| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 61 | Dual action inhibitor | JP11587493 | 1993-05-18 | JP3487611B2 | 2004-01-19 | エドワード・ダブリュー・ペトリロ・ジュニア; ジェフリー・エイ・ロブル; ジョエル・シー・バリッシュ; デニス・イー・リオノ; ドナルド・エス・カラネウスキ |
| 62 | n- heterocyclic derivatives as Nos inhibitors | JP2001518702 | 2000-08-24 | JP2003507476A | 2003-02-25 | オー． アーナイズ，ダミアン; イエ，ビン; デイビッド エリクソン，シャウン; エイチ．ジェイ． オールマイヤー，マイケル; ツャオ，ツーチュン; ディー． ディビー，デイビッド; ジェイ． デブリン，ジェイムズ; エルウッド ザ サード ドーレ，ローランド; パーキンソン，ジョン; マドハブ パラドカール，ビドヤドハール; パン，コンファ; ビー． フィリップス，ゲイリー; ジェイ． ボールドウィン，ジョン; マクミラン，カーク; エム． モリッセイ，マイケル |
| (57)【要約】 式(Ya)で示されるN-複素環式誘導体や他のN-複素環化合物を一酸化窒素シンターゼの阻害剤として開示している。 これらの化合物を含む製剤組成物、一酸化窒素シンターゼ阻害剤としてのこれらの化合物の使用法、及びこれらの化合物の製法もまた開示している。 | ||||||
| 63 | n- heterocyclic derivatives as Nos inhibitor | JP53685398 | 1998-02-19 | JP2002515058A | 2002-05-21 | マッドーハヴ パラドカー ヴィディアドハー; マクミラン カーク; ビー フィリップス ギャリー; パン ゴングア; ジェイ デヴリン ジェイムズ; デイヴィッド エリクソン ショーン; ジェイ ボールドウィン ジョン; パーキンソン ジョン; オー アーナイズ ダミアン; チャオ ツーチュン; ディー ダヴェイ デイヴィッド; イェー ビン; エイチ ジェイ オールマイアー マイケル; エム モリッセイ マイケル; エルウッド ザ サード ドル ローランド |
| (57)【要約】 本明細書中には、式（Ｉ）： | ||||||
| 64 | Production of thiazine-indigo compound and its new intermediate | JP2000058620 | 2000-03-03 | JP2000344757A | 2000-12-12 | BORCHERT TILL; KAUL BANSI LAL; PIASTRA BRUNO; WOLF VALERIE |
| PROBLEM TO BE SOLVED: To provide a thiazine-indigo compound according to a method using an environmentally-friendly aqueous base by reacting specific two kinds of compounds in the presence of an aqueous system. SOLUTION: Each compound of a compound of formula I [R1 is an atom necessary to form (substituted)aromatic or aliphatic carbon ring or heterocyclic ring; R3 is H, a 1-12C alkyl or phenyl; R5 is an leaving group usually used for substitution reaction of carbonyl carbon atom; Hal is Cl or Br] and a compound of formula II is reacted with a compound of formula III (R2 is same as R1; R4 is a metal ion selected from Na+, K+ and Zn2+) in the presence of an aqueous system to provide the objective compound of formula IV or formula V. The reaction is carried out preferably at 1:1 molar ratio of reactant in water in the presence of an acidic catalyst, at about 0-150°C, more preferably 10-40°C. COPYRIGHT: (C)2000,JPO | ||||||
| 65 | Metalloproteinase inhibitors, pharmaceutical compositions containing them and their use as medicaments, as well as processes and intermediates useful in their preparation | JP52140597 | 1996-12-05 | JP2000502330A | 2000-02-29 | ズーク，スコット・イー; ダグニーノ，レイモンド，ジュニアー; ディーソン，マイケル・イー; ベンター，スティーブン・エル; メルニック，マイケル・ジェイ |
| (57)【要約】 本発明は、式（１）の化合物（式中、ＺはＯまたはＳであり；ＶはＣ *およびＮと一緒に６個の環原子を有する環を形成する二価の基であり、ここでＣ *およびＮ以外の環原子はそれぞれ独立して、置換されていないか、または適する置換基で置換されており、これら他の環原子のうち少なくとも１個はＯ、ＮおよびＳから選択される異種原子であり、残りは炭素原子であり；Ａｒはアリールまたはヘテロアリール基である）ならびにその薬剤学的に許容しうるプロドラッグ、塩類および溶媒和物に関する。 本発明はさらに、これらの化合物の薬剤学的に許容しうるプロドラッグ、塩類および溶媒和物に関する。 本発明はまた、式（１）の化合物またはその薬剤学的に許容しうるプロドラッグ、塩もしくは溶媒和物を投与することによりメタロプロテイナーゼ活性を阻害する方法に関する。 本発明はさらに、有効量のこれらの化合物、プロドラッグ、塩類および溶媒和物を含む薬剤組成物に関する。 本発明はさらに、有効量のこれらの化合物、プロドラッグ、塩類および溶媒和物を製造するのに有用な方法および中間体に関する。 | ||||||
| 66 | Compounds useful as anti-proliferative agents and garft inhibitor | JP50597596 | 1995-07-28 | JPH10503762A | 1998-04-07 | ディー． ヴァーニー，マイケル; ロミネス，ウイリアム，エイチ． |
| Compounds of the Formula I, which are in equilibrium with their 4-hydroxy tautomers and are in the form of diastereomeric mixtures, and their pharmaceutically acceptable salts are potent GARFT inhibitors: <IMAGE> (I) wherein A, Z, X, and R1 and R2 are defined in the specification. These compounds and their salts are useful as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents. The invention also relates to compounds useful as intermediates for preparing such compounds, and to their synthesis. | ||||||
| 67 | 6- (substituted methylene) penems and intermediates | JP51063794 | 1993-10-20 | JPH08502504A | 1996-03-19 | ハリントン，フランク・ピーター; ブルーム，ナイジェル・ジョン・ペリーマン |
| (57)【要約】 式（Ｉ）： ［式中、Ｒ 1は、水素または有機置換基であり；Ｒ 2は、一般式（ａ）： （式中、Ｒ 4およびＲ 5は、独立して、水素、または前記環系における水素原子を置換する１以上の置換基であり；ｍは、２または３であり；ｐは、０、１または２である）で示される縮合二環式複素環系であり；Ｒ 3は、水素、塩形成カチオンまたはエステル形成基であり；記号＝／＝は、二重結合がＥまたはＺのいずれかの配置であることを示す］で示される化合物。 | ||||||
| 68 | Nitromethylene derivatives, their preparation and insecticide | JP1862885 | 1985-02-04 | JPH0649699B2 | 1994-06-29 | 伸三 利部; 真一 坪井; 紘三 塩川; 晃一 盛家 |
| 69 | 3-thioxo-benzothiazine derivative | JP20042686 | 1986-08-27 | JPS6357579A | 1988-03-12 | IWAO JUNICHI; ISO TADASHI; KAWASHIMA YOICHI |
| NEW MATERIAL:The 3-thioxobenzothiazine derivative of formula I (R<1> is H, lower alkyl, lower alkoxy, halogen, nitro, etc.; R<2> is H, lower alkyl, lower alkoxy, cyano, etc.; R<3> is H, lower alkyl or -A-R<7>; R<4> and R<5> are H, hydroxy, lower alkyl, lower alkoxy, etc.; R<7> is hydroxy, halogen, lower alkoxy, etc.; A is lower alkylene). EXAMPLE:3,4-Dihydro-2-{ 5-methoxy-2-[ 4-[ N-methyl-N-[2-[(3,4-methylenedioxy) phenoxy]ethyl]amino]butoxy]phenyl}-4-methyl-3-thioxo-2H-1,4-benzothiaz ine. USE:The compound exhibits platelet coagulation inhibiting and calcium antagonistic activities and is useful as a remedy for circulatory diseases. PREPARATION:The compound of formula I can be produced by reacting the compound of formula II e.g. with a Lawesson's reagent. | ||||||
| 70 | Benzoxazino or benzothiazinorifamycin derivative | JP18116586 | 1986-07-31 | JPS6335578A | 1988-02-16 | YAMANE TAKEHIKO; KONDO HIDEO; HASHIZUME TAKUSHI; YAMASHITA KATSUJI; HOSOE KAZUNORI; WATANABE KIYOSHI |
| NEW MATERIAL:The compound of formula I (n is 1-5; X is O or S; R<1> and R<2> are H, 1-4C alkyl or 1-4C hydroxyalkyl) and its salt. USE:A medicine. An antibacterial agent. It is a solid having dark red color, soluble in a number of organic solvents, exhibiting strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria and having low toxicity. It can be used as a production raw material for novel rifamycin derivative of formula II having strong antibacterial activity. It is administered at a rate of 10mg-10g of the active component daily for adult. PREPARATION:The compound of formula I can be produced by reacting a rifamycin derivative of formula III with an amine of formula IV in an organic solvent such as methanol in the presence of a reducing agent such as sodium cyanoborohydride at room temperature for 30min - about 1 month, thereby effecting reductive amination reaction. | ||||||
| 71 | 1,3-thiazine or 1,3-oxazine derivative | JP26223785 | 1985-11-20 | JPS62120374A | 1987-06-01 | SHIRAKI MASAMI; ABE YUKIO; KAWAHARA KIMINORI; YAMANAKA TSUTOMU |
| NEW MATERIAL:A compound expressed by formula I [Z is S or O; R<1> is H, lower alkyl or phenyl which may have a substituent group, e.g. halogen, etc.; R<2> is H, lower alkyl, cycloalkyl which may have lower alkyl, (CH2)mNR<3>R<4> or (CH2)nAr; R<3> and R<4> are lower alkyl or heterocyclic ring which may contain further O as a hetero atom in NR<3>R<4>; m is 2 or 3; Ar is pyridyl or phenyl which may have a substituent group, e.g. halogen, etc.; n is 0, 1 or 2; X is H, halogen or lower alkoxy] and an acid addition salt thereof. EXAMPLE:5-Methyl-5-(4-chlorophenyl)-2-[ 2-(2-pyridyl)ethylimino ]-3,4,5,6-tetrahy dro-1H-1,3-thiazine. USE:A remedy for cardiopathy (increasing agent for coronary blood stream, cardiotonic agent, anti-inflammatory agent or diuretic agent). PREPARATION:A compound expressed by formula II is reacted with a compound expressed by the formula R<2>NCS to give a compound expressed by formula III, which is cyclized to afford the aimed compound expressed by formula I. | ||||||
| 72 | Novel spiroimidazolidine-2,5-dione derivative and production thereof | JP6620485 | 1985-03-29 | JPS61233684A | 1986-10-17 | IRIKURA TSUTOMU; TAKAGI KOICHI; OKAMURA HISAYA; FUJIMORI SHIZUYOSHI; HIRATA YOSHIHIRO |
| NEW MATERIAL:An imidazolidine-2,5-dione derivative shown by the formula I (R1 is H, nitro, chlorosulfonyl, sulfamoyl, halogen, lower alkyl, lower alkoxy, or N-lower alkylsulfamoyl; R2 is H, halogen, lower alkyl, or lower alkoxy; R3 is H, lower alkyl, or aryl; x is methylene, O, S, sulfinyl, or sulfonyl) linked with spiro bond and its salt. EXAMPLE:5', 6'-Dihydrospiro[imidazolidine-4, 1'-[4H]pyrrolo[3, 2, 1-ij]quinoline]-2,2',5(1'H)-trione. USE:Showing ihibitory action on aldose reductase, useful as a remedy and preventive for diabetic complication. Having no antivulsant action, capable of being administered for a long period. PREPARATION:A compound shown by the formula II is reacted with a metallic cyanide and ammonium carbonate, etc., to give a compound shown by the formula. | ||||||
| 73 | Novel 1,4-thiazine derivative | JP6467985 | 1985-03-28 | JPS61225174A | 1986-10-06 | TAKASE MUNEAKI; YOSHIOKA KIMITOMO; YAMAZAKI HIROSUKE |
| NEW MATERIAL:A compound shown by the formula I (R1 and R2 are H, alkyl, alkoxy, amino, OH, 5-membered hetero ring residue, etc.; R3 is H, or lower alkyl; R4 is H, or lower alkyl; R5 is N-containing hetero ring residue) and its acid addition salt. EXAMPLE:2,5-Dimethyl-6-(4-pyridyl)-2H-1,4-thiazin-3(4H)-one. USE:A cardiac. PREPARATION:A compound shown by the formula II is reacted with a com pound shown by the formula A-X' [A is CXnH3-n-CH2-O-CO- (X is halogen; n is 1-3); X' is halogen] at normal temperature at normal pressure for 1-7hr, to give a compound shown by the formula I where R5 is A-R5' (R5' is N- containing hetero ring residue), etc. | ||||||
| 74 | Nitromethylene derivative, production thereof and insecticide | JP1862885 | 1985-02-04 | JPS61178982A | 1986-08-11 | SHIOKAWA KOZO; TSUBOI SHINICHI; TOSHIBE SHINZO; SEIKE KOUICHI |
| NEW MATERIAL:A compound expressed by formula I (R is H or alkyl; X is alkyl, alkoxy, alkylthio, alkenyl, etc. which may be substituted by halogen or halogen, nitro or cyano, etc.; l is 1, 2, 3 or 4; m is 2, 3 or 4; X is not halogen when l is 1 and all Xs are not halogen at the same time when l is 2, 3 or 4). EXAMPLE: 3-(2-Methyl-5-pyridylmethyl)-2-(nitromethylene)thiazolidine. USE: An insecticide capable of exhibiting improved insecticidal effect particularly on injurious insects of the order Hemiptera, e.g. aphids, planthoppers, leaf- hoppers, etc. PREPARATION: A compound expressed by formula II is reacted with a compound expressed by formula III (R' is lower alkyl or benzyl, two R's together represent ≥2C lower alkylene, or together with X may form a ring) in a suitable inert organic solvent at 0W100°C to give the aimed compound expressed by formula I. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 75 | Nitromethylene derivative, intermediate therefor, production thereof and insecticide | JP1862785 | 1985-02-04 | JPS61178981A | 1986-08-11 | SHIOKAWA KOZO; TSUBOI SHINICHI; TOSHIBE SHINZO; SEIKE KOUICHI |
| NEW MATERIAL:A compound expressed by formula I (R is H or alkyl; X is halogen; l is 1, 2, 3 or 4; m is 2, 3 or 4). EXAMPLE: 3-(2-Chloro-5-pyridylmethyl)2-nitromethylenetetrahydro-H-1,3-t hiazine. USE: An insecticide capable of exhibiting improved insecticidal effect particularly on injurious insects of the order Hemiptera, e.g. aphids, planthoppers, leaf- hoppers, etc. PREPARATION: A compound expressed by formula II is reacted with a compound expressed by formula III (R' is lower alkyl or benzyl; two R's together may represent ≥2C lower alkylene or together with S may form a ring) in a suitable inert organic solvent at 0W100°C to give the aimed compound expressed by formula I. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 76 | 1,2-benzothiazine-3-carboxamide derivative | JP146085 | 1985-01-10 | JPS61161281A | 1986-07-21 | KIKAZAWA KAZUO; HIIRAGI MINEJI; IRINO OSAMU; NAKAZATO KIKUO; KANEZUKA SATOYUKI; OBA SEIICHI; WAKIZAKA KIKUO; MURAYAMA YUU; RYUTSUU MASAKATSU |
| NEW MATERIAL:The compound of formula I (R1 is 5-chloro-3-methyl-2-pyridyl, 3,5-dichloro-6-methyl-2-pyridyl, 4-propyl-2-pyridyl, etc.; R2 is lower alkyl). EXAMPLE:4-Hydroxy-2-methyl-N-( 5-chloro-3-methyl-2-pyridyl )-2H-1, 2-benzothia zine-3-carboxamide-1,1-dioxide. USE:An anti-inflammatory agent. It is a low-toxic compound having low side effects such as digestive tract disorder, and useful for the remedy of inflammation of mammals. PREPARATION:The compound of formula I can be produced by condensing 1,2-benzoxazine-3-carboxylic acid of formula II or its reactive derivative with e.g. an acid chloride, acid anhydride or the amine of formula III. | ||||||
| 77 | Pyridothiazinorifamycin derivative, and pharmaceutical application thereof | JP26243684 | 1984-12-11 | JPS61140588A | 1986-06-27 | KITAMURA MIKIYA; TAGUCHI MASAHIRO; TONOMURA MIKIO; TSUKAMOTO GORO |
| NEW MATERIAL:The compound of formula I. USE:A tuberculostat. It exhibits strong growth inhibiting activity against Mycobacterium tuberculosis, and extremely strong bactericidal effect even to the bacteria of resting stage. It is transferred readily to the pulmonary tissue which is a tissue liable to be attached by tubercursos, by oral administration. It has low toxicity. PREPARATION:The objective compound can be prepared according to the reac tion formula, by reacting the 3-halogenorifamycin S of formula II (X is halogen) (a starting material) with 3-amino-pyridine-2-thiol of formula III in a polar organic solvent such as formamide, preferably in the presence of a basic sub stance such as sodium bicarbonate, usually at 0-40 deg.C, preferably treating the reaction product with an oxidizing agent such as manganese dioxide to obtain the pyridothiazinorifamycin of formula IV, and reacting the compound with N-ethylisopropylamine of formula V in a polar solvent such as DMF, usually at 0-40 deg.C for 10hr-10 days. | ||||||
| 78 | Novel compound and its preparation | JP20847084 | 1984-10-03 | JPS6185394A | 1986-04-30 | HASEGAWA TORU; HARADA SETSUO |
| NEW MATERIAL:The antibiotic substance TAN-528B of formula having the following characteristics. Apperance, orange yellow crystalline powder; meting point, 170W175°C (decomposition); specific rotation, [α] 27$D-32°±5° (C=0.10, in chloroform); elemental analysis (%), C 59.86, H 6.48, N 1.98, S 3.52; molecular formla, C 37H 47NO 13S; molecular weight, 745.84; solubility, easily soluble in ace tone, ethyl acetate, dichloro-methane, and dimethyl sulfoxide, ahrdly soluble in water and hexane; color reaction, positive to Barton reaction and magnesium acetate reaction, negative to ninhydrin reaction, Dragendorff reaction, etc.; etc. USE: Antibafterial agent effective mainly to Gram-positive bacterial and applicable by oral administration. PREPARATION: Streptomyces albolongus CM-11 strain (FERM P-7877) is cultured preferably in a liquid medium by submerged technique at 6W8 pH and 17W30°C for 24W72hr. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 79 | Novel 1, 4-thiazine derivative and its preparation | JP20878184 | 1984-10-04 | JPS6185386A | 1986-04-30 | TAKASE MUNEAKI; YOSHIOKA KIMITOMO; YAMAZAKI HIROSUKE |
| NEW MATERIAL:The compound of formula I (R1 and R2 are H or lower alkyl; R3 is residue of nitrogen-containing hetero-ring) and its salt. EXAMPLE:5-Methyl-6-(4-quinolinyl)2-2H-1, 4-thiazin-3(4H)-one. USE:Remedy for cardiopathy. It increases the myocardial systole, and has low acute toxicity. PREPARATION:The objective compound can be prepared by reacting the compound of formula II [e.g. 5-methyl-2H-1, 4-thiazin-3(4H)-one, etc.] with the compound of formula AX' [A is CXnH3-nCH2OCO (X is halogen; n is 1-3); X' is halogen other than X] (e.g. 2,2,2-trichloroethyl chloroformate) and the compound of formula R3H (e.g. quinoline) preferably for 1-7hr, and reacting the resultant compound of formula III (R3' is dihydro residue of nitrogen-containing hetero-ring) with sulfur preferably at 140-180 deg.C for 1-5hr. | ||||||
| 80 | Piperazine derivative and its acid adduct | JP4796684 | 1984-03-13 | JPS60193975A | 1985-10-02 | FUKAMI JIICHI; INOUE SHINYA; NITSUTA KAZUMASA; NAKAO KENICHIROU; KIKUMOTO RIYOUJI |
| NEW MATERIAL:A piperazine derivative of formula I [R 1 is OH, OR 3 (R 3 is 1W 3C alkyl), SR 3, SOR 3, SO 2R 3; R 2 is C(=O)NH 2, CSNH 2, C(=O)NHR 4 (R 4 is 1W 3C alkyl), R 1 and NHR 2 may incorporate to form a group of formula II (A is formula III), formula IV, formula V; X is C=O, C(OH)H; Ar is pyridyl, phenyl; n is 3W5] and its acid adduct. EXAMPLE: 5-[4-(4-Phenyl-1-piperazinyl)butyryl]-2-methoxy-N-carbamoylaniline. USE: Hypotensor. PREPARATION: For example, the reaction of ω-halogenoalkanoylbenzene of formula VI (X is halogen) with a piperazine of formula VII gives a compound of formula I where Z is C=O. COPYRIGHT: (C)1985,JPO&Japio | ||||||
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