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11.发明申请LYSINE DEMETHYLASE INHIBITORS SUCH AS CYCLYLCYLOPROPAMINE DERIVATIVES FOR USE IN THE TREATMENT OF INFLAMMATORY DISEASES OR CONDITIONS 审中-公开赖氨酸脱乙酰酶抑制剂，如用于治疗炎症性疾病或病症的环丙氯喹啉衍生物
公开(公告)号：WO2012156531A3
公开(公告)日：2013-01-10
申请号：PCT/EP2012059377
申请日：2012-05-21
申请人： ORYZON GENOMICS SA , MAES TAMARA , MARTINELL PEDEMONTE MARC , CASTRO-PALOMINO LARIA JULIO CESAR
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/44 , A61K31/495 , A61P7/02
CPC分类号： C07D295/192 , A61K31/135 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/44 , A61K31/4418 , A61K31/495 , A61K45/06 , C07C215/64 , C07C237/06 , C07C311/08 , C07D207/14 , C07D213/38
摘要： The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
摘要翻译： 本发明涉及用于治疗或预防炎症和炎性疾病或病症的方法和组合物。 特别地，本发明涉及用于治疗或预防炎症和炎性疾病或病症的LSD1抑制剂，例如2-环丙基环丙烷-1-胺衍生物，苯乙肼衍生物和炔丙胺衍生物。
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12.发明申请ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE 审中-公开基于ARYLCYCLOPROPYLAMINE的LSD1的DEMETHYLASE抑制剂及其医疗用途
公开(公告)号：WO2012013728A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/062949
申请日：2011-07-27
申请人： ORYZON GENOMICS S.A. , ORTEGA MUÑOZ, Alberto , FYFE, Matthew, Colin, Thor , MARTINELL PEDEMONTE, Marc , TIRAPU FERNANDEZ DE LA CUESTA, Iñigo , ESTIARTE-MARTÍNEZ, Maria de los Ángeles
发明人： ORTEGA MUÑOZ, Alberto , FYFE, Matthew, Colin, Thor , MARTINELL PEDEMONTE, Marc , TIRAPU FERNANDEZ DE LA CUESTA, Iñigo , ESTIARTE-MARTÍNEZ, Maria de los Ángeles
IPC分类号： C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D261/14 , C07D263/48 , C07D277/40 , C07D285/12 , C07D401/12 , C07D413/12 , C07D417/12 , C07D271/07 , C07D271/113 , C07D253/07 , A61K31/44
CPC分类号： C07D417/12 , A61K31/422 , A61K31/4245 , A61K31/433 , C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/113 , C07D277/40 , C07D285/08 , C07D285/12 , C07D285/135 , C07D401/12 , C07D413/12
摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g ., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
摘要翻译： 本发明涉及（异）芳基环丙胺化合物，特别包括本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症，神经疾病或病症， 或病毒感染。 因此，在一个具体方面，本发明涉及式（II），（III），（IV），（V），（VI），（VII），（VIII），（IX）。
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13.发明申请CRYSTAL STRUCTURE OF THE ATPASE DOMAIN OF PROTEINS OF THE HSP70 FAMILY 审中-公开HSP70家族蛋白ATPase结构域的晶体结构
公开(公告)号：WO2009095452A1
公开(公告)日：2009-08-06
申请号：PCT/EP2009/051032
申请日：2009-01-29
申请人： CRYSTAX PHARMACEUTICALS, S.L. , SOLER LÓPEZ, Montserrat , BONIN, Irena , MARTINELL PEDEMONTE, Marc , AYMAMÍ BOFARULL, Juan
IPC分类号： C07K14/435 , G06F19/00 , C12N15/09
CPC分类号： C07K14/435 , C07K14/47 , C07K2299/00 , C12N9/14 , Y02A90/26
摘要： A mutant protein of the Hsp70 family, which comprises the amino acid sequence from amino acid 1 to amino acid 380 that corresponds to an ATPase domain, wherein at positions 60 and 261 the amino acid residues have been mutated to cysteines, being all the positions defined from the initiation of the translation of the protein. The invention also relates to a crystal of the mutant protein of the Hsp70 family, and to methods of identifying potential ligand compounds able to be further used in the preparation of medicaments for the treatment of cancer and some related diseases.
摘要翻译： Hsp70家族的突变蛋白，其包含对应于ATP酶结构域的氨基酸1至氨基酸380的氨基酸序列，其中在位置60和261处氨基酸残基已被突变 到半胱氨酸，是从蛋白质翻译起始定义的所有位置。 本发明还涉及Hsp70家族的突变蛋白的晶体，并且涉及鉴定能够进一步用于制备用于治疗癌症和一些相关疾病的药物的潜在配体化合物的方法。
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14.发明申请LYSINE DEMETHYLASE INHIBITORS SUCH AS CYCLYLCYLOPROPAMINE DERIVATIVES FOR USE IN THE TREATMENT OF THROMBOSIS AND CARDIOVASCULAR DISEASES 审中-公开赖氨酸脱乙酰酶抑制剂如循环氯吡啶衍生物用于治疗血栓形成和心血管疾病
公开(公告)号：WO2012156537A3
公开(公告)日：2013-01-10
申请号：PCT/EP2012059414
申请日：2012-05-21
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/44 , A61K31/495 , A61P7/02
CPC分类号： A61K31/495 , A61K31/135 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/4418 , A61K45/06
摘要： The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.
摘要翻译： 本发明涉及用于治疗或预防血栓形成，血栓形成，血栓形成事件或并发症或心血管疾病或事件的方法和组合物。 特别地，本发明涉及用于治疗或预防血栓形成，血栓形成，血栓形成事件或并发症或心血管疾病的LSD抑制剂，例如2-环基丙基-1-胺衍生物，苯乙肼衍生物和炔丙胺衍生物 疾病或事件。
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15.发明申请
公开(公告)号：WO2012156531A2
公开(公告)日：2012-11-22
申请号：PCT/EP2012/059377
申请日：2012-05-21
申请人： ORYZON GENOMICS, S.A. , MAES, Tamara , MARTINELL PEDEMONTE, Marc , CASTRO-PALOMINO LARIA, Julio César
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/44 , A61K31/495 , A61P7/02
CPC分类号： C07D295/192 , A61K31/135 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/44 , A61K31/4418 , A61K31/495 , A61K45/06 , C07C215/64 , C07C237/06 , C07C311/08 , C07D207/14 , C07D213/38
摘要： The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD l inhibitor for use in treating or preventing inflammation and inflammatory diseases or conditions.
摘要翻译： 本发明涉及用于治疗或预防炎症和炎性疾病或病症的方法和组合物。 特别地，本发明涉及用于治疗或预防炎症和炎性疾病或病症的LSD1抑制剂。
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16.发明申请
公开(公告)号：WO2012107498A1
公开(公告)日：2012-08-16
申请号：PCT/EP2012/052144
申请日：2012-02-08
申请人： ORYZON GENOMICS S.A. , BAKER, Jonathan, Alleman , CASTRO PALOMINO, Julio , FYFE, Matthew, Colin, Thor , MAES, Tamara , MARTINELL PEDEMONTE, Marc
发明人： BAKER, Jonathan, Alleman , CASTRO PALOMINO, Julio , FYFE, Matthew, Colin, Thor , MAES, Tamara , MARTINELL PEDEMONTE, Marc
IPC分类号： A61K31/135 , A61P35/02
CPC分类号： C07D295/195 , A61K31/00 , A61K31/131 , A61K31/135 , A61K31/138 , A61K31/15 , A61K31/164 , A61K31/18 , A61K31/40 , A61K31/4418 , A61K31/495 , A61K45/06 , C07D207/14 , C07D213/38
摘要： The invention relates to methods and compositions for the treatment or prevention of diseases and disorders associated with myeloproliferative disorders. In particular, the invention relates to an LSD 1 inhibitor for use in treating or preventing Philadelphia chromosome negative myeloproliferative disorders.
摘要翻译： 本发明涉及用于治疗或预防与骨髓增殖性疾病相关的疾病和病症的方法和组合物。 具体而言，本发明涉及用于治疗或预防费城染色体阴性骨髓增殖性疾病的LSD1抑制剂。
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公开(公告)号：WO2012045883A1
公开(公告)日：2012-04-12
申请号：PCT/EP2011/067608
申请日：2011-10-07
申请人： ORYZON GENOMICS S.A. , CASTRO-PALOMINO LARIA, Julio , FYFE, Matthew, Colin, Thor , MARTINELL PEDEMONTE, Marc , ORTEGA MUÑOZ, Alberto , VALLS VIDAL, Núria
发明人： CASTRO-PALOMINO LARIA, Julio , FYFE, Matthew, Colin, Thor , MARTINELL PEDEMONTE, Marc , ORTEGA MUÑOZ, Alberto , VALLS VIDAL, Núria
IPC分类号： C07D213/74 , C07D401/12 , C07C211/53 , C07C211/55 , C07C211/56 , C07C217/92 , C07C237/30 , C07C255/58 , A61K31/4418 , A61K31/4439 , A61K31/136 , A61K31/137 , A61P25/00 , A61P31/12 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/136 , A61K31/166 , A61K31/277 , A61K31/4418 , C07C211/52 , C07C211/53 , C07C211/55 , C07C211/56 , C07C217/92 , C07C237/30 , C07C255/58 , C07D213/74 , C07D401/12
摘要： The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
摘要翻译： 本发明涉及环丙胺化合物，特别是本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症。
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公开(公告)号：WO2009080722A3
公开(公告)日：2009-11-26
申请号：PCT/EP2008067952
申请日：2008-12-18
申请人： CRYSTAX PHARMACEUTICALS S L , AYMAMI BOFARULL JUAN , NICOLAS CHEVALIER FRANCK CAMIL , SOLER LOPEZ MONTSERRAT , LUQUE GARROFE MARIA TERESA , MARTINELL PEDEMONTE MARC
发明人： AYMAMI BOFARULL JUAN , NICOLAS CHEVALIER FRANCK CAMILLE , SOLER LOPEZ MONTSERRAT , LUQUE GARROFE MARIA TERESA , MARTINELL PEDEMONTE MARC
IPC分类号： C07C57/40 , A61K31/192 , A61P35/00 , C07C59/52 , C07C69/734 , C07C229/42 , C07C233/54 , C07C237/40 , C07C255/54 , C07C311/16 , C07C311/21 , C07D209/18 , C07D213/30 , C07D307/54 , C07D333/24
CPC分类号： C07C311/16 , C07C57/30 , C07C57/40 , C07C57/42 , C07C57/58 , C07C59/52 , C07C59/64 , C07C59/66 , C07C59/68 , C07C69/612 , C07C69/734 , C07C229/42 , C07C233/54 , C07C237/40 , C07C255/54 , C07C311/21 , C07D209/18 , C07D213/30 , C07D213/55 , C07D307/54 , C07D333/24 , C07D333/34
摘要： The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: -(CH2)1-4-, (C2-C4)-alkenyl, (C2-C4)alkynyl, -S-(CH2)1-3-#, and - (CH2)1-3-O-#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: - (CH2)2-4-, -S-(CH2)1-3#, and -O-(CH2)1-3-#,; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: -OR4. The compounds of formula (I) are useful in the treatment of cancer.
摘要翻译： 本发明提供了新的式（I）化合物，其中：R 1是衍生自一种已知环系的基团; R2是任选取代的苯基; （CH2）1-4-，（C2-C4）链烯基，（C2-C4）链炔基，-S-（CH2）1-3-和 - （ CH 2）1-3 O-＃; 其中符号＃表示Xn与R1连接的位置; Yn是选自以下的二价基团： - （CH2）2-4 - ， - S-（CH2）1-3-和-O-（CH2）1-3-。 其中符号＃表示Yn与R2连接的位置; 且R3是选自由以下组成的组的基团：-OR4。 式（I）化合物可用于治疗癌症。
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公开(公告)号：WO2009007399A1
公开(公告)日：2009-01-15
申请号：PCT/EP2008/058924
申请日：2008-07-09
申请人： CRYSTAX PHARMACEUTICALS, S.L. , MARTINELL PEDEMONTE, Marc , NAVARRO MUÑOZ, Isabel , SOLER LÓPEZ, Montserrat , MORMENEO JULIÁN, David , ROSOL, Malgorzata , LLEBARIA SOLDEVILA, Amadeo , AYMAMÍ BOFARULL, Juan
发明人： MARTINELL PEDEMONTE, Marc , NAVARRO MUÑOZ, Isabel , SOLER LÓPEZ, Montserrat , MORMENEO JULIÁN, David , ROSOL, Malgorzata , LLEBARIA SOLDEVILA, Amadeo , AYMAMÍ BOFARULL, Juan
IPC分类号： C07D233/88 , C07D405/12 , C07D405/14 , A61K31/4178 , A61K31/4164 , A61P35/00 , C07D401/12 , C07D417/12
CPC分类号： C07D417/12 , C07D209/48 , C07D233/90 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The invention provides novel compounds of formula (I) wherein: one of the a, b, c or d members is a nitrogen atom and the remaining members are carbon atoms; and R 3 is a radical selected from the group consisting of: -S-R 14 and -CH 2 -R 15 .The compounds of formula (I) are useful for treating diseases mediated by a heat shock protein 90 (Hsp 90).
摘要翻译： 本发明提供新的式（I）化合物，其中：a，b，c或d中的一个是氮原子，其余的成员是碳原子; 并且R 3是选自-S-R 14和-CH 2 -R 15的基团。式（I）化合物可用于治疗由热休克蛋白90（Hsp90）介导的疾病。
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