05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
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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 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & 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 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & 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.
4.
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 - 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
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 - 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 31/4458 - Non-condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & 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 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & 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 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & 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
9.
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 - 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 only aliphatic carbon atoms
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
11.
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 - 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
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 - 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
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 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
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 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
15.
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 - 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
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
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 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
17.
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 - 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 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
18.
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 - 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 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
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 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
C07D 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
