Pola Chemical Industries, Inc.

Masashi Tamai

Takayuki Namiki

Naoki Hiyama

Satoshi Ichinomiya

Masayuki Yuasa

Yukio Kawazu

Kenichi Kishii

Takako Takakuwa

Mayumi Sugio

Tomoaki Yahiro

Makoto Kimura

Mariko Harada

Norio Funayama

Kyoko Taneda

Yuko Saitoh

Kouji Yokoyama

Masaki Mitani

Yu Ikeda

Tomomi Kato

Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent. At least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group. When one of R1 and R2 is an oxo group, the other is not present. R3 is selected from a hydrogen atom, and a Chydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms. The number of R3's present in the compound corresponds to X and, when two or more R3's are present, the R3's are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.

Melanin production inhibitor

Biphenyl derivatives represented by the following formula (1): wherein Rrepresents a Calkyl group, Rrepresents a substituted or unsubstituted aromatic hydrocarbon, or cycloalkyl group, Rrepresents a tetrazolyl group, &#x2014;NHCOCF, &#x2014;NHSOCFor &#x2014;SONHCONHRin which Rrepresents a substituted or unsubstituted aromatic hydrocarbon group, and Z represents a single bond, a Calkylene group or &#x2014;SONH&#x2014;, and salts thereof; and ACAT inhibitors and medicines containing them as active ingredients. The compounds according to the present invention possess excellent ACAT inhibitory activities, and are useful as preventives and/or therapeutics for diseases cased by the enhancement of ACAT activity, for example, hypercholesterolemia, atherosclerosis and the like.

Biphenyl derivatives

The invention relates to a therapeutic and preventive medicament for respiratory diseases, comprising, as an active ingredient, a compound represented by the general formula (1):

Pyrrolo&lsqb;3,2-e&rsqb;pyrazolo&lsqb;1,5-a&rsqb;pyrimidine remedies/preventives for respiratory diseases

The invention relates to compounds represented by the following general formula (1): ##STR1## wherein R.sup.1 represents an alkyl group, R.sup.2 represents an amino group, alkyl group or the like, and R.sup.3 represents a nitro group, amino group, heterocyclic group, alkylsulfonylamino group or the like, or salts thereof, medicines comprising such a compound, a preparation process of the compounds, and intermediates useful for preparation thereof. The compounds (1) are useful for the prevention and treatment of a respiratory disease.

Pyrrolopyrazolopyrimidine compound and medicine comprising the same as

Growing community of inventors

Yokohama, Japan

Masashi Tamai