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11. 发明授权

US4749788A Process for the preparation of aryl-pyrido(1,4) benzodiazepines 失效
标题翻译：芳基 - 吡啶并（1,4）苯并二氮杂的制备方法
公开(公告)号：US4749788A
公开(公告)日：1988-06-07
申请号：US37794
申请日：1987-04-13
申请人： Young S. Lo , William J. Welstead, Jr.
发明人： Young S. Lo , William J. Welstead, Jr.
IPC分类号： C07D213/75 , C07D405/12 , C07D471/04
CPC分类号： C07D213/75 , C07D471/04
摘要： A process is described wherein pyrido[1,4]benzodiazepines having the formula: ##STR1## wherein Q is NR.sup.1 R.sup.2 or ##STR2## are prepared from unsubstituted pyridobenzodiazepinones by alkylation reaction with halo-alkyl-Q followed by acylation of the other nitrogen; breaking the ring with an aryl Grignard reagent and recyclizing to add the aryl radical and form the azepine ring. Novel intermediates are thereby disclosed.

12. 发明授权

US4622394A Oxygen analogs of cephalosporins 失效
标题翻译：头孢菌素的氧类似物
公开(公告)号：US4622394A
公开(公告)日：1986-11-11
申请号：US856749
申请日：1977-12-02
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-amino-cephalosporanic acid and biologically active derivatives thereof can be formed from esters of 7-amino-cephalosporanic acid. Esters of 7-oxocephalosporanic acid can be formed by diazotization of an ester or 7-amino-cephalosporanic 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-amino-cephalosporins 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酯或7-氨基 - 头孢烷酸的重氮化形成，并且在与水混溶的有机溶剂中与次卤酸和碱形成的重氮化合物接触。然后通过将上述酯还原成相应的7β-羟基 - 头孢菌素形成通过羟基修饰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来形成7-氨基 - 头孢菌素的氧类似物。

13. 发明授权

US4518603A [2-[(Nitropyridinyl)amino]phenyl]arylmethanones in a process for preparing pyrido[1,4]benzodiazepines 失效
标题翻译： [2 - [（硝基吡啶基）氨基]苯基]芳基甲酮在制备吡啶并[1,4]苯并二氮杂
公开(公告)号：US4518603A
公开(公告)日：1985-05-21
申请号：US541215
申请日：1983-12-23
申请人： Young S. Lo , Chandler R. Taylor, Jr.
发明人： Young S. Lo , Chandler R. Taylor, Jr.
IPC分类号： C07D213/74 , C07D471/04 , A61K31/38 , A61K31/40 , A61K31/44 , A61K31/495
CPC分类号： C07D213/74 , C07D471/04
摘要： [2-[(Nitropyridinyl)amino]phenyl]arylmethanones as chemical intermediates and/or having antidepressant activity having the formula: ##STR1## wherein; B is carbonyl, thioxomethyl, ketal or thioketal,R is hydrogen or --alk.sup.1 -Q,Q is hydrogen, --NR.sup.1 R.sup.2 or halogen are disclosed in a process for preparing pyrido[1,4]benzodiazepines.
摘要翻译： [2 - [（硝基吡啶基）氨基]苯基]芳基甲酮作为化学中间体和/或具有下式的抗抑郁活性：其中： B是羰基，硫代甲基，缩酮或硫缩酮，R是氢或-alk1-Q，Q是氢，-NR1R2或卤素在制备吡啶并[1,4]苯并二氮杂的方法中公开。

14. 发明授权

US4143046A Carbon and oxygen analogs of penicillin 失效
标题翻译：苯并咪唑的碳和氧气类似物
公开(公告)号：US4143046A
公开(公告)日：1979-03-06
申请号：US779828
申请日：1977-03-21
申请人： John C. Sheehan , Young S. Lo
发明人： John C. Sheehan , Young S. Lo
IPC分类号： C07D499/32 , A61K31/43 , A61P31/04 , C07C45/00 , C07D499/00 , C07D499/86 , C07D499/861 , C07D499/87 , C07D499/897 , C07F9/535 , C07F9/54 , C07D277/04
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.-phenoxyacetoxypenicillanic 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.

15. 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。

16. 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。

17. 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.

18. 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。

19. 发明授权

US4594189A Process for preparing 3-phenoxy-1-azetidines and carboxamide derivatives 失效
标题翻译：制备3-苯氧基-1-氮杂环丁烷和羧酰胺衍生物的方法
公开(公告)号：US4594189A
公开(公告)日：1986-06-10
申请号：US511077
申请日：1983-07-06
申请人： Young S. Lo , Richard P. Mays
发明人： Young S. Lo , Richard P. Mays
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： An improved process is disclosed for preparing 3-phenoxyazetidines which utilizes a phase transfer catalyst to add the phenoxy group to azetidine blocked in the 1-position by a diphenylmethane group and utilizes a stabilizing tertiary amine base to prevent dimerization during hydrogenolysis to remove the blocking group. The crude product containing diphenylmethane may be used without purification to prepare 3-phenoxy-1-azetidinecarboxamides.
摘要翻译：公开了一种改进的制备3-苯氧基氮杂环丁烷的方法，其使用相转移催化剂将苯氧基加成到通过二苯基甲烷基在1位上被氮杂环丁烷封端的氮杂环丁烷，并利用稳定的叔胺碱来防止在氢解期间的二聚化以除去封闭基团。含有二苯基甲烷的粗产物可以不经纯化用于制备3-苯氧基-1-氮杂环丁烷甲酰胺。

20. 发明授权

US4480100A [2-[(Nitropyridinyl)amino]phenyl]arymethanones 失效
标题翻译： [2 - [（硝基吡啶基）氨基]苯基]芳甲酮
公开(公告)号：US4480100A
公开(公告)日：1984-10-30
申请号：US431997
申请日：1982-09-30
申请人： Young S. Lo , Chandler R. Taylor, Jr.
发明人： Young S. Lo , Chandler R. Taylor, Jr.
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4433 , A61P25/24 , A61P25/26 , C07D213/74 , C07D409/12 , C07D471/04 , C07D213/61
CPC分类号： C07D213/74 , C07D471/04
摘要： [2-[(Nitropyridinyl)amino]phenyl]arylmethanones as chemical intermediates and/or having antidepressant activity having the formula: ##STR1## wherein: B is carbonyl, thioxomethyl, ketal or thioketal,R is hydrogen or -alk.sup.1 -Q,Q is hydrogen, --NR.sup.1 R.sup.2 or halogenare disclosed in a process for preparing pyrido[1,4]benzodiazepines.
摘要翻译： [2 - [（硝基吡啶基）氨基]苯基]芳基甲酮作为化学中间体和/或具有下式的抗抑郁活性：其中：B为羰基，硫代甲基，缩酮或硫缩酮，R为氢或-alk1-Q，Q 在制备吡啶并[1,4]苯并二氮杂的方法中公开了-NR1R2或卤素。

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