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1. 发明授权

US5593970A Heterocyclic anthracycline analogs 失效
标题翻译：杂环蒽环类似物
公开(公告)号：US5593970A
公开(公告)日：1997-01-14
申请号：US263925
申请日：1994-06-20
申请人： Giorgio Attardo , Jean-Louis Kraus , Marc Courchesne , Serge Lamonthe , Jean-Fran.cedilla.ois Lavall ee , Elaine Lebeau , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Bernard Belleau, deceased
发明人： Giorgio Attardo , Jean-Louis Kraus , Marc Courchesne , Serge Lamonthe , Jean-Fran.cedilla.ois Lavall ee , Elaine Lebeau , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Bernard Belleau, deceased
IPC分类号： C07H3/06 , C07H15/244 , C07M15/24 , A61K31/70
CPC分类号： C07H15/244 , C07H3/06
摘要： Novel pyrano heterocyclic anthracycline derivatives are described, which are useful in the treatment of cancer and tumors, such as breast cancer, leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer, and melanoma. As well, these compounds may be used ex vivo for the treatment of cancerous bone marrow before retransplanting said marrow in a patient. Pharmaceutical compositions and methods of preparing the compounds are also described.
摘要翻译：描述了新的吡喃杂环蒽环类衍生物，其可用于治疗癌症和肿瘤，例如乳腺癌，白血病，肺癌，结肠癌，卵巢癌，肾癌和黑素瘤。同样，这些化合物也可以离体用于治疗癌性骨髓，然后再将患者骨髓再次移植。还描述了制备化合物的药物组合物和方法。

2. 发明授权

US5606037A Processes antineoplastic heteronaphthoquinones 失效
标题翻译：处理抗肿瘤异黄酮
公开(公告)号：US5606037A
公开(公告)日：1997-02-25
申请号：US401492
申请日：1995-03-10
申请人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavall ee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean L. Kraus
发明人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavall ee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean L. Kraus
IPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08 , C07H1/00 , C07C50/22
CPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08
摘要： This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.
摘要翻译：本发明涉及萘醌衍生物，制备这些衍生物的方法和中间体，以及这些衍生物作为哺乳动物抗肿瘤剂的用途。

3. 发明授权

US5736523A Antineoplastic heteronapthoquinones 失效
标题翻译：抗肿瘤异二氢醌
公开(公告)号：US5736523A
公开(公告)日：1998-04-07
申请号：US401493
申请日：1995-03-10
申请人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavallee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean Louis Kraus
发明人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavallee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean Louis Kraus
IPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08 , A61K31/70 , C07H15/24
CPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08
摘要： This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.
摘要翻译：本发明涉及萘醌衍生物，制备这些衍生物的方法和中间体，以及这些衍生物作为哺乳动物抗肿瘤剂的用途。

4. 发明授权

US06630488B1 Quinolizinones as integrin inhibitors 失效
标题翻译：喹诺酮类作为整联蛋白抑制剂
公开(公告)号：US06630488B1
公开(公告)日：2003-10-07
申请号：US09805780
申请日：2001-03-20
申请人： Serge Lamothe , Boulos Zacharie , Giorgio Attardo , Denis Labrecque , Marc Courchesne , Guy Falardeau , Rabindra Rej , Shaun Abbott
发明人： Serge Lamothe , Boulos Zacharie , Giorgio Attardo , Denis Labrecque , Marc Courchesne , Guy Falardeau , Rabindra Rej , Shaun Abbott
IPC分类号： C07D45502
CPC分类号： C07D455/02
摘要： The present invention is directed towards novel compounds that are effective inhibitors of integrins, particularly &agr;IIb&bgr;3 or &agr;v integrins such as &agr;v&bgr;3 and &agr;v&bgr;5. One embodiment of the present invention comprises a compound of formula (I) or formula (II) or a pharmaceutically acceptable salt, solvate, or metabolic precursor thereof. R1, R2, R3, and R4 are defined herein.
摘要翻译：本发明涉及作为整合素的有效抑制剂的新化合物，特别是αIIbbeta3或alphav整联蛋白，例如alphavbeta3和alphavbeta5。本发明的一个实施方案包括式（I）或式（II）化合物或其药学上可接受的盐，溶剂合物或代谢前体。 R1，R2，R3和R4在本文中定义。

5. 发明申请

US20050256034A1 Dioxolane analogs for improved inter-cellular delivery 审中-公开
标题翻译：二氧杂环戊烷类似物用于改善细胞内递送
公开(公告)号：US20050256034A1
公开(公告)日：2005-11-17
申请号：US11149193
申请日：2005-06-10
申请人： Giorgio Attardo , Boulos Zacharie , Rabindra Rej , Jean-Francois Lavallee , Louis Vaillancourt , Real Denis , Sophie Levesque
发明人： Giorgio Attardo , Boulos Zacharie , Rabindra Rej , Jean-Francois Lavallee , Louis Vaillancourt , Real Denis , Sophie Levesque
IPC分类号： A61K31/513 , A61K31/675 , A61K31/7068 , A61K38/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D405/04 , C07D405/14 , C07D473/18 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/06 , A61K38/16
CPC分类号： C07D405/04 , C07D473/18 , C07F9/65515 , C07F9/65586 , C07F9/65616
摘要： Dioxolane analogs of the following formula: wherein R1 and R2 are defined herein, are useful in the treatment of cancer. For example, the compounds can be used to treat patients with cancer in which the cancer cells are deficient in nucleoside or nucleoside base transporters.
摘要翻译：下式的二氧杂环戊烷类似物：其中R1和R2如本文所定义，可用于治疗癌症。例如，这些化合物可用于治疗癌细胞中核苷或核苷碱基转运蛋白缺乏的癌症患者。

6. 发明授权

US07476741B2 Substituted 4H-chromens, 2H-chromenes, chromans and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的4H-色素，2H-色烯，着色剂和类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US07476741B2
公开(公告)日：2009-01-13
申请号：US10514426
申请日：2003-05-16
申请人： Sui Xiong Cai , Songchun Jiang , Giorgio Attardo , Réal Denis , Richard Storer , Rabindra Rej
发明人： Sui Xiong Cai , Songchun Jiang , Giorgio Attardo , Réal Denis , Richard Storer , Rabindra Rej
IPC分类号： C07D405/00
CPC分类号： C07D311/04 , C07D311/74 , C07D311/76
摘要： The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R5, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及其中R5，A，B，X，Y，Z和虚线由本文定义的通式（I）表示的取代的4H-色烯，2H-色烯，色满及其类似物。本发明还涉及具有式（I）的化合物是胱天蛋白酶的激活剂和凋亡诱导剂的发现。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

7. 发明申请

US20050176750A1 Substituted 4h-chromens, 2h-chromenes, chromans and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：作为胱天蛋白酶的活化剂和细胞凋亡诱导剂的取代的4h-色调，2h-色烯，着色剂和类似物及其用途
公开(公告)号：US20050176750A1
公开(公告)日：2005-08-11
申请号：US10514426
申请日：2003-05-16
申请人： Sui Cai , Songchun Jiang , Giorgio Attardo , Real Denis , Richard Storer , Rabindra Rej
发明人： Sui Cai , Songchun Jiang , Giorgio Attardo , Real Denis , Richard Storer , Rabindra Rej
IPC分类号： A61K31/353 , A61K31/407 , A61K31/4188 , A61K31/4741 , C07D311/04 , C07D311/74 , C07D311/76
CPC分类号： C07D311/04 , C07D311/74 , C07D311/76
摘要： The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R5, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及由通式（I）表示的取代的4H-色烯，2H-色烯，着色剂及其类似物，其中R 5，A，B，X，Y，Z和虚线线条在本文中定义。本发明还涉及具有式（I）的化合物是胱天蛋白酶的激活剂和凋亡诱导剂的发现。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

8. 发明申请

US20120164103A1 Compounds and Methods for the Treatment or Prevention of Flavivirus Infections 失效
标题翻译：用于治疗或预防黄病毒感染的化合物和方法
公开(公告)号：US20120164103A1
公开(公告)日：2012-06-28
申请号：US13416565
申请日：2012-03-09
申请人： Real Denis , Carl Poisson , Sanjoy Kumar Das , Irina Motorina , Rabindra Rej , Constantin G. Yannopoulos , Laval Chan Chun Kong
发明人： Real Denis , Carl Poisson , Sanjoy Kumar Das , Irina Motorina , Rabindra Rej , Constantin G. Yannopoulos , Laval Chan Chun Kong
IPC分类号： A61K31/381 , C07D413/12 , C07D409/12 , C07D409/14 , A61K31/5377 , A61K31/4196 , A61K31/4535 , A61K31/41 , A61K31/4184 , A61K31/506 , A61K31/4545 , A61K39/00 , A61K31/7088 , A61K38/21 , A61K38/20 , A61K38/13 , A61K31/7056 , A61K38/22 , A61K39/12 , A61P31/14 , C07D409/08 , C07D471/04 , A61K31/437 , A61K36/28 , A61K31/7105 , A61P37/04 , A61P1/16 , A61P37/02 , C07D333/38
CPC分类号： C07D471/04 , C07D333/38 , C07D409/04 , C07D409/12 , C07D409/14
摘要： Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.
摘要翻译：由式I表示的化合物或其药学上可接受的盐和溶剂化物，其中R 1，X，Y，Y 1和Z如本文所定义，可用于治疗黄病毒科病毒感染。

9. 发明授权

US06444656B1 Antiviral phosphonate nucleotides 失效
标题翻译：抗病毒膦酸核苷酸
公开(公告)号：US06444656B1
公开(公告)日：2002-09-03
申请号：US09534490
申请日：2000-03-24
申请人： Nghe Nguyen-Ba , Rabindra Rej
发明人： Nghe Nguyen-Ba , Rabindra Rej
IPC分类号： A61K31525
CPC分类号： C07H15/04 , C07H19/04 , C07H19/06 , C07H19/16
摘要： The present invention relates to a novel nucleotide analogue having the general formula (I) and pharmaceutically acceptable salts, esters, or salt of such esters: wherein n, X, Q U R1′, R1, Z and R2 are defined here within. The compounds object of the present invention may be a single enantiomers or as mixtures of said enantiomers, the compounds may have a &agr;D, &agr;-L, &bgr;-D, &bgr;-L, R or S configuration at each chiral center or mixtures thereof. This invention also relates to pharmaceutical compositions containing them, alone or in combination with other therapeutic agents, and their use as antiviral agents, particularly against HIV and/or HBV infections in mammals.
摘要翻译：本发明涉及具有通式（I）的新型核苷酸类似物和这些酯的药学上可接受的盐，酯或盐：其中n，X，Q U R1'，R1，Z和R2在此定义。本发明的化合物可以是单一对映异构体或作为所述对映体的混合物，所述化合物可以在每个手性中心具有αD，α-L，β-D，β-L，R或S构型或其混合物。本发明还涉及含有它们的单独或与其它治疗剂组合的药物组合物，以及它们作为抗病毒剂的用途，特别是用于哺乳动物中的HIV和/或HBV感染。

10. 发明授权

US08158675B2 Compounds and methods for the treatment or prevention of Flavivirus infections 失效
标题翻译：用于治疗或预防黄病毒感染的化合物和方法
公开(公告)号：US08158675B2
公开(公告)日：2012-04-17
申请号：US12508893
申请日：2009-07-24
申请人： Real Denis , Carl Poisson , Sanjoy Kumar Das , Irina Motorina , Rabindra Rej , Constantin G. Yannopoulos , Laval Chan Chun Kong
发明人： Real Denis , Carl Poisson , Sanjoy Kumar Das , Irina Motorina , Rabindra Rej , Constantin G. Yannopoulos , Laval Chan Chun Kong
IPC分类号： A61K31/38 , C07D333/42
CPC分类号： C07D471/04 , C07D333/38 , C07D409/04 , C07D409/12 , C07D409/14
摘要： Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.
摘要翻译：由式I表示的化合物或其药学上可接受的盐和溶剂合物，其中R1，X，Y，Y1和Z如本文所定义，可用于治疗黄病毒科病毒感染。

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