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1. 发明授权

US07101878B1 Non-peptide GNRH agents, methods and intermediates for their preparation 失效
标题翻译：非肽GNRH剂，其制备方法和中间体
公开(公告)号：US07101878B1
公开(公告)日：2006-09-05
申请号：US09763216
申请日：1999-08-20
申请人： Mark Brian Anderson , Haresh N. Vazir , David Robert Luthin , Genevieve DeGuzman Paderes , Ved P. Pathak , Lance Christopher Christie , Yufeng Hong , Eileen Valenzuela Tompkins , Haitao Li , James Faust
发明人： Mark Brian Anderson , Haresh N. Vazir , David Robert Luthin , Genevieve DeGuzman Paderes , Ved P. Pathak , Lance Christopher Christie , Yufeng Hong , Eileen Valenzuela Tompkins , Haitao Li , James Faust
IPC分类号： C07D405/12 , C07D307/68 , A61K31/34 , A61K31/505 , A61P5/04
CPC分类号： C07D307/68 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
摘要翻译：描述了能抑制促性腺激素释放激素作用的非肽GnRH剂。这些化合物及其药学上可接受的盐，多聚体，前药和活性代谢物适用于治疗哺乳动物生殖障碍和类固醇激素依赖性肿瘤以及调节生育能力，其中指出促性腺激素释放的抑制。还描述了合成化合物的方法和可用于其制备的中间体。

2. 发明授权

US5837690A Derivatives of triterpenoid acids and uses thereof. 失效
标题翻译：三萜酸的衍生物及其用途。
公开(公告)号：US5837690A
公开(公告)日：1998-11-17
申请号：US465893
申请日：1995-06-06
申请人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
发明人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
IPC分类号： C07D335/02 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/44 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K47/48 , A61K51/04 , A61P29/00 , A61P35/00 , A61P37/06 , C07D211/06 , C07D211/68 , C07D211/80 , C07D309/10 , C07H17/00 , C07H17/02 , C07H17/04 , C07J63/00 , A61K31/705 , G01N33/53
CPC分类号： A61K51/0491 , A61K47/48023 , A61K47/48123 , C07D309/10 , C07J63/008 , A61K2121/00 , A61K2123/00 , Y10S514/885 , Y10S514/889
摘要： Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory process as well as applications for the diagnosis of disease.
摘要翻译：描述了三萜酸衍生物，其表现出双重排斥性活性，特别是选择蛋白配体和白细胞三烯生物合成抑制活性，因此具有治疗或预防某些疾病（包括癌症和与炎症过程相关的疾病）以及诊断应用的显着应用的疾病

3. 发明授权

US5763582A Derivatives of triterpenoid acids and uses thereof 失效
公开(公告)号：US5763582A
公开(公告)日：1998-06-09
申请号：US466843
申请日：1995-06-06
申请人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
发明人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
IPC分类号： C07D335/02 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/44 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K47/48 , A61K51/04 , A61P29/00 , A61P35/00 , A61P37/06 , C07D211/06 , C07D211/68 , C07D211/80 , C07D309/10 , C07H17/00 , C07H17/02 , C07H17/04 , C07J63/00 , C07H15/256 , C07H1/00
CPC分类号： A61K51/0491 , A61K47/48023 , A61K47/48123 , C07D309/10 , C07J63/008 , A61K2121/00 , A61K2123/00 , Y10S514/885 , Y10S514/889
摘要： Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory process as well as applications for the diagnosis of disease.

4. 发明授权

US06646137B1 Non-peptide GnRH agents 失效
标题翻译：非肽GnRH剂
公开(公告)号：US06646137B1
公开(公告)日：2003-11-11
申请号：US09717072
申请日：2000-11-22
申请人： Mark Brian Anderson , Alexander Polinsky , Yufeng Hong , Vlad Edward Gregor
发明人： Mark Brian Anderson , Alexander Polinsky , Yufeng Hong , Vlad Edward Gregor
IPC分类号： C07D30702
CPC分类号： C07D213/82 , C07C279/12 , C07D207/34 , C07D209/42 , C07D215/12 , C07D231/14 , C07D231/16 , C07D261/10 , C07D307/00 , C07D307/68 , C07D307/71 , C07D307/91 , C07D317/68 , C07D319/18 , C07D333/38 , C07D333/70 , C07D405/12 , C07D409/12
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
摘要翻译：能够抑制促性腺激素释放激素作用的非肽GnRH剂具有以下通式，其中X1，X2，Y和Z是定义的变量：这些化合物及其药学上可接受的盐，多聚体，前药和活性代谢物适合于治疗哺乳动物生殖障碍和类固醇激素依赖性肿瘤以及调节生育能力，其中指出促性腺激素释放的抑制。还描述了合成化合物的方法和可用于其制备的中间体。

5. 发明授权

US06218426B1 Non-peptide GnRH agents 失效
标题翻译：非肽GnRH剂
公开(公告)号：US06218426B1
公开(公告)日：2001-04-17
申请号：US09259206
申请日：1999-03-01
申请人： Mark Brian Anderson , Alexander Polinsky , Yufeng Hong , Vlad Edward Gregor
发明人： Mark Brian Anderson , Alexander Polinsky , Yufeng Hong , Vlad Edward Gregor
IPC分类号： A01N4306
CPC分类号： C07D213/82 , C07C279/12 , C07D207/34 , C07D209/42 , C07D215/12 , C07D231/14 , C07D231/16 , C07D261/10 , C07D307/00 , C07D307/68 , C07D307/71 , C07D307/91 , C07D317/68 , C07D319/18 , C07D333/38 , C07D333/70 , C07D405/12 , C07D409/12
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
摘要翻译：能够抑制促性腺激素释放激素作用的非肽GnRH剂具有以下通式，其中X1，X2，Y是定义的变量：这些化合物及其药学上可接受的盐，多聚体，前药和活性代谢物是适用于治疗哺乳动物生殖障碍和类固醇激素依赖性肿瘤以及调节生育能力，其中指出促性腺激素释放的抑制。还描述了合成化合物的方法和可用于其制备的中间体。

6. 发明授权

US5963087A Gain control circuit and method for providing gain control of a variable amplifier using a pilot signal 失效
标题翻译：增益控制电路和方法，用于使用导频信号提供可变放大器的增益控制
公开(公告)号：US5963087A
公开(公告)日：1999-10-05
申请号：US87172
申请日：1998-05-29
申请人： Mark Brian Anderson
发明人： Mark Brian Anderson
IPC分类号： H03G3/20 , H03G3/00 , H03F3/66
CPC分类号： H03G3/005
摘要： The present invention provides for a gain control circuit (10) and method for providing gain control of a variable amplification circuit (16) using a pilot signal. A pilot signal is added to the received signal. The pilot signal has at least a minimum signal level which when added to the signal received insures the sampled input signal has a level above the point where offset or low power errors are experienced. Preferably the pilot signal will be a sinusoidal signal having a frequency within the operational bandwidth of the amplifier (16), but outside the frequency range of the input signal.
摘要翻译：本发明提供一种增益控制电路（10）以及使用导频信号提供可变放大电路（16）的增益控制的方法。导频信号加到接收信号上。导频信号至少具有最小信号电平，当被加到接收到的信号时，确保采样输入信号具有高于偏移或低功率误差的点的电平。优选地，导频信号将是具有在放大器（16）的工作带宽之内但在输入信号的频率范围之外的频率的正弦信号。

7. 发明授权

US5643884A Lupane triterpenoid derivatives 失效
标题翻译： Lupane三萜衍生物
公开(公告)号：US5643884A
公开(公告)日：1997-07-01
申请号：US105095
申请日：1993-08-09
申请人： Mark Brian Anderson , John Henry Musser
发明人： Mark Brian Anderson , John Henry Musser
IPC分类号： C07D335/02 , A61K31/38 , A61K31/382 , A61K31/445 , A61K31/4458 , A61K31/4468 , A61K51/00 , A61K51/04 , A61P29/00 , A61P35/00 , A61P43/00 , C07D211/40 , C07D211/56 , C07D211/60 , C07D309/10 , C07J13/00 , A61K31/705 , C07J17/00
CPC分类号： C07D309/10 , A61K51/0478 , A61K2121/00
摘要： This invention relates generally to the field of medicinal chemistry, and more specifically to derivatives of a subclass of triterpenoid acids that have multi-medicament properties, that is derivatives of the lupane, betulinic acid, formulations containing such, and their use to prevent or treat certain diseases, and preferably to derivatives or analogues of betulinic acid, that have the following structural formula (1): ##STR1## wherein: Y is OR.sup.1, NR.sup.1.sub.2, O.sup.- M.sup.1 ;R.sup.1 is H, LOWER ALKYL,M.sup.1 is Na.sup.+, K.sup.+, Mg.sup.++, Ca.sup.++ ions;each R.sup.2 is independently CH.sub.2 OR.sub.1 or CH.sub.3 ;each R.sup.3 is independently H, CH.sub.3, lower alkyl, COY, CH.sub.2 OH, CH.sub.2 OCH.sub.2 CH=CH.sub.2, CH.sub.2 OSO.sub.3.sup.- M.sup.1 ;each Z is independently NHR.sup.1.sub.2, NR.sup.1 Ac, NR.sup.1 Bz, H, OCH.sub.3, lower alkyl, OH, OSO.sub.3.sup.- M.sup.1, OCH.sub.2 CH=CH.sub.2, OCH.sub.2 CO.sub.2 H or O-glucoside;each X is independently O, S, NR.sup.1 or NR.sub.2.sup.1each W is independently C=O, C=CR.sup.1.sub.2, CR.sup.1 CR.sup.1.sub.3, CR.sup.1 -CR.sup.1.sub.2 OR.sup.1, COR.sup.1 -CR.sup.1 OR.sup.1, COR.sup.1 CR.sup.1.sub.2 OR.sup.1, CR.sup.1 CR.sup.1.sub.2 NR.sup.1.sub.2, CR.sup.1 CR.sup.1.sub.2 OCR.sup.1 COY, CHR.sup.4 ;R.sup.4 is H, OH, OSO.sub.3.sup.- M.sup.1, or NH(CH.sub.2)nNH.sub.2, where n=1-8, or NH-Ph-NH.sub.2 where Ph=an phenyl or naphthyl rings substituted with up to 3 amine functionalities and the remaining substitutions can be H, R.sup.1, R.sup.2 or COY;R.sup.5 and R.sup.6 are independently H, CH.sub.3, or taken together form a 5 or 6 membered carbocyclic ring.
摘要翻译：本发明一般涉及药物化学领域，更具体地涉及具有多种药物性质的三萜酸类亚类的衍生物，即十六烷，桦木酸，含有这些物质的制剂及其用于预防或治疗的用途的衍生物某些疾病，优选具有下列结构式（1）的桦树酸衍生物或类似物：其中：Y是OR 1，NR 12，O-M 1; R1为H，低级烷基，M1为Na +，K +，Mg ++，Ca ++离子; 每个R 2独立地是CH 2 OR 1或CH 3; 每个R 3独立地是H，CH 3，低级烷基，COY，CH 2 OH，CH 2 OCH 2 CH = CH 2，CH 2 OSO 3 -M 1; 每个Z独立地是NHR12，NR1Ac，NR1Bz，H，OCH3，低级烷基，OH，OSO3-M1，OCH2CH = CH2，OCH2CO2H或O-葡萄糖苷; 每个X独立地为O，S，NR1或NR21，每个W独立地为C = O，C = CR12，CR1CR13，CR1-CR12OR1，COR1-CR1OR1，COR1CR12OR1，CR1CR12NR12，CR1CR12OCR1COY，CHR4; R4是H，OH，OSO3-M1或NH（CH2）nNH2，其中n = 1-8或NH-Ph-NH2，其中Ph =被至多3个胺官能团取代的苯基或萘环，并且其余的取代可以为H，R1，R2或COY; R5和R6独立地为H，CH3，或一起形成5或6元碳环。

8. 发明申请

US20110190392A1 Polysaccharide Based Antimicrobial Formulations 审中-公开
标题翻译：多糖类抗微生物剂
公开(公告)号：US20110190392A1
公开(公告)日：2011-08-04
申请号：US13019963
申请日：2011-02-02
申请人： Azar Najafi , Bahram Memarzadeh , Sarah A. Ibrahim , Mark Brian Anderson
发明人： Azar Najafi , Bahram Memarzadeh , Sarah A. Ibrahim , Mark Brian Anderson
IPC分类号： A61K31/255 , A61P31/00 , A61P27/02 , A61P17/10
CPC分类号： A61K31/185 , A01N41/08 , A01N59/00 , A61K8/416 , A61K8/46 , A61K8/466 , A61K8/49 , A61K8/4926 , A61K8/4946 , A61K8/55 , A61K9/0048 , A61K31/14 , A61K31/145 , A61K31/4166 , A61K31/421 , A61K31/4425 , A61K31/66 , A61K47/36 , A61K2800/74 , A61L2/16 , A61L2202/24 , A61Q19/00 , A01N25/04 , A01N2300/00
摘要： Described herein are antimicrobial formulations or compositions comprising an N-halogenated or N,N-dihalogenated amine compound and a saccharide-based gelling agent. Methods of using such formulations, including a method of preventing or treating an infection caused by a bacterial, a microbial, a sporal, a fungal or a viral activity, are also disclosed.
摘要翻译：本文描述的是抗微生物制剂或包含N-卤化或N，N-二卤代胺化合物和糖类胶凝剂的组合物。还公开了使用这些制剂的方法，包括预防或治疗由细菌，微生物，真菌，真菌或病毒活性引起的感染的方法。

9. 发明授权

US5679644A Methods of treating diseases using triterpenoid acid derivatives 失效
标题翻译：使用三萜酸衍生物治疗疾病的方法
公开(公告)号：US5679644A
公开(公告)日：1997-10-21
申请号：US469137
申请日：1995-06-06
申请人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
发明人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
IPC分类号： C07D335/02 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/44 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K47/48 , A61K51/04 , A61P29/00 , A61P35/00 , A61P37/06 , C07D211/06 , C07D211/68 , C07D211/80 , C07D309/10 , C07H17/00 , C07H17/02 , C07H17/04 , C07J63/00 , A61K31/705
CPC分类号： A61K51/0491 , A61K47/48023 , A61K47/48123 , C07D309/10 , C07J63/008 , A61K2121/00 , A61K2123/00 , Y10S514/885 , Y10S514/889
摘要： Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory process as well as applications for the diagnosis of disease.
摘要翻译：描述了三萜酸衍生物，其表现出双重排斥性活性，特别是选择蛋白配体和白细胞三烯生物合成抑制活性，因此具有治疗或预防某些疾病（包括癌症和与炎症过程相关的疾病）以及诊断应用的显着应用的疾病

10. 发明授权

US5688922A Substituted fucopyranosides 失效
标题翻译：取代的fucopyranosides
公开(公告)号：US5688922A
公开(公告)日：1997-11-18
申请号：US466859
申请日：1995-06-06
申请人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
发明人： Narasinga Rao , Mark Brian Anderson , John Henry Musser
IPC分类号： C07D335/02 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/44 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K47/48 , A61K51/04 , A61P29/00 , A61P35/00 , A61P37/06 , C07D211/06 , C07D211/68 , C07D211/80 , C07D309/10 , C07H17/00 , C07H17/02 , C07H17/04 , C07J63/00 , C07D3/02 , C07G1/00
CPC分类号： A61K51/0491 , A61K47/48023 , A61K47/48123 , C07D309/10 , C07J63/008 , A61K2121/00 , A61K2123/00 , Y10S514/885 , Y10S514/889
摘要： 2-Chloromethyl-3-(tri-O-benzyl-.alpha.-L-C-fucopyranoside)-1-propene and methods of making the same are described. Methods of combining this substituted fucopyranose with triterpenoid acid also are described.
摘要翻译：描述了2-氯甲基-3-（三-O-苄基-α-R1-C-fucopyranoside）-1-丙烯及其制备方法。还描述了将该取代的赤藓糖与三萜酸组合的方法。

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