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Indole patents



      

This page is updated frequently with new Indole-related patent applications.




Date/App# patent app List of recent Indole-related patents
05/19/16
20160137653 
 Immunoregulatory agents patent thumbnailnew patent Immunoregulatory agents
Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided..
Flexus Biosciences, Inc.


05/19/16
20160137652 
 Immunoregulatory agents patent thumbnailnew patent Immunoregulatory agents
Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided..
Flexus Biosciences, Inc.


05/19/16
20160137601 
 Method for providing stable isoindole derivatives patent thumbnailnew patent Method for providing stable isoindole derivatives
Method for producing an isoindole derivative, the isoindole derivative obtainable by the methods, a methods for stabilizing an isoindole derivative, and methods for detection and/or quantification of macromolecules.. .
Fraunhofer-gesellschaft Zur Foerderung Der Angewandten Forschung E.v


05/19/16
20160137595 
 Ido inhibitors patent thumbnailnew patent Ido inhibitors
There are disclosed compounds of formula (i) that modulate or inhibit the enzymatic activity of indoleamine 2,3-di-oxygenase (ido), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.. .
Bristol-myers Squibb Company


05/12/16
20160130269 
 7-azaindole derivatives patent thumbnail7-azaindole derivatives
Compounds of the formula (i) in which r, r1, r2 and r3 have the meanings indicated in claim 1, are inhibitors of pdk1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.. .
Merck Patent Gmbh


05/12/16
20160130226 
 Spiro-substituted oxindole derivatives having ampk activity patent thumbnailSpiro-substituted oxindole derivatives having ampk activity
The present invention relates to compounds of formula (i), which have valuable pharmacological properties, in particular are activators of ampk and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2..
Boehringer Ingelheim International Gmbh


05/12/16
20160128979 
 Modified release formulation patent thumbnailModified release formulation
Drug products in the form of modified release formulations comprising the drug substance (-)-(3ar,4s,7ar)-4-hydroxy-4m-tolylethynyl-octahydro-indole-1-carboxylic acid methyl ester (afq056), as well as processes for making such drug products are provided. The drug products are useful in treating patients with parkinson's disease and exhibiting l-dopa induced dyskinesia..

05/05/16
20160126468 
 Indenoindole derivative and organic electroluminescent element patent thumbnailIndenoindole derivative and organic electroluminescent element
According to the present invention, there are provided an indenoindole derivative represented by the following general formula (1); and an organic electroluminescent element including a pair of electrodes and at least one organic layer sandwiched therebetween, wherein the above compound is used as a constituent material for the at least one organic layer. The indenoindole derivative of the present invention provides an organic compound, which is excellent in hole injection/transport performance, has electron blocking capability, is highly stable in a thin film state, and excels in heat resistance, as a material for a high efficiency, high durability organic electroluminescent element.
Hodogaya Chemical Co., Ltd.


05/05/16
20160120976 
 Combination therapy with anti-cd74 and anti-cd20 antibodies in patients with relapsed and refractory b-cell non-hodgkin's lymphoma patent thumbnailCombination therapy with anti-cd74 and anti-cd20 antibodies in patients with relapsed and refractory b-cell non-hodgkin's lymphoma
The present invention concerns methods of treating relapsed/resistant non-hodgkin's lymphoma using combination therapy with an anti-cd20 antibody or fragment and an anti-cd74 antibody or fragment. In preferred embodiments, the antibody combination is administered along with at least one other therapeutic agent.
Immunomedics, Inc.


04/28/16
20160115162 
 Radiosynthesis of tau radiopharmaceuticals patent thumbnailRadiosynthesis of tau radiopharmaceuticals
This disclosure relates to a one-step method for preparing the tau radiopharmaceutical, [18f]t807, using an unprotected or protected precursor (e.g., tertbutyl 7-(6-nitropyridin-3-yl)-sh-pyrido[4,3-b]indole-5-carboxylate). An improved one-step synthesis method to prepare [18f]t807 was achieved with a protected (e.g., t-boc) precursor, offering increased solubility, a faster synthesis as well as simpler purification and automation.
The General Hospital Corporation


04/28/16
20160115156 

Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof


This invention relates to certain metabolites of n-(1-methyl-5-(trifluoromethyl)-1h-pyrazol-3-yl)-5-((6-((methyl-amino)methyl)pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide in particular, the present invention relates to pharmaceutical compositions comprising these metabolites, as well as processes for their preparation and their use in the treatment of diseases.. .
Novartis Ag


04/28/16
20160115126 

Indole carboxamide compounds


Or a salt thereof, wherein: x is cr4 or n; r1, r2, r3, r4, and a are defined herein. Also disclosed are methods of using such compounds as inhibitors of bruton's tyrosine kinase (btk), and pharmaceutical compositions comprising such compounds.

04/21/16
20160107991 

Processes and intermediates for preparing indole pharmaceuticals


The invention described herein pertains to processes and intermediates for preparing indole containing pharmaceuticals, particularly to processes and intermediates for preparing selective estrogen receptor modulators, such as bazedoxifene.. .

04/21/16
20160106869 

Fluorescent solid lipid nanoparticles composition and preparation thereof


The present invention discloses a solid lipid nanoparticle (sln) comprising: a) a solid lipid core comprising at least a glyceride and/or at least a fatty acid; b) a mixture of amphiphilic components forming a shell around said core a); c) an alkaline-earth complex with a compound of formula i and/or ii: d) at least a fluorescent dye selected from: a cyanine fluorescent dye and/or a polyetherocyclic compound selected from: coumarin, pyrano, quinoline, pyranoquinoline, indole and pyranoindole derivates in acid form or a pharmaceutically acceptable salt thereof. These nanoparticles allow a prolonged blood circulation half-life, show enhanced photostability and improved fluorescence signal.

04/21/16
20160106731 

Tricyclic indole mcl-1 inhibitors and uses thereof


The present invention provides for compounds that inhibit the activity of an anti-apoptotic bcl-2 family member myeloid cell leukemia-1 (mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of mcl-1 protein..

04/21/16
20160106711 

3-3-di-substituted-oxindoles as inhibitors of translation initiation


Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using diaryloxindole compounds are described..

04/14/16
20160102077 

Indole-3-carboxamides as kinase inhibitors


Or a pharmaceutically acceptable salt thereof, wherein r1, r2, r3, r4, r5, r6, r7, r8, r9 and x are as defined herein. The compounds of formula i are useful as receptor tyrosine kinase (rtk) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases..

04/14/16
20160102054 

Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2)


Inhibitors of protein tyrosine phosphatases are disclosed. The inhibitors include hydroxyindole carboxylic acids having a linker and an amine scaffold that are potent inhibitors of src homology 2-domain containing protein tyrosine phosphatase-2..

04/14/16
20160101083 

Anti-parasitic methods and compositions utilizing diindolylmethane-related indoles


The present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing diindolylmethane-related indoles. Additive and synergistic interaction of diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections.

04/07/16
20160098514 

Predictive test for aggressiveness or indolence of prostate cancer from mass spectrometry of blood-based sample


A programmed computer functioning as a classifier operates on mass spectral data obtained from a blood-based patient sample to predict indolence or aggressiveness of prostate cancer. Methods of generating the classifier and conducting a test on a blood-based sample from a prostate cancer patient using the classifier are described..
Biodesix, Inc.


04/07/16
20160096828 

Indole-1-carboxamides as kinase inhibitors


Or a pharmaceutically acceptable salt thereof, wherein r1, r2, r3, r4, r5, r6, r7, and x are as defined herein. The compounds of formula i are useful as receptor tyrosine kinase (rtk) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases..

03/31/16
20160091494 

Diagnostic hepatic cancer


Methods and kits for analysing a sample from a test subject. The methods involve determining the level of at least one compound selected from the group consisting of n-acetylglutamate, methionine, acetylcarnitine, indole-3-acetate, 2-oxoglutarate, anserine, aspartate and butyrate in the sample from the test subject; and comparing the level of the at least one compound determined to at least one control level, wherein the levels of the at least one compound are indicative of whether the subject has hepatic cancer..
Imperial Innovations Ltd


03/31/16
20160089368 

Treatment of mastocytosis with masitinib


The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including the administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen.. .
Ab Science


03/24/16
20160084779 

Nuclear magnetic resonance implemented synthetic indole and indazole cannabinoid detection, identification, and quantification


The present invention provides a method for detecting synthetic indole and indazole cannabinoids in a sample known or suspected to contain a synthetic indole or indazole cannabinoid. A deuterated solvent is added to the solid sample, creating a suspension.
Hofstra University


03/24/16
20160083363 

Substituted indoles as selective protease activated receptor 4 (par-4) antagonists


Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition..
Vanderbilt University


03/17/16
20160075711 

Compounds for the inhibition of indoleamine-2,3-dioxygenase


The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of ido, and for the treatment of ido-related disorders.. .
Merck Patent Gmbh


03/17/16
20160075709 

Pyrazino[1,2-a]indole compounds, their preparation and use in medicaments


Wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.. .

03/17/16
20160075703 

Substituted azaindoleoxoacetic piperazine derivatives


These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or hiv entry inhibitors. More particularly, the present invention relates to the treatment of hiv and aids..

03/10/16
20160068809 

Use of zeburaline for the treatment of autoimmune diseases or immune rejection of transplants


The invention relates to the use of 1-(β-d-ribofuranosyl)-1,2-dihydropyrimidin-2-one derivative or mimetic or an analogue, derivatives, metabolites, variants or salts thereof for the manufacturing of a medicament to increase the amount of indoleamine 2,3-dioxygenase (ido) production in order to induce immunological tolerance as well as a method of treating a mammal in need thereof.. .
Idogen Ab


03/10/16
20160068531 

Novel aza-oxo-indoles for the treatment and prophylaxis of respiratory syncytial virus infection


Wherein r1, r2, r3, r4, r5, r6, w1, w2, w3, a and x are as described herein, compositions including the compounds and methods of using the compounds.. .

03/03/16
20160060268 

Pyrazino[1,2-a]indole compounds, their preparation and use in medicaments


Wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.. .

03/03/16
20160060266 

Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization


Presently provided are inhibitors of ido and tdo and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase and tryptophan 2,3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.. .
Newlink Genetics Corporation


03/03/16
20160060237 

Ido inhibitors


There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (ido), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention. Formula (i)..
Bristol-myers Squibb Company


03/03/16
20160058770 

Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for treating lymphomas


—use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of non-hodgkin's lymphoma (nhl), particularly 1st line, 2nd line, relapsed, refractory, indolent or aggressive non-hodgkin's lymphoma (nhl), in particular follicular lymphoma (fl), chronic lymphocytic leukaemia (cll), marginal zone lymphoma (mzl), diffuse large b-cell lymphoma (dlbcl), mantle cell lymphoma (mcl), transformed lymphoma (tl), or peripheral t-cell lymphoma (ptcl); —combinations of a) said compound and b) one or more further active agents; —a pharmaceutical composition comprising said compound as a sole active agent for the treatment of non-hodgkin's lymphoma (nhl), particularly 1st line, 2nd line, relapsed, refractory, indolent or aggressive non-hodgkin's lymphoma (nhl), in particular follicular lymphoma (fl), chronic lymphocytic leukaemia (cll), marginal zone lymphoma (mzl), diffuse large b-cell lymphoma (dlbcl), mantle cell lymphoma (mcl), transformed lymphoma (tl), or peripheral t-cell lymphoma (ptcl); —a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; —use of biomarkers involved in the modification of the expression of pi3k isoforms, btk and ikk, bcr activation, bcr downstream activation of nfkb pathway, c-myc, ezh2, for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity and/or to overcome resistance; and —a method of determining the level of a component of one or more of the expression of pi3k isoforms, btk and ikk, bcr activation, bcr downstream activation of nfkb pathway, c-myc, ezh2.. .
Bayer Pharma Aktiengesellschaft


02/25/16
20160052938 

Spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors


Wherein the groups r1 to r7, a, v, w, x, y, n, r and q are as defined herein, their use as inhibitors of mdm2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.. .

02/25/16
20160051600 

Gelatinous mixture of probiotics and prebiotics with synergic symbiotic action for treating chronic renal disease


The invention relates to the fields of application of health, biotechnology and nutrition, the aim of the invention being to provide a gelatinous mixture of probiotics and prebiotics with synergic symbiotic action for the treatment of chronic renal disease, the characteristics and components thereof reducing the concentration of uremic toxins, improving the renal function of the patient with an increase in urea, creatinine, uric acid, p-cresols or indoles in the blood. The gelatinous mixture of probiotics and prebiotics with synergic symbiotic action for the treatment of chronic renal disease is easier to administrate orally as it does not require the consumption of liquids for the administration thereof, reducing liquid retention.
Nutrimentos Inteligentes, S.a. De C.v.


02/18/16
20160046648 

4-phenylpiperidines, their preparation and use


The present invention provides a compound having the structure: (structurally represented) wherein r1, r2, r3, r4, and r5 are each independently h, halogen, cf3 or c1-c4 alkyl; r6 is h, oh, or halogen; b is a substituted or unsubstituted heterobicycle, pyridazine, pyrazole, pyrazine, thiadiazole, or triazole, wherein the heterobicycle is other than chloro substituted indole; and the pyrazole, when substituted, is substituted with other than trifluoromethyl, or a pharmaceutically acceptable salt thereof.. .
The Trustees Of Columbia University In The City Of New York


02/18/16
20160046596 

Inhibitors of the kynurenine pathway


The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds.
Curadev Pharma Private Ltd.


02/11/16
20160039840 

Pyrimidine compounds and pyrimido indole compounds and methods of use


Wherein r is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the s is replaced by ch2, and optionally comprising a pharmaceutically acceptable salt, hydrate, or solvate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof..

02/11/16
20160039755 

Oxindole compounds, solvent-free synthesis and use thereof


The present invention discloses oxindole compounds and a single step, one pot reaction for the synthesis of oxindole derivates via a solvent free passerini reaction of isocyanides, isatins and carboxylic acids.. .
Council Of Scientific & Industrial Research


02/04/16
20160030446 

Pyrido [4,3-b]indole and pyrido [3,4-b] indole derivatives and methods of use


This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder..
Medivation Technologies, Inc.


02/04/16
20160030389 

Use of indole compounds for fat reduction and skin and soft tissue tightening


The present invention relates to indole compounds and compositions and uses thereof, including uses of the indole compounds and compositions for the reduction or removal of localized fat deposits and/or tightening of skin and soft tissue laxity in subjects. The indole compounds can be employed, for example, in the cosmetic sector or for producing pharmaceutical products..
Alevere Medical Corporation


01/28/16
20160024086 

Azaindole retinoic acid receptor-related orphan receptor modulators and uses thereof


As well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of retinoic acid receptor-related orphan receptor regulated diseases and disorders..

01/28/16
20160024083 

Compounds and methods for treating cancers


Provided are carbazole and carbazole-like compounds (e.g., pyridoindole and pyrrolodipyridine) compounds, that can be used to selectively kill cancer cells, specifically androgen-receptor expressing prostate cancer cells. Also provided is a method of treating ar-positive prostate cancer in a subject diagnosed with or suspected of having ar positive or negative cancer, comprising administering an effective amount of a carbazole and carbazole-like compound to said subject..
Health Research, Inc.


01/28/16
20160024075 

Indole and benzofuran fused isoquinuclidene derivatives and processes for preparing them


Provided herein are indole and benzofuran fused isoquinuclidene derivatives. Also provided herein are processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (−) and (+) noribogaine or a salt thereof, in substantially enantiomerically pure forms..
Demerx,inc.


01/28/16
20160024058 

Process for preparing benzofuran-2-carboxamide derivatives


Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of benzofuran-2-carboxamide derivatives and their intermediates, or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of vilazodone or a pharmaceutically acceptable salt thereof in high yield and purity.
Symed Labs Limited


01/28/16
20160024008 

Process for preparing benzofuran-2-carboxamide derivatives


Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of benzofuran-2-carboxamide derivatives and their intermediates, or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of vilazodone or a pharmaceutically acceptable salt thereof in high yield and purity.
Symed Labs Limited


01/28/16
20160022671 

Treatment of mastocytosis with masitinib


The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen.. .
Ab Science


01/28/16
20160022619 

Inhibitors of indoleamine 2,3-dioxygenase (ido)


There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (ido), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.. .
Bristol-myers Squibb Company


01/21/16
20160016972 

Cyclic n-acyl o-amino phenol cbi derivative


A group of cyclic n-acyl o-amino phenol cbi derivatives were synthesized and shown to be pro-drugs, subject to reductive activation by cleavage of a n—o bond, effectively releasing the free drug in functional in vitro cellular assays for cytotoxic activity approaching the activity of the free drug, yet remain essentially stable to ex vivo dna alkylation conditions. Assessment of the in vivo antitumor activity of a representative pro-drug indicates that a contemplated pro-drug approaches the potency and exceeds the efficacy of the free drug itself (cbi-indole2), indicating that the inactive pro-drugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo..
The Scripps Research Linstitute


01/21/16
20160016940 

Indole and indazole compounds that activate ampk


The present invention relates to indole and indazole compounds of formula (i) that activate 5′ adenosine monophosphate-activated protein kinase (ampk). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of ampk..
Pfizer, Inc.


01/21/16
20160015814 

Fast-acting insulin formulation comprising a substituted anionic compound and a polyanionic compound


A composition, in aqueous solution, comprising insulin in hexameric form, at least one substituted anionic compound and at least one polyanionic compound, said substituted anionic compound consisting of a discrete number n of between 1 and 8 of identical or different saccharide units, linked via identical or different glycoside bonds, said saccharide unit or one of said saccharide units being in open, oxidized or reduced form, said compound comprising salifiable carboxyl groups and said substituted anionic compound bearing on its reductive chain end at least one radical aa resulting from an aromatic amino acid comprising a phenyl or an indole, which may or may not be substituted, or an aromatic amino acid derivative comprising a phenyl or an indole, which may or may not be substituted.. .
Adocia


01/14/16
20160008359 

Azaindoles useful as inhibitors of janus kinases


The present invention relates to compounds useful as inhibitors of protein kinases, particularly of jak family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders..
Vertex Pharmaceuticals Incorporated


01/14/16
20160008334 

Preparations for the treatment of sleep-related respiratory disorders


The present invention is directed to combinations of sedating antihistamines and at least one, and preferably two or more dietary supplements, which can be indole-based, such as tryptophan, 5-hydroxytryptophan, serotonin, n-acetyl-5-hydroxytryptamine and melatonin, and to their use for treating and thereby improving the health and quality of life of those suffering from sleep-related respiratory disorders, characterized by abnormal breathing during sleep. These include snoring, sleep disordered breathing, sleep apneas, upper airway resistance syndrome, obstructive sleep apnea, central sleep apnea and obesity hypoventilation syndrome and associated ailments..
Requis Pharmaceuticals Inc.


01/07/16
20160002735 

Materials and methods for assessing progression of prostate cancer


Methods of distinguishing and identifying a patient with aggressive/indolent, prostatic adenocarcinoma comprising contacting a sample from the patient with a set of detectably labeled probes under hybridization conditions and determining the presence of chromosomal abnormalities in the sample; sets of probes for use in such methods; and kits comprising a set of probes and instructions for distinguishing or identifying a patient as having aggressive/indolent, prostatic adenocarcinoma.. .
Abbott Molecular Inc.


01/07/16
20160002249 

Fused imidazole derivatives useful as ido inhibitors


Presently provided are ido inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (ido) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.. .
Newlink Genetics Corporation


01/07/16
20160002224 

Novel indole derivatives useful as anti-diabetic agents


Novel compounds of the structural formula (i) are activators of amp-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the ampk-activated protein kinase. The compounds of the present invention may be useful in the treatment of type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension..
Merck Sharp & Dohme Corp.


01/07/16
20160002202 

2',6'-dioxo-3'-deutero-piperdin-3-yl-isoindoline compounds


The present application describes 2-(2′,6′-dioxo-3′-deutero-piperidin-3′-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.. .
Deuterx, Llc


01/07/16
20160000764 

New spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors


Wherein the groups r1 to r3, r7, u, v, w, x, y, n and q are as defined herein, their use as inhibitors of mdm2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.. .

12/31/15
20150374710 

Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds and methods of using the same in the treatemnt and/or prevention of cardiovascular diseases


Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (pcsk9), as well as therapeutic methods for use of such compounds to reduce ldl-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (cvd), including treatment of hypercholesterolemia. Examples of compounds include thiadiazole, isoxazole, 1,2,4-triazole, thiazole, indole, pyrazole, and pyrrolinone derivatives..
Shifa Biomedical Corporation


12/24/15
20150368255 

Halogenated indole and benzofuran derivatives of isoquinuclidene and processes for preparing them


Provided herein are halogenated indole and benzofuran derivatives of isoquinuclidene and intermediates thereto, and processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (−) and (+) noribogaine, in substantially enantiomerically pure forms.. .
Demerx, Inc.


12/24/15
20150368195 

Indoline compounds for treatment and/or prevention of inflammation diseases


The invention is based on the discovery that 1-arylsulfonyl-5-(n-hydroxyacrylamide)indolines and 1-arylsulfonyl-5-(n-hydroxyacrylamide)indoles has great potential as a novel agent to be used in the treatment of inflammation-associated diseases, particularly, inflammatory arthritis and fibrosis.. .
Taipei Medical University


12/24/15
20150366198 

Parasiticidal compositions comprising indole derivatives, methods and uses thereof


The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one indole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof..
Merial, Inc.




Indole topics: Indole Derivatives, Tryptophan, Pharmaceutically Acceptable Salt, Protease Inhibitors, Antivirals, Antiinfective, Pharmaceutical Formulations, Protease Inhibitor, Pharmaceutical Formulation, Immunomodulator, Entry Inhibitors, Piperazine, Cycloalkyl, Alkyl Group, Carbon Atoms

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