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1. 发明授权

US5747490A Alpha 1b adrenergic receptor antagonists 失效
标题翻译： α1b肾上腺素能受体拮抗剂
公开(公告)号：US5747490A
公开(公告)日：1998-05-05
申请号：US716041
申请日：1996-09-19
申请人： Mark G. Bock , Michael A. Patane , William C. Lumma
发明人： Mark G. Bock , Michael A. Patane , William C. Lumma
IPC分类号： C07D403/04 , C07D405/14 , A61K31/535 , A01N43/60 , C07D239/72 , C07D415/00
CPC分类号： C07D403/04 , C07D405/14
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display submicromolar affinity for the human alpha 1b adrenergic receptor subtype while displaying at least five-fold lower affinity for the human alpha 1d and alpha 1a adrenergic receptor subtypes, and many other G-protein coupled human receptors. One application of these compounds is in the treatment of hypertension. More specifically, these compounds display selectivity for lowering blood pressure without, for example, substantially affecting urethral pressure.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α1b肾上腺素能受体拮抗剂的用途。这些化合物对人α1b肾上腺素能受体亚型显示亚微摩尔亲和力，同时对人α1d和α1a肾上腺素能受体亚型和许多其它G蛋白偶联的人受体显示出至少五倍的亲和力。这些化合物的一种应用是治疗高血压。更具体地，这些化合物显示出降低血压的选择性，而不会例如显着影响尿道压力。

2. 发明授权

US6143750A 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.

3. 发明授权

US5977115A Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US5977115A
公开(公告)日：1999-11-02
申请号：US973624
申请日：1997-12-04
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello , Randall C. Newton
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello , Randall C. Newton
IPC分类号： A61K31/445 , A61P13/02 , A61P15/00 , C07D211/64 , C07D295/155 , A61K31/495 , C07D295/12
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective 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 orthostatic 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.
摘要翻译： PCT No.PCT / US96 / 09425 Sec。 371 1997年12月4日第 102（e）1997年12月4日PCT PCT 1996年6月6日PCT公布。出版物WO96 / 40136 日期：1996年12月19日本发明涉及某些新型化合物及其衍生物，其合成及其作为选择性α-1a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。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。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。

4. 发明授权

US5661163A Alpha-1a adrenergic receptor antagonists 失效
标题翻译： α-1a肾上腺素受体拮抗剂
公开(公告)号：US5661163A
公开(公告)日：1997-08-26
申请号：US488272
申请日：1995-06-07
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello
IPC分类号： A61K31/445 , A61P13/02 , A61P15/00 , C07D211/64 , C07D295/155 , C07D211/36
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective 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 orthostatic 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.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α-1a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。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。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。

5. 发明授权

US06358959B1 Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists 失效
标题翻译：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。

6. 发明授权

US06228870B1 Oxazolidinones useful as alpha 1a adrenoceptor antagonists 失效
标题翻译：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。

7. 发明授权

US06214832B1 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.

8. 发明授权

US5922722A Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US5922722A
公开(公告)日：1999-07-13
申请号：US66477
申请日：1998-04-22
申请人： Mark G. Bock , Michael A. Patane , Rose Ann Ponticello
发明人： Mark G. Bock , Michael A. Patane , Rose Ann Ponticello
IPC分类号： A61K31/451 , A61K31/495 , A61K31/58 , A61K31/445
CPC分类号： A61K31/495 , A61K31/451 , A61K31/58
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These componds 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.
摘要翻译： PCT No.PCT / US96 / 18321 Sec。 371日期：1998年4月22日 102（e）1998年4月22日PCT PCT 1996年11月12日PCT公布。 WO97 / 17967 PCT公开号日期1997年5月22日本发明涉及某些新型化合物及其衍生物，其合成及其作为选择性α1α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。

9. 发明授权

US5620993A Alpha-1a adrenergic receptor antagonists 失效
标题翻译： α-1a肾上腺素受体拮抗剂
公开(公告)号：US5620993A
公开(公告)日：1997-04-15
申请号：US488267
申请日：1995-06-07
申请人： Michael A. Patane , Mark G. Bock , Roger M. Friedinger
发明人： Michael A. Patane , Mark G. Bock , Roger M. Friedinger
IPC分类号： A61K31/445 , A61K31/58 , A61P11/00 , C07D211/60 , C07D417/06 , C07D211/42
CPC分类号： C07D417/06 , A61K31/58 , C07D211/60
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective 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 orthostatic hypotension. One such tissue is found surrounding the urethral fining. 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.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α-1a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。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道澄清。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。

10. 发明授权

US06436962B1 Arylhydantoin derivatives and uses thereof 失效
标题翻译：芳基乙内酰脲衍生物及其用途
公开(公告)号：US06436962B1
公开(公告)日：2002-08-20
申请号：US09671518
申请日：2000-09-27
申请人： Jacob M. Hoffman , Mark G. Bock , Robert M. DiPardo , Linda S. Payne , Michael A. Patane
发明人： Jacob M. Hoffman , Mark G. Bock , Robert M. DiPardo , Linda S. Payne , Michael A. Patane
IPC分类号： A61K31445
CPC分类号： C07D401/06 , A61K45/06 , C07D233/76 , C07D401/14 , C07D471/10
摘要： Arylhydantoin derivatives and their pharmaceutically acceptable salts 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 typically 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：公开了乙内酰脲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。这些化合物通常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。

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