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81. 发明申请

US20040092762A1 Polyhaloalkylaryls 审中-公开
标题翻译：多卤烷基芳基
公开(公告)号：US20040092762A1
公开(公告)日：2004-05-13
申请号：US10703835
申请日：2003-11-07
发明人： Albrecht Marhold , Axel Pleschke
IPC分类号： C07C235/34 , C07C237/38
CPC分类号： C07C231/12 , C07C209/68 , C07C233/15 , C07C2601/04 , C07C2601/08
摘要： The present invention relates to polyhaloalkylaryls, to a process for preparing them and to the use of the polyhaloalkylaryls for preparing active ingredients.
摘要翻译：本发明涉及多卤烷基芳基，其制备方法和多卤烷基芳基用于制备活性成分的用途。

82. 发明授权

US06693210B2 Triphenylphosphine derivative, production process therefor, palladium complex thereof, and process for producing biaryl derivative 失效
标题翻译：三苯基膦衍生物，其制备方法，其钯络合物，以及生产联芳基衍生物的方法
公开(公告)号：US06693210B2
公开(公告)日：2004-02-17
申请号：US10221678
申请日：2002-09-13
申请人： Norio Miyaura
发明人： Norio Miyaura
IPC分类号： C07F950
CPC分类号： C07F9/5022 , C07B37/04 , C07C17/263 , C07C37/18 , C07C41/30 , C07C45/68 , C07C51/353 , C07C205/06 , C07C209/68 , C07C303/30 , C07D213/06 , C07F9/5027 , C07C25/18 , C07C47/546 , C07C49/784 , C07C63/331 , C07C211/48 , C07C309/66 , C07C43/205 , C07C39/15
摘要： Provided are a novel triphenyl phosphine derivative synthesized from a triphenylphosphine and a hydroxy-containing lactone; a palladium and a nickel complexes comprising the derivative as a ligand; and a process for preparing a biaryl derivative using the complex as a catalyst. A product can be easily separated from a catalyst or a phosphorus compound, and biaryl derivative can be synthesized in a higher yield, by using the complex of the present invention as a catalyst.
摘要翻译：提供由三苯基膦和含羟基的内酯合成的新型三苯基膦衍生物; 包含该衍生物作为配体的钯和镍络合物; 以及使用该络合物作为催化剂制备联芳基衍生物的方法。通过使用本发明的络合物作为催化剂，可以容易地从催化剂或磷化合物中分离产物，并且可以以更高的收率合成联芳基衍生物。

83. 发明申请

US20030176722A1 Process for preparation of 1,5-diaminonaphthalenes 失效
标题翻译：制备1,5-二氨基萘的方法
公开(公告)号：US20030176722A1
公开(公告)日：2003-09-18
申请号：US10312852
申请日：2003-01-02
发明人： Satoshi Inoki , Yoshio Motoyama
IPC分类号： C07C255/42 , C07C229/38 , C07C211/49
CPC分类号： C07C209/52 , C07C201/12 , C07C209/36 , C07C209/40 , C07C209/68 , C07C211/58 , C07C249/02 , C07C249/08 , C07C2602/10 , C07C251/44 , C07C251/20 , C07C205/06 , C07C205/45 , C07C205/56
摘要： In a process where an ortho-alkylnitrobenzene derivative and a vinyl compound as starting materials are used to prepare a 1,5-diaminonaphthalene derivative via a 4-(2-nitrobenzene)propane derivative and a 5-nitro-1-tetralone derivative, the ortho-alkylnitrobenzene derivative and a vinyl compound having an electron withdrawing group such as an acrylonitrile derivative and an acrylate may be reacted in the presence of a base to provide an aromatic nitro compound. An aromatic nitro compound such as 4-(2-nitrobenzene)butanonitrile thus obtained may be cyclized to safely, cost-effectively and selectively provide a 5-nitro-1-tetralone derivative without forming any isomer. Furthermore, from the 5-nitro-1-tetralone derivative, a 1,5-diaminonaphthalene derivative may be prepared without forming any isomer.
摘要翻译：在使用原烷基硝基苯衍生物和乙烯基化合物作为原料的方法中，通过4-（2-硝基苯）丙烷衍生物和5-硝基-1-四氢萘酮衍生物制备1,5-二氨基萘衍生物，正烷基硝基苯衍生物和具有吸电子基团的乙烯基化合物如丙烯腈衍生物和丙烯酸酯可以在碱的存在下反应以提供芳族硝基化合物。如此获得的芳族硝基化合物如4-（2-硝基苯）丁腈可以环化以安全，成本有效地选择性地提供5-硝基-1-四氢萘酮衍生物而不形成任何异构体。此外，从5-硝基-1-四氢萘酮衍生物可以制备1,5-二氨基萘衍生物而不形成任何异构体。

84. 发明申请

US20030149107A1 Compounds for the treatment of metabolic disorders 有权
公开(公告)号：US20030149107A1
公开(公告)日：2003-08-07
申请号：US10167839
申请日：2002-06-12
发明人： Shalini Sharma , Reid W. von Borstel
IPC分类号： A61K031/195 , A61K031/137 , C07C225/16 , C07C229/34
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

85. 发明授权

US06515181B2 Process for the preparation of terbinafine 失效
标题翻译：制备特比萘芬的方法
公开(公告)号：US06515181B2
公开(公告)日：2003-02-04
申请号：US10085699
申请日：2002-02-28
申请人： Graziano Castaldi , Giuseppe Barreca , Renzo Rossi
发明人： Graziano Castaldi , Giuseppe Barreca , Renzo Rossi
IPC分类号： C07C21100
CPC分类号： C07C209/68 , C07C211/27
摘要： A process for the preparation of terbinafine which comprises the reaction of tert-butylacetylene with a compound of formula (II) characterized in that the reaction is carried out in the presence of copper (I) salts and of a base, in the absence of palladium.
摘要翻译：一种制备特比萘芬的方法，其包括叔丁基乙炔与式（II）化合物的反应，其特征在于反应在不存在钯的情况下在铜（I）盐和碱的存在下进行。

86. 发明授权

US06506940B1 Process for converting stereoisomers of sertraline into sertraline 失效
标题翻译：将舍曲林的立体异构体转化为舍曲林的方法
公开(公告)号：US06506940B1
公开(公告)日：2003-01-14
申请号：US09709812
申请日：2000-11-10
申请人： Kanaksinh J. Jadav , Trinadha Rao Chitturi , Rajamannar Thennati
发明人： Kanaksinh J. Jadav , Trinadha Rao Chitturi , Rajamannar Thennati
IPC分类号： C07C21100
CPC分类号： C07C209/68 , C07C2602/10 , Y02P20/582 , C07C211/29 , C07C211/42
摘要： A process for converting the cis (1R, 4R), trans (1S, 4R), and trans (1R, 4S) stereoisomers of sertraline into sertraline comprises, starting with an initial reaction mixture which contains at least one of these stereoisomers, converting the sertraline stereoisomers into an imine form of sertraline. The imine form of sertraline is then reduced so that sertraline and at least one sertraline stereoisomer byproduct is produced in the reaction mixture. The sertraline is then recovered from the reaction mixture, e.g., by fractional crystallization (followed by resolution of sertraline from the cis (1R, 4R) stereoisomer, if necessary). The reaction mixture is then recycled through the same steps so that sertraline is produced from its stereoisomers in an asymptotic yield.
摘要翻译：将舍曲林的顺式（1R，4R），反式（1S，4R）和反式（1R，4S）立体异构体转化为舍曲林的方法包括，从含有至少一种这些立体异构体的初始反应混合物开始，舍曲林立体异构体转化为亚胺形式的舍曲林。然后减少舍曲林的亚胺形式，使得在反应混合物中产生舍曲林和至少一种舍曲林立体异构体副产物。然后从反应混合物中回收舍曲林，例如通过分步结晶（如果需要的话从顺式（1R，4R）立体异构体中分离出舍曲林）。然后将反应混合物通过相同的步骤循环使得舍曲林以其渐进收率从其立体异构体产生。

87. 发明申请

US20020120166A1 Racemization of optically active amines 失效
标题翻译：光学活性胺的外消旋化
公开(公告)号：US20020120166A1
公开(公告)日：2002-08-29
申请号：US10012344
申请日：2001-12-12
发明人： Frank Funke , Shelue Liang , Andreas Kramer , Rainer Sturmer , Arthur Hohn
IPC分类号： C07C29/68
CPC分类号： C07C213/02 , B01J23/80 , B01J35/023 , B01J37/0009 , B01J37/0201 , B01J37/031 , B01J37/035 , C07B2200/07 , C07C209/68 , C07C209/88 , C07C217/08 , C07C211/07
摘要： Optically active amines of the formula I 1 where R1 and R2 are different and R1, R2, R3 are alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl and heterocyclic radicals and R3 may also be hydrogen (H), with the radicals being able to bear substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, aryloxy, amino, alkylamino and dialkylamino, are racemized by reacting the optically active amine I in the presence of hydrogen and a hydrogenation or dehydrogenation catalyst at elevated temperature, wherein the catalyst comprises the active components copper and zinc oxide and a support material.
摘要翻译：其中R1和R2不同且R1，R2，R3是烷基，环烷基，芳基烷基，芳基，杂芳基和杂环基的式I的光活性胺，R 3也可以是氢（H），其中基团能够带有取代基选自由烷基，环烷基，烷氧基，芳氧基，氨基，烷基氨基和二烷基氨基组成的组，通过使光学活性胺I在氢气和氢化或脱氢催化剂的存在下在升高的温度下反应进行外消旋化，其中催化剂包含活性组分铜和氧化锌和支撑材料。

88. 发明申请

US20020072516A1 Selective protein tyrosine phosphatatase inhibitors 失效
标题翻译：选择性蛋白酪氨酸磷酸酶抑制剂
公开(公告)号：US20020072516A1
公开(公告)日：2002-06-13
申请号：US09941471
申请日：2001-08-29
发明人： Gang Liu , Bruce G. Szczepankiewicz , Zhonghua Pei , Zhili Xin , David A. Janowick
IPC分类号： A61K031/55 , A61K031/47 , A61K031/473 , A61K031/4035 , A61K031/215 , C07D223/18 , C07D223/16
CPC分类号： C07C209/68 , C07C233/56 , C07C235/74 , C07C237/22 , C07C237/24 , C07C237/42 , C07C271/20 , C07C271/22 , C07C275/24 , C07C311/06 , C07C311/47 , C07C317/40 , C07C323/59 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D211/20 , C07D241/18 , C07D265/06 , C07D295/135 , C07D295/155 , C07D295/185 , C07D319/18
摘要： Compounds of formula (I) 1 or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.
摘要翻译：式（I）化合物或其治疗上可接受的盐是选择性蛋白酪氨酸激酶-B（PTP1B）抑制剂。公开了化合物的制备，含有该化合物的组合物和使用该化合物治疗病症。

89. 发明授权

US06388153B2 Alpha-methylstyrene dimer derivatives 失效
标题翻译： α-甲基苯乙烯二聚体衍生物
公开(公告)号：US06388153B2
公开(公告)日：2002-05-14
申请号：US09851549
申请日：2001-05-09
申请人： Alexei Alexeyevich Gridnev
发明人： Alexei Alexeyevich Gridnev
IPC分类号： C07C1552
CPC分类号： C09D125/02 , C07C2/04 , C07C15/50 , C07C209/68 , C07C263/16 , C07C275/24 , C07C2531/22 , C08F12/12 , C07C211/50 , C07C265/14
摘要： The present invention relates to a method of making alpha-methylstyrene dimers by combining a cobalt catalyst, a free-radical initiator and an alpha-methylstyrene monomer, in an inert atmosphere, to form a mixture. The mixture is heated to a temperature in the range of 65° C. to 140° C. to form alpha methyl styrene dimers. The present invention also relates to the products produced by this inventive method.
摘要翻译：本发明涉及通过在惰性气氛中组合钴催化剂，自由基引发剂和α-甲基苯乙烯单体来制备α-甲基苯乙烯二聚体以形成混合物的方法。将混合物加热至65℃至140℃的温度，以形成α-甲基苯乙烯二聚体。本发明还涉及通过本发明方法生产的产品。

90. 发明授权

US06350910B1 Stereospecific isomerisation of allylamines with the aid of immobilized phosphorated chiral ligands 失效
标题翻译：借助于固定化的磷酸化手性配体，烯丙胺的立体特异性异构化
公开(公告)号：US06350910B1
公开(公告)日：2002-02-26
申请号：US09588687
申请日：2000-06-07
申请人： Christian Chapuis
发明人： Christian Chapuis
IPC分类号： C07F902
CPC分类号： B01J31/06 , B01J31/1658 , B01J31/2452 , B01J31/28 , B01J2231/52 , B01J2531/0266 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07C209/68 , C07C249/02 , C07F9/5027
摘要： The present invention describes a method for stereospecific isomerisation of prochiral allylamines into enamines and chiral imines, by using catalysts of Rh, Ir and Ru having phosphine chiral ligands immobilised on a solid material. The immobilised ligands are derivatives of phosphines of the type bis(diphenylphosphino)biaryl such as, for example, the phosphine known by the name BINAP. The method is particularly suitable for the production of optically active citronellal which may be obtained in optical purities above 95%.
摘要翻译：本发明描述了通过使用固定在固体材料上的具有膦手性配体的Rh，Ir和Ru的催化剂，将前手性烯丙胺立体特异性异构化成烯胺和手性亚胺的方法。固定化的配体是双（二苯基膦基）联芳基类型的膦的衍生物，例如已知的名称为BINAP的膦。该方法特别适用于光学纯度高于95％的光学活性香茅醛的制备。

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