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    Pyrazolopyrimidine compounds and their use as PDE10 inhibitors
    1.
    发明授权
    Pyrazolopyrimidine compounds and their use as PDE10 inhibitors 有权
    吡唑并嘧啶化合物及其作为PDE10抑制剂的用途

    公开(公告)号：US08969376B2

    公开(公告)日：2015-03-03

    申请号：US13579095

    申请日：2011-02-25

    Applicant: Eiji Kawanishi ,  Mitsuya Hongu ,  Yoshihito Tanaka

    Inventor： Eiji Kawanishi ,  Mitsuya Hongu ,  Yoshihito Tanaka

    IPC: A61K31/415 ,  C07D293/00 ,  C07D487/00 ,  C07D487/04

    CPC classification number: C07D487/04

    Abstract: The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.

    Abstract translation: 本发明涉及由式[I]表示的化合物：其中：R 1是氢，卤素，低级烷基或氰基; 环A是任选取代的杂环基; 环B是任选取代的3至6元单环基团; 并且Y是任选取代的氨基，任选取代的环状氨基，任选取代的脂族3至6元单环氧基，任选取代的低级烷基或任选取代的低级烷基-O-或其药学上可接受的盐，以及它们作为PDE10抑制剂的用途。

    Kinase inhibitors
    3.
    发明授权
    Kinase inhibitors 有权
    激酶抑制剂

    公开(公告)号：US07901894B2

    公开(公告)日：2011-03-08

    申请号：US11261858

    申请日：2005-10-27

    Applicant: David G. Hangauer ,  Karen L. Milkiewicz

    Inventor： David G. Hangauer ,  Karen L. Milkiewicz

    IPC: G01N33/53 ,  C12Q1/48 ,  C12P7/38 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07D293/00 ,  C07D421/00

    CPC classification number: C12Q1/485 ,  G01N2500/04

    Abstract: The present invention provides a method for identifying inhibitors of protein kinases. Methods are also provided for inhibiting protein kinase activity. Specific non-peptide protein tyrosine kinase inhibitors are provided. The protein kinases produced using the method of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, atherosclerosis, or immune system activity.

    Abstract translation: 本发明提供了鉴定蛋白激酶抑制剂的方法。 还提供了用于抑制蛋白激酶活性的方法。 提供了特异性的非肽蛋白酪氨酸激酶抑制剂。 使用本发明的方法产生的蛋白激酶可用于治疗患者的许多病症，包括癌症，牛皮癣，动脉粥样硬化或免疫系统活性。

    Substrates for thioredoxin reductase
    4.
    发明授权
    Substrates for thioredoxin reductase 有权
    硫氧还蛋白还原酶底物

    公开(公告)号：US07671211B1

    公开(公告)日：2010-03-02

    申请号：US09926218

    申请日：2000-03-31

    Applicant: Arne Holmgren ,  Marjan H. Amiri ,  Hiroyuki Masayasu

    Inventor： Arne Holmgren ,  Marjan H. Amiri ,  Hiroyuki Masayasu

    IPC: C07D293/00

    CPC classification number: C07D293/04 ,  A61K31/166 ,  A61K31/167 ,  C07C391/02 ,  C12N9/0036 ,  C12P9/00

    Abstract: A substrate for thioredoxin reductase which comprises a compound represented by the following general formula (I) or (I′): wherein R1 and R2 independently represent a hydrogen atom, a halogen atom, a trifluoromethyl group and the like; R3 represents an aryl group, an aromatic heterocyclic group and the like; R4 represents a hydrogen atom, a hydroxyl group, a —S-α-amino acid group and the like; R5 represents a hydrogen atom or a C1-C6 alkyl group; Y represents oxygen atom or sulfur atom; n represents an integer of from 0 to 5; and the selenium atom may be oxidized, whose example includes 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a ring-opened form thereof. The substrate is reduced by thioredoxin reductase in the presence of NADPH and enhances peroxidase activity of thioredoxin reductase.

    Abstract translation: 用于硫氧还蛋白还原酶的底物，其包含由以下通式（I）或（I'）表示的化合物：其中R 1和R 2独立地表示氢原子，卤素原子，三氟甲基等; R3表示芳基，芳香族杂环基等; R4表示氢原子，羟基，-S-α-氨基酸基等; R5表示氢原子或C1-C6烷基; Y表示氧原子或硫原子; n表示0〜5的整数， 并且硒原子可被氧化，其实例包括2-苯基-1,2-苯并异硒唑-3（2H） - 酮或其开环形式。 在NADPH存在下，底物被硫氧还蛋白还原酶还原，提高硫氧还蛋白还原酶的过氧化物酶活性。

    Imidazoline corrosion inhibitors
    6.
    发明申请
    Imidazoline corrosion inhibitors 有权
    咪唑啉缓蚀剂

    公开(公告)号：US20040200996A1

    公开(公告)日：2004-10-14

    申请号：US10411748

    申请日：2003-04-11

    Inventor： George Richard Meyer

    IPC: C23F011/14 ,  C07D293/00 ,  C09K003/00

    CPC classification number: C23F11/149 ,  C07D233/06

    Abstract: This invention provides a series of novel acrylated, substituted imidazoline corrosion inhibitors of the formula: 1 wherein R1 is an alkyl radical having from 2 to 8 carbon atoms; R2 is a radical derived from a fatty acid; and R3 is a radical derived from an unsaturated acid and a method for inhibiting corrosion in metallic flow lines through the introduction of such inhibitors into a system wherein corrosion is sought to be precluded.

    Abstract translation: 本发明提供一系列新颖的丙烯酸酯化的下式的咪唑啉缓蚀剂：其中R1是具有2-8个碳原子的烷基; R2是衍生自脂肪酸的基团; 并且R3是衍生自不饱和酸的基团和通过将这种抑制剂引入到其中寻求排除腐蚀的体系中来抑制金属流动管线中的腐蚀的方法。

    Thioimidazolidine derivatives as light stabilizers for polymers
    7.
    发明申请
    Thioimidazolidine derivatives as light stabilizers for polymers 失效
    硫代咪唑烷衍生物作为聚合物的光稳定剂

    公开(公告)号：US20030109609A1

    公开(公告)日：2003-06-12

    申请号：US10182074

    申请日：2002-07-23

    Inventor： Dario Lazzari ,  Graziano Zagnoni

    IPC: C07D293/00 ,  C08K005/34

    CPC classification number: C07D405/14 ,  C07D233/42 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C08K5/378 ,  G03C1/346

    Abstract: A compound of the formula (I) wherein G1, G2, G3 and G4 are independently of one another C1-C18alkyl or C5-C12cycloalkyl or the radicals G1 and G2 and the radicals G3 and G4 form independently of one another, together with the carbon atom they are attached to, C5-C12cycloalkyl; R is hydrogen, C1-C18alkyl, oxyl, nullOH, nullCH2CN, C3-C6alkenyl, C3-C8alkynyl, C7-C12phenylalkyl unsubstituted or substituted on the phenyl radical by C1-C4alkyl and/or C1-C4alkoxy; C1-C8acyl, C1-C18alkoxy, C1-C18hydroxyalkoxy, C2-C18alkenyloxy, C5-C12cycloalkoxy, C7-C12phenylalkoxy unsubstituted or substituted on the phenyl radical by C1-C4alkyl and/or C1-C4alkoxy: C1-C18alkanoyloxy, (C1-C18alkoxy)carbonyl, glycidyl or a group nullCH2CH(OH)(G) with G being hydrogen, methyl or phenyl; n is 1, 2, 3 or 4; and X is an organic radical of a valency equal to n; and when n is 2, 3 or 4, each of the radicals G1, G2, G3, G4 and R can have the same or a different meaning in the units of the formula (II), is useful for stabilizing an organic material against degradation induced by light, heat or oxidation.

    Abstract translation: 式（I）的化合物，其中G1，G2，G3和G4彼此独立地为C1-C18烷基或C5-C12环烷基，或者基团G1和G2以及基团G3和G4彼此独立地形成，与碳 它们连接的原子，C 5 -C 12环烷基; R是氢，C1-C18烷基，氧基，-OH，-CH2CN，C3-C6链烯基，C3-C8炔基，未被取代或被C1-C4烷基和/或C1-C4烷氧基取代在苯基上的C7-C12苯基; C 1 -C 8烷基和C 1 -C 4烷氧基，C 1 -C 18烷氧基，C 1 -C 18烷氧基，C 1 -C 18烷氧基，C 1 -C 18烷氧基，C 5 -C 12环烷氧基，未被取代或被C 1 -C 4烷基和/ 羰基，缩水甘油基或基团-CH 2 CH（OH）（G），其中G为氢，甲基或苯基; n为1,2,3或4; 并且X是化合价等于n的有机基团; 当n为2,3或4时，基团G1，G2，G3，G4和R中的每一个在式（II）的单元中可以具有相同或不同的含义，可用于稳定有机材料以防止降解 由光，热或氧化引起的。

    Imidazolium cations, processes for their preparation, and uses therefor
    9.
    发明授权
    Imidazolium cations, processes for their preparation, and uses therefor 失效
    咪唑鎓阳离子，其制备方法及其用途

    公开(公告)号：US5874587A

    公开(公告)日：1999-02-23

    申请号：US673687

    申请日：1996-06-25

    Applicant: Robert J. Donovan ,  Robert J. Morgan

    Inventor： Robert J. Donovan ,  Robert J. Morgan

    IPC: C07D233/54 ,  C07D233/61 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D491/04 ,  C07D519/00 ,  C07D233/00 ,  C07D293/00 ,  C07D345/00

    CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/04

    Abstract: Novel imidazolium compounds of the formula ##STR1## wherein A represents the atomic group necessary to form a heteroaromatic ring, which may be optionally substituted by one or more R substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; B is an optional substituent which represents the atomic group necessary to form a heteroaromatic ring or a double or triple carbon-nitrogen bond, which may optionally be substituted by one or more R' substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; C is an optional substituent which represents the atomic group necessary to form an aromatic or heteroaromatic ring, which may optionally be substituted by one or more R"" substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substituents; R" and R'" are each independently a lower alkyl or aryl group, or together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 5 to 7 members, which may optionally contain a sulfur, oxygen, silicon, selenium or an additional nitrogen atom; and X is an anion; are useful in a variety of industrial and medical applications.

    Abstract translation: 式（I）的新型咪唑鎓化合物其中A表示形成杂芳环所必需的原子团，其可以任选地被一个或多个选自以下的R取代基取代：芳基，杂芳基，低级烷基，羟基 ，卤化物或羧基取代基; B是可选择的取代基，其表示形成杂芳环或双或三碳 - 氮键所必需的原子团，其可以任选地被一个或多个R'取代基取代，所述取代基选自芳基，杂芳基，低级烷基 ，羟基，卤化物或羧基取代基; C是可选的取代基，其表示形成芳族或杂芳族环所必需的原子团，其可任选被一个或多个选自芳基，杂芳基，低级烷基，羟基，卤化物的R“'取代基取代 ，或羧基取代基; R“和R”“各自独立地为低级烷基或芳基，或与它们所连接的氮原子一起形成具有5至7个成员的杂环，其可任选地含有硫，氧， 硅，硒或另外的氮原子; X为阴离子; 可用于各种工业和医疗应用。

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