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51.发明授权公开(公告)号：US07786156B2
公开(公告)日：2010-08-31
申请号：US10586958
申请日：2005-01-27
IPC分类号： A61K31/41 , C07D249/00 , C07D249/08
CPC分类号： C07D209/14 , C07D209/16 , C07D209/34 , C07D231/12 , C07D233/56 , C07D249/08 , C07D403/06 , Y02P20/55
摘要： The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], or a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B] wherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent. In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
摘要翻译： 本发明涉及一种制备式[A]的1,2,4-三唑-1-基化合物或其盐的方法，其中R 3和R 4各自为氢或低级烷基，所述方法包括 使式[B]的肼化合物其中R是氢或酰基，R2是氢或保护基，是氢或低级烷基，R6是氢或COOR7或其盐与1,2,4 三唑基形成试剂。 此外，还提出了用于合成抗偏头痛药物利扎曲坦的新型中间体及其合成方法。
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52.发明申请Process For Preparing Porphyrin Derivatives, Such As Protoporphyrin (IX) And Synthesis Intermediates 有权制备卟啉衍生物，如原卟啉（IX）和合成中间体的方法公开(公告)号：US20080242857A1
公开(公告)日：2008-10-02
申请号：US12057574
申请日：2008-03-28
IPC分类号： C07D487/22
CPC分类号： C07D207/34 , C07D487/22
摘要： The present invention relates to a process for preparing a porphyrin of formula (I), optionally in the form of a salt with an alkali metal and/or in the form of a metal complex: in which: R and R′ are as defined in claim 1, comprising: a step of condensation, in an acidic medium, between a dipyrromethane of formula (II): in which R′b is as defined above for (I), and a dipyrromethane of formula (III): in which R″ is as defined in claim 1, and also the compounds of formula (III).
摘要翻译： 本发明涉及一种制备式（I）卟啉的方法，任选地以与碱金属和/或金属络合物形式的盐形式：其中：R和R'如 权利要求1的方法，包括：在酸性介质中在式（II）的二吡咯甲烷之间缩合的步骤：其中R'b如上文对（I）所定义，和式（III）的二吡咯烷：其中R “如权利要求1中所定义，还有式（III）化合物。
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公开(公告)号：US20070123711A1
公开(公告)日：2007-05-31
申请号：US10586958
申请日：2005-01-27
IPC分类号： C07D403/02
CPC分类号： C07D209/14 , C07D209/16 , C07D209/34 , C07D231/12 , C07D233/56 , C07D249/08 , C07D403/06 , Y02P20/55
摘要： The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], or a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B] wherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent. In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
摘要翻译： 本发明涉及一种制备式[A]的1,2,4-三唑-1-基化合物或其盐的方法，其中R 3和R 4各自为氢或低级烷基，所述方法包括 使式[B]的肼化合物其中R是氢或酰基，R2是氢或保护基，是氢或低级烷基，R6是氢或COOR7或其盐与1,2,4 三唑基形成试剂。 此外，还提出了用于合成抗偏头痛药物利扎曲坦的新型中间体及其合成方法。
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公开(公告)号：US07098325B2
公开(公告)日：2006-08-29
申请号：US10266027
申请日：2002-10-07
申请人： Pierre Martin , Francois J Natt
发明人： Pierre Martin , Francois J Natt
IPC分类号： C07H21/00 , C07D417/00 , C07D285/08
CPC分类号： C07H21/00 , C07F9/165 , C07F9/17 , Y02P20/582
摘要： The invention relates to a process for the sulfurization of phosphorus-containing compounds which comprises contacting the phosphorus compound to be sulfurized with a sulfur transfer reagent of formula (I) wherein R1 is aryl which can be substituted by halo, (C1–C6) alkyl or (C1-C6) alkoxy, and R2 is (C1–C6) alkyl, which could also form a cyclic ring together with R1, in a solvent or a mixture of solvents.
摘要翻译： 本发明涉及含磷化合物的硫化方法，其包括使待硫化的磷化合物与式（I）的硫转移试剂接触，其中R 1是可以被 卤素，（C 1 -C 6 -C 6）烷基或（C 1 -C 6 -C 6）烷氧基，R （C 1 -C 6 -C 6）烷基，其也可以与R 1一起形成环， ，在溶剂或溶剂的混合物中。
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公开(公告)号：US20050159374A1
公开(公告)日：2005-07-21
申请号：US10696488
申请日：2003-10-29
CPC分类号： C07H21/00
摘要： The invention relates to an oligonucleotide derivative which comprises at least one nucleoside building block of the formula (I) The invention furthermore relates to nucleoside building blocks, intermediates and processes for preparing the oligonucleotide derivatives and the nucleoside building blocks. The invention also relates to pharmaceutical compositions and to uses of the oligonucleotide derivatives and the nucleoside building blocks.
摘要翻译： 本发明涉及包含至少一种式（I）核苷结构单元的寡核苷酸衍生物。本发明还涉及核苷结构单元，中间体和制备寡核苷酸衍生物和核苷结构单元的方法。 本发明还涉及药物组合物以及寡核苷酸衍生物和核苷结构单元的用途。
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公开(公告)号：US4812580A
公开(公告)日：1989-03-14
申请号：US93449
申请日：1987-09-04
申请人： Pierre Martin
发明人： Pierre Martin
IPC分类号： A01N43/36 , C07C67/00 , C07C223/02 , C07C229/30 , C07C253/00 , C07C255/24 , C07C255/30 , C07C255/58 , C07D207/32 , C07D207/33 , C07D207/333 , C07D207/335 , C07D207/34
CPC分类号： C07D207/333 , C07C255/00 , C07D207/335 , C07D207/34
摘要： The invention relates to a process for the preparation of 4-phenylpyrrole derivatives of the formula I ##STR1## wherein R.sub.n, R.sub.1 and R.sub.2 are as defined in claim 1, which comprises reacting a phenacylamine of formula II ##STR2## with a compound of formula IIIT--CH.dbd.CH--R.sub.1 (III)to give an intermediate of formula IV ##STR3## and cyclizing said intermediate, in the presence of a base, to give the compound I. Important intermediates and novel final products are also described.
摘要翻译： 本发明涉及制备式I（I）的4-苯基吡咯衍生物的方法，其中Rn，R 1和R 2如权利要求1所定义，其包括使式II的苯甲酰胺（II） ）与式III的化合物T-CH = CH-R 1（III）反应，得到式IV的中间体（IV），并在碱的存在下使所述中间体环化，得到化合物I.重要的中间体 还描述了新的最终产品。
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公开(公告)号：US4595755A
公开(公告)日：1986-06-17
申请号：US759976
申请日：1985-07-29
申请人： Pierre Martin
发明人： Pierre Martin
IPC分类号： C07D471/06
CPC分类号： C07D471/06
摘要： There is described a novel process for producing 1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one (4-lilolidone), usable as fungicide and corresponding to the formula ##STR1## as well as novel 5-halo-1,2,3-(1,2-dihydropyrrolo)-4-quinolones of the formula ##STR2## in which "Hal" is chlorine or bromine, which are formed as intermediates during the process.
摘要翻译： 描述了用于制备1,2,5,6-四氢-4H-吡咯并[3,2,1-ij] - 喹啉-4-酮（4-二烯醇）的新方法，其可用作杀真菌剂并对应于式 ＆lt; IMAGE＆gt;以及式“IMAGE”的新的5-卤代-1,2,3-（1,2-二氢吡咯并）-4-喹诺酮，其中“Hal”是氯或溴，它们作为中间体形成 的过程。
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58.发明授权4-(2',2,2'-Trihalogenoethyl)-cyclobutane-1-sulfonic acid salts with optically active bases 失效4-（2'，2,2'-三卤代乙基） - 环丁烷-1-磺酸盐与光学活性碱
公开(公告)号：US4335057A
公开(公告)日：1982-06-15
申请号：US219803
申请日：1980-12-24
IPC分类号： C07C69/74 , C07B31/00 , C07B57/00 , C07C45/45 , C07C45/54 , C07C45/67 , C07C51/00 , C07C51/48 , C07C61/15 , C07C61/40 , C07C67/00 , C07C69/635 , C07C69/743 , C07C253/00 , C07C255/38 , C07C255/39 , C07C255/53 , C07C301/00 , C07C303/10 , C07C303/32 , C07C309/25 , C07C313/00 , C07C321/24 , C07D307/42 , C07D307/45 , C07D333/04 , C07D333/16 , C07D333/32 , C07C143/20
CPC分类号： C07C45/67 , C07C309/00 , C07C45/45 , C07C45/54 , C07C51/00
摘要： There is described a new process for the preparation of optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids substituted in the 3 position, and derivatives thereof. A racemate of certain cyclobutanones is reacted with a sulfurous acid salt of an optically active base to obtain a mixture of diastereomeric 4-(2',2',2'-trihalogenoethyl)-cyclobutane-2-sulfonic acid salts; this mixture is then separated into the pure diastereomeric sulfonic acid salts. Either the pure diastereomeric sulfonic acid salts are converted directly to the desired optically active products, or the optically active cyclobutanones obtained from the pure diastereomeric sulfonic acids salts by decomposition are converted, in the presence of a base, to the desired product. Optionally, the product, optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-2-carboxylic acids can be converted to their 1',2'-dibromo derivatives.
摘要翻译： 描述了制备在3位上被取代的光学活性的2-（2'，2'-二卤代乙烯基） - 环丙烷-1-羧酸及其衍生物的新方法。 某些环丁酮的外消旋物与光学活性碱的亚硫酸盐反应，得到非对映异构体4-（2'，2'，2'-三卤代乙基） - 环丁烷-2-磺酸盐的混合物; 然后将该混合物分离成纯的非对映体磺酸盐。 将纯的非对映异构体磺酸盐直接转化为所需的光学活性产物，或通过分解从纯非对映异构体磺酸盐获得的光学活性环丁酮在碱的存在下转化为所需产物。 任选地，产物光学活性的2-（2'，2'-二卤代乙烯基） - 环丙烷-2-羧酸可以转化为它们的1'，2'-二溴衍生物。
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59.发明授权Process for preparing prophyrin derivatives, such as protoprophyrin (IX) and synthesis intermediates 有权制备卟啉衍生物的方法，如protoprophyrin（IX）和合成中间体公开(公告)号：US08420805B2
公开(公告)日：2013-04-16
申请号：US13218149
申请日：2011-08-25
IPC分类号： C07D487/22
CPC分类号： C07D207/34 , C07D487/22
摘要： The present invention relates to a process for preparing a porphyrin of formula (I), optionally in the form of a salt with an alkali metal and/or in the form of a metal complex: in which: R and R′ are as defined in claim 1, comprising: a step of condensation, in an acidic medium, between a dipyrromethane of formula (II): in which R′b is as defined above for (I), and a dipyrromethane of formula (III): in which R″ is as defined in claim 1, and also the compounds of formula (III).
摘要翻译： 本发明涉及一种制备式（I）卟啉的方法，任选地以与碱金属和/或金属络合物形式的盐形式：其中：R和R'如 权利要求1的方法，包括：在酸性介质中在式（II）的二吡咯甲烷之间缩合的步骤：其中R'b如上文对（I）所定义，和式（III）的二吡咯烷：其中R “如权利要求1所定义，也可以是式（III）化合物。
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公开(公告)号：US08299021B2
公开(公告)日：2012-10-30
申请号：US13450885
申请日：2012-04-19
申请人： Lawrence M Blatt , Scott D Seiwert , Steven W Andrews , Pierre Martin , Andreas Schumacher , Bradley Barnett , C. Todd Eary , Robert Kaus , Timothy Kercher , Weidong Liu , Michael Lyon , Paul Nichols , Bin Wang , Tarek Sammakia , April Kennedy , Yutong Jiang
发明人： Lawrence M Blatt , Scott D Seiwert , Steven W Andrews , Pierre Martin , Andreas Schumacher , Bradley Barnett , C. Todd Eary , Robert Kaus , Timothy Kercher , Weidong Liu , Michael Lyon , Paul Nichols , Bin Wang , Tarek Sammakia , April Kennedy , Yutong Jiang
IPC分类号： A61K38/00
CPC分类号： C07K5/0806 , A61K38/00 , A61K38/1793 , A61K38/212 , A61K38/217 , A61K38/2292 , A61K38/55 , C07D471/04 , C07D487/04 , C07K5/0804 , A61K2300/00
摘要： The embodiments provide compounds of the general Formulae I through general Formula VIII, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
摘要翻译： 实施方案提供通式I至通式VIII的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。
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