37results about How to "Reduced dosage requirements" patented technology

A compound of the formula:or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M-, (C3-C7)cycloalkyl-M-, (C2-C6)alkenyl-M-, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M-, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M-, aryl-M-, aromatic or non-aromatic heterocyclic-M-, aryl-(C1-C5)alkyl-M- or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M-, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

A compound of the formula: or a pharmaceutically acceptable salt, ester or ether thereof, wherein R1 through R12 are independently hydrogen or the like; X1 and X2 are independently CH2 or the like; R13 is hydrogen or the like; or R12 and R13 taken together with three ring atoms of the quinoline ring separating said substituents form a heterocyclic ring; R14 and R15 are hydrogen or the like or these groups taken together form oxo; and the dotted line represents a single or double bond. These compounds are ligands for ORL-1 receptor and especially are antagonists for said receptor.

A compound of the formula:or a pharmaceutically acceptable salt thereof, whereinR1 and R2 are independently selected from hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl and the like; R3 and R4 are independently selected from hydrogen, halo(C1-C10)alkyl, optionally substituted (C1-C6)alkyl and the like, or R3 and R4, together with the nitrogen atom to which they are attached, form an optionally substituted fully saturated, partially saturated or fully unsaturated heterocyclic ring; and R5 is (C4-C11)cycloalkyl and the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

The invention relates to compounds of the formula 1

• [0001]
  • or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R¹, R², R³ and R⁴ are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.

The invention discloses a plasma exchanging adsorption filtration purification system provided with a plasma storage bag and an application method of the purification system. The method includes two steps of plasma components separation returning cycle and high-speed plasma purification regeneration cycle. Plasma components are separated by a selective membrane plasma separator; flow speed difference between a plasma separation cycle and a plasma purification circle is set by the specific plasma storage bag; high-speed plasma adsorption filtration purification treatment is performed by a high-throughput filter and an active carbon-resin absorptive device in a purification circle; and plasma subjected to cycle treatment for multiple times can be exchanged back to a human body through the separation returning circle. By the aid of the purification system and the application method thereof, autologous plasma waste generated in a plasma exchanging purification process can be purified continuously and effectively, and plasma consumption is reduced. The high-throughput filter and an adsorption column are connected in series to purify the plasma; load on a subsequent adsorber is reduced; and varied inflammatory factors, macromolecular toxins and the like combined by micromolecules, middle molecules and proteins which are generated from hepatic failure are eliminated as well, so that the purification efficiency of the whole system is greatly improved.

The invention relates to compounds of the Formula 1

and to pharmaceutically acceptable salts and solvates thereof, wherein A, X², X⁴, X⁵ and X¹ are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4).

The invention features methods for decreasing necrosis. The invention also features methods for treating a subject with a condition in which necrosis occurs. The invention further features chemical compounds used to decrease necrosis.

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis, and intermediates are also disclosed.

There is provided compounds of formula (I), wherein A₁, A₄, A_4a, A₅, B¹, B^1a, B², B^2a, B³, B^3a, B⁴, B^4a and R³ have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

The present invention provides novel 3,4-disubstituted-1H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula I, and the pharmaceutically acceptable salts thereof

wherein R¹, R², R³, R⁴ and X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

The invention relates to the technical field of polypropylene, in particular to a polypropylene halogen-free flame-retardant material and a preparation method thereof, and the polypropylene halogen-free flame-retardant material comprises the following raw materials: polypropylene, a halogen-free flame retardant, a toughening agent, a compatilizer, a nucleating agent and an antioxidant. According to the toughening agent disclosed by the invention, the prepared polypropylene material has a hierarchical structure of nano silicon dioxide-polyurethane-nano aluminum hydroxide-polypropylene, nano silicon dioxide and nano aluminum hydroxide are used as rigid bodies, so that stress concentration points are more easily generated, and crazes are formed at the periphery to absorb impact energy; the polyurethane serving as an interlayer can better absorb impact energy in two directions and is favorable for stopping crazing, so that the impact resistance of the polypropylene is greatly improved; besides, polyurethane is used as an elastomer, so that the elongation at break of polypropylene can be improved, and nano aluminum hydroxide is used as a synergistic flame retardant, so that the dosage requirement of the halogen-free flame retardant can be reduced, the mechanical property of polypropylene is improved, and the V0-grade flame retardant property is maintained.

The invention provides a preparation method of Mn<4+>-activated fluoride fluorescent powder. The preparation method provided by the invention does not need to form a saturated solution of A2MF6, so that the requirement of the use amount of raw materials is greatly reduced; in the preparation process, the target product can be synthesized at room temperature and is convenient to synthesize; a precipitating agent is added, so that the preparation is more convenient, the operation is simpler, the synthetic steps are simplified, and the prepared fluorescent powder has better optical properties; the fluoride fluorescent powder can be well excited by ultraviolet light to blue light, especially the blue light, and has strong red light emission, wherein the red light emission peak is in the wavelength range from 600 to 650 nm; the method has the advantages of a simple preparation process and short consumed time; and the prepared material has a high luminescence quantum yield and is suitable for industrial large-scale preparation.

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I;

as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

There is provided compounds of formula (I), wherein A¹, A², A³, A⁴, n, the dotted lines, B¹, B^1a, B², B^2a, B³, B^3a, B⁴, B^4a, R² and R³ have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

The invention provides a feed additive for reducing the excretion quantity of nitrogen and phosphorus in animal waste, and application of the feed additive. On the basis of low protein daily ration, histidine, beta-alanine and a complex enzyme preparation are added, so that the excretion quantity and the excretion rate of nitrogen and phosphorus in animal waste can be reduced. The feed additive for reducing the excretion quantity of nitrogen and phosphorus in animal waste is low in cost and environmentally friendly; furthermore, after the feed additive is adopted, the balance of amino acid in the daily ration is maintained, and the nutritional requirement of growth and development of animals can be met, so that the feed additive has high popularization and application values.

The invention provides an online pH measurement device of a high-temperature strong-washing neutralization solution. The device comprises a measuring sampling tube, a pH meter, a pneumatic telescopicprotecting sleeve for fixing the pH meter and a cleaning control device, wherein a water inlet, a water outlet, a testing hole and a drain outlet are formed in the measuring sampling tube; the pH meter is fixedly arranged on a push rod of the pneumatic telescopic protecting sleeve; the pneumatic telescopic protecting sleeve is arranged at the testing hole and detachably connected with the measuring sampling tube, and a washing water inlet and a washing water outlet are formed in the pneumatic telescopic protecting sleeve; the washing water inlet is connected with clear water through a water pipe, a washing water electromagnetic valve is arranged at the washing water inlet, and the washing water outlet is connected with a trench through a water pipe; the cleaning control device comprises aDCS control system, and the DCS control system is provided with a main relay and a cleaning relay. Online measurement of the high-temperature strong-washing neutralization solution is realized, and the device is simple in structure, capable of performing automatic cleaning, convenient to operate, long in online testing time, stable in operation and accurate in measurement result, can reduce blocking and provides convenience for environment-friendly drainage.

The present invention provides novel cyclic substituted imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof, wherein R¹, R², R⁴, R⁵, R⁶, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

The present invention relates to one image comparing method for optical director, and several pixels in the center of the image are used as comparison target so that the optical indicator may be manufactured in lower cost while considering memory requirement and calculation speed. The method of the present invention includes the steps of: sampling the several pixels in the center of the image Pn; comparing the sampled pixels with those in the comparison area formed through expanding from the central pixels by M pixels in both horizontal and vertical directions in the image Pn+1; and calculating the moving distance and direction of the optical director between the image Pn and the image Pn+1.

The invention discloses a method for increasing reducing sugar content of straws. The method comprises the following steps carried out in sequence: 1, performing electron beam irradiation on the straws; 2, putting the straws into a hydrochloric acid solution with the volume concentration of 30-35% to perform acidification for 12-24 hours, and performing stewing for 2-6 hours at a starting temperature of 50 DEG C and a heating rate of 0.5 DEG C/min; and 3, adjusting the pH value and temperature of a stewed straw solution to 4.9 and 60 DEG C or below respectively, adding cellulase to the straw solution according to a mass ratio of the cellulase to the straws of 6-9 : 1,000, and performing enzymolysis for 5-24 hours, wherein the filter paper enzyme activity of the cellulase is 1,400-1,500 FPU/g. According to the method, the tissue structures of the straws are greatly changed and destroyed; the utilization amount of the cellulase is reduced; the production cost is reduced; the reducing sugar content in the straws is greatly increased after processing; and the method is suitable for industrial production.

A₃ agonists having Formula I are described herein as well as methods of using such A₃ agonists and pharmaceutical compositions containing such A₃ agonists.

The A₃ agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia.

The present invention discloses radioligands of 9-arylsulfone of the formula (X) or a pharmaceutically acceptable salt or enantiomer thereof, which are useful in diagnosing depression, obesity and other CNS disorders.