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公开(公告)号：US5585501A
公开(公告)日：1996-12-17
申请号：US453773
申请日：1995-05-30
申请人： Mitsuaki Ohtani , Takaharu Matsuura , Yoshinori Hamada , Isamu Yamada , Teruo Sakata , Kimio Takahashi , Morio Kishi
发明人： Mitsuaki Ohtani , Takaharu Matsuura , Yoshinori Hamada , Isamu Yamada , Teruo Sakata , Kimio Takahashi , Morio Kishi
IPC分类号： C07D307/935 , C07D307/83
CPC分类号： C07D307/935
摘要： A method for reduction of an allyl alcohol-type compound, specific to its allylic hydroxyl group, being carried out without any side reactions such as reduction of other portions of the compound or allylic rearrangement, which comprises treating the compound with trialkylsilane in the presence of AlX.sub.3, wherein X refers to a halogen atom.
摘要翻译： 一种还原其烯丙基羟基特异性烯丙醇型化合物的方法进行而无任何副反应，例如化合物其它部分的还原或烯丙基重排，其包括在三烷基硅烷存在下处理该化合物 AlX3，其中X表示卤素原子。
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公开(公告)号：US5124462A
公开(公告)日：1992-06-23
申请号：US690295
申请日：1991-06-18
IPC分类号： B01J23/04 , C07B61/00 , C07C303/36 , C07C303/38 , C07C311/20 , C07D493/08
CPC分类号： C07D493/08 , C07C311/20
摘要： A process for preparing a compound of Formula (I): ##STR1## wherein R' is optionally protected --CH.sub.2 OH or --COOH; R.sup.2 is phenyl or substituted phenyl; and Y is oxygen, methylene, or substituted methylene, which comprises treating a norbornyl acid amide of formula (II): ##STR2## wherein R is optionally protected --CH.sub.2 OH or --COOR.sup.1 ; R.sup.1 is hydrogen or ester-forming group; and Y is oxygen, methylene, or substituted methylene under the reaction conditions for the Hofmann Rearrangement, and then with a substituted sulfonyl halide of formula (III):R.sup.2 SO.sub.2 X (III)wherein R.sup.2 is phenyl or substituted phenyl; and X is halogen atom.
摘要翻译： PCT No.PCT / JP90 / 01330 Sec。 371日期1991年6月18日 102（e）1991年6月18日PCT 1990年10月16日PCT PCT。 公开号WO91 / 05765 日本公开日1991年5月2日。一种制备式（I）化合物的方法：其中R'任选地保护-CH 2 OH或-COOH; R2是苯基或取代的苯基; 其中Y是氧，亚甲基或取代的亚甲基，其包括处理式（II）的降冰片基酰胺：其中R是任选保护的-CH 2 OH或-COOR 1; R1是氢或酯形成基团; 并且在Hofmann重排的反应条件下，Y是氧，亚甲基或取代的亚甲基，然后用式（III）的取代磺酰卤：R2SO2X（Ⅲ）其中R2是苯基或取代的苯基; X为卤素原子。
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公开(公告)号：US5241104A
公开(公告)日：1993-08-31
申请号：US903139
申请日：1992-06-23
申请人： Mitsuaki Ohtani , Takaharu Matsuura
发明人： Mitsuaki Ohtani , Takaharu Matsuura
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.
摘要翻译： 式III的二羧酸的光学活性单酯：可用作制备光学活性天然产物或药物的中间体; 其制备方法的不对称合成方法的特征在于酸酐与（R） - 或（S） - 芳基乙酸衍生物的反应; 并声称其关键物质。
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公开(公告)号：US5117039A
公开(公告)日：1992-05-26
申请号：US447518
申请日：1989-12-07
IPC分类号： C07C69/753
CPC分类号： C07C69/753 , Y02P20/55
摘要： An optically active ester of arylacetic acid of the fomula: ##STR1## wherein R.sup.1 is hydrogen or optionally substituted C.sub.1 -C.sub.2 alkyl or phenyl or taken together to from C.sub.2 -C.sub.6 alkylene, or C.sub.2 C.sub.4 -C.sub.6 alkenylene, or bicyclic-ring; R.sup.2 is hydrogen or methyl; X is single bond or Ch.sub.2, C.dbd.O, N--R.sup.4, O, S, CHNHR.sup.4, CHCH.sub.3, CH--Ar, or CHOR.sup.5 (provided that when X is single bond or CH.sub.2, C.dbd.O, N--R.sup.4, O, or S, R.sup.1 and R.sup.2 are not simultaneouly hydrogen or methyl); R.sup.3 is hydrogen, optionally substituted alkyl, or optionally substituted aralkyl; R.sup.4 is hydrogen or amino protecting group; R.sup.5 is hydrogen or hydroxy protecting group; and Ar is optionally substituted aryl; prepared by the reaction of a 94 symmetric acid anhydride with an (R)-or (S)-arylacetic acid derivative in high optical purity; useful as a intermediate for the various optically active natural products and medicines.
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公开(公告)号：US5175341A
公开(公告)日：1992-12-29
申请号：US718366
申请日：1991-06-20
申请人： Mitsuaki Ohtani , Takaharu Matsuura
发明人： Mitsuaki Ohtani , Takaharu Matsuura
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.
摘要翻译： 式III的二羧酸的光学活性单酯：可用作制备光学活性天然产物或药物的中间体; 其制备方法的不对称合成方法的特征在于酸酐与（R） - 或（S） - 芳基乙酸衍生物的反应; 并声称其关键物质。
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6.发明授权Compound and composition of substituted hexenoic acid derivatives useful for treating thromboxane A.sub.2 mediated diseases 失效用于治疗血栓素A2介导的疾病的取代的己烯酸衍生物的化合物和组成
公开(公告)号：US5002972A
公开(公告)日：1991-03-26
申请号：US476545
申请日：1990-02-07
IPC分类号： A61K31/195 , A61P7/02 , A61P9/00 , A61P11/00 , A61P43/00 , C07C303/36 , C07C311/20 , C07C311/29 , C07C405/00 , C07D257/04
CPC分类号： C07D257/04 , C07C311/20 , C07C405/0091 , C07C2102/42 , Y10S514/822 , Y10S514/826 , Y10S514/929
摘要： Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.
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公开(公告)号：US4916231A
公开(公告)日：1990-04-10
申请号：US377409
申请日：1989-07-10
申请人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Takaharu Matsuura , Sanji Hagishita , Kaoru Seno
发明人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Takaharu Matsuura , Sanji Hagishita , Kaoru Seno
IPC分类号： C07D257/04 , C07D493/08
CPC分类号： C07D257/04 , C07D493/08
摘要： Tetrazole derivatives represented by the formula: ##STR1## wherein R is naphthyl or phenyl optionally substituted by phenyl, lower alkyo, halogen, lower alkoxy, hydroxy or acetoxy; X is methylene, dimethylmethylene or oxygen; n is an integer of 0 or 1; and p and r each is an integer of 0 or 1 and q is an integer of 1 or 2 provided that p+q+r=2; or a tautomer in tetrazole ring and a pharmaceutically acceptable salt thereof, which are useful as TXA.sub.2 receptor antagonist.
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公开(公告)号：US5047574A
公开(公告)日：1991-09-10
申请号：US448867
申请日：1989-12-12
申请人： Mitsuaki Ohtani , Takaharu Matsuura
发明人： Mitsuaki Ohtani , Takaharu Matsuura
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.
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公开(公告)号：US5534654A
公开(公告)日：1996-07-09
申请号：US98272
申请日：1993-08-03
IPC分类号： C07C59/64 , C07C259/06 , C07C271/28 , C07C311/08 , C07C311/19 , C07C311/21 , C07C311/29 , C07D209/18 , A61K31/18 , C07C259/04 , C07C311/30
CPC分类号： C07C311/19 , C07C259/06 , C07C271/28 , C07C311/08 , C07C311/21 , C07C311/29 , C07C59/64 , C07D209/18
摘要： A novel hydroxamic acid compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof having cell growth inhibition, vascularization inhibition activities and the like.The compounds of the present invention possess inhibitory activities against the growth of vascular endothelial cells and the expression of lymphocyte adhesive factors and the detransforming activity of cells transformed by ras gene, and inhibit the cell growth and are effective on inflammation and tumor.
摘要翻译： PCT No.PCT / JP92 / 01593 Sec。 371日期1993年8月3日 102（e）日期1993年8月3日PCT提交1992年12月7日PCT公布。 公开号WO91 / 12075 日期：1992年6月24日。具有细胞生长抑制，血管形成抑制活性等的新颖的下式的异羟肟酸化合物：其具有下式：（I）或其药学上可接受的盐。 本发明化合物对血管内皮细胞的生长和淋巴细胞粘附因子的表达以及由ras基因转化的细胞的转化活性具有抑制作用，抑制细胞生长，对炎症和肿瘤有效。
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公开(公告)号：US5183909A
公开(公告)日：1993-02-02
申请号：US718365
申请日：1991-06-20
申请人： Mitsuaki Ohtani , Takaharu Matsuura
发明人： Mitsuaki Ohtani , Takaharu Matsuura
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.
摘要翻译： 式III的二羧酸的光学活性单酯：可用作制备光学活性天然产物或药物的中间体; 其制备方法的不对称合成方法的特征在于酸酐与（R） - 或（S） - 芳基乙酸衍生物的反应; 并声称其关键物质。
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