EP0303697A1 — Derivatives of physiologically active substance k…

Claim 1

Independent Claim 765 words

A K-252 derivative represented by formula (I) and a pharmacologically acceptable salt thereof wherein: R 1 represents hydrogen, methyl, hydroxy, hydroxymethyl, lower alkoxy, bromine, chlorine or - NR 5 R 6 (wherein either R 5 or R 6 is hydrogen and the other is hydrogen, carbamoyl or lower alkylaminocarbonyl, or both are lower alkyl) and R is hydrogen, or R 1 and R 3 are the same and represent hydroxy, lower alkoxy or amino; R 2 is hydrogen or amino; R 4 is hydrogen, chlorine, carbamoyl, lower alkyl, amino or -CH 2 CH 2 R 7 (wherein R is bromine, amino, di-lower alkylamino, hydroxy or hydroxy-substituted lower alkylamino); W 1 and W 2 are hydrogen or both are combined together to represent oxygen; X is hydrogen, formyl, lower alkoxycarbonyl, (wherein R 8 and R 9 are independently hydrogen, lower alkyl or hydroxy-substituted lower alkyl, or R is hydrogen and R 9 is hydroxy), -CH 2 A {wherein A is hydroxy, azido, lower alkylthio, lower alkylsulfenyl, [wherein either R 10 or R 11 is hydrogen and the other is hydrogen, lower alkyl, allyl, carboxylic acid-substituted lower alkyl, dihydroxy-substituted lower alkyl, a residue of an a-amino acid in which the hydroxy of the carboxylic acid is removed or lower alkoxycarbonyl-substituted lower alkyl; or both are lower alkyl or chlorine-substituted lower alkyl; or R 10 and R 11 are combined together to form -CH 2 CH 2 -B-CH 2 CH 2 - (wherein B is -CH 2 -, -NH-, -S- or -0-)], -N= C H-NMe 2 (wherein Me is methyl), -OCOCH 2 CH 2 CO 2 H or or -CH=N-R 12 (wherein R 12 is hydroxy, amino, guanidino or 2-imidazolylamino); Y is hydroxy or carbamoyloxy; or X and Y are combined together to form, as -X-Y-, O=, -CH 2 O-, -CH 2 OCOO-, -CH 2 -O-CS-O-, -CH 2 -NR 13 -CO-O- [wherein R 13 is hydrogen, lower alkyl, allyl, formylmethyl, -CH 2 CH(OH)-CH 2 OH, alkylthio); with the proviso that: when W 1 and W 2 are combined together to represent oxygen, R 1 , R 2 and R 3 are all hydrogen; when R 4 is lower alkyl, amino or -CH 2 CH 2 R 7 , W 1 and W 2 are combined together to represent oxygen; when Y is carbamoyloxy, R 1 , R 2 , R 3 , W 1 and W 2 are all hydrogen, R 4 is carbamoyl and X is lower alkoxycarbonyl; when R 4 is chlorine, R 1 , R 2 , R 3 , W 1 and W 2 are all hydrogen and X is lower alkoxycarbonyl; when X is hydrogen, formyl, (wherein R 8a and R 9a are independently hydrogen, lower alkyl, hydroxy-substituted lower alkyl) or CH 2 Aa (wherein the Aa representation is the same as the above A representation excluding hydroxy and amino) or -CH=N-R 12 , R 1 , R 2 , R 3 , R 4 , W 1 and W 2 are all hydrogen; when X is CONHOH, R 1 , R 2 , R 3 and R 4 are all hydrogen; when X is lower alkoxycarbonyl, R 4 is hydrogen, chlorine, carbamoyl, lower alkyl or -CH 2 CH 2 R 7a (wherein R 7a is bromine or di-lower alkylamino); when X is aminomethyl, R 1 , R 2 and R 3 are hydrogen, and when W 1 and W 2 are combined together to represent oxygen, R 4 is hydrogen or amino and when W 1 and W 2 are hydrogen, R 4 is hydrogen; when X and Y are combined together to represent, as -X-Y-, -O-, -CH 2 -O-, -CH 2 -O-CO-O-, -CH 2 -O-CS-O-, -CH 2 -NR 13a -CO-O- (wherein the R 13a representation is the same as the above R 13 representation excluding hydrogen and lower alkyl), -CH 2 -NH-CS-O-, -CH 2 -O-SO-O- or R 1 , R 2 , R 3 , R 4 , W 1 and W 2 are all hydrogen; when X and Y are combined together to represent, as -X-Y-, -CH 2 -NR 13b- CO-O- (wherein R 13b is hydrogen or lower alkyl), R 1 , R 2 , R 3 and R 4 are all hydrogen; when R is methyl, hydroxy, hydroxymethyl, lower alkoxy, bromine, chlorine or -NR 5 R 6 , R 2 and R 4 are hydrogen; when R 2 is amino, R 1 and R 4 are hydrogen; and the combinations wherein R 1 , R 2 , R 3 , R 4 , W 1 and W 2 are hydrogen, X is methoxycarbonyl and Y is hydroxy are excluded.

Claim 2

Dependent Claim 765 words

A K-252 derivative represented by formula (I) and a pharmacologically acceptable salt thereof wherein: R 1 represents hydrogen, methyl, hydroxy, hydroxymethyl, lower alkoxy, bromine, chlorine or - NR 5 R 6 (wherein either R 5 or R 6 is hydrogen and the other is hydrogen, carbamoyl or lower alkylaminocarbonyl, or both are lower alkyl) and R is hydrogen, or R 1 and R 3 are the same and represent hydroxy, lower alkoxy or amino; R 2 is hydrogen or amino; R 4 is hydrogen, chlorine, carbamoyl, lower alkyl, amino or -CH 2 CH 2 R 7 (wherein R is bromine, amino, di-lower alkylamino, hydroxy or hydroxy-substituted lower alkylamino); W 1 and W 2 are hydrogen or both are combined together to represent oxygen; X is hydrogen, formyl, lower alkoxycarbonyl, (wherein R 8 and R 9 are independently hydrogen, lower alkyl or hydroxy-substituted lower alkyl, or R is hydrogen and R 9 is hydroxy), -CH 2 A {wherein A is hydroxy, azido, lower alkylthio, lower alkylsulfenyl, [wherein either R 10 or R 11 is hydrogen and the other is hydrogen, lower alkyl, allyl, carboxylic acid-substituted lower alkyl, dihydroxy-substituted lower alkyl, a residue of an a-amino acid in which the hydroxy of the carboxylic acid is removed or lower alkoxycarbonyl-substituted lower alkyl; or both are lower alkyl or chlorine-substituted lower alkyl; or R 10 and R 11 are combined together to form -CH 2 CH 2 -B-CH 2 CH 2 - (wherein B is -CH 2 -, -NH-, -S- or -0-)], -N= C H-NMe 2 (wherein Me is methyl), -OCOCH 2 CH 2 CO 2 H or or -CH=N-R 12 (wherein R 12 is hydroxy, amino, guanidino or 2-imidazolylamino); Y is hydroxy or carbamoyloxy; or X and Y are combined together to form, as -X-Y-, O=, -CH 2 O-, -CH 2 OCOO-, -CH 2 -O-CS-O-, -CH 2 -NR 13 -CO-O- [wherein R 13 is hydrogen, lower alkyl, allyl, formylmethyl, -CH 2 CH(OH)-CH 2 OH, alkylthio); with the proviso that: when W 1 and W 2 are combined together to represent oxygen, R 1 , R 2 and R 3 are all hydrogen; when R 4 is lower alkyl, amino or -CH 2 CH 2 R 7 , W 1 and W 2 are combined together to represent oxygen; when Y is carbamoyloxy, R 1 , R 2 , R 3 , W 1 and W 2 are all hydrogen, R 4 is carbamoyl and X is lower alkoxycarbonyl; when R 4 is chlorine, R 1 , R 2 , R 3 , W 1 and W 2 are all hydrogen and X is lower alkoxycarbonyl; when X is hydrogen, formyl, (wherein R 8a and R 9a are independently hydrogen, lower alkyl, hydroxy-substituted lower alkyl) or CH 2 Aa (wherein the Aa representation is the same as the above A representation excluding hydroxy and amino) or -CH=N-R 12 , R 1 , R 2 , R 3 , R 4 , W 1 and W 2 are all hydrogen; when X is CONHOH, R 1 , R 2 , R 3 and R 4 are all hydrogen; when X is lower alkoxycarbonyl, R 4 is hydrogen, chlorine, carbamoyl, lower alkyl or -CH 2 CH 2 R 7a (wherein R 7a is bromine or di-lower alkylamino); when X is aminomethyl, R 1 , R 2 and R 3 are hydrogen, and when W 1 and W 2 are combined together to represent oxygen, R 4 is hydrogen or amino and when W 1 and W 2 are hydrogen, R 4 is hydrogen; when X and Y are combined together to represent, as -X-Y-, -O-, -CH 2 -O-, -CH 2 -O-CO-O-, -CH 2 -O-CS-O-, -CH 2 -NR 13a -CO-O- (wherein the R 13a representation is the same as the above R 13 representation excluding hydrogen and lower alkyl), -CH 2 -NH-CS-O-, -CH 2 -O-SO-O- or R 1 , R 2 , R 3 , R 4 , W 1 and W 2 are all hydrogen; when X and Y are combined together to represent, as -X-Y-, -CH 2 -NR 13b- CO-O- (wherein R 13b is hydrogen or lower alkyl), R 1 , R 2 , R 3 and R 4 are all hydrogen; when R is methyl, hydroxy, hydroxymethyl, lower alkoxy, bromine, chlorine or -NR 5 R 6 , R 2 and R 4 are hydrogen; when R 2 is amino, R 1 and R 4 are hydrogen; and the combinations wherein R 1 , R 2 , R 3 , R 4 , W 1 and W 2 are hydrogen, X is methoxycarbonyl and Y is hydroxy are excluded.

Claim 3

Dependent Claim 136 words

A compound represented by formula (Ia) and a pharmacologically acceptable salt thereof: {wherein Xa is alkoxycarbonyl having 3 to 6 carbon atoms, (wherein R 8 and R 9 are independently hydrogen, lower alkyl or hydroxy-substituted lower alkyl, or R 8 is hydrogen and R 9 is hydroxy), or -CH 2 Ab [wherein Ab is hydroxy, azido, lower alkylthio, lower alkylsulfenyl, (wherein either R 10a or R 11a is hydrogen and the other is hydrogen, lower alkyl, or both are lower alkyl; or R 10a and R 11a are combined together to form -CH 2 CH 2 -0-CH 2 CH 2 -)]; and Ya is hydroxy; or Xa and Ya are combined together to form, as -Xa-Ya-, -0-, -CH 2 -0-, -CH 2 O-CO-O-, -CH 2 -O-CS-O-, -CH 2 -NH-CO-O- or -CH 2 -O-SO-O-}. (Inventors: Group A)

Claim 4

Dependent Claim 136 words

A compound represented by formula (Ia) and a pharmacologically acceptable salt thereof: {wherein Xa is alkoxycarbonyl having 3 to 6 carbon atoms, (wherein R 8 and R 9 are independently hydrogen, lower alkyl or hydroxy-substituted lower alkyl, or R 8 is hydrogen and R 9 is hydroxy), or -CH 2 Ab [wherein Ab is hydroxy, azido, lower alkylthio, lower alkylsulfenyl, (wherein either R 10a or R 11a is hydrogen and the other is hydrogen, lower alkyl, or both are lower alkyl; or R 10a and R 11a are combined together to form -CH 2 CH 2 -0-CH 2 CH 2 -)]; and Ya is hydroxy; or Xa and Ya are combined together to form, as -Xa-Ya-, -0-, -CH 2 -0-, -CH 2 O-CO-O-, -CH 2 -O-CS-O-, -CH 2 -NH-CO-O- or -CH 2 -O-SO-O-}. (Inventors: Group A)

Claim 5

Dependent Claim 371 words

A K-252 derivative represented by formula (Ib) and a pharmacologically acceptable salt thereof: [wherein R la represents hydrogen, methyl, hydroxymethyl, bromine, hydroxy, lower alkoxy or -NR 5 R 6 (wherein either R S or R 6 is hydrogen and the other is hydrogen, carbamoyl or lower alkylaminocarbonyl, or both are lower alkyl) and R 3 is hydrogen, or R 1a and R 3 are the same and represent hydroxy, lower alkoxy or amino; R 4a is hydrogen, chlorine, carbamoyl or lower alkyl; W 1 and W 2 are hydrogen or both are combined together to represent oxygen; Xb is formyl, hydroxymethyl, lower alkoxycarbonyl, -CH=N-R 12 (wherein R 12 is hydroxy, amino, guanidino or 2-imidazolylamino), and Yb is hydroxy or carbamoyloxy, or Xb and Yb are combined together to form, as -Xb-Yb-, -CH 2 -NH-CS-O- or R l4 a -CH2-N=C-O- (wherein R 14a is lower alkylthio); with the proviso that: when W 1 and W 2 are oxygen, both R 1a and R 3 are hydrogen, Xb is lower alkoxycarbonyl or hydroxymethyl, R 4a is hydrogen or lower alkyl and Yb is hydroxy; when Yb is carbamoyloxy, R 1a , R 3 , W 1 and W 2 are all hydrogen, R 4a is carbamoyl and Xb is lower alkoxycarbonyl; when R 4a is chlorine, R 1a , R 3 , W 1 and W 2 are all hydrogen and Xb is lower alkoxycarbonyl; when R 4a is lower alkyl, R 1a and R 3 are hydrogen, W 1 and W 2 are oxygen and Xb is lower alkoxycarbonyl or hydroxymethyl; when Xb is formyl or -CH=N-R 12 , R 1a , R 3 , R 4a , W 1 and W 2 are all hydrogen; when Xb is hydroxymethyl, R 1a and R3 are hydrogen and W 1 and W 2 are oxygen; when Xb and Yb are combined together to form, as -Xb-Yb-, R 14a -CH 2 -NH-CS-0- or -CH 2 -N=C-O-, R 1a , R 3 , R 4a , W 1 and W 2 are all hydrogen; and the combinations wherein R 1a , R 3 , R 4a , W 1 and W 2 are all hydrogen and Xb is lower alkoxycarbonyl are excluded]. (Inventors: Group B)

Claim 6

Dependent Claim 371 words

A K-252 derivative represented by formula (Ib) and a pharmacologically acceptable salt thereof: [wherein R la represents hydrogen, methyl, hydroxymethyl, bromine, hydroxy, lower alkoxy or -NR 5 R 6 (wherein either R S or R 6 is hydrogen and the other is hydrogen, carbamoyl or lower alkylaminocarbonyl, or both are lower alkyl) and R 3 is hydrogen, or R 1a and R 3 are the same and represent hydroxy, lower alkoxy or amino; R 4a is hydrogen, chlorine, carbamoyl or lower alkyl; W 1 and W 2 are hydrogen or both are combined together to represent oxygen; Xb is formyl, hydroxymethyl, lower alkoxycarbonyl, -CH=N-R 12 (wherein R 12 is hydroxy, amino, guanidino or 2-imidazolylamino), and Yb is hydroxy or carbamoyloxy, or Xb and Yb are combined together to form, as -Xb-Yb-, -CH 2 -NH-CS-O- or R l4 a -CH2-N=C-O- (wherein R 14a is lower alkylthio); with the proviso that: when W 1 and W 2 are oxygen, both R 1a and R 3 are hydrogen, Xb is lower alkoxycarbonyl or hydroxymethyl, R 4a is hydrogen or lower alkyl and Yb is hydroxy; when Yb is carbamoyloxy, R 1a , R 3 , W 1 and W 2 are all hydrogen, R 4a is carbamoyl and Xb is lower alkoxycarbonyl; when R 4a is chlorine, R 1a , R 3 , W 1 and W 2 are all hydrogen and Xb is lower alkoxycarbonyl; when R 4a is lower alkyl, R 1a and R 3 are hydrogen, W 1 and W 2 are oxygen and Xb is lower alkoxycarbonyl or hydroxymethyl; when Xb is formyl or -CH=N-R 12 , R 1a , R 3 , R 4a , W 1 and W 2 are all hydrogen; when Xb is hydroxymethyl, R 1a and R3 are hydrogen and W 1 and W 2 are oxygen; when Xb and Yb are combined together to form, as -Xb-Yb-, R 14a -CH 2 -NH-CS-0- or -CH 2 -N=C-O-, R 1a , R 3 , R 4a , W 1 and W 2 are all hydrogen; and the combinations wherein R 1a , R 3 , R 4a , W 1 and W 2 are all hydrogen and Xb is lower alkoxycarbonyl are excluded]. (Inventors: Group B)

Claim 7

Dependent Claim 723 words

A K-252 derivative represented by formula (Ic) and a pharmacologically acceptable salt thereof: wherein R 1b represents hydrogen, methyl, hydroxy, chlorine, hydroxymethyl, lower alkoxy, bromine or -N R S R 6 (wherein either R 5 or R 6 is hydrogen and the other is hydrogen, carbamoyl or lower alkylaminocarbonyl, or both are lower alkyl) and R 3a is hydrogen, or R1b and R 3a are the same and represent hydroxy, lower alkoxy or amino; R is hydrogen or amino; R 4b is hydrogen, amino or -CH 2 CH 2 R 7 (wherein R 7 is bromine, amino, di-lower alkylamino, hydroxy or hydroxy-substituted lower alkylamino); W 1 and W 2 are hydrogen or both are combined together to represent oxygen; Xc is hydrogen, lower alkoxycarbonyl, hydroxyaminocarbonyl or CH 2 Ad {wherein Ad-is hydroxy, [wherein either R 10b or R 11b is hydrogen and the other is hydrogen, allyl, carboxylic acid-substituted lower alkyl, dihydroxy-substituted lower alkyl, a residue of an a-amino acid in which the hydroxy of the carboxylic acid is removed or lower alkoxycarbonyl-substituted lower alkyl; or both are chlorine-substituted lower alkyl; or R 10b and R 11b are combined together to form -CH 2 CH 2 -BA-CH 2 CH 2 - (wherein Ba is -CH 2 -, -NH- or -S-)], -N= C H-NMe 2 , -OCOCH 2 CH 2 CO 2 H or Yc is hydroxy; or Xc and Yc are combined together to form, as -Xc-Yc-, -CH 2 -NR 13c- CO-O- [wherein R 13c is lower alkyl, allyl, formylmethyl, -CH 2 CH(OH)-CH 2 OH, (wherein R 14b is lower alkyl); with the proviso that: when W 1 and W 2 are oxygen, R 1b, R 2 and R 3a are all hydrogen; when R 4b is amino or -CH 2 CH 2 R 7 , W 1 and W 2 are oxygen; when R 1b is methyl, hydroxy, hydroxymethyl, lower alkoxy, bromine or -NR 5 R 6 , R 2 and R 4b are hydrogen and Xc is hydroxymethyl; when R 1b is chlorine, R and R 4b are hydrogen and Xc is lower alkoxycarbonyl or hydroxymethyl; when R 2 is amino, R 1b and R 4b are hydrogen and Xc is lower alkoxycarbonyl or hydroxymethyl; when Xc is hydrogen or CH 2 Ae (wherein the Ae representation is the same as the above Ad representation excluding hydroxy and amino), R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are all hydrogen; when Xc is hydroxyaminocarbonyl, R 1b , R 2 , R 3a and R 4b are all hydrogen and W 1 and W 2 are oxygen; when Xc is lower alkoxycarbonyl and W 1 and W 2 are oxygen, R 4b is -CH 2 CH 2 R 7a (wherein R 7a is bromine or di-lower alkylamino); when Xc is aminomethyl, R 1b , R 2 and R 3a are hydrogen, W 1 and W 2 are oxygen and R 4b is hydrogen or amino; when Xc is hydroxymethyl and W 1 and W 2 are oxygen, R 4b is amino or -CH 2 CH 2 R 7 ; when Xc and Yc are combined together to represent, as -Xc-Yc-, -CH 2 -NR 13d- CO-O- (wherein the R 13d representation is the same as the above R 13c representation excluding lower alkyl) or R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are all hydrogen; when Xc and Yc are combined together to represent, as -Xc-Yc-, -CH 2 -N R 13e- CO-O- (wherein R 13e is lower alkyl), R 1b , R 2 , R 3a and R 4b are hydrogen and W 1 and W 2 are oxygen; and the combinations wherein R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are hydrogen, Xc is methoxycarbonyl and Yc is hydroxy and the combinations wherein R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are hydrogen, Xc is hydroxymethyl and Yc is hydroxy are removed. (Inventors: Group C) Inventors: Group A - Tadashi Hirata, Mitsuru Takahashi, Chikara Murakata, Hiroshi Kase, Koji Yamada, Kazuyuki Iwahashi Group B - inventors of Group A and Kenichi Mochida Group C - Chikara Murakata, Akira Sato, Mitsuru Takahashi, Eiji Kobayashi, Makoto Morimoto, Shiro Akinaga

Claim 8

Dependent Claim 723 words

A K-252 derivative represented by formula (Ic) and a pharmacologically acceptable salt thereof: wherein R 1b represents hydrogen, methyl, hydroxy, chlorine, hydroxymethyl, lower alkoxy, bromine or -N R S R 6 (wherein either R 5 or R 6 is hydrogen and the other is hydrogen, carbamoyl or lower alkylaminocarbonyl, or both are lower alkyl) and R 3a is hydrogen, or R1b and R 3a are the same and represent hydroxy, lower alkoxy or amino; R is hydrogen or amino; R 4b is hydrogen, amino or -CH 2 CH 2 R 7 (wherein R 7 is bromine, amino, di-lower alkylamino, hydroxy or hydroxy-substituted lower alkylamino); W 1 and W 2 are hydrogen or both are combined together to represent oxygen; Xc is hydrogen, lower alkoxycarbonyl, hydroxyaminocarbonyl or CH 2 Ad {wherein Ad-is hydroxy, [wherein either R 10b or R 11b is hydrogen and the other is hydrogen, allyl, carboxylic acid-substituted lower alkyl, dihydroxy-substituted lower alkyl, a residue of an a-amino acid in which the hydroxy of the carboxylic acid is removed or lower alkoxycarbonyl-substituted lower alkyl; or both are chlorine-substituted lower alkyl; or R 10b and R 11b are combined together to form -CH 2 CH 2 -BA-CH 2 CH 2 - (wherein Ba is -CH 2 -, -NH- or -S-)], -N= C H-NMe 2 , -OCOCH 2 CH 2 CO 2 H or Yc is hydroxy; or Xc and Yc are combined together to form, as -Xc-Yc-, -CH 2 -NR 13c- CO-O- [wherein R 13c is lower alkyl, allyl, formylmethyl, -CH 2 CH(OH)-CH 2 OH, (wherein R 14b is lower alkyl); with the proviso that: when W 1 and W 2 are oxygen, R 1b, R 2 and R 3a are all hydrogen; when R 4b is amino or -CH 2 CH 2 R 7 , W 1 and W 2 are oxygen; when R 1b is methyl, hydroxy, hydroxymethyl, lower alkoxy, bromine or -NR 5 R 6 , R 2 and R 4b are hydrogen and Xc is hydroxymethyl; when R 1b is chlorine, R and R 4b are hydrogen and Xc is lower alkoxycarbonyl or hydroxymethyl; when R 2 is amino, R 1b and R 4b are hydrogen and Xc is lower alkoxycarbonyl or hydroxymethyl; when Xc is hydrogen or CH 2 Ae (wherein the Ae representation is the same as the above Ad representation excluding hydroxy and amino), R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are all hydrogen; when Xc is hydroxyaminocarbonyl, R 1b , R 2 , R 3a and R 4b are all hydrogen and W 1 and W 2 are oxygen; when Xc is lower alkoxycarbonyl and W 1 and W 2 are oxygen, R 4b is -CH 2 CH 2 R 7a (wherein R 7a is bromine or di-lower alkylamino); when Xc is aminomethyl, R 1b , R 2 and R 3a are hydrogen, W 1 and W 2 are oxygen and R 4b is hydrogen or amino; when Xc is hydroxymethyl and W 1 and W 2 are oxygen, R 4b is amino or -CH 2 CH 2 R 7 ; when Xc and Yc are combined together to represent, as -Xc-Yc-, -CH 2 -NR 13d- CO-O- (wherein the R 13d representation is the same as the above R 13c representation excluding lower alkyl) or R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are all hydrogen; when Xc and Yc are combined together to represent, as -Xc-Yc-, -CH 2 -N R 13e- CO-O- (wherein R 13e is lower alkyl), R 1b , R 2 , R 3a and R 4b are hydrogen and W 1 and W 2 are oxygen; and the combinations wherein R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are hydrogen, Xc is methoxycarbonyl and Yc is hydroxy and the combinations wherein R 1b , R 2 , R 3a , R 4b , W 1 and W 2 are hydrogen, Xc is hydroxymethyl and Yc is hydroxy are removed. (Inventors: Group C) Inventors: Group A - Tadashi Hirata, Mitsuru Takahashi, Chikara Murakata, Hiroshi Kase, Koji Yamada, Kazuyuki Iwahashi Group B - inventors of Group A and Kenichi Mochida Group C - Chikara Murakata, Akira Sato, Mitsuru Takahashi, Eiji Kobayashi, Makoto Morimoto, Shiro Akinaga

Derivatives of physiologically active substance k-252

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