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1. 发明授权

US5773474A Potent inducers of terminal differentiation and method of use thereof 失效
标题翻译：终末分化的潜在诱导剂及其使用方法
公开(公告)号：US5773474A
公开(公告)日：1998-06-30
申请号：US485620
申请日：1995-06-07
申请人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind
发明人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind
IPC分类号： C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D239/62 , C07D243/08 , A61K31/165
CPC分类号： C07D239/62 , C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D243/08
摘要： The invention provides a class of compounds and compositions thereof having the structure: ##STR1## wherein A is: ##STR2## The invention also concerns a method of selectively inducing terminal differentiation of neoplastic cells thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable conditions with an amount of the compound to selectively induce terminal differentiation. It also provides a method of treating a patient having a tumor characterized by proliferatoin of neoplastic cells comprising administration of an amount of the compound effective to inhibit proliferation and suppress oncogenicity of neoplastic cells.
摘要翻译：本发明提供了一类具有以下结构的化合物及其组合物：其中A为：本发明还涉及选择性诱导肿瘤细胞的终末分化从而抑制这种细胞增殖的方法，其包括使细胞下合适的条件与一定量的化合物选择性诱导终末分化。它还提供了一种治疗具有特征在于肿瘤细胞增殖物的肿瘤的患者的方法，包括施用一定量的有效抑制增殖的化合物并抑制肿瘤细胞的致癌性。

2. 发明授权

US07199134B2 Hydroxamic acid compounds and methods of use thereof 失效
公开(公告)号：US07199134B2
公开(公告)日：2007-04-03
申请号：US10817688
申请日：2004-04-01
申请人： Ronald Breslow , Thomas A. Miller , Sandro Belvedere , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
发明人： Ronald Breslow , Thomas A. Miller , Sandro Belvedere , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
IPC分类号： C07D215/38 , C07D215/36 , A61K31/47 , A61K31/44
CPC分类号： C07D211/02 , C07D215/38 , C07D401/12
摘要： The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

3. 发明授权

US07124068B2 Crystal structure of a deacetylase and inhibitors thereof 失效
公开(公告)号：US07124068B2
公开(公告)日：2006-10-17
申请号：US10095109
申请日：2002-03-08
申请人： Nikola Pavletich , Michael Finnin , Jill Donigian , Victoria M. Richon , Richard A. Rifkind , Paul A. Marks , Ronald Breslow
发明人： Nikola Pavletich , Michael Finnin , Jill Donigian , Victoria M. Richon , Richard A. Rifkind , Paul A. Marks , Ronald Breslow
IPC分类号： G06G7/48
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.

4. 发明授权

US6087367A Potent inducers of terminal differentiation and methods of use thereof 失效
标题翻译：终末分化的潜在诱导剂及其使用方法
公开(公告)号：US6087367A
公开(公告)日：2000-07-11
申请号：US314195
申请日：1999-05-18
申请人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind , Branko Jursic
发明人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind , Branko Jursic
IPC分类号： C07D295/18 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/167 , A61K31/192 , A61K31/197 , A61K31/20 , A61K31/216 , A61K31/221 , A61K31/275 , A61K31/277 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/4453 , A61K31/52 , A61P35/00 , A61P35/02 , A61P43/00 , C07C229/24 , C07C229/30 , C07C233/05 , C07C233/06 , C07C233/07 , C07C233/15 , C07C233/25 , C07C233/34 , C07C233/36 , C07C233/43 , C07C233/54 , C07C233/64 , C07C233/92 , C07C237/04 , C07C237/42 , C07C255/19 , C07C255/42 , C07C255/44 , C07C255/60 , C07C259/06 , C07C259/08 , C07C259/10 , C07C271/10 , C07C271/28 , C07C275/28 , C07D211/16 , C07D211/26 , C07D211/32 , C07D213/56 , C07D213/75 , C07D277/02 , C07D277/20 , C07D277/44 , C07D277/46 , C07D295/185 , C07D487/04 , C07D519/00 , A01N43/90 , A01N37/18 , A01N43/40
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 , C07D211/32 , C07D277/46 , C07D295/185 , C07C2101/14
摘要： The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 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 R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 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 invention 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终末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。

5. 发明授权

US5668179A Potent inducers of terminal differentiation and method of use thereof 失效
标题翻译：终末分化的潜在诱导剂及其使用方法
公开(公告)号：US5668179A
公开(公告)日：1997-09-16
申请号：US485619
申请日：1995-06-07
申请人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind
发明人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind
IPC分类号： C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D239/62 , C07D243/08 , A61K31/16
CPC分类号： C07D239/62 , C07C233/05 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07D231/32 , C07D243/08
摘要： The invention also concerns a method of selectively inducing terminal 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 effect 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.
摘要翻译：其中R，R 1和R 4各自为氢原子或甲基，乙基或丙基，R和R 1相同，R和R 4相同或不同; 本发明还涉及一种选择性诱导肿瘤细胞的终末分化并从而抑制这些细胞增殖的方法，其包括在合适条件下将细胞与一定量的化合物作用选择性地接触诱导终末分化。此外，本发明提供了一种治疗肿瘤特征在于肿瘤细胞增殖的患者的方法，其包括给予患者一定量的有效选择性诱导这些肿瘤细胞的终末分化，从而抑制其增殖并抑制致癌性的化合物。最后，本发明提供一种药物组合物，其包含药学上可接受的载体和化合物，其量有效量小于在患者中引起毒性的量。

6. 发明授权

US5700811A Potent inducers of terminal differentiation and method of use thereof 失效
标题翻译：终末分化的潜在诱导剂及其使用方法
公开(公告)号：US5700811A
公开(公告)日：1997-12-23
申请号：US246363
申请日：1994-05-19
申请人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind
发明人： Ronald Breslow , Paul A. Marks , Richard A. Rifkind
IPC分类号： C07D295/18 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/167 , A61K31/192 , A61K31/197 , A61K31/20 , A61K31/216 , A61K31/221 , A61K31/275 , A61K31/277 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/4453 , A61K31/52 , A61P35/00 , A61P35/02 , A61P43/00 , C07C229/24 , C07C229/30 , C07C233/05 , C07C233/06 , C07C233/07 , C07C233/15 , C07C233/25 , C07C233/34 , C07C233/36 , C07C233/43 , C07C233/54 , C07C233/64 , C07C233/92 , C07C237/04 , C07C237/42 , C07C255/19 , C07C255/42 , C07C255/44 , C07C255/60 , C07C259/06 , C07C259/08 , C07C259/10 , C07C271/10 , C07C271/28 , C07C275/28 , C07D211/16 , C07D211/26 , C07D211/32 , C07D213/56 , C07D213/75 , C07D277/02 , C07D277/20 , C07D277/44 , C07D277/46 , C07D295/185 , C07D487/04 , C07D519/00 , A01N43/90 , A01N43/42 , C07C233/00 , C07D277/04
CPC分类号： C07D295/185 , A61K31/16 , A61K31/164 , 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 , C07D211/32 , C07D213/75 , C07D277/46 , C07C2101/14
摘要： This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及具有以下结构的化合物：其中R 1和R 2彼此独立地相同或不同; 当R 1和R 2相同时，各自为取代或未取代的芳氨基，环烷基氨基，吡啶氨基，哌啶子基，9-嘌呤-6-胺或噻唑氨基; 当R1和R2不同时，R1 = R3-N-R4，n为约4至约8的整数。本发明还提供选择性诱导肿瘤细胞的终末分化，从而抑制这些细胞增殖的方法。本发明还提供包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。

7. 发明授权

US5608108A Potent inducers of terminal differentiation and method of use thereof 失效
标题翻译：终末分化的潜在诱导剂及其使用方法
公开(公告)号：US5608108A
公开(公告)日：1997-03-04
申请号：US424556
申请日：1995-04-17
申请人： Paul A. Marks , Richard A. Rifkind , Ronald Breslow , Branko Jursic
发明人： Paul A. Marks , Richard A. Rifkind , Ronald Breslow , Branko Jursic
IPC分类号： C07C233/05 , C07C233/07 , C07C233/36 , C07C235/74 , C07C243/28 , C07C259/06 , C07C259/08 , C07C259/10 , C07D231/32 , C07D231/36 , C07D239/60 , C07D239/62 , C07D243/08 , A61K31/19
CPC分类号： C07C235/74 , C07C233/05 , C07C233/07 , C07C233/36 , C07C243/28 , C07C259/06 , C07C259/08 , C07C259/10 , C07D231/32 , C07D231/36 , C07D239/60 , 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 effect 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.
摘要翻译：本发明提供化合物，其中几种属于具有两个或更多个非极性组分的类，其通过极性基团连接并且在化合物的末端具有极性基团。本发明还包括选择性诱导肿瘤细胞的终末分化并从而抑制这些细胞增殖的方法，其包括在合适条件下使细胞与一定量的化合物效应接触以选择性诱导终末分化。此外，本发明提供了一种治疗肿瘤特征在于肿瘤细胞增殖的患者的方法，其包括给予患者一定量的有效选择性诱导这些肿瘤细胞的终末分化，从而抑制其增殖并抑制致癌性的化合物。最后，本发明提供一种药物组合物，其包含药学上可接受的载体和化合物，其量有效量小于在患者中引起毒性的量。

8. 发明授权

US5330744A Method for increasing sensitivity to chemically induced terminal differentiation 失效
标题翻译：增加化学诱导终末分化敏感性的方法
公开(公告)号：US5330744A
公开(公告)日：1994-07-19
申请号：US270643
申请日：1988-11-14
申请人： Sandro Pontremoli , Ronald Breslow , Paul A. Marks , Richard A. Rifkind
发明人： Sandro Pontremoli , Ronald Breslow , Paul A. Marks , Richard A. Rifkind
IPC分类号： A61K31/16 , A61K31/475 , A61K49/00 , A61K31/205
CPC分类号： A61K31/475 , A61K31/16
摘要： The present invention provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises treating the cells so as to render them resistant to an antitumor agent and contacting the resulting resistant cells under suitable conditions with an amount of a compound effective to selectively induce terminal differentiation of such cells. The compound has a structure:[R-A ]-B-[A.sub.1 -B.sub.1 -].sub.a [A.sub.2 -B.sub.2 -].sub.b [A.sub.3 -R.sub.1 ].The invention also concerns a method of treating a patient having a tumor characterized by proliferation of neoplastic which comprises administering to the patient an amount of an antitumor agent to render the cells resistant to the antitumor agent and subsequently administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells and thereby inhibit their proliferation.
摘要翻译：本发明提供了选择性诱导肿瘤细胞的终末分化并由此抑制这些细胞增殖的方法，包括治疗细胞以使其对抗肿瘤剂具有抗性，并在合适的条件下使得到的抗性细胞与一定量的有效选择性诱导这些细胞的终末分化的化合物。化合物具有以下结构：[R-A] -B- [A1-B1-] a [A2-B2-] b [A3-R1]。本发明还涉及一种治疗具有以肿瘤增殖为特征的肿瘤的患者的方法，其包括向患者施用一定量的抗肿瘤剂以使细胞对抗肿瘤剂具有抗性，并且随后向患者施用一定量的化合物有效地选择性诱导这些肿瘤细胞的末端分化，从而抑制其增殖。

9. 发明授权

US09499479B2 Molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1 有权
公开(公告)号：US09499479B2
公开(公告)日：2016-11-22
申请号：US14349291
申请日：2012-10-03
申请人： Ronald Breslow , Paul A. Marks
发明人： Ronald Breslow , Paul A. Marks
IPC分类号： C07C25/10 , C07C259/08 , C07C259/10 , C07D215/40 , C07D235/06 , C07D209/08 , C07D209/18 , C07C259/06 , C07C275/64 , C07D209/24 , C07D209/42 , C07D215/06
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-β-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.

10. 发明授权

US07345174B2 Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof 有权
标题翻译：细胞分化剂和组蛋白脱乙酰酶抑制剂及其使用方法
公开(公告)号：US07345174B2
公开(公告)日：2008-03-18
申请号：US11474043
申请日：2006-06-22
申请人： Ronald Breslow , Sandro Belvedere , Leland Gershell , Thomas A. Miller , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
发明人： Ronald Breslow , Sandro Belvedere , Leland Gershell , Thomas A. Miller , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
IPC分类号： C07D221/02 , C07D211/00 , C07D211/60 , C07C233/60 , A61K31/02 , A61K31/12 , A61K31/22
CPC分类号： C07D213/75 , C07C233/07 , C07C233/13 , C07C235/74 , C07C237/12 , C07C237/22 , C07C259/06 , C07C271/22 , C07C311/03 , C07C311/06 , C07C311/42 , C07C327/32 , C07C2601/14 , C07D213/82 , C07D215/38 , C07D215/40 , C07D215/54 , C07D231/12 , C07D231/40 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/46 , C07D333/38 , C07F9/2458 , C07F9/4465
摘要： The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention 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：本发明提供具有下式的化合物：其中R 1和R 2各自为取代或未取代的芳基，环烷基，环烷基氨基，石脑油，吡啶氨基，哌啶子基，叔丁基，芳氧基，芳基烷氧基或吡啶基; 其中A是酰氨基部分，-O - ， - S - ， - NH-或-CH 2 - 。并且其中n为3至8的整数。本发明还提供了选择性诱导肿瘤细胞的生长停滞，末端分化和/或凋亡并从而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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