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5-(benz-(z)-ylidene)-thiazolidin-4-one derivatives as immunosuppressant agents (Fri, 25 Jun 2010)
Patent 547962 Disclosed is a pharmaceutical composition containing at least one thiazolidin-4-one derivative of the General Formula (I) wherein the substituents are defined in the specification and an inert carrier material. Also disclosed are thiazolidine-4-one derivatives and the use of a thiazolidin-4-one derivative of general formula (I) for the preparation of a medicament for use in the prevention or treatment of disorders associated with an activated immune system.
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Pyrimidine-sulfamides and their use as endothelian receptor antagonist (Fri, 27 Jun 2008)
Patent 540937 Disclosed are compounds of general formula I wherein: R1 represents lower alkyl-O-(CH2)n-, cycloalkyl-O-(CH2)n, or cycloalkyl-CH2-O-(CH2)n-; R2 represents -CH3 or Ra-Y-(CH2)m; R3 represents aryl or heteroaryl; R4 represents hydrogen, trifluoromethyl, lower alkyl, lower alkyl-amino, lower alkyloxy, lower alkyloxy-lower alkyloxy, hydroxy-lower alkyloxy, lower alkylsulfinyl, lower alkylthio, lower alkylthio-lower alkyl, hydroxy-lower alkyl, lower alkyloxy-lower alkyl, hydroxy-lower alkyloxy-lower alkyl, hydroxy-lower alkylamino, lower alkylamino-lower alkyl, amino, di-lower alkylamino, [N-(hydroxyloweralkyl)-N-(lower alkyl)]-amino, aryl, arylamino, aryl-lower alkylamino, aryl-thio, aryl-lower alkylthio, aryloxy, aryl-lower alkyloxy, aryl-lower alkyl, arylsulfinyl, heteroaryl, heteroaryl-oxy, heteroarylamino, heteroarylthio, heteroaryl-lower alkyl, heteroarylsulfinyl, heterocyclyl, heterocyclyl-lower alkyloxy, heterocyclyloxy, heterocyclylamino, heterocyclyl-lower alkylamino, heterocyclylthio, heterocyclyllower alkylthio, heterocyclyl-lower alkyl, heterocyclylsulfinyl, cycloalkyl, cycloalkyloxy, cycloalkyl-lower alkyloxy, cycloalkylamino, cycloalkyl-lower alkylamino, cycloalkylthio, cycloalkyl-lower alkylthio, cycloalkyl-lower alkyl, or cycloalkylsulfinyl; R6 represents hydrogen or methyl; X represents oxygen, sulphur, -CH2- or a bond; Y represents a bond, -O-, -NH-, -SO2-NH-, -NH-SO2-NH-, -O-CO-, -CO-O-, -0-CO-NH-, -NH-CO-0-, and -NH-CO-NH-; n represents the integers 2, 3, or 4; m represents the integers 2, 3, or 4; and Ra represents aryl, heteroaryl, lower alkyl, cycloalkyl, or hydrogen...
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PHARMACEUTICAL COMPOSITIONS COMPRISING 5-(BENZ-(Z)-YLIDENE)-THIAZOLIDIN-4-ONE DERIVATIVES, SOME SUCH NEW COMPOUNDS AND THEIR USE IN THE MANUFACTURE OF MEDICAMENTS FOR TREATING DISORDERS ASSOCIATED WITH THE IMMUNE SYSTEM (Tue, 05 Sep 2006)

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Thiazolidin-4-one-derivatives (Thu, 21 Nov 2013)
The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.
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NEW PROCESS FOR THE PREPARATION OF 2-CYCLOPENTYL-6-METHOXY-ISONICOTINIC ACID (Thu, 14 May 2015)
The present invention relates to new processes for the preparation of 2-cyclopentyl-6-methoxy-isonicotinic acid, which is a useful intermediate for the synthesis of pyridine-4-yl derivatives as immunomodulating agent. Moreover, the present invention also relates to new intermediates used in those processes.
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Quinolone derivatives (Thu, 03 Mar 2016)
The invention relates to antibacterial compounds of formula I embedded image wherein R1, U, V and A are as defined in the description, to pharmaceutical compositions containing them and uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections.
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Process for manufacturing a naphthyridine derivative (Thu, 22 Jan 2015)
The invention relates to a process and synthetic intermediates that can be used for manufacturing the compound of formula (1-6) which is a synthetic intermediate useful in the preparation of antibiotic compounds. embedded image
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5-amino-2-(1-hydroxy-ethyl)-tetrahydropyran derivatives (Thu, 06 Oct 2011)
The invention relates to antibacterial compounds of formula I embedded image wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.
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Indole carboxamide derivatives as P2X<sub>7 </sub>receptor antagonists (Thu, 03 Dec 2015)
The invention relates to indole carboxamide derivatives of formula (I), embedded image wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
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2-oxo-oxazolidin-3,5-diyl antibiotic derivatives (Thu, 19 Feb 2015)
The invention relates to antibacterial compounds of formula I embedded image wherein R1a represents H or carboxy and R1b represents H, or R1a and R1b represent together either the group *—C(O)—NH—S—# or the group *—C(OH)═N—S—# wherein “*” represents the point of attachment of R1a and “#” represents the point of attachment of R1b; R2 represents H, (C1-C3)alkyl, hydroxy-(C1-C3)alkyl, benzyl or (C3-C5)cycloalkyl; R3 represents H or halogen; U represents N or CR4; wherein R4 is H or (C1-C3)alkoxy; A represents CH, B represents NH and m represents 1 or 2 and n represents 1 or 2; or A represents N, B is absent, m represents 2 and n represents 2; Y represents CH or N; and Q represents O or S; and salts of such compounds.
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Thiazolidin-4-one derivatives (Thu, 13 Nov 2008)
The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.
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PYRIDINE COMPOUNDS (Fri, 11 Sep 2009)
The invention relates to pyridine compounds, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Process for preparing a pyrimidine intermediate (Thu, 26 May 2016)
The invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 embedded image or a salt thereof, which involves the use of a liquid-liquid extraction using methyl iso-butyl ketone. Said compound of formula I-2 or its salt can be used to prepare macitentan.
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PYRIDINE COMPOUNDS (Wed, 22 Dec 2010)
The invention relates to pyridine compounds, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Antibacterial 1<i>H</i>-indazole and 1<i>H</i>-indole derivatives (Thu, 02 Feb 2017)
The invention relates to antibacterial compounds of formula I embedded image wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below embedded image wherein A is a bond, CH2CH2, CH═CH or C≡C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl, 1-(2-aminoacetyl)azetidin-3-yl, 1-glycylazetidin-3-yl, 1-(2-amino-2-methylpropanoyl)azetidin-3-yl, 3-(2-aminoacetamido)cyclopentyl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl or 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl; and salts thereof.
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ANTIBACTERIAL 1H-INDAZOLE AND 1H-INDOLE DERIVATIVES (Thu, 25 Jun 2015)
The invention relates to antibacterial compounds of formula (I) wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below wherein A is a bond, CH2CH2, CH=CH or C≡C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1 -hydroxymethyl- cycloprop-l-yl, l-((phosphonooxy)methyl)cyclopropyl, l-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2 -hydroxymethyl-cycloprop- 1-yl, 1,2-dihydroxy ethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan- 3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [l,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1 -hydroxymethyl-cycloprop- 1 -yl, 1 -aminomethyl-cycloprop- 1-yl, iraws-2-hydroxymethyl- cycloprop-l-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1 -(2-hydroxyacetyl)azetidin- 3-yl, l-(2-aminoacetyl)azetidin-3-yl, l-glycylazetidin-3-yl, l-(2-amino- 2-methylpropanoyl)azetidin-3-yl, 3-(2-aminoacetamido)cyclopentyl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl or 3-hydroxymethylbicyclo [1,1, 1]pentan-1-yl; and salts thereof.
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Stereoselective synthesis of substituted pyrrolidines (Wed, 17 Jun 2015)
The present invention relates to a halo-lactonization process for the stereoselective preparation of protected 1-(halo-methyl)-3-oxo-2-oxa-5-azabicyclo[2.2.1]heptane derivatives of formula (II) wherein Hal and R 1 are as defined in the description. The invention further relates to the novel compounds of formula (II), and to their further transformation to the compounds of formula (III) wherein R 1 , R 2 , R 3 , and R 4 are as defined in the description.
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NOVEL PYRIMIDINE DERIVATIVES (Thu, 07 May 2009)

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NOVEL PYRIMIDINE DERIVATIVES (Wed, 18 Aug 2010)
The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Forumla (I) wherein A represents Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII) or Formula (IX)
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Pyrimidine derivatives (Thu, 16 Sep 2010)
The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII) or Formula (IX) embedded image
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