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51. 发明申请

US20100227892A1 Compounds, Compositions and Methods for Treatment and Prevention of Orthopoxvirus Infections and Associated Diseases 有权
标题翻译：用于治疗和预防正痘病毒感染和相关疾病的化合物，组合物和方法
公开(公告)号：US20100227892A1
公开(公告)日：2010-09-09
申请号：US12752462
申请日：2010-04-01
申请人： Robert Jordan , Thomas R. Bailey , Susan R. Rippin
发明人： Robert Jordan , Thomas R. Bailey , Susan R. Rippin
IPC分类号： A61K31/4439 , A61K31/343 , C07D307/77 , A61K31/403 , C07D209/56 , C07D401/12 , C07D209/48 , A61K31/4178 , C07D277/593 , A61P31/12
CPC分类号： A61K31/403 , A61K31/407 , A61K31/4439
摘要： Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
摘要翻译：使用二，三和四环酰肼衍生物和类似物的方法以及含有它们的药物组合物用于治疗或预防病毒感染和与之相关的疾病，特别是由正痘病毒引起的那些病毒感染和相关疾病。

52. 发明申请

US20100168413A1 ONE-POT SYNTHESIS OF BENZISOINDOLENINES USED IN THE PREPARATION OF NAPHTHALOCYANINES 失效
标题翻译：用于制备萘二甲酸的苯并咪唑的一步合成
公开(公告)号：US20100168413A1
公开(公告)日：2010-07-01
申请号：US12709509
申请日：2010-02-21
申请人： Sutharsiny Indusegaram , Simone Charlotte Vonwiller , Damon Donald Ridley , Kia Silverbrook
发明人： Sutharsiny Indusegaram , Simone Charlotte Vonwiller , Damon Donald Ridley , Kia Silverbrook
IPC分类号： C09B47/073 , C07D209/56
CPC分类号： C09B47/06 , C09D11/50
摘要： A method of effecting a one-pot conversion of a tetrahydronaphthalic anhydride of formula (I): to a nitrate salt of a benzisoindolenine of formula (II): The method comprises heating the tetrahydronaphthalic anhydride of formula (I) with a reagent mixture comprising ammonium nitrate so as to effecting concomitant dehydrogenation during the conversion.
摘要翻译：一种将式（I）的四氢化邻苯二甲酸酐转化为式（II）的苯并异吲哚宁的硝酸盐的方法：该方法包括用包含铵的试剂混合物加热式（I）的四氢邻苯二甲酸酐硝酸盐，以便在转化期间进行伴随的脱氢。

53. 发明申请

US20100168096A1 ACYLGUANIDINE DERIVATIVE OR SALT THEREOF 失效
标题翻译：乙酰胺衍生物或其盐
公开(公告)号：US20100168096A1
公开(公告)日：2010-07-01
申请号：US11997956
申请日：2006-08-07
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
IPC分类号： A61K31/5377 , C07C69/76 , C07D209/56 , C07D401/02 , C07D413/02 , C07D221/16 , C07D211/00 , A61K31/24 , A61K31/403 , A61K31/4439 , A61K31/4355 , A61P1/06 , A61P1/12
CPC分类号： C07D209/88 , C07D221/16 , C07D265/38 , C07D333/78 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D471/04 , C07D491/10 , C07D495/10
摘要： [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine.[Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
摘要翻译： [问题]提供可用于预防和/或治疗5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛 [解决方法]发现具有三环结构的酰基胍衍生物或其药学上可接受的盐具有对5-HT 2B受体和5-HT7受体的强拮抗作用。此外，与单次使用对任一受体选择性拮抗剂的情况相比，本发明对两种受体具有拮抗作用的化合物显示出优异的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。

54. 发明申请

US20100113476A1 CHEMICAL LINKERS WITH SINGLE AMINO ACIDS AND CONJUGATES THEREOF 有权
标题翻译：具有单一氨基酸的化学连接体及其结合体
公开(公告)号：US20100113476A1
公开(公告)日：2010-05-06
申请号：US12528316
申请日：2008-02-20
申请人： Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Nils Lonberg , Qian Zhang
发明人： Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Nils Lonberg , Qian Zhang
IPC分类号： A61K31/496 , C07D209/56 , C07K16/00 , A61K31/403 , C12N5/00 , C07D403/02 , A61P35/00
CPC分类号： C07D405/14 , A61K47/65 , A61K47/6889 , C07D403/14 , C07D487/04 , C07K1/13
摘要： The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
摘要翻译：本公开提供了药物 - 配体缀合物，其是有效的细胞毒素并且包括药物和配体之间的接头，其中接头具有单个氨基酸。本公开还涉及含有药物 - 配体缀合物的组合物以及使用它们的治疗方法。

55. 发明申请

US20100048916A1 HIGH-PURITY TEXAPHYRIN METAL COMPLEXES 有权
标题翻译：高纯度丝印金属复合物
公开(公告)号：US20100048916A1
公开(公告)日：2010-02-25
申请号：US12611896
申请日：2009-11-03
申请人： Hugo MADDEN , Greg HEMMI , Tarak MODY
发明人： Hugo MADDEN , Greg HEMMI , Tarak MODY
IPC分类号： C07D209/56 , C07C43/20
CPC分类号： C07F5/00 , A61K31/555 , A61K45/00 , C07C41/16 , C07C43/2055 , C07C205/37 , C07D487/22 , C07F5/003
摘要： Disclosed herein are the methods and compositions for the improved synthesis of texaphyrin metal complexes. The improved synthesis results in high-purity compositions of texaphyrin metal complexes in which more than about 98% of the texaphyrin metal complexes in the composition have the same structure and/or the same molecular weight. Further described herein are pharmaceutical compositions comprising such high-purity compositions, and the use of such high-purity compositions in the treatment of cancer and cardiovascular diseases and disorders.
摘要翻译：本文公开了用于改进合成特沙弗林金属络合物的方法和组合物。改进的合成导致特沙弗林金属络合物的高纯度组合物，其中组合物中超过约98％的特沙弗林金属络合物具有相同的结构和/或相同的分子量。本文进一步描述的是包含这种高纯度组合物的药物组合物，以及这些高纯度组合物在治疗癌症和心血管疾病和病症中的用途。

56. 发明授权

US07655661B2 Prodrugs of CC-1065 analogs 失效
标题翻译： CC-1065类似物的前药
公开(公告)号：US07655661B2
公开(公告)日：2010-02-02
申请号：US12144612
申请日：2008-06-23
申请人： Robert Yongxin Zhao , Ravi V. J. Chari
发明人： Robert Yongxin Zhao , Ravi V. J. Chari
IPC分类号： A61K31/497 , C07D209/56
CPC分类号： C07D307/85 , A61K31/407 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/675 , A61K47/545 , A61K47/548 , A61K47/60 , C07D209/42 , C07D209/60 , C07D403/14 , C07D405/12 , C07F9/5728 , C07F9/65583 , Y02A50/423 , Y02A50/491 , Y02P20/55
摘要： Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.
摘要翻译：具有可切割保护基的抗肿瘤抗生素CC-1065类似物的前药，例如哌嗪基氨基甲酸酯，4-哌啶子基 - 哌啶子基氨基甲酸酯或磷酸酯，其中保护基团赋予增强的水溶性和在前药上的稳定性，其中前药还具有可与细胞结合试剂例如抗体缀合的部分，例如二硫化物。还描述了这种前药缀合物的治疗用途; 这种细胞毒性药物的前药具有治疗用途，因为它们可以将细胞毒性前药递送至特定的细胞群，以靶向方式酶促转化成细胞毒性药物。

57. 发明申请

US20090275142A1 COMPOSITIONS AND METHODS FOR BIODETECTION BY NUCLEIC ACID-TEMPLATED CHEMISTRY 失效
标题翻译：通过核酸化学化学的生物防治的组合物和方法
公开(公告)号：US20090275142A1
公开(公告)日：2009-11-05
申请号：US12391898
申请日：2009-02-24
申请人： Yumei Huang , James M. Coull
发明人： Yumei Huang , James M. Coull
IPC分类号： G01N33/68 , G01N33/00 , C07D209/04 , C07H21/04 , C07C229/40 , C07D207/46 , C07D209/56
CPC分类号： C07H21/04 , C07D209/08 , C07D209/14 , C07D209/56 , C07D209/58 , C09B23/0091 , C09B23/105 , G01N33/5308 , G01N33/533 , Y10T436/143333 , Y10T436/145555
摘要： The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.
摘要翻译：本发明提供了通过核酸模板化学，例如通过产生荧光聚甲炔染料来检测生物学靶标（例如核酸和蛋白质）的组合物和方法。

58. 发明授权

US07550500B2 Bicyclic and tricyclic amines as modulators of chemokine receptor activity 有权
标题翻译：双环和三环胺作为趋化因子受体活性的调节剂
公开(公告)号：US07550500B2
公开(公告)日：2009-06-23
申请号：US11225227
申请日：2005-09-13
申请人： John V Duncia , Joseph B Santella, III , Daniel S Gardner , Dean A Wacker
发明人： John V Duncia , Joseph B Santella, III , Daniel S Gardner , Dean A Wacker
IPC分类号： C07D209/56 , A61K31/40 , A61D29/00
CPC分类号： C07D451/02 , C07D209/60 , C07D209/62 , C07D221/08 , C07D221/18 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D453/06 , C07D471/08
摘要： The present application describes modulators of CCR3 of formula (I): A—E—NR1—G (I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.
摘要翻译：本申请描述了式（I）的CCR3的调节剂：<？in-line-formula description =“In-line Formulas”end =“lead”？> AE-NR1-G（I）<βin-line-formula 描述=“内联式”末端=“尾”→其药学上可接受的盐形式，可用于预防炎性疾病如哮喘和其他过敏性疾病。

59. 发明申请

US20090149660A1 OPTICAL RECORDING MATERIAL AND OPTICAL RECORDING MEDIA 审中-公开
标题翻译：光学记录材料和光学记录介质
公开(公告)号：US20090149660A1
公开(公告)日：2009-06-11
申请号：US12067754
申请日：2006-09-25
申请人： Masahiro Shinkai , Atsushi Monden , Motohiro Inoue
发明人： Masahiro Shinkai , Atsushi Monden , Motohiro Inoue
IPC分类号： C07D209/56
CPC分类号： G11B7/249 , C09B23/0075 , C09B23/06 , C09B45/14 , C09B67/0041 , G11B7/2467 , G11B7/2472 , G11B7/2532 , G11B2007/24612
摘要： An optical recording medium provided with a recording layer that comprises a cation represented by the following general formula (1) and a chelate compound of an azo compound represented by the following general formula (2) and a metal. In the formulas, R1-R4 each independently represent a monovalent group represented by Chemical Formula (10) below or other groups, R5 and R6 each independently represent an optionally substituted alkyl group or other groups, R7 represents a hydrogen atom or other groups, Q1 and Q2 each independently represent a group that forms an optionally substituted benzene ring or other groups, at least one from among R1-R4 is a monovalent group represented by Chemical Formula (10) below, [Chemical Formula 2] [CH2═CH—CH2 (10) and at least one of Ar1 and Ar2 is an aryl or other group having a substituent capable of coordinating with a metal atom.
摘要翻译：一种具有记录层的光记录介质，该记录层包括由以下通式（1）表示的阳离子和由以下通式（2）表示的偶氮化合物的螯合化合物和金属。式中，R 1 -R 4各自独立地表示由下述化学式（10）表示的一价基团或其它基团，R 5和R 6各自独立地表示任选取代的烷基或其它基团，R 7表示氢原子或其它基团，Q 1 和Q2各自独立地表示形成任选取代的苯环或其它基团的基团，R 1 -R 4中的至少一个为下述化学式（10）表示的一价基团，<β在线式描述=“In “公式”end =“lead”？> [化学式2] <？in-line-formula description =“In-line Formulas”end =“tail”？> <？in-line-formula description =“In- 线公式“end =”lead“？> [CH2-CH-CH2（10）<？in-line-formula description =”In-line Formulas“end =”tail“？>和Ar1和Ar2中的至少一个是具有能够与金属原子配位的取代基的芳基或其它基团。

60. 发明申请

US20090054652A1 Cyanine Compound and Optical Recording Material 失效
标题翻译：花青化合物和光学记录材料
公开(公告)号：US20090054652A1
公开(公告)日：2009-02-26
申请号：US12295449
申请日：2007-03-23
申请人： Toru Yano , Satoshi Yanagisawa , Yohei Aoyama , Koichi Shigeno
发明人： Toru Yano , Satoshi Yanagisawa , Yohei Aoyama , Koichi Shigeno
IPC分类号： C07D215/00 , C07D417/02 , C07D209/56 , C07D263/52 , C07D235/02
CPC分类号： C07F17/02 , C09B23/04 , G11B7/2467 , G11B7/2472 , G11B7/249 , G11B7/2492 , G11B7/2495
摘要： A cyanine compound is represented by formula (I): A1: benzene or naphthalene ring. A3: 5- or 6-membered ring. R1, R2: hydrogen atom and the like. R7: an alkyl group and the like. R12: a substituent by formula (II) or (II′). R20: a hydrogen atom and the like. Anq-: a q-valent anion. q: 1 or 2; p: a coefficient for neutral charge. In formula (II): bond between L and T is a double, conjugated double, or triple bond. L: carbon atom. T: carbon, oxygen, sulfur, or nitrogen atom. x, y, z: 0 or 1. s: 0-4. R13: hydrogen atom and the like. R14, R15, and R16: hydrogen atom and the like. In formula (II′), the bond between L′ and T′ is a double or conjugated double bond. L′: carbon atom. T′: carbon, oxygen, nitrogen atom. s′: 0-4. Ring containing L′ and T′: 5-membered ring, may contain a heteroatom.
摘要翻译：花青化合物由式（I）表示：A1：苯或萘环。 A3：5-或6-元环。 R1，R2：氢原子等。 R7：烷基等。 R 12：式（II）或（II'）的取代基。 R 20：氢原子等。 Anq-：q价阴离子。 q：1或2; p：中性电荷系数。在式（II）中：L和T之间的键是双键，共轭双键或三键。 L：碳原子 T：碳，氧，硫或氮原子。 x，y，z：0或1. s：0-4。 R 13：氢原子等。 R14，R15和R16：氢原子等。在式（II'）中，L'和T'之间的键是双键或共轭双键。 L'：碳原子。 T'：碳，氧，氮原子。 s'：0-4。含有L'和T'的环：5元环可含有杂原子。

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