892 results about "Indole Compound" patented technology

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.

This invention provides a compound of the following formula:and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4 alkylidene; Q is C1-6 alkyl, C3-7 cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1 is hydrogen, C1-6 alkyl or the like; R2 is hydrogen, C1-4 alkyl, C(O)R5 wherein R5 is C1-22 alkyl or C2-22 alkenyl, halosubstituted C1-8 alkyl, halosubstituted C2-8alkenyl, -Y-C3-7 cycloalkyl, -Y-C3-7 cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4 alkyl, hydroxy, C1-4 alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula -Y-Q is not methyl or ethyl when X is hydrogen; L is oxygen; R1 is hydrogen; and R2 is acetyl.This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds

The invention discloses 20 kinds of 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl, discloses a preparation method of the 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl, discloses an effect of the 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl in inhibiting invasion and metastasis of a tumor cell, discloses an activity of the 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl in inhibiting weight gain of a tumor body of a S180-bearing mouse, and discloses an anti-tumor pulmonary metastasis activity and an anti-inflammatory activity. The compound has an excellent application prospect in preparing an antitumor drug, an anti-tumor metastasis drug and an anti-inflammatory drug.

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.

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.

Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.

Benzoimidazole and indole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

In certain embodiments, the invention is directed to a method for treating a protein folding disorder comprising administering to a subject a compound of the formulas disclosed. In preferred embodiments, the compounds are bis-indole compounds.

This invention provides a compound of the following formula:or the pharmaceutically acceptable salts thereof wherein A is C 1-6 alkylene or -NR1-; Z is C(=L)R2, or SO2R3; U is CH or N; W and Y are independently selected from -CH2-, O, S and -N-R1; m is 1, 2 or 3; q and r are independently 0, 1 or 2; X is independently selected from halogen, C1-4 alkyl, halo-substituted C1-4 alkyl, hydroxy, C1-4 alkoxy, halo-substituted C1-4 alkoxy or the like; n is 1 or 2; L is oxygen or sulfur; R1 is hydrogen or C1-4 alkyl; R2 is hydroxy, C1-6alkyl, halo-substituted C1-6 alkyl, C1-6 alkoxy, halo-substituted C1-6 alkoxy, C3-7 cycloalkoxy, C1-4 alkyl(C3-7 cycloalkoxy), -NR4R5 or the like; R3 is C1-6 alkyl or halo-substituted C1-6 alkyl; and R4 and R5 are independently selected from hydrogen, C1-6 alkyl and halo-substituted C1-6alkyl.This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

Disclosed are a 1,6-substituted indole compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of cancers caused by abnormal cell growth comprising the compound as an effective ingredient.Since the novel indole compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.

Methods for preparing oxindole and thio-oxindole compounds are provided, which compounds are useful as precursors to useful pharmaceutical compounds. Specifically provided are methods for preparing 5-pyrrole-3,3-oxindole compounds and 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile. Also provided are methods for preparing iminobenzo[b]thiophene and benzo[b]thiophenone compounds.

This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

The invention provides a winged insect attractant which is composed of components with the following parts by weight: 0.000001 to 90 percent of glucide compound; 0.000001 to 50 percent of amino acids; 0.000001 to 50 percent of proteinic compound; 0.000001 to 30 percent of vitamin compound; 0.000001 to 60 percent of alcohols; 0.000001 to 50 percent of acid compound; 0.000001 to 40 percent of ester compound; 0.000001 to 40 percent of ethers; 0.000001 to 50 percent of ammonia compound; 0.000001 to 20 percent of indole compound; 0.001 to 10 percent of antiseptic; 0. 1 to 90 percent of plant juice; and 1 to 90 percent of water. The winged insect attractant provided by the invention is applicable to various pernicious winged insects such as the mosquito, the fly, the scalewing, the white fly, etc., and has strong attraction, simple and convenient use, and no poison to people and animals.

Administration of a cruciferous indole compound can reduce undesirable toxic side effects inherent in the anti-tumor therapy with ET-743 before during or after administration of the ET-743.

The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I) wherein: X, R and R1 are defined herein with a substituted acetylene of formula (II) wherein R2 and R3 in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);

Disclosed is an electroluminescent device comprising a light-emitting layer containing a light emitting phosphorescent material that contains an organometallic complex comprising iridium and an indole compound with an unsubstituted phenyl ring or comprising Ir, Rh, Os, Ru, Pt, and Pd and an isoindole compound. The invention further comprises compositions of certain such complexes as well as a display or area lighting devices and a process for emitting light. The organometallic materials function as useful phosphorescent light emitting materials in electroluminescent devices.

Personal care compositions comprising a dipeptide; one or more of the following: a pentapeptide, a second dipeptide, a vitamin B3 compound, a hexamindine compound, and / or a sugar amine; and a dermatologically acceptable carrier. Methods of using such compositions to treat the condition of keratinous tissue. In certain embodiments, the C terminal amino acid of said dipeptide is threonine.

The present invention relates to a flame-resistant and heat-resistant copper clad laminate preparation method, which comprises: adopting nanometer silica foam, dodecyl benzenesulfonic acid, bismuth nitrate pentahydrate, methyl trichlorosilane and polyoxyethylene sorbitan monooleate as a raw materials to obtain a filler; adopting DOPO, a bisphenol A cyanate ester monomer, a phenol compound, a m-nitrobenzene sulfonic acid pyridine salt, 2,3-epoxy cyclopentyl cyclopentyl ether and dimethyl phosphonate as raw materials to obtain a resin prepolymer; adding the filler to o-phthalic acid diglycidyl este to obtain an active filler; mixing the resin prepolymer and an indole compound, and then adding the active filler and isomeric undecanol polyoxyethylene ether phosphate potassium salt to obtain a composite system; and carrying out hot pressing molding on the composite system, a reinforced material and metal foil to obtain the flame-resistant and heat-resistant copper clad laminate, wherein the flame-resistant and heat-resistant copper clad laminate has characteristics of excellent flame retardant property and excellent heat resistance, and meets the development applications of the flame-resistant and heat-resistant copper clad laminate.

The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I):in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.

Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like.A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:wherein each symbol is as described in the specification.

A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.

This invention provides a compound of the following formula:or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, -NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; and n is 0, 1, 2, 3 and 4.This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

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.

It is an object of the present invention to provide an interlayer film for a laminated glass which can reduce transmittance of ultraviolet rays having wavelength of 380 to 400 nm and has excellent durability to light exposure while maintaining high visible light transmittance.The interlayer film for a laminated glass of the present invention is an interlayer film for a laminated glass,which comprises a thermoplastic resin and an indole compound having a structure represented by the following general Chemical Formula (1):wherein R1 represents an alkyl group having 1 to 3 of carbon atoms, and R2 represents hydrogen, an alkyl group having 1 to 10 of carbon atoms, or an aralkyl group having 7 to 10 of carbon atoms.

The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

The present invention relates to a compound represented by the formula (I),wherein all symbols are as defined in the description,a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and / or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.