5-fluorouracil derivative
    11.
    发明授权
    5-fluorouracil derivative 有权
    5-氟尿嘧啶衍生物

    公开(公告)号:US08889699B2

    公开(公告)日:2014-11-18

    申请号:US13419691

    申请日:2012-03-14

    IPC分类号: C07D401/14 A61K31/513

    CPC分类号: C07D401/14 Y02P20/55

    摘要: The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.

    摘要翻译: 本发明提供了抗肿瘤效果和毒性之间具有优异平衡性的新型抗代谢抗癌剂。 具体而言,本发明提供含有作为活性成分的式(I)表示的5-氟尿嘧啶衍生物或其盐的药物:其中,R1表示氢原子或羟基的保护基,R2表示低级 烷氧基 - 低级烷基或四氢呋喃基,X表示碳原子或氮原子,Y表示卤素原子或氰基。

    Transmission control system, subscriber-side communication device, and office-side communication device
    12.
    发明授权
    Transmission control system, subscriber-side communication device, and office-side communication device 有权
    传输控制系统,用户侧通信设备以及办公室通信设备

    公开(公告)号:US08654785B2

    公开(公告)日:2014-02-18

    申请号:US12926903

    申请日:2010-12-16

    IPC分类号: H04J3/00

    摘要: Provided is a subscriber-side communication device including a subscriber-side processing unit that continuously performs signal processing regardless of computer restart and includes a transmission processing unit that performs a data transmission process according to transmission control information contained in a received signal from the office-side communication device. Also provided is an office-side communication device including an office-side processing unit that continuously performs signal processing regardless of computer restart, and a transmission control information computing unit that computes transmission control information for each subscriber-side communication device, the office-side processing unit including a transmission control information storing unit that stores transmission control information of each subscriber-side communication device computed by the transmission control information computing unit, and a transmission control processing unit that performs a transmission control process with each subscriber-side communication device by using the transmission control information of each subscriber-side communication device stored in the transmission control information storing unit.

    摘要翻译: 提供一种用户侧通信装置,包括:无论计算机重新启动,连续执行信号处理的用户侧处理单元,并且包括发送处理单元,该发送处理单元根据来自办公室的接收信号中包含的发送控制信息进行数据发送处理, 侧通信设备。 还提供了一种办公室侧通信装置,其包括不管计算机重启而连续执行信号处理的办公室侧处理单元,以及计算每个用户侧通信装置的发送控制信息的发送控制信息计算单元, 处理单元,包括存储由发送控制信息计算单元计算出的每个用户侧通信设备的发送控制信息的发送控制信息存储单元,以及发送控制处理单元,其通过每个用户侧通信设备进行发送控制处理 使用存储在发送控制信息存储单元中的每个用户侧通信设备的发送控制信息。

    2 .beta.-substituted thiomethylpenicillin derivatives and their
preparation and use
    14.
    发明授权
    2 .beta.-substituted thiomethylpenicillin derivatives and their preparation and use 失效
    2β-取代的硫代甲基青霉素衍生物及其制备和用途

    公开(公告)号:US4861768A

    公开(公告)日:1989-08-29

    申请号:US16114

    申请日:1987-02-18

    IPC分类号: C07D499/00 C07D499/86

    CPC分类号: C07D499/00

    摘要: Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.

    摘要翻译: 公开了下式的青霉素衍生物:其中n是0,1或2的整数; Y是氰基,低级酰基,单 - 或二 - 低级烷硫基氨基甲酰基,其中R1是氢原子,低级烷基,苯基,基 - (CH2)m-OR2或 - (CH 2)m COOR 2(m为1〜6的整数,R2为氢原子或青霉素衍生物通常使用的青霉素羧酸酯形成基)或被选自上述的至少一种的苯基 由低级烷基,卤素原子和低级烷氧基组成; 和R是氢原子或青霉素羧酸酯形成基团或其盐。 它们可用作β-内酰胺酶抑制剂。

    Meat casing with internal release coating
    16.
    发明授权
    Meat casing with internal release coating 失效
    肉套与内部释放涂层

    公开(公告)号:US3945404A

    公开(公告)日:1976-03-23

    申请号:US447149

    申请日:1974-03-01

    摘要: A tubular casing for sausage, ham or like processed meat mass is coated internally with a water-soluble complex chromium compound with a view to improved peelability, among other purposes, of the casing from the meat mass encased therein. The complex chromium compound may first be diluted with water, with the pH of the resulting aqueous solution regulated as required by the addition of a slight amount of caustic soda or the like. The thus-prepared coating fluid is coated in a suitable fashion on the internal surface of the tubular meat casing, which may be either cellulosic or fibrous, and the coated casing is then dried as by hot drafts of air.

    摘要翻译: 用于香肠,火腿或类似加工肉块的管状肠衣在内部涂覆有水溶性复合铬化合物,以改进壳体从包裹在其中的肉块的其它目的的剥离性。 可以首先用水稀释复合的铬化合物,通过加入少量苛性钠等,根据需要调节所得水溶液的pH。 如此制备的涂布液以合适的方式涂覆在管状肉类外壳的内表面上,其可以是纤维素或纤维状物质,然后涂覆的外壳通过空气的热风干燥。

    Transmission control system, subscriber-side communication device, and office-side communication device
    17.
    发明申请
    Transmission control system, subscriber-side communication device, and office-side communication device 有权
    传输控制系统,用户侧通信设备和办公室通信设备

    公开(公告)号:US20110150482A1

    公开(公告)日:2011-06-23

    申请号:US12926903

    申请日:2010-12-16

    IPC分类号: H04J14/02

    摘要: Provided is a subscriber-side communication device including a subscriber-side processing unit that continuously performs signal processing regardless of computer restart and includes a transmission processing unit that performs a data transmission process according to transmission control information contained in a received signal from the office-side communication device. Also provided is an office-side communication device including an office-side processing unit that continuously performs signal processing regardless of computer restart, and a transmission control information computing unit that computes transmission control information for each subscriber-side communication device, the office-side processing unit including a transmission control information storing unit that stores transmission control information of each subscriber-side communication device computed by the transmission control information computing unit, and a transmission control processing unit that performs a transmission control process with each subscriber-side communication device by using the transmission control information of each subscriber-side communication device stored in the transmission control information storing unit.

    摘要翻译: 提供一种用户侧通信装置,包括:无论计算机重新启动,连续执行信号处理的用户侧处理单元,并且包括发送处理单元,该发送处理单元根据来自办公室的接收信号中包含的发送控制信息进行数据发送处理, 侧通信设备。 还提供了一种办公室侧通信装置,其包括不管计算机重启而连续执行信号处理的办公室侧处理单元,以及计算每个用户侧通信装置的发送控制信息的发送控制信息计算单元, 处理单元,包括存储由发送控制信息计算单元计算出的每个用户侧通信设备的发送控制信息的发送控制信息存储单元,以及发送控制处理单元,其通过每个用户侧通信设备进行发送控制处理 使用存储在发送控制信息存储单元中的每个用户侧通信设备的发送控制信息。

    Process for preparing substance GM-95
    18.
    发明授权
    Process for preparing substance GM-95 失效
    制造物质GM-95的方法

    公开(公告)号:US06818764B2

    公开(公告)日:2004-11-16

    申请号:US10433500

    申请日:2003-06-03

    IPC分类号: C07D51322

    摘要: A method of manufacturing substance GM-95 having general formula [I], comprising (a) deprotecting a macrocyclic compound having general formula [II] (wherein, R1's are the same or different and each represents a lower alkyl group, and R2 represents a thiol protecting group) by removing acetal protecting groups (the R1's) thereof, and forming an oxazole ring through an intramolecular cyclization reaction between produced formyl group and an amide group, and (b) deprotecting a resulting macrocyclic compound having general formula [III] (wherein, R2 is as mentioned above) by removing the thiol protecting group (R2) thereof, and forming a thiazoline ring through an intramolecular cyclization reaction between a thiol group thus produced and an amide group.

    摘要翻译: 制备具有通式[I]的物质GM-95的方法,包括(a)使通式[II]的大环化合物脱保护(其中,R 1相同或不同,各自表示低级烷基 ,R 2表示硫醇保护基),除去缩醛保护基(R 1),通过产生的甲酰基和酰胺基之间的分子内环化反应形成恶唑环,(b )通过除去其中的硫醇保护基(R 2),使所得的具有通式[III](其中R 2如上所述)的大环化合物脱保护,并通过分子内环化反应形成噻唑啉环 由此产生的硫醇基团和酰胺基团。

    Benzimidazole derivatives and pharmacologically acceptable salts thereof
    19.
    发明授权
    Benzimidazole derivatives and pharmacologically acceptable salts thereof 失效
    苯并咪唑衍生物及其药理学上可接受的盐

    公开(公告)号:US06248768B1

    公开(公告)日:2001-06-19

    申请号:US09341277

    申请日:1999-07-07

    IPC分类号: A61K314184

    摘要: This invention provides a compound having both IL-4 production inhibitory activity and PDE (IV) inhibitory activity, represented by formula (I): and a pharmaceutical composition or a therapeutic agent for acute and chronic inflammatory diseases and an anti-allergic or anti-inflammatory agent, each of which comprising an effective amount of the compound and a pharmacological carrier. It also provides use of the compound of formula (I) for the production of the aforementioned pharmaceutical composition or therapeutic agent for acute and chronic inflammatory diseases and anti-allergic or anti-inflammatory agent, and a method for treating acute and chronic inflammatory diseases.

    摘要翻译: 本发明提供具有由式(I)表示的IL-4产生抑制活性和PDE(IV)抑制活性两者的化合物:以及用于急性和慢性炎性疾病的药物组合物或治疗剂和抗过敏或抗 - 每一种都包含有效量的化合物和药理学载体。 还提供式(I)化合物用于制备上述药物组合物或急性和慢性炎性疾病和抗过敏或抗炎剂的治疗剂,以及治疗急性和慢性炎性疾病的方法。

    Epoxysuccinamide derivative or salt thereof
    20.
    发明授权
    Epoxysuccinamide derivative or salt thereof 失效
    环氧琥珀酰胺衍生物或其盐

    公开(公告)号:US6110967A

    公开(公告)日:2000-08-29

    申请号:US202607

    申请日:1998-12-17

    CPC分类号: C07D303/48

    摘要: The invention relates an epoxysuccinamide derivative represented by a formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl or aminoalkyl group, R.sup.2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R.sup.3 and R.sup.4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.

    摘要翻译: PCT No.PCT / JP98 / 01778 Sec。 371日期1998年12月17日第 102(e)1998年12月17日日期PCT提交1998年4月17日PCT公布。 第WO98 / 47887号公报 日期:1998年10月29日本发明涉及由式(I)表示的环氧琥珀酰胺衍生物:其中R1表示氢原子,烷基或氨基烷基,R2表示可以被取代的氨基烷基,可以被取代的芳基, 可以被取代的杂环基,可以被取代的芳烷基或被可被取代的杂环取代的烷基,或者可以被R 1和R 2形成可以被取代的含氮杂环,和 相邻的氮原子和R3和R4彼此相同或不同,并且独立地表示氢原子或烷基或芳烷基或其盐,其制备方法和包含这种衍生物或盐的药物 作为活性成分。 该化合物对组织蛋白酶L及其家族酶具有特异性抑制活性,可用作预防和治疗代谢性骨病如骨质疏松症和高钙血症的药剂。