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1. 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。

2. 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。

3. 发明申请

WO0187845A3 N-CONTAINING HETEROCYCLIC COMPOUNDS AND THEIR USE AS 5-HT ANTAGONISTS 审中-公开
标题翻译：含N-杂环化合物及其作为5-HT拮抗剂使用
公开(公告)号：WO0187845A3
公开(公告)日：2002-08-29
申请号：PCT/JP0104002
申请日：2001-05-14
申请人： FUJISAWA PHARMACEUTICAL CO , YAMADA AKIRA , SPEARS GLEN , HAYASHIDA HISASHI , TOMISHIMA MASAKI , ITO KIYOTAKA , IMANISHI MASASHI
发明人： YAMADA AKIRA , SPEARS GLEN , HAYASHIDA HISASHI , TOMISHIMA MASAKI , ITO KIYOTAKA , IMANISHI MASASHI
IPC分类号： A61P43/00 , C07D217/08 , C07D237/26 , C07D261/20 , C07D277/60 , C07D277/82 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D521/00 , C07D217/22 , A61K31/395 , C07D237/34
CPC分类号： C07D277/60 , C07D217/08 , C07D231/12 , C07D233/56 , C07D237/26 , C07D249/08 , C07D261/20 , C07D277/82 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04
摘要： A compound of the formula (I): wherein A is a hydrogen atom, an optionally substituted, unsaturated, N-containing heterocyclic group or a group of the formula (a) : wherein R is an optionally substituted aryl group or an optionally substituted heterocyclic group;M is -(CH2)n-, -(CH2)n-O-(CH2)m- or -(CH2)n-NH-(CH2)m-, wherein n and m are independently 0,1 or 2; Q is an optionally substituted cycloalkylene group, an optionally substituted arylene group or an optionally substituted divalent heterocyclic group; andthe moiety of the formula (b): is an optionally substituted, unsaturated, mono-, di-, tri- or tetra-cyclic, N-containing heterocyclic group which may contain additional hetero atom(s) selected from the group consisting of nitrogen, oxygen and sulfur atoms as the ring member(s), its prodrug or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的化合物：其中A是氢原子，任选取代的，不饱和的含N杂环基或式（a）的基团：其中R是任选取代的芳基或任选取代的杂环基团; M是 - （CH 2）n - ， - （CH 2）n O-（CH 2）m - 或 - （CH 2）n -NH-（CH 2）m - ，其中n和m独立地为0,1或2; Q是任选取代的亚环烷基，任选取代的亚芳基或任选取代的二价杂环基; 和式（b）的部分：是任选取代的，不饱和的，单，二，三或四环的含N的杂环基团，其可以含有另外的选自氮的杂原子，作为环成员的氧和硫原子，其前药或其药学上可接受的盐。

4. 发明申请

WO1998024785A1 INDOLE-UREA DERIVATIVES WITH 5-HT ANTAGONIST PROPERTIES 审中-公开
标题翻译：具有5-HT拮抗剂性质的吲哚类衍生物
公开(公告)号：WO1998024785A1
公开(公告)日：1998-06-11
申请号：PCT/JP1997004390
申请日：1997-12-02
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , ITO, Kiyotaka , SPEARS, Glen, W. , YAMANAKA, Toshio , HARADA, Keiko , NODA, Yuka , SASAKI, Hiroshi , TAKAHASHI, Fumie , KATO, Masayuki
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D403/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： A compound of formula (I) wherein R and R are each hydrogen or linked together to form ethylene, R is hydrogen or lower alkyl, R is heterocyclic group, R is hydrogen or nitro, and X is CH or N, and pharmaceutically acceptable salts thereof, which has pharmacological activities such as 5-hydroxytryptamine (5-HT) antagonism.
摘要翻译：式（I）化合物，其中R 1和R 2各自为氢或连接在一起形成乙烯，R 3为氢或低级烷基，R 4为杂环基，R 5为氢或硝基，X是CH或N，以及其药学上可接受的盐，其具有5-羟基色胺（5-HT）拮抗作用。

5. 发明申请

WO1997022373A1 DRIVE UNIT FOR MEDICAL EQUIPMENT 审中-公开
标题翻译：医疗设备驱动单元
公开(公告)号：WO1997022373A1
公开(公告)日：1997-06-26
申请号：PCT/JP1996003605
申请日：1996-12-10
申请人： NIPPON ZEON CO., LTD. , MIYATA, Shinichi , ITO, Kiyotaka
发明人： NIPPON ZEON CO., LTD.
IPC分类号： A61M01/10
CPC分类号： A61M1/106 , A61M1/107 , A61M1/1072 , A61M1/1086 , A61M1/125
摘要： A drive unit for medical equipment in which, when a pressure detected by a conduit pressure sensor (15) becomes lower than a predetermined value, a first solenoid valve (63) is closed and a second solenoid valve (68) is opened, so that a conduit (18) is replenished with a gas from a secondary gas tank (64), and the amount of gas to be supplied is calculated based upon a change in the pressure detected by a tank pressure sensor (65). In using the equipment, the leakage of gas under normal condition can be easily distinguished from the leakage of gas under abnormal condition. Desirably, the drive unit has a gas supply device (60) which detects the pressure in the conduit (18) at a timing of changing a balloon (22) from the contracted state over to the inflated state and replenishes the conduit (18) with the gas so that the detected pressure will reach a predetermined value, and further has a control unit (10b) for changing the desired value. Preferably, when the interval between inflation and contraction of the balloon (22) is short, the inflation drive is stopped for one pulse, the pressure in the balloon is stabilized and is then detected, and the gas is replenished based upon this pressure. Preferably, the drive unit has a pressure transmission device having vent grooves (52, 54) to permit the residual fluid existing in the intimate contact between a diaphragm (46) and a first inner surface (49) or a second inner surface (51) to escape to an input port (48) or to an output port (50).
摘要翻译：一种用于医疗设备的驱动单元，其中当由管道压力传感器（15）检测到的压力变得低于预定值时，关闭第一电磁阀（63）并打开第二电磁阀（68），使得补充来自二次气体罐（64）的气体的管道（18），并且基于由罐式压力传感器（65）检测到的压力变化来计算要供给的气体量。在使用设备时，气体在正常状态下的泄漏可以很容易地与异常情况下的气体泄漏区分开来。理想地，驱动单元具有气体供给装置（60），其在将气囊（22）从收缩状态改变到膨胀状态的时刻检测导管（18）中的压力，并且用使得检测到的压力将达到预定值，并且还具有用于改变期望值的控制单元（10b）。优选地，当气球（22）的充气和收缩之间的间隔短时，一个脉冲的充气驱动停止，气囊中的压力被稳定并被检测，并且基于该压力补充气体。优选地，驱动单元具有压力传递装置，其具有排气槽（52,54），以允许存在于隔膜（46）和第一内表面（49）或第二内表面（51）之间紧密接触的残留流体，逃逸到输入端口（48）或输出端口（50）。

6. 发明申请

WO1996039382A1 UREA DERIVATIVES AS 5-HT ANTAGONISTS 审中-公开
标题翻译：尿素衍生物作为5-HT拮抗剂
公开(公告)号：WO1996039382A1
公开(公告)日：1996-12-12
申请号：PCT/JP1996001500
申请日：1996-06-04
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , ITO, Kiyotaka , SPEARS, Glen, W. , YAMANAKA, Toshio , HARADA, Keiko , HOTTA, Yuka , KATO, Masayuki
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/08
CPC分类号： C07D307/79 , C07C275/42 , C07C327/48 , C07C327/58 , C07D209/08 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12
摘要： A compound of formula (I) wherein R is cyano, thiocarbamoyl, a group of formula (a) in which R is hydrogen, lower alkyl which may have optionally substituted aryl, acyl, optionally substituted aryl, lower alkylthio or 1-lower alkylindolyl, A is lower alkylene, and m and n are each 0 or 1, a group of the formula -A -R in which R is morpholino, piperidino, 4-arylpiperazin-1-yl, phthalimido, 1,2,3,4-tetrahydroquinolin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl or imidazol-1-yl, and A is lower alkylene, or a group of formula (b) in which R and R are each hydrogen, optionally substituted aryl, acyl, pyridyl(lower)alkyl, thienyl(lower)alkyl, 3,4-dihydroisoquinolinyl, (lower alkylimino) (optionally substituted aryl) methyl or lower alkyl which may have optionally substituted aryl, and A is lower alkylene, and R is hydrogen; or R and R are linked together to form (1), (2), or (3), in which R is amino or acylamino, and R is hydrogen, acyl or lower alkyl which may have optionally substituted aryl, and R is 1-lower alkylindolyl, benzofuranyl, dihydrobenzofuranyl, or optionally substituted aryl, and a pharmaceutically acceptable salt thereof, which is useful as a medicament for prophylactic and therapeutic treatment of 5-HT mediated diseases.
摘要翻译：式（I）化合物，其中R 1为氰基，硫代氨基甲酰基，其中R 4为氢的式（a）基团，可具有任选取代的芳基的低级烷基，酰基，任选取代的芳基，低级烷硫基或1-低级烷基吲哚基，A 1为低级亚烷基，m和n各自为0或1，式-A 2 -R 5的基团，其中R 5为吗啉代，哌啶子基， 4-芳基哌嗪-1-基，苯二甲酰亚氨基，1,2,3,4-四氢喹啉-1-基，1,2,3,4-四氢异喹啉-2-基或咪唑-1-基，A 2是低级亚烷基或式（b）的基团，其中R 6和R 7各自为氢，任选取代的芳基，酰基，吡啶基（低级）烷基，噻吩基（低级）烷基，3,4-二氢异喹啉基，（低级烷基亚氨基）（任选取代的芳基）甲基或可以具有任选取代的芳基的低级烷基，A 3是低级亚烷基，R 2是氢; 或R 1和R 2连接在一起形成（1），（2）或（3），其中R 8是氨基或酰氨基，R 9是氢，酰基或低级可以具有任选取代的芳基的烷基，R 3是1-低级烷基吲哚基，苯并呋喃基，二氢苯并呋喃基或任选取代的芳基及其药学上可接受的盐，其可用作5-HT的预防和治疗性治疗药物介导的疾病。

7. 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。

8. 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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