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1. 发明申请

WO2023083465A1 A STABLE FORMULATION OF P2S5·2C5H5N 审中-公开
公开(公告)号：WO2023083465A1
公开(公告)日：2023-05-19
申请号：PCT/EP2021/081607
申请日：2021-11-12
申请人： VIRONOVA THIONATION AB
发明人： BERGMAN, Jan , KINGI, Ngarita
IPC分类号： C07F9/58 , C07B45/00 , C07C327/00 , C07D201/00
摘要： A P2S5·2C5H5N stock formulation comprising a solution of P2S5·2C5H5N in sulfolane, a process for preparing the formulation, and the use of the formulation in a thionating reaction.

2. 发明申请

WO0198235A3 3,4-DIHYDROXYBENZYL-SUBSTITUTED CARBONIC ACID DERIVATIVES AND THE USE THEREOF AS ANTIOXIDANTS 审中-公开
标题翻译： 3,4-二羟基 - 取代二氧化碳衍生物及其抗氧化剂
公开(公告)号：WO0198235A3
公开(公告)日：2002-05-23
申请号：PCT/EP0106568
申请日：2001-06-11
申请人： HAARMANN & REIMER GMBH , LEY JAKOB PETER , JOHNCOCK WILLIAM , LANGNER ROLAND
发明人： LEY JAKOB PETER , JOHNCOCK WILLIAM , LANGNER ROLAND
IPC分类号： A01N1/00 , A23L33/10 , A61K8/00 , A61K8/30 , A61K8/33 , A61K8/41 , A61K8/44 , A61K8/46 , A61K8/49 , A61K31/17 , A61K31/27 , A61K31/325 , A61K47/08 , A61K47/16 , A61K47/18 , A61K47/20 , A61Q3/00 , A61Q3/02 , A61Q5/00 , A61Q17/00 , A61Q17/04 , A61Q19/00 , A61Q19/08 , C07C269/04 , C07C271/06 , C07C271/16 , C07C271/34 , C07C275/10 , C07C279/08 , C07C279/10 , C07C327/00 , C07C333/04 , C07C333/20 , C07C335/00 , C07C335/12 , C09K15/04 , C09K15/20 , C09K15/24 , C09K15/26 , C09K15/28 , A61K7/00
CPC分类号： A61K8/44 , A23L33/10 , A61K8/46 , A61K9/0014 , A61K47/18 , A61K2800/522 , A61Q17/00 , A61Q17/04 , C07C271/16 , C07C271/34 , C07C335/12 , C09K15/20 , C09K15/26
摘要： The invention relates to 3,4-dihydroxybenzyl-substituted carbonic acid derivatives, to their production, and to their use as antioxidants or free-radical scavengers, especially in cosmetic and pharmaceutical preparations and in foodstuffs and stimulants, to protect cells and tissues from the harmful effects of radicals and reactive oxygen compounds that accelerate aging. The invention further relates to cosmetic and pharmaceutical preparations and to foodstuffs and stimulants that comprises the inventive 3,4-dihydroxybenzyl-substituted carbonic acid derivatives.
摘要翻译：本发明涉及在化妆品和药物制剂和食品中的3,4-二羟基苄基取代的碳酸衍生物，它们的制备，它们作为抗氧化剂或自由基清除剂的用途，特别用于保护细胞和组织免受自由基老化加速有害影响和活性氧。本发明还涉及化妆品和药物制剂以及食品和饮料，其包含这些3,4-二羟基苄基取代的碳酸衍生物。

3. 发明申请

WO2007095178A3 METHOXYPOLYETHYLENE GLYCOL THIOESTER CHELATE AND USES THEREOF 审中-公开
标题翻译：甲氧基乙基乙二醇硫酸酯及其用途
公开(公告)号：WO2007095178A3
公开(公告)日：2008-04-17
申请号：PCT/US2007003682
申请日：2007-02-14
申请人： EASTERN VIRGINIA MED SCHOOL , SCHELLENBERG KARL A , LATTANZIO FRANK A , SHAEFER JAMES
发明人： SCHELLENBERG KARL A , LATTANZIO FRANK A , SHAEFER JAMES
IPC分类号： A61K31/21 , A61L27/54 , C07C327/00
CPC分类号： C07C327/28 , A61K31/16
摘要： The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to remove electrons from free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca++ that may be released from organelles. These chelate esters will also have utility in reducing intraocular pressure in glaucoma patients.
摘要翻译：本发明一般涉及保护细胞，组织和器官免受与辐射或化学疗法相关的电离或其它损害剂或引起产生自由基或氧化剂如过氧化物的各种器官的退行性疾病或过程的破坏作用，超氧化物阴离子，羟基自由基或一氧化氮，或重金属阳离子。更具体地，本发明涉及甲氧基聚乙二醇硫酯螯合甲酯，其可用作通过穿透细胞膜从自由基氧化剂中除去电子并去除可能与过氧化物反应以产生反应性羟基的重金属的组织损伤的保护剂，或者去除可能从细胞器中释放的Ca ++。这些螯合酯也可用于降低青光眼患者的眼内压。

4. 发明申请

WO2005073185A1 NOVEL ALKYL- AND ARYL-THIOTRIFLUOROACETATES AND PROCESS 审中-公开
标题翻译：新型的碱金属和芳基三氟乙酸酯和方法
公开(公告)号：WO2005073185A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/001012
申请日：2005-01-12
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHARMA, Padam N. , GUBLO, Edward J. , BOETTGER, Susan D. , RACHA, Saibaba , USHER, John
发明人： SHARMA, Padam N. , GUBLO, Edward J. , BOETTGER, Susan D. , RACHA, Saibaba , USHER, John
IPC分类号： C07C327/00
CPC分类号： C07C327/22 , C07C231/02 , C07C2603/74 , Y02P20/55 , C07C233/48
摘要： Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure [Formula (I)], wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate. In addition, a process for protecting a primary or secondary amino group or a primary or secondary hydroxyl group or an amino alcohol with a trifluoroacetyl protecting group is provided wherein a primary or secondary amine, amino acid, a primary or secondary alcohol or an amino alcohol is treated with a C3 to C19 alkyl- or aryl-thiotrifluoroacetate in basic aqueous solution.
摘要翻译：提供具有[式（I）]结构的新颖的C 3 -C 19烷基 - 和芳基 - 三油酸乙酯，其中Q是C 9 -C 19烷基或芳基，并且是胺，氨基酸的氨基或羟基官能团的有用的保护剂或伯或仲醇或氨基醇，以使肽或蛋白质中能够形成酰胺键，其可用作筛选剂，药物和化妆品。还提供了制备C 3 -C 19烷基 - 和芳基 - 三硫代三氟乙酸盐的方法，其中在有机碱如吡啶，溶剂如二氯甲烷（DCM））存在下，用三氟乙酸酐（TFAA）处理C 3 -C 19烷基硫醇或芳基硫醇，和二甲基氨基吡啶（DMAP）作为催化剂形成所需的C 3 -C 19烷基 - 或芳基 - 三硫代三氟乙酸盐。另外，提供了用三氟乙酰基保护基保护伯或仲氨基或伯或仲羟基或氨基醇的方法，其中伯胺或仲胺，氨基酸，伯或仲醇或氨基醇在碱性水溶液中用C3至C19烷基 - 或芳基 - 三硫代三氟乙酸盐处理。

5. 发明申请

WO98056234A1 METHODS AND COMPOSITIONS TO PROTECT CROPS AGAINST PLANT-PARASITIC NEMATODES 审中-公开
标题翻译：保护植物寄生虫的作物的方法和组合物
公开(公告)号：WO98056234A1
公开(公告)日：1998-12-17
申请号：PCT/US1998/011795
申请日：1998-06-09
IPC分类号： A01N37/44 , A01N37/46 , A01N47/12 , C07C229/12 , C07C229/14 , C07C229/34 , C07C233/83 , C07C271/22 , A01G13/00 , C07C205/00 , C07C229/00 , C07C233/00 , C07C327/00
CPC分类号： A01N47/12 , A01N37/44 , A01N37/46 , C07C229/12 , C07C229/14 , C07C229/34 , C07C233/83 , C07C271/22 , C07C2601/14
摘要： A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of beta -amino butyric acid or derivatives thereof to the crop or its locus.
摘要翻译：通过诱导作物的局部和系统抗性来保护作物免受植物寄生线虫攻击的方法，包括将含有有效量的β-氨基丁酸或其衍生物的组合物施用于作物或其基因座。

6. 发明申请

WO2007095584A3 Histone Deacetylase Inhibitors 审中-公开
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：WO2007095584A3
公开(公告)日：2009-05-22
申请号：PCT/US2007062152
申请日：2007-02-14
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
IPC分类号： C07C309/00 , C07C233/00 , C07C235/00 , C07C327/00
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for exmaple. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
摘要翻译：鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。这些化合物包括酯键，使它们对酯酶的失活敏感。因此，这些化合物特别可用于治疗皮肤病。当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。这些化合物及其药物组合物特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。本发明还提供了制备本发明化合物及其中间体的方法。

7. 发明申请

WO2008024302A8 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
标题翻译：用于治疗增生性疾病的化合物
公开(公告)号：WO2008024302A8
公开(公告)日：2008-05-08
申请号：PCT/US2007018362
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP , SUN LIJUN , KOYA KEIZO , CHEN SHOUJUN , DEMKO ZACHARY , XIA ZHI-QIANG
发明人： SUN LIJUN , KOYA KEIZO , CHEN SHOUJUN , DEMKO ZACHARY , XIA ZHI-QIANG
IPC分类号： C07D213/86 , A61K31/16 , A61K31/165 , C07C243/24 , C07C327/00 , C07D207/416 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/30 , C07D333/36 , C07D333/38
CPC分类号： C07C327/56 , C07C243/24 , C07C255/56 , C07C255/58 , C07C337/02 , C07C337/06 , C07C2601/02 , C07C2601/14 , C07D207/34 , C07D213/81 , C07D213/86 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/38 , C07D333/36 , C07D333/38
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了使用本发明化合物治疗患有增殖性疾病如癌症的受试者的化合物和方法，以及用于治疗响应于Hsp70诱导和/或自然杀伤诱导的病症的方法。此外，公开了包含本发明化合物和药学上可接受的载体的药物组合物。

8. 发明申请

WO2008024302A3 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
公开(公告)号：WO2008024302A3
公开(公告)日：2008-02-28
申请号：PCT/US2007/018362
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , KOYA, Keizo , CHEN, Shoujun , DEMKO, Zachary , XIA, Zhi-qiang
发明人： SUN, Lijun , KOYA, Keizo , CHEN, Shoujun , DEMKO, Zachary , XIA, Zhi-qiang
IPC分类号： C07D213/86 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/30 , C07D333/36 , C07D333/38 , C07D207/416 , C07C243/24 , C07C327/00 , A61K31/16 , A61K31/165
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

9. 发明申请

WO99029294A1 LONG-ACTING, CHEMICAL-RESISTANT SKIN EMOLLIENTS, MOISTURIZERS, AND STRENGTHENERS 审中-公开
标题翻译：长效，耐化学品皮肤护理，保湿和加强剂
公开(公告)号：WO99029294A1
公开(公告)日：1999-06-17
申请号：PCT/US1998/018962
申请日：1998-09-10
IPC分类号： A61K8/00 , A61K8/30 , A61K8/46 , A61K8/49 , A61K31/235 , A61P17/10 , A61P39/06 , A61Q19/00 , A61Q19/08 , C07C323/50 , C07C323/54 , C07C327/00 , A61K7/48
CPC分类号： A61Q19/00 , A61K8/46 , A61K8/86 , A61K2800/522 , A61K2800/94 , A61Q17/00 , A61Q17/02 , A61Q17/04 , A61Q19/04 , A61Q19/08 , C08G65/334 , Y10S514/844
摘要： The present invention relates to compounds that are two-part molecules, and compositions containing such compounds, in which one part is designed to become covalently bonded to the skin (bonding agent) and the other part (a characteristic use agent) is designed to impart some characteristic use, such as emolliency, moisturizing effect, anti-acne, anti-wrinkle, anti-pain, antimicrobial, antifungal, antiviral, anti-irritation, skin tanning and skin lightening effects, extended protection of the skin (e.g., from ultraviolet light, by incorporation of a sunscreen component; from toxic and/or irritating substances; from insects and skin parasites, by incorporation of insecticides and/or insect repellants; from free radicals or other agents, as in aging, by incorporation of antioxidants), or dyeing of hair, skin nails, wool or fur. The covalently bonded part may also be useful to impart skin strengthening effect (e.g., from shear forces) or as wound healing agents.
摘要翻译：本发明涉及两部分分子的化合物和含有这种化合物的组合物，其中一部分被设计成与皮肤共价结合（粘合剂），另一部分（特征用途剂）被设计成赋予一些特殊用途，如润肤，保湿效果，抗痤疮，抗皱，抗疼痛，抗菌，抗真菌，抗病毒，抗刺激，皮肤晒黑和护肤效果，延长皮肤保护（如紫外线通过掺入防晒组分;来自有毒和/或刺激性物质;通过掺入杀虫剂和/或驱虫剂;来自昆虫和皮肤寄生虫;通过引入抗氧化剂从自由基或其它试剂，如在老化中）或染发头发，皮指甲，羊毛或毛皮。共价键合部分也可用于赋予皮肤强化效果（例如，来自剪切力）或作为伤口愈合剂。

10. 发明申请

WO2012017400A1 SYNTHESIS OF ACYL-PANTETHEINE DERIVATIVES AND THE USE THEREOF IN THE SYNTHESIS OF ACYL-COENZYME A DERIVATIVES 审中-公开
标题翻译：乙酰苯胺衍生物的合成及其在乙酰苯胺衍生物合成中的应用
公开(公告)号：WO2012017400A1
公开(公告)日：2012-02-09
申请号：PCT/IB2011/053458
申请日：2011-08-03
申请人： NORTH-WEST UNIVERSITY , VAN DIJK, Alberdina Aike , BADENHORST, Christoffel Petrus Stephanus
发明人： VAN DIJK, Alberdina Aike , BADENHORST, Christoffel Petrus Stephanus
IPC分类号： C07C327/00 , C07H19/20
CPC分类号： C07H19/20 , C07C327/30
摘要： The present invention relates to a novel synthesis method for acyl-pantetheine derivatives. The present invention further relates to the use of said synthesized acyl-pantetheine derivatives as a starting material in the enzymatic synthesis of acyl-coenzyme A derivatives. According to a first aspect thereof, the present invention provides a method for the synthesis of acyl-pantetheine derivatives, the method including the steps of: a) providing a source of pantetheine; b) providing a source of acyl ester; and c) contacting the source of pantetheine with the source of acyl ester to form the corresponding acyl-pantetheine derivative, having the general formula (I), wherein R is an acyl group.The present invention also provides a method for the synthesis of acyl-coenzyme A derivatives as well as the use of a source of pantetheine and a source of acyl ester in the preparation steps of these two methods.
摘要翻译：本发明涉及一种新颖的酰基 - 泛菌胺衍生物的合成方法。本发明还涉及在酰基辅酶A衍生物的酶合成中所述合成的酰基 - 潘太炔衍生物作为起始原料的用途。根据本发明的第一个方面，本发明提供了一种合成酰基泛美他啶衍生物的方法，所述方法包括以下步骤：a）提供泛特甜胺源; b）提供酰基酯源; 和c）将氨基甜菜碱与酰基酯源接触以形成具有通式（I）的相应酰基 - 泛菌胺衍生物，其中R是酰基。本发明还提供了一种合成酰基的方法 - 辅酶A衍生物，以及在这两种方法的制备步骤中使用泛菌碱源和酰基酯源的用途。

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