• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Novel substituted benzamides of the formula <IMAGE> XXI wherein R1, R2, R3, R4, R5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful in disorders relating to impaired gastric motility.
    公开号:SU1605925A3
    申请号:SU884355470
    申请日:1988-03-18
    公开日:1990-11-07
    发明作者:Монкович Иво；Виллнер Дэвид
    申请人:Бристоль-Мейерз Сквибо Компани (Фирма)；
    IPC主号:
    专利说明:

    Table 1
    The number of animals 4
    Editor A. Motesh
    Compiled by V.M. Kusheva, Tehred L. Serdyukova
    Order 3458
    Circulation 315
    VNIIPI State Committee for Inventions and Discoveries at the State Committee on Science and Technology of the USSR 113035, Moscow, Zh-35, Raushsk nab. 4/5
    Production and Publishing Combine Patent, Uzhgorod, st. Gagarin, tO.I
    table 2
    Proofreader M.Maksimishinets
    Subscription
    权利要求:
    Claims (2)
    [1]
    <claim-text> Formula of Invention </ claim-text><claim-text> Method for producing a substituted bin - </ claim-text><claim-text> or its pharmaceutically acceptable <sup>! </ sup> salts, or its solvate, characterized in that the compound </ claim-text><claim-text> demethylated and the resulting compound of the formula </ claim-text><claim-text> 10 </ claim-text><claim-text> 9., 1605925 </ claim-text><claim-text> interact with the compound, where b is the removed group, </ claim-text><claim-text> formula in the presence of a base, followed by isolation of the target product or transfer it to a pharmaceutically acceptable salt or solvate. </ claim-text><claim-text> Table 1 </ claim-text><claim-text> Example Connection </ claim-text><claim-text> N-spiperone </ claim-text><claim-text> substitution </ claim-text><claim-text> IR </ claim-text><claim-text> nM </ claim-text><claim-text> Antagonism to </ claim-text><claim-text> apomorphine-induced vomiting in dogs <sup> </ sup> H <sub> I </ sub>, mg / kg, </ claim-text><claim-text> p. </ claim-text><claim-text> Antagonism of dysplatin-induced vomiting in ferrets </ claim-text><claim-text> Dose, mg / kg, i.v.
    [2]
    ‘2 (number of animals 3) </ claim-text><claim-text> Protection, </ claim-text><claim-text> 7 </ claim-text><table border = "1"><tr> <td>1 </ td> <td>&gt; 1000 </ td> <td>&gt; 3 </ td> <td>3 </ td> <td>95 </ td> </ tr><tr> <td>2 </ td> <td>&gt; 1000 </ td> <td>&gt; 3 </ td> <td>3 </ td> <td>100 </ td> </ tr><tr> <td>Methaclopr amide </ td> <td>310 </ td> <td>0.5 </ td> <td>3 * </ td> <td>89 </ td> </ tr><tr> <td>Alizaprid </ td> <td>290 </ td> <td>0.3 </ td> <td>3 </ td> <td>27 </ td> </ tr><tr> <td>Klebobrid </ td> <td>11 </ td> <td>0.04 </ td> <td>3 </ td> <td>70 </ td> </ tr><tr> <td>Domperidone </ td> <td>4.1 </ td> <td>0.2 </ td> <td>3 </ td> <td>50 </ td> </ tr></ table><claim-text> * Number of animals 4. </ claim-text><claim-text> Table 2 </ claim-text><table border = "1"><tr> <td rowspan = "2"><claim-text> Connection </ claim-text> </ td> <td colspan = "2"><claim-text> Subcutaneous </ claim-text> </ td> <td colspan = "2"><claim-text> introduction * &quot; </ claim-text> </ td> <td colspan = "2"><claim-text> Oral </ claim-text> </ td> <td><claim-text> ** </ claim-text><claim-text> introduction </ claim-text> </ td> </ tr><tr> <td><claim-text> Number </ claim-text> </ td> <td><claim-text> Dose <sub> y </ sub> νπίκτ · </ claim-text> </ td> <td><claim-text> 2 </ claim-text> </ td> <td><claim-text> Protection, </ claim-text><claim-text> 7 </ claim-text> </ td> <td><claim-text> Number </ claim-text> </ td> <td><claim-text> Dose, </ claim-text><claim-text> mg / kg · </ claim-text> </ td> <td><claim-text> Protection, 7 </ claim-text> </ td> </ tr><tr> <td><claim-text> 1 </ claim-text> </ td> <td><claim-text> 2 </ claim-text> </ td> <td><claim-text> 0.084 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 95 </ claim-text> </ td> <td><claim-text> 2 </ claim-text> </ td> <td><claim-text> 0.1 </ claim-text> </ td> <td><claim-text> 93 </ claim-text> </ td> </ tr><tr> <td><claim-text> </ claim-text> </ td> <td><claim-text> 2 </ claim-text> </ td> <td><claim-text> 0.030 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 100 </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> </ tr><tr> <td><claim-text> </ claim-text> </ td> <td><claim-text> 2 </ claim-text> </ td> <td><claim-text> 0.010 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 92 </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> </ tr><tr> <td><claim-text> </ claim-text> </ td> <td><claim-text> 2 · </ claim-text> </ td> <td><claim-text> 0.008 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 46 </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> </ tr><tr> <td><claim-text> Metoclopramide </ claim-text> </ td> <td><claim-text> 4 </ claim-text> </ td> <td><claim-text> 2.5 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 92 </ claim-text> </ td> <td><claim-text> 3 </ claim-text> </ td> <td><claim-text> 8.5 </ claim-text> </ td> <td><claim-text> 86 </ claim-text> </ td> </ tr><tr> <td><claim-text> </ claim-text> </ td> <td><claim-text> 3 </ claim-text> </ td> <td><claim-text> 0.8 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 92 </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> </ tr><tr> <td><claim-text> </ claim-text> </ td> <td><claim-text> 4 </ claim-text> </ td> <td><claim-text> 0.2 </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> 58 </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> <td><claim-text> - </ claim-text> </ td> </ tr><tr> <td colspan = "2"><claim-text> Compound dose per </ claim-text> </ td> <td colspan = "4"><claim-text> 1 h before cisplatin administration, </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> </ tr><tr> <td colspan = "2"><claim-text> Compound dose per </ claim-text> </ td> <td><claim-text> 5 min to </ claim-text> </ td> <td colspan = "3"><claim-text> cisplatin administration. </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> <td><claim-text> </ claim-text> </ td> </ tr><tr> <td><claim-text> </ claim-text> </ td> <td colspan = "3">
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    FR1525M|1961-07-25|1962-11-16|Ile De France|New antiemetic drugs.|
    US3966957A|1972-04-03|1976-06-29|A. H. Robins Company, Incorporated|Method for controlling emesis with N-benzamides and thiobenzamides|
    US4189495A|1974-09-17|1980-02-19|Synthelabo|2-Methoxy-benzamide derivatives|
    GB1507462A|1974-03-21|1978-04-12|Gallardo Antonio Sa|N-heterocyclic substituted benzamides methods for their preparation and compositions containing them|
    US4039672A|1975-01-11|1977-08-02|Societe D'etudes Scientifiques Et Industrielles De L'ile-De-France|N- 2-methoxy 4,5-azimido benzamide and its pharmaceutically acceptable salts|
    US4197243A|1975-04-02|1980-04-08|Yamanouchi Pharmaceutical Co., Ltd.|N-1-Benzyl-3-pyrrolidinyl-4-dimethylamino benzamide derivatives|
    FR2313935B1|1975-06-10|1979-04-27|Ile De France|
    FI763021A|1975-11-03|1977-05-04|Thomae Gmbh Dr K|
    FR2342064B1|1976-02-26|1979-10-05|Buzas Andre|
    GB1574418A|1976-11-16|1980-09-03|Anphar Sa|Piperidine derivatives|
    US4207327A|1977-08-19|1980-06-10|A. H. Robins Company, Inc.|N-benzamides and their amino precursors|
    EP0067615B1|1981-06-17|1986-01-08|Beecham Group Plc|Alkylthio derivatives of azabicyclobenzamides, their preparation and pharmaceutical compositions|
    CA1183847A|1981-10-01|1985-03-12|Georges Van Daele|N-benzamide derivatives|
    JPH0326195B2|1982-09-09|1991-04-10|Suntory Ltd|
    US4593034A|1984-04-06|1986-06-03|A. H. Robins Company, Inc.|2-alkoxy-N-benzamides and thiobenzamides|
    US4808624A|1984-06-28|1989-02-28|Bristol-Myers Company|Pharmacologically active substituted benzamides|
    US4820715A|1984-06-28|1989-04-11|Bristol-Myers Company|Anti-emetic quinuclidinyl benzamides|
    US4605652A|1985-02-04|1986-08-12|A. H. Robins Company, Inc.|Method of enhancing memory or correcting memory deficiency with arylamido -azabicycloalkanes|
    DE385517T1|1985-03-14|1991-07-25|Beecham Group P.L.C., Brentford, Middlesex, Gb|MEDICINES FOR TREATING EMERGENCY.|
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    GB8718345D0|1987-08-03|1987-09-09|Fordonal Sa|N-substituted benzamides|
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    EP0303445A1|1987-08-13|1989-02-15|Walton S.A.|Clebopride transdermal patch|
    JPH02207065A|1989-02-07|1990-08-16|Teikoku Chem Ind Corp Ltd|Benzamide derivative|
    AU632387B2|1989-12-05|1992-12-24|Marion Merrell Dow Inc.|Pyridinium hydrochloride metoclopramide demethylation|
    US5236931A|1992-03-26|1993-08-17|A. H. Robins Company, Incorporated|2-substituted benzamide and benzoate derivatives of 3-aminoquinuclidine and 3-quinuclidinol|
    SK164795A3|1993-06-23|1996-10-01|Chugai Pharmaceutical Co Ltd|Benzene derivatives|
    JP3235913B2|1993-07-30|2001-12-04|エーザイ株式会社|Aminobenzoic acid derivative|
    US5723103A|1994-12-09|1998-03-03|Vanderbilt University|Substituted benzamides and radioligand analogs and methods of use|
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    US6852716B2|2002-02-15|2005-02-08|Pfizer Inc|Substituted-aryl compounds for treatment of disease|
    AU2003214936A1|2002-02-20|2003-09-09|Pharmacia And Upjohn Company|Azabicyclic compounds with alfa7 nicotinic acetylcholine receptor activity|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    US07/051,880|US4820715A|1984-06-28|1987-05-18|Anti-emetic quinuclidinyl benzamides|
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