| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 21 | Substituted 1*111diaminoundecane*its manufacture and its use | JP13366779 | 1979-10-18 | JPS5555127A | 1980-04-22 | JIYOZEFU PAAIFUAA; DEIITERU RAINAA |
| 22 | 아지리딘으로부터 1,2-디아미노프로판 알코올을 제조하는방법 | KR1020000046394 | 2000-08-10 | KR1020000063913A | 2000-11-06 | 이원구; 신성호; 하현준 |
| PURPOSE: A manufacturing method of 1,2-diaminopropane alcohol from aziridine is provided. Thereby, 1,2-diaminopropane alcohol is produced in high yield of over 99% which is useful in synthesizing high value added precision product such as hydromethylpyperazine and D-threo-phenyl-2-decanoilamino-3-morpholino-1-propanol. CONSTITUTION: 1,2-diaminoalcohol derivative of formula (2) is prepared from aziridine of formula (1) wherein, R comprises hydrogen, alkyl, phenyl and propenyl. 2(R)-N-£(1S)-phenylethyl|amino-3-azido-1(R)-methylpropanol(1,2-diaminopropane alcohol) is prepared from aziridine by: dissolving 201mg of N-£(1S)-phenylethyl|aziridine-2(R)-£1(R)-methyl|methanol to methylenechloride, and adding 0.25ml of azidotrimethylic acid; shaking the compound for 12hrs at room temperature, and treating with 1N of hydrochloric acid; shaking for 1hr again; neutralizing the solution with sodium hydrogen carbonate, extracting twice with 5ml of methylenechloride; drying the organic layer with anhydrous magnesium sulfate; concentrating under decompression after filtering; refining to get 154g of objective material in the type of oil. | ||||||
| 23 | 입체 장애 아민 에테르의 제조 | KR1019990006156 | 1999-02-24 | KR1019990072904A | 1999-09-27 | 제다,알레산드로; 페리,지안루카; 사라,마씨밀라노 |
| 본 발명은 하기 화학식(2)의 화합물을 산화시키는 것을 특징으로 하는 하기 화학식(1)의 화합물의 제조방법에 관한 것이다:
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| 24 | 트리클로로니트로소메탄의 존재하에 시클로도데칸을 광화학 니트로소화시킴에 의한 라우릴락탐의 제조 방법 | KR1019970008784 | 1997-03-14 | KR1019970065515A | 1997-10-13 | 올리비에쟝 |
| 본 발명은 주제는 니트로소화제가 트리클로로니트로소메탄임을 특징으로 하고, 염산의 존재하에 시클로도데칸을 광화학 니트로소화시킴으로써 시클로도데카논 옥심을 제조하는 방법에 관한 것이다. | ||||||
| 25 | Epothilone derivatives | JP2007156260 | 2007-06-13 | JP4885067B2 | 2012-02-29 | グレゴリー・ディ・バイト; ジェイムズ・エイ・ジョンソン; スーン−フーン・キム; ロバート・エム・ボルジレリ |
| The present invention relates to compounds of the formula <CHEM> Q is selected from the group consisting of <CHEM> G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, <CHEM> W is O or NR15; X is O or H,H; Y is selected from the group consisting of O; H,OR16; OR17,OR17; NOR18; H,NOR19; H,NR20R21; H,H; or CHR22; OR17 OR17 can be a cyclic ketal; Z1, and Z2 are selected from the group consisting of CH2, O, NR23, S, or SO2, wherein only one of Z and Z2 is a heteroatom; B1 and B2 are selected from the group consisting of OR24, or OCOR25, or O2CNR26R27; when B1 is H and Y is OH, H they can form a six-membered ring ketal or acetal; D is selected from the group consisting of NR28R29, NR30COR31 or saturated heterocycle R1, R2, R3, R4, R5, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26, and R27 are selected from the group H, alkyl, substituted alkyl, or aryl and when R1 and R2 are alkyl can be joined to form a cycloalkyl; R3 and R4 are alkyl can be joined to form a cycloalkyl; R9, R10, R16, R17, R24, R25, and R31 are selected from the group H, alkyl, or substituted alkyl; R8, R11, R12, R28, R30, R32, R33, and R30 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R15, R23 and R29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R32C=O, R33SO2, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein W and X are both O; and R1, R2, R7, are H; and R3, R4, R6, are methyl; and R8, is H or methyl; and Z1, and Z2, are CH2; and G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and Q is as defined above are excluded. | ||||||
| 26 | Lipophilic derivative of the chelating mono amide | JP2007527646 | 2005-06-07 | JP2008502726A | 2008-01-31 | ウィリアム ディー． マギー; デニス パトリック リリー |
| 磁気共鳴画像を得るための、ナノ粒子または微粒子乳剤と結合するのに有用な化合物は、シグナルの緩和度の制御を可能にし、粒子成分と容易に結合する。 この化合物はキレート化部分のアキラル誘導体から都合よく調製される。 | ||||||
| 27 | Neuroprotective macrocyclic compounds and methods of use thereof | JP2006507261 | 2004-03-16 | JP2006523213A | 2006-10-12 | ポール ダブリュ アール ハリス; マーガレット アン ブリンブル |
| 本発明の実施態様は巨大環を含む新規ペプチドミメティックスを提供する。 このような化合物は神経保護性であり、神経細胞変性及び／又は死滅を特徴とする疾患、障害及びその他の症状の治療のための治療薬としての実用性を有する。 また、これらの化合物はこのような症状の治療に有益な薬物の製造に有益である。 | ||||||
| 28 | Epothilone derivatives | JP50867399 | 1998-06-16 | JP2002512634A | 2002-04-23 | キム，スーン−フーン; ジョンソン，ジェイムズ・エイ; バイト，グレゴリー・ディ; ボルジレリ，ロバート・エム |
| The present invention relates to compounds of the formula <CHEM> Q is selected from the group consisting of <CHEM> G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, <CHEM> W is O or NR15; X is O or H,H; Y is selected from the group consisting of O; H,OR16; OR17,OR17; NOR18; H,NOR19; H,NR20R21; H,H; or CHR22; OR17 OR17 can be a cyclic ketal; Z1, and Z2 are selected from the group consisting of CH2, O, NR23, S, or SO2, wherein only one of Z and Z2 is a heteroatom; B1 and B2 are selected from the group consisting of OR24, or OCOR25, or O2CNR26R27; when B1 is H and Y is OH, H they can form a six-membered ring ketal or acetal; D is selected from the group consisting of NR28R29, NR30COR31 or saturated heterocycle R1, R2, R3, R4, R5, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26, and R27 are selected from the group H, alkyl, substituted alkyl, or aryl and when R1 and R2 are alkyl can be joined to form a cycloalkyl; R3 and R4 are alkyl can be joined to form a cycloalkyl; R9, R10, R16, R17, R24, R25, and R31 are selected from the group H, alkyl, or substituted alkyl; R8, R11, R12, R28, R30, R32, R33, and R30 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R15, R23 and R29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R32C=O, R33SO2, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein W and X are both O; and R1, R2, R7, are H; and R3, R4, R6, are methyl; and R8, is H or methyl; and Z1, and Z2, are CH2; and G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and Q is as defined above are excluded. | ||||||
| 29 | Protease inhibitor of retrovirus | JP34250893 | 1993-12-14 | JPH07330733A | 1995-12-19 | MAIKERU PIITAA TOROBA; ROBAATO II BABIN; NAN TSUANGU; SUCHIIBUN AARU SHIYOU; ARAN UIZUNAA |
| PURPOSE: To obtain a novel compound that is an inhibitor of HIV retrovirus protease and useful in the treatment of AIDS. CONSTITUTION: This compound is represented by formula I [Z is a single bond, O, NH; X is hydroxyl and Y is H, -CH 2OH, X and Y together form an epoxide-(CH 2O); R 1 is H, a 1-7C alkyl; R 2 is H, OH or the like; R 3 is formula II (R 6 is an alkyl; R 7 is H, an alkyl; R 8 is H, an alkyl); R 4 is a Q-1-7C alkyl (Q is O, a single bond); R 5 is formula II; (a), (b), (c) are each 0-3], typically [S-(R*,R*)]-[2-methylbutyl-1-[[(2-pyridinylmethyl)amino]carbonyl]butyl]carbamic 1,1-dimethyl ester. The compound of formula I is prepared by oxidizing a compound of formula III with osmium tetroxide. COPYRIGHT: (C)1995,JPO | ||||||
| 30 | Polycyclic amine compound, its enantiomer, its preparation and pharmaceutic composition containing those | JP11382092 | 1992-05-06 | JPH05186425A | 1993-07-27 | ZABIE EMON ARUTO; PATORITSUKU GEERU; BANSANTSUO PUROIETSUTO; PIEERU GUURAUITSUKU |
| PURPOSE: To provide a new polycyclicamine compd. which has pharmaceutically floating properties like a neurokinin receptor antagonist and is useful for the treatment for substance P-dependent and neurokinin-dependent pathological conditions. CONSTITUTION: The compd. is expressed by formula I, wherein Y is Cy-N, Cy-CH 2-N, Ar-(CH 2) x-CX (Cy is phenyl, cycloalkyl, etc., which may have substituents; Ar is phenyl, pyridyl, etc., which may have substituents; (x) is 0 or 1; X is H, OH, alkoxy, acyloxy, CN, etc.); (m) is 2, 3; Ar' is phenyl, thienyl, naphthyl, etc., which may have substituents; (n) is 0 to 3; (p) is 1, 2; Q is 0 or two H; T is CO, CH 2; (q) is 0 to 3; Z is phenyl or naphthyl which may have substituents, or pyridinyl, indolyl, etc. The compd. is, form example, 5-[2-(4- benzylpiperidin-1-yl)ethyl]-5-(3,4-dichlorophenyl)-1-benzylpiperidinone salt. The compd. of formula I with T being CO is obtd. by the reaction of a compd. expressed by formula I and a compd. expressed by formula III. COPYRIGHT: (C)1993,JPO | ||||||
| 31 | Koshuyozai | JP18923881 | 1981-11-27 | JPH0227328B2 | 1990-06-15 | OOTAKE NOZOMI; SETO HARUO; SASAKI TETSUO; SUGITA MASANORI; NATORI YOHEI |
| 32 | JPS6021993B2 - | JP11049273 | 1973-10-03 | JPS6021993B2 | 1985-05-30 | FUJIMOTO YASUO; NAKANO KINICHI; URAKAWA CHIKAHIRO |
| 33 | Compound analogous to macbecin and its preparation | JP9671182 | 1982-06-04 | JPS58212793A | 1983-12-10 | MUROI MASAYUKI; TANIDA SEIICHI; HASEGAWA TOORU |
| PURPOSE:To prepare a compound analogous to macbecin, a novel antibiotic showing activity against Gram-positive bacteria, fungi, and protozoans, by cultivating a microorganism belonging to the genus Actinosynnema. CONSTITUTION:A microorganism such as Actinosynnema sp.No.C-33196 strain (FERM-P 166) belonging to the genus Actinosynnema, capable of producing a compound analogous to macbecin, is innoculated into a medium, cultivated under aerobic conditions at about 6.5-7.5 pH at about 20-32 deg.C for about 48-96hrs, and antibiotic C-33196E-6, E-6-R, E-7, or E-7-R shown by the formula (one of R1, R2, and R3 is methyl, the other two are H; X is 2,5-dioxo-3,6-cyclohexadiene-1,3- diyl, 2,5-dihydroxy-1,3-phenylene) or their mixture is collected from the culture. | ||||||
| 34 | Novel antitumor substance and its preparation | JP18923881 | 1981-11-27 | JPS5892662A | 1983-06-02 | OOTAKE NOZOMI; SETO HARUO; SASAKI TETSUO; SUGITA MASANORI; NATORI YOHEI |
| NEW MATERIAL:T-23-ISubstance shown by the formulaI. Appearance and properties: amorphous yellowish powder. Specific rotatory power[α]D: 91.8 (CHCl 3, C=1.0%). Melting point: 117°C (decomposition). Solubility in solvent: easily soluble in CHCl 3, CH 3OH, C 2H 5OH, (CH 3) 2O and ethyl acetate, slightly soluble in benzene and ether, insoluble in water, petroleum ether, and hexane. USE: Especially hopeful as an antitumor agent. PROCESS: T-23-II Substance shown by the formula II, a fermentation product of Streptomyces rishiriensis T-23 strain (FERM-P 6141) of a novel strain belonging to the genus Streptomyces rishiriensis, is oxidezed to give a compouns shown by the formulaIchemically easily. COPYRIGHT: (C)1983,JPO&Japio | ||||||
| 35 | JPS511719B1 - | JP6571674 | 1974-06-10 | JPS511719B1 | 1976-01-20 | |
| 36 | JPS511718B1 - | JP6571574 | 1974-06-10 | JPS511718B1 | 1976-01-20 | |
| 37 | Novel ansamycin derivatives and the method for mutational biosynthesis thereof | KR20090008002 | 2009-02-02 | KR20100088869A | 2010-08-11 | LEE HONG SUB; PARK JOON TAE; HONG SOO JUNG; MOON AN NA; KANG JAE HOON; HONG YOUNG SOO; HWANG BANG YEON; LEE DONG HO |
| PURPOSE: A method for preparing novel ansamycin derivative using 3-amino-5-hydroxybenzoic acid(AHBA) biosynthesis gene mutant strain is provided. CONSTITUTION: A non-quinone geldamycin derivative, 17-hydroxy-17-demethoxy-18,21-deketone-geldanamycin(ID-6203) is denoted by chemical formula. The compound is produced by Streptomyces hygriscopicus AC2(deposit number: KCTC 10676BP). The mutated Streptomyces hygriscopicus AC2 is a strain in which AHBA biosynthesis gene is deleted. An anticancer drug contains the non-quinone geldamycin derivative compound as an active ingredient. | ||||||
| 38 | 입체 장애 아민 에테르의 제조 | KR1019990006156 | 1999-02-24 | KR100561146B1 | 2006-03-15 | 제다,알레산드로; 페리,지안루카; 사라,마씨밀라노 |
| 본 발명은 하기 화학식(2)의 화합물을 산화시키는 것을 특징으로 하는 하기 화학식(1)의 화합물의 제조방법에 관한 것이다:
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| 39 | 트리클로로니트로소메탄의 존재하에 시클로도데칸을 광화학 니트로소화시킴에 의한 라우릴락탐의 제조 방법 | KR1019970008784 | 1997-03-14 | KR100204133B1 | 1999-06-15 | 올리비에쟝 |
| 본 발명의 주체는 니트로소화제가 트리클로로니트로소메탄임을 특징으로 하고, 염산의 존재하에 시클로도데칸을 광화학 니트로소화시킴으로써 시클로도데스카논 옥심을 제조하는 방법에 관한 것이다. | ||||||
| 40 | Epothilone derivatives | JP50867399 | 1998-06-16 | JP4090514B2 | 2008-05-28 | キム，スーン−フーン; ジョンソン，ジェイムズ・エイ; バイト，グレゴリー・ディ; ボルジレリ，ロバート・エム |
| The present invention relates to compounds of the formula <CHEM> Q is selected from the group consisting of <CHEM> G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, <CHEM> W is O or NR15; X is O or H,H; Y is selected from the group consisting of O; H,OR16; OR17,OR17; NOR18; H,NOR19; H,NR20R21; H,H; or CHR22; OR17 OR17 can be a cyclic ketal; Z1, and Z2 are selected from the group consisting of CH2, O, NR23, S, or SO2, wherein only one of Z and Z2 is a heteroatom; B1 and B2 are selected from the group consisting of OR24, or OCOR25, or O2CNR26R27; when B1 is H and Y is OH, H they can form a six-membered ring ketal or acetal; D is selected from the group consisting of NR28R29, NR30COR31 or saturated heterocycle R1, R2, R3, R4, R5, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26, and R27 are selected from the group H, alkyl, substituted alkyl, or aryl and when R1 and R2 are alkyl can be joined to form a cycloalkyl; R3 and R4 are alkyl can be joined to form a cycloalkyl; R9, R10, R16, R17, R24, R25, and R31 are selected from the group H, alkyl, or substituted alkyl; R8, R11, R12, R28, R30, R32, R33, and R30 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R15, R23 and R29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R32C=O, R33SO2, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein W and X are both O; and R1, R2, R7, are H; and R3, R4, R6, are methyl; and R8, is H or methyl; and Z1, and Z2, are CH2; and G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and Q is as defined above are excluded. | ||||||
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