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201 results about "Substituted amide" patented technology

A secondary or tertiary amide; peptide linkages are substituted amides. Want to thank TFD for its existence? Tell a friend about us , add a link to this page, or visit the webmaster's page for free fun content .

Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases

InactiveUS20040229839A1Sufficient inhibitionBiocideSugar derivativesPurinePolymerase L
Provided are compounds represented by: X is O, S or NR6, R1 is H or (CH2)mR5, R2, R2', R3 and R3' are independently NO2, N3 or (CH2)mR5, OH R4 is H, OR6, SR6, NR6R6a, CN, C(O)OR6, C(O)NR6R6a, R6, OR7 or (CH2)nR7, R5 is H, halo, OR6, SR6, NR6R6a, CN, C(O)OR6, C(O)NR6R6a, R6, OR7 or (CH2)mR7, R6 and R6a are individually H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl or substituted aryl, R7 is: R8 is H, F, SR9 or OR9, R9 is H, alkyl, alkenyl, alkynyl, aryl or hydroxyprotecting group, Y is H, CH3 or (CH2)mR5, Z is O or S W is CH2, CF2, CHF or O, m is 0-4, B is adenine, guanine, cytosine, uracil, thymine, modified purines and pyrimidines substituted pyridines, five membered heterocycles substituted by at least one of amines, substituted amines, amides, substituted amides, esters, halogens, alkyls, ethers; and pharmaceutically acceptable salts thereof and prodrugs thereof. These ring systems may be substituted.
Owner:BIOCRYST PHARM INC

Preparation of acrylic acid derivatives from alpha-or beta-hydroxy carboxylic acids

The invention is directed to a process for the preparation of α,β-unsaturated acids, esters and amides from α- or β-hydroxycarboxylic acids or esters or precursors in high yields and high selectivity. The α,β-unsaturated acids or esters are optionally prepared in the presence of specific dehydration and / or esterification catalysts. The α,β-unsaturated amides or substituted amides are prepared optionally in the presence of a dehydration and / or amidation catalyst. The source of α- or β-hydroxycarboxylic acids or precusor is preferably from a renewable resource. The precursor is defined herein.
Owner:CIBA SPECIALTY CHEM WATER TRATMENTS

Method for attachment of biomolecules to medical device surfaces

A method for making a medical device having at least one biomolecule immobilized on a substrate surface is provided. One method of the present invention includes immobilizing a biomolecule comprising an unsubstituted amide moiety on a biomaterial surface. Another method of the present invention includes immobilizing a biomolecule on a biomaterial surface comprising an unsubstituted amide moiety. Still another method of the present invention may be employed to crosslink biomolecules comprising unsubstituted amide moieties immobilized on medical device surfaces. Additionally, one method of the present invention may be employed to crosslink biomolecules comprising unsubstituted amide moieties in solution, thereby forming a crosslinked biomaterial or a crosslinked medical device coating.
Owner:MEDTRONIC INC

Rho kinase inhibitors

ActiveUS20100041645A1Inhibiting kinase activityBiocideSenses disorderUrea derivativesGlaucoma
Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
Owner:BOEHRINGER INGELHEIM INT GMBH

Amide Derivatives and Pharmaceutical Use Thereof

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and / or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA

N, N-disubstituted amides that inhibit the binding of integrins to their receptors

A method for the inhibition of the binding of .alpha..sub.4.beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4.beta..sub.1 is involved.
Owner:ENCYSIVE PHARMA INC

Substituted amide beta secretase inhibitors

Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Owner:MERCK SHARP & DOHME LLC

Liquid and Semi-Solid Pharmaceutical Formulations for Oral Administration of a Substituted Amide

N-[1S,2S]-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-trifluoromethyl]pyridine-2-yl}oxy}propanamide (Compound I) has surprisingly improved solubility and bioavailability in a lipophilic vehicle comprising a pharmaceutically acceptable digestible oil, a surfactant, or a cosolvent, or a mixture of any two or more thereof. In one embodiment of the present invention are self-emulsifying or self-microemulsifying composition comprising 1) Compound I; 2) a surfactant having an HLB of 1 to 8; and 3) a surfactant having an HLB of over 8 to 20; and optionally, 4) a digestible oil and / or cosolvent and / or antioxidant or preservative.
Owner:MERCK SHARP & DOHME CORP

Lubricant compositions

Lubricant compositions comprise a lubricant base oil, and (A) a mono substituted amide type bissuccinimide in an amount from 0.5 to 20 percent by mass, (B) zinc dithiophosphate in an amount from 0.05 to 0.3 percent by mass of phosphorus, and (C) a metal-based detergent in an amount form 0.5 to 4.0 percent by mass of sulfated ash, based on the total mass of the composition. Lubricant compositions preferably further comprises (D) a dispersant type viscosity index improver in an amount from 0.1 to 20 percent by mass, based on the total mass of the composition.
Owner:NIPPON MITSUBISHI OIL CORP

Lubricant compositions

Lubricant compositions comprise a lubricant base oil, and (A) a mono substituted amide type bissuccinimide in an amount from 0.5 to 20 percent by mass, (B) zinc dithiophosphate in an amount from 0.05 to 0.3 percent by mass of phosphorus, and (C) a metal-based detergent in an amount form 0.5 to 4.0 percent by mass of sulfated ash, based on the total mass of the composition. Lubricant compositions preferably further comprises (D) a dispersant type viscosity index improver in an amount from 0.1 to 20 percent by mass, based on the total mass of the composition.
Owner:NIPPON MITSUBISHI OIL CORP

Pharmaceutical use of substituted amides

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA

Substituted amides

Novel compounds of the structural formula (I) are antagonists and / or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Owner:MERCK SHARP & DOHME CORP

Aromatic and heteroaromatic substituted amides

The invention is the compounds2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1λ6-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1λ6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide.Compounds of the invention are useful in pharmaceutical compositions for the treatment of migraine, rheumatoid arthritis, asthma, bronchial hyperreactivity, inflammatory bowel disease or for the treatment of disorders including Parkinson's disease, anxiety, depression, pain, headache, Alzheimer's disease, multiple sclerosis, edema, allergic rhinitis, Crohn's disease, ocular injury, ocular inflammatory diseases, psychosis, motion sickness, induced vomiting, emesis, urinary incontinence, psychoimmunologic or psychosomatic disorders, cancer, withdrawal symptoms of addictive drugs from opiates or nicotine, traumatic brain injury or benign prostatic hyperplasia.
Owner:F HOFFMANN LA ROCHE & CO AG

Pharmaceutical use of substituted amides

The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and / or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA

Pharmaceutical use of substituted amides

The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and / or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA

Solid-phase synthesis method of exenatide

The invention provides a solid-phase synthesis method of exenatide, which comprises the following steps: 1) preparing Fmoc-Ser(tBu)-amino resin from initial raw materials Fmoc-Ser(tBu)-OH and amino resin with the substitution degree of 0.3-1.2mmol / g; 2) after removing Fmoc protecting group from the Fmoc-Ser(tBu)-amino resin, sequentially connecting Fmoc amino resins and at least one amino-protected Fmoc amino resin or dipeptide with temporarily substituted amide N in a peptide sequence, and removing Fmoc to obtain the exenatide amino resin of which the side chain is fully protected; and 3) removing the side chain protecting group from the resin, and precipitating with ice aether, thereby obtaining the exenatide. The synthesis method has the advantages of high efficiency, simple reaction operation and easy after-treatment, and is suitable for industrial production.
Owner:NANJING UNIV OF TECH +1

Method for attachment of biomolecules to medical device surfaces

A method for making a medical device having at least one biomolecule immobilized on a substrate surface is provided. One method of the present invention includes immobilizing a biomolecule comprising an unsubstituted amide moiety on a biomaterial surface. Another method of the present invention includes immobilizing a biomolecule on a biomaterial surface comprising an unsubstituted amide moiety. Still another method of the present invention may be employed to crosslink biomolecules comprising unsubstituted amide moieties immobilized on medical device surfaces. Additionally, one method of the present invention may be employed to crosslink biomolecules comprising unsubstituted amide moieties in solution, thereby forming a crosslinked biomaterial or a crosslinked medical device coating.
Owner:MEDTRONIC INC

Substituted Amide Compounds

Substituted amide compounds corresponding to formula I:processes for preparing them, pharmaceutical compositions containing these compounds, and the use of substituted amide derivatives for the preparation of medicaments for the treatment of pain and various other conditions.
Owner:GRUNENTHAL GMBH

Liquid and semi-solid pharmaceutical formulations for oral administration of a substituted amide

3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(Trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)-octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (Compound I) has surprisingly improved solubility, bioavailability and stability in an ampiphilic vehicle that can include propylene glycol, a propylene glycol sparing agent, an antioxidant, or a mixture thereof. In one embodiment of the present invention is a solution comprising the active or a pharmaceutically acceptable salt or solvate thereof, and an amphiphilic agent, said amphiphilic agent being a fatty acid ester of glycerol, propylene glycol or sorbitol.
Owner:MERCK SHARP & DOHME CORP

Fiberglass composites with improved flame resistance from phosphorous-containing materials and methods of making the same

Fiberglass products with increased flame resistance are described. The products may include fiberglass-containing thermal insulation that include a plurality of glass fibers coated with a phosphorous-containing flame retardant. The flame retardant may include an organophosphorous compound having a substituted or unsubstituted organophosphorous group bonded to a substituted or unsubstituted amide group by a substituted or unsubstituted alkyl group. The fiberglass products may further include fiberglass composites that are about 50 wt. % to about 98 wt. % glass fibers, about 2 wt. % to about 50 wt. % of a binder; and a phosphorous-containing flame retardant. Also described are methods of making fiberglass products with increased flame resistance. These methods may include the steps of contacting glass fibers and / or fiberglass products with a flame retardant mixture that includes a phosphorous-containing compound.
Owner:JOHNS MANVILLE CORP

Polarizing plate, manufacturing method therefor, optical film and image display

The invention provides a polarizing plate using active energy ray-cured adhesive to adhere polarizing sheet and transparent protective film and having good adhesion. The polarizing plate is a polarizing plate provided with a transparent protective film placed on at least one side of the polarizer; and an adhesive layer and an adhesion facilitating layer interposed in this order from the polarizer side between the polarizer and the transparent protective film, wherein the adhesive layer is formed with an active energy ray-curable adhesive that contains a hydroxyl group-containing N-substituted amide monomer as a curable component, and the adhesion facilitating layer is formed with a polymer resin composition that contains 100 parts by weight of a polymer resin and 3 to 30 parts by weight of an organosilane compound having at least one functional group selected from an acryloyl group, a methacryloyl group, a vinyl group, and a mercapto group.
Owner:NITTO DENKO CORP

Heterocyclic amides with anti-tuberculosis activity

Compounds having the general structure: wherein A is selected from the group consisting of oxygen, sulfur, and NR15, and R15 is selected from the group consisting of H, alkyl, aryl, substituted alkyl, and substituted aryl; B,D, and E are each independently selected from the group consisting of CH, nitrogen, sulfur and oxygen; R1 is selected from the group consisting of nitro, halo, alkyl ester, arylsulfanyl, arylsulfinyl, arylsulfonyl and sulfonic acid; t is an integer from 1 to 3; and X is a substituted amide, and methods of using the novel compounds for treating infections caused by microorganisms, including Mycobacterium tuberculosis.
Owner:UNIV OF TENNESSEE RES FOUND +1

N-Oxides of Kappa Receptor Peptides

Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide. A preferred compound, which has an affinity for the KOR at least 1,000 times its affinity for the mu opioid receptor and an IC50 for CYP3 A4 of greater than about 10 micromolar, is H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide
Owner:CARA THERAPEUTICS
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