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    Process for making dihydropyrimidinones
    1.
    发明授权
    Process for making dihydropyrimidinones 失效
    制备二氢嘧啶酮的方法

    公开(公告)号：US5786472A

    公开(公告)日：1998-07-28

    申请号：US766400

    申请日：1996-12-12

    申请人： Essa Hsinyi Hu ,  Daniel R. Sidler ,  Ulf H. Dolling ,  Michael A. Patane

    发明人： Essa Hsinyi Hu ,  Daniel R. Sidler ,  Ulf H. Dolling ,  Michael A. Patane

    IPC分类号： C07D239/22 ,  C07D239/36

    CPC分类号： C07D239/22

    摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu.sub.2 O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.

    摘要翻译： 本发明提供了通过将β-酮酯或二酮组合形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法， 醛和尿素在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）​​的存在下进行。 反应通常在溶剂中在一锅中进行，以更高的产率提供二氢嘧啶酮，并且比以前已知的方法更容易处理。

    Alpha 1a adrenergic receptor antagonists
    5.
    发明授权
    Alpha 1a adrenergic receptor antagonists 失效

    公开(公告)号：US6143750A

    公开(公告)日：2000-11-07

    申请号：US98780

    申请日：1998-06-17

    申请人： Michael A. Patane ,  Mark G. Bock

    发明人： Michael A. Patane ,  Mark G. Bock

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  A61K31/505 ,  A01N43/54 ,  C07D239/02 ,  C07D403/00 ,  C07D491/00

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14

    摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

    Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
    7.
    发明授权
    Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists 失效
    可用作α1a肾上腺素受体拮抗剂的多氮杂萘酮衍生物

    公开(公告)号：US06358959B1

    公开(公告)日：2002-03-19

    申请号：US09481991

    申请日：2000-01-11

    申请人： Mark G. Bock ,  Michael A. Patane ,  Thomas G. Steele

    发明人： Mark G. Bock ,  Michael A. Patane ,  Thomas G. Steele

    IPC分类号： C07D23980

    CPC分类号： C07D401/12 ,  C07D239/82 ,  C07D401/14 ,  C07D403/12

    摘要： Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

    摘要翻译： 公开了二氢 - 聚氮杂萘-2-酮化合物（例如二氢喹唑啉-2-酮和二氢蝶啶-2-酮衍生物）及其药学上可接受的盐。 还描述了这些化合物的合成及其作为α1a肾上腺素能受体拮抗剂的用途。 这些化合物的一个应用是治疗良性前列腺增生。 这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。 发现一个这样的组织围绕尿道衬里。 因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。 通过与人类5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

    Oxazolidinones useful as alpha 1a adrenoceptor antagonists
    8.
    发明授权
    Oxazolidinones useful as alpha 1a adrenoceptor antagonists 失效
    可用作α1a肾上腺素受体拮抗剂的恶唑烷酮

    公开(公告)号：US06228870B1

    公开(公告)日：2001-05-08

    申请号：US09437841

    申请日：1999-11-10

    申请人： Jennie B. Nerenberg ,  Mark G. Bock ,  Michael A. Patane ,  Harold G. Selnick

    发明人： Jennie B. Nerenberg ,  Mark G. Bock ,  Michael A. Patane ,  Harold G. Selnick

    IPC分类号： A61K31445

    CPC分类号： C07D413/12

    摘要： Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

    摘要翻译： 公开了新的羟甲基 - 和烷氧基甲基 - 恶唑烷酮化合物及其药学上可接受的盐。 还描述了这些化合物的合成及其作为α1a肾上腺素能受体拮抗剂的用途。 这些化合物的一个应用是治疗良性前列腺增生。 这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。 发现一个这样的组织围绕尿道衬里。 因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。 通过与人类5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

    Bis-piperidinyl-pyrimidin-2-ones as alpha 1a adrenergic receptor antagonists
    10.
    发明授权
    Bis-piperidinyl-pyrimidin-2-ones as alpha 1a adrenergic receptor antagonists 失效

    公开(公告)号：US06214832B1

    公开(公告)日：2001-04-10

    申请号：US09099660

    申请日：1998-06-17

    申请人： Michael A. Patane ,  Mark G. Bock

    发明人： Michael A. Patane ,  Mark G. Bock

    IPC分类号： C01D46114

    CPC分类号： C07D401/14 ,  C07D413/14

    摘要： Pyrimidinone, oxazolidinone, and (alkyl)aryl derivatives, their synthesis, and their use as alpha 1a adrenergic receptor antagonists are disclosed. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved. Among the disclosed derivatives are piperidinyl aminoalkylpiperidinyl pyrimidinones, including those of formula: R1 is selected from unsubstituted, mono- or poly-substituted phenyl wherein the substituents on the phenyl are independently selected from halogen, CF3, cyano, nitro, N(R7)2, NR7COR19, NR7CON(R19)2, NR7SO2R19, NR7SO2N(R19)2, OR6, (CH2)0-4CO2R7, (CH2)0-4CON(R7)2, or C1-4 alkyl; or unsubstituted, mono- or poly-substituted pyridyl, pyrazinyl, thienyl, thiazolyl, furanyl, quinazolinyl or naphthyl wherein the substituents on the pyridyl, pyrazinyl, thienyl, thiazolyl, furanyl, quinazolinyl or naphthyl are independently selected from CF3, cyano, nitro, amino, (CH2)0-4CO2R7, (CH2)0-4CON(R7)2, (CH2)0-4SO2N(R7)2, (CH2)0-4SO2R6, phenyl, OR6, halogen, C1-4 alkyl or C3-8 cycloalkyl; m and p are each integers from zero to two, wherein the sum m+p=2; n and o are each integers from zero to two, wherein the sum n+o=2; q is an integer of from zero to three, provided that when q is zero, R26 is hydrogen; s is an integer of from zero to four; and E, G, J, L, M, W, X, R2, R3, R4, R5, R6, R7, R8, R11, R12, R13, R14, R15, R16, R19 and R26 are defined herein.