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|| List of recent Indole-related patents
|Oxindole compounds carrying a nitrogen-bound spiro substituent and use thereof for treating vasopressin-related diseases|
The present invention also relates to pharmaceutical compositions comprising the novel substituted oxindole derivatives of the formula i, and to their use for the treatment of vasopressin-related disorders. .
|Prodrugs of substituted azaindoleoxoacetic piperazine derivatives|
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives.
Bristol-myers Squibb Company
|Indole compounds for use in treating inflammation and cancer|
Provided herein are compounds, comprising formula (i) or formula (ii), and their pharmaceutically acceptable salts. Also provided are pharmaceutical compositions comprising a pharmaceutically acceptable excipient and at least one compound of formula (i) and (ii), singly or in combination with other pharmaceutically active ingredients, such as anti-inflammatory agents or anticancer agents.
Board Of Trustees Of The University Of Arkansas
|Improved 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
|Indole carboxamide derivatives as p2x7 receptor antagonist|
Wherein r1, r2, r3, r4, r5 and r6 are as defined in the description, their preparation and their use as pharmaceutically active compounds.. .
|Indolealkylamino-withasteroid conjugates and use|
A group of indolealkylamino-withasteroid conjugates, isolated and purified from withania somnifera, are described. A synthetic method of making an indolealkylamino-withasteroid compound is provided.
|Fluorescent isoindoline dyes|
The present invention provides a new class of excited state intramolecular charge transfer (esipt) dye compounds based on mono or dihydroxy substituted 1,3-bisiminoisoindole motif and metal complexes containing such compounds as ligands. The present invention also provides oleds containing the compound and/or metal complex as the emissive material..
The University Of Southern California
|Indole and indoline-type piperidine compounds and uses thereof|
The disclosure relates to indole-type piperidine compounds, indoline-type piperidine compounds and related piperidine-type bicyclic compounds containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an indole-type piperidine compound, indoline-type piperidine compound or related piperidine-type bicyclic compound containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring.. .
|Compounds and methods for treatment of hypertension|
Hydrogenated pyrido[4,3-b]indoles and pyrido[3,4-b]indoles are described. The compounds may bind to and are adrenergic receptor α2b antagonists.
Medivation Technologies, Inc.
|N-heterocyclic carbene-catalyzed synthesis of 2-aryl indoles|
Transition metal-free catalytic methods for access to 2-arylindole compounds.. .
Where the various groups are defined herein, and which are useful for treating cancer.. .
Diagnostic markers of indolent prostate cancer
A 3-gene prognostic panel has been identified that together accurately predicted the outcome of low gleason score prostate tumors as either truly indolent or at a high risk of becoming aggressive. The 3-gene prognostic panel was validated on independent cohorts confirmed its independent prognostic value, as well as its ability to improve prognosis with currently used clinical nomograms.
The Trustees Of Columbia University In The City Of New York
3,5-diarylazaindoles as dyrk1a protein inhibitors for the treatment of cognitive deficiencies associated with down's syndrome and with alzheimer's disease
The present invention relates to a compound of formula (i′) or a pharmaceutically acceptable salt, solvate or hydrate thereof, in which: x3 is f, oh or sh, y3 is f, oh or sh, x1, x2, x4, x5, y1, y2, y4 and y5 are, independently of one another, h, f, cl, br, oh or sh, and 1 to 2 groups among the x1, x2, x4 and x5 radicals are other than h and/or 1 to 2 groups among the y1, y2, y4 and y5 radicals are other than h. The present invention also relates to a compound of formula (i′) for use as a medicament, in particular in the prevention and/or treatment of cognitive disorders associated with a dysfunction of the dyrk1a protein..
Universite Paris Diderot Paris 7
New derivatives of indole for the treatment of cancer, viral infections and lung diseases
The present invention relates to a new class of indole derivatives, having a particular mklp2 inhibition profile and useful as a therapeutic agent, in particular for the treatment of cancer, viral infections and lung diseases.. .
Indole derivatives as inhibitors of histone deacetylase
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (hdac8). Also described herein are methods of using such hdac8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of hdac8 activity..
Genetic assay to determine prognosis in polycythemia vera patients
The presently disclosed subject matter provides a genetic assay to determine the prognosis in polycythemia vera (pv) patients with an indolent form of pv. This assay involves measuring certain messenger rnas (mrnas) in blood cells, such as white blood cells.
Pictet-spengler ligation for protein chemical modification
Aldehyde- and ketone-functionalized proteins are promising new substrates for the development of chemically modified biotherapeutics and protein-based materials. Their reactive carbonyl groups are typically conjugated with a-effect nucleophiles, such as substituted hydrazines and alkoxyamines, to generate hydrazones and oximes, respectively.
Spiro-oxindole compounds and their use as therapeutic agents
This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.. .
New spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors
Wherein the groups r1 to r7, v, w, x, y, n and q are 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.. .
Azaindole derivatives as jak3 inhibitors
The present disclosure provides compounds that are jak3 inhibitors and therefore useful for the treatment of diseases treatable by inhibition of jak3 such as cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds..
Indole compounds and their use as antimicrobials
indole compounds of formula i, as well as compositions including the compounds and methods for their use, are disclosed that are useful for treating bacterial and/or fungal infections. Indole compounds of formula i, compositions and methods are disclosed that also are useful for killing or inhibiting the growth of bacteria and/or fungus:.
Compound; tautomer and geometric isomer thereof; salt of said compound, tautomer, or geometric isomer; manufacturing said compound, tautomer, isomer, or salt; antimicrobial agent; and anti-infective drug
The present invention provides compounds belonging to 3-acyloxyindole compounds or 3-acyl-4-hydroxycoumarin compounds, a tautomer or geometric isomer thereof, or a salt thereof and methods for producing the same, which compounds are useful as antibacterial agent and as therapeutic drugs against infectious diseases.. .
Use of gtf21 mutations in the prognosis of thymic cancers
Disclosed are methods of determining the prognosis of thymic cancer in a subject comprising detecting a mutation in the general transcription factor iii (gtf2i) genetic sequence or protein. The presence of a gtf2i mutation indicates that the thymic cancer is indolent..
Prognostic individuals with prostate cancer
The present invention relates generally to the detection and identification of various forms of genetic markers, and various forms of proteins, which have the potential utility as diagnostic markers. By determining the level of a plurality of biomarkers and genetic markers in a patient sample, and combining the obtained values according to a predefined formula, it is possible to forecast if it is likely that the prostate cancer patient will require active therapy like radiation therapy or surgery.
Processes and intermediates for producing azaindoles
The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of janus kinases (jak).. .
2-oxo-2,3-dihydro-indoles for the treatment of cns disorders
As well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.. .
Indole derivatives and use thereof
And pharmaceutically acceptable salts and solvates thereof, wherein r1e, r1f, a, x, y, z, and w4 are defined as set forth in the specification. The invention also provides the use of compounds of formula i and the pharmaceutically acceptable salts and solvates thereof to treat pain.
Compounds and methods of use thereof
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..
Substituted indole derivatives
The present invention relates to substituted indole derivatives, to processes for their production, to new stable forms, their use as pharmaceuticals and to pharmaceutical compositions comprising them.. .
7-substituted indole mcl-1 inhibitors
Compounds which inhibit the activity of anti-apoptotic mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated mcl-1 protein are disclosed.. .
Oxindole inhibitors of tyrosine kinase
The present invention relates to new oxindole inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.. .
1h-indole-3-carboxamide derivatives and use thereof as p2y12 antagonists
And to the use thereof as p2y 12 receptor antagonists for the treatment of cardiovascular diseases.. .
The present invention relates to compounds for use as therapeutic agents, particularly in the treatment and/or prevention of proliferative disorders, such as cancer, especially brain cancers/tumours, wherein the compounds are generally defined by the formula i: wherein a is an aryl or heteroaryl ring system; and r1 to r4 are various possible substituent groups, provided that at least one of an r2 group, the r3 group, or an r4 group is or comprises a hydroxy, amino, nh(rx), or mercapto group.. .
University Of Central Lancashire
Compounds and methods for treatment of hypertension
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α2b antagonists.
Medivation Technologies, Inc.
Use of the aminoalkylindole jwh-073-m4 and related compounds as neutral cb1 recptor antagonists for the treatment of alcoholism, drug abuse, obesity, and obesity-related diseases
Novel alkylindoles that bind tightly to cannabinoid receptors and are neutral antagonists for the cannabinoid 1 receptor and agonists for the cannabinoid 2 receptor are provided. These compounds are useful for treating alcoholism and drug abuse and for treating obesity..
The University Of Kansas
Organic electroluminescent device
In which ind101 represents a substituted or unsubstituted indole ring, l101 represents a linking group, ind101 and l101 are connected to each other at 2- or 3-position of ind101, and n101 represents an integer of 2 or more.. .
Molecular signature for aggressive squamous cell carcinomas of the head and neck
The present invention encompasses methods of classifying hnscc tumors, such as oscc tumors, as aggressive or, alternatively, indolent.. .
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..
Oxindole compounds and compositions comprising the same
These compounds are believed to exhibit antioxidant properties. A composition comprises an organic material and a compound conforming to the structure of formula (i)..
Gut barrier dysfunction treatment and prevention
Methods are disclosed for treating and preventing gut barrier dysfunction or an illness associated with gut barrier dysfunction in a subject comprising administering to the subject bacterium that produce an indole or an indole metabolite and for identifying compounds and bacteria for use in treatment and prevention of gut barrier dysfunction or an illness associated with gut barrier dysfunction.. .
Albert Einstein College Of Medicine Of Yeshiva University
Pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives and methods of use
This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. 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.
Isotopologues of isoindole derivatives
Provided herein are isoindole derivatives, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided..
Nitrogen-containing heterocyclic derivative, organic electroluminescence element material using same, and organic electroluminescence element and electronic device using same
A nitrogen-containing heterocyclic derivative in which an indole structure is fused to a benzophenanthrene ring is a novel material useful as a material for organic electroluminescence devices for the production of organic electroluminescence devices and electronic equipment.. .
Idemitsu Kosan Co., Ltd.
7-azaindole-2,7-naphthyridine derivative for the treatment of tumours
The compound 4-(2-methyl-1h-pyrrolo[2,3-b]pyridin-3-yl)-2,7-naphthyridin-1-ylamine and pharmaceutically usable salts and/or tautomers thereof. The use of this compound for the treatment of tumours, tumour growth, tumour metastases and/or aids..
Merck Patent Gmbh
4-(indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
The invention provides novel indole-and benzimidazole-substituted diaminopyrimidines of formula i, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds treatment of diseases including cancer; wherein r1-r3 are as defined in the specification.. .
Noviga Research Ab
Process for preparation of perindopril intermediate
The present invention relates to an improved process for the preparation of (2s,3as,7as)-1-[(2s)-2-[[(1s)-1-(ethoxycarbonyl)butyl]amino]3-s-oxopropyl]octahydro-1h-indole-2-carboxylic acid benzyl ester (the compound of formula ii) comprising reacting (2s,3as,7as)-octahydro-1h-indole-2-carboxylic acid phenylmethyl ester 4-methylbenzenesulfonate (the compound of formula iii) with n-[(s)-ethoxycarbonyl-1-butyl]-(s)-alanine (the compound of formula iv), using 1-hydroxybenzotriazole (hobt), dicyclohexylcarbodimide (dcc) and triethylamine in the presence of toluene as a solvent at a temperature of 5-40° c.. .
Piramal Enterprises Limited
Processes for the preparation of 3-alkyl indoles
This invention provides processes for preparation of 3-alkyl indoles of formula 1: wherein a1, a2 and a3 are independently selected from the group consisting of: h, x, or1, cn, conr22 and c02r3; r1 is c1-c6 alkyl; r2 is h or c1-c6 alkyl; r3 is c1-c6 alkyl; lg is a leaving group; x is a halogen; and n is 1, 2 or 3.. .
Apotex Pharmachem Inc.
Novel spirooxindole derivative and process for producing the same
Disclosed is a compound of formula i: wherein r1?, r2?, r3?, r4?, r5?, n and m are defined herein. The compound of formula i is prepared by a concise, catalytic enantioselective formal hetero-diels-alder (hda) reactions of enones with isatins and is useful for making pharmaceutical composition for the treatment of proliferative diseases..
Okinawa Institute Of Science And Technology School Corporation
9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
And the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein r1a, a, b1, b2, g, x1, y1, y2, and y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula i to treat a condition or disorder responsive to inhibition of bet bromodomains.
Process for photocatalytic acceptor-free dehydrogenation of hydrocarbazoles and hydroindoles
A process for the photocatalytic acceptor-free dehydrogenation of hydrocarbazoles and hydroindoles is provided, wherein a hydrocarbazole or hydroindole is irradiated in the presence of a catalyst that is a rhodium complex containing organic phosphorus(iii) compounds as ligands.. .
Evonik Industries Ag
Novel compound and organic electroluminescence device including thesame
The present invention relates to a novel indole-based compound having excellent hole injection and transport capabilities, light-emitting capabilities, and the like, and an organic electroluminescence device which includes the indole-based compound in one or more organic material layers thereof so as to improve characteristics such as light-emitting efficiency, driving voltage, and lifespan.. .
Azaindoles as respiratory syncytial virus antiviral agents
Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.. .
And pharmaceutically acceptable salts thereof, wherein l, r1, r2, r3, r4, r5, r6, and r7 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with metap2..
Substituted oxindole derivatives, medicaments containing said derivatives and use thereof
The invention relates to novel oxindole derivatives of general formula (i), wherein the substituents r1, r2, a, b, and y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases..
Abbvie Deutschland Gmbh & Co. Kg
6-aminoindole derivatives as trp channel antagonists
And pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (i) as well as pharmaceutical compositions containing such compounds.
Process of producing cycloalkylcarboxamido-indole compounds
The present invention features processes for preparing compounds, such as (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl)cyclopropanecarboxamide (compound 1), useful for treating cftr mediated diseases such as cystic fibrosis.. .
Vertex Pharmaceuticals Incorporated
The invention provides a 1,3,5-substituted indole wherein the substituent at position 1 is a c6 to c12 alkyl group; the substituent at position 3 is ch2nr1r2 wherein r1 is h or c1 to c3 alkyl, r1 being optionally substituted with —oh, —sh, —nh2 or nhalkyl, wherein alkyl is a c1 to c4 alkyl group, and r2 is c1 to c3 alkyl or (ch2)n bonded to position 2 of the indole, wherein n is 1, 2 or 3; and the substituent at position 5 is either an optionally substituted nitrogen containing heteroaromatic ring or an aminosulfonylphenyl group or an alkylsulfonylphenyl group.. .
National University Of Singapore
Ipa as a therapeutic agent, as a protective agent, and as a biomarker of disease risk
indole-3-propionic acid as a marker and for treatment for huntington disease.. .
Counterpoint Health Solutions, Inc.
Methods of treating pain associated with osteoarthritis of a joint with a topical formulation of a spiro-oxindole compound
Are disclosed. The methods provide excellent penetration of the spiro-oxindole compound into the synovial membrane of the affected joint to effectively reduce the severity of the pain and/or to alleviate the pain with minimal or negligible systemic exposure..
Azaindole carboxylic acid amides and azaindole thiocarboxylic acid amides for use as insecticides and acaricides
In which r1 to r6, a, y, x, q1, q2, n and m are each as defined in the description and to a process for their preparation and to their use as insecticides and acaricides.. .
Organic electroluminescent materials and devices
A luminescent compound that is a metal complex with ligands containing pyrrole or indole in the structure, where the pyrrole or inidole has an aromatic substitutent that has at least one ortho substitution is disclosed.. .
Universal Display Corporation
Organic light-emitting compound and organic electroluminescent device using same
The present invention relates to a novel indole-based compound having excellent hole injection and transport capabilities, light-emission, and other properties, and to an organic electroluminescent device the luminous efficiency, driving voltage, service life, and other characteristics of which are improved due to containing the compound in one or more organic material layers.. .
Crystals of dispiropyrrolidine derivatives
Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of mdm2 are provided. The present invention provides crystals of (3′r,4′s,5′r)-n-[(3r,6s)-6-carbamoyltetrahydro-2h-pyran-3-yl]-6″-chloro-4′-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2″-oxo-1″,2″-dihydrodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indole]-5′-carboxamide or a salt thereof which inhibits mdm2 and has anti-tumor activity.
Daiichi Sankyo Company, Limited
Indole-substituted pyrrolopyrimidinyl inhibitors of uba6
Disclosed are chemical entities that inhibit uba6, each of which is a compound of formula /: formula (i) or a pharmaceutically acceptable salt thereof, wherein r*1 is —h or —ch3; and y is formula (ii) or formula (iii), wherein r2 is —h, —ch3 or c1-4 alkyloxycarbonyl; and rs7.1, rs7.2 and rs8.1 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers..
Millennium Pharmaceuticals, Inc.
N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
The present invention relates to compounds according to formula i and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of rorgammat-mediated diseases or conditions..
Merck Sharp & Dohme Corp.
Histamine 4 receptor partial agonists, inverse agonists or antagonists for use in treating non-autoimmune uveitis
The invention provides a compound which is a histamine 4 receptor antagonist, partial agonist or inverse agonist, for use in the treatment of non-autoimmune uveitis. The compound preferably has a structural core comprising a substituted pyrimidine group, such as an aminopyrimidine, diaminopyrimidine or triaminopyrimidine group, a thienopyrimidine, a furopyrimidine, a benzimidazole, an aryl or heteroaryl-fused pyrimidine, an indole, a bicyclic heteroaryl-substituted imidazole or a quinazoline group..
Ucl Business Plc
Indole carboxamide derivative
The present inventors have conducted studies on mt1 and/or mt2 receptor agonists, and have found that an indole carboxamide compound has an mt1 and/or mt2 receptor agonistic action, thereby completing the present invention. The indole carboxamide compound of the present invention has the mt1 and/or mt2 receptor agonistic action as well as a low cns penetration, and therefore, it can be used as an agent for preventing and/or treating urological diseases; in one embodiment, lower urinary tract symptoms; in another embodiment, urine storage symptom, in another embodiment, urinary incontinence; in a still another embodiment, stress urinary incontinence; and the like..
Process for preparing substituted indole derivatives
The present invention relates to a process for preparing substituted indole derivatives. More particularly, the invention refers to a new method to synthesize indole-derivatives by oxidative c—h-functionalization..
Studiengesellschaft Kohle Mbh
Indole and azaindole derivative having ampk-activating activity
R4, r7 and r8 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or the like.. .
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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