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51. 发明授权

US08383786B2 Pesticidal compositions 有权
公开(公告)号：US08383786B2
公开(公告)日：2013-02-26
申请号：US12703880
申请日：2010-02-11
申请人： Gary D. Crouse , Thomas C. Sparks , CaSandra Lee McLeod , David A. Demeter , Zoltan L. Benko , Debra L. Camper
发明人： Gary D. Crouse , Thomas C. Sparks , CaSandra Lee McLeod , David A. Demeter , Zoltan L. Benko , Debra L. Camper
IPC分类号： C07H15/203 , C07H15/00 , C07H17/02 , A61K31/7034 , A61K31/7042 , A61K31/70 , A61K31/415 , C07D309/00
CPC分类号： C07H15/04 , A01N43/54 , A01N43/56 , A01N43/82 , C07H15/203 , C07H15/26
摘要： The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.

52. 发明申请

US20130035304A1 SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS 审中-公开
公开(公告)号：US20130035304A1
公开(公告)日：2013-02-07
申请号：US13576116
申请日：2011-01-31
申请人： Loren D. Walensky , Michelle L. Stewart , Nicole Cohen
发明人： Loren D. Walensky , Michelle L. Stewart , Nicole Cohen
IPC分类号： A61K31/7034 , C07D311/30 , A61K31/352 , A61P35/00 , C07C255/42 , A61K31/26 , C07D407/04 , A61K31/351 , C07J43/00 , A61K31/58 , C07D493/04 , A61K31/366 , C07C321/30 , A61K31/10 , C07C39/16 , A61K31/055 , C07H15/203 , C07D405/14 , A61K31/498 , A61K31/53 , C07D409/12 , A61K31/5415 , C07D279/06 , A61K31/54 , C07D409/14 , A61K31/55 , C12N5/071
CPC分类号： C07D513/04 , C07C251/20 , C07C251/84 , C07C311/20 , C07C335/16 , C07C337/08 , C07C2602/10 , C07D239/60 , C07D249/12 , C07D277/34 , C07D279/06 , C07D307/54 , C07D327/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

53. 发明申请

US20120289471A1 NOVEL COMPOUNDS WITH HIGH THERAPEUTIC INDEX 审中-公开
标题翻译：具有高效治疗指数的新型化合物
公开(公告)号：US20120289471A1
公开(公告)日：2012-11-15
申请号：US13449791
申请日：2012-04-18
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： C07K7/64 , A61K31/702 , A61K38/13 , C07D499/68 , A61K31/43 , C07H17/08 , A61K31/7048 , C07C229/36 , A61K31/223 , C07D207/16 , A61K31/401 , C07C69/612 , A61K31/24 , C07C69/757 , A61K31/215 , A61K31/616 , C07D491/16 , A61K31/436 , C07D495/04 , A61K31/4365 , C07J71/00 , A61K31/58 , A61P29/00 , A61P37/06 , C07H15/203
CPC分类号： A61K38/12 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616 , Y02A50/411
摘要： The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译：本发明涉及由与其上具有羟基，氨基，羧基或酰化衍生物的药物或药物结合的氨基酸组成的新型治疗化合物。这些高治疗指数衍生物与其制备的药物具有相同的效用，并且它们具有增强的药理学和药物性质。事实上，本发明的新型药物衍生物增强至少一种如本文所定义的治疗质量。本发明还涉及含有其的药物组合物。

54. 发明申请

US20120258043A1 Linkable Lewis X Analogs 审中-公开
标题翻译：可连接的Lewis X类似物
公开(公告)号：US20120258043A1
公开(公告)日：2012-10-11
申请号：US13456747
申请日：2012-04-26
申请人： Ramachandran RANGANATHAN , Kondareddiar RAMALINGAM , Radhakrishna PILLAI , Edmund R. MARINELLI , Rolf E. SWENSON
发明人： Ramachandran RANGANATHAN , Kondareddiar RAMALINGAM , Radhakrishna PILLAI , Edmund R. MARINELLI , Rolf E. SWENSON
IPC分类号： C07H15/203 , C07H23/00 , A61K49/00 , A61K31/7034 , A61K51/04 , A61P9/10 , A61P35/00 , A61P3/10 , A61P3/04 , A61P19/02 , A61P17/06 , A61P17/00 , C07K17/10 , A61P29/00
CPC分类号： C07H15/04 , A61K49/0002 , C07H7/02 , C07H15/00
摘要： Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.
摘要翻译：本文公开了一类可连接的四糖化合物，其包括唾液酸基路易斯X（SLeX）的氨基苯基糖苷和相关类似物。这些化合物具有可共轭的亲核基团，使其可用于制备多聚体SLeX组合物。特别地，所公开的SLeX化合物可用于通过将选择蛋白结合配体缀合物连接到报告基因部分如造影剂，放射诊断剂或细胞毒性或化学治疗剂来制备。本发明的SLeX化合物和缀合物显示出与天然唾液酸LeX相似的选择蛋白结合，因此可用于诊断和治疗选择素介导的病症和相关病症。

55. 发明申请

US20120190043A1 ENZYMATIC SUBSTRATES FOR MULTIPLE DETECTION SYSTEMS 有权
标题翻译：多种检测系统的酶基质
公开(公告)号：US20120190043A1
公开(公告)日：2012-07-26
申请号：US13438029
申请日：2012-04-03
申请人： Blas Cerda , Mark Norman Bobrow
发明人： Blas Cerda , Mark Norman Bobrow
IPC分类号： G01N33/573 , C12Q1/00 , C12Q1/34 , C07H15/203
CPC分类号： C12Q1/34 , C07C237/22 , C07H15/203 , C07K5/06 , C07K19/00 , G01N2333/924 , G01N2458/15
摘要： An inventive substrate is provided which includes a substrate compound of formula A-B1-B2-B3-B4: wherein A is a sugar moiety; B1 is a linker moiety allowing the conjugation of moiety A and the remaining structure of the substrate; B2 is a linker moiety with a free reactive amino group so as to be available for reaction with carboxylic acids or detectable tags; B3 contains a permanently charged element such as a quaternary ammonium group so as to increase sensitivity for mass spectrometry analysis; and B4 of various carbon length conferring specificity amongst individual substrates in detection methods. Also provided is a molecule of the formula B1-B2-B3-B4, with similar structural characteristics to an enzymatic product produced by the action of a target enzyme on an inventive substrate. Further provided are methods for using inventive substrates for detecting enzymatic activity.
摘要翻译：提供了本发明的底物，其包括式A-B1-B2-B3-B4的底物化合物：其中A是糖部分; B1是连接部分，允许部分A与底物的剩余结构共轭; B2是具有游离反应性氨基的接头部分，以便可用于与羧酸或可检测标签反应; B3含有永久带电元件如季铵基，以提高质谱分析的灵敏度; 和各种碳长度的B4在检测方法中在各个底物之间赋予特异性。还提供了式B1-B2-B3-B4的分子，其与通过靶酶在本发明底物上的作用产生的酶产物具有相似的结构特征。还提供了使用本发明的底物检测酶活性的方法。

56. 发明申请

US20120053330A1 Chemical Process 审中-公开
标题翻译：化学工艺
公开(公告)号：US20120053330A1
公开(公告)日：2012-03-01
申请号：US13265001
申请日：2010-04-29
申请人： Daniel Edward Patterson , Michael S. McClure , Jeremiah David Powers , Claire Frances Crawford , Malcolm Brian Berry
发明人： Daniel Edward Patterson , Michael S. McClure , Jeremiah David Powers , Claire Frances Crawford , Malcolm Brian Berry
IPC分类号： C07H17/02 , C07H15/04 , C07H15/26 , C07H15/203
CPC分类号： C07D409/04 , C07H1/00 , C07H15/04 , C07H15/203 , C07H17/02
摘要： Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes and intermediates for preparing the same.
摘要翻译：本文公开的是制备吡喃葡萄糖氧吡唑衍生物的方法。特别地，本发明涉及具有SGLT2抑制活性的吡喃葡萄糖氧吡唑衍生物及其制备方法和中间体。

57. 发明申请

US20110251068A1 PARASITIC PLANT CONTROL AGENT AND PARASITIC PLANT CONTROL METHOD 审中-公开
标题翻译： PARASITIC植物控制剂和PARASITIC植物控制方法
公开(公告)号：US20110251068A1
公开(公告)日：2011-10-13
申请号：US13125337
申请日：2009-10-05
申请人： Atsushi Okazawa , Joseph Benesh
发明人： Atsushi Okazawa , Joseph Benesh
IPC分类号： A01N43/58 , C07D303/14 , C07D237/04 , C07D211/76 , A01P21/00 , C07D487/04 , A01N43/40 , A01N43/20 , A01N43/16 , A01N43/90 , C07D211/46 , C07H15/203
CPC分类号： C07D211/76 , A01N43/16 , A01N43/20 , A01N43/40 , A01N43/58 , A01N43/90 , C07D211/46 , C07D237/04 , C07D303/14 , C07D487/04
摘要： Disclosed is a parasitic plant control agent which can control a parasitic plant effectively. Also disclosed is a parasitic plant control method. A parasitic plant can be controlled by inhibiting the metabolism of gentianose in the parasitic plant to inhibit the germination of the parasitic plant.
摘要翻译：公开了一种可有效控制寄生植物的寄生植物控制剂。还公开了寄生植物控制方法。寄生植物可以通过抑制寄生植物中龙胆草的代谢来抑制寄生植物的发芽来控制。

58. 发明申请

US20110237529A1 Adenosine Analogs and Their Use 失效
标题翻译：腺苷类似物及其用途
公开(公告)号：US20110237529A1
公开(公告)日：2011-09-29
申请号：US12515033
申请日：2007-11-16
申请人： Efrat Ben-Zeev , Vincent Jacques , Yael Marantz , A. Sekar Reddy , Zhaoda Zhang , Oren Becker , Dilara Mccauley , Pini Orbach , Sharon Shacham , Ashis K. Saha , Michael Xie
发明人： Efrat Ben-Zeev , Vincent Jacques , Yael Marantz , A. Sekar Reddy , Zhaoda Zhang , Oren Becker , Dilara Mccauley , Pini Orbach , Sharon Shacham , Ashis K. Saha , Michael Xie
IPC分类号： A61K31/7076 , C07H15/203 , C07H7/04 , C07H7/06 , C07H17/02 , C07H19/20 , A61K31/7064 , A61P11/00 , A61P1/04 , A61P1/02 , A61P1/00 , A61P1/10 , C12N5/071
CPC分类号： A61K31/7076 , A61K31/7034 , A61K31/7072 , C07H15/203 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： The invention provides adenosine analog compounds that act at P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.
摘要翻译：本发明提供了在P2Y受体（例如P2Y2受体）上起作用的腺苷类似物化合物，包括药物组合物; （COPD），哮喘，便秘，慢性特发性便秘，口干（口腔干燥症），牙龈疾病，以及由辐射和化学治疗癌症引起的胃肠道问题。

59. 发明申请

US20090291904A1 CHEMICAL DERIVATIVES OF JASMONATE, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：佐剂的化学衍生物，药物组合物及其使用方法
公开(公告)号：US20090291904A1
公开(公告)日：2009-11-26
申请号：US12095908
申请日：2006-12-07
申请人： Yoel Kashman , Eliezer Flescher , Max Herzberg
发明人： Yoel Kashman , Eliezer Flescher , Max Herzberg
IPC分类号： A61K31/7004 , C07D215/48 , C07H15/203 , A61K31/47 , C12N5/06 , A61P35/00
CPC分类号： C07D215/32 , C07C49/493 , C07C69/007 , C07C69/716 , C07C69/738 , C07C235/78 , C07C2601/02 , C07C2601/08 , C07F7/1804 , C07H13/08
摘要： The present invention relates to novel jasmonate derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers.
摘要翻译：本发明涉及新颖的茉莉酸衍生物，其制备方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物，特别是作为预防和治疗癌症的化学治疗剂的方法。

60. 发明申请

US20090029006A1 Oral Cavity Stimulating Substance 有权
标题翻译：口腔刺激物质
公开(公告)号：US20090029006A1
公开(公告)日：2009-01-29
申请号：US11791651
申请日：2005-11-29
申请人： Norihiko Kageyama , Takako Inui , Koichi Nakahara , Hajime Komura
发明人： Norihiko Kageyama , Takako Inui , Koichi Nakahara , Hajime Komura
IPC分类号： C07H15/26 , C07H15/203 , C12C7/00 , A23L2/00
CPC分类号： C12C5/026 , A23L2/56 , A23L27/2052 , C07H15/203 , C12C5/00 , C12C7/042
摘要： A novel compound causing an oral cavity stimulus such as acridness, which is expressed by the following structural formula (I):
摘要翻译：引起口腔刺激如痤疮的新型化合物，其由以下结构式（I）表示：

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