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1. 发明授权

US4977268A Boron dipeptide compounds 失效
标题翻译：硼二肽化合物
公开(公告)号：US4977268A
公开(公告)日：1990-12-11
申请号：US179555
申请日：1988-04-08
申请人： Andrew T. McPhail , Bernard F. Spielvogel , Iris H. Hall
发明人： Andrew T. McPhail , Bernard F. Spielvogel , Iris H. Hall
IPC分类号： C07F5/02
CPC分类号： C07F5/027
摘要： Novel boron dipeptide analogs and their corresponding amide derivatives which exhibit significant antihyperlipidemic and antineoplastic activities. Methods for preparing the boron containing compounds are disclosed as well as methods for utilizing the compounds to induce antihyperlipidemic and antineoplastic activity.

2. 发明授权

US4587359A Amine-carbamoylborane adducts 失效
标题翻译：胺 - 氨基甲酰基硼烷加成物
公开(公告)号：US4587359A
公开(公告)日：1986-05-06
申请号：US611247
申请日：1984-05-17
申请人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
发明人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
IPC分类号： C07F5/02
CPC分类号： C07F5/027
摘要： This invention involves amine-carbamoylborane compounds of the formulaR.sub.1 R.sub.2 NH.BH.sub.2 C(O)NHR.sub.3wherein R.sub.1 and R.sub.2 are hydrogen or certain alkyl moieties and R..3 is an alkyl. A process for their preparation involving an amine displacement reaction is also described. A method of use and pharmaceutical compositions containing the subject compounds are also described.
摘要翻译：本发明涉及式R1R2NH.BH2C（O）NHR3的胺 - 氨基甲酰基硼烷化合物，其中R 1和R 2是氢或某些烷基部分，且R 3是烷基。还描述了其涉及胺置换反应的制备方法。还描述了使用方法和含有本发明化合物的药物组合物。

3. 发明授权

US4647555A Esters of boron analogues of amino acids 失效
标题翻译：氨基酸的硼类似物的酯
公开(公告)号：US4647555A
公开(公告)日：1987-03-03
申请号：US664647
申请日：1984-10-25
申请人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
发明人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
IPC分类号： A61K31/69 , C07F5/02 , C07F7/18 , A61K31/695 , A01N55/00
CPC分类号： C07F5/027 , A61K31/69 , C07F7/1896
摘要： Ester analogues of boron analogues of amino acid are disclosed. Also disced is a method of forming the ester analogues in high yield by condensation of the corresponding acids and alcohols with dicylohexylcarbodiimide at room temperature in dichloromethane. The disclosed compounds have shown interesting biological activities, in particular, hypolipidemic activity as well as significant antitumor and antiarthritic activities.
摘要翻译：公开了氨基酸的硼类似物的酯类似物。还公开了通过相应的酸和醇与二氰基己基碳二亚胺在室温下在二氯甲烷中缩合形成酯类似物的方法。所公开的化合物已显示有趣的生物活性，特别是降血脂活性以及显着的抗肿瘤和抗关节炎活性。

4. 发明授权

US4368194A Pharmacologically active amine boranes 失效
标题翻译：药理活性胺硼烷
公开(公告)号：US4368194A
公开(公告)日：1983-01-11
申请号：US284279
申请日：1981-07-17
申请人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
发明人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
IPC分类号： C07F5/00 , C07F5/02
CPC分类号： C07F5/006 , C07F5/027
摘要： The use of a mine boranes to inhibit the inflammation process is disclosed.hese boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz., 10.sup.-6 M.Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.
摘要翻译：公开了使用矿物硼烷抑制炎症过程。这些硼烷是α-氨基酸的硼类似物，有效地阻断了以下：一般炎症，诱发的关节炎和与炎症疼痛相关的扭动反射。与胸膜炎相关的炎症也受到抑制。硼类似物在体外显示以抑制溶酶体酶从肝脏和多形核嗜中性粒细胞（PMN）的释放。此外，前列腺素合成被这些化合物以低浓度，即10-6M阻断。肝氧化磷酸化过程也被这些化合物解偶联，但是PMN迁移在10-4M不变。环磷酸腺苷的升高 PMNs与体内抗关节炎活性呈正相关。啮齿类动物的研究表明，这些硼类似物可以以安全的治疗剂量使用。本发明的范围包括几种化合物本身。

5. 发明授权

US4855493A Pharmacological active amine-carboxyboranes 失效
标题翻译：药理活性胺 - 羧基硼烷
公开(公告)号：US4855493A
公开(公告)日：1989-08-08
申请号：US882562
申请日：1986-07-07
申请人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
发明人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
IPC分类号： C07F5/00 , C07F5/02
CPC分类号： C07F5/006 , C07F5/027
摘要： Amine-carboxyboranes (boron analogues of amino acids) which demonstrate sificant antitumor and antihyperlipidemic (cholesterol and /or triglyceride lowering) activities are disclosed.
摘要翻译：公开了显示出显着的抗肿瘤和抗高脂血症（胆固醇和/或甘油三酯降低）活性的胺羧基硼烷（氨基酸的硼类似物）。

6. 发明授权

US4550186A Binuclear copper (II) carboxylates formed from amine-carboxyboranes 失效
标题翻译：由胺 - 羧基硼烷形成的双核铜（II）羧酸盐
公开(公告)号：US4550186A
公开(公告)日：1985-10-29
申请号：US512729
申请日：1983-07-11
申请人： Andrew T. McPhail , Bernard F. Spielvogel , Iris H. Hall
发明人： Andrew T. McPhail , Bernard F. Spielvogel , Iris H. Hall
IPC分类号： C07F5/02 , C07F1/08
CPC分类号： C07F5/027
摘要： A compound of the formula[Cu(R.sub.3 NBH.sub.2 CO.sub.2).sub.2. R.sub.3 NBH.sub.2 CO.sub.2 H].sub.2wherein each R independently represents H, C.sub.1 -C.sub.10 alkyl, or phenyl and L represents a non-toxic Lewis base capable of forming a coordinate bond with the copper with the provisos that any two or three R attached to the same nitrogen may represent a C.sub.4 -C.sub.5 alkylene group containing up to 2 non-cumulative double bonds optionally having 1 or 2 carbons replaced by oxygen or nitrogen, that any 3 R attached to the same nitrogen when taken together with the nitrogen may represent a 6-membered aromatic ring containing 1, 2 or 3 nitrogen atoms, and that any R containing a carbon atom may be substituted with a hydroxyl, ether, ester, carboxyl, or amino functional group is disclosed along with methods of making these compounds and methods of using these compounds as antihyperlipidemic agents and antineoplastic agents.
摘要翻译：式[Cu（R 3 NBH 2 CO 2）2）的化合物。 R3NBH2CO2H] 2，其中每个R独立地表示H，C1-C10烷基或苯基，L表示能够与铜形成配位键的无毒路易斯碱，条件是连接到相同氮的任何两个或三个R可以表示含有至多2个非累积双键的C4-C5亚烷基，任选具有1或2个碳被氧或氮取代，当与氮一起连接到相同氮时的任何3R可以表示6元芳族含有1,2或3个氮原子的环，并且含有碳原子的任何R可以被羟基，醚，酯，羧基或氨基官能团取代，以及制备这些化合物的方法和使用这些化合物的方法作为抗高脂血症药和抗肿瘤药。

7. 发明授权

US4312989A Pharmacologically active amine boranes 失效
标题翻译：药理活性胺硼烷
公开(公告)号：US4312989A
公开(公告)日：1982-01-26
申请号：US68356
申请日：1979-08-21
申请人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
发明人： Bernard F. Spielvogel , Andrew T. McPhail , Iris H. Hall
IPC分类号： C07F5/00 , C07F5/02 , A61K31/69
CPC分类号： C07F5/006 , C07F5/027
摘要： The use of amine boranes to inhibit the inflammation process is disclosed. These boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz, 10.sup.-6 M.Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.
摘要翻译：公开了使用胺硼烷来抑制炎症过程。这些硼烷是α-氨基酸的硼类似物，有效地阻断了以下：一般炎症，诱发的关节炎和与炎症疼痛相关的扭动反射。与胸膜炎相关的炎症也受到抑制。硼类似物在体外显示以抑制溶酶体酶从肝脏和多形核嗜中性粒细胞（PMN）的释放。此外，前列腺素合成被这些化合物以低浓度（即10-6M）阻断。肝氧化磷酸化过程也被这些化合物解偶联，但PMN迁移在10-4M不变。 PMN中环磷酸腺苷的升高与体内抗关节炎活性呈正相关。啮齿动物的研究表明，这些硼类似物可以以安全的治疗剂量使用。本发明的范围包括几种化合物本身。

8. 发明授权

US4539414A 1H-Cyclopenta[b]benzofuran derivative and its analog 失效
标题翻译： 1H-环戊二烯并[b]苯并呋喃衍生物及其类似物
公开(公告)号：US4539414A
公开(公告)日：1985-09-03
申请号：US542140
申请日：1983-10-14
申请人： Ming L. King , Chin-Chih Chiang , Han-Chin Ling , Masahito Ochiai , Eiichi Fujita , Andrew T. McPhail
发明人： Ming L. King , Chin-Chih Chiang , Han-Chin Ling , Masahito Ochiai , Eiichi Fujita , Andrew T. McPhail
IPC分类号： A61K31/16 , A61K31/165 , A61K31/34 , A61K31/343 , A61K36/00 , A61K36/18 , A61P17/16 , A61P35/00 , A61P35/02 , C07C235/40 , C07D307/93 , C07C103/737
CPC分类号： C07D307/93
摘要： Substantially pure compounds having the general formula ##STR1## wherein (1) ##STR2## R.sup.2 is .beta.-hydroxy and R.sup.3 and R.sup.4 together form an oxygen bridge, or (2) ##STR3## R.sup.2 and R.sup.3 together form an additional carbon-carbon bond, and R.sup.4 is hydroxy, are disclosed. These compounds exhibit antileukemic activity against P388 lymphocytic leukemia in CDF.sub.1 mice and inhibitory activity in vitro against cells derived from human epidermoid carcinoma of the nasopharynx(KB) cells.
摘要翻译：具有通式的基本上纯的化合物其中（1）R 2是β-羟基，并且R 3和R 4一起形成氧桥，或（2）R 2和R 3一起形成额外的碳 - 碳键，R4为羟基。这些化合物在CDF1小鼠中表现出对P388淋巴细胞性白血病的抗白血病活性，并且在体外对来自鼻咽（KB）细胞的人表皮样癌的细胞具有抑制活性。

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