公开号/公开日

EP0627406 A1 1994-12-07 [EP-627406]EP0627406 A4 1995-04-12 [EP-627406]EP0627406 B1 1998-10-28 [EP-627406] / 1994-12-071995-04-121998-10-28

申请号/申请日

1993EP-0923035 / 1993-10-18

发明人

FUJITA TETSURO;SASAKI SHIGEO;YONETA MASAHIKO;MISHINA TADASHI;ADACHI KUNITOMO;CHIBA KENJI;

申请人

YOSHITOMI PHARMACEUTICAL;

主分类号

IPC分类号

A01N-033/02A01N-043/40A01N-043/60A01N-057/00C07C-215/10C07C-215/18C07C-215/20C07C-215/24C07C-215/26C07C-215/28C07C-215/34C07C-215/42C07C-215/54C07C-215/56C07C-215/68C07C-217/28C07C-217/30C07C-217/34C07C-217/48C07C-217/52C07C-217/64C07

摘要

(EP-627406) A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient.  In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R<2>, R<3>, R<4> and R<5>, which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl.  The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields. <CHEM>

机翻摘要

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地址

代理人

代理机构

;

优先权号

1992JP-0283281 1992-10-21 1993JP-0179427 1993-07-20 1993WO-JP01515 1993-10-18

主权利要求

(EP-627406)  1. A 2-amino-1,3-propanediol compound of the formula (see diagramm 1 page 448) wherein R is an optionally substituted straight- or branched carbons chain which may have, in the chain, a bond, a hetero atom or a group selected from the group consisting of a double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, carbonyl, optionally substituted arylene, optionally substituted cycloalkylene, optionally substituted heteroarylene and an alicycle thereof, and which may be substituted, at the chain end thereof, by a double bond, a triple bond, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heteroaryl or an alicycle thereof;  an optionally substituted aryl, an optionally substituted cycloalkyl, an optionally substituted heteroaryl or an alicycle thereof;  and R**2, R**3, R**4 and R**5   are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, or R**4 and R**5 may be bonded to form an alkylene chain which may be substituted by alkyl, aryl or aralkyl;   wherein the optionally substituted straight- or branched carbon chain may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxyimino, hydroxy, carboxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted cycloalkyl, optionally substituted heteroaryl and an alicycle thereof;  the aforementioned optionally substituted arylene, optionally substituted cycloalkylene, optionally substituted heteroarylene and an alicycle thereof may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxy and carboxy;  and the optionally substituted aryl, optionally substituted aryloxy, optionally substituted cycloalkyl, optionally substituted heteroaryl and an alicycle thereof may have a substituent selected from the group consisting of alkyl, alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxy and carboxy;   provided that when R is C1-C5 alkyl, the alkyl should be  substituted and when R is furylmethyl, phenylmethyl or phenylmethyl substituted by lower alkyl, lower alkoxy, chloro, hydroxy or amino, one of R**2 and R**3 is not methyl or ethyl;  or a pharmaceutically acceptable salt thereof.  2. A 2-amino-1,3-propanediol compound of Claim 1, having the formula (see diagramm 1 page 450) wherein R**1 is an optionally substituted straight- or branched carbon chain which may have, in the chain, a bond, a hetero atom or a group selected from the group consisting of a double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, carbonyl, optionally substituted arylene, optionally substituted cycloalkylene, optionally substituted heteroarylene and an alicycle thereof, and which may be substituted, at the chain end (omega -position) thereof, by a double bond, a triple bond, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heteroaryl or an alicycle thereof;  an optionally substituted aryl, an optionally substituted cycloalkyl, an optionally substituted heteroaryl or an alicycle thereof;  and R**2, R**3, R**4 and R**5    are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, or R**4 and R**5 may be bonded to form an alkylene chain which may be substituted by alkyl, aryl or aralkyl;  wherein the optionally substituted straight- or branched carbon chain may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxyimino, hydroxy, carboxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted cycloalkyl, optionally substituted heteroaryl and an alicycle thereof;  and the aforementioned optionally substituted arylene, optionally substituted cycloalkylene, optionally substituted heteroarylene, an alicycle thereof, optionally substituted aryl, optionally substituted aryloxy, optionally substituted cycloalkyl, optionally substituted heteroaryl and an alicycle thereof may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxy and carboxy;   provided that when R**1 is C1-C4 alkyl, the alkyl should be substituted and when R**1 is furyl, phenyl or phenyl substituted  by lower alkyl, lower alkoxy, chloro, hydroxy or amino, one of R**2 and R**3 is not methyl or ethyl;  or a pharmaceutically acceptable salt thereof.  3. A 2-amino-1,3-propanediol compound of Claim 1 or 2, having the formula (see diagramm 1 page 452) wherein R**1a is an optionally substituted straight- or branched carbon chain which may have, in the chain, a bond, a hetero atom or a group selected from the group consisting of a double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, carbonyl, optionally substituted phenylene and optionally substituted cycloalkylene;  an optionally substituted phenyl or an optionally substituted cycloalkyl;  and R**2a, R**3a, R**4a and R**5a   are the same or different and each is a hydrogen, an alkyl, an acyl or an alkoxycarbonyl;  wherein the optionally substituted phenyl and optionally substituted cycloalkyl may have a substituent selected from the group consisting of optionally substituted straight- or branched carbon chain which may have, in the chain, a bond, a hetero atom or a group selected from the group consisting of a  double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, carbonyl, optionally substituted phenylene and optionally substituted cycloalkylene;  alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, nitro, halogen, amino, hydroxy, carboxy, optionally substituted phenyl, optionally substituted phenoxy and optionally substituted cycloalkyl;  the optionally substituted carbon chain may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, nitro, halogen, amino, hydroxy, carboxy, optionally substituted phenyl, optionally substituted phenoxy and optionally substituted cycloalkyl;  and the aforementioned optionally substituted phenylene, optionally substituted cycloalkylene, optionally substituted phenyl, optionally substituted phenoxy and optionally substituted cycloalkyl may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, nitro, halogen, amino, hydroxy and carboxy;   provided that when R**1a is C1-C4 alkyl, the alkyl should be substituted and when R**1a is furyl, phenyl or phenyl substituted  by lower alkyl, lower alkoxy, chloro, hydroxy or amino, one of R**2a and R**3a is not methyl or ethyl;  or a pharmaceutically acceptable salt thereof.  4. A 2-amino-1,3-propanediol compound of Claim 3, having the formula (see diagramm 1 page 454) wherein R**1b is an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted phenyl or an optionally substituted cycloalkyl, and R**2b, R**3b, R**4b and R**5b   are the same or different and each is a hydrogen, an alkyl or an acyl;  wherein the optionally substituted alkyl, optionally substituted alkenyl and optionally substituted alkynyl may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxy, carboxy, optionally substituted phenyl and optionally substituted cycloalkyl;  and the aforementioned optionally substituted phenyl and optionally substituted cycloalkyl may have 1 to 3 substituents selected from the group consisting of  alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, nitro, halogen, amino, hydroxy and carboxy;  provided that when R**1b is C1-C4 alkyl, the alkyl should be substituted and when R**1b is furyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, chloro, hydroxy or amino, one of R**2b and R**3b is not methyl or ethyl;  or a pharmaceutically acceptable salt thereof.  5. A 2-amino-1,3-propanediol compound of any one of Claims 1, 2, 3 and 4, having the formula (see diagramm 1 page 455) wherein Ra is a straight- or branched chain alkyl having 12 to 22 carbon atoms, which may have, in the chain, a bond or a hetero atom selected from the group consisting of a double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, and carbonyl, and which may have, as a substituent, alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxyimino, hydroxy or carboxy, and  R**2b, R**3b, R**4b and R**5b   are the same or different and each is a hydrogen, an alkyl or an acyl;  or a pharmaceutically acceptable salt thereof.  6. A 2-amino-1,3-propanediol compound of Claim 5, having the formula (see diagramm 1 page 456) wherein Rb is a straight- or branched chain alkyl having 13 to 20 carbon atoms, which may have, in the chain, an oxygen atom and which may have, as a substituent, nitro, halogen, amino, hydroxy or carboxy, and R**2c and R**3c   are the same or different and each is a hydrogen or an alkyl, or a pharmaceutically acceptable salt thereof.  7. A 2-amino-1,3-propanediol compound of Claim 5 or 6, having the formula (see diagramm 2 page 456) wherein Rc is a straight- or branched chain alkyl having 13 to 20 carbon atoms or a straight- or branched chain alkyl having 13 to 20 carbon atoms which is substituted by  halogen, or a pharmaceutically acceptable salt thereof.  8. A 2-amino-1,3-propanediol compound of any one of Claims 5, 6 and 7, which is selected from the group consisting of  2-amino-2-tridecyl-1,3-propanediol,  2-amino-2-tetradecyl-1,3-propanediol,  2-amino-2-pentadecyl-1,3-propanediol,  2-amino-2-hexadecyl-1,3-propanediol,  2-amino-2-heptadecyl-1,3-propanediol,  2-amino-2-octadecyl-1,3-propanediol,  2-amino-2-nonadecyl-1,3-propanediol,  2-amino-2-icosyl-1,3-propanediol,  2-amino-2-(12-fluorododecyl)-1,3-propanediol and  2-amino-2-(14-fluorotetradecyl)-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  9. A 2-amino-1,3-propanediol compound of any one of Claims 1, 2, 3 and 4, having the formula (see diagramm 1 page 457) wherein Rd is a phenylalkyl, a substituted phenylalkyl, a cycloalkylalkyl, a substituted cycloalkylalkyl, a heteroarylalkyl, a substituted heteroarylalkyl, a heterocyclic alkyl or a substituted heterocyclic alkyl, wherein the alkyl moiety may have, in the carbon chain, a bond or a hetero atom selected from the group consisting of a double  bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, and carbonyl, and may have, as a substituent, alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxy or carboxy;  and the substituted phenylalkyl, substituted cycloalkylalkyl, substituted heteroarylalkyl and substituted heterocyclic alkyl may have a substituent selected from the group consisting of alkyl, alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, haloaralkyloxy, aralkyloxyalkyl, phenoxyalkyl, phenoxyalkoxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxy and carboxy;  or a pharmaceutically acceptable salt thereof.  10. A 2-amino-1,3-propanediol compound of Claim 9, having the formula (see diagramm 1 page 458) wherein Re is a phenylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms;  a phenylalkyl which may be substituted by a straight- or branched chain C6-C20 alkyl optionally substituted by  halogen, a straight- or branched chain C6-C20 alkoxy optionally substituted by halogen, a straight- or branched chain C6-C20 alkenyloxy, phenylalkoxy, halophenylalkoxy, phenylalkoxyalkyl, phenoxyalkoxy or phenoxyalkyl;  a cycloalkylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms;  a cycloalkylalkyl substituted by a straight- or branched chain alkyl having 6 to 20 carbon atoms;  a heteroarylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms;  a heteroarylalkyl substituted by a straight- or branched chain alkyl having 6 to 20 carbon atoms;  a heterocyclic alkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms, or a heterocyclic alkyl substituted by a straight- or branched chain alkyl having 6 to 20 carbon atoms;  wherein the alkyl moiety may have, in the carbon chain, a bond or a hetero atom selected from the group consisting of a double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, and carbonyl, and may have, as a substituent, alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxy or carboxy;  or a pharmaceutically acceptable salt thereof.  11. A 2-amino-1,3-propanediol compound of Claim 9 or 10, having  the formula (see diagramm 1 page 460) wherein Rf is a phenylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms which may have, in the carbon chain, one or two oxygen atoms;  a phenylalkyl which may be substituted by a straight- or branched chain C6-C20 alkyl optionally substituted by halogen, a straight- or branched chain C6-C20 alkoxy optionally substituted by halogen, a straight- or branched chain C6-C20 alkenyloxy, phenylalkoxy, halophenylalkoxy, phenylalkoxyalkyl, phenoxyalkoxy or phenoxyalkyl;  a cycloalkylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms which may have, in the carbon chain, one or two oxygen atoms;  a cycloalkylalkyl substituted by a straight- or branched chain alkyl having 6 to 20 carbon atoms;  a heteroarylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms which may have, in the carbon chain, one or two oxygen atoms;  a heteroarylalkyl substituted by a straight- or branched chain alkyl having 6 to 20 carbon atoms;  a heterocyclic alkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms  which may have, in the carbon chain, one or two oxygen atoms, or a heterocyclic alkyl substituted by a straight- or branched chain alkyl having 6 to 20 carbon atoms;  wherein the alkyl moiety may have, in the carbon chain, a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxy and carboxy;  or a pharmaceutically acceptable salt thereof.  12. A 2-amino-1,3-propanediol compound of any one of Claims 9, 10 and 11, having the formula (see diagramm 1 page 461) wherein Rg is a phenylalkyl wherein the alkyl moiety is a straight- or branched chain having 6 to 20 carbon atoms which may have, in the carbon chain, one or two oxygen atoms;  a phenylalkyl which may be substituted by a straight- or branched chain C6-C14 alkyl optionally substituted by halogen, a straight- or branched chain C6-C14 alkoxy optionally substituted by halogen, a straight- or branched chain C6-C14 alkenyloxy, phenylalkoxy, halophenylalkoxy, phenylalkoxyalkyl, phenoxyalkoxy or phenoxyalkyl;  a cycloalkylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms;  a cycloalkylalkyl substituted by  a straight- or branched chain alkyl having 6 to 14 carbon atoms;  a heteroarylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms;  a heteroarylalkyl substituted by a straight- or branched chain alkyl having 6 to 14 carbon atoms;  a heterocyclic alkyl wherein the alkyl moiety has 6 to 20 carbon atoms, or a heterocyclic alkyl substituted by a straight- or branched chain alkyl having 6 to 14 carbon atoms;  or a pharmaceutically acceptable salt thereof.  13. A 2-amino-1,3-propanediol compound of Claim 12, having the formula (see diagramm 1 page 462) wherein Rh is a phenylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms, a phenylalkoxyalkyl wherein the alkyl moiety and alkoxy moiety have 6 to 20 carbon atoms in total, a phenoxyalkyl wherein the alkyl moiety has 6 to 20 carbon atoms or a phenoxyalkoxyalkyl wherein the alkyl moiety and alkoxy moiety have 6 to 20 carbon atoms in total, or a pharmaceutically acceptable salt thereof.  14. A 2-amino-1,3-propanediol compound of Claim 13, which is selected from the group consisting of  2-amino-2-(8-phenyloctyl )-1,3-propanediol,  2-amino-2-(9-phenylnonyl)-1,3-propanediol,   2-amino-2-(10-phenyldecyl)-1,3-propanediol,  2-amino-2-(11-phenylundecyl)-1,3-propanediol,  2-amino-2-(12-phenyldodecyl)-1,3-propanediol,  2-amino-2-(13-phenyltridecyl)-1,3-propanediol,  2-amino-2-(14-phenyltetradecyl)-1,3-propanediol,  2-amino-2-(15-phenylpentadecyl)-1,3-propanediol,  2-amino-2-(16-phenylhexadecyl)-1,3-propanediol,  2-amino-2-[6-(8-phenyloctyloxy)hexyl]-1,3-propanediol,  2-amino-2-(8-phenylmethyloxyoctyl)-1,3-propanediol,  2-amino-2-(9-phenoxynonyl)-1,3-propanediol,  2-amino-2-(12-phenoxydodecyl)-1,3-propanediol and  2-amino-2-[6-(2-phenoxyethyloxy)hexyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  15. A 2-amino-1,3-propanediol compound of Claim 13, which is selected from the group consisting of  2-amino-2-(10-phenyldecyl)-1,3-propanediol,  2-amino-2-(13-phenyltridecyl)-1,3-propanediol,  2-amino-2-[6-(8-phenyloctyloxy)hexyl]-1,3-propanediol,  2-amino-2-(8-phenylmethyloxyoctyl)-1,3-propanediol,  2-amino-2-(9-phenoxynonyl)-1,3-propanediol,  2-Amino-2-(12-phenoxydodecyl)-1,3-propanediol and  2-amino-2-[6-(2-phenoxyethyloxy)hexyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  16. A 2-amino-1,3-propanediol compound of Claim 12, having the formula  (see diagramm 1 page 464) wherein Ri is a phenylalkyl substituted by a straight- or branched chain C6-C14 alkyl optionally substituted by halogen, a straight- or branched chain C6-C14 alkoxy optionally substituted by halogen or a straight- or branched chain C6-C14 alkenyloxy, wherein the alkyl moiety of phenylalkyl may be substituted by hydroxy, or a pharmaceutically acceptable salt thereof.  17. A 2-amino-1,3-propanediol compound of Claim 16, having the formula (see diagramm 2 page 464) wherein Rj is a phenylalkyl substituted by a straight- or branched chain C6-C14 alkyl optionally substituted by halogen, a straight- or branched chain C6-C14 alkoxy optionally substituted by halogen or a straight- or branched chain C6-C14 alkenyloxy, wherein the alkyl moiety is a C2-C6 alkyl optionally substituted by hydroxy, or a pharmaceutically acceptable salt thereof.  18. A 2-amino-1,3-propanediol compound of Claim 16 or 17, which is selected from the group consisting of   2-amino-2-[2-(4-heptylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-nonylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-decylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-undecylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-dodecylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-tridecylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-tetradecylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-hexyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-heptyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-octyloxyphenyl)ethyl)-1,3-propanediol,  2-amino-2-[2-(4-nonyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-decyloxyphenyl)ethyl]-1,3-propanediol,,  2-amino-2-[2-(4-undecyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-dodecyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-tridecyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(8-fluorooctyl)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(12-fluorododecyl)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(7-fluoroheptyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(11-fluoroundecyloxy)phenyl)ethyl]-1,3-propanediol and  2-amino-2-[2-(4-(7-octenyloxy)phenyl)ethyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  19. A 2-amino-1,3-propanediol compound of Claim 16 or 17, which is selected from the group consisting of  2-amino-2-[2-(4-heptylphenyl)ethyl]-1,3-propanediol,   2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-nonylphenyl)ethyl]-1,3-propanediol,  2amino-2-[2-(4-decylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-undecylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-dodecylphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-heptyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-octyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-nonyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-undecyloxyphenyl)ethyl]-1,3-propanediol and  2-amino-2-[2-(4-(7-octenyloxy)phenyl)ethyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  20. A 2-amino-1,3-propanediol compound of Claim 12, having the formula (see diagramm 1 page 466) wherein Rk is a phenylalkyl substituted by phenylalkoxy, halophenylalkoxy, phenylalkoxyalkyl, phenoxyalkoxy or phenoxyalkyl, or a pharmaceutically acceptable salt thereof.  21. A 2-amino-1,3-propanediol compound of Claim 20, having the formula (see diagramm 2 page 466) wherein  Rl is a phenylalkyl substituted by phenylalkoxy wherein the alkoxy moiety has 2 to 8 carbon atoms, halophenylalkoxy wherein the alkoxy moiety has 2 to 8 carbon atoms, phenylalkoxyalkyl wherein the alkoxy moiety and alkyl moiety have 2 to 8 carbon atoms in total, phenoxyalkoxy wherein the alkoxy moiety has 2 to 8 carbon atoms or phenoxyalkyl wherein the alkyl moiety has 2 to 8 carbon atoms, where the alkyl moiety has 2 to 6 carbon atoms, or a pharmaceutically acceptable salt thereof.  22. A 2-amino-1,3-propanediol compound of Claim 20 or 21, which is selected from the group consisting of  2-amino-2-[2-(4-phenylmethyloxyphenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(2-phenylethyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(3-phenylpropyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(4-phenylbutyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(5-phenylpentyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(6-phenylhexyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(7-phenylheptyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(8-phenyloctyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[4-(6-(4-fluorophenyl)hexyloxy)phenyl)ethyl]-1,3-propanediol, 2-amino-2-[2-(4-(5-phenylpentyloxymethyl)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(4-phenoxybutyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(5-phenoxypentyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(6-phenoxyhexyloxy)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(7-phenoxyheptyloxy)phenyl)ethyl]-1,3-propanediol,   2-amino-2-[2-(4-(4-phenoxybutyl)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(5-phenoxypentyl)phenyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-(6-phenoxyhexyl)phenyl))ethyl]-1,3-propanediol, and  2-amino-2-[2-(4-(7-phenoxyheptyl)phenyl)ethyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  23. A 2-amino-1,3-propanediol compound of Claim20 or 21, which is selected from the group consisting of 2-amino-2-[2-(4-(6-phenylhexyloxy)phenyl)ethyl]-1,3-propanediol and 2-amino-2-[2-(4-(5-phenylpentyloxymethyl)phenyl))ethyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  24. A 2-amino-1,3-propanediol compound of Claim 12, having the formula (see diagramm 1 page 468) wherein Rm is an alkyl-substituted cycloalkylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms in total, or a pharmaceutically acceptable salt thereof.  25. A 2-amino-1,3-propanediol compound of Claim 24, which is selected from the group consisting of  2-amino-2-[3-(4-heptylcyclohexyl)propyl]-1,3-propanediol,  2-amino-2-[4-(4-butylcyclohexyl)butyl]-1,3-propanediol,  2-amino-2-[2-(4-octylcyclohexyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(4-nonylcyclohexyl))ethyl]-1,3-propanediol and  2-amino-2-[2-(4-dodecylcyclohexyl))ethyl]-1,3-propanediol, or a  pharmaceutically acceptable salt thereof.  26. A 2-amino-1,3-propanediol compound of Claim 12, having the formula (see diagramm 1 page 469) wherein Rn is a 1-alkyl-substituted piperidin-4-ylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms in total, or a pharmaceutically acceptable salt thereof.  27. A 2-amino-1,3-propanediol compound of Claim 26, which is selected from the group consisting of 2-amino-2-[2-(1-octylpiperidin-4-yl)ethyl]-1,3-propanediol, and 2-amino-2-[2-(1-dodecylpiperidin-4-yl)ethyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  28. A 2-amino-1,3-propanediol compound of Claim 12, having the formula (see diagramm 2 page 469) wherein Ro is a thienylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms, an alkyl-substituted thienylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms in total, a pyridylalkyl wherein the alkyl moiety has 6 to 20 carbon atoms or an alkyl-substituted pyridylalkyl wherein the  alkyl moiety has 6 to 20 carbon atoms in total, or a pharmaceutically acceptable salt thereof.  29. A 2-amino-1,3-propanediol compound of Claim 28, which is selected from the group consisting of  2-amino-2-[2-(5-octyl-2-thienyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(5-nonyl-2-thienyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(5-decyl-2-thienyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(5-dodecyl-2-thienyl)ethyl]-1,3-propanediol,  2-amino-2-[13-(2-thienyl)tridecyl]-1,3-propanediol,  2-amino-2-[2-(5-octyl-2-pyridyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(5-decyl-2-pyridyl)ethyl]-1,3-propanediol,  2-amio-2-[13-(2-pyridyl)tridecyl]-1,3-propanediol,  2-amino-2-[2-(2-octyl-5-pyridyl)ethyl]-1,3-propanediol,  2-amino-2-[2-(2-decyl-5-pyridyl)ethyl]-1,3-propanediol and  2-amino-2-[13-(3-pyridyl)tridecyl]-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  30. A 2-amino-1,3-propanediol compound of Claim 1 or 2, having the formula (see diagramm 1 page 470) wherein Rp is a phenyl substituted by C6-C18 alkyl, a cycloalkyl, a heteroaryl or a heterocycle, or a pharmaceutically acceptable salt thereof.  31. A 2-amino-1,3-propanediol compound of Claim 30, having the  formula (see diagramm 1 page 471) wherein Rq is a phenyl substituted by C6-C18 alkyl, or a pharmaceutically acceptable salt thereof.  32. A 2-amino-1,3-propanediol compound of Claim 30 or 31, which is selected from the group consisting of  2-amino-2-(4-decylphenyl)-1,3-propanediol,  2-amino-2-(4-dodecylphenyl)-1,3-propanediol,  2-amino-2-(4-tetradecylphenyl)-1,3-propanediol and  2-amino-2-(4-hexadecylphenyl)-1,3-propanediol, or a pharmaceutically acceptable salt thereof.  33. A 2-amino-1,3-propanediol compound of Claim 1 or 2, having the formula (see diagramm 2 page 471) wherein R**1 is an optionally substituted straight- or branched carbon chain which may have, in the chain, a bond, a hetero atom or a group selected from the group consisting of a double bond, a triple bond, oxygen, sulfur, sulfinyl, sulfonyl, -N(R**6)- where R**6 is hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl, and carbonyl, optionally substituted  arylene, optionally substituted cycloalkylene, optionally substituted heteroarylene and an alicycle thereof, and which may be substituted, at the chain end (omega -position) thereof, by a double bond, a triple bond, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heteroaryl or an alicycle thereof, an optionally substituted aryl, an optionally substituted cycloalkyl, an optionally substituted heteroaryl or an alicycle thereof, and R**2a, R**3a, R**4a and R**5a   are the same or different and each is a hydrogen, an alkyl, an acyl or an alkoxycarbonyl;  wherein the optionally substituted straight- or branched carbon chain may have a substituent selected from the group consisting of alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, alkylenedioxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, haloalkyl, haloalkoxy, nitro, halogen, amino, hydroxyimino, hydroxy, carboxy, optionally substituted aryl, optionally substituted arylo(...)

法律状态

(EP-627406) LEGAL DETAILS FOR EP0627406  Actual or expected expiration date=2013-10-18    Legal state=DEAD    Status=EXPIRED     Event publication date=1993-10-18  Event code=EP/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=EP EP93923035  Application date=1993-10-18  Standardized application number=1993EP-0923035     Event publication date=1994-12-07  Event code=EP/A1  Event type=Examination events  Application published with search report  Publication country=EP  Publication number=EP0627406  Publication stage Code=A1  Publication date=1994-12-07  Standardized publication number=EP-627406     Event publication date=1994-12-07  Event code=EP/17P  Event indicator=Pos  Event type=Examination events  Request for examination filed Pruefungsantrag gestellt  Effective date of the event=1994-06-16     Event publication date=1994-12-07  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE    Event publication date=1995-04-12  Event code=EP/A4  Event indicator=Pos  Event type=Examination events  Supplementary search report Ergaenzender recherchenbericht  Publication country=EP  Publication number=EP0627406  Publication stage Code=A4  Publication date=1995-04-12  Standardized publication number=EP-627406     Event publication date=1995-04-12  Event code=EP/A4  Event indicator=Pos  Event type=Administrative notifications  Supplementary search report Despatch of supplementary search report    Event publication date=1995-04-12  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE    Event publication date=1996-09-11  Event code=EP/17Q  Event indicator=Pos  Event type=Examination events  First examination report Erster pruefungsbescheid  Effective date of the event=1996-07-30     Event publication date=1998-10-28  Event code=EP/B1  Event indicator=Pos  Event type=Event indicating In Force  Patent specification  Publication country=EP  Publication number=EP0627406  Publication stage Code=B1  Publication date=1998-10-28  Standardized publication number=EP-627406     Event publication date=1998-10-28  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE    Event publication date=1998-12-02  Event code=EP/K1C1  Event type=Corrections  Correction of patent application (title page) published  Effective date of the event=1994-12-07     Event publication date=1998-12-02  Event code=EP/RAP2  Event type=Change of name or address  Event type=Reassignment  Transfer of rights of an EP granted patent Patentinhaber uebertragung (korr.)    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