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31.发明授权Heterocyclic substituted 2-acylamino-5-thiazoles, their preparation and pharmaceutical compositions containing them 失效杂环取代的2-酰基氨基-5-噻唑，其制备方法和含有它们的药物组合物
公开(公告)号：US5380736A
公开(公告)日：1995-01-10
申请号：US205408
申请日：1994-03-03
IPC分类号： A61K31/425 , A61K31/426 , A61K31/427 , A61P1/00 , A61P1/04 , A61P1/18 , A61P25/04 , A61P29/00 , A61P35/00 , A61P43/00 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/46 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
CPC分类号： C07D417/06 , C07D277/40 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Heterocyclic substituted 2-acylamino-5-thiazoles, their preparation and pharmaceutical compositions containing them.A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
摘要翻译： 杂环取代的2-酰基氨基-5-噻唑，其制备方法和含有它们的药物组合物。 下式的2-酰基氨基噻唑：取代的烷基; RIV是未取代或取代的环烷基，芳基如苯基或杂环基; RV是取代的烷基，取代的羧基如酯或酰胺; 或RIV和RV一起表示可在苯基上取代的苯氧基亚烷基; Z是杂环的。 吲哚基 或化合物（I）的盐。
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32.发明授权Substituted 1-phenyl-3-pyrazolecarboxamides active on neurotensin receptors, their preparation and pharamaceutical compositions containing them 失效对神经降压素受体有活性的取代的1-苯基-3-吡唑酰胺，其制剂和含有它们的药用组合物公开(公告)号：US06172239B2
公开(公告)日：2001-01-09
申请号：US09374697
申请日：1999-08-16
申请人： Bernard Labeeuw , Danielle Gully , Francis JeanJean , Jean-Charles Molimard , Robert Boigegrain
发明人： Bernard Labeeuw , Danielle Gully , Francis JeanJean , Jean-Charles Molimard , Robert Boigegrain
IPC分类号： C07D23114
CPC分类号： C07D401/10 , C07C243/22 , C07C255/66 , C07C309/45 , C07C309/47 , C07C311/21 , C07C2601/02 , C07C2601/08 , C07C2602/10 , C07D231/14 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/04 , C07D453/02
摘要： The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.
摘要翻译： 本发明涉及下式的化合物：该化合物对神经降压素受体具有强烈的亲和力。
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公开(公告)号：US5965579A
公开(公告)日：1999-10-12
申请号：US976309
申请日：1997-11-21
申请人： Bernard Labeeuw , Danielle Gully , Francis Jeanjean , Jean-Charles Molimard , Robert Boigegrain
发明人： Bernard Labeeuw , Danielle Gully , Francis Jeanjean , Jean-Charles Molimard , Robert Boigegrain
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/435 , A61K31/439 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , A61P1/00 , A61P25/00 , A61P35/00 , A61P43/00 , C07C61/20 , C07C62/34 , C07C243/22 , C07C255/66 , C07C309/45 , C07C309/47 , C07C311/21 , C07D231/12 , C07D231/14 , C07D231/38 , C07D233/62 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/04 , C07D413/12 , C07D453/02
CPC分类号： C07D401/10 , C07C243/22 , C07C255/66 , C07C309/45 , C07C309/47 , C07C311/21 , C07D231/14 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/04 , C07D453/02 , C07C2101/02 , C07C2101/08 , C07C2102/10
摘要： The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.
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34.发明授权
公开(公告)号：US5744493A
公开(公告)日：1998-04-28
申请号：US775150
申请日：1996-12-31
IPC分类号： A61K31/415 , A61K31/41 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P1/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/18 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D409/04 , C07D413/14 , C07D417/04 , C07D453/02 , C07D453/06 , C07D495/04
CPC分类号： C07D403/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/06 , Y02P20/55
摘要： The present invention relates to new pyrazole derivatives possessing an amide group substituted with an amino acid or one of its derivatives at position 3 and variously substituted in positions 1, 2, 4 or 5 of the pyrazole ring, to a process for preparing these and to pharmaceutical compositions containing the said pyrazole derivatives as an active ingredient.
摘要翻译： 本发明涉及具有酰胺基的新的吡唑衍生物，其被取代为吡唑环的氨基酸或其位置3的衍生物，或其取代的吡唑环的第1,2,4或5位，其制备方法和 含有所述吡唑衍生物作为活性成分的药物组合物。
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公开(公告)号：US5656631A
公开(公告)日：1997-08-12
申请号：US473580
申请日：1995-06-07
申请人： Robert Boigegrain , Roger Brodin , Jean Paul Kan , Dominique Olliero , Camille Georges Wermuth , Jean-Jacques Bourguignon , Paul Worms
发明人： Robert Boigegrain , Roger Brodin , Jean Paul Kan , Dominique Olliero , Camille Georges Wermuth , Jean-Jacques Bourguignon , Paul Worms
IPC分类号： C07D237/04 , C07D237/12 , C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D451/02 , C07D451/04 , C07D487/04 , A61K31/50
CPC分类号： C07D237/04 , C07D237/12 , C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D451/02 , C07D451/04 , C07D487/04
摘要： The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
摘要翻译： 本发明涉及可用作胆碱能受体的配体，特别是M1型受体的下式的哒嗪衍生物：（I）图像（IA）（ⅠB）。
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36.发明授权Substituted 1-naphthyl-3-pyrazolecarboxamides which are active on neurotensin 失效在神经降压素上有活性的取代的1-萘基-3-吡唑酰胺
公开(公告)号：US5585497A
公开(公告)日：1996-12-17
申请号：US442105
申请日：1995-05-16
申请人： Bernard Labeeuw , Danielle Gully , Francis Jeanjean , Jean-Charles Molimard , Robert Boigegrain
发明人： Bernard Labeeuw , Danielle Gully , Francis Jeanjean , Jean-Charles Molimard , Robert Boigegrain
IPC分类号： A61K31/415 , A61K31/435 , A61P1/00 , A61P1/04 , A61P1/06 , A61P1/14 , A61P25/00 , A61P25/18 , A61P43/00 , C07C243/22 , C07C255/66 , C07D231/14 , C07D401/04 , C07D401/14 , C07D231/12 , C07D403/12 , C07D413/10
CPC分类号： C07D401/04 , C07C243/22 , C07C255/66 , C07D231/14
摘要： The invention relates to substituted 1-naphyl-3-pyrazolecarboxamides of formula I: ##STR1## These compounds are useful for the treatment of neuropsychiatric disorders, especially those associated with a dysfunction of the dopaminergic systems.
摘要翻译： 本发明涉及式I的取代的1-萘基-3-吡唑酰胺：这些化合物可用于治疗神经精神障碍，特别是与多巴胺能系统的功能障碍相关的疾病。
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37.发明授权Use of 5-alkylpyridazine derivatives as drugs active on the cholinergic system 失效作为药物活性成分的5-烷基吡啶衍生物的使用
公开(公告)号：US5081119A
公开(公告)日：1992-01-14
申请号：US475490
申请日：1990-02-07
IPC分类号： A61K31/50 , A61K31/535 , A61P25/28 , C07D237/20
CPC分类号： A61K31/50 , A61K31/535 , C07D237/20
摘要： The invention relates to the use of 5-alkylpyridazine derivatives of the formula ##STR1## in which R.sub.1 is a C.sub.1 -C.sub.4 alkyl group or a phenyl group and R.sub.2 and R.sub.3 independently are a C.sub.1 -C.sub.4 alkyl group, or R.sub.2 and R.sub.3, taken with the nitrogen atom to which they are bonded, form a morpholino group, or one of their pharmaceutically acceptable salts, for the preparation of pharmaceutical compositions for combating pathological conditions associated with a cortical cholinergic deficiency, especially for the treatment of degenerative syndromes associated with senescence.
摘要翻译： 本发明涉及式（Ⅱ）的5-烷基哒嗪衍生物，其中R 1是C 1 -C 4烷基或苯基，R 2和R 3独立地是C 1 -C 4烷基，或R 2和 R3与其键合的氮原子一起形成吗啉基或其药学上可接受的盐之一，用于制备用于对抗与皮层胆碱能缺乏相关的病理状况的药物组合物，特别是用于治疗退行性综合征 与衰老有关。
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