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    METHOD FOR PRODUCING CYCLIC LACTAMS
    73.
    发明申请
    METHOD FOR PRODUCING CYCLIC LACTAMS 审中-公开
    用于生产环内酰胺

    公开(公告)号：WO01083444A1

    公开(公告)日：2001-11-08

    申请号：PCT/EP2001/004841

    申请日：2001-04-30

    IPC: C07D223/10 ,  C07B61/00 ,  C07D201/08 ,  C07D207/263 ,  C07D211/76 ,  C07D225/02

    CPC classification number: C07D201/08

    Abstract: The invention relates to a method for producing cyclic lactams of the formula (II), wherein n and m may each represent 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of n + m is at least 3, preferably at least 4, R and R represent C1-C6 alkyl, C5-C7 cycloalkyl or C6-C12 aryl groups, by reacting a compound of the formula (I), wherein R , R , m and n have the meaning indicated above, and R represents nitrile groups, carboxylic acid amide groups and carboxylic acid groups, with water vapor in the gaseous phase. The inventive method is further characterized in that a) the compound (I) is reacted with water vapor in the gaseous phase, adding an organic diluent (III) before or after the reaction, which diluent has a miscibility gap under certain quantitative, pressure and temperature conditions, said reaction resulting in a mixture (IV) that contains a lactam (II), b) adjusting the mixture (IV) before or after the removal of ammonia to quantitative, pressure and temperature conditions under which the diluent (III) and water are present in a liquid form and have a miscibility gap, and obtaining a two-phase system consisting of a phase (V) that has a higher proportion of diluent (III) than water, and a phase (VI) that has a higher proportion of water than diluent (III), c) separating phase (V) from phase (VI) and, d) removing from phase (V) the diluent (III) and optionally by-products selected from the group of the low-boilers, high-boilers and unreacted compound (I), and obtaining a lactam (II).

    Abstract translation: 一种用于制备式（II），其中n和m的环状内酰胺过程各自为0，1，2，3，4，5，6，7，8和9可以具有和n + m的和至少为3， 优选至少4，R <1>和R <2> C 1 -C 6 - 烷基，代表C 5 -C 7环烷基或C 6 -C 12 - 芳基，通过将式（I）化合物进行反应，其中R <1 >，R <2>，m和n是如上，R腈，羧酰胺和羧酸基团的意思是与水蒸汽在气相中通过使作为定义，与在气相中的水蒸汽，其特征在于：a）化合物（I） 之前或有机稀释剂（III）的反应之后被添加，含有水在一定的量，压力和温度条件下混溶隙，以得到混合物（IV），其包括内酰胺（II），b）将该混合物（ 转换后的IV）之前或在数量，压力和温度条件的去除氨之后在其下Verdünnungsm edium（III）和水的液体，并表现出混溶性间隙，得到的两两相体系包括包含稀释剂（III）比水高的比例的相（V），和一个相（VI）含有水的比例较高 具有作为稀释剂（III）中，c）相（V）（相VI）被分离出来和d）的相位（V），所述稀释剂（III）和任选的副产物选自低锅炉，高沸点和未反应的Verbindug的组中选择 （I）分离，得到内酰胺（II）。

    METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS
    74.
    发明申请
    METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
    代谢谷氨酸受体拮抗剂

    公开(公告)号：WO00069816A1

    公开(公告)日：2000-11-23

    申请号：PCT/US2000/008223

    申请日：2000-05-17

    IPC: C07D205/06 ,  C07D205/085 ,  C07D207/26 ,  C07D207/273 ,  C07D211/76 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  A61K31/40 ,  A61K31/445 ,  C07D207/24 ,  C07D207/40

    CPC classification number: C07D207/273 ,  C07D205/06 ,  C07D205/085 ,  C07D211/76 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12

    Abstract: This invention relates to a novel series of compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of stimulation of the human Group I metabotropic glutamate receptors, especially those designated as mGluR5. This invention also provides methods for the treatment of such disorders, as well as pharmaceutical formulations which employ the novel metabotropic glutamate receptor antagonists to which the present invention relates.

    Abstract translation: 本发明涉及一种新的一系列化合物，其可用于治疗或预防与人I代谢型谷氨酸受体（特别是称为mGluR5）的过度刺激相关的生理障碍。 本发明还提供了治疗这种病症的方法，以及使用本发明涉及的新型代谢型谷氨酸受体拮抗剂的药物制剂。

    DIPHENYL-2-PIPERIDINONE AND -2-PYRROLIDINONE DERIVATIVES HAVING ANTI-CONVULSANT AND NEUROPROTECTIVE ACTIVITY
    76.
    发明申请
    DIPHENYL-2-PIPERIDINONE AND -2-PYRROLIDINONE DERIVATIVES HAVING ANTI-CONVULSANT AND NEUROPROTECTIVE ACTIVITY 审中-公开
    具有抗生素和神经保护活性的二苯基-2-哌啶酮和2,3-吡咯烷酮衍生物

    公开(公告)号：WO1995023135A1

    公开(公告)日：1995-08-31

    申请号：PCT/GB1994000387

    申请日：1994-02-28

    Applicant: FISONS CORPORATION ,  FISONS PLC ,  MURRAY, Robert, John ,  SCHMIESING, Richard, Jon

    Inventor： FISONS CORPORATION ,  FISONS PLC

    IPC: C07D211/76

    CPC classification number: C07D207/27 ,  C07D211/76

    Abstract: Compounds of formula (I), wherein two of R , R , R and R independently represent phenyl optionally substituted by one or more groups selected from halogen, hydroxy, nitro, amino, C1-6alkyl and C1-6alkoxy; and the ramainder of R , R , R and R independently represent hydrogen or C1-6alkyl; R and R independently represent hydrogen, C1-6alkyl or C3-6cycloalkyl, or R and R together with the nitrogen atom to which they are attached form a C4-6N heterocycle; m is 1 or 2; and n is 1, 2 or 3; and pharmaceutically acceptable acid addition salt thereof; are useful in the treatment of neurodegenerative disorders, particularly epilepsy.

    Abstract translation: 式（I）化合物，其中R 1，R 2，R 3和R 4中的两个独立地表示任选被一个或多个选自卤素，羟基，硝基，氨基，C 1 -6-烷基和C 1-6烷氧基; R 1，R 2，R 3和R 4的分子独立地表示氢或C 1-6烷基; R 5和R 6独立地表示氢，C 1-6烷基或C 3-6环烷基，或R 5和R 6与它们所连接的氮原子一起形成C 4-6-6杂环; m为1或2; n为1,2或3; 及其药学上可接受的酸加成盐; 可用于治疗神经变性疾病，特别是癫痫。

    NOVEL 4-PIPERIDINYL SUBSTITUTED LACTAMES AS NEUROKININ 2 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF ASTHMA
    77.
    发明申请
    NOVEL 4-PIPERIDINYL SUBSTITUTED LACTAMES AS NEUROKININ 2 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF ASTHMA 审中-公开
    新型4-哌啶基取代的LACTAMES作为治疗ASTHMA的神经营养素2受体拮抗剂

    公开(公告)号：WO1995012577A1

    公开(公告)日：1995-05-11

    申请号：PCT/GB1994002382

    申请日：1994-10-31

    Applicant: ZENECA LIMITED

    Inventor： ZENECA LIMITED ,  MILLER, Scott, Carson

    IPC: C07D211/76

    CPC classification number: C07D401/04 ,  C07D211/76 ,  C07D403/04 ,  Y10S514/826

    Abstract: Compounds of formula (I), wherein J, B, L, X m and M have any of the meanings given in the specification, their N -oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula (I) and intermediates.

    Abstract translation: 式（I）化合物，其中J，B，L，X m和M具有说明书中给出的任何含义，它们的N-氧化物及其药学上可接受的盐是神经激肽的非肽拮抗剂 并且可用于治疗哮喘等。还公开了药物组合物，制备式（I）化合物和中间体的方法。

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