Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Compounds and compositions for delivering active agents

A hair dye composition containing a triazene dissociative direct dye represented by general formula (1): A-N=N-NH-B (1) wherein A and B are each a monocyclic or a bicyclic aromatic heterocyclic group that may have a substituent or a monocyclic or a bicyclic aryl group that may have a substituent and contain none of a carboxy group, a sulfo group and a quaternary ammonium group; and A and B each bind to a triazene-1,3-diyl group represented by -N=N-NH- via a carbon atom within A and B each. A and B may be the same or different.

Hair-dye composition

The present invention relates to an oral delivery system, and in particular to modified amino acids or peptides for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids or peptides can form non-covalent mixtures or microspheres with active biological agents. These mixtures or microspheres are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids and peptides are also disclosed.

Modified amino acids for drug delivery

The present invention relates to a delivery system, and in particular to carboxylic acids for use as a delivery system of sensitive agents such as bioactive peptides. The carboxylic acids and salts can form non-covalent mixtures with biologically-active agents. These mixtures are suitable for oral administration of biologically active agents to animals.

Acids and acid salts and their use in delivery systems

A method of separating semiconductor elements (2) formed in a wafer of semiconductor material (1). A score (8) is formed in a surface (3) of the wafer (1) through local evaporation of semiconductor material by means of heat originating from radiation (10). This radiation (10) is generated by a laser (11) and focused on the wafer (1) by means of an optical system (12). The wafer (1) is moved relative to the radiation (10) focused thereon along a path (9) which follows the score (8) to be formed. The radiation (10) of the laser (11) is focused on the wafer (1) in the form of at least two beams (14 and 15), the wafer (1) being moved relative to the beams (14 and 15) such that the beams (14 and 15) travel the same path (9) one after the other. A deeper score (8) can be formed thereby than by an unsplit beam of the same energy as the two beams together.

Laser separation of semiconductor elements formed in a wafer of semiconductor material

NEW MATERIAL:A phenylacetic acid derivative of formula I (R 1 and R 2 are H or lower alkyl; M is carboxyl, carbamoyl, hydroxyaminocarbonyl or lower alkoxycarbonyl; A and B are H, lower alkyl or aryl). EXAMPLE: 3-(Thiazol-2-yl)-2-hydroxyphenylacetic acid. USE: Useful as a medicine having analgesic, anti-inflammatory, antipyretic, antithrombotic and antiallergic action, etc. with high safety. PROCESS: A compound of formula II is allylated in the presence of a base in a solvent, e.g. acetone, to give a compound of formula III, which is then subjected to the Claisen rearrangement under heating at 100W300°C. The reaction product is then alkylated with an alkyl halide in the presence of a base to afford a compound of formula IV, which is then oxidized in a mixed solvent of water with acetic acid in the presence of an oxidizing agent to give the compound of formula I . COPYRIGHT: (C)1984,JPO&Japio

Novel phenylacetic acid derivative

PURPOSE: A nonsteroid antiallergic agent with small side effect, comprising 4- cyclohexene carboxylic acid derivative as an active ingredient. CONSTITUTION: A nonsteroid antiallergic agnet comprising a compound (e.g., 4- propionly-3-cyclohexene carboxylic acid methyl ester, 4-n-pentyl-3-cyclohexene carboxylic acid) shown by the formula (R 1 is H or methyl; R 2 is H, methyl, or ethyl; R 3 is H, methyl, isopropyl, t-butyl, propionly, etc.) as an active ingredient. A human does is 50W900mg/day. Various kinds of side effects caused by long-term administration of a steroid drug, e.g., adrenal cortical hormones, can be prevented. USE: Ameliorants of liver function, antifivrinolysins, atitumor agents, and antiallergic agents for diseases caused by immunological deficiency, e.g, articular rheumatism, autoimmune disease, asthma, nephritis, etc. COPYRIGHT: (C)1980,JPO&Japio

Novel antiallergic agent

NEW MATERIAL:A compound expressed by formula I (X is S, SO, SO2, O or NH; R is antiphlogistic and analgesic compound having carboxyl group at the end; l is 1-15; m is 2-15; n is 2-7) EXAMPLE:2-[{2-(2-Oxo-1-pyrrolidinyl)ethyl}thio] ethyl-d-2-(6-methoxy-2-naphthyl) propionate USE:An antiphlogistics and analgesic remarkably reduced in side effect such as gastic disease PREPARATION:An antiphlogistic and analgesic compound having carboxyl group at the end is reacted with thionyl chloride in an inert solvent (eg benzene or toluene) which does not participate in reaction under reflux for 1-5hr to give aid chloride compound, which is then reacted with azacycloalkane-2-one derivative expressed by formula II in the presence of a dehalogenating agent to provide the compound expressed by formula I

Production of azacycloalkane-2-one compound

NEW MATERIAL:An azacycloalkane derivative of formula I (R is alkyl; m is 2, 3 or 4; n is integer of 1W15; R is 5W11C alkyl when n is 1W3). EXAMPLE: 1-(2-Nonylthioethyl)azacyclopentan-2-one. USE: An absorbefacient having remarkable effect to promote the impregnation and permeation of drug in a bio-membrane, extremely low topical toxicity and systemic toxicity to bio-membrane and high safety. PREPARATION: The compound of formula I can be produced by reacting a compound of formula IV (n is integer of 2W15) with a compound of formula RSH in a solvent inert to the reaction (e.g. benzene, toluene, etc.) in the presence of a radical polymerization initiator (e.g. benzoyl peroxide, azobisisobutyronitrile, etc.) at 0W150°C for 2W18hr in nitrogen atmosphere or in the absence of the atmosphere. COPYRIGHT: (C)1987,JPO&Japio

Azacycloalkane derivative and absorbefacient containing said derivative as active component

NEW MATERIAL:A quinazoline derivative of formula I (X is H, halogen, nitro; R is alkyl, substituted alkyl, aralkyl, halogen-substituted phenyl; R is cyclic amino). EXAMPLE:1-(p-Chlorobenzyl)-2-morpholinomethyl-4-oxo-1,4-dihydroquinazo line. USE:Medicines having anti-inflammatory, CNS-depressing, and anti-histaminic activities. PROCESS:The compound I is prepared by reacting a 1-substituted-2-halomethyl-4- oxo-1,4-dihydroquinazoline derivative II (1 mole) with a cyclic amine III (2 moles) in an organic solvent such as benzene, toluene, etc., at a temperature near the boiling point of the solvent for 2-8 hours.

Yatani Terumi

Papers

Novel phenylacetic acid derivative

Novel antiallergic agent

Production of azacycloalkane-2-one compound

Azacycloalkane derivative and absorbefacient containing said derivative as active component

Novel quinazoline derivatives