Shiseido Company, Limited

Masaru Suetsugu

Hiroshi Fukui

Satoshi Amano

Hirotada Fukunishi

Mikiko Kaminuma

Minoru Fukuda

Shunsuke Iriyama

Eijiro Hara

Tomiyuki Nanba

Kazuhisa Ohno

Masato Hatao

Shinji Inomata

Haruhiko Inoue

Masumi Koishi

Toshii Iida

Toshihiko Nakane

Makoto Tsunenaga

Eiichiro Yagi

Shigenori Kumagai

Yuji Matsushita

Takuya Hiruma

Haruo Ogawa

Shigeru Mugikura

Hiroyuki Yokoyama

Keiko Sakai

Yutaka Okunuki

Rumiko Kaku

Susumu Takada

Yuki Shibata

Toshihide Ebisawa

Tadao Ohta

Satoshi Shinojima

Fujihiro Kanda

Yoshio Yahata

Yoshihiro Morikawa

Kenichi Tomita

Okihiko Sakamoto

Naoto Hanyu

Kiyoshi Sato

Manami Ohnuma

Takao Higashi

Nobuhiko Ochiai

Osamu Moro

Chika Katagiri

Rikako Suzuki

Toshihiro Tanaka

Kenji Kitamura

Naoe Akiyama

Yuki Yamase

Masayuki Asaike

Norimichi Koizumi

Keiko Takada

Tsuneo Suehiro

Yuji Katsuta

A heparanase activity inhibitor containing, as an active ingredient, a 4-alkylresorcinol represented by formula (I): wherein R represents a C1-6 linear or branched alkyl group.

Heparanase activity inhibitor, wrinkle improving agent containing same, and pharmaceutical composition

The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin-inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of &#x3b2;-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of &#x3b2;-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.

Parakeratosis inhibitor, pore-shrinking agent and external composition for skin

A heparanase activity inhibitor comprising, as an active ingredient, a cyclic carboxamide derivative represented by formula (I): wherein n is an integer of 1 to 3, Ris hydrogen or a C1-6 hydrocarbon group optionally substituted with hydroxyl, X is &#x2014;CH&#x2014; or a group represented by &#x2014;N(R)&#x2014;, and Ris hydrogen or a C1-6 hydrocarbon group optionally substituted with hydroxyl,or a salt thereof.

Heparanase activity inhibitor

The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a &#x3b2;-diketone compound (3) to produce the pyrimidinylpyrazole compound: 

Method for producing pyrimidinylpyrazole compounds

To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives. Further, there are provided a parakeratosis inhibitor, a pore reducing agent and a skin roughness preventing/ameliorating agent each comprising at least one compound selected from the group consisting of specified glycine derivatives and salts thereof and specified aminosulfuric acid derivatives and salts thereof. Still further, there are provided skin preparations for external use comprising these compounds.

Parakeratosis inhibitor and skin preparation for external use

The present invention provides a compound that has a high whitening effect and is excellent in safety and stability and provides an external preparation for skin comprising the same. The compound of the present invention is a 4-alkylresorcinol derivative represented by formula (1) or a salt thereof: 

4-alkylresorcinol derivative and external preparation for skin containing the same

The present invention provides an agent for preventing and alleviating wrinkles which has excellent effects of preventing and alleviating wrinkles formed by decreased barrier function of the skin owing to aging or photo aging, that is graphic wrinkles or linear wrinkles. The agent for preventing and alleviating wrinkles consisting of one or more compounds selected from the group consisting of gamma-aminobutyric acid derivatives represented by the following formula (1) or N,N,N-trimethyl gamma-aminobutyric acid represented by the following formula (3) and salts thereof: wherein Rand Rindependently represent any of a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a benzyloxycarbonyl group, a cyclohexyl group, a cyclohexanemethyl group, a cyclohexanecarbonyl group, a guanidino group formed with nitrogen atom in the formula (1), an ureido group formed with nitrogen atom in the formula (1), and a group represented by following formula (2). Additionally, Rand Rmay jointly form a piperidine ring, morpholine ring, or pyrrolidine ring. Both of Rand Rare not simultaneously a hydrogen atom.

Agent for alleviating wrinkles

The present invention provides a composition for external application to skin containing one type or two or more types of compounds selected from the group consisting of aminoacetoamide compounds represented by the following general formula (1) and salts thereof. 

Composition for external application to skin

The present invention is benzilidene malonamide represented by the following formula (1) and salts thereof, an ultraviolet absorbent consisting of said new compound, and an external preparation containing this ultraviolet absorbent. The object of the present invention is to provide a new ultraviolet absorbent that is highly soluble in water, has superior absorption capacity over a wide ultraviolet wavelength range, has no absorption in the visible region, and is also highly stable and safe. 

Benzylidene malonamide and salt thereof, ultraviolet ray absorbent, and agent for external application to the skin

Ultraviolet absorbent, photostabilizer, ultraviolet ray-absorbing composition, photostabilized composition and external preparation for skin

Pyridazine derivatives and related composition

Pyridazine derivatives, manufacturing method and related composition

An endermic liniment containing at least one type of phenylalanine compound, and/or its salt, is disclosed. This endermic liniment has a melanin production suppression effect and is superior in terms of its skin whitening effect as in preventing and/or improving chloasma, freckles and pigmentation in the skin after sunburn. It is also stable and highly safe.

Endermic liniment

An external preparation for the skin comprising at least one of the glycosides or hydroxysaliyclic acid and/or the glycosides of aliphatic esters of hydroxysalicylic acid represented by the following formula 1: ##STR1## wherein R.sub.1 represents one selected from the group consisting of saturated hydrocarbon group and an unsaturated hydrocarbon group which have 1 to 20 carbon atoms and which may be either a straight-chain or a branched chain, and one of R.sub.2 and R.sub.3 represents a sugar residue and the other hydrogen. The external preparation for the skin has an excellent whitening effect and/or an excellent skin care effect.

External preparation for skin

Growing community of inventors

Yokohama, Japan

Masaru Suetsugu