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    • 2. 发明申请
    • AZAINDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY
    • 具有PGD2受体拮抗活性的氨基衍生物
    • US20110028717A1
    • 2011-02-03
    • US12904647
    • 2010-10-14
    • Akira KugimiyaItsuo MakinoNaohiro Onodera
    • Akira KugimiyaItsuo MakinoNaohiro Onodera
    • C07D471/04
    • C07D471/04
    • The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.A compound of the general formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1═X2—X3═X4— is a formula of —C(R1)═C(R2)—C(R3)═N— etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is optionally substituted C1-C6 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is optionally substituted C1-C6 alky etc.; R9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.
    • 本发明产生具有DP受体拮抗活性的氮杂吲哚衍生物和包含所述化合物作为活性成分的药物组合物,并进一步提供治疗过敏性疾病的治疗剂。 通式(I)的化合物,其中环A是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; -X 1 = X 2 -X 3 = X 4 - 的式为-C(R 1)= C(R 2)-C(R 3)= N-等的式 R1,R2,R3,R4和R5独立地是氢原子或卤素原子等; R6是任选取代的C 1 -C 6烷氧基等; R7独立地为卤素原子等; R8是任选取代的C 1 -C 6烷基等; R9是羧基等。 M是磺酰基等。 Y是单键等; L1,L2和L3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q为0等; 其药学上可接受的盐或水合物。
    • 4. 发明授权
    • Azaindole derivative having PGD2 receptor antagonistic activity
    • 具有PGD2受体拮抗活性的阿维醇衍生物
    • US07842692B2
    • 2010-11-30
    • US11989132
    • 2006-07-20
    • Akira KugimiyaItsuo MakinoNaohiro Onodera
    • Akira KugimiyaItsuo MakinoNaohiro Onodera
    • C07D471/04A61K31/5377A61K31/437
    • C07D471/04
    • The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.A compound of the general formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1═X2—X3═X4— is a formula of —C(R1)═C(R2)—C(R3)═N— etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is optionally substituted C1-C6 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is optionally substituted C1-C6 alkyl etc.; R9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.
    • 本发明产生具有DP受体拮抗活性的氮杂吲哚衍生物和包含所述化合物作为活性成分的药物组合物,并进一步提供治疗过敏性疾病的治疗剂。 通式(I)的化合物,其中环A是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; -X 1 = X 2 -X 3 = X 4 - 的式为-C(R 1)= C(R 2)-C(R 3)= N-等的式 R1,R2,R3,R4和R5独立地是氢原子或卤素原子等; R6是任选取代的C 1 -C 6烷氧基等; R7独立地为卤素原子等; R8是任选取代的C 1 -C 6烷基等; R9是羧基等。 M是磺酰基等。 Y是单键等; L1,L2和L3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q为0等; 其药学上可接受的盐或水合物。
    • 6. 发明授权
    • 4,1-Benzoxazepines and compositions
    • 4,1-苯并氧氮杂和组合物
    • US4374842A
    • 1983-02-22
    • US250299
    • 1981-04-02
    • Kentaro HiraiShigeru MatsutaniItsuo MakinoTeruyuki Ishiba
    • Kentaro HiraiShigeru MatsutaniItsuo MakinoTeruyuki Ishiba
    • C07D267/14C07D498/04A61K31/55C07D498/14
    • C07D267/14
    • 4,1-Benzoxazepines of the following formula are central nervous system drugs: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl; X is hydrogen, halogen, or nitro; Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle;R.sup.2 is C.sub.1 to C.sub.5 alkyl;and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl;with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl).
    • 下式的4,1-苯并氧氮杂是中枢神经系统药物:其中R是氢或C1至C5烷基; X是氢,卤素或硝基; Y是苯基,2-卤代苯基,4-卤代苯基,2-三氟甲基苯基或吡啶基; 并且是下列基团:其中Q是氧,硫或亚肼基,条件是当Y是苯基或2-卤代苯基且R是氢时,Q是 氧还不硫; R1是氢,卤素,C1至C5烷基,C1至C5烷硫基,5-或6-元杂环或被选自卤素,羟基,巯基,C1的取代基取代的C1至C5烷基 C 1-5烷酰氧基,C 1至C 5烷硫基,C 7至C 9芳烷基二硫代,C 2至C 10二烷基氨基,C 3至C 15二烷基氨基烷氧基,C 3至C 15二烷基氨基烷硫基以及5-或6-元杂环; R 2为C 1至C 5烷基; 并且R 3为C 1至C 5烷基或C 3至C 10二烷基氨基烷基;条件是当R 1为C 1至C 5烷基且R为氢时,Y不为苯基或2-卤代苯基)。
    • 8. 发明授权
    • Underwater detecting apparatus, depth measuring apparatus and display apparatus
    • 水下检测装置,深度测量装置及显示装置
    • US06595315B1
    • 2003-07-22
    • US09662627
    • 2000-09-15
    • Hiroyasu FujimotoHiroshi NaganoMakoto ObuchiItsuo Makino
    • Hiroyasu FujimotoHiroshi NaganoMakoto ObuchiItsuo Makino
    • G01S1500
    • G01S15/96G01S7/6218G01S7/6272G01S7/64G01S15/08G01S15/87
    • A screen on which water depth information obtained from an echo signal is historically displayed and a screen on which fish school detection information obtained from an echo signal is displayed, are displayed side by side on a display screen of a display instrument or either one is displayed by switching. Thus, a large amount of information is displayed on a limited space of a small display instrument efficiently and effectively and to be easy to see. Further, when a water depth value becomes a set value of an alarm water depth mark or less, an alarm is displayed on the display screen of the display instrument, and an alarm is given by sound. At the same time as this, the brilliance of the display screen is raised to the maximum brilliance to make the screen brighter, so that the contents of the alarm are made easy to see. Thus, quick measures can be taken in an emergency. Moreover, after a mode is set to a help mode by a mode switch, when any one of keys in an operation portion is pushed, guidance of the function, operation procedure, and the like of the pushed key is displayed on a display portion. Thus, the guidance as to the key can be displayed by a simple operation in a help mode.
    • 历史上显示从回波信号获得的水深信息的屏幕和显示从回波信号获得的鱼学校检测信息的屏幕并排地显示在显示器具的显示屏幕上或者显示 通过切换。 因此,在小型显示装置的有限空间中有效且高效地显示大量的信息并且易于看见。 此外,当水深值成为报警水深标记的设定值以下时,在显示装置的显示画面上显示报警,并且通过声音给出报警。 与此同时,显示屏的亮度提高到最大的亮度,使屏幕更亮,使报警的内容变得容易看清。 因此,在紧急情况下可以采取快速措施。 此外,在通过模式切换将模式设置为帮助模式之后,当按下操作部中的任何一个键时,在显示部分上显示所推动的键的功能,操作过程等的引导。 因此,可以通过在帮助模式中的简单操作来显示关于键的指导。