| 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 | STEREOSELECTIVE RING OPENING REACTIONS | PCT/US1999/018305 | 1999-08-13 | WO00009463A1 | 2000-02-24 | |
| The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile, selected from the group consisting of water, alcohols, carboxylic acids, and thiols, and a racemic or diastereomeric mixture of a cyclic substrate in the presence of a non-racemic, chiral catalyst to effect a kinetic resolution of the cyclic substrate. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides. | ||||||
| 62 | The combination of cholesterol biosynthesis inhibitors and β- lactam cholesterol absorption inhibitor | JP51530594 | 1993-12-21 | JP3992728B2 | 2007-10-17 | デイヴィス，ハリー・アール |
| PCT No. PCT/US93/12291 Sec. 371 Date Jun. 20, 1995 Sec. 102(e) Date Jun. 20, 1995 PCT Filed Dec. 21, 1993 PCT Pub. No. WO94/14433 PCT Pub. Date Jul. 7, 1994Methods of reducing plasma cholesterol levels and treating or preventing atherosclerosis comprising administering an effective amount of a combination of a cholesterol biosynthesis inhibitor and a beta -lactam cholesterol absorption inhibitor, as well as pharmaceutical compositions and kits useful in those methods, are disclosed. | ||||||
| 63 | Stereoselective ring-opening reaction | JP2000564918 | 1999-08-13 | JP2002522515A | 2002-07-23 | エヌ ジャコブソン，エリック; エフ ラーロー，ジェイ; 信 徳永 |
| (57)【要約】 本発明は、概して、水、アルコール、カルボン酸、およびチオールからなる群より選択される求核体、および環状基質のラセミまたはジアステレオ混合物を非ラセミキラル触媒の存在下で反応させて、該環状基質の速度論的分割を行う工程を含む、立体選択的またはレジオ選択的化学合成方法に関する。 本発明はまた、エポキシドのラセミおよびジアステレオ混合物の加水分解速度論的分割にも関する。 | ||||||
| 64 | Production of nitrogen-containing bicyclic compound | JP13469796 | 1996-05-29 | JPH08311061A | 1996-11-26 | TAUNREE PII KARUBAATOSON; JIYON EMU DOOMAGARA; TOMASU EFU MITSUKU; JIEFURII BII NIKORUSU |
| PROBLEM TO BE SOLVED: To obtain the subject compound having antibacterial activity and useful as a therapeutic agent for bacterial infectious diseases. SOLUTION: (A) A compound of formula I (X is CH, CCl, CF or CO-1-3C alkyl; Y is F; R 1 is H, a 1-6C alkyl or cation; R 2 is a 1-4C alkyl or 3-6C cycloalkyl; L is an eliminable group) is reacted with (B) an amine of the formula Z-H (Z is a group of formula II or formula III; R 3 is H, a 1-4C alkyl or 3-6C cycloalkyl; R 4 is H, a 1-4C alkyl, 2-4C hydroxyalkyl, trifluoroethyl or the like; R 5 is H or a 1-3C alkyl; R 6 is H or a 1-3C alkyl) to obtain (C) the objective compound of formula IV. One of the compounds of formula IV, e.g. 7-[3-(aminomethyl)-1-pyrrolidinyl]-1-ethyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acid, is obtained by reaction between 6,7-difluoro-1-ethyl-1,4- dihyciro-4-oxc-3-quinolinecarboxylic acid and 3-pyrrolidinemethanamine. COPYRIGHT: (C)1996,JPO | ||||||
| 65 | The combination of cholesterol biosynthesis inhibitors and β- lactam cholesterol absorption inhibitor | JP51530594 | 1993-12-21 | JPH08505141A | 1996-06-04 | デイヴィス，ハリー・アール |
| PCT No. PCT/US93/12291 Sec. 371 Date Jun. 20, 1995 Sec. 102(e) Date Jun. 20, 1995 PCT Filed Dec. 21, 1993 PCT Pub. No. WO94/14433 PCT Pub. Date Jul. 7, 1994Methods of reducing plasma cholesterol levels and treating or preventing atherosclerosis comprising administering an effective amount of a combination of a cholesterol biosynthesis inhibitor and a beta -lactam cholesterol absorption inhibitor, as well as pharmaceutical compositions and kits useful in those methods, are disclosed. | ||||||
| 66 | Radiosensitizer | JP3449985 | 1985-02-25 | JPH07103027B2 | 1995-11-08 | 豊 中原; 凌治 木村; 恒雄 椿本; 源信 皆川; 勤 鍵谷; 公一 阪野; 量一 鴛海 |
| 67 | Intermediates useful in the preparation of nitrogen-Motoo ring compound | JP5358791 | 1991-02-27 | JPH0662561B2 | 1994-08-17 | ジエフリー・ビー・ニコルス; ジヨン・エム・ドーマガラ; タウンレー・ピー・カルバートソン; トマス・エフ・ミツク |
| 68 | The novel β- lactam compound | JP12311785 | 1985-06-06 | JPH0635432B2 | 1994-05-11 | SUNAKAWA JUN; MATSUMURA HARUKI; SETA AKINORI; SASAKI AKIRA |
| 69 | JPH0533717B2 - | JP19982884 | 1984-09-25 | JPH0533717B2 | 1993-05-20 | YOSHIDA MAKOTO; TAMURA TOSHA; IWAMOTO HIDENORI; TSUKAMOTO SHINICHI; YAMAMOTO MINORU; KAGAMI SOICHI |
| 70 | JPH0451555B2 - | JP6866385 | 1985-04-01 | JPH0451555B2 | 1992-08-19 | NIWA TATSUSHI; KATAGIRI SHINYA; KATO TETSUZO; SHIDORI YOSHASU |
| 71 | JPH041749B2 - | JP22035483 | 1983-11-21 | JPH041749B2 | 1992-01-14 | MATSUMURA KYOTOSHI; KYOKAWA HIROSHI; SUZUKI DAISUKE; SHIMABAYASHI AKIHIRO; YONEMOTO YOSHIMASA |
| 72 | Optically active beta-lactam | JP19119786 | 1986-08-16 | JPS6348274A | 1988-02-29 | YOSHIOKA TAKEO; FUKAGAWA YASUO; ISHIKURA TOMOYUKI |
| NEW MATERIAL:An optically active β-lactam compound of formula I or formula II [R 1 is alkyl or aralkyl; R 2 is COOR 5 (R 5 is alkyl or aralkyl) or SO 2R 6 (R 6 is alkyl or aryl); R 3 and R 4 are H, alkyl, cycloalkyl, aryl or aralkyl or R 3 and R 4 together form an alkylene; Z is H or amino-protecting group]. EXAMPLE: (3R, 4R)-4-[(1S)-1,2-dihydroxy-1,2-o-isopropylidene]ethyl-3-(N-methoxy carbonyl-N-methyl)amino-1-(4-methoxy)phenyl-2-azetidinone. USE: A production intermediate for a novel 6-disubstituted aminocarbapenem antibiotic substance. PREPARATION: The compound of formula I or formula II can be produced e.g. by reacting a reactive derivative of glycine derivative of formula III with a compound of formula IV or formula V. COPYRIGHT: (C)1988,JPO&Japio | ||||||
| 73 | Tetrahydrofurancarboxylic acid derivative and production thereof | JP24263586 | 1986-10-13 | JPS62201886A | 1987-09-05 | TAMURA NORIKAZU; KAWANO YASUHIKO; YOSHIOKA KOICHI |
| NEW MATERIAL:A compound expressed by formula I (R<1> is amino or organic residue through N; R<2> is H, lower alkoxy or formylamino; R<3> and R<4> are H or organic residue; R<5> is COOH or a group derived therefrom; X is chemical bond, O or the formula >N-R<6> (R<6> is lower alkyl)] or salt thereof. EXAMPLE:4-Nitrobenzyl 2-[(3S,4S)-4-acetoxy-3-benzyloxycarbonylamino-2-oxo-1- azetidinyl]-5-oxo-2-tetrahydrofurancarboxylate. USE:A low toxic antimicrobial agent against Gram-positive and Gram-negative bacteria. PREPARATION:A compound expressed by formula II (R<1>' is organic residue through N; X' is H, OH or -NHR<6>) is reacted with a compound expressed by formula III (R<5>' is a group derived from COOH) or a compound expressed by formula IV (Y is eliminative group). | ||||||
| 74 | Beta-lactame derivative | JP23986 | 1986-01-07 | JPS62158277A | 1987-07-14 | TERAJIMA ATSURO; ITO YOSHIO; KIMURA YOSHIICHI; SAKAI KUNIKAZU; HIYAMA TAMEJIROU |
| NEW MATERIAL:A compound of formula I (R is protecting group for hydroxyl). EXAMPLE: (1'R,3S,4R)-3-1'-(t-Butyldimethylsilyloxy)ethyl-4-1"-(tiazolid ine-2-thione- 3-carbonyl)ethyl-azetidine-2-one. USE: A synthetic intermediate of 1β-methylcarbapenem which discloses excellent antibacterial action. PREPARATION: The reaction of 4-acetoxy-β-lactame derivative of formula II with 3-propionylthiazolidine-2-thione tin(II) enolate stereospecifically gives the compound of formula I. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 75 | Heterocyclic compound, manufacture and insecticidal and nematodicidal drug | JP29357886 | 1986-12-11 | JPS62153270A | 1987-07-08 | MAIKERU DORAISUDERU TAANBOORU; AIAN TOREBOAA KEI |
| 76 | Azetidinone derivative | JP22728085 | 1985-10-12 | JPS6287563A | 1987-04-22 | KAWASHIMA YUTAKA; SATO MASAKAZU; HATADA YUICHI; HASATO IKUKO; NAKAJIMA YOSHIMOTO; SODA KAORU |
| NEW MATERIAL:The compound of formula I (R is phenyl, substituted phenyl, lower alkyl, cycloalkyl or 3-pyridyl; wavy line represents E- or Z-configuration). EXAMPLE:(E)-4-methyl-3-(2-hydroxyiminopropylidene)-1-phenyl-2-azetidin one. USE:Platelet coagulation inhibitor. PREPARATION:The compound of formula I can be produced by the hydroxylamination of a novel compound of formula II with e.g. hydroxylamine hydrochloride. | ||||||
| 77 | Enantioselective manufacture of 1-beta-methylcarbapenem antibiotic intermediate | JP6983986 | 1986-03-29 | JPS61275267A | 1986-12-05 | SHINKAI ICHIRO; TOOMASU ENU ZARUTSUMAN; RERIA EMU FUENTESU |
| 78 | 3-aryloxyazetidinecarboxamide-containing composition as muscle relaxant and antianxiety | JP4390686 | 1986-02-28 | JPS61205254A | 1986-09-11 | CHIYANDORAA ROI TEIRAA JIYUNIA; ARUBAATO DANKAN KEERU JIYUNIAA; DEEBITSUDO NOOSHIIN JIYONSON; HARORUDO FUITSUSHIYAA SUTOUFUA |
| 79 | Novel4-oxo-2-azetidinecarboxylic acid derivative | JP19982884 | 1984-09-25 | JPS6178786A | 1986-04-22 | YOSHIDA MAKOTO; TAMURA TOSHIYA; IWAMOTO HIDENORI; TSUKAMOTO SHINICHI; YAMAMOTO MINORU; KAGAMI SOICHI |
| NEW MATERIAL:A compound shown by the formula I [R<1> and R<2> are lower alkyl; R<3> is imidazolyl shown by the formula II or formula III (R<4> is H, or lower alkyl); Y is OH, lower alkoxy, amino, etc.] and its salt. EXAMPLE:N<alpha>-[(S)-3,3-Dimethyl-4-oxo-2-acetidinylcarbonyl]--L- histidyl-L-prolin amide. USE:An improver for disturbance of consciousness in schizophrenia, depression, etc., an improver for hypobulia, dejection, etc. PREPARATION:For example, a compound shown by the formula (V and a compound shown by the formula V as starting raw materials are reacted, the prepared intermediate and a compound shown by the formula VI are subjected to peptide synthesis reaction preferably by azide method. | ||||||
| 80 | 1,3-substituted-2-imidazolidinone derivative, agent for promoting gastroenteric movement, and its preparation | JP15384484 | 1984-07-24 | JPS6133172A | 1986-02-17 | TOMIYAMA TAKESHI; TOMIYAMA ITARU |
| NEW MATERIAL:The 1,3-substituted-2-imidazolidinone derivative of formula I [A is formula II W formula V (R 1 is H or Cl; R 2 and R 3 are Cl, CH 3 or CH 3O); B is di-lower alkylamino, substituted azetidyl, pyrrolidino, piperazino, piperidyl or morpholino; n is 0 or 1; m is 2 or 3] and its pharmacologically permissible acid addition salt. EXAMPLE: 1-(5-Chloropyridin-2-yl)-3-(2-pyrrolidinoethyl)-2-imidazolidinone. USE: Agent for promoting the gastroenteric movement. PREPARATION: The compound of formula I can be prepared by reacting the compound of formula VI [Y is A-(CH 2)n or B-(CH 2)n] with the compound of formula X-Z [X is halogen; when Y is A-(CH 2)n, then Z is B-(CH 2)m, and when Y is B-(CH 2)m, Z is A-(CH 2)n]. COPYRIGHT: (C)1986,JPO&Japio | ||||||
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