摘要:
The invention provides hydroquinone derivatives of formula (I), processes of preparation, as well as pharmaceutical compositions and methods of treating and/or preventing e.g. autoimmune, immunological, rheumatology, vascular, ophthalmologic, fibrotic, metabolic and gastro-intestinal disorders, neuroinflammatory and neurodegenerative diseases, neoplasms and cancer associated disorders, hormone related diseases and immunological disorders resulting from viral and bacterial infectious diseases and complications thereof.
wherein: R a , R b = H, acyl or aryl alkyl; R 1 = COOR 4 , (CH 2 ) n COOR 4 , SO 3 H, (CH 2 ) n SO 3 H or CONH-R 10 ; R 2 and R 3 = H or R 5 , with the proviso that when one of R 2 and R 3 is R 5 , the other is H; R 4 = H, alkyl or aryl alkyl; R 5 = R 6 , R 7 or R 8 ; R 6 = CONH-R 9 , CONHCOR 9 , CONH(CH 2 ) n - R 9 , CONHCH(COOR 4 )(CH 2 ) k R 9 or heteroaryl-R 9 ; k = 0-4; R 7 = optionally substituted benzoheteroaryl ; R 8 = (CH 2 ) m X(CH 2 ) p R 9 ; X = O, S, SO 2 , NH, NAc or N(CH 2 ) q R 9 ; R 9 = optionally substituted aryl, heteroaryl or cycloalkyl ; R 10 = optionally substituted aryl or heteroaryl ; n, m, p and q = independently 1-4.
摘要:
This invention provides for a compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein R 1 -R 4 , n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
摘要:
This invention provides for a compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein R 1 -R 4 , n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
摘要:
Provided is a novel therapeutic agent for glaucoma, which has sGC-activating action. A therapeutic agent for glaucoma or an ocular hypotensive agent, which contains, as an effective component, a compound represented by Formula (I-a) or Formula (I-b) and having a LogD value of more than 1.5 and less than 2.5, or a pharmaceutically acceptable salt thereof. [In formulae (I-a) and (I-b), each symbol is as defined in the description.]
摘要:
Provided is a pharmaceutical agent containing a compound represented by general formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof. A compound represented by general formula (1) , a pharmaceutically acceptable salt thereof or a solvate thereof; wherein Ar represents an aryl group, or a 5- or 6-membered heteroaryl group containing a nitrogen atom, an oxygen atom or a sulfur atom; Y represents, for example, a hydrogen atom or a C 1 -C 6 alkyl group; A represents a C 1 -C 3 alkylene chain which may be substituted with two C 1 -C 2 alkyl groups; X represents a hydrogen atom or a halogen atom; V represents an oxygen atom or a methylene chain; and R represents a group selected from the formulae below.
摘要:
The present invention relates to a preparation method of 4-aminomethylbenzoic acid comprising the following steps: preparing 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate); reacting the 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate) with hydroxyamine to oximate the same; and contact reducing 4-carboxylbenzaldehyde oxime or an alkyl ester oxime thereof obtained by the oximation, through hydrogen in a sodium hydroxide aqueous solution. Since methyl 4-hydroxyiminomethylbenzoate is reacted as a raw material in the presence of an alkali, hydrogen of a relatively low pressure can be used and a purification process is also simple, thereby enabling preparation of 4-aminomethylbenzoic acid with a low cost and high yield.
摘要:
The present invention provides a process for preparing primary amines, comprising the steps of A) providing a solution of a primary alcohol in a fluid, non-gaseous phase, B) contacting the phase with free ammonia and/or at least one ammonia-releasing compound and a homogeneous catalyst, and optionally C) isolating the primary amine formed in step B), characterized in that the volume ratio of the volume of the liquid phase to the volume of the gas phase in step B is greater than 0.05 and/or that step B is carried out at pressures greater than 10 bar.
摘要:
The invention relates to novel forms of 4-({(4-carboxybutyl)[2-(2-{[4-(2-phenylethyl)benzyl]oxy}phenyl)ethyl]amino}methyl)benzoic acid, especially modification I, methods for the production thereof, medicaments containing the same, and the use thereof for fighting diseases.
摘要:
The invention relates to tri-amino-pyrimidine derivatives of the general formula (I) in which Y, R3, W, R4a, R5a, R4b, R5b, n and m are variable. These compounds have a phosphatase CDC25 inhibiting activity and can thus be used as drugs for diseases in which CDC25 are involved. The invention also relates to pharmaceutical compositions containing said products, and to the use thereof for preparing a drug.