公开(公告)号：US20030187267A1

公开(公告)日：2003-10-02

申请号：US10240014

申请日：2002-12-05

发明人： Didier Babin ,  Yannick Benedetti ,  Fabienne Chatreaux ,  John Bernard Weston

IPC分类号： C07D47/14

CPC分类号： C07D249/08 ,  C07C45/29 ,  C07D217/04 ,  C07D231/12 ,  C07D233/56 ,  C07C49/457

摘要： The invention concerns compounds of formula (I) wherein: pnull1 or 2; X, X1 and X2 represent N or CHnull; R1, R2, R3, R4, R5 and R6 represent a hydrogen atom, a halogen atom, alkyl, O-alkyl, Snull(O)nalkyl, alkenyl, O-alkenyl, Snull(O)nalkenyl, alkynyl, O-alkynyl, Snull(O)nalkynyl; nnull0, 1 or 2, or NO2, NH2 or CnullN or R1, R2, R3 or R5, R6 form a cycle, or R4A can be cycloalkyl, heterocycle, aryl, O-aryl or oxygenated or nitrogenated chain; R7 represents H, OH, SO3H or OPO(OH)2; A and Bnullhydrogen or oxygenated or nitrogenated chain; C and Dnullhydrogen, halogen or alkyl or together form with the carbons bearing them a cycle. The compounds of formula (I) have antifungal properties.

摘要翻译： 本发明涉及式（I）的化合物，其中：p = 1或2; X，X1和X2表示N或CH =; R1，R2，R3，R4，R5和R6表示氢原子，卤素原子，烷基，O-烷基，S-（O）n烷基，烯基，O-烯基，S-（O） 炔基，S-（O）n炔基; n = 0,1或2，或NO2，NH2或C = N或R1，R2，R3或R5，R6形成一个周期，或者R4A可以是环烷基，杂环，芳基，O-芳基或含氧或氮化链; R 7表示H，OH，SO 3 H或OPO（OH）2; A和B =氢或氧化或氮化链; C和D =氢，卤素或烷基，或与碳一起形成带有它们的循环。 式（I）化合物具有抗真菌性质。

公开(公告)号：US20030171330A1

公开(公告)日：2003-09-11

申请号：US10080191

申请日：2002-02-19

申请人： SANKYO COMPANY, LIMITED

发明人： Hitoshi Hotoda ,  Masakatsu Kaneko ,  Masatoshi Inukai ,  Yasunori Muramatsu ,  Yukio Utsui ,  Satoshi Ohya

IPC分类号： A61K031/7072 ,  C07H019/073 ,  A61K031/513 ,  C07D47/14

CPC分类号： C07H19/06

摘要： A compound of formula (I) 1 wherein R1 and R2 represent a hydrogen atom or an aryl, a heterocyclic, an alkyl or an alkenyl, which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl and X1 and X2 represent an oxygen atom, a sulfur atom or a nitrogen containing group, a pharmaceutically acceptable derivative thereof or a salt thereof. A pharmaceutical composition comprising the compound for the prevention or treatment of a bacterial infection. A method for the prevention or treatment of a bacterial infection in a warm-blooded animal comprising administering a pharmacologically effective amount of the compound.

摘要翻译： 式（I）的化合物，其中R 1和R 2表示氢原子或任选被取代的芳基，杂环，烷基或链烯基，R 3表示氢原子或羟基 X 1和X 2表示氧原子，硫原子或含氮基团，其药学上可接受的衍生物或其盐。 一种药物组合物，其包含用于预防或治疗细菌感染的化合物。 一种预防或治疗温血动物细菌感染的方法，包括施用药理学有效量的化合物。

公开(公告)号：US20040142926A1

公开(公告)日：2004-07-22

申请号：US10659537

申请日：2003-09-10

发明人： Deborah Ann Evrard ,  Dahui Zhou ,  Gary Paul Stack ,  Aranapakam Madumbai Venkatesan ,  Amedeo A. Failli ,  Susan Christman Croce

IPC分类号： A61K031/551 ,  A61K031/496 ,  C07D47/14

CPC分类号： C07D491/04 ,  Y02P20/582

摘要： Compounds of the formula I: 1 are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 式I化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和抑郁症），焦虑症，恐慌症，创伤后应激障碍，经前期焦虑症（也称为月经前） 综合征），注意缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症和神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍及相关 疾病

公开(公告)号：US20030018050A1

公开(公告)日：2003-01-23

申请号：US10223046

申请日：2002-08-16

申请人： H. Lundbeck A/S

发明人： Ejner Knud Moltzen ,  Jens Kristian Perregaard ,  Ivan Mikkelsen ,  Garrick Paul Smith

IPC分类号： A61K031/454 ,  C07D47/14

CPC分类号： C07D405/12 ,  C07D405/14 ,  C07D409/12

摘要： The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) 1 or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.

摘要翻译： 本发明涉及具有式（I）的吲哚和2,3-二氢吲哚衍生物或其任何对映体或其任何混合物或其酸加成盐，其中A，R 1，R 2，R 3，W，X ，Y和Z如说明书所述。 该化合物是有效的5-羟色胺再摄取抑制剂，具有5-HT1A受体拮抗作用。

公开(公告)号：US20020183528A1

公开(公告)日：2002-12-05

申请号：US09997667

申请日：2001-11-28

发明人： Albert Gordon Anderson

IPC分类号： C07D47/14

CPC分类号： C07D307/33 ,  C07D315/00 ,  C07D493/10 ,  C08F8/30

摘要： The rate of aminolysis of butyrolactones is predictably adjusted by attaching a substituent having a known field effect value (F) to the alpha position before reacting the substituted buytrolactone with an amine. The aminolysis product is a gamma-hydroxy amide. The resulting materials are useful as the cross-linking agents in a variety of coatings and coatings processes.

公开(公告)号：US20020045752A1

公开(公告)日：2002-04-18

申请号：US09973766

申请日：2001-10-11

申请人： Nissan Chemical Industries, Ltd.

发明人： Hisao Ikeda ,  Yasuhiro Gunji ,  Motohiko Hidaka

IPC分类号： C07D47/14

CPC分类号： C07D251/34

摘要： A process for producing null-form tris-(2,3-epoxypropyl)-isocyanurate crystals containing from 2 to 15 wt % of a-form tris-(2,3-epoxypropyl)-isocyanurate in the interior of the crystals, which comprises the following steps (A), (B), (C) and (D): (A) a step of reacting cyanuric acid with epichlorohydrin to form an addition product of cyanuric acid and epichlorohydrin, followed by dehydrochlorination to obtain a reaction solution containing tris-(2,3-epoxypropyl)-isocyanurate, (B) a step of removing epichlorohydrin from the reaction solution containing tris-(2,3-epoxypropyl)isocyanurate obtained in step (A), and dissolving the obtained tris-(2,3-epoxypropyl)-isocyanurate in a solvent, (C) a step of gradually cooling the liquid obtained in step (B) at a cooling rate within 20null C./hr for crystallization, followed by filtration to obtain crystals, and (D) a step of washing and drying the crystals obtained in step (C).

摘要翻译： 在晶体内部生成含有2至15重量％的α-形式的三 - （2,3-环氧丙基） - 异氰脲酸酯的β-型三 - （2,3-环氧丙基） - 异氰脲酸酯晶体的方法，其包括 以下步骤（A），（B），（C）和（D）：（A）使三聚氰酸与表氯醇反应形成氰尿酸和表氯醇的加成产物，然后进行脱氯化氢以获得含 （2,3-环氧丙基） - 异氰脲酸酯，（B）从步骤（A）中得到的含有三（2,3-环氧丙基）异氰脲酸酯的反应溶液中除去表氯醇，并将得到的三 - （2 ，3-环氧丙基） - 异氰脲酸酯，（C）将步骤（B）中得到的液体以20℃/小时的冷却速度逐渐冷却以进行结晶，然后过滤得到晶体，（ D）洗涤和干燥步骤（C）中获得的晶体的步骤。

公开(公告)号：US20020111485A1

公开(公告)日：2002-08-15

申请号：US10118260

申请日：2002-04-09

申请人： Nissan Chemical Industries Limited

发明人： Hisao Ikeda ,  Motohiko Hidaka ,  Atsumi Aoki

IPC分类号： C07D47/14

CPC分类号： C07D405/14

摘要： Optically active null-type tris-(2,3-epoxypropyl)-isocyanurate is obtained by a method of reacting isocyanuric acid with an optically active epihalohydrin, or a method of optically resolving a racemic modification of tris-(2,3-epoxypropyl)-isocyanurate by using an amylose or cellulose derivative. It is a method for producing a high melting point type tris-(2,3-epoxypropyl)-isocyanurate obtained by mixing two enantiomers of optically active null-type tris-(2,3-epoxypropyl)-isocyanurate.

公开(公告)号：US20020077478A1

公开(公告)日：2002-06-20

申请号：US09820137

申请日：2001-03-28

发明人： Robert L. Dow ,  Steven R. Schneider

IPC分类号： C07F007/02 ,  C07D47/14 ,  C07D47/02

CPC分类号： C07F7/1892 ,  C07F7/1804 ,  C07F7/188 ,  Y02P20/55

摘要： A process for preparing a compound of the formula 1 wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of P-adrenergic receptor agonists.

摘要翻译： 制备下式化合物的方法其中n，R1，R2，R3和X如上定义，用作P-肾上腺素能受体激动剂合成中的中间体。

公开(公告)号：US20020042430A1

公开(公告)日：2002-04-11

申请号：US09933094

申请日：2001-08-20

发明人： Jean-Paul Rene Marie Bosmans ,  Christopher John Love ,  Marc Gustaaf Celine Verdonck ,  Joannes Adrianus Jacobus Schuurkes

IPC分类号： A61K031/4545 ,  A61K031/453 ,  A61K031/4525 ,  C07D47/02 ,  C07D47/14

CPC分类号： C07D401/06 ,  C07D211/22 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14

摘要： This invention concerns the compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula nullAlknullR4, nullAlknullNR5R6, 1-R6-4-piperidinyl, AlknullXnullR7, nullAlknullYnullC(nullO)nullR9, or nullAlknullYnullC(nullO)nullNR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Arnull, di(Ar)methyl, Arnulloxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen, C1-6alkyl or Ar; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, C1-6alkyl or Ar; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

摘要翻译： 本发明涉及式I化合物的N-氧化物形式，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是C 1-6烷氧基，C 2-6烯基氧基或C 2-6炔基氧基; R 2是氢或C 1-6烷氧基，或者当R 1和R 2一起形成式2的二价基团时，其中在所述二价基团中，一个或两个氢原子可以被C 1-6烷基取代，R 3是氢或卤素; L是C3-6环烷基，C5-6环烷酮，任选被芳基取代的C2-6烯基，或L是式-Alk-R4，-Alk-NR5R6，1-R6-4-哌啶基，Alk-X-R7， - Alk-YC（= O）-R9或-Alk-YC（= O）-NR11R12，其中每个Alk是C1-12烷二基; R4是氢，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环烷酮，Ar-，二（Ar）甲基，Ar-氧基或Het1; R5是氢或C1-6烷基; R6是Het2; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基，Ar或Het 2; X是O，S，SO 2或NR 8; 所述R8为氢，C1-6烷基或Ar; R 9为氢，C 1-6烷基，C 3-6环烷基，Ar，ArC 1-6烷基，二（Ar）甲基，C 1-6烷氧基或羟基; Y是NR10或直接键; 所述R 10为氢，C 1-6烷基或Ar; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基，Ar或ArC 1-6烷基，或R 11和R 12与带有R 11的氮原子结合

公开(公告)号：US20020042396A1

公开(公告)日：2002-04-11

申请号：US09995564

申请日：2001-11-29

申请人： Astra AB

发明人： David Gustafsson ,  Jan-Erik Nystrom

IPC分类号： A61K031/695 ,  C07F007/02 ,  C07D47/14 ,  A61K031/454 ,  A61K031/4015

CPC分类号： C07D211/60 ,  C07D205/04 ,  C07D207/16

摘要： There is provided amino acid derivatives of formula I, 1 wherein p, q, R1, R2, R3, R4, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as hirombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

摘要翻译： 提供式I的氨基酸衍生物，其中p，q，R 1，R 2，R 3，R 4，Y，n和B具有在描述中给出的含义，其可用作胰蛋白酶样蛋白酶的竞争性抑制剂，例如hirombin， 特别是在需要抑制凝血酶（例如血栓形成）或作为抗凝剂的条件的治疗中。