784 results about "Diabetic complication" patented technology

Use of 6-desaturated n-6 fatty acids, especially gammalinolenic acid (GLA), dihomogammalinolenic acid (DGLA) or arachidonic acid (AA), together with a pharmaceutically acceptable material reducing intracellular levels of sorbitol in the body, particularly an aldose reductase inhibitor, in the treatment of (including prophylactic treatment), and in the preparation of medicaments for the treatment of (including prophylactic treatment), the long-term complications of diabetes mellitus. Pharmaceutical compositions of said materials. The ascorbate esters of 6-desaturated n-6 fatty acids (other than GLA or DGLA) per se.

The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. ##STR1## In the formula, W is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.ident.C--; R.sup.1 is: ##STR2## (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R.sup.5 and R.sup.6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R.sup.2 is an amino group, etc. which maybe substituted with a lower alkyl group, etc.; R.sup.3 is a cycloalkyl group, an optionally substituted aryl group, etc.; and R.sup.4 is a lower alkyl group etc. ##STR3##

The present invention discloses a treatment for syndrome-X, and resulting complications, that include hyperlipidemia, hypertension, central obesity, hyperinsulinemia and impaired glucose intolerance. Diabetic complications include excess proinsulin levels.

The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.

A 5-membered heteroaromatic ring compound represented by the formula [I]wherein V is CH or N; W is S or O; R1 and R2 are each H etc.; X is —N(R4)—, —O—, —S—, —SO2—N(R5)—, —CO—N(R7)— etc.; L is wherein R20, R21, R22 and R25 are each H etc.; E is aryl or heteroaromatic ring group; R is —COOH etc.; B is aryl etc.; R3 is H etc.; Y is —C(R13)(R14)—N(R12)—C(R13)(R14)—O—, —N(R11)—, —O— etc.; A is alkylene; and Z is aryl etc., a prodrug thereof and a pharmaceutically acceptable salt thereof. The compound [I] has a superior protein tyrosine phosphatase 1B inhibitory activity and is useful as a therapeutic agent for diabetes, diabetic complications, hyperlipidemia, obesity and the like.

The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.

The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents , or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.

Compostions of GLA and / or other EFAs with TA or related compounds, and their use in therapy or nutrition or in preparation of composition for therapy or nutrition, especially to improve cell membrane EFA concentration and / or (particularly in diabetic complications) impaired nerve function and blood flow.

The present invention provides phenol derivatives represented by the following general formula or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like, and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof. In the chemical structure, R1 and R2 represent H, OH, NH2, etc.; R3and R4represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G); E1 represents H or F; and E2 represents H, F, or a methyl group, etc.

The present invention provides novel benzene compounds presented by the following formulas, and analogs thereof, that exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hypertension, arteriosclerosis), hypertension, and arteriosclerosis.

The present invention relates to an azole compound represented by the formula [I]wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.

The present invention provides pyrazole derivatives represented by the general formula:wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula:or a group represented by the general formula:while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula:wherein P represents a hydrogen atom or a group forming a prodrug; R1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

Provided is an herbal extract-based composition comprising an extract of Gynostemma pentaphyllum, an extract of Crataegus pinnatifidia (hawthorn), an extract of Camellia sinensis (green tea), and an extract of Momordica charantia (bitter melon). The composition may further comprise an extract of mulberry (Morus species). Also provided is a process for preparing a herbal extract-based composition which comprises separately extracting each of hawthorn, green tea, Gynostemma pentaphyllum, mulberry, and bitter melon; drying extraction eluates obtained from the extracting of each of the herbal components to obtain organic residues in forming a hawthorn extract powder, green tea extract powder, a Gynostemma pentaphyllum extract powder, a mulberry extract powder, and a bitter melon powder; and combining the green tea extract powder, the Gynostemma Pentaphyllum extract powder, the hawthorn extract powder, the mulberry extract powder, and the bitter melon powder in desired proportions to form the herbal extract-based composition which, when taken orally, has health-promoting effects including anti-diabetic effects that include, but are not limited to, decreasing visceral fat, reducing hyperglycemia, and reducing the occurrence and severity of diabetic complications, associated with type 2 diabetes.

Described herein is a compound of Formula I, which is the metformin salt of the naturally occurring endogenous biological compound, (R)-(+) α lipoic acid, pharmaceutical compositions containing the compound of Formula I, and methods of treatment of diabetes or diabetic complications with the compound of Formula I.

The present invention relates to an azole compound represented by the formula [I]wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.

The present invention provides fused heterocyclic derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 to R4 represent H, OH, an amino group, etc.; R5 and R6 represent H, OH, a halogen atom, an option ally substituted alkyl group, etc.; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; the following ring (R1) represents a group represented by the following ring (R2); G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

A compound represented by the formula (I) wherein one of R1 and R2 is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group; W is a bond or a divalent aliphatic hydrocarbon group; Y is a group of the formula: —OR3 (wherein R3 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.

The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action.That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I); (wherein R1 represents e.g. an amino group which may be substituted with an alkyl group; R2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.

The invention belongs to the field of biofermentation engineering. A pharmaceutical medium and a fungal strain which have blood sugar lowering efficacy are used as bidirectional fermentation raw materials, wherein the pharmaceutical medium is mainly composed of the following raw materials: cornel, gynostemma, momordica grosvenori, winged euony twigs, balsam pear and polyrhachis vicina; the fungalstrain is composed of the following strains: inonotus obliquus, cordyceps, phellinus igniarius, polystictus versicolor, and grifola frondosa; and bi-directional multi-fungi fermentation is carried out between multiple edible and pharmaceutical fungi and Chinese herbal medicines by a bidirectional fermentation process, thus organisms in two kingdoms or three kingdoms are organically combined to obtain an entirely new blood-sugar-lowering pharmaceutical mycoplasm product. The obtained product can generate 1+1>2 physiological function efficiency for hypoimmunity, has the actions of obviously lowering blood sugar but not increasing insulin concentration, has significant positive effects on helping treating and controlling diabetic complications, and can be used as an oral medicament for preventing and treating diabetes or a health-care product for adjusting blood sugar.

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:wherein R1, R2 and R3 represent a hydrogen atom or a halogen atom; R4 represents a lower alkyl group or a halo(lower alkyl) group; and R5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

There is provided a heteroaryl 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.

The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.

An agent for treating or ameliorating diabetic complications which contains at least one potassium channel activator as an active ingredient. The drug is expected to show a therapeutic or ameliorating action on diabetic complications such as retinopathy, neuropathy, nephropathy, peripheral circulation disorders, and skin ulcerations; it also proves effective in preventing, ameliorating, alleviating and gaining recovery from various symptoms and abnormalities caused by those diseases, as exemplified by blindness, proteinurea, pain, numbness, psychroesthesia, intermittent claudication and gangrene.

The present invention relates to Pyridyl-Substituted Porphyrin Compounds, compositions comprising an effective amount of a Pyridyl-Substituted Porphyrin Compound and methods for treating or preventing injury due to exposure to a reactive species, erectile dysfunction due to surgery, lung disease, hyperoxia, neurodegenerative disease, liver disease, myocardial damage during cardioplegia, an inflammatory condition, a reperfusion injury, an ischemic condition, a cardiovascular disease, diabetes, a diabetic complication, cancer, a side effect of cancer chemotherapy, or a radiation-induced injury, or to prolong the half-life of an oxidation-prone compound, comprising administering to a subject in need thereof an effective amount of a Pyridyl-Substituted Porphyrin Compound.

A novel compound of the formula:wherein ring Q is an optionally substituted pyridine ring;One of R0, R1 and R2 is -Y0-Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group;Y0 is a bond or an optionally substituted bivalent hydrocarbon group;Z0 is a basic group which may be bonded via oxygen, nitrogen, -CO-, -CS-, -SO2N(R3)- (where R3 is hydrogen or an optionally substituted hydrocarbon group), or S(O)n (wherein n is to 0, 1 or 2);......... is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.

The invention provides conditioning powder suitable of being eaten by a diabetic patient. The conditioning powder comprises 6-12 parts of water-soluble dietary fiber extractive, 0.1-1 part of wheat germ extractive, 0.1-1.5 parts of soybean protein isolate, 1-3 parts of secalin, 0.5-2 part of vegetable fat powder, 0.2-1.5 parts of Chinese yam extractive, 0.2-1 part of sealwort extractive, 0.2-1 part of mulberry leaf extractive, 0.2-1 part of polygonatum odoratum extractive, 0.1-1 part of medlar extractive, 0.1-0.3 part of flaxseed gum, 0.5-2 parts of L-arabinose, 0.09-0.3 part of yeast and 0.001-0.006 part of zinc gluconate. The conditioning powder is low in carbohydrate content, has abundant nutrients, is particularly suitable for serving as food of the diabetic patent, has the remarkable hypoglycemic effect and the conditioning function, has the prevention and treatment functions on various diabetic complications, and particularly has the good conditioning effect on a diabetes type nephropathy patient. The nutrients of the conditioning powder are easy to digest and absorb. The conditioning powder is convenient to eat and good in taste.

A method of screening for disorders of glucose metabolism such as impaired glucose tolerance and diabetes allows prevention, or early detection and treatment of diabetic complications such as cardiovascular disease, retinopathy, and other disorders of the major organs and systems. A mathematical algorithm evaluates the shape of a subject's glucose profile and classifies the profile into one of several predefined clusters, each cluster corresponding either to a normal condition or one of several abnormal conditions. The series of blood glucose values making up the glucose tolerance curve may be measured using any glucose analyzer including: invasive, minimally invasive and noninvasive types. The method is executed on a processing device programmed to perform the steps of the method. Depending on the outcome of the screening, a subject may be provided with additional information concerning their condition and / or counseled to consult further with their health care provider.

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:wherein one of Q and T represents a group represented by the general formula:while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.