de cycles aromatiques à six chaînons substitués par des groupes alkyle
Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib
as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
C07D 231/12 - Composés hétérocycliques contenant des cycles diazole-1, 2 ou diazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant deux ou trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle
C07C 309/04 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone acycliques d'un squelette carboné acyclique saturé contenant un seul groupe sulfo
C07C 309/30 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone de cycles aromatiques à six chaînons d'un squelette carboné de cycles aromatiques à six chaînons non condensés de cycles aromatiques à six chaînons substitués par des groupes alkyle
The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.
The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.
Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.
Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
13.
Process for preparing AG-10, its intermediates, and salts thereof
Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib
as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
C07D 231/12 - Composés hétérocycliques contenant des cycles diazole-1, 2 ou diazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant deux ou trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle
C07C 309/04 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone acycliques d'un squelette carboné acyclique saturé contenant un seul groupe sulfo
C07C 309/30 - Acides sulfoniques ayant des groupes sulfo liés à des atomes de carbone de cycles aromatiques à six chaînons d'un squelette carboné de cycles aromatiques à six chaînons non condensés de cycles aromatiques à six chaînons substitués par des groupes alkyle
14.
PROCESSES FOR PREPARING AG-10, ITS INTERMEDIATES, AND SALTS THEREOF
Provided herein are improved processes for the preparation of a compound of Formula IX (AG- 10). Also provided herein are pharmaceutically acceptable salts of Formula (I) and Formula (lb) as well as crystalline types of Formula IX (AG- 10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
brevets
