Terumo Kabushiki Kaisha

Shimadzu Corporation

Kyoto University

Kabushiki Kaisha Yakult Honsha

Masashi Isozaki

Shigenori Nozawa

Shingo Koyama

Tetsuro Kawanishi

Keisuke Yoshino

Isamu Endo

Masazumi Miyakoshi

Hirokazu Hasegawa

Seigo Sawada

Eiichi Ozeki

Keiko Yamashita

Kazunori Koiwai

Takeshi Matsuzaki

Shunsaku Kimura

Hiroyuki Ohnishi

Ikuo Kato

Ryoichi Nanba

Nobuyuki Nakata

Tadashi Okumura

Yoshiyuki Shikata

Keiichi Nakazawa

Katsuyoshi Sugizaki

Naoya Mikami

Harue Akasofu

Ryohei Yanoshita

Masayuki Fujitake, Deceased

Norio Arakawa

Yukari Yoshiyama

Masayo Kondo

Hitoshi Akitsu

Kazuhiro Shimizu

Ryoji Fushimi

Kyoko Taguchi

A coating composition for drug eluting medical devices, which is capable of forming a drug coating layer that is not susceptible to peeling during delivery to a target tissue is provided. This coating composition contains: a water-insoluble drug; at least one selected from the group consisting of hyaluronic acid, alkanoyl hyaluronic acids obtained by substituting at least part of hydrogen atoms in the hydroxyl groups of hyaluronic acid with an alkanoyl group, and salts of hyaluronic acid and the alkanoyl hyaluronic acids; and at least one selected from the group consisting of amino-acid esters and salts thereof. A drug coating layer, a medical device and a method of treatment are also provided.

Coating composition and medical device

The present invention provides a novel amphiphilic substance, a nanoparticle using the novel amphiphilic substance, which can be used as a nanocarrier having high biocompatibility, a drug delivery system and a probe useful for the system, and, a molecular imaging system and a probe useful for the system. An amphiphilic block polymer comprising a hydrophilic block; and a hydrophobic block, wherein the hydrophilic block is a hydrophilic polypeptide chain having 10 or more sarcosine units, and the hydrophobic block is a hydrophobic molecular chain comprising units selected from the group consisting of amino acid units and hydroxyl acid units as essential structural units, and having 5 or more of the essential structural units.

Amphiphilic substance, and drug delivery system and molecular imaging system using the same

A liposome preparation is provided. This liposome preparation is capable of stably encapsulating a drug which is unstable under an acidic condition, and such stable encapsulation is realized without detracting the effect realized by the modification of the membrane by a hydrophilic macromolecule such as stability in blood. More specifically, the liposome preparation comprises a unilamellar vesicle formed from a lipid bilayer comprising a phospholipid as its main membrane component, and an interior aqueous phase of the vesicle at a pH of up to 5. The liposome has a drug loaded therein, and the vesicle is modified with a hydrophilic macromolecule only on its exterior surface.

Liposome preparation

Provided is an irinotecan formulation capable of supporting irinotecan and/or a salt thereof in a closed vesicle carrier at a high concentration and existing in blood for a long period of time by dramatically improved retentivity in blood compared to a conventionally known irinotecan liposome formulation. That is, an irinotecan formulation including a closed vesicle formed by a lipid membrane, in which irinotecan and/or a salt thereof is encapsulated at a concentration of at least 0.07 mol/mol (drug mol/membrane total lipid mol). There is an ion gradient between an inner aqueous phase and an outer aqueous phase in the irinotecan formulation. The closed vesicle is preferably liposome, in which only the outer surface of the liposome is preferably modified with a surface-modifying agent containing a hydrophilic polymer.

Irinotecan preparation

A process for preparing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying the resulting reaction product with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatography wherein R represents an alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.

Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative

Disclosed herein is a process for production of an O-alkylrapamycin derivative represented by the general formula (1) below by reaction between rapamycin and alkyl triflate in an organic solvent, characterized in that the reaction is carried out in the presence of trialkylamine. (where R denotes alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.) This process is capable of producing O-alkylrapamycin derivative efficiently owing to improvement in reaction yields for O-alkylation.

Process for production of O-alkylated rapamycin derivatives

Novel amidine derivatives of the formula (1); and drug carriers such as liposomes or emulsions comprising the derivatives, which can enclose genetic materials or drugs and transfer them to cells or affected sites efficiently and safely,

Amidine derivatives and drug carriers comprising the same

Illustrative examples of the N-(3-pyridylalkyl)sulfonamide derivative are represented by the following formulae [II] and [III]: ##STR1## The derivatives are available for a thromboxane A.sub.2 production inhibitor, a thromboxane A.sub.2 antagonist, a prostaglandin H.sub.2 antagonist, an anti-thrombus agent, a thrombus-preventing agent and an anti-allergy agent.

N-(3-pyridylalkyl)sulfonamide compounds which have useful pharmaceutical

Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 and R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.x --CHR.sub.3 --(CH.sub.2).sub.y -- in which R.sub.3 represents hydrogen or a lower alkyl group and x and y represent an integer of 0 to 2, respectively, A represents the formula --CH.dbd.CH-- or --CH.dbd.N--, 1 is 1 or 2, m represents an integer of 0 to 2 and n represents an integer of 1 to 5. The thiourea derivatives possess an antiulcer activity and an antimicrobial activity against Helicobacter pyroli and are useful as an antiulcer agent and an antimicrobial agent against Helicobacter pyroli.

Thiourea derivatives and antimicrobial agent and antiulcer agent

Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof. The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.

Thiourea derivatives and antimicrobial agent and antulcer agent

Novel phenoxypropylamine derivative having the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom, a hydroxy group, a lower alkyl group or a lower alkoxy group, and R.sub.3 and R.sub.4 represent a lower alkyl group, or R.sub.3 and R.sub.4 taken together represent a group having the formula (CH.sub.2).sub.m wherein m represents 4 or 5, and n represents an integer of from 2 to 6 or a pharmaceutically acceptable salt thereof. The compounds are useful as a 5-lipoxygenase inhibitor and an antiulcer agent.

Phenoxypropylamine derivatives or salts thereof and antiulcer agents

Growing community of inventors

Kanagawa, Japan

Masashi Isozaki