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1. 发明授权

EP1339686B1 CYANOGUANIDINE PRODRUGS 有权
标题翻译：双氰胺前体药物
公开(公告)号：EP1339686B1
公开(公告)日：2015-09-16
申请号：EP01983436.5
申请日：2001-11-14
申请人： LEO PHARMA A/S
发明人： BINDERUP, Ernst, Torndal , HJARNAA, Pernill-Julia, Vig
IPC分类号： C07D213/75 , A61K31/44 , A61P35/00
CPC分类号： C07D213/75 , C07D211/84 , C07D213/50 , C07D217/22

2. 发明公开

EP1507759A1 CYANOGUANIDINE PRODUGS 审中-公开
标题翻译：氰基胍产品
公开(公告)号：EP1507759A1
公开(公告)日：2005-02-23
申请号：EP03720293.4
申请日：2003-05-15
申请人： LEO PHARMA A/S
发明人： BINDERUP, Ernst, Torndal
IPC分类号： C07D213/02 , A61K31/4425 , A61P35/00
CPC分类号： C07D213/75
摘要： Pyridyl cyanoguanidine compounds according to formula I wherein A, R1, R2, R5, R6, X1, X2, X3, X4, Y1, Y2, Y3, Y4 and n are as indicated in the description are useful as produgs in human and veterinary therapy of poliferative disease such as cancers.
摘要翻译：其中A，R 1，R 2，R 5，R 6，X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和n如说明书中所示的吡啶基氰基胍化合物可用作人和兽医疗法诸如癌症之类的增殖性疾病。

3. 发明申请

WO2006024296A1 EPIMERISATION OF ALLYLIC ALCOHOLS 审中-公开
标题翻译：各种酒精的消除
公开(公告)号：WO2006024296A1
公开(公告)日：2006-03-09
申请号：PCT/DK2005/000533
申请日：2005-08-22
申请人： LEO PHARMA A/S , PEDERSEN, Henrik , BRETTING, Claus, Aage, Svensgaard , BINDERUP, Ernst, Torndal
发明人： PEDERSEN, Henrik , BRETTING, Claus, Aage, Svensgaard , BINDERUP, Ernst, Torndal
IPC分类号： C07C401/00 , C07J9/00
CPC分类号： C07J9/00 , C07C401/00 , C07C2601/02
摘要： The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituent is at the 24 position. The invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol by said epimerisation processes.
摘要翻译：本发明涉及在不对称烯丙基碳上具有羟基取代基的化合物的差向异构化方法，例如可用于合成维甲酸类似物的化合物，其中差向异构羟基取代基在24位。本发明还涉及通过所述差向异构化方法生产可用于合成卡泊三醇的中间体的方法。

4. 发明授权

EP1789384B1 EPIMERISATION OF ALLYLIC ALCOHOLS 失效
标题翻译： EPIMERISATION VON ALLYLALKOHOLEN
公开(公告)号：EP1789384B1
公开(公告)日：2008-10-15
申请号：EP05770141.9
申请日：2005-08-22
申请人： LEO PHARMA A/S
发明人： PEDERSEN, Henrik , BRETTING, Claus, Aage, Svensgaard , BINDERUP, Ernst, Torndal
IPC分类号： C07C401/00 , C07J9/00
CPC分类号： C07J9/00 , C07C401/00 , C07C2601/02
摘要： The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituent is at the 24 position. The invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol by said epimerisation processes.
摘要翻译：本发明涉及在不对称烯丙基碳上具有羟基取代基的化合物的差向异构化方法，例如可用于合成维甲酸类似物的化合物，其中差向异构羟基取代基位于24位。本发明还涉及通过所述差向异构化方法制备可用于合成卡泊三醇的中间体的方法。

5. 发明公开

EP1789384A1 EPIMERISATION OF ALLYLIC ALCOHOLS 失效
标题翻译：烯丙醇差向异构
公开(公告)号：EP1789384A1
公开(公告)日：2007-05-30
申请号：EP05770141.9
申请日：2005-08-22
申请人： LEO PHARMA A/S
发明人： PEDERSEN, Henrik , BRETTING, Claus, Aage, Svensgaard , BINDERUP, Ernst, Torndal
IPC分类号： C07C401/00 , C07J9/00
CPC分类号： C07J9/00 , C07C401/00 , C07C2601/02
摘要： The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituent is at the 24 position. The invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol by said epimerisation processes.

6. 发明公开

EP1255732A1 USE OF VITAMIN D-DERIVATIVES IN THE TREATMENT OF OSTEOPOROSIS AND RELATED BONE DISORDERS, AS WELL AS NOVEL VITAMIN D3-DERIVATIVES 审中-公开
标题翻译：维生素D衍生物在骨质疏松症和相关的骨疾病的治疗，随着新的维生素D3衍生物
公开(公告)号：EP1255732A1
公开(公告)日：2002-11-13
申请号：EP01948978.0
申请日：2001-01-31
申请人： Leo Pharma A/S
发明人： GRUE-SORENSEN, Gunnar , PEDERSEN, Henrik , BINDERUP, Ernst, Torndal , TRANHOLM, Mikael
IPC分类号： C07C401/00 , A61K31/593 , A61P19/10
CPC分类号： A61K31/593 , A61K31/59 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： Compounds of the formula (I) wherein X represents hydrogen or hydroxy; Y represents oxygen or sulphur or oxidized sulphur selected from the groups S(O) and S(O2); R?1 and R2¿, which may be the same or different, represent hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated, C¿1?-C6-hydrocarbon; or R?1 and R2, together with the carbon atom to which they are attached (marked with an asterisk in formula (I)), bearing the group X, form a C3-C8 carbocyclic ring; Q represents a diradical residue after removal of 2 hydrogen atoms from a straight, branched or cyclic, saturated or unsaturated C1-C8-hydrocarbon; R?3¿ represents hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated C¿1?-C6-hydrocarbon; R?1, R2¿ and/or Q is optionally substituted with one or more deuterium or fluorine atoms; and n is 0 or 1; and derivatives of the compounds of formula (I) in which one or more hydroxy groups have been transformed into -O-acyl or -O-glycosyl groups, or a phosphate ester, such masked groups being hydrolyzable in vivo; may be used for the preparation of a medicament for the treatment and/or prophylaxis of osteoporosis and related bone disorders.
摘要翻译：式I worin X darstellt氢或羟基的化合物; ÿdarstellt氧或硫或者选自基团S（O）和S（O _{2 ）选择氧化的硫; [R ^{1 和R ^{2 ，其可以是相同或不同，代表氢或选自直链，支链或环状，饱和或不饱和除去一个氢原子后的残基，C _{1 -C _{6 - 烃; 或R ^{1 和R ^{2 ，连同它们所连接的碳原子（标有上式中星号I）带有基团X，形成C < SUB> 3 -C _{8 碳环; Q darstellt双基残基，从直链，支链或环状，饱和或不饱和的C _{除去2个氢原子后1 -C _{8 - 烃; 且R ^{3 darstellt氢或选自直链，支链或环状，饱和或不饱和的C _{1 -C _{6 - 烃; 可用于制备用于治疗和/或预防骨质疏松症和相关骨疾病的药物的制备。}}}}}}}}}}}}}

7. 发明申请

WO2006105796A1 NOVEL INDOLINONE DERIVATIVES 审中-公开
标题翻译：新的吲哚啉酮衍生物
公开(公告)号：WO2006105796A1
公开(公告)日：2006-10-12
申请号：PCT/DK2006/000199
申请日：2006-04-07
申请人： LEO PHARMA A/S , DUVOLD, Laetitia, Maud, Elysa , HAVEZ, Sophie, Elisbeth , BINDERUP, Ernst, Torndal , ANDERSEN, Grith, Krøyer
发明人： DUVOLD, Laetitia, Maud, Elysa , HAVEZ, Sophie, Elisbeth , BINDERUP, Ernst, Torndal , ANDERSEN, Grith, Krøyer
IPC分类号： C07D209/34 , C07D401/14 , C07D401/12 , C07D405/14 , A61K31/40 , A61P29/00
CPC分类号： C07D401/14 , C07D209/34 , C07D401/12 , C07D405/14
摘要： The invention relates to novel indolinone derivatives of formula (I), wherein X, R1, R2, R3, R4, R5, Re, Ri', Ri , FV/ R4'/ FV and R6' are as shown herein, as well as their use in the treatment of inflammatory autoimmune diseases, in particular by administration via the oral route.
摘要翻译：本发明涉及式（I）的新的吲哚啉酮衍生物，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R'，R 1，R F，R 4'/ FV和R 6'如本文所示，它们用于治疗炎性自身免疫性疾病，特别是通过口服途径给药。

8. 发明申请

WO2003097602A1 CYANOGUANIDINE PRODUGS 审中-公开
公开(公告)号：WO2003097602A1
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000319
申请日：2003-05-15
申请人： LEO PHARMA A/S , BINDERUP, Ernst, Torndal
发明人： BINDERUP, Ernst, Torndal
IPC分类号： C07D213/02
CPC分类号： C07D213/75
摘要： Pyridyl cyanoguanidine compounds according to formula I wherein A, R 1 , R 2 , R 5 , R 6 , X 1 , X 2 , X 3 , X 4, Y 1 , Y 2 , Y 3 , Y 4 and n are as indicated in the description are useful as produgs in human and veterinary therapy of poliferative disease such as cancers.
摘要翻译：其中A，R 1，R 2，R 5，R 6，X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和n如说明书中所示的式I的吡啶基氰基胍化合物可用作人和兽医疗法的复发性疾病如癌症。

9. 发明申请

WO2004037781A1 VITAMIN D ANALOGUES, COMPOSITIONS COMPRISING SAID ANALOGUES AND THEIR USE 审中-公开
标题翻译：维生素D类似物，包含类似物的组合物及其用途
公开(公告)号：WO2004037781A1
公开(公告)日：2004-05-06
申请号：PCT/DK2003/000718
申请日：2003-10-23
申请人： LEO PHARMA A/S , BINDERUP, Ernst, Torndal , HANSEN, Kai, Holst , BRETTING, Claus, Aage, Svensgaard , CALVERLEY, Martin, John
发明人： BINDERUP, Ernst, Torndal , HANSEN, Kai, Holst , BRETTING, Claus, Aage, Svensgaard , CALVERLEY, Martin, John
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , A61K31/59 , A61K31/593
摘要： Compounds according to formula I: in which formula R1 and R2, which may be the same or different, represent halogen, (C 1 -C 6 ) 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 (C 3 -C 6 )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 (C 1 -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 CH 2 or H 2 ; the configuration is the 3-position corresponds to the same configuration as in natural vitamine D 3 (normal), or the configuration in the configuration in the 3-position is opposite to that of natural vitamin D 3 (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.
摘要翻译：根据式I的化合物：其中可以相同或不同的式R 1和R 2表示卤素，（C 1 -C 6）烃基，任选被一个或多个氟原子上的一个或两个羟基取代，或者与它们所连接的碳原子，R 1和R 2形成（C 3 -C 6）碳环，R 1和R 2中的一个与R 3一起形成直接键，从而构成三键或R1和R2 代表氢; 当不与R 1和R 2中的一个直接键合时，R 3表示氢或（C 1 -C 3）烃基; X表示（E） - 亚乙基，（Z） - 亚乙基，亚乙炔基或键; Y和Z独立地表示氢或甲基; 以虚线描绘C＃16和C＃17之间的键，以说明所述键可以是单键，在这种情况下，环取代基的投影为β或双键; A表示羟基，氟或氢; B表示CH 2或H 2; 该配置是与天然维生素D3（正常）相同的配置，或3位置的配置与天然维生素D3（epi）相反的配置; 条件是当X表示（E） - 亚乙基或（Z） - 亚乙基时，R 1和R 2中的一个与R 3一起可以不形成直接键，从而构成三键; 进一步的条件是当X表示键R1和R2不是氢时; 进一步的条件是式I化合物不是3（S） - 羟基-9,10-半胱胆甾-5（Z），7（E），10（19），22（E），24-戊烯 ; 并且其前体药物和立体异构形式与其在治疗中的用途一起提供，以及它们在制备药物中的用途。

10. 发明申请

WO2003097601A1 CYANOGUANIDINE PRODRUGS 审中-公开
公开(公告)号：WO2003097601A1
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000318
申请日：2003-05-15
申请人： LEO PHARMA A/S , BINDERUP, Ernst, Torndal , DUVOLD, Tore
发明人： BINDERUP, Ernst, Torndal , DUVOLD, Tore
IPC分类号： C07D213/02
CPC分类号： C07D213/75 , A61K31/444
摘要： Pyridyl cyanoguanidine compounds of the general formula I wherein A, X 1 , X 2 , X 3 , Y 1 , Y 2 , Y 3 , R 1 , R 2 , R 5 , R 6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.
摘要翻译：其中A，X 1，X 2，X 3，Y 1，Y 2，Y 3，R 1，R 2，R 5，R 6和n如说明书中所示的通式I的吡啶基氰基胍化合物适合作为增殖性疾病的人和兽医疗法中的前药如癌症。

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