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    • 1. 发明授权
    • Thiophenopyrimidines
    • 噻吩并嘧啶
    • US06469166B2
    • 2002-10-22
    • US09896250
    • 2001-06-29
    • Thomas R. WebbChen ChenJames R. McCarthyTerence J. Moran
    • Thomas R. WebbChen ChenJames R. McCarthyTerence J. Moran
    • C07D49504
    • C07D495/04
    • 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 C1-6alkyl, 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).
    • 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; R5是C1-6烷基,单或二(C3-6环烷基)甲基,Ar1CH2,C1-6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。
    • 2. 发明授权
    • Pyrazolopyrimidines as CRF receptor antagonists
    • 吡唑并嘧啶作为CRF受体拮抗剂
    • US06664261B2
    • 2003-12-16
    • US09117717
    • 1999-03-02
    • Chen ChenThomas R. WebbJames R. McCarthyTerence J. MoranKeith M. WilcoxenCharles Huang
    • Chen ChenThomas R. WebbJames R. McCarthyTerence J. MoranKeith M. WilcoxenCharles Huang
    • A61K31505
    • C07D487/04
    • 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).
    • 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。
    • 3. 发明授权
    • Thiophenopyrimidines
    • 噻吩并嘧啶
    • US06255310B1
    • 2001-07-03
    • US09117715
    • 1998-12-28
    • Thomas R. WebbChen ChenJames R. McCarthyTerence J. Moran
    • Thomas R. WebbChen ChenJames R. McCarthyTerence J. Moran
    • A61K31519
    • C07D495/04
    • 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).
    • 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。
    • 4. 发明授权
    • Amino substituted pyrimidines and triazines
    • 氨基取代的嘧啶和三嗪
    • US06288060B1
    • 2001-09-11
    • US09051672
    • 1998-04-15
    • Thomas R. WebbTerence J. MoranJames R. McCarthy
    • Thomas R. WebbTerence J. MoranJames R. McCarthy
    • A61K31505
    • C07D239/42C07D239/49C07D251/14
    • 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).
    • 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。
    • 6. 发明授权
    • CRF antagonistic thiophenopyridines
    • CRF拮抗性噻吩并吡啶类
    • US06211195B1
    • 2001-04-03
    • US09403400
    • 1999-10-19
    • Thomas R. WebbJames R. McCarthy
    • Thomas R. WebbJames R. McCarthy
    • A01N4342
    • C07D495/04
    • 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).
    • 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。