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Patent
Actelion Pharmaceuticals | Date: 2014-12-18

The invention relates to antibacterial compounds of formula I wherein X is N or CH; R^(1 )is H or halogen; R^(2 )is alkynyloxy or the group M; R^(3 )is H or halogen; M is one of the groups M^(A )and M^(B )represented below wherein A is a bond, CH_(2)CH_(2), CHCH or CC; R^(1A )is H or halogen; R^(2A )is H, alkoxy or halogen; R^(3A )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 R^(1B )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.


Patent
Actelion Pharmaceuticals | Date: 2015-05-13

The invention relates to antibacterial compounds of formula I wherein R^(1 )is H or halogen; R^(2 )is the group M; R^(3 )is H or halogen; M is M^(A )or M^(B ) wherein A is a bond or CC; R^(1A )is H or halogen; R^(2A )is H, alkoxy or halogen; R^(3A )is H, alkoxy, hydroxyalkoxy, hydroxyalkyl, 1,2-dihydroxyethyl, dialkylamino, 1-hydroxymethyl-cycloprop-1-yl, 1-((dimethylglycyl)oxy)methyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, morpholin-4-ylalkyl or morpholin-4-ylalkoxy; and R^(1B )is a group as defined in claim 1; and salts thereof.


Patent
Actelion Pharmaceuticals | Date: 2016-01-13

The invention relates to the use of macitentan in combination with radiotherapy or with both radiotherapy and a cytotoxic therapy agent (such as temozolomide or paclitaxel) in the treatment of malignant glioma, in particular glioblastoma multiforme.


Patent
Actelion Pharmaceuticals | Date: 2015-08-19

The invention relates to a process for manufacturing the compound of formula I_(1)-C_(6))alkyl or benzyl, or a salt thereof, said process comprising the reaction of the compound of formula I-1_(1)-C_(6))alkyl or benzyl, or a salt of said compound of formula I-2, in the presence of tetra-n-butyl ammonium fluoride hydrate and of a base. The invention further relates to the compound of formula I-1 and uses thereof.


The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R^(1 )and R^(2 )are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D_(2 )receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.


Patent
Actelion Pharmaceuticals | Date: 2015-02-13

The invention relates to a process for manufacturing the compound of formula I wherein R is H, (C_(1)-C_(6))alkyl or benzyl, or a salt thereof, said process comprising the reaction of the compound of formula I-1 wherein X is Br, Cl or F, or a salt thereof, with the compound of formula I-2 wherein R is H, (C_(1)-C_(6))alkyl or benzyl, or a salt thereof, in the presence of a base, and, when X is Br or Cl, in the presence of tetra-n-butyl ammonium fluoride hydrate or cesium fluoride. The invention further relates to the compound of formula I-1 and uses thereof.


The present invention relates to a new synthetic intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare the compound of formula I-3 which is an important synthetic intermediate used in the preparation of macitentan.


Patent
Actelion Pharmaceuticals | Date: 2015-06-17

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)^(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)^(1), R^(2), R^(3), and R^(4) are as defined in the description.


Patent
Actelion Pharmaceuticals | Date: 2016-04-21

The invention relates to compounds of formula I wherein ^(6 )or N; R^(0 )is H or, if ^(1 )is H or halogen; U is CH or N when _(2), NH or NR^(g); R^(2 )is H, alkylcarbonyl or CH_(2)R^(3); R^(3 )is H, alkyl or hydroxyalkyl; R^(4 )is H or, if n is not 0 and R^(5 )is H, may also be OH; R^(5 )is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R^(6 )is hydroxyalkyl, carboxy, alkoxycarbonyl or (CH_(2))_(q)NR^(7)R^(8), q being 1, 2 or 3 and each of R^(7 )and R^(8 )independently being H or alkyl or R^(7 )and R^(8 )forming with the N atom bearing them a ring; R^(9 )is alkyl or hydroxyalkyl; A is (CH_(2))_(p), CH_(2)CH_(2)CH(OH) or COCH_(2)CH(OH); G is substituted phenyl or G^(1 )or G^(2) wherein Q is O or S and X is CH or N; and Y^(1), Y^(2 )and Y^(3 )may each be CH or N; and n is 0 when A is CH_(2)CH_(2)CH(OH) or COCH_(2)CH(OH), and n is 0, 1 or 2 when A is (CH_(2))_(p), p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts thereof.


Patent
Actelion Pharmaceuticals | Date: 2016-01-20

The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof

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