The present disclosure provides a modified-release pharmaceutical composition comprising 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, and a pharmaceutically-acceptable excipient. The present disclosure methods of treating conditions associated with RyRs, including, for example, cardiac disorder or disease, a musculoskeletal disorder or disease, cancer associated muscle weakness, malignant hyperthermia, and diabetes.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Pharmaceutical preparations for restoring normal intracellular calcium regulation; Chemical preparations for pharmaceutical purposes; Chemical preparations for medical purposes; Chemical preparations for pharmaceutical or medical purposes for restoring normal intracellular calcium regulation; Chemical preparations for restoring normal intracellular calcium regulation; Pharmaceutical preparations for the treatment of diseases of the musculo-skeletal system; Pharmaceutical preparations for the treatment of Musculo-skeletal disorders; Pharmaceutical preparations for the prevention of disorders of the Musculo-skeletal system; Pharmaceutical preparations for the treatment of cardiovascular disorders; Pharmaceutical preparations for the treatment of diseases of the cardio-vascular system; Pharmaceutical preparations for the prevention of disorders of the cardio-vascular system; Pharmaceutical preparations for the prevention of diseases of the cardio-vascular system; Muscle relaxants; Skeletal muscle relaxants; Pharmaceutical preparations for the treatment of muscle fatigue; Pharmaceutical preparations for the prevention of muscle fatigue; Pharmaceutical preparations for the treatment of cognitive disorders; Pharmaceutical preparations for the treatment of bone disorders; Pharmaceutical preparations for the prevention of cognitive disorders; Pharmaceutical preparations for the prevention of bone disorders; Pharmaceutical preparations for medical purposes; Medicinal preparations for restoring normal intracellular calcium regulation; Medicinal preparations for the treatment of diseases of the musculo-skeletal system; Medicinal preparations for the treatment of Musculo-skeletal disorders; Medicinal preparations for the prevention of disorders of the Musculo-skeletal system; Medicinal preparations for the treatment of cardiovascular disorders; Medicinal preparations for the treatment of diseases of the cardio-vascular system; Medicinal preparations for the prevention of disorders of the cardio-vascular system; Medicinal preparations for the prevention of diseases of the cardio-vascular system; Medicinal preparations for the treatment of muscle fatigue; Medicinal preparations for the prevention of muscle fatigue; Medicinal preparations for the treatment of cognitive disorders; Medicinal preparations for the treatment of bone disorders; Medicinal preparations for the prevention of cognitive disorders; Medicinal preparations for the prevention of bone disorders; Chemical preparations for pharmaceutical or medical purposes for cardiovascular disorders and diseases; Chemical preparations for pharmaceutical or medical purposes for skeletal muscle disorders and diseases; Chemical preparations for pharmaceutical or medical purposes for muscle fatigue; Chemical preparations for pharmaceutical or medical purposes for cognitive disorders; Chemical preparations for pharmaceutical or medical purposes for bone disorders. Pharmaceutical research and development.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Pharmaceutical preparations for restoring normal intracellular calcium regulation; Chemical preparations for pharmaceutical purposes; Chemical preparations for medical purposes; Chemical preparations for pharmaceutical or medical purposes for restoring normal intracellular calcium regulation; Chemical preparations for restoring normal intracellular calcium regulation; Pharmaceutical preparations for the treatment of diseases of the musculo-skeletal system; Pharmaceutical preparations for the treatment of Musculo-skeletal disorders; Pharmaceutical preparations for the prevention of disorders of the Musculo-skeletal system; Pharmaceutical preparations for the treatment of cardiovascular disorders; Pharmaceutical preparations for the treatment of diseases of the cardio-vascular system; Pharmaceutical preparations for the prevention of disorders of the cardio-vascular system; Pharmaceutical preparations for the prevention of diseases of the cardio-vascular system; Muscle relaxants; Skeletal muscle relaxants; Pharmaceutical preparations for the treatment of muscle fatigue; Pharmaceutical preparations for the prevention of muscle fatigue; Pharmaceutical preparations for the treatment of cognitive disorders; Pharmaceutical preparations for the treatment of bone disorders; Pharmaceutical preparations for the prevention of cognitive disorders; Pharmaceutical preparations for the prevention of bone disorders; Pharmaceutical preparations for medical purposes; Medicinal preparations for restoring normal intracellular calcium regulation; Medicinal preparations for the treatment of diseases of the musculo-skeletal system; Medicinal preparations for the treatment of Musculo-skeletal disorders; Medicinal preparations for the prevention of disorders of the Musculo-skeletal system; Medicinal preparations for the treatment of cardiovascular disorders; Medicinal preparations for the treatment of diseases of the cardio-vascular system; Medicinal preparations for the prevention of disorders of the cardio-vascular system; Medicinal preparations for the prevention of diseases of the cardio-vascular system; Medicinal preparations for the treatment of muscle fatigue; Medicinal preparations for the prevention of muscle fatigue; Medicinal preparations for the treatment of cognitive disorders; Medicinal preparations for the treatment of bone disorders; Medicinal preparations for the prevention of cognitive disorders; Medicinal preparations for the prevention of bone disorders; Chemical preparations for pharmaceutical or medical purposes for cardiovascular disorders and diseases; Chemical preparations for pharmaceutical or medical purposes for skeletal muscle disorders and diseases; Chemical preparations for pharmaceutical or medical purposes for muscle fatigue; Chemical preparations for pharmaceutical or medical purposes for cognitive disorders; Chemical preparations for pharmaceutical or medical purposes for bone disorders. Pharmaceutical research and development.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Pharmaceutical preparations for restoring normal intracellular calcium regulation; Chemical preparations for pharmaceutical purposes; Chemical preparations for medical purposes; Chemical preparations for pharmaceutical or medical purposes for restoring normal intracellular calcium regulation; Chemical preparations for restoring normal intracellular calcium regulation; Pharmaceutical preparations for the treatment of diseases of the musculo-skeletal system; Pharmaceutical preparations for the treatment of Musculo-skeletal disorders; Pharmaceutical preparations for the prevention of disorders of the Musculo-skeletal system; Pharmaceutical preparations for the treatment of cardiovascular disorders; Pharmaceutical preparations for the treatment of diseases of the cardio-vascular system; Pharmaceutical preparations for the prevention of disorders of the cardio-vascular system; Pharmaceutical preparations for the prevention of diseases of the cardio-vascular system; Muscle relaxants; Skeletal muscle relaxants; Pharmaceutical preparations for the treatment of muscle fatigue; Pharmaceutical preparations for the prevention of muscle fatigue; Pharmaceutical preparations for the treatment of cognitive disorders; Pharmaceutical preparations for the treatment of bone disorders; Pharmaceutical preparations for the prevention of cognitive disorders; Pharmaceutical preparations for the prevention of bone disorders; Pharmaceutical preparations for medical purposes; Medicinal preparations for restoring normal intracellular calcium regulation; Medicinal preparations for the treatment of diseases of the musculo-skeletal system; Medicinal preparations for the treatment of Musculo-skeletal disorders; Medicinal preparations for the prevention of disorders of the Musculo-skeletal system; Medicinal preparations for the treatment of cardiovascular disorders; Medicinal preparations for the treatment of diseases of the cardio-vascular system; Medicinal preparations for the prevention of disorders of the cardio-vascular system; Medicinal preparations for the prevention of diseases of the cardio-vascular system; Medicinal preparations for the treatment of muscle fatigue; Medicinal preparations for the prevention of muscle fatigue; Medicinal preparations for the treatment of cognitive disorders; Medicinal preparations for the treatment of bone disorders; Medicinal preparations for the prevention of cognitive disorders; Medicinal preparations for the prevention of bone disorders; Chemical preparations for pharmaceutical or medical purposes for cardiovascular disorders and diseases; Chemical preparations for pharmaceutical or medical purposes for skeletal muscle disorders and diseases; Chemical preparations for pharmaceutical or medical purposes for muscle fatigue; Chemical preparations for pharmaceutical or medical purposes for cognitive disorders; Chemical preparations for pharmaceutical or medical purposes for bone disorders. Pharmaceutical research and development.
5.
CRYSTALLINE FORMS OF A RYANODINE RECEPTOR MODULATOR AND USES THEREOF
The present disclosure relates to crystalline forms of the compound 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, pharmaceutical compositions comprising these compounds and uses thereof to treat diseases and conditions associated with Ryanodine Receptor (RyR) dysfunction, in particular cardiac and musculoskeletal disorders and diseases.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
The present disclosure provides methods of treating catecholaminergic polymorphic ventricular tachycardia, comprising administering a pharmaceutical composition comprising, in a unit dosage form, a therapeutically effective amount of 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-1(5H)yl)methyl]benzoic acid hemifumarate, and a pharmaceutically acceptable excipient.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61K 31/4458 - Pipéridines non condensées, p. ex. pipérocaïne substituées uniquement en position 2, p. ex. méthylphénidate
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
chemical preparations for pharmaceutical or medical purposes, namely, for cardiovascular disorders and diseases, skeletal muscle disorders and diseases, muscle fatigue, cognitive disorders and bone disorders; pharmaceutical preparations for the treatment and prevention of cardiovascular disorders and diseases, skeletal muscle disorders and diseases, muscle fatigue, cognitive disorders and bone disorders; Chemical preparations for pharmaceutical or medical purposes, namely, for restoring normal intracellular calcium regulation; pharmaceutical preparations for that restoring normal intracellular calcium regulation Pharmaceutical research and development
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
chemical preparations for pharmaceutical or medical purposes, namely, for cardiovascular disorders and diseases, skeletal muscle disorders and diseases, muscle fatigue, cognitive disorders and bone disorders; Chemical preparations for pharmaceutical or medical purposes, namely, for restoring normal intracellular calcium regulation; pharmaceutical preparations for the treatment and prevention of cardiovascular disorders and diseases, skeletal muscle disorders and diseases, muscle fatigue, cognitive disorders and bone disorders; pharmaceutical preparations for that restoring normal intracellular calcium regulation Pharmaceutical research and development
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
pharmaceutical preparations for that restoring normal intracellular calcium regulation; Chemical preparations for pharmaceutical or medical purposes, namely, for restoring normal intracellular calcium regulation; pharmaceutical preparations for the treatment and prevention of cardiovascular disorders and diseases, skeletal muscle disorders and diseases, muscle fatigue, cognitive disorders and bone disorders; chemical preparations for pharmaceutical or medical purposes, namely, for cardiovascular disorders and diseases, skeletal muscle disorders and diseases, muscle fatigue, cognitive disorders and bone disorders Pharmaceutical research and development
10.
AGENTS FOR TREATING DISORDERS INVOLVING RYANODINE RECEPTORS
The present disclosure relates to 1,4-oxazepane and 1,4-thiazepane derivatives and their use to treat disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel signaling in cells. The present disclosure also discloses pharmaceutical compositions comprising these compounds and uses thereof to treat diseases and conditions associated with RyR dysfunction, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
The present disclosure relates to 1,4-benzothiazepine derivatives and use thereof to treat conditions associated with ryanodine receptors that regulate calcium channel functioning in cells.
C07D 417/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
12.
Pharmaceutical compositions comprising a ryanodine receptor modulator and uses thereof
The present disclosure provides a modified-release pharmaceutical composition comprising 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, and a pharmaceutically-acceptable excipient. The present disclosure methods of treating conditions associated with RyRs, including, for example, cardiac disorder or disease, a musculoskeletal disorder or disease, cancer associated muscle weakness, malignant hyperthermia, and diabetes.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
13.
Pharmaceutical compositions comprising a ryanodine receptor modulator and uses thereof
The present disclosure provides a modified-release pharmaceutical composition comprising 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, and a pharmaceutically-acceptable excipient. The present disclosure methods of treating conditions associated with RyRs, including, for example, cardiac disorder or disease, a musculoskeletal disorder or disease, cancer associated muscle weakness, malignant hyperthermia, and diabetes.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
14.
Crystalline forms of a ryanodine receptor modulator and uses thereof
The present disclosure relates to crystalline forms of the compound 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, pharmaceutical compositions comprising these compounds and uses thereof to treat diseases and conditions associated with Ryanodine Receptor (RyR) dysfunction, in particular cardiac and musculoskeletal disorders and diseases.
C07D 281/10 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle à six chaînons
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61P 9/00 - Médicaments pour le traitement des troubles du système cardiovasculaire
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
15.
Crystalline forms of a ryanodine receptor modulator and uses thereof
The present disclosure relates to crystalline forms of the compound 4-[(7-methoxy-2,3-dihydro-1, 4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, pharmaceutical compositions comprising these compounds and uses thereof to treat diseases and conditions associated with Ryanodine Receptor (RyR) dysfunction, in particular cardiac and musculoskeletal disorders and diseases.
C07D 281/10 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle à six chaînons
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61P 9/00 - Médicaments pour le traitement des troubles du système cardiovasculaire
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
16.
Pharmaceutical compositions comprising a ryanodine receptor modulator and uses thereof
The present disclosure provides a modified-release pharmaceutical composition comprising 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, and a pharmaceutically-acceptable excipient. The present disclosure methods of treating conditions associated with RyRs, including, for example, cardiac disorder or disease, a musculoskeletal disorder or disease, cancer associated muscle weakness, malignant hyperthermia, and diabetes.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
17.
Crystalline forms of a Ryanodine receptor modulator and uses thereof
The present disclosure relates to crystalline forms of the compound 4-[(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)yl)methyl]benzoic acid hemifumarate, pharmaceutical compositions comprising these compounds and uses thereof to treat diseases and conditions associated with Ryanodine Receptor (RyR) dysfunction, in particular cardiac and musculoskeletal disorders and diseases.
C07D 281/10 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle à six chaînons
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
A61P 9/00 - Médicaments pour le traitement des troubles du système cardiovasculaire
A61P 21/00 - Médicaments pour le traitement des troubles du système musculaire ou neuromusculaire
18.
Process for preparing benzothiazepines from gamma-aminoalkylbenzenes
The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula:
by reacting a [2-(acylaminoethyl)thio]arene of formula
with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula
then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
C07D 281/10 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle à six chaînons
19.
Agents for treating disorders involving modulation of ryanodine receptors
The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
C07D 281/10 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle à six chaînons
A61K 31/7088 - Composés ayant au moins trois nucléosides ou nucléotides
The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula:
by reacting a [2-(acylaminoethyl)thio]arene of formula
with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula
then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.
C07D 281/08 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques
C07D 281/10 - Cycles à sept chaînons comportant les hétéro-atomes en positions 1, 4 condensés avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle à six chaînons
