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51. 发明授权

US09695135B2 Therapeutic catechols 有权
公开(公告)号：US09695135B2
公开(公告)日：2017-07-04
申请号：US14709108
申请日：2015-05-11
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
发明人： Edmond J. LaVoie , Eddy Arnold , Joseph D. Bauman , John E. Kerrigan , Ajit K. Parhi , Kalyan Das , Cody Kelley , Dishaben V. Patel
IPC分类号： C07D257/04 , C07C205/22 , C07C255/53 , C07C39/15 , C07C39/367 , C07C205/26
CPC分类号： C07D257/04 , C07C39/15 , C07C39/367 , C07C205/22 , C07C205/26 , C07C255/53
摘要： The invention provides compounds of formula I: and salts thereof wherein R1-R4 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts, and methods for their use in therapy. The compounds have useful antiviral properties.

52. 发明授权

US09458128B2 Catechol O-methyltransferase activity inhibiting compounds 有权
标题翻译：儿茶酚O-甲基转移酶活性抑制化合物
公开(公告)号：US09458128B2
公开(公告)日：2016-10-04
申请号：US14403023
申请日：2013-05-23
申请人： Orion Corporation
发明人： Marko Ahlmark , David Din Belle , Mika Kauppala , Anne Luiro , Taina Pajunen , Jarmo Pystynen , Eija Tiainen , Matti Vaismaa , Josef Messinger
IPC分类号： C07C205/56 , C07C255/57 , C07C255/53 , C07C255/51 , C07C229/42 , C07D333/60 , C07C255/54 , C07D333/24 , C07C311/29 , C07D207/337 , C07D277/30 , C07D295/192 , C07D213/57 , C07D307/54 , C07D307/80 , C07D309/06 , C07D309/12 , C07D231/12 , C07D231/14 , C07D333/28 , C07D333/70 , C07D277/34 , C07D277/74 , C07D211/14 , C07D295/155 , C07D213/62 , C07C255/59 , C07C309/66 , C07C317/46 , C07C323/62 , A61K31/198 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/382 , A61K31/40 , A61K31/5377 , C07C323/29 , C07D307/81 , C07D309/22
CPC分类号： A61K31/277 , A61K31/198 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/382 , A61K31/40 , A61K31/5377 , C07C255/53 , C07C255/54 , C07C255/57 , C07C255/59 , C07C309/66 , C07C311/29 , C07C317/46 , C07C323/29 , C07C323/62 , C07D207/337 , C07D211/14 , C07D213/57 , C07D213/62 , C07D231/12 , C07D231/14 , C07D277/30 , C07D277/34 , C07D277/74 , C07D295/155 , C07D295/192 , C07D307/54 , C07D307/80 , C07D307/81 , C07D309/06 , C07D309/12 , C07D309/22 , C07D333/24 , C07D333/28 , C07D333/60 , C07D333/70
摘要： Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.
摘要翻译：式（I）化合物，其中R 1如权利要求中所定义，表现出COMT酶抑制活性，因此可用作COMT抑制剂。还公开了治疗方法和药物剂型。

53. 发明授权

US09440913B2 Dihydroxybenzene derivatives and antiprotozoal agent comprising same as active ingredient 有权
标题翻译：二羟基苯衍生物和包含与活性成分相同的抗原虫剂
公开(公告)号：US09440913B2
公开(公告)日：2016-09-13
申请号：US13882647
申请日：2011-11-01
申请人： Hiroyuki Saimoto , Kiyoshi Kita , Yoshisada Yabu , Masaichi Yamamoto
发明人： Hiroyuki Saimoto , Kiyoshi Kita , Yoshisada Yabu , Masaichi Yamamoto
IPC分类号： C07C255/53 , C07C47/27 , C07C49/248 , C07C59/90 , A61K31/11 , A61K31/12 , A61K31/192 , A61K31/216 , A61K31/336 , A61K31/351 , A61K31/357 , A61P33/00 , C07C47/56 , C07C59/74 , C07C69/738 , A61K45/06 , A61K31/047 , C07C47/575 , C07C49/258 , C07C49/835 , C07C49/84
CPC分类号： C07C255/53 , A61K31/047 , A61K45/06 , C07C47/27 , C07C47/56 , C07C47/575 , C07C49/248 , C07C49/258 , C07C49/835 , C07C49/84 , C07C59/74 , C07C59/90 , C07C69/738 , A61K2300/00
摘要： Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(═O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.

54. 发明申请

US20160052865A1 CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS 有权
公开(公告)号：US20160052865A1
公开(公告)日：2016-02-25
申请号：US14640395
申请日：2015-03-06
申请人： Oryzon Genomics, S.A.
发明人： Matthew Colin Thor FYFE , Alberto ORTEGA MUÑOZ , Julio CASTRO-PALOMINO LARIA , Marc MARTINELL PEDEMONTE , Maria de los Angeles ESTIARTE-MARTINEZ , Nuria VALLS VIDAL
IPC分类号： C07C211/40 , C07C311/09 , C07C311/08 , C07C255/59 , C07C215/64 , C07C311/21
CPC分类号： C07C211/40 , C07B2200/07 , C07C215/64 , C07C217/74 , C07C255/53 , C07C255/54 , C07C255/59 , C07C311/08 , C07C311/09 , C07C311/21 , C07C2601/02 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/57 , C07D213/64 , C07D239/26 , C07D277/28 , C07D333/20 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/10
摘要： The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.

55. 发明申请

US20150366834A1 Opsin-Binding Ligands, Compositions and Methods of Use 有权
标题翻译：组合物和使用方法
公开(公告)号：US20150366834A1
公开(公告)日：2015-12-24
申请号：US14825699
申请日：2015-08-13
申请人： BIKAM PHARMACEUTICALS, INC.
发明人： David S. GARVEY
IPC分类号： A61K31/277 , A61K31/045 , A61K31/12
CPC分类号： C07D333/22 , A61K31/045 , A61K31/12 , A61K31/277 , C07C25/06 , C07C25/13 , C07C25/18 , C07C33/14 , C07C33/34 , C07C33/50 , C07C43/23 , C07C49/792 , C07C49/813 , C07C49/84 , C07C255/53 , C07C255/56 , C07C259/18 , C07C2601/14 , C07C2601/16 , C07D307/42 , C07D307/46 , C07D333/16
摘要： Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
摘要翻译：公开的化合物可用于治疗由眼睛中累积的毒性视觉循环产物引起或与其相关的眼部疾病，例如干性成人黄斑变性，以及由突变视蛋白质蛋白质错误折叠引起或与之相关的病症，以及 /或视蛋白蛋白质的错位。还描述了这些化合物单独或与其它治疗剂组合的组合物，以及使用这些化合物和/或组合物的治疗方法。还公开了合成这些试剂的方法。

56. 发明申请

US20150329491A1 FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：氟化合物及其药物用途
公开(公告)号：US20150329491A1
公开(公告)日：2015-11-19
申请号：US14484666
申请日：2014-09-12
申请人： JAPAN TOBACCO INC.
发明人： Takahisa MOTOMURA , Hironobu NAGAMORI , Koichi SUZAWA , Hirotsugu ITO , Toru MORITA , Satoru KOBAYASHI , Hisashi SHINKAI
IPC分类号： C07D231/12
CPC分类号： C07D205/04 , A61K31/045 , A61K31/05 , A61K31/085 , A61K31/10 , A61K31/121 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/192 , A61K31/235 , A61K31/277 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4523 , A61K31/5375 , C07C35/52 , C07C39/42 , C07C43/23 , C07C43/253 , C07C49/83 , C07C59/56 , C07C59/72 , C07C65/17 , C07C69/712 , C07C69/732 , C07C69/76 , C07C215/44 , C07C215/70 , C07C217/20 , C07C233/18 , C07C233/25 , C07C235/42 , C07C235/66 , C07C255/12 , C07C255/53 , C07C259/10 , C07C271/16 , C07C271/30 , C07C311/04 , C07C317/22 , C07C2603/18 , C07D207/04 , C07D211/06 , C07D213/30 , C07D213/56 , C07D231/12 , C07D239/26 , C07D249/08 , C07D257/04 , C07D263/32 , C07D271/06 , C07D271/10 , C07D275/02 , C07D295/08 , C07D295/18 , C07D295/192 , C07D333/22 , C07D401/06 , C07D401/12 , C07D403/12 , C07F7/081
摘要： The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
摘要翻译：本发明提供了用于预防或治疗糖尿病，糖尿病并发症，胰岛素抵抗综合征，代谢综合征，高血糖症，血脂异常，动脉粥样硬化，心力衰竭，心肌病，心肌缺血，脑缺血，脑中风，肺动脉高压，高乳酸血症，线粒体疾病，线粒体性脑病或癌症，即PDHK抑制剂等。由下式[I]表示的化合物或其药学上可接受的盐或其溶剂化物：其中每个符号如说明书中所定义。

57. 发明申请

US20150315146A1 USE OF SUBSTITUTED 1-(ARYL ETHYNYL)-, 1-(HETEROARYL ETHYNYL)-, 1-(HETEROCYCLYL ETHYNYL)- AND 1-(CYCLOALKENYLETHYNYL)-BICYCLOALKANOLS AS ACTIVE AGENTS AGAINST ABIOTIC PLANT STRESS 审中-公开
标题翻译：取代的1-（芳基乙烯基） - ，1-（异丁基乙烯基） - ，1-（杂芳基乙烯基） - 和1-（环己基烯丙基） - 二烷基甘氨酸作为对生物植物应激的活性剂的使用
公开(公告)号：US20150315146A1
公开(公告)日：2015-11-05
申请号：US14647837
申请日：2013-12-02
申请人： BAYER CROPSCIENCE AG
发明人： Jens FRACKENPOHL , Thomas MUELLER , Jan DITTGEN , Dirk SCHMUTZLER , Juan Pedro RUIZ-SANTAELLA MORENO , Martin Jeffrey HILLS
IPC分类号： C07D213/30 , A01N31/06 , C07C43/295 , A01N31/14 , A01N43/20 , A01N43/36 , A01N43/40 , C07D207/16 , C07D211/60 , C07D305/08 , C07C35/29 , C07C233/64
CPC分类号： C07D213/30 , A01N31/06 , A01N31/14 , A01N37/36 , A01N41/06 , A01N43/20 , A01N43/36 , A01N43/40 , A01N45/02 , C07C35/29 , C07C43/295 , C07C65/19 , C07C69/757 , C07C69/76 , C07C205/13 , C07C215/70 , C07C233/25 , C07C233/60 , C07C233/64 , C07C235/42 , C07C251/48 , C07C255/36 , C07C255/53 , C07C271/28 , C07C311/08 , C07C311/29 , C07C323/18 , C07C331/28 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07C2602/20 , C07C2602/42 , C07C2603/64 , C07C2603/68 , C07C2603/74 , C07C2603/94 , C07D207/16 , C07D211/60 , C07D295/192 , C07D305/08 , C07D333/38
摘要： The invention relates to the use of substituted 1-(arylethynyl)-, 1-(heteroarylethynyl)-, 1-(heterocyclylethynyl)- and 1-(cycloalkenylethynyl)bicycloalkanols or salts thereof where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress and/or for increasing plant yield.
摘要翻译：本发明涉及取代的1-（芳基乙炔基） - ，1-（杂芳基乙炔基） - ，1-（杂烯基乙炔基） - 和1-（环烯基乙炔基）双链烷醇或其盐，其中通式（I）中的基团对应于描述中给出的定义，用于增强植物对非生物胁迫的胁迫耐受性和/或用于提高植物产量。

58. 发明授权

US08957239B2 Process for the eco-friendly preparation of 3, 5-dibromo-4-hydroxybenzonitrile 有权
标题翻译：环保制备3,5-二溴-4-羟基苄腈的方法
公开(公告)号：US08957239B2
公开(公告)日：2015-02-17
申请号：US13981647
申请日：2010-02-25
申请人： Subbarayappa Adimurthy , Gadde Ramachandraiah , Girdhar Joshi , Rajendra Patil , Maheshkumar Ramniklal Gandhi , Mallampati Subbareddy , Pratyush Maiti
发明人： Subbarayappa Adimurthy , Gadde Ramachandraiah , Girdhar Joshi , Rajendra Patil , Maheshkumar Ramniklal Gandhi , Mallampati Subbareddy , Pratyush Maiti
IPC分类号： C07C17/02 , C07C25/02 , C07C253/30
CPC分类号： C07C253/30 , C07C255/53
摘要： A highly pure 3,5-dibromo-4-hydroxybenzonitrile (bromoxynil) has been prepared in high yield from 4-hydroxybenzonitrile using eco-friendly brominating reagent comprising of 2:1 mole ratio of bromide to bromate salts in aqueous acidic medium without any catalyst under ambient conditions with no work up procedure. The product 3,5-dibromo-4-hydroxybenzonitrile was obtained in 91-99% yield with melting point 189-191° C. and more than 99% purity by gas chromatographic analysis without any purification.
摘要翻译：使用环氧友好的溴化试剂，以不含任何催化剂的含水酸性介质中的2:1摩尔比的溴化物与溴酸盐组合，从4-羟基苄腈得到高纯度3,5-二溴-4-羟基苄腈（溴苯腈）在环境条件下，无需处理程序。得到产物3,5-二溴-4-羟基苄腈，其熔点为189-191℃，纯度为991-99％，气相色谱分析纯度为99％以上。

59. 发明申请

US20130331596A1 PROCESS FOR THE ECO-FRIENDLY PREPARATION OF 3, 5-DIBROMO-4-HYDROXYBENZONITRILE 有权
标题翻译：生物友好制备3,5-二溴-4-羟基苯并噻唑的方法
公开(公告)号：US20130331596A1
公开(公告)日：2013-12-12
申请号：US13981647
申请日：2010-02-25
申请人： Subbarayappa Adimurthy , Gadde Ramachandraiah , Girdhar Joshi , Rajendra Patil , Maheshkumar Ramniklal Gandhi , Mallampati Subrareddy , Pratyush Maiti
发明人： Subbarayappa Adimurthy , Gadde Ramachandraiah , Girdhar Joshi , Rajendra Patil , Maheshkumar Ramniklal Gandhi , Mallampati Subrareddy , Pratyush Maiti
IPC分类号： C07C253/30
CPC分类号： C07C253/30 , C07C255/53
摘要： A highly pure 3,5-dibromo-4-hydroxybenzonitrile (bromoxynil) has been prepared in high yield from 4-hydroxybenzonitrile using eco-friendly brominating reagent comprising of 2:1 mole ratio of bromide to bromate salts in aqueous acidic medium without any catalyst under ambient conditions with no work up procedure. The product 3,5-dibromo-4-hydroxybenzonitrile was obtained in 91-99% yield with melting point 189-191° C. and more than 99% purity by gas chromatographic analysis without any purification.
摘要翻译：使用环氧友好的溴化试剂，以不含任何催化剂的含水酸性介质中的2:1摩尔比的溴化物与溴酸盐组合，从4-羟基苄腈得到高纯度3,5-二溴-4-羟基苄腈（溴苯腈）在环境条件下，无需处理程序。得到产物3,5-二溴-4-羟基苄腈，其熔点为189-191℃，纯度为991-99％，气相色谱分析纯度为99％以上。

60. 发明授权

US08288569B2 Carbonyl asymmetric alkylation 有权
标题翻译：羰基不对称烷基化
公开(公告)号：US08288569B2
公开(公告)日：2012-10-16
申请号：US12223096
申请日：2007-01-22
申请人： Martin Albert , Hubert Sturm , Andreas Berger , Peter Kremminger
发明人： Martin Albert , Hubert Sturm , Andreas Berger , Peter Kremminger
IPC分类号： C07D307/87 , C07F5/02
CPC分类号： C07C255/56 , C07C215/30 , C07C255/53 , C07D307/87
摘要： This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.
摘要翻译：本发明涉及羰基的立体选择性烷基化方法和中间体。本发明特别允许立体选择性制备抗抑郁药物依他普仑。已经发现硼酸或硼酸衍生物是用于将手性基团连接到含有待烷基化羰基的化合物的有用的桥连元件。因此，所述硼酸盐和硼酸盐可用于在含有羰基和能够与硼酸或硼酸衍生物反应的锚定基团的化合物中羰基的不对称烷基化方法。不对称烷基化可以通过将待烷基化的羰基和能够与硼酸或硼酸衍生物反应的锚定基团与硼酸或硼酸衍生物反应，加入手性醇，并加入有机金属化合物。在烷基化反应之后，可以通过水解容易地除去硼酸盐和硼酸盐。

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