| ArQule, Inc. Patent applications |
| Patent application number | Title | Published |
|---|
| 20140031551 | Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions and Methods for Preparing and Using Same - The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. | 01-30-2014 |
| 20130281699 | Highly Pure Pyrroloquinolinyl-Pyrrole-2,5-Dione and Pyrroloquinolinyl-Pyrrolidine-2,5-Dione and Methods of Preparing Same - The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin- | 10-24-2013 |
| 20130150310 | 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 proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent. | 06-13-2013 |
| 20130011481 | Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Formulations and Methods for Preparing and Using Same - The present invention provides pyrroloquinolinyl-pyrrole-2,5-dione formulations and methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of the formulations containing pyrroloquinolinyl-pyrrole-2,5-dione compounds. | 01-10-2013 |
| 20120329793 | Substituted Imidazopyridinyl Compounds - The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 12-27-2012 |
| 20120259606 | Novel Kinase Inhibition Models and Their Uses - The present invention provides a c-Met inhibition model. The invention further provides a method to derive inhibition models for other kinases. The kinase inhibition models of the present invention can be used to design or screen for inhibitors for kinases. | 10-11-2012 |
| 20120165278 | Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same - The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 06-28-2012 |
| 20120108574 | Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds - The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 05-03-2012 |
| 20120021432 | Phosphorylated NF45 Biomarkers, Antibodies And Methods Of Using Same - The present invention relates to isolated phosphorylated NF45 peptides and isolated phosphorylation site-specific antibody or antigen-binding portion thereof that specifically binds a phosphorylated NF45 protein. The present invention also relates to methods of utilizing these antibodies to determine the therapeutic efficacy of a candidate compound and methods for screening for candidate compounds that increase the phosphorylation of NF45 protein in a cell. | 01-26-2012 |
| 20120015935 | Substituted Tetrahydropyrazolo-Pyrido-Azepine Compounds - The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 01-19-2012 |
| 20120004191 | Combinational Compositions And Methods For Treatment Of Cancer - The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent. | 01-05-2012 |
| 20110301194 | Method for Determining Treatment Efficacy - The present invention provides a method for determining the efficacy of a c-Met inhibitor in treating a cell proliferative disorder, comprising: a) administering to a subject in need thereof a therapeutically effective amount of the c-Met inhibitor, or a pharmaceutically acceptable salt, prodrug or metabolite thereof, either alone or in combination with a therapeutically effective amount of a second anti-proliferative agent; and b) measuring the concentration of hepatocyte growth factor (HGF) in the serum from the subject, wherein if the concentration of serum HGF does not decrease, or if the concentration of serum HGF increases, the c-Met inhibitor is efficacious in treating the cell proliferative disorder. | 12-08-2011 |
| 20110301160 | Inhibitors of P38 and Methods of Using the Same - In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity. | 12-08-2011 |
| 20110245236 | Substituted Benzo-Pyrido-Triazolo-Diazepine Compounds - The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 10-06-2011 |
| 20110217300 | Quinazolinone Compounds and Methods of Use Thereof - The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a quinazolinone compound of the present invention | 09-08-2011 |
| 20110172203 | Substituted Imidazopyridinyl-Aminopyridine Compounds - The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 07-14-2011 |
| 20110166137 | Substituted Naphthalenyl-Pyrimidine Compounds - The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 07-07-2011 |
| 20110166127 | Substituted Benzo-Pyrimido-Tetrazolo-Diazepine Compounds - The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 07-07-2011 |
| 20110160242 | Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same - The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin- | 06-30-2011 |
| 20110160237 | Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
| 20110160226 | Substituted Triazolo-Pyrimidine Compounds - The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
| 20110160215 | Substituted Triazolo-Pyrazine Compounds - The present invention relates to substituted triazolo-pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
| 20110160203 | Substituted Pyrrolo-Aminopyrimidine Compounds - The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
| 20110105470 | Novel Lapachone Compounds And Methods of Use Thereof - The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as β-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione). | 05-05-2011 |
| 20110034513 | Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production - Compounds of Formula (I), | 02-10-2011 |
| 20100311754 | 1,4-Disubstituted Naphthalenes as Inhibitors of P38 Map Kinase - Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof. | 12-09-2010 |
| 20100297075 | COMBINATIONAL COMPOSITIONS AND METHODS FOR TREATMENT OF CANCER - The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent. | 11-25-2010 |
| 20100261710 | HDAC Inhibitors - The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention. | 10-14-2010 |
| 20100249153 | SUBSTITUTED INDOLO-PIPERIDINE COMPOUNDS - The present invention relates to substituted indolo-piperidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-piperidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100249127 | SUBSTITUTED INDOLO-PYRIDINONE COMPOUNDS - The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100249120 | SUBSTITUTED PYRAZOLO-PYRROLO-PYRIDINE-DIONE COMPOUNDS - The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100249115 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100249110 | SUBSTITUTED PYRAZOLO-PYRIMIDINE COMPOUNDS - The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100249109 | SUBSTITUTED TETRAHYDROPYRAZOLO-PYRIDO-AZEPINE COMPOUNDS - The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100249108 | SUBSTITUTED DIPYRIDO-PYRIMIDO-DIAZEPINE AND BENZO-PYRIDO-PYRIMIDO COMPOUNDS - The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
| 20100239526 | SUBSTITUTED IMIDAZOLYL-5,6-DIHYDROBENZO[N]ISOQUINOLINE COMPOUNDS - The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 09-23-2010 |
| 20100239525 | SUBSTITUTED 5,6-DIHYDRO-6-PHENYLBENZO[F]ISOQUINOLIN-2-AMINE COMPOUNDS - The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 09-23-2010 |
| 20100221251 | Compositions and Methods for Treatment of Cancer - The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention. | 09-02-2010 |
| 20100183603 | Compositions and Methods for the Treatment of Cancer - The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention. (Ia) (Ib) (IIa) (IIIb) Where U is independently selected from: (I) or (II) | 07-22-2010 |
| 20100183600 | RAF Inhibitors and Their Uses - The present invention provides imidazooxazole and imidazothiazole compounds and their syntheses. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAF | 07-22-2010 |
| 20100178291 | Pyrrolidinone, Pyrrolidine-2, 5-Dione, Pyrrolidine and Thiosuccinimide Derivatives, Compositions and Methods for Treatment of Cancer - The present invention relates to pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosucciniroide compounds of formulae (I)-(IV), and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compound of the present invention. | 07-15-2010 |
| 20100172867 | SUBSTITUTED 1H-PYRAZOLO[3,4-D]PYRIMIDINE-6-AMINE COMPOUNDS - The present invention relates to substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 07-08-2010 |
| 20100120725 | Substituted Phenylsulfonamide Inhibitors of Beta Amyloid Production - Compounds of Formula I, | 05-13-2010 |
| 20100022594 | HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION - Compounds of Formula (I), | 01-28-2010 |
| 20090226395 | Pharmaceutical compositions of beta-lapachone and beta-lapachone analogs with improved tumor targeting potential - The present invention relates to polymer-modified quinone-containing and carbonyl-containing therapeutic agents, including polymer-modified β-lapachone compounds, and methods of treating cancer by administering the polymer-modified therapeutic agents to a subject. Polymer-modification of therapeutic agents, such as β-lapachone compounds, provides effective transport of polymer-modified therapeutic agents to tumor cells or tumor tissues by exploiting the EPR effect in tumor tissues. | 09-10-2009 |
| 20090176801 | NOVEL LAPACHONE COMPOUNDS AND METHODS OF USE THEREOF - The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions. | 07-09-2009 |
| 20090136499 | RAF Inhibitors and Uses Thereof - The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAF | 05-28-2009 |
| 20090130117 | Substituted Tetrazole Compounds and Uses Thereof - The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention. | 05-21-2009 |
| 20090130097 | Quinazolinone Compounds and Methods of Use Thereof - The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a quinazolinone compound of the present invention | 05-21-2009 |
