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81. 发明授权

US5248830A Enantioselective preparation of acetylenic or olefinic substituted cycloalkenyl dihydroxybutyrates and 4-hydroxy-tetrahydro-pyran-2-ones 失效
标题翻译：炔属或烯烃取代的环烯基二羟基丁酸酯和4-羟基 - 四氢 - 吡喃-2-酮的对映选择性制备
公开(公告)号：US5248830A
公开(公告)日：1993-09-28
申请号：US902752
申请日：1992-06-23
申请人： John Ullrich , John R. Regan
发明人： John Ullrich , John R. Regan
IPC分类号： C07C45/58 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C69/732 , C07C69/738 , C07C205/45 , C07F7/08 , C07F7/18 , C07F9/30 , C07F9/32
CPC分类号： C07F9/3223 , C07C205/45 , C07C45/58 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C69/732 , C07C69/738 , C07F7/0818 , C07F7/186 , C07F9/303
摘要： Disclosed are intermediates and a process of making an anticholesterolemic compound of the formula ##STR1## the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.
摘要翻译：公开了中间体和制备下式的抗胆固醇血型化合物的方法：由其衍生的相应的开环羟基酸及其药学上可接受的盐。

82. 发明授权

US5231198A Asymmetric synthesis of hexahydrodibenzofurans by stereospecific inversion of ortho substituted 2-phenylcyclohexanols 失效
标题翻译：通过邻位取代的2-苯基环己醇的立体特异性反转不对称合成六氢二苯并呋喃
公开(公告)号：US5231198A
公开(公告)日：1993-07-27
申请号：US909541
申请日：1992-07-06
申请人： Mattew R. Powers , Frederick A. Golec
发明人： Mattew R. Powers , Frederick A. Golec
IPC分类号： C12P7/22 , C12P41/00
CPC分类号： C12P7/22 , C12P41/004
摘要： This invention relates to the stereospecific process for the preparation, separation and purification of hexahydrodibenzofurans which are used in the preparation of the 5HT.sub.3 compounds. More specifically, the present invention relates to a process for the preparation of substantially optically pure cishexahydrodibenzofuran compounds including at least two chiral fused ring centers which comprises the acidic catalyzed stereospecific ring closure by the intra-molecular inversion of a gamma, i.e. 2', carbon atom of a 2-[(2'-leaving group)cycloalkyl]phenol.
摘要翻译：本发明涉及用于制备5HT3化合物的六氢二苯并呋喃的制备，分离和纯化的立体特异性方法。更具体地说，本发明涉及一种制备基本上光学纯的顺式六氢二苯并呋喃化合物的方法，其包括至少两个手性稠环中心，其包含通过γ分子内反转的酸性催化的立体特异性闭环，即2' 原子的2 - [（2'-离去基团）环烷基]苯酚。

83. 发明授权

US5217982A Compounds having antihypertensive properties 失效
标题翻译：具有抗高血压性质的化合物
公开(公告)号：US5217982A
公开(公告)日：1993-06-08
申请号：US614323
申请日：1990-11-15
申请人： Cynthia A. Fink , Alfred P. Spada
发明人： Cynthia A. Fink , Alfred P. Spada
IPC分类号： C07D473/00 , C07H19/052 , C07H19/16
CPC分类号： C07D473/00 , C07H19/052 , C07H19/16
摘要： This invention relates to compounds which are derivatives of cyclopentane which are useful as antihypertensive agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension.
摘要翻译：本发明涉及可用作抗高血压剂的作为环戊烷衍生物的化合物，包括这些化合物的药物组合物及其在治疗高血压中的用途。

84. 发明授权

US5216015A Compounds having hypocholesterolemic properties 失效
标题翻译：具有低胆固醇血性的化合物
公开(公告)号：US5216015A
公开(公告)日：1993-06-01
申请号：US650494
申请日：1991-02-05
申请人： Daniel G. McGarry , Francis A. Volz , John R. Regan , Michael N. Chang
发明人： Daniel G. McGarry , Francis A. Volz , John R. Regan , Michael N. Chang
IPC分类号： C07J9/00 , C07J13/00 , C07J17/00 , C07J31/00 , C07J51/00 , C07J63/00
CPC分类号： C07J9/00 , C07J13/005 , C07J17/00 , C07J31/006 , C07J51/00 , C07J63/008 , C07J9/005
摘要： This invention relates to compounds which are steroidyl derivatives of 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one and the corresponding ring-opened hydroxy acid form thereof which are useful as antihypercholesterolemic agents, to pharmaceutical compositions including such compounds, and to their use in treating hypercholesterolemia.
摘要翻译：本发明涉及作为抗高胆固醇血症药物使用的4-羟基-3,4,5,6-四氢-2H-吡喃-2-酮的类固醇衍生物及其相应的开环羟基酸形式的化合物，包括这些化合物的组合物及其在治疗高胆固醇血症中的用途。

85. 发明授权

US5125466A Product-dispensing method and apparatus 失效
标题翻译：产品分配方法和装置
公开(公告)号：US5125466A
公开(公告)日：1992-06-30
申请号：US649304
申请日：1991-01-30
申请人： George R. Felt , Donna K. Multhauf , Sudhakar S. Wagle
发明人： George R. Felt , Donna K. Multhauf , Sudhakar S. Wagle
IPC分类号： G01F19/00 , G01F23/04 , G01F23/64
CPC分类号： G01F19/00 , G01F23/04 , G01F23/64
摘要： An aerosol spray dispenser of flowable pharmaceutical product is provided with a flotation stabilizing arrangement such that it will float in water in a stabilized erect position even when empty of product; a scale is associated with the dispenser so that the depth at which it floats can be read by comparing the position of the surface of the water in which it floats with graduations on the scale. The stabilizing action may be obtained by placing the dispenser in a floatable bottom-weighted vial, with the scale located in the exterior of the vial, and the combination of vial and dispenser then floated in water. In other embodiments the vial need not be used, in which case the dispenser itself may be bottom-weighted to assure its stabilized erect flotation and the scale placed on the exterior of the dispenser; or, a cap may be provided for the dispenser which is positioned on the dispenser while both are floated in the water, the cap being top-weighted so that the assembly floats stably upside-down. In the latter case the graduations may be placed on the dispenser, or on a strip integral with the cap extending along the outside of the dispenser; alternatively, the cap may be provided with an integral skirt which extends completely around the dispenser and to its bottom end, with the scale located on the exterior of the skirt.
摘要翻译：可流动药物产品的气溶胶喷雾分配器具有浮选稳定装置，使得即使在空的产品时也能以稳定的直立位置在水中漂浮; 比例尺与分配器相关联，因此可以通过比较其浮动的水面与刻度上的刻度的位置来读取其浮动深度。稳定作用可以通过将分配器放置在可浮动的底部加重的小瓶中，其中秤位于小瓶的外部，并且小瓶和分配器的组合器然后漂浮在水中而获得。在其他实施例中，不需要使用小瓶，在这种情况下，分配器本身可以是底部加权的，以确保其稳定的直立浮选和刻度放置在分配器的外部上; 或者，可以为位于分配器上的分配器提供盖子，同时两者都浮在水中，盖子被顶部加重，使得组件稳定地上下颠倒。在后一种情况下，刻度可以放置在分配器上，或者放置在与分配器的外部延伸的与盖一体的条上; 或者，盖可以设置有整体裙部，其完全围绕分配器延伸到其底端，其中秤位于裙部的外部。

86. 发明授权

US5041453A Quinolinyl-benzoheterobicyclic derivatives as antagonists of leukotriene D4 失效
标题翻译：喹啉基 - 苯并双环衍生物作为白三烯D4的拮抗剂
公开(公告)号：US5041453A
公开(公告)日：1991-08-20
申请号：US532464
申请日：1990-05-30
申请人： Fu-Chih Huang , Keith S. Learn , Ashvin V. Gavai
发明人： Fu-Chih Huang , Keith S. Learn , Ashvin V. Gavai
IPC分类号： A61K31/47 , A61P29/00 , A61P37/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D411/10 , C07D411/12 , C07D411/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D417/12 , C07D417/14 , C07D419/10 , C07D419/12
CPC分类号： C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： This invention relates to certain quinolinyl-benzoheterobicyclic compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists and/or as mediator release inhibitors useful as anti-inflammatory and anti-allergic agents.
摘要翻译：本发明涉及某些喹啉基 - 苯并双环化合物及其作为有价药物，特别是作为脂氧合酶抑制剂和/或白三烯拮抗剂和/或用作抗炎和抗过敏剂的介质释放抑制剂的用途。

87. 发明授权

US5015638A Naphtheridinone- and pyridooxazinone-pyridone compounds, cardiotonic compositions including same, and their uses 失效
标题翻译：萘啶酮和吡啶并恶嗪酮 - 吡啶酮化合物，包括它们的强心剂组合物及其用途
公开(公告)号：US5015638A
公开(公告)日：1991-05-14
申请号：US432070
申请日：1989-11-03
申请人： Alfred P. Spada , William L. Studt , Henry F. Campbell , Donald E. Kuhla , Thomas Tucker
发明人： Alfred P. Spada , William L. Studt , Henry F. Campbell , Donald E. Kuhla , Thomas Tucker
IPC分类号： C07D471/04 , C07D498/04
CPC分类号： C07D471/04
摘要： This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.
摘要翻译：本发明涉及可用作治疗充血性心力衰竭的强心剂的取代吡啶并恶嗪酮和萘乙酮吡喃酮，使用所述化合物增加心脏收缩力的方法以及包含其的药物组合物。

88. 发明授权

US5006642A Purification of von Willebrand Factor by affinity chromatography 失效
标题翻译：通过亲和层析法纯化血管性血友病因子
公开(公告)号：US5006642A
公开(公告)日：1991-04-09
申请号：US205881
申请日：1988-06-13
申请人： Jack Newman , David L. Farb
发明人： Jack Newman , David L. Farb
IPC分类号： A61K38/00 , C07K14/755
CPC分类号： C07K14/755 , A61K38/00
摘要： A method of preparing von Willebrand Factor by disassociating it from a chaotropic agent in solution therewith and preferably treating the same under controlled temperature either in liquid or lyophilized form.
摘要翻译：将von Willebrand因子与溶液中的离液剂分离，优选在液体或冻干形式的受控温度下进行处理。

89. 发明授权

US5002944A Compounds having cardiotonic activity 失效
标题翻译：化合物具有强心活性
公开(公告)号：US5002944A
公开(公告)日：1991-03-26
申请号：US350366
申请日：1989-05-11
申请人： Alfred P. Spada , Henry F. Campbell , Donald E. Kuhla , William L. Studt , William C. Faith , Bruce F. Molino
发明人： Alfred P. Spada , Henry F. Campbell , Donald E. Kuhla , William L. Studt , William C. Faith , Bruce F. Molino
IPC分类号： C07D471/04 , C07D475/00
CPC分类号： C07D471/04 , C07D475/00
摘要： Compounds useful for increasing cardiotonic contractility in humans or other animals and pharmaceutical compositions including these compounds are disclosed. The compounds have the general structure: ##STR1## where A is ##STR2## R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9, and R.sub.10 are H, lower alkyl of 1-4 carbon atoms, phenyl, substituted phenyl, phenyl lower alkyl of 1-4 carbon atoms or substituted phenyl lower alkyl of 1-4 carbon atoms; and n is 0 or 1.
摘要翻译：公开了可用于增加人或其他动物的强心收缩性的化合物和包括这些化合物的药物组合物。这些化合物具有以下通式：其中A为R 1，R 2，R 3，R 4，R 9和R 10为H，1-4个碳原子的低级烷基，苯基，取代的苯基，苯基低级 1-4个碳原子的烷基或1-4个碳原子的取代的苯基低级烷基; n为0或1。

90. 发明授权

US5001222A Des-17-histidine-calcitonin 失效
标题翻译： Des-17-组氨酸降钙素
公开(公告)号：US5001222A
公开(公告)日：1991-03-19
申请号：US197538
申请日：1988-05-23
申请人： Ronald C. Orlowski , Robert L. Colescott
发明人： Ronald C. Orlowski , Robert L. Colescott
IPC分类号： A61K38/23 , A61K38/00 , A61P3/00 , A61P43/00 , C07K14/575 , C07K14/585
CPC分类号： C07K14/585 , A61K38/00
摘要： New peptides are disclosed which have biological activity of the same type as known calcitonins and which do not have a histidine in position 17. The position 17 histidine is omitted. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.

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