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1.发明授权6- and/or 7-substituted-1,2,3,4,4A,9B-hexahydro-8-hydroxydibenzofuran-3-ols as inhibitors of leukotriene biosynthesis 失效6-和/或7-取代-1,2,3,4,4A，9B-六氢-8-羟基二苯并呋喃-3-醇作为白细胞三烯生物合成的抑制剂
公开(公告)号：US4978679A
公开(公告)日：1990-12-18
申请号：US411787
申请日：1989-09-25
IPC分类号： A61K31/34 , A61K31/343 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/08 , C07D307/77 , C07D307/91
CPC分类号： C07D307/77 , C07D307/91
摘要： Positions 7- and/or 6-substituted 1,2,3,4,4a,9b-Hexahydro-8-hydroxydibenzofuran-3-ols and analogs of that general structure are described.These compounds are found to be potent inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful in the treatment of a variety of inflammatory conditions.
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公开(公告)号：US4812442A
公开(公告)日：1989-03-14
申请号：US45941
申请日：1987-05-04
申请人： Joshua S. Boger , Ben E. Evans , Mark G. Bock
发明人： Joshua S. Boger , Ben E. Evans , Mark G. Bock
IPC分类号： A61K38/00 , C07D233/54 , C07F9/30 , C07F9/32 , C07F9/40 , C07F9/48 , C07F9/6506 , C07K5/02 , C07K5/065 , C07K7/02 , C07K5/06 , C07K5/08 , C07D241/04 , C07D265/30 , C07D211/30 , C07D211/70 , C07D263/02 , C07D207/04
CPC分类号： C07D233/64 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3217 , C07F9/3223 , C07F9/4006 , C07F9/4816 , C07F9/4833 , C07F9/65067 , C07K5/0227 , C07K5/06078 , C07K7/02 , A61K38/00 , Y10S530/86
摘要： Enzyme tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems employing the novel tripeptides.
摘要翻译： 下式的酶三肽及其类似物抑制肾素，可用于治疗各种形式的肾素相关性高血压，醛固酮增多症和充血性心力衰竭; 含有这些肾素抑制肽的组合物，任选与其它抗高血压药物组合; 以及治疗高血压，醛固酮增多症或充血性心力衰竭的方法，或者在使用新型三肽的这些问题中建立肾素作为致病因素。
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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：US4596674A
公开(公告)日：1986-06-24
申请号：US649388
申请日：1984-09-11
IPC分类号： C07K14/00 , A61K39/29 , A61K39/385 , C07K7/06 , C07K7/08 , C07K14/02 , C07K14/10 , C07K14/18 , C07K16/00 , C07K17/02 , C07K19/00 , G01N33/576 , C07K7/10
CPC分类号： C07K14/005 , A61K39/385 , G01N33/5768 , A61K2039/6081 , C12N2770/32422 , C12N2770/32434 , Y10S530/807 , Y10S930/223
摘要： Synthetic peptides, containing amino acid residues 15 to 21, 75-80 and 101-107 of the hepatitis A virus (HAV) VP1 structural protein sequence, was prepared and chemically conjugated to a protein carrier molecule. The peptide-carrier conjugate, when inoculated into test animals, gives rise to a specific anti-peptide IgG antibody response. These anti-peptide antibodies bind directly to intact hepatitis A virions, bind to purified and denatured VP1, compete with polyspecific antibody derived from human HAV immune sera, and are capable of neutralizing the infectivity of the virus. The peptide is useful as a synthetic subunit immunogen that stimulates an immune response against HAV.
摘要翻译： 制备含有甲型肝炎病毒（HAV）VP1结构蛋白序列的15至21,75-80和101-107的氨基酸残基的合成肽，并与蛋白质载体分子化学偶联。 肽 - 载体缀合物当接种到测试动物中时产生特异性抗肽IgG抗体应答。 这些抗肽抗体直接与完整的甲型肝炎病毒粒子结合，结合纯化和变性的VP1，与源自人HAV免疫血清的多特异性抗体竞争，并且能够中和病毒的感染性。 该肽可用作刺激针对HAV的免疫应答的合成亚单位免疫原。
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公开(公告)号：US5723459A
公开(公告)日：1998-03-03
申请号：US377315
申请日：1995-01-24
IPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00 , A61K31/54 , A61K31/535 , C07D401/02 , C07D403/02
CPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
摘要翻译： 本发明涉及具有广泛有用生物活性的新化合物。 这些化合物可以维持，增加或恢复细胞对治疗或预防剂的敏感性。 它们还可以抑制，修饰或显着降低免疫应答，包括哺乳动物的自身免疫反应。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于治疗多药耐药性细胞，用于预防多药耐药性的发展，用于多药耐药性癌症治疗以及用于预防或治疗移植物 排斥反应和各种自身免疫性疾病。
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公开(公告)号：US5620971A
公开(公告)日：1997-04-15
申请号：US217982
申请日：1994-03-25
IPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00 , A61K31/54 , A61K31/535 , C07D403/06 , C07D403/14
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
摘要翻译： 本发明涉及具有广泛有用生物活性的新化合物。 这些化合物可以维持，增加或恢复细胞对治疗或预防剂的敏感性。 它们还可以抑制，修饰或显着降低免疫应答，包括哺乳动物的自身免疫反应。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于治疗多药耐药性细胞，用于预防多药耐药性的发展，用于多药耐药性癌症治疗以及用于预防或治疗移植物 排斥反应和各种自身免疫性疾病。
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7.发明授权Trans 2,3-disubstituted-2,3-dihydro-5-hydroxy-benzofurans as inhibitors of leukotriene biosynthesis 失效作为白三烯生物合成的抑制剂的2,3-二取代-2,3-二氢-5-羟基 - 苯并呋喃代替
公开(公告)号：US4975457A
公开(公告)日：1990-12-04
申请号：US411788
申请日：1989-09-25
IPC分类号： C07D307/78 , A61K31/34 , A61K31/343 , A61K31/385 , A61P29/00 , A61P37/08 , A61P43/00 , C07D307/79 , C07D307/80 , C07D307/92 , C07D409/06
CPC分类号： C07D307/79 , C07D307/80 , C07D409/06
摘要： Certain trans-2,3-disubstituted-2,3-dihydro-5-hydroxybenzofurans are described. The synthesis involves an intramolecular Michael addition to yield the thermodynamic trans isomer. The compounds were found to be inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful for the treatment of various inflammatory diseases.
摘要翻译： 描述了某些反式-2,3-二取代-2,3-二氢-5-羟基苯并呋喃。 该合成涉及分子内迈克尔加成以产生热力学反式异构体。 发现这些化合物是5-脂氧合酶的抑制剂，5-脂氧合酶是白三烯生物合成所必需的酶，可用于治疗各种炎性疾病。
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公开(公告)号：US4668770A
公开(公告)日：1987-05-26
申请号：US608321
申请日：1984-05-08
申请人： Joshua S. Boger , Daniel F. Veber , Ben E. Evans
发明人： Joshua S. Boger , Daniel F. Veber , Ben E. Evans
CPC分类号： C07K5/0227 , Y10S530/86
摘要： Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
摘要翻译： 式“IMAGE”的肾素抑制肽及其类似物抑制肾素，并且可用于治疗各种形式的肾素相关性高血压和醛固酮增多症。
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公开(公告)号：US4470971A
公开(公告)日：1984-09-11
申请号：US413632
申请日：1982-09-03
申请人： Joshua S. Boger , Daniel F. Veber
发明人： Joshua S. Boger , Daniel F. Veber
IPC分类号： A61K38/00 , C07K5/02 , C07K7/02 , C07C103/52 , A61K37/02
CPC分类号： C07K5/0227 , C07K7/02 , A61K38/00 , Y10S530/86
摘要： Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
摘要翻译： 式（I）的肾素抑制肽及其类似物抑制肾素，并且可用于治疗各种形式的肾素相关性高血压和醛固酮增多症。
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公开(公告)号：US5192773A
公开(公告)日：1993-03-09
申请号：US547814
申请日：1990-07-02
IPC分类号： A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及对FK-506结合蛋白（FKBP）具有亲和力的新一类免疫抑制化合物。 一旦结合到该蛋白质上，免疫抑制化合物抑制FKBP的脯氨酰基顺式 - 反式异构酶（旋转异构酶）活性并抑制T细胞活化。 因此，本发明的化合物可用作免疫抑制药物，以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物中各种自身免疫性疾病。
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