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1. 发明专利

CA3048729C SUBSTITUTED BICYCLIC PYRIMIDINE-BASED COMPOUNDS AND COMPOSITIONS AND USES THEREOF 未知
公开(公告)号：CA3048729C
公开(公告)日：2023-01-03
申请号：CA3048729
申请日：2018-01-26
申请人： TSANTRIZOS YOULA S , SEBAG MICHAEL
发明人： TSANTRIZOS YOULA S , SEBAG MICHAEL
IPC分类号： C07F9/6561 , A61K31/675 , A61P35/00
摘要： Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as potent inhibitors of hGGPPS by inhibiting geranylgeranylation of proteins and inhibiting the biosynthesis of GGPP. The application is directed to these compounds, to compositions comprising these compounds, and to their use, in particular as medicaments for use in the treatment of cancer and other conditions which are treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.

2. 发明专利

CA3048729A1 SUBSTITUTED BICYCLIC PYRIMIDINE-BASED COMPOUNDS AND COMPOSITIONS AND USES THEREOF 未知
公开(公告)号：CA3048729A1
公开(公告)日：2018-08-02
申请号：CA3048729
申请日：2018-01-26
申请人： TSANTRIZOS YOULA S , SEBAG MICHAEL
发明人： TSANTRIZOS YOULA S , SEBAG MICHAEL
IPC分类号： C07F9/6561 , A61K31/675 , A61P35/00
摘要： Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as potent inhibitors of hGGPPS by inhibiting geranylgeranylation of proteins and inhibiting the biosynthesis of GGPP. The application is directed to these compounds, to compositions comprising these compounds, and to their use, in particular as medicaments for use in the treatment of cancer and other conditions which are treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.

3. 发明专利

CA2018161A1 BIOFUNGICIDAL COMPOSITION 未知
公开(公告)号：CA2018161A1
公开(公告)日：1990-12-05
申请号：CA2018161
申请日：1990-06-04
申请人： FORTIN J ANDRE , OGILVIE KELVIN K , TSANTRIZOS YOULA S , KOPE HARRY H
发明人： FORTIN J ANDRE , OGILVIE KELVIN K , TSANTRIZOS YOULA S , KOPE HARRY H
IPC分类号： A01N37/36 , A01N37/38 , A01N37/42 , A01N63/04 , A01N37/10 , A61K31/19
摘要： The invention relates to a biofungicidal composition characterized by its capacity to arrest the growth and/or destroy the cell wall of pathogenic fungi, comprises a composition of a compound of the formula I wherein R1 is selected from the group consisting of and R2 is -H or -OH and mixtures thereof in association with an inert carrier, and to a method for arresting the growth and/or destroying the cell wall of pathogenic fungi by applying thereto a biofungicidal amount of the composition of a compound of formula I in association with an inert carrier.

4. 发明申请

WO0009543A3 HEPATITIS C INHIBITOR TRI-PEPTIDES 审中-公开
标题翻译： HEPATITIS C抑制剂TRI-PEPTIDES
公开(公告)号：WO0009543A3
公开(公告)日：2000-05-25
申请号：PCT/CA9900736
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM CA LTD , LLINAS BRUNET MONTSE , BAILEY MURRAY D , CAMERON DALE , FAUCHER ANNE MARIE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , POUPART MARC ANDRE , RANCOURT JEAN , TSANTRIZOS YOULA S , WERNIC DOMINIK M , SIMONEAU BRUNO
发明人： LLINAS-BRUNET MONTSE , BAILEY MURRAY D , CAMERON DALE , FAUCHER ANNE-MARIE , GHIRO ELISE , GOUDREAU NATHALIE , HALMOS TEDDY , POUPART MARC-ANDRE , RANCOURT JEAN , TSANTRIZOS YOULA S , WERNIC DOMINIK M , SIMONEAU BRUNO
IPC分类号： C12N15/09 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K38/06 , A61K38/21 , A61P1/16 , A61P31/12 , A61P31/14 , C07C229/48 , C07K1/06 , C07K5/08 , C07K5/083 , C07K5/087 , C12N9/50 , C12N9/99 , C12P21/02 , C12P41/00
CPC分类号： C12P13/02 , A61K38/21 , A61K45/06 , C07D207/16 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C12P41/005 , A61K2300/00
摘要： Racemates, diastereoisomers and optical isomers of a compound of formula (I) wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4-C(O)-; a carboxyl of formula R4-O-C(O)-; an amide of formula R4-N(R5)-C(O)-; a thioamide of formula R4-N(R5)-C(S)-;or a sulfonyl of formula R4-SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2-R20, NH-R20, O-R20or S-R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：式（I）化合物的外消旋物，非对映异构体和光学异构体，其中B是H，C6或C10芳基，C7-16芳烷基; Het或（低级烷基）-Het，其全部任选被C 1-6烷基取代; C 1-6烷氧基; C 1-6烷酰基; 羟基; 羟; 光环; 卤代; 硝基; 氰基; 氰; 任选被C 1-6烷基取代的氨基; 酰胺基; 或（低级烷基）酰胺; 或B是式R4-C（O） - 的酰基衍生物; 式R4-O-C（O） - 的羧基; 式R 4 -N（R 5）-C（O） - 的酰胺; 式R 4 -N（R 5）-C（S） - 的硫代酰胺;或式R4-SO2的磺酰基; R5是H或C1-6烷基; Y为H或C 1-6烷基; R 3是C 1-8烷基，C 3-7环烷基或C 4-10烷基环烷基，其全部被羟基，C 1-6烷氧基，C 1-6硫代烷基，酰氨基，（低级烷基）酰氨基，C 6或C 10芳基取代，或C7-16芳烷基; R2是CH2-R20，NH-R20，O-R20或S-R20，其中R20是饱和或不饱和的C3-7环烷基或C4-10（烷基环烷基），它们全部是任选的一，二或三取代 R 21或R 20为任选取代的C 6或C 10芳基或C 7-14芳烷基，或R 20为Het或（低级烷基）-Het，均为任选取代的Het或（低级烷基）-Het; 羧基; 羧基（低级烷基）; C6或C10芳基，C7-14芳烷基或Het，所述芳基，芳烷基或Het任选被取代; 并且R 1是H; C 1-6烷基，C 3-7环烷基，C 2-6烯基或C 2-6炔基，全部被卤素取代; 或其药学上可接受的盐或酯。

5. 发明申请

WO9907734A3 HEPATITIS C INHIBITOR PEPTIDE ANALOGUES 审中-公开
标题翻译： HEPATITIS C抑制肽类似物
公开(公告)号：WO9907734A3
公开(公告)日：1999-05-20
申请号：PCT/CA9800764
申请日：1998-08-10
申请人： BOEHRINGER INGELHEIM CA LTD , LLINAS BRUNET MONTSE , BAILEY MURRAY DOUGLAS , HALMOS TEDDY , POUPART MARC ANDRE , TSANTRIZOS YOULA
发明人： LLINAS-BRUNET MONTSE , BAILEY MURRAY DOUGLAS , HALMOS TEDDY , POUPART MARC-ANDRE , TSANTRIZOS YOULA
IPC分类号： A61K45/00 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K38/21 , A61P31/14 , C07K7/06 , C07K14/18 , A61K38/04 , A61K38/16 , C07K5/093 , C07K5/107
CPC分类号： C07K7/06 , A61K38/00 , C07K14/005 , C12N2770/24222
摘要： Compound of formula (I) active against the Hepatitis C virus, wherein B is an acyl derivative; a is 0 or 1; R6, when present, is carboxy(lower)alkyl; b is 0 or 1; R5, when present, is C1-6 alkyl, or carboxy(lower)alkyl; Y is H or C1-6 alkyl; R4 is C1-10 alkyl; R3 is C1-10 alkyl; W is -NH-CH(R2)-C(O)-, wherein R2 is C1-6 alkyl; C6 or C10 aryl; C7-16 aralkyl; or carboxy(lower)alkyl; or W is a proline derivative; Q is a group of the formula -Z(R1)-C(O)-R13, wherein Z is CH or N; R1 is C1-6 alkyl or C1-6 alkenyl both optionally substituted with thio or halo; and R13 is an activated carbonyl substituent, or Q is a phosphonate group of the formula -CH(R1)-P(O)R15R16 wherein R15 and R16 are independently C6-20 aryloxy; and R1 is as defined above.
摘要翻译：对丙型肝炎病毒有活性的式（I）化合物，其中B为酰基衍生物; a是0或1; 当存在时，R 6为羧基（低级）烷基; b为0或1; 当存在时，R 5为C 1-6烷基或羧基（低级）烷基; Y是H或C 1-6烷基; R4是C1-10烷基; R3是C1-10烷基; W是-NH-CH（R 2）-C（O） - ，其中R 2是C 1-6烷基; C6或C10芳基; C7-16芳烷基; 或羧基（低级）烷基; 或W是脯氨酸衍生物; Q是式-Z（R1）-C（O）-R13的基团，其中Z是CH或N; R 1是任选被硫或卤代取代的C 1-6烷基或C 1-6链烯基; 并且R 13是活化的羰基取代基，或Q是式-CH（R 1）-P（O）R 15 R 16的膦酸酯基团，其中R 15和R 16独立地是C 6-20芳氧基; 并且R 1如上所定义。

6. 发明申请

WO2004108673A2 INHIBITORS OF PAPILLOMA VIRUS 审中-公开
标题翻译： PAPILLOMA病毒的抑制剂
公开(公告)号：WO2004108673A2
公开(公告)日：2004-12-16
申请号：PCT/CA2004000839
申请日：2004-06-07
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , TSANTRIZOS YOULA S , FAUCHER ANNE-MARIE , RANCOURT JEAN , WHITE PETER
发明人： TSANTRIZOS YOULA S , FAUCHER ANNE-MARIE , RANCOURT JEAN , WHITE PETER
IPC分类号： A61K31/451 , C07D211/38 , C07D211/46 , C07D295/135 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/36 , C07D211/00
CPC分类号： C07C235/34 , A61K31/451 , C07D211/38 , C07D211/46 , C07D295/135 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/36
摘要： The use of a compound of formula (II): or its enantiomers or diastereoisomers thereof, or salts or pharmaceutically-acceptable esters thereof, in the treatment or prevention of a papilloma virus infection, particularly human papilloma virus in a mammal, wherein R ; X4; X5; X6; R ; R ; W; Z; Y; T; and R are defined herein. The present invention also provides novel compounds, pharmaceutical compositions and methods for using these compounds and compositions in the treatment or prevention of papilloma virus infection. More particularly, the present invention provides compounds, compositions and methods for inhibiting papilloma virus DNA replication by interfering with the E1-E2 protein-protein interaction essential for viral DNA replication.
摘要翻译：式（II）化合物或其对映体或非对映异构体或其盐或药学上可接受的酯在哺乳动物中治疗或预防乳头状瘤病毒感染，特别是人乳头状瘤病毒中的用途，其中R 11 >; X4; X5; X6; [R <13>; [R <14>; 瓦; Z者除外; Ÿ; 吨; 和R 18在本文中定义。本发明还提供了用于治疗或预防乳头状瘤病毒感染的新化合物，药物组合物和使用这些化合物和组合物的方法。更具体地，本发明提供通过干扰病毒DNA复制所必需的E1-E2蛋白质 - 蛋白质相互作用来抑制乳头状瘤病毒DNA复制的化合物，组合物和方法。

7. 发明申请

WO2003007945A1 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2003007945A1
公开(公告)日：2003-01-30
申请号：PCT/CA2002/001129
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM (CANADA) LTD. , BEAULIEU, Pierre, Louis , FAZAL, Gulrez , GOULET, Sylvie , KUKOLJ, George , POIRIER, Martin , TSANTRIZOS, Youla, S.
发明人： BEAULIEU, Pierre, Louis , FAZAL, Gulrez , GOULET, Sylvie , KUKOLJ, George , POIRIER, Martin , TSANTRIZOS, Youla, S.
IPC分类号： A61K31/4184
CPC分类号： C07D401/04 , C07D235/18 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04
摘要： An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula (I): wherein R 1 is selected from: H, haloalkyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 3-7 )cycloalkyl, (C 2-6 )alkynyl, (C 5-7 )cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 6-10 )bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR 5 , wherein R 5 is H, halogen, haloalkyl, (C 1-6 )alkyl, (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; X is N or CR 5 ; D is N or CR 5 ; each of Y 1 and Y 2 is independently O or S; Z is O, N, or NR z wherein R z is H, (C 1-6 )alkyl, (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; R 3 and R 4 are each independently H, (C 1-6 )alkyl, first (C 3-7 )cycloalkyl, 6- or 10-membered aryl, Het (C 1-6 )alkyl-6- or 10-membered aryl, (C 1-6 )alkyl-Het; or each R 3 and R 4 are independently covalently bonded together to form second (C 3-7 )cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R 3 or R 4 are independently covalently bonded thereto to form a nitrogen-containing heterocycle; R 7 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; or R 7 is covalently bonded to either of R 3 or R 4 to form a heterocycle; A is (C 1-6 ) alkyl-CONHR 8 wherein R 8 is-6- or 10-membered aryl, or Het; or A is a 6- or 10-membered aryl, or Het said aryl or Het being optionally substituted; or a salt or a derivative thereof; such compounds being potent inhibitors of HCV NS5B polymerase.
摘要翻译：由式（I）表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中R 1选自：H，卤代烷基，（C 1-6）烷基，（C 2-6）烯基，（C 3 -C 6） 7）环烷基，（C 2-6）炔基，（C 5-7）环烯基，6或10元芳基，Het全部被取代; R 2选自（C 1-6）烷基，（C 3-7）环烷基，（C 6-10）双环烷基，6-或10-元芳基，或任选取代的Het; B是N或CR 5，其中R 5是H，卤素，卤代烷基，（C 1-6）烷基，（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基; X为N或CR <5>; D为N或CR 5; Y1和Y2各自独立地为O或S; Z是O，N或NR z，其中R z是H，（C 1-6）烷基，（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基; R 3和R 4各自独立地为H，（C 1-6）烷基，第一（C 3-7）环烷基，6-或10-元芳基，Het（C 1-6）烷基-6-或10- （C 1-6）烷基-Het; 或每个R 3和R 4独立地共价键合在一起形成全部任意取代的第二（C 3-7）环烷基或杂环; 或当Z为N时，R 3或R 4独立地与其共价键合形成含氮杂环; R 7是H，（C 1-6烷基），（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基; 或R 7共价键合到R 3或R 4中的任一个以形成杂环; A是（C 1-6）烷基-CONHR 8，其中R 8是6-元或10元芳基，或Het; 或A是6-或10-元芳基，或Het表示芳基或Het任选被取代; 或其盐或衍生物; 这些化合物是HCV NS5B聚合酶的有效抑制剂。

8. 发明申请

WO9907733A2 HEPATITIS C INHIBITOR PEPTIDES 审中-公开
标题翻译：丙型肝炎C抑制剂肽
公开(公告)号：WO9907733A2
公开(公告)日：1999-02-18
申请号：PCT/CA9800765
申请日：1998-08-10
申请人： BOEHRINGER INGELHEIM CA LTD , LLINAS BRUNET MONTSE , POUPART MARC ANDRE , RANCOURT JEAN , SIMONEAU BRUNO , TSANTRIZOS YOULA , WERNIC DOMINIK
发明人： LLINAS-BRUNET MONTSE , POUPART MARC-ANDRE , RANCOURT JEAN , SIMONEAU BRUNO , TSANTRIZOS YOULA , WERNIC DOMINIK
IPC分类号： A61K38/00 , A61K38/21 , A61P1/16 , A61P31/12 , C07K5/078 , C07K5/083 , C07K5/103 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/18 , C07K7/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/06139 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/08 , C07K14/005 , C12N2770/24222
摘要： Compound of formula (I) active against the Hepatitis C virus, wherein when Q is CH2, a is 0, b is 0 and B is an amide derivative; or when Q is N-Y wherein Y is H or C1-6 alkyl, then B is an acyl derivative; R6, when present, is C1-6 alkyl substituted with carboxyl; R5, when present, is C1-6 alkyl optionally substituted with carboxyl; when Q is either CH2 or N-Y, then Z is oxo or thioxo; R4 is C1-10alkyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); R3 is C1-10 alkyl optionally substituted with carboxyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); W is a proline derivative; R1' is hydrogen, and R1 is C1-6 alkyl optionnaly substituted with thiol; or R1 is C2-6 alkenyl; or R1' and R1 together form a 3- to 6-membered ring; and A is hydroxy or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：式（I）化合物对丙型肝炎病毒具有活性，其中当Q为CH2时，a为0，b为0且B为酰胺衍生物; 或当Q是N-Y，其中Y是H或C 1-6烷基时，则B是酰基衍生物; 当R6存在时，是被羧基取代的C1-6烷基; R5在存在时为任选被羧基取代的C1-6烷基; 当Q是CH2或N-Y时，则Z是氧代或硫代; R4是C1-10烷基，C3-7环烷基或C4-10（烷基环烷基）; R3为任选被羧基，C3-7环烷基或C4-10（烷基环烷基）取代的C1-10烷基; W是脯氨酸衍生物; R1'为氢，并且R1为选择性地被硫醇取代的C1-6烷基; 或者R1是C2-6链烯基; 或者R1'和R1一起形成3至6元环; A是羟基或其药学上可接受的盐或酯。

9. 发明公开

EP1105422A1 HEPATITIS C INHIBITOR PEPTIDES 有权
标题翻译： HEPATITIS C抑制肽
公开(公告)号：EP1105422A1
公开(公告)日：2001-06-13
申请号：EP99938085.0
申请日：1999-08-09
申请人： BOEHRINGER INGELHEIM (CANADA) LTD. , LLinas-Brunet, Montse , Bailey, Murray D. , Cameron, Dale , Ghiro, Elise , Goudreau, Nathalie , Poupart, Marc-André , Rancourt, Jean , Tsantrizos, Youla S.
发明人： LLINAS-BRUNET, Montse , BAILEY, Murray, D. , CAMERON, Dale , GHIRO, Elise , GOUDREAU, Nathalie , POUPART, Marc-André , RANCOURT, Jean , TSANTRIZOS, Youla, S.
IPC分类号： C07K14/81 , C07K5/10 , C07K7/06 , A61K38/55 , A61P31/14
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1016
摘要： Formula (I) wherein a is 0 or 1; b is 0 or 1; Y is H or C1-6 alkyl; B is H, an acyl derivative or a sulfonyl derivative; W is hydroxy or a N-substituted amino; or a pharmaceutically acceptable salt or ester thereof, for use in the treatment of hepatitis C virus (HCV) infection.

10. 发明申请

WO2007131350A1 INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION 审中-公开
标题翻译：人类免疫缺陷病毒复制的抑制剂
公开(公告)号：WO2007131350A1
公开(公告)日：2007-11-22
申请号：PCT/CA2007/000845
申请日：2007-05-14
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BOEHRINGER INGELHEIM PHARMA GmbH & CO KG , TSANTRIZOS, Youla, S. , BOES, Michael , BROCHU, Christian , FENWICK, Craig , MALENFANT, Eric , MASON, Stephen , PESANT, Marc
发明人： TSANTRIZOS, Youla, S. , BOES, Michael , BROCHU, Christian , FENWICK, Craig , MALENFANT, Eric , MASON, Stephen , PESANT, Marc
IPC分类号： C07D311/08 , A61K31/352 , A61K31/47 , A61P31/18 , C07D215/22
CPC分类号： C07D215/22 , C07D215/14 , C07D215/18 , C07D215/227 , C07D311/08 , C07D311/12 , C07D311/14 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D413/12
摘要： The invention relates to compounds of formula (I) their derivatives comprising a detectable label, their compositions and their use in the treatment of human immunodeficiency virus (HIV) infection. In particular, the invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.
摘要翻译：本发明涉及式（I）化合物及其组合物及其在治疗人类免疫缺陷病毒（HIV）感染中的用途的衍生物。特别地，本发明提供HIV复制的新型抑制剂，含有这些化合物的药物组合物和使用这些化合物治疗HIV感染的方法。

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