专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 发明授权

US4602092A 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：US4602092A
公开(公告)日：1986-07-22
申请号：US693418
申请日：1985-01-22
申请人： John K. Thottathil , Jerome L. Moniot
发明人： John K. Thottathil , Jerome L. Moniot
IPC分类号： C07F9/30 , C07F9/572 , C07F9/62 , C07F9/32
CPC分类号： C07F9/62 , C07F9/301 , C07F9/306 , 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 an alkylating agent of the structure ##STR2## wherein Hal is Cl, Br or I, n is 0 or 1, R.sup.2 is H or lower alkyl, and Z is H, lower alkyl, --CO.sub.2 R.sup.3 (wherein R.sup.3 is H or lower alkyl), ##STR3## (wherein R.sup.4 is H, lower alkyl, aryl or arylalkyl), --CN, or ##STR4## (wherein R.sup.5 and R.sup.6 may be 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.5 and R.sup.6 is other than H, or R.sup.5 and R.sup.6 can be taken with the N-atom to form a 5-, 6- or 7-membered heterocyclic ring which 5-, 6- or 7-membered N-containing ring may or may not contain a CO.sub.2 R.sup.3 group and 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 phosphinic acid intermediate of the structure ##STR5## wherein R, R.sup.1, R.sup.2, n 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 其中Hal为Cl，Br或I，n为0或1，R2为H或低级烷基，Z为H，较低级为低级烷基，芳基，芳基烷基，环烷基或环烷基烷基烷基，-CO 2 R 3（其中R 3为H或低级烷基），其中R 4为H，低级烷基，芳基或芳基烷基，-CN或（其中R 5和R 6可以相同或不同，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 5和R 6中的至少一个不是H，或者R 5和R 6可以与N-原子一起形成 5-，6-或7-元含N的环可以含有或不含有CO 2 R 3基团的5-，6-或7-元杂环并且在甲硅烷基化剂的存在下，哪个5-或6-元含N的环可以或不可以与芳基环稠合），以形成结构式的次膦酸中间体，其中R，R 1，R 2 ，n和Z如上所定义。

32. 发明授权

US4588819A Process and intermediates for preparing trans-4-substituted-s-prolines 失效
标题翻译：制备反式-4-取代-β-脯氨酸的方法和中间体
公开(公告)号：US4588819A
公开(公告)日：1986-05-13
申请号：US672989
申请日：1984-11-19
申请人： John K. Thottathil
发明人： John K. Thottathil
IPC分类号： C07D207/08 , C07D207/16 , C07D498/04 , C07D207/12
CPC分类号： C07D207/08 , C07D207/16
摘要： 4-Substituted proline derivatives having the formula ##STR1## can be prepared by reacting the compound having the formula ##STR2## with a compound having the formula ##STR3## to obtain a compound having the formula ##STR4## (a novel intermediate), alkylating that compound to obtain a compound having the formula ##STR5## (a novel intermediate), converting that compound to a compound having the formula ##STR6## (a novel intermediate), and oxidizing that compound to yield the desired proline having the formula ##STR7## wherein R.sub.1 is alkyl, cycloalkyl, aryl or arylalkyl, R.sub.1 ' is alkyl, cycloalkenyl, aryl or arylalkyl, R.sub.2 is alkyl, aryl, arylalkyl or cycloalkyl and R.sub.3 is hydrogen, alkyl, aryl, arylalkyl or cycloalkyl.
摘要翻译：具有式“IMAGE”的4-取代的脯氨酸衍生物可以通过使具有式“IMAGE”的化合物与具有式“IMAGE”的化合物反应得到具有式“IMAGE”（新型中间体）的化合物，烷基化该化合物获得具有式“IMAGE”（新型中间体）的化合物，将该化合物转化为具有式“IMAGE”的化合物（新的中间体），并氧化该化合物，得到所需的具有式其中R1是烷基，环烷基，芳基或芳基烷基，R1'是烷基，环烯基，芳基或芳基烷基，R2是烷基，芳基，芳烷基或环烷基，R3是氢，烷基，芳基，芳烷基或环烷基。

33. 发明申请

US20120220634A1 Taxane Compounds, Compositions And Methods 有权
公开(公告)号：US20120220634A1
公开(公告)日：2012-08-30
申请号：US13455455
申请日：2012-04-25
申请人： John K. Thottathil , Raymond P. Warrell
发明人： John K. Thottathil , Raymond P. Warrell
IPC分类号： A61K31/443 , A61P35/00 , C07D493/04
CPC分类号： C07D493/06 , A61K31/335 , A61K31/337 , C07D205/08 , C07D305/14 , C07D407/02 , C07D493/08
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.

34. 发明授权

US06639082B2 Methods for the preparation of biphenyl isoxazole sulfonamides 失效
公开(公告)号：US06639082B2
公开(公告)日：2003-10-28
申请号：US09967387
申请日：2001-09-28
申请人： Richard P. Polniaszek , Xuebao Wang , John K. Thottathil , Theodor Denzel
发明人： Richard P. Polniaszek , Xuebao Wang , John K. Thottathil , Theodor Denzel
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07D261/16 , C07F5/025
摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.

35. 发明授权

US06313308B1 Methods for the preparation of biphenyl isoxazole sulfonamides 失效
标题翻译：联苯异恶唑磺酰胺的制备方法
公开(公告)号：US06313308B1
公开(公告)日：2001-11-06
申请号：US09528819
申请日：2000-03-20
申请人： Ambarish Singh , Chien-Kuang Chen , John A. Grosso , Edward J. Delaney , Xuebao Wang , Richard P. Polniaszek , John K. Thottathil
发明人： Ambarish Singh , Chien-Kuang Chen , John A. Grosso , Edward J. Delaney , Xuebao Wang , Richard P. Polniaszek , John K. Thottathil
IPC分类号： C07D26116
CPC分类号： C07D413/12 , C07C303/22 , C07D261/16 , C07D263/32 , C07D263/50 , C07C309/32
摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates therof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension, congestive heart failure and male erectile dysfunction.
摘要翻译：联苯异恶唑磺酰胺和中间体的制备方法。本发明还涉及通过这些方法制备的新型中间体。通过本方法制备的联苯异恶唑磺酰胺是内皮素拮抗剂，尤其用于治疗高血压，充血性心力衰竭和男性勃起功能障碍。

36. 发明授权

US5892106A Preparation of 3-fluoro oxindole derivatives 失效
标题翻译： 3-氟羟吲哚衍生物的制备
公开(公告)号：US5892106A
公开(公告)日：1999-04-06
申请号：US99472
申请日：1998-06-18
申请人： Yadagiri R. Pendri , Eduardo J. Martinez , John K. Thottathil , Piyasena Hewawasam
发明人： Yadagiri R. Pendri , Eduardo J. Martinez , John K. Thottathil , Piyasena Hewawasam
IPC分类号： C07C205/56 , C07D209/34 , C07C205/06
CPC分类号： C07C201/12 , C07C227/04 , C07D209/34 , Y02P20/55
摘要： The present invention relates to novel intermediates of the formula ##STR1## wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.
摘要翻译：本发明涉及式（IMAGE）的新型中间体，其中波状键（+ Z）表示外消旋物，（R） - 对映异构体或（S） - 对映体; R为氢，羧基保护基或加成盐的阳离子; 或其溶剂合物; 以及在制备某些3-氟羟吲哚衍生物的方法中的用途。

37. 发明授权

US5808095A Preparation of 3-fluoro oxindole derivatives 失效
公开(公告)号：US5808095A
公开(公告)日：1998-09-15
申请号：US946393
申请日：1997-10-07
申请人： Yadagiri R. Pendri , Eduardo J. Martinez , John K. Thottathil , Piyasena Hewawasam
发明人： Yadagiri R. Pendri , Eduardo J. Martinez , John K. Thottathil , Piyasena Hewawasam
IPC分类号： C07C205/56 , C07D209/34 , C07D209/12
CPC分类号： C07C201/12 , C07C227/04 , C07D209/34 , Y02P20/55
摘要： The present invention relates to novel intermediates of the formula ##STR1## wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.

38. 发明授权

US5399725A 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates useful in the preparation of anti-thrombotic and anti-vasospastic compounds and method for preparing same 失效
标题翻译：可用于制备抗血栓形成和抗血管痉挛性化合物的7-氧杂双环庚烷羧酸前列腺素类似物中间体及其制备方法
公开(公告)号：US5399725A
公开(公告)日：1995-03-21
申请号：US226091
申请日：1994-04-20
申请人： Michael A. Poss , Paul D. Pansegrau , Shaopeng Wang , John K. Thottathil , Janak Singh , Richard H. Mueller
发明人： Michael A. Poss , Paul D. Pansegrau , Shaopeng Wang , John K. Thottathil , Janak Singh , Richard H. Mueller
IPC分类号： C07D491/18 , C07D493/08 , C07D493/18 , C07D307/10 , C07D317/12
CPC分类号： C07D493/08
摘要： A method is provided for preparing carboxylic acid intermediates of the structure ##STR1## wherein an aldehyde of the structure ##STR2## is prepared and subjected to a Horner-Emmons reaction to form the ester of the structure ##STR3## and the ester is hydrogenated to the carboxylic acid which may be used in making the final anti-thrombotic--anti-vasospastic compounds.
摘要翻译：提供了一种制备结构“IMAGE”的羧酸中间体的方法，其中制备了结构“醛”的醛，并进行霍纳 - 埃蒙斯反应以形成结构“酯”的酯，并将酯氢化成可用于制备最终抗血栓形成 - 抗血管痉挛型化合物的羧酸。

39. 发明授权

US5274155A Intramolecular arbuzov process for the preparation of intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors 失效
标题翻译：用于制备可用于制备含磷HMG-COA还原酶抑制剂的中间体的分子内arbuzov方法
公开(公告)号：US5274155A
公开(公告)日：1993-12-28
申请号：US986402
申请日：1992-12-07
申请人： John K. Thottathil , David Kronenthal
发明人： John K. Thottathil , David Kronenthal
IPC分类号： C07F9/30 , C07F9/572 , C07F9/6503 , C07F9/6506 , C07F9/6596 , C07F7/08 , C07F7/18
CPC分类号： C07F9/6596 , C07F9/301 , C07F9/5728 , C07F9/65033 , C07F9/65062
摘要： A process for the preparation of compounds of formula ##STR1## and pharmaceutically acceptable salts thereof; wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 O-- (where O is linked to Z); Z is a hydrophobic anchor R.sub.1 is hydrogen, alkyl, cycloalkyl or aryl; comprising the steps of:(A) reacting a compound of formula ##STR2## with a compound of formula ##STR3## or a compound of formula ##STR4## in the presence of an amine base or an alkali metal hydride in an organic solvent to form a compound having the formula ##STR5## (B) heating the compound of formula IX at a temperature of from about 100.degree. C. to about 200.degree. C., to form a compound of formula ##STR6## and (C) quenching the compounds of formula VIII with an acid provides the compounds of formula I.
摘要翻译：制备式I化合物及其药学上可接受的盐的方法; 其中X是-CH 2 - ， - CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - ， - CH = CH - ， - C 3BOND C或-CH 2 O-（其中O连接到Z）; Z是疏水锚，R1是氢，烷基，环烷基或芳基; 包括以下步骤：（A）使式II化合物与式VII化合物或式VI的化合物在胺碱或碱金属氢化物的存在下在有机物中反应溶剂以形成具有式（VII）的化合物（B）在约100℃至约200℃的温度下加热式IX的化合物，以形成式VIII的化合物和（ C）用酸淬灭式VIII化合物，得到式Ⅰ化合物。

40. 发明授权

US5266710A (Exo,exo)-7-oxabicyclo[2.2.1]heptane-2,3-dimethanol; monoacyl ester and diacyl ester 失效
标题翻译：（Exo，外）-7-氧杂双环[2.2.1]庚烷-2,3-二甲醇; 单酰基酯和二酰基酯
公开(公告)号：US5266710A
公开(公告)日：1993-11-30
申请号：US737616
申请日：1991-07-30
申请人： Ramesh N. Patel , Laszlo J. Szarka , John K. Thottathil , David Kronenthal
发明人： Ramesh N. Patel , Laszlo J. Szarka , John K. Thottathil , David Kronenthal
IPC分类号： C07D493/08 , C07D493/18 , C12P17/18 , C12P41/00 , C07D307/93
CPC分类号： C07D493/08 , C12P17/181 , C12P41/004
摘要： Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]amino]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.
摘要翻译：本文公开了一种制备式“IMAGE”的新单酯的方法，其中在一种或多种能够选择性水解-OC（O））的水溶性酶或微生物的存在下水解相关新的二酯， -R1基团，其中所述处理在包含具有所述酶或微生物的水相和在所述二酯的水中不混溶的有机相的双相溶剂系统中进行。还公开了制备[1S- [1α，2α（Z），3α，4α]] -7 - [[[[[[（1-氧代庚基）氨基]乙酰基]氨基]甲基-7 - 氧杂双环 - [2.2.1]庚-2-基] -5-庚烯酸。

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