396 results about "Sulfonylurea" patented technology

This invention is directed to a novel method and composition for the treatment of diabetes mellitus (Type I, Impaired Glucose Tolerance ["IGT"]and Type II). More specifically, this invention pertains to a novel method of treating diabetes mellitus by incorporating a therapeutic amount of one or more insulin sensitizers along with one or more of an orally ingested insulin, an injected insulin, a sulfonylurea, a biguanide or an alpha-glucosidase inhibitor for the treatment of diabetes mellitus.

The invention describes formulations that include either metformin, sulfonylurea or a biguanide-sulfonylurea combination as one active ingredient in addition to specific, other active ingredients. The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of the included biguanide (metformin) and / or sulfonylurea in the prevention and treatment of insulin resistance and diabetes mellitus. The carefully chosen additional active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and those adverse incidences associated with the concurrent use of metformin and / or the sulfonylureas. When clinically administered, the invention will provide therapeutic levels of metformin and of a sulfonylurea, alone or in combination, and broaden their usefulness. The invention will retard the progression of insulin resistance to type 2 diabetes, and reduce the serious microvascular and macrovascular complications commonly associated with insulin resistance syndrome and diabetes mellitus.

The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them.In the formula, A is hydrogen atom, a halogen atom, a C1-C4 alkyl or alkoxy group which may be substituted with a halogen atom, or cyano group; B is an optionally substituted aryl group or monocyclic heteroaryl group, or:(wherein, the ring Q is an aromatic ring which may have nitrogen atom; and the ring M is a ring sharing a double bond with the ring Q, which ring may have a heteroatom; and the rings Q and M may share nitrogen atom); K is a single bond; T, W, X and Y are the same as or different from each other and each is =C(D)- (wherein, D is hydrogen or a halogen atom) or nitrogen atom; U and V are the same as or different from each other and each is =C(D)-, nitrogen atom, -CH2-, oxygen atom or -CO-; Z is a single bond or -CO-NH-; and R1 is hydrogen atom, etc.

The invention relates to a herbicide composition, containing sulfonylurea or salt thereof, pyridine and cyhalofop-butyl as active ingredients with the weight ratio of 0.1 to 5: 0.1 to 10: 0.1 to 10. Compared with herbicides with single dose, the weed control effect of the herbicide composition of the invention is obviously improved, thereby reducing the using dosage, reducing the influence degreefor the environment while reducing the pesticide cost, simultaneously enlarging weed control spectrum, and having good control efficiency for Gramineae and broadleaf weeds in rice paddy fields.

The invention relates to a herbicide composition, containing sulfonylurea or salt thereof, pyridine and penoxsulam as active ingredients with the weight ratio of 0.1 to 5: 0.1 to 10: 0.1 to 10. Compared with herbicides with single dose, the weed control effect of the herbicide composition of the invention is obviously improved, thereby reducing the using dosage, reducing the influence degree for the environment while reducing the pesticide cost, simultaneously enlarging weed control spectrum, and having good control efficiency for Gramineae and broadleaf weeds in rice paddy fields.

Disclosed in a controlled release sulfonylurea formulation. In certain embodiments, the invention comprises: (a) a core comprising: (i) a sulfonylurea or a pharmaceutically acceptable salt thereof; (ii) a pharmaceutically acceptable polymer; (b) a membrane surrounding the core which is permeable to the sulfonylurea and gastrointestinal fluid, wherein said dosage form provides a mean time to maximum plasma concentration (Tmax) of said sulfonylurea.

This invention provides a pharmaceutical agent containing, in combination, a sulfonamide compound and other therapeutic agent, preferably, at least one compound represented by the formula (I): R1—SO2—NH—CO-A1-CH2—R2 [each symbol is as defined in the specification] or a pharmaceutically acceptable salt thereof, and at least one pharmaceutical agent selected from the group consisting of an α-glucosidase inhibitor, an insulin secretagogue, a sulfonylurea and a biguanide, which has a superior therapeutic effect.

The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.

A mutant acetolactate synthase (ALS) enzyme that confers cross-resistance to all sulfonylurea, imidazolinone, pyrimidinyloxybenzoate, triazolopyrimidine and sulfonylamino-carbonyl-triazolinone herbicides is provided. The mutant enzyme contains an aspartic acid to glutamic acid substitution mutation at a newly identified conserved region of the ALS enzyme. A gene encoding the enzyme is also provided, as are transgenic plants that have been genetically engineered to contain and express the gene. The transgenic plants are cross-resistant to sulfonylurea, imidazolinone, pyrimidinyloxybenzoate, triazolopyrimidine and sulfonylamino-carbonyl-triazolinone herbicides.

This invention is directed to a novel method and composition for the treatment of diabetes mellitus (Type I, Impaired Glucose Tolerance ["IGT"] and Type II). More specifically, this invention pertains to a novel method of treating diabetes mellitus by incorporating a therapeutic amount of one or more insulin sensitizers along with one or more of an orally ingested insulin, an injected insulin, a sulfonylurea, a biguanide or an alpha-glucosidase inhibitor for the treatment of diabetes mellitus.

The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of biguanides (metformin) and / or sulfonylureas in the prevention and treatment of insulin resistance and diabetes mellitus, alone or in combination, as a nutrient for humans. The carefully chosen active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and with the clinical use of biguanides (metformin) and / or the sulfonylureas. These modules are: (1) Mitochondrial Metabolic Group, (2) Plasma and Mitochondrial Membrane Integrity Group, (3) Nocturnal Group and, (4) Insulin Alternative Group. When used in concert with a biguanide, a sulfonylurea or with a combination of both, the invention will broaden the clinical usefulness of these drugs. The invention will retard the progression of insulin resistance to type 2 diabetes, and reduce the serious microvascular and macrovascular complications commonly associated with insulin resistance syndrome and diabetes mellitus.

Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and / or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

The invention discloses a haloxyfop-r-methyl-containing herbicide composition. The haloxyfop-r-methyl-containing herbicide composition is utilized for controlling gramineous weeds, broad-leaved weeds and sedge weeds in broad-leaved crop fields. The haloxyfop-r-methyl-containing herbicide composition comprises active components of 1, a compound A, wherein the compound A is haloxyfop-r-methyl, and 2, a herbicide mixed synergistic active component B, wherein the herbicide mixed synergistic active component B is one or more of diphenyl ether herbicides, sulfonylurea herbicides or benzothiazine dione herbicides. A weight ratio of haloxyfop-r-methyl to the herbicide mixed synergistic active component B is (1 to 30%): (0.5 to 50%). The haloxyfop-r-methyl-containing herbicide composition can be processed into all realizable dosage forms. The haloxyfop-r-methyl-containing herbicide composition can be widely utilized for controlling gramineous weeds such as barnyard grass, green bristlegrass, alopecurus aequalis, crabgrass, annual bluegrass and moleplant seed, broad-leaved weeds such as purslane, solanum nigrum, cocklebur, bindweed, chenopodium album and goosegrass herb, and sedge weeds in soybean and peanut fields, wherein the broad-leaved weeds are difficult to be controlled. The haloxyfop-r-methyl-containing herbicide composition has the characteristics of wide weed control spectrum, safety on crops, and high efficiency.

Provided, among other things, is a formulation or kit comprising: (a) a pharmaceutically effective dosage of one or more a glucose-level-controlling bioactive agents selected from an α-glucodase inhibitor, sulfonylurea, meglitinide, thiazolidinediones, biguanide, insulin, dual PPARα / γ agonist, PPARγ agonist or insulin secretagogue; and (b) a pharmaceutically effective dosage of (i) one or more of an antihypertensive bioactive agent selected from an ACE inhibitor, calcium channel blocker, beta blocker, angiotension II receptor antagonist or diuretic, or (ii) one or more of an anti-dyslipidemia bioactive agent selected from a HMG-CoA reductase inhibitor, bile acid sequestrant, fibric acid derivative, sterol, cholesterol absorption inhibitor, MTP inhibitor or nicotinic acid derivative; wherein: in the case of (i) a combination of a first bioactive agent of group (a) that is metformin with a second bioactive agent of group (b), or (ii) a combination of a first bioactive agent of group (a) that is a thiazolidinedione or dual PPARα / γ agonist with an angiotension II receptor antagonist, one or more of the following applies: (I) one of the first bioactive agent or the second bioactive agent is formulated for sustained release, and the other is formulated for immediate release, each formulated for once-a-day dosing; or (II) the co-formulation or kit comprises (A) a biguanide and a thiazolidinedione and (B) one or more group (b) bioactive agents.

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 selected from one or more of betaines, lipidic betaines, betaine lipids and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, .alpha.-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.

The invention provides a metformin hydrochloride / voglibose sugar-lowering oral preparation composition and a preparation method thereof. The weight ratio of two main medicines is 8000:1-375:1, preferably 2500:1-625:1. Except for the main medicines, the composition also can further contain commonly used medicine accessories, such as a binder, a filling agent, a disintegrating agent, a lubricant, a flavoring agent, a wetting agent and a flow agent, and the obtained composition can be prepared into tablets, granules, soft and hard capsules, sustained and controlled release preparations, optimum enteric-coated tablets, enteric-coated granules and enteric-coated soft and hard capsules by conventional methods. The composition provided by the invention has action mechanism complementation of the main medicines, multiple target points, good compliance of patients, and the like. The sugar-lowering oral preparation composition can be used for the first-line therapy of type 2 diabetes, or can be used for second-line therapy under the condition that the metformin hydrochloride or sulfonylurea medicines fail to singly and effectively control blood sugar; and the sugar-lowering oral preparation composition is especially suitable for the therapy of diabetic patients suffering from latent autoimmune diabetes in adults (LADA) and hyperinsulinemia.

The invention relates, in part, to pharmaceutical compositions that comprise a combination of pantethine, or a derivative thereof, and a second active agent. Examples of second active agents include, but are not limited to, statins, fibrates, glitazones, biguanides, sulfonylureas, dyslipidemic controlling compounds, small peptides of the invention, and combinations thereof. The invention also relates to methods for treating, preventing, or managing cholesterol, dyslipidemia, and related disorders.

The invention discloses a herbicide composed by mixing glyphosate, aryloxy-phenoxy-propionic acid herbicidal substances and sulfonylurea herbicidal substances, the weight content being 65-90% of glyphosate, 3-15% of aryloxy-phenoxy-propionic acid herbicidal substances and 5-20% of sulfonylurea herbicidal substances. The herbicide of the invention has perfect eradication effect to various worst weeds, is particularly suitable for controlling the two worst weeds such as Leersia oryzoides and triquetrousc murdannia herb, and is widely used for rice field, ridge, abandoned fields, mulberry garden and tree parks.

The invention relates to a herbicide composition, containing sulfonylurea or salt thereof, pyridine and acetochlor as active ingredients with the weight ratio of 0.1 to 5: 0.1 to 10: 0.1 to 10. Compared with herbicides with single dose, the weed control effect of the herbicide composition of the invention is obviously improved, thereby reducing the using dosage, reducing the influence degree for the environment while reducing the pesticide cost, simultaneously enlarging weed control spectrum, and having good control efficiency for Gramineae and broadleaf weeds in rice paddy fields.

Methods of treating diseases such as diabetes are disclosed. Methods of modulating elevated fructosamine levels, elevated HbA1c levels, impaired glucose tolerance, and impaired fasting glucose are also disclosed. In some embodiments, methods include co-administration of a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide, a sulfonylurea and insulin, or pharmaceutically acceptable salts thereof. Drug products including a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide, a sulfonylurea and insulin, or pharmaceutically acceptable salts thereof, in combination are also disclosed.

A composite herbicide for corn field contains phenyloxyacetic acid kind of herbicide chosen from 2,4-D sodium, MCPA, MCPA sodium, 2,4-D butylate, etc, and sulfonylurea kind of herbicide chosen from nicosulfuron, rimsulfuron, etc in weight ratio of (1-80):1. The preparation is wattable powder and soluble powder.

The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, A is hydrogen atom, a halogen atom, a C1-C4 alkyl or alkoxy group which may be substituted with a halogen atom, or cyano group; B is an optionally substituted aryl group or monocyclic heteroaryl group, or: (wherein, the ring Q is an aromatic ring which may have nitrogen atom; and the ring M is a ring sharing a double bond with the ring Q, which ring may have a heteroatom; and the rings Q and M may share nitrogen atom); K is a single bond; T, W, X and Y are the same as or different from each other and each is =C(D)- (wherein, D is hydrogen or a halogen atom) or nitrogen atom; U and V are the same as or different from each other and each is =C(D)-, nitrogen atom, -CH2-, oxygen atom or -CO-; Z is a single bond or -CO-NH-; and R1 is hydrogen atom, etc.

The present invention relates to herbicidally active compositions, which comprise 3-[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)pyrazol-4-ylmethylsulfonyl]-4,5-dihydro-5,5-dimethyl-1,2-oxazole [common name pyroxasulfone] and at least one herbicide B which is selected from the groups ofb.1 imidazolinone herbicides;b.2 sulfonylurea herbicides;b.3 triazolopyrimidine herbicides;b.4 pyrimidinylbenzoate herbicides; andb.5 sulfonylaminocarbonyltriazolinone herbicides.The invention furthermore relates to the use of a composition as defined herein for controlling undesirable vegetation in crops.

The invention relates to a solid preparation of a novel sterilant herbicide composition employing saflufenacil and glyphosate and containing a herbicide auxiliary agent. The solid preparation comprises the two effective compositions saflufenacil and glyphosate, the auxiliary agent and a carrier. The two effective compositions saflufenacil and glyphosate account for 10%-70% by weight of the composition, and the weight ratio of saflufenacil to glyphosate is 1:5-1:40. The solid preparation of the herbicide composition containing saflufenacil and glyphosate employs a particulate agent, a wettable powder and a water-dispersable granule as a product form. The herbicide auxiliary agent is a combination of at least two or more of a plant-resource spray auxiliary agent, a plant-source SD auxiliary agent, an alkyl glycoside surfactant, a trisiloxane surfactant, a tallow amine surfactant, betain, amino oligosaccharin and a penetrating agent JFC. The herbicide composition containing the herbicide auxiliary agent has excellent control efficacy on common gramineae and broad leaf weeds, and especially on weeds generating drug resistance on herbicides such as glyphosate, sulfonylureas, triazines and the like.

The present invention relates to the field of pesticide herbicides, and discloses a herbicide composition and a herbicide containing the herbicide composition, the herbicide composition comprises a component A and a component B, the component A is a triketone compound shown as formula (I), and the component B is at least one selected from the group consisting of triazine herbicides, hydroxybenzonitrile herbicides, triazolinone herbicides, diphenyl ether herbicides, pyridinecarboxylic acid herbicides, phenoxycarboxylic acid herbicides, benzoic acid herbicides, pyridine herbicides, chloroacetamide herbicides, sulfonylurea herbicides, triazolopyrimidine herbicides, bentazone, mesotrione and topramezone. The herbicide composition can broaden the herbicidal spectrum and can improve the controleffect and retard the occurrence of weed drug resistance and anti-drug property.

The invention relates to a preparation method of 6-substituted-2-trifluoromethylbenzenesulfonyl chloride as a key intermediate of sulfonamide or sulfonylurea herbicides. The method comprises the following steps: 6-fluoro-2-trifluoromethylbenzenethioether is formed through fluorine displacement and sulfenyl group substitution of a raw material 2,3-dichlorobenzotrifluoride, chlorine oxidative chloridization or substitution of 6-fluoro-2-trifluoromethylbenzenethioether is carried out, and then chlorine oxidative chloridization of the finally obtained material is carried out to obtain the above product. The method has the advantages of easily available raw materials, simple process, high yield and low cost.

Compositions and methods for conferring herbicide resistance or tolerance to plants, plant cells, tissues and seeds are provided. Compositions include transgenic plants, plant cells, tissues, and seeds that have been transformed with a nucleic acid molecule encoding a cytochrome P450 or variant thereof that confers herbicide resistance or tolerance, alone or in combination with one or more additional nucleic acid molecules encoding polypeptides that confer desirable traits. In particular, the cytochrome P450 or variant thereof confers resistance or tolerance to HPPD inhibitors, benzothiadiazinones, sulfonylureas, and other classes of herbicides. The additional polypeptide may also confer resistance or tolerance to an herbicide, including HPPD inhibitors and other herbicides. Methods are also provided for the production and use of the herbicide resistant or tolerant plants, plant cells, tissues and seeds of the invention.

The invention provides an acquisition method for transgenic gramineous crops capable of being selectively perished, comprising the following steps: when target genes are expressed, expression of genes participating in herbicide detoxification in the transgenic gramineous crops is inhibited by utilization of antisense RNA or RNAi means, and the transgenic gramineous crops capable of being selectively perished are obtained. The invention mainly has the advantages that: the transgenic gramineous crops acquired by utilization of the method can be selectively perished by Bentazon or sulphuryl carbamide herbicide as required, thereby transmission of the transgenic gramineous crops and interfusion to non-transgenic gramineous crops are prevented, and the method has great significance in transgenic crop research later on.