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1. 发明授权

US06177567B1 Method for preparing oxycodone 有权
公开(公告)号：US06177567B1
公开(公告)日：2001-01-23
申请号：US09419409
申请日：1999-10-15
申请人： Fang-Ting Chiu , Young S. Lo
发明人： Fang-Ting Chiu , Young S. Lo
IPC分类号： C07D47100
CPC分类号： C07D489/06
摘要： A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.

2. 发明授权

US5192785A Sulfamates as antiglaucoma agents 失效
标题翻译：磺胺酸盐作为抗青光眼剂
公开(公告)号：US5192785A
公开(公告)日：1993-03-09
申请号：US712855
申请日：1991-06-10
申请人： Young S. Lo , Joseph C. Nolan , Dwight A. Shamblee
发明人： Young S. Lo , Joseph C. Nolan , Dwight A. Shamblee
IPC分类号： A61K31/10 , A61K31/255 , A61K31/325 , A61K31/41 , A61K31/415 , A61K31/425 , C07D207/26 , C07D207/27 , C07D209/08 , C07D213/30 , C07D213/65 , C07D215/26 , C07D233/54 , C07D277/14 , C07D285/10 , C07D311/16 , C07D319/20 , C07D521/00
CPC分类号： C07D207/27 , A61K31/10 , A61K31/255 , A61K31/325 , A61K31/41 , A61K31/415 , A61K31/425 , C07D209/08 , C07D213/30 , C07D213/65 , C07D215/26 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/14 , C07D285/10 , C07D311/16 , C07D319/20
摘要： Sulfamate esters of the formula(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is aryloxyalkyl, p is the number of unreacted hydroxy groups present on the alkyl moiety and may be zero, z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups attached to carbons of the alkyl moiety and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy, and the like are useful in treating glaucoma.
摘要翻译：式（HO）pA- [OSO2NR1R2] z的氨基磺酸酯，其中A是芳氧基烷基，p是烷基部分上存在的未反应羟基的数目，可以是零，z是连接的-OS（O）2 NRR1R 2基团的数目至烷基部分的碳原子并且总是至少一个; R1和R2选自氢，低级烷基，羧基等可用于治疗青光眼。

3. 发明授权

US4966979A Process for synthesis of azetidine and novel intermediates therefor 失效
标题翻译：合成氮杂环丁烷的方法及其新型中间体
公开(公告)号：US4966979A
公开(公告)日：1990-10-30
申请号：US341994
申请日：1989-04-24
申请人： Young S. Lo , Dwight A. Shamblee , David H. Causey , Richard P. Mays
发明人： Young S. Lo , Dwight A. Shamblee , David H. Causey , Richard P. Mays
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.
摘要翻译：描述了一种制备氮杂环丁烷和2或3个甲基和乙基氮杂环丁烷游离碱的新方法，该方法是通过使具有适当体积的提供连接到甲基碳上的取代基的芳基甲基胺和在热的有机溶剂中在一个和三个位置上具有离去基团的合适的丙烷衍生物含有非亲核碱和一定量的足以促进氮杂环丁烷环形成的水，得到N-保护的氮杂环丁烷，并在酸性条件下通过氢解脱保护，得到氮杂环丁烷的酸性盐，然后从热的搅拌中闪蒸出氮杂环丁烷强碱溶液或浆液并冷凝，得到液氮氮杂环丁烷碱。

4. 发明授权

US4870181A Process for the preparation of 2-alkoxy-N-(1-azabicyclo[2.2.2])octan-3-yl)aminobenzamides 失效
标题翻译：制备2-烷氧基-N-（1-氮杂双环[2.2.2]）辛-3-基）氨基苯甲酰胺的方法
公开(公告)号：US4870181A
公开(公告)日：1989-09-26
申请号：US697943
申请日：1985-02-04
申请人： Young S. Lo
发明人： Young S. Lo
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A process for the preparation of 2-alkoxy-N-(1-azabicyclo[2.2.2]octan-3-yl)aminobenzamides, which are gastric pharmaceuticals in monogastric animals having the formula: ##STR1## wherein R is hydrogen or loweralkyl, R.sup.1 is loweralkyl,R.sup.2 is hydrogen, halo or loweralkoxy,Am is amino, methylamino or dimethylaminois disclosed wherein in the initial step an appropriate monoprotonated 3-aminoquinuclidine strong acid salt and an appropriate amino benzoic acid all in a 50-90 vol. % pyridine in water solution are reacted in the presence of N,N'-dialkylcarbodiimide. The free base may be obtained by conventional procedures from the mixtures with minimal purification effort.
摘要翻译：在单胃动物中制备2-烷氧基-N-（1-氮杂双环[2.2.2]辛-3-基）氨基苯甲酰胺的方法，其为具有下式的单胃动物：其中R为氢或低级烷基， R 1是低级烷基，R 2是氢，卤素或低级烷氧基，Am是氨基，甲基氨基或二甲基氨基，其中在初始步骤中，合适的单质子化的3-氨基奎宁环酸强酸盐和适当的氨基苯甲酸都在50-90vol。％吡啶水溶液在N，N'-二烷基碳二亚胺的存在下反应。游离碱可以通过常规方法从混合物中以最少的纯化力获得。

5. 发明授权

US4456755A 7-Oxygen analogs of cephalosporins 失效
标题翻译：头孢菌素的7-氧类似物
公开(公告)号：US4456755A
公开(公告)日：1984-06-26
申请号：US494507
申请日：1974-08-05
申请人： John C. Sheehan , Young S. Lo
发明人： John C. Sheehan , Young S. Lo
IPC分类号： C07D501/00 , A61K31/545
CPC分类号： C07D501/00 , Y02P20/55
摘要： In accordance with this invention, it has been found that the oxygen analog of 7-aminocephalosporanic acid and biologically active derivatives thereof can be formed from esters of 7-aminocephalosporanic acid. Esters of 7-oxocephalosporanic acid can be formed by diazotization of an ester of 7-aminocephalosporanic acid and contact of the diazo compound so formed with a hypohalous acid and a base in a water miscible organic solvent. Oxygen analogs of 7-aminocephalosporins isolated as esters are then formed by reducing the aforesaid ester to the corresponding 7.beta.-hydroxy-cephalosporanate and then forming the desired analog by introduction of a side chain via hydroxyl group modification. Oxygen analogs of 7-aminocephalosporins are then formed by regeneration of the acid via protective group removal.
摘要翻译：根据本发明，已经发现7-氨基头孢烷酸的氧类似物及其生物活性衍生物可以由7-氨基头孢烷酸的酯形成。 7-氧代头孢烷酸的酯可以通过7-氨基头孢烷酸的酯的重氮化和与水混溶的有机溶剂中与次卤酸和碱形成的重氮化合物的接触形成。然后通过将上述酯还原成相应的7β-羟基 - 头孢菌素，然后通过羟基改性引入侧链形成所需的类似物，形成作为酯分离的7-氨基头孢菌素的氧类似物。然后通过去除保护基团再生酸形成7-氨基头孢菌素的氧类似物。

6. 发明授权

US4282149A Carbon and oxygen analogs of penicillin 失效
标题翻译：青霉素的碳和氧类似物
公开(公告)号：US4282149A
公开(公告)日：1981-08-04
申请号：US946438
申请日：1978-09-27
申请人： John C. Sheehan , Young S. Lo
发明人： John C. Sheehan , Young S. Lo
IPC分类号： C07C45/00 , C07D499/00 , C07F9/535 , C07F9/54
CPC分类号： C07F9/5352 , C07C45/00 , C07D499/00 , C07F9/5407
摘要： In accordance with this invention, it has been found that carbon and oxygen analogs of 6.beta.-aminopenicillanic acid and biologically active derivatives thereof can be formed from esters of 6-oxopenicillanic acid. For example, 6.beta.-phenoxyacetoxy-penicillanic acid--an oxygen analog of penicillin V and 6.beta.-phenoxyacetylmethylpenicillanic acid--a carbon analog of penicillin V, may be formed from an ester of 6-oxopenicillanate. The ester of 6-oxopenicillanic acid is formed by a diiospropyl carbodiimide/dimethyl sulfoxide oxidation of the corresponding ester of 6.alpha.-hydroxypenicillanic acid. The oxygen analogs are formed by reducing the ester of 6-oxopenicillanic acid to the corresponding 6.beta.-hydroxypenicillanate and then forming the desired analog by acylation. The carbon analogs are formed by a Wittig reaction of the ester of 6-oxopenicillanic acid with a suitable acylmethylenetriphenylphosphorane followed by saturation of the newly formed double bond and removal of the protective ester group.
摘要翻译：根据本发明，已经发现6β-氨基青霉烷酸的碳和氧类似物及其生物活性衍生物可以由6-氧代青霉烷酸的酯形成。例如，可以由6-氧代青霉烷酸酯形成6β-苯氧基乙酰氧基 - 青霉烷酸 - 青霉素V的氧类似物和6β-苯氧基乙酰基甲基青霉烷酸 - 青霉素V的碳类似物。 6-氧代青霉烷酸的酯由6α-羟基青霉烷酸的相应酯的二亚丙基碳二亚胺/二甲基亚砜氧化形成。通过将6-氧代青霉烷酸的酯还原成相应的6β-羟基青霉烷酸形成氧类似物，然后通过酰化形成所需的类似物。碳类似物通过6-氧代青霉烷酸的酯与合适的酰基亚甲基三苯基正膦的维蒂希反应形成，接着饱和新形成的双键并除去保护酯基。

7. 发明授权

US5273993A Compounds having one or more aminosulfonyloxy radicals useful as pharmaceuticals 失效
标题翻译：具有一个或多个可用作药物的氨基磺酰氧基的化合物
公开(公告)号：US5273993A
公开(公告)日：1993-12-28
申请号：US965140
申请日：1992-11-19
申请人： Young S. Lo , Joseph C. Nolan , William J. Welstead, Jr. , David A. Walsh , Dwight A. Shamblee , Ibrahim M. Uwaydah
发明人： Young S. Lo , Joseph C. Nolan , William J. Welstead, Jr. , David A. Walsh , Dwight A. Shamblee , Ibrahim M. Uwaydah
IPC分类号： A61K31/255 , A61K31/33 , C07C307/02 , C07D207/26 , C07D207/27 , C07D209/08 , C07D211/22 , C07D213/65 , C07D215/26 , C07D233/54 , C07D277/24 , C07D277/28 , C07D285/10 , C07D311/16 , C07D319/20 , C07D521/00 , C07H11/00 , A61K31/415
CPC分类号： C07D207/27 , A61K31/255 , A61K31/33 , C07C307/02 , C07D209/08 , C07D211/22 , C07D213/65 , C07D215/26 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/24 , C07D277/28 , C07D285/10 , C07D311/16 , C07D319/20 , C07H11/00
摘要： Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.
摘要翻译：治疗慢性关节炎和骨质疏松症的方法，其利用了下列通式所示的已知和新型化合物：（HO）pA - [ - OS（O）2NR1R2] z其中A包括宽范围的值，包括但不限于芳基，低级烷基，环烷基和碳水化合物，包括蔗糖和果糖; p等于分子上包含的未反应羟基的数目，可以为零; z是-OS（O）2NR1R2基团的数目，并且总是至少一个; R1和R2选自氢，低级烷基，羧基等; 提供了一种制备该化合物的新方法，其中将适当的氨基磺酸芳基酯与羟基取代的A基团反应，羟基取代的A基团可含有或不含有保护的羧基，氨基或羟基取代基，在含有叔胺碱的非质子溶剂中。还提供了用于治疗慢性关节炎和骨质疏松症的药物组合物。

8. 发明授权

US5206374A Process for preparing tetrazolylphenylboronic acid intermediates 失效
标题翻译：四唑基苯基硼酸中间体的制备方法
公开(公告)号：US5206374A
公开(公告)日：1993-04-27
申请号：US911813
申请日：1992-07-10
申请人： Young S. Lo
发明人： Young S. Lo
IPC分类号： C07F5/02 , C07F5/05
CPC分类号： C07F5/05 , C07F5/025
摘要： Method for the preparation of novel tetrazolyphenylboronic acids such as the compound 2-(2'-triphenylmethyl-2'H-tetrazol-5'-yl)phenylboronic acid.
摘要翻译：制备新型四唑基苯基硼酸如化合物2-（2'-三苯基甲基-2'H-四唑-5'-基）苯基硼酸的方法。

9. 发明授权

US5183903A Urea fusion process for the synthesis of 3-phenoxy-1-azetidinecarboxamides 失效
标题翻译：用于合成3-苯氧基-1-氮杂环丁烷甲酰胺的尿素融合方法
公开(公告)号：US5183903A
公开(公告)日：1993-02-02
申请号：US798674
申请日：1991-11-26
申请人： William J. Welstead, Jr. , Young S. Lo
发明人： William J. Welstead, Jr. , Young S. Lo
IPC分类号： A61K31/395 , A61K31/397 , A61P25/08 , C07D205/04
CPC分类号： C07D205/04
摘要： This invention relates to an improved process for the preparation of 3-phenoxy-1-azetidinecarboxamides of Formula I which are useful ##STR1## in the treatment of epileptic seizures. Under Formula I, n is 1 to 3, X is H, halogen, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, acetyl, or aminocarbonyl, and R is H or methyl. This process involves heating a 3-phenoxyazetidine with urea to obtain the Formula I compound. Urea is inexpensive and easily removed by washing the solid Formula I product with water.

10. 发明授权

US5025031A Aryl and aryloxyalkyl sulfamate esters useful as anticonvulsants 失效
标题翻译：用作抗惊厥药的芳基和芳氧基烷基氨基磺酸酯酯
公开(公告)号：US5025031A
公开(公告)日：1991-06-18
申请号：US443146
申请日：1989-11-30
申请人： Young S. Lo , David A. Walsh , Ibrahim M. Uwaydah
发明人： Young S. Lo , David A. Walsh , Ibrahim M. Uwaydah
IPC分类号： A61K31/255 , A61K31/415 , C07C307/02 , C07D215/26 , C07D233/22 , C07D233/54 , C07D285/10 , C07D311/18 , C07D521/00
CPC分类号： C07D233/64 , A61K31/255 , A61K31/415 , C07C307/02 , C07D215/26 , C07D231/12 , C07D233/22 , C07D233/56 , C07D249/08 , C07D285/10 , C07D311/18
摘要： Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula:(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO.sub.2 NR.sup.1 R.sup.2) wherein R.sup.1 and R.sup.2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O.sub.2)NR.sup.1 R.sup.2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.
摘要翻译：本文公开了一种用药物组合物治疗惊厥的方法，所述药物组合物含有下式化合物：（HO）pA- [OSO 2 NR 1 R 2] z，其中A是芳基，芳基烷基或芳氧基烷基，并被一个或多个碳原子取代，氨基磺酸酯基（-OSO2NR1R2）其中R1和R2相同或不同，为氢或低级烷基，其中p为0或1，为未经处理的羟基数，z为1或2，为-OS（O 2）NR 1 R 2的数目团体芳基选自苯基，取代的苯基，吡啶基，萘基，喹啉基等。苯基取代基选自氢，卤素，羟基，苯基，苯氧基，苯甲酰基，低级烷基，低级烷氧基，羧基，氨基，低级烷基氨基，二低级烷基氨基，乙酰氨基，氰基，硝基，低级烷氧基羰基，氨基磺酰基，咪唑基，三唑基等。还描述了以前未公开的新型化合物。

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