689results about How to "Long duration of action" patented technology

The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

This invention provides compounds of formula I:wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formulaThese compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Disclosed herein is an injectable long-acting analgesic composition comprising: (a) a ketorolac ester derivative of formula (I),  wherein  R is a straight-chain or branched saturated or unsaturated C1-C20 aliphatic group optionally substituted with a C6-C10 aryl group; and (b) a pharmaceutically acceptable oil vehicle. The composition can provide a longer duration of action and, therefore, is suitable for use in the treatment of long-lasting pains and inflammations.

The invention discloses an environmental-protective composite inhibiting antisludging agent, which comprises the following parts: inhibiting component, antisludging component and deionized water, wherein the inhibiting component is composed of one or more materials in the molybdate, tungstate, borate, organic substituted carboxylic acid or organic heterocyclic compound; the inhibiting component contains one or more materials in the natural macromolecular compound, epoxy succinic acid or acroleic acid ternary copolymer.

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.

A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9alpha,11alpha-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HCl (Benzenacetonitrile, (±)-alpha[3[[2-(3,4-dimethoxyphenyl) ethyl]methylamino]propyl]-3,4-dimethoxy-alpha-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.

Disclosed herein are novel buprenorphine monocarboxylic ester derivatives and dibuprenorphine dicarboxylic ester derivatives which exert a longer analgesic effect as compared to buprenorphine hydrochloride. Also disclosed are the processes for synthesizing the novel ester derivatives of buprenorphine, and long-acting analgesic pharmaceutical compositions containing a compound selected from buprenorphine base and the novel ester derivatives of buprenorphine.

This invention provides compounds of formula I:wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Pharmaceutical compositions for oral-transmucosally administering methadone. For oral transmucosal delivery, the compositions comprise an oral dissolution agent and methadone in a dosage formulation. The dissolution agent generally causes the formulation to break down or dissolve in the oral cavity. The formulation is buffered to a pH of at least 6 for substantial absorption of the methadone through the oral mucosal tissue from the dissolved dosage form.

The present invention relates to the S-isomers of anesthetic compounds, the methods of treatment therewith, the compounds being useful for inducing local anesthesia, analgesia and sleep.

The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I)or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and / or energy balance and body weight related diseases, disorders and / or conditions, including obesity, overweight and diseases, disorders and / or conditions associated with obesity and / or overweight, such as type 2 diabetes and metabolic syndrome.

A method for fermentation of lactic acid from a sugar-containing fermentation liquid in a fermentor by means of lactic acid-forming bacteria, in which whey protein is present or is added as a nutrient substrate for the lactic acid-forming bacteria, wherein at least one protease is added to the fermentor during the fermentation, so that hydrolysis of protein to amino acids takes place simultaneously with the fermentation of sugar into organic acid, and wherein lactic acid resulting from the fermentation is isolated from the fermentation liquid. Ammonia is preferably added to result in the formation of ammonium lactate, and lactic acid is preferably isolated by a process comprising ultra filtration, ion exchange, conventional electrodialysis and electrodialysis with bipolar membranes.

This invention provides compounds of formula I:wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are mescaline receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

The invention relates generally to novel compositions and methods comprising one or more cyclohexanehexol and one or more NSAID. The compositions and methods provide beneficial effects in the treatment and prevention of diseases involving a disorder in protein folding and / or aggregation, and / or amyloid formation, deposition, accumulation, or persistence, in particular neurodegenerative diseases.

The present invention relates to prodrugs of parent drug compounds containing heteroaromatic NH groups.

This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].

To effectively and reliably acquire detailed images of plural moving subjects in the case where a fixed camera or a pan / tilt camera for searching the moving subject and another pan / tilt camera for taking an image of the details of the moving subject by zooming the moving subjects are used to detect the moving subjects. An imaging system including a sensor camera, a zoom camera, and a controller that controls the sensor camera and zoom camera, and includes a moving subject detection unit extracting the position and the size of a moving subject from a sensor image, an imaging angle of view calculation unit determining one imaging angle of view based on plural moving subjects extracted by the moving subject detection unit, a unit allowing the zoom camera to perform imaging of the area specified depending on the position of the angle, moving speed, and size determined by the imaging angle of view calculation unit, a unit managing the order of the imaging operation of the zoom camera, a unit holding the imaging angle of view for a given time at the time when all the moving subjects in the imaging angle of view become static, and a unit calculating the imaging position in the imaging area of the sensor camera, and assigns ID to an imaging angle of view, assigns the same angle of view ID to the imaging angle even after the moving subject becomes static, controls the priority of the imaging operation of the imaging angle of view including the same moving subject, and allows the zoom camera to take an image of a tracking target in the imaging area of the sensor camera while performing wide-angle imaging with the sensor camera.

The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.A proton pump inhibitor containing a compound represented by the formula (I)wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms X1 and X2 are each a carbon atom or a nitrogen atom, a ring-constituting atom X3 is a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, R1 is an optionally substituted aryl group or an optionally substituted heteroaryl group, R2 is an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, R3 is an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X1, X2 and X3, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.

Compounds of formula (I) and pharmaceutically acceptable salts thereof:wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.A compound represented by the formula (I) or a salt thereof:wherein ring A is a saturated or unsaturated 5-membered heterocycle containing, as a ring-constituting atom besides carbon atoms, at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, the ring-constituting atoms X1 and X2 are the same or different and each is C or N, the ring-constituting atoms X3 and X4 are the same or different and each is C, N, 0 or S (provided that a pyrrole ring wherein X1 is N is excluded from ring A), and when the ring-constituting atom X3 or X4 is C or N, each ring-constituting atom optionally has substituent(s) selected from an optionally substituted alkyl, an acyl, an optionally substituted hydroxy, an optionally substituted mercapto, an optionally substituted amino, a halogen, a cyano and a nitro;R1 and R2 are each a cyclic group optionally having substituent(s); R3 and R4 are each H or alkyl, or R3 and R4 form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.

The application provides formulations for the topical administration of an active agent comprising at least one steroid, in the form of topical sprays that are propellant-free, and / or substantially non-foaming, and / or alcohol-free. The present application also provides processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.

The invention relates to an ecological air purification system having a case body, an air outlet, a fan and plants. The case body is dual-layer structured having an inner chamber, an outer chamber, and a nutrient solution container, the nutrient solution container is fixed at the upper part of the inner chamber where plant culturing medium is arranged; the outer chamber is an air circulation pathway set outside having a circulation chamber, sterilizing chamber, and an exhausting chamber, a fan is set in the exhausting chamber, the air outlet is arranged at the side wall of the exhausting chamber. The present invention discloses a method for purifying air by the purification method. The invention can purify air by making use of the leaf part of plants, and also can give full play to abilities of the plants and greatly improve the ability of plants to treat toxic substances, thereby changing the impression that the efficiency of plants purifying air is comparatively low. The invention has advantages such as high air purifying efficiency, littler pollution, and convenient maintenance.

The invention belongs to the technical field of potato cultivation, and discloses an application of a biodegradable weeding mulching film in potato cultivation. The mulching film comprises the following components in percentage by mass: 70-97% of biodegradable resin A and 3-30% of biodegradable herbicide master batches, wherein the biodegradable herbicide master batches are prepared by a method comprising the following steps: mixing 10-60% of a herbicide with 0.5-7% of a surfactant A, and performing ultrasonic activation; and mixing 25-75% of biodegradable resin B and 1-10% of a surfactant B at a high speed, and performing extrusion and granulation, thereby obtaining the herbicide master batches, wherein the mass ratio of the surfactant A (the hydrophilic-lipophilic balance value is 7-10) to the surfactant B (the hydrophilic-lipophilic balance value is 3-6) is (1:1)-(1:2). As the biodegradable weeding mulching film is used in potato cultivation, the problems that weeds can grow out from furrow surfaces and environment pollution can be caused by common plastics can be effectively prevented, and the labor cost can be lowered.