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    • 2. 发明授权
    • Antihypertensive quinazoline derivatives
    • 抗高血压喹唑啉衍生物
    • US4189484A
    • 1980-02-19
    • US956326
    • 1978-10-31
    • Susumu MizogamiHidetoshi HiranumaTetsuo SekiyaMitsuo Hanazuka
    • Susumu MizogamiHidetoshi HiranumaTetsuo SekiyaMitsuo Hanazuka
    • C07D239/95C07D295/185C07D307/54C07D317/60A61K31/505C09B23/16C09B55/00
    • C07D295/185C07D239/95C07D307/54C07D317/60
    • Novel quinazoline compounds and antihypertensive compositions containing said compounds are disclosed; said compounds having the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group having 1-5 carbon atoms;R.sup.2 is a group of the formula ##STR2## in which Y is a hydrogen atom, an alkyl group of 1-5 carbon atoms, an alkoxy group of 1-5 carbon atoms, an alkenyloxy group, a methylenedioxy group, a nitro group, a halogen atom, a trifluoromethyl group, an acyloxy group, a hydroxy group, an unsubstituted or substituted amino group or a condensed benzene nucleus and m is an integer of 1-3 inclusive, or a group of the formula ##STR3## in which X is an oxygen atom, a sulfur atom or a carbon-nitrogen double bond and Z is a hydrogen atom, an alkyl group of 1-5 carbon atoms, an alkoxy group of 1-5 carbon atoms, a nitro group or a halogen atom; and n is an integer of 2-3 inclusive;provided that, when R.sup.2 is the said group ##STR4## n is 2 and R.sup.1 is a hydrogen atom or, when R.sup.2 is the said group ##STR5## n is 2 or 3 and R.sup.1 is a hydrogen atom or the said alkyl group and a pharmaceutically acceptable acid addition salt thereof.
    • 公开了含有所述化合物的新型喹唑啉化合物和抗高血压组合物; 所述具有下式的化合物:其中R 1是氢原子或具有1-5个碳原子的烷基; R2是式中Y为氢原子,1-5个碳原子的烷基,1-5个碳原子的烷氧基,烯氧基,亚甲二氧基,硝基, 卤素原子,三氟甲基,酰氧基,羟基,未取代或取代的氨基或稠合的苯核,m是1-3的整数,或下式的组合:IMAGE>其中X 是氧原子,硫原子或碳 - 氮双键,Z是氢原子,1-5个碳原子的烷基,1-5个碳原子的烷氧基,硝基或卤素原子; n为2-3以下的整数。 条件是当R2是所述基团时,n是2,R 1是氢原子,或者当R 2是所述基团时,n是2或3,并且R 1是氢原子或所述烷基和 其药学上可接受的酸加成盐。
    • 10. 发明授权
    • 2-Phenylalkyl-3-aminoalkyl-4(3H)-quinazolinone compound
    • 2-苯基烷基-3-氨基烷基-4(3H) - 喹唑啉酮化合物
    • US4668682A
    • 1987-05-26
    • US753708
    • 1985-07-10
    • Tetsuo SekiyaMikio TsutsuiDaijiro HoriiAkira Ishibashi
    • Tetsuo SekiyaMikio TsutsuiDaijiro HoriiAkira Ishibashi
    • C07D239/91A61K31/505A61K31/517A61P3/00A61P3/14A61P9/08A61P9/12A61P11/08C07D239/90C07D401/06
    • C07D239/90
    • Disclosed are a 2-phenylalkyl-3-aminoalkyl-4(3H)-quinazolinone compound of Formula (1): ##STR1## wherein, X represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a benzyloxy group, a halogen atom or a hydroxy group; Y represents an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a benzyloxy group, a halogen atom or a nitro group; R.sup.1 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; R.sup.2 represents an alkyl group having 1 to 5 carbon atoms or a group of Formula (2) ##STR2## [wherein, Z represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms or a halogen atom; d is an integer of 1 to 3; and l is an integer of 1 to 5]; or R.sup.1 and R.sup.2 represent together with the nitrogen atom to which they are attached, a cyclic amino group of the formula: ##STR3## [wherein, A represents an alkylene group having 2 to 6 carbon atoms or a group of the formula --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --]; a and b are independently an integer of 1 to 3; and n and m are independently an integer of 1 to 5, or a pharmaceutically acceptable acid addition salt thereof, a process for preparing said compound, a composition comprising said compound as an active ingredient and a method of treatment by use of said compound.The compounds of the present invention have calcium antagonistic, vasodilative, and antihypertensive activities.
    • 公开了式(1)的2-苯基烷基-3-氨基烷基-4(3H) - 喹唑啉酮化合物:其中X表示氢原子,具有1至5个碳原子的烷基,具有1个 至5个碳原子,苯氧基,苄氧基,卤原子或羟基; Y表示碳原子数1〜5的烷基,碳原子数1〜5的烷氧基,苄氧基,卤素原子或硝基。 R1表示氢原子或碳原子数1〜5的烷基。 R 2表示碳原子数1〜5的烷基或式(2)的基团[其中,Z表示氢原子,碳原子数1〜5的烷基,碳原子数1〜5的烷氧基 或卤素原子; d为1〜3的整数, l为1〜5的整数]。 或者R 1和R 2与它们所连接的氮原子一起表示下式的环状氨基:其中A表示碳原子数为2〜6的亚烷基或式 - (CH 2 )2-O-(CH 2)2 - ]; a和b独立地为1〜3的整数; n和m独立地为1〜5的整数,或其药学上可接受的酸加成盐,制备所述化合物的方法,包含所述化合物作为活性成分的组合物和使用所述化合物的方法。 本发明的化合物具有钙拮抗,血管扩张和抗高血压活性。