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1.发明授权3-amidopyrazole derivatives, process for preparing these and pharmaceutical compositions containing them 失效3-酰氨基吡唑衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5744491A
公开(公告)日：1998-04-28
申请号：US778105
申请日：1997-01-02
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：US5616592A
公开(公告)日：1997-04-01
申请号：US394756
申请日：1995-02-27
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 , A61K31/47
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.
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3.发明授权Substituted 1-phenyl-3-pyrazolecarboxamides active on neurotensin receptors, their preparation and pharmaceutical 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物组合物
公开(公告)号：US5723483A
公开(公告)日：1998-03-03
申请号：US630761
申请日：1996-04-10
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 , A01N43/56
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 new substituted 1-phenyl-3-pyrazolecarboxamides having a great affinity for human neurotensin receptors, to a process for preparing them and to pharmaceutical compositions containing them as active principles. More particularly, this invention relates to the discovery that the affinity for neurotensin receptors, especially human neurotensin receptors, is increased by substituting the phenyl group of 1-phenyl-3-pyrazolecarboxamide compounds with particular groups.
摘要翻译： 本发明涉及对人神经降压素受体具有很大亲和力的新的取代的1-苯基-3-吡唑酰胺，其制备方法和含有它们作为活性成分的药物组合物。 更具体地，本发明涉及通过用特定基团取代1-苯基-3-吡唑甲酰胺化合物的苯基来增加对神经降压素受体，特别是人神经降压素受体的亲和性的发现。
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公开(公告)号：US5635526A
公开(公告)日：1997-06-03
申请号：US393829
申请日：1995-02-24
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 , C07D231/18 , C07D231/20
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.
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5.发明授权Substituted 1-naphthyl-3-pyrazolecarboxamides which are active on neurotensin, their preparation and pharmaceutical compositions containing them 失效在神经丝氨酸上具有活性的取代的1-萘基-3-吡唑酰胺，其制备方法和含有它们的药物组合物
公开(公告)号：US5502059A
公开(公告)日：1996-03-26
申请号：US320270
申请日：1994-10-11
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 , C07D231/10 , A61K31/44 , A61K31/535 , C07D403/00 , C07D413/00 , C07D471/16
CPC分类号： C07D401/04 , C07C243/22 , C07C255/66 , C07D231/14
摘要： The invention relates to substituted 1-naphthyl-3-pyrazolecarboxamides of formula I: ##STR1## Application: 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：应用：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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6.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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8.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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9.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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10.发明授权Hydrazine derivative compounds as intermediates for preparing substituted 1-phenyl-3-pyrazolecarboxamides active on neurotensin receptors 失效肼衍生物作为制备在神经降压素受体上有活性的取代的1-苯基-3-吡唑酰胺的中间体
公开(公告)号：US5936123A
公开(公告)日：1999-08-10
申请号：US976714
申请日：1997-11-24
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： This invention relates to intermediate compounds which are useful for making substituted 1-phenyl-3-pyrazolecarboxamides. The compounds of the invention have the formula: ##STR1## in which: R'.sub.2 and R'.sub.3 each independently represent a hydrogen, a (C.sub.1 -C.sub.6)alkyl, a (C.sub.3 -C.sub.8)cycloalkyl, a (C.sub.3 -C.sub.8)cycloalkylmethyl;or R'.sub.2 and R'.sub.3 together constitute a trimethylene, tetramethylene or pentamethylene group;R.sub.y is at position 4 or at position 5 and represents a group chosen from: cyano, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, benzyloxycarbonyl, sulpho, (C.sub.1 -C.sub.4)alkylsulphonylamino, (C.sub.1 -C.sub.4)alkylphenylsulphonylamino, carbamoyl, (C.sub.1 -C.sub.4)alkylcarboxamido; on condition that R'.sub.2 and R'.sub.3 do not simultaneously represent hydrogen and on condition that R'.sub.2 is other than methyl when R.sub.y is a sulpho group. The salts of the above compounds are also part of the invention.
摘要翻译： 本发明涉及可用于制备取代的1-苯基-3-吡唑酰胺的中间体化合物。 本发明的化合物具有下式：其中：R'2和R'3各自独立地表示氢，（C1-C6）烷基，（C3-C8）环烷基，（C3-C8）环烷基甲基; 或R'2和R'3一起构成三亚甲基，四亚甲基或五亚甲基; （C 1 -C 4）烷基磺酰基氨基，（C 1 -C 4）烷基苯基磺酰基氨基，氨基甲酰基，（C 1 -C 4）烷氧基羰基，（C 1 -C 4） C4）烷基酰胺基; 在R'2和R'3不同时表示氢的条件下，并且当R y是磺基时，R'2不同于甲基的条件。 上述化合物的盐也是本发明的一部分。
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