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    • 2. 发明申请
    • PYRIDAZINONE DERIVATIVE
    • 吡咯烷酮衍生物
    • WO1995019969A1
    • 1995-07-27
    • PCT/JP1995000069
    • 1995-01-24
    • NISSAN CHEMICAL INDUSTRIES, LTD.TANIKAWA, KeizoMATSUMOTO, TakashiMATSUMOTO, HirooTSURUZOE, NobutomoNAKABEPPU, Hitoshi
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • C07D237/22
    • C07D401/12C07D237/22
    • A pyridazinone derivative represented by general formula (I) and an antithrombocytic agent containing the same, wherein R represents hydrogen or C1-C4 alkyl; X represents hydrogen, chlorine or bromine; An represents pyridyl or phenyl substituted by OR (R representing hydrogen or C1-C4 alkyl) and A (representing hydrogen, halogen, C1-C4 alkyl or OR (R representing hydrogen or C1-C4 alkyl)); Y represents C1-C8 alkylene wherein one carbon atom on the straight chain is substituted by one OR group (R being as defined as above); and Z and Z represent each independently hydrogen, halogen, C1-C4 alkyl or OR (R being as defined above). This compound has a potent antithrombocytic activity and an excellent safety and is used as the active ingredient of a preventive or remedy for various thrombotic diseases.
    • 由通式(I)表示的哒嗪酮衍生物和含有它的抗血栓形成剂,其中R表示氢或C1-C4烷基; X表示氢,氯或溴; A代表由OR 1取代的吡啶基或苯基(R 1代表氢或C 1 -C 4烷基)和A(代表氢,卤素,C 1 -C 4烷基或OR 2(R 2代表氢或C 1 -C4烷基)); Y表示直链上的一个碳原子被一个OR 1基团取代的C1-C8亚烷基(R 1如上所定义); Z 1和Z 2各自独立地表示氢,卤素,C 1 -C 4烷基或OR 1(R 1如上所定义)。 该化合物具有有效的抗血栓形成细胞活性和优异的安全性,并被用作各种血栓性疾病的预防或治疗的活性成分。
    • 3. 发明申请
    • CHROMAN DERIVATIVES
    • WO1998004542A1
    • 1998-02-05
    • PCT/JP1997002583
    • 1997-07-25
    • NISSAN CHEMICAL INDUSTRIES, LTD.TANIKAWA, KeizoOHRAI, KazuhikoSATO, MasayukiYAMASHITA, ToruYANAGIHARA, Kazufumi
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • C07D311/70
    • C07D405/04C07D311/70C07D405/12C07D407/12C07D409/12C07F7/1804
    • The present invention relates to chroman derivatives of formula (I): wherein R represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C3-6 alkoxymethyl group, etc.; R and R each independently represent a hydrogen atom, a C1-6 alkyl group, etc.; R represents a hydroxyl group or a C1-6 alkylcarbonyloxyl group or forms a bond together with R ; R represents a hydrogen atom or forms a bond together with R ; R and R each independently represent a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a phenyl group, etc.; n is 0 or an integer of 1, 2, 3, or 4; W represents a phenyl group, etc.; X represents C=O, CH2, SO2, etc.; Y represents NR (in which R represents a hydrogen atom, a C1-4 alkyl group, a phenyl group, etc.), etc.; Z does not exist or represents CH2 or NR (R represents a hydrogen atom, a C1-4 alkyl group, or a phenyl group, etc.) or their salts.
    • 本发明涉及式(I)的苯并二氢吡喃衍生物:其中R 1表示氢原子,卤素原子,C 1-6烷基,C 1-6烷氧基,C 3-6烷氧基甲基等。 ; R 3和R 4各自独立地表示氢原子,C 1-6烷基等; R 5代表羟基或C 1-6烷基羰基氧基或与R 5一起形成键; R 6表示氢原子或与R 5一起形成键; R 7和R 8各自独立地表示氢原子,C 1-6烷基,C 3-6环烷基,苯基等; n为0或1,2,3或4的整数; W表示苯基等; X表示C = O,CH 2,SO 2等; Y表示NR 17(其中R 17表示氢原子,C 1-4烷基,苯基等)等; Z不存在或表示CH 2或NR 18(R 18表示氢原子,C 1-4烷基或苯基等)或其盐。
    • 4. 发明申请
    • TRIS(SUBSTITUTED PHENYL)BISMUTH DERIVATIVE
    • TRIS(取代苯乙烯)双酚衍生物
    • WO1995006053A1
    • 1995-03-02
    • PCT/JP1994001381
    • 1994-08-22
    • NISSAN CHEMICAL INDUSTRIES, LTD.SUZUKI, HitomiMAEDA, KouichiTANIKAWA, KeizoMIYAJI, Katsuaki
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • C07F09/94
    • A61K49/04C07F9/94Y10S424/90
    • A tris(substituted phenyl)bismuth derivative represented by general formula (I) and, if any, a pharmaceutically acceptable salt thereof, wherein X represents Y -NR R [wherein Y represents -SO2- or -C(=O)-; and R and R represent each independently hydrogen, C1-C4 alkyl or A-Z (wherein A represents alkylene which has 2-6 carbon atoms in total and may have a branch having at least two carbon atoms, and Z represents OR (wherein R represents SiR R R (wherein R , R and R represent each independently C1-C4 alkyl or phenyl), hydrogen or C1-C4 alkyl) or NR R (wherein R and R represent each independently hydrogen or C1-C4 alkyl)), provided the case where R and R are both hydrogen atoms is excepted], -O-CHR -OR (wherein R represents C1-C4 alkyl, and R is as defined above) or Y -A-Z [wherein Y represents O, -S(O)n- (wherein n represents an integer of 0 or 2) or -NR - (wherein R is as defined above), and A and Z are each as defined above]; and X and X represent each independently hydrogen or any substituent defined above with respect to X . This compound has an excellent performance as a radio-logical contrast medium and is useful as an X-ray contrast medium for injecting into a blood vessel, urinary tract, and so forth.
    • 由通式(I)表示的三(取代的苯基)铋衍生物和(如果有的话)其药学上可接受的盐,其中X 1表示Y 1 -NR 1 R 2 [其中Y 1 >表示-SO 2 - 或-C(= O) - ; 并且R 1和R 2各自独立地表示氢,C 1 -C 4烷基或AZ(其中A表示总共具有2-6个碳原子并且可具有至少两个碳原子的支链的亚烷基,Z表示 OR 3(其中R 3表示SiR 4 R 5 R 6(其中R 4,R 5和R 6各自独立地为C 1 -C 4烷基或苯基), 氢或C 1 -C 4烷基)或NR 7 R 8(其中R 7和R 8各自独立地表示氢或C 1 -C 4烷基)),条件是其中R 1和R 2, 2>均为氢原子除外],-O-CHR 7 -OR 9(其中R 9表示C 1 -C 4烷基,R 7如上定义)或Y 2 - AZ [其中Y 2表示O,-S(O)n - (其中n表示0或2的整数)或-NR 1 - (其中R 1如上所定义),A和 Z各自如上所定义); X 2和X 3各自独立地表示氢或相对于X 1定义的任何取代基。 该化合物作为无线电逻辑造影剂具有优异的性能,并且可用作用于注射到血管,尿道等中的X射线造影剂。
    • 5. 发明申请
    • THERAPEUTIC AGENT FOR CARDIAC FAILURE
    • 治疗失败的治疗剂
    • WO1997023209A1
    • 1997-07-03
    • PCT/JP1996003761
    • 1996-12-24
    • NISSAN CHEMICAL INDUSTRIES, LTD.TANIKAWA, KeizoOHRAI, KazuhikoSATO, MasayukiYAMASHITA, Toru
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • A61K31/35
    • C07D311/68A61K31/353A61K31/397A61K31/4025A61K31/453A61K31/55
    • A therapeutic agent for cardiac failure comprising as the active ingredient either a benzopyran derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R and R each independently represent hydrogen, halogeno, nitro, cyano, amino, C1-6 alkylcarbonylamino, etc.; R and R each independently represents hydrogen, C1-6 alkyl, or phenyl, or R and R are bonded together to form C3-6 cycloalkyl in cooperation with the carbon atom bonded thereto; R represents hydroxy, C1-6 alkoxy, or C1-6 alkylcarbonyloxy, or R is bonded to R to form a bond; R represents hydrogen, or R is bonded to R to form a bond; and R and R each independently represent hydrogen or C1-6 alkyl, or R and R are bonded together to form pyrrolidinyl, imidazolidinyl, pyrazolidinyl, piperidyl, piperazinyl, etc. in cooperation with the nitrogen atom bonded thereto, or R and R are bonded together to form, in cooperation with the nitrogen atom bonded thereto, pyrrole ring optionally substituted with R (where R has the same meaning as R ).
    • 一种用于心力衰竭的治疗剂,其包含作为活性成分的通式(I)表示的苯并吡喃衍生物或其药理学上可接受的盐,其中R 1和R 2各自独立地表示氢,卤素,硝基,氰基, 氨基,C 1-6烷基羰基氨基等; R 3和R 4各自独立地表示氢,C 1-6烷基或苯基,或者R 3和R 4与键合的碳原子一起形成C 3-6环烷基; R 5表示羟基,C 1-6烷氧基或C 1-6烷基羰基氧基,或R 5与R 6结合形成键; R 6表示氢,或R 6与R 5键合形成键; R 7和R 8各自独立地表示氢或C 1-6烷基,或者R 7和R 8结合在一起形成吡咯烷基,咪唑烷基,吡唑烷基,哌啶基,哌嗪基等,与 与其键合的氮原子或R 7和R 8键合在一起,以与其键合的氮原子一起形成任选被R 9取代的吡咯环(其中R 9具有相同的含义 作为R 1)。
    • 6. 发明申请
    • PYRAZOLONE DERIVATIVES
    • 吡唑啉酮衍生物
    • WO1997013757A1
    • 1997-04-17
    • PCT/JP1996002944
    • 1996-10-11
    • NISSAN CHEMICAL INDUSTRIES, LTD.TANIKAWA, KeizoMATSUMOTO, TakashiNAKAMURA, MasumiASADA, YasunoriSHUDO, Norimasa
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • C07D231/22
    • C07D231/12C07D231/14C07D231/20C07D231/22C07D401/04C07D401/06C07D401/14C07D403/04
    • Pyrazolone derivatives represented by general formula (I) or salts thereof which have antiplatelet aggregation effects and thus are useful as a preventive or remedy for various thrombotic diseases. In said formula (I) X and X represents (a), wherein A represents cyano, cyano(C1-4 alkyl), amino, amino-(C1-4 alkyl), amidino, guanidino, etc.; and R and R independently represents each hydrogen, halogeno, C1-6 alkyl, etc.; another of X and X represents C1-6 alkyl, C3-6 alkenyl, aryl(C1-4 alkyl) or aryl; one of Y and Y represents (b), wherein Q represents oxygen or sulfur; Z represents oxygen, -NR - or -CHR -; Z represents cyclic C3-7 alkylene, C1-3 alkylene, -CH2CO-, -CH2CH2CO-, etc.; Z represents oxygen, sulfur, sulfinyl, sulfonyl, etc.; Z represents C1-3 alkylene, etc.; and Z represents carboxyl, etc.; and another of Y and Y represents D-E-, wherein E represents a bond, C1-4 alkylene, phenylene, etc.; and D represents hydrogen, C1-6 alkyl, etc.
    • 具有抗血小板聚集效应的由通式(I)表示的吡唑啉酮衍生物或其盐,因此可用作各种血栓形成疾病的预防或治疗。 在所述式(I)中,X 1和X 2代表(a),其中A表示氰基,氰基(C 1-4烷基),氨基,氨基 - (C 1-4烷基),脒基,胍基等 ; R 1和R 2各自独立地表示氢,卤代C 1-6烷基等; X 1和X 2中的另一个表示C 1-6烷基,C 3-6烯基,芳基(C 1-4烷基)或芳基; Y 1和Y 2中的一个表示(b),其中Q表示氧或硫; Z 1表示氧,-NR 7 - 或-CHR 7 - ; Z 2表示环状C 3-7亚烷基,C 1-3亚烷基,-CH 2 CO-,-CH 2 CH 2 CO-等; Z 3表示氧,硫,亚磺酰基,磺酰基等; Z 4表示C 1-3亚烷基等。 Z 5表示羧基等。 Y 1和Y 2中的另一个表示D-E-,其中E表示键,C 1-4亚烷基,亚苯基等; D表示氢,C 1-6烷基等。
    • 9. 发明申请
    • BENZOPYRAN DERIVATIVES
    • BENZOPYRAN衍生物
    • WO1996034871A1
    • 1996-11-07
    • PCT/JP1996001180
    • 1996-04-30
    • NISSAN CHEMICAL INDUSTRIES, LTD.TANIKAWA, KeizoOHRAI, KazuhikoSATO, MasayukiHORIUCHI, TakashiYAMASHITA, Toru
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • C07D498/04
    • C07D498/04
    • Benzopyran derivatives of formula (I), wherein X and X are absent or represent an oxygen atom; X represents an oxygen atom, a sulfur atom, a nitrogen atom (said nitrogen atom is unsubstituted or substituted by a hydrogen atom or C1-C4 alkyl group), carbonyl or thiocarbonyl; A represents a hydroxyl group or may form a single bond together with B; B represents a hydrogen atom or may form a single bond together with A; Y represents 1-pyrrolyl group, 1-pyrazolyl group, 1-imidazolyl group, 1-(1,2,3-triazolyl) group or 1-(1,2,4-triazolyl) group which is unsubstituted or substituted by R ; R and R independently represent a hydrogen atom, a phenyl group or a C1-C4 alkyl group; R represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group and medicines for treating cardiac insufficiency containing said compound as an active ingredient. The compounds have a strong activity of reinforcing the contraction of cardiac muscles and a strong activity of reducing the heart rate. As the compounds are not toxic, they are useful medicines for treating cardiac insufficiency.
    • 式(I)的苯并吡喃衍生物,其中X 1和X 2不存在或表示氧原子; X表示氧原子,硫原子,氮原子(所述氮原子未被取代或被氢原子或C1-C4烷基取代),羰基或硫代羰基; A表示羟基或可与B一起形成单键; B代表氢原子或与A形成单键; Y表示未取代或被R 1取代的1-吡咯基,1-吡唑基,1-咪唑基,1-(1,2,3-三唑基)或1-(1,2,4-三唑基) 3>; R 1和R 2独立地表示氢原子,苯基或C 1 -C 4烷基; R 3表示氢原子,卤素原子,C 1 -C 6烷基和用于治疗含有所述化合物作为有效成分的心功能不全的药物。 这些化合物具有强化心肌收缩的活性和降低心率的强烈活性。 由于化合物没有毒性,它们是治疗心功能不全的有用药物。
    • 10. 发明申请
    • MELAMINE POLYMETAPHOSPHATE AND PROCESS FOR ITS PRODUCTION
    • 聚甲基丙烯酸甲酯及其生产工艺
    • WO1997044377A1
    • 1997-11-27
    • PCT/JP1997001712
    • 1997-05-21
    • NISSAN CHEMICAL INDUSTRIES, LTD.SUZUKI, KeitaroSHISHIDO, KoujiSHINDO, Masuo
    • NISSAN CHEMICAL INDUSTRIES, LTD.
    • C08G79/02
    • C08K5/34928C08G79/02C08K5/529
    • A melamine polymetaphosphate having a solubility of from 0.01 to 0.10 g/100 ml in water at 25 DEG C, a pH of from 2.5 to 4.5 in the form of a 10 wt.% aqueous slurry at 25 DEG C and a melamine content of from 1.0 to 1.1 mol per mol of phosphorus atom. A process for producing such a melamine polymetaphosphate, which comprises the following steps (a) and (b): (a) a step of mixing melamine, urea and an aqueous orthophosphoric acid solution containing at least 40 wt.% of orthophosphoric acid, in such a ratio that melamine is from 1.0 to 1.5 mol per mol of orthophosphoric acid and urea is from 0.1 to 1.5 mol per mol of orthophosphoric acid, at a temperature of from 0 to 140 DEG C, to form a reaction mixture, and stirring the reaction mixture at a temperature of from 0 to 140 DEG C, while removing water, to obtain a powdery product of a double salt of orthophosphoric acid with melamine and urea; and (b) a step of calcining the powdery product obtained in step (a) at a temperature of from 240 to 340 DEG C for from 0.1 to 30 hours, while preventing agglomeration, to obtain a melamine polymetaphosphate.
    • 在25℃下在水中溶解度为0.01至0.10g / 100ml,pH为2.5至4.5,在25℃下为10重量%含水浆料形式的三聚氰胺聚偏磷酸钠,三聚氰胺含量为 每摩尔磷原子为1.0-1.1摩尔。 一种制备这种三聚氰胺聚偏磷酸盐的方法,其包括以下步骤(a)和(b):(a)将含有至少40重量%正磷酸的三聚氰胺,尿素和正磷酸水溶液混合在 三聚氰胺的摩尔比为每摩尔正磷酸为1.0〜1.5摩尔,尿素为0.1〜1.5摩尔/升正磷酸,温度为0〜140℃,形成反应混合物,搅拌 反应混合物在0-140℃的温度下,同时除去水,得到正磷酸的双重盐与三聚氰胺和尿素的粉末状产物; 和(b)在240〜340℃的温度下煅烧步骤(a)中得到的粉末状产物0.1〜30小时,同时防止团聚,得到三聚氰胺聚偏磷酸酯的工序。