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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

JP2002193947A BENZIMIDAZOLE DERIVATIVE 失效
公开(公告)号：JP2002193947A
公开(公告)日：2002-07-10
申请号：JP2000395417
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： C07D235/12 , A61K31/4184 , A61P5/14 , A61P9/10 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D235/18
摘要： PROBLEM TO BE SOLVED: To provide a compound used as an antagonist for VEGF receptor so as to treat disease concerned with vascularization induced by VEGF and to improve unhealthy condition induced by VEGF. SOLUTION: This compound is represented by formula (1) [wherein, R1 is hydrogen or a 1-6C alkyl, R2 is hydrogen atom or formula (2) (wherein, R4 is hydrogen or a 1-6C alkyl), and n is an integer of 0 to 2], and contains an allowable salt for medicine.

3. 发明专利

JP2002193922A SUBSTITUTED BENZOIC ACID DERIVATIVE 失效
公开(公告)号：JP2002193922A
公开(公告)日：2002-07-10
申请号：JP2000395415
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： C07D307/68 , A61K31/196 , A61K31/245 , A61K31/341 , A61P5/14 , A61P9/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C69/92 , C07C229/60 , C07C233/07 , C07C321/28
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 hydrogen atom, hydroxy group or a group represented by formula R4S (R4 is a 1-6C alkyl group); R3 is a 14-20C alkyl group; X is oxygen atom or a group represented by the formula: R5N [R5 is hydrogen atom, a 1-6C alkyl group, a group represented by the formula: R6CO (R6 is hydrogen atom, a 1-6C alkyl group, a 2-6C alkoxyalkyl group, a 2-6C alkoxycarbonylalkyl group or 2-furyl group) or R7SO2 (R7 is a 1-6C alkyl group)]; and n is an integral number of 1 to 3} and its medicinally acceptable salt are included.

4. 发明专利

JP2001072653A AMINOBENZOIC ACID DERIVATIVE 失效
公开(公告)号：JP2001072653A
公开(公告)日：2001-03-21
申请号：JP2000201419
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： C07D213/80 , A61K31/245 , A61K31/27 , A61K31/44 , A61P3/10 , A61P5/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/04 , A61P43/00 , C07C235/38 , C07C317/50 , C07C323/63
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound having antagonistic actions on vascular endothelial growth factor(VEGF) receptors, capable of inhibiting the VEGF-dependent vascular endothelial cell growth and neovascularization and suppressing the acceleration of vascular permeability with the VEGF and useful for the treatment, etc., of diabetic retinopathy, etc. SOLUTION: This compound is represented by formula I [R1 is H or a 1-6C alkyl; R2 is H, a 1-6C alkyl or the like; R3 is an 8-25C alkyl or the like; R4 is H or OR9 (R9 is H, a 1-6C alkyl or the like); A is a group represented by S(O)qR15 (q is 0-2; R15 is a 1-6C alkyl or the like) or the like; X is O, a single bond or the like; Y is O, CONH or the like; n is 0-15], e.g. a compound represented by formula II. The compound represented by formula I, e.g. A is the group represented by S(O)qR15 is obtained as a compound represented by formula V by carrying out a condensing reaction of a compound represented by formula III [A' is a group represented by S(O)qR15] with a compound represented by formula IV by using a condensing agent such as 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrcshloride and 1- hydroxybenzotriazole.

5. 发明专利

JPH10310598A STEROL COMPOUND 失效
公开(公告)号：JPH10310598A
公开(公告)日：1998-11-24
申请号：JP5729198
申请日：1998-03-10
申请人： TAISHO PHARMA CO LTD
发明人： ASANUMA HAJIME , WADA HISAYA , YAMADA TAIJI
IPC分类号： A61K31/58 , A61P35/00 , C07J17/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound comprising a specific sterol compound capable of efficiently and stereoselectively synthesizing by organic synthetic chemical method, having excellent in vivo antitumor action and useful as a medicine such as anticancer agent. SOLUTION: This new sterol compound is represented by formula I (R is nonyl or decyl) and has excellent in vivo antiulcer action and is capable of stereoselectively synthesizing by organic synthetic chemical method and is useful as a medicine, etc., e.g. anticancer agent. The compound is obtained by using 3β,12β-dihydroxy-5 α-pregnan20 one as a starting material, protecting the hydroxyl group, reacting the compound with a Grignard feagent to afford a substance having alcohol at 20 position, dehydrating the substance to provide 20,22(E)-olefin substance of formula of formula III, oxidizing the substance to afford 20,22-epoxy substance, protecting hydroxyl group, subjecting the epoxy substance to hydrochloric acid treatment, oxidizing the resultant 3β,12β-diacetoxyallyl alcohol substance of formula IV to provide 20, 21-epoxy substance and deprotecting the resultant substance.

6. 发明专利

JPH10251294A CIS-STEROL COMPOUND 失效
公开(公告)号：JPH10251294A
公开(公告)日：1998-09-22
申请号：JP5722097
申请日：1997-03-12
申请人： TAISHO PHARMA CO LTD
发明人： ASANUMA HAJIME , WADA HISAYA , YAMADA TAIJI
IPC分类号： A61K31/58 , A61K35/56 , A61P35/00 , C07J17/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound, comprising a specific cis-sterol compound capable of being efficiently and stereoselectively synthesized according to an organic synthetic chemical method using deoxycholic acid as a raw material, having antitumor actions and useful as an antitumor agent, etc. SOLUTION: This new cis-sterol compound is represented by formula I (R is a 1-13C alkyl), has antitumor actions and is useful as a medicine, etc., such as an antitumor agent. The cis-sterol compound is obtained by converting a 3α,12α- diacetoxy-5β-pregn-20-one, derived from deoxycholic acid and represented by formula II (Ac is acetyl) used as a starting substance into a ketal derivative with an acidic catalyst, treating the resultant ketal derivative with a base, providing a derivative having OH at the 3-position, protecting the OH, affording a derivative having OH at the 12-position, oxidizing the prepared derivative, providing a ketonic derivative at the 12-position, reducing the ketonic derivative, affording a derivative having β-OH at the 12-position, deprotecting the 20-position, reacting the produced ketone group with a Grignard reagent, affording a derivative having OH at the 20-position, dehydrating the resultant derivative, providing an unsaturated group, epoxidizing the unsaturated group, affording a compound represented by formula III and converting the steric configuration of the substituent group R.

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

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)

10. 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.

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