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|| List of recent Indole-related patents
|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.
Wherein r1 is h or optionally substituted alkyl; r2, r3, r4 are each independently selected from h, —o-alkyl, —s-alkyl, alkyl, halo, —cf3, and —cn; g is —cr12r13—nr5— or —nr5—cr12r13; r5 is h, optionally substituted alkyl, optionally substituted heterocycle, —c(═o)—r6, —c(═o)—o—r7, or —c(═o)—nr19r20; r6 and r7 are each optionally substituted alkyl or optionally substituted heterocycle; r8, r9, r10, r11, r12, r13, r19 and r20 are each independently selected from h or optionally substituted alkyl; r14 and r15 are each independently h or halogen; l is —ch2—o—, —ch2ch2—, —ch═ch— or a bond; and b is aryl or heteroaryl or cycloalkyl; with the proviso that, when l is a direct bond, b cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.. .
|Antihistamines combined with dietary supplements for improved health|
The present invention provides combinations comprising a sedating antihistamine and selected indole-based natural products such as l-tryptophan, 5-hydroxytryptophan and melatonin, along with pharmaceutically acceptable calcium and magnesium salts and selected b vitamins. These combinations are useful in providing a medicament for improving sleep in mammals, especially humans..
|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..
|5,6-disubstituted oxindole-derivatives and use thereof for treating vasopressin-dependent diseases|
The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.. .
This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles.
|7-azaindole derivatives suitable for treatment of cancers|
Compounds of the formula (i) in which r1, r2 and r3 have the meanings indicated in claim 1, are inhibitors of pdk1 and cell proliferation/cell vitality and can be employed treatment of tumours.. .
|Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them|
A, r3, r4, r5, r6 and r7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases..
|(aza)indole derivative and use thereof for medical purposes|
The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (i) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
|Tyrosine phosphatase inhibitors and uses thereof to modulate the activity of enzymesp involved in the pathology of mycobacterium tuberculosis|
A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological ph and have good bioavailability characteristics.
|Polymorphic form of 5-(4-[4-(5-cyano-1h-indol-3-yl) butyl] piperazin-1-yl) benzofuran-2-carboxamide and process for preparing thereof|
The present invention provides a solid state form-z of 5-(4-[4-(5-cyano-1h-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide. The present invention also provides a process for preparing form-z of 5-(4-[4-(5-cyano-1h-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide comprising the steps of i) reacting solid state form of 5-(1-piperazinyl)benzofuran-2-carboxamide or its salts with 3-(4-chlorobutyl)-1h-indole-5-carbonitrile an organic solvent in presence of a base to obtain crude vilazodone free base; ii) purifying the crude vilazodone free base of step (i) in an organic solvent; iii) treating the purified vilazodone free base of step (ii) with an organic solvent to obtain solid state form-z of vilazodone.
|Compounds useful as inhibitors of indoleamine 2,3-dioxygenase|
Wherein the variables are as defined herein.. .
|Substituted indole derivatives|
The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.. .
|Substituted benzofurans, benzothiophenes, benzoselenophenes and indoles and their use as tubulin polymerisation inhibitors|
The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.. .
|Nitrogenated aromatic heterocyclic derivative, and organic electroluminescent element using same|
A nitrogen-containing aromatic heterocyclic derivative in which a nitrogen atom of an indenocarbazole skeleton optionally having a hetero atom or an indenoindole skeleton optionally having a hetero atom is bonded to a dibenzofuran or a dibenzothiophene directly or indirectly. The derivative realizes an organic el device with a high emission efficiency and a long lifetime..
|Rubber composition and pneumatic tire|
A rubber composition contains diene-based rubber, silica, a sulfur-containing silane coupling agent, and an amine compound. The amine compound is indole, indigo, and derivatives thereof each of which is represented by a predetermined formula.
|Compounds and methods of treating diabetes|
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 antagonists of the adrenergic receptor a2a.
|Compound and method for modulating opioid receptor activity|
The invention provides a compound of formula (i), wherein r1 is h, c(nh)nh2, an amino acid, or a peptide; x is oh, nh2, nhr2, nr2r3, an amino acid, or a peptide; r2 and r3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each r4 and r5 is independently h or ch3; z is 2-amino-2,3-dihydro-1h-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5h-benzoannulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1h-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that x is not nh2 when r1 is h, r4 is h, r5 is ch3, z is aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided..
|Spiro-oxindole mdm2 antagonists|
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and mdm2, and their use as therapeutics for the treatment of cancer and other diseases..
|Novel substituted indole derivatives as gamma secretase modulators|
The present invention is concerned with novel substituted indole derivatives of formula (i) wherein r1, r2, r3, a1, a2, a3, y and x have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators.
|Treatment of mastocytosis with masitinib|
The present invention relates to the treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, in particular in an appropriate dosage regimen.. .
|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..
|Pharmaceutical formulations of substituted azaindoleoxoacetic piperazine derivatives with protease inhibitors|
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.
|Anhydrous lenalidomide form-i|
Anhydrous polymorphic form-i of anti cancer drug, lenalidomide whose chemical name is 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-i of lenalidomide are also disclosed..
|Indoleamine derivatives for the treatment of central nervous system diseases|
The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.. .
|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.. .
|N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same|
This invention relates to n-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed..
|Macrocyclic indole derivatives useful as hepatitis c virus inhibitors|
The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in hcv therapy.. .
|Indolecarboxamides and benzimidazolecarboxamides as insecticides and acaricides|
In which r1 to r6, a, y, x, g, n and m are each as defined in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.. .
|Azepino[4,5-b]indoles and methods of use|
This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles.
|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.
|Processes for the preparation of isoindole compounds and isotopologues thereof|
Processes for the preparation of certain isoindole compounds, and isotopologues thereof, are provided. In some embodiments, the processes comprise catalytic assymetrical hydrogenation with hydrogen gas or deuterium gas in a solvent containing exchangeable proton or deuterium for proton-deuterium exchange..
|Amino-substituted-alkyloxy-benzo[e]pyrido[4,3-b]indole derivatives as new potent kinase inhibitors|
The present invention relates to a new class of benzo[e]pyrido-indole, the amino-substituted-alkyloxy-benzo[e]pyrido[4,3-b]indole derivatives, having a particular kinase inhibition profile and useful as a therapeutic agent, in particular an anti-tumoral agent.. .
|Azaindole derivatives as tyrosine kinase inhibitors|
The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular blk, bmx, egfr, her2, her4, itk, jak3, tec, btk, and txk and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts..
|Process for preparing 6-iodo-2-oxindole|
Disclosed is a method for the synthesis of 6-iodo-2-oxindole useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed is a novel intermediate used in the synthesis of this compound..
|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 indoleanine 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 immunosupression associated with an infectious disease.. .
|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.
|Novel indole derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating metabolic diseases containing same as active ingredient|
The present invention relates to an indole derivative, the indole derivative according to the present invention effectively inhibits the activity of diacylglycerol acyltransferase (dgat) which induces metabolic diseases, such as obesity, diabetes, hyperlipidemia, or fatty liver and the like in lipid metabolism, thereby effectively regulating lipid metabolism and energy metabolism, and thus can be useful in pharmaceutical compositions for preventing or treating metabolic disease.. .
|Substituted azaindole compounds, salts, pharmaceutical compositions thereof and methods of use|
The present invention provides substituted azaindole prodrugs, methods of making said prodrugs, pharmaceutical compositions of said prodrugs and methods of using said prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer.. .
|Substituted indole compounds having nos inhibitory activity|
The present invention features inhibitors of nitric oxide synthase (nos), particularly those that selectively inhibit neuronal nitric oxide synthase (nnos) in preference to other nos isoforms. The nos inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, cabg, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (cpsp), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia..
|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.. .
|Process for the preparation of morpholino sulfonyl indole derivatives|
The present invention relates to a process for the preparation of the compounds of formula (i) which are morpholino sulphonyl indole derivatives. The compounds of formula (i) are capable of inhibiting, modulating or regulating insulin-like-growth factor i receptors or insulin receptors.
|Crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation|
The present invention relates to a crystalline form of a pharmaceutically acceptable salt of a morpholino sulphonyl indole derivative, that is capable of inhibiting, modulating and/or regulating insulin-like-growth factor i receptor and insulin receptor. The present invention also relates to a process for the preparation of the crystalline form of said compound.
|Insulin-like growth factor-1 receptor inhibitors|
The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating insulin-like-growth factor i receptor and insulin receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety.
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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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