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1. 发明申请

WO1992013839A1 DIHYDROPYRIDINE COMPOUNDS, AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：二氢吡啶化合物及其制备方法
公开(公告)号：WO1992013839A1
公开(公告)日：1992-08-20
申请号：PCT/JP1992000076
申请日：1992-01-28
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD. , ITO, Kiyotaka , AKAMATSU, Hidekazu , INOUE, Keizo , ONOMURA, Osamu , HAMATANI, Takeshi , UEDA, Yoichiro , ESUMI, Kimio
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： The invention relates to dihydropyridines of formula (I) wherein W represents a cyano or halo alkyl group in which the alkyl group has 1 to 6 carbon atoms; R represents an alkyl group having 1 to 6 carbon atoms; R and R , which may be the same or different, each represents an alkyl group having 1 to 6 carbon atoms; X and Y, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a halogen atom or a nitro group; Ar represents an optionally substituted aryl group and A represents an alkylene group having 1 to 10 carbon atoms; or an acid addition salt thereof. The invention also includes methods of producing the said dihydropyridines.
摘要翻译：本发明涉及式（I）的二氢吡啶，其中W表示烷基具有1至6个碳原子的氰基或卤代烷基; R 1表示碳原子数1〜6的烷基， R 2和R 3可以相同或不同，各自表示具有1至6个碳原子的烷基; X和Y可以相同或不同，各自表示氢原子，具有1-6个碳原子的烷基，卤素原子或硝基; Ar表示可以具有取代基的芳基，A表示碳原子数1〜10的亚烷基。或其酸加成盐。本发明还包括生产所述二氢吡啶的方法。

2. 发明申请

WO1995023869A1 PROCESS FOR PRODUCING (R)-2-AMINO-1-PHENYLETHANOL OR HALOGENATED DERIVATIVE THEREOF, PROCESS FOR PRODUCING OPTICALLY ACTIVE PHENYLSERINE OR HALOGENATED DERIVATIVE THEREOF, AND NOVEL COMPOUND 3-(3-CHLOROPHENYL)SERINE 审中-公开
标题翻译：用于制备（R）-2-氨基-1-苯基乙醇或其衍生物衍生物的方法，用于生产光学活性苯基或其衍生物的方法，以及3-（3-氯苯乙烯）新型化合物
公开(公告)号：WO1995023869A1
公开(公告)日：1995-09-08
申请号：PCT/JP1995000337
申请日：1995-03-02
申请人： DAICEL CHEMICAL INDUSTRIES, LTD. , NIKAIDO, Teruyuki , KAWADA, Naoki , HAMATANI, Takeshi , UEDA, Yoichiro
发明人： DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C12P13/00
CPC分类号： C12P13/001 , C12P13/06 , C12P41/00
摘要： (R)-2-Amino-1-phenylethanol or a halogenated derivative thereof is produced by treating threo-3-phenylserine or an enantiomeric mixture of halogenated derivatives thereof with a tyrosine decarboxylase or a microorganism of the genus Enterococcus, Lactobacillus, Providencia, Fusarium or Gibberella. Optically active threo-3-phenylserine or halogenated derivative thereof is produced by leaving intact only one of the enantiomers of an enantiomeric mixture of a halogenated derivative of threo-3-phenylserine. A novel substance, 3-(3-chlorophenyl)serine, is produced which functions as a reaction substrate in the above process. The process enables (R)-2-amino-1-phenylethanol or a halogenated derivative thereof and optically active threo-3-phenylserine or halogenated derivative thereof to be obtained at a low cost on an industrial level.
摘要翻译：（R）-2-氨基-1-苯基乙醇或其卤代衍生物是通过将苏氨酸-3-苯基丝氨酸或其卤代衍生物的对映异构体混合物与酪氨酸脱羧酶或肠球菌属，乳杆菌属，普罗威登氏菌属，镰刀菌属的微生物或赤霉素。通过仅保留苏式-3-苯基丝氨酸的卤代衍生物的对映异构体混合物的完整的一个对映异构体来制备光学活性的苏氨酸-3-苯基丝氨酸或其卤代衍生物。制备了在上述方法中用作反应底物的新物质3-（3-氯苯基）丝氨酸。该方法可以在工业上以低成本获得（R）-2-氨基-1-苯基乙醇或其卤化衍生物和光学活性的苏氨酸-3-苯基丝氨酸或其卤代衍生物。

3. 发明申请

WO1993015064A1 1,3-OXAZIN-4-ONE DERIVATIVE, HERBICIDE CONTAINING THE SAME, AND NOVEL INTERMEDIATE FOR PRODUCING THE SAME 审中-公开
标题翻译：含有它们的1,3-氧杂环己烯-4-酮衍生物，除草剂，以及用于生产它的新型中间体
公开(公告)号：WO1993015064A1
公开(公告)日：1993-08-05
申请号：PCT/JP1993000105
申请日：1993-01-28
申请人： MITSUBISHI PETROCHEMICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD. , HASEBE, Hirokazu , HAMATANI, Takeshi , HAYASHIZAKI, Keiichi , USUI, Yoshihiro , YASUMOTO, Chiharu , GO, Atsushi , HIKIDO, Mitsuru , TAMURA, Kumiko , JIKIHARA, Kazuo
发明人： MITSUBISHI PETROCHEMICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D265/05
CPC分类号： A01N43/86 , C07C251/04 , C07D265/06 , C07D265/10 , C07D319/06
摘要： A 1,3-oxazin-4-one derivative, represented by general formula (I), which is useful as a herbicide because it has a wide herbicidal spectrum and a potent herbicidal activity and is highly safe for useful crops, wherein R represents lower alkyl, lower alkenyl, lower alkynyl, optionally substituted aryl or optionally substituted aralkyl; R represents hydrogen or lower alkyl; R represents lower alkyl, optionally substituted aryl or optionally substituted aralkyl; and R and R represent each independently lower alkyl, or R and R are combined with each other to represent, together with the carbon atom to which they are bonded, a 3- to 8-membered carbocyclic group which may have a lower alkyl branch.
摘要翻译：由通式（I）表示的1,3-恶嗪-4-酮衍生物，其可用作除草剂，因为它具有宽的除草谱和强的除草活性，对有用的作物是高度安全的，其中R 1 表示低级烷基，低级烯基，低级炔基，任选取代的芳基或任选取代的芳烷基; R 2表示氢或低级烷基; R 3表示低级烷基，任选取代的芳基或任选取代的芳烷基; R 4和R 5各自独立地表示低级烷基，或者R 4和R 5彼此结合，与它们所键合的碳原子一起表示3-8 可以具有低级烷基支链的碳环基团。

4. 发明申请

WO1995020576A1 4-(2-(3-ARYLOXY-2-HYDROXYPROPYLAMINO ALKYLOXY)-5-NITROPHENYL)-1,4-DIHYDROPYRIDINES AS ANTIHYPERTENSIVE AGENTS 审中-公开
标题翻译： 4-（2-（3-氰基-2-羟基丙烯酰氧基）-5-硝基苯基）-1,4-二氢吡啶作为抗菌剂
公开(公告)号：WO1995020576A1
公开(公告)日：1995-08-03
申请号：PCT/JP1995000100
申请日：1995-01-27
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD. , ITO, Kiyotaka , AKAMATSU, Hidekazu , INOUE, Keizo , ONOMURA, Osamu , HAMATANI, Takeshi , UEDA, Yoichiro , ESUMI, Kimio
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D211/90
CPC分类号： C07D401/12 , C07D211/90
摘要： A dihydropyridine compound of formula (I), wherein: (1) W represents a cyano or halo lower alkyl group; R represents a lower alkyl group; R and R , which may be the same or different, each represents a lower alkyl group; A represents an alkylene group having 1 to 10 carbon atoms; Ar represents an indolyl group, an oxotetrahydronaphthyl group, or a hydroxyl-, cyano-, nitro- or acetyl substituted phenyl group, or (2) W represents a cyano or trifluoromethyl group, R , R and R each represents a methyl group, A represents a tetramethylene group, and Ar represents a 2-tolyl or 2-chlorophenyl group, or (3) W represents a trifluoromethyl group, R and R each represents a methyl group, R represents a methyl or ethyl group, A represents a hexamethylene group, and Ar represents a phenyl group, or (4) W represents a trifluoromethyl group, R and R each represents a methyl group, R represents an isopropyl group, A represents a tetramethylene group, and Ar represents a phenyl group, or an acid addition salt thereof. The invention also provides the individual optical isomers of the compounds of formula (I). The invention further includes processes for the production of the above compounds, pharmaceutical compositions containing same and the use thereof.
摘要翻译：式（I）的二氢吡啶化合物，其中：（1）W表示氰基或卤代低级烷基; R 1表示低级烷基; R 2和R 3可以相同或不同，各自表示低级烷基; A表示碳原子数1〜10的亚烷基。 Ar表示吲哚基，氧代四氢萘基或羟基，氰基，硝基或乙酰基取代的苯基，或（2）W表示氰基或三氟甲基，R 1，R 2， 3>各自表示甲基，A表示四亚甲基，Ar表示2-甲苯基或2-氯苯基，或（3）W表示三氟甲基，R 1和R 3各自表示甲基基团，R 2表示甲基或乙基，A表示六亚甲基，Ar表示苯基，或（4）W表示三氟甲基，R 1和R 2各自表示甲基 R 3表示异丙基，A表示四亚甲基，Ar表示苯基或其酸加成盐。本发明还提供式（I）化合物的各个光学异构体。本发明还包括生产上述化合物的方法，含有它们的药物组合物及其用途。

5. 发明申请

WO1994002463A1 ANTIHYPERTENSIVE 1,4-DIHYDROPYRIDINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：抗真菌的1,4-二氢吡啶衍生物及其制备方法
公开(公告)号：WO1994002463A1
公开(公告)日：1994-02-03
申请号：PCT/JP1993001057
申请日：1993-07-27
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD. , ITO, Kiyotaka , AKAMATSU, Hidekazu , INOUE, Keizo , ONOMURA, Osamu , HAMATANI, Takeshi , UEDA, Yoichira , ESUMI, Kimio
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D211/90
CPC分类号： C07D401/04 , C07D211/90 , C07D401/12
摘要： An antihypertensive dihydropyridine compound of formula (1) characterised in that one of W or R represents a halo (lower) alkyl group (especially CF3); the other of W or R represents a lower alkyl group; R represents a lower alkyl group; R represents a hydrogen atom or a lower alkyl group; Ar represents an optionally substituted aryl group; A represents a cyclo(lower)alkylene group, a lower or higher alkylene group optionally interrupted by a member selected from the group consisting of oxa, imino, substituted imino, a heterocyclic group, a vinylene group, a phenylene group, an -0-phenylene-group, a phenylene-0-group, an -0-phenylene-0-group (the phenylene group in each of which may contain a lower alkoxy substituent) and a group of the formula: -Het-Q- (wherein Het is a bivalent heterocyclic group, and Q is a lower alkylene group); B represents a direct link or -CH2O-; Ar represents a pyridyl group or a phenyl group of formula (2) wherein X and Y, which may be the same or different, each represents a hydrogen atom, a halogen atom, a halo(lower)alkyl group, a lower alkoxy group which may contain an amino substituent, or a nitro group, and acid addition salts thereof.
摘要翻译：式（1）的抗高血压二氢吡啶化合物，其特征在于W或R 1中的一个表示卤代（低级）烷基（特别是CF 3）。 W或R 1中的另一个表示低级烷基; R 2表示低级烷基; R 3表示氢原子或低级烷基; Ar 2表示任选取代的芳基; A表示环（低级）亚烷基，低级或高级亚烷基，任选地被选自氧杂，亚氨基，取代亚氨基，杂环基，亚乙烯基，亚苯基，-O-亚烷基，亚苯基，亚苯基-O-基，-O-亚苯基-O-基（各自可以含有低级烷氧基取代基的亚苯基）和式-Het-Q-（其中Het 是二价杂环基，Q是低级亚烷基）; B代表直链或-CH2O-; Ar 1表示式（2）的吡啶基或苯基，其中X和Y可以相同或不同，表示氢原子，卤素原子，卤代（低级）烷基，低级可以含有氨基取代基的烷氧基或硝基，及其酸加成盐。

6. 发明申请

WO1993003014A1 DIHYDROPYRIDINE DERIVATIVES, AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：二氢吡啶衍生物及其制备方法
公开(公告)号：WO1993003014A1
公开(公告)日：1993-02-18
申请号：PCT/JP1992001023
申请日：1992-08-10
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD. , ITO, Kiyotaka , AKAMATSU, Hidekazu , INOUE, Keizo , ONOMURA, Osamu , HAMATANI, Takeshi , UEDA, Yoichiro , ESUMI, Kimio
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： A dihydropyridine compound of formula (I) wherein W represents a cyano or halo alkyl group, the alkyl group of which is straight chained or branched and contains 1 to 6 carbon atoms; R, R and R , which may be the same or different, each represent a saturated hydrocarbon group which is straight chained or branched and which contains 1 to 6 carbon atoms; X and Y, which may be the same or different, each represents a hydrogen atom, a halogen atom, a halo alkyl group in which the alkyl group is straight chained or branched and contains 1 to 6 carbon atoms, or a nitro group; Ar represents a phenylene group which may contain a methoxy substituent; A represents -O- or -NH-; B represents a direct link or a straight chained or branched bivalent paraffinic hydrocarbon residue of 1 to 10 carbon atoms and A represents a direct link, oxa, imino, substituted imino, amido, substituted amido, oxyalkylenoxy group, a lower or higher straight chained or branched bivalent paraffinic hydrocarbon residue having respectively 2 to 6 or 7to 12 carbon atoms optionally interrupted by oxa, imino, substituted imino, amido, substituted amido or a heterocyclic group, or a group of the formula: -Het-Q- (wherein Het is a bivalent heterocyclic group and Q is a direct link or a straight-chained or branched bivalent paraffinic hydrocarbon residue having 2 to 6 carbon atoms); or acid addition salts thereof. The invention also includes methods for preparing the above dihydropyridine derivatives.
摘要翻译：式（I）的二氢吡啶化合物，其中W表示氰基或卤代烷基，其烷基是直链或支链并含有1至6个碳原子; R 1，R 2和R 2可以相同或不同，表示直链或支链并且含有1至6个碳原子的饱和烃基; X和Y可以相同或不同，分别表示氢原子，卤素原子，烷基直链或支链并含有1-6个碳原子的卤代烷基或硝基; Ar表示可以含有甲氧基取代基的亚苯基; A表示-O-或-NH-; B代表1-10个碳原子的直链或直链或支链二价链烷烃残基，A 1代表直链，氧杂，亚氨基，取代亚氨基，酰氨基，取代的酰氨基，氧亚烷基氧基，低级或更高级具有任选地被氧杂，亚氨基，取代的亚氨基，酰氨基，取代的酰胺基或杂环基中断的分别具有2至6或7至12个碳原子的直链或支链二价链烷烃残基，或下式基团：-Het-Q-（其中Het是二价杂环基团，Q是具有2-6个碳原子的直链或直链或支链二价链烷烃残基）; 或其酸加成盐。本发明还包括制备上述二氢吡啶衍生物的方法。

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