901 results about "Tripeptide" patented technology

The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.

The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.

Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t-butyl or —CH2—C(CH3)3 or —CH2-cyclopentyl; R3 is t-butyl or cyclohexyl and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.

Pharmaceutical, personal care and cosmetic compositions containing a tripeptide and a tetrapeptide are useful for treating visible signs of aging including wrinkles, stretch marks and dark circles.

The five component composition consisting essentially of: (1) Water soluble antioxidant vitamin C or ascorbic acid, or any of its forms or derivatives, or mixtures thereof. (2) Oil soluble antioxidant vitamin E or Alpha-tocophorol, or any of its forms or derivatives, or mixtures thereof. (3) The element selenium, or a chemical (or composition) containing it, or mixtures thereof. The most preferred chemical containing selenium is dimethyl selenide and mixtures thereof. The words "dimethyl selenide" here and hereinafter mean dimethyl selenide and / or it's oxidation products, including dimethyl selenoxide. (4) A sulfur amino acid, in any form, or a sulfur peptide, or a sulfur protein, or any of their derivatives, or mixtures thereof. The mixture of methionine and cysteine, which contains as impurities some seleno-methionine and some selenocysteine, is preferred,-the tripeptide glutathione containing cysteine is also preferred. (5) Another antioxidant, other than vitamin C and other than vitamin E, which is synthetic or natural and water soluble or oil soluble, or a mixture of such antioxidants, or a combination of such forms thereof. The mixtures of butylated hydroxyanisole and ethoxyquin is preferred.

The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The present invention provides a highly dispersible formulation comprising an active agent and a dipeptide or tripeptide comprising at least two leucyl residues. The composition of the invention possesses superior aerosol properties and is thus preferred for aerosolized administration to the lung. Also provided are a method for (i) increasing the dispersibility of an active-agent containing formulation for administration to the lung, and (ii) delivery of the composition to the lungs of a subject.

The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

A dipeptide or tripeptide carrier system for active agent delivery to cells has an N-terminus natural amino acid and an active agent covalently bonded to a side chain of one of the remaining amino acid bases. The system is amenable to formulation as an oral administrant. The active agent being a therapeutic, a fluorescent dye, or contrast agent where the active agent has a molecular weight of less than 500 atomic mass units. An optional linker is provided intermediate between the active agent and the linking side chain.

Cleaning compositions comprising (A) N-long-chain acyl neutral amino acid or a salt thereof, (B) N-long-chain acyl neutral amino acid dipeptide or a salt thereof, and (C) N-long-chain acyl neutral amino acid tripeptide or a salt thereof provide abundant foam, are excellent in foam retaining properties, and furnish a cleaned and dried body or hair with both a smooth feeling and a moist feeling. Compositions which further comprise (D) a higher fatty acid having 8 to 22 carbon atoms or a salt thereof exhibit enhanced creamy properties in foam quality. N-long-chain acyl neutral amino acids or salts thereof may be conveniently prepared by mixing a neutral amino acid, a long-chain fatty acid, and at least one of an alkaline substance selected from sodium hydroxide and potassium hydroxide, and maintaining the mixture with heating, while removing the water produced during the reaction, with no catalyst being employed.

Life-threatening hepatotoxicity in the setting of acetaminophen overdose is due to depletion of glutathione (GSH), a vital cysteine-containing tripeptide that protects cells and organs against oxidant injury. Rapid administration of N-acetylcysteine (NAC), which provides the cysteine necessary to replenish the depleted GSH, is the standard of care for preventing injury in acetaminophen overdose. Beneficial effects of NAC treatment have also been demonstrated in respiratory, cardiovascular, endocrine and infectious and other diseases. In fact, over fifty randomized placebo-controlled trials conducted in diverse clinical settings document positive responses to NAC treatment. The present invention relates to cysteine / glutathione (GSH) deficiency as a previously unrecognized clinical entity that can complicate the course of commonly encountered diseases and methods of treatment of this generalized deficiency involving administering N-acetylcysteine (NAC) or a pharmaceutically acceptable salt or derivative to a subject in need thereof and monitoring the subjects appropriate glutathione blood levels as needed.

The present invention relates to the use of one or more tripeptides selected from the group consisting of NLys-Pro-ValC, NLys-Pro-ThrC and NpGLu-His-ProC for the reduction of oxidative stress. The above tripeptides are particularly useful for the treatment of a disease or damage caused by oxidative stress; such as vitiligo, scleroderma, necrosis, or erythema; furthermore, a disease or damage of the hair, like premature hair loss or premature formation of grey hair. Furthermore the invention relates the cosmetic use of the above tripeptides, in particular against skin aging. Further the invention relates cosmetic compositions containing at least one of said tripeptides.

The invention discloses an antiageing and repairing polypeptide facial mask essence. The polypeptide facial mask essence contains the following seven active components of peptides: dipeptide diaminobutyryl benzylamide diacetate, palmitoyl tripeptide-5, palmitoyl tetrapeptide-7, pentapeptide-3, hexapeptide-11, heptapeptide-6, acetyl octapeptide-3. The polypeptide facial mask essence disclosed by the invention has the functions of effectively lifting the facial contour, resisting facial wrinkles, restoring the firmness and elasticity of the facial skin, making the facial skin be smooth and delicate and changing the state of the facial skin on the whole. The invention further discloses a preparation method of the antiageing and repairing polypeptide facial mask essence.

Disclosed are compositions and methods for their use that can be used in cosmetic applications. The composition can include an effective amount of a Centella asiatica stem cells to reduce the activity of hyaluronidase in skin, an effective amount of tetradecyl aminobutyroylvalylamino butyric urea trifluoroacetate or Alpinia galanga leaf extract to promote the production of hyaluronic acid in skin, an effective amount of tripeptide-1 to promote the production of fibronectin and laminin in skin, and a dermatologically acceptable vehicle.

The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6 or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24) alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or —NH—; or XR5 with X=O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I).

The present invention concerns dicarboxylic acid linked amino acid and peptide prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, decreasing the adverse GI side effects of the opioid analgesic and increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are also provided. In one embodiment, prodrugs having the amino acid side chains of valine, leucine, isoleucine and glycine; and mono-, di- and tripeptides thereof are provided.

The invention relates to the technical field of cosmetics, and discloses a nona-oligopeptide composition for skin repairing and application thereof. The nona-oligopeptide composition is prepared from, by weight, 1-30 parts of palmitoyl-tripeptide-1, 1-30 parts of tripeptide-1 copper, 1-50 parts of palmitoyl-tripeptide, 1-30 parts of carnosine, 1-30 parts of acetyl tetrapeptide-5, 1-30 parts of palmitoyl-tetrapeptide-7, 0.1-30 parts of acetyl hexapeptide-8, 0.1-30 parts of nonapeptide-1, and 1-30 parts of nisin. The nona-oligopeptide composition has the effect of a cell factor sample, affects the growth of skin flora, is applied to dermatology and skin beautifying, and has the effects of repairing skin lesion, adjusting metabolism and inhibiting skin condition conditioned pathogen growth.

The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The invention discloses a polypeptide composition for repairing, whitening and removing wrinkles. The polypeptide composition for repairing, whitening and removing the wrinkles is prepared from the following components is percentage by weight: a repairing polypeptide composition, a collagen supplementing polypeptide composition, a wrinkle removing polypeptide composition, a skin-brightening polypeptide composition, a small molecular active substance, a skin-care activating agent, a pH (Potential of Hydrogen) regulator, a plurality of auxiliary agents and the balance of water, wherein the repairing polypeptide composition comprises palmitoyl tetrapeptide-7 and tripeptide-1-copper; the collagen supplementing polypeptide composition comprises palmitoyl tripeptide-1, palmitoyl tripeptide-5 andpalmitoyl pentapeptide-4; the wrinkle removing polypeptide composition comprises acetyl hexapeptide-8, dipeptide diaminobutyroyl benzylamide diacetate and melittin; the skin-brightening polypeptide composition comprises nonapeptide-1, carnosine and tetrapeptide-30. According to the polypeptide composition disclosed by the invention, a novel formula is formed through adjusting ratios of differentpolypeptide components, so that polypeptide effects with different focuses and different applicable ranges; the monarch, minister, assistant and guide thought in traditional Chinese medical science isapplied to the polypeptide composition, so that the formula is diversified and the maximum applicability and applicable range are realized.

Fluorinated oligopeptides, especially those having 4,4-difluoro-2-amino butyric acid at the C terminus, may be effective inhibitors of hepatitis C virus NS3 protease. Examples of hexapeptides of the invention, optimized for binding in the S1 specificity pocket of the enzyme, may display IC50s at the sub-micromolar level. Embodiments of tripeptides of the invention, having a keto-acid group at the C-terminus are, likewise, potent inhibitors of NS3 protease.

The present invention provides a highly dispersible formulation comprising an active agent and a dipeptide or tripeptide comprising at least two leucyl residues. The composition of the invention possesses superior aerosol properties and is thus preferred for aerosolized administration to the lung. Also provided are a method for (i) increasing the dispersibility of an active-agent containing formulation for administration to the lung, and (ii) delivery of the composition to the lungs of a subject.

The present invention is directed to a prevention and treatment for dermatological disorders. One aspect of this invention involves a dermatological treatment comprising one or more polypeptides with an amino acid sequence including KPV (SEQ. ID. NO. 1), MEHFRWGKPV (SEQ. ID. NO. 2), HFRWGKPV (SEQ. ID. NO. 3), or SYSMEHFRWGKPV (SEQ. ID. NO. 4) for the treatment and prevention of dermatological disorders. The polypeptides are at a level to effectively treat the cutaneous inflammation and are carried by a carrier. The one or more polypeptides can also be a dimer formed from any of the amino acid sequence above.

Prodrugs of tapentadol with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with the tapentadol prodrugs are provided herein. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with tapentadol administration, as well as increasing the oral bioavailability of tapentadol are provided herein.

The invention provides compositions for stimulating the formation of one or more extracellular matrix components that contain a lipoaminoacid derivative of the tripeptide carnosine such as N-Octanoyl Carnosine. Also provided are compositions containing N-Octanoyl Carnosine in combination with selected tripeptide and / or tetrapeptides as well as pharmaceutical and / or cosmetic compositions containing such compositions. The invention further provides methods of using the compositions and compositions of the invention to treat, alleviate, and / or ameliorate a symptom, condition, disorder, or disease of the skin or mucosa, wherein the symptom, condition, disorder, or disease is associated with changes in extracellular matrix components.

The invention relates to a method for preparing Semaglutide through solid and liquid combination, and solves the technical problems that in the process for synthesizing long-sequence polypeptide by the existing technology, the synthesis period is long; the purification difficulty is high; the yield is low. The method for preparing Semaglutide through solid and liquid combination provided by the invention is characterized in that firstly, Lys and resin are condensed in an Alloc-Lys(Fmoc)-OH form by adopting a solid phase synthesis method; Fmoc protecting groups on epsilon-NH2 are removed; sidechain connection is performed; cracking is performed to obtain Alloc-Lys(PEG-PEG-gamma-Glu(OtBu)-Monobutyl octadecanate)-OH; meanwhile, 10 dipeptide or tripeptide or tetrapeptide fragments are simultaneously synthesized by a liquid phase synthesis method; then, the condensation reaction of the synthesized peptide fragments and single amino acid is performed by using the resin as a carrier; the 15-step solid phase condensation reaction is reduced in the process; the generation of lacked peptide impurities is reduced; the product purity and the yield are improved; meanwhile, the generation of the impurities of [+Gly]-Semaglutide and [+Ala]-Semaglutide is effectively avoided; the purification difficulty is greatly reduced. The method is widely applied to the technical field of polypeptide medicine preparation.

The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The invention discloses a beverage capable of maintaining beauty and nourishing the skin and a preparing method of the beverage. The beverage capable of maintaining beauty and nourishing the skin is prepared from collagen tripeptide, chitosan oligosaccharide, gamma-aminobutyric acid, fish collagen peptide and skipjack elastin peptide. The beverage achieves great effects of adjusting and repairingthe skin of the human body in combination with multiple collagen nutrients, vitamin C and nutrient substances resistant to sugar and oxidation required for the human body.

The invention discloses a compound anti-wrinkle anti-aging essence containing a plurality of small molecular peptides and a preparation method of the essence. The essence comprises the following raw materials in percentage by weight: 0.1-0.2% of sodium hyaluronate; 0.2-0.3% of acrylic acid (ester) / C10-30 alkanol acrylate cross-linked polymer; 5-7% of glycerol; 4-6% of 1,3-butanediol; 0.3-0.5% ofdipeptide diaminobutyl benzyl amide diacetate; 0.2-0.3% of palmitoyl tetrapeptide-5; 0.3-0.5% of palmitoyl tripeptide-1; 0.3-0.5% of palmitoyl pentapeptide-4; 0.1-0.3% of carnosine; 0.1-0.3% of serine; 0.1-0.3% of arginine; 0.1-0.3% of nicotinamide; 0.2-0.3% of a preservative and the rest of deionized water. The skin of a human body is repaired in an all-round way, so that good and rapid wrinkle removal and aging resistance effects are achieved.

The invention comprises a substrate for detection of micro-organisms, wherein said substrate comprises a set of molecular markers linked, optionally with linker molecules or moeieties, to a di-, or tripeptide consisting of amino acids X1 and X2, or X1, X2 and X3, in which one of them, for example X1, is a D-amino acid and the others, for example X2 and X3, may be any D- or L-amino acid. Said substrate preferably is used for the detection of Bacillus anthracis. Alternatively, the invention is directed to a substrate for detection of micro-organisms, more specifically P. aeruginosa, wherein said substrate comprises a set of molecular markers linked, optionally with linker molecules or moeities to a tri- tetra or pentapeptide consisting of glycine amino acids. The invention further comprises methods for detection of micro-organisms, specifically Bacillus anthracis and Pseudomonas aeruginosa, with the substrates of the invention and use of the substrate(s) in such a method.