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11. 发明授权

US08481722B2 High stability polyionic liquid salts 有权
标题翻译：高稳定性聚离子液体盐
公开(公告)号：US08481722B2
公开(公告)日：2013-07-09
申请号：US13324469
申请日：2011-12-13
申请人： Daniel W Armstrong , Junmin Huang
发明人： Daniel W Armstrong , Junmin Huang
IPC分类号： C07D243/04 , C07D207/04 , C07C211/44 , C07F9/02
CPC分类号： C07F9/5449 , B01J20/286 , B01J20/292 , C07C215/40 , C07C305/06 , C07C309/05 , C07D207/08 , C07D233/64 , C07D275/06 , C07D291/06 , C07D295/12 , C07D471/02 , Y02P20/542
摘要： Polyionic liquid salts are provided comprising polycationic or polyanionic molecules. Further provided are solvents comprising one or more polyionic liquid salts, and the use of such polyionic liquid salts as stationary phases in gas chromatography, and as a reagent in electrospray ionization-mass spectrometry (ESI-MS).
摘要翻译：提供了包含聚阳离子或聚阴离子分子的聚离子液体盐。还提供了包含一种或多种聚离子液体盐的溶剂，以及在气相色谱法中作为固定相使用这种聚离子液体盐，以及作为电喷雾离子化 - 质谱法（ESI-MS）中的试剂。

12. 发明授权

US08314250B2 Sultam derivatives 有权
标题翻译：苏丹衍生物
公开(公告)号：US08314250B2
公开(公告)日：2012-11-20
申请号：US12905120
申请日：2010-10-15
申请人： Kevin W. Anderson , Paul Gillespie , Nicholas J. S. Huby , Norman Kong , John L. Roberts , Pamela L. Rossman , Sung-Sau So
发明人： Kevin W. Anderson , Paul Gillespie , Nicholas J. S. Huby , Norman Kong , John L. Roberts , Pamela L. Rossman , Sung-Sau So
IPC分类号： C07D285/01 , C07D417/06 , A61K31/425 , A61K31/4535 , A61K31/4523
CPC分类号： C07D275/06
摘要： The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.
摘要翻译：本发明涉及具有细胞毒活性的根据式1的化合物。该化合物可用于治疗癌症。

13. 发明申请

US20120190847A1 TRIARYLMETHANE ANALOGS AND THEIR USE IN TREATING CANCERS 有权
标题翻译：三叉戟类似物及其在治疗癌症中的应用
公开(公告)号：US20120190847A1
公开(公告)日：2012-07-26
申请号：US13412895
申请日：2012-03-06
申请人： Jack L. Arbiser
发明人： Jack L. Arbiser
IPC分类号： C07D223/28
CPC分类号： A61K31/55 , A61K9/127 , A61K31/136 , A61K31/14 , A61K31/353 , A61K31/404 , A61K31/422 , A61K31/428 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/54 , A61K31/553 , A61K31/662 , C07D215/26 , C07D215/46 , C07D223/26 , C07D223/28 , C07D263/32 , C07D275/06 , C07D279/28 , C07D311/36 , C07F9/4056 , C07F9/4059 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。化合物是三苯甲烷类似物。化合物和组合物可用于治疗和/或预防多种癌症，包括耐药性癌症，炎性，退行性和血管性疾病，包括各种眼部疾病和寄生虫感染。代表性的三苯甲烷类似物包括各种染料，激素，糖，肽，寡核苷酸，氨基酸，核苷酸，核苷和多元醇的三苯基甲烷类似物。据信这些化合物通过抑制tNOX表达，ROS的作用和/或HIF2的产生起作用。因此，这些化合物是用于各种癌症和其它疾病的新型治疗剂。

14. 发明授权

US08173679B2 Indazoles, benzisoxazoles and benzisothiazoles and their use as estrogenic agents 失效
标题翻译：吲唑，苯并异恶唑和苯并异噻唑及其作为雌激素剂的用途
公开(公告)号：US08173679B2
公开(公告)日：2012-05-08
申请号：US13152433
申请日：2011-06-03
申请人： Benoit Rondot , Jean Lafay , Paule Bonnet , Thierry Clerc , Igor Duc , Eric Duranti , Francois Puccio , Jacqueline Shields , Christian Blot , Philippe Maillos
发明人： Benoit Rondot , Jean Lafay , Paule Bonnet , Thierry Clerc , Igor Duc , Eric Duranti , Francois Puccio , Jacqueline Shields , Christian Blot , Philippe Maillos
IPC分类号： A61K31/454 , A61K31/428 , A61K31/423 , A61K31/416 , C07D261/20 , C07D401/06 , C07D275/04 , C07D413/12 , C07D231/56
CPC分类号： C07D231/56 , C07D261/20 , C07D275/04 , C07D275/06 , C07D491/06
摘要： The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.
摘要翻译：本发明涉及式（I）化合物：其中R1，R2，R3，X，Y和A如说明书中所定义。这些化合物是雌激素受体的调节剂。

15. 发明申请

US20120077856A1 PHARMACEUTICAL PRODUCT 审中-公开
标题翻译：药用产品
公开(公告)号：US20120077856A1
公开(公告)日：2012-03-29
申请号：US13309936
申请日：2011-12-02
申请人： Yuji IIZAWA , Masayuki Ii , Tomohiro Kawamoto
发明人： Yuji IIZAWA , Masayuki Ii , Tomohiro Kawamoto
IPC分类号： A61K31/215 , A61K31/41 , A61K31/4196 , A61K31/428 , A61P29/00 , A61P31/00 , A61P9/00 , A61P37/06 , A61P25/00 , A61P17/02 , A61P19/02 , A61P1/04 , A61P9/10 , A61P1/18 , A61P13/12 , A61P3/10 , A61P25/16 , A61P35/02 , A61P35/00 , A61P11/00 , A61P17/06 , A61K31/4192
CPC分类号： C07D249/06 , A61K31/216 , A61K31/41 , A61K31/4192 , A61K31/428 , A61K45/06 , C07D249/08 , C07D257/04 , C07D275/06 , A61K2300/00
摘要： An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II) wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
摘要翻译：用于抑制各种细胞因子（IL-8等）和炎性介质的产生的药剂，抑制COX-II等的表达的试剂或各种磷酸化酶（ATF2等）的抑制剂，其中含有TLR信号传导抑制物质，优选式（I）或式（II）表示的化合物，其中各符号如说明书中所定义，或其盐或其前药。

16. 发明授权

US08138182B2 Diketohydrazine derivative compounds and drugs containing the compounds as the active ingredient 失效
标题翻译：二酮肼衍生物化合物和含有这些化合物作为活性成分的药物
公开(公告)号：US08138182B2
公开(公告)日：2012-03-20
申请号：US12566416
申请日：2009-09-24
申请人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
发明人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
IPC分类号： C07D207/22 , C07D233/32 , C07D263/20 , C07D265/33 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/65583 , Y02A50/411
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译：本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病，肝或胆道疾病，骨质或关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性障碍性肺疾病）。

17. 发明授权

US08119568B2 3-amino-1,2-benzisothiazole compounds for combating animal pest II 失效
标题翻译：用于对抗动物害虫的3-氨基-1,2-苯并异噻唑化合物II
公开(公告)号：US08119568B2
公开(公告)日：2012-02-21
申请号：US12523802
申请日：2008-01-14
申请人： Wolfgang von Deyn , Matthias Pohlman , Florian Kaiser , Joachim Dickhaut , Douglas D. Anspaugh , Deborah L. Culbertson , Hassan Oloumi-Sadeghi
发明人： Wolfgang von Deyn , Matthias Pohlman , Florian Kaiser , Joachim Dickhaut , Douglas D. Anspaugh , Deborah L. Culbertson , Hassan Oloumi-Sadeghi
IPC分类号： A01N43/80 , C07D275/06
CPC分类号： C07D417/14 , A01N43/80 , A01N43/90 , C07D275/04 , C07D275/06 , C07D417/12
摘要： The invention provides 3-amino-1,2-benzisothiazole compounds of formula (I) wherein n, R1, R2, R3, R4 and A are defined as in the description. The invention provides further agricultural compositions comprising an amount of at least one compound of the formula (I) or an enantiomer, diastereomer or salt thereof; the use of a compound of formula (I) or an enantiomer, diastereomer or salt thereof for combating animal pests; a method of combating animal pests which comprises contacting the animal pests, their habit, breeding ground, food supply, plant, seed, soil, area, material or environment in which the animal pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from animal attack or infestation with a pesticidally effective amount of at least one compound of the formula (I) or an enantiomer, diastereomer or salt thereof; a method for protecting crops from attack or infestation by animal pests, which comprises contacting a crop with a pesticidally effective amount of at least one compound of the formula (I) or an enantiomer, diastereomer or salt thereof; a method for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects comprising contacting the seeds before sowing and/or after pregermination with at least one compound of the formula (I), or the enantiomers, diastereomers or salts thereof; and seeds comprising a compound of the formula I or an enantiomer, diastereomer or salt thereof.
摘要翻译：本发明提供式（I）的3-氨基-1,2-苯并异噻唑化合物，其中n，R 1，R 2，R 3，R 4和A如描述中所定义。本发明提供了包含一定量的至少一种式（I）化合物或其对映异构体，非对映体或其盐的进一步农业组合物; 使用式（I）化合物或其对映异构体，非对映体或其盐来防治动物害虫; 一种防治动物害虫的方法，包括使动物有害生物，其习惯，繁殖地，食物供应，植物，种子，土壤，区域，动物害虫生长或可能生长的区域，物质或环境，或材料，植物，种子，土壤，表面或空间，以防止动物攻击或侵袭与杀虫有效量的至少一种式（I）化合物或其对映体，非对映体或其盐; 包括使作物与杀虫有效量的至少一种式（I）化合物或其对映异构体，非对映异构体或其盐接触的方法，用于保护作物不被动物害虫侵袭或侵染。包括防止种子从土壤昆虫和幼苗根和土壤和叶面昆虫的芽中保护种子的方法，包括在种子播种前和/或之后与种子接种后与至少一种式（I）的化合物或对映异构体接触，非对映体或其盐; 和包含式I化合物或其对映体，非对映体或其盐的种子。

18. 发明申请

US20120015911A1 METHOD AND COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES 有权
标题翻译：用于治疗淀粉样相关疾病的方法和组合物
公开(公告)号：US20120015911A1
公开(公告)日：2012-01-19
申请号：US13237576
申请日：2011-09-20
申请人： Xianqi Kong , Xinfu Wu , Abderrahim Bouzide , Isabelle Valade , David Migneault , Francine Gervais , Daniel Delorme , Benoit Bachand , Mohamed Atfani , Sophie Levesque , Bita Samim
发明人： Xianqi Kong , Xinfu Wu , Abderrahim Bouzide , Isabelle Valade , David Migneault , Francine Gervais , Daniel Delorme , Benoit Bachand , Mohamed Atfani , Sophie Levesque , Bita Samim
IPC分类号： A61K31/655 , A61K31/437 , A61K31/4462 , A61K31/4184 , A61K31/40 , A61K31/381 , A61K31/341 , A61K31/22 , A61K31/195 , A61K31/13 , C07C245/10 , C07D471/04 , C07D211/96 , A61K31/4458 , C07D235/28 , C07D207/46 , C07D409/06 , C07D333/20 , C07D307/66 , C07C317/28 , C07C309/23 , C07D307/22 , A61P43/00 , A61P25/28 , A61P25/00 , A61P27/02 , A61P3/10 , A61K31/56
CPC分类号： C07C309/19 , C07C309/14 , C07C309/21 , C07C309/24 , C07C309/26 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D207/333 , C07D209/08 , C07D209/16 , C07D209/36 , C07D209/44 , C07D209/48 , C07D209/86 , C07D211/06 , C07D211/14 , C07D211/18 , C07D211/34 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/70 , C07D211/82 , C07D213/04 , C07D213/20 , C07D213/50 , C07D213/75 , C07D213/82 , C07D217/04 , C07D219/10 , C07D231/44 , C07D233/54 , C07D235/28 , C07D257/04 , C07D275/06 , C07D277/66 , C07D295/073 , C07D295/088 , C07D307/14 , C07D307/52 , C07D317/58 , C07D327/04 , C07D327/06 , C07D327/08 , C07D333/20 , C07D333/34 , C07D409/04 , C07D471/04 , C07D471/08 , C07K5/06
摘要： Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
摘要翻译：描述了治疗或预防淀粉样蛋白相关疾病的方法，化合物，药物组合物和试剂盒。

19. 发明申请

US20110319326A1 DERIVATIVES OF BENZOTHIAZINES, PREPARATION THEREOF AND APPLICATION THEREOF AS DRUGS 有权
标题翻译：苯扎林的衍生物，其制备及其作为药物的应用
公开(公告)号：US20110319326A1
公开(公告)日：2011-12-29
申请号：US13254473
申请日：2010-03-02
申请人： Michel Perez , Marie Lamothe , Didier Junquero , Yves Rival
发明人： Michel Perez , Marie Lamothe , Didier Junquero , Yves Rival
IPC分类号： A61K31/5415 , C07D417/12 , C07D417/04 , A61K38/28 , A61P3/10 , A61P1/18 , A61P3/06 , A61P9/12 , A61P9/10 , A61P27/06 , A61P35/00 , C07D279/02 , A61P3/04
CPC分类号： C07D275/06
摘要： The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11β-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R′4 represent a hydrogen.
摘要翻译：本发明的目的是不仅在酶水平而且在细胞水平上具有抑制11＆lt; bgr--HSD1能力的苯并噻嗪衍生物。本发明的化合物具有通式（I）。其中R1表示氢或OR1表示酯或醚。 R 2表示萘基或1,2,3,4-四氢 - 萘或联苯基或苯基吡啶或取代的苯基。 R3表示甲基或乙基; R 4和R 4代表氢。

20. 发明授权

US08044100B2 Methods and compositions for treating amyloid-related diseases 有权
标题翻译：用于治疗淀粉样蛋白相关疾病的方法和组合物
公开(公告)号：US08044100B2
公开(公告)日：2011-10-25
申请号：US11316693
申请日：2005-12-21
申请人： Xianqi Kong , Xinfu Wu , Abderrahim Bouzide , Isabelle Valade , David Migneault , Francine Gervais , Daniel Delorme , Benoit Bachand , Mohamed Atfani , Sophie Levesque , Bita Samim
发明人： Xianqi Kong , Xinfu Wu , Abderrahim Bouzide , Isabelle Valade , David Migneault , Francine Gervais , Daniel Delorme , Benoit Bachand , Mohamed Atfani , Sophie Levesque , Bita Samim
IPC分类号： A61K31/185 , C07C309/14 , A61P25/28
CPC分类号： C07C309/19 , C07C309/14 , C07C309/21 , C07C309/24 , C07C309/26 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D207/333 , C07D209/08 , C07D209/16 , C07D209/36 , C07D209/44 , C07D209/48 , C07D209/86 , C07D211/06 , C07D211/14 , C07D211/18 , C07D211/34 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/70 , C07D211/82 , C07D213/04 , C07D213/20 , C07D213/50 , C07D213/75 , C07D213/82 , C07D217/04 , C07D219/10 , C07D231/44 , C07D233/54 , C07D235/28 , C07D257/04 , C07D275/06 , C07D277/66 , C07D295/073 , C07D295/088 , C07D307/14 , C07D307/52 , C07D317/58 , C07D327/04 , C07D327/06 , C07D327/08 , C07D333/20 , C07D333/34 , C07D409/04 , C07D471/04 , C07D471/08 , C07K5/06
摘要： Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
摘要翻译：描述了治疗或预防淀粉样蛋白相关疾病的方法，化合物，药物组合物和试剂盒。

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