专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US4885364A Resolution process for benzazepine intermediates 失效
标题翻译：苯并氮杂中间体的拆分方法
公开(公告)号：US4885364A
公开(公告)日：1989-12-05
申请号：US275493
申请日：1988-11-23
申请人： John K. Thottathil
发明人： John K. Thottathil
IPC分类号： C07D223/16 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D417/00
CPC分类号： C07D223/16 , Y02P20/582
摘要： In accordance with the present invention an improved process for preparing resolved compounds of the formula ##STR1## being the cis(+) isomer, is disclosed, wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, diarylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, ##STR2## fluoro substituted alkoxy, fluoro substituted alkyl, (cycloalkyl)alkoxy --NO.sub.2, NX.sub.3 X.sub.4, --S(O).sub.m alkyl, ##STR3## m is 0, 1 or 2; X.sub.1 and X.sub.2 are each independently hydrogen, alkyl, aryl or heteroaryl, or X.sub.1 and X.sub.2 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl;X.sub.3 and X.sub.4 are each independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or ##STR4## X.sub.5 is hydroxy, alkoxy, aryloxy, amino, alkylamino or dialkylamino; andX.sub.6 is alkyl, alkoxy or aryloxy; with the proviso that if R.sub.4 is a 7-alkyl group, it must have a tertiary carbon atom bonded to the ring.

42. 发明授权

US4740332A Process for preparing phosphonous acids 失效
标题翻译：制备膦酸的方法
公开(公告)号：US4740332A
公开(公告)日：1988-04-26
申请号：US4513
申请日：1987-01-20
申请人： John K. Thottathil
发明人： John K. Thottathil
IPC分类号： C07F9/48
CPC分类号： C07F9/48
摘要： A process is provided for preparing phosphonous acids of the structure wherein R.sub.1 is lower alkyl or arylalkyl ##STR1## which are useful in preparing phosphinic and phosphonic acid ACE inhibitors, which process includes the steps of treating an olefin of the structure R.sub.1 --CH.dbd.CH.sub.2 wherein R.sub.2 is lower alkyl or arylalkyl with a phosphorus-containing reagent such as sodium hypophosphite or hypophosphorous acid in the presence of an organic alcohol solvent such as ethanol or methanol, and a radical initiator such as azobisisobutyronitrile, under acidic conditions, preferably at the reflux temperature of the organic solvent, to form the phosphonous acid without forming the alkyl ester.
摘要翻译：提供了一种用于制备结构中的膦酸的方法，其中R1是可用于制备次膦酸和膦酸ACE抑制剂的低级烷基或芳基烷基，该方法包括以下步骤：处理结构R1-CH = CH2 其中R2在有机醇溶剂如乙醇或甲醇存在下，和诸如偶氮二异丁腈的自由基引发剂，优选在回流下使用含磷试剂如次磷酸钠或次磷酸，其中R 2为低级烷基或芳烷基有机溶剂的温度，形成不形成烷基酯的膦酸。

43. 发明授权

US4670193A Process for preparing phosphonic acids 失效
标题翻译：制备膦酸的方法
公开(公告)号：US4670193A
公开(公告)日：1987-06-02
申请号：US861795
申请日：1986-05-12
申请人： John K. Thottathil
发明人： John K. Thottathil
IPC分类号： C07F9/38 , C07F9/40
CPC分类号： C07F9/4087 , C07F9/38 , C07F9/4075
摘要： A process for preparing phosphonic acids of the structure ##STR1## wherein R.sub.1 is lower alkyl, aryl, cycloalkyl or arylalkyl, and R.sub.2 is H, benzyl or ##STR2## by oxidizing the corresponding phosphonous acid ##STR3## employing as the oxidizing agent potassium permanganate or sodium periodate.
摘要翻译：制备结构为“IMAGE”的膦酸的方法，其中R 1为低级烷基，芳基，环烷基或芳基烷基，R 2为H，苄基或者通过氧化相应的膦酸作为氧化剂高锰酸钾或高碘酸钠。

44. 发明授权

US4625038A (25-trans)-4-substituted-2-pyrrolidines-methanols 失效
标题翻译：（25-反式）-4-取代-2-吡咯烷子 - 甲醇
公开(公告)号：US4625038A
公开(公告)日：1986-11-25
申请号：US812701
申请日：1985-12-23
申请人： John K. Thottathil
发明人： John K. Thottathil
IPC分类号： C07D207/08 , C07D207/16 , C07D498/04
CPC分类号： C07D207/08 , C07D207/16
摘要： Disclosed herein are novel chemical intermediates having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl, aryl or arylalkyl.
摘要翻译：本文公开了具有式“IMAGE”的新型化学中间体，其中R 1是烷基，环烷基，芳基或芳基烷基。

45. 发明授权

US4594199A Method for making phosphinic acid intermediates 失效
标题翻译：制备次膦酸中间体的方法
公开(公告)号：US4594199A
公开(公告)日：1986-06-10
申请号：US693419
申请日：1985-01-22
申请人： John K. Thottathil
发明人： John K. Thottathil
IPC分类号： C07F9/30 , C07F9/32 , C07F9/572 , C07F9/62 , C07F9/65
CPC分类号： C07F9/62 , C07F9/301 , C07F9/303 , C07F9/304 , C07F9/306 , C07F9/3211 , C07F9/3223 , C07F9/3241 , C07F9/5721 , C07F9/5728
摘要： A method is provided for preparing phosphinic acid prodrug intermediates which are useful in preparing phosphinic acid angiotensin-converting enzyme inhibitors which method includes the step of coupling a phosphonous acid or its ester of the structure ##STR1## wherein R is H or lower alkyl and R.sup.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl, with a conjugated compound of the structure ##STR2## wherein R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each is independently H, lower alkyl or aryl, and Z is --CO.sub.2 R.sup.5 (wherein R.sup.5 is H or lower alkyl), ##STR3## (wherein R.sup.6 is H, lower alkyl aryl or arylalkyl), ##STR4## (wherein R.sup.7 and R.sup.8 are the same or different and are selected from the group consisting of H, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkylalkyl and at least one of R.sup.7 and R.sup.8 is other than H, or R.sup.7 and R.sup.8 can be taken together with N to form a 5-, 6- or 7-membered heterocyclic ring ##STR5## which may or may not include a COOR.sup.5 substituent, which 5- or 6-membered N-containing ring may or may not be fused to an aryl ring), in the presence of a silylating agent, to form the phosphonic acid intermediate of the structure ##STR6## wherein R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 and Z are as defined above.
摘要翻译：提供了用于制备次膦酸前体药物中间体的方法，其可用于制备次膦酸血管紧张素转换酶抑制剂，该方法包括使结构式“IMAGE”的膦酸或其酯偶联的步骤，其中R是H或低级烷基和R1 与低级烷基，芳基，芳基烷基，环烷基或环烷基烷基的结合，与结构为“IMAGE”的共轭化合物，其中R2，R3和R4可以相同或不同，并且各自独立地为H，低级烷基或芳基，Z为-CO 2 R 5 （其中R 5为H或低级烷基），其中R 6为H，低级烷基芳基或芳烷基，其中R 7和R 8相同或不同，选自H，低级烷基，芳基，芳基 - 低级烷基，环烷基或环烷基烷基，并且R 7和R 8中的至少一个不是H，或者R 7和R 8可与N一起形成5-，6-或7-元杂环， IMAGE>其可以包括或不包括COOR5取代基，其5-或6 在甲硅烷基化剂的存在下，在甲硅烷基化剂存在下，形成其中R，R 1，R 2，R 3和R 4以及Z的结构的膦酸中间体如上所述。

46. 发明授权

US11020386B2 Methods and compositions for preventing opioid abuse 有权
公开(公告)号：US11020386B2
公开(公告)日：2021-06-01
申请号：US15431624
申请日：2017-02-13
申请人： Albany Molecular Research, Inc. , John K. Thottathil
发明人： Matthew Surman , Kathryn Golden , Paolo Pasetto , Xiaomin Jin , Xiaowu Jiang , Fatoumata Camara , John K. Thottathil
IPC分类号： A61K31/485 , C07D489/08 , A61K47/54
摘要： Abuse-resistant opioid compounds, drug delivery systems, pharmaceutical compositions comprising an opioid covalently bound to a chemical moiety are provided. Methods of delivering an active ingredient to a subject and methods of preventing opioid abuse are also provided.

47. 发明申请

US20170157116A1 METHODS AND COMPOSITIONS FOR PREVENTING OPIOID ABUSE 审中-公开
公开(公告)号：US20170157116A1
公开(公告)日：2017-06-08
申请号：US15431572
申请日：2017-02-13
申请人： John K. Thottathil , Albany Molecular Research, Inc.
发明人： Matthew Surman , John K. Thottathil , Kathryn Golden , Paolo Pasetto , Xiaomin Jin , Xiaowu Jiang , Fatoumata Camara
IPC分类号： A61K31/485 , C07D489/08
CPC分类号： A61K31/485 , A61K47/542 , C07D489/08
摘要： Abuse-resistant opioid compounds, drug delivery systems, pharmaceutical compositions comprising an opioid covalently bound to a chemical moiety are provided. Methods of delivering an active ingredient to a subject and methods of preventing opioid abuse are also provided.

48. 发明申请

US20120004429A1 Taxane Compounds, Compositions And Methods 有权
标题翻译：紫杉烷化合物，组合物和方法
公开(公告)号：US20120004429A1
公开(公告)日：2012-01-05
申请号：US13170830
申请日：2011-06-28
申请人： John K. Thottathil , Raymond P. Warrell, JR.
发明人： John K. Thottathil , Raymond P. Warrell, JR.
IPC分类号： C07D317/70
CPC分类号： C07D493/08 , C07D205/08 , C07D305/14 , C07D401/04 , C07D407/02
摘要： The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
摘要翻译：本发明提供了一种制备口服可用的五环紫杉烷化合物的方法，以及可用于其制备的中间体。

49. 发明授权

US06365750B1 Methods for the preparation of taxanes using oxazolidine intermediates 失效
标题翻译：使用恶唑烷中间体制备紫杉烷的方法
公开(公告)号：US06365750B1
公开(公告)日：2002-04-02
申请号：US09315712
申请日：1999-05-20
申请人： John K. Thottathil , Ivan D. Trifunovich
发明人： John K. Thottathil , Ivan D. Trifunovich
IPC分类号： C07D26306
CPC分类号： C07D263/04 , C07C233/87 , C07D305/14 , C07D413/12 , C07F7/1892
摘要： Novel oxazolidines finding utility as intermediates in the preparation of C-13 acyloxy sidechain-bearing taxanes such as paclitaxel and analogs thereof. The present invention also relates to novel methods of coupling the oxazolidines to form the aforementioned taxanes, and to methods of preparing the oxazolidines.
摘要翻译：在制备C-13酰氧基侧链紫杉烷如紫杉醇及其类似物时，新型恶唑烷可用作中间体。本发明还涉及偶联恶唑烷以形成上述紫杉烷的新方法，以及制备恶唑烷的方法。

50. 发明授权

US5869734A Preparation of optically active (S)-(-) and (R)-(+)-deoxyspergualin and novel intermediates thereof 失效
标题翻译：光学活性（S） - （ - ）和（R） - （+） - 脱氧精胍菌素的制备及其新型中间体
公开(公告)号：US5869734A
公开(公告)日：1999-02-09
申请号：US715175
申请日：1996-09-23
申请人： Xuebao Wang , John K. Thottathil
发明人： Xuebao Wang , John K. Thottathil
IPC分类号： A61K31/16 , A61P35/00 , C07C277/00 , C07C277/08 , C07C279/14 , C07C279/24
CPC分类号： C07C279/24 , C07C277/08 , C07C279/14 , C07B2200/07
摘要： A process for preparing optically active (S)-(-) and (R)-(+)-deoxyspergualin and salts thereof of the formula I ##STR1## by reacting a compound of formula II ##STR2## with a compound of formula III ##STR3## in the presence of a condensing/dehydrating agent and an organic or inorganic base in an organic solvent to form a compound of formula IV ##STR4## which can then be converted to the desired final product of formula I via deprotection and hydrogenolysis. The invention also comprises the compounds of the formula II, IV and VII ##STR5##
摘要翻译：通过使式II化合物与式III化合物反应来制备式I的光学活性（S） - （ - ）和（R） - （+） - 脱氧精胍菌素及其盐。 IMAGE>在冷凝/脱水剂和有机或无机碱存在下在有机溶剂中形成式IV化合物，然后通过脱保护和氢解将其转化为所需的式I的最终产物。本发明还包括式II，IV和VII化合物

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式