Chiral 4-boronophenylalanine (BPA) derivative and method for producing same, and method for producing 18F-labeled BPA using said derivative
    71.
    发明授权
    Chiral 4-boronophenylalanine (BPA) derivative and method for producing same, and method for producing 18F-labeled BPA using said derivative 有权
    手性4-硼苯丙氨酸(BPA)衍生物及其制备方法,以及使用所述衍生物制备18F标记的BPA的方法

    公开(公告)号:US09409926B2

    公开(公告)日:2016-08-09

    申请号:US14435678

    申请日:2013-10-08

    Abstract: Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing 18F-2-fluoro-4-borono-L-phenylalanine (18F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR3R4, BX3− or BX3−M+ (wherein X represents a halogen atom, and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R1 represents a hydrogen atom or a protecting group PG1; R2 represents a hydrogen atom or a protecting group PG2; R3 and R4 independently represent OH, or R3, R4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO2, NH2, Sn(R6)3, N═N—NR7R8, OSO2R9, NR10R11, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18F-labeled BPA.

    Abstract translation: 提供:新型手性4-硼苯丙氨酸(BPA)衍生物; 一种制备衍生物的方法; 以及使用该衍生物制备18F-2-氟-4-硼羟-L-苯丙氨酸(18F标记的BPA; 18F-BPA)的方法。 制备由式(1)表示的化合物。 在该式中,R表示BR 3 R 4,BX 3 - 或BX 3 -M +(其中X表示卤原子,M +表示一价单原子阳离子,多原子阳离子或络合阳离子)。 R1表示氢原子或保护基PG1; R2表示氢原子或保护基PG2; R3和R4独立地表示OH,或R3,R4和B一起形成用作保护基的环; Y表示卤素原子,NO 2,NH 2,Sn(R 6)3,N = N-NR 7 R 8,OSO 2 R 9,NR 10 R 11,取代或未取代的苯基碘基或取代或未取代的杂环碘基。 使化合物与氟化试剂反应以制备18F标记的BPA。

    RICE COOKING METHOD
    74.
    发明申请
    RICE COOKING METHOD 审中-公开
    米饭烹饪方法

    公开(公告)号:US20150110937A1

    公开(公告)日:2015-04-23

    申请号:US14398071

    申请日:2013-02-06

    CPC classification number: A23L5/13 A23L7/10 A23L7/196 A23V2002/00

    Abstract: [Problem] To provide cooked rice in which aging can be suppressed without using low-amylose rice and which shows little deterioration in taste even after storing at ordinary or low temperatures.[Solution] In a rice cooking device provided with a conveying means such as a conveyor for conveying rice having been soaked in water, a steamer for steaming the rice on the conveyor with hot steam, and a water sprinkler for supplying warm water to the rice on the conveyor in the steamer, warm water is poured in an amount exceeding the amount required for cooking the rice in the aforesaid step for steaming in the steamer so as to wash away amylose eluted from the rice.

    Abstract translation: [问题]提供可以抑制老化的米饭,而不使用低直链淀粉米,即使在常温或低温下储存后也几乎没有味道劣化。 [解决方案]在具有输送装置的输送装置例如用于输送已经浸泡在水中的米的米饭烹调装置中,用热蒸汽在蒸汽输送机上蒸煮米的蒸笼和用于向米饭供应温水的喷水器 在蒸笼中的输送机上,在上述蒸汽蒸发步骤中,将温水倒入超过烹煮米的量,以便洗掉从米中洗脱的直链淀粉。

    BORON-CONTAINING COMPOUND
    77.
    发明申请

    公开(公告)号:US20190177341A1

    公开(公告)日:2019-06-13

    申请号:US16320989

    申请日:2017-07-20

    Abstract: To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent B—H; —R1 represents —(CH2)n-X1—R3 (n represents an integer of 0 to 6; X1 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; R3 represents C6-C20 alkyl, hydroxy C6-C20 alkyl, amino C6-C20 alkyl, azido C6-C20 alkyl, hydroxycarbonyl C6-C20 alkyl, or the like), or a group having a repeating sequence of —(CH2)2—O— 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and —R2 is —(CH2)m-X2—R4 (m represents an integer from 0 to 8; X2 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; and R4 represents a tumor recognition moiety), or does not existare prepared and used.

    METHOD FOR PRODUCING FLUORINATED COMPOUND
    78.
    发明申请

    公开(公告)号:US20190071376A1

    公开(公告)日:2019-03-07

    申请号:US16082389

    申请日:2017-03-08

    Abstract: This invention solves the problem of providing an efficient, new method for producing a fluoromethylene-containing compound. The problem can be solved by a method for producing a compound represented by formula (1) or a ring-closed or ring-opened derivative of the compound, wherein R1 represents an organic group, RX represents hydrogen or fluorine, R2a, R2b, R2c, and R2d are the same or different, and each represents —Y—R21 or —N(—R22)2, or R2b and R2c may join together to form a bond, wherein Y represents a bond, oxygen, or sulfur, R21 represents hydrogen or an organic group, and R22, in each occurrence, is the same or different and represents hydrogen or an organic group; the method comprising step A of reacting a compound represented by formula (2), wherein X represents a leaving group, and other symbols are as defined above, with a compound represented by formula (3), wherein the symbols are as defined above, in the presence of a reducing agent under light irradiation.

    ANALYSIS PLATE, ANALYSIS METHOD, AND METHOD OF MANUFACTURING ANALYSIS PLATE

    公开(公告)号:US20190033213A1

    公开(公告)日:2019-01-31

    申请号:US16072590

    申请日:2017-02-06

    Abstract: An analysis plate including: a substrate; and a molecule immobilized on a surface of the substrate, the molecule specifically recognizing a measurement target substance, wherein the substrate includes a selective reflection layer in at least part of the layer thereof. Preferably, the surface of the substrate has a concavo-convex structure capable of exhibiting a structural color. Preferably, a band of light reflection caused by a selective reflectivity of the selective reflection layer falls within a band of light reflection caused by the concavo-convex structure. Also provided are an analysis method using the same and a production method thereof.

    NON-PEPTIDIC GAPDH AGGREGATION INHIBITOR
    80.
    发明申请

    公开(公告)号:US20180116981A1

    公开(公告)日:2018-05-03

    申请号:US15574651

    申请日:2016-06-08

    Abstract: [Problem] Provided is a non-peptide compound, which can be used as a GAPDH aggregation inhibitor, [Solution] Provided is a GAPDH aggregation inhibitor including as an active ingredient a compound represented by the chemical formula 1 wherein R1, R2, and R3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, a polysulfurized derivative thereof, or a pharmaceutically acceptable salt thereof. The present compound has a GAPDH aggregation inhibitory activity to suppress intracerebral aggregation of various proteins involved in cerebral neurodegenerative diseases, thereby contributing to improvement in various brain neurological diseases associated with aggregation of these proteins such as Alzheimer's disease, Parkinson's disease, and cerebral infarction, and prevention of advanced seriousness of these diseases.

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