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1. 发明专利

JP2006056894A Substituted isoquinoline-3-carboxamide, method for producing the same, and use of the same as pharmaceutical 有权
标题翻译：取代的异喹啉-3-羧酰胺，其生产方法及其作为药物的用途
公开(公告)号：JP2006056894A
公开(公告)日：2006-03-02
申请号：JP2005254578
申请日：2005-09-02
申请人： Fibrogen Inc , ファイブロゲンインコーポレイテッドFibrogen,Inc.
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG , WERNER ULRICH DR
IPC分类号： C07D217/26 , A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P43/00 , C07K5/078
CPC分类号： C07K5/06139 , A61K38/00 , C07D217/26
摘要： PROBLEM TO BE SOLVED: To provide a new isoquinoline-3-carboxamide expressed by formula I and its physiologically active salt. SOLUTION: This isoquinoline-3-carboxamide is produced by reaction of a corresponding quinoline-2-carboxylic acid with an aminocarboxylic acid ester and other processes. The produced compound is useful as a strong prolyl-4-hydroxylase inhibitor which does not cause steatosis. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供由式I表示的新的异喹啉-3-甲酰胺及其生理活性盐。解决方案：通过相应的喹啉-2-羧酸与氨基羧酸酯的反应和其它方法制备该异喹啉-3-甲酰胺。所产生的化合物可用作不引起脂肪变性的强脯氨酰-4-羟化酶抑制剂。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

ES2328156T3 AMIDAS DE ACIDO ISOQUINOLIN-3-CARBOXILICO SUSTITUIDAS, SU PREPARACION Y SU USO COMO MEDICAMENTOS. 未知
公开(公告)号：ES2328156T3
公开(公告)日：2009-11-10
申请号：ES05004047
申请日：1998-10-16
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , WERNER ULRICH DR
IPC分类号： C07K5/078 , A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P11/00 , A61P15/00 , A61P17/00 , A61P43/00 , C07D217/26
摘要： Compuestos de la fórmula Ia ** ver fórmula** en que significan R 1 hidrógeno o cloro, R 2 alquilo (C1-C8), alcoxi (C1-C8), cloro, trifluorometilo, hidroxi o benciloxi, que eventualmente está sustituido con sustituyentes de la serie alquilo (C1-C5), alcoxi (C1-C5), o fluoroalcoxi de la fórmula -O - [CH2]x- CfH(2f+1-g)Fg, con x = 0 ó 1, f = 1-5 y g = 1 a (2f+1), R 3 hidrógeno, alquilo (C1-C8), alcoxi (C1-C8), flúor, cloro, ciano, trifluorometilo, hidroxi o benciloxi, que eventualmente está sustituido con sustituyentes de la serie alquilo (C1-C5), alcoxi (C1-C5), o fluoroalcoxi de la fórmula -O - [CH2]x - CfH(2f+1-g)Fg, en donde x, f y g están definidos como antes, R 4 y R 5 hidrógeno, alquilo (C1-C5), flúor, cloro, bromo, trifluorometilo, ciano, alcoxi (C1-C5) o fluoroalcoxi de la fórmula -O- [CH2]x - CfH(2f+1-g)Fg, en donde x, f y g están definidos como antes, incluidas las sales fisiológicamente eficaces.

3. 发明专利

ES2245471T3 AMIDAS DE ACIDO ISOQUINOLIN-3-CARBOXILICO SUSTITUIDAS, SU PREPARACION Y SU USO COMO MEDICAMENTOS. 未知
公开(公告)号：ES2245471T3
公开(公告)日：2006-01-01
申请号：ES98119591
申请日：1998-10-16
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , WERNER ULRICH DR
IPC分类号： A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P11/00 , A61P15/00 , A61P17/00 , A61P43/00 , C07D217/26 , C07K5/078
摘要： NUEVAS AMIDAS DE ACIDOS ISOQUINOLIN - 3 - CARBOXILICOS DE FORMULA I EN LA CUAL R 1 ES HIDROGENO O CLORO, R 2 ES HIDROGENO, ALQUILO, ALCOXI, CLORO, TRIFLUOROMETILO, HIDROXI O BENCILOXI, EL CUAL PUEDE ESTAR OPCIONALMENTE SUSTITUIDO, O FLUOROALCOXI DE FORMULA O - [CH 2 ] X C F H (2F+ 1-G) F G , SIENDO X = 0 Y 1, F =1 - 5 Y G = 1 HASTA (2F+1), R 3 ES HIDROGENO, ALQUILO, ALCOXI, FLUOR, CLORO, CIANO, TRIFLUOROMETILO, HIDROXI O BENCILOXI, QUE PUEDE ESTAR OPCIONALMENTE SUSTITUIDO, O FLUOROALCOXI DE LA FORMULA ANTERIOR, R SUP,4 Y R 5 SON HIDROGENO, ALQUILO, FLUOR, CLORO, BROMO, TR IFLUOROMETILO, CIANO, ALCOXI O FLUOROALCOXI DE LA FORMULA ANTERIOR, INCLUYE LAS SALES FISIOLOGICAMENTE ACEPTABLES; SON INHIBIDORES POTENTES DE LA PROLIL - 4 - HIDROXILASA, QUE NO CAUSAN ESTEATOSIS.

4. 发明专利

DE59814365D1 未知
公开(公告)号：DE59814365D1
公开(公告)日：2009-07-16
申请号：DE59814365
申请日：1998-10-16
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , WERNER ULRICH DR
IPC分类号： C07K5/078 , A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P11/00 , A61P15/00 , A61P17/00 , A61P43/00 , C07D217/26
摘要： N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives (I) are new. N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives of formula (I) and their salts are new. [Image] A : COOH or CH 2OH; R 1>H or Cl; R 2>H, 1-8C alkyl, 1-8C alkoxy, Cl, CF 3, OH, benzyloxy (optionally substituted by 1-5C alkyl or 1-5C alkoxy) or fluoroalkoxy of formula -O(CH 2) x-Q; x : 0 or 1; Q : 1-5C alkyl, substituted by 1-11 F; R 3>F, CN or as for R 2>; and R 4>, R 5>H, 1-5C alkyl, F, Cl, Br, CF 3, CN, 1-5C alkoxy or -O(CH 2) x-Q. Independent claims are included for the preparation of (I). ACTIVITY : Antiinflammatory; Hepatotropic; Nephrotropic; Dermatological; Vulnerary; Antiarteriosclerotic. In a carbon tetrachloride-induced liver fibrosis model in the rat, N-((1-chloro-4-hydroxy-isoquinolin-3-yl)-carbonyl)-glycine (Ia) at a dose of 2 x 20 mg/kg i.p. per day for 2 weeks inhibited the production of hydroxyproline (as a indicator of collagen production) in the liver by 67%. (Ia) caused no steatosis of the liver when administered to rats at 2 x 25 mg/kg i.p. for 6 weeks. MECHANISM OF ACTION : Prolyl-4-hydroxylase inhibitor; Collagen biosynthesis inhibitor.

5. 发明专利

DK0911340T3 未知
公开(公告)号：DK0911340T3
公开(公告)日：2005-11-07
申请号：DK98119591
申请日：1998-10-16
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , WERNER ULRICH DR
IPC分类号： A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P11/00 , A61P15/00 , A61P17/00 , A61P43/00 , C07D217/26 , C07K5/078
摘要： N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives (I) are new. N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives of formula (I) and their salts are new. [Image] A : COOH or CH 2OH; R 1>H or Cl; R 2>H, 1-8C alkyl, 1-8C alkoxy, Cl, CF 3, OH, benzyloxy (optionally substituted by 1-5C alkyl or 1-5C alkoxy) or fluoroalkoxy of formula -O(CH 2) x-Q; x : 0 or 1; Q : 1-5C alkyl, substituted by 1-11 F; R 3>F, CN or as for R 2>; and R 4>, R 5>H, 1-5C alkyl, F, Cl, Br, CF 3, CN, 1-5C alkoxy or -O(CH 2) x-Q. Independent claims are included for the preparation of (I). ACTIVITY : Antiinflammatory; Hepatotropic; Nephrotropic; Dermatological; Vulnerary; Antiarteriosclerotic. In a carbon tetrachloride-induced liver fibrosis model in the rat, N-((1-chloro-4-hydroxy-isoquinolin-3-yl)-carbonyl)-glycine (Ia) at a dose of 2 x 20 mg/kg i.p. per day for 2 weeks inhibited the production of hydroxyproline (as a indicator of collagen production) in the liver by 67%. (Ia) caused no steatosis of the liver when administered to rats at 2 x 25 mg/kg i.p. for 6 weeks. MECHANISM OF ACTION : Prolyl-4-hydroxylase inhibitor; Collagen biosynthesis inhibitor.

6. 发明专利

AT263155T 未知
公开(公告)号：AT263155T
公开(公告)日：2004-04-15
申请号：AT96115110
申请日：1996-09-20
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , BICKEL MARTIN DR
IPC分类号： A61K31/47 , A61P1/16 , A61P11/00 , A61P17/00 , A61P37/00 , A61P43/00 , C07D215/16 , C07D215/48 , C07D215/60 , C07K5/078
摘要： 3-Hydroxyquinoline-2-carboxamide derivs. (I) and their salts are new. A =1-4C alkylene (opt. mono- or disubstd. by V, 1-6C hydroxyalkyl, Ph, benzyl, OPh, benzyloxy, anilino, N-methylanilino, SPh, SOPh or SO2Ph; or opt. monosubstd. by 6-12C aryl, 6-12C aryloxy, 7-11C aralkyl or 7-11C aralkoxy (all opt. mono- to penta- substd. by V, OCF2Cl or O-CF2-CHFCl); or 1 or more Rx); V = halo, CN, NO2, CF3, 1-6C alkyl, 1-6C alkoxy, -O-(CH2)x-CfH(2f+1-g)Halg, 1-6C alkylthio, 1-6C alkylsulphinyl, 1-6C alkylsulphonyl, 1-6C alkylcarbonyl, 1-6C alkoxycarbonyl, CONH2 (opt. mono- or disubstd. by 1-4C alkyl), 1-6C alkylcarbonyloxy, 3-8C cycloalkyl or SO2NH2 (opt. mono- or disubstd. by 1-4C alkyl); B = COOH, CONHCOR''', CONHSOR''', CONHSO2R''', NHSO2CF3, tetrazolyl, imidazolyl or 3-hydroxyisoxazolyl; R''' = aryl, heteroaryl, 3-7C cycloalkyl or 1-4C alkyl, opt. monosubstd. by 6-12C aryl, heteroaryl, OH, SH, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, alkylsulphinyl or alkylsulphonyl, CF3, Cl, Br, F, I, NO2, COOH, 2-5C alkoxycarbonyl, mono- or di- (1-4C alkyl)amino or 1-4C perfluoroalkyl; R1-R5 =H, OH, halo, CN, CF3, NO2, COOH, V', OV', 1-12C alkyl or alkoxy (both substd. by 3-8C cycloalkyl, 3-8C cycloalkoxy or 1-20C alkoxy), 3-8C cycloalkyl-1-8C alkyl-1-6C alkoxy, 7-16C aralkenyl; 7-16C aralkynyl, retinyloxy, 1-12C alkoxy-1-12C alkyl, 1-12C alkoxy-1-8C alkoxy-1-8C alkyl, OV', 1-6C alkoxy (substd. by 6-12C aryloxy or 7-16C aralkoxy), 1-16C hydroxyalkyl, 1-8C alkyl (substd. by 6-16C aryloxy or 7-16C aralkoxy), 1-6C alkyl (substd. by OCyc-substd. 1-8C alkoxy, 1-12C alkyl-thio, -sulphinyl, -sulphonyl, 6-12C arylthio, etc., -O-(CH2)x-CfH(2f+1-g)Halg, 1-6C chlorofluoroalkoxy, COV', COCyc, cinnamoyl, COOV', COOCyc, OCOV", OCOCyc, cinnamoyloxy, OCOOV', OCOOCyc, CONH2 (opt. mono- or disubstd., by 1-12C alkyl or by 3-8C cycloalkyl), CONE, COÄNRq-CHRx-COÜs-T, carbamoyloxy (opt. mono- or disubstd. by 1-12C alkyl), OCONHCyc, NRyRz, 1-8C alkyl (substd. by 1-12C alkanoylamino, etc.), 1-20C alkyl-thio, -sulphinyl, -sulphonyl, 6-12C arylthio, etc.; or 2 adjacent gps. of R1-R5 form 3-5C n-alkylene or n-alkenylene (opt. with 1 or 2 CH2 replaced by O, S, SO, SO2 or NR'); V' = 1-20 C alkyl, 2-20C alkenyl or 2-20C alkynyl; V" = 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl; Cyc = 3-8C cycloalkyl, 6-12C aryl or 7-16C aralkyl; E = 3-7C n-alkylene (opt. with one CH2 replaced by O, S, 1-8C alkylimino, N(Cyc), 3-8C cycloalkyl-1-12C alkylimino or 1-12C alkoxy-1-6C alkylimino); Rx = L- or D- alpha -amino acid substit.; T = OH, OR, or NRqRq; Rq = independently H, 6-12C aryl, 7-11C aralkyl, 1-8C alkyl, 3-8C cycloalkyl, (+)-dehydroabietyl, 1-8C alkyl (substd. by 1-8C alkoxy, 7-12C aralkoxy or 6-12C aryloxy), 1-10C alkanoyl, opt. substd. 7-16C aralkanoyl or opt. substd. 6-12C aroyl; or Rq+Rq = 3-7C n-alkylene (opt. with one CH2 replaced by O, S, SO, SO2, N-acylimino, etc.); R' = H, 6-12C aryl, 1-8C alkyl (opt. substd. by 1-8C alkoxy, 7-12C aralkoxy or 6-12C aryloxy), 1-10C alkanoyl, opt. substd. 7-16C aralkanoyl or opt. substd. 6-12C aroyl; Ry, Rz = V", 1-12C alkoxy, 3-8C cycloalkyl, 6-12C aryl, 7-11C aralkyl, 7-12C aralkoxy, 1-12C alkanoyl, 3-8C cycloalkanoyl, 6-12C aroyl or 7-16C aralkanoyl; or Ry+Rz = 3-6C n-alkylene, opt. with 1 CH2 replaced by O, S, N-(1-4C alkyl)carbonylimino or N-(1-4C alkoxy)carbonylimino; f = 1-8; g = 0 - (2f+1); m = 0 or 1; s = 1-5; x = 0-3; aryl gps. are all opt. substd., (where two of the substits. may be fused to form a CH2 chain (opt. with a CH2 replaced by O, S, SO, SO2 or NR') or CH=CH-CH=CH).

7. 发明专利

DK1538160T3 未知
公开(公告)号：DK1538160T3
公开(公告)日：2009-10-05
申请号：DK05004047
申请日：1998-10-16
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , WERNER ULRICH DR
IPC分类号： C07K5/078 , A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P11/00 , A61P15/00 , A61P17/00 , A61P43/00 , C07D217/26
摘要： N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives (I) are new. N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives of formula (I) and their salts are new. [Image] A : COOH or CH 2OH; R 1>H or Cl; R 2>H, 1-8C alkyl, 1-8C alkoxy, Cl, CF 3, OH, benzyloxy (optionally substituted by 1-5C alkyl or 1-5C alkoxy) or fluoroalkoxy of formula -O(CH 2) x-Q; x : 0 or 1; Q : 1-5C alkyl, substituted by 1-11 F; R 3>F, CN or as for R 2>; and R 4>, R 5>H, 1-5C alkyl, F, Cl, Br, CF 3, CN, 1-5C alkoxy or -O(CH 2) x-Q. Independent claims are included for the preparation of (I). ACTIVITY : Antiinflammatory; Hepatotropic; Nephrotropic; Dermatological; Vulnerary; Antiarteriosclerotic. In a carbon tetrachloride-induced liver fibrosis model in the rat, N-((1-chloro-4-hydroxy-isoquinolin-3-yl)-carbonyl)-glycine (Ia) at a dose of 2 x 20 mg/kg i.p. per day for 2 weeks inhibited the production of hydroxyproline (as a indicator of collagen production) in the liver by 67%. (Ia) caused no steatosis of the liver when administered to rats at 2 x 25 mg/kg i.p. for 6 weeks. MECHANISM OF ACTION : Prolyl-4-hydroxylase inhibitor; Collagen biosynthesis inhibitor.

8. 发明专利

AT299148T 未知
公开(公告)号：AT299148T
公开(公告)日：2005-07-15
申请号：AT98119591
申请日：1998-10-16
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , WERNER ULRICH DR
IPC分类号： A61K31/00 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/05 , A61P1/00 , A61P1/16 , A61P11/00 , A61P15/00 , A61P17/00 , A61P43/00 , C07D217/26 , C07K5/078
摘要： N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives (I) are new. N-(Carboxymethyl or 2-hydroxyethyl)-4-hydroxy-isoquinoline-3-carboxamide derivatives of formula (I) and their salts are new. [Image] A : COOH or CH 2OH; R 1>H or Cl; R 2>H, 1-8C alkyl, 1-8C alkoxy, Cl, CF 3, OH, benzyloxy (optionally substituted by 1-5C alkyl or 1-5C alkoxy) or fluoroalkoxy of formula -O(CH 2) x-Q; x : 0 or 1; Q : 1-5C alkyl, substituted by 1-11 F; R 3>F, CN or as for R 2>; and R 4>, R 5>H, 1-5C alkyl, F, Cl, Br, CF 3, CN, 1-5C alkoxy or -O(CH 2) x-Q. Independent claims are included for the preparation of (I). ACTIVITY : Antiinflammatory; Hepatotropic; Nephrotropic; Dermatological; Vulnerary; Antiarteriosclerotic. In a carbon tetrachloride-induced liver fibrosis model in the rat, N-((1-chloro-4-hydroxy-isoquinolin-3-yl)-carbonyl)-glycine (Ia) at a dose of 2 x 20 mg/kg i.p. per day for 2 weeks inhibited the production of hydroxyproline (as a indicator of collagen production) in the liver by 67%. (Ia) caused no steatosis of the liver when administered to rats at 2 x 25 mg/kg i.p. for 6 weeks. MECHANISM OF ACTION : Prolyl-4-hydroxylase inhibitor; Collagen biosynthesis inhibitor.

9. 发明专利

ES2215184T3 未知
公开(公告)号：ES2215184T3
公开(公告)日：2004-10-01
申请号：ES96115110
申请日：1996-09-20
申请人： FIBROGEN INC
发明人： WEIDMANN KLAUS DR , BARINGHAUS KARL-HEINZ DR , TSCHANK GEORG DR , BICKEL MARTIN DR
IPC分类号： A61K31/47 , A61P1/16 , A61P11/00 , A61P17/00 , A61P37/00 , A61P43/00 , C07D215/16 , C07D215/48 , C07D215/60 , C07K5/078
摘要： 3-Hydroxyquinoline-2-carboxamide derivs. (I) and their salts are new. A =1-4C alkylene (opt. mono- or disubstd. by V, 1-6C hydroxyalkyl, Ph, benzyl, OPh, benzyloxy, anilino, N-methylanilino, SPh, SOPh or SO2Ph; or opt. monosubstd. by 6-12C aryl, 6-12C aryloxy, 7-11C aralkyl or 7-11C aralkoxy (all opt. mono- to penta- substd. by V, OCF2Cl or O-CF2-CHFCl); or 1 or more Rx); V = halo, CN, NO2, CF3, 1-6C alkyl, 1-6C alkoxy, -O-(CH2)x-CfH(2f+1-g)Halg, 1-6C alkylthio, 1-6C alkylsulphinyl, 1-6C alkylsulphonyl, 1-6C alkylcarbonyl, 1-6C alkoxycarbonyl, CONH2 (opt. mono- or disubstd. by 1-4C alkyl), 1-6C alkylcarbonyloxy, 3-8C cycloalkyl or SO2NH2 (opt. mono- or disubstd. by 1-4C alkyl); B = COOH, CONHCOR''', CONHSOR''', CONHSO2R''', NHSO2CF3, tetrazolyl, imidazolyl or 3-hydroxyisoxazolyl; R''' = aryl, heteroaryl, 3-7C cycloalkyl or 1-4C alkyl, opt. monosubstd. by 6-12C aryl, heteroaryl, OH, SH, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, alkylsulphinyl or alkylsulphonyl, CF3, Cl, Br, F, I, NO2, COOH, 2-5C alkoxycarbonyl, mono- or di- (1-4C alkyl)amino or 1-4C perfluoroalkyl; R1-R5 =H, OH, halo, CN, CF3, NO2, COOH, V', OV', 1-12C alkyl or alkoxy (both substd. by 3-8C cycloalkyl, 3-8C cycloalkoxy or 1-20C alkoxy), 3-8C cycloalkyl-1-8C alkyl-1-6C alkoxy, 7-16C aralkenyl; 7-16C aralkynyl, retinyloxy, 1-12C alkoxy-1-12C alkyl, 1-12C alkoxy-1-8C alkoxy-1-8C alkyl, OV', 1-6C alkoxy (substd. by 6-12C aryloxy or 7-16C aralkoxy), 1-16C hydroxyalkyl, 1-8C alkyl (substd. by 6-16C aryloxy or 7-16C aralkoxy), 1-6C alkyl (substd. by OCyc-substd. 1-8C alkoxy, 1-12C alkyl-thio, -sulphinyl, -sulphonyl, 6-12C arylthio, etc., -O-(CH2)x-CfH(2f+1-g)Halg, 1-6C chlorofluoroalkoxy, COV', COCyc, cinnamoyl, COOV', COOCyc, OCOV", OCOCyc, cinnamoyloxy, OCOOV', OCOOCyc, CONH2 (opt. mono- or disubstd., by 1-12C alkyl or by 3-8C cycloalkyl), CONE, COÄNRq-CHRx-COÜs-T, carbamoyloxy (opt. mono- or disubstd. by 1-12C alkyl), OCONHCyc, NRyRz, 1-8C alkyl (substd. by 1-12C alkanoylamino, etc.), 1-20C alkyl-thio, -sulphinyl, -sulphonyl, 6-12C arylthio, etc.; or 2 adjacent gps. of R1-R5 form 3-5C n-alkylene or n-alkenylene (opt. with 1 or 2 CH2 replaced by O, S, SO, SO2 or NR'); V' = 1-20 C alkyl, 2-20C alkenyl or 2-20C alkynyl; V" = 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl; Cyc = 3-8C cycloalkyl, 6-12C aryl or 7-16C aralkyl; E = 3-7C n-alkylene (opt. with one CH2 replaced by O, S, 1-8C alkylimino, N(Cyc), 3-8C cycloalkyl-1-12C alkylimino or 1-12C alkoxy-1-6C alkylimino); Rx = L- or D- alpha -amino acid substit.; T = OH, OR, or NRqRq; Rq = independently H, 6-12C aryl, 7-11C aralkyl, 1-8C alkyl, 3-8C cycloalkyl, (+)-dehydroabietyl, 1-8C alkyl (substd. by 1-8C alkoxy, 7-12C aralkoxy or 6-12C aryloxy), 1-10C alkanoyl, opt. substd. 7-16C aralkanoyl or opt. substd. 6-12C aroyl; or Rq+Rq = 3-7C n-alkylene (opt. with one CH2 replaced by O, S, SO, SO2, N-acylimino, etc.); R' = H, 6-12C aryl, 1-8C alkyl (opt. substd. by 1-8C alkoxy, 7-12C aralkoxy or 6-12C aryloxy), 1-10C alkanoyl, opt. substd. 7-16C aralkanoyl or opt. substd. 6-12C aroyl; Ry, Rz = V", 1-12C alkoxy, 3-8C cycloalkyl, 6-12C aryl, 7-11C aralkyl, 7-12C aralkoxy, 1-12C alkanoyl, 3-8C cycloalkanoyl, 6-12C aroyl or 7-16C aralkanoyl; or Ry+Rz = 3-6C n-alkylene, opt. with 1 CH2 replaced by O, S, N-(1-4C alkyl)carbonylimino or N-(1-4C alkoxy)carbonylimino; f = 1-8; g = 0 - (2f+1); m = 0 or 1; s = 1-5; x = 0-3; aryl gps. are all opt. substd., (where two of the substits. may be fused to form a CH2 chain (opt. with a CH2 replaced by O, S, SO, SO2 or NR') or CH=CH-CH=CH).

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