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Crystalline forms of an antiviral compound (Thu, 21 Sep 2017)
Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: embedded image Also provided are processes of manufacture and methods of using the crystalline forms.
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Nucleobase phosphonate analogs for antiviral treatment (Fri, 27 Nov 2009)
Patent 544988 Disclosed is a compound of the formula (I) wherein X2 is selected from O, NR and S; Y1 is independently O, S, NR, or N-R2; Y2 is independently O, NR, N-NR2-S(O)M2-, or ���S(O)M2-S(O)M2-; NUCLEOBASE is selected from adenine, guanine, aminopurine, 2-amino-6-chloropurine, 2,6-diaminopurine, hypoxanthine, isoguanine, 6-thioguanine, O6-methylguanine and N6-methyladenine, and wherein the rest of the substituents are disclosed within the specification or a pharmaceutically acceptable salt thereof. Also disclosed is the use of the above compound in the manufacture of a medicament for the treatment or prevention of the symptoms or effects of HIV infection in an infected animal.
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Process for preparing an A2A-adenosine receptor agonist and its polymorphs (Wed, 17 Apr 2013)
Disclosed is a synthesis suitable for large scale manufacture of an A2A- adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
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CRYSTALLINE FORMS OF A MACROCYCLIC HCV NS3 INHIBITING TRIPEPTIDE (Thu, 02 Jul 2015)
Crystalline forms of the anti-HCV compound (1R,5S,8S,9S,10R,22aR )-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6] dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the crystalline forms.
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Process for preparing an A2A-Adenosine receptor agonist and its polymorphs (Thu, 28 Aug 2008)
Disclosed is a synthesis suitable for large scale manufacture of an A2A- adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
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Pharmaceutical compositions comprising a JAK inhibitor (Thu, 20 Sep 2018)
Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.
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Process for preparing an A2A-adenosine receptor agonist and its polymorphs (Fri, 30 Sep 2011)
Patent 570239 Disclosed is (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide monohydrate. Further disclosed is a method for its preparation which comprises reacting ethyl 1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxyrnethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazole-4-carboxylate with aqueous methylamine in a sealed pressure reactor, wherein the reaction is conducted at an initial temperature of about 0-5��C followed by warming to about 50-70��C.
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Process for preparing an A<sub>2A</sub>-adenosine receptor agonist and its polymorphs (Thu, 21 Oct 2010)
Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
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Crystalline forms of an antiviral compound (Thu, 25 Jun 2015)
Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: embedded image Also provided are processes of manufacture and methods of using the crystalline forms.
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Preparation of alkyl-substituted 2-deoxy-2-fluoro-D-ribofuranosyl pyrimidines and purines and their derivatives (Fri, 28 May 2010)
Patent 552927 Disclosed is a compound according to Formula (I) wherein, the substituents are disclosed within the specification. The process for preparing the compound and intermediates used in the process are also disclosed. The compounds are alkyl-substituted 2-deoxy-2-fluro-D-ribofuranosyl pyrimidine and purine derivatives. The compound of Formula (I) is an anti-HCV inhibitor.
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PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR (Thu, 20 Sep 2018)
Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.
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Nucleic acid ligand complexes (Thu, 03 Jul 2003)
This invention discloses a method for preparing a therapeutic or diagnostic complex comprised of a nucleic acid ligand and a lipophilic compound or non-immunogenic, high molecular weight compound by identifying a nucleic acid ligand by SELEX methodology and associating the nucleic acid ligand with a lipophilic compound or a non-immunogenic, high molecular weight compound. The invention further discloses complexes comprising one or more nucleic acid ligands in association with a lipophilic compound or non-immunogenic, high molecular weight compound.
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PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR (Thu, 20 Sep 2018)
Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.
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Pre-organized tricyclic integrase inhibitor compounds (Fri, 31 Aug 2007)
Patent 539264 Tricyclic compounds according to the structure shown below in formula (I), protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site. The variables shown in formula (I) are further defined in the specification.
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TENASCIN-C NUCLEIC ACID LIGANDS (Wed, 24 Apr 2002)
Methods are described for the identification and preparation of nucleic acid ligands to tenascin-C. Included in the invention are specific RNA ligands to tenascin-C identified by the SELEX method. Further included in the invention are methods for detecting the presence of a disease condition in a biological tissue in which tenascin-C is expressed.
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Solid forms of an antiviral compound (Thu, 15 Jan 2015)
Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H- benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: (Compound (I)). Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.
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SOLID FORMS OF AN ANTIVIRAL COMPOUND (Thu, 12 Dec 2013)
Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H- benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: (Compound (I)). Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.
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Phosphatidylinositol 3-kinase inhibitors (Thu, 26 Jun 2014)
The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), embedded image or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.
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Fused heterocyclic compounds as ion channel modulators (Thu, 25 Jun 2015)
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: embedded image wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
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Phosphatidylinositol 3-kinase inhibitors (Thu, 26 Jun 2014)
The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), embedded image or pharmaceutically acceptable salts thereof, in which n, m, R1, R2, and R3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.
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