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Polycyclo ring system having the hetero ring as one of the cyclos

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514241000 - Hetero ring is six-membered consisting of three nitrogens and three carbon atoms

514242000 - Asymmetrical (e.g., 1,2,4-triazine, etc.)

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Entries
DocumentTitleDate
20120184556SUBSTITUTED ENZOIMIDAZOLESULFONAMIDES AND SUBSTITUTED INDOLESULFONAMIDES AS MGLUR4 POTENTIATORS - Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.07-19-2012
20100081661HEME OXYGENASE INHIBITORS, SCREENING METHODS FOR HEME OXYGENASE INHIBITORS AND METHODS OF USE OF HEME OXYGENASE INHIBITORS FOR ANTIMICROBIAL THERAPY - Inhibitors of microbial heme oxygenase and their use for treatment of microbial infections and bioremediation. The inhibitors of microbial heme oxygenase are useful against a new class of antimicrobial agents to target infections that are persistently difficult to combat with the current spectrum of antimicrobial agents. Screening methods for selecting inhibitors of microbial heme oxygenase.04-01-2010
20100113454PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I05-06-2010
20100113455Method of reducing intraosseous hypertension - A method of treating bone pain caused by osteoarthritis by administering to a patient an effective amount of a composition containing a bone edema medication, such as a vasoactive medication or phosphodiesterase inhibitor, including a PDE-5 inhibitor.05-06-2010
20100113453Sublingual Formulations of D-Cycloserine and Methods of Using Same - The invention provides methods and compositions for treating anxiety-related disorders in a subject. The methods include sublingually administering D-cycloserine to a subject with the anxiety-related disorder, either alone or in combination with extinction training.05-06-2010
20130035340sGC STIMULATORS OR sGC ACTIVATORS ALONE AND IN COMBINATION WITH PDE5 INHBITORS FOR THE TREATMENT OF CYSTIC FIBROSIS - The present invention relates to soluble guanylate cyclase (sGC) and to phosphodiesterases (PDEs) and the pharmacology of sGC stimulators, sGC activators and PDE inhibitors. More particularly, the invention relates to the use of sGC stimulators and sGC activators in combination with PDE5 inhibitors for preparation of medicaments for the treatment of Cystic Fibrosis (CF).02-07-2013
20100113452COMPOUNDS FOR TREATING PULMONARY HYPERTENSION - The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent.05-06-2010
20100105689NOVEL 1,4- AND 1,5-DIARYLSUBSTITUTED 1,2,3-TRIAZOLES USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel 1,4- and 1,5-diarylsubstituted 1,2,3-triazole derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels.04-29-2010
20080312239METHODS FOR THE TREATMENT OF ERECTILE DYSFUNCTION USING FISPEMIFENE - A method of treatment of erectile dysfunction (ED) comprises the step of administering fispemifene to a subject in need thereof in an amount effective to raise the subject's testosterone level. Fispemifene may be used in combination with a PDE-5 inhibitor in individuals who have failed to respond sufficiently to conventional ED treatment. Methods are also disclosed of treating ED by administering clomifene, enclomifene, ospemifene, toremifene and mixtures thereof in combination with a PDE-5 inhibitor.12-18-2008
201002677283-SUBSTITUTED-1,2,3-TRIAZIN-4-ONE'S AND 3 SUBSTITUTED 1,3-PYRIMIDINONE'S FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.10-21-2010
20100130498AGONISTS OF BITTER TASTE RECEPTORS AND USES THEREOF - The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.05-27-2010
20110009412MACROPHAGE MIGRATION INHIBITORY FACTOR ANTAGONISTS AND METHODS OF USING SAME - Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases.01-13-2011
20130059854Dosage Form for Insertion Into the Mouth - Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, particularly anti-migraine agents to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.03-07-2013
20110015197mTOR INHIBITOR SALT FORMS - Salt forms of mTOR inhibitors of the Formula (I):01-20-2011
20090062288PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH - The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.03-05-2009
20090156604FUSED BICYCLIC IMIDAZOLES - Compounds of formula (I)06-18-2009
20100035882INHIBITION OF PDE2A - The invention relates to the use of PDE2A inhibitors for the manufacture of a medicament for the treatment and/or prophylaxis of coronary diseases, especially stable and unstable angina pectoris, acute myocardial infarction, prophylaxis of myocardial infarction, heart failure, and high blood pressure and the sequelae of atherosclerosis, and vascular disorders, disorders of the kidney, especially renal failure, inflammatory disorders, erectile dysfunction and prevention of sudden heart death.02-11-2010
20110028479SUBSTITUTED PYRROLOTRIAZINES AND THEIR USE - The present application relates to new, substituted pyrrolo[2,1-f][1,2,4]triazine derivatives of the formula (I) as prostacyclin (PGI02-03-2011
20090221587NOVEL INSECTICIDES - Compounds of formula (I), wherein the substituents are as defined in claim (09-03-2009
20110294816PYRROLOTRIAZINE KINASE INHIBITORS - The present invention provides compounds of formula I12-01-2011
20110294815PROSTACYCLIN ANALOGS - This invention relates to novel prostacyclin analogs and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel prostacyclin analogs that are derivatives of treprostinil. This invention also provides compositions comprising a compound of this invention and a carrier and the use disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering analogues of prostacyclin, such as treprostinil.12-01-2011
20100137318BICYCLIC HETEROCYCLIC COMPOUND - A compound of a formula (I):06-03-2010
20090247531CRYSTALLINE FORMS OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TR- IAZIN-6-YLOXY]-1-METHYLETHYL ESTER - Crystalline form, Form N-1, of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising the Form N-1 of Compound I as well as a method of using the Form N-1 of Compound I in the treatment of cancer and other proliferative diseases.10-01-2009
20110263605Azabicyclo[2.2.1]Heptane Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.10-27-2011
20120035178Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.02-09-2012
20120108594PROCESS FOR PREPARING SALTS OF 4-[[5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL]AMINO]-5-METHYL-N-PROPY- LPYRROLO[2,1-f][1,2,4]TRIAZINE-6-CARBOXAMIDE AND NOVEL STABLE FORMS PRODUCED THEREIN - Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well.05-03-2012
20100081662PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I04-01-2010
20100099679FUSED BICYCLIC mTOR INHIBITORS - Compounds represented by Formula (I)04-22-2010
20090291955Azacyclohexane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. 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; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.11-26-2009
20120289509HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR - Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.11-15-2012
20100137319PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH - The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.06-03-2010
20090170853NOVEL INHIBITORS OF KINASES - The present invention provides compounds of formula I,07-02-2009
20090312331PROCESS FOR PREPARING SALTS OF 4-[[5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL]AMINO]-5-METHYL-N-PROPY- LPYRROLO[2,1-f][1,2,4]TRIAZINE-6-CARBOXAMIDE AND NOVEL STABLE FORMS PRODUCED THEREIN - Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well.12-17-2009
20100144736NOVEL BIPHENYL THIO-UREA DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS - The invention relates to novel biphenyl thio-urea derivatives of Formula (I), wherein A represents hydroxy or tetrazolyl; R06-10-2010
20090181972Novel Inhibitors of Cysteine Proteases, the Pharmaceutical Compositions Thereof and their Therapeutic Applications - The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.07-16-2009
20120196867COMPOSITION COMPRISING A PDE4 INHIBITOR AND A PDE5 INHIBITOR - The claimed subject matter relates to pharmaceutical compositions comprising a PDE4 inhibitor and a PDE5 inhibitor and the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.08-02-2012
20120035177TABLET FORMULATION FOR P38 INHIBITOR AND METHOD - A tablet formulation is provided which includes a medicament which is a pharmaceutically acceptable salt of a p38 inhibitor, such as the p38 HCl salt of the structure Formula (I) and which has good physical stability when stored at up to 25 C./60% RH in closed containers with desiccant. The tablet formulation will contain crospovidone as a tablet disintegrant, which, unlike croscarmellose sodium, will not cause disproportionation of the HCl salt to the free base of P38 inhibitor and thus will have acceptable dissolution properties even after storage at room temperature.02-09-2012
20090163504Method for healing a wound using a phosphodiesterase type five inhibitor - A method for healing a wound comprising the step of topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises a first medicament characterized as a phosphodiesterase type five inhibitor and pharmaceutically acceptable salts thereof.06-25-2009
20080234277NOVEL AZA-PYRIDOPYRIMIDINONE DERIVATIVES - The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I):09-25-2008
20090181971Inhibitors of Histone Deacetylase - The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.07-16-2009
20120077814SULFONAMIDE, SULFAMATE, AND SULFAMOTHIOATE DERIVATIVES - The disclosure provides biologically active compounds of formula (I):03-29-2012
20110144113TRIAZOLOTRIAZINES AS KINASE INHIBITORS - The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.06-16-2011
20090253704PYRROLOTRIAZINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses pyrrolotriazinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I:10-08-2009
201201968662-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses - The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.08-02-2012
20090082354PYRAZOLO[5, 1-C] [1,2,4] TRIAZINES, METHODS FOR PREPARATION AND USE THEREOF - A pyrazolo[5,1-c][1,2,4]triazine compound of formula A:03-26-2009
20100184769PDE INHIBITORS FOR THE TREATMENT OF HEARING IMPAIRMENT - The invention provides pharmacological compositions comprising PDE-5 inhibitors for the treatment of hearing impairment i.e. hearing loss and tinnitus. The invention also provides methods of screening for such PDE-5 inhibitors for use in the preparation of medicaments for the treatment of hearing impairment i.e. hearing loss and tinnitus.07-22-2010
20090076011DEUTERIUM-ENRICHED TIRAPAZAMINE - The present application describes deuterium-enriched tirapazamine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090258877TRIAZOLOTRIAZINES AND TRIAZOLOPYRAZINES AND THEIR USE - The invention relates to substituted triazolotriazines and triazolopyrazines and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular haematologic disorders, preferably of leukopenias and neutropenias.10-15-2009
20110003820PYRAZOLOPYRIMIDINES, A PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICINE - The invention relates to pyrazolopyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.01-06-2011
20110039855Tetrahydrocyclopenta[b]indole Androgen Receptor Modulators - The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.02-17-2011
20110245253METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.10-06-2011
20090215783COMPOSITION FOR INDUCTION OR INHIBITION OF STEM CELL DIFFERENTIATION - The present invention relates to composition and methods for inducing or inhibiting differentiation of stem cells. The invention also relates to applications in the treatment of medical conditions, e.g., osteoporosis, bone fracture, bone injuries, myocardiac infarction, cardiomyopathy, degenerative muscle diseases, myopathy, and urinary incontinence.08-27-2009
20090215782Use of PDE-5 Inhibitors for Endothelial Repair of Tissues Impaired by Trauma or Disease - The invention relates generally to neovascularization and endothelial repair of tissues impaired by trauma or disease. Particularly, the invention relates to the function of endothelial progenitor cells in neovascularization and endothelial repair. More particularly, the invention relates to methods and pharmaceutical compositions for the treatment of tissues impaired by trauma or disease. In particular, the present invention relates to the use of a type V phosphodiesterase inhibitor in the preparation of a medicament for the treatment of a condition which is susceptible to the treatment with circulating EPCs wherein the treatment is effected by the proliferation of endothelial progenitor cells.08-27-2009
20090215781ALPHA-HELIX MIMETICS AND METHODS RELATING TO THE TREATMENT OF FIBROSIS - The invention provides α-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R08-27-2009
20110082147SUBSTITUTED IMIDAZOTRIAZINES - This invention relates to novel substituted imidazotriazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing partial-agonist activity at the GABA α2, α3 and α5 subtype receptors, and antagonist activity at the al subtype receptor.04-07-2011
20110046141USE OF PDE5 INHIBITORS FOR TREATING CIRCADIAN RHYTHM DISORDERS - A method of altering circadian rhythm in a mammal is provided. In certain embodiments, the method comprising: administering to the mammal a PDE5 inhibitor, e.g., sildenafil, vardenafil, tadalafil or zaprinast. The method may be employed to prevent a circadian rhythm disorders including, but not limited to transmeridian flight disorder (i.e., “jet-lag”), shiftwork-related disorder, seasonal affected disorder and insomnia by phase delay or phase advance.02-24-2011
20110065709AURORA KINASE MODULATORS AND METHOD OF USE - The present invention relates to chemical compounds having a general formula I03-17-2011
20130165445Aurora Kinase Modulators and Method of Use - The present invention relates to chemical compounds having a general formula I06-27-2013
20110257185REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.10-20-2011
20110028480ORODISPERSABLE FORMULATIONS OF PHOSPHODIESTERASE-5 (PDE-5) INHIBITORS - Orodisperable formulations of phosphodiesterase-5 (PDE-5) inhibitors and methods of manufacturing such are provided. Further, an improved dosage form and method of treating sexual dysfunction are provided.02-03-2011
20110257184SHP-2 PHOSPHATASE INHIBITOR - A method of treating SHP-2 phosphatase associated diseases in a subject includes administering a SHP-2 inhibitor to the subject.10-20-2011
20120302571CRYSTALLINE FORMS OF (S)-1-(4-(5-CYCLOPROPYL-1H-PYRAZOL-3-YLAMINO)PYRROLO[1,2-f][1,2,4]TRIAZIN- -2-YL)-N-(6-FLUOROPYRIDIN-3-YL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE - Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.11-29-2012
20120302570HETEROCYCLIC OXIME COMPOUNDS - The invention relates to compounds of formula (I) and salts thereof:11-29-2012
20100179152Novel use for PDE5 inhibitors - The present invention is concerned with the use of PDE5 inhibitors in medicine.07-15-2010
201000163232-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS - The application claims a compound of the formula01-21-2010
20090291956SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)-IMIDAZO[1,2-b][1,2,- 4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME - The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.11-26-2009
20080293723SPIROINDOLINONE DERIVATIVES - There are provided spiroindolinone derivatives of the formula11-27-2008
20090018136METHODS AND COMPOSITIONS FOR THE TREATMENT OF VASCULAR DISEASE - The present invention is directed to a novel methods and compositions for the therapeutic intervention of vascular complications associated with diabetes, hyperlipidemias, and various cardiovascular disorders including but not limited to recalcitrant hypertension, coronary artery disease, pulmonary arterial hypertension, congestive heart failure, and hemolytic anemias. More specifically, the specification describes methods and compositions for treating such vascular disorders using compositions comprising BH4 and derivative thereof. Combination therapies of BH4 and other therapeutic regimens are contemplated.01-15-2009
20100234381BIOMARKERS AND METHODS FOR DETERMINING SENSITIVITY TO VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2 MODULATORS - A method for predicting the likelihood a mammal will respond therapeutically to a method of treating cancer comprising administering a VEGFR-2 modulator or a dual VEGFR-2/FGFR-1 modulator wherein the method comprises: (a) measuring in the mammal the level of FGF2; (b) either comparing the level of FGF2 in the sample relative to a standard to permit assignment of the sample to either being a member of an FGF2 positive class or an FGF2 negative class, or comparing the level of FGF2 in the sample relative to a standard, wherein assignment of the mammal to the FGF2 positive sample class or a determination that the mammal has an elevated level of FGF2, indicates an increased likelihood the patient will respond therapeutically to the cancer treatment. Methods of predicting whether a mammal has received an efficacious dose of a VEGFR-2 modulator or a dual VEGFR-2/FGFR-1 modulator is also disclosed, in addition to kits comprising these methods.09-16-2010
20080249096Pharmaceutical Forms with Improved Pharmacokinetic Properties - The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.10-09-2008
20120004233TRICYCLIC COMPOUNDS AS ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are antagonists of PGD01-05-2012
20110166144Pyrimidotriazinediones and Pyrimidopyrimidinediones and Methods of Using the Same - The present disclosure is directed to pyrimidotriazinediones and pyrimidopyrimidinediones having a formula (I), (II), or (III), or a mixture or pharmaceutically acceptable salt or hydrate thereof, and to methods of treating cancer comprising administering the same.07-07-2011
20120015949COMPOSITION AND METHOD OF DECREASING RENAL ISCHEMIC DAMAGE - A method of decreasing renal ischemic damage comprising a) identifying an organism having a kidney that is susceptible to renal ischemic damage from an ischemic event; and b) administering to the organism one or more than one effective dose of an agent prior to the ischemic event; where administering to the organism the one or more than one effective dose of the agent serves to at least partially protect the organism's kidney from damage during a subsequent ischemic event. A composition for decreasing renal ischemic damage comprising one or more than one phosphodiesterase inhibitor, and one or more than one HMG-CoA reductase inhibitor.01-19-2012
20120157458IMIDAZOTRIAZINONE COMPOUNDS - The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.06-21-2012
20110009413CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS - Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ═NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria.01-13-2011
20120208819HETEROCYCLIC COMPOUNDS USEFUL AS PDK1 INHIBITORS - The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.08-16-2012
20110065708HETEROCYCLIC OXIME COMPOUNDS - The invention relates to compounds of formula (I) and salts thereof:03-17-2011
20120122872Treatment or Prevention of Fungal Infections with PDK1 Inhibitors - Provided are methods of treating or preventing a fungal infection in a subject. The methods comprise identifying a subject with or at risk of developing a fungal infection and administering to the subject a therapeutically effective amount of an inhibitor or a fungal phosphoinositide-dependent kinase 1 (PDK-1) or a homolog thereof. Inhibition of the fungal PDK-1 or homolog thereof results in the treatment or prevention of a fungal infection in the subject. Also provided are compositions comprising an inhibitor of a fungal phosphoinositide-dependent kinase 1 (PDK-1) or a homolog thereof, and a pharmaceutically acceptable carrier.05-17-2012
20100093738Fungicidal Compounds and Fungicidal Compositions - The present invention relates to compounds of the formula I04-15-2010
20090131442Method of Treating Bone Pain Caused by Osteoarthritis - A method of treating bone pain caused by osteoarthritis by administering to a patient an effective amount of a composition containing a bone edema medication, such as a vasoactive medication or phosphodiesterase inhibitor, including a PDE-5 inhibitor.05-21-2009
20110183983HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR - Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.07-28-2011
20120252816USE OF PHOSPHODIESTERASE INHIBITORS FOR TREATING MULTIDRUG RESISTANCE - The present invention relates to methods of treating multidrug resistance in cancerous cells with phosphodiesterase (PDE) inhibitors, e.g., PDE5 inhibitors. More specifically, the invention relates to methods of treating multidrug resistance that arises, e.g., during administration of chemotherapeutic/antineoplastic (anticancer) agents for treatment of cancer, with a PDE5 inhibitor (e.g., sildenafil, vardenafil, and tadalafil). The invention also relates to methods of treating cancer, e.g., multidrug resistant cancer, using a PDE5 inhibitor in combination with an antineoplastic therapeutic agent. Further, the invention relates to pharmaceutical compositions for treating multidrug resistant cancers comprising a PDE5 inhibitor, or a combination of a PDE5 inhibitor and an antineoplastic agent.10-04-2012
20100048575NOVEL TETRACYCLIC INHIBITORS OF CYSTEINE PROTEASES, THE PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR THERAPEUTIC APPLICATIONS - The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use: Formula (I) wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim 02-25-2010
20100273800PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING CANCER THROUGH INHIBITION OF AURORA KINASE - This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly Cancer.10-28-2010
20120220595Deuterated Tyrosine Kinase Inhibitors - Compounds of Formula I, as shown below and defined herein: enriched in deuterium, and pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by IGF-1R and/or IR.08-30-2012
20120220594METHODS FOR TREATING CANCER IN PATIENTS HAVING IGF-1R INHIBITOR RESISTANCE - A method for treating cancer comprising identifying a mammal that overexpresses breast cancer resistance protein; and administering to said mammal a pharmaceutical composition comprising a therapeutically effective amount of ixabepilone. In one aspect, the mammal is not administered an agent that is susceptible to breast cancer resistance protein overexpression resistance. In another aspect, the cancer is a solid tumor.08-30-2012
20100240662REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.09-23-2010
20110003821PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I01-06-2011
20110212967IMIDAZO[1,2-B][1,2,4]TRIAZINES AS C-MET INHIBITORS - The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.09-01-2011
20100234382COMPOSITION COMPRISING A PDE4 INHIBITOR AND A PDE5 INHIBITOR - The invention relates to the combined administration of a PDE4 inhibitor and a PDE5 inhibitor for the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.09-16-2010
20110245252PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I10-06-2011
20130012515Fused Bicyclic Pyridine and Pyrazine Derivatives as Kinase Inhibitors - A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.01-10-2013
20130172356COMBINATION OF EGCG OR METHYLATED EGCG AND A PDE INHIBITOR - Disclosed is a medicament characterized by the combination of: epigallocatechin gallate, methylated epigallocatechin gallate, or a pharmacologically permitted salt thereof; and a phosphodiesterase inhibitor.07-04-2013
20080234276Heterocyclic Triazines as Hypoxic Selective Protein Kinase Inhibitors - The invention relates to novel heterocyclic triazines which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation by administering effective amounts of such compounds.09-25-2008
20130131064Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.05-23-2013
20080221108Anthranilic Acid Derivatives As Hm74A Receptor Agonists - Therapeutically active anthranilic acid derivatives of Formula (I) wherein R09-11-2008
20130116257METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.05-09-2013
20130096129ACTIVATORS OF CLASS I HISTONE DEACETLYASES (HDACS) AND USES THEREOF - The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).04-18-2013
20130123264COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY BOWEL DISORDERS AND INTESTINAL CANCERS - Compositions and formulations useful for treating inflammatory bowel diseases, intestinal cancers, and improving the integrity of the luminal surface of the gastrointestinal tract are disclosed. Typically, the composition increases level of cGMP in the intestinal mucosa or increases the activity of a PKG, preferably PKG2, in the intestinal mucosa. Preferably, the composition includes a phosphodiesterase type 5 (PDE5) inhibitor and is targeted to the intestinal mucosa, for example by enteric coating or attachment of an intestinal specific targeting moiety.05-16-2013
200802004682-Substituted 5-Membered Heteroaryl Carboxylates as Hm74a Receptor Agonists - Therapeutically active heteroaryl carboxylic acid derivatives of Formula (I) wherein R08-21-2008
20130150370TASTE-MASKED PHARMACEUTICAL FORMULATION HAVING ACCELERATED ONSET OF ACTION - Pharmaceutical composition for oral administration comprises at least one phosphodiesterase inhibitor and at least one sugar alcohol selected from mannitol, sorbitol, xylitol, maltitol, lactitol, erythritol, threitol and Isomalt, and sodium hydrogen carbonate as pharmaceutical excipients in the following weight proportions: phosphodiesterase inhibitor: about 10 to about 150 parts by weight in total; sugar alcohol: about 50 to about 600 parts by weight in total; and sodium hydrogen carbonate: about 2 to about 100 parts by weight. The above composition for use in a method of treating male erectile dysfunction with an accelerated onset of action is also disclosed.06-13-2013
20130150369Benzotriazine Oxides as Drugs Targeting Mycobacterium Tuberculosis - Benzotriazine doxides are disclosed as drugs targeting 06-13-2013
20130158037COMPOUNDS AND METHODS FOR TREATING TUBERCULOSIS INFECTION - The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of 06-20-2013
20120022071Treatment of Comorbid Premature Ejaculation and Erectile Dysfunction - The invention provides a method of treating comorbid premature ejaculation and erectile dysfunction. In particular, the method comprises administering an effective amount of a tramadol material and an effective amount of a phosphodiesterase inhibitor. The invention also provides a pharmaceutical composition comprising a pharmaceutically-acceptable carrier, a tramadol material and a phosphodiesterase inhibitor. The invention further provides a kit comprising a tramadol material and a phosphodiesterase inhibitor.01-26-2012
20120088770ALPHA HELIX MIMETICS AND METHODS RELATING THERETO - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.04-12-2012
20130210824Substituted fused imidazoles and pyrazoles and use thereof - The present application relates to novel substituted fused imidazoles and pyrazoles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.08-15-2013

Patent applications in class Polycyclo ring system having the hetero ring as one of the cyclos