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1. 发明授权

US5753714A Polyamine derivatives 失效
标题翻译：多胺衍生物
公开(公告)号：US5753714A
公开(公告)日：1998-05-19
申请号：US213386
申请日：1994-03-15
申请人： David M. Stemerick , Alan J. Bitonti , Michael L. Edwards , Peter P. McCann , Albert Sjoerdsma
发明人： David M. Stemerick , Alan J. Bitonti , Michael L. Edwards , Peter P. McCann , Albert Sjoerdsma
IPC分类号： C07C211/09 , C07C211/14 , A61K31/135 , C07C211/43
CPC分类号： C07C211/09 , C07C211/14
摘要： This invention relates to certain polyamine derivatives, to the methods and intermediates useful for their preparation, and to their use in treating diseases caused by infestation with a variety of parasitic protozoa.
摘要翻译：本发明涉及某些多胺衍生物，对其制备有用的方法和中间体及其用于治疗由多种寄生原虫感染引起的疾病的用途。

2. 发明授权

US5214050A Esters of castanospermine in the treatment of cerebral malaria 失效
标题翻译：睾丸精胺治疗脑疟疾
公开(公告)号：US5214050A
公开(公告)日：1993-05-25
申请号：US846656
申请日：1992-03-05
申请人： Alan J. Bitonti , Peter P. McCann , Albert Sjoerdsma
发明人： Alan J. Bitonti , Peter P. McCann , Albert Sjoerdsma
IPC分类号： A61K31/36 , A61K31/445
CPC分类号： A61K31/445 , A61K31/36
摘要： Red blood cells which are infected with the parasite P. falciparum cause the cells to become sticky and less deformable. This results in a build-up of cells on the vascular wall and creates occlusions to blood flow which are thought to cause the cerebral, renal and liver complications of P. falciparum infections. Certain esters of castanospermine prevent or reduce the adhesion of falciparum infected blood cells to the vascular endothelial wall and are a useful adjunct in the treatment of malaria.
摘要翻译：被恶性疟原虫感染的红细胞导致细胞变得粘稠且变形少。这导致血管壁上的细胞积聚并且产生被认为引起恶性疟原虫感染的脑，肾和肝并发症的血流阻塞。睾丸精胺的某些酯防止或减少恶性疟原虫感染的血细胞对血管内皮壁的粘附，并且是治疗疟疾的有用辅助物质。

3. 发明授权

US5373005A Despiramine in the treatment of drug-resistant malarial infections 失效
标题翻译：治疗耐药疟疾感染的绝食
公开(公告)号：US5373005A
公开(公告)日：1994-12-13
申请号：US26950
申请日：1993-03-05
申请人： Peter P. McCann , Albert Sjoerdsma , Alan J. Bitonti
发明人： Peter P. McCann , Albert Sjoerdsma , Alan J. Bitonti
IPC分类号： A61K45/06 , A61K31/55 , A61K31/47
CPC分类号： A61K45/06
摘要： Drug-resistant malarial infection in humans can be effectively treated with standard antimalarial agents if administered in conjunction with desipramine.
摘要翻译：如果与地昔帕明联合给药，可以用标准抗疟药物有效地治疗人类的耐药性疟疾感染。

4. 发明授权

US4935449A N-2,3-butadienyl tri- and tetraaminoalkane derivatives 失效
标题翻译： N-2,3-丁二烯基三 - 和四氨基烷烃衍生物
公开(公告)号：US4935449A
公开(公告)日：1990-06-19
申请号：US228620
申请日：1988-08-04
申请人： Philippe Bey , David M. Stemerick , Michael L. Edwards , Alan J. Bitonti
发明人： Philippe Bey , David M. Stemerick , Michael L. Edwards , Alan J. Bitonti
IPC分类号： C12N9/99 , A01N33/04 , A61K31/13 , A61K31/16 , A61P33/02 , A61P43/00 , C07C67/00 , C07C209/00 , C07C209/62 , C07C211/21 , C07C211/22 , C07C231/00 , C07C231/12 , C07C233/36 , C07C233/38
CPC分类号： C07C211/21 , A01N33/04 , A61K31/13 , Y10S514/895
摘要： The importance of polyamines in biological systems is discussed as well as the implications of polyamines in the treatment of various diseases. Novel N-substituted-2,3-butadienyl tri- and tetra-aminoalkanes are disclosed as well as their use inthe treatment of diseases and the pharmaceutical compositions.

5. 发明授权

US5607925A Treatment of carcinoma by administration of 2'-halomethylidenyl-2'-deoxynucleosides 失效
标题翻译：通过给予2'-卤代亚甲基-2'-脱氧核苷治疗癌症
公开(公告)号：US5607925A
公开(公告)日：1997-03-04
申请号：US333017
申请日：1994-11-01
申请人： Donald P. Matthews , Alan J. Bitonti , Michael L. Edwards , James R. McCarthy
发明人： Donald P. Matthews , Alan J. Bitonti , Michael L. Edwards , James R. McCarthy
IPC分类号： C07H19/06 , C07H19/16 , A61K31/70
CPC分类号： C07H19/06 , C07H19/16
摘要： This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
摘要翻译：本发明涉及某些新的2'-卤代亚甲基，2'-亚乙基和2'-乙炔基胞苷，尿苷和鸟苷衍生物及其组合物，其可用于治疗患有肿瘤或病毒疾病状态的患者。

6. 发明授权

US07566565B2 PC5 as a factor IX propeptide processing enzyme 有权
标题翻译： PC5作为因子IX前肽加工酶
公开(公告)号：US07566565B2
公开(公告)日：2009-07-28
申请号：US11728045
申请日：2007-03-23
申请人： Robert T. Peters , Alan J. Bitonti
发明人： Robert T. Peters , Alan J. Bitonti
IPC分类号： C12N15/00 , C12N5/00
CPC分类号： C12N9/644 , C07K2319/30 , C12N9/6454 , C12Y304/21022
摘要： Compositions and methods for preparing Factor IX, Factor IX-containing fusion proteins, and Factor IX-containing conjugates with processing of Factor IX propeptide by PC5, are provided. In one embodiment PC5 is used to process a precursor polypeptide for a Factor IX-Fc monomer-dimer hybrid.
摘要翻译：提供了通过PC5处理因子IX前体肽制备因子IX，含因子IX的融合蛋白和含有因子IX的缀合物的组合物和方法。在一个实施方案中，PC5用于处理因子IX-Fc单体 - 二聚体杂交体的前体多肽。

7. 发明授权

US06479487B1 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines 失效
标题翻译： 6,9-二取代的2- [反 - （4-氨基环己基）氨基]嘌呤
公开(公告)号：US06479487B1
公开(公告)日：2002-11-12
申请号：US09247053
申请日：1999-02-09
申请人： Jennifer A. Dumont , Alan J. Bitonti , David R. Borcherding , Norton P. Peet , H. Randall Munson, Jr. , Patrick W. Shum
发明人： Jennifer A. Dumont , Alan J. Bitonti , David R. Borcherding , Norton P. Peet , H. Randall Munson, Jr. , Patrick W. Shum
IPC分类号： C07D47316
CPC分类号： C07D473/00
摘要： The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or R3R4N—R5- wherein R2 is selected from the group consisting of C9-C12 alkyl, Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C1-C4 alkyl, and wherein each C9-C12 alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E, wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each E is independently selected from the group consisting of Hal, OH, and C1-C8 alkyl; R3 and R4 are selected from the group consisting of hydrogen, C1-C4 alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen; R5 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl, cyclopentenyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof, with the proviso that when R2 is the group wherein n is 1 or greater; R1 is isopropyl or cyclopentyl; R6 is hydrogen, C1-C4 alkyl, or (CH2)m-phenyl; and Z is phenyl, heterocycle, or cycloalkyl, that Z is substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of In addition, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.
摘要翻译：本发明提供新的式（I）化合物，其中R选自R2，R2NH-或R3R4N-R5-，其中R2选自C9-C12烷基，Z选自的苯基，杂环，环烷基和萘烷; 并且M选自氢，C 1 -C 4烷基，并且其中每个C 9 -C 12烷基或Z任选被1至3个可以相同或不同的取代基取代，并且其选自 D，E，其中每个D独立地选自三氟甲基，三氟甲氧基和C 1 -C 4烷氧基; 每个E独立地选自Hal，OH和C 1 -C 8烷基; R 3和R 4选自氢，C 1 -C 4烷基和（CH 2）y - 苯基，其中y是整数0 -8，条件是R3和R4不都是氢; R5是C1-C8亚烷基; 并且R 1选自环戊基，环戊烯基和异丙基，以及其药学上可接受的盐，旋光异构体和水合物，条件是当R 2是n为1或更大的基团时; R1是异丙基或环戊基; R6是氢，C1-C4烷基或（CH2）m-苯基; Z是苯基，杂环或环烷基，Z被1至3个可以相同或不同的取代基取代，并且选自由以下组成的组。另外，本发明提供抑制细胞周期蛋白依赖性激酶的方法，特别是cdk-2。本发明还提供了一种预防神经元细胞凋亡的方法和抑制肿瘤发生的方法。

8. 发明授权

US5681863A Non-metabolizable clomiphene analogs for treatment of tamoxifen-resistant tumors 失效
标题翻译：不可代谢的克罗米酚类似物用于治疗他莫西芬抗性肿瘤
公开(公告)号：US5681863A
公开(公告)日：1997-10-28
申请号：US350192
申请日：1994-12-05
申请人： Alan J. Bitonti , Russell J. Baumann
发明人： Alan J. Bitonti , Russell J. Baumann
IPC分类号： A61K31/135 , A61K31/138 , A61P35/00 , A61P43/00 , C07C211/48 , C07C323/25
CPC分类号： C07C323/25 , A61K31/135 , C07C211/48
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each selected from the group consisting of C.sub.1 -C.sub.2 lower alkyl; X is NH or S; and n is a whole number within the range of 1-4 inclusive; and when n=0, X is (CH.sub.2).sub.3 and the pharmaceutically acceptable salts thereof have been shown to be effective in treating tamoxifen resistant tumors.
摘要翻译：下式的化合物：其中R 1和R 2各自选自C 1 -C 2低级烷基; X是NH或S; n为1-4以下的整数; 并且当n = 0时，X是（CH 2）3，并且其药学上可接受的盐已显示在治疗他莫昔芬抗性肿瘤方面是有效的。

9. 发明申请

US20110182896A1 CLOTTING FACTOR-Fc CHIMERIC PROTEINS TO TREAT HEMOPHILIA 有权
标题翻译：衣原体Fc Fc基因蛋白治疗HEMOPHILIA
公开(公告)号：US20110182896A1
公开(公告)日：2011-07-28
申请号：US12949564
申请日：2010-11-18
申请人： DANIEL S. RIVERA , Robert T. Peters , Alan J. Bitonti
发明人： DANIEL S. RIVERA , Robert T. Peters , Alan J. Bitonti
IPC分类号： A61K39/395 , C07K19/00 , C12N9/96 , C12P21/00 , C07H21/04 , C12N15/85 , C12N5/10 , C12N1/00 , A61P7/04
CPC分类号： C12N9/6437 , A61K38/36 , A61K38/4846 , A61K45/06 , A61K47/6815 , A61K47/6835 , A61K2039/60 , C07K14/745 , C07K16/18 , C07K2319/30 , C12N9/644 , C12N9/6454 , C12Y304/21021 , C12Y304/21022
摘要： The invention relates to a chimeric protein comprising at least one clotting factor and at least a portion of an immunoglobulin constant region. The invention relates to a method of treating a hemostatic disorder comprising administering a therapeutically effective amount of a chimeric protein wherein the chimeric protein comprises at least one clotting factor and at least a portion of an immunoglobulin constant region.
摘要翻译：本发明涉及包含至少一种凝血因子和至少一部分免疫球蛋白恒定区的嵌合蛋白。本发明涉及一种治疗止血障碍的方法，包括施用治疗有效量的嵌合蛋白，其中所述嵌合蛋白包含至少一种凝血因子和至少一部分免疫球蛋白恒定区。

10. 发明授权

US5693674A Method of using triaryl-ethylene derivatives in the treatment and prevention of osteoporosis 失效
标题翻译：三芳基 - 乙烯衍生物在治疗和预防骨质疏松症方面的应用
公开(公告)号：US5693674A
公开(公告)日：1997-12-02
申请号：US662092
申请日：1996-06-12
申请人： Alan J. Bitonti
发明人： Alan J. Bitonti
IPC分类号： C07D295/08 , A61K31/135 , A61K31/136 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/4453 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P19/10 , A61P43/00 , C07C217/18
CPC分类号： A61K31/5375 , A61K31/136 , A61K31/138 , A61K31/40 , A61K31/4453 , A61K31/495
摘要： The present invention relates to a method of using triaryl-ethylene derivatives in the treatment or prevention bone tissue loss or osteoporosis.
摘要翻译：本发明涉及使用三芳基 - 乙烯衍生物来治疗或预防骨组织损失或骨质疏松症的方法。

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