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61. 发明申请

US20170260124A1 NO- AND H2S- RELEASING COMPOUNDS 审中-公开
公开(公告)号：US20170260124A1
公开(公告)日：2017-09-14
申请号：US15605195
申请日：2017-05-25
申请人： RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
发明人： Khosrow Kashfi , Ravinder Kodela
IPC分类号： C07C203/04 , C07F9/6558 , C07D413/12 , C07D339/04 , C07D271/08 , C07C331/28 , C07C327/48 , A61K31/655 , C07F9/6578
CPC分类号： C07C203/04 , A61K31/655 , C07C327/48 , C07C331/28 , C07D271/08 , C07D339/04 , C07D413/12 , C07F9/65583 , C07F9/6578
摘要： This disclosure relates to compounds containing both an NO-releasing moiety and an H2S-releasing moiety and the use of such compounds in treating inflammatory diseases, including cancers.

62. 发明授权

US09458102B2 Derivatives of tetracaine 有权
标题翻译：丁卡因的衍生物
公开(公告)号：US09458102B2
公开(公告)日：2016-10-04
申请号：US13715334
申请日：2012-12-14
申请人： OREGON HEALTH & SCEINCE UNIVERSITY , WILLAMETTE UNIVERSITY
发明人： Jeffrey Karpen , Sarah Kirk , Adriana Andrade , Michelle Schaffer , Kenneth Melich
IPC分类号： A61K31/01 , A61K31/075 , A61K31/095 , A61K31/13 , A61K31/16 , A61K31/21 , C07C327/48 , C07C237/34 , C07C229/60 , C07C229/64 , C07C255/58
CPC分类号： C07C327/48 , A61K31/01 , A61K31/075 , A61K31/095 , A61K31/13 , A61K31/16 , A61K31/21 , C07C229/60 , C07C229/64 , C07C237/34 , C07C255/58
摘要： Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.
摘要翻译：本文公开了丁卡因的衍生物，其中尤其是阻断环核苷酸门控（CNG）通道，并且可用于治疗特征在于过度活跃的CNG通道如视网膜变性疾病的疾病。

63. 发明授权

US09089133B2 Insecticide for agricultural or horticultural use and method of use thereof 有权
标题翻译：农业或园艺用杀虫剂及其使用方法
公开(公告)号：US09089133B2
公开(公告)日：2015-07-28
申请号：US13419063
申请日：2012-03-13
申请人： Kei Yoshida , Takeo Wakita , Hiroyuki Katsuta , Akiyoshi Kai , Yutaka Chiba , Kiyoshi Takahashi , Hiroko Kato , Nobuyuki Kawahara , Michikazu Nomura , Hidenori Daido , Junji Maki , Shinichi Banba , Atsuko Kawahara
发明人： Kei Yoshida , Takeo Wakita , Hiroyuki Katsuta , Akiyoshi Kai , Yutaka Chiba , Kiyoshi Takahashi , Hiroko Kato , Nobuyuki Kawahara , Michikazu Nomura , Hidenori Daido , Junji Maki , Shinichi Banba , Atsuko Kawahara
IPC分类号： C07C233/65 , C07C211/52 , C07C237/40 , C07C317/44 , C07C327/48 , C07C333/08 , C07C323/33 , A01N47/20 , C07C211/47 , C07C211/48 , C07C215/68 , C07C265/12 , C07C271/28 , C07C317/18 , C07C317/36 , C07C317/40 , C07C323/12 , C07C323/36 , C07C323/42 , C07D213/81
CPC分类号： A01N47/20 , C07C211/47 , C07C211/48 , C07C215/68 , C07C237/40 , C07C265/12 , C07C271/28 , C07C317/18 , C07C317/36 , C07C317/40 , C07C323/12 , C07C323/36 , C07C323/42 , C07C327/48 , C07C333/08 , C07C2601/04 , C07C2601/08 , C07D213/81
摘要： Aniline derivatives represented by formula (8) and formula (9): The aniline derivatives can be used as insecticides.
摘要翻译：由式（8）和式（9）表示的苯胺衍生物：苯胺衍生物可用作杀虫剂。

64. 发明申请

US20120078013A1 METHOD FOR PRODUCING 4-SUBSTITUTED BENZOTHIOAMIDE DERIVATIVE 审中-公开
标题翻译：生产4-取代苯并二恶英衍生物的方法
公开(公告)号：US20120078013A1
公开(公告)日：2012-03-29
申请号：US13376743
申请日：2010-06-08
申请人： Satoshi Sugiura
发明人： Satoshi Sugiura
IPC分类号： C07C327/48
CPC分类号： C07C327/48
摘要： Disclosed is a method appropriate for safely, economically and easily producing at a high yield a 4-substituted benzothioamide derivative which is useful as an intermediate in the production of a 2-(3-cyanophenyl)thiazole derivative useful as a drug for gout. Specifically disclosed is a method for producing a 4-substituted benzothioamide derivative represented by formula (A).
摘要翻译：公开了一种适合安全，经济和容易地以高产率生产4-取代的苯并硫代酰胺衍生物的方法，其可用作制备用作痛风药物的2-（3-氰基苯基）噻唑衍生物作为中间体。具体公开了由式（A）表示的4-取代苯并硫代酰胺衍生物的制造方法。

65. 发明申请

US20110319616A1 THIAZOLE DERIVATIVE AND PROCESS FOR PRODUCING SAME 有权
标题翻译：噻唑衍生物及其生产方法
公开(公告)号：US20110319616A1
公开(公告)日：2011-12-29
申请号：US13255202
申请日：2010-03-08
申请人： Toshiaki Murai
发明人： Toshiaki Murai
IPC分类号： C07D417/04 , C07D417/14 , C07C327/42 , C07D409/12 , C07D295/194 , C07D213/59 , C07D401/12 , C07D277/18 , C07C327/48
CPC分类号： C07D277/18 , C07D277/42 , C07D417/04 , C07D417/14
摘要： An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.
摘要翻译：目的是通过简化的生产方法提供由容易获得的原料制备的噻唑衍生物。提供一种制备由通式（I）表示的新型噻唑衍生物的方法，其特征在于将强碱加入由通式（II）表示的硫代酰胺，并将该混合物与通式（III）和一种新的噻唑衍生物。

66. 发明申请

US20110144373A1 WATER-SOLUBLE DEGRADABLE PHOTO-CROSSLINKER 审中-公开
标题翻译：水溶性可降解照相机
公开(公告)号：US20110144373A1
公开(公告)日：2011-06-16
申请号：US12965020
申请日：2010-12-10
申请人： Dale G. Swan , Emily Rose Rolfes Meyering , Aleksey V. Kurdyumov , Peter H. Duquette , Robert W. Hergenrother , Toni M. Heyer
发明人： Dale G. Swan , Emily Rose Rolfes Meyering , Aleksey V. Kurdyumov , Peter H. Duquette , Robert W. Hergenrother , Toni M. Heyer
IPC分类号： C07C271/58 , C07C309/61 , C07C69/78 , C07C327/48
CPC分类号： G03F7/031 , C07C309/42 , C07C333/08 , C08F2/50 , G03F7/165
摘要： Described herein is a degradable linking agent that includes a core molecule with one or more charged groups; and one or more photoreactive groups covalently attached to the core molecule by one or more degradable linkers.
摘要翻译：本文描述的是可降解的连接剂，其包括具有一个或多个带电基团的核心分子; 和一个或多个可通过一个或多个可降解接头与核心分子共价连接的光反应基团。

67. 发明授权

US06919339B2 ABCA-1 elevating compounds 失效
标题翻译： ABCA-1升高化合物
公开(公告)号：US06919339B2
公开(公告)日：2005-07-19
申请号：US10005064
申请日：2001-12-04
申请人： Michael Campbell , Prabha N. Ibrahim , Jeff A. Zablocki , Richard Lawn
发明人： Michael Campbell , Prabha N. Ibrahim , Jeff A. Zablocki , Richard Lawn
IPC分类号： A61K45/00 , A61K31/085 , A61K31/136 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/357 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/53 , A61K45/06 , A61P3/06 , A61P9/00 , A61P9/10 , A61P43/00 , C07C237/04 , C07C237/06 , C07C237/22 , C07C237/40 , C07C275/26 , C07C311/20 , C07C323/36 , C07C323/40 , C07C323/60 , C07C327/42 , C07C327/44 , C07C327/48 , C07C335/16 , C07D215/38 , C07D217/24 , C07D239/48 , C07D251/16 , C07D251/22 , C07D251/52 , C07D319/08 , C07D319/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
CPC分类号： C07D319/08 , A61K31/53 , A61K45/06 , C07C237/06 , C07C237/22 , C07C237/40 , C07C275/26 , C07C311/20 , C07C323/36 , C07C323/40 , C07C323/60 , C07C327/42 , C07C327/48 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07C2602/40 , C07C2602/42 , C07C2603/74 , C07D251/16 , C07D251/52 , C07D409/12 , A61K2300/00
摘要： The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.
摘要翻译：本发明提供了提高ABCA-1基因的细胞表达，促进来自细胞的胆固醇流出并增加哺乳动物，特别是人的血浆中的HDL水平的化合物。该化合物可用于治疗冠状动脉疾病。

68. 发明申请

US20040127739A1 Novel n-p-propargyloxyphenethyl-thioacetic acid amides 失效
标题翻译：新型对 - 丙酰氧基苯乙基 - 硫代乙酸酰胺
公开(公告)号：US20040127739A1
公开(公告)日：2004-07-01
申请号：US10472577
申请日：2003-09-23
发明人： Walter Kunz , Clemens Lamberth , Fredrik Cederbaum , Martin Zeller
IPC分类号： C07C327/48
CPC分类号： C07C327/44 , A01N37/36 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/30 , A01N43/32 , A01N43/40 , A01N43/54
摘要： The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkynylsulfonyl or a group nullOnullCOnullR11, nullOnullCOnullOnullR11 or nullOnullCOnullCOnullOnullR11 wherein R11 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. 1
摘要翻译：本发明涉及通式（I）的N-炔丙氧基 - 苯乙基硫代乙酰胺衍生物，其包括其旋光异构体和这些异构体的混合物，其中R 1为氢，烷基，环烷基或任选取代的芳基，R 2和R 3各自独立地为氢或烷基，R4是烷基，烯基或炔基，R5，R6，R7和R8各自独立地是氢或烷基，R9是氢，任选取代的烷基，任选取代的烯基或任选取代的炔基，R 10是任选取代的芳基或任选取代的杂芳基，Z是羟基，任选取代的芳氧基，任选取代的烷氧基，任选取代的炔氧基，任选取代的芳硫基，任选取代的烷硫基，任选取代的炔硫基，任选取代的烷基亚磺酰基，任选取代的烯基亚磺酰基，任选取代的炔基亚磺酰基，任选取代的烷基磺酰基，，选择取代的炔基磺酰基或基团-O-CO-R11，-O-CO-O-R11或-O-CO-CO-O-R11，其中R11是氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基或任选地取代的杂芳基。这些化合物具有有用的植物保护性质，并且可有利地用于农业实践中以控制或防止植物病原微生物特别是真菌侵染植物。

69. 发明申请

US20040014975A1 Synthesis of selective androgen receptor modulators 有权
标题翻译：选择性雄激素受体调节剂的合成
公开(公告)号：US20040014975A1
公开(公告)日：2004-01-22
申请号：US10277108
申请日：2002-10-22
发明人： James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
IPC分类号： C07F009/28 , C07D209/14 , C07D209/04 , C07D215/20 , C07D215/16 , C07C391/02 , C07C327/48 , C07C311/45 , C07C271/26
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N30/7233 , G01N33/5438 , G01N33/74 , G01N2030/8813
摘要： The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
摘要翻译：本发明涉及一种用于制备新型雄激素受体靶向剂（ARTA）的合成方法，其表现出雄激素受体的非甾族化合物的雄激素和合成代谢活性。这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防慢性肌肉消瘦; e）降低前列腺癌的发生率，停止或导致消退; f）口服雄激素替代和/或其他临床治疗和/或诊断领域。本发明的方法适用于大规模制备，因为所有步骤都产生高纯度的化合物，因此避免了复杂的纯化方法，从而降低产率。因此，本发明提供了可用于工业大规模合成的非甾体激动剂化合物的合成方法，并以高产率提供高纯度产品。

70. 发明申请

US20030119914A1 Taxol enhancer compounds 失效
标题翻译：紫杉醇增强剂化合物
公开(公告)号：US20030119914A1
公开(公告)日：2003-06-26
申请号：US10193075
申请日：2002-07-10
申请人： Shionogi BioResearch Corp.
发明人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono
IPC分类号： A61K031/16 , C07C327/48
CPC分类号： A61K47/48176 , A61K31/16 , A61K31/165 , A61K31/277 , A61K31/337 , A61K31/381 , A61K31/44 , A61K31/505 , A61K31/53 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D305/14 , C07D307/68 , C07D333/38 , C07D333/68 , C07D407/12
摘要： Disclosed is a compound represented by the Structural Formula (I): 1 Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >CnullZ groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or nullC(R7R8)null. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently nullH, an aliphatic or substituted aliphatic group, or R7 is nullH and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is nullO or nullS. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.
摘要翻译：公开了由结构式（I）表示的化合物：Y是共价键，亚苯基或取代或未取代的直链烃基。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选Y为共价键或-C（R 7 R 8） - 。 R 1和R 2独立地是芳基或取代的芳基，R 3和R 4独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了通过向受试者施用结构式（I）的化合物与紫杉醇或紫杉醇的类似物组合治疗患有癌症的受试者的方法。

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