公开(公告)号：US06635635B2

公开(公告)日：2003-10-21

申请号：US09916479

申请日：2001-07-27

申请人： Alex Cordi ,  Patrice Desos ,  François Lefoulon ,  Pierre Lestage

发明人： Alex Cordi ,  Patrice Desos ,  François Lefoulon ,  Pierre Lestage

IPC分类号： C07D51304

CPC分类号： C07D513/04

摘要： Compound of formula (I): wherein: R1 represents hydroxy, RCO—O— or RCO—NRa—, R2 represents hydrogen, halogen, or hydroxy, R′CO—O or R′CO—NR′a—, R and R′, which may be identical or different, represent linear or branched (C1-C6)alkyl optionally substituted by aryl, linear or branched (C2-C6)alkenyl optionally substituted by aryl, linear or branched (C1-C6)perhaloalkyl, (C3-C7)cycloalkyl, adamantyl, aryl or heteroaryl, Ra and R′a, which may be identical or different, represent hydrogen or linear or branched (C1-C6)alkyl, linear or branched (C1-C6)perhaloalkyl, linear or branched (C1-C6)acyl, aryl or heteroaryl, its isomer and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as AMPA modulators.

摘要翻译： 式（I）化合物：其中：R1代表羟基，RCO-O-或RCO-NRa-，R2代表氢，卤素或羟基，R'CO-O或R'CO-NR'a-，R和R （C 1 -C 6）烷基，任选被芳基，直链或支链（C 1 -C 6）全卤代烷基取代的直链或支链（C 1 -C 6）烷基，任选被芳基，直链或支链（C 2 -C 6） -C 7）环烷基，金刚烷基，芳基或杂芳基，R a和R a可以相同或不同，表示氢或直链或支链（C1-C6）烷基，直链或支链（C1-C6）全卤代烷基，直链或支链 （C 1 -C 6）酰基，芳基或杂芳基，其异构体和其药学上可接受的酸或碱的加成盐和含有它们的药物可用作AMPA调节剂。

公开(公告)号：US06657064B2

公开(公告)日：2003-12-02

申请号：US10117335

申请日：2002-04-08

申请人： Matthias Gerlach ,  Corinna Maul

发明人： Matthias Gerlach ,  Corinna Maul

IPC分类号： C07D51304

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07F9/6561 ,  C40B40/00

摘要： A novel bicyclic imidazo-5-yl-amine derivative of Formula I, wherein X denotes CR5, N or S, and Y in the case where X denotes S, denotes CR6 or N and in all other cases denotes N, and methods for preparation thereof are disclosed. Also disclosed are methods for treating pain using the compound of Formula I, and pharmaceutical compositions comprising the compound of Formula I.

摘要翻译： 式I的新型二环咪唑-5-基 - 胺衍生物，其中X表示CR 5，N或S，在X表示S的情况下为Y，表示CR 6或N，在所有其他情况下表示 N及其制备方法。 还公开了使用式I化合物治疗疼痛的方法和包含式I化合物的药物组合物。

公开(公告)号：US06191124B1

公开(公告)日：2001-02-20

申请号：US09180809

申请日：1997-04-07

申请人： Herman W. Smith

发明人： Herman W. Smith

IPC分类号： C07D51304

CPC分类号： C07D513/04

摘要： The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R1 is —H or —CH3; wherein R2 is —H or —CH3; or wherein R1 and R2 taken together are (a) formula (II), or (b) formula (III).

摘要翻译： 本发明涉及用于抑制哺乳动物细胞中的逆转录病毒的咪唑并[2,1-b]苯并噻唑-3-甲醇和咪唑并[2,1-b]噻唑-5-甲醇衍生物的式（I）化合物 感染所述逆转录病毒，其中R1是-H或-CH3; 其中R2是-H或-CH3; 或其中R 1和R 2一起是（a）式（II）或（b）式（III）。

公开(公告)号：US06828326B2

公开(公告)日：2004-12-07

申请号：US10634225

申请日：2003-08-05

申请人： Joseph Armand Picard ,  Michael William Wilson

发明人： Joseph Armand Picard ,  Michael William Wilson

IPC分类号： C07D51304

CPC分类号： C07D487/04 ,  C07D513/04

摘要： The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.

摘要翻译： 本发明涉及式I，B，X，Y和R 1的稠合双环金属蛋白酶抑制剂如说明书中所定义，以及治疗关节炎，炎症，癌症和其它病症的药物组合物和方法。

公开(公告)号：US06770642B2

公开(公告)日：2004-08-03

申请号：US10323369

申请日：2002-12-19

申请人： Derek Cecil Cole ,  Joseph Raymond Stock ,  William Joseph Lennox ,  Ping Zhou

发明人： Derek Cecil Cole ,  Joseph Raymond Stock ,  William Joseph Lennox ,  Ping Zhou

IPC分类号： C07D51304

CPC分类号： C07D471/04 ,  C07D513/04

摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

摘要翻译： 本发明提供式I化合物及其用于治疗与5-HT 6受体有关或受其影响的病症的用途。

公开(公告)号：US06743913B2

公开(公告)日：2004-06-01

申请号：US10421929

申请日：2003-04-24

申请人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

IPC分类号： C07D51304

CPC分类号： C07D513/04 ,  C07D207/36

摘要： A pyrrolesulfonamide compound having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with &agr;1-blocking action and serotonin-2 receptor antagonistic action in combination.

摘要翻译： 具有下式（I）的吡咯磺酰胺化合物：其中由具有以下结构的吡咯环表示的环P：其中A表示亚烷基，亚烯基或亚炔基; Y表示W表示CH，C =或N的基团; 当W为CH或N时，m代表0或1，当W为C =时，m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基; l代表0或1; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但当不存在键时，Z1表示H，Z2表示OH或Z1，Z2组合在一起表示O或NOR5基团，其中R5表示 H或烷基，芳烷基或芳基; R代表H，烷基，环烷基，环烷基 - 烷基或芳烷基。 化合物（1）对迄今为止报道的并且具有α1-阻断作用和5-羟色胺-2受体拮抗作用的药物的效力，对5-羟色胺2受体以外的受体的选择性，毒性，副作用等改善 组合。

公开(公告)号：US06790850B1

公开(公告)日：2004-09-14

申请号：US10089571

申请日：2002-03-29

申请人： Paul Andrew Willis ,  Roger Victor Bonnert ,  Simon Fraser Hunt ,  Iain Alistair Stewart Walters

发明人： Paul Andrew Willis ,  Roger Victor Bonnert ,  Simon Fraser Hunt ,  Iain Alistair Stewart Walters

IPC分类号： C07D51304

CPC分类号： C07D513/04

摘要： The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

摘要翻译： 本发明提供某些式（I）的噻唑并嘧啶化合物或其药学上可接受的盐或溶剂合物; 制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：US06747023B1

公开(公告)日：2004-06-08

申请号：US09762888

申请日：2001-02-12

申请人： Syozo Kobayashi ,  Satoshi Komoriya ,  Noriyasu Haginoya ,  Masanori Suzuki ,  Toshiharu Yoshino ,  Takayasu Nagahara ,  Tsutomu Nagata ,  Haruhiko Horino ,  Masayuki Ito ,  Akiyoshi Mochizuki

发明人： Syozo Kobayashi ,  Satoshi Komoriya ,  Noriyasu Haginoya ,  Masanori Suzuki ,  Toshiharu Yoshino ,  Takayasu Nagahara ,  Tsutomu Nagata ,  Haruhiko Horino ,  Masayuki Ito ,  Akiyoshi Mochizuki

IPC分类号： C07D51304

CPC分类号： C07D207/08 ,  C07D207/12 ,  C07D207/22 ,  C07D211/34 ,  C07D211/70 ,  C07D213/56 ,  C07D213/61 ,  C07D213/73 ,  C07D213/75 ,  C07D213/82 ,  C07D213/84 ,  C07D213/89 ,  C07D233/18 ,  C07D233/64 ,  C07D233/88 ,  C07D239/42 ,  C07D239/48 ,  C07D243/08 ,  C07D277/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Described in the present invention are a sulfonyl derivative represented by the following formula (I): Q1—Q2—T1—Q3—SO2—QA  (I) [wherein Q1 represents a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group, 5- or 6-membered heterocyclic group, dicyclic fused ring or tricyclic fused ring group which may have a substituent; Q2 represents a single bond, an oxygen atom, a sulfur atom, a linear or branched C1-6 alkylene group or the like; QA represents an arylalkenyl group which may have a substituent or a heteroarylalkenyl group which may have a substituent; and T1 represents a carbonyl group or the like] and a medicament comprising the same. The compound has strong FXa inhibitory action, provides prompt, sufficient and long-lasting anti-thrombus effects when orally administered, and has low side effects and is therefore useful as an excellent anticoagulant.

摘要翻译： 在本发明中描述的是由下式（I）表示的磺酰基衍生物：其中Q 1表示饱和或不饱和的5或6元环烃基，5或6元杂环基，双环稠合 可以具有取代基的环或三环稠环; Q 2表示单键，氧原子，硫原子，直链或支链C 1-6亚烷基等; Q表示芳基烯基 其可以具有取代基或可以具有取代基的杂芳基烯基; 和T 1表示羰基等]和包含该羰基的药物。 该化合物具有强的FXa抑制作用，在口服给药时提供及时，充足和持久的抗血栓作用，副作用小，因此可用作优异的抗凝血剂。

公开(公告)号：US06710041B2

公开(公告)日：2004-03-23

申请号：US10343627

申请日：2003-02-03

申请人： Patrizia Minetti ,  Assunta Di Cesare ,  Domenico Mastroianni ,  Giuseppe Campiani ,  Vito Nacci

发明人： Patrizia Minetti ,  Assunta Di Cesare ,  Domenico Mastroianni ,  Giuseppe Campiani ,  Vito Nacci

IPC分类号： C07D51304

CPC分类号： C07D513/04

摘要： A compound of formula (I): where: R=H, Cl, Br, F, I, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, or C5-C6 cycloalkyl; R1 =C1-C4 dialkylamine, where the alkyl groups are the same or different from one another, 4-alkyl-1-piperazinyl, 4-hydroxyalkyl-1-piperazinyl, 1-imidazolyl, 4-alkyl-1-piperidinyl, or 4-alkyl-1-homopiperazinyl; R2 =H, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, or CH=NOH; R3 =H, CHO; or the pharmaceutically acceptable salts thereof.

摘要翻译： 式（I）化合物：其中：R = H，Cl，Br，F，I，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基或C 5 -C 6环烷基; R1 = C1-C4二烷基胺，其中烷基彼此相同或不同，4-烷基-1-哌嗪基，4-羟基烷基-1-哌嗪基，1-咪唑基，4-烷基-1-哌啶基或4 - 烷基-1-高哌嗪基; R2 = H，C1-C4烷氧基，C1-C4烷硫基，C1-C4烷基，CHO或CH = NOH; R3 = H，CHO; 或其药学上可接受的盐。

公开(公告)号：US06583138B1

公开(公告)日：2003-06-24

申请号：US09622458

申请日：2001-01-04

申请人： Mitsuaki Miyamoto ,  Tatsuya Yoshiuchi ,  Keizo Sato ,  Motohiro Soejima ,  Takashi Sato ,  Koichi Kikuchi ,  Hiroyuki Yoshimura ,  Katsuhiro Moriya ,  Yoshinori Sakuma ,  Shigeru Akasofu ,  Koji Yamada

发明人： Mitsuaki Miyamoto ,  Tatsuya Yoshiuchi ,  Keizo Sato ,  Motohiro Soejima ,  Takashi Sato ,  Koichi Kikuchi ,  Hiroyuki Yoshimura ,  Katsuhiro Moriya ,  Yoshinori Sakuma ,  Shigeru Akasofu ,  Koji Yamada

IPC分类号： C07D51304

CPC分类号： C07D513/04

摘要： The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like. Further, the heterocyclic ring condensed benzothiazine compound of the present invention, its pharmacologically acceptable salt or hydrates thereof is represented by the following formula: In the formula, the ring Het represents an unsaturated heterocyclic ring; R1 and R2 are the same as or different from each other, and each represents halogen atom, a lower alkyl group that may be substituted with a halogen atom, a lower alkoxy group that may be substituted with a halogen atom, a lower alkyl lower alkoxy group, cyano group; D represents a lower alkylene group and the like that may have a substituent; Q represents, for example, the formula —NR20R2 (in the formula, R20 and R21 are the same as or different from each other, and each represents hydrogen atom, a lower alkyl group that may be substituted with a halogen atom, an aryl group that may have a substituent, an arylalkyl group that may have a substituent, a heteroaryl group that may have a substituent or a heteroarylalkyl group that may have a substituent, or R20 and R21 may form a 3- to 8-membered ring along with the nitrogen atom to which they are bound); and x represents an integer of from 1 to 2.

摘要翻译： 本发明提供一种新颖的杂环稠合苯并噻嗪化合物，其对组胺，白细胞三烯等参与的疾病的预防或治疗有效。 本发明的杂环稠合苯并噻嗪化合物或其药理学上可接受的盐对于预防或治疗其中化学介质如组胺，白三烯等参与的疾病是有效的，例如哮喘，过敏性鼻炎， 特应性皮炎，荨麻疹，花粉症，胃肠道过敏，食物过敏等。 此外，本发明的杂环稠合苯并噻嗪化合物，其药理学上可接受的盐或其水合物由下式表示：式中，环Het表示不饱和杂环; R1和R2彼此相同或不同，各自表示卤素原子，可以被卤素原子取代的低级烷基，可被卤素原子取代的低级烷氧基，低级烷基低级烷氧基 基团，氰基; D表示可以具有取代基的低级亚烷基等; Q表示例如式-NR20R2（式中，R20和R21彼此相同或不同，各自表示氢原子，可被卤素原子取代的低级烷基，芳基 可以具有取代基的芳基烷基，可以具有取代基的芳基烷基，可以具有取代基的杂芳基或可以具有取代基的杂芳基烷基，或者R20和R21可以与 氮原子）; x表示1〜2的整数。