| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | 8-Chloro-1,5-benzothiazepine derivatives | US610856 | 1984-05-16 | US4567175A | 1986-01-28 | Mikio Takeda; Tokuro Oh-ishi; Hiromichi Nakajima; Taku Nagao |
| Novel 8-chloro-1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or a group of the formula: R.sup.4 CO--, each of R.sup.2 and R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and a pharmaceutically acceptable acid addition salt thereof are useful as hypotensive agents and/or coronary or cerebral vasodilators. | ||||||
| 82 | Intermediates for the preparation of biotin | US324326 | 1981-11-23 | US4382031A | 1983-05-03 | Enrico G. Baggiolini; Hsi L. Lee; Milan R. Uskokovic |
| A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates. | ||||||
| 83 | Intermediate racemates for the preparation of biotin and a process for their preparation | US150116 | 1980-05-15 | US4284557A | 1981-08-18 | Enrico G. Baggiolini; Hsi L. Lee; Milan R. Uskokovic |
| A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates. | ||||||
| 84 | Carbamate esters of 2-oxyimino-3-keto-1,4-diheterocyclics | US3790566D | 1971-08-12 | US3790566A | 1974-02-05 | BELLINA R |
| CHEMICAL COMPOUNDS OF THE CLASS OF CARBAMATE ESTERS OF 2-OXYIMINO-3-KETO-1,4-DIHETEROCYCLICS, SUCH AS 2METHYLCARBAMOYLOXYIMINO-4METHYL -3 - THIOMORPHOLINONE USEFUL IN CONTROLLING PESTS SUCH AS INSECTS AND NEMATODES.
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| 85 | Dibenzoazathiacycloalkane carboxamides and related oxa compounds | US3452046D | 1966-04-29 | US3452046A | 1969-06-24 | YALE HARRY L; BERNSTEIN JACK |
| 86 | Novel 4, 1-benzothiazepin-2(1h)-ones and 4, 1-benzothiazepines | US53572266 | 1966-03-21 | US3400119A | 1968-09-03 | WILHELM WENNER; RADOJE USKOKOVIC MILAN |
| 87 | Benzothiazocinones, related compounds and their preparation | US20923562 | 1962-07-11 | US3155649A | 1964-11-03 | JOHN KRAPCHO; TURK CHESTER F |
| 88 | Macrocyclic lactam and its pharmaceutical use | JP2006538745 | 2004-11-04 | JP4628366B2 | 2011-02-09 | 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 |
| 89 | Crystalline dibenzothiazepine derivative and use thereof as antipsychotic agent | JP2008313248 | 2008-12-09 | JP2009102345A | 2009-05-14 | SNAPE EVAN WILLIAM |
| PROBLEM TO BE SOLVED: To provide crystalline 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b, f][1, 4]thiazepine which can be used for the treatment of psychoses. SOLUTION: The crystalline 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b, f][1, 4]thiazepine (I) can be manufactured by crystallizing 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b, f][1, 4]thiazepine from a non-aromatic solvent, for example, ethyl acetate, isobutyl acetate, methyl isobutyl ketone or methyl t-butyl ether, preferably in the absence of water. The manufactured crystalline substance may be converted into a pharmaceutically acceptable salt, for example, a fumarate. COPYRIGHT: (C)2009,JPO&INPIT | ||||||
| 90 | The method of generating the c1-c15- fragment and its derivatives of epothilone | JP2006518018 | 2004-06-19 | JP2009513498A | 2009-04-02 | クラール，ウルリヒ; シュベーデ，ボルフガンク; スクバラ，ベルナー; ブフマン，ベルント |
| 本発明は、エポチロンのC 1 -C 15フラグメント及びその誘導体の製造方法に関して、ここでC 1 -C 6フラグメントがC 7 -C 12フラグメントに結合され、C 1 -C 12フラグメントが形成され、次に、C 13 -C 15 、フラグメントにより転換され、生成されるべきC 1 -C 15エポチロン中間体生成物が形成される。 このようにして生成されたC 1 -C 15エポチロン中間体生成物は、既知方法に従って、固有の活性成分に転換され得る。 本発明はまた、その対応するC 1 -C 12フラグメントにも関する。 | ||||||
| 91 | Tricyclic benzazepine-Basopuretsushin antagonist | JP19588694 | 1994-07-28 | JP3630449B2 | 2005-03-16 | ジエイ・デイ・アルブライト; シユエメイ・ドウ; フク−ワ・サム; マービン・エフ・レイク |
| 92 | Substituted with sugar residues 1,4-benzothiazepine 1,1-dioxide derivatives, processes for their preparation, pharmaceutical and its use including it | JP2000610842 | 2000-03-23 | JP2002541248A | 2002-12-03 | ヴェンデリン・フリック; ハイナー・グロムビク; ハンス−ルートヴィヒ・シェーファー; フーベルト・ホイアー |
| (57)【要約】 本発明は、置換された１,４−ベンゾチアゼピン−１,１−ジオキシド誘導体およびその酸付加塩に関する。 本発明は式（Ｉ）の１,４−ベンゾチアゼピン−１,１−ジオキシド誘導体（式中、Ｒ 1 、Ｒ 2 、Ｒ 3およびＺは明細書に記載した意味を有する）、その生理的に許容される塩および生理的に機能性の誘導体、ならびにその製造方法を開示する。 これらの化合物は例えば高脂質血症剤として使用するのに適している。 【化１】 | ||||||
| 93 | Pharmaceutical group of compounds | JP51195998 | 1997-08-29 | JP2002514175A | 2002-05-14 | アル―アウォー，リマ・エス; エールハート，ウィリアム・ジェイ; ゴットゥムッカラ，サバラジュ・ブイ; シー，チュアン; トス，ジョン・イー; ノーマン，ブライアン・エイチ; バスデバン，ベンカトラガバン; ペイテル，ビノッド・エフ; マルティネリ，マイケル・ジェイ; マンロー，ジョン・イー; ムーア，リチャード・イー; モーアー，エリック・ディ; レイ，ジェイムズ・イー |
| (57)【要約】 本発明は微小管系の崩壊に、抗新生物剤として、ならびにガンの処置に有用な新規クリプトフィシン化合物を提供する。 本発明はさらに新規クリプトフィシン化合物を投与するための製剤を提供する。 | ||||||
| 94 | Use of as a crystalline dibenzothiazepine derivatives and its anti-psychotic drugs | JP2000505140 | 1998-07-28 | JP2001512109A | 2001-08-21 | ウィリアム スネイプ エヴァン |
| (57)【要約】 結晶性１１−（４−［２−（２−ヒドロキシエトキシ）エチル］−１−ピペラジニル）−ジベンゾ［ｂ，ｆ］［１，４］チアゼピン（Ｉ）は、好ましくは水の不在下で非芳香族溶剤、例えばエチルアセテート、イソブチルアセテート、メチルイソブチルケトンまたはメチルｔ−ブチルエーテルから１１−（４−［２−（２−ヒドロキシエトキシ）エチル］−１−ピペラジニル）−ジベンゾ［ｂ，ｆ］［１，４］チアゼピンを晶出されることによって製造することができる。 製造された結晶性物質は製薬学的に認容性の塩、例えばフマル酸塩に変換されてもよい。 結晶性１１−（４−［２−（２−ヒドロキシエトキシ）エチル］−１−ピペラジニル）−ジベンゾ［ｂ，ｆ］［１，４］チアゼピンは、精神病の治療のために使用されることができる。 【化１】 | ||||||
| 95 | The novel 8-substituted-2-aminotetralins | JP50869890 | 1990-05-23 | JP2818692B2 | 1998-10-30 | アンデン，ニルス―エリーク; ヴアツルゴールダ，カール・イエルク; ハクセル，ウーリ・アルフ; バツクルンド・ヒヨーク，ベリツト・クリステイーナ・エリサベート; ビヨルク，アンナ・レーナ・マリア; ヒルヴエル，スヴエン―エリーク; ペルソン，エヴア・マリエ; メリン，エヴア・シヤーロツタ; ユイ，ホン; リウ，イエ |
| 96 | Dual action inhibitor | JP11587493 | 1993-05-18 | JPH0656790A | 1994-03-01 | DONARUDO ESU KARANEUSUKI; JIYOERU SHII BARITSUSHIYU; EDOWAADO DABURIYUU PETORIRO JI; JIEFURII EI ROBURU; DENISU II RIONO |
| PURPOSE: To obtain new compds. useful as dual inhibitors having inhibitory activity against angiotensin converting enzyme and neutral endopeptidase in the treatment of hypertension, congestive heart failure, hepatocirrhosis, etc. CONSTITUTION: The new compds. are compds. of formula I {R 1 is H, a group of formula II [R 3 is alkyl, aryl-(CH 2) m-[(m) is 0-6] or the like] or the like; R 2 and R 19 are each H, alkyl or the like; (n) is 0 or 1 but (n) is 0 when both R 2 and R 19 are other than H; and X 1 is a group of formula III or IV [Y 2 is CH 3, O or the like; (w) is 1 or 2; and R 12 is H, substd. alkyl or the like] or the like}, e.g. [S-(R*,R*)]-2,3,4,5-tetrahydro-3-[(2-mercapto-1-oxohexyl)amino]-2- oxo-1H-benzazepine-1-acetic acid. A compd. of the formula I (R 1 is a group of the formula II and R 19 is H) is obtd. by reacting an acylmercaptocarboxylic acid of formula V with an intermediate of the formula H-X 2 (R 2 in X 1 is an ester protecting group) and releasing the protecting group R 12 from the resultant product. COPYRIGHT: (C)1994,JPO | ||||||
| 97 | Composition to reduce risk of clot formation in diagnostic procedure | JP13484592 | 1992-05-27 | JPH05222011A | 1993-08-31 | RAMACHIYANDORAN ESU RANGANASAN; MAIKERU EFU TSUIIDORU; POORU DABURIYUU UEDEKINGU; RADAKURISHIYUNA PIRAI |
| PURPOSE: To provide the subject composition containing, as active component, anti-coagulant nonionic contrast agents, wherein some of the agents are new compounds, and having the ability to reduce the risk of clot formation in diagnostic procedures(in detail, X-ray impermeable compounds are needed in the diagnostic procedures). CONSTITUTION: The composition is comprised of (A) anti-coagulant nonionic contrast agents and (B) pharmaceutically acceptable carriers, wherein the compounds used as components of A are iodinated phenyl-compounds having a heterocyclic group, preferably the compounds having radical of formula I (the hetro cyclic group is formula II-VI; R, R' are H, alkyl, OH, alkoxy, hydroxyalkyl or alkoxyalkyl; X 1 is =N-CO-H, =N-CO-alkyl, S, or O; X 2 is X 1 or CH 2; (n) is 1-4, or (n) is 0-4 when X 2 is CH 2; (n) is 0-3; (s),(p) are each 2-5; (g), (r) are each 1 or 2) or its dimer, wherein some of the compounds mentioned above are new compounds. The compound of formula IV [R 1 is CONR 4R 6; R 2 is CONR 6R 7, etc.; R 4, R 5 are each H, CH 3, etc.; R 6, R 7 are each H, CH 2CH(OH)CH 2OH, etc.] in the compounds mentioned above are new compounds. COPYRIGHT: (C)1993,JPO | ||||||
| 98 | Cyclic renin inhibitor including 2-substituted(3s,4s)-4-amino-5-cycohexyl-3-hydroxy pentanoic acid, 2-substituted(3s,4s)-5-cyclohexyl-3,4-dihydroxypentanoic acid, 2-substituted(4s,5s)-5-amino 6-cyclohexyl-4-hydroxyhexanoic acid, or analogs thereof | JP41928890 | 1990-12-10 | JPH04217961A | 1992-08-07 | UIRIAMU JIEE GURIINRII; RARUFU EE RIBUERO; AN II UEBAA |
| PURPOSE: To provide new compounds which inhibit the angiotensinogen-cutting action of the natural proteolytic enzyme, renin. CONSTITUTION: This compound is represented by formula I [A is H, Het (Het is 5-7 membered monocyclic ring having one or two Ns, 7-10 membered bicyclic ring), aryl or the like; B is formula II-formula IV or the like; A together with my form formula V, formula VI (R 3 is H, alkyl, aryl or the like; R 11 is H, alkyl; Q is CO, SO 2; (r) and (m) are each 0-2) or the like; R 1 is alkyl, aryl, cycloalkyl, 5-6 membered saturated heterocycle; R 15 is alkyl, aryl, imidazol-4-yl, or the like; D is single bond, O, S, NH, CH=CH or the like; Z is NH 2, OH, OPO 3H 2, alkyl or the like; W is NR 23 (R 23 is H, alkyl; V is formula VII (Y is O, NH, absence, or the like; (x) and (y) are each 0-1; (z) is 0-4; R 5 is H, alkyl, aryl or the like; R 10 is H, OH, aryl or the like), SO 2NH 2 or the like]. The compound is effectively used for the medical treatments of hypertension, congestive heart failure or the like relating to renin. COPYRIGHT: (C)1992,JPO | ||||||
| 99 | 12-membered heterocyclic lactam derivative and 8-membered heterocyclic compound | JP31462990 | 1990-11-20 | JPH04187680A | 1992-07-06 | OISHI TAKESHI; OOTSUKA YASUHISA; IIMORI TAKAMASA; KOBAYASHI SHOGO; SETSUHARA KENICHI |
| NEW MATERIAL:Compounds of formula I [R is H, alkyl, aralkyl; R 2 is lower alkyl; X, Y are O, CH 2, NCO 2R 3 (R 3 is lower alkyl); n is 0, 1] and II (W is H, group of formula III). USE: An intermediate capable of being converted into medicines and agricultural chemicals or other useful physiologically active substances. PREPARATION: After the OH group of a compound of formula IV is, if necessary, changed into an active derivative group, the compound of formula IV is cyclized to prepare the compound of formula I wherein R 1 is H. COPYRIGHT: (C)1992,JPO&Japio | ||||||
| 100 | JPH04500362A - | JP50869890 | 1990-05-23 | JPH04500362A | 1992-01-23 | |
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