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    Reagent for froth flotation of bituminous coal
    21.
    发明授权
    Reagent for froth flotation of bituminous coal 失效
    烟煤泡沫浮选试剂

    公开(公告)号：US4372864A

    公开(公告)日：1983-02-08

    申请号：US860899

    申请日：1977-12-15

    申请人： James R. McCarthy

    发明人： James R. McCarthy

    IPC分类号： B03B9/00 ,  B03D1/002 ,  B03D1/012 ,  B03D1/02 ,  B03D1/00

    CPC分类号： B03D1/02 ,  B03B9/005 ,  B03D1/002 ,  B03D1/006 ,  B03D1/018 ,  B03D2203/08

    摘要： A reagent and a method for using the reagent for treating a solid material disposed in a liquid medium and having an oxygen-controlled surface condition. The reagent includes a liquid hydrocarbon, a reducing material and an activator material. The liquid hydrocarbon such as mineral oil has a specific gravity different from the specific gravity of the liquid medium. The reducing material such as phosphorous pentasulfide is present in an amount sufficient to establish a reducing environment around the solid material for breaking the oxygen control on the surface of the solid material. The activator material such as zinc thiophosphate is present in an amount sufficient to establish an electrostatic charge on the solid material after the oxygen-controlled surface condition has been broken. A more specific feature of the invention is directed to the method of flotation of extremely fine bituminous coal having an oxygen-controlled surface condition. The reagent is used in the conventional froth flotation equipment of the prior art.

    摘要翻译： 一种试剂和使用该试剂处理设置在液体介质中并具有氧控制表面状态的固体材料的方法。 试剂包括液体烃，还原材料和活化剂材料。 液体烃如矿物油的比重与液体介质的比重不同。 诸如五硫化二磷的还原材料以足以在固体材料周围建立还原环境的量存在，以破坏固体材料表面上的氧气控制。 催化剂材料如硫代磷酸锌存在的量足以在氧气受控表面状态被破坏之后在固体材料上形成静电电荷。 本发明的更具体的特征涉及具有氧控制表面状态的极细煤烟的浮选方法。 该试剂用于现有技术的常规泡沫浮选设备中。

    Pyrazolopyrimidines as CRF receptor antagonists
    22.
    发明授权
    Pyrazolopyrimidines as CRF receptor antagonists 有权
    吡唑并嘧啶作为CRF受体拮抗剂

    公开(公告)号：US06664261B2

    公开(公告)日：2003-12-16

    申请号：US09117717

    申请日：1999-03-02

    申请人： Chen Chen ,  Thomas R. Webb ,  James R. McCarthy ,  Terence J. Moran ,  Keith M. Wilcoxen ,  Charles Huang

    发明人： Chen Chen ,  Thomas R. Webb ,  James R. McCarthy ,  Terence J. Moran ,  Keith M. Wilcoxen ,  Charles Huang

    IPC分类号： A61K31505

    CPC分类号： C07D487/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula —Alk—O—CO—Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

    摘要翻译： 本发明涉及包括其立​​体异构体及其药学上可接受的酸加成盐形式的化合物，其中R 1为NR 4 R 5或OR 5。 R 2是C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基; R 3是氢，C 1-6烷基，C 1-6烷基磺酰基，C 1-6烷基磺酰基或C 1-6烷硫基; R 4是氢，C 1-6烷基，一或二（C 3-6环烷基）甲基，C 3-6环烷基，C 3-6烯基，羟基C 1-6烷基，C 1-6烷基羰氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 5为C 1-6烷基，单或二（C 3-6环烷基）甲基，Ar 1 CH 2，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基， 吗啉基，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar 1的基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

    Amino substituted pyrimidines and triazines
    23.
    发明授权
    Amino substituted pyrimidines and triazines 失效
    氨基取代的嘧啶和三嗪

    公开(公告)号：US06288060B1

    公开(公告)日：2001-09-11

    申请号：US09051672

    申请日：1998-04-15

    申请人： Thomas R. Webb ,  Terence J. Moran ,  James R. McCarthy

    发明人： Thomas R. Webb ,  Terence J. Moran ,  James R. McCarthy

    IPC分类号： A61K31505

    CPC分类号： C07D239/42 ,  C07D239/49 ,  C07D251/14

    摘要： Pyrimidines and triazines of formula (I) wherein R is C1-6alkyl, amino, mono- or diC1-6alkylamino; R1 is hydrogen, C1-6alkyl, C3-6alkenyl, hydroxyC1-6alkyl or C1-6alkyloxy-C1-6alkyl; R2 is C1-6alkyl, mono- or diC3-6cycloalkylmethyl, phenylmethyl, substituted phenylmethyl, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C3-6alkenyl; or R1 and R2 taken together with the nitrogen to which they are attached may form a pyrrolidinyl, morpholinyl or piperidinyl group; X is N or CR3; R3 is hydrogen or C1-6alkyl; R4 is phenyl or substituted phenyl; A is  or —CR7R8— wherein R5 and R6 each independently are hydrogen or C1-4alkyl; R7 is hydrogen or OH, R8 is hydrogen or C1-6alkyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing these compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

    摘要翻译： 式（I）的嘧啶和三嗪，其中R是C 1-6烷基，氨基，单或二C 1-6烷基氨基; R 1是氢，C 1-6烷基，C 3-6烯基，羟基C 1-6烷基或C 1-6烷氧基-C 1-6烷基; R 2是C 1-6烷基，单或二C 3-6环烷基甲基，苯甲基，取代的苯基甲基，C 1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基羰基C 1-6烷基，C 3-6烯基; 或者R 1和R 2与它们所连接的氮一起形成吡咯烷基，吗啉基或哌啶基; X为N或CR 3; R3是氢或C1-6烷基; R4是苯基或取代的苯基; A是或-CR 7 R 8 - 其中R 5和R 6各自独立地为氢或C 1-4烷基; R7是氢或OH，R8是氢或C1-6烷基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

    Thiophenopyrimidines
    24.
    发明授权
    Thiophenopyrimidines 失效
    噻吩并嘧啶

    公开(公告)号：US06255310B1

    公开(公告)日：2001-07-03

    申请号：US09117715

    申请日：1998-12-28

    申请人： Thomas R. Webb ,  Chen Chen ,  James R. McCarthy ,  Terence J. Moran

    发明人： Thomas R. Webb ,  Chen Chen ,  James R. McCarthy ,  Terence J. Moran

    IPC分类号： A61K31519

    CPC分类号： C07D495/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula —Alk—O—CO—Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

    摘要翻译： 本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物，其中X是S，SO或SO 2; R1是NR4R5或OR5; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基亚磺酰基或C1-6烷硫基; R4是氢，C1-6烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 5是C 1-8烷基，一或二（C 3-6环烷基）甲基，Ar 1 CH 2，C 1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，吗啉基，单或 二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar1基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar是苯基，取代的苯基，吡啶基或取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

    CRF antagonistic thiophenopyridines
    25.
    发明授权
    CRF antagonistic thiophenopyridines 失效
    CRF拮抗性噻吩并吡啶类

    公开(公告)号：US06211195B1

    公开(公告)日：2001-04-03

    申请号：US09403400

    申请日：1999-10-19

    申请人： Thomas R. Webb ,  James R. McCarthy

    发明人： Thomas R. Webb ,  James R. McCarthy

    IPC分类号： A01N4342

    CPC分类号： C07D495/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S or SO2; R1 is C1-6alkyl, NR5R6, OR6 or SR6; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R5 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C1-6alkyl or C1-6alkyloxyC1-6alkyl; and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

    摘要翻译： 本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的组合物，其中X是S或SO 2; R1是C1-6烷基，NR5R6，OR6或SR6; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R4是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基磺酰基或C1-6烷硫基; R5是氢，C1-8烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基，一或二（C 3-6环烷基）甲基，Ar 2 CH 2，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，单或二 C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基; 或者R 5和R 6与它们所连接的氮原子一起形成吡咯烷基，哌啶基，高哌啶基或吗啉基，任选被C 1-6烷基或C 1-6烷氧基C 1-6烷基取代; Ar 1和Ar 2各自为任意取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。