674 results about "Hyperlipemias" patented technology

Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

The present invention relates to compounds of the general formula I B--(CH--R.sup.1).sub.n--C(.dbd.X.sup.2)--D (I) and pharmaceutically acceptable salts thereof including stereoisomers, to the use of the compounds for the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidosis, diabetes mellitus, diabetic neuropathy and nephropathy and of sequelae caused by diabetes mellitus in mammals.

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.

A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

A compound of the formula wherein R1 is: R5 is: and n, m, Z, R8, R9, R10 and R11 are as defined herein, useful in the treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia, particularly, myocardial ischemia.

The present invention relates to the development of a targeted delivery system for the oral delivery of probiotics or therapeutic agent for various indications, including and not limited to active and prophylaxis treatment of Clostridium difficile infection, antibiotic associated diarrhea, irritable bowel syndrome, Crohn's disease, intestinal flora replacement, supplemental flora treatments for patients taking antibiotics, and for restoration of balance and signaling between the intestinal microbiome and the intestinal cells in patients under treatment of metabolic syndrome manifestations, specifically diabetes, insulin resistance, obesity, hyperlipidemia and hypertension.

Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

The present invention relates to a method of making novel dipeptidyl peptidase-IV ("DPP-IV') inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.

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.

Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and EG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.

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.

A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and / or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and / or gamma mediated diseases, disorders and conditions.

The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and / or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and / or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and / or nitrogen via a bond or moiety that cannot be hydrolyzed.

A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and / or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and / or gamma mediated diseases, disorders and conditions.

Methods of treating a host suffering from hyperlipidemia resulting from elevated levels of at least one of VLDL and triglycerides are provided. In the subject methods, an effective amount of agent that reduces the level of active apoE, e.g. apoE inhibitor or apoE expression inhibitor, is administered to the host. The subject methods find particular use in the treatment of hosts suffering from Type IV or Type IIb hyperlipidemia. Also provided are non-human transgenic animal models for hyperlipidemia, as well as methods for making and using the subject animal models, e.g. in therapeutic agent screening applications.

Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.

Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.

The present invention includes peptidomimetic compound compositions and methods of making and using peptidomimetic compounds to modulate the activity of a peptide receptor for the treatment of one or more of hyperglycemia, insulin resistance, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoproteinemia or other symptoms that relate to the function of the targeted receptor. The peptidomimetic includes an oligo-benzamide compound having at least three optionally substituted benzamides.

The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and / or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.

A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.

The present invention is directed to a compound of formula I, or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Thioketals and thioethers are provided that inhibit the expression of VCAM-1, and which can be used in the treatment of VCAM-1 mediated diseases including inflammatory disorders, cardiovascular diseases, occular diseases, autoimmune diseases, neurological disorders, and cancer. The compounds also can be used to treat hyperlipidemia and / or hypercholesterolemia.

The invention relates to flour suitable for obese patients. The special meal flour for preparing foods for obese patients is prepared in the by uniformly mixing power made of rhizoma polygonati, semencassiae, gingko, raw hawthorn, tuckahoe, white lablab bean, Chinese yam and semen coicis with whole wheat (with a husk), oat, azuki bean and black bean. The flour can be used for producing various foods suitable for obese patients to eat as a principle food. The flour has the obvious effects of systemically adjusting lipid metabolism and glucose metabolism, losing weight, lowering blood fat, improving microcirculation and eliminating radicals. The special meal flour is suitable for patients with adiposity, adiposis hepatica, hyperlipemia, high blood viscosity, hypertension and diabetes mellitus, and for middle-aged and old people to keep healthy and eat.

Described are a number of compositions, namely a konjac mannan mixture, a ginseng composition, and a composition comprising konjac mannan and American ginseng. Methods of use of these compositions are described including their use for reducing blood glucose in non-diabetic and diabetic individuals, as well as reducing postprandial blood glucose in such individuals. Applications in the treatment of hyperlipidemia, high blood pressure, an increase in nitric oxide, Syndrome X and cardiovascular disease are also described. Various other applications of the compositions and methods are also described.

The present invention relate to the use of a combination of an inhibitor of miR-122 and an inhibitor of VLDL assembly, for the treatment of HCV, hyperlipidemia and hypercholesterolemia.

A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1″) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

The invention provides pharmaceutical compositions, methods for the treatment of, and related diagnostics and computer-implementable systems that relate to, the treatment of a variety of metabolic syndromes, including hyperlipidemia, weight gain, obesity, insulin resistance, hypertension, atherosclerosis, fatty liver diseases and certain chronic inflammatory states. In an additional aspect of the invention, compositions and methods of treatment are calibrated to the ileal brake response to surgical intervention e.g. Roux-en-Y gastric bypass (RYGB)) as both activate the ileal brake, which acts in the gastrointestinal tract and the liver of a mammal to control metabolic syndrome manifestations and thereby reverse or ameliorate the cardiovascular damage (atherosclerosis, hypertension, lipid accumulation, and the like) resulting from progression of metabolic syndrome. The net benefit is the potential to treat all of the common manifestations of metabolic syndrome, including Type 2 diabetes and obesity, with one medicament, which contains glucose as an activation agent for the ileal brake. The ileal brake is the controller for progression of metabolic syndrome, and both RYGB surgery and the oral formulation act beneficially on the metabolic syndrome manifestations via this pathway. Disclosed as well are combination medicaments that act synergistically on the ileal brake and the manifestations of metabolic syndrome.In other aspects, the invention provides ileal brake hormone releasing compositions, methods of treatment, diagnostics, and related systems useful in selective control of appetite, stabilizing blood glucose and insulin levels, and treating gastrointestinal disorders in a similar manner to RYGB surgery, but having at least 20% of the potency to stimulate the hormonal response of the ileal brake of humans.

Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and / or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive impairment, decreased libido, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

The invention provides an oligosaccharide oat beverage capable of treating hyperlipoidemia and hyperglycemia and improving gastrointestinal tract function and a manufacturing method thereof by hydrolysis of three enzymes and fine grinding. The manufacturing method comprises the following steps: carrying out fine grinding on the oat meal to obtain the powder of which the average particle size is less than about 100 mu m, dissolving the oat powder in water to form oat slurry, and adding alpha-amylase, beta-amylase and trans-glucosidase to carry out enzyme treatment, thereby obtaining the oat beverage with rich functional components. The oligosaccharide oat beverage integrally reserves oat beta-dextran, and also contains oligo-isomaltose component of which the content is higher than that in common oat products. The manufacturing method can integrally reserve the nutritional components of the whole oat grains and omit the filter operation, thereby being beneficial to increasing the utilization ratio of raw materials; and the method is completed under the conditions of fermentation and sterilization in the optimal short time, thereby avoiding the possibility of rancidity of oat slurry in the processing procedure. When the oligosaccharide oat beverage is used for human testing for assessing physiologic effect, the test proves that the oligosaccharide oat beverage can lower the total cholesterol, low-density lipoprotein cholesterol, triglyceride and fasting blood-glucose value in blood. The oligosaccharide oat beverage tastes savoury, thick and smooth like milk, and maintains the natural flavor of oat; and thus, the invention changes the traditional way for eating oat, greatly raises the nutrition health-care value of oat processed products, and has the potentials of preventing and treating hyperlipoidemia, hyperglycemia and other life-style related diseases and improving the gastrointestinal tract function.