2236 results about "Lactone formation" patented technology

Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.

Coatings are provided in which surfaces may be activated by covalently bonding a silane derivative to the metal surface, covalently bonding a lactone polymer to the silane derivative by in situ ring opening polymerization, and depositing at least one layer of a polyester on the bonded lactone. Biologically active agents may be deposited with the polyester layers. Such coated surfaces may be useful in medical devices, in particular stents.

To a resist composition, an alkali-soluble polymer having fluorinated ester-containing lactone units incorporated therein is included as an additive. The resist composition forms a resist film having a reduced contact angle after development. The resist film prevents water penetration during immersion lithography.

Coatings are provided in which surfaces may be activated by covalently bonding a silane derivative to the metal surface, covalently bonding a lactone polymer to the silane derivative by in situ ring opening polymerization, and depositing at least one layer of poly(lactide-co-caprolactone) copolymer on the bonded lactone. Biologically active agents may be disposed with the poly(lactide-co-caprolactone) copolymer layers. Such coated surfaces may be useful in medical devices, in particular stents.

Embodiments of the invention relate to a composition, a process of making the composition, and to the use of the composition. The compositions include a molecular complex formed between an alkaline pharmaceutical drug and at least one selected from a hydroxyacid, a polyhydroxy acid, a related acid, a lactone, or combinations thereof. The compositions provide improved bioavailability and improved delivery of the drug into the cutaneous tissues.

PCT No. PCT / JP97 / 02858 Sec. 371 Date Oct. 30, 1997 Sec. 102(e) Date Oct. 30, 1997 PCT Filed Aug. 19, 1997 PCT Pub. No. WO98 / 07705 PCT Pub. Date Feb. 26, 1998A compound of the formula: wherein Q is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1; Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group; Z1 is a C1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain; Z2 is an optionally substituted C1-3 alkylene group; Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; one of R1 and R2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; or R1 and R2 taken together with adjacent -c=c- form a ring; and ring A is a benzene ring which may be substituted in addition to R1 and R2; or a salt thereof.

The present invention provides (i) processes for preparing a 2′-deoxy-2′-fluoro-2′-methyl-D-ribonolactone derivatives, (ii) conversion of intermediate lactones to nucleosides with potent anti-HCV activity, and their analogues, and (iii) methods to prepare the anti-HCV nucleosides containing the 2′-deoxy-2′-fluoro-2′-C-methyl-β-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.

The invention discloses an eremophilane lactone compound with chemical name as 3beta-chiretta acyloxy group-eremophile-7(11)-alkylene-12, 8beta-lactone-14-acid, which can inhibit the biological activity of HL-60, CNE, KB, Hela and P338D1.

A method for preparing a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids, or a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other without the spacer, characterized in that an organic amine salt of the polysaccharide derivative having carboxyl groups is reacted with the drug compound or the spacer bound to the drug compound in a non-aqueous system. The reaction between the polysaccharide derivative having carboxyl groups and the drug compound bound with the spacer or the like can be carried out in high yields, and when a drug compound having a lactone ring is subjected to the reaction, side reactions can be reduced.

The present invention provides a chemically amplified resist composition comprising: a resin (A) which contains no fluorine atom and a structural unit (a1) having an acid-labile group, a resin (B) which contains a structural unit (b2) having a fluorine-containing group and at least one structural unit selected from a structural unit (b1) having an acid-labile group, a structural unit (b3) having a hydroxyl group and a structural unit (b4) having a lactone structure, and an acid generator.

The present invention provides a water-soluble film which comprises a modified polyvinyl alcohol containing an N-vinylamide monomer unit in an amount of 1 to 10 mole percent, and a carboxyl group and a lactone group in a total amount of 0.020 to 4.0 mole percent in the molecule, and having a degree of polymerization of 300 to 3000, and a degree of hydrolysis of 75 to 99.5 mole percent. Further, the present invention provides a package obtained by packaging an acidic substance, a chlorine-containing compound, or the like using the water-soluble film.

A positive photosensitive composition comprising: (A) a resin having at least one repeating unit having a specific lactone structure at a side chain and being capable of decomposing by the action of an acid to increase the solubility in an alkali developer; and (B) a compound capable of generating a specific acid upon irradiation with an actinic ray or a radiation, and a pattern-forming method using the positive photosensitive composition, are provided.

The present invention is directed toward cyanoacrylate-based tissue adhesive or sealant compositions comprising cyanoacrylate-capped heterochain polymers, such as those comprising one or more oxyalkylene, alkylene carbonate, and ester-units derived from cyclic lactones. Such compositions can be radiochemically sterilized and used in repairing internal organs or tissue blocking body conduits.

There is provided a positive type resist composition formed by dissolving (A) a resin component with a unit derived from a (meth)acrylate ester in the principal chain, for which the solubility in alkali increases under the action of acid, and (B) an acid generator component which generates acid on exposure, in an organic solvent component (C), wherein the resin component (A) is a copolymer comprising (a1) a unit derived from a (meth)acrylate ester comprising an acid dissociable, dissolution inhibiting group containing a polycyclic group, (a2) a unit derived from a (meth)acrylate ester comprising a lactone containing monocyclic group or polycyclic group, (a3) a unit derived from a (meth)acrylate ester comprising a hydroxyl group containing polycyclic group, and (a4) a unit derived from a (meth)acrylate ester comprising a polycyclic group which is different from the unit (a1), the unit (a2) and the unit (a3). This composition provides a chemically amplified positive type resist composition which displays excellent resolution, enables the depth of focus range of an isolated resist pattern to be improved, and enables the proximity effect to be suppressed.

The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-o-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.

The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.

A water soluble package formed from a copolymeric polyvinyl alcohol film, wherein the comonomer comprises a carboxylate function, the package containing a substantially non-aqueous liquid composition which comprises: at least one ionic ingredient with an exchangeable hydrogen ion; and a molar excess (with respect to the amount of exchangeable hydrogen ions in the at least one ionic ingredient) of a stabilizing compound effective for combining with the exchangeable hydrogen ions to hinder the formation of lactones within the film, but can be as low as 95 mole % if the stabilizing compound comprises an inorganic base and / or ammonium hydroxide.

Lactone-containing compounds having formula (1) are novel wherein R1 is H, F, methyl or trifluoromethyl, R2 and R3 are monovalent hydrocarbon groups, or R2 and R3 may together form an aliphatic hydrocarbon ring, R4 is H or CO2R5, R5 is a monovalent hydrocarbon group, W is CH2, O or S, and k1 is 0 or 1. They are useful as monomers to produce polymers which are transparent to radiation≦500 nm. Radiation-sensitive resist compositions comprising the polymers as base resin exhibit excellent properties including resolution, pattern edge roughness, pattern density dependency and exposure margin.

The invention relates to compositions and methods useful for treating a variety of cosmetic conditions and dermatological disorders, where the composition includes a phenyl glycine derivative represented by the following formula:wherein, R1 and R2 are independently H, I, F, Cl, Br, OH, SH, NH2, NHNH2, alkyl, aralkyl, alkoxy, acetoxy, acyloxy group having 1 to 9 carbon atoms, and being attached at the 2, 3 or 4 position of the phenyl group, whereby when R1 and / or R2 are OH, SH, NH2, they may be acetylated or acylated with 1 to 9 carbon atoms; R3 is H, formyl, acetyl, propanoyl, acyl, alkyl, aralkyl or an aryl group having 1 to 9 carbon atoms; R4 is OH, NH2, NHOH, NHNH2, or OR; where R is an alkyl, aralkyl or aryl group having 1 to 9 carbon atoms; the H attached to any carbon or nitrogen atom may be substituted by I, F, Cl, Br, OH, SH, NH2, NHNH2, an alkyl, aralkyl, alkoxy or acyl group having 1 to 9 carbon atoms. Phenyl-glycine and its derivatives may be present as isomeric D or L, non-isomeric or racemic DL, as a free acid, salt, lactone, amide or ester form.

1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is =CH- or =N-, Y is -NH-, -NR<4>-, -S-, -O-, -CH=N-, -N=CH-, -N=N-, -CH=CH-, etc., R<1 >is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R<2 >is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R<3 >is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R<3 >and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.

Embodiments of the invention relate to a composition, a process of making the composition, and to the use of the composition. The compositions include a molecular complex formed between an alkaline pharmaceutical drug and at least one selected from a hydroxyacid, a polyhydroxy acid, a related acid, a lactone, or combinations thereof. The compositions provide improved bioavailability and improved delivery of the drug into the cutaneous tissues.

A topical insect repellent with extended duration of protection was obtained from mixtures of molecules based on two or more volatile repellent organic molecular species occurring naturally on the human skin surface. The novel repellent comprises mixtures of lower, intermediate, and higher volatility organic molecules. Active ingredients for formulations are obtained from homologous series of carboxylic acids, alcohols, ketones, and lactones which span a similar range of volatility and which occur naturally on the skin surface. Volatile silicone fluid imparts mildness and water repellency to the repellent formulations. The new natural repellent exhibits the longevity and repellency that is comparable to N,N-diethyl-m-toluamide (DEET), a synthetic compound employed in almost all commercial formulations, but the inventive natural repellent is more acceptable than DEET, which has an unpleasant odor and imparts a greasy feel to the skin. The inventive insect repellent, formulated in a volatile silicone fluid, was shown to repel and incapacitate stable flies. This finding demonstrated that repellency was not limited to mosquitoes, but extends to other biting flies or insects, thus demonstrating the utility of the novel insect repellent for protecting pets and livestock as well as humans.

A natural formulation of compounds that would to modulate inflammation is disclosed. The formulation would also inhibit expression of COX-2, inhibit synthesis of prostaglandins selectively in target cells, and inhibit inflammatory response selectively in target cells. The compositions containing at least one fraction isolated or derived from hops. Other embodiments relate to combinations of components, including at least one fraction isolated or derived from hops, tryptanthrin and conjugates thereof, rosemary, an extract or compound derived from rosemary, a triterpene species, or a diterpene lactone or derivatives or conjugates thereof.

This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocylic lactone compound from the fermentation broth. The compounds produced by this process include a compound of the following formula:The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.