Exelixis, Inc. Patent applications |
Patent application number | Title | Published |
20160022662 | Cabozantinib Dosage Form and Use in the Treatment of Cancer - This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer. | 01-28-2016 |
20160000772 | Methods of Using C-Met Modulators - Methods of treating cancer by administering a compound of Formula I, | 01-07-2016 |
20140378436 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 12-25-2014 |
20140303172 | Phosphatidylinositol 3-Kinase Inhibitors for the Treatment of Lymphoproliferative Malignancies - Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein. | 10-09-2014 |
20140303151 | Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 10-09-2014 |
20140302012 | Combination Therapies for Treating Hematologic Malignancies Using Pyridopyrimidinone Inhibitors of PI3K/mTOR with Bendamustine and/or Rituximab - The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of Formula (I): in combination with one or both of bendamustine and rituximab. | 10-09-2014 |
20140296265 | Method of Treating Lymphoma Using Pyridopyrimidinone Inhibitors of PI3K/mTOR - The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I: | 10-02-2014 |
20140275527 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 09-18-2014 |
20140271665 | Combinations of Kinase Inhibitors for the Treatment of Cancer - The present invention provides methods of treating cancer by administering a compound of formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with an inhibitor that targets HER2 and/or HER3. | 09-18-2014 |
20140200242 | Processes for Preparing Quinoline Compounds and Pharmaceutical Compositions Containing Such Compounds - The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2. | 07-17-2014 |
20140186407 | C-Met Modulator Pharmaceutical Compositions - Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed. | 07-03-2014 |
20140179736 | Method of Treating Cancer and Bone Cancer Pain - This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I. | 06-26-2014 |
20140155378 | c-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 06-05-2014 |
20140121239 | METHOD OF TREATING LUNG ADENOCARCINOMA - This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: | 05-01-2014 |
20140107100 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture | 04-17-2014 |
20140100215 | Methods of Using PI3K and MEK Modulators - The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K. | 04-10-2014 |
20140080810 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: (I) and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens. | 03-20-2014 |
20140066444 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF. | 03-06-2014 |
20140066431 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens. | 03-06-2014 |
20140058103 | Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 02-27-2014 |
20140057908 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF. | 02-27-2014 |
20140045825 | Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 02-13-2014 |
20140024637 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 01-23-2014 |
20140018347 | BENZOXAZEPINES AS INHIBITORS OF mTOR AND METHODS OF THEIR USE AND MANUFACTURE - The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural Formula (I) wherein the variables are as defined herein. | 01-16-2014 |
20130343988 | Pyrido [2, 3-D] pyrimidin-7-one compounds as inhibitors of P13K-Alpha for the treament of cancer - The invention is directed to Compounds of Formula (I). The invention provides compounds that inhibit, regulate, and/or modulate P13K that are useful in the treatment of hyperproliferative diseases, such as cancer. | 12-26-2013 |
20130330377 | C-Met Modulator Pharmaceutical Compositions - Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed. | 12-12-2013 |
20130252940 | c-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 09-26-2013 |
20130212716 | PFKs as Modifiers of the IGFR Pathway and Methods of Use - Human PFK genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of PFK are provided. | 08-15-2013 |
20130172371 | Methods of Treating Cancer Using Pyridopyrimidinone Inhibitors of PI3K and mTOR in Combination with Autophagy Inhibitors - The invention provides compounds of Formula I: | 07-04-2013 |
20130165440 | JAK1 Inhibitors - JAK1 inhibitors of structural formula (I), wherein Ar | 06-27-2013 |
20130143881 | Hydrated Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxam- ide - This invention relates crystalline hydrates of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Compound (I). The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline hydrate of Compound (I) and a pharmaceutically acceptable excipient. | 06-06-2013 |
20130030172 | Methods of Preparing Quinoline Derivatives - Methods of preparing compounds of formula i(1): | 01-31-2013 |
20120302545 | Method of Using PI3K and MEK Modulators - The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K. | 11-29-2012 |
20120282179 | Methods of Using C-Met Modulators - Methods of treating cancer by administering a compound of Formula I, | 11-08-2012 |
20120270872 | Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxam- ide - This invention relates to three crystalline forms of N—[3-fluoro-4-((6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl|oxy)phenyl]—N′—(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. Compound (I), designated as Form A, Form B, and Form C. The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline form of Compound (I) and a pharmaceutically acceptable excipient. | 10-25-2012 |
20120258953 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK-transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer. | 10-11-2012 |
20120252840 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1. | 10-04-2012 |
20120184523 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 07-19-2012 |
20120107827 | PSMCs As Modifiers of the RB Pathway and Methods of Use - Human PSMC genes are identified as modulators of the RB pathway, and thus are therapeutic targets for disorders associated with defective RB function. Methods for identifying modulators of RB, comprising screening for agents that modulate the activity of PSMC are provided. | 05-03-2012 |
20120070368 | Methods of Using C-Met Modulators - Disclosed are methods of treating cancer by administering a compound of Formula I, | 03-22-2012 |
20120064025 | Quinazolinone Modulators Of Nuclear Receptors - Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors. | 03-15-2012 |
20120035212 | (L)-Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide - Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane- | 02-09-2012 |
20120022065 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 01-26-2012 |
20110301188 | Synergistic Effects Between Sphingosine-1-Phosphate Receptor Antagonists and Antimicrotubule Agents - This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent. | 12-08-2011 |
20110301128 | Pyrrole Derivatives As Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 12-08-2011 |
20110288076 | Sphingosine-1-Phosphate Receptor Antagonists - This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists. | 11-24-2011 |
20110263673 | Atropisomers of (Hydroxyalkyl) Pyrrole Derivatives - The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R | 10-27-2011 |
20110263558 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 10-27-2011 |
20110263544 | 1-Phenylpyrrole Derivatives - The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R | 10-27-2011 |
20110237608 | Pyridopyrimidinone Inhibitors of PI3Kalpha - The invention is directed to Compounds of Formula I: | 09-29-2011 |
20110207712 | Phosphatidylinositol 3-Kinase Inhibitors And Methods Of Their Use - The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. | 08-25-2011 |
20110201599 | CDK Modulators - A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof. | 08-18-2011 |
20110167505 | GFATS As Modifiers of the AXIN Pathway and Methods of Use - Human GFAT genes are identified as modulators of the Axin pathway, and thus are therapeutic targets for disorders associated with defective Axin function. Methods for identifying modulators of Axin, comprising screening for agents that modulate the activity of GFAT are provided. | 07-07-2011 |
20110159508 | GFATS as Modifiers of the P53 Pathway and Methods of Use - Human GFAT genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of GFAT are provided. | 06-30-2011 |
20110144128 | Heterocyclic Carboxamide Compounds as Steroid Nuclear Receptors Ligands - Heterocyclic carboxamide compounds are described herein as being useful in modulating the activity of steroid nuclear receptors. Pharmaceutical compositions containing the compounds, methods of using the compounds and processes for making the compounds are also described. | 06-16-2011 |
20110135629 | EYA2S As Modifiers of the PTEN/AKT Pathway and Methods of Use - Human MPTENAKT genes are identified as modulators of the PTEN/AKT pathway, and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT, comprising screening for agents that modulate the activity of MPTENAKT are provided. | 06-09-2011 |
20110123434 | COMBINATION THERAPIES COMPRISING QUINOXALINE INHIBITORS OF P13K-ALPHA FOR USE IN THE TREATMENT OF CANCER - The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments. | 05-26-2011 |
20110111402 | KIFS as Modifiers of the RHO Pathway and Methods of Use - Human KIF23 genes are identified as modulators of the RHO pathway, and thus are therapeutic targets for disorders associated with defective RHO function. Methods for identifying modulators of RHO, comprising screening for agents that modulate the activity of KIF23 are provided. | 05-12-2011 |
20110077233 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 03-31-2011 |
20110071145 | Raf Modulators And Methods Of Use - The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention. | 03-24-2011 |
20110059066 | PAKs as Modifiers of the CHK Pathway and Methods of Use - Human PAK genes are identified as modulators of the CHK pathway, and thus are therapeutic targets for disorders associated with defective CHK function. Methods for identifying modulators of CHK, comprising screening for agents that modulate the activity of PAK are provided. | 03-10-2011 |
20110033853 | CSNKS As Modifiers of the RAC Pathway and Methods of Use - Human CSNK genes are identified as modulators of the RAC pathway, and thus are therapeutic targets for disorders associated with defective RAC function. Methods for identifying modulators of RAC, comprising screening for agents that modulate the activity of CSNK are provided. | 02-10-2011 |
20110021525 | P70S6 Kinase Modulators and Method of Use - The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. | 01-27-2011 |
20100331295 | MODULATORS OF LXR - Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. | 12-30-2010 |
20100325743 | Marks as modifiers of the p53 pathway and methods of use - Human MARK genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of MARK are provided. | 12-23-2010 |
20100305093 | Inhibitors of mTOR and Methods of Making and Using - The invention is directed to Compounds of Formula I: | 12-02-2010 |
20100298290 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: | 11-25-2010 |
20100275275 | HADHs as Modifiers of the p21 Pathway and Methods of Use - Human HADH genes are identified as modulators of the p21 pathway, and thus are therapeutic targets for disorders associated with defective p21 function. Methods for identifying modulators of p21, comprising screening for agents that modulate the activity of HADH are provided. | 10-28-2010 |
20100249096 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 09-30-2010 |
20100249071 | Modulators of S1P and Methods of Making And Using - The invention is directed to Compounds of Formula I: | 09-30-2010 |
20100209420 | METHODS OF TREATING CANCER USING PYRIDOPYRIMIDINONE INHIBITORS OF P13K ALPHA - The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments. | 08-19-2010 |
20100183583 | GALK1S AS MODIFIERS OF THE PTEN/AKT PATHWAY AND METHODS OF USE - Human GALK1 genes are identified as modulators of the PTEN/AKT pathway, and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT, comprising screening for agents that modulate the activity of GALK1 are provided. | 07-22-2010 |
20100173824 | Azepinoindole Derivatives As Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 07-08-2010 |
20100160369 | S1P1 Agonists and Methods of Making And Using - The invention is directed to Compounds of Formula I: | 06-24-2010 |
20100159470 | SCDs As Modifiers of the p53 Pathway and Methods of Use - Human SCD genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of SCD are provided. | 06-24-2010 |
20100150827 | PYRIDO [2, 3-D] PYRIMIDIN-7-ONE COMPOUNDS AS INHIBITORS OF P13K-ALPHA FOR THE TREATMENT OF CANCER - The invention is directed to a Compound of Formula I, II, or III. The invention provides compounds that inhibit, regulate, and/or modulate PI3K that are useful in the treatment of hyperproliferatives diseases, such as cancer. | 06-17-2010 |
20100144770 | Pyrimidinones as Casein Kinase II (CK2) Modulators - A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways. | 06-10-2010 |
20100136136 | JAK-2 Modulators and Methods of Use - This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention. | 06-03-2010 |
20100135954 | 6-Phenylpyrimidinones as PIM Modulators - A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R | 06-03-2010 |
20100122354 | CDC6S AS MODIFIERS OF THE PTEN/AKT PATHWAY AND METHODS OF USE - Human CDC6 genes are identified as modulators of the PTEN/AKT pathway, and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT, comprising screening for agents that modulate the activity of CDC6 are provided. | 05-13-2010 |
20100105675 | 11 BETA-HSD1 MODULATORS -
A compound according to Formula I:
| 04-29-2010 |
20100087456 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3K-ALPHA and mTOR - The invention is directed to Compounds of Formula I: | 04-08-2010 |
20100075964 | IMIDAZOLE BASED LXR MODULATORS - Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R | 03-25-2010 |
20100075947 | Methods of Using PI3K and MEK Modulators - The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K. | 03-25-2010 |
20100069367 | LXR and FXR Modulators - Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R | 03-18-2010 |
20090326218 | Azepinoindole and Pyridoindole Derivatives as Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 12-31-2009 |
20090298830 | 4-Aryl-2-Amino-Pyrimidnes or 4-Aryl-2-Aminoalkyl-Pyrimidines as Jak-2 Modulators and Methods of Use - This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R | 12-03-2009 |
20090247559 | Benzofuropyrimidinones - A compound according to formula I: | 10-01-2009 |
20090247515 | 11 Beta-HSD1 Modulators - A compound according to Formula A: | 10-01-2009 |
20090232828 | Methods of Using IGFIR and ABL Kinase Modulators - The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell transplantation, and one or more chemotherapeutic agent(s). | 09-17-2009 |
20090203577 | Azepinoindole Derivatives As Pharmaceutical Agents - The present invention relates to compounds of formula I, which exhibit affinity for the farnesoid X receptor. | 08-13-2009 |
20090202563 | C20ORF23 as modifier of the IGFR pathway and methods of use - Human C20ORF23 genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of C20ORF23 are provided. | 08-13-2009 |
20090197870 | Pharmaceutical Compositions - Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists, or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as described above in the Summary of the Invention, are compounds of formula (I). | 08-06-2009 |
20090186905 | ANAPLASTIC LYMPHOMA KINASE MODULATORS AND METHODS OF USE - The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R | 07-23-2009 |
20090170896 | c-Met modulators and methods of use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 07-02-2009 |
20090156576 | Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases - Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer. | 06-18-2009 |
20090149413 | RORS as Modifiers of the p21 Pathway and Methods of Use - Human ROR genes are identified as modulators of the p21 pathway, and thus are therapeutic targets for disorders associated with defective p21 function. Methods for identifying modulators of p21, comprising screening for agents that modulate the activity of ROR are provided. | 06-11-2009 |
20090142272 | Pfks as modifiers of the igfr pathway and methods of use - Human PFK genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of PFK are provided. | 06-04-2009 |
20090105299 | c-MET MODULATORS AND METHODS OF USE - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 04-23-2009 |
20090105211 | INHIBITORS OF HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I | 04-23-2009 |
20090068186 | MAP3Ks as modifiers of the p53 pathway and methods of use - Human MAP3K genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of MAP3K are provided. | 03-12-2009 |
20090062274 | Pyridopyrimidinone inhibitors of pi3kalpha - The invention is directed to Compounds of Formula I and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 03-05-2009 |
20090053239 | ACACS As Modifiers of the IGF Pathway and Methods of Use - Human MPTEN genes are identified as modulators of the PTEN pathway, and thus are therapeutic targets for disorders associated with defective PTEN function. Methods for identifying modulators of PTEN, comprising screening for agents that modulate the activity of MPTEN are provided. | 02-26-2009 |
20090042918 | Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3 - Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R | 02-12-2009 |
20090028844 | GALNTS AS MODIFIERS OF THE IGFR PATHWAY AND METHODS OF USE - Human MIGFR genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of MIGFR are provided. | 01-29-2009 |
20090025096 | P4HAS AS MODIFIERS OF THE IGFR PATHWAY AND METHODS OF USE - Human P4HA genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of P4HA are provided. | 01-22-2009 |
20090022737 | ALDOS AS MODIFIERS OF THE IGF PATHWAY AND METHODS OF USE - Human ALDO genes are identified as modulators of the IGF pathway, and thus are therapeutic targets for disorders associated with defective IGF function. Methods for identifying modulators of IGF, comprising screening for agents that modulate the activity of ALDO are provided. | 01-22-2009 |
20090019558 | PGDS AS MODIFIERS OF THE PTEN PATHWAY AND METHODS OF USE - Human PGD genes are identified as modulators of the PTEN pathway, and thus are therapeutic targets for disorders associated with defective PTEN function. Methods for identifying modulators of PTEN, comprising screening for agents that modulate the activity of PGD are provided. | 01-15-2009 |
20090013416 | PDES AS MODIFIERS OF THE IGFR PATHWAYS AND METHODS OF USE - Human PDE genes are identified as modulators of the IGFR pathway and thus are therapeutic targets for disorders associated with defective IGFR function Methods for identifying modulators of IGFR comprising screening for agents that modulate the activity of PDE are provided | 01-08-2009 |
20090004180 | Kifs as Modifiers of the Rho Pathway and Methods of Use - Human KIF23 genes are identified as modulators of the RHO pathway, and thus are therapeutic targets for disorders associated with defective RHO function. Methods for identifying modulators of RHO, comprising screening for agents that modulate the activity of KIF23 are provided. | 01-01-2009 |
20080317738 | Mylks as Modifiers of Branching Morphogenesis and Methods of Use - Human MYLK genes are identified as modulators of branching morphogenesis, and thus are therapeutic targets for disorders associated with defective branching morphogenesis function. Methods for identifying modulators of branching morphogenesis, comprising screening for agents that modulate the activity of MYLK are provided. | 12-25-2008 |
20080274122 | Plks as Modifiers of the Beta Catenin Pathway and Methods of Use - Human PLK genes are identified as modulators of the beta catenin pathway, and thus are therapeutic targets for disorders associated with defective beta catenin function. Methods for identifying modulators of beta catenin, comprising screening for agents that modulate the activity of PLK are provided. | 11-06-2008 |
20080263684 | Pik4ca As Modifier of the Rac Pathway and Methods of Use - Human PIK4CA genes are identified as modulators of the RAC pathway, and thus are therapeutic targets for disorders associated with defective RAC function. Methods for identifying modulators of RAC, comprising screening for agents that modulate the activity of PIK4CA are provided. | 10-23-2008 |
20080249079 | Pyrimidine Derivatives As Kinase Modulators and Method of Use -
The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR | 10-09-2008 |
20080241131 | SPHKS as modifiers of the p53 pathway and methods of use - Human SPHK genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of SPHK are provided. | 10-02-2008 |
20080234270 | Pyrrole Derivatives As Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 09-25-2008 |