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1.发明申请公开(公告)号：US20110065961A1
公开(公告)日：2011-03-17
申请号：US12991931
申请日：2009-05-14
IPC分类号： C07F9/50
CPC分类号： C25B3/04 , C07F9/5022 , C07F9/509 , C07F9/65515 , Y02P20/582
摘要： Disclosed is a process for producing a phosphine derivative from a phosphine oxide derivative, which comprises the following steps: (I) mixing a phosphine oxide derivative represented by formula (1) with a chlorinating agent in a polar organic solvent to cause the reaction between these components; and (II-1) adding a salt of a metal having an ionization tendency equal to or lower than that of aluminum to the reaction mixture and carrying out the reductive reaction in the presence of aluminum or (II-2) subjecting the reaction mixture to electrolytic reduction, thereby producing a phosphine derivative represented by formula (2). ArnR3-nP═O (1) ArnR3-nP (2) In formulae (1) and (2), Ar represents an aryl group such as a phenyl group, a phenyl group having a substituent, a heteroaromatic ring group, and a heteroaromatic ring group having a substituent; R represents an aliphatic hydrocarbon group or an aliphatic hydrocarbon group having a substituent; and n represents an integer of 0 to 3.
摘要翻译： 公开了一种由氧化膦衍生物制备膦衍生物的方法，其包括以下步骤：（I）将式（1）表示的氧化膦衍生物与氯化剂在极性有机溶剂中混合，引起它们之间的反应 组件; 和（II-1）将具有等于或低于铝的电离倾向的金属的盐加入到反应混合物中并在铝的存在下进行还原反应或（II-2）使反应混合物 电解还原，从而制得由式（2）表示的膦衍生物。 ArnR3-nP=O（1）ArnR3-nP（2）式（1）和（2）中，Ar表示苯基，具有取代基的苯基，杂芳环，杂芳基等芳基 具有取代基的环基; R表示脂肪族烃基或具有取代基的脂族烃基; n表示0〜3的整数。
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公开(公告)号：US4533731A
公开(公告)日：1985-08-06
申请号：US475945
申请日：1983-03-16
IPC分类号： C07D231/56 , C07D295/067 , C07D295/092 , C07D401/06 , C07D403/04 , C07D413/06
CPC分类号： C07D231/56 , C07D295/067 , C07D295/088 , C07D401/06 , C07D403/04
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## group wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## group in ##STR4## group may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent;Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group;Z.sub.2 is a hydrogen atom or an amino group;when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.sub.2 are both amino groups;when Z.sub.1 and Z.sub.2 are both hydrogen atoms, the ##STR5## group in either W.sub.1 or W.sub.2 is a morpholino group; when Z.sub.1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z.sub.2 is a hydrogen atom;when Z.sub.1 is an amino group, Z.sub.2 is a hydrogen atom or an amino group;when Z.sub.1 is a methyl group, a methoxy group or an amino group, Z.sub.1 is in the 5-position; when Z.sub.1 is an iodine atom, Z.sub.1 is in the 5- or 7-position; and when Z.sub.1 and Z.sub.2 are both amino groups, Z.sub.1 and Z.sub.2 are in the 5- and 7-positions; and the physiologically acceptable acid addition salt thereof which compounds have pharmaceutical utility, e.g.: treating inflammation.
摘要翻译： 式（I）的化合物：其中W1和W2各自独立地是氢原子或其中Y是n-C1-6亚烷基或n-C1-6亚烷基的基团 具有C 1-6烷基取代基的基团; 并且R 1和R 2各自独立地为氢原子或C 1-6烷基，并且
基团中的 基团可以形成选自吗啉代，吡咯烷子基，哌啶子基，高哌啶基和哌嗪基的饱和杂环 除了吗啉代基以外的饱和杂环可以具有至少一个C 1-4烷基，羟基或卤素原子作为取代基; Z1是氢原子，氯原子，溴原子，碘原子，羟基，氨基，C1-3烷基或甲氧基; Z2是氢原子或氨基; 当W1和W2都是氢原子时，Z1是羟基或碘原子，Z2是氢原子，或Z1和Z2都是氨基; 当Z1和Z2都是氢原子时，W1或W2中的“IMAGE”基团是吗啉基; 当Z1是氯原子，羟基，碘原子，甲基或甲氧基时，Z2是氢原子; 当Z 1为氨基时，Z 2为氢原子或氨基; 当Z1是甲基时，甲氧基或氨基，Z1位于5-位; 当Z1为碘原子时，Z1为5-或7-位; 当Z 1和Z 2都是氨基时，Z 1和Z 2在5-和7-位; 和其生理上可接受的酸加成盐，其化合物具有药用效用，例如：治疗炎症。 -
公开(公告)号：US4751302A
公开(公告)日：1988-06-14
申请号：US739061
申请日：1985-05-29
IPC分类号： C07D231/56 , C07D295/067 , C07D295/092 , C07D401/06 , C07D403/04 , A61K31/415 , C07C87/00
CPC分类号： C07D231/56 , C07D295/067 , C07D295/088 , C07D401/06 , C07D403/04
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent;Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group;Z.sub.2 is a hydrogen atom or an amino group;when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.sub.2 are both amino groups;when Z.sub.1 and Z.sub.2 are both hydrogen atoms, the ##STR4## in either W.sub.1 or W.sub.2 is a morpholino group; when Z.sub.1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z.sub.2 is a hydrogen atom;when Z.sub.1 is an amino group, Z.sub.2 is a hydrogen atom or an amino group;when Z.sub.1 is a methyl group, a methoxy group or an amino group, Z.sub.1 is in the 5-position; when Z.sub.1 is an iodine atom, Z.sub.1 is in the 5- or 7-position; and when Z.sub.1 and Z.sub.2 are both amino groups, Z.sub.1 and Z.sub.2 are in the 5- and 7-positions;and the physiologically acceptable acid addition salt thereof.
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公开(公告)号：US5621103A
公开(公告)日：1997-04-15
申请号：US307779
申请日：1994-12-28
IPC分类号： C07D495/04 , A61K31/44 , C07D471/04
CPC分类号： C07D495/04
摘要： A tetrahydropyridine derivative having substituents on three rings represented by the following formula (1): ##STR1## (wherein A represents sulfur atom, sulfoxide group or sulfone group; R.sub.1 represents an amino group substituted with a specific substituent or a specific aliphatic oxy group; R.sub.2 and R.sub.3 each represents hydrogen atom or a hydroxy group; and m and n are each an integer of from 0 to 4; provided that when m and n are 2 or above, R.sub.2 's and R.sub.3 's may be either the same or different from each other respectively, that when A is sulfur atom and R.sub.1 is cyclohexylamino group and R.sub.2 is hydrogen atom, R.sub.3 is hydroxy group, that when A is sulfoxide group and R.sub.1 is cyclohexylamino group or 4-hydroxycyclohexylamino group, R.sub.2 is hydrogen atom and R.sub.3 is hydrogen atom or hydroxy group and that when A is sulfone group and R.sub.1 is cyclohexylamino group, R.sub.2 and R.sub.3 are each hydrogen atom) and an acid addition salt thereof is to be provided, thereby a compound which is useful as a psychotropic drug having anxiolytic and learning-improvement effects is to be provided.
摘要翻译： PCT No.PCT / JP92 / 00460 Sec。 371日期1994年12月28日第 102（e）日期1994年12月28日PCT提交1992年4月10日PCT公布。 公开号WO93 / 21189 日期：1993年10月28日由下式（1）表示的三环上具有取代基的四氢吡啶衍生物：其中A表示硫原子，亚砜基或砜基; R1表示被特定取代基取代的氨基或 特定的脂族氧基; R2和R3各自表示氢原子或羟基; m和n各自为0〜4的整数;条件是当m和n为2以上时，R2和R3可以相同 或分别不同，当A为硫原子且R 1为环己基氨基且R 2为氢原子时，R 3为羟基，当A为亚砜基且R 1为环己基氨基或4-羟基环己基氨基时，R 2为氢原子 R 3为氢原子或羟基，当A为砜基且R 1为环己基氨基时，R 2和R 3各自为氢原子）和其酸加成盐，由此可用作Psyc 提供具有抗焦虑和学习改善效果的热性药物。
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公开(公告)号：US5126448A
公开(公告)日：1992-06-30
申请号：US414892
申请日：1989-09-29
申请人： Showa Ueki , Hiromu Kawakubo , Katsuya Okazaki , Tadashi Nagatani
发明人： Showa Ueki , Hiromu Kawakubo , Katsuya Okazaki , Tadashi Nagatani
IPC分类号： C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D491/04 , C07D495/04
摘要： This invention relates to novel pyridine derivatives and 1,2,3,4-tetrahydropyridine derivatives shown by following general formula (I) or (II) and salts thereof which are useful as psychotropic medicaments: ##STR1## wherein A is S or O; R.sub.1 represents an unsubstituted or substituted alkoxy, amino, hydrazino, or 6- or 7-membered heterocyclic group having one or two nitrogen atoms with the proviso that R.sub.1 is not an alkoxy group in formula (I); R.sub.2 and R.sub.3 each represents a hydrogen atom or an unsubstituted or substituted alkyl, aryl, alkenyl, acyl, arylcarbonyl group; and m and n each represents an integer of from 0 to 4.
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公开(公告)号：US4585869A
公开(公告)日：1986-04-29
申请号：US636420
申请日：1984-07-31
IPC分类号： C07D231/56 , C07D295/092 , C07D401/06 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , C07D295/088
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## and the pharmaceutically acceptable acid addition salt thereof having antiinflammatory, analgesic and digestive tract ulcer suppressing activity.
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公开(公告)号：US4549023A
公开(公告)日：1985-10-22
申请号：US636293
申请日：1984-07-31
IPC分类号： C07D231/56 , C07D295/092 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , C07D295/088
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## and the pharmaceutically acceptable acid addition salt thereof.
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8.发明授权公开(公告)号：US08426629B2
公开(公告)日：2013-04-23
申请号：US12991931
申请日：2009-05-14
IPC分类号： C07F9/28
CPC分类号： C25B3/04 , C07F9/5022 , C07F9/509 , C07F9/65515 , Y02P20/582
摘要： Disclosed is a process for producing a phosphine derivative from a phosphine oxide derivative, which comprises the following steps: (I) mixing a phosphine oxide derivative represented by formula (1) with a chlorinating agent in a polar organic solvent to cause the reaction between these components; and (II-1) adding a salt of a metal having an ionization tendency equal to or lower than that of aluminum to the reaction mixture and carrying out the reductive reaction in the presence of aluminum or (II-2) subjecting the reaction mixture to electrolytic reduction, thereby producing a phosphine derivative represented by formula (2). ArnR3-nP═O (1) ArnR3-nP (2) In formulae (1) and (2), Ar represents an aryl group such as a phenyl group, a phenyl group having a substituent, a heteroaromatic ring group, and a heteroaromatic ring group having a substituent; R represents an aliphatic hydrocarbon group or an aliphatic hydrocarbon group having a substituent; and n represents an integer of 0 to 3.
摘要翻译： 公开了一种由氧化膦衍生物制备膦衍生物的方法，其包括以下步骤：（I）将式（1）表示的氧化膦衍生物与氯化剂在极性有机溶剂中混合，引起它们之间的反应 组件; 和（II-1）将具有等于或低于铝的电离倾向的金属的盐加入到反应混合物中并在铝的存在下进行还原反应或（II-2）使反应混合物 电解还原，从而制得由式（2）表示的膦衍生物。 ArnR3-nP = O（1）ArnR3-nP（2）在式（1）和（2）中，Ar表示芳基，例如苯基，具有取代基的苯基，杂芳族环基和杂芳族 具有取代基的环基; R表示脂肪族烃基或具有取代基的脂族烃基; n表示0〜3的整数。
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公开(公告)号：US5942505A
公开(公告)日：1999-08-24
申请号：US930910
申请日：1997-10-14
申请人： Hiromu Kawakubo , Masaru Ohno
发明人： Hiromu Kawakubo , Masaru Ohno
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Disclosed is a 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate having a water content of from 2.5 to 15.5% by weight represented by the following formula (I): ##STR1## wherein n means a number in the range of from 1/2 to 3. Since the 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate of the present invention has excellent shapeability as compared to a 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride anhydride, a tablet having satisfactory hardness can be obtained even with a relatively low compression pressure in a tableting process. Further, due to a reduction in the compression pressure needed for tableting, various advantages are brought about, such as improved disintegratability of the resultant tablet when the tablet is orally taken, so that good dissolution of 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride from the tablet can be achieved, as well as suppression of abrasion of the die and punch used in producing tablets by compression, and the like.
摘要翻译： PCT No.PCT / JP96 / 01698 Sec。 371日期1997年10月14日第 102（e）1997年10月14日PCT PCT 1996年6月19日PCT公布。 公开号WO97 / 02260 日期1997年1月23日公开是由下式（I）表示的水含量为2.5〜15.5重量％的1-（5-异喹啉磺酰基）高哌嗪盐酸氢氯化物，其中n表示在+ 由于本发明的1-（5-异喹啉磺酰基）高哌嗪盐酸水合物与1-（5-异喹啉磺酰基）高哌嗪盐酸酐相比具有优异的成形性，所以具有令人满意的硬度的片剂 即使在压片过程中压缩压力相对较低也能获得。 此外，由于压片所需的压缩压力降低，导致了各种优点，例如当口服片剂时所得片剂的崩解性提高，从而使得1-（5-异喹啉磺酰基）高哌嗪盐酸盐从 可以实现片剂，以及通过压缩抑制用于制造片剂的模具和冲头的磨损等。
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公开(公告)号：US4474964A
公开(公告)日：1984-10-02
申请号：US569524
申请日：1984-01-09
IPC分类号： C07D231/56 , C07D295/092 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , C07D295/088
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## group wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## group wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## group; and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## group; and the pharmaceutically acceptable acid addition salt thereof having antiinflammatory, analgesic and digestive tract ulcer suppressing activity.
摘要翻译： 式（I）的化合物：其中W1是氢原子或其中Y是C1-6亚烷基或具有C1-6烷基的C1-6亚烷基的基团 取代基; 并且R 1和R 2各自独立地为氢原子或C 1-6烷基，并且R 1和R 2可以与相邻的氮原子一起形成C 4-6杂环或含氮的C 4-6杂环，并且C 4-6 杂环可以具有至少一个C 1-6烷基，羟基或卤素原子; W2是氢原子或其中Z是C1-6亚烷基或具有C1-6烷基取代基的C1-6亚烷基的基团; 并且R 3和R 4各自独立地为氢原子或C 1-6烷基，并且R 3和R 4可以与相邻的氮原子一起形成C 4-6杂环或含氮的C 4-6杂环，且C 4-6 杂环可以具有至少一个C 1-6烷基，羟基或卤素原子; 当W1是氢原子时，W2是
组; 当W2是氢原子时，W1是 组; 和其药学上可接受的酸加成盐具有抗炎，止痛和消化道溃疡抑制活性。
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