Class / Patent application number | Description | Number of patent applications / Date published |
514252060 | Polycyclo ring system having the additional five-membered hetero ring as one of the cyclos | 54 |
20080280918 | Pyridazin-3(2H)-One Derivatives and Their Use as Pde4 Inhibitors - The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatilis, psoriasis or irritable bowel disease. | 11-13-2008 |
20080293731 | Organic Compounds - The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) | 11-27-2008 |
20090036461 | Use of Azabicyclo Hexane Derivatives - The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof: | 02-05-2009 |
20090042897 | Chemical Compounds - The present invention relates to novel compounds or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of:
| 02-12-2009 |
20090111825 | THIOPHENE 1,2,4-TRIAZOLE DERIVATIVES AS MODULATORS OF MGLUR5 - The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds. | 04-30-2009 |
20090124629 | 3-(1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: | 05-14-2009 |
20090176794 | 1H-INDOL-1-YL-UREA COMPOUNDS - Compounds of formula (I): | 07-09-2009 |
20090239877 | NOVEL 1,2,4-TRIAZOLE DERIVATIVES AND PROCESS OF MANUFACTURING THEREOF - The invention provides 1,2,4-triazole compounds, compositions containing those compounds, methods of treating diseases and/or disorders with those compounds and processes of manufacturing 1,2,4-triazole compounds. | 09-24-2009 |
20090270408 | AMIDE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS AND METHODS OF USE THEREOF - The invention relates to novel amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions. | 10-29-2009 |
20090286800 | Glucokinase Activators - Compounds are provided for use with glucokinase that comprise the formula: | 11-19-2009 |
20090312339 | BENZIMIDAZOLE CANNABINOID AGONISTS BEARING A SUBSTITUTED HETEROCYCLIC GROUP - The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans. | 12-17-2009 |
20100022550 | TETRAHYDROCARBAZOLE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS - The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of formula (I). | 01-28-2010 |
20100035889 | Use of PDE III Inhibitors For The Treatment of Asymptomatic (Occult) Heart Failure - The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca | 02-11-2010 |
20100093747 | METHOD OF INDUCING NEGATIVE CHEMOTAXIS - The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound having the Formula (I), (II), (III) or (IV). | 04-15-2010 |
20100144748 | METHODS INVOLVING ALDOSE REDUCTASE INHIBITORS - Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma. | 06-10-2010 |
20100152195 | Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors - The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: | 06-17-2010 |
20100152196 | Novel Fused Pyrrolocarbazoles - The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles. | 06-17-2010 |
20100160336 | Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors - The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: | 06-24-2010 |
20100222358 | OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES - Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein. | 09-02-2010 |
20100273806 | TETRAHYDROCYCLOPENTA[B]INDOL-3-YL CARBOXYLIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS - The present invention relates to certain (1,2,4-oxadiazol-3-yl)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases. | 10-28-2010 |
20100273807 | Use of PDE III Inhibitors for the Treatment of Asymptomatic (Occult) Heart Failure - The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca | 10-28-2010 |
20110009418 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - The present invention discloses compounds of formula: | 01-13-2011 |
20110015203 | Viral Polymerase Inhibitors - An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: | 01-20-2011 |
20110021532 | NOVEL SUBSTITUTED HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Substituted heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I). | 01-27-2011 |
20110028486 | INDOLES AS MODULATORS OF NICOTICIC ACETYLCHOLINE RECEPTOR SUBTYPE ALPHA-7 - The present invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-5-(trifluoromethyl)-2-pyrimidinecarboxamide. | 02-03-2011 |
20110071156 | HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM - The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R | 03-24-2011 |
20110152283 | CRYSTALLINE PIMOBENDAN, PROCESS FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITION AND USE - The invention relates to a pharmaceutical composition containing pimobendan as an active ingredient. The invention also relates to a crystalline form of pimobendan, as well as to a combination of said crystalline form with at least one other therapeutically active ingredient. Moreover, the invention relates to uses of said crystalline form, as well as to a pharmaceutical composition containing it. Finally, the invention relates to a process for preparing a crystalline form of pimobendan. | 06-23-2011 |
20110207738 | ANNELATED PYRROLIDIN SULFONAMIDES WITH OXADIAZOLONE HEADGROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system. | 08-25-2011 |
20110245263 | 2-HETEROARYL-PYRROLO[3,4-C]PYRROLE DERIVATIVES AND THEIR USE AS SCD - The invention relates to heterocyclic derivatives of formula I | 10-06-2011 |
20110251207 | BIARYL-SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA 2C ADRENERGIC RECEPTOR MODULATORS - In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions. | 10-13-2011 |
20110251208 | PHOSPHODIESTERASE TYPE III (PDE III) INHIBITORS OR CA2+-SENSITIZING AGENTS FOR THE TREATMENT OF HYPERTROPHIC CARDIOMYOPATHY - The present invention relates to a phosphodiesterase type III (PDE III) inhibitor and/or Ca | 10-13-2011 |
20110257193 | FUSED IMIDAZOLE DERIVATIVES AS TRPV3 ANTAGONIST - The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. | 10-20-2011 |
20120172368 | Bis-Benzimidazole Derivatives - Inhibitors of HCV replication of formula I | 07-05-2012 |
20120225887 | Glucokinase Activators - Compounds are provided for use with glucokinase that comprise the formula: | 09-06-2012 |
20120252817 | DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES - Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. | 10-04-2012 |
20120302576 | AMPK MODULATORS - The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): | 11-29-2012 |
20130090342 | BIPHENYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES - The invention relates to new derivatives of formula (I), | 04-11-2013 |
20130197008 | 3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR AGONISTS - There is provided a compound of Formula I(a) or I(b): | 08-01-2013 |
20130261129 | CHEMOKINE RECEPTOR ANTAGONISTS - Disclosed herein are chemokine receptor antagonists of formula (I) | 10-03-2013 |
20130324545 | METHODS FOR THE REGULATION OF THE PROSTAGLANDIN F SYNTHASE (PGFS) ACTIVITY OF AKR1B1 AND USES THEREOF - AKR1B1 (EC 1.1.1.21) is an aldose reductase that has mainly been associated with the polyol pathway, and more recently with lipid deperoxidation. We have discovered that the primary activity of this enzyme is rather a PGFS activity, catalyzing the transformation of PGH | 12-05-2013 |
20140045859 | Glucokinase Activators - Compounds are provided for use with glucokinase that comprise the formula: | 02-13-2014 |
20140088112 | ALKYNE BENZOTRIAZOLE DERIVATIVES - The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 03-27-2014 |
20140235648 | LIQUID PREPARATION COMPRISING PIMOBENDAN - A liquid preparation includes an etherified cyclodextrin derivative and a substituted benzimidazol, where the etherified cyclodextrin derivative is one of alpha-, beta, and gamma-cyclodextrin ether. | 08-21-2014 |
20140296246 | BENZIMIDAZOLONE DERIVATIVES AS BROMODOMAIN INHIBITORS - This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) | 10-02-2014 |
20150025082 | PRESERVED ETHERIFIED CYCLODEXTRIN DERIVATIVES CONTAINING LIQUID AQUEOUS PHARMACEUTICAL COMPOSITION - The present invention is directed to a preserved liquid aqueous pharmaceutical composition comprising one or more etherified cyclodextrin derivatives; one or more water-soluble preservatives; preferably selected from the group consisting of sorbic acid or salts thereof, preferably sodium sorbate, potassium sorbate, calcium sorbate; benzoic acid or salts thereof, preferably sodium benzoate; benzalkonium chloride; benzethonium chloride; cetylpyridinium chloride; sodium metabisulfite; sodium acetate; parabenes and salts thereof, preferably methylparabene, ethylparabene, propylparabene, butylparabene, butylparabene sodium; or combinations thereof; and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form. | 01-22-2015 |
20150099758 | Alpha 7 Nicotinic Acetylcholine Receptor Allosteric Modulators, Their Derivatives and Uses Thereof - The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I. | 04-09-2015 |
20150119402 | ALPHA 7 NICOTINIC ACETYLCHOLINE ALLOSTERIC MODULATORS, THEIR DERIVATIVES AND USES THEREOF - The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I. | 04-30-2015 |
20150307451 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. | 10-29-2015 |
20150307506 | 3-OXO-TETRAHYDRO-FURO[3,2-B]PYRROL-4(5H)-YL) DERIVATIVES II - The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors exhibiting a pronounced CatK-inhibition, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 10-29-2015 |
20160009667 | SUBSTITUTED BENZOXAZOLES AND METHODS OF USE THEREOF | 01-14-2016 |
20160009735 | Glucokinase Activators | 01-14-2016 |
20160031868 | BENZIMIDAZOLONE DERIVATIVES AS BROMODOMAIN INHIBITORS - This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R | 02-04-2016 |
20160130214 | 1,3-DIAMINOCYCLOPENTANE CARBOXAMIDE DERIVATIVES - Compounds of the formula I | 05-12-2016 |
20160151365 | TRIZOL-1-OL ANALOGS ANTI-RETROVIRAL LATENCY DRUGS | 06-02-2016 |