Method for producing hexahydro-2-OXO-1H-thieno[3,4-D]imidazole-4-pentanoic acid
    3.
    发明授权
    Method for producing hexahydro-2-OXO-1H-thieno[3,4-D]imidazole-4-pentanoic acid 失效
    六氢-2-OXO-1H-噻吩并[3,4-D]咪唑-4-戊酸的制备方法

    公开(公告)号:US06333417B1

    公开(公告)日:2001-12-25

    申请号:US09471251

    申请日:1999-12-23

    IPC分类号: C07D49504

    CPC分类号: C07D495/04

    摘要: There is disclosed a process for producing hexahydro-2-oxo-1H-thieno[3,4-d]imidazole-4-pentanoic acid of the formula (2): which is characterized by contacting a compound of the formula (1): wherein R1 and R2 represent a hydrogen atom or a benzyl group, but R1 and R2do not simultaneously represent a hydrogen atom, and R3 represents a hydrogen atom or a carboxyl group, with sulfuric acid in the presence of an aromatic hydrocarbon.

    摘要翻译: 公开了式(2)的六氢-2-氧代-1H-噻吩并[3,4-d]咪唑-4-戊酸的制备方法:其特征在于使式(1)的化合物: 其中R 1和R 2表示氢原子或苄基,但是在芳香烃存在下,R 1和R 2不同时表示氢原子,并且R 3表示氢原子或羧基。

    Pyridine and pyrimidine derivatives and their use as inhibitors of cytokine mediated disease
    4.
    发明授权
    Pyridine and pyrimidine derivatives and their use as inhibitors of cytokine mediated disease 失效
    吡啶和嘧啶衍生物及其作为细胞因子介导的疾病的抑制剂的用途

    公开(公告)号:US06784174B1

    公开(公告)日:2004-08-31

    申请号:US09937018

    申请日:2001-09-20

    申请人: John G Cumming

    发明人: John G Cumming

    IPC分类号: C07D49504

    摘要: This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from oxygen, sulphur and nitrogen; m is 0-2; R1 is a group such as hydroxy, halo, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; each of R2 and R3 is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl; R4 is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, amino and N-C1-6alkylamino; R5 is a group such as hydrogen, halo, trifluoromethyl, cyano, nitro, amino and hydroxy, and q is 0-4; or a pharmaceutically acceptable salt or an in vivo cleavable ester thereof; processes for its preparation, a pharmaceutical composition containing it and its use in the treatment of diseases or medical conditions mediated by cytokines.

    摘要翻译: 本发明涉及式(I)的双环化合物,其中:G为N,CH或C(CN); 环X是含有1,2或3个选自氧,硫和氮的杂原子的5-或6-元稠合杂芳环; m为0-2; R 1是羟基,卤素,三氟甲基,氰基,巯基,硝基,氨基,羧基和氨基甲酰基等基团。 R 2和R 3各自为氢,卤素,C 1-6烷基,C 2-6烯基或C 2-6炔基; R 4是氢,羟基,C 1-6烷基,C 1-6烷氧基,氨基和N-C 1-6烷基氨基; R 5为氢,卤素,三氟甲基,氰基,硝基,氨基和羟基的基团,q为0-4; 或其药学上可接受的盐或其体内可裂解的酯; 其制备方法,含有它的药物组合物及其在治疗由细胞因子介导的疾病或医学病症中的用途。

    Method for producing thienopyrimidines
    5.
    发明授权
    Method for producing thienopyrimidines 失效
    噻吩并嘧啶的制备方法

    公开(公告)号:US06689885B2

    公开(公告)日:2004-02-10

    申请号:US10149125

    申请日:2002-10-21

    IPC分类号: C07D49504

    CPC分类号: C07D495/04

    摘要: The invention relates to a process for preparing compounds of the formula I In this process a 2-aminobenzothiophene-3-carboxylic ester of the formula II is reacted with a nitrile of the formula III N≡C—R1   III in solution or suspension in a solvent in the presence of an acid.

    摘要翻译: 本发明涉及一种制备式I化合物的方法。在该方法中,式II的2-氨基苯并噻吩-3-羧酸酯与溶液或悬浮液中的式III的腈在溶剂中在酸存在下反应。

    Fungicides
    6.
    发明授权
    Fungicides 失效
    杀菌剂

    公开(公告)号:US06541630B1

    公开(公告)日:2003-04-01

    申请号:US10172891

    申请日:2002-06-13

    IPC分类号: C07D49504

    CPC分类号: C07D495/04 A01N43/90

    摘要: The invention provides the use in combating fungi of compounds of general formula I wherein R1 is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, Ra, Ra3Si, RaS or RaO, where Ra is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; Z is oxygen or sulfur; M is a thiophene ring; and R3 and R4, which may be the same or different, have the same meaning as Ra or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group ORc or S(O)mRc, where Rc has the same meaning as Ra or is hydrogen or acyl and m is 0, 1 or 2; or R3 and R4 together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R1 is hydrogen.

    摘要翻译: 本发明提供了用于对抗通式I化合物的用途,其中R 1是氢,羟基,酰基,酰氧基,任选取代的氨基,R a,R 3 Si,RaS或RaO,其中R a是任选取代的烷基,任选取代的链烯基, 炔基,任选取代的环烷基,任选取代的环烯基,任选取代的芳基或任选取代的杂环基; Z是氧或硫; M是噻吩环; 和R 3和R 4可以相同或不同,具有与R a相同的含义或可以是任选取代的氨基,氢,卤素,氰基,硝基或基团OR c或S(O)m R c,其中R c具有相同的含义 为Ra或为氢或酰基,m为0,1或2; 或R 3和R 4与它们所连接的原子一起形成任选取代的碳环或杂环; 以及R1为氢的化合物的互变异构体。

    Benzothieno[3,2-c]pyridines as &agr;2 antagonists
    7.
    发明授权
    Benzothieno[3,2-c]pyridines as &agr;2 antagonists 有权
    苯并噻吩并[3,2-c]吡啶作为α2拮抗剂

    公开(公告)号:US06774129B2

    公开(公告)日:2004-08-10

    申请号:US10123338

    申请日:2002-04-16

    IPC分类号: C07D49504

    CPC分类号: C07D495/04

    摘要: The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.

    摘要翻译: 本发明涉及配制N-氧化物的化合物,其药学上可接受的加成盐和立体化学异构形式,其中每个R 1独立地是氢,卤素,C 1-6烷基,硝基,羟基或C 1-4烷氧基; Alk是C1-6烷二基; n为1或2; p为0,1或2; D是具有中枢性α2-肾上腺素受体拮抗剂活性的任选取代的单环,双环或三环含氮杂环。 它还涉及它们的制备,包含它们的组合物及其作为药物的用途。

    Compounds
    10.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号:US06342601B1

    公开(公告)日:2002-01-29

    申请号:US09214755

    申请日:1999-01-12

    IPC分类号: C07D49504

    摘要: The invention provides certain pyrrolo-, thieno-, furano- and pyrazolo-[3,4-d]pyridazinones, processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.

    摘要翻译: 本发明提供某些吡咯并噻吩并呋喃并吡唑并[3,4-d]哒嗪酮,其制备方法,含有它们的药物组合物,制备药物组合物的方法和涉及其用途的治疗方法。