Abstract: Methods for increasing urine flow are disclosed, comprising administration of an effective amount of GLP-1, an exendin, or an exendin or GLP-1 agonist. Methods for increasing urinary sodium excretion and decreasing urinary potassium concentration are also disclosed. The methods are useful for treating conditions or disorders associated with toxic hypervolemia,such as renal failure, congestive heart failure, nephrotic syndrome, cirrhosis, pulmonary edema, and hypertension. The present invention also relates to methods for inducing an inotropic response comprising administration of an effective amount of GLP-1, an exendin, or an exendin or GLP-1 agonist. These methods are useful for treating conditions or disorders that can be alleviated by an increase in cardiac contractility such as congestive heart failure. Pharmaceutical compositions for use in the methods of the invention are also disclosed.

Abstract: The invention relates to treatment of patients in need of increasing insulin sensitivity by administration of growth hormone or analogues thereof, preferably human growth hormone, in a low dose and the use of growth hormone or analogues thereof, preferably human growth hormone, for the manufacturing of a medicament useful for increasing insulin sensitivity in low dose therapy. The patient is preferably a normal subject, i.e. not growth hormone deficient patient and/or a non-obese patients. By low dose therapy is preferably meant less than 0.008 mg/kg/day, preferably 0.007 mg/kg/day or less, more preferably 0.005 mg/kg/day or less and most preferably 0.003 mg/kg/day or less. The therapy is preferably performed during short term treatment, preferably less than one month.

Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.

Abstract: The invention relates to insulin analogs exhibiting enhanced zinc binding capacity and to stable zinc complexes thereof having a retarded activity in comparison with human insulin. The invention further relates to a method for the production of said insulin analogs and to their use, particularly in pharmaceutical preparations for therapy of type I and type II diabetes mellitus.

Abstract: Systemic delivery of insulin to a mammalian host is accomplished by inhalation of a dry powder of insulin. It has been found that dry insulin powders are rapidly absorbed through the alveolar regions of the lungs.

Abstract: Use of vardenafil or a pharmaceutical composition thereof in the preparation of a medicament for the curative, palliative or prophylactic treatment of type 2 diabetes mellitus.

Abstract: The invention relates to a method of preparing a xenotransplantable porcine islet preparation capable upon xenotransplantation of producing porcine insulin in an appropriate recipient mammal, the method including or comprising: (i) harvesting the pancreas of piglets at or near full term gestation, and (ii) extracting islets from a culture of the harvested pancreas using a suitable collagenase, (iii) the culture of the harvested pancreas being a) of mechanically reduced harvested pancreas, and b) a supportive mammalian albumin substantially free of non-human microbiological agents,wherein (at least some stage in the method) the islets are associated with Sertoli cells.

Abstract: The invention relates to a method for screening therapeutic agents, defined as SCAP antagonists, for use in combating diseases associated with elevated lipid levels, said method comprising detecting or assaying the extent or result of transcriptional activity or binding between a control SCAP antagonist and SCAP, in the presence of and absence of said agent. Also claimed are therapeuic agents which are antagonists of SCAP, identified by such a method and their use in combating diseases associated with elevated lipid levels.

Abstract: The present invention relates to the use of native hepoxilins and of hepoxilin analogs for the regulation of insulin secretion and to the use of hepoxilin analogs as anti-inflammatory, anti-diabetic and anti-thrombotic compounds.

Abstract: This invention relates to compositions and methods comprising “lymphotoxin-&bgr; receptor blocking agents”, which block lymphotoxin-&bgr; receptor signalling. Lymphotoxin-&bgr; receptor blocking agents are useful for treating lymphocyte-mediated immunological diseases, and more particularly, for inhibiting Th1 cell-mediated immune responses. This invention relates to soluble forms of the lymphotoxin-&bgr; receptor extracellular domain that act as lymphotoxin-&bgr; receptor blocking agents. This invention also relates to the use of antibodies directed against either the lymphotoxin-&bgr; receptor or its ligand, surface lymphotoxin, that act as lymphotoxin-&bgr; receptor blocking agents. A novel screening method for selecting soluble receptors, antibodies and other agents that block LT-&bgr; receptor signalling is provided.

Abstract: This invention relates to therapeutic agents for diabetes comprising a 2-(N-cyanoimino)thiazolidine-4-one derivatives represented by formula I or a solvate or a pharmaceutically acceptable salt thereof as an active ingredient: wherein ring A represents a benzene ring, a condensed ring, or a heterocyclic ring, each of which may be substituted by one or more substituents selected from a straight or branched C1-C4 alkyl group, a haloalkyl group, a halogen atom or —OR5, R1 represents a single bond, an oxygen atom, a sulfur atom, a methyne group, a straight or branched C1-C4 alkylene or alkenylene group optionally substituted by a phenyl group, R6—X, X—R6, X—R6—X, R6—X—R6, —C(═O)—NR7— or —NR7—C(═O)—, R2 and R3 are the same or different and each represents a hydrogen atom, a C1-C4 alkyl group, —OR8 or a halogen atom, R4 represents a hydrogen atom or a C1-C4 alkyl group, R5 represents a hydrogen atom o

Abstract: A composition for use by animals, including humans, to alleviate pain and/or inflammation around a painful joint, joint replacement surgery site, muscle, tendon, and/or ligament. A method to ameliorate pain and/or inflammation in or around a joint, muscle, tendon, and/or ligament, by topically applying Applicant's composition.

Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.

Abstract: A method for treating postprandial hyperglycemia in diabetes mellitus in a human which employs a combination of an aerosolizable topical insulin and a short-acting oral hypoglycemic agent as a regimen taken adjacent to mealtime.

Abstract: The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, &agr;-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.

Abstract: This invention relates to medicinal aerosol and more formulation and more particularly, to a medicinal aerosol formulation containing rosiglitazone maleate and a fluid carrier.

Abstract: The present invention provides the use of (−)(3-trihalomethylphenoxy)(4-halophenyl)acetic acid derivatives and compositions in the treatment of insulin resistance, Type 2 diabetes and hyperlipidemia.

Abstract: A tablet composition containing N-(trans-4-isopropylcyclohexanecarbonyl)-D-phenylalanine and low substituted hydroxypropylcellulose is disclosed. This tablet composition is rapidly disintegrated in the stomach after the administration and absorbed without being influenced by meals to inhibit the rise of the blood sugar levels of diabetics after meals.

Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.

Abstract: Processes for conveniently and economically producing L-arabinose, enzyme-treated products containing L-arabinose, diet foods and diabetic foods containing L-arabinose with dietary fiber, and fruit or vegetable juices containing L-arabinose are provided. (1) A process for producing L-arabinose by treating a natural material containing arabinan, arabinoxylan or arabinogalactan with an enzyme having an activity of acting on natural substances containing arabinan, arabinoxylan or arabinogalactan and thus releasing L-arabinose to give L-arabinose, characterized in that the above-described natural substance is directly treated with the above-described enzyme without separating or extracting arabinan, arabinoxylan or arabinogalactan.

Abstract: 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.

Abstract: The present invention provides the use of (−) (3-trihalomethylphenoxy) (4-halophenyl) acetic acid derivatives and compositions in the treatment of insulin resistance, Type 2 diabetes, hyperlipidemia and hyperuricemia. It further provides (−) (3-trihalomethylphenoxy) (4-halophenyl) acetic acid derivatives that are useful for the treatment of insulin resistance, Type 2 diabetes, hyperlipidemia and hyperuricemia.

Abstract: Methods and compositions are provided for modulating blood insulin levels of animals by targeting the gene and gene products of cathepsins, particularly cathepsins L, K, and S, and especially cathepsin L. The method comprises: administering to the animal an agent that reduces an in vivo level of cathepsin L activity such that the blood insulin level of the animal is reduced. The method can be used to treat hyperinsulinmia and related diseases such as insulin resistance, type II diabetes, and hyperglycermia.

Abstract: The present invention relates to insulin derivatives in which a lipophilic group having from 12 to 40 carbon atoms is attached to the &agr;-amino group of the N-terminal amino acid in the B-chain or to the carboxy group of the C-terminal amino acid in the B-chain have a protracted profile of action.

Abstract: In a powder formulation for use in a dry powder inhaler, a pharmaceutical acts as its own carrier, so that use of lactose or other excipients are not needed. The dry powder formulation has a single active pharmaceutical compound having two major populations in particle size distribution: microfine particles of the active pharmaceutical, of 1-10 microns in diameter, and larger carrier particles, also of the active pharmaceutical compound. The carrier particles provide a long acting, delayed onset, and optionally therapeutic effect via the GI tract, while the microfine particles provide a fast onset effect via the lung.

Abstract: A novel glucopyranoside, 2,6-dihydroxy-2-(P-hydroxybenzyl)-3(2H) benzofuran-7-C-&bgr;-D-glucopyranoside of the formula 1 isolated from Pterocarpus marsupium and to a process for the isolation thereof is disclosed. The invention also relates to a pharmaceutical composition containing 2,6-dihydroxy-2-(P-hydroxybenzyl)-3(2H)benzofuran-7-C-&bgr;-D-glucopyranoside and to method for the treatment of diabetes using said compound.

Abstract: A device for cell implantation has a housing containing a matrix which isolates the cells in the housing; the housing has a window which comprises a membrane which permits passage of nutrients for the cells into the matrix from a location externally of the housing; the housing has an injection port permitting injection of cells into the matrix in the housing. The device may be employed, for example, to facilitate islet implantation in the treatment of diabetes mellitus.

Abstract: The present invention is directed to the use of certain pyrido[1,2-a]-pyrazine derivatives, also described as bis-azabicyclic compounds and defined by the formula (I) herein, in the treatment of Parkinson's disease, attention deficit hyperactivity disorder and microadenomas in mammals, and to related compositions.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.

Abstract: It has been newly found out that ascochlorin, which is a publicly known fat-soluble antibiotic, and its homologues serve as a ligand of retinoid X receptor and react in vivo with the amino group of serum protein to form Schiff bases without showing any side effect of retinoid. Ascochlorin and its homologues are usable in treating and/or preventing a disease or condition which can be relieved by the retinoid X receptor ligand-dependent gene transcriptional regulation (for example, diseases caused by the expression of insulin resistance, hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune disease, Ca metabolic disorder, complication of diabetes, arteriosclerosis, etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet &bgr;-cells and, therefore, are usable in making these cells to sustain the insulin productivity.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:

Abstract: The present invention provides a novel dithiocarbamamte disulfide dimer useful in various therapeutic treatments, either alone or in combination with other active agents. In one method, the disulfide derivative of a dithiocarbamate is coadministered with an agent that inactivates (or inhibits the production of) species that induce the expression of nitric oxide synthase to reduce the production of such species, while, at the same time reducing nitric oxide levels in the subject. In another embodiment, free iron ion levels are reduced in a subject by administration of a disulfide derivative of a dithiocarbamate(s) to scavenge free iron ions, for example, in subjects undergoing anthracycline chemotherapy. In another embodiment, cyanide levels are reduced in a subject by administration of a disulfide derivative of a dithiocarbamate so as to bind cyanide in the subject. In a further aspect, the present invention relates to compositions and formulations useful in such therapeutic methods.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.

Abstract: A method of treating in a human or animal a condition capable of treatment by oral or nasal inhalation has been found. The method comprises administering a medicinal aerosol formulation comprising a selected medicament under conditions where the amount of the selected drug delivered to the site of action, e.g. the lungs, is maximized.

Abstract: The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

Abstract: The invention is directed to an improved infant formula containing a lipid blend that softens the firmer stools associated with typical infant formula. A specific formula in accordance with the invention comprises carbohydrates, proteins, vitamins and minerals and a lipid mixture of high oleic safflower oil, soy oil and coconut oil at specific levels and ratios. The invention also discloses novel mixtures of fatty acids that provides infant stool patterns more closely resembling the breast-fed infant.

Abstract: The use of at least one &ggr;-RAR receptor-specific agonist ligand to prepare a pharmaceutical composition for increasing the rate of apoptosis in at least one cell population in which apoptosis may be induced by activating &ggr;-RAR receptors is disclosed. The composition is particularly useful for treating a disease or disorder related to an insufficient rate of apoptosis in at least one cell population in which apoptosis may be induced by activating &ggr;-RAR receptors. The use of at least one &ggr;-RAR receptor-specific agonist ligand as the apoptosis inducer in a cosmetic composition is also disclosed. Said composition may be used to prevent and/or control photo-ageing or chronological ageing of the skin.

Abstract: Advanced glycation endproducts (AGEs) have been implicated in the pathogenesis of a variety of debilitating diseases such as diabetes, atherosclerosis, Alzheimer's and rheumatoid arthritis, as well as in the normal aging process. Five compounds are here reported to be active in breaking AGE-protein cross-links. These compounds are L-bis-[4-(4-chlorobenzamido-phenoxyisobutyryl)cystine] (LR20); 4-(3,5-dichlorophenylureido)phenoxyisobutyryl-1-amido-cyclohexane-1-carboxylic acid (LR23); methylene bis [4,4′-(2-chlorophenylureido-phenoxyisobutyric acid)] (LR90); 5-arninosalicylic acid (5-ASA); and metformin. These compounds may be used to reverse the debilitating effects of those diseases in which AGEs are formed.

Abstract: A medicinal formulation is disclosed. The formulation comprises (a) a protein or peptide medicament; (b) a fluid carrier for containing said medicament; and a stabilizer selected from an amino acid, a derivative thereof or a mixture of the foregoing.

Abstract: A low dose antidiabetic pharmaceutical formulation is provided, especially adapted for treating Type II diabetes in drug naive patients, which includes a combination of metformin (employed in a reduced amount (less than 800 mg metformin per day) compared to that employed in generally accepted medical practice) and at least one other antidiabetic agent such as a sulfonyl urea, for example, glyburide, which combination provides at least about substantially equivalent efficacy in treating diabetes in drug naive patients, as do antidiabetic formulations containing metformin employed in dosages prescribed in generally accepted medical practice for first line therapy in treating diabetes, but with substantially reduced side effects, such as hypoglycemia and/or gastrointestinal distress.

Abstract: This invention relates the use of glucagon-like peptides such as GLP-1, a GLP-1 analog, or a GLP-1 derivative in methods and compositions for reducing body weight.

Abstract: The invention relates to the herbal composition which consists of: Centaurii umbellatum, Gentianaceae (centaury plant), Teraxacum officinale, Asteraceae (dandelion root), Juniperi communis L, Cupresaceae (juniper berry), Urticae dioica L, Urticeae (nettle plant), Urticae dioica L, Urticaceae (nettle root), Cichorium intybus L, Cichoriaceae (chicory root), Morus nigra L, Moraceae, (mulberry leaf), Achilleae millefolium L, Asteraceae (yarrow flower), Vaccinium myrtillus L, Ericaceae (bilberry leaf), Phaseolus vulgaris L, Fabaceae (bean pods), Valeriana officinalis L, Valerlanaceae (Valerian root).

Abstract: This invention relates to a medicinal aerosol formulation and more particularly, to a medicinal aerosol formulation containing a troglitazone medicament and a fluid carrier.

Abstract: A novel glucopyranoside, 6-hydroxy-2-p-hydroxybenzylbenzofuran-7-C-&bgr;-D-glucopyranoside of the formula 1 isolated from Pterocarpus marsupium and to a process for the isolation thereof is disclosed. The invention also relates to a pharmaceutical composition containing 6-hydroxy-2-p-hydroxybenzylbenzofuran-7-C-&bgr;-D-glucopyranoside and to method for the treatment of diabetes using said compound.

Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (I) or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; to a composition, respectively, which comprises nateglinide and a pharmaceutically acceptable carrier and to a process of making such composition; the use of such combination or composition for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; the use of such combination or composition for

Abstract: Methods and compositions for treating diabetes mellitus in a patient in need thereof are provided. The methods include administering to a patient a composition providing a gastrin/CCK receptor ligand, e.g., a gastrin, and/or an epidermal growth factor (EGF) receptor ligand, e.g., TGF-&agr;, in an amount sufficient to effect differentiation of pancreatic islet precursor cells to mature insulin-secreting cells. The composition can be administered systemically or expressed in situ by cells transgenically supplemented with one or both of a gastrin/CCK receptor ligand gene, e.g., a preprogastrin peptide precursor gene and an EGF receptor ligand gene, e.g., a TGF-&agr; gene. The methods also include transplanting into a patient cultured pancreatic islets in which mature insulin-secreting beta cells are proliferated by exposure to a gastrin/CCK receptor ligand and an EGF receptor ligand.

Abstract: A composition is disclosed that comprises a mixture of polypeptides of opposite charge and an excipient selected from the group consisting of arginine, lysine, glutamic acid, sodium dodecyl sulfate, beta-hydroxy cyclodextrin, and beta-cyclodextrin sulfobutyl ether.

Abstract: A method for reducing mammalian serum total cholesterol, LDL cholesterol, apolipoprotein B and triglyceride levels, by ingesting a stabilized rice bran derivative selected from the group consisting of an enzyme treated stabilized rice bran, an insolubilized fraction and mixtures thereof, thereby reducing serum total cholesterol, LDL cholesterol, apolipoprotein B and triglyceride levels in said mammal.

Abstract: The present invention provides a monomeric insulin analog formulation stabilized against aggregation in which the buffering agent is either TRIS or arginine. The stable formulations of the present invention are useful for treating diabetes, and are particularly advantageous in treatment regimes requiring lengthy chemical and physical stability, such as, in continuous infusion systems.