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    • 1. 发明授权
    • Benzopyran compound and its pharmaceutical use
    • 苯并吡喃化合物及其药物用途
    • US5021432A
    • 1991-06-04
    • US340271
    • 1989-04-19
    • Tsutomu YamanakaToshio SekiTohru NakajimaOsamu Yaoka
    • Tsutomu YamanakaToshio SekiTohru NakajimaOsamu Yaoka
    • C07D311/68A61K31/35A61K31/352A61K31/443A61K31/4433A61K31/455A61K31/50A61K31/535A61P9/08A61P9/10A61P9/12A61P25/02C07D311/70C07D311/96C07D405/04C07D405/12C07D407/12C07D409/12
    • C07D405/12C07D311/68C07D407/12
    • A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 (wherein R.sup.1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R.sup.2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxy-carbonyl-lower alkyl, an aryl or a heteroaryl); R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.sup.6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkylcarbamoyloxy and R.sup.7 represents hydrogen, or R.sup.6 and R.sup.7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, and alkanoyl, an aroyl, a halo-alkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, and arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use.The compounds of the present invention exhibit remarkable and long lasting antihypertensive actions and peripheral vascular relaxant actions and therefore are useful as therapeutic medicines for hypertensive. Since they also display selective coronary vasodilating actions and the duration of actions are very long, they are of use as therapeutic medicines for cardiovascular disturbances such as angina pectoris and cardiac insufficiency.
    • 2. 发明授权
    • Benzopyran compound and its pharmaceutical use
    • 苯并吡喃化合物及其药物用途
    • US5318969A
    • 1994-06-07
    • US897253
    • 1992-06-11
    • Tsutomu YamanakaToshio SekiTohru NakajimaOsamu Yaoka
    • Tsutomu YamanakaToshio SekiTohru NakajimaOsamu Yaoka
    • C07D311/68A61K31/35A61K31/352A61K31/443A61K31/4433A61K31/455A61K31/50A61K31/535A61P9/08A61P9/10A61P9/12A61P25/02C07D311/70C07D311/96C07D405/04C07D405/12C07D407/12C07D409/12
    • C07D405/12C07D311/68C07D407/12
    • A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 ; R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.sup.6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkylcarbamoyloxy and R.sup.7 represents hydrogen, or R.sup.6 and R.sup.7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, an alkanoyl, an aroyl, a halo-alkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use.
    • 通式(I)的苯并吡喃化合物其中A表示-OR1或-NH-COR2; R 3表示氢,低级烷基,低级烷氧基,氨基,一或二低级烷基氨基,氨基 - 低级烷基,羟基 - 低级烷基,卤代低级烷基,低级烷氧基 - 低级烷基,酰氧基 低级烷基,低级烷氧基羰基 - 低级烷基,芳基或杂芳基,或R2和R3组合在一起形成具有1至2个碳原子的亚烷基; R4和R5相同或不同,分别表示氢或低级烷基,或者组合在一起形成具有2-5个碳原子的亚烷基; R6表示羟基,甲酰氧基,烷酰氧基,卤代烷酰氧基,低级烷氧基羰氧基,芳酰氧基,杂芳氧基,氨基甲酰氧基,一或二低级烷基氨基甲酰氧基,R7表示氢,或R6和R7组合在一起形成键,X和 Y分别相同或不同,分别表示氢,卤素,硝基,氰基,低级烷基,低级烷氧基,卤代低级烷基,羧基,甲酰基,烷酰基,芳酰基,卤代烷酰基,氨基甲酰基, 低级烷基亚磺酰基,芳基亚磺酰基,低级烷基磺酰基,芳基磺酰基,亚磺酰氨基或单 - 或二 - 低级烷基亚磺酰氨基,或其药学上可接受的盐及其药物用途。
    • 3. 发明授权
    • Benzopyran compound and its pharmaceutical use
    • US5143936A
    • 1992-09-01
    • US672657
    • 1991-03-21
    • Tsutomu YamanakaToshio SekiTohru NakajimaOsamu Yaoka
    • Tsutomu YamanakaToshio SekiTohru NakajimaOsamu Yaoka
    • C07D311/68A61K31/35A61K31/352A61K31/443A61K31/4433A61K31/455A61K31/50A61K31/535A61P9/08A61P9/10A61P9/12A61P25/02C07D311/70C07D311/96C07D405/04C07D405/12C07D407/12C07D409/12
    • C07D405/12C07D311/68C07D407/12
    • A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 (wherein R.sup.1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R.sup.2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl); R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.sup.6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkycarbamoyloxy and R.sup.7 represents hydrogen, or R.sup.6 and R.sup.7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, an alkanoyl, an aroyl, a halo-alkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use.The compounds of the present invention exhibit remarkable and long lasting antihypertensive actions and peripheral vascular relaxant actions and therefore are useful as therapeutic medicines for hypertensive. Since they also display selective coronary vasodilating actions and the duration of actions are very long, they are of use as therapeutic medicines for cardiovascular disturbances such as angina pectoris and cardiac insufficiency.
    • 4. 发明授权
    • Ortho-aminomethylphenol compounds
    • 邻氨基甲基苯酚化合物
    • US4709095A
    • 1987-11-24
    • US853809
    • 1986-03-25
    • Tsutomu YamanakaOsamu Yaoka
    • Tsutomu YamanakaOsamu Yaoka
    • A61K31/15A61K31/35A61K31/352A61K31/47A61P7/10A61P9/12A61P25/04A61P29/00C07C67/00C07C239/00C07C251/48C07D215/42C07D311/68C07C131/00
    • C07D311/68
    • Ortho-aminomethylphenol compounds of the formula: ##STR1## wherein X is hydrogen or halogen, R is hydrogen or alkyl having 1 to 4 carbon atoms and A is alkyl having 1 to 4 carbon atoms, phenyl, benzyl or a bivalent radical selected from --(CH.sub.2).sub.3 -- and --O(CH.sub.2).sub.2 -- and joined together with the 3 or 5 position of the benzene nucleus to form a bicycle, or pharmaceutically acceptable salts thereof, a method of preparing said compounds and a pharmaceutical composition containing said compounds, are disclosed.Such compounds exhibit antiinflammatory, analgesic, diuretic and antihypertensive activities, so they are useful in the treatment for diseases caused by inflammation, edema or hypertension.
    • PCT No.PCT / JP85 / 00440 Sec。 371日期:1986年3月25日 102(e)日期1986年3月25日PCT提交1985年8月2日PCT公布。 出版物WO86 / 01201 日本:1986年2月27日。下式的邻氨基甲基苯酚化合物:其中X是氢或卤素,R是氢或具有1至4个碳原子的烷基,A是具有1至4个碳原子的烷基,苯基,苄基 或选自 - (CH 2)3 - 和-O(CH 2)2 - 的二价基团并且与苯核的3或5位相连接以形成自行车或其药学上可接受的盐,制备所述化合物的方法 和含有所述化合物的药物组合物。 这些化合物表现出抗炎,止痛,利尿和抗高血压活性,因此它们可用于治疗由炎症,水肿或高血压引起的疾病。
    • 7. 发明授权
    • Oxodiazine compounds and pharmaceutical compositions thereof
    • Oxodiazine化合物及其药物组合物
    • US4713381A
    • 1987-12-15
    • US867170
    • 1986-05-27
    • Hideki AoMinoru ObataTsutomu YamanakaHiroshi Mikashima
    • Hideki AoMinoru ObataTsutomu YamanakaHiroshi Mikashima
    • C07D471/04C07D487/04C07D513/04A61K31/535A61K31/54
    • C07D471/04C07D487/04C07D513/04
    • An oxodiazine compound of the formula: ##STR1## or a pharamceutically acceptable acid addition salt thereof, wherein each of R.sup.1 and R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkoxy, phenyl-C.sub.1-4 alkyl-oxy which may be optionally substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus, or phenyl which may be substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus; X is --S--, --CH.dbd.N-- or --C(R.sup.3).dbd.C(R.sup.4)--, where each of R.sup.3 and R.sup.4 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkoxy or phenyl-C.sub.1-4 alkyl-oxy which may be optionally substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus; and one of A and B is oxygen, sulfur or --NH-- and the other is --C(R.sup.5) (R.sup.6)--, where each of R.sup.5 and R.sup.6 is hydrogen or C.sub.1-4 alkyl.Such compounds are useful as antithrombotic agents, antianginal agents, coronary circulation improving agent, cerebral circulation improving agents, peripheral circulation improving agents, analgesics and antiinflammatory agents.
    • 下式的氧代二嗪化合物或其药学上可接受的酸加成盐,其中R 1和R 2各自为氢,卤素,C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基-C 1-4烷氧基, 苯基-C 1-4烷基氧基,其可任选被至少一个选自以下的取代基取代:苯基核上的卤素,C 1-4烷基和C 1-4烷氧基,或可被至少一个 选自苯基核上的卤素,C 1-4烷基和C 1-4烷氧基的取代基; X是-S-, -​​ CH = N-或-C(R 3)= C(R 4) - ,其中R 3和R 4各自是氢,卤素,C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基 - C 1-4烷氧基或苯基-C 1-4烷氧基,其可任选被至少一个选自苯基核上的卤素,C 1-4烷基和C 1-4烷氧基的取代基取代; A和B之一是氧,硫或-NH-,另一个是-C(R 5)(R 6) - ,其中R 5和R 6各自是氢或C 1-4烷基。 这些化合物可用作抗血栓形成剂,抗心绞痛剂,冠状循环改善剂,脑循环改善剂,外周循环改善剂,止痛剂和抗炎剂。
    • 8. 发明授权
    • 2,5-Di-substituted 4-oxazolealkanoic acid and esters
    • 2,5-二取代的4-恶唑烷酸和酯
    • US4012412A
    • 1977-03-15
    • US557692
    • 1975-03-12
    • Tsutomu YamanakaToshihiro KobayakawaMitsuhiro KonishiKuniki Ikeda
    • Tsutomu YamanakaToshihiro KobayakawaMitsuhiro KonishiKuniki Ikeda
    • A61K31/421C07D263/42
    • C07D263/42Y10S514/822
    • 2,5-Di-substituted 4-oxazolealkanoic acids and esters thereof of the formula: ##STR1## WHEREIN M REPRESENTS AN INTEGER OF 1 TO 2; R.sup.1 represents an alkyl group having 1 to 4 carbon atoms; n represents an integer of 1 to 2; R represents a mono- or di-substituted phenyl group (in which the substituents are selected from the group consisting of a halogen atom, a methyl group, a methoxy group, a nitro group, a trifluoromethyl group, a phenyl group, a halogen-substituted phenyl group, a phenoxy group and a halogen-substituted phenoxy group), a pyridyl group, a halogen-substituted pyridyl group, a furyl group, a halogen-substituted furyl group, a thienyl group, a halogen-substituted thienyl group, a naphthyl group or a halogen-substituted naphthyl group; when m represents an integer of 1, Y represents an hydrogen atom, an alkyl group having 1 to 2 carbon atoms, a benzyl group or a pyridylmethyl group; and when m represents an integer of 2, Y represents a trimethylene group. These compounds are useful as drugs for the treatment of arteriosclerosis, thrombosis and hypertension with lipid metabolism disorder.
    • 2,5-二取代的4-恶唑烷酸及其酯,具有下式:其中M代表1至2的整数; R1表示碳原子数1〜4的烷基。 n表示1〜2的整数, R表示单取代或二取代的苯基(其中取代基选自卤素原子,甲基,甲氧基,硝基,三氟甲基,苯基, 取代苯基,苯氧基和卤素取代的苯氧基),吡啶基,卤素取代的吡啶基,呋喃基,卤素取代的呋喃基,噻吩基,卤素取代的噻吩基, 萘基或卤素取代的萘基; 当m表示1的整数时,Y表示氢原子,碳原子数1〜2的烷基,苄基或吡啶基甲基。 当m表示2的整数时,Y表示三亚甲基。 这些化合物可用作用于治疗动脉硬化,血栓形成和高血压与脂质代谢紊乱的药物。