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61. 发明申请

US20040198808A1 Halogenated triptolide derivatives as immunomodulators and anticancer agents 失效
标题翻译：卤代雷公藤内酯衍生物作为免疫调节剂和抗癌剂
公开(公告)号：US20040198808A1
公开(公告)日：2004-10-07
申请号：US10786663
申请日：2004-02-23
发明人： Dongcheng Dai , John H. Musser
IPC分类号： A61K031/365 , C07D491/14
CPC分类号： C07D493/22
摘要： Compounds having the structure I: 1 are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, CnullO, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, CnullO, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, CnullO, COOH, CH2F, CHF2 and CF3; such that: at least one of R1nullR13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.
摘要翻译：具有结构I的化合物可用于诱导细胞死亡（凋亡）和免疫抑制。在结构I中，CR 1 R 2选自CHOH，C = O，CHF，CF 2和C（CF 3）OH; CR 6和CR 13选自CH，COH和CF; CR 7 R 8，CR 9 R 10和CR 11 R 12选自CH 2，CHOH，C = O，CHF和CF 2; 并且CR 3 R 4 R 5选自CH 3，CH 2 OH，C = O，COOH，CH 2 F，CHF 2和CF 3; 使得：R 1 -R 13中的至少一个包含氟; 不多于两个CR 3 R 4 R 5，CR 6，CR 7 R 8，CR 9 R 10，CR 11 R 12，且CR 13包含氟或氧; 并且当CR 1 R 2是CHOH时，CR 3 R 4不是CH 2 F。

62. 发明申请

US20040132998A1 Compositions and methods for separating amines and amino acids from their counter-enantiomers 失效
标题翻译：用于从其对映异构体中分离胺和氨基酸的组合物和方法
公开(公告)号：US20040132998A1
公开(公告)日：2004-07-08
申请号：US10664045
申请日：2003-09-16
发明人： Ronald L. Bruening , Krzysztof E. Krakowiak
IPC分类号： C07D491/14 , C07C229/02
CPC分类号： C07B57/00 , A61K31/045 , A61K31/40 , C07D323/00 , C07D498/08
摘要： Diketo- and pyridine-containing chiral crown ligands having at least two chiral bulky groups attached to two different chiral carbon atoms of the crown that are covalently bonded to or coated on suitable solid supports, and further coated by hydrophobic organic solvents are disclosed. These compositions and associated methods are characterized by selectivity of several target amine or amino acid enantiomers over their counter-enantiomers and derivatives. The composition preferably has an null-value greater than or equal to 4. This allows for the separation of such enantiomers with non-chromatographic resin bed separations of three separation stages or less.
摘要翻译：含有二酮和吡啶的手性冠配体，其具有至少两个连接到冠上两个不同手性碳原子的手性大体积基团，其共价键合或涂覆在合适的固体载体上，并进一步用疏水性有机溶剂涂覆。这些组合物和相关方法的特征在于几种靶胺或氨基酸对映异构体对其对映异构体和衍生物的选择性。组合物优选具有大于或等于4的α值。这允许用三个分离阶段或更少的非层析树脂床分离来分离这些对映异构体。

63. 发明申请

US20040077863A1 Chemical methods 有权
标题翻译：化学方法
公开(公告)号：US20040077863A1
公开(公告)日：2004-04-22
申请号：US10363433
申请日：2003-12-02
发明人： Peter Scammells , Nicholas Gathergood , Justin Ripper
IPC分类号： A23L001/00 , C07D491/14
CPC分类号： C07D489/02
摘要： This invention relates to a method for N-demethylating an N-methyl morphinane comprising the steps of: (i) treating said N-methyl morphinane with an oxidizing agent to form the N-oxide morphinane; and (ii) treating said N-oxide morphinane with a reducing agent. This invention also relates to a method for oxidizing a null7-morphinane compound to a null6, null8-morphinane compound, comprising the steps of treating said null7-morphinane with null-MnO2 for a time and under conditions sufficient to oxidize said null7morphinane, and treating the null-MnO2 with glycol or a derivative thereof, and/or an inorganic salt.
摘要翻译：本发明涉及一种N-甲基吗啡烷N-去甲基化方法，包括以下步骤：（i）用氧化剂处理所述N-甲基吗啡烷以形成N-氧化物吗啡烷; 和（ii）用还原剂处理所述N-氧化物吗啡烷。本发明还涉及将Delta7-吗啉化合物氧化成δ6，δ8 - 吗啉化合物的方法，该方法包括以下步骤：用γ-MnO 2处理所述δ7 - 吗啉时间和条件下，足以氧化所述的δ7吗啡烷，并用二醇或其衍生物和/或无机盐处理γ-MnO 2。

64. 发明申请

US20040043498A1 Reagent for determining singlet oxygen 审中-公开
标题翻译：用于测定单线态氧的试剂
公开(公告)号：US20040043498A1
公开(公告)日：2004-03-04
申请号：US10362214
申请日：2003-08-27
发明人： Tetsuo Nagano , Yasuteru Urano , Kumi Tanaka
IPC分类号： G01N033/00 , C07D491/14
CPC分类号： C07D493/08 , C07D311/82 , C07D493/10 , Y10T436/20
摘要： Compounds useful as agents for measurement of singlet oxygen, which are represented by the following general formula (I): 1 wherein R1, R2, R3, R4, R5, and R6 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, R7 and R8 independently represent a C1-4 alkyl group, and R9 represents a hydrogen atom, a C1-12 alkanoyl group, or acetoxymethyl group, or salts thereof.
摘要翻译：用作测量单线态氧的试剂的化合物，其由以下通式（I）表示：其中R 1，R 2，R 3，R 4，R 5和R 独立地表示氢原子，卤素原子，C 1-6烷基或C 1-6烷氧基，R 7和R 8独立地表示C 1-4烷基，R 9 >表示氢原子，C1-12烷酰基或乙酰氧基甲基，或其盐。

65. 发明申请

US20040019056A1 Anititumoral analogs of et-743 有权
标题翻译： et-743的抗肿瘤类似物
公开(公告)号：US20040019056A1
公开(公告)日：2004-01-29
申请号：US10257857
申请日：2003-03-31
发明人： Ignacio Manzanares , Maria Jesus Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
IPC分类号： A61K031/498 , C07D491/14
CPC分类号： C07D491/18 , C07D471/18 , C07D471/22 , C07D491/22 , C07D497/22
摘要： Antitumour compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.
摘要翻译：抗肿瘤化合物具有式（ⅩⅣ）的五元稠环甙元结构。本发明化合物缺乏在ecteinascidins中发现的1,4桥连基团。它们在C-1位具有选自任选保护或衍生的氨基亚甲基或任选保护或衍生的羟基亚甲基的取代基。

66. 发明申请

US20040014747A1 CRF receptor antagonists and methods relating thereto 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：US20040014747A1
公开(公告)日：2004-01-22
申请号：US10357315
申请日：2003-02-03
申请人： Neurocrine Biosciences, Inc.
发明人： Mustapha Haddach
IPC分类号： A61K031/549 , A61K031/53 , A61K031/542 , C07D498/14 , C07D491/14 , C07D487/14
CPC分类号： C07D487/16 , C07D498/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke. The CRF receptor antagonists of this invention have the following structure: 1 including stereoisomers and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, A, and X are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗多种疾病，包括治疗在温血动物如中风中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有以下结构：包括立体异构体及其药学上可接受的盐，其中m，R，R 1，R 2，A和X如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

67. 发明申请

US20030216421A1 Cascade esters of camptothecins and methods of treating cancer using these compounds 有权
标题翻译：喜树碱的级联酯和使用这些化合物治疗癌症的方法
公开(公告)号：US20030216421A1
公开(公告)日：2003-11-20
申请号：US10139778
申请日：2002-05-06
发明人： Zhisong Cao , Beppino C. Giovanella
IPC分类号： C07D491/14 , A61K031/4745
CPC分类号： C07D491/22
摘要： Cascade esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment are also described.
摘要翻译：描述了喜树碱的级联酯。还描述了制备这些化合物并将其用于癌症治疗中的方法。

68. 发明申请

US20030164481A1 Ophthalmic filter materials 失效
标题翻译：眼科过滤材料
公开(公告)号：US20030164481A1
公开(公告)日：2003-09-04
申请号：US10044595
申请日：2002-01-09
发明人： Thomas G. Havens , David J. Kerko , Brent M. Wedding
IPC分类号： G03C001/00 , F21V009/00 , C07D491/14
CPC分类号： G02B5/23 , C09K9/02 , C09K2211/1425 , C09K2211/1433
摘要： Disclosed is a photochromic plastic ophthalmic lenses having polymer matrices with an effective amount of at least one photochromic agent distributed therein, applied thereto or associated therewith and at least one ophthalmic filtering dye applied thereto, associated therewith or distributed therein the lens. A group of the filter lenses have dominant wavelengthes between 570 and 605 nm and color purity between 50% and 75%. Another lens product of the present invention is particularly suitable for patients suffering from retinitis pigmentosa. The lenses of the present invention are particularly suitable for individuals bothered by strong or variable illumination intensity.
摘要翻译：公开了一种光致变色塑料眼镜片，其具有聚合物基质，其具有分散在其中的有效量的至少一种光致变色剂，施用于其上或与其相关联，以及至少一种与其相关联或分布在其中的眼科过滤染料。一组滤镜在570和605nm之间具有显着的波长，色纯度在50％和75％之间。本发明的另一种镜片产品特别适用于患有色素性视网膜炎的患者。本发明的镜片特别适用于被强烈或可变的照明强度打扰的个人。

69. 发明申请

US20030144304A1 Novel hexacyclic compounds 失效
标题翻译：新六环化合物
公开(公告)号：US20030144304A1
公开(公告)日：2003-07-31
申请号：US10304672
申请日：2002-11-26
发明人： Takeshi Murata , Satoshi Niizuma , Nobuo Shimma , Hitomi Suda , Masao Tsukazaki
IPC分类号： A61K031/519 , C07D491/14
CPC分类号： C07D491/22
摘要： The present invention relates to hexacyclic compound of the formula null1null, 1 wherein Z, R3 and R4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式[1]的六环化合物及其药学上可接受的盐，其中Z，R 3和R 4如此鉴定。这些化合物可用于治疗细胞增殖性疾病。

70. 发明申请

US20030139412A1 Tricyclic imidazopyridines 失效
标题翻译：三环咪唑并吡啶
公开(公告)号：US20030139412A1
公开(公告)日：2003-07-24
申请号：US10182654
申请日：2002-10-04
发明人： J?ouml;rg Senn-Bilfinger , Wilm Buhr , Reinhard Huber , Ernst Sturm
IPC分类号： A61K031/5377 , A61K031/4745 , C07D491/14 , C07D471/14
CPC分类号： C07D471/14
摘要： 1 Compounds of formula (1), in which the substituents as defined in the description are useful for preventing and treating gastrointestinal disorders.
摘要翻译：式（1）的化合物，其中描述中定义的取代基可用于预防和治疗胃肠道疾病

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