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| Benzofuroindole derivative and organic electroluminescence device|
According to the present invention, there are provided a benzofuroindole derivative represented by the following general formula (1); and an organic el device comprising a pair of electrodes and at least one organic layer sandwiched therebetween, wherein the above derivative is used as a constituent material for the at least one organic layer. The benzofuroindole derivative of the present invention is useful as a constituent material for a hole injection layer, a hole transport layer, an electron blocking layer or a luminous layer of an organic el device.
Hodogaya Chemical Co., Ltd.
|Organometallic complex, light-emitting element, light-emitting device, electronic device, and lighting device|
Provided is an organometallic complex which emits light with a short wavelength and has high emission efficiency and high heat resistance. The organometallic complex includes a central metal; and a first ligand, a second ligand, a third ligand, and a fourth ligand which are coordinated to the central metal.
Semiconductor Energy Laboratory Co., Ltd.
Where r1 to r4, m and n have the same meanings as those defined in the description.. .
The present inventors have studied on mt1 and/or mt2 receptor agonists, and have confirmed that indole compounds have the activity. As a result, the present invention is accomplished.
|Synthetic methods for spiro-oxindole compounds|
This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.. .
Xenon Pharmaceuticals Inc.
|Bicyclic heteroaryl indole analogues useful as ror gamma modulators|
The present disclosure is directed to compounds of formula (i) and pharmaceutically acceptable salts thereof, wherein x, x1, m, r2, r3, r4, r5, m, n, and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (rorγt). These compounds prevent, inhibit, or suppress the action of rorγt and are therefore useful in the treatment of rorγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, copd, asthma, rheumatoid arthritis, colitis, multiple sclerosis, neurodegenerative diseases and cancer..
Glenmark Pharmaceuticals S.a.
|Aryl substituted indoles and the use thereof|
The invention relates to aryl and heteroaryl substituted compounds of formula (i), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein g, r1, and z1-z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of formula (i) to treat a disorder responsive to the blockade of sodium channels.
Purdue Pharma L.p.
|Indole amide derivatives and related compounds for use in the treatment of neurodegenerative diseases|
This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders.
|Antihistamines in combination with a range of substances for improved health|
The present invention provides for novel combinations comprising an antihistamine with selected pharmaceutical and nutraceutical agents which alleviate some of the symptoms experienced by menopausal women, optionally combined further with a range of indole-based natural products such as l-tryptophan, 5-hydroxytryptophan and melatonin. These mixtures may be enriched further with pharmaceutically acceptable calcium and magnesium salts as well as selected b vitamins.
Requis Pharmaceuticals, Inc.
|Oxindole derivatives, preparation thereof and therapeutic use in the treatment of ampk-related diseases|
The present invention relates to compounds corresponding to formula (i). Process for the preparation thereof and therapeutic use thereof.
Spirocyclic compounds containing spiro[indolyl-3,1'-pyrrolo[3,4-c]pyrrole] core and sulphur-containing amino acid residues
The present invention relates to spirocyclic compounds on the basis of 2-oxindole derivatives containing a spiro[indolyl-3,1′-pyrrolo[3,4-c]-pyrrole] core and biogenic sulphur-containing amino acid residues, which display a glucocorticoid-mimicking action by influencing 11β-hsd1 enzyme cortisone->cortisol conversion, or by inhibiting grs- or gitr- or mineralocorticoid receptors, or other targets, but do not interfere with steroidal haemostasis in hpa; and compositions containing same and their use for therapy as part of undifferentiated stroke therapy (in the absence of final verification of the stroke subtype) at various stages of acute ischemic stroke (ais), during the period of recovery from stroke and craniocerebral trauma, in patients with chronic cerebrovascular pathology (against a background of diabetes), in combinational therapy for alzheimer's disease and encephalopathy of various origin (discirculatory, alcoholic, infectious-toxic), and diabetes, combinational therapy for retinal degenerative eye diseases, as part of combinational therapy for metabolic syndrome (obesity, in patients suffering from cushing's syndrome, reaven metabolic syndrome (also known as syndrome x or insulin resistance syndrome) and other diseases where gcs hormones play a key role.. .
N-benzyl tryptanthrin derivative, and preparation method and application thereof
The present invention relates to an n-benzyl tryptanthrin derivative, and preparation method and use thereof. The n-benzyl tryptanthrin derivative of the present invention is characterized in that the derivative has a structural general formula as represented by formula 1, wherein each group is defined as in the specification.
7-azaindole or 4,7-diazaindole derivatives as ikk epsilon and tbk1 inhibitor and pharmaceutical composition comprising same
Provided are 7-azaindole or 4,7-diazaindole derivatives as an ikkε (i-kappa-b kinase epsilon) and tbk1 (tank-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits ikkε and tbk1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, cns cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, b-cell or t-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation..
Green Cross Corporation
Process for large scale production of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1h-indole dimesylate monohydrate
A process suitable for adoption to large scale manufacture of 1-[(2-bromophenyl-sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1h-indole dimesylate monohydrate, which is a selective 5-ht6 receptor antagonist intended for the symptomatic treatment of alzheimer's disease and other disorders of memory and cognition like attention deficient hyperactivity, parkinson's and schizophrenia.. .
Suven Life Sciences Limited
Where the various groups are defined herein, and which are useful for treating cancer.. .
Organometallic complex, light-emitting element, light-emitting device, electronic device, and lighting device
As a novel substance having a novel skeleton, an organometallic complex with high emission efficiency is provided. The organometallic complex includes a metal and a ligand.
Semiconductor Energy Laboratory Co., Ltd.
Novel azaindole derivatives as selective histone deacetylase (hdac) inhibitors and pharmaceutical compositions comprising the same
The present invention relates to novel azaindole derivatives, and more particularly, to novel azaindole derivatives having histone deacetylase (hdac) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof or solvates thereof, the use thereof for the preparation of pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the pharmaceutical compositions, and methods for preparing the novel azaindole derivatives. The novel azaindole derivatives according to the present invention are selective histone deacetylase (hdac) inhibitors, and may be used as agents for treating malignant tumor diseases, inflammatory diseases, rheumatoid arthritis, and neurodegenerative diseases..
Chong Kun Dang Pharmaceutical Corp.
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
This disclosure features herbicidal compositions including one or more indole auxins and methods of making and using the same.. .
Suncor Energy Inc.
Conjugate comprising folic acid and indole-3-carbinol for medical use
Conjugates of indole-3-carbinol are described for medical use and, particularly, for the prevention and treatment of neoplastic, inflammatory, cardiovascular diseases and other diseases, and of the metabolic syndrome.. .
Dom Terry International S.r.l.
Oxindole inhibitors of tyrosine kinase
The present invention relates to new oxindole inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.. .
Auspex Pharmaceuticals, Inc.
Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds and methods of using the same in the treatment 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
Benzopyridoindole derivative and organic electroluminescent element
According to the present invention, there are provided a benzopyridoindole derivative represented by the following general formula (1); and an organic el element including a pair of electrodes and at least one organic layer sandwiched therebetween, wherein the above derivative is used as a constituent material for the at least one organic layer. The benzopyridoindole derivative of the present invention is excellent in electron injection/transport performance, has hole blocking capability, is highly stable in a thin film state, and excels in various characteristics.
Hodogaya Chemical Co., Ltd.
Copolyesterimides derived from aromatic dicarboxylic acids and aliphatic glycols and films made therefrom
A film comprising a copolyester wherein said copolyester comprises repeating units derived from an aliphatic glycol, an aromatic dicarboxylic acid, and a comonomer (m) selected from the group consisting of n,n′-bis-(2-hydroxyalkyl)-bicyclo-[2,2,2]-oct-7-ene-2,3,5,6-tetracarboxylic diimide (bodi) and 2-hydroxyalkyl-2-[p-(2-hydroxyethoxycarbonyl)phenyl]-1,3-dioxo-2h-isoindole-5-carboxylate (doic), wherein the number of carbon atoms is the 2-hydroxyalkyl group is 2, 3 or 4, and wherein comonomer (m) constitutes a proportion of the glycol fraction of the copolyester.. .
Dupont Teijin Films U.s. Limited Partnership
Azaindoles as respiratory syncytial virus antiviral agents
Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.. .
Hydrazinyl-indole compounds and methods for producing a conjugate
The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same..
Redwood Bioscience, Inc.
Formulations of azaindole compounds
A pharmaceutical composition comprises: a) 5 wt % to 95 wt % of a hcl salt of compound (1).xh2o by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt % to 95 wt % of a filler by the weight of the pharmaceutical composition. Another pharmaceutical composition comprises: a) 1 mg/ml to 20 mg/ml of compound (1) in water; and b) 0.01 m to 0.1 m of a pharmaceutically acceptable ph modifier.
Vertex Pharmaceuticals Incorporated
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
4-azaindole derivatives which are modulators of muscarinic acetylcholine receptor (machr) m1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as alzheimer-type dementia (ad) or dementia with lewy bodies (dlb), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.. .
Eisai R&d Management Co., Ltd.
Indoles as respiratory syncytial virus antiviral agents
The prodrugs, n-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.. .
Breast cancer cell growth-inhibiting enzyme inhibitors, the production thereof, and use thereof
Novel enzyme inhibitors for treatment of breast cancer combine the inhibition of enzymes that combat aggressive breast cell growth both synergistically and additively. Pyrido-annulated indoles developed act in a selectively inhibiting manner on the enzymes her2 and/or brk in the nanomolar to picomolar concentration range in screening more than 200 kinases of the human kinome.
Thieno[2,3-e]indole derivatives as new antitumor agents
The present invention relates to a novel class of alkylating agents comprising a thieno[2,3-e]indole moiety tethered to a dna-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them.
Nerviano Medical Sciences S.r.l.
Novel aza-oxo-indoles for the treatment and prophylaxis of respiratory syncytial virus infection
Wherein r1, r2, r3, r4, w and x are as described herein, compositions including the compounds and methods of using the compounds.. .
Pharmaceutically Acceptable Salt
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