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1. 发明申请

WO2008089390A1 NEW CLASSICAL ANTIFOLATES 审中-公开
标题翻译：新古典抗氧化剂
公开(公告)号：WO2008089390A1
公开(公告)日：2008-07-24
申请号：PCT/US2008/051408
申请日：2008-01-18
申请人： CHELSEA THERAPEUTICS, INC. , ROBERTS, Michael, J. , PEDDER, Simon
发明人： ROBERTS, Michael, J. , PEDDER, Simon
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention is directed to antifolate compounds having the structure of formula (I). wherein: X is CHR9 or NR9; Y1, Y2, and Y3 independently are O or S; V1 and V2 independently are O, S, or NZ; Z is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R1 and R2 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R3 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, hydroxyl, or halo; and R4, R5, R6, R7, Rs, and R9 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, acyl, -C(O)-alkyl, - C(O)-alkenyl, or -C(O)-alkynyl; as well as pharmaceutically acceptable esters, amides, salts, solvates, and prodrugs thereof. The compounds are useful in pharmaceutical compositions and in methods of treating multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.
摘要翻译：本发明涉及具有式（I）结构的抗叶酸化合物。其中：X是CHR 9或NR 9; Y1，Y2和Y3独立地为O或S; V1和V2独立为O，S或NZ; Z是H，任选取代的烷基，任选取代的烯基，任选取代的炔基或烷芳基; R 1和R 2独立地为H，任选取代的烷基，任选取代的烯基，任选取代的炔基或烷芳基; R 3是H，任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的烷氧基，羟基或卤素; R 4，R 5，R 6，R 7，R 5和R 9独立地为H，任选取代的烷基，任选取代的烯基，任选取代的炔基，酰基，-C（O） - 烷基，-C（O） - 烯基或-C （O） - 炔基; 以及其药学上可接受的酯，酰胺，盐，溶剂合物和前药。该化合物可用于药物组合物和治疗多种病症的方法，包括异常细胞增殖，炎性疾病，哮喘和关节炎。

2. 发明申请

WO2003003412A3 INDUCTIVE SIGNATURE MEASUREMENT CIRCUIT 审中-公开
公开(公告)号：WO2003003412A3
公开(公告)日：2003-01-09
申请号：PCT/US2002/020716
申请日：2002-06-28
申请人： INDUCTIVE SIGNATURE TECHNOLOGIES, INC. , HILLIARD, Steven, R. , ROBERTS, Michael, J. , YEREM, Geoffrey, C.
发明人： HILLIARD, Steven, R. , ROBERTS, Michael, J. , YEREM, Geoffrey, C.
IPC分类号： G01R27/26
摘要： An apparatus (10) for measuring the inductance of a wire-loop (102) (202) with noise-cancellation, auto-calibration and wireless communication features, or detector circuit. The apparatus (10) measures the effective change in inductance in a wire-loop (102) (202) as a vehicle passes over the wire-loop (102) (202) to produce an inductive signature (704) corresponding to a vehicle.

3. 发明申请

WO2012145123A1 BUBBLING BED CATALYTIC HYDROPYROLYSIS PROCESS UTILIZING LARGER CATALYST PARTICLES AND SMALLER BIOMASS PARTICLES FEATURING AN ANTI-SLUGGING REACTOR 审中-公开
标题翻译：使用催化剂水解微生物催化剂的方法使用较大的催化剂颗粒和小型生物质颗粒特种抗反应剂
公开(公告)号：WO2012145123A1
公开(公告)日：2012-10-26
申请号：PCT/US2012/030386
申请日：2012-03-23
申请人： GAS TECHNOLOGY INSTITUTE , MARKER, Terry, L. , FELIX, Larry, G. , LINCK, Martin, B. , ROBERTS, Michael, J.
发明人： MARKER, Terry, L. , FELIX, Larry, G. , LINCK, Martin, B. , ROBERTS, Michael, J.
IPC分类号： C10G1/06 , C10G1/08 , B01J8/18 , B01J8/34 , C10G3/00
CPC分类号： C10G1/06 , B01J8/1809 , B01J8/34 , B01J23/755 , B01J23/882 , B01J2208/00061 , B01J2208/00115 , B01J2208/00548 , B01J2208/0084 , B01J2219/00252 , C10G1/002 , C10G1/086 , C10G1/10 , C10G3/45 , C10G3/46 , C10G3/50 , C10G3/57 , C10G2300/1003 , C10G2300/1014 , C10G2300/1018 , C10G2300/202 , C10G2400/02 , C10G2400/04 , C10G2400/08 , C10L1/04 , C10L2200/0469 , C10L2290/02 , Y02E50/14 , Y02E50/32 , Y02P30/20
摘要： This invention relates to a process for thermochemically transforming biomass or other oxygenated feedstocks into high quality liquid hydrocarbon fuels. In particular, a catalytic hydropyrolysis reactor, containing a deep bed of fluidized catalyst particles is utilized to accept particles of biomass or other oxygenated feedstocks that are significantly smaller than the particles of catalyst in the fluidized bed. The reactor features an insert or other structure disposed within the reactor vessel that inhibits slugging of the bed and thereby minimizes attrition of the catalyst. Within the bed, the biomass feedstock is converted into a vapor-phase product, containing hydrocarbon molecules and other process vapors, and an entrained solid char product, which is separated from the vapor stream after the vapor stream has been exhausted from the top of the reactor. When the product vapor stream is cooled to ambient temperatures, a significant proportion of the hydrocarbons in the product vapor stream can be recovered as a liquid stream of hydrophobic hydrocarbons, with properties consistent with those of gasoline, kerosene, and diesel fuel. Separate streams of gasoline, kerosene, and diesel fuel may also be obtained, either via selective condensation of each type of fuel, or via later distillation of the combined hydrocarbon liquid.
摘要翻译：本发明涉及将生物质或其它含氧原料热化学变换成高质量液体烃燃料的方法。特别地，使用含有流化催化剂颗粒的深层的催化加氢热解反应器来接受显着小于流化床中的催化剂颗粒的生物质或其它含氧原料的颗粒。反应器具有设置在反应器容器内的插入物或其它结构，其抑制床的压块，从而使催化剂的磨损最小化。在床内，生物质原料转化为含有烃分子和其他工艺蒸气的气相产物，以及夹带的固体焦炭产物，其在蒸气流已经从蒸汽流的顶部排出之后与蒸气流分离反应堆。当产物蒸气流被冷却到环境温度时，产物蒸气流中的相当大比例的烃可作为疏水性烃的液体流回收，其特性与汽油，煤油和柴油燃料的性质一致。也可以通过每种类型的燃料的选择性冷凝，或通过以后的组合烃液体的蒸馏来获得单独的汽油，煤油和柴油燃料。

4. 发明申请

WO2012078708A1 COMBINATION COMPRISING METHOTREXATE AND AN ANTIFOLATE COMPOUND 审中-公开
标题翻译：包含甲基睾酮和抗疲劳性化合物的组合
公开(公告)号：WO2012078708A1
公开(公告)日：2012-06-14
申请号：PCT/US2011/063650
申请日：2011-12-07
申请人： CHELSEA THERAPEUTICS, INC. , ROBERTS, Michael, J. , ROWSE, Gerry
发明人： ROBERTS, Michael, J. , ROWSE, Gerry
IPC分类号： A61K31/517 , A61K31/519 , A61P29/00
CPC分类号： A61K31/519 , A61K31/517 , A61K2300/00
摘要： The present invention provides combinations of active agents, such combinations comprising one or more antifolate compounds. The particularly can include methotrexate and one or more further antifolate compounds. In specific embodiments, the combinations are useful for treating certain conditions, such as rheumatoid arthritis. The invention also provides articles useful to provide the combinations in desirable dosage forms and combinations. The combinations further may be useful in the treatment of further conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.
摘要翻译：本发明提供活性剂的组合，这种组合包含一种或多种抗叶酸化合物。特别可以包括甲氨蝶呤和一种或多种另外的抗叶酸化合物。在具体实施方案中，这些组合可用于治疗某些病症，例如类风湿性关节炎。本发明还提供可用于提供所需剂型和组合的组合的制品。组合进一步可用于治疗其他病症，包括异常细胞增殖，炎性疾病，哮喘和关节炎。

5. 发明申请

WO2008137923A3 DROXIDOPA AND PHARMACEUTICAL COMPOSITION THEREOF FOR THE TREATMENT OF MOOD DISORDERS, SLEEP DISORDERS, OR ATTENTION DEFICIT DISORDERS 审中-公开
标题翻译：治疗恶臭症，睡眠障碍或注意缺陷性疾病的杀虫剂及其药物组合物
公开(公告)号：WO2008137923A3
公开(公告)日：2009-04-09
申请号：PCT/US2008062879
申请日：2008-05-07
申请人： CHELSEA THERAPEUTICS INC , ROBERTS MICHAEL J , PEDDER SIMON
发明人： ROBERTS MICHAEL J , PEDDER SIMON
IPC分类号： A61K31/138 , A61K31/195 , A61K31/198 , A61K31/275 , A61K31/345
CPC分类号： A61K31/198 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/195 , A61K31/275 , A61K31/277 , A61K31/345 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： The present invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, for the treatment of conditions, such as mood disorders, sleep disorders, or attention deficit disorders. In certain embodiments, the compositions useful in the methods of the invention comprise droxidopa and a compound selected from the group consisting of DOPA decarboxylase inhibiting compounds, catechol-0-methyltransferase inhibiting compounds, cholinesterase inhibiting compounds, monoamine oxidase inhibiting compounds, norepinephrine reuptake inhibiting compounds, selective serotonin reuptake inhibiting compounds, tricyclic antidepressant compounds, serotonin norepinephrine reuptake inhibiting compounds, norepinephrine dopamine reuptake inhibiting compound, noradrenergic and specific serotonergic antidepressants, and combinations thereof. The inventive compositions are particularly useful in the treatment of depression, narcolepsy, insomnia, and Attention Deficit/Hyperactivity Disorder (AD/HD).
摘要翻译：本发明提供药物组合物，其包含单独的droxidopa或与一种或多种其它活性成分组合用于治疗诸如情绪障碍，睡眠障碍或注意力缺陷障碍的病症的药物组合物。在某些实施方案中，可用于本发明方法的组合物包含伏多昔巴和选自DOPA脱羧酶抑制化合物，儿茶酚-O-甲基转移酶抑制化合物，胆碱酯酶抑制化合物，单胺氧化酶抑制化合物，去甲肾上腺素再摄取抑制化合物，选择性5-羟色胺再摄取抑制化合物，三环抗抑郁化合物，5-羟色胺去甲肾上腺素再摄取抑制化合物，去甲肾上腺素多巴胺再摄取抑制化合物，去甲肾上腺素能和特异性5-羟色胺能抗抑郁药，及其组合。本发明的组合物特别可用于治疗抑郁症，发作性睡病，失眠和注意力缺陷/多动障碍（AD / HD）。

6. 发明申请

WO2008112773A3 DROXIDOPA AND PHARMACEUTICAL COMPOSITION THEREOF FOR THE TREATMENT OF NEURALLY MEDIATED HYPOTENSION 审中-公开
标题翻译：用于治疗神经介入性高血压的抗氧化剂及其药物组合物
公开(公告)号：WO2008112773A3
公开(公告)日：2009-01-29
申请号：PCT/US2008056675
申请日：2008-03-12
申请人： CHELSEA THERAPEUTICS INC , ROBERTS MICHAEL J , PEDDER SIMON
发明人： ROBERTS MICHAEL J , PEDDER SIMON
IPC分类号： A61K31/15 , A61K31/198 , A61K31/275 , A61K31/407 , A61P9/02
CPC分类号： A61K45/06 , A61K31/15 , A61K31/198 , A61K31/275 , A61K31/277 , A61K31/407 , A61K31/4409 , A61K31/4425 , A61K2300/00
摘要： The present invention is directed to methods of treating neurally mediated hypotension. In particular, the invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, that can be administered to a patient for the treatment of neurally mediated hypotension.
摘要翻译：本发明涉及治疗神经介导的低血压的方法。特别地，本发明提供药物组合物，其包含单独的达洛西多或与一种或多种其它活性成分组合，其可施用于患者以治疗神经介导的低血压。

7. 发明申请

WO2006029385A2 METABOLICALLY INERT ANTIFOLATES FOR TREATING DISORDERS OF ABNORMAL CELLULAR PROLIFERATION AND INFLAMMATION 审中-公开
标题翻译：用于治疗异常细胞增生和炎症疾病的代谢性抗体
公开(公告)号：WO2006029385A2
公开(公告)日：2006-03-16
申请号：PCT/US2005/032352
申请日：2005-09-08
申请人： CHELSEA THERAPEUTICS, INC. , ROBERTS, Michael, J. , PEDDER, Simon
发明人： ROBERTS, Michael, J. , PEDDER, Simon
IPC分类号： A61K31/517
CPC分类号： C07D239/95
摘要： The present invention provides compositions and methods for the treatment of disorders of abnormal cell proliferation and/or inflammation, such as psoriasis and inflammatory bowel disease, in a human or other host animals.
摘要翻译：本发明提供了用于治疗人或其他宿主动物中异常细胞增殖和/或炎症疾病如牛皮癣和炎症性肠病的组合物和方法。

8. 发明申请

WO2005021556A2 MODIFIED PROTEASE INHIBITORS 审中-公开
标题翻译：修饰的蛋白酶抑制剂
公开(公告)号：WO2005021556A2
公开(公告)日：2005-03-10
申请号：PCT/US2004028256
申请日：2004-08-30
申请人： DYAX CORP , LADNER ROBERT C , SATO AARON K , AMARAL MICHELLE , BOSSARD MARY J , ROBERTS MICHAEL J , ZHANG YAN , LEY ARTHUR C
发明人： LADNER ROBERT C , SATO AARON K , AMARAL MICHELLE , BOSSARD MARY J , ROBERTS MICHAEL J , ZHANG YAN , LEY ARTHUR C
IPC分类号： A61K38/00 , A61K47/48 , A61K49/00 , C07F20060101 , C07K14/00 , C07K14/81 , C12N9/00 , C12N9/66 , C07F
CPC分类号： C07K14/8114 , A61K38/00 , A61K47/60 , A61K49/0002
摘要： DX-890 inhibits elastase. DX-890 can be attached a single polyethylene glycol moiety. The polyethylene glycol is at least 18 kDa in molecular weight and is attached to the polypeptide by a single covalent bond to the N-terminus of the polypeptide.
摘要翻译： DX-890抑制弹性蛋白酶。 DX-890可以连接一个单一的聚乙二醇部分。聚乙二醇的分子量至少为18kDa，并且通过与多肽的N末端单一共价键与多肽连接。

9. 发明申请

WO2004076474A3 POLYETHYLENE GLYCOL MODIFIED INTERFERON COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：聚乙烯甘油改性干扰素组合物及其使用方法
公开(公告)号：WO2004076474A3
公开(公告)日：2005-01-06
申请号：PCT/US2004005649
申请日：2004-02-24
申请人： INTERMUNE INC , VAN VLASSELAER PETER , ROBERTS MICHAEL J , VISOR GARY , CHARLES STEPHEN A
发明人： VAN VLASSELAER PETER , ROBERTS MICHAEL J , VISOR GARY , CHARLES STEPHEN A
IPC分类号： A61K38/00 , A61K47/48 , C07K20060101 , C07K1/107 , C07K1/113 , C07K14/56
CPC分类号： C07K14/56 , A61K38/00 , A61K47/60
摘要： Interferon alpha (IFN-alpha) linked to a linear polyethylene glycol (PEG) molecule having a nominal molecular weight of about 30 kD, and compositions comprising the same, are provided. The invention further provides methods of treating a viral infection with the subject PEG-modified IFN-alpha.
摘要翻译：提供了与标称分子量为约30kD的线性聚乙二醇（PEG）分子连接的干扰素α（IFN-α）和包含其的组合物。本发明还提供用受试者PEG修饰的IFN-α治疗病毒感染的方法。

10. 发明申请

WO9955377A9 POLYOL-IFN-BETA CONJUGATES 审中-公开
标题翻译：多聚-γ-干扰素结合物
公开(公告)号：WO9955377A9
公开(公告)日：2000-03-02
申请号：PCT/US9909161
申请日：1999-04-28
申请人： APPLIED RESEARCH SYSTEMS , EL TAYAR NABIL , ROBERTS MICHAEL J , HARRIS MILTON , SAWLIVICH WAYNE
发明人： EL TAYAR NABIL , ROBERTS MICHAEL J , HARRIS MILTON , SAWLIVICH WAYNE
IPC分类号： A61K47/34 , A61K38/21 , A61K47/48 , A61P31/00 , A61P35/00 , A61P37/06 , A61P39/00
CPC分类号： A61K47/60 , Y10S514/825 , Y10S514/903
摘要： PEG-IFN- beta conjugates, where a PEG moiety is covalently bound to Cys of human IFN- beta , are produced by a process of site specific PEGylation with a thiol reactive PEGylating agent. A pharmaceutical composition and a method for treating infections, tumors and autoimmune and inflammatory diseases are also provided. The invention further relates to a method for the stepwise attachment of PEG moieties in series to a polypeptide, and more particularly to IFN- beta .
摘要翻译：其中PEG部分与人IFN-β的Cys 17共价结合的PEG-IFN-β缀合物通过用硫醇反应性聚乙二醇化剂进行位点特异性PEG化的方法产生。还提供了用于治疗感染，肿瘤和自身免疫性和炎性疾病的药物组合物和方法。本发明还涉及将PEG部分逐步连接到多肽，更具体地涉及IFN-β的方法。

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