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1. 发明申请

WO2007022638A1 BENZODIAZEPINE AND BENZOPIPERAZINE ANALOG INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译：苯甲酸脱乙酰酶的苯并嗪和苯并吡嗪类似物抑制剂
公开(公告)号：WO2007022638A1
公开(公告)日：2007-03-01
申请号：PCT/CA2006/001402
申请日：2006-08-25
申请人： METHYLGENE INC. , LEIT, Silvana , WAHHAB, Amal , ALLAN, Martin , SMIL, David , TESSIER, Pierre , DEZIEL, Robert , CHANTIGNY, Yves, André
发明人： LEIT, Silvana , WAHHAB, Amal , ALLAN, Martin , SMIL, David , TESSIER, Pierre , DEZIEL, Robert , CHANTIGNY, Yves, André
IPC分类号： C07D243/14 , C07D241/44 , C07D207/16 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D241/44 , C07D223/16 , C07D241/50 , C07D243/10 , C07D243/14 , C07D243/24 , C07D243/30 , C07D401/12 , C07D403/04 , C07D403/06 , C07D409/06 , C07D409/12 , C07D409/14
摘要： This invention relates to compounds for the inhibition of histone deacetylase More particularly, the invention provides for compounds of formula (I): wherein A, B, D, E, X 1 , X 2 , X 3 , X 4 and n are as defined in the specification A method of inhibiting histone deacetylase in a cell, the method comprising contacting the cell with a compound of formula (I), in an amount sufficient to inhibit histone deacetylase, is also disclosed.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物更具体地说，本发明提供了式（I）化合物：其中A，B，D，E，X 1，X 2， / SUP>，X 3，X 4和n如说明书中所限定的抑制细胞中组蛋白脱乙酰酶的方法，该方法包括使细胞与化合物的式（I）化合物，其量足以抑制组蛋白脱乙酰酶。

2. 发明申请

WO2007143822A1 SULFAMIDE AND SULFAMATE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：磺酰胺和磺酰胺衍生物作为脱乙酰壳多糖酶抑制剂
公开(公告)号：WO2007143822A1
公开(公告)日：2007-12-21
申请号：PCT/CA2007/001024
申请日：2007-06-14
申请人： METHYLGENE INC. , SMIL, David , LEIT, Silvana , AJAMIAN, Alain , ALLAN, Martin , CHANTIGNY, Yves, André , DEZIEL, Robert , THERRIEN, Eric , WAHHAB, Amal , MANKU, Sukhdev
发明人： SMIL, David , LEIT, Silvana , AJAMIAN, Alain , ALLAN, Martin , CHANTIGNY, Yves, André , DEZIEL, Robert , THERRIEN, Eric , WAHHAB, Amal , MANKU, Sukhdev
IPC分类号： C07D277/46 , A61K31/185 , A61K31/417 , A61K31/4184 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/47 , A61K31/4709 , C07D215/40 , C07D233/64 , C07D235/14 , C07D271/06 , C07D277/28 , C07D307/06 , C07D401/12 , C07D417/02
CPC分类号： C07D215/38 , C07C307/06 , C07C2603/32 , C07C2603/74 , C07D209/14 , C07D215/42 , C07D215/48 , C07D223/26 , C07D233/61 , C07D235/14 , C07D249/08 , C07D261/14 , C07D263/56 , C07D263/60 , C07D271/06 , C07D271/10 , C07D273/01 , C07D277/46 , C07D277/56 , C07D277/82 , C07D285/12 , C07D307/85 , C07D401/12 , C07D405/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I), and racemic and scalemic mixtures, diastereomers and enantiomers thereof: (I) or an N-oxide, hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof, wherein Y, L, Z, W, M, R a , R b and R c are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地说，本发明提供式（I）化合物及其外消旋和可饱和的混合物，非对映异构体和对映体：（I）或其N-氧化物，水合物，溶剂合物，药学上可接受的盐，前药或复合物，其中Y， L，Z，W，M，R a，R b和R c如本说明书中所定义。

3. 发明申请

WO2006102760A1 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2006102760A1
公开(公告)日：2006-10-05
申请号：PCT/CA2006/000483
申请日：2006-03-31
申请人： METHYLGENE INC. , LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DÉZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
发明人： LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DÉZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
IPC分类号： C07D417/04 , A61K31/18 , A61K31/166 , A61K31/195 , A61K31/34 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/505 , C07C237/38 , C07C311/21 , C07C323/33 , C07C323/60 , C07D207/16 , C07D209/30 , C07D209/42 , C07D211/22 , C07D215/38 , C07D217/12 , C07D235/04 , C07D239/08 , C07D241/40 , C07D277/82 , C07D285/12 , C07D317/46 , C07D319/14 , C07D333/32 , C07D403/06 , C07D409/06 , C07D413/04
CPC分类号： C07D209/14 , C07C237/22 , C07C309/51 , C07C311/13 , C07C311/29 , C07C311/46 , C07C311/51 , C07C311/59 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/60 , C07C2601/14 , C07C2603/32 , C07D209/42 , C07D209/46 , C07D213/30 , C07D213/32 , C07D213/40 , C07D213/70 , C07D213/89 , C07D215/40 , C07D235/14 , C07D239/38 , C07D241/52 , C07D277/82 , C07D285/12 , C07D285/135 , C07D295/185 , C07D307/42 , C07D307/81 , C07D317/58 , C07D333/16 , C07D333/24 , C07D333/34 , C07D401/06 , C07D405/12 , C07D409/06 , C07D409/12
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I); wherein Y, L, Z, W, X, Q, R 1 , R 2 and R 3 are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地，本发明提供式（I）的化合物; 其中Y，L，Z，W，X，Q，R 1，R 2和R 3均如说明书中所定义。

4. 发明申请

WO2009026701A1 SIRTUIN INHIBITORS 审中-公开
标题翻译： SIRTUIN抑制剂
公开(公告)号：WO2009026701A1
公开(公告)日：2009-03-05
申请号：PCT/CA2008/001520
申请日：2008-08-29
申请人： METHYLGENE INC. , DEZIEL, Robert , RAHIL, Jubrail , WAHHAB, Amal , ALLAN, Martin , NGUYEN, Nathalie
发明人： DEZIEL, Robert , RAHIL, Jubrail , WAHHAB, Amal , ALLAN, Martin , NGUYEN, Nathalie
IPC分类号： C07D235/14 , A61K31/395 , A61P3/04 , A61P3/10 , A61P35/00 , C07C327/42 , C07D233/64 , C07D249/08 , C07D277/46 , C07D403/02 , C07D417/02
CPC分类号： C07D277/46 , C07C271/22 , C07C327/42 , C07D213/75 , C07D215/40 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/88 , C07D235/14 , C07D249/08 , C07D261/14 , C07D263/10 , C07D277/42 , C07D277/82 , C07D311/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D417/04 , C07D417/12 , C07D473/00
摘要： This invention relates to compounds and methods for the inhibition of sirtuin enzymatic activity. More particularly, the invention provides for compounds of formula (I), Y __ L __ Z __ D, and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein Y, L, Z and D are as defined in the specification.
摘要翻译：本发明涉及抑制沉默调节蛋白酶活性的化合物和方法。更具体地说，本发明提供式（I）化合物，其中Y，L，Z，D和N-氧化物，水合物，溶剂合物，药学上可接受的盐，前体药物和复合物，以及外消旋和可比混合物，非对映异构体和对映异构体，其中Y， Z和D如说明书中所定义。

5. 发明申请

WO2008104077A1 SMALL MOLECULE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASES (PRMTS) 审中-公开
标题翻译：蛋白质亚甲基转移酶的小分子抑制剂（PRMTS）
公开(公告)号：WO2008104077A1
公开(公告)日：2008-09-04
申请号：PCT/CA2008/000384
申请日：2008-02-28
申请人： METHYLGENE INC. , WAHHAB, Amal , THERRIEN, Eric , ALLAN, Martin , MANKU, Sukhdev
发明人： WAHHAB, Amal , THERRIEN, Eric , ALLAN, Martin , MANKU, Sukhdev
IPC分类号： C07D231/14 , A61K31/415 , A61K31/435 , A61P31/00 , A61P35/00 , A61P37/00 , C07D211/26 , C07D231/22 , C07D235/18 , C07D401/00 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
CPC分类号： C07D409/04 , C07D211/26 , C07D231/14 , C07D231/22 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.
摘要翻译：本发明涉及可用作具有选自式（I），式（II）和式（III）的式的蛋白质精氨酸甲基转移酶的抑制剂的化合物，以及外消旋混合物，非对映异构体，对映异构体和互变异构体以及N 氧化物，水合物，溶剂化物，药学上可接受的盐，前药和复合物。所述化合物可用作PRMT和/或CARM-1的抑制剂。本发明还涉及包含这些化合物的组合物及其使用方法。

6. 发明公开

EP1940805A1 BENZODIAZEPINE AND BENZOPIPERAZINE ANALOG INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译：组蛋白去乙酰苯二氮卓和BENZOPIPERAZINANALOGA作为抑制剂
公开(公告)号：EP1940805A1
公开(公告)日：2008-07-09
申请号：EP06790581.0
申请日：2006-08-25
申请人： Methylgene, Inc.
发明人： LEIT, Silvana , WAHHAB, Amal , ALLAN, Martin , SMIL, David , TESSIER, Pierre , DEZIEL, Robert , CHANTIGNY, Yves, André
IPC分类号： C07D243/14 , C07D241/44 , C07D207/16 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D241/44 , C07D223/16 , C07D241/50 , C07D243/10 , C07D243/14 , C07D243/24 , C07D243/30 , C07D401/12 , C07D403/04 , C07D403/06 , C07D409/06 , C07D409/12 , C07D409/14
摘要： This invention relates to compounds for the inhibition of histone deacetylase More particularly, the invention provides for compounds of formula (I): wherein A, B, D, E, X1, X2, X3, X4 and n are as defined in the specification A method of inhibiting histone deacetylase in a cell, the method comprising contacting the cell with a compound of formula (I), in an amount sufficient to inhibit histone deacetylase, is also disclosed.

7. 发明公开

EP1863804A1 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：EP1863804A1
公开(公告)日：2007-12-12
申请号：EP06741367.4
申请日：2006-03-31
申请人： Methylgene, Inc.
发明人： LEIT DE MORADEI, Silvana, Marcela , TESSIER, Pierre , SMIL, David , WAHHAB, Amal , DEZIEL, Robert , MANKU, Sukhdev , MANCUSO, John , THERRIEN, Eric , ALLAN, Martin , CHANTIGNY, Yves, Andre , AJAMIAN, Alain , BEAULIEU, Patrick
IPC分类号： C07D417/04 , A61K31/18 , A61K31/66 , A61K31/195 , A61K31/34 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/505 , C07C237/38 , C07C311/21 , C07C323/33 , C07C323/60 , C07D207/16
CPC分类号： C07D209/14 , C07C237/22 , C07C309/51 , C07C311/13 , C07C311/29 , C07C311/46 , C07C311/51 , C07C311/59 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/60 , C07C2601/14 , C07C2603/32 , C07D209/42 , C07D209/46 , C07D213/30 , C07D213/32 , C07D213/40 , C07D213/70 , C07D213/89 , C07D215/40 , C07D235/14 , C07D239/38 , C07D241/52 , C07D277/82 , C07D285/12 , C07D285/135 , C07D295/185 , C07D307/42 , C07D307/81 , C07D317/58 , C07D333/16 , C07D333/24 , C07D333/34 , C07D401/06 , C07D405/12 , C07D409/06 , C07D409/12
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I); wherein Y, L, Z, W, X, Q, R1, R2 and R3 are as defined in the specification.
摘要翻译：本发明涉及用于抑制组蛋白脱乙酰酶的化合物。更具体地说，本发明提供了式（I）的化合物; 其中Y，L，Z，W，X，Q，R1，R2和R3如说明书中所定义。

8. 发明公开

EP2137158A1 SMALL MOLECULE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASES (PRMTS) 审中-公开
标题翻译：蛋白质精氨酸甲基转移酶的小分子抑制剂（PRMTS）
公开(公告)号：EP2137158A1
公开(公告)日：2009-12-30
申请号：EP08714235.2
申请日：2008-02-28
申请人： MethylGene Inc.
发明人： WAHHAB, Amal , THERRIEN, Eric , ALLAN, Martin , MANKU, Sukhdev
IPC分类号： C07D231/14 , A61K31/415 , A61K31/435 , A61P31/00 , A61P35/00 , A61P37/00 , C07D211/26 , C07D231/22 , C07D235/18 , C07D401/00 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
CPC分类号： C07D409/04 , C07D211/26 , C07D231/14 , C07D231/22 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.
摘要翻译：本发明涉及用作蛋白质精氨酸甲基转移酶抑制剂的化合物，其具有选自式（I），式（II）和式（III）的结构式以及其外消旋混合物，非对映异构体，对映异构体和互变异构体以及N 如本文所定义的 - 氧化物，水合物，溶剂化物，药学上可接受的盐，前药和复合物。所述化合物可用作PRMT和/或CARM-1的抑制剂。本发明还涉及包含这些化合物的组合物及其使用方法。

9. 发明申请

WO2015179734A1 METHODS FOR MAKING CONJUGATES FROM DISULFIDE-CONTAINING PROTEINS 审中-公开
标题翻译：从含有蛋白质的蛋白质制备结合物的方法
公开(公告)号：WO2015179734A1
公开(公告)日：2015-11-26
申请号：PCT/US2015/032126
申请日：2015-05-22
申请人： NOVARTIS AG , HU, Qi-Ying , ALLAN, Martin
发明人： HU, Qi-Ying , ALLAN, Martin
IPC分类号： A61K47/48
CPC分类号： A61K38/05 , A61K47/68 , A61K47/6803 , A61K47/6849 , A61K47/6855
摘要： The invention provides methods to prepare protein conjugates from proteins having at least four accessible cysteine residues. In one embodiment, an antibody with four reducible disulfide linkages is reduced to provide four pairs of free cysteines. Each pair of free cysteines is reacted with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of each pair together though a 3-carbon tether with a reactive ketone. A pair of these reactive ketones are linked together with and used to attach a single payload molecule, thus conjugating the antibody to two payload groups. This method gives a stabilized antibody conjugate with high selectivity for a ratio of two payloads per antibody.
摘要翻译：本发明提供了从具有至少四个可及半胱氨酸残基的蛋白质制备蛋白质缀合物的方法。在一个实施方案中，减少具有四个可还原二硫键的抗体以提供四对游离半胱氨酸。每对游离半胱氨酸与1,3-二卤代丙酮或类似的反应物反应，每一对硫原子通过3-碳链与反应性酮连接在一起。一对这些反应性酮与一个有效载荷分子连接在一起并用于附着一个有效载荷分子，从而使抗体与两个有效负载组共轭。该方法给出了每抗体两种有效载体比例具有高选择性的稳定的抗体缀合物。

10. 发明申请

WO2013009564A1 TYROSINE LIGATION PROCESS 审中-公开
标题翻译：酪氨酸生物过程
公开(公告)号：WO2013009564A1
公开(公告)日：2013-01-17
申请号：PCT/US2012/045549
申请日：2012-07-05
申请人： NOVARTIS AG , ADAMO, Roberto , ALLAN, Martin , BERTI, Francesco , DANIELI, Elisa , HU, Qi-Ying
发明人： ADAMO, Roberto , ALLAN, Martin , BERTI, Francesco , DANIELI, Elisa , HU, Qi-Ying
IPC分类号： A61K47/48 , A61K39/02 , A61K39/00 , A61P31/00
CPC分类号： A61K47/4833 , A61K39/385 , A61K47/51 , A61K47/54 , A61K47/549 , A61K47/593 , A61K47/62 , A61K47/64 , A61K47/6415 , A61K47/646 , A61K2039/505
摘要： A process is provided for preparing a conjugate of Formula (I-A) or (I) comprising a polypeptide (or a protein) containing n number of tyrosine units, where n is an integer greater than or equal to 1, dispersed within the amino acid chain having an amino terminus end (A 1 ) and an acid terminus end (A 2 ) of the protein or polypeptide (either the amino or acid terminus end can be the at least one tyrosine unit) and having a weight average molecular weight equal to or greater than 10,000 Daltons (10 kDa), wherein the conjugate comprises a number m of tyrosine conjugates (modified tyrosine residues) as depicted in Formula (I-A) or (I), where m is at least one and is less than or equal to n: where X, Lg, L and R are as defined herein.
摘要翻译：提供了制备包含分散在氨基酸链中的n个大于或等于1的整数的n个酪氨酸单元的多肽（或蛋白质）的式（IA）或（I）的缀合物的方法，具有氨基末端（A1）和蛋白质或多肽的酸性末端（A2）（氨基酸或酸性末端可以是至少一个酪氨酸单元），并且其重均分子量等于或大于 10,000道尔顿（10kDa），其中所述缀合物包含数个m个如式（IA）或（I）所示的酪氨酸缀合物（修饰的酪氨酸残基），其中m为至少一个且小于或等于n：其中 X，Lg，L和R如本文所定义。

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