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21. 发明专利

SI1730108T1 Stereoselektivna sinteza analogov vitamina D 未知
公开(公告)号：SI1730108T1
公开(公告)日：2008-08-31
申请号：SI200530248
申请日：2005-03-10
申请人： LEO PHARMA AS
发明人： SABROE THOMAS PETER , CALVERLEY MARTIN JOHN
IPC分类号： C07C401/00 , C07B31/00 , C07D333/00 , C07D333/72

22. 发明专利

BRPI0507318A 未知
公开(公告)号：BRPI0507318A
公开(公告)日：2007-06-26
申请号：BRPI0507318
申请日：2005-03-10
申请人： LEO PHARMA AS
发明人： SABROE THOMAS PETER , CALVERLEY MARTIN JOHN
IPC分类号： C07C401/00 , C07B31/00 , C07D333/72
摘要： The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.

23. 发明专利

CA2561590A1 NOVEL METHOD FOR THE PREPARATION OF INTERMEDIATES USEFUL FORTHE SYNTHESIS OF VITAMIN D ANALOGUES 未知
公开(公告)号：CA2561590A1
公开(公告)日：2005-10-13
申请号：CA2561590
申请日：2005-03-23
申请人： LEO PHARMA AS
发明人： PEDERSEN HENRIK , CALVERLEY MARTIN JOHN , DEUSSEN HEINZ-JOSEF WILHELM , SABROE THOMAS PETER , HANSEN ERIK TORNGAARD
IPC分类号： C07C401/00 , C07B37/00
摘要： The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.

24. 发明专利

AU2003273781A1 VITAMIN D ANALOGUES, COMPOSITIONS COMPRISING SAID ANALOGUES AND THEIR USE 未知
公开(公告)号：AU2003273781A1
公开(公告)日：2004-05-13
申请号：AU2003273781
申请日：2003-10-23
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL , HANSEN KAI HOLST , BRETTING CLAUS AAGE SVENSGAARD , CALVERLEY MARTIN JOHN
IPC分类号： C07C401/00 , A61K31/59 , A61K31/593 , A61P5/20
摘要： Compounds according to formula I: in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6) hydrocarbyl, optionally substituted with one or two hydroxyl group on one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; the bond between C#16 and C#17 is depicted with a dotted line to illustrate that said bond may be either a single bond, in which case the projection of the ring substituents is beta, or a double bond; A represents hydroxyl, fluorine or hydrogen; B represents CH2 or H2; the configuration is the 3-position corresponds to the same configuration as in natural vitamine D3 (normal), or the configuration in the configuration in the 3-position is opposite to that of natural vitamin D3(epi); with the proviso that when X represents (E)-ethylene or (Z)-ethylene, one of R1 and R2 taken together with R3 may not form a direct bond, such that a triple bond is constituted; with the further proviso that when X represents a bond R1 ands R2 are nor hydrogen; with the further proviso that the compound of formula I is not 3(S)-hyroxy-9, 10-secocholesta-5(Z),7(E),10(19),22(E),24-penta-ene; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

25. 发明专利

MY139521A STEREOSELECTIVE SYNTHESIS OF VITAMIN D ANALOGUES 未知
公开(公告)号：MY139521A
公开(公告)日：2009-10-30
申请号：MYPI20050998
申请日：2005-03-10
申请人： LEO PHARMA AS
发明人： SABROE THOMAS PETER , CALVERLEY MARTIN JOHN
IPC分类号： C07C401/00
摘要： THE PRESENT INVENTION RELATES TO INTERMEDIATES USEFUL FOR THE SYNTHESIS OF CALCIPOTRIOL OR CALCIPOTRIOL MONOHYDRATE, TO METHODS OF PRODUCING SAID INTERMEDIATES, AND TO METHODS OF STEREOSELECTIVELY REDUCING SAID INTERMEDIATES.

26. 发明专利

CA2561590C NOVEL METHOD FOR THE PREPARATION OF INTERMEDIATES USEFUL FORTHE SYNTHESIS OF VITAMIN D ANALOGUES 未知
公开(公告)号：CA2561590C
公开(公告)日：2008-11-18
申请号：CA2561590
申请日：2005-03-23
申请人： LEO PHARMA AS
发明人： PEDERSEN HENRIK , DEUSSEN HEINZ-JOSEF WILHELM , CALVERLEY MARTIN JOHN , SABROE THOMAS PETER , HANSEN ERIK TORNGAARD
IPC分类号： C07F9/40 , C07B37/00 , C07C49/242 , C07C49/255 , C07C401/00 , C07D333/72
摘要： The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.

27. 发明专利

HK1098124A1 NOVEL METHOD FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE SYNTHESIS OF VITAMIN D ANALOGUES 未知
公开(公告)号：HK1098124A1
公开(公告)日：2007-07-13
申请号：HK07104323
申请日：2007-04-24
申请人： LEO PHARMA AS
发明人： HANSEN ERIK TORNGARD , SABROE THOMAS PETER , CALVERLEY MARTIN JOHN , PEDERSEN HENDRIK , DEUSSEN HEINZ-JOZEF WILHELM
IPC分类号： C07B37/00 , C07C20060101 , C07C401/00
摘要： The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.

28. 发明专利

MXPA06010824A METODO NOVEDOSO PARA LA PREPARACION DE INTERMEDIARIOS UTILES PARA LA SINTESIS DE ANALOGOS DE VITAMINA D. 未知
公开(公告)号：MXPA06010824A
公开(公告)日：2007-01-17
申请号：MXPA06010824
申请日：2005-03-23
申请人： LEO PHARMA AS
发明人： PEDERSEN HENRIK , CALVERLEY MARTIN JOHN , SABROE THOMAS PETER , HANSEN ERIK TORNGAARD , DEUSSEN HEINZ-JOSEF WILHELM
IPC分类号： C07C401/00 , C07B37/00
摘要： La presente invencion se relaciona con novedosos metodos para la preparacion de intermediarios que son utiles en la sintesis del calcipotriol. La presente invencion se relaciona asimismo con el uso de los intermediarios producidos con dichos metodos para la elaboracion del calcipotriol o calcipotriol monohidrato.

29. 发明专利

PL376148A1 VITAMIN D ANALOGUES, COMPOSITIONS COMPRISING SAID ANALOGUES AND THEIR USE 未知
公开(公告)号：PL376148A1
公开(公告)日：2005-12-27
申请号：PL37614803
申请日：2003-10-23
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL , HANSEN KAI HOLST , BRETTING CLAUS AAGE SVENSGAARD , CALVERLEY MARTIN JOHN
IPC分类号： C07C401/00 , A61K31/59 , A61K31/593 , A61P5/20 , C07D401/00
摘要： Compounds according to formula I: in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6) hydrocarbyl, optionally substituted with one or two hydroxyl group on one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; the bond between C#16 and C#17 is depicted with a dotted line to illustrate that said bond may be either a single bond, in which case the projection of the ring substituents is beta, or a double bond; A represents hydroxyl, fluorine or hydrogen; B represents CH2 or H2; the configuration is the 3-position corresponds to the same configuration as in natural vitamine D3 (normal), or the configuration in the configuration in the 3-position is opposite to that of natural vitamin D3(epi); with the proviso that when X represents (E)-ethylene or (Z)-ethylene, one of R1 and R2 taken together with R3 may not form a direct bond, such that a triple bond is constituted; with the further proviso that when X represents a bond R1 ands R2 are nor hydrogen; with the further proviso that the compound of formula I is not 3(S)-hyroxy-9, 10-secocholesta-5(Z),7(E),10(19),22(E),24-penta-ene; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

30. 发明专利

BR0315553A 未知
公开(公告)号：BR0315553A
公开(公告)日：2005-08-23
申请号：BR0315553
申请日：2003-10-23
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL , HANSEN KAI HOLST , BRETTING CLAUS AAGE SVENSGARD , CALVERLEY MARTIN JOHN
IPC分类号： C07C401/00 , A61K31/59 , A61K31/593 , A61P5/20
摘要： Compounds according to formula I: in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6) hydrocarbyl, optionally substituted with one or two hydroxyl group on one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; the bond between C#16 and C#17 is depicted with a dotted line to illustrate that said bond may be either a single bond, in which case the projection of the ring substituents is beta, or a double bond; A represents hydroxyl, fluorine or hydrogen; B represents CH2 or H2; the configuration is the 3-position corresponds to the same configuration as in natural vitamine D3 (normal), or the configuration in the configuration in the 3-position is opposite to that of natural vitamin D3(epi); with the proviso that when X represents (E)-ethylene or (Z)-ethylene, one of R1 and R2 taken together with R3 may not form a direct bond, such that a triple bond is constituted; with the further proviso that when X represents a bond R1 ands R2 are nor hydrogen; with the further proviso that the compound of formula I is not 3(S)-hyroxy-9, 10-secocholesta-5(Z),7(E),10(19),22(E),24-penta-ene; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

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