CAS: 25115-74-6; 4-Oxo-1-Phenylcyclohexanecarbonitrile

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Methyl 5-Cyano-5-(4-Chlorophenyl)-2-Oxocyclohexanecarboxylate置于硫酸体系中,用 正己烷,5-氰基-2-氧代-5-苯基环己烷羧酸甲酯,溶剂黄146,乙酸乙酯 用作溶剂,以75%的收率获得4-氰-4-苯基环己酮
参考文献:4-Amino-4-Phenylcyclohexanone Ketal Compositions And Process Of Use
标题:4-Amino-4-Phenylcyclohexanone Ketal Compositions And Process Of Use
摘要:一类新的4-氨基-4-芳基环己酮,它们的缩醛和酸盐已经合成,并发现对于缓解动物的疼痛很有用.它们的镇痛活性似乎是很高的,并且一些还表现出对镇痛引起的心血管,呼吸和行为抑制有用的麻醉拮抗活性.其中几种显示出混合的镇痛和麻醉拮抗活性.该类化合物的首选化合物是4-(间羟基苯基)-4-二甲氨基环己酮乙二醚缩醛,以及4-(间羟基苯基)-4-(正丁基甲基氨基)环己酮乙二醚缩醛,作为游离碱和其盐酸盐形式.描述了合成和中间体的过程.披露了单位剂量形式和治疗方法.

专利信息

专利号:US-6172066-B1
优先权日:1996-05-16
标 题:Dihydropyrimidines and uses thereof
发明人：NAGARATHNAM DHANAPALAN; WONG WAI C; MIAO SHOU WU; PATANE MICHAEL A; GLUCHOWSKI CHARLES
权利人:SYNAPTIC PHARMA CORP
摘要:This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

专利号:US-6228861-B1
优先权日:1995-11-16
标题 :Dihydropyrimidines and uses thereof
发明人：NAGARATHNAM DHANAPALAN; WONG WAI C; MIAO SHOU WU; GLUCHOWSKI CHARLES; PATANE MICHAEL A
权利人:SYNAPTIC PHARMA CORP
摘要:This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

专利号:US-6255315-B1
优先权日:1997-06-18
标题:Alpha 1a adrenergic receptor antagonists
发明人：PATANE MICHAEL A; SELNICK HAROLD G; BOCK MARK G
权利人:MERCK & CO INC
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 relductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

专利号:US-6080760-A
优先权日:1997-06-18
标题:Alpha 1A adrenergic receptor antagonists
发明人：PATANE MICHAEL A; BOCK MARK G
权利人:MERCK & CO INC
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.

专利号:US-6245773-B1
优先权日:1996-05-16
标题:5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
发明人：WONG WAI C; LAGU BHARAT; NAGARATHNAM DHANAPALAN; MARZABADI MOHAMMAD R; GLUCHOWSKI CHARLES
权利人:SYNAPTIC PHARMA CORP
摘要:This invention is directed to dihydropyrimidine compounds of the following formula: n which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

专利号:WO-9717969-A1
优先权日:1995-11-16
标题 :Dihydropyrimidines and uses thereof
发明人：NAGARATHNAM DHANAPALAN; WONG WAI C; MIAO SHOU WU; PATANE MICHAEL A; GLUCHOWSKI CHARLES
权利人:SYNAPTIC PHARMA CORP; MERCK & CO INC; NAGARATHNAM DHANAPALAN; WONG WAI C; MIAO SHOU WU; PATANE MICHAEL A; GLUCHOWSKI CHARLES
摘要:This invention is directed to dihydropyrimidine compounds which are selective antagonists for human alpha 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of begnin prostatic hyperplasia, impotency, cardiac arrythmia and for the treatment of any disease where the antagonism of the alpha 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.