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1. 发明公开

EP2571352A1 SELECTIVE HDAC INHIBITORS 审中-公开
标题翻译：选择性HDAC抑制剂
公开(公告)号：EP2571352A1
公开(公告)日：2013-03-27
申请号：EP11784333.4
申请日：2011-05-20
申请人： Sloan-Kettering Institute for Cancer Research , Sloan-kettering Institute For Cancer Research
发明人： BRESLOW, Ronald , MARKS, Paul, A. , ABHILASH, K., G. , WANG, Jianing
IPC分类号： A01N37/18
CPC分类号： C07C235/74 , C07C233/54 , C07C237/22 , C07C259/06 , C07C2601/08 , C07C2602/26 , C07D215/08 , C07D215/40 , C07D333/38 , C07D401/12 , C07D403/12 , C07D405/12
摘要： This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.

3. 发明授权

EP1443928B1 TREATMENT OF NEURODEGENERATIVE DISEASES AND CANCER OF THE BRAIN 有权
标题翻译：神经退行性疾病的治疗和癌症的脑
公开(公告)号：EP1443928B1
公开(公告)日：2011-07-27
申请号：EP02778601.1
申请日：2002-10-16
申请人： Sloan-Kettering Institute For Cancer Research
发明人： RICHON, Victoria, M. , MARKS, Paul, A. , RIFKIND, Richard, A.
IPC分类号： A61K31/47 , A61K31/166 , A61K31/167 , A61K31/19 , A61K31/4406 , A61K31/4709 , A61P35/00
CPC分类号： A61K31/16 , A61K31/00 , A61K31/166 , A61K31/167 , A61K31/19 , A61K31/4406 , A61K31/47 , A61K31/4709
摘要： The present application is directed to a method of inhibiting HDAC in the brain of a mammal. The method comprises administering to a mammal a HDAC inhibiting amount of a histone deacetylase inhibitor compound. The present application is further directed to a method of treating diseases of the central nervous system (CNS) comprising administering to a individual in need of treatment a therapeutically effective amount of an inhibitor of HDAC. In particular embodiments, the CNS disease is a neurodegenerative disease. In further embodiments, the neurogenerative disease is an inherited neurodegenerative disease, such as those inherited neurodegenerative diseases which are polyglutamine expansion diseases. In other embodiments, the disorder is cancer of the brain. The individual is a mammal, such as a primate or human.

4. 发明授权

EP0594577B1 NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHOD OF USE THEREOF 失效转让
标题翻译：新的高效电感终末分化及使用方法
公开(公告)号：EP0594577B1
公开(公告)日：1998-12-30
申请号：EP91901442.3
申请日：1990-11-14
申请人： Sloan-Kettering Institute For Cancer Research , THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
发明人： MARKS, Paul, A. , RIFKIND, Richard, A. , BRESLOW, Ronald , JURSIC, Branko
IPC分类号： C07C69/34 , C07C229/24 , C07C233/04 , C07C235/20 , A61K31/22
CPC分类号： C07C233/36 , C07C233/05 , C07C233/07 , C07C243/28 , C07C259/06 , C07C259/08 , C07D231/32 , C07D239/62 , C07D243/08
摘要： The invention provides compounds, several of which belong to a class having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concents a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effective to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound in an amount effective less than an amount which would cause toxicity in the patient.

5. 发明授权

EP2451451B1 HDAC 6 INHIBITOR-BASED METHODS FOR TREATING CANCER 失效转让
标题翻译：基于过程FOR HDAC抑制剂6癌症治疗
公开(公告)号：EP2451451B1
公开(公告)日：2016-08-17
申请号：EP10797676.3
申请日：2010-07-02
申请人： Sloan-Kettering Institute for Cancer Research
发明人： MARKS, Paul, A. , NAMDAR, Mandana , XU, Weisheng
IPC分类号： A61K31/19 , A61K31/167 , A61K31/422 , A61K31/704 , A61K31/7048 , A61K45/06 , A61P35/00
CPC分类号： A61K31/704 , A61K31/167 , A61K31/19 , A61K31/422 , A61K31/7048 , A61K45/06 , A61K2300/00

6. 发明公开

EP0594577A1 NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHOD OF USE THEREOF 失效转让
标题翻译：新的有效因子来诱导终末分化和它们的用途。
公开(公告)号：EP0594577A1
公开(公告)日：1994-05-04
申请号：EP91901442.0
申请日：1990-11-14
申请人： Sloan-Kettering Institute For Cancer Research , THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
发明人： MARKS, Paul, A. , RIFKIND, Richard, A. , BRESLOW, Ronald , JURSIC, Branko
IPC分类号： A61K31 , A61P35 , C07C69 , C07C229 , C07C233 , C07C235 , C07C243 , C07C259 , C07D231 , C07D239 , C07D243
CPC分类号： C07C233/36 , C07C233/05 , C07C233/07 , C07C243/28 , C07C259/06 , C07C259/08 , C07D231/32 , C07D239/62 , C07D243/08
摘要： Sont décrits des composés dont certains appartiennent à une classe présentant deux composants non polaires ou plus, connectés par un groupe polaire et dotés de groupes polaires aux terminaisons du composé. L'invention concerne également un procédé d'induction sélective d'une différenciation de terminaisons de cellules néoplastiques, et par conséquent d'inhibition de la prolifération desdites cellules, consistant à mettre en contact les cellules dans des conditions adaptées, avec une quantité du composé suffisante pour induire sélectivement une différenciation de terminaisons. De plus, l'invention concerne un procédé de traitement d'un patient présentant une tumeur caractérisée par la prolifération de cellules néoplastiques, consistant à administrer au patient une dose du composant suffisante pour induire sélectivement la différenciation des terminaisons desdites cellules néoplastiques, inhibant ainsi leur prolifération et supprimant l'oncogénicité. En outre, l'invention concerne une préparation pharmaceutique comprenant un excipient acceptable en pharmacologie, ainsi que le composé en une dose efficace, inférieure à une dose susceptible de provoquer une toxicité chez le patient.

7. 发明公开

EP2763531A1 NOVEL MOLECULES THAT SELECTIVELY INHIBIT HISTONE DEACETYLASE 6 RELATIVE TO HISTONE DEACETYLASE 1 审中-公开
标题翻译：的新分子FOR组蛋白脱乙酰6的相对于组蛋白脱乙酰1选择性抑制
公开(公告)号：EP2763531A1
公开(公告)日：2014-08-13
申请号：EP12838935.0
申请日：2012-10-03
申请人： The Trustees of Columbia University in the City of New York , Sloan Kettering Institute For Cancer Research
发明人： BRESLOW, Ronald , MARKS, Paul, A.
IPC分类号： A01N37/18
CPC分类号： C07C259/10 , C07C259/06 , C07C275/64 , C07C2602/10 , C07D209/08 , C07D209/18 , C07D209/24 , C07D209/42 , C07D215/06 , C07D215/40 , C07D235/06
摘要： This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(═O)—R6, —NH—C(═O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(═S)R7, —C(═O)—NR5R6, —CH2—C(═O)—NR5R6, —C(═NR5)R6, —P(═O)(OR5)(OR6), —P(OR5)(OR6), —C(═S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(═O)OR8, C(═O)R8, —C(═O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present or absent, and when present is —O—, —S—, —CH2—, —C(O)——NH—, —NH—NH—, —NHC(═O)—, —C(═O)NH—, —NHC(═O)CH2NH—, —NHC(═O)CH2C(═O)—, —N(OH)—, —CH2CH2— or —NHC(═O)CH═CH—; and R4 is alkyl, —OR11 or —NH—OR11, wherein R11 is H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, aryl, heteroaryl, or heterocyclyl, and when Q is —Ar1—Z—, Z is absent, Ar1 is phenyl, R2 and R3 are H, n=1, and R4 is —NHOH, then R1 is other than carbazole, tetrahydro-&bgr;-carboline, tetrahydro-γ-carboline, —C(═O)—NR5R6 and —NR5—C(═O)—R6, wherein one of R5 or R6 is quinoline and the other of R5 or R6 is H; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有以下结构的化合物：其中R1是H，卤素，-NR 5 R 6，-NR 5 C（= O）-R 6，-NH-C（= O）-OR 7，-OR 7，-NO 2，-CN， -SR 7，-SO 2 R 7，-CO 2 R 7，CF 3，-SOR7，-POR7，-C（= S）R 7，-C（= O）-NR 5 R 6，-CH 2 -C（= O）-NR5R6，（-C═NR5 （）R 6，-P = O）（OR 5）（OR 6），P（OR 5）（OR 6）， - C（= S）R 7，C 1-5烷基，C 2-5烯基，C 2-5炔基，芳基，杂芳基，或杂环基，worin R5，R6，和R7和各自独立地为H，C 1-5烷基，C 2-5烯基，C 2-5炔基，杂烷基，环烷基，杂环，芳基或杂芳基; m是从0至2的整数; R2和R3是各自独立地为H，卤素，-NH 2，-CX 3，-C（= O）OR 8，C（= O）R8，-C（= O）NR 9 R 10，C 1-10烷基，C 2-10烯基，C 2-10炔基，杂烷基，芳基，杂芳基，或杂环基; 其中X是Cl，Br或F; R8，R9和R10各自独立地为H，C 1-5烷基，C 2-5烯基，C 2-5炔基，杂烷基，环烷基，杂环，芳基或杂芳基; Q是-Ar1-Z或-Z-AR1-Z，worin Ar 1是芳基或杂芳基; 和Z在每次出现时独立地为存在或不存在，并且当存在时是-O - ， - S - ， - CH 2 - ， - C（O） - NH - ， - NH-NH - ， - NHC（= O） - ，-C（= O）NH-，-NHC（= O）CH 2 NH-，-NHC（= O）CH 2 C（= O） - ， - N（OH） - ，-CH 2 CH 2或-NHC（= O）CH = CH-; 且R 4是烷基，-OR 11或-NH-OR11，R11 worin是H，C 1-10烷基，C 2-10烯基，C 2-10炔基，芳基，杂芳基，或杂环基，并且当Q是-Ar1-Z-， Z不存在; Ar 1为苯基，R 2和R 3是H，n = 1时，R4为-NHOH，那么R 1不是咔唑，四氢-β-咔啉，四氢γ咔啉，-C其他（= O） -NR5R6和-NR 5 C（= O）-R 6，worin R5或R6中的一个是喹啉和其它R5或R6是H; 或其药学上可接受的盐。

8. 发明授权

EP1212357B1 CRYSTAL STRUCTURE OF A DEACETYLASE AND INHIBITORS THEREOF 有权
标题翻译：晶体结构的脱乙酰基酶及其抑制剂的
公开(公告)号：EP1212357B1
公开(公告)日：2007-05-02
申请号：EP00968344.2
申请日：2000-09-08
申请人： Sloan-Kettering Institute For Cancer Research , The Trustees of Columbia University in the City of New York
发明人： PAVLETICH, Nikola , FINNIN, Michael , DONIGIAN, Jill , RICHON, Victoria , RIFKIND, Richard, A. , MARKS, Paul, A. , BRESLOW, Ronald
IPC分类号： C07K14/00 , C12N9/16 , G01N33/50
CPC分类号： C12N9/16
摘要： The present invention provides three-dimensional structural information from the hyperthermophilic bacterium Aquifex aeolicus which is a histone deacetylase-like protein (HDLP). HDLP shares 35.2% amino acid sequence identity with human histone deacetylase (HDAC1). The present invention further provides three-dimensional structural information of HDLP bound by inhibitor molecules. The three-dimensional structural information of the present invention is useful to design, isolate and screen deacetylase inhibitor compounds capable of inhibiting HDLP, HDAC family members and HDLP-related molecules. The invention also relates to nucleic acids encoding a mutant HDLP which facilitates the determination of the three-dimensional structure of HDLP in the presence of a zinc atom.

9. 发明公开

EP1667680A2 COMBINATION METHODS OF TREATING CANCER 审中-公开
标题翻译：复合体方法治疗癌症的
公开(公告)号：EP1667680A2
公开(公告)日：2006-06-14
申请号：EP04780925.6
申请日：2004-08-12
申请人： Aton Pharma, Inc. , Sloan-Kettering Institute For Cancer Research
发明人： BACOPOULOS, Nicholas G. , CHIAO, Judy, H. , MARKS, Paul, A. , MILLER, Thomas, A. , PARADISE, Carolyn, M. , RICHON, Victoria, M. , RIFKIND, Richard, A.
IPC分类号： A61K31/44 , A61K31/19
CPC分类号： A61K45/06 , A61K9/0019 , A61K31/167 , A61K31/19 , A61K31/522 , A61K31/57 , A61K31/7068 , A61K31/7072 , A61K38/00 , A61K2300/00
摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, in a first treatment procedure, and a second amount of an anti-cancer agent in a second treatment procedure. The first and second amounts together comprise a therapeutically effective amount. The effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

10. 发明授权

EP0642509B1 NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHODS OF USE THEREOF 有权转让
标题翻译： NEVER VERWENDUNG的NETEN POTENTE INDUKTOREN DER TERMINALEN DIFFERENZIERUNG
公开(公告)号：EP0642509B1
公开(公告)日：1999-08-11
申请号：EP92922033.3
申请日：1992-10-05
申请人： Sloan-Kettering Institute For Cancer Research , The Trustees of Columbia University in the City of New York
发明人： BRESLOW, Ronald , MARKS, Paul, A. , RIFKIND, Richard, A. , JURSIC, Branko
IPC分类号： C07D473/02 , C07D211/26 , C07D211/28 , C07D211/30 , C07D277/20 , C07D277/44 , C07D277/02 , C07C271/02 , C07C271/08 , C07C271/10 , C07D213/75 , C07D277/46 , C07D295/18 , C07C259/06 , C07C259/10 , C07C233/05 , C07C233/07 , A61K31/16 , A61K31/44 , A61K31/15
CPC分类号： C07D213/75 , A61K31/16 , A61K31/164 , A61K31/167 , A61K31/197 , A61K31/221 , A61K31/277 , A61K31/427 , A61K31/4453 , C07C233/05 , C07C233/06 , C07C233/07 , C07C233/15 , C07C233/25 , C07C233/36 , C07C233/43 , C07C233/54 , C07C233/92 , C07C237/42 , C07C255/42 , C07C255/44 , C07C255/60 , C07C259/06 , C07C259/08 , C07C259/10 , C07C275/28 , C07C2601/14 , C07D211/32 , C07D277/46 , C07D295/185
摘要： The present invention provides the compound having structure (I), wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1 = R3-N-R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present inventtion provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
摘要翻译：本发明提供具有以下结构的化合物：其中R1和R2各自独立地相同或不同; 当R 1和R 2相同时，各自为取代或未取代的芳基氨基，环烷基氨基，吡啶氨基，哌啶子基，9-嘌呤-6-胺或硫代唑氨基; 当R1和R2不同时，R1 = R3-N-R4，其中R3和R4各自独立地相同或不同，为氢原子，羟基，取代或未取代的支链或非支链烷基，烯基，环烷基，芳基，烷氧基，芳氧基，芳基烷氧基或吡啶基，或R3和R4键合在一起形成哌啶基，R2是羟基氨基，羟基，氨基，烷基氨基，二烷基氨基或烷氧基; 并且n为约4至约8的整数。本发明还提供了选择性诱导肿瘤细胞的末端分化并由此抑制这些细胞增殖的方法。此外，本发明提供了治疗具有以肿瘤细胞增殖为特征的肿瘤的患者的方法。最后，本发明提供包含药学上可接受的载体和治疗上可接受量的上述化合物的药物组合物。

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