PATENTSCOPE: EN_ALL:nmr AND PA:actelion

NADPH OXIDASE 4 INHIBITORS (Fri, 30 Dec 2016)
The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.
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CXCR7 RECEPTOR MODULATORS (Fri, 10 Jun 2016)
The present invention relates to derivatives of formula (I) wherein (R1)n, ring (A), Y1, Y2, X, R4, L1, L2, and Ar1 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
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ANTIBACTERIAL BENZOTHIAZOLE DERIVATIVES (Fri, 27 May 2016)
The invention relates to antibacterial compounds formula (I) wherein R1 is the group M, whereby M is one of the groups MA and MB represented below wherein A is a bond or C≡C; R1A is H or halogen; R2A is H or halogen; R3A is H, alkoxy, hydroxyalkoxy, hydroxyalkyl, dihydroxyalkyl, 2-hydroxyacetamido, substituted cycloprop-1-yl or substituted oxetan-3-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, dialkylaminoalkyl, substituted cycloprop-1-yl, substituted cyclobutan-1-yl, substituted oxetan-3-yl, 3-hydroxythietan-3-yl, substituted azetidin-3-yl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl, 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl, 4-hydroxytetrahydro-2H-pyran-4-yl, (3R,6S)-3-aminotetrahydro-2H-pyran-6-yl, piperidin-4-yl or 1-(2-hydroxyacetyl)piperidin-4-yl; and salts thereof.
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ANTIBACTERIAL BASIC BIAROMATIC DERIVATIVES WITH AMINOALKOXY SUBSTITUTION (Fri, 22 Apr 2016)
The invention relates to antibacterial compounds of formula I wherein R1a, R2a, R2b, R3a, R3b, R4, R5, U1, U2, U3, U4, V1, V2, V3, V4, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
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TRIAZOLE COMPOUNDS AS T-TYPE CALCIUM CHANNEL BLOCKERS (Fri, 25 Mar 2016)
The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
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PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS (Fri, 11 Dec 2015)
The invention relates to compounds of formula (I) Formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
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ANTIBACTERIAL QUINAZOLINE-4(3H)-ONE DERIVATIVES (Fri, 20 Nov 2015)
The invention relates to antibacterial compounds of formula I, wherein R1 is H or halogen; R2 is the group M; R3 is H or halogen; M is MA or MB wherein A is a bond or C≡C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A 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 R1B is a group as defined in claim 1; and salts thereof.
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8-(PIPERAZIN-1-YL)-1,2,3,4-TETRAHYDRO-ISOQUINOLINE DERIVATIVES (Fri, 02 Oct 2015)
The invention relates to compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
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AZAINDOLE ACETIC ACID DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS (Fri, 25 Sep 2015)
The present invention relates to azaindole acetic acid derivatives of formula (I), (I) wherein R1 and R2 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
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1,2-DIHYDRO-3H-PYRROLO[1,2-C]IMIDAZOL-3-ONE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS (Sat, 12 Sep 2015)
The invention relates to antibacterial compounds of formula (I), wherein R1 is one of the groups represented below (AA), wherein A is a bond, CH=CH or C≡C; U is N or CH; V is N or CH; W represents N or CH; and R1A, R2A, R3A, R1B and R1C are as defined in the claims; and salts thereof.
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PROCESS FOR MANUFACTURING PYRIMIDINE SULFAMIDE DERIVATIVES (Fri, 21 Aug 2015)
The invention relates to a process for manufacturing the compound of formula I wherein R is H, (C1-C6)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, C1-C6)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.
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ANTIBACTERIAL 1H-INDAZOLE AND 1H-INDOLE DERIVATIVES (Fri, 26 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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CRYSTALLINE FORM OF (S)-(2-(6-CHLORO-7-METHYL-1H-BENZO[D]IMIDAZOL-2-YL)-2-METHYLPYRROLIDIN-1 -YL)(5-METHOXY-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)METHANONE AND ITS USE AS OREXIN RECEPTOR ANTAGONISTS (Fri, 12 Jun 2015)
The invention relates to crystalline forms of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2- yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone, processes for the preparation thereof, pharmaceutical compositions containing such crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as orexin receptor antagonists.
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USE OF BENZIMIDAZOLE-PROLINE DERIVATIVES (Fri, 12 Jun 2015)
The present invention relates to compounds of the formula (I), wherein Ar1 and Ar2 are as described in the description and to their use as pharmaceuticals for the treatment of sundown syndrome. The invention also relates to the preparation of such compounds and of pharmaceutically acceptable salts thereof.
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CRYSTALLINE SALT FORM OF (S)-(2-(6-CHLORO-7-METHYL-1 H-BENZO[D]IMIDAZOL-2-YL)-2-METHYLPYRROLIDIN-1 -YL)(5-METHOXY-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)METHANONE AS OREXIN RECEPTOR ANTAGONIST (Fri, 12 Jun 2015)
The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1 H-benzo[d]imidazol- 2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.
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ANTIBACTERIAL 2H-INDAZOLE DERIVATIVES (Fri, 20 Mar 2015)
The invention relates to antibacterial compounds of formula (I) wherein R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups (A, B, C, D) wherein A is a bond, CH2 CH2, CH=CH or C≡C and R1A, R2A, R3A, R1B and R1C are as defined in claim 1; and salts thereof.
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BENZIMIDAZOLYL-METHYL UREA DERIVATIVES AS ALX RECEPTOR AGONISTS (Fri, 13 Feb 2015)
The present invention relates to benzimidazolyl-methyl urea derivatives of formula (I), wherein n, D, E, R1, R2, R3, R4, R6, R7, R8 and R9 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
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1-(PIPERAZIN-1-YL)-2-([1,2,4]TRIAZOL-1-YL)-ETHANONE DERIVATIVES (Fri, 30 Jan 2015)
The invention relates to compounds of Formula (I) wherein X, Y, R1, R2, R3, R4 and R5 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
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PIPERAZINE SUBSTITUTED BRIDGED SPIRO[2.4]HEPTANE DERIVATIVES AS ALX RECEPTOR AGONISTS (Fri, 23 Jan 2015)
The present invention relates to a piperazine substituted bridged spiro[2.4] heptane derivative of formula (I), its preparation and its use as pharmaceutically active compound.
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PROCESS FOR PREPARING A PYRIMIDINE INTERMEDIATE (Fri, 16 Jan 2015)
The present invention relates to a process for preparing a pyrimidine 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 macitentan. Macitentan (chemical names: N-[5-(4-bromophenyl)-6-[2-[(5-bromo- 2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl] -N'-propylsulfamide or N-[5-(4-bromophenyl)- 6- {2- [(5 -bromopyrimidin-2-yl)oxy] ethoxy } pyrimidin-4-yl] -N'-propylsulfuric diamide) is an endothelin receptor antagonist that has notably been approved by the US Food and Drug Administration and the European Commission for the treatment of pulmonary arterial hypertension. It has been first disclosed in WO 02/053557. The last step of one of the potential preparation routes described in WO 02/053557, called "Possibility A" and "Possibility B", can be summarised as shown in Scheme Al hereafter.
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