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1. 发明授权

US06469170B1 Method for preparing oxycodone 有权
公开(公告)号：US06469170B1
公开(公告)日：2002-10-22
申请号：US10152140
申请日：2002-05-21
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

US5194446A Compounds having one or more aminosulfaonyloxy radicals useful as pharmaceuticals 失效
标题翻译：具有一个或多个氨基磺酰氧基的化合物可用作药物
公开(公告)号：US5194446A
公开(公告)日：1993-03-16
申请号：US734846
申请日：1991-07-24
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 , C07D277/14 , C07D277/24 , C07D277/28 , C07D285/10 , C07D311/16 , C07D319/20 , C07D521/00 , C07H11/00
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 , C07D277/14 , C07D277/24 , C07D277/28 , C07D285/10 , C07D311/16 , C07D319/20 , C07H11/00 , Y10S514/825
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。

3. 发明授权

US4990683A Process for preparing 3-pyrrolidinols 失效
标题翻译：制备3-吡咯烷醇的方法
公开(公告)号：US4990683A
公开(公告)日：1991-02-05
申请号：US141740
申请日：1988-01-11
申请人： Young S. Lo
发明人： Young S. Lo
IPC分类号： C07C255/12 , C07D207/12
CPC分类号： C07C255/00 , C07D207/12
摘要： A novel process is disclosed for the preparation of 3-pyrrolidinol compounds selected from the group having the formula: ##STR1## wherein: R is selected from hydrogen, loweralkyl, loweralkenyl, cycloalkyl, cycloalkyl-loweralkyl, phenyl-loweralkyl and substituted phenyl-loweralkyl; R.sup.1, R.sup.2, and R.sup.3 are selected from hydrogen, loweralkyl, and loweralkenyl; and the optical isomers thereof. In the process, 4-amino-3-hydroxybutyronitriles are reductively cyclized with Raney nickel to produce the 3-pyrrolidinol compound.
摘要翻译：公开了一种制备选自下列基团的3-吡咯烷醇化合物的新方法：其中：R选自氢，低级烷基，低级烯基，环烷基，环烷基 - 低级烷基，苯基 - 低级烷基和取代的苯基 - 低级烷基 ; R1，R2和R3选自氢，低级烷基和低级烯基; 及其旋光异构体。在此过程中，4-氨基-3-羟基亚丁腈与阮内镍还原环化生成3-吡咯烷醇化合物。

4. 发明授权

US4870189A 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：US4870189A
公开(公告)日：1989-09-26
申请号：US7596
申请日：1987-01-28
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.

5. 发明授权

US4628100A Intermediates for the preparation of aryl substituted pyrido[1,4]benzodiazepines 失效
标题翻译：用于制备芳基取代的吡啶并[1,4]苯并二氮杂卓的中间体
公开(公告)号：US4628100A
公开(公告)日：1986-12-09
申请号：US748790
申请日：1985-06-26
申请人： Young S. Lo
发明人： Young S. Lo
IPC分类号： C07D213/74 , C07D471/04 , C07D213/75
CPC分类号： C07D213/74 , C07D471/04
摘要： Intermediates for preparing pyrido [1,4] benzodiazepines having antidepressant activity are disclosed of the formula ##STR1## wherein, R is hydrogen, loweralkyl, --alk.sup.1 --NR.sup.1 R.sup.2, --alk.sup.1 --N.dbd.CH--OC.sub.2 H.sub.5 or ##STR2## R.sup.1 and R.sup.2 are loweralkyl, --C(O)--O--loweralkyl or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom may form a 1-piperidinyl, 1-phthalimido, 1-pyrrolidinyl, 4-morpholino, 1-piperazinyl or 4-substituted-1-piperazinyl;Ar is 2, 3 or 4-pyridinyl, 2 or 3-thienyl, phenyl or phenyl substituted by 1 to 3 radicals selected from halo, loweralkyl, loweralkoxy, trifluoromethyl or nitro and may be the same or different;alk.sup.1 is a straight or branched hydrocarbon chain containing 1-8 carbon atoms;Z is hydrogen, halogen, loweralkyl, loweralkoxy, hydroxy or nitro;Y is hydrogen or 1-2 radicals selected from loweralkyl, loweralkoxy or hydroxy and may be the same or different,and the acid addition salts thereof.
摘要翻译：公开了具有抗抑郁活性的吡啶并[1,4]苯并二氮杂的中间体，其中R为氢，低级烷基，-alk1-NR1R2，-alk1-N = CH-OC2H5或R1和R2为低级烷基，-C（O）-O-低级烷基或R 1和R 2与相邻氮原子一起可以形成1-哌啶基，1-邻苯二甲酰亚氨基，1-吡咯烷基，4-吗啉代，1-哌嗪基或4-取代-1 哌嗪基 Ar是2,3或4-吡啶基，2或3-噻吩基，苯基或被1至3个选自卤素，低级烷基，低级烷氧基，三氟甲基或硝基的基团取代的苯基，可以相同或不同; alk1是含有1-8个碳原子的直链或支链烃链; Z是氢，卤素，低级烷基，低级烷氧基，羟基或硝基; Y是氢或选自低级烷基，低级烷氧基或羟基的1-2个基团，并且可以相同或不同，及其酸加成盐。

6. 发明授权

US4610819A Process for the preparation of aromatic-1,4-oxazepinones and thiones 失效
标题翻译：制备芳香-1,4-氧氮杂和硫堇的方法
公开(公告)号：US4610819A
公开(公告)日：1986-09-09
申请号：US652017
申请日：1984-09-19
申请人： Young S. Lo , Albert D. Cale, Jr.
发明人： Young S. Lo , Albert D. Cale, Jr.
IPC分类号： A61K31/55 , A61P43/00 , C07D213/80 , C07D213/82 , C07D267/14 , C07D498/04 , C07D281/10 , C07D413/06 , C07D417/06 , C07D513/04
CPC分类号： C07D213/80 , C07D213/82 , C07D267/14
摘要： A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.
摘要翻译：制备具有下式的1,4-氧杂氮杂酮和硫杂的方法：其中A是选自苯，萘，喹啉或吡啶的芳环; n为1〜3; Z是氨基; R是氢，低级烷基，环烷基或苯基低级烷基; 并且R4和R5是氢，并且公开了从氯代芳族羧酸盐和链烷醇胺开始的低级烷基。

7. 发明授权

US4361514A Carbon analogs of penicillin 失效
标题翻译：青霉素的碳类似物
公开(公告)号：US4361514A
公开(公告)日：1982-11-30
申请号：US234979
申请日：1981-02-17
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 , A61K31/425
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.
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。

8. 发明授权

US07282583B2 Process for making 5,11-Dihydro-11-ethyl-5-methyl-8{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-di pyrido[3,2-b:2′,3′-e][1,4]diazepin-6-one 有权
标题翻译：制备5,11-二氢-11-乙基-5-甲基-8（2 - {（1-氧代-4-喹啉基）氧基}乙基} -6H-二吡啶并[3,2-b：2' 3'-e] [1,4]二氮杂-6-酮
公开(公告)号：US07282583B2
公开(公告)日：2007-10-16
申请号：US11560536
申请日：2006-11-16
申请人： Saeed Ahmad , Robert Frederick Boswell, Jr. , Jack Delbert Brown , Cary Mark Davis , Kai Oliver Donsbach , Bernard Franklin Gupton , Christopher Peter Johnson, III , Ahmad Khodabocus , Vithalanand R. Kulkarni , Young S. Lo
发明人： Saeed Ahmad , Robert Frederick Boswell, Jr. , Jack Delbert Brown , Cary Mark Davis , Kai Oliver Donsbach , Bernard Franklin Gupton , Christopher Peter Johnson, III , Ahmad Khodabocus , Vithalanand R. Kulkarni , Young S. Lo
IPC分类号： C07D471/14 , C07D215/16 , C07D211/72 , C07D211/84
CPC分类号： C07D471/14 , C07D213/80 , C07D401/12 , C07D401/14
摘要： An improved process for making 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-di pyrido[3,2-b:2′,3′-e][1,4]diazepin-6-one.
摘要翻译：制备5,11-二氢-11-乙基-5-甲基-8- {2 - {（1-氧代-4-喹啉基）氧基}乙基} -6H-二吡啶并[3,2-b： 2'，3'-e] [1,4]二氮杂-6-酮。

9. 发明授权

US06262266B1 Method for preparing oxycodone 有权
公开(公告)号：US06262266B1
公开(公告)日：2001-07-17
申请号：US09667997
申请日：2000-09-22
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.

10. 发明授权

US5130439A Tetrazolylphenylboronic acid intermediates for the synthesis of AII receptor antagonists 失效
标题翻译：四唑基苯基硼酸中间体用于合成AII受体拮抗剂
公开(公告)号：US5130439A
公开(公告)日：1992-07-14
申请号：US793514
申请日：1991-11-18
申请人： Young S. Lo , Lucius T. Rossano
发明人： Young S. Lo , Lucius T. Rossano
IPC分类号： C07F5/02 , C07F5/05
CPC分类号： C07F5/025 , C07F5/05
摘要： Novel tetrazolylphenylboronic acids, methods for their preparation, and their use in the syntheses of angiotensin II receptor antagonists are disclosed.
摘要翻译：公开了新型四唑基苯基硼酸，其制备方法及其在合成血管紧张素II受体拮抗剂中的用途。

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