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    Estrogen receptor modulators
    2.
    发明授权
    Estrogen receptor modulators 有权
    雌激素受体调节剂

    公开(公告)号：US07923568B2

    公开(公告)日：2011-04-12

    申请号：US11992879

    申请日：2006-09-29

    申请人： Mark L. Greenlee ,  Dongfang Meng ,  Dann L. Parker, Jr. ,  Wanying Sun ,  Kenneth J. Wildonger ,  Robert R. Wilkening

    发明人： Mark L. Greenlee ,  Dongfang Meng ,  Dann L. Parker, Jr. ,  Wanying Sun ,  Kenneth J. Wildonger ,  Robert R. Wilkening

    IPC分类号： C07D249/16 ,  A61K31/416 ,  A61K31/4192

    CPC分类号： C07D249/16 ,  C07D231/54 ,  C07D235/02 ,  C07D405/04 ,  C07D413/04

    摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

    摘要翻译： 本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。 本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病， 软骨变性，子宫内膜异位症，子宫肌瘤病，热潮红，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎症性肠病， 性功能障碍，高血压，视网膜变性和癌症，特别是乳腺，子宫和前列腺。

    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    4.
    发明授权
    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
    碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法

    公开(公告)号：US06294529B1

    公开(公告)日：2001-09-25

    申请号：US09421690

    申请日：1999-10-07

    申请人： Lovji D. Cama ,  Ronald W. Ratcliffe ,  Robert R. Wilkening ,  Kenneth J. Wildonger ,  Wanying Sun

    发明人： Lovji D. Cama ,  Ronald W. Ratcliffe ,  Robert R. Wilkening ,  Kenneth J. Wildonger ,  Wanying Sun

    IPC分类号： C07D47714

    CPC分类号： C07D477/14

    摘要： Compounds of formula I are disclosed. as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B, wherein A-Q-L-B represents a side chain wherein: A is a C1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of —O—, —S—, NRa—, —C(O)— and —CH═CH—; Q represents  in which: b is 2 or 3; and X− is a charge balancing group; L represents a C1-8 alkylene group, unsubstituted or substituted with 1-3 Rc groups, and is interrupted or terminated by 1-3 of —CH═CH—, —C(O)—, —C(O)NRd—, —Het(Re)—, —C(O)—Het(Re)—, —C(O)NRa—Het(Re)—, —O—,—S—, —S(O)—, —SO2—, —CO2—, NRa—, —N+(Ra)2— B represents The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).

    摘要翻译： 公开了式I的化合物以及其药学上可接受的盐。 萘并磺胺被包括至少一个阳离子基团-AQLB的各种取代基取代，其中AQLB表示侧链，其中：A是直链或支链的C1-6亚烷基，并且任选地被1-2的-O-O - ， - S - ，NR a - ， - C（O） - 和-CH = CH-; Q表示其中：b为2或3; X为电荷平衡基团; L为C1-8亚烷基 并且被1-3个R c基团取代，并被1-3个-CH = CH-，-C（O） - ， - C（O）NR d - ， - H（Re） - ， - C（O）-Het（Re） - ， - C（O）NR a -Het（Re） - ， - O - ， - S - ， - S（O） - ， - SO 2 - ， - -N +（Ra）2-B代表本发明的碳青霉烯类对敏感细菌生物有效，包括耐甲氧西林金黄色葡萄球菌（MRSA），耐甲氧西林葡萄球菌（MRSE）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。

    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    5.
    发明授权
    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
    碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法

    公开(公告)号：US5994345A

    公开(公告)日：1999-11-30

    申请号：US168419

    申请日：1998-10-08

    申请人： Lovji D. Cama ,  Robert R. Wilkening ,  Ronald W. Ratcliffe ,  Kenneth J. Wildonger ,  Wanying Sun

    发明人： Lovji D. Cama ,  Robert R. Wilkening ,  Ronald W. Ratcliffe ,  Kenneth J. Wildonger ,  Wanying Sun

    IPC分类号： C07D477/14 ,  C07D521/00 ,  A61K31/395 ,  A61K31/695 ,  C07D519/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D477/14

    摘要： Carbapenems substituted with a naphthosultam at position 2 and linked through a CH.sub.2 group are disclosed. Pharmaceutical compositions and methods of treatment are also included. The naphthosultam is substituted with at least one cationic group --A--Q--L--B. ##STR1## A--Q--L--B represents a side chain wherein in part: A is a C.sub.1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of --O--, --S--, NR.sup.a --, --C(O)-- and CH.dbd.CH--Q is ##STR2## L represents a C.sub.1-8 alkylene group, straight or branched, and unsubstituted or substituted with 1-3 R.sup.c groups andB represents ##STR3## The carbapenems of the present invention are useful against gram positive microorganisms, especially methicillin resistant Staphylococci.

    摘要翻译： 公开了在位置2被萘并磺隆取代并通过CH2基团连接的碳青霉烯。 还包括药物组合物和治疗方法。 萘磺酸钠被至少一个阳离子基团-A-Q-L-B取代。 AQLB表示侧链，其中部分是：A是直链或支链的C1-6亚烷基，并且任选地被1-2，-O - ， - NR - ， - C（O） - 或 CH = CH-Q是L表示直链或支链的未取代或被1-3个Rc基团取代的C 1-8亚烷基，B表示本发明的碳青霉烯类可用于革兰氏阳性微生物，特别是耐甲氧西林葡萄球菌。

    Monomeric and polymeric cyclic amine and-halamine compounds
    7.
    发明授权
    Monomeric and polymeric cyclic amine and-halamine compounds 失效
    单体和聚合环胺和卤胺化合物

    公开(公告)号：US5670646A

    公开(公告)日：1997-09-23

    申请号：US474302

    申请日：1995-06-07

    申请人： Shelby D. Worley ,  Gang Sun ,  Wanying Sun ,  Tay-Yuan Chen

    发明人： Shelby D. Worley ,  Gang Sun ,  Wanying Sun ,  Tay-Yuan Chen

    IPC分类号： A01N59/00 ,  C07D233/74 ,  C07D251/10 ,  C07D251/20 ,  C07D263/22 ,  C08F8/30 ,  C08F8/48 ,  C08F12/26 ,  C07D235/02

    CPC分类号： C07D233/74 ,  A01N59/00 ,  C07D251/20 ,  C08F12/26 ,  C08F8/30 ,  C08F8/48 ,  Y02W10/37

    摘要： Cyclic amine monomers and polymers and N-halamine biocidal polymer compounds are provided. Methods of making and using the same wherein the functional groups unhalogenated or halogenated hydantoins, triazine diones, imidazolidinones, and pyrimidinones are substituted onto inexpensive polymer units such as polystyrene, polyethylene, and modified polymethacrylamide are provided. The cyclic amine monomers and polymers can be utilized to form the biocidal N-halamine polymers. These N-halamine polymers are stable, insoluble biocides which release only small amounts of free halogen and other impurities. They can be useful as disinfectants for potable water, swimming pools, hot tubs, industrial water systems, cooling towers, air-conditioning systems, gas streams, paints, oils, ointments, fabrics, rubber materials, sterile bandages, coatings, hard surfaces, liners of containers, and the like.

    摘要翻译： 提供了环胺单体和聚合物以及N-卤胺杀生物聚合物化合物。 提供了制备和使用其的方法，其中将官能团的未卤化或卤代乙内酰脲，三嗪二酮，咪唑烷酮和嘧啶酮取代到廉价的聚合物单元如聚苯乙烯，聚乙烯和改性的聚甲基丙烯酰胺上。 环胺单体和聚合物可用于形成杀生物N-卤代胺聚合物。 这些N-卤代胺聚合物是仅释放少量游离卤素和其它杂质的稳定的不溶性杀生物剂。 它们可用作饮用水，游泳池，热水浴缸​​，工业水系统，冷却塔，空调系统，气体流，油漆，油，软膏，织物，橡胶材料，无菌绷带，涂层，硬表面的消毒剂， 容器内衬等。

    Monomeric and polymeric cyclic amine and N-halamine compounds
    10.
    发明授权
    Monomeric and polymeric cyclic amine and N-halamine compounds 失效
    单体和聚合环胺和N-卤代胺化合物

    公开(公告)号：US06294185B1

    公开(公告)日：2001-09-25

    申请号：US08310657

    申请日：1994-09-22

    申请人： Shelby D. Worley ,  Gang Sun ,  Wanying Sun ,  Tay-Yuan Chen

    发明人： Shelby D. Worley ,  Gang Sun ,  Wanying Sun ,  Tay-Yuan Chen

    IPC分类号： A01N2500

    CPC分类号： C07D233/74 ,  A01N59/00 ,  C07D251/20 ,  C08F8/30 ,  C08F8/48 ,  C08F12/26 ,  Y02W10/37

    摘要： Cyclic amine monomers and polymers and N-halamine biocidal polymer compounds are provided. Methods of making and using the same wherein the functional groups unhalogenated or halogenated hydantoins, triazine diones, imidazolidinones, and pyrimidinones are substituted onto inexpensive polymer units such as polystyrene, polyethylene, and modified polymethacrylamide are provided. The cyclic amine monomers and polymers can be utilized to form the biocidal N-halamine polymers. These N-halamine polymers are stable, insoluble biocides which release only small amounts of free halogen and other impurities. They can be useful as disinfectants for potable water, swimming pools, hot tubs, industrial water systems, cooling towers, air-conditioning systems, gas streams, paints, oils, ointments, fabrics, rubber materials, sterile bandages, coatings, hard surfaces, liners of containers, and the like.

    摘要翻译： 提供了环胺单体和聚合物以及N-卤胺杀生物聚合物化合物。 提供了制备和使用其的方法，其中将官能团的未卤化或卤代乙内酰脲，三嗪二酮，咪唑烷酮和嘧啶酮取代到廉价的聚合物单元如聚苯乙烯，聚乙烯和改性的聚甲基丙烯酰胺上。 环胺单体和聚合物可用于形成杀生物N-卤代胺聚合物。 这些N-卤代胺聚合物是仅释放少量游离卤素和其它杂质的稳定的不溶性杀生物剂。 它们可用作饮用水，游泳池，热水浴缸​​，工业水系统，冷却塔，空调系统，气体流，油漆，油，软膏，织物，橡胶材料，无菌绷带，涂层，硬表面的消毒剂， 容器内衬等。