| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 514416000 | The ring nitrogen is bonded directly to nonshared ring carbons of the five-membered hetero ring (e.g., isoindole, etc.) | 53 |
| 20080200531 | CDKI pathway inhibitors as inhibitors of tumor cell growth - The invention provides new methods for inhibiting the CDKI pathway and specifically inhibiting tumor cell growth. The invention further provides new and specific inhibitors of tumor cell growth, as well as means for discovery of additional such inhibitors. The present inventors have surprisingly discovered that Cyclin-Dependent Kinase 3 (CDK3) is specifically required for tumor cell growth, in contrast to other members of the CDK family. | 08-21-2008 |
| 20080221196 | PHARMACEUTICALLY ACTIVE ISOINDOLINE DERIVATIVES - Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an α-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNFα and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)2-methylsulfonylethyl]4,5-diaminoisoindoline-1,3-dione. | 09-11-2008 |
| 20080234358 | NAPHTHALENE DERIVATIVES - A compound of formula (I) | 09-25-2008 |
| 20090030063 | Combined pharmaceutical preparation for treatment of type 2 diabetes - For controlling the condition of type 2 diabetes, a pharmaceutical including a combination of mitiglinide, a pharmacologically acceptable salt thereof or a hydrate thereof and an α-glucosidase inhibitor such as voglibose or acarbose, and a therapeutic method using the pharmaceutical are provided. The pharmaceutical according to the present invention has an extremely strong effect of decreasing a morning fasting blood glucose level, a postprandial blood glucose level and HbA | 01-29-2009 |
| 20090030064 | Sugar-coated preparation - A preparation wherein an active ingredient unstable to oxygen is stabilized by coating a portion containing the active ingredient unstable to oxygen with a sugar-coated layer containing (1) sugar alcohol as a sugar-coating base material and (2) a binder is provided. | 01-29-2009 |
| 20090176858 | HCV PROTEASE INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 07-09-2009 |
| 20090203761 | PROCESS FOR PREPARING (3-OXO-2,3-DIHYDRO-1H-ISOINDOL-1-YL) ACETYLGUANIDINE DERIVATIVES - The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I | 08-13-2009 |
| 20090239926 | METHODS FOR THE TREATMENT OF PSORIASIS OR PSORIATIC ARTHRITIS USING CYCLOPROPYL-N-CARBOXAMIDE - Methods of treating, managing or preventing psoriasis or psoriatic arthritis are disclosed. Specific methods encompass the administration of cyclopropyl-N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindoline-4-yl}carboxamide, alone or in combination with a second active agent. Pharmaceutical compositions and single unit dosage forms are also disclosed. | 09-24-2009 |
| 20100076051 | ISOINDOLINONE KINASE INHIBITORS - Compounds having the formula | 03-25-2010 |
| 20100144825 | Renin Inhibitors - The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors. | 06-10-2010 |
| 20100210705 | Pyrrole and Isoindole Carboxamide Derivatives as P2X7 Modulators - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: | 08-19-2010 |
| 20100267800 | N-Alkyl-Hydroxamic Acid-Isoindolyl Compounds and Their Pharmaceutical Uses - The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4. | 10-21-2010 |
| 20110172284 | METHODS FOR TREATING SPINAL MUSCULAR ATROPHY - Described herein are methods for the identification or validation of compounds capable of causing ribosomal frameshifting and the use of said compounds to produce a stabilized SMNΔEx7 protein and treat Spinal Muscular Atrophy. | 07-14-2011 |
| 20110213005 | METHODS FOR TREATING VIRAL INFECTIONS - The present invention relates to compounds that modulate ribosomal frameshifting and nucleic acid constructs for use in methods for identifying or validation such compounds. In particular, the present invention relates to the use of nucleic acid constructs to identify or validate compounds capable of modulating the efficiency of programmed ribosomal frameshifting and the use of said compounds to inhibit the replication or infectivity of viruses that employ programmed ribosomal frameshifting. | 09-01-2011 |
| 20140378521 | USE OF NK-1 RECEPTOR ANTAGONISTS IN PRURITUS - The invention relates to methods for treating pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist. | 12-25-2014 |
| 514417000 | Plural chalcogens bonded directly to ring carbons of the five-membered hetero ring (e.g., phthalimide, etc.) | 38 |
| 20080207730 | Methods of using (+)-2-[1-(3-Ethoxy-4 methoxyphenyl)-2-methylsulfonylethyl]-4 acetylaminoisoindoline 1,3-dione - Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 08-28-2008 |
| 20080234359 | Solid forms comprising (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2- methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions thereof, and uses thereof - Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 09-25-2008 |
| 20080242719 | Methods of Using (+)-2-[1-(3-Ethoxy-4-Methoxyphenyl)-2-Methylsulfonylethyl]-4-Acetylaminoisoindoline- 1,3-Dione - Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 10-02-2008 |
| 20080280967 | Substituted acylhydroxamic acids and method of reducing TNFalpha levels - Imido and amido substituted acylhydroxamic acids which reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate. | 11-13-2008 |
| 20080306134 | THALIDOMIDE ANALOGS FOR TREATING VASCULAR ABNORMALITIES - Thalidomide analog compounds having a general structure | 12-11-2008 |
| 20090036512 | FUNGICIDAL ACTIVE COMPOUND COMBINATION - Active compound combinations comprising an oxime ether derivative of the formula (I) and captan and their use as fungicides are described. | 02-05-2009 |
| 20100035958 | Novel Compounds And Compositions Thereof - The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water. | 02-11-2010 |
| 20100152271 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and OR | 06-17-2010 |
| 20100160405 | METHODS OF USING (+)-2-[1-(3-ETHOXY-4-METHOXYPHENYL)-2-METHYLSULFONYLETHYL]-4-ACETYLAMINOI- SOINDOLINE 1,3-DIONE - Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 06-24-2010 |
| 20100273853 | NOVEL ISOINDOL DERIVATIVES AS EP4 RECEPTOR AGONISTS - A compound of formula (1) or a pharmaceutically acceptable derivative thereof, | 10-28-2010 |
| 20100324107 | USE OF PHTHALIMIDE AND/OR SULPHONAMIDE DERIVATIVES IN THE TREATMENT OF DISEASES WHICH REQUIRE REDUCING THE TNF-alpha LEVELS AND AN EXOGENOUS SOURCE OF NITRIC OXIDE, PHTHALIMIDE DERIVATIVES, SULPHONAMIDE DERIVATIVES, AND A METHOD FOR OBTAINING A SULPHONAMIDE DERIVATIVE - The present invention refers to the use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, which have important activities in increasing the gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-α levels and an exogenous source of nitric oxide. More particularly, the present invention describes the use of such phthalimide and/or sulphonamide derivatives for the treatment of sickle-cell disease. The invention also has as a novel characteristic the disclosure of new functionalized phthalimide derivatives designed from the prototypes thalidomide and hydroxyurea, and designed rationally through the strategy of molecular hybridization for the treatment of said diseases. The invention still discloses a new method for obtaining a specific sulphonamide derivative which can be used in the preparation of a drug for the treatment of diseases which require reducing the levels of the TNF-α factor and an exogenous source of nitric oxide. | 12-23-2010 |
| 20100324108 | SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES - This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. | 12-23-2010 |
| 20110003878 | NOVEL DERIVATIVES OF PHTHALIMIDE AS HISTONE DEACETYLASE INHIBITORS - The invention relates to novel compounds of general formula (I), or one of the salts thereof, particularly one of the pharmaceutically acceptable salts thereof, or one of the corresponding solvates thereof. These compounds are inhibitors of the histone deacetylase enzymes and are suitable as pharmacologically active agents in a medicament for the treatment and/or prophylaxis of disorders or diseases associated with histone deacetylases. The invention also relates to a process for obtaining the mentioned compounds and the pharmaceutical compositions containing them. | 01-06-2011 |
| 20110124702 | Nanosuspension of a Poorly Soluble Drug via Microfluidization Process - Provided are compositions and methods for preparation and administration of an oral nanosuspension of a poorly soluble drug with improved bioavailability. The method is optimized through microfluidization process with water soluble polymeric excipients in the absence of surfactants. | 05-26-2011 |
| 20110130436 | CASPASE INHIBITORS AND USES THEREOF - This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: | 06-02-2011 |
| 20110190368 | Organosulfur Compounds, a Method of Making Organosulfur Compounds and their Use for Inhibiting the Growth of Tumour Cells - Organosulfur compounds of the general formula (2) are described, wherein R | 08-04-2011 |
| 20110224274 | New Therapeutic Agents - A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53. | 09-15-2011 |
| 20110269811 | INHIBITORS OF SEMICARBAZIDE-SENSITIVE AMINE OXIDASE (SSAO) AND VAP-1 MEDIATED ADHESION USEFUL FOR TREATMENT AND PREVENTION OF DISEASES - Compositions and methods of using compositions for treatment of inflammatory diseases and immune disorders are provided. Allylamino compounds are disclosed which are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein 1 (VAP-1). The compounds have therapeutic utility in suppressing inflammation and inflammatory responses, and in treatment of several disorders, including multiple sclerosis and stroke. | 11-03-2011 |
| 20110319465 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and OR | 12-29-2011 |
| 20120035238 | COMPOUNDS AND METHODS FOR TREATING CANCER AND VIRAL INFECTIONS - The present application relates to the use of one or more compounds of Formula (I) or pharmaceutically acceptable solvates or prodrugs thereof, for treating cancer or for treating or preventing a viral infection. | 02-09-2012 |
| 20120101144 | SOLID FORMS COMPRISING (+)-2-[1-(3-ETHOXY-4-METHOXYPHENYL)-2-METHYLSULFONYLETHYL]-4-ACETYLAMINOI- SOINDOLINE-1,3-DIONE, COMPOSITIONS THEREOF, AND USES THEREOF - Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 04-26-2012 |
| 20120165385 | Novel Compounds And Compositions Thereof - The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water. | 06-28-2012 |
| 20120252864 | SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES - This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. | 10-04-2012 |
| 20130035363 | Thalidomide Analogs - Thalidomide analogs that modulate tumor necrosis factor alpha (TNFα) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs. | 02-07-2013 |
| 20130345282 | SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES - This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. | 12-26-2013 |
| 20140011857 | SMALL MOLECULES AS EPIGENETIC MODULATORS OF LYSINE-SPECIFIC DEMETHYLASE 1 AND METHODS OF TREATING DISORDERS - The invention provides for novel compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer. | 01-09-2014 |
| 20140018404 | CONTROLLED RELEASE ORAL DOSAGE FORMS OF POORLY SOLUBLE DRUGS AND USES THEREOF - Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders. | 01-16-2014 |
| 20140024695 | METHODS OF TREATING ARTHRITIC CONDITIONS USING (+)-2-[1-(3-ETHOXY-4-METHOXYPHENYL)-2-METHYLSULFONYLETHYL]-4-ACETYLAMINOI- SOINDOLINE 1,3-DIONE - Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 01-23-2014 |
| 20140100259 | SOLID FORMS COMPRISING (+)-2-[1-(3-ETHOXY-4-METHOXYPHENYL)-2-METHYLSULFONYLETHYL]-4-ACETYLAMINOI- SOINDOLINE-1,3-DIONE, COMPOSITIONS THEREOF, AND USES THEREOF - Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 04-10-2014 |
| 20140155454 | HAND WASH COMPOSITIONS - Hand wash compositions including ε-phthalimido-peroxyhexanoic acid are described herein. | 06-05-2014 |
| 20140187599 | METHODS FOR TREATING DISEASES USING ISOINDOLINE COMPOUNDS - Methods of treating a disease selected from dermatomyositis, prurigo nodularis, pyoderma gangrenosum, alopecia areata, hidradenitis suppurtiva, rosacea, lichen planus, giant cell arteritis, Sjogren's syndrome, gout, chronic prostatitis, posterior uveitis, vulvodynia and interstitial cystitis in a human are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, cyclopropyl {2-[(15)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide or a combination thereof, or a pharmaceutically acceptable prodrug, metabolite, polymorph, salt, solvate or clathrate thereof. | 07-03-2014 |
| 20140194485 | ISOTOPOLOGUES OF ISOINDOLE DERIVATIVES - Provided herein are isoindole derivatives, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided. | 07-10-2014 |
| 20140194486 | THERAPEUTIC AGENTS - A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53. | 07-10-2014 |
| 20140303226 | KCNQ CHANNELS AS THERAPEUTIC TARGETS - The present disclosure relates to methods and compositions for modulating the activity of KCNQ channels as a means for reducing the effects of aberrant KCNQ channel function associated with epilepsy, deafness and arrhythmias including but not limited to, Long-QT syndrome (“LQTS”), and atrial fibrillation. The present disclosure also relates to the discovery of certain regions of KCNQ channels that interact with various channel stimulating molecules such as, ATP, and PIP | 10-09-2014 |
| 20140371287 | METHODS OF USING (+)-2-[1-(3-ETHOXY-4-METHOXYPHENYL)-2-ETHYLSULFONYLETHYL]-4-ACETYLAMINOIS- OINDOLINE-1,3-DIONE - Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4. | 12-18-2014 |
| 20150105438 | SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES - This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. | 04-16-2015 |
| 20150306226 | COMPOSITION - The present invention relates to compositions comprising compound (I) and processes for the preparation thereof. | 10-29-2015 |
| 20160128981 | CONTROLLED RELEASE ORAL DOSAGE FORMS OF POORLY SOLUBLE DRUGS AND USES THEREOF - Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders. | 05-12-2016 |
