Method of treating tumors using O-substituted fumagillol derivatives
    91.
    发明授权
    Method of treating tumors using O-substituted fumagillol derivatives 失效
    使用O-取代的烟曲霉醇衍生物治疗肿瘤的方法

    公开(公告)号:US6017954A

    公开(公告)日:2000-01-25

    申请号:US940123

    申请日:1992-09-03

    摘要: This invention relates to methods of using O-substituted fumagillol derivatives or salts thereof preferably, O-(N-chloroacetylcarbamoyl) fumagillol, O-(N-chloroacetylcarbamoyl)dihydrofumagillol or O-(N-chloracetylcarbamoyl)-6'b-hydroxyfumagillol, which have angiogenesis inhibitory activity, in the treatment and prevention of various diseases caused or advanced by abnormally hyperactive angiogenesis, especially various inflammatory diseases (rheumatism, psoriasis, etc.), diabetic retinopathy and cancer and other angiogenesis-dependent tumors, especially Kaposi's sarcoma, breast cancer, colon cancer.

    摘要翻译: 本发明涉及使用O-取代的烟曲霉醇衍生物或其盐优选O-(N-氯乙酰基氨基甲酰基)烟曲霉醇,O-(N-氯乙酰基氨基甲酰基)二氢烟曲霉素或O-(N-氯乙酰基氨基甲酰基)-6'-羟基烟曲霉素的方法,其中 具有血管生成抑制活性,用于治疗和预防由异常血液生成异常引起或促进的各种疾病,特别是各种炎性疾病(风湿病,牛皮癣等),糖尿病性视网膜病变和癌症以及其它血管生成依赖性肿瘤,特别是卡波西肉瘤,乳腺癌 癌症,结肠癌。

    Syllable-beat-point synchronized rule-based speech synthesis from coded
utterance-speed-independent phoneme combination parameters
    92.
    发明授权
    Syllable-beat-point synchronized rule-based speech synthesis from coded utterance-speed-independent phoneme combination parameters 失效
    基于编码话音速度独立音素组合参数的音节点同步规则语音合成

    公开(公告)号:US5682502A

    公开(公告)日:1997-10-28

    申请号:US490140

    申请日:1995-06-14

    CPC分类号: G10L13/06 G10L21/04

    摘要: In a speech synthesizer, each frame for generating a speech waveform has an expansion degree to which the frame is expanded or compressed in accordance with the production speed of synthetic speech. In accordance with the set speech production speed, the time interval between beat synchronization points is determined on the basis of the speed of the speech to be produced, and the time length of each frame present between the beat synchronization points is determined on the basis of the expansion degree of the frame. Parameters for producing a speech waveform in each frame are properly generated by the time length determined for the frame. In the speech synthesizer for outputting a speech signal by coupling phonemes constituted by one or a plurality of frames having phoneme vowel-consonant combination parameters (VcV, cV, or V) of the speech waveform, the number of frames can be held constant regardless of a change in the speech production speed. This prevents degradation in the tone quality or a variation in the processing quantity resulting from a change in the speech production speed.

    摘要翻译: 在语音合成器中,用于产生语音波形的每个帧具有根据合成语音的生产速度来扩展或压缩帧的扩展度。 根据设定的语音生成速度,基于要产生的语音的速度来确定拍子同步点之间的时间间隔,并且基于在拍子同步点之间存在的每个帧的时间长度 框架的扩展程度。 用于产生每帧中的语音波形的参数通过为帧确定的时间长度适当地产生。 在语音合成器中,通过将由语音波形的音素元音辅音组合参数(VcV,cV或V)组成的一个或多个帧构成的音素耦合到语音信号中,可以将帧数保持不变,而不管 演讲生产速度的变化。 这防止了语音质量的劣化或由语音生成速度的变化导致的处理量的变化。

    Low baking temperature hardenable aluminum alloy sheet for press-forming
    93.
    发明授权
    Low baking temperature hardenable aluminum alloy sheet for press-forming 失效
    低烘烤温度可淬火的铝合金板用于压制成型

    公开(公告)号:US5580402A

    公开(公告)日:1996-12-03

    申请号:US156034

    申请日:1993-11-19

    CPC分类号: C22F1/04 C22C21/06 C22F1/047

    摘要: Disclosed is an aluminum alloy sheet having a chemical composition of an Si-containing Al--Mg--CU alloy. The aluminum alloy sheet exhibits a streak-shaped modulated structure at a diffraction grating points of an Al--Cu--Mg--system compound in the electron beam diffraction grating image. The above mentioned streak can be generated efficiently when the alloy essentially consists of 1.5 to 3.5% by weight of Mg, 0.3 to 1.0% by weight of Cu, 0.05 to 0.6% by weight of Si, and the balance of Al and inevitable impurities, and the ratio of Mg/Cu is in the range of 2 to 7. The alloy contains 0.01-0.50% of at least one element selected from the group consisting of Sn, Cd, and In.

    摘要翻译: 公开了具有含Si的Al-Mg-Cu合金的化学组​​成的铝合金板。 铝合金板在电子束衍射光栅图像中的Al-Cu-Mg系化合物的衍射光栅点处呈现条纹状的调制结构。 当合金基本上由Mg,0.3〜1.0重量%的Cu,0.05〜0.6重量%的Si,余量的Al和不可避免的杂质组成时,能够有效地产生上述条纹, 并且Mg / Cu的比例在2〜7的范围内。该合金含有0.01-0.50%的选自Sn,Cd和In中的至少一种元素。

    Method for analyzing nucleic acid or protein and apparatus therefor
    94.
    发明授权
    Method for analyzing nucleic acid or protein and apparatus therefor 失效
    分析核酸或蛋白质的方法及其设备

    公开(公告)号:US5458761A

    公开(公告)日:1995-10-17

    申请号:US378973

    申请日:1995-01-27

    IPC分类号: G01N27/447 G01N27/26

    摘要: Analysis of a nucleic acid samples having thousands of bases is conducted by capillary electrophoresis. The electrophoretic section is provided with a first capillary filled with an agarose gel and a second capillary filled with a polyacrylamide gel. An on-column detector is incorporated with the second capillary for optical detection. To fill a capillary with a gel, a solution is fed under high pressure from a first flow channel through a switching valve into a second flow channel connected to the capillary. To inject a sample in the capillary, a sample injector is connected to a switching valve passage, and a buffer solution is connected to the capillary through a flow channel and the switching valve. After switching the valve, the first passage is incorporated into the flow channel between the buffer solution and the capillary being filled. Then, the sample is electro-kinetically injected into the capillary. When conducting genetic polymorphism by electrophoresis, temperature control elements are provided to maintain the capillary at a predetermined temperature and a DNA sample device is provided to heat the sample to a temperature higher than a disassociation temperature thereof for directly injecting the heated sample into the capillary.

    摘要翻译: 通过毛细管电泳分析具有数千个碱基的核酸样品。 电泳部分设置有填充有琼脂糖凝胶的第一毛细管和填充有聚丙烯酰胺凝胶的第二毛细管。 柱内检测器与第二毛细管并入,用于光学检测。 为了用凝胶填充毛细管,将溶液在高压下从第一流动通道通过切换阀进入连接到毛细管的第二流动通道。 为了在毛细管中注入样品,将样品注射器连接到切换阀通道,并且缓冲溶液通过流动通道和切换阀连接到毛细管。 在切换阀之后,第一通道被并入缓冲溶液和被填充的毛细管之间的流动通道中。 然后,将样品电动注射到毛细管中。 当通过电泳进行遗传多态性时,提供温度控制元件以将毛细管保持在预定温度,并且提供DNA样品装置以将样品加热到高于其解离温度的温度,以将加热的样品直接喷射到毛细管中。

    Driving circuit for solid-state image sensor and counter circuit used
therein
    95.
    发明授权
    Driving circuit for solid-state image sensor and counter circuit used therein 失效
    其中使用的固态图像传感器和计数器电路的驱动电路

    公开(公告)号:US5249054A

    公开(公告)日:1993-09-28

    申请号:US796574

    申请日:1991-11-22

    CPC分类号: H04N5/335 H03K23/005

    摘要: A counter circuit which incurs a uniform number of logic changes whether the clock signal is rising or falling is used in both a first counter circuit for measuring the reference signal for horizontal scanning period and a second counter circuit for measuring signals in the vertical blanking period. Since the number of logic changes of the flip-flops with respect to the clock signal is uniform, a driving circuit for a solid-state image sensor is realized in which noise in the vertical blanking period does not appear in the video period even if by using 1H delay line.

    摘要翻译: 在用于测量水平扫描周期的参考信号的第一计数器电路和用于在垂直消隐周期中测量信号的第二计数器电路两者中都使用引起统计数量的逻辑改变的计数器电路,不管时钟信号是上升还是下降。 由于触发器相对于时钟信号的逻辑变化的数量是均匀的,因此实现了用于固态图像传感器的驱动电路,其中垂直消隐期间的噪声在视频周期内不出现,即使通过 使用1H延迟线。

    6-epifumagillols and the pharmaceutical use thereof
    97.
    发明授权
    6-epifumagillols and the pharmaceutical use thereof 失效
    6-EPIFUMAGILLOLS及其药物用途

    公开(公告)号:US5204345A

    公开(公告)日:1993-04-20

    申请号:US489010

    申请日:1990-03-06

    IPC分类号: C07D303/22 C07D405/12

    CPC分类号: C07D303/22 C07D405/12

    摘要: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 is hydrogen atom, an optionally substituted aliphatic hydrocarbon residue or an optionally substituted acyl group, or a salt thereof.The compound (I) of the invention has, among others, angiogenesis inhibiting activity, cell-proliferation inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

    Fumagillol derivatives and pharmaceutical compositions thereof
    98.
    发明授权
    Fumagillol derivatives and pharmaceutical compositions thereof 失效
    烟曲霉醇衍生物及其药物组合物

    公开(公告)号:US5166172A

    公开(公告)日:1992-11-24

    申请号:US662120

    申请日:1991-02-28

    摘要: The present invention is related to a compound of the formula ##STR1## wherein R.sup.1 is a 2-methyl-1-propenyl or isobutyl group which may be substituted and R.sup.2 is (1) a substituted alkanoyl group, (2) a substituted aroyl group having at least one substituent selected from the group consisting of C.sub.2-6 alkyl, amino, halogen, hydroxyl, lower alkoxy, cyano, carbamoyl and carboxyl, (3) an aromatic heterocycle-carbonyl, which may optionally be substituted, (4) a carbamoyl group, which may optionally be substituted, (5) an alkyl group, which may optionally be substituted, (6) a benzenesulfonyl group, which may optionally be substituted, (7) an alkylsulfonyl group, which may optionally be substituted, (8) a sulfamoyl group, which may optionally be substituted, (9) an alkoxycarbonyl group, which may optionally be substituted or (10) a phenoxycarbonyl group, which may optionally be substituted; or a salt thereof.The compound (I) has a strong angiogenesis inhibitory activity.

    摘要翻译: 本发明涉及下式化合物:其中R1是可被取代的2-甲基-1-丙烯基或异丁基,R2是(1)取代的烷酰基,(2)取代的芳酰基 具有至少一个选自C 2-6烷基,氨基,卤素,羟基,低级烷氧基,氰基,氨基甲酰基和羧基的取代基的取代基,(3)可任意取代的芳族杂环羰基,(4) 可任选被取代的(5)可任选被取代的烷基,(6)可任意被取代的苯磺酰基,(7)可任意被取代的烷基磺酰基,(8) )可任选被取代的氨磺酰基,(9)可任选被取代的烷氧基羰基或可任选被取代的(10)苯氧基羰基; 或其盐。 化合物(I)具有强的血管生成抑制活性。

    Film-shape soap
    99.
    发明授权
    Film-shape soap 失效
    胶片形肥皂

    公开(公告)号:US5062986A

    公开(公告)日:1991-11-05

    申请号:US505471

    申请日:1990-04-06

    CPC分类号: C11D17/06 C11D9/225

    摘要: The present invention relates to a film-shape soap comprising (a) a water soluble polymer and (b) a soap; said water soluble polymer is a polyester of polyether polyol having an average molecular weight of more than about 1,000 and a polycarboxylic acid, and has a weight average molecular weight of not less than about 20,000, which has a rapid soluble time in water in spite of a lower equilibrium moisture content, excellent washability, little stimulation to a skin, flexible (not brittle) and stable properties, and is suitable for a portable type toilet soap, disposable soap and the like.

    摘要翻译: 本发明涉及一种膜状皂,其包含(a)水溶性聚合物和(b)皂; 所述水溶性聚合物是平均分子量大于约1,000的聚醚多元醇的聚酯和多元羧酸,并且具有不低于约20,000的重均分子量,其在水中具有快速的溶解时间,尽管 较低的平衡含水量,优异的可洗性,对皮肤刺激小,柔软(不脆)和稳定性能,适用于便携式厕所肥皂,一次性肥皂等。

    Oxazoleacetic acid derivatives
    100.
    发明授权
    Oxazoleacetic acid derivatives 失效
    恶唑乙酸衍生物

    公开(公告)号:US4602027A

    公开(公告)日:1986-07-22

    申请号:US501012

    申请日:1983-06-06

    CPC分类号: C07D263/32 C07D263/40

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is (A) a group of the formula, ##STR2## wherein R.sup.4 is H, a halogen or trifluoromethyl group, or (B) a group of the formula, ##STR3## wherein n is 0 or an integer of 1 to 3; R.sup.5 is H or an alkyl group of 1 to 6 carbon atoms; respective R.sup.6 and R.sup.7 are an alkyl group of 1 to 6 carbon atoms, an alkenyl group of 2 to 6 carbon atoms, a cycloalkyl group of 3 to 7 carbon atoms, or a cycloalkenyl group of 5 to 7 carbon atoms; R.sup.6 and R.sup.7 may be combined with the neighboring carbon atom to represent a cycloalkyl group of 3 to 7 carbon atoms; a cycloalkenyl group of 5 to 7 carbon atoms, a bicycloalkyl group of 7 to 10 carbon atoms, or a bicycloalkenyl group of 7 to 10 carbon atoms; R.sup.2 is an alkyl group of 1 to 6 carbon atoms; and R.sup.3 is H, an alkyl group of 1 to 6 carbon atoms or an aralkyl group, or a pharmaceutically acceptable salt thereof. The compound has hypoglycemic, glucose tolerance improving and insulin sensitivity potentiating activities.

    摘要翻译: 下式的化合物,其中R 1是(A)下式的基团,其中R 4是H,卤素或三氟甲基,或(B)下式的基团,其中n 为0或1〜3的整数; R5是H或1-6个碳原子的烷基; 各自的R 6和R 7为碳原子数1〜6的烷基,碳原子数2〜6的烯基,碳原子数3〜7的环烷基或碳原子数为5〜7的环烯基。 R6和R7可以与相邻的碳原子结合,代表3-7个碳原子的环烷基; 具有5至7个碳原子的环烯基,7至10个碳原子的双环烷基或7至10个碳原子的双环烯基; R2是1-6个碳原子的烷基; R3为H,1〜6个碳原子的烷基或芳烷基,或其药学上可接受的盐。 该化合物具有降血糖,葡萄糖耐量提高和胰岛素敏感性增强活性。