- NLRP3 INHIBITORS
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The present application relates to compounds with NLRP3inhibitory activity and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present application further relates to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3inhibition.
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- New preparation method of 4-aminoindan compound
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The invention relates to a new preparation method of a 4-aminoindan compound. 4-Aminoindan is an important medical intermediate. With carboxybenzaldehyde as an initial raw material, through esterification, condensation, cyclization, reduction elimination, Curtius rearrangement, an amidogen deprotection reaction and a hydrogenation reaction in sequence, the 4-aminoindan is prepared. According to the method, the problems of difficult generation of isomers, difficult separation of substitution products and the like in a traditional method are solved, the whole preparation method is convenient toimplement, the yield is high, and the method has great industrial prospects.
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- NOVEL COMPOUNDS
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The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
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- NOVEL COMPOUNDS
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The present invention relates to substituted 5-membered nitrogen containing heteroaryl compounds, such as sulfonyl triazoles, where the heteroaryl ring is further substituted, optionally via a linking group such as -NH-, with a cyclic group which in turn is substituted at the α-position. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.
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- Methods and Compositions for Treatment of Scleritis and Related Disorders
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The present teachings relate to the field of anti-inflammatory substances and more particularly to compounds that are useful for the treatment of scleritis, a scleritis symptom, or a scleritis-related disorder. In one aspect, methods of treating scleritis, a scleritis symptom, or a scleritis-related disorder generally include administering to a subject a compound of Formula I: or a pharmaceutically acceptable salt, hydrate or ester thereof, wherein W1, W2, R1, L, X, Y, Z, and n1 are defined as described herein.
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Page/Page column 17
(2008/12/05)
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- ARYL FLUOROETHYL UREAS ACTING AS ALPHA 2 ADRENERGIC AGENTS
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The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
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Page/Page column 28-29
(2008/12/07)
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- 2,4-DI(AMINOPHENYL) PYRIMIDINES AS PLK INHIBITORS
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The invention relates to compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1, and R3 are defined as indicated in claim 1. Said compounds are used for the treatment of diseases characterized by excessive or anomalous cell proliferation. Also disclosed is the use of the inventive compounds for producing a medicament having said properties.
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Page/Page column 35-36
(2008/06/13)
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- Methods and compositions for selectin inhibition
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The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: wherein the constituent variables are defined herein.
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Page/Page column 17
(2008/06/13)
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- 1-Acyl-2-imidazolines and their manufacture
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The invention relates to 1-acyl-2-imidazolines, processes for their manufacture, and their use as intermediates.
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- On the galenical development of a nose spray from N-(2-imidazolin-2-yl)-N-(4-indanyl)amine monohydrochloride (indanazoline)
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An account is given of the aim of the galenical development of the new remedy, indanazolin nose-spray. The description of the quality of the active ingredient N-(2-imidazolin-2-yl)-N-(4-indanyl)amine monohydrochloride (indanazoline, Farial) and the dosage form allows a pharmaceutical evaluation. The descriptions of the organoleptic, physical and chemical properties of the active substance are given in detail. The formulation, the procedures for manufacturing, and the specifications for the packaging materials give some idea of the galenical aspects. The quality of the finished dosage form is defined by means of product specifications relating to the identity, purity, and potency, and is proved by suitably designed stability studies. Finally a detailed summary is made of the analytical methods which were used.
- Dechow,Lammerhirt,Pich,Schikarski
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p. 1738 - 1746
(2007/10/02)
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