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1. 发明申请

WO0242265A3 CYANOGUANIDINE PRODRUGS 审中-公开
公开(公告)号：WO0242265A3
公开(公告)日：2002-08-15
申请号：PCT/DK0100750
申请日：2001-11-14
申请人： LEO PHARMA AS , BINDERUP ERNST TORNDAL , HJARNAA PERNILL-JULIA VIG
发明人： BINDERUP ERNST TORNDAL , HJARNAA PERNILL-JULIA VIG
IPC分类号： A61K31/196 , A61K31/198 , A61K31/282 , A61K31/337 , A61K31/4422 , A61K31/4425 , A61K31/475 , A61K31/513 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/84 , C07D213/50 , C07D213/74 , C07D213/75 , C07D217/22 , A61K31/44
CPC分类号： C07D213/75 , C07D211/84 , C07D213/50 , C07D217/22
摘要： The invention relates to compounds of formula (I), wherein X1 and X2 independently represent a bond; a straight, branched and/or cyclic hydrocarbon diradical, optionally substituted with one or more hydroxy, halogen, nitro, amino, cyano, aminosulfonyl, alkylsulfonylamino, alkylcarbonyl, formyl, aminocarbonyl or alkylcarbonylamino; a heteroarylene or non-aromatic heterocyclic hydrocarbon diradical, all of which are optionally substituted with one or more straight, branched and/or cyclic non-aromatic hycrocarbon radical, hydroxyl, halogen, amino, nitro, cyano, aminosulfonyl, alkylsulfonylamino, alkylcarbonyl, formyl, aminocarbonyl or alkylcarbonylamino; Y1 and Y2 independently represent a bond, an ether diradical (R'-O-R''), an amine diradical (R'-N-R''), O, S, S(O), S(O)2, C(O), NH-CO, CO-NH, SO2-N(R'), methylene or N(R')-SO2 wherein R' et R'' independently represent straight or branched hydrocarbon diradicals containing up to 4 carbon atoms; Y3 represents O, O-C(O), C(O)-O, N(R8), R8 being hydrogen or C1-4alkyl; R1 represents hydrogen or straight, branched and/or cyclic alkyl, optionally substituted with phenyl; or an aromatic hydrocarbon radical; R2 represents aryl, heteroaryl or a non-aromatic heterocyclic hydrocarbon radical, all of which are optionally substituted; tetrahydropyranyloxy, di-(C1-4 alkoxy)phosphinoyloxy or C1-4 alkoxycarbonylamino; R3 represents hydrogen; a straight, branched and/or cyclic hydrocarbon radical, optionally substituted with one or more amino, hydroxy, carboxy, halogen, nitro, cyano, alcoxy, aminocarbonyl, C1-4alkoxycarbonyl, C1-4alkoxycarbonylamino, sulfo, hydroxysulfonyloxy, dihydroxyphosphinoyloxy, phosphono, sulfamino, aminosulfonyl, aminoacylamino or dialkoxyphosphinoyl; heteroaryl or a non-aromatic heterocyclic hydrocarbon radical, all of which are optionally substituted with one or more straight, branched and/or cyclic hydrocarbon radical, amino, hydroxy, carboxy, halogen, nitro, cyano, alkoxy, aminocarbonyl, C1-4alkoxycarbonyl, C1-4alkoxycarbonylamino, sulfo, hydroxysulfonyloxy, dihydroxyphosphinoyloxy, phosphono, sulfamino, aminosulfonyl, aminoacylamino or dialkoxyphosphinoyl; (a) wherein s is an integer from 1 to 200; R6 is hydrogen or an optionally substituted non-aromatic hydrocarbon radical; R7 Is independently hydrogen or methyl; R4 and R5 Independently represent hydrogen; a straight, branched and/or cyclic hydrocarbon radical, optionally substituted with halogen, hydroxyl, halogen, amino, nitro or cyano; A represents hydrogen, an optionally substituted, straight, branched and/or cyclic hydrocarbon radical, hydroxy, halogen, nitro, cyano, heteroaryl, heteroaralkyl or thiol; m and r are independently integers from 0 to 4; and n is 0 or 1; Z- is a pharmaceutically acceptable anion, such as chloride, bromide, iodide, sulfate, methanesulfonate, p-toluenesulfonate, nitrate or phosphate. The compounds are well suited as prodrugs in human and veterinary therapy.
摘要翻译：本发明涉及式（I）化合物，其中X 1和X 2独立地表示键; 任选被一个或多个羟基，卤素，硝基，氨基，氰基，氨基磺酰基，烷基磺酰基氨基，烷基羰基，甲酰基，氨基羰基或烷基羰基氨基取代的直链，支链和/ 所有这些都可以被一个或多个直链，支链和/或环状的非芳族羟基羰基，羟基，卤素，氨基，硝基，氰基，氨基磺酰基，烷基磺酰基氨基，烷基羰基，甲酰基，氨基羰基或烷基羰基氨基; Y1和Y2独立地表示键，醚二价（R'-O-R“），胺二价（R'-N-R”），O，S，S（O），S（O）2 ，C（O），NH-CO，CO-NH，SO2-N（R'），亚甲基或N（R'） - SO 2，其中R'和R'独立地表示含有至多4个碳的直链或支链烃基原子; Y 3表示O，O-C（O），C（O）-O，N（R 8），R 8为氢或C 1-4烷基; R 1表示氢或任选被苯基取代的直链，支链和/或环状烷基; 或芳族烃基; R 2表示芳基，杂芳基或非芳族杂环烃基，所有这些都是任选取代的; 二（C 1-4烷氧基）膦酰氧基或C 1-4烷氧基羰基氨基; R3表示氢; 任选被一个或多个氨基，羟基，羧基，卤素，硝基，氰基，烷氧基，氨基羰基，C 1-4烷氧基羰基，C 1-4烷氧基羰基氨基，磺基，羟基磺酰氧基，二羟基亚磷酰基氧基，膦酰基，磺基氨基取代的直链，支链和/或环状烃基氨基磺酰基，氨基酰氨基或二烷氧基膦酰基; 杂芳基或非芳族杂环烃基，它们全部被一个或多个直链，支链和/或环状烃基，氨基，羟基，羧基，卤素，硝基，氰基，烷氧基，氨基羰基，C 1-4烷氧基羰基， C 1-4烷氧基羰基氨基，磺基，羟基磺酰氧基，二羟基磷酰氧基，膦酰基，磺氨基，氨基磺酰基，氨基酰氨基或二烷氧基膦酰基; （a）其中s是1至200的整数; R6是氢或任选取代的非芳族烃基; R7独立地是氢或甲基; R4和R5独立代表氢; 任选被卤素，羟基，卤素，氨基，硝基或氰基取代的直链，支链和/或环状烃基; A表示氢，任选取代的直链，支链和/或环状烃基，羟基，卤素，硝基，氰基，杂芳基，杂芳烷基或硫醇; m和r独立地为0至4的整数; 并且n为0或1; Z-是药学上可接受的阴离子，例如氯化物，溴化物，碘化物，硫酸盐，甲磺酸盐，对甲苯磺酸盐，硝酸盐或磷酸盐。该化合物在人和兽医治疗中非常适合作为前药。

3. 发明专利

CA2426601C CYANOGUANIDINE PRODRUGS 未知
公开(公告)号：CA2426601C
公开(公告)日：2015-01-13
申请号：CA2426601
申请日：2001-11-14
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL , HJARNAA PERNILLE-JULIA VIG
IPC分类号： C07D213/75 , A61K31/196 , A61K31/198 , A61K31/282 , A61K31/337 , A61K31/44 , A61K31/4422 , A61K31/4425 , A61K31/475 , A61K31/513 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/84 , C07D213/50 , C07D213/74 , C07D217/22
摘要： The invention relates to compounds of formula (I), wherein X1 and X2 independently represent a bond; a straight, branched and/or cyclic hydrocarbon diradical, optionally substituted with one or more hydroxy, halogen, nitro, amino, cyano, aminosulfonyl, alkylsulfonylamino, alkylcarbonyl, formyl, aminocarbonyl or alkylcarbonylamino; a heteroarylene or non-aromatic heterocyclic hydrocarbon diradical, all of which are optionally substituted with one or more straight, branched and/or cyclic non-aromatic hycrocarbon radical, hydroxyl, halogen, amino, nitro, cyano, aminosulfonyl, alkylsulfonylamino, alkylcarbonyl, formyl, aminocarbonyl or alkylcarbonylamino; Y1 and Y2 independently represent a bond, an ether diradical (R'-O-R''), an amine diradical (R'-N-R''), O, S, S(O), S(O)2, C(O), NH-CO, CO-NH, SO2-N(R'), methylene or N(R')-SO2 wherein R' et R'' independently represent straight or branched hydrocarbon diradicals containing up to 4 carbon atoms; Y3 represents O, O-C(O), C(O)-O, N(R8), R8 being hydrogen or C1-4alkyl; R1 represents hydrogen or straight, branched and/or cyclic alkyl, optionally substituted with phenyl; or an aromatic hydrocarbon radical; R2 represents aryl, heteroaryl or a non-aromatic heterocyclic hydrocarbon radical, all of which are optionally substituted; tetrahydropyranyloxy, di-(C1-4 alkoxy)phosphinoyloxy or C1-4 alkoxycarbonylamino; R3 represents hydrogen; a straight, branched and/or cyclic hydrocarbon radical, optionally substituted with one or more amino, hydroxy, carboxy, halogen, nitro, cyano, alcoxy, aminocarbonyl, C1-4alkoxycarbonyl, C1-4alkoxycarbonylamino, sulfo, hydroxysulfonyloxy, dihydroxyphosphinoyloxy, phosphono, sulfamino, aminosulfonyl, aminoacylamino or dialkoxyphosphinoyl; heteroaryl or a non-aromatic heterocyclic hydrocarbon radical, all of which are optionally substituted with one or more straight, branched and/or cyclic hydrocarbon radical, amino, hydroxy, carboxy, halogen, nitro, cyano, alkoxy, aminocarbonyl, C1-4alkoxycarbonyl, C1-4alkoxycarbonylamino, sulfo, hydroxysulfonyloxy, dihydroxyphosphinoyloxy, phosphono, sulfamino, aminosulfonyl, aminoacylamino or dialkoxyphosphinoyl; (a) wherein s is an integer from 1 to 200; R6 is hydrogen or an optionally substituted non-aromatic hydrocarbon radical; R7 Is independently hydrogen or methyl; R4 and R5 Independently represent hydrogen; a straight, branched and/or cyclic hydrocarbon radical, optionally substituted with halogen, hydroxyl, halogen, amino, nitro or cyano; A represents hydrogen, an optionally substituted, straight, branched and/or cyclic hydrocarbon radical, hydroxy, halogen, nitro, cyano, heteroaryl, heteroaralkyl or thiol; m and r are independently integers from 0 to 4; and n is 0 or 1; Z- is a pharmaceutically acceptable anion, such as chloride, bromide, iodide, sulfate, methanesulfonate, p-toluenesulfonate, nitrate or phosphate. The compounds are well suited as prodrugs in human and veterinary therapy.

4. 发明专利

CA2572607C EPIMERISATION OF ALLYLIC ALCOHOLS 未知
公开(公告)号：CA2572607C
公开(公告)日：2010-06-01
申请号：CA2572607
申请日：2005-08-22
申请人： LEO PHARMA AS
发明人： PEDERSEN HENRIK , BRETTING CLAUS AAGE SVENSGAARD , BINDERUP ERNST TORNDAL
IPC分类号： C07C401/00 , A61K31/59
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 substituents is at the 24 position. The invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol (I) or calcipotriol monohydrate (I-hydrate) by said epimerization processes (see formula I), (see formula I-hydrate)

5. 发明专利

AU2003273781B2 Vitamin D analogues, compositions comprising said analogues and their use 未知
公开(公告)号：AU2003273781B2
公开(公告)日：2010-04-29
申请号：AU2003273781
申请日：2003-10-23
申请人： LEO PHARMA AS
发明人： BRETTING CLAUS AAGE SVENSGAARD , BINDERUP ERNST TORNDAL , HANSEN KAI HOLST , 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.

6. 发明专利

ES2290454T3 PROFARMACOS DE CIANOGUANIDINA. 未知
公开(公告)号：ES2290454T3
公开(公告)日：2008-02-16
申请号：ES03722311
申请日：2003-05-15
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL , DUVOLD TORE
IPC分类号： C07D211/22 , A61K31/196 , C07D213/02 , A61K31/198 , A61K31/282 , A61K31/337 , A61K31/4425 , A61K31/4545 , A61K31/475 , A61K31/513 , A61K31/593 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K45/00 , A61P1/04 , A61P1/16 , A61P7/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P35/02 , C07C271/16 , C07D211/62 , C07D213/75 , C07D401/12
摘要： Un compuesto de acuerdo con la fórmula I en la que X1 es un radical divalente derivado de un hidrocarburo lineal, ramificado y/o cíclico, sustituido opcionalmente con uno o más sustituyentes seleccionados de hidroxi, halógeno, nitro, amino o ciano; X2 es un enlace; un radical divalente derivado de un hidrocarburo lineal, ramificado y/o cíclico, sustituido opcionalmente con uno o más sustituyentes seleccionados de hidroxi, halógeno, nitro, amino, ciano, aminosulfonilo, alquilsulfonilamino, alquilcarbonilo, formilo, aminocarbonilo o alquilcarbonilamino; un heteroarileno o un radical divalente derivado de un hidrocarburo heterocíclico no aromático, todos ellos sustituidos opcionalmente con uno o más sustituyentes seleccionados de radical divalente de un hidrocarburo no aromático lineal, ramificado y/o cíclico, hidroxilo, halógeno, amino, nitro, ciano, aminosulfonilo, alquilsulfonilamino, alquilcarbonilo, formilo, aminocarbonilo o alquilcarbonilamino; X3 es un radical divalente derivado de un hidrocarburo lineal, ramificado y/o cíclico, sustituido opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, halógeno, nitro, amino, ciano, aminosulfonilo, alquilsulfonilamino, alquilcarbonilo, formilo, aminocarbonilo o alquilcarbonilamino, con la condición de que cuando n es cero, X3 puede ser también un enlace; Y1 es un enlace, O, S, S(O), S(O)2, C(O), NH-C(O) o C(O)-NH; Y2 es un enlace, un radical éter divalente (R''-O-R''''), un radical amino divalente (R''-N-R''''), O, S, S(O), S(O)2, C(O), NH-C(O), C(O)-NH, SO2-N(R'') o N(R'')-SO2, en los que R'' y R'''' son independientemente radicales divalentes derivados de un hidrocarburo lineal o ramificado que contiene hasta 4 átomos de carbono.

7. 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.

8. 发明专利

CA2485351A1 CYANOGUANIDINE PRODRUGS 未知
公开(公告)号：CA2485351A1
公开(公告)日：2003-11-27
申请号：CA2485351
申请日：2003-05-15
申请人： LEO PHARMA AS
发明人： DUVOLD TORE , BINDERUP ERNST TORNDAL
IPC分类号： C07D211/22 , A61K31/196 , A61K31/198 , A61K31/282 , A61K31/337 , A61K31/4425 , A61K31/4545 , A61K31/475 , A61K31/513 , A61K31/593 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K45/00 , A61P1/04 , A61P1/16 , A61P7/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P35/02 , C07C271/16 , C07D211/62 , C07D213/02 , C07D213/75 , C07D401/12
摘要： Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseas es such as cancers.

9. 发明专利

CA2484671A1 CYANOGUANIDINE PRODRUGS 未知
公开(公告)号：CA2484671A1
公开(公告)日：2003-11-27
申请号：CA2484671
申请日：2003-05-15
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL
IPC分类号： C07D213/02 , A61K31/4425 , A61K31/444 , A61K45/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D213/75 , C07D401/12
摘要： Pyridyl cyanoguanidine compounds according to formula I wherein A, R1, R2, R 5, 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 diseas e such as cancers.

10. 发明专利

AU1494702A Cyanoguanidine prodrugs 未知
公开(公告)号：AU1494702A
公开(公告)日：2002-06-03
申请号：AU1494702
申请日：2001-11-12
申请人： LEO PHARMA AS
发明人： BINDERUP ERNST TORNDAL , HJARNAA PERNILL-JULIA VIG
IPC分类号： A61K31/196 , A61K31/198 , A61K31/282 , A61K31/337 , A61K31/4422 , A61K31/4425 , A61K31/475 , A61K31/513 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/84 , C07D213/50 , C07D213/74 , C07D213/75 , C07D217/22
摘要： The invention relates to compounds formula I or formula II wherein R 1 -R 5 , X 1 -X 2 , Y 1 -Y 3 , A, Z - , n, m and r are as defined herein. The compounds are well suited as prodrugs in human and veterinary therapy.

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