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公开(公告)号:US20130178468A1
公开(公告)日:2013-07-11
申请号:US13606929
申请日:2012-09-07
申请人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaccs , Wei Han , Melissa Egbertson , Richard Pracitto
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaccs , Wei Han , Melissa Egbertson , Richard Pracitto
IPC分类号: C07D471/14 , C07D498/14
CPC分类号: C07D471/14 , A61K31/4353 , A61K31/4375 , C07D498/14
摘要: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 式I的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂:其中键A,环A,R 1,R 2和R 3在本文中定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防,治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:US06436962B1
公开(公告)日:2002-08-20
申请号:US09671518
申请日:2000-09-27
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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公开(公告)号:US5668148A
公开(公告)日:1997-09-16
申请号:US425969
申请日:1995-04-20
IPC分类号: A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61P5/00 , A61P13/02 , A61P15/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , A61K31/415 , A61K31/42 , A61K31/425 , C07D409/04
CPC分类号: C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要: Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1## wherein: Ar1 and Ar2 can be independantly aromatic, heteroaromatic, or condensed heteroaromatic unsubstituted or substituted with amino, alkoxy, sulfonamido, alkyl, heteroalkyl, halo;m is 0 or 1;n is 0, 1, or 2;het is an aromatic or nonaromatic heterocyclic ring, substituted with alkyl, halo, or alkoxy substituents; andX is a branched or straight chain aliphatic or halogen substituent.
摘要翻译: 特异性结合人α1a肾上腺素能受体的化合物,包括有效降低良性前列腺肥大症状的化合物包括下式的化合物:其中:Ar1和Ar2可以是独立的芳族,杂芳族或未被取代或被氨基取代的稠合杂芳族, 烷氧基,亚磺酰氨基,烷基,杂烷基,卤素; m为0或1; n为0,1或2; het是被烷基,卤素或烷氧基取代的芳族或非芳族杂环; X是支链或直链脂族或卤素取代基。
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公开(公告)号:US5665720A
公开(公告)日:1997-09-09
申请号:US458529
申请日:1995-06-02
IPC分类号: A61K31/535 , A61K31/536 , A61K45/06 , C07D265/18
CPC分类号: C07D265/18 , A61K31/535 , A61K31/536 , A61K31/70 , A61K45/06 , Y10S514/934
摘要: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译: 某些苯并恶嗪酮可用于抑制HIV逆转录酶(包括其抗性品种),预防或治疗艾滋病毒感染和艾滋病治疗,作为化合物,药学上可接受的盐,药物组合物成分,无论是否与 其他抗病毒药物,免疫调节剂,抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号:US4705892A
公开(公告)日:1987-11-10
申请号:US915829
申请日:1986-10-16
申请人: Joshua S. Boger , Linda S. Payne
发明人: Joshua S. Boger , Linda S. Payne
IPC分类号: C07C101/24
CPC分类号: C07C227/20 , Y10S530/86
摘要: An improved process for preparing .alpha.,.omega.-diamino acids, such as D,L-homolysine, 2,8-diaminooctanoic acid, ornithine, lysine, or the like, comprising reaction of phthalic anhydride and an amino alcohol in a hydrocarbon solvent; treatment of the resulting phthalimide--N--(CH.sub.2).sub.n --OH derivative, without isolation thereof, with phosphorus tribromide or phosphorous pentachloride; alkylation of diethyl acetamidomalonate with the phthalimide--N--(CH.sub.2).sub.n --chloride or --bromide of the previous step, in the presence of, particularly, sodium hydride/dimethylformamide; standard acid hydrolysis and decarboxylation; selective protection via copper(II) chelation, N-specific acylation with benzyl chloroformate, and decomposition of the amino acid-copper(II) complex with alkaline thioacetamide; standard t-butoxycarbonyl acylation; and deprotection to obtain the desired .alpha.,.omega.-diamino acids.
摘要翻译: 包括制备α,ω-二氨基酸如D,L-高赖氨酸,2,8-二氨基辛酸,鸟氨酸,赖氨酸等的改进方法,包括邻苯二甲酸酐和氨基醇在烃溶剂中的反应; 用三溴化磷或五氯化磷处理所得的邻苯二甲酰亚胺-N-(CH 2)n -OH衍生物,不分离; 在上述步骤的邻苯二甲酰亚胺-N-(CH 2)n - 氯化物或溴化物中,在特别是氢化钠/二甲基甲酰胺的存在下烷基化乙酰氨基马来酸二乙酯; 标准酸水解和脱羧; 通过铜(II)螯合的选择性保护,氯甲酸苄酯的N-特异性酰化和氨基酸 - 铜(II)配合物与碱性硫代乙酰胺的分解; 标准叔丁氧羰基酰化; 并去保护,得到所需的α,ω-二氨基酸。
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公开(公告)号:US07879839B2
公开(公告)日:2011-02-01
申请号:US11658114
申请日:2005-07-27
申请人: Christopher J. Dinsmore , Jeffrey M. Bergman , Douglas C. Beshore , B. Wesley Trotter , Kausik K. Nanda , Richard Isaacs , Linda S. Payne , Lou Anne Neilson , Zhicai Wu , Mark T. Bilodeau , Peter J. Manley , Adrienne E. Balitza
发明人: Christopher J. Dinsmore , Jeffrey M. Bergman , Douglas C. Beshore , B. Wesley Trotter , Kausik K. Nanda , Richard Isaacs , Linda S. Payne , Lou Anne Neilson , Zhicai Wu , Mark T. Bilodeau , Peter J. Manley , Adrienne E. Balitza
IPC分类号: C07D401/14 , A61K31/438
CPC分类号: C07D213/36 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/55 , C07D213/56 , C07D213/64 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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公开(公告)号:US20100216834A1
公开(公告)日:2010-08-26
申请号:US12445594
申请日:2007-10-15
IPC分类号: A61K31/4375 , C07D471/14 , C07D471/04 , A61P31/18
CPC分类号: C07D471/14
摘要: Stereoisomers of compounds of Formula I are disclosed: wherein V1, V2, R5a, R5b, R5c, R8 and R9b are defined herein and wherein the stereoisomer contains 2 chiral centers in the 8-membered ring and one of the chiral centers is due to the presence of a chiral ring carbon. The isomers are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 公开了式I化合物的立体异构体:其中V1,V2,R5a,R5b,R5c,R8和R9b在本文中定义,其中立体异构体在8元环中含有2个手性中心,并且其中一个手性中心是由于 存在手性环碳。 异构体是HIV整合酶和HIV复制抑制剂的抑制剂,可用于预防或治疗艾滋病毒感染以及艾滋病的发病或进展的预防,治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:US07781457B2
公开(公告)日:2010-08-24
申请号:US10572343
申请日:2004-09-22
申请人: Richard Isaacs , Christopher J. Dinsmore , Charles J. McIntyre , Linda S. Payne , David A. Claremon
发明人: Richard Isaacs , Christopher J. Dinsmore , Charles J. McIntyre , Linda S. Payne , David A. Claremon
IPC分类号: C07D217/16 , A61K31/47
CPC分类号: C07D217/26 , C07D217/24 , C07D401/04 , C07D401/06 , C07D417/04
摘要: The present invention relates to compounds having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译: 本发明涉及具有结构式(I)的化合物,其可用作治疗心律失常的钾通道抑制剂等。
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公开(公告)号:US20090054399A1
公开(公告)日:2009-02-26
申请号:US11920032
申请日:2006-05-05
申请人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C.A. Isaacs , Wei Han , Melissa Egbertson , Richard Pracitto
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C.A. Isaacs , Wei Han , Melissa Egbertson , Richard Pracitto
IPC分类号: A61K31/5383 , C07D471/14 , A61K31/551 , A61K31/4985 , A61K31/4375 , C07D498/14
CPC分类号: C07D471/14 , A61K31/4353 , A61K31/4375 , C07D498/14
摘要: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 式(I)的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂:其中键A,环A,R 1,R 2和R 3在本文中定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防,治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:US08293731B2
公开(公告)日:2012-10-23
申请号:US13107512
申请日:2011-05-13
申请人: Joseph P. Vacca , John S. Wai , Linda S. Payne
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne
IPC分类号: A01N43/62 , A61K31/55 , C07D487/00
CPC分类号: C07D471/14 , A61K31/4353 , A61K31/4375 , C07D498/14
摘要: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 式I的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂:其中键A,环A,R 1,R 2和R 3在本文中定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防,治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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