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    • 21. 发明授权
    • Fused bicyclic compound
    • 稠合双环化合物
    • US08410166B2
    • 2013-04-02
    • US13561662
    • 2012-07-30
    • Yoichi TakahashiNobumasa AwaiHidenori AkatsukaTakayuki KawaguchiToru Iljima
    • Yoichi TakahashiNobumasa AwaiHidenori AkatsukaTakayuki KawaguchiToru Iljima
    • C07D265/00
    • C07D265/16C07D311/20C07D311/58C07D311/96C07D405/14C07D413/04
    • Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]: wherein ring A is benzene having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is alkylsulfonylamino, etc., R2 and R3 are (a) the same of different and are hydrogen, alkyl, or optionally substituted aryl, or (b) combined with each other to form an oxo group or (c) combined with each other at its terminal together with the adjacent carbon atom to form cycloalkyl, X is ═N—, ═C(R4)— or —CH(R4)—, R4 is (a) hydrogen, (b) cyano, (c) halogen, (d) alkyl, (e) alkenyl, (f) cycloalkyl, (g) alkanoyl, (h) carbamoyl, or (i) cycloalkenyl, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, useful e.g. as an antihypertensive agent.
    • 具有式[I]的矿物质类皮质激素受体(MR)的亲和性的稠合双环化合物:其中环A是具有取代基R 1的苯,与相邻的6元杂环稠合,并且进一步任选具有除 R 1,R 1是烷基磺酰基氨基等,R 2和R 3是(a)不同的并且是氢,烷基或任选取代的芳基,或(b)彼此结合形成氧代基或(c)与 X是= N - , - C(R4) - 或-CH(R4) - ,R4是(a)氢,(b)氰基,(c) 卤素,(d)烷基,(e)烯基,(f)环烷基,(g)烷酰基,(h)氨基甲酰基或(i)环烯基,Ar是任选取代的芳族环状基团,虚线表示存在或不存在 双键或其药学上可接受的盐,例如, 作为抗高血压药。
    • 22. 发明授权
    • Fused bicyclic compound
    • 稠合双环化合物
    • US08258131B2
    • 2012-09-04
    • US12671479
    • 2008-07-21
    • Yoichi TakahashiNobumasa AwaiHidenori AkatsukaTakayuki KawaguchiToru Iijima
    • Yoichi TakahashiNobumasa AwaiHidenori AkatsukaTakayuki KawaguchiToru Iijima
    • C07D265/16A61K31/352A61K31/353
    • C07D265/16C07D311/20C07D311/58C07D311/96C07D405/14C07D413/04
    • The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc., R2 and R3 are (a) the same of different and a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, (b) combined each other to form an oxo group or (c) combined each other at its terminal together with the adjacent carbon atom to form a cycloalkyl group, X is a group of ═N—, ═C(R4)— or —CH(R4)—, R4 is (a) a hydrogen atom, (b) a cyano group, (c) a halogen atom, (d) an alkyl group, (e) an alkenyl group, (f) a cycloalkyl group (g) an alkanoyl group, (h) a carbamoyl group or (i) a cycloalkenyl group, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, which is useful as an antihypertensive agent etc.
    • 本发明提供了对式[I]所示的对矿物质类皮质激素(MR)的受体具有亲和性的新的稠合双环化合物:其中环A是具有取代基R 1的苯环,与相邻的6元 杂环,并且还可任选地具有除R1以外的取代基,R 1是烷基磺酰基氨基等,R 2和R 3是(a)不同的,和氢原子,烷基或取代或未取代的芳基, (b)彼此组合以形成氧代基团,或(c)在其末端与相邻的碳原子一起相互结合形成环烷基,X是一个= N - , - C(R 4) - 或 - CH(R4) - ,R4是(a)氢原子,(b)氰基,(c)卤原子,(d)烷基,(e)烯基,(f)环烷基 g)烷酰基,(h)氨基甲酰基或(i)环烯基,Ar是任选取代的芳环基,虚线表示存在或不存在 双键或其药学上可接受的盐,其可用作抗高血压剂等。
    • 28. 发明授权
    • Camptothecin derivatives
    • 喜树碱衍生物
    • US06617456B1
    • 2003-09-09
    • US09624012
    • 2000-07-21
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • Kenji TsujiharaTakayuki KawaguchiSatoshi OkunoToshiro Yano
    • C07D49800
    • C08B37/0018A61K47/61A61K47/65C08B37/0021
    • A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.
    • 包含式[I]化合物的喜树碱衍生物:其中R1,R2,R3,R4和R5是(A)相邻的两个基团结合形成亚烷基,或两者都是H,其余三个基团之一是-Xn -Alkm-R6,另外两个为H,烷基或卤素,或(B)相邻的两个基团结合形成亚烷基,所述亚烷基的一个碳原子被-Xn-Alkm-R6取代,并且 剩余的三个基团是H,烷基或卤素,并且(A)或(B)中的一个或两个亚烷基的-CH 2可以任选地被-O - , - S-或-NH-替代,X是-O - 或-NH-,Alk为亚烷基或-OH,m和n均为0或1,或m为1,n为0,喜树碱化合物通过氨基酸或肽与具有羧基的多糖结合 ,或其药学上可接受的盐。 所述喜树碱衍生物显示出增强的抗肿瘤活性,但副作用很少,可用作药物。
    • 30. 发明授权
    • Data read circuit for semiconductor storage device
    • 半导体存储器件的数据读取电路
    • US5068831A
    • 1991-11-26
    • US550025
    • 1990-07-09
    • Satoru HoshiMasami MasudaTakayuki Kawaguchi
    • Satoru HoshiMasami MasudaTakayuki Kawaguchi
    • G11C11/41G11C7/06G11C7/12G11C7/22G11C11/409G11C11/417H01L21/8242H01L27/10H01L27/108
    • G11C7/12G11C7/06G11C7/22
    • In a data read circuit, for a semiconductor storage device, data of a memory cell (11) selected according to an address is inputted to a sense amplifier (22) via a pair of complementary first data lines (N1 to N6). The sense amplifier outputs the inputted and amplified data to a pair of complementary second data lines (N7, N8). First switching means (Tr3) equalizes the pair of complementary first data lines (N5, N6) at the input side of the sense amplifier (22) by making the first data lines conductive with respect to each other. Second switching means (Tr4) equalizes the pair of complementary second data lines (N7, N8) by making the second data lines conductive with respect to each other. Third switching means (Tr5, Tr6) equalizes by making the pair of first data lines (N5, N6) at the input side of the sense amplifier (22) and corresponding ones of the pair of second data lines (N7, N8) conductive with respect to each other. Second equalizing pulse generator means (42) generates a second equalizing pulse (.PHI..sub.eq ') when the address is changed, and turns on the first switch means (Tr3) by applying the second equalizing pulse to a control terminal of the first switch means. First equalizing pulse generator means (41) generates a first equalizing pulse (.PHI..sub.eq) when the address is changed, and turns on the second and third switching means (Tr4, Tr5, Tr6) by applying the second equalizing pulse to gate terminals of the second and third switching means. The load capacitance ]C(.PHI..sub.eq ')] connected to an output terminal of the second equalizing pulse generating means (42) is set smaller than the load capacitance [C(.PHI..sub.eq)] connected to an output terminal of the first equalizing pulse generator means (41). The number of stages of logical circuits constituting the second equalizing pulse generator means (42) is smaller than the number of stages of logical circuits constituting the first equalizing pulse generator means (41). Accordingly, with this data read circuit for a semiconductor storage device, the second equalizing pulse (.PHI..sub.eq ') from the second equalizing pulse generator means (42) is established earlier than the first equalizing pulse (.PHI..sub.eq) from the first equalizing pulse generator means (41).