| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 101 | JPH0214350B2 - | JP50017382 | 1981-12-12 | JPH0214350B2 | 1990-04-06 | UIIRINHA YOHANESU FUBERUTASU |
| 102 | Production of 1,5-benzothiazepine derivative | JP20202787 | 1987-08-12 | JPS6445376A | 1989-02-17 | INOUE HIROZUMI; HARADA TSUNEHIRO; NAGASAWA MASAAKI |
| PURPOSE:To readily obtain the titled compound useful as a medicinal compound having excellent hypotensive, cerebral coronary vasodilator and/or blood platelet agglutination inhibitory action, by reacting a specific compound with amines as raw materials. CONSTITUTION:An compound expressed by formula I (R<1> is lower alkyl or lower alkoxy; R<2> is H or lower alkanoyl; either of R<3> and R<4> is lower alkyl or halogen and the other is H; X' is reactive residue) is reacted with an amine expressed by formula II (R<5> and R<6> are lower alkyl) or salt thereof in a suitable solvent in the presence or absence of a deacidifying agent, preferably at ambient temperature - while being heated to afford the aimed compound, expressed by formula III and useful for treating.preventing cerebropathy, such as cerebral vasospasm, cerebral ischemia or cerebral infraction, and cardiopathy, such as angina pectoris. The above-mentioned compound is treated with an acid to provide an acid addition salt. Furthermore, since the aforementioned reaction proceeds without accompanying racemization, the aimed compound can also be obtained as an optically active substance by using the optically active compound expressed by formula I. | ||||||
| 103 | Production of 1,5-benzothiazepine derivative | JP184586 | 1986-01-07 | JPS62161776A | 1987-07-17 | INOUE HIROZUMI; OTSUKA HISAO |
| PURPOSE: To economically obtain the titled compound useful as a hypotensor, a cerebral or coronary vasodilator and a platelet coagulation inhibitor, by alkylating 4-hydroxyphenyl group of a compound corresponding to the titled compound to 4-alkoxyphenyl group. CONSTITUTION: The compound of formula II (R 1 is lower alkyl; R 2 is H or lower alkanoyl; X 1 is H or lower alkyl) or its salt useful for the remedy amelio ration or prevention of cerebral diseases such as hypertension, cerebrovascular contraction, etc., cardiac diseases such as stenocardia or thromotic diseases such as cerebral thrombosis, etc., can be produced by alkylating the compound of formula I (R 3 is H or lower alkanoyl; X 2 is H, alkyl or protecting group), removing X 2 when it is a protecting group, optionally removing R 3 when it is lower alkanolyl group and optionally converting the product to its salt. Since the reaction can be performed without causing racemization, an optical isomer can be produced by using an optically active raw material. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 104 | Production of perhydro-1,4-thiazepine derivative | JP21357186 | 1986-09-10 | JPS62161775A | 1987-07-17 | YANAGISAWA HIROAKI; ISHIHARA SADAO; ANDO AKIKO; KANEZAKI TAKUO |
| PURPOSE:To obtain the titled compound having ACE inhibiting activity and useful as a hypotensive agent in high yield, by using a specific compound such as 6-amino-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepine, etc., as raw material. CONSTITUTION:The objective compound of formula V can be produced by (1) condensing a compound of formula I (R<1> is alkyl, cycloalkyl or aralkyl; R<2> is carboxyl-protecting group; R<3> is aryl or halogen-substituted alkyl) [e.g. 2-(p-nitrobenzenesulfonyloxy)-4-phynyl-butyric acid ethyl ester] with a compound of formula II (R<4> and R<5> are H, alkyl, cycloalkyl, aryl or heterocyclic group) in the presence of a desulfonation agent, (2) condensing the resultant compound of formula III with a compound of formula IV (X is halogen; R<6> is carboxyl- protecting group) in the presence of a base and (3) removing the carboxyl- protecting group R<6> from the condensation product. | ||||||
| 105 | JPS6145609B2 - | JP6736978 | 1978-06-05 | JPS6145609B2 | 1986-10-08 | SATO HIRONOBU; TOMITA KUNYUKI; KOBAYASHI SHINSAKU |
| 106 | 1-azaerythrinane derivative | JP18444585 | 1985-08-21 | JPS61112084A | 1986-05-30 | MURAI HIROSHI; MATSUMURA SHINGO; MORITA IWAO; KAZUNO KENJI; ENOMOTO HIROSHI; KIMURA KIYOSHI; KIMURA YUTAKA |
| NEW MATERIAL:The compound of formula I (Y is O or S; R1, R2 and R3 are H, lower alkoxy, halogen or OH; R4 is H, lower alkoxycarbonyl, lower alkyl, etc.). EXAMPLE:1-Ethoxycarbonyl-8-oxo-1-aza-11a-oxa-C-homoerythrinan. USE:An analgesic having low toxicity and excellent analgesic effect. PREPARATION:The compound of formula I can be prepared by condensing the 3-piperidone derivative of formula II (R7 and R8 are lower alkyl) with the amine of formula III in an inert solvent such as toluene under heating, and cyclizing the product by heating under acidic condition in the presence of a polyphosphoric acid, etc., at 30-250 deg.C. | ||||||
| 107 | 2,5-benzothiazonine derviative | JP15539483 | 1983-08-25 | JPS6048979A | 1985-03-16 | OKITSU MITSUTO; HIROTSU ICHIROU |
| NEW MATERIAL:A compound shown by the formula I (X is H, or halogen; R is H, or lower alkyl; Y is group shown by the formula II or group shown by the formula III). EXAMPLE: 1,3,4,5,6,7-Hexahydro-2,5-benzothiazonin. USE: A drug for circulatory system. Having an inhibitoy action on blood platelet aggregation, an inhibitory action on contraction of extracted intestine, vasodilating action on crown blood, etc. PREPARATION: A phenylthiomorpholin-3-one shown by the formula IV is reacted with a methyl halide such as methyl iodide, methyl bromide, etc. and silver perchlorate, silver 4-fluoroborate, Meerwein reagent, etc. to give a methylsulfonium salt shown by the formula V (Z⊖ is inorganic anion). It is heated in the presence of a base (e.g., sodium amide, etc.) to give a compound shown by the formula I . COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 108 | Novel medium-membered ring amidosulfide compound and synthetic method thereof | JP20078782 | 1982-11-15 | JPS5890571A | 1983-05-30 | OOISHI TAKESHI; OOTSUKA YASUHISA |
| NEW MATERIAL:A medium-membered ring amidosulfide compound expressed by formulaI[R is H or methyl; (n) is 8, 9, 10 or 12]. USE: A synthetic intermediate for useful medium-ring membered ketones, e.g. perfumes. PROCESS: An o-mercaptomethylaniline expressed by formula II or a disulfide thereof is reacted with a bromic acid chloride expressed by formula III in the presence of a base, e.g. triethylamine or pyridine, in a solvent, e.g. tetrahydrofuran (THF) or ether, to give a compound expressed by formula IV or a disulfide thereof, which is then subjected to the ring closure with an alkali, e.g. sodium ethoxide or sodium isopropoxide, in a mixed solvent of ethanol, etc. with dioxane, etc. to afford the compound expressed by formulaI(R is H). The resultant compound is then methylated to give the compound expressed by formulaI(R is methyl). COPYRIGHT: (C)1983,JPO&Japio | ||||||
| 109 | JPS5817754B2 - | JP8661079 | 1979-07-09 | JPS5817754B2 | 1983-04-09 | OOISHI TAKESHI; OOTSUKA YASUHISA |
| 110 | JPS5812264B2 - | JP8660979 | 1979-07-09 | JPS5812264B2 | 1983-03-07 | OOISHI TAKESHI; OOTSUKA YASUHISA |
| 111 | Novel medium-ring amidosulfide compound and its synthesis | JP8661079 | 1979-07-09 | JPS5612378A | 1981-02-06 | OOISHI TAKESHI; OOTSUKA YASUO |
| NEW MATERIAL:A compound shown by the formula I (R is H or CH 3; n is integer of 8W12). USE: An intermediate for medium-ring skeleton synthesis, especially for medium- membered ketone synthesis useful as a raw material of perfume. PROCESS: A compound shown by the formula II or its disulfide is reacted with a compound shown by the formula Br(CH 2) n-1COCl to give a compound shown by the formula III or its disulfide, which is treated with an alkali and subjected to ring closure to give a compound shown by the formula I wherein R is H. The compound shown by the formula I is methylated to give a compound shown by the formula I wherein R is CH 3. COPYRIGHT: (C)1981,JPO&Japio | ||||||
| 112 | Novel manufacture of novel thiophene derivative and biotin | JP6971180 | 1980-05-27 | JPS55162788A | 1980-12-18 | ENRIKO GIUSETSUPE BAGIORINI; HASHI RIN RII; MIRAN RADOJIE USUKOKOBITSUKU |
| 113 | Macrocyclic compounds having an aspartic protease inhibitory activity and their pharmaceutical use | JP2006518098 | 2004-07-02 | JP2009513510A | 2009-04-02 | クラウディア・ベッチュアールト; マリナ・ティンテルノート−ブロムライ |
| 本発明は、式Ｉ
【化１】 〔式中、Ｒ １は(Ｃ １−８ )アルキル、(Ｃ １−４ )アルコキシ(Ｃ １−４ )アルキル、ヒドロキシ(Ｃ １−６ )アルキル、(Ｃ １−４ )アルキルチオ(Ｃ １−４ )アルキル、(Ｃ １−６ )アルケニル、(Ｃ ３−７ )シクロアルキル、(Ｃ ３−７ )シクロアルキル(Ｃ １−４ )アルキル、ピペリジニルまたはピロリジニルであり、Ｒ ２およびＲ ４は、独立して水素または所望により置換されている(Ｃ １−８ )アルキル、(Ｃ ３−７ )シクロアルキル、(Ｃ ３−７ )シクロアルキル(Ｃ １−４ )アルキル、アリール、アリール(Ｃ １−４ )アルキル、ヘテロアリールまたはヘテロアリール(Ｃ １−４ )アルキルであるか、またはＲ ２およびＲ ４は、それらが結合している窒素と一体となって、所望により置換されているピペリジノ、ピロリジニル、モルホリノまたはピペラジニル基を形成し、Ｒ ３は水素または(Ｃ １−４ )アルキルであり、Ｘ １はＣＨ ２であり、Ｘ ２はＣＨ ２ 、Ｏ、Ｓ、ＣＯ、ＣＯＯ、ＯＣＯ、ＮＨＣＯ、ＣＯＮＨ、またはＮＲ(ここで、Ｒは水素または(Ｃ １−４ )アルキルである)であり、Ｙは(Ｃ １−８ )アルキレンまたは(Ｃ １−８ )アルキレンオキシ(Ｃ １−６ )アルキレン、(Ｃ １−８ )アルケニレンまたは(Ｃ １−８ )アルケニレンオキシ(Ｃ １−６ )アルキレンであり、Ａｒは独立してヒドロキシまたはハロゲンでモノ−、ジ−またはトリ置換されているフェニル環であり、それにより、Ｘ １およびＸ ２は、互いにメタまたはパラ位にあり、そして、ＺはＣＯであり、ＡＡは天然または非天然アルファ−アミノ酸であり、そしてｎは０または１であるか、またはＺはＳＯ ２であり、ＡＡは所望により置換されているエチレンカルボニル基(窒素をメチレン基で置換することによる天然または非天然アルファ−アミノ酸由来)であり、そしてｎは１である。 〕の大環状化合物；これらの化合物の製造法；これらを含む医薬組成物および組み合わせ；およびベータ−アミロイド産生および／または凝集に関連する神経障害および血管障害の処置におけるそれらの使用に関する。 |
||||||
| 114 | Macrocyclic lactam and its pharmaceutical use | JP2006538745 | 2004-11-04 | JP2007510002A | 2007-04-19 | イヴ・オーベルソン; クラウディア・ベッチャルト; クルト・ラウメン; シーム・ヤーコプ・フェーンストラ; トーマス・イョット・トロクスラー; マリーナ・ティンテルノット−ブロムライ; ライナー・マッハウアー; ラルフ・グラットハル |
| 本発明は、遊離塩形または酸付加塩形の、式(Ｉ)
【化１】 (式中、Ｒ １ 、Ｒ ２ 、Ｒ ３ 、Ｕ、Ｖ、Ｗ、Ｘ、Ｙ、Ｚおよびｎは明細書で定義の通りであり、大環状環に含まれる環原子の数は１４個、１５個、１６個または１７個である)の新規大環状化合物、それらの製造法、医薬としてのそれらの使用およびそれらを含む医薬組成物に関する。 |
||||||
| 115 | 1,4-heterocyclic metalloprotease inhibitor | JP51171298 | 1997-08-22 | JP2000516252A | 2000-12-05 | アルムステッド，ニール，グレゴリー．; タイウォ，イエツンデ，オラビシ．; チォン，メンヤン．; デ，ビィスワナス．; ネイチャス，マイケル，ジョージ．; ピクル，スタニスロウ．; マシューズ，ランドール，ストライカー． |
| (57)【要約】 本発明は、メタロプロテアーゼ類の阻害剤として有用な、請求の範囲に記載の式（Ｉ）の化合物、またはその光学異性体、ジアステレオマー、または鏡像異性体、その薬剤学的に許容可能な塩、またはその生物加水分解性のアミド、エステル、またはイミドを提供する。 また、薬剤組成物、前記化合物またはそれを含有する薬剤組成物を用いて、メタロプロテアーゼ活性に特徴的な疾患、障害および状態を治療する方法を開示する。 | ||||||
| 116 | Heterocyclic metalloprotease inhibitor | JP51171198 | 1997-08-22 | JP2000515166A | 2000-11-14 | アルムステッド，ニール，グレゴリー．; タイウォ，イエツンデ，オラビシ．; チォン，メンヤン．; デ，ビィスワナス．; ネイチャス，マイケル，ジョージ．; ピクル，スタニスロウ．; マシューズ，ランドール，ストライカー． |
| (57)【要約】 本発明は、メタロプロテアーゼ類の阻害剤として有用な、請求の範囲に記載の式（Ｉ）の化合物、またはその光学異性体、ジアステレオマー、または鏡像異性体、あるいはその薬剤学的に許容可能な塩、またはその生物加水分解性のアミド、エステル、またはイミドを提供する。 また、医薬組成物および前記化合物またはそれを含有する医薬組成物を用いて、メタロプロテアーゼ活性に特徴的な疾患、障害および状態を治療する方法を開示する。 | ||||||
| 117 | Hypolipemic 1,4-benzothiazepine-1,1-dioxide | JP6266598 | 1998-03-13 | JPH10279568A | 1998-10-20 | FALK EUGEN; ENHSEN ALFONS; STENGELIN SIEGFRIED; GLOMBIK HEINER |
| PROBLEM TO BE SOLVED: To obtain a new compound capable of reducing the concentration of an (ultra) low density lipoprotein cholesterol in plasma or serum and useful for treating and preventing hyperlipemia such as atherosclerosis. SOLUTION: This compound is represented by formula I {R 1 and R 2 are each a straight-chain 1-6C alkyl; R 3 is H or OR 11 [R 11 is H or a (substituted) 1-6C alkyl]; R 4 is pyridyl or a (substituted) phenyl; R 5, R 6 and R 8 are each H, a halogen, cyano, etc.; R 7 is represented by formula II (R 16 is COOH, CH 2OH, etc.), etc.; X is NH or O; R 9 and R 10 are each H or 1-6C alkyl}. The objective compound is prepared by acylating or alkylating a compound represented by formula III at the group X-H according to the standard method or glycosylating or glucuronidating the compound represented by formula III at the group X-H and then eliminating the protecting group, especially hydroxyl group and amino functional group. COPYRIGHT: (C)1998,JPO | ||||||
| 118 | Manufacturing method of perhydro-1,4-thiazepine derivatives | JP21357186 | 1986-09-10 | JPH07113020B2 | 1995-12-06 | YANAGISAWA HIROAKI; ISHIHARA SADAO; ANDO AKIKO; KANEZAKI TAKUO |
| 119 | Cyclic renin inhibitor containing 2-substituted (3s,4s)-4-amino-5-cyclohexyl-3-hydroxy pentanoic acid, 2-substitutued (3s,4s)-5-cyclo-hexyl-3,4-dihydroxy pentanoic acid or 2-substituted (4s,5s)-5-amino-6-cyclohexyl-4-hydroxyhexanoic acid or its analogs | JP15208892 | 1992-06-11 | JPH06157481A | 1994-06-03 | UIRIAMU JIEE GURIINRII; AN II UEEBAA; RARUFU EE RIBUERO; RIFU YANGU |
| PURPOSE: To prepare a novel compound inhibiting the angiotensinogen-cleaving action of renin. CONSTITUTION: The compound has the formula I [wherein A is H, aryl or the like; B is -CH 2-, the formula II (wherein R 3 is H, 1-4C alkyl or the like; R 11 is H, 1-4C alkyl; r is of from 0 to 2); D is a single bond, -NH-CO-NH- or the like; Z is -NH 2, -OH or the like; W is -O-, -NR 23 (wherein R 23 is H, 1-4C alkyl); V is the formula III (Y is O, NH or the like; R 5 is H, 1-4C alkyl or the like; R 10 is H or OH; x and y are each 0 or 1; z is of from 0 to 4) or the like; R 15 is 1-4C alkyl, aryl or the like; R 1 is 1-4C alkyl, aryl or the like; n is 0 or 1; s is 0 or 1; t is of from 1 to 4]. For example, the compound is the formula IV (wherein A-B is the formula V, V is the formula VI). The compound of the formula I is produced by starting with for example chirarity oxazolidinon and optical active aldehyde to produce 2-substituted ACHPA analogs, then converting to amide derivative and protected amino derivative, obtaining a cyclic precursor, cyclizing them, removing the protect group, and coupling with carbonic acid or the like. COPYRIGHT: (C)1994,JPO | ||||||
| 120 | JPH0573749B2 - | JP184586 | 1986-01-07 | JPH0573749B2 | 1993-10-15 | INOE HIROZUMI; OOTSUKA HISAO |
QQ群二维码
意见反馈
意见反馈