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1. 发明授权

US09227969B2 Compounds and compositions as inhibitors of MEK 有权
标题翻译：化合物和组合物作为MEK的抑制剂
公开(公告)号：US09227969B2
公开(公告)日：2016-01-05
申请号：US14451563
申请日：2014-08-05
申请人： Mark Gary Bock , Henrik Moebitz , Sunil Kumar Panigrahi , Ramulu Poddutoori , Susanta Samajdar
发明人： Mark Gary Bock , Henrik Moebitz , Sunil Kumar Panigrahi , Ramulu Poddutoori , Susanta Samajdar
IPC分类号： C07D471/04 , A61K31/53 , A61K31/4745 , A61K31/506 , A61K31/513 , A61K31/437 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4745 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/53 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
摘要翻译：本发明涉及式I化合物：其中n，R1，R2，R3a，R4和R5定义在发明概述中; 能够抑制MEK的活性。本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来控制过度增殖性疾病如癌症的方法。

2. 发明授权

US08466183B2 Modulators of sphingosine phosphate receptors 有权
公开(公告)号：US08466183B2
公开(公告)日：2013-06-18
申请号：US13605427
申请日：2012-09-06
申请人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： A61K31/4245 , C07D271/06
CPC分类号： C07D271/06 , A61K31/4245 , C07D263/32 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： Compounds of the following generic structure are provided: Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.

3. 发明申请

US20050222133A1 PROCESS FOR PREPARING PYRROLO[2, 1-C] [1,4] BENZODIAZEPINE HYBRIDS 有权
标题翻译：制备吡咯并[2,1-C] [1,4]苯并咪唑杂交物的方法
公开(公告)号：US20050222133A1
公开(公告)日：2005-10-06
申请号：US10812842
申请日：2004-03-30
申请人： Ahmed Kamal , Ramulu Poddutoori , Srinivas Olepu
发明人： Ahmed Kamal , Ramulu Poddutoori , Srinivas Olepu
IPC分类号： A61K31/55 , A61K31/551 , A61P35/00 , C07D487/00 , C07D487/02 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as DNA sequence selective agents which are useful as potential antitumour agents. In particular, the present invention relates to a process for the preparation of new pyrrolo [2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. These compounds have the formula XIV shown below:
摘要翻译：新颖的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物以及制备新的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物的方法是不合适的。更具体地说，本发明涉及一种制备新吡咯并[2,1-c] [1,4]苯并二氮杂杂环的方法，作为可用作潜在抗肿瘤剂的DNA序列选择剂。特别地，本发明涉及制备新的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物作为潜在的抗肿瘤剂的方法。这些化合物具有如下的式XIV：

4. 发明授权

US08470878B2 Heterocyclic sulfonamide derivatives 失效
标题翻译：杂环磺酰胺衍生物
公开(公告)号：US08470878B2
公开(公告)日：2013-06-25
申请号：US13491205
申请日：2012-06-07
申请人： Ramulu Poddutoori , Can Wang , Xianglin Zhao
发明人： Ramulu Poddutoori , Can Wang , Xianglin Zhao
IPC分类号： A61K31/343 , C07D307/79
CPC分类号： A61K45/06 , C07D307/79
摘要： The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.
摘要翻译：本发明涉及化合物及其药学上可接受的盐。这些化合物已被证明是MEK的抑制剂，因此可用于治疗过度增殖性疾病如癌症和炎症。

5. 发明申请

US20120329839A1 NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS 有权
标题翻译：磷酸肌磷酸受体的新型调节剂
公开(公告)号：US20120329839A1
公开(公告)日：2012-12-27
申请号：US13605427
申请日：2012-09-06
申请人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： A61K31/4245 , A61P11/00 , A61P37/06 , C07D271/06 , A61P25/00
CPC分类号： C07D271/06 , A61K31/4245 , C07D263/32 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
摘要翻译：提供激活亚型1的鞘氨醇-1-磷酸受体的化合物。某些化合物选择性地激活了关于鞘氨醇 - 1-磷酸受体亚型3的受体亚型1。本发明化合物的用途和方法用于治疗病症，其中在医学上指示S1P1的活化，激动，抑制或拮抗作用。

6. 发明授权

US06800622B1 Pyrene-linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids useful as anti-cancer agents 有权
标题翻译：芘连接的吡咯并[2,1-c] [1,4]苯并二氮杂杂环用作抗癌剂
公开(公告)号：US06800622B1
公开(公告)日：2004-10-05
申请号：US10396129
申请日：2003-03-25
申请人： Ahmed Kamal , Ramesh Gujjar , Ramulu Poddutoori , Srinivas Olepu
发明人： Ahmed Kamal , Ramesh Gujjar , Ramulu Poddutoori , Srinivas Olepu
IPC分类号： C07D48700
CPC分类号： C07D487/04 , A61K31/551
摘要： The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[N-(1″-pyrenyl)-alkane-3′-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, anticancer (antitumour) activity. The structural formula of this novel pyrrolo[2,1-c][1,4]benzodiazepine is given below:
摘要翻译：本发明涉及一种制备用作抗肿瘤剂的新型吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物的方法。本发明还涉及制备新的吡咯并[2,1-c] [1,4]苯并二氮杂作为潜在抗肿瘤剂的方法。更具体地，其提供了制备7-甲氧基-8- [N-（1“ - 芘基） - 烷烃-3'-甲酰胺] - 氧 - （11aS）-1,2,3,11a- 四联吡咯并吡喃并[2,1-c] [1,4]苯并二氮杂-酮，这些化合物具有脂肪族链长度变化，并且还描述了DNA结合，抗癌（抗肿瘤）活性。该新型吡咯并[2,1-c] [1,4]苯并二氮杂的结构式如下：

7. 发明授权

US06362331B1 Process for the preparation of antitumor agents 有权
标题翻译：制备抗肿瘤剂的方法
公开(公告)号：US06362331B1
公开(公告)日：2002-03-26
申请号：US09822782
申请日：2001-03-30
申请人： Ahmed Kamal , Chakravarthy Laxman Nallan , Ramesh Gujjar , Ramulu Poddutoori , Srinivas Olepu
发明人： Ahmed Kamal , Chakravarthy Laxman Nallan , Ramesh Gujjar , Ramulu Poddutoori , Srinivas Olepu
IPC分类号： C07D51900
CPC分类号： C07D519/00
摘要： The present invention provides a process for the preparation of a novel pyrrolo[2,1-c][1,4]benzodiazepine of formula VI wherein R is H, OII, OAc and R1 is H, and n is 3 to 5, by reacting (2S)-N-[4-hydroxy-5-methoxy-2-nitrobenzyl]-pyrrolidine-2-carboxy-carbaldehyde diethyl thioacetal with a dibromoalkane, isolating (2S)-N-[4-(3-bromoalkoxy)-5-methoxy-2-nitrobenzoyl]pyrrolidine-2-carboxy carbaldehyde diethyl thioacetal so formed and reacting the isolate with a dilactam, isolating 8-{[(2S)-N-5-methoxy-2-nitrobenzoyl]pyrrolidin-2-carbaldehyde diethylthioacetal}-alkoxy-7-methoxy-2,3,5,10,11,11a-hydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11 dione, reducing the above nitro compound, isolating the 8-{[(2S)-N-5-methoxy-2-aminobenzoyl]pyrrolidin-2-carbaldehyde diethylthioacetal]-alkoxy-7-methoxy-2,3,5,10,11,11a-hydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione, reacting the amino compound above with a deprotecting agent to obtain the pyrrolo[2,1-c][1,4]benzodiazepines of formula VI wherein R, R1 and n are as stated above.
摘要翻译：本发明提供制备式Ⅵ的新型吡咯并[2,1-c] [1,4]苯并二氮杂的方法，其中R为H，OII，OAc和R 1为H，n为3至5，通过反应（2S）-N- [4-羟基-5-甲氧基-2-硝基苄基] - 吡咯烷-2-羧基 - 甲醛二乙基硫代缩醛与二溴烷烃，分离（2S）-N- [4-（3-溴烷氧基）-5 - 甲氧基-2-硝基苯甲酰基]吡咯烷-2-羧基甲醛二乙基硫代缩醛，并使分离物与二酰胺反应，分离8 - {[（2S）-N-5-甲氧基-2-硝基苯甲酰基]吡咯烷-2-甲醛二乙硫基缩醛 } - 烷氧基-7-甲氧基-2,3,5,10,11,11a-氢-1H-吡咯并[2,1-c] [1,4]苯并二氮杂-5,11-二酮，还原上述硝基化合物，分离8 - {[（2S）-N-5-甲氧基-2-氨基苯甲酰基]吡咯烷-2-甲醛二乙硫基缩醛] - 烷氧基-7-甲氧基-2,3,5,10,11,11a-氢-1H- 吡咯并[2,1-c] [1,4]苯并二氮杂-5,11-二酮，使上述氨基化合物与脱保护剂反应，得到式VI的吡咯并[2,1-c] [1,4]苯并二氮杂其中 R，R1和n如上所述。

8. 发明授权

US08530503B2 Modulators of sphingosine phosphate receptors 有权
标题翻译：磷酸肌酐受体的调节剂
公开(公告)号：US08530503B2
公开(公告)日：2013-09-10
申请号：US13605358
申请日：2012-09-06
申请人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： A61K31/4245 , C07D271/06
CPC分类号： C07D271/06 , A61K31/4245 , C07D263/32 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： Compounds of the following generic structure are provided: Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.
摘要翻译：提供以下通用结构的化合物：这样的化合物活化亚型1（S1P1）的鞘氨醇-1-磷酸受体，并且可用于治疗由S1P1活化介导的病态。更具体地，这些化合物有益于治疗例如多发性硬化，移植排斥和/或成人呼吸综合征。

9. 发明申请

US20120329838A1 NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS 有权
公开(公告)号：US20120329838A1
公开(公告)日：2012-12-27
申请号：US13605358
申请日：2012-09-06
申请人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： C07D271/06 , A61P37/06 , A61P25/00 , A61P11/00 , A61K31/4245 , C12N5/071
CPC分类号： C07D271/06 , A61K31/4245 , C07D263/32 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

10. 发明申请

US20050222132A1 C8 - linked pyrrolo[2,1-c][1,4]benzodiazepine-acridone/acridine hybrids 失效
标题翻译： C8-连接的吡咯并[2,1-c] [1,4]苯并二氮杂吖啶酮/吖啶杂合物
公开(公告)号：US20050222132A1
公开(公告)日：2005-10-06
申请号：US10812841
申请日：2004-03-30
申请人： Ahmed Kamal , Srinivas Olepu , Ramulu Poddutoori , Ramesh Gujjar , Praveen Pogula
发明人： Ahmed Kamal , Srinivas Olepu , Ramulu Poddutoori , Ramesh Gujjar , Praveen Pogula
IPC分类号： A61K31/551 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides novel pyrrolo-[2,1-c][1,4]benzodiazepine hybrids useful as anti-tumour agents and a process for the preparation thereof.
摘要翻译：本发明提供了可用作抗肿瘤剂的新颖的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物及其制备方法。

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