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61. 发明专利

JPS6354321A BLOOD SUGAR LOWERING AGENT 失效
公开(公告)号：JPS6354321A
公开(公告)日：1988-03-08
申请号：JP6183386
申请日：1986-03-19
申请人： AJINOMOTO KK
发明人： TOYOSHIMA SHIGERU , SETO YOSHIKO , SHINKAI HISASHI , TOI KOUJI , KUMASHIRO IZUMI
IPC分类号： A61K31/455 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/22 , A61K31/33 , A61K31/365 , A61K31/4406 , A61K31/4409 , A61P3/08 , A61P3/10 , C07C67/00 , C07C231/00 , C07C233/47 , C07C233/63 , C07C233/81 , C07C233/82 , C07C235/12 , C07C235/40 , C07D213/82 , C07D307/84 , C07D307/85 , C07D307/88 , C07D521/00
摘要： PURPOSE:To obtain a blood sugar lowering agent useful as a remedy for diabetes, capable of being orally administrated, having low side effects, comprising a D-phenylalanine derivative including a novel compound. CONSTITUTION:A blood sugar lowering agent containing a compound shown by formula I [R is H, 1-5C alkyl, 6-12C aryl, 6-12C aralkyl, group shown by formula II, CH2CO2R , CH(CH3)-OCO-R or CH2-OCO-C(CH3); R is aryl, heterocyclic 6-membered group, heterocyclic 5-membered group, cycloalkyl or cycloalkenyl which main contain substituent group; R is H or lower alkyl], a salt thereof or a derivative which can be converted into the compound in human or animal body, such as N-(4-toluyl)-D-phenylalanine, as an active ingredi ent. A dose of the compound is generally 0.1-1,000mg per adult and 0.2-2,000mg is administered daily several times dividedly.

62. 发明专利

JPS62242653A PRODUCTION OF 5-HYDROXYNORVALINE DERIVATIVE 失效
公开(公告)号：JPS62242653A
公开(公告)日：1987-10-23
申请号：JP8604986
申请日：1986-04-16
申请人： KOHJIN CO
发明人： SATO TADASHI
IPC分类号： C07C271/22 , C07C67/00 , C07C231/00 , C07C231/12 , C07C233/46 , C07C233/47 , C07C233/82 , C07C239/00 , C07C301/00 , C07C303/40 , C07C311/19
摘要： PURPOSE:To obtain a compound useful as an intermediate for synthesizing proline, by reducing an N-substituted glutamic acid 5-ester with sodium boron hydride which is inexpensive, readily handleable, usable in an aqueous system has easy reaction operation. CONSTITUTION:A compound shown by formula I (R is benzoyl, benzyloxycarbonyl, tolysulfonyl or acetyl; R' is methyl or ethyl) is reduced with sodium boron hydride in a solvent such as water, alcohol, etc., at -10 deg.C - room temperature for 1 - 5hr to give the aimed substance shown by formula II. The reaction is carried out by using a little excess molar amount based on the compound shown by the formula I of sodium boron hydride.

63. 发明专利

JPS6136747B2 失效
公开(公告)号：JPS6136747B2
公开(公告)日：1986-08-20
申请号：JP3894079
申请日：1979-03-30
申请人： TANABE SEIYAKU CO
发明人： SENHATA ICHIRO , YAMADA SHIGEKI , PPONGO CHIKARA
IPC分类号： C07D207/16 , B01J31/00 , B01J31/04 , C07B31/00 , C07B57/00 , C07B61/00 , C07C67/00 , C07C231/00 , C07C231/18 , C07C231/20 , C07C233/47 , C07C233/82

64. 发明专利

JPS59212744A Shift reagent for nmr 失效
标题翻译： NMR转移试剂
公开(公告)号：JPS59212744A
公开(公告)日：1984-12-01
申请号：JP8864983
申请日：1983-05-19
申请人： Sumitomo Chem Co Ltd
发明人： OOI TAKAFUMI , TAKAI RIYOUZOU , KITAHARA HAJIME , YAMAMOTO SEIYA , MORIGUCHI KOUICHI
IPC分类号： C07C69/007 , C07C67/00 , C07C227/00 , C07C231/00 , C07C233/05 , C07C233/07 , C07C233/46 , C07C233/65 , C07C233/82 , C07C235/06 , C07C235/16 , C07C237/22 , G01R33/28 , G01N24/02
CPC分类号： G01R33/281
摘要： PURPOSE:To obtain a titled reagent having a good performance which is easy to synthesize and use by using specific derivatives of carboxylic acid ester or amide which are optically active as a shift reagent for nuclear magnetic resonance spectrometry. CONSTITUTION:The optically active compds. shown in the formulas I , II, and III[R1 is alkyl, haloalkyl, alkylamine, or arylamino, R2 is alkyl, R3 is (substitution) phenyl or naphthyl, X is O or -NH-, * is asymmetric carbon, R4 is alkyl, aralkyl, or aryl, Y is same as X, R5 is alkyl or aryl] are used as the shift reagent for NMR. The compds. of the formulas I -III are easy to synthesize with high separative power in the NMR analysis of an enantiomer of an asymmetric compd. When an enantiomer to be separated has amido groups coupled to 3,5-dinitrophenyl group and an asymmetric carbon, R1 of the compds. of the formulas I and II may preferably be CH3 or CF3.
摘要翻译：目的：通过使用光学活性的羧酸酯或酰胺的特定衍生物作为核磁共振光谱法的转移试剂，获得具有良好性能的易于合成和使用的标题试剂。构成：光学活性物质如式I，II和III所示[R1为烷基，卤代烷基，烷基胺或芳基氨基，R2为烷基，R3为（取代）苯基或萘基，X为O或-NH-，*为不对称碳，R4为烷基，芳烷基或芳基，Y与X相同，R 5为烷基或芳基]用作NMR的转移试剂。杂技在不对称化合物的对映异构体的NMR分析中，式I-III易于以高分离能力合成。当待分离的对映体具有与3,5-二硝基苯基和不对称碳偶联的酰胺基时，该化合物的R1。式I和II可优选为CH 3或CF 3。

65. 发明专利

JPS5718651A PREPARATION OF PHENYLGLYCINE DERIVATIVE 失效
公开(公告)号：JPS5718651A
公开(公告)日：1982-01-30
申请号：JP9262580
申请日：1980-07-09
申请人： NIPPON KAYAKU KK
发明人： NISHIZAWA RINZOU , SUGIMURA HIDEO
IPC分类号： C07C271/22 , C07C67/00 , C07C227/00 , C07C227/18 , C07C227/20 , C07C229/36 , C07C231/00 , C07C231/12 , C07C233/47 , C07C233/80 , C07C233/82 , C07C239/00 , C07C271/26 , C07C301/00 , C07C303/40 , C07C311/19
摘要： PURPOSE:To obtain the titled compound useful as an intermediate for a medicine readily in high yield, by decarboxylating an N-protected 4-(1-carboxy-1-hydroxymethyl)-3-hydroxyphenylglycine oxidatively, and removing the protecting group from the resultant decarboxylated compound. CONSTITUTION:An N-protected 4-(1-carboxy-1-hydroxymethyl)-3-hydroxyphenylglycine, e.g. N-formy-4-(1-carboxyl-1-hydroxymethyl)-3-hydroxyphenylglycine, of formula I (R1 is protecting group of the amino group) is decarboxylated oxidatively in a solvent, e.g. acetone or methanol, and the protecting group of the decarboxylated compound is removed to give the aimed substance of formula II. The novel starting compound of formula I is obtained by reacting an n-protected 3- hydroxyphenylglycine of formula III with glyoxylic acid. USE:Useful as a synthetic intermediate for Forphenicine , penicillin derivatives, cephalosporin derivatives, etc.

66. 发明专利

JPS50116442A 失效
公开(公告)号：JPS50116442A
公开(公告)日：1975-09-11
申请号：JP1328575
申请日：1975-01-31
IPC分类号： C07D295/18 , A61K31/165 , A61K31/395 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/81 , C07C233/82 , C07C235/52 , C07C237/20 , C07C237/22 , C07D295/08 , C07D295/092 , C07D295/185 , C07D295/192

67. 发明专利

JPS50116441A 失效
公开(公告)号：JPS50116441A
公开(公告)日：1975-09-11
申请号：JP1326675
申请日：1975-01-31
IPC分类号： C07D295/18 , A61K31/165 , A61K31/395 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/81 , C07C233/82 , C07C235/52 , C07C237/20 , C07C237/22 , C07D295/08 , C07D295/092 , C07D295/185 , C07D295/192

68. 发明专利

JPS4868543A 失效
公开(公告)号：JPS4868543A
公开(公告)日：1973-09-18
申请号：JP12705772
申请日：1972-12-18
IPC分类号： C07C231/20 , C07C20060101 , C07C233/82

69. 发明授权

US06878718B2 Phenylalanine enamide derivatives 失效
标题翻译：苯丙氨酸烯酰胺衍生物
公开(公告)号：US06878718B2
公开(公告)日：2005-04-12
申请号：US10081072
申请日：2002-02-22
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： A61K31/198 , A61K31/4375 , A61K31/44 , A61K31/4406 , A61K31/497 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07C229/34 , C07C229/46 , C07C233/82 , C07C321/22 , C07C323/30 , C07D213/81 , C07D213/89 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R 1是Ar 1 Ar 2 Ar 2 AlK-，其中：Ar 1是任选取代的芳族或杂芳族基团; 2>是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或杂亚芳基; Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中 R是羧酸（-CO 2 H）或其衍生物或生物试剂; X是-O-或-S-原子或-N（R 2） - 基团，其中：R x，R y，和R a可以相同或不同，各自为氢原子或任选的取代基;或R z为前述定义的原子或基团，R x和R y连接在一起形成任选取代的螺环连接的脂环族或杂环脂族基团;及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病或涉及其中的疾病细胞的适当生长或迁移。

70. 发明授权

US5973160A Methods for the preparation of novel sidechain-bearing taxanes 失效
标题翻译：制备新型侧链紫杉烷的方法
公开(公告)号：US5973160A
公开(公告)日：1999-10-26
申请号：US600787
申请日：1996-02-13
申请人： Michael A. Poss , Jerome L. Moniot , Ivan D. Trifunovich , David J. Kucera , John K. Thottahil , Shu-Hui Chen , Jianmei Wei
发明人： Michael A. Poss , Jerome L. Moniot , Ivan D. Trifunovich , David J. Kucera , John K. Thottahil , Shu-Hui Chen , Jianmei Wei
IPC分类号： C07C233/82 , C07C271/22 , C07D305/14 , C07D407/12 , C07D409/12 , C07D413/12
CPC分类号： C07D407/12 , C07C233/82 , C07C271/22 , C07D305/14 , C07D409/12 , C07D413/12
摘要： Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.
摘要翻译：用于制备侧链紫杉烷的新方法，包括制备恶唑啉化合物，将恶唑啉化合物与在C-13直接键合的羟基的紫杉烷结合以形成含有恶唑啉侧链的紫杉烷，并开启恶唑啉环恶唑啉侧链紫杉烷如此形成。还提供了通过本发明的方法制备的新型化合物。

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