96 results about "Cotransporter" patented technology

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and / or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and / or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and / or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and / or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

The present invention relates to methods and compositions for treating disorders of the central and / or peripheral nervous system by administering agents that are effective in reducing the effective amount, inactivating, and / or inhibiting the activity of a Na+—K+—2CT (NKCC) cotransporter. In certain embodiments, the Na+—K+—2Cl− co-transporter is NKCC1.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and / or inhibiting the activity of a Na+—K+-2Cl− (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl− co-transporter is NKCC1.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The invention belongs to the technical filed of medicines, and concretely relates to optically pure benzyl-4-chlorophenyl C-glucoside derivatives represented by formula (II) and formula (III), a method for preparing the above compounds and intermediates thereof, a medicinal preparation and a medicinal composition containing the compounds, and an application of the optically pure benzyl-4-chlorophenyl C-glucoside derivatives in the preparation of medicines for treating and / or preventing insulin-dependent diabetes, non-insulin dependent diabetes, insulin resistance diseases or obesity, various diabetes and relevant diseases as a sodium-glucose cotransporter (SGLT) inhibitor.

The present invention provides novel type IIc Na / Pi cotransporters. These cotransporters are important Pi transporters that are highly expressed during the growth period from the weaning stage to the adult stage. Furthermore, the present invention provides FGF23 and mutants thereof as factors that regulate the expression of type II Na / Pi cotransporters. FGF23 suppresses Pi reabsorption through suppression of type II Na / Pi cotransporter expression in kidneys. Therefore, FGF23 can be used as a target substance for regulating Pi reabsorption in kidneys. The present invention provides important factors for the development of preventive and therapeutic agents for hyperphosphatemia or hypophosphatemia.

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.

The present invention relates to a method for dual inhibition of sodium-dependent glucose cotransporter 1 (SGLT1) and sodium-dependent glucose cotransporter 2 (SGLT2) present in the intestine and kidney by using the compound of formula I or a pharmaceutically acceptable salt or a prodrug thereof:wherein ring A, ring B, X and Y have the same meanings as defined in the specification.

The present invention provides pyrazole derivatives represented by the general formula:wherein R1 represents H, an optionally substituted C1-6 alkyl, etc.; one of Q and T represents a group selected from the following:and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.;R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium / glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.

Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

The present invention provides methods for using chloride ion uptake modulators to treat disorders that are mediated by a sodium / potassium / chloride cotransporter.

The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and / or inhibiting the activity of a Na+—K+-2Cl− (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl− co-transporter is NKCC1.

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na<+>-glucose cotransporter inhibitor, especially for a therapeutic and / or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl, etc.; one of Q and T represents a group selected from the following: , and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.; R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium / glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.

Methods and products for the attenuation or treatment of pain and the reduction of nociception are described. The methods and products are based on the modulation of CNS intracellular chloride levels. The methods and products may also relate to modulation of the activity and / or expression of a chloride transporter, such as the KCC2 potassium-chloride cotransporter. Also described herein are commercial packages and uses based on such modulation. Related methods for identifying or characterizing a compound for the treatment of pain, the reduction of nociception and the diagnosis and prognostication of pain are also described.