SALT AND CRYSTAL OF TRIAZOLOPYRAZINE DERIVATIVE

    公开(公告)号:US20210094955A1

    公开(公告)日:2021-04-01

    申请号:US16755799

    申请日:2018-10-12

    IPC分类号: C07D487/04 C07C62/04

    摘要: [Problem] Provided are a salt of (4-fluorophenyl)[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]methanone, and a crystal of the salt.
    [Element for Solution] Salts of (4-fluorophenyl)[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]methanone with various acids have been studied. As a result, a pharmaceutically acceptable salt of the compound and a crystal of the salt have been found.
    That is, the present invention relates to a salt of the compound and a crystal of the salt. Furthermore, the present invention relates to a pharmaceutical composition including a salt of the compound or a crystal of the salt, and one or more excipients.

    Process for resolution of chiral alcohols or phenols or chiral lactonic
compounds
    4.
    发明授权
    Process for resolution of chiral alcohols or phenols or chiral lactonic compounds 失效
    手性醇或酚或手性内酯化合物的拆分方法

    公开(公告)号:US4540797A

    公开(公告)日:1985-09-10

    申请号:US447442

    申请日:1982-12-06

    摘要: Novel ethers of organic compounds containing chiral atoms of the formula ##STR1## wherein A is a hydrocarbonated chain of 1 to 10 groups, the said chain containing one or more heteroatoms, one or more unsaturations, the assembly of the groups constituting the chain may represent a mono- or polycyclic system, including a system of the spiro or endo type, the chain A can contain one or more chiral atoms or the lactone moiety can present a chirality due to the dissymmetric spatial configuration of the whole of the molecule and Z is selected from the group consisting of primary, secondary or tertiary alcohol moiety containing at least an asymmetric carbon atom, a phenol moiety substituted comprising at least one asymmetric carbon atom and a substituted alcohol or phenol moiety with a chirality due to the dissymmetric spatial configuration of the whole of the molecule, with the proviso Z is not (R) or (S) .alpha.-cyano-3-phenoxy-benzyl when A is ##STR2## which are useful for the resolution of compounds of the formulae ##STR3## wherein A and Z have the above definitions and X is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms.

    摘要翻译: 含有式(I)的手性原子的有机化合物的新型醚,其中A是1至10个基团的烃化链,所述链含有一个或多个杂原子,一个或多个不饱和基团,构成链的基团的组合 代表单环或多环系统,包括螺或内型的系统,链A可以含有一个或多个手性原子,或者内酯部分可以由于整个分子和Z的不对称空间构型而呈现手性 选自含有至少不对称碳原子的伯,仲或叔醇部分,被至少一个不对称碳原子取代的苯酚部分和具有由于不对称空间构型引起的手性的取代的醇或苯酚部分 整个分子,条件是Z不是(R)或(S)α-氰基-3-苯氧基 - 苄基,当A是,它们对分辨率o有用 f化合物,其中A和Z具有上述定义,X选自氢和1至4个碳原子的烷基。

    Novel chiral ethers and their use in resolution of alcohols and phenols
    5.
    发明授权
    Novel chiral ethers and their use in resolution of alcohols and phenols 失效
    新型手性醚及其在醇和酚的拆分中的应用

    公开(公告)号:US4265817A

    公开(公告)日:1981-05-05

    申请号:US21833

    申请日:1979-03-19

    摘要: Novel ethers of organic compounds containing chiral atoms of the formula ##STR1## wherein A is a hydrocarbonated chain of 1 to 10 groups, the said chain containing one or more heteroatoms, one or more unsaturations, the assembly of the groups constituting the chain may represent a mono- or polycyclic system, including a system of the spiro or endo type, the chain A can contain one or more chiral atoms or the lactone moiety can present a chirality due to the dissymetric spatial configuration of the whole of the molecule and Z is selected from the group consisting of primary, secondary or tertiary alcohol moiety containing at least an asymetric carbon atom, a phenol moiety substituted comprising at least one asymetric carbon atom and an substituted alcohol or phenol moiety with a chirality due to the dissymetric spatial configuration of the whole of the molecule, with the proviso Z is not (R) or (S) .alpha.-cyano-3-phenoxy-benzyl when A is ##STR2## which are useful for the resolution of compounds of the formulae ##STR3## wherein A and Z have the above definitions and X is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms.

    摘要翻译: 含有式(I)的手性原子的有机化合物的新型醚,其中A是1至10个基团的烃化链,所述链含有一个或多个杂原子,一个或多个不饱和基团,构成链的基团的组合 代表单环或多环系统,包括螺或内型的系统,链A可以含有一个或多个手性原子,或者内酯部分可以呈现手性,这是由于整个分子的不对称空间结构和Z 选自包含至少一个不对称碳原子的伯,仲或叔醇部分,被至少一个不对称碳原子取代的苯酚部分和具有手性的取代的醇或苯酚部分,这些部分具有由于不对称空间构型的手性 整个分子,条件是Z不是(R)或(S)α-氰基-3-苯氧基 - 苄基,当A是,其可用于分辨c 其中A和Z具有上述定义并且X选自氢和1至4个碳原子的烷基的式的化合物。

    TASTE-IMPROVING AGENT FOR POTASSIUM SALT OR POTASSIUM SALT-CONTAINING FOOD OR DRINK
    6.
    发明申请
    TASTE-IMPROVING AGENT FOR POTASSIUM SALT OR POTASSIUM SALT-CONTAINING FOOD OR DRINK 审中-公开
    硫酸钾或含盐食品或饮料的改性剂

    公开(公告)号:US20110104361A1

    公开(公告)日:2011-05-05

    申请号:US13001071

    申请日:2009-06-23

    摘要: The invention improves the unpleasant taste characteristic of potassium salts without affecting the original flavor of foods or drinks and increases the value of potassium salt as a salt substitute, in order to provide means and a salt composition for reducing sodium in foods and drinks.By adding one or more of the following: quinic acid or a quinic acid-containing composition, spilanthol or a spilanthol-containing plant extract or plant essential oil, or an Allium plant extract, to a potassium salt or a potassium salt-containing food or drink, the unpleasant tastes such as acrid taste and metallic taste characteristic of potassium salts are improved while the salt flavor and taste are augmented.

    摘要翻译: 本发明改善了钾盐的令人不愉快的味道特征,而不影响食品或饮料的原始风味,并提高了作为盐替代物的钾盐的价值,以提供用于减少食品和饮料中的钠的方法和盐组合物。 通过添加一种或多种以下物质:将含有奎尼酸或含奎尼酸的组合物,西兰替康或含有稀释素的植物精油或植物精油或葱属植物提取物加入钾盐或含钾盐的食物中,或 饮料中,改善了钾盐的刺激味道和金属味道特征的不愉快的味道,同时增加了盐味和味道。

    Potassium channel opener
    7.
    发明授权
    Potassium channel opener 失效
    钾通道开启剂

    公开(公告)号:US07495127B2

    公开(公告)日:2009-02-24

    申请号:US11353189

    申请日:2006-02-14

    IPC分类号: C07C62/02 C07C62/04 C07C62/06

    CPC分类号: A61K31/19

    摘要: A potassium channel opener including a compound (e.g., pimaric acid) represented by the formula [I]: wherein R1, R2, R3, R4, R5, R6 and R7 are each independently hydrogen, alkyl, alkenyl, halogen, hydroxy, halogenated alkyl, hydroxyalkyl, aminoalkyl, alkoxy, aryl, heteroaryl, acyl, carboxyl, alkoxycarbonyl, hydroxamate, sulfo, carbamoyl, sulfonamide, aldehyde, or nitrile; or R4 and R5 may be bonded to each other to form a ring; or R6 and R7 may be bonded to each other to form a ring; and all of three bonds represented by are single bonds, or one of the three bonds is double bond and the other bonds are single bonds, or a physiologically acceptable salt thereof as an effective ingredient.

    摘要翻译: 钾通道开放剂,其包含由式[I]表示的化合物(例如,海松酸):其中R1,R2,R3,R4,R5,R6和R7各自独立地为氢,烷基,烯基,卤素,羟基,卤代烷基 ,羟基烷基,氨基烷基,烷氧基,芳基,杂芳基,酰基,羧基,烷氧基羰基,异羟肟酸酯,磺基,氨基甲酰基,磺酰胺,醛或腈; 或者R 4和R 5可以彼此键合形成环; 或者R 6和R 7可以彼此键合形成环; 并且由是单键,或三键之一是双键,另一个键是单键,或其生理学上可接受的盐作为有效成分。

    Production of para-cresol
    10.
    发明授权
    Production of para-cresol 失效
    对甲酚的生产

    公开(公告)号:US4532209A

    公开(公告)日:1985-07-30

    申请号:US415129

    申请日:1982-09-07

    申请人: Scott Hagedorn

    发明人: Scott Hagedorn

    摘要: The present invention provides a process for the production of p-cresol in a quantitative yield, which involves the acidification of an aqueous solution of 4-methylcyclohexa-3,5-diene-1,2-diol-1-carboxylic acid under ambient conditions of temperature and pressure to cause spontaneous decomposition of the starting material to p-cresol. The 4-methylcyclohexa-3,5-diene-1,2-diol-1-carboxylic acid is produced by the conversion of p-xylene with the microorganism, Pseudomonas putida Biotype A strain ATCC No. 39119.

    摘要翻译: 本发明提供了一种以定量产率生产对甲酚的方法,其包括在环境条件下酸化4-甲基环己-3,5-二烯-1,2-二醇-1-羧酸的水溶液 的温度和压力使原料自发分解成对甲酚。 4-甲基环己-3,5-二烯-1,2-二醇-1-羧酸是通过与微生物恶臭假单胞菌生物型A株ATCC No. 39119的对二甲苯的转化来制备的。