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1. 发明公开

EP0691963A1 HEPOXILIN ANALOGS USEFUL AS ANTI-INFLAMMATORY AGENTS 失效
标题翻译： Hepoxilin类似物有用抗发炎剂
公开(公告)号：EP0691963A1
公开(公告)日：1996-01-17
申请号：EP94912660.0
申请日：1994-03-28
申请人： Pace-Asciak, Cecil, R. , Demin, Peter, M.
发明人： Pace-Asciak, Cecil, R. , Demin, Peter, M.
IPC分类号： C07C45 , C07C47 , C07C69 , C07D303 , C07D331
CPC分类号： C07D331/02 , C07C45/29 , C07C45/292 , C07C47/45 , C07C69/732 , C07D303/42
摘要： Compounds of general structure (a) and (b) are disclosed, wherein X is O, Cn, NH, or S, wherein n is 1, 2, 3 or 4; R1 is OH, CH3, CH2OH, N3 or CH2N3; R3 is H or CH3; R5 is Y-R2, wherein Y is a six-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum of three; R2 is C1-C10 alkyl OH, C1-C10 alkyl N3 or COOR4, wherein R4 is H, a branched or unbranched C1-C10 alkyl (including substituted alkyl radicals), cycloalkyl, preferably C5 OC C6 cycloalkyl, or a five- or six-membered aryl radical (including substituted aryl radicals), i.e. R2 is COOH or an ester of R4; R6 is a seven-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum or three; and (c) indicates a single, double or triple bond. The compounds are analogs of hepoxilins and are used to modulate hepoxilin activity, for example in the control of inflammation or other processes mediated by intracellular calcium levels.

2. 发明申请

WO2007118335A9 HEPOXILIN ANALOG ENANTIOMERS 审中-公开
标题翻译：胡萝卜素类似物
公开(公告)号：WO2007118335A9
公开(公告)日：2008-06-26
申请号：PCT/CA2007000668
申请日：2007-04-19
申请人： EVOLVA S A , PACE-ASCIAK CECIL , DEMIN PETER , SORENSEN ALEXANDRA SANTANA , MEYER JEAN-PHILIPPE
发明人： PACE-ASCIAK CECIL , DEMIN PETER , SORENSEN ALEXANDRA SANTANA , MEYER JEAN-PHILIPPE
IPC分类号： C07C69/732 , A61K31/215 , A61K31/336 , A61P35/00 , C07C67/48 , C07C303/38
CPC分类号： C07C69/732 , C07C2601/02
摘要： The present invention relates to enantiomeric forms of hepoxilin analogs of Formula I-VIII, pharmaceutical compositions thereof, a method for the separation of said enantiomeric forms of hepoxilin analogs comprising applying said hepoxilin to a chiral phase HPLC column and eluting said hepoxilin with an alkane and alcohol solvent mixture. Said enantiomeric forms of hepoxilin analogs of Formula I-VIII were found to be useful in controlling the biological effects of PPAR mediated transcriptional control for the treatment of diseases such as cancer, thromboxane-mediated diseases and for modulating intracellular calcium concentration.
摘要翻译：本发明涉及式I-VIII的肝素类似物的对映体形式，其药物组合物，用于分离所述对映异构形式的肝素类似物的方法，包括将所述肝素应用于手性HPLC柱并用烷烃洗脱所述肝素，酒精溶剂混合物。发现式I-VIII的肝素类似物的所述对映体形式可用于控制PPAR介导的转录控制对于治疗诸如癌症，血栓烷介导的疾病和调节细胞内钙浓度的疾病的生物学作用。

3. 发明申请

WO1994022848A1 HEPOXILIN ANALOGS USEFUL AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：抗氧化剂类似物作为抗炎药物有用
公开(公告)号：WO1994022848A1
公开(公告)日：1994-10-13
申请号：PCT/IB1994000085
申请日：1994-03-28
申请人： PACE-ASCIAK, Cecil, R. , DEMIN, Peter, M.
IPC分类号： C07D303/38
CPC分类号： C07D331/02 , C07C45/29 , C07C45/292 , C07C47/45 , C07C69/732 , C07D303/42
摘要： Compounds of general structure (a) and (b) are disclosed, wherein X is O, Cn, NH, or S, wherein n is 1, 2, 3 or 4; R1 is OH, CH3, CH2OH, N3 or CH2N3; R3 is H or CH3; R5 is Y-R2, wherein Y is a six-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum of three; R2 is C1-C10 alkyl OH, C1-C10 alkyl N3 or COOR4, wherein R4 is H, a branched or unbranched C1-C10 alkyl (including substituted alkyl radicals), cycloalkyl, preferably C5 OC C6 cycloalkyl, or a five- or six-membered aryl radical (including substituted aryl radicals), i.e. R2 is COOH or an ester of R4; R6 is a seven-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum or three; and (c) indicates a single, double or triple bond. The compounds are analogs of hepoxilins and are used to modulate hepoxilin activity, for example in the control of inflammation or other processes mediated by intracellular calcium levels.
摘要翻译：公开了通式（a）和（b）的化合物，其中X是O，Cn，NH或S，其中n是1,2,3或4; R1是OH，CH3，CH2OH，N3或CH2N3; R3是H或CH3; R5是Y-R2，其中Y是任选含有多达三个双键或三键的六碳链或最多三个的双键和三键的混合物; R 2是C 1 -C 10烷基OH，C 1 -C 10烷基N 3或COOR 4，其中R 4是H，支链或非支链C 1 -C 10烷基（包括取代的烷基），环烷基，优选C 5 -C 6环烷基，或五或六（包括取代的芳基），即R2是COOH或R4的酯; R6是任选地含有多达三个双键或三键或高达三个或更多的双键和三键的混合物的七碳链; 和（c）表示单键，双键或三键。这些化合物是肝素的类似物，用于调节肝素活性，例如在控制炎症或由细胞内钙水平介导的其它过程中。

4. 发明申请

WO2004032911A2 INHIBITION OF VASCULAR ENDOTHELIAL GROWTH FACTOR 审中-公开
标题翻译：血管内皮生长因子的抑制作用
公开(公告)号：WO2004032911A2
公开(公告)日：2004-04-22
申请号：PCT/CA2003/001558
申请日：2003-10-10
申请人： THE HOSPITAL FOR SICK CHILDREN , ROIFMAN, Chaim, M. , SIMON, Amos, J. , DEMIN, Peter, M. , ROUNOVA, Olga, B.
发明人： ROIFMAN, Chaim, M. , SIMON, Amos, J. , DEMIN, Peter, M. , ROUNOVA, Olga, B.
IPC分类号： A61K31/165
CPC分类号： A61K31/662 , A61K31/137 , A61K31/165 , A61K31/216 , A61K31/277
摘要： This invention relates to therapeutic organic compounds and inhibition of secretion of vascular endothelial grown factor (VEGF) and its effects, including angiogenesis.
摘要翻译：本发明涉及治疗性有机化合物和抑制血管内皮生长因子（VEGF）的分泌及其作用，包括血管生成。

5. 发明申请

WO0179158A2 NOVEL COMPOUNDS FOR MODULATING CELL PROLIFERATION 审中-公开
标题翻译：用于调节细胞增殖的新型化合物
公开(公告)号：WO0179158A2
公开(公告)日：2001-10-25
申请号：PCT/CA0100516
申请日：2001-04-12
申请人： HSC RES DEV LP , ROIFMAN CHAIM M , GRUNBERGER THOMAS , ROUNOVA OLGA , DEMIN PETER , SHARFE NIGEL
发明人： ROIFMAN CHAIM M , GRUNBERGER THOMAS , ROUNOVA OLGA , DEMIN PETER , SHARFE NIGEL
IPC分类号： A61K31/695 , A61K31/09 , A61K31/11 , A61K31/277 , A61K31/40 , A61K31/537 , A61K31/66 , A61P7/00 , A61P19/00 , A61P35/00 , A61P35/02 , A61P35/04 , C07C45/29 , C07C255/19 , C07C255/41 , C07C255/42 , C07C327/44 , C07F7/18 , C07C255/00
CPC分类号： C07F7/1852 , C07C45/292 , C07C255/41 , C07C255/42 , C07C327/44 , Y02P20/582 , C07C47/277
摘要： Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed. The compounds are of Formula (I).
摘要翻译：公开了可用于治疗各种细胞增殖性疾病如癌症的新型苯乙烯基丙烯腈化合物。化合物为式（I）。

6. 发明申请

WO2005092904A1 NOVEL COMPOUNDS FOR MODULATING CELL PROLIFERATION 审中-公开
标题翻译：用于调节细胞增殖的新型化合物
公开(公告)号：WO2005092904A1
公开(公告)日：2005-10-06
申请号：PCT/CA2005/000423
申请日：2005-03-22
申请人： HSC RESEARCH AND DEVELOPMENT LIMITED PARTNERSHIP , ROIFMAN, Chaim, M , DEMIN, Peter , FREYWALD, Andrew , GRUNBERGER, Thomas , ROUNOVA, Olga , SHARFE, Nigel
发明人： ROIFMAN, Chaim, M , DEMIN, Peter , FREYWALD, Andrew , GRUNBERGER, Thomas , ROUNOVA, Olga , SHARFE, Nigel
IPC分类号： C07F9/40
CPC分类号： C07C255/41 , C07C255/42 , C07C317/46 , C07C327/44 , C07D213/40 , C07D307/52 , C07D317/58 , C07D317/60 , C07F7/1852 , C07F9/3826 , C07F9/4015
摘要： Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
摘要翻译：公开了可用于治疗各种细胞增殖性疾病如癌症的新型苯乙烯基丙烯腈化合物。

7. 发明申请

WO2005012234A1 COMPOUNDS FOR MODULATING CELL PROLIFERATION 审中-公开
标题翻译：用于调节细胞增殖的化合物
公开(公告)号：WO2005012234A1
公开(公告)日：2005-02-10
申请号：PCT/CA2004/001431
申请日：2004-07-30
申请人： THE HOSPITAL FOR SICK CHILDREN , ROIFMAN, Chaim, M. , DEMIN, Peter , ROUNOVA, Olga , GRUNBERGER, Thomas , CIMPEAN, Octavian, Laurand
发明人： ROIFMAN, Chaim, M. , DEMIN, Peter , ROUNOVA, Olga , GRUNBERGER, Thomas , CIMPEAN, Octavian, Laurand
IPC分类号： C07C255/41
CPC分类号： A61K31/4402 , C07C255/41 , C07C323/46 , C07D213/71
摘要： Compounds having the Formula (I) or (III) wherein R 1 , R 2 and R 3 are each independently selected from H, OH, C 1-6 alkyl, C 1-6 alkoxy, NH 2 , NH-(C l-6 a1kyl), N(C 1-6 a1kyl)(C 1-6 alkyl), SH, S-C 1-6 alkyl, NO 2 , CF 3 , OCF 3 , and halo; R 4 is unsubstituted Ar or Ar substituted with 1-4 substituents independently selected from C 1-6 alkyl, C 1-6 alkoxy and halo; X is selected from (CH 2 CH 2 O)n and (CH)n, and n = 1-4, salts, solvates and hydrates thereof, useful for modulating or inhibiting cell proliferation, are described.
摘要翻译：具有式（I）或（III）的化合物其中R 1，R 2和R 3各自独立地选自H，OH，C 1-6烷基，C 1-6烷氧基，NH 2，NH-（Cl- C 1-6烷基），N（C 1-6烷基）（C 1-6烷基），SH，S-C 1-6烷基，NO 2，CF 3，OCF 3和卤素; R 4是未取代的Ar或Ar，其被1-4个独立地选自C 1-6烷基，C 1-6烷氧基和卤素的取代基取代; 描述了可用于调节或抑制细胞增殖的（CH 2 CH 2 O）n和（CH）n和n = 1-4，其盐，溶剂合物和水合物。

8. 发明申请

WO2006029516A1 NOVEL COMPOUNDS USEFUL FOR MODULATING ABNORMAL CELL PROLIFERATION 审中-公开
标题翻译：用于调节异常细胞增殖的新型化合物
公开(公告)号：WO2006029516A1
公开(公告)日：2006-03-23
申请号：PCT/CA2005/001395
申请日：2005-09-14
申请人： THE HOSPITAL FOR SICK CHILDREN , ROIFMAN, Chaim , DEMIN, Peter , ROUNOVA, Olga , GRUNBERGER, Tom
发明人： ROIFMAN, Chaim , DEMIN, Peter , ROUNOVA, Olga , GRUNBERGER, Tom
IPC分类号： C07C235/34
CPC分类号： C07C235/34
摘要： There is described compounds of Formula (I), and salts, solvates and hydrates thereof wherein Formula (I): R 1 , R 2 and R 3 are each independently selected from OH, C 1- 6 alkyl, OC 1- 6 alkyl, OC(O)C 1 _ 6 alkyl, C(O)OC 1 _ 6 alkyl, NH 2 , NH-C 1-6 alkyl, N(C 1-6 alkyl)(C 1-6 alkyl), C(O)NHC 1-6 alkyl, C(O)N(C 1-6 alkyl)(C 1-6 alkyl), SH, SC 1-6 alkyl, NO 2 , CF 3 , OCF 3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1-4 substituents independently selected from OH, C 1-6 alkyl, C 1-6 alkoxy, C 1-3 alkylenedioxy, NH 2 , NHC 1-6 alkyl, N(C 1-6 alkyl)(C 1-6 alkyl), SH, S-C 1-6 alkyl, NO 2, CF 3 , OCF 3 and halogen. The compounds of Formula (I) are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.
摘要翻译：描述了式（I）的化合物及其盐，溶剂合物和水合物，其中式（I）：R

9. 发明申请

WO2003030895A1 STYRYL ACRYLONITRILE COMPOUNDS AND THEIR USE TO PROMOTE MYELOPOIESIS 审中-公开
标题翻译： STYRYL ACRYLONITRILE化合物及其用于促进MYELOPOIESISIS
公开(公告)号：WO2003030895A1
公开(公告)日：2003-04-17
申请号：PCT/CA2002/001548
申请日：2002-10-11
申请人： THE HOSPITAL FOR SICK CHILDREN , ROIFMAN, Chaim, M. , GRUNBERGER, Thomas , SHARFE, Nigel , ROUNOVA, Olga, B. , DEMIN, Peter, M. , FREYWALD, Andrew
发明人： ROIFMAN, Chaim, M. , GRUNBERGER, Thomas , SHARFE, Nigel , ROUNOVA, Olga, B. , DEMIN, Peter, M. , FREYWALD, Andrew
IPC分类号： A61K31/277
CPC分类号： A61K31/277
摘要： The invention relates to the use of organic compounds, styryl acrylonitrile compounds to promote myelopoiesis. These compounds thefore may be used to treat a subject suffering from neutropenia and other conditions which would benefit from increased myelopoieses. Moreover, the compounds may be used to treat hematopoietic cells ex-vivo to promote myelopoiesis and therefore may be used advantageously in bone marrow or peripheral blood stem cell transplant.
摘要翻译：本发明涉及使用有机化合物，苯乙烯基丙烯腈化合物来促进骨髓细胞生成。这些化合物以前可用于治疗患有中性粒细胞减少症的受试者和可从增加的骨髓细胞中获益的其它病症。此外，该化合物可用于离体治疗造血细胞以促进骨髓生成，因此可有利地用于骨髓或外周血干细胞移植。

10. 发明申请

US20050014690A1 Styryl acrylonitrile compounds and their use to promote myelopoiesis 审中-公开
标题翻译：苯乙烯基丙烯腈化合物及其用于促进骨髓细胞生成的用途
公开(公告)号：US20050014690A1
公开(公告)日：2005-01-20
申请号：US10492251
申请日：2002-10-11
申请人： Chaim Roifman , Thomas Grunberger , Nigel Sharfe , Olga Rounova , Demin Peter , Andrew Freywald
发明人： Chaim Roifman , Thomas Grunberger , Nigel Sharfe , Olga Rounova , Demin Peter , Andrew Freywald
IPC分类号： A61K31/277 , A61K38/17 , A61P15/06
CPC分类号： A61K31/277
摘要： The invention relates to the use of organic compounds, styryl acrylonitrile compounds to promote myelopoiesis. These compounds thefore may be used to treat a subject suffering from neutropenia and other conditions which would benefit from increased myelopoieses. Moreover, the compounds may be used to treat hematopoietic cells ex-vivo to promote myelopoiesis and therefore may be used advantageously in bone marrow or peripheral blood stem cell transplant.
摘要翻译：本发明涉及有机化合物，苯乙烯基丙烯腈化合物促进骨髓生成的用途。这些化合物以前可用于治疗患有中性粒细胞减少症的受试者和可从增加的骨髓细胞中获益的其它病症。此外，该化合物可用于离体治疗造血细胞以促进骨髓生成，因此可有利地用于骨髓或外周血干细胞移植。

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