Tanabe Seiyaku Company, Limited

Tanabe Seivaku Co., Ltd.

Kenji Tsujihara

Takayuki Kawaguchi

Sumihiro Nomura

Motoaki Ohashi

Yoshihisa Arai

Mitsuya Hongu

Satoshi Okuno

Toshiro Yano

Kenji Arakawa

Masakatsu Ozeki

Masanori Inamasu

Tomiki Hashiyama

Kunio Saito

Noriyuki Nakanishi

Kunihiko Ozaki

Naoyuki Harada

Nobuyuki Funami

Mamoru Matsumoto

Osamu Ohtsuki

Tadashi Nakatani

Koji Oda

Tetsuo Yamaguchi

Mikio Takeda

Akira Suzuki

Saburo Matsuda

Shigeyuki Ishikawa

Akira Oku

Kozo Oka

Satoshi Furuuchi

Tamio Morikawa

Nitrogen-containing fused heterocyclic carboxylic acid having an absolute configuration of 'R' of the formula [XIX]: wherein Y is substituted or unsubstituted arylsulfonyl group or an alkylsulfonyl group, and n is 0 or 1, or a salt thereof.

Nitrogen-containing fused heterocyclic carboxylic acids having an absolute configuration of 'R'

S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof

Camptothecin derivatives

A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound &lsqb;II&rsqb;:

A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R.sup.0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of 'R'(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: ##STR2## wherein the symbols are as defined above.

S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and

A propiophenone derivative of the formula (I): ##STR1## wherein OX is a hydroxy group which may optionally be protected, Y is a lower alkyl group, and Z is a .beta.-D-glucopyranosyl group wherein one or more hydroxy groups may optionally be protected, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

Propiophenone derivatives and process for preparing the same

A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound �II!: ##STR1## wherein R.sup.o is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of 'R'(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound �I!: ##STR2## wherein the symbols are as defined above.

A camptothecin derivative comprising a compound of the formula �I!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.

A camptothecin derivative comprising a compound of the formula �I!: ##STR1## wherein R.sup.1 is a substituted or unsubstituted lower alkyl group, X.sup.1 is a group of the formula: --NHR.sup.2 (R.sup.2 is a hydrogen atom or a lower alkyl group) or a group of --OH, and Alk is a straight chain or branched chain alkylene group having optionally an oxygen atom in the chain thereof, bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects unlike conventional anticancer agents, and hence, these compounds are extremely useful as a medicament.

A propiophenone derivative of the formula �I!: ##STR1## wherein X is O, S or methylene, OY is a protected or unprotected OH, Z is .beta.-D-glucopyranosyl or 4-O-(.alpha.-D-glucopyranosyl)-.beta.-D-glucopyranosyl or wherein one or more hydroxy groups of these groups may optionally be acylated, and the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

Propiophenone derivative and a process for preparing the same

A propiophenone derivative the formula �I!: ##STR1## wherein R' is a lower alkanoyl group and R' is a hydrogen atom, or R' is a hydrogen atom and R' is a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

Propiophenone derivative and processes for preparing the same

Disclosed is a hair-growing (restoration) agent which comprises a carnitine compound represented by the formula (I): ##STR1## wherein R.sup.1 to R.sup.3 each represent an alkyl group having 1 to 6 carbon atoms; R.sup.4 represents an aliphatic acyl group having 3 to 31 carbon atoms which may be substituted; R.sup.5 represents an alkyl group having 3 to 31 carbon atoms which may be substituted, or an alkenyl group having 3 to 31 carbon atoms which may be substituted; and X.sup.- represents an anion of a pharmaceutically acceptable acid, as an active ingredient.

Hair-growth agent

Growing community of inventors

Urawa, Japan

Kenji Tsujihara