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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

WO9900373A8 BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO9900373A8
公开(公告)日：2000-07-20
申请号：PCT/JP9802885
申请日：1998-06-26
申请人： FUJISAWA PHARMACEUTICAL CO , YAMASAKI NORITSUGU , IMOTO TAKAFUMI , OKU TERUO , KATAYAMA AKIRA , KAYAKIRI HIROSHI , ONOMURA OSAMU , HIRAMURA TAKAHIRO , NISHIKAWA MASAHIRO , SAWADA HITOSHI
发明人： YAMASAKI NORITSUGU , IMOTO TAKAFUMI , OKU TERUO , KATAYAMA AKIRA , KAYAKIRI HIROSHI , ONOMURA OSAMU , HIRAMURA TAKAHIRO , NISHIKAWA MASAHIRO , SAWADA HITOSHI
IPC分类号： A61K31/4184 , A61K31/4725 , A61P3/10 , C07D235/08 , C07D401/06 , C07D405/10 , C07D409/10 , C07D409/12 , A61K31/415 , A61K31/47 , C07D235/26 , C07D235/28
CPC分类号： C07D401/06 , C07D235/08 , C07D405/10 , C07D409/10 , C07D409/12
摘要： New benzimidazole derivatives of general formula (I) or salts thereof, useful as medicines, wherein R1 is alkyl or the like; R2 is aromatic ring-containing lower alkyl which may be substituted; R3 is alkyl or the like; and -X- is a group of general formula (V) or the like.
摘要翻译：用作药物的通式（I）的新的苯并咪唑衍生物或其盐，其中R 1是烷基等; R2是可被取代的含芳环的低级烷基; R3是烷基等; 和-X-是通式（V）等的基团。

3. 发明申请

WO1998015530A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO1998015530A1
公开(公告)日：1998-04-16
申请号：PCT/JP1997003592
申请日：1997-10-07
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YAMASAKI, Noritsugu , IMOTO, Takafumi , MURAI, Yoshiyuki , HIRAMURA, Takahiro , ONOMURA, Osamu , NISHIKAWA, Masahiro , OKU, Teruo , SAWADA, Kouzou , KAYAKIRI, Hiroshi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/08
CPC分类号： C07D401/06 , C07D209/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Novel indole derivatives represented by general formula (V) or pharmaceutically acceptable salts thereof. Because of having hypoglycemic or PDE5-inhibitory activities, these compouds or salts thereof are useful as remedies for impaired glucose tolerance, diabetes, complication of diabetes, insulin resistant syndrome, hyperlipidemia, atherosclerosis, cardiovascular diseases, hyper glycemia, hypertension; diseases characterized by angina pectoris, high blood pressure, pulmonary hypertension, congestive heart failure, glomerular diseases, tubular interstitial diseases, renal insufficiency, atherosclerosis, angiostenosis, peripheral vascular diseases, cerebral stroke, chronic reversible obstructive diseases, allergic rhinitis, urticaria, glaucoma or intestinal motility disorders; sexual impotence, complication of diabetes, osteoporosis, nephritis, cancerous cachexia or post-PTCA reconstriction, wherein R13 to R15 represent each: 1) hydrogen, 2) lower alkyl, lower alkylthio or lower alkoxy-substituted lower alkyl, or 3) lower alkyl, hydroxy, hydroxylated lower alkyl, lower alkyloxy, etc. bonded to or substituted by aryl or a heterocycle; provided that R13 to R15 do not represent hydrogen at the same time; R16 represents: 1) hydrogen, or 2) lower alkyl; and R17 represents optionally esterified carboxy.
摘要翻译：由通式（V）表示的新型吲哚衍生物或其药学上可接受的盐。由于具有低血糖或PDE5抑制活性，这些化合物或其盐可用作葡萄糖耐量降低，糖尿病，糖尿病并发症，胰岛素抵抗综合征，高脂血症，动脉粥样硬化，心血管疾病，高血糖症，高血压症的补救措施; 特征为心绞痛，高血压，肺动脉高压，充血性心力衰竭，肾小球疾病，肾小管间质疾病，肾功能不全，动脉粥样硬化，血管狭窄症，外周血管疾病，脑中风，慢性可逆性阻塞性疾病，过敏性鼻炎，荨麻疹，青光眼或肠蠕动障碍; 性功能障碍，糖尿病并发症，骨质疏松症，肾炎，癌性恶病质或PTCA后重建，其中R13至R15各自表示：1）氢，2）低级烷基，低级烷硫基或低级烷氧基取代的低级烷基，或3）低级烷基，羟基，羟基化的低级烷基，低级烷氧基等，与芳基或杂环结合或取代; 条件是R13至R15不同时代表氢; R16表示：1）氢，或2）低级烷基; R 17代表任意酯化的羧基。

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

WO1995023793A1 2-ISOXAZOLINE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME, AND PROCESS FOR PRODUCING RELATED DERIVATIVES FROM THE SAME 审中-公开
标题翻译： 2-异辛唑衍生物及其制备方法及其制备相关衍生物的方法
公开(公告)号：WO1995023793A1
公开(公告)日：1995-09-08
申请号：PCT/JP1995000331
申请日：1995-03-02
申请人： DAICEL CHEMICAL INDUSTRIES, LTD. , MURAI, Yoshiyuki , NISHIKAWA, Masahiro , UEDA, Yoichiro , ONOMURA, Osamu , TAKASE, Ichiro
发明人： DAICEL CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D261/04
CPC分类号： C07C269/06 , C07C213/00 , C07C213/10 , C07C273/1854 , C07D261/04 , C07C215/08 , C07C215/28
摘要： An intermediate useful for synthesizing a 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivative serving as an intermediate for preparing medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors; and a process for producing the above derivative from the above intermediate. Specifically, the invention provides a 2-isoxazoline derivative represented by general formula [1] and a process for producing the 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivative represented by general formula [6] by reducing the above derivative [1]; wherein Ph represents phenyl; and R and R represent each independently hydrogen, acyl, alkyloxycarbonyl, arylalkyloxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylalkylaminocarbonyl, arylaminocarbonyl, alkyl, arylalkyl, aryl, alkylsulfonyl, arylalkylsulfonyl or arylsulfonyl, or R and R are combined together to represent divalent acyl.
摘要翻译：可用于合成作为制备药物的中间体的2,5-二氨基-1,6-二苯基-3-羟基己烷衍生物的中间体，包括人免疫缺陷病毒（HIV）蛋白酶抑制剂等逆转录病毒蛋白酶抑制剂; 以及由上述中间体制备上述衍生物的方法。具体地说，本发明提供由通式[1]表示的2-异恶唑啉衍生物和通式（6）所示的通式[6]所示的2,5-二氨基-1,6-二苯基-3-羟基己烷衍生物的制造方法，衍生物[1]; 其中Ph表示苯基; 和R 1和R 2各自独立地表示氢，酰基，烷氧基羰基，芳基烷氧基羰基，芳氧基羰基，烷基氨基羰基，芳基烷基氨基羰基，芳基氨基羰基，烷基，芳基烷基，芳基，烷基磺酰基，芳基烷基磺酰基或芳基磺酰基，或R 1和R 2 >组合在一起代表二价酰基。

6. 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。

7. 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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