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1. 发明授权

US4595695A 1'-ethoxycarbonyloxyethyl ester of valproic acid, its preparation and pharmaceutical compositions containing it 失效
标题翻译：丙戊酸的1'-乙氧基羰基氧基乙酯，其制备方法和含有它的药物组合物
公开(公告)号：US4595695A
公开(公告)日：1986-06-17
申请号：US552336
申请日：1983-11-16
申请人： David Ladkani , Haim Yellin , Ben Z. Weiner
发明人： David Ladkani , Haim Yellin , Ben Z. Weiner
IPC分类号： A61K31/265 , A61K31/22 , A61P25/08 , C07C68/06 , C07C69/96 , C07C69/00
CPC分类号： C07C68/06 , A61K31/22 , C07C69/96
摘要： 1'-Ethoxycarbonyloxyethyl ester of di-n-propylacetic acid, also known as valproic acid. The novel compound is prepared by reacting valproic acid with 1-haloethyl ethyl carbonate. There are also provided pharmaceutical compositions for oral administration containing the said ester.
摘要翻译：二正丙基乙酸的1'-乙氧羰基氧基乙酯，也称为丙戊酸。该新化合物是通过使丙戊酸与碳酸1-卤代乙基酯反应来制备的。还提供含有所述酯的用于口服给药的药物组合物。

2. 发明授权

US4851426A Ethoxycarbonyloxy ethyl esters of non-steroidal anti-inflammatory carboxylic acids and pharmaceutical compositions thereof 失效
标题翻译：非甾族抗炎羧酸的乙氧基羰氧基乙酯及其药物组合物
公开(公告)号：US4851426A
公开(公告)日：1989-07-25
申请号：US810393
申请日：1986-02-12
申请人： David Ladkani , Haim Yellin , Ben Z. Weiner , David Avnir
发明人： David Ladkani , Haim Yellin , Ben Z. Weiner , David Avnir
IPC分类号： A61K31/22 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61P25/04 , A61P29/00 , C07C67/00 , C07C68/06 , C07C69/96 , C07C209/74 , C07C211/56 , C07C229/38 , C07C229/58 , C07C313/00 , C07C317/44 , C07D207/32 , C07D207/337 , C07D209/26 , C07D209/28
CPC分类号： C07C68/06 , A61K31/22 , C07C229/38 , C07C229/58 , C07C69/96 , C07D207/337 , C07D209/26 , C07D209/28
摘要： Novel esters of the general formula ##STR1## in which ##STR2## is the acyl residue of a non-steroidal anti-inflammatory compound containing a carboxylic acid function. The novel esters are prepared by reacting an acide R--COOH when R is as above, with 1-haloethyl ethyl carbonate. There are also provided pharmaceutical compositions containing any of the said novel esters.
摘要翻译：新颖的通式（I）的酯，其中是含有羧酸官能团的非甾族抗炎化合物的酰基残基。当R如上所述时，通过使酰基R-COOH与1-卤代乙基碳酸乙酯反应来制备新的酯。还提供含有任何所述新型酯的药物组合物。

3. 发明授权

US4997824A Combination of cholecalciferol derivatives for the treatment of renal bone disease 失效
标题翻译：胆钙化甾醇衍生物联合用于治疗肾脏骨病
公开(公告)号：US4997824A
公开(公告)日：1991-03-05
申请号：US76459
申请日：1987-07-22
申请人： Mordecai Popovtzer , Ben Z. Weiner , Shmuel Edelstein , Zeev Mazor , David Ladkani , Benjamin Shalita , John A. Kanis
发明人： Mordecai Popovtzer , Ben Z. Weiner , Shmuel Edelstein , Zeev Mazor , David Ladkani , Benjamin Shalita , John A. Kanis
IPC分类号： A61K31/59 , A61P3/00 , A61P13/02 , A61P15/00 , A61P43/00
CPC分类号： A61K31/59
摘要： A method and composition for an improved treatment of human renal osteodystrophy, comprising the administration of 6-40 mcg/d (micrograms per day) of 24,25(OH).sub.2 D.sub.3 in combination with amounts of 1-alpha(OH)D.sub. 3 or 1,25(OH).sub.2 D.sub.3 or DHT.sub.2, which will maintain in the serum of patients the calcium concentration at 10-11 mg/dl (milligrams per deciliter) and the phosphate concentration at 5.5-6.0 mg/dl (milligrams per deciliter) and the numerical multiplication product of calcium x phosphate not more than 60-65.

4. 发明授权

US4900814A Synthesis of podophyllotoxin derivatives 失效
标题翻译：鬼臼毒素衍生物的合成
公开(公告)号：US4900814A
公开(公告)日：1990-02-13
申请号：US943203
申请日：1986-12-15
申请人： Jeffrey Sterling , Abraham Nudelman , Jaacov Herzig , Ehud Keinan , Ben Z. Weiner
发明人： Jeffrey Sterling , Abraham Nudelman , Jaacov Herzig , Ehud Keinan , Ben Z. Weiner
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P35/00 , C07D493/04 , C07H17/04
CPC分类号： C07H17/04
摘要： There is provided a novel process for the production of the epipodophyllotoxin glycosides, Etoposide and Teniposide. There are further provided certain novel 4'-demethylepipodophyllotoxin derivatives of the following formula ##STR1## where W is hydrogen or 2,3-di-O-acetyl-4,6,O-ethylidene-D-glucopyran-1-yl. These intermediates are easily transformed into Etoposide and Teniposide and into further derivatives of this series.
摘要翻译：提供了一种生产表鬼臼毒苷，依托泊苷和替尼泊苷的新方法。还提供了下列式（IMAGE）的某些新型的4'-去甲表鬼臼毒素衍生物，其中W是氢或2,3-二-O-乙酰基-4,6，O-亚乙基-D-吡喃葡萄糖-1-基。这些中间体很容易转化成依托泊苷和替尼泊苷，并转化为该系列的其他衍生物。

5. 发明授权

US4734509A Preparation of 4(5)-hydroxymethyl-5(4)-methylimidazole 失效
标题翻译： 4（5） - 羟甲基-5（4） - 甲基咪唑的制备
公开(公告)号：US4734509A
公开(公告)日：1988-03-29
申请号：US854537
申请日：1986-04-22
申请人： Jacob Herzig , Ben Z. Weiner , Stephan Cherkez , Abraham Antebi
发明人： Jacob Herzig , Ben Z. Weiner , Stephan Cherkez , Abraham Antebi
IPC分类号： C07D233/54 , C07D233/64
CPC分类号： C07D233/64
摘要： 4(5)-Hydroxymethyl-5(4)-methylimidazole (MHI) is prepared by a process comprising the steps of:(a) reacting 4-methylimidazole (MI) with from 1.05 to 1.1 moles of formaldehyde or an equivalent amount of paraformaldehyde per mole of MI, in a concentrated aqueous NaCl solution in the presence of a catalytically effective amount of a strong inorganic base, at a temperature from about 20.degree. to about 60.degree. C.;(b) neutralizing the reaction mixture with concentrated aqueous hydrochloric acid to a pH of 8.5-8.9 to obtain a precipitate of MHI free base; and(c) separating the precipitate thus obtained from the aqueous solution and washing it with cold water or acetone.The MHI free base thus obtained can further be converted to an acid addition salt thereof.
摘要翻译： 4（5） - 羟甲基-5（4） - 甲基咪唑（MHI）通过包括以下步骤的方法制备：（a）使4-甲基咪唑（MI）与1.05-1.1摩尔甲醛或当量的多聚甲醛在约20℃至约60℃的温度下，在催化有效量的强无机碱的存在下，在浓的NaCl水溶液中，每摩尔MI。（b）用浓盐酸水溶液中和反应混合物至pH 8.5-8.9，得到游离碱的游离碱沉淀物; 和（c）从水溶液中分离由此获得的沉淀物并用冷水或丙酮洗涤。由此获得的MHI游离碱可进一步转化为其酸加成盐。

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