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9024022 Substrates of O6-alkylguanine-DNA alkyltransferase and mutants thereof  
The invention relates to compounds of formula (I′): in which A, L2, M and B are as defined in the description. These compounds are substrates of O6-alkylguanine-DNA alkyltransferase and mutants...
9006259 N1-sulfonyl-5-fluoropyrimidinone derivatives  
This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
9000002 N1-substituted-5-fluoro-2-oxopyrimidinone-1(2H)-carboxamide derivatives  
This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamide s and their derivatives and to the use of these compounds as fungicides.
9000160 Process for the preparation of 2-amino-5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidine from 4-chloro-2,5-dimethoxypyrimidine  
2-Amino-5,8-dialkoxy[1,2,4]-triazolo[1,5-c]pyrimidines are manufactured from 4-chloro-2,5-dialkoxypyrimidines in a process that avoids hydrazine and cyanogen halide.
8975250 5 oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives as CaMKII kinase inhibitors for treating cardiovascular diseases  
The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.
8952018 Pharmaceutical combination of MEK inhibitor and B-Raf inhibitors  
A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimet hyl;...
8952028 Methods of treating chemoresistance and relapse in cancer cells  
Methods of treating or preventing chemoresistance or relapse growth of cancer cells are provided. Methods of treating or preventing resistance to tyrosine kinase based chemotherapeutic treatment...
8946242 Spiro[2.4]heptanes for treatment of flaviviridae infections  
Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an...
8933090 1-aza-bicyclo[3.3.1]nonanes  
The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as...
8921384 Spiro[2.4]heptanes for treatment of flaviviridae infections  
Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an...
8916579 5-fluoropyrimidinone derivatives  
This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
8912207 2-aldoximino-5-fluoropyrimidine derivatives  
This present disclosure is related to the field of 2-aldoximino-5-fluoropyrimidines and their derivatives and to the use of these compounds as fungicides.
8889860 3′-OH unblocked, fast photocleavable terminating nucleotides and methods for nucleic acid sequencing  
The present invention relates generally to 3′-OH unblocked, labeled and unlabeled nucleotides and nucleosides with 5-methoxy-substituted nitrobenzyl-based photocleavable terminating groups for use...
8889741 Cycloalkane derivatives  
Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease. The present invention provides...
8865731 Inhibitor of analgesic tolerance  
Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a...
8835450 Combination of inhibitor of B-Raf and an inhibitor of Akt in the treatment of cancer  
The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method...
8816074 2′-fluoro-6′-methylene carbocyclic nucleosides and methods of treating viral infections  
The present invention relates to 2′-Fluoro-6′-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number...
8796452 Preparation of lamivudine form I  
A thermodynamically controlled process for preparing Form I polymorph of lamivudine is described, wherein the process involves crystallizing Form I at a temperature of from about 0° C. to about...
8796298 Combination of a B-Raf inhibitor: N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1- dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide and the Akt inhibitor: N-{ (1S)-2-amino-1-[(3- fluorophenyl)methyl]ethyl}-5-chIoro-4-(4-chIoro- 1 -methyl- 1 H-pyrazol-5-yl)-2-10 thiophenecarboxamide useful in the treatment of cancer  
The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method...
8785467 Alkoxy pyrimidine PDE10 inhibitors  
The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10...
8785444 Thiazoles and pyrazoles useful as kinase inhibitors  
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and...
8779127 Processes for preparing substituted pyrimidines  
The present invention provides a facile process for the preparation of tri- and tetra—substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora...
8754078 Compositions and methods for treatment of cancer  
The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell...
8748411 Antineoplastic compounds and pharmaceutical compositions thereof  
Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the...
8748604 Process for stereoselective synthesis of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine  
The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cy tosine and pharmaceutically acceptable salts thereof.
8748603 Crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]THIO]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfonamide  
There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihy droxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-am ide anhydrate. Such compounds/forms...
8735579 Benzamides, production thereof, and use thereof as medicaments  
Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the...
8703781 Pharmaceutical combination of MEK inhibitor and B-RAF inhibitors  
A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimet hyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimid in-1-yl]phenyl}acetamide,...
8686155 Aurora kinase modulators and method of use  
The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating...
8673926 Spiro[2.4]heptanes for treatment of flaviviridae infections  
Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an...
8653267 Co-crystal compound of optical device  
The present invention discloses a co-crystal compound of optical devices. The co-crystal compound is crystallized out with hydrogen bonding by a temperature fluctuation method after mixing small...
8637535 Polymorphic and other crystalline forms of cis-FTC  
Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder...
8618103 Inhibitors of JAK  
The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK...
8609864 Hydroxamic acid derivatives  
The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these...
8604192 Cyclohexenyl nucleic acids analogs  
The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic...
8586600 Heterocyclic compounds and uses thereof  
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
8575342 HIV inhibiting 5-heterocyclyl pyrimidines  
Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4-...
8575338 Pyrimidine, pyridine and triazine derivatives as maxi-K channel openers  
A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently...
8557833 Aminopyrimidines useful as kinase inhibitors  
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and...
8552020 N1-substituted-5-fluoro-2-oxopyrimidinone-1(2H)-carboxamide derivatives  
This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamide s and their derivatives and to the use of these compounds as fungicides.
8518885 Heterocyclic peptide ketoamides  
A novel class of peptide α-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula...
8492390 Synthesis of locked nucleic acid derivatives  
The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α-L-oxy-LNA, amino-LNA, α-L-amino-LNA, thio-LNA, α-L-thio-LNA, seleno-LNA and methylene LNA,...
8481554 Solid oral dosage forms of lamivudine  
The present invention relates to the oral solid pharmaceutical composition comprising lamivudine or a pharmaceutically acceptable salt thereof with isomalt as a filler. The present invention also...
8470839 N1-acyl-5-fluoropyrimidinone derivatives  
This present disclosure is related to the field of N1-acyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
8455507 Aminopyrimidines useful as kinase inhibitors  
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and...
8431588 Cyclopropyl polymerase inhibitors  
Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl;R3 and R4 are hydrogen, —C(═O)R5, or —C(═O)CHR6—NH2; orR3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester;...
8410123 Pyrimidine sulphonamide derivatives as chemokine receptor modulators  
A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of...
8399655 Process and methods for the preparation of optically active cis-2-hydroxymethyl-4-(cytosin-1′-yl)-1,3-oxathiolane or pharmaceutically acceptable salts thereof  
There is provided a method for resolving a compound of formula III, in the cis configuration: There is also provided a process for producing optically active compound of formula I or II: wherein:...
8383633 Aminopyrimidines useful as kinase inhibitors  
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and...
8354524 Synthesis of selenium-derivatized nucleosides, nucleotides, phosphoramidites, triphosphates and nucleic acids  
The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids...