Other

Yamanouchi Pharmaceutical Company Ltd.

Kuraray Co., Ltd.

Hiroshi Maeda

Kayaku Antibiotics Research Co., Ltd.

Amano Pharmaceutical Co., Ltd.

Mitsubishi Gas Chemical Company, Inc.

Kirin Brewery Company, Limited

Dojindo Laboratories

Kayaku Antibiotic Research Co., Ltd.

Biodynamic Research Foundation

Kirin-seagram Limited

Pfizer Corporation

Maeda, Hiroshi

Takaaki Akaike

Nakao Ishida

Fujio Suzuki

Ryunosuke Kanamaru

Jun Fang

Minoru Ueda

Hideaki Nakamura

Toshihiko Yoshitake

Tomohiro Sawa

Makoto Hashizume

Masaharu Murata

Steffen Hackbarth

Toshimitsu Konno

Toshikatsu Fujii

Ituro Mizutani

Katsuhide Nishi

Haibo Qin

Khaled Greish

Tatsuya Oda

Yoichi Miyamoto

Hideyuki Tanaka

Junsuke Tone

Hiroitsu Kawata

Masayoshi Aruga

Teizi Urakami

Kazumi Sasamoto

Osamu Asami

Masayasu Inoue

Jun Sekino

Shunji Hasumi

Kiichiro Oka

Akira Okada

Shohei Tanaka

Ken Iwai

Go Ohtani

Ken Okumura

Keizo Sato

Tetsuya Tsukamoto

Yoshiki Katayama

Masaki Yoshida

Masae Tatematsu

Yasuhiro Matsumura

Ikuharu Sasaki

Mitsugu Kobayashi

Hideo Nishigoori

Chieko Yoshida

Ryusuke Tsunoda

John Philip Dirlam

The present invention provides a formulation having excellent solubility and/or stability of a macromolecular drug, and more specifically, a pharmaceutical composition containing a macromolecular drug, a dissolution-enhancing and/or stabilizing agent, and an aqueous solvent, wherein the dissolution-enhancing and/or stabilizing agent is at least one selected from the group consisting of (1) proteins, (2) synthetic polymers, (3) sugars or sugar alcohols, (4) inorganic salts, (5) amino acids, (6) phospholipids, (7) aliphatic alcohols, (8) medium-chain fatty acids, and (9) mucopolysaccharides.

Pharmaceutical composition containing macromolecular drug

The present invention provides a fluorescent molecular probe for efficient fluorescent detection (visualization) of tumors or for implementing fluorescent detection and photodynamic treatment, more specifically, the present invention provides a macromolecular fluorescent molecular probe for fluorescent detection of tumor, comprising a complex comprising a fluorescent molecule and a biocompatible macromolecule.

Polymer-type fluorescent molecule probe

The present invention provides a group of novel SMA derivatives and a covalent conjugate of the derivatives and an active substance. More specifically, the present invention provides: an SMA derivative which contains (i) a styrene-maleic acid copolymer (SMA) and (ii) a side chain (b) that contains a functional group (a) selected from among &#x2014;NH2, &#x2014;SH, &#x2014;OH, &#x2014;COOH, &#x2014;NH&#x2014;(C&#x2550;NH)&#x2014;NHand &#x2014;C(CH&#x2014;OH)and introduced into a carboxyl group of a maleic acid residue of the SMA via an amide bond or an ester bond, and wherein when a plurality of side chain (b) is introduced into the SMA, the side chains (b) may be identical or different from each other; and a conjugate of this SMA derivative and an active substance.

Derivative of styrene-maleic acid copolymer

The present invention provides a fluorescent molecular probe for efficient fluorescent detection (visualization) of tumors or for implementing fluorescent detection and photodynamic treatment, more specifically, the present invention provides a macromolecular fluorescent molecular probe for fluorescent detection of tumor, comprising a complex comprising a fluorescent molecule and a biocompatibie macromolecule.

An anti-inflammatory agent or cancer-preventive agent comprising 4-vinyl-2,6-dimethoxyphenol of the formula (1): or a PD thereof.

Anti-inflammatory agent and cancer-preventive agent comprising canolol or prodrug thereof and pharmaceutical, cosmetic and food comprising the same

The present invention provides a polymeric agent which can incorporate a large amount of a drug, accumulate selectively in a tumor site, and has a molecular size of more than that for renal excretion. A metalloporphyrin derivative (such as zinc protoporphyrin) is associated with a styrene-maleic acid copolymer via non-covalent bond to give a SMA micelle complex, allowing provision of a polymeric pharmaceutical agent for treatment of cancer with a large amount of the drug incorporated. The SMA micelle complex can be produced by a method, wherein the metalloporphyrin derivative reacts with the styrene-maleic acid copolymer in the absence of a condensation agent under an alkaline condition, solubilized, adjusted to have a pH of 6-8, and subjected to a procedure for separating a polymer component to recover the micelle complex component for the polymeric pharmaceutical agent.

Polymeric pharmaceutical agent for treatment of cancer and method for production of the same

The present invention relates to polymeric antitumor agent which is formed in polymeric micelle complex by intermolecular bonding or mutual interaction between styrene maleic acid copolymer (SMA) and low molecule antitumor agent which is anthracyclins drug such as pirarubicin, doxorubicm, epirbicin, daunorbicin, acralbicin, or alkaloid antitumor agent such as cis-platinum, and taxol These polymeric antitumor agents may improve specificity to cancer cells so that it improves antitumor effect, while it may not be concentrated at normal organ or tissue, so that adverse effect may be diminished. These polymeric antitumor agents may be prepared by dissolving SMA and low molecule antitumor agent in aqueous solution, then in the presence of aqueous soluble carbodiimide, amino acids, or polyamine, adjusting pH to form micelle complex and recovering polymer fraction.

Antitumor agent and process for producing the same

An antitumor agent, which is a combination of an oxidoreductase, such as xanthine oxidase chemically conjugated to a polymer such as poly ethylene glycol, for initial administration and accumulation in the tumor tissue followed by administration and of a substrate for the oxidoreductase which releases reactive oxygen species. Improved tumor selective cytotoxic activity results.

Antitumor agents

Anticancer agents which contain as the active ingredient, a heme oxygenase inhibitory metalloporphyrin derivatives which are conjugated with amphipathic or water-soluble polymers (in particular, Zn-protoporphyrin (ZnPP) conjugated with polyethylene glycol). Because of being conjugated to amphipathic or water-soluble polymers, such as polyethylene glycol, the active ingredient can be administered by intravenous injection and can exert a remarkable anticancer effect owing to tumor selective delivery.

Antitumor agents and process for producing the same

An antitumor agent, which is a combination of an oxidoreductase, such as xanthine oxidase chemically conjugated to a polymer such as poly ethylene glycol, for initial administration and accumulation in the tumor tissue followed by administration of a substrate for the oxidoreductase which releases reactive oxygen species. Improved tumor selective cytotoxic activity results.

A method for treatment of viral infections which comprises administering to the patients being suffering from said viral infections an effective amount of one or more substances selected from the group consisting of nitric oxide scavengers and nitric oxide synthase inhibitors. Said method for treatment of viral infections is useful in viral infections induced by influenza virus, herpes virus, hepatitis virus, cytomegalovirus, human immunodeficiency virus, etc.

Agent for treatment of viral infections

Antihypertensive agents containing as its active ingredient the 4-amino-6-hydroxypyrazolo �3,4-d!pyrimidine(AHPP) or its derivatives represented by the general formula (I) below. ##STR1## where R is hydrogen atom, alkyl group or aryl group.

Method for treating hypertension using pyrazolopyrimidine derivatives

This invention offers the compounds which exhibit a coronary blood vessel dilating action which is long-acting. (Constitution) Novel imidazolinoxyl derivatives represented by a general formula (1). A compound A in which R is COOH is given in an example. ##STR1## (Merit) The compounds of the present invention can be directly administered, after diluting to a suitable concentration with a phosphate buffer or the like, to blood vessel which is required to be relaxed and dilated whereby a significant and long-acting relaxing action is resulted though, in a blood flow, they are quickly inactivated and excreted and no side effect is noted.

Imidazolinoxyl derivatives

2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide derivatives and

A composition for oral administration to cancer patients includes a neocarzinostatin derivative and from 0.1 and 100 ml per mg of the neocarzinostatin derivative of at least one fatty acid glyceride which has from 6 to 20 carbon atoms and which is noniodized. The composition is effective in the treatment of cancer by oral administration, including a solid cancerous tumor.

Neocarzinostatin derivative composition for oral administration

Growing community of inventors

Kumamoto, Japan

Hiroshi Maeda