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    Chimeric amino acid analogues
    14.
    发明授权
    Chimeric amino acid analogues 失效
    CHIMERIC氨基酸类似物

    公开(公告)号：US5120859A

    公开(公告)日：1992-06-09

    申请号：US411088

    申请日：1989-09-22

    Applicant: Thomas R. Webb

    Inventor： Thomas R. Webb

    IPC: A61K38/00 ,  A61P7/02 ,  C07D207/16 ,  C07K5/117 ,  C07K7/06

    CPC classification number: C07K7/06 ,  C07D207/16 ,  C07K5/1024 ,  A61K38/00

    Abstract: A chimeric amino acid analogue is provided suitable for incorporating into peptides which compound is represented by Formula 1: ##STR1## where P.sub.1 is preferably an amine protecting agent, and P.sub.2 and P.sub.3 are preferably amine or guanidine protecting agents. X can be OH, halide, or preferably an activating group suitable for conjugating the compound of Formula 1 to a peptide by conventional means, and m and n are 0-1 and 0-2 respectively.Peptides containing the chimeric amino acid analog are provided and include a platelet-aggregation inhibitor represented byAaa.sub.1 -CPdl-Gly-Asp-Aaa.sub.2where Aaa.sub.1 is Gly or H, Cpdl is the compound of Formula 1 which has been deprotected and Aaa.sub.2 is a hydrophobic amino acid preferably Val.

    Abstract translation: 提供了一种嵌合氨基酸类似物，其适于掺入到化合物由式1表示的肽中：其中P1优选为胺保护剂，P2和P3优选为胺或胍保护剂。 X可以是OH，卤化物，或优选是适合于通过常规方法将式1化合物与肽缀合的活化基团，m和n分别为0-1和0-2。 提供含有嵌合氨基酸类似物的肽，包括由Aaa1-CPd1-Gly-Asp-Aaa2表示的血小板聚集抑制剂，其中Aaa1为Gly或H，Cpd1为脱保护的式1化合物，Aaa2为疏水基 氨基酸优选为Val。

    Support for solid-phase oligonucleotide synthesis
    15.
    发明授权
    Support for solid-phase oligonucleotide synthesis 失效

    公开(公告)号：US4659774A

    公开(公告)日：1987-04-21

    申请号：US794016

    申请日：1985-11-01

    Applicant: Thomas R. Webb ,  Chien-Pin S. Hsu

    Inventor： Thomas R. Webb ,  Chien-Pin S. Hsu

    IPC: C07H21/00 ,  C08F8/32 ,  C07H21/02

    CPC classification number: C07H21/00 ,  C08F8/32

    Abstract: This invention relates to a support for oligonucleotide synthesis and more particularly to a necleoside-linker/polymer support composite having the general formulaP'--S'wherein P' is a polymer support which bears oxirane, aziridine or episulfide groups or which contains good leaving groups for nucleophilic displacement; and S' is a nucleoside-linker having the general formulaW--(CH.sub.2).sub.a --X--(CH.sub.2).sub.b --Y--(CH.sub.2).sub.c --Zwherein W and Z each independently comprise a nucleophile; X and Y which, independently may or may not be present, comprise groups of high hydrophilicity; and a, b, c are integers from 0 to 9, wherein a plus b plus c exceeds 6.

    Pyrazolopyrimidines as CRF receptor antagonists
    17.
    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

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

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

    IPC: A61K31505

    CPC classification number: C07D487/04

    Abstract: 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).

    Abstract translation: 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
    18.
    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

    Applicant: Thomas R. Webb ,  Terence J. Moran ,  James R. McCarthy

    Inventor： Thomas R. Webb ,  Terence J. Moran ,  James R. McCarthy

    IPC: A61K31505

    CPC classification number: C07D239/42 ,  C07D239/49 ,  C07D251/14

    Abstract: 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).

    Abstract translation: 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
    19.
    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

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

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

    IPC: A61K31519

    CPC classification number: C07D495/04

    Abstract: 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).

    Abstract translation: 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
    20.
    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

    Applicant: Thomas R. Webb ,  James R. McCarthy

    Inventor： Thomas R. Webb ,  James R. McCarthy

    IPC: A01N4342

    CPC classification number: C07D495/04

    Abstract: 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).

    Abstract translation: 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。

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