Class / Patent application number | Description | Number of patent applications / Date published |
514082000 | Quinolinyl or isoquinolinyl (including hydrogenated) | 57 |
20080300222 | Phosphoantigen Salts Of Organic Bases And Methods For Their Crystallization - The invention provides novel phosphoantigen salts and novel crystalline phases of phosphoantigens salts, that the latter including non-solvated polymorphs, and solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, novel phosphoantigen crystalline phases. Methods of using such compositions for the treatment of disease, immunostimulatory or immune response modifying use are also provided. The invention also provides method for obtaining phosphoantigen crystals as well as highly pure phosphoantigen compositions. | 12-04-2008 |
20080318906 | BISPHOSPHONATE COMPOUNDS AND METHODS FOR BONE RESORPTION DISEASES, CANCER, BONE PAIN, IMMUNE DISORDERS, AND INFECTIOUS DISEASES - Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as | 12-25-2008 |
20090036409 | Novel inhibitors of chymase - The present invention is directed to a compound of formula (I), | 02-05-2009 |
20090099133 | Isoquinolines Derivatives as Igf-1R Inhibitors - Compounds of the formula (I) were synthesized. They were found to down-regulate or inhibit the expression or function of the IGF-1 receptor. | 04-16-2009 |
20090099134 | TREATMENT OF DNA DAMAGE RELATED DISORDERS - The present invention provides methods and compositions for prophylaxis and treatment of a variety of disorders including DNA damage related disorders, cancer, ischemia, oxidative stress, atherosclerosis, and stroke using a chloroquine compound. | 04-16-2009 |
20090197834 | QUINOLONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - [Problem] To provide a compound having excellent platelet aggregation inhibitory activity. | 08-06-2009 |
20090253655 | QUINOLINONE FARNESYL TRANSFERASE INHIBITORS FOR THE TREATMENT OF SYNUCLEINOPATHIES AND OTHER INDICATIONS - Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. | 10-08-2009 |
20090275537 | Certain chemical entities, compositions, and methods - Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described. | 11-05-2009 |
20100022477 | FUSED AROMATIC PTP-1B INHIBITORS - The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes. | 01-28-2010 |
20100048510 | DISSOLUTION OF AMYLOID FIBRILS BY FLAVONOIDS AND OTHER COMPOUNDS - Methods for disrupting amyloid fibrils in a subject, comprising combining an effective amount of a β-2 microglobulin fibril disrupting compound with a medium associated with the subject, are disclosed. The invention also relates to combining the β-2 microglobulin fibril disrupting compound ex vivo with the blood during dialysis treatment of an animal. It also relates to methods for determining which compounds are effective at disrupting amyloid fibrils in a medium. | 02-25-2010 |
20100075926 | ACTIVATION OF HISTONE DEACETYLASE 1 (HDAC1) PROTECTS AGAINST DNA DAMAGE AND INCREASES NEURONAL SURVIVAL - The invention provides methods and compounds for the treatment of neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (Amyotrophic Lateral Sclerosis), traumatic brain injury, ischemic brain injury or a stroke. In one aspect the compounds are HDAC1 activators. Exemplary HDAC1 activators include metal chelators, iron chelators, deferoxamin, flavonoids, compounds comprising a catechol moity, ginkgetin K, Chembridge 5104434, sciadopilysin, tetrahydrogamboic acid, TAM-11, LY 235959, CGS 19755, SK&F 97541, etidronic acid, levonordefrin, methyldopa, ampicillin trihydrate, D-aspartic acid, gamma-D-glutamylaminomethylsulfonic acid, phenazopyridine to hydrochloride, oxalamine citrate salt, podophyllotoxin, SK&F 97541, (+-)-4-amino-3-(5-chloro-2-thienyl)-butanoic acid, (RS)-(tetrazol-5-yl) glycine, R(+)-SKF-81297, gambogic acid, and derivatives thereof. | 03-25-2010 |
20100152138 | CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT - Disclosed are compounds of the formula | 06-17-2010 |
20100168065 | QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 07-01-2010 |
20100204183 | Substituted Phosphonates and Their Use In Decreasing Amyloid Aggregates - The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease. | 08-12-2010 |
20100240614 | Indole Compounds Bearing Aryl or Heteroaryl Groups Having Sphingosine 1-Phosphate (S1P) Receptor Biological Activity - The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 09-23-2010 |
20100261677 | ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS - The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups R | 10-14-2010 |
20100317624 | HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF - Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 12-16-2010 |
20100323989 | PHARMACEUTICAL COMBINATIONS USEFUL FOR TREATING HCV - This invention relates to combinations of Compound 1 and Compound 2 which are useful for treating hepatitis C virus infection. | 12-23-2010 |
20110015156 | HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHOLOGICAL DISORDERS - Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed. | 01-20-2011 |
20110082112 | ANTIVIRAL PHOSPHINATE COMPOUNDS - The invention is related to a method of treating disorders associated with hepatitis C by administering to an individual a pharmaceutical composition which comprises a therapeutically effective amount of an anti-viral phosphinate compound. | 04-07-2011 |
20110172193 | PRO-DRUGS OF (E)-7-(3-(2-AMINO-1-FLUOROETHYLIDENE)PIPERIDIN-1-YL)-1-CYCLOPROPYL-6-FLUO- RO-8-METHOXY-4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXYLIC ACID - The present invention is directed to pro-drugs of (E)-7-(3-(2-amino-1-fluoroethylidene)piperidin-1-yl)-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, pharmaceutical compositions containing them and the use of said pro-drugs and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes. | 07-14-2011 |
20120040936 | CYCLIC COMPOUND HAVING SUBSTITUTED PHENYL GROUP - Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: | 02-16-2012 |
20120094958 | QUINOLINES AS INHIBITORS OF FARNESYL PYROPHOSPHATE SYNTHASE - The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof. | 04-19-2012 |
20120135964 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described. | 05-31-2012 |
20120178717 | 4-QUINOLINEMETHANOLS AS ANTI-MALARIAL AGENTS - The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases. | 07-12-2012 |
20120264715 | SUBSTITUTED BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 10-18-2012 |
20120264716 | PHENYL BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 10-18-2012 |
20130053348 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described. | 02-28-2013 |
20130065857 | NOVEL DXR INHIBITORS FOR ANTIMICROBIAL THERAPY - The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In specific embodiments, the compositions are electron-deficient heterocyclic rings. | 03-14-2013 |
20130096089 | Heterocyclic Compounds for the Treatment of Neurological and Psychological Disorders - Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed. | 04-18-2013 |
20130131018 | SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS - The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds. | 05-23-2013 |
20130150330 | DECOQUINATE PRODRUGS - A compound can include a structure having decoquinate coupled to a prodrug moiety, or derivative or isomer or pharmaceutically acceptable salt thereof. The compound can be a decoquinate prodrug. The decoquinate prodrug can have a structure of any of the formulae described herein. The decoquinate prodrug can be synthesized in any manner, such as a synthetic method that includes Scheme 1A or Scheme 1B and Schemes 2, 3, and/or 4. The decoquinate prodrug can be prepared into a pharmaceutical composition with a pharmaceutically acceptable carrier, such as an aqueous composition. The decoquinate prodrug can be used for inhibiting or treating a parasitic infection, such as a malarial infection or a coccidian infection. | 06-13-2013 |
20130157980 | SUBSTITUTED INDOLE DERIVATIVES - The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. | 06-20-2013 |
20130203703 | 1,2-DIHYDRO-4-HYDROXY-2-OXO-QUINOLINE-3-CARBOXANILIDES AS AHR ACTIVATORS - The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment. | 08-08-2013 |
20130303484 | Prodrugs of Modulators of ABC Transporters - The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-14-2013 |
20130331359 | Phosphorus-Containing Group-Substituted Quinoline, Its Preparation process, medical composition containing the compounds and application - Phosphorus-containing group-substituted quinolines of formula (I) are provided in the present invention. The preparation process and application of the compound, and formulation comprising phosphorus-containing group-substituted quinolines are also disclosed. The compounds are protein kinase inhibitor and can be used for treating protein kinase abnormal activity-associated diseases, such as tumor, etc. | 12-12-2013 |
20130338108 | PHENYL BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 12-19-2013 |
20130338109 | SUBSTITUTED BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 12-19-2013 |
20140018320 | TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY - There are disclosed compound of Formula (1): A | 01-16-2014 |
20140080788 | NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS - Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R | 03-20-2014 |
20140100195 | Heterobicyclic sphingosine 1-phosphate analogs - Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors. | 04-10-2014 |
20140107074 | COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS - The present disclosure is directed to compounds of the structure (X): | 04-17-2014 |
20140179634 | SUBSTITUTED INDOLE DERIVATIVES - The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. | 06-26-2014 |
20140200199 | 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. | 07-17-2014 |
20140243289 | PRODRUGS OF MODULATORS OF ABC TRANSPORTERS - The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 08-28-2014 |
20140274960 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments. | 09-18-2014 |
20150031648 | PHOSPHATE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I): | 01-29-2015 |
20150045325 | FUSED AROMATIC PTP-1B INHIBITORS - The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes. | 02-12-2015 |
20150119365 | NOVEL ACTIVATORS OF GLUCOKINASE - The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same. | 04-30-2015 |
20150148313 | MACROCYCLIC FACTOR VIIA INHIBITORS - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments. | 05-28-2015 |
20150320875 | Prodrugs of NH-Acidic Compounds: Ester, Carbonate, Carbamate and Phosphonate Derivatives - The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment. | 11-12-2015 |
20150336898 | Prodrugs of Modulators of ABC Transporters - The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-26-2015 |
20150374724 | ARENE RUTHENIUM (II) DERIVATIVES CONTAINING IMINOPHOSPHORANE LIGANDS AND THEIR USE IN CANCER THERAPY - A method for providing a therapeutic benefit for a subject having a cancer is provided. A compound with an arene ruthenium (II) compound with an iminophosphorane ligand is administered to the subject. | 12-31-2015 |
20160024060 | BENZOTHIOPHENE DERIVATIVE - [Problem to be Solved] | 01-28-2016 |
20160130288 | OXAZOLIDINONE-QUINOLONE HYBRID ANTIBACTERIALS FOR THE PARENTERAL TREATMENT OR PROPHYLAXIS OF BACTERIAL DISEASES - The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials. | 05-12-2016 |
20160137616 | BICYCLIC 1,3,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE RECEPTORS' MODULATORS - The present invention relates to bicyclic 1,3,4-oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 05-19-2016 |
20160145279 | STAT6 INHIBITORS - The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer. | 05-26-2016 |