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The bicyclo ring system consists of the five-membered hetero ring and a benzene ring (e.g., indole, etc.)

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

514359000 - Five-membered hetero ring containing at least one nitrogen ring atom (e.g., 1,2,3-triazoles, etc.)

514408000 - The five-membered hetero ring consists of one nitrogen and four carbons

514410000 - Polycyclo ring system having the five-membered hetero ring as one of the cyclos

514412000 - Bicyclo ring system having the five-membered hetero ring as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514419000 C=X bonded directly or indirectly by an acyclic carbon or carbon chain to ring carbon of the five-membered hetero ring (e.g., tryptophan, etc.) (X is chalcogen) 87
514416000 The ring nitrogen is bonded directly to nonshared ring carbons of the five-membered hetero ring (e.g., isoindole, etc.) 38
514418000 Chalcogen bonded directly to ring carbon of the five-membered hetero ring 28
Entries
DocumentTitleDate
20120184591METHODS FOR TREATING PROSTATITIS - It has been discovered that silodosin is effective in treating patients having symptoms associated with prostatitis with silodosin or a pharmaceutically acceptable salt thereof. In a preferred embodiment, patients are treated with 4 mg once daily.07-19-2012
20100137398USE OF HDAC INHIBITORS FOR THE TREATMENT OF GASTROINTESTINAL CANCERS - The present invention relates to the use of an HDAC inhibitor for the preparation of a medicament for the treatment of gastrointestinal cancers; a method of treating a warm-blooded animal, especially a human, having gastrointestinal cancer, comprising administering to said animal a therapeutically effective amount of an HDAC inhibitor, especially a compound of formula (I) as defined herein; and to a pharmaceutical composition and a commercial package.06-03-2010
20110190367NOVEL USE OF 3,3'-DIINDOLYLMETHANE - Use of DIM and/or its derivatives for prevention, treatment and/or delay of age-related hearing loss in mammals.08-04-2011
20100144824GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.06-10-2010
20090192211CYCLOOXYGENASE-2 INHIBITOR/HISTONE DEACETYLASE INHIBITOR COMBINATION - The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of pre-malignant colon lesions or a colon cancer or other malignancies in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.07-30-2009
20090192210POLYMORPHS OF N-HYDROXY-3-[4-[[[2-(2-METHYL-1H-INDOL-3-YL)ETHYL]AMINO]METHYL]PHENYL]-2E- -2-PROPENAMIDE - Polymorphic forms of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide free base and salts thereof are prepared by various processes.07-30-2009
20100076050SOLID BETALAIN COMPOSITIONS AND METHODS - Solid, free-flowing, and substantially completely dissolvable preparations with high betalain content are presented. Most typically, the betalain profile of the preparations is near natural and includes betalains in an amount of between 10-40 wt %. As the preparations of the inventive subject matter maintain chemical stability and flowability over extended periods of time, it should be noted that the betalain preparations are now amenable to compounding in small and measured quantities. Furthermore, new biological activities of betalains are shown, and especially include significant induction of SIRT and reduction of serum triglyceride.03-25-2010
20130158092New Oral Formulation - The present invention relates to a pharmaceutical composition, in particular to a composition for administering active agents which are poorly soluble in aqueous media, and/or which are acid sensitive.06-20-2013
20130072539Anti-Cancer Tamoxifen-Melatonin Hybrid Ligand - A particularly constructed tamoxifen-melatonin hybrid ligand gives new and unexpectedly improved results in the prevention and treatment of cancer, particularly breast cancer. The hybrid ligand comprises either tamoxifen or 4-hydroxy-tamoxifen and also melatonin, with the tamoxifen or 5-hydroxy-tamoxifen and melatonin's being linked by an unsubstituted C03-21-2013
20090076122PARP Modulators and Treatment of Cancer - The invention relates to a method of modulating poly(ADP-ribose)polymerase-1 (PARP-1) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger-1 of the PARP-1 enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's π-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc-1 finger of PARP-1 and does not contain benzamide or lactam substituents.03-19-2009
20110021596Topical therapy for migraine - The invention is directed to formulations and methods of treating a migraine and/or cluster headache with a serotonin agonist, pharmaceutically acceptable salt thereof, or derivative thereof.01-27-2011
20090012146SOLUBILITY-ENHANCED PHARMACEUTICAL COMPOSITIONS COMPRISING ZAFIRLUKAST - Stable pharmaceutical compositions comprising zafirlukast and pharmaceutically acceptable salts, solvates, polymorphs, enantiomers or mixtures thereof, together with one or more pharmaceutically acceptable polymers, and processes for their preparation.01-08-2009
20110130435TIME-RELEASED MEDICATION FOR APPLYING TO CRUSTACEAN OVARIAN DEVELOPMENT - A time-released medication for applying to crustacean ovarian development comprises a covering oil and a serotonin-related reagent. The covering oil is coated with the serotonin-related reagent and provides a sustainable releasing effect for the serotonin-related reagent. The serotonin-related reagent is selected from a group of serotonin, a precursor of serotonin, a derivative of serotonin and an agonist of serotonin. The coating relationship between the serotonin-related reagent and the covering oil makes them become a time-released medication.06-02-2011
20100227906C-substituted Diindolylmethane Compositions and Methods for the Treatment of Multiple Cancers - The present embodiment of the invention is generally directed to compositions comprising suspensions of poorly water soluble compounds recrystallized in nanoparticulate sizes ranging from 0.1 to 5 μm. In addition, the embodiment of the invention is directed to methods for preparation and administration of these compositions to a patient for prevention and treatment of disease states. In particular, the embodiment of the invention is directed to compositions comprising suspensions of poorly water-soluble compounds, such as antimitotics and antibiotics, in nanoparticulates and methods of prevention and treatment of chronic disease states, such as cancer, by intraperitoneal and intravenous administration of such compositions09-09-2010
20120289573METHODS FOR TREATMENT WITH BUCINDOLOL BASED ON GENETIC TARGETING - The present invention concerns the use of methods for evaluating bucindolol treatment for a patient, particularly one with heart failure. It concerns methods for determining whether to administer or prescribe bucindolol to a patient based on whether the patient is homozygous for the Arg 389 polymorphism in the β1-adrenergic receptor (AR).11-15-2012
20110288144USE OF HDAC INHIBITORS FOR THE TREATMENT OF MELANOMA - The invention relates to the use of an HDAC inhibitor, more specifically or a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for the treatment of melanoma; the use of an HDAC inhibitor or a pharmaceutically acceptable salt thereof in the treatment of melanoma; a method of treating warm-blooded animals including mammals, especially humans, suffering from melanoma by administering to a said animal in need of such treatment a dose effective against said disease of an HDAC inhibitor or a pharmaceutically acceptable salt thereof.11-24-2011
20100035957Methods for the Use of Inhibitors of Cytosolic Phospholipase A2 - This invention provides methods for the use of substituted indole compounds of the general formula:02-11-2010
20100035956Compounds Having CRTH2 Antagonist Activity - Compounds of general formula (I) wherein R is phenyl optionally substituted with one or more halo substituents; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.02-11-2010
20090318527INDOLE COMPOUNDS AND METHODS OF USE THEREOF - Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.12-24-2009
20090082419DEUTERIUM-ENRICHED TEGASEROD - The present application describes deuterium-enriched tegaserod, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20100087504Use of Diindolylmethane (DIM) Compounds and Derivatives as Neuroprotective Agents - Presented herein are diindolylmethane derivative compounds useful for the prevention and or treatment of neurological conditions, including neurological conditions related to neuroinflammation. One such neurological condition is Parkinson's disease.04-08-2010
20100298401GALENICAL FORM FOR THE ADMINISTRATION OF TRIPTANS BY BUCCAL TRANSMUCOUS MEANS - The object of the invention is a galenical form for the administration by buccal transmucous means of at least one active ingredient of the triptan family, comprising at least: 11-25-2010
20090221665Organic Compounds - The present invention relates to a combination of a 5-HT4 receptor agonist and a cholinesterase inhibitor and pharmaceutical compositions and formulations containing the combination. The pharmaceutical combination may be employed for the treatment of altered gastrointestinal motility, sensitivity, secretion or abdominal disorders. The dosage is preferably oral. The preferred 5-HT09-03-2009
20080319044Compounds and Methods of Use Thereof - Indole boronic acid compounds, and analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.12-25-2008
20080207729Indole Derivatives Having Antitumor Activity - Indole derivatives of Formula (I+A) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.08-28-2008
20090298905Nitrogenatd trans-stilbene analogs, method for the obtention and medical applications thereof - This invention is related to new nitrogenated trans-stilbene analog compounds, more specifically, imine, pyrrol and Indole derivatives, with procedures for the preparation and use thereof as pharmaceutical compositions for the treatment and/or chemoprevention of those mammalian diseases such as cancer, fibrosclerosis and acute/chronic inflammation, graft-versus-host reaction, ischemic-reperfusion tissue injury in stroke and heart attack, neurodegeneration, and during organ transplantation, whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable oxidative stress, angiogenic and proliferative responses.12-03-2009
20090281159USE OF HDAC INHIBITORS FOR THE TREATMENT OF LYMPHOMAS - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I):11-12-2009
20090286847ONCOGENIC RAS-SPECIFIC CYTOTOXIC COMPOUND AND METHODS OF USE THEREOF - Embodiments of the present invention provide for methods and compositions comprising an Oncorasin, such as 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1) and/or its analogs or derivatives.11-19-2009
200802751023-ACYLINDOLE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The invention relates to compounds of formula (I), wherein X, R11-06-2008
201102077931-AMINOCYCLOHEXANE DERIVATIVES FOR THE TREATMENT OF SLEEP DISORDERS. - The present invention relates to the treatment of an individual afflicted with sleep disorders associated with tinnitus and/or neurological diseases comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.08-25-2011
20090264495ORAL SUSTAINED-RELEASE PHARMACEUTICAL COMPOSITION OF INDAPAMIDE, PRODUCTION AND USE THEREOF - An oral sustained-release pharmaceutical composition of indapamide and a process for producing the foregoing pharmaceutical composition are provided. The pharmaceutical composition comprises indapamide in an amount between 0.2% and 4% (w/w) of the composition, a hydrophilic polymer in an amount between 10 % and 30% (w/w) of the composition, a dry binding agent in an amount between 2% and 20% (w/w) of the composition, and an erosion modifier in an amount between 40% and 80% (w/w) of the composition. The sustained-release pharmaceutical composition of indapamide could be obtained at lower expenditure and produced in a safe and economical manner.10-22-2009
20090118350Biomarkers for Identifying Efficacy of Tegaserod in Patients with Chronic Constipation - Pharmacogenetics was used to evaluate the effect of polymorphisms in select candidate genes on the response of patients with chronic constipation to tegaserod (Zelmac®/Zelnorm®). The analysis identified twelve single nucleotide polymorphisms (SNPs) in six genes (HTR4, HTR3B, MLN, AQP3, SLC12A2, SCNN1A) that were associated with at least a 60% response rate to tegaserod and an odds ratios of 5 or greater (compared to placebo) after 4 weeks of treatment. The identified genes display a wide range of different functions, including serotonin signaling, secretion and motility, all of which are important in maintaining the normal function of the gastrointestinal tract. Thus, these data imply that chronic constipation may result from a variety of pathophysiological mechanisms related to variants in the above identified genes, all of which respond well to treatment with tegaserod. Patients without these variants do not respond to treatment significantly more than they do to placebo, which could indicate that their chronic constipation is not due to pathophysiological mechanisms but rather to environmental or possibly psychological factors. Patients with these variants are also less likely to respond to placebo, again implying that these variants are associated with a true pathophysiology.05-07-2009
20090005430Receptor Blocker and Vasodilator Comprising Indole Derivative as Active Ingredient - It is intended to find a compound that is structurally simpler than yohimbine, a pentacyclic condensed heterocyclic compound, and has an effect similar to that of yohimbine.01-01-2009
20090023796Analogs of Indole-3-Carbinol Metabolites as Chemotherapeutic and Chemopreventive Agents - Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds has the structure of formula (IV)01-22-2009
20090054510METHOD FOR IDENTIFYING COMPOUNDS FOR THE TREATMENT OF DEPRESSION - An assay for identifying compounds with increased efficacy in the treatment of depression is disclosed. The assay comprises the steps of determining whether a test compound inhibits SERT and whether it inhibits with an allosteric site ion SERT.02-26-2009
20080234357Indole derivatives substituted with long-chain alcohols and medicaments containing them - Provided is an indole long-chain alcohol, or a hydrate or an isomer thereof, represented by the following formula (I):09-25-2008
20090105327Dibenzocycloheptane compounds and pharmaceuticals containing these compounds - The present invention relates to compounds of the formula I04-23-2009
20090258922COMPOUND EXHIBITING PGD2 RECEPTOR ANTAGONIST - A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like.10-15-2009
20100179209Pactimibe medicaments for preventing/treating a disease due to sebaceous gland dysfunction in humans or animals - Administration of at least one compound selected from N-(1-octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2-dimethylpropanamide (pactimibe) of formula (I):07-15-2010
20100179208Use of HDAC Inhibitors for the Treatment of Bone Destruction - The present invention relates to the use of HDAC inhibitors for the treatment of bone destruction caused by cancer, inflammatory diseases and osteoporosis.07-15-2010
20100216861AMINO ARYLSULFONAMIDE COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS - The present invention relates to novel amino arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them: The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The compounds of the invention are useful in the treatment of various disorders that are related to 5-HT08-26-2010
20090247602COSMETIC USE OF CONJUGATED COMPOUNDS OF INDOLIC AUXINS - The invention has for object the cosmetic use and as neurotrophic agent of at least an indolic auxin conjugate with general formula (I):10-01-2009
20100137399PREVENTIVE AND/OR THERAPEUTIC AGENT FOR URINE COLLECTION DISORDER ACCOMPANYING LOWER URINARY TRACT OBSTRUCTION - An agent for the treatment of urine collection disorders associated with lower urinary tract obstructive disease, characterized by containing an indoline derivative represented by the following general formula (I):06-03-2010
20090076121DEUTERIUM-ENRICHED SUMATRIPTAN - The present application describes deuterium-enriched sumatriptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090076123Medical Compositions for Intravesical Treatment of Bladder Cancer - Anti-cancer coating compositions comprising 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-[1H-indole-4,7-dione]propenol (E09) are disclosed. More specifically, the coating compositions comprise EO9 and a formulation vehicle. The formulation vehicle improves the solubility and stability of EO9. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.03-19-2009
20090069400Indole Sulfonamide Modulators of Progesterone Receptors - Compounds of Formula (I), wherein n is 1 or 2, and R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, their preparation, pharmaceutical compositions, and methods of use are disclosed.03-12-2009
20110245315INDOLYL OR INDOLINYL HYDROXAMATE COMPOUNDS - Indolyl or indolinyl compounds of formula (I):10-06-2011
20110039908Inhibiting Amyloid-Beta Peptide/Rage Interaction At The Blood-Brain Barrier - Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-β peptide (Aβ) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of Aβ in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving Aβ/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of Aβ into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.02-17-2011
20110124701USE OF HDAC INHIBITORS FOR THE TREATMENT OF LYMPHOMAS - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I):05-26-2011
20090306170SYNTHESIS OF TEGASEROD OR A SALT THEREOF - The present invention relates to a novel process for the synthesis of 1-((5-methoxy-1H-indol-3-yl)methyleneamino)-3-pentyl-guanidine, commonly known as tegaserod, which is used as a gastroprokinetic, and salts thereof. The present invention also relates to tegaserod and salts thereof having an HPLC purity of about 95% or more. The present invention further relates to pharmaceutical compositions comprising tegaserod or a salt thereof, second medical uses of tegaserod or a salt thereof, and methods of treating or preventing irritable bowel syndrome using tegaserod or a salt thereof.12-10-2009
20100063127Antioxidant Properties of Tryptophan from Human Milk - As tryptophan is not available in sufficient amounts in infant formula or other replacement milks, we describe herein the supplementation of these milks to attain a Trp concentration similar to that of human milk. Such supplemented milks provide greater protection against free radicals.03-11-2010
20110077281Formulations Comprising Triptain Compounds - The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides T03-31-2011
20100120886ARYL-SUBSTITUTED SULFONAMIDES FOR THE TREATMENT OF COGNITIVE OR FOOD INGESTION RELATED DISORDERS - The present invention relates to aryl-substituted sulfonamides with 5-HT05-13-2010
20110251254NOVEL SALT OF TEGASEROD - The present invention relates to a novel salt of tegaserod, namely tegaserod suberate, and to processes for the preparation thereof. The invention also relates to crystalline forms of the novel salt and to pharmaceutical compositions comprising the novel salt. Further, the invention relates to uses of said compositions in treating patients suffering from gastrointestinal disorders.10-13-2011
20100069458COMBINATION OF LBH589 WITH OTHER THERAPEUTIC AGENTS FOR TREATING CANCER - The invention relates to a combination comprising the N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.03-18-2010
20080242717METHODS FOR TREATING BENIGN PROSTATIC HYPERPLASIA - Patients having symptoms associated with benign prostatic hyperplasia can be treated with a once daily composition containing silodosin or a pharmaceutically acceptable salt thereof.10-02-2008
20110054002ALKYL INDOLE-3-CARBINOL-DERIVED ANTITUMOR AGENTS - Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I:03-03-2011
20100324106COMPOUNDS - The present invention relates to novel indole derivatives having pharmacological activity, processes for their preparation, compositions containing them and the use of these compounds in the treatment of estrogen receptor beta mediated diseases.12-23-2010
20100331387LYOPHILIZED PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions that include a poorly water-soluble therapeutic compound, an aqueous solvent, an chelator/antioxidant, a buffer or buffer component, and a bulking agent. The pharmaceutical compositions can be orally ingested or administered parenterally. The pharmaceutical compositions can further be lyophilized to form a pharmaceutically acceptable cake that can be administered orally, e.g., as a solid oral dosage form; or reconstituted and administered parenterally, e.g. as a single i.v. bolus or iv infusion, or administered orally, e.g. as a drink solution.12-30-2010
20090176857Use of Organic Compounds - The invention relates to a pharmaceutical composition, use, or method in the treatment of Irritable Bowel Syndrome (IBS) characterized by mixed or alternating bowel habits based on a modification of the Rome II criteria (IBS-M), with 5-hydroxytryptamine type-4 receptor agonists (07-09-2009
20100022613Compounds Having CRTH2 Antagonist Activity - Compounds of general formula (I)01-28-2010
20080262071Pindolol for the Treating Premenstrual Syndrome and Premenstrual Dysphoric Disorder - In accordance with the present invention, it has been discovered that pindolol provides a highly effective treatment for PMS and/or PMDD. As such, the present invention generally relates to methods and compositions for treating and/or preventing PMS, or symptoms associated therewith including premenstrual tension or premenstrual dysphoria. The methods and compositions of the invention also involves the use of pindolol, a known beta adrenergic blocker, in combination with known contraceptives.10-23-2008
20110306648APOPTOSIS INHIBITOR - Disclosed is an apoptosis inhibitor containing an indole derivative represented by the following formula (1) or a salt thereof as an active ingredient, wherein R12-15-2011
20120010262CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND - The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.01-12-2012
20120309809PROCESS AND PRODUCT - A method of processing an active ingredient, the method comprising submitting a pharmaceutically active ingredient in the absence of excipients and/or additives to compression and shearing forces. The invention also relates to compositions comprising an active prepared by the method.12-06-2012
20120316215COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISORDERS - Disclosed are methods for treating a subject suffering from phenylketonuria and/or phenylalanemia. The methods include, in part, enterally administering to the subject a LNAA supplement in which the weight ratio of Leu to Val is greater than 2:1; in which the weight ratio of Leu to iLeu is greater than 3:1; or which includes one or more LNAAs and which further includes Lys. LNAA supplements are also disclosed. Also disclosed are methods for treating a subject suffering from a condition involving a metabolic disorder involving the metabolism of a first amino acid X. The method includes enterally administering to the subject a composition which (i) is substantially free from the first amino acid X and (ii) which includes a second amino acid Y that competes with amino acid X at a gastrointestinal tract transporter.12-13-2012
200901315057-Amido-isoindolyl Compounds and Their Pharmaceutical Uses - The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.05-21-2009
20090131504USE OF MELATONIN-CONTAINING ORAL SUPPLEMENT WITH ANIMALS - The diet of a healthy non-human animal is supplemented with a melatonin-containing supplement by providing a dietary supplement containing melatonin in an amount from about 0.1 mg to about 12 mg/kg of body weight of the animal and administering the dietary supplement to the animal at a regular interval. The selected interval may be daily, weekly, monthly, or seasonally. The melatonin-containing supplement is in the form of a pill, a tablet, a capsule, a powder, a liquid, or is incorporated into food or food pellets. The method is practiced on cats and dogs.05-21-2009
20110184039PHARMACEUTICAL FORMULATION - A pharmaceutical composition comprising: a) a 5-HT1 agonist; b) an NSAID; and c) a disintegrant characterised in that the disintegrant comprises between about 15 to about 50% w/w based on the weight of the composition, said composition optionally comprising one or more other pharmaceutically acceptable excipients.07-28-2011
20100048663Substituted Aryl-Indole Compounds and Their Kynurenine/Kynuramine-Like Metabolites As Therapeutic Agents - This invention is directed to substituted aryl compounds, which are linked to a substituted indole moiety by various linkers, and the kynurenine/kynuramine-like metabolites of these agents, their preparation and pharmaceutical compositions containing these compounds. This invention further is directed to the pharmaceutical use of the compounds for inhibiting GSK3β kinase and/or modulating N-methyl-D-aspartate (NMDA) channel activities for the treatment of neurodegenerative and other disorders.02-25-2010
20120178787MELATONIN AND ITS USE IN PREVENTING POSTOPERATIVE COMPLICATIONS - The invention relates to the use of melatonin, either alone or in combination with at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof, for the manufacture of a medicament for the therapeutic treatment, prophylactic treatment and/or prevention of postoperative infectious and/or non-infections complications induced by surgical interventions wherein the infectious complications may be pneumonia, wound infection (wound dehiscence), intra-abdominal abscess, and urinary tract infections (UTI) or wherein the non-infectious complication may be anastomotic leak, a pharmaceutical formulation comprising melatonin and at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof and a method for the therapeutic and/or prophylactic treatment of postoperative infectious and/or non-infectious complications induced by surgical interventions.07-12-2012
20090082418DEUTERIUM-ENRICHED FLUVASTATIN - The present application describes deuterium-enriched fluvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20100292292Treatment of Neurodegenerative Diseases Using Indatraline Analogs - Methods and compositions useful in the treatment or prevention of synucleinopathies, such as Parkinson's disease, diffuse Lewy body disease, and multiple system atrophy, or other neurodegenerative diseases (e.g., amyotrophic lateral sclerosis, Huntington's disease, and Alzheimer's disease) are provided. The treatment including administering to a subject an indatraline derivative that inhibits the aggregation of α-synuclein.11-18-2010
20120252862Dissolvable Film Strip Comprising Natural Components - The present invention relates to film strips which comprise natural product formulations and can be absorbed from oral mucosa. The said film strip can be used with the aim of preventing and treating diseases in a short time, by being absorbed rapidly when it is applied from the oral mucosa at lower dosages than the dosage forms known.10-04-2012
20120252863TRIPTANS FOR THE TREATMENT OF PSORIASIS - The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration.10-04-2012
20080300291POTENT INDOLE-3-CARBINOL-DERIVED ANTITUMOR AGENTS - Compounds and methods for treating cancer and inducing apoptosis in unwanted rapidly proliferating cells. The compounds are shown in formula I:12-04-2008
20090318526Use of cannabinoid receptor agonists as hypothermia inducing drugs for the treatment of ischemia - The present invention relates to the use of a cannabinoid receptor agonist for use in induction of hypothermia in a human being for the prophylaxis and treatment of ischemia.12-24-2009
20110319464METHODS FOR TREATING BENIGN PROSTATIC HYPERPLASIA - Patients having symptoms associated with benign prostatic hyperplasia can be treated with a once daily composition containing silodosin or a pharmaceutically acceptable salt thereof.12-29-2011
20090215853Flavopereirine and alstonine combinations in the treatment and prevention of prostate cancer - A method and composition for preventing prostate cancer and/or reducing PSA levels and/or alleviating the symptoms of BPH (Benign Prostatic Hyperplasia) or PIN (prostatic intraepithelial neoplasia) by administration of an effective amount of a mixture of flavopereirine and alstonine. A method and composition for treating low-grade prostate cancer and preventing the onset of metastatic disease and/or reducing the doubling time of PSA levels in men with positive biopsies showing relatively low Gleason scores and morphologies characteristic of non-invasive, slow-progressing prostate cancer. The flavopereirine and alstonine can be in the form of natural extracts derived from 08-27-2009
20080242718System and method for using platelet biomarkers for diagnosis and treatment of neuro-psychiatric conditions - The invention concerns in-vitro evaluation of intracellular biomarkers by doing blood testing. Concentrations of neurotransmitters in the platelet cells are utilized to identify chemical imbalance in the central nervous system. In one embodiment of the invention, testing data is analyzed by proprietary software algorithms by physicians and related health care professionals to diagnose and treat sufferers of chemical imbalance objectively. In another embodiment of the invention the testing and software predetermines risks of developing various neuropsychiatric conditions, like depression, Parkinson's, Alzheimer's, bipolar disorder, ADD/ADHD, autism, asperger's syndrome, OCD and other anxiety disorders, muscle disorders, etc.10-02-2008
20090156657ANTI-INFLAMMATORY COMPOSITION - The present invention provides a method of improving or preventing various conditions through suppression of the expression of inflammatory cytokines based on the action mechanism of suppression of NF-κB activation. The present invention provides a composition for suppressing NF-κB activation, containing a serotonin derivative such as feruloyl serotonin (N-feruloyl serotonin) and p-coumaroyl serotonin (N-(p-coumaroyl)serotonin), a composition for suppressing the expression of VCAM-1 and/or MCP-1 via NF-κB, containing the serotonin derivative and an anti-inflammatory composition containing the serotonin derivative. The composition of the present invention can be used as a pharmaceutical agent or a food.06-18-2009
200802343562-PHENYL-3,3,3-TRIFLUORO-2-HYDROXY-PROPIONIC ACID DERIVATIVES - The present invention a method of treating anxiety by administering compounds that are active on the GABA09-25-2008
20080227845CYCLOOXYGENASE-2 INHIBITOR/HISTONE DEACETYLASE INHIBITOR COMBINATION - The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of pre-malignant colon lesions or a colon cancer or other malignancies in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.09-18-2008
20080227844Methods for Treatment with Bucindolol Based on Genetic Targeting - The present invention concerns the use of methods for evaluating bucindolol treatment for a patient, particularly one with heart failure. It concerns methods for determining whether to administer or prescribe bucindolol to a patient based on whether the patient is homozygous for the Arg 389 polymorphism in the β1-adrenergic receptor (AR).09-18-2008
200802211951,2-DIARYLACETYLENE DERIVATIVES OF ACYLTRYPTOPHANOLS - The present invention relates to acyltryptophanols of the general formula I,09-11-2008
20080221194Novel Potassium channel Blockers and Uses Thereof - The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells.09-11-2008
20130096175Compounds and Methods for Altering Lifespan of Eukaryotic Organisms - Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.04-18-2013
20110275691METHODS OF TREATING HEADACHES USING 5-HT AGONISTS IN COMBINATION WITH LONG-ACTING NSAIDS - The invention is directed to methods and compositions that can be used in the treatment of headaches. In particular, methods and compositions are described involving the combination of a long-acting NSAID and a 5-HT111-10-2011
20130150423TOPICAL THERAPY FOR MIGRAINE - The invention is directed to formulations and methods of treating a migraine and/or cluster headache with a serotonin agonist, pharmaceutically acceptable salt thereof, or derivative thereof.06-13-2013
20100286225DIAZENIUMDIOLATE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. - Compounds of formula (I):11-11-2010
20100292291FORMULATIONS OF DEACETYLASE INHIBITORS - The present invention provides a stable parenteral formulation of histone deacetylase inhibitors.11-18-2010
20130123326ALLOSTERIC BINDING COMPOUNDS - The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.05-16-2013
20120029047USE OF HDAC INHIBITORS FOR THE TREATMENT OF BONE DESTRUCTION - The present invention relates to the use of HDAC inhibitors for the treatment of bone destruction caused by cancer, inflammatory diseases and osteoporosis.02-02-2012
20130197052TRYPTAMINE DERIVATIVES, THEIR PREPARATION AND THEIR USE IN GASTROPATHY - The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage.08-01-2013
20120046331Antifungal Agents and Uses Thereof - This invention relates to new antifungal agents, compositions thereof, and methods for inhibiting the growth of fungi involved in infection and disease of keratinized tissue, such as onychomycosis. The invention also relates to new antifungal agents, compositions thereof, and methods for treating and/or preventing fungal infection and/or disease of keratinized tissue, such as onychomycosis. The invention further relates to a kit comprising said antifungal agent and use of said kit in treatment of fungal infection and/or disease of keratinized tissue, such as onychomycosis.02-23-2012
20120071537New Oral Formulation - The present invention relates to a pharmaceutical composition, in particular to a composition for administering active agents which are poorly soluble in aqueous media, and/or which are acid sensitive.03-22-2012
20120095070PREVENTION AND TREATMENT OF SARCOPENIA - The present invention provides a means for prevention and treatment of sarcopenia by administration of a substance that both reduces the sensibility of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propanol, tertalol, or bopindolol are preferred for this purpose.04-19-2012

Patent applications in class The bicyclo ring system consists of the five-membered hetero ring and a benzene ring (e.g., indole, etc.)

Patent applications in all subclasses The bicyclo ring system consists of the five-membered hetero ring and a benzene ring (e.g., indole, etc.)