INCYTE CORPORATION Patent applications |
Patent application number | Title | Published |
20160137626 | BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 05-19-2016 |
20160046650 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 02-18-2016 |
20160000795 | TREATMENT OF B-CELL MALIGNANCIES BY A COMBINATION JAK AND PI3K INHIBITORS - This invention relates to methods of treating B-cell malignancies using a combination of inhibitors of JAK1 and/or JAK2 and inhibitors of PI3Kδ. | 01-07-2016 |
20150361094 | BICYCLIC HETEROARYLAMINOALKYL PHENYL DERIVATIVES AS PI3K INHIBITORS - This application relates to derivatives of Formula I: | 12-17-2015 |
20150344497 | PROCESSES OF PREPARING A JAK1 INHIBITOR AND NEW FORMS THERETO - This invention relates to processes for preparing a JAK1 inhibitor having Formula Ia: | 12-03-2015 |
20150342952 | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 - This invention relates to JAK selective inhibitors for use in treatment of chronic neutrophilic leukemia and atypical chronic myeloid leukemia in patients. | 12-03-2015 |
20150307493 | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS - The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 10-29-2015 |
20150291701 | METHODS FOR TREATING DISORDERS ASSOCIATED WITH HUMAN SIGNAL PEPTIDE-CONTAINING MOLECULES - The invention provides human signal peptide-containing proteins (HSPP) and polynucleotides which identify and encode HSPP. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with expression of HSPP. | 10-15-2015 |
20150284390 | N-(1-(SUBSTITUTED-PHENYL)ETHYL)-9H-PURIN-6-AMINES AS PI3K INHIBITORS - The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases. | 10-08-2015 |
20150250790 | TOPICAL FORMULATION FOR A JAK INHIBITOR - This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders. | 09-10-2015 |
20150225411 | AZETIDINYL PHENYL, PYRIDYL OR PYRAZINYL CARBOXAMIDE DERIVATIVES AS JAK INHIBITORS - The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 08-13-2015 |
20150225401 | CYCLOPROPYLAMINES AS LSD1 INHIBITORS - The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. | 08-13-2015 |
20150225394 | CYCLOPROPYLAMINES AS LSD1 INHIBITORS - The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. | 08-13-2015 |
20150225379 | CYCLOPROPYLAMINES AS LSD1 INHIBITORS - The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. | 08-13-2015 |
20150225375 | CYCLOPROPYLAMINES AS LSD1 INHIBITORS - The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. | 08-13-2015 |
20150218174 | PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS - The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases. | 08-06-2015 |
20150210692 | Spirocycles as Inhibitors of 11-beta Hydroxyl Steroid Dehydrogenase Type 1 - The present invention relates to certain spirocyclic compounds that are inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases. | 07-30-2015 |
20150190378 | 1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase - The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. | 07-09-2015 |
20150175604 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 06-25-2015 |
20150148375 | BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 05-28-2015 |
20150148372 | BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 05-28-2015 |
20150148342 | BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 05-28-2015 |
20150133674 | PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR - The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders. | 05-14-2015 |
20150087632 | CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINES DERIVATIVES AS JAK INHIBITORS - The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: | 03-26-2015 |
20150065484 | SUSTAINED RELEASE DOSAGE FORMS FOR A JAK1 INHIBITOR - This invention relates to sustained release dosage forms comprising {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and doses and methods related thereto. | 03-05-2015 |
20150065447 | SURVIVAL BENEFIT IN PATIENTS WITH SOLID TUMORS WITH ELEVATED C-REACTIVE PROTEIN LEVELS - This application relates to methods of increasing survival or progression-free survival in a patient with a solid tumor, wherein the patient has an elevated serum concentration of C-reactive protein (CRP), by administering a JAK inhibitor or an inhibitor of IL-6 signaling to the patient, as well as methods of predicting survival benefit in these patients from such therapy. | 03-05-2015 |
20150057265 | FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 02-26-2015 |
20150025056 | SUBSTITUTED CYCLIC HYDROXAMATES AS INHIBITORS OF MATRIX METALLOPROTEINASES - The present invention provides compounds of the formula I: | 01-22-2015 |
20150017173 | ANTIBODIES TO HUMAN TRANSMEMBRANE PROTEINS - The invention provides human transmembrane proteins (HTMPN) and polynucleotides which identify and encode HTMPN. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with expression of HTMPN. | 01-15-2015 |
20150011540 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 01-08-2015 |
20140377292 | MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME - The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. | 12-25-2014 |
20140371216 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 12-18-2014 |
20140343030 | BIPYRAZOLE DERIVATIVES AS JAK INHIBITORS - The present invention provides compounds of Formula I: | 11-20-2014 |
20140315962 | 1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase - The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. | 10-23-2014 |
20140275127 | SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused derivatives of Formula I: | 09-18-2014 |
20140275031 | PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS - The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 09-18-2014 |
20140275030 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 09-18-2014 |
20140256941 | PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR - This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 09-11-2014 |
20140249132 | USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS - The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: | 09-04-2014 |
20140243360 | Heteroaryl Substituted Pyrrolo[2,3-B] Pyridines And Pyrrolo[2,3-B] Pyrimidines As Janus Kinase Inhibitors - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 08-28-2014 |
20140243308 | SUBSTITUTED IMIDAZOPYRIDAZINES AND BENZIMIDAZOLES AS INHIBITORS OF FGFR3 - The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases. | 08-28-2014 |
20140242086 | POLYNUCLEOTIDES ENCODING SIGNAL PEPTIDE-CONTAINING MOLECULES - The invention provides human signal peptide-containing proteins (HSPP) and polynucleotides which identify and encode HSPP. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with expression of HSPP. | 08-28-2014 |
20140221379 | N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: | 08-07-2014 |
20140200227 | THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 07-17-2014 |
20140200216 | BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 07-17-2014 |
20140187530 | AZA Spiro Alkane Derivatives as Inhibitors of Metalloproteases - The present invention provides a compound of Formula I or Formula II: | 07-03-2014 |
20140171409 | AZETIDINYL PHENYL, PYRIDYL OR PYRAZINYL CARBOXAMIDE DERIVATIVES AS JAK INHIBITORS - The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 06-19-2014 |
20140171405 | Fused Pyrazoles as FGFR Inhibitors - The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 06-19-2014 |
20140155404 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 06-05-2014 |
20140155377 | 3-CYCLOALKYLAMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: | 06-05-2014 |
20140155288 | METHODS FOR DIAGNOSING CANCER - The invention provides cDNAs which encodes a signal peptide-containing proteins. It also provides for the use of a cDNA, protein, and antibody in the diagnosis, prognosis, treatment and evaluation of therapies for cancer. The invention further provides vectors and host cells for the production of the protein and transgenic model systems. | 06-05-2014 |
20140135350 | SUSTAINED-RELEASE DOSAGE FORMS OF RUXOLITINIB - The present invention relates to sustained-release formulations and dosage forms of ruxolitinib, or a pharmaceutically acceptable salt thereof, which are useful in the treatment of Janus kinase-associated diseases such as myeloproliferative disorders. | 05-15-2014 |
20140121222 | PYRIMIDINONES AS PI3K INHIBITORS - The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases. | 05-01-2014 |
20140121198 | TRICYCLIC FUSED THIOPHENE DERIVATIVES AS JAK INHIBITORS - The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 05-01-2014 |
20140066448 | SUBSTITUTED DIAMINO-PYRIMIDINE AND DIAMINO-PYRIDINE DERIVATIVES AS PI3K INHIBITORS - The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R | 03-06-2014 |
20140057912 | PYRIMIDINE-4,6-DIAMINE DERIVATIVES AS PI3K INHIBITORS - The present invention provides pyrimidine-4,6-diamine derivatives of Formula (I): wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases. | 02-27-2014 |
20140056906 | SECRETED PROTEINS - The invention provides human secreted proteins (SECP) and polynucleotides which identify and encode SECP. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with aberrant expression of SECP. | 02-27-2014 |
20140045814 | PYRAZINE DERIVATIVES AS FGFR INHIBITORS - The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 02-13-2014 |
20140031344 | AZEPINE INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 01-30-2014 |
20140023663 | 1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3-Dioxygenase - The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. | 01-23-2014 |
20140018374 | Heteroaryl Substituted Pyrrolo[2,3-B]Pyridines And Pyrrolo[2,3-B]Pyrimidines As Janus Kinase Inhibitors - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 01-16-2014 |
20140005210 | Heteroaryl Substituted Pyrrolo[2,3-B] Pyridines And Pyrrolo[2,3-B] Pyrimidines As Janus Kinase Inhibitors | 01-02-2014 |
20140005166 | PIPERIDINYLCYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE DERIVATIVES AS JAK INHIBITORS | 01-02-2014 |
20130345224 | IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS - The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer. | 12-26-2013 |
20130345157 | HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROP- ANENITRILE - The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile. | 12-26-2013 |
20130324515 | IMIDAZOTRIAZINES AND IMIDAZOPYRIMIDINES AS KINASE INHIBITORS - The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. | 12-05-2013 |
20130253193 | PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS - The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases. | 09-26-2013 |
20130253191 | PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS - The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases. | 09-26-2013 |
20130253190 | PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS - The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases. | 09-26-2013 |
20130244999 | Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds of Formula I: | 09-19-2013 |
20130244927 | POLYNUCLEOTIDES ENCODING SIGNAL PEPTIDE-CONTAINING MOLECULES - The invention provides human signal peptide-containing proteins (HSPP) and polynucleotides which identify and encode HSPP. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with expression of HSPP. | 09-19-2013 |
20130243781 | SIGNAL PEPTIDE-CONTAINING PROTEINS - The invention provides cDNAs which encodes a signal peptide-containing proteins. It also provides for the use of a cDNA, protein, and antibody in the diagnosis, prognosis, treatment and evaluation of therapies for cancer. The invention further provides vectors and host cells for the production of the protein and transgenic model systems. | 09-19-2013 |
20130225556 | AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS - The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer. | 08-29-2013 |
20130224769 | METHODS OF USING CHEMOKINE PANEC-1 ANTIBODIES - The present invention provides nucleotide and amino acid sequences that identify and encode novel expressed chemokines (PANEC-1 and PANEC-2) from human pancreas cells. The present invention also provides for antisense molecules to the nucleotide sequences which encode PANEC-1 and PANEC-2, expression vectors for the production of purified PANEC-1 and PANEC-2, antibodies capable of binding specifically to PANEC-1 and PANEC-2, hybridization probes or oligonucleotides for the detection of PANEC-1- or PANEC-2-encoding nucleotide sequences, genetically engineered host cells for the expression of PANEC-1 and PANEC-2, diagnostic tests for chemokine activation based on PANEC-1- and PANEC-2-encoding nucleic acid molecules and antibodies capable of binding specifically to the protein. | 08-29-2013 |
20130190250 | Polynucleotides Encoding Human Signal Peptide-Containing Proteins - The invention provides a human signal peptide-containing proteins (SIGP) and polynucleotides which identify and encode SIGP. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for treating or preventing disorders associated with expression of SIGP. | 07-25-2013 |
20130177590 | N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE - The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases. | 07-11-2013 |
20130137681 | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 05-30-2013 |
20130123246 | MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME - The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. | 05-16-2013 |
20130116230 | 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to 3-aminopyrrolidine derivatives of the formula I: | 05-09-2013 |
20130096144 | ISOINDOLINONE AND PYRROLOPYRIDINONE DERIVATIVES AS AKT INHIBITORS - The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases. | 04-18-2013 |
20130060026 | PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR - This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 03-07-2013 |
20130059835 | HETEROCYCLYLAMINES AS PI3K INHIBITORS - The present invention provides heterocyclylamine derivatives of Formula I: | 03-07-2013 |
20130058942 | HUMAN BETA-ADRENERGIC RECEPTOR KINASE POLYPEPTIDE AND METHODS - Various embodiments of the invention provide human kinases and phosphatases (KPP) polypeptides and polynucleotides which identify and encode KPP. Embodiments of the invention also provide expression vectors, host cells, antibodies, agonists, and antagonists. Other embodiments provide methods for diagnosing, treating, or preventing disorders associated with aberrant expression of KPP. | 03-07-2013 |
20130045963 | Cyclohexyl Azetidine Derivatives as JAK Inhibitors - The present invention provides cyclohexyl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 02-21-2013 |
20130040973 | JAK PI3K/mTOR COMBINATION THERAPY - Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy. | 02-14-2013 |
20130018068 | SPIROCYCLES AS INHIBITORS OF 11-BETA HYDROXYL STEROID DEHYDROGENASE TYPE 1 - The present invention relates to certain spirocyclic compounds that are inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases. | 01-17-2013 |
20130018034 | AZETIDINYL PHENYL, PYRIDYL OR PYRAZINYL CARBOXAMIDE DERIVATIVES AS JAK INHIBITORS - The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 01-17-2013 |
20120329782 | AZEPINE INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-27-2012 |
20120301464 | JANUS KINASE INHIBITORS FOR TREATMENT OF DRY EYE AND OTHER EYE RELATED DISEASES - Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor. | 11-29-2012 |
20120295912 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 11-22-2012 |
20120122858 | LACTAM COMPOUNDS AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 05-17-2012 |
20120040964 | N-SUBSTITUTED PIPERIDINES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 02-16-2012 |
20120035172 | Purinone Derivatives as HM74A Agonists - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 02-09-2012 |
20120015928 | Amido Compounds And Their Use As Pharmaceuticals - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 01-19-2012 |
20110251215 | MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I: | 10-13-2011 |
20110212967 | IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS - The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer. | 09-01-2011 |
20110207754 | CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES AS JANUS KINASE INHIBITORS - The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders. | 08-25-2011 |
20110136781 | IMIDAZOTRIAZINES AND IMIDAZOPYRIMIDINES AS KINASE INHIBITORS - The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. | 06-09-2011 |
20110086810 | HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d] PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile. | 04-14-2011 |
20110082159 | METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYL- PROPANENITRILE - The present invention provides active metabolites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 04-07-2011 |
20100240671 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to substituted heterocyclic compounds of Formula I or XI: | 09-23-2010 |
20100190804 | MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I: | 07-29-2010 |
20100173901 | Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds of Formula I: | 07-08-2010 |
20100137401 | 2-METHYLPROP ANAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 06-03-2010 |
20100119503 | 3-AMINOCYCLOPENTANECARBOXAMIDES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention is directed to compounds of Formula I: | 05-13-2010 |
20090318405 | 4-PYRAZOLYL-N-ARYLPYRIMIDIN-2-AMINES AND 4-PYRAZOLYL-N-HETEROARYLPYRIMIDIN-2-AMINES AS JANUS KINASE INHIBITORS - The present invention provides substituted bicyclic heteroaryl compounds, including, for example, 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines that modulate the activity of kinases and are useful in the treatment of diseases related to activity of kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-24-2009 |
20090291946 | LACTAM COMPOUNDS AND THEIR USE AS PHARMACEUTICALS - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 11-26-2009 |
20090286778 | MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I: | 11-19-2009 |
20090286774 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 11-19-2009 |
20090124649 | AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES - The present invention provides a compound of Formula I or Formula II: | 05-14-2009 |
20090088446 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 04-02-2009 |
20090076269 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 03-19-2009 |
20080318991 | SPIROCYCLES AS INHIBITORS OF 11-BETA HYDROXYL STEROID DEHYDROGENASE TYPE 1 - The present invention relates to certain spirocyclic compounds that are inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases. | 12-25-2008 |
20080312259 | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-18-2008 |
20080312258 | METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides active metablites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-18-2008 |
20080255154 | Amido Compounds And Their Use As Pharmaceuticals - The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. | 10-16-2008 |
20080214546 | N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE - The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. | 09-04-2008 |