专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

JP2002193923A AMINOBENZOIC ACID DERIVATIVE 失效
公开(公告)号：JP2002193923A
公开(公告)日：2002-07-10
申请号：JP2000395413
申请日：2000-12-26
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , ASANUMA HAJIME , TAKAYAMA TETSUO , SATO MASAKAZU , YAMAGISHI TAKEHIRO , SHIBUYA MASASHI
IPC分类号： C07D307/85 , A61K31/196 , A61K31/245 , A61K31/343 , A61K31/403 , A61K31/404 , A61P5/14 , A61P9/10 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07C323/63 , C07D209/08 , C07D209/42
摘要： PROBLEM TO BE SOLVED: To provide a compound used as a VEGF receptor antagonist for the treatment of diseases which the vascularization induced by VEGF participates in and the improvement of morbid symptoms induced by the VEGF. SOLUTION: The compound represented by formula (1) R1 is hydrogen atom or a 1-6C alkyl group; R2 is a group represented by the formula: R5S (R5 is a 1-6C alkyl group) or a group represented by formula (2) (R6 is hydrogen atom or a 1-6C alkyl group); R3 is hydrogen atom or a 1-6C alkyl group; R4 is a 14-20C alkyl group; X is a group represented by formula (3) or formula (4) [Y is oxygen atom or a group represented by the general formula: NR7 (R7 is hydrogen atom or single bond)]; A is oxygen atom or a group represented by the formula: N(R8)CO (R8 is hydrogen atom or a 1-6C alkyl group); and n is zero or 1} and its medicinally acceptable salt are included.

2. 发明专利

JPH1072487A STEROL COMPOUND 失效
公开(公告)号：JPH1072487A
公开(公告)日：1998-03-17
申请号：JP23241296
申请日：1996-09-03
申请人： TAISHO PHARMA CO LTD
发明人： YAMADA TAIJI , WADA HISAYA
IPC分类号： A61K31/58 , A61P35/00 , C07J17/00
摘要： PROBLEM TO BE SOLVED: To obtain a new sterol compound consisting of a specific sterol compound capable of being synthesized by an organic synthetic chemical method in a good efficiency and also stereoselectivity, having a growth inhibiting effect on tumor cells and useful as a medicine such as an anticancer agent, etc. SOLUTION: This is a new sterol compound of formula 1 capable of being synthesized by an organic synthetic chemical method in a good efficiency and also stereoselectivity, having an antitumor effect and useful as an anticancer agent. The compound is obtained by using 3α,12α-diacetoxy-5β-pregnan-20-one expressed by formula II (Ac is acetyl) as a starting material, adjusting protecting groups in the compound, reacting with a cyclopropane compound of formula III in the presence of Li and naphthalene to produce a compound expressed by formula IV, then oxidizing an unsaturated bond to form an epoxy group after protecting hydroxyl group, displacing the epoxy group and then removing the protecting group.

3. 发明专利

JP2002193801A DERIVATIVE OF AMINOPHENYL ACETIC ACID 失效
公开(公告)号：JP2002193801A
公开(公告)日：2002-07-10
申请号：JP2000395414
申请日：2000-12-26
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , ASANUMA HAJIME , TAKAYAMA TETSUO , SATO MASAKAZU , YAMAGISHI TAKEHIRO , SHIBUYA MASASHI
IPC分类号： A61P5/14 , A61K31/216 , A61P9/00 , A61P9/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/04
摘要： PROBLEM TO BE SOLVED: To provide a derivative used as a VEGF(vascular endothelial growth factor) receptor antagonist for treatment of disease participating with vascularization introduced by VEGF and amelioration of a pathosis induced by the VEGF. SOLUTION: This compound or its pharmaceutically permissible salt is expressed by formula (1). (R1 is H or a 1-6C alkyl group, R2 is a 14-20C alkyl group, n is 1 or 2)

4. 发明专利

JPH0959295A STEROID DERIVATIVE 失效
公开(公告)号：JPH0959295A
公开(公告)日：1997-03-04
申请号：JP11516596
申请日：1996-05-10
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , ASANUMA HAJIME , YOKOO CHIHIRO , YAMADA TAIJI
IPC分类号： A61K31/575 , A61P35/00 , C07J9/00
摘要： PROBLEM TO BE SOLVED: To obtain a new steroid derivative stereoselectively synthesizable in high efficiency by an organic synthetic chemical means, having simplified structure of the side chain at 17 position, exhibiting excellent antitumor action and useful as an antitumor agent, etc. SOLUTION: The objective compound is a new steroid derivative (salt) expressed by formula I (R is a 1-13C alkyl; A is hydroxyl group or a group easily hydrolyzable to form hydroxyl group; X and Y together form oxo or a 2-3C alkylenedioxy or X and Y are each H, hydroxy, a 1-5C alkoxy or a group easily hydrolyzable to form hydroxyl group; Y is H when X is hydroxyl group, etc.; X is H when Y is hydroxyl group, etc.; Y is a 1-5C alkoxy when X is a 1-5C alkoxy). The compound is useful as an antitumor agent, etc. The compound can be synthesized in high efficiency and stereoselectivity by using a steroid expressed by formula II as a starting substance and subjecting the substance to various reactions using organic synthetic chemical means.

5. 发明专利

JPH08333386A STEROID DERIVATIVE 失效
公开(公告)号：JPH08333386A
公开(公告)日：1996-12-17
申请号：JP14469495
申请日：1995-06-12
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , YOKOO CHIHIRO , YAMADA TAIJI
IPC分类号： A61K31/575 , A61P35/00 , C07J17/00
摘要： PURPOSE: To obtain a new steroid derivative useful for medicines having an antitumor action, etc. CONSTITUTION: A compound of formula I (R is a 1-4C alkyl; X, Y are hydroxyl group, a group capable of being easily hydrolyzed to form the hydroxyl group). For example, a compound of formula II. The compound of formula I is obtained by producing an allyl alcohol compound of formula IV from 3β,12β-dihydroxy-5α- pregnan-20-one of formula III as a starting raw material and subsequently reacting the compound of formula IV with m-chloroperbenzoic acid in the presence of a base such as sodium bicarbonate.

6. 发明专利

JPH07224087A STEROID DERIVATIVE 失效
公开(公告)号：JPH07224087A
公开(公告)日：1995-08-22
申请号：JP31015894
申请日：1994-12-14
申请人： TAISHO PHARMA CO LTD
发明人： YOKOO CHIHIRO , WADA HISAYA , MITOME HIDEMICHI , SANO TATSUHIKO , HATAYAMA KATSUO , YAMADA TAIJI
IPC分类号： A61K31/58 , A61K35/56 , A61K35/655 , A61P35/00 , C07J17/00 , C07J75/00
摘要： PURPOSE:To obtain a new steroid derivative efficiently and stereoselectively synthesizable by synthetic organic chemical technique without the need for using natural substance-derived materials with problems such as concerning resource security, having proliferation inhibitory activity against oncocytes, thus useful as an antineoplastic agent etc. CONSTITUTION:This new steroid derivative having antineoplastic activity is expressed by formula I (R is a 1-13C alkyl; A is hydroxyl group or a group becoming hydroxyl group through ready hydrolysis; X and Y are combined into oxo or a 2-3C alkylenedioxy; X is hydroxyl, a 1-5C alkoxyl or a group becoming hydroxyl group through ready hydrolysis; Y is H or 1-5C alkoxyl; when X is hydroxyl or a group becoming hydroxyl through ready hydrolysis, Y is H; when X is a 1-5C alkoxyl, Y is also a 1-5C alkoxyl). This new compound can be obtained by protecting the hydroxyl group of 3beta,12beta-dihydroxy-5alpha- pregnan-20-one followed by alkylation with a Grignard reagent and dehydration and then Oppenauer oxidation of the product which is, in turn, treated with a peroxide.

7. 发明专利

JP2002193800A VEGF RECEPTOR ANTAGONIST 失效
公开(公告)号：JP2002193800A
公开(公告)日：2002-07-10
申请号：JP2000391704
申请日：2000-12-22
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , ASANUMA HAJIME , TAKAYAMA TETSUO , SATO MASAKAZU , YAMAGISHI TAKEHIRO , SHIBUYA MASASHI
IPC分类号： A61P7/00 , A61K31/192 , A61K31/216 , A61K31/27 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/00 , A61P17/06 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07C235/38 , C07C313/36 , C07C323/59
摘要： PROBLEM TO BE SOLVED: To provide a vascular endothelial growth factor(VEGF) receptor antagonist for therapy of diseases relating to vascularization or vascular permeability sthenia. SOLUTION: This VEGF receptor antagonist is characterized by containing a compound represented by the formula (1) R1 is H, a 1-6C alkyl or the like; R2 is H, a 1-6C alkyl or the like; R3 is an 8-25C alkyl or the like; R4 is H, OR9 or CO2R10 (wherein, R9 and R10 are each H or a 1-6C alkyl); A is S(O)qR15 [wherein, q is 0, 1 or 2; R15 is a 1-6C alkyl, a phenyl 1-3C alkyl or (CH2)mOR16 (wherein, m is 2 or 3; R16 is H or methoxymethyl)]; X is O, single bond, CH=CH, CO or NR27 (wherein, R27 is H or t-butoxycarbonyl); Y is O, CONH, NHCO or NR28 (wherein, R28 is H or t-butoxycarbonyl); and n is an integer of 0-15} or a pharmaceutically acceptable salt thereof as an active ingredient.

8. 发明专利

JP2001072587A VEGF RECEPTOR ANTAGONIST 失效
公开(公告)号：JP2001072587A
公开(公告)日：2001-03-21
申请号：JP2000201418
申请日：2000-07-03
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , ASANUMA HAJIME , TAKAYAMA TETSUO , SATO MASAKAZU , YAMAGISHI TAKEHIRO , SHIBUYA MASASHI
IPC分类号： C12Q1/02 , A61K31/196 , A61K31/245 , A61P27/02 , A61P29/00 , A61P35/00 , C07C235/80 , C07C323/63 , C12Q1/48
摘要： PROBLEM TO BE SOLVED: To obtain the subject antagonist inhibiting the binding of VEGF as a specific propagating factor of vascular endothelial cells with its receptor, and useful for the treatment of a disease associated with the angiogenesis induced by the VEGF and the improvement of morbid symptoms associated with the enhancement of the vascular permeability by incorporating a specific benzoic acid derivative. SOLUTION: This VEGF receptor antagonist is obtained by incorporating a compound of formula I [R1 is H, COOR5 (R5 is H or a 1-6C alkyl) or OR6 (R6 is H or a 1-6C alkyl); R2 is H or COOR7 (R7 is H or a 1-6C alkyl); R3 is H or a 1-6C alkyl; R4 is a 8-25C alkyl; X is O, S or NH; Y is O or NHCO] or its pharmaceutically permissible salt. The compound of the formula I is obtained by reacting a compound of formula IV obtained by using a compound of formula II and a nitro compound of formula III (halo is a halogen) as starting materials, with a ketoester of formula V (R is a lower alkyl) in the presence or absence of an inert solvent at a temperature between 100-200 deg.C.

9. 发明专利

JPH08113589A NEW TAXOL DERIVATIVE 失效
公开(公告)号：JPH08113589A
公开(公告)日：1996-05-07
申请号：JP21600895
申请日：1995-08-24
申请人： TAISHO PHARMA CO LTD , CHUGOKU IGAKU KAGAKUIN YAKUBUT
发明人： MIKUCHI MORIKIMI , WADA HISAYA , SEKIGUCHI YOSHIISA , YOKOO CHIHIRO , HATAYAMA KATSUO
IPC分类号： C07H17/04 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P35/00

10. 发明专利

JP2002255917A SUBSTITUTED PHENYLALKANOYL ANILIDE DERIVATIVE 审中-公开
公开(公告)号：JP2002255917A
公开(公告)日：2002-09-11
申请号：JP2001353075
申请日：2001-11-19
申请人： TAISHO PHARMA CO LTD
发明人： WADA HISAYA , ASANUMA HAJIME , TAKAYAMA TETSUO , SATO MASAKAZU , YAMAGISHI TAKEHIRO , SHIBUYA MASASHI
IPC分类号： C07D295/14 , A61K31/196 , A61K31/216 , A61K31/495 , A61P5/16 , A61P9/00 , A61P9/10 , A61P19/02 , A61P29/00 , A61P35/00 , C07C59/68 , C07C235/38 , C07C321/28
摘要： PROBLEM TO BE SOLVED: To obtain a compound used as a vascular endothelial growth factor(VEGF) receptor antagonist for treating diseases associated with neovascularization induced by the VEGF and ameliorating pathogenic symptoms induced by the VEGF. SOLUTION: This compound is represented by the following formula [wherein, R is hydrogen atom or a 1-6C alkyl group; R is a 1-6C alkyl group; R is hydrogen atom or a 1-6C alkyl group; R is phenyl group, benzyl group or a 1-18C alkyl group; A is oxygen atom or sulfur atom; n is 1 or 2; X is oxygen atom or a group represented by the formula N(R )C=O (wherein, R is a 1-6C alkyl group); m is an integer of 1-18; Y denotes oxygen atom, sulfur atom, a single bond, a group represented by the formula NR (wherein, R is a 1-18C alkyl group), 1,4-henylenedioxy group, 1,3-phenylenedioxy group or 1,4-piperazinyl group] or its pharmaceutically acceptable salt.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式