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1. 发明专利

DE3770724D1 未知
公开(公告)号：DE3770724D1
公开(公告)日：1991-07-18
申请号：DE3770724
申请日：1987-07-23
申请人： SUMITOMO CHEMICAL CO , SUMITOMO PHARMA
发明人： ENOMOTO MASAO , MURAOKA MASAMI , ONO KEIICHI , KOJIMA ATSUYUKI , ATSUMI TOSHIO , KOMURO YOSHIHIRO , SANEMITSU YUZURU , MIZUTANI MASATO
IPC分类号： A61K31/425 , A61K31/44 , A61P1/04 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , C07D417/04

2. 发明专利

AT64392T 未知
公开(公告)号：AT64392T
公开(公告)日：1991-06-15
申请号：AT87306508
申请日：1987-07-23
申请人： SUMITOMO PHARMA , SUMITOMO CHEMICAL CO
发明人： ENOMOTO MASAO , MURAOKA MASAMI , ONO KEIICHI , KOJIMA ATSUYUKI , ATSUMI TOSHIO , KOMURO YOSHIHIRO , SANEMITSU YUZURU , MIZUTANI MASATO
IPC分类号： A61K31/425 , A61K31/44 , A61P1/04 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , C07D417/04

3. 发明专利

JPS63225373A NOVEL THIAZOLIDIN-4-ONE-DERIVATIVE AND ACID ADDITION SALT THEREOF 失效
公开(公告)号：JPS63225373A
公开(公告)日：1988-09-20
申请号：JP14830387
申请日：1987-06-15
申请人： SUMITOMO PHARMA , SUMITOMO CHEMICAL CO
发明人： ENOMOTO MASAO , MURAOKA MASAMI , ONO KEIICHI , KOJIMA ATSUYUKI , ATAMI TOSHIO , KOMURO YOSHIHIRO , SANEMITSU MINORU , MIZUTANI MASATO
IPC分类号： A61K31/425 , A61K31/44 , A61P1/04 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , C07D417/04
摘要： NEW MATERIAL:The compound of formula I [Ar is aryl which may have substit uent group (halogen or lower alkoxy); X is straight or branched lower alkylene or single bond; R is H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, acyldioxy, di-lower alkylamino, OH or aryl which may be substituted with lower alkoxy; Py is pyridyl] and its acid addition salt. EXAMPLE:5-(4-Chlorophenyl)-3-methyl-2-(3-pyridyl)thiazolidin-4-one. USE:A drug having strong and selective antagonistic activity against platelet activation factor (PAF) and useful for the prevention and remedy of PAF- induced diseases such as various inflammation, circulatory diseases, allergic diseases and gastrointestinal ulcer. PREPARATION:The compound of formula I can be produced by cyclizing a compound of formula II and a compound of formula III in an organic solvent.

4. 发明专利

JPH01190679A OPTICALLY ACTIVE NOVEL THIAZOLIDINE-4-ONE DERIVATIVE AND ACID-ADDITION SALT THEREOF 失效
公开(公告)号：JPH01190679A
公开(公告)日：1989-07-31
申请号：JP1244488
申请日：1988-01-22
申请人： SUMITOMO PHARMA , SUMITOMO CHEMICAL CO
发明人： ENOMOTO MASAO , MURAOKA MASAMI , ONO KEIICHI , KOJIMA ATSUYUKI , ATAMI TOSHIO , KOMURO YOSHIHIRO , SANEMITSU MINORU , MIZUTANI MASATO , TANABE AKIRA
IPC分类号： C07D213/53 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61P1/04 , A61P7/02 , A61P11/00 , A61P29/00 , C07D417/04
摘要： NEW MATERIAL:A compound expressed by formula I [Ar is aryl (substituted by halogen or lower alkoxy); X is straight-chain or branched chain lower alkylene or single bond; R is H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, acyloxy, OH, aryl, etc.; Py is pyridyl] and acid-addition salt thereof. EXAMPLE:(+)-cis-5-(4-Chlorophenyl)-3-methyl-2-(3-pyridyl)-thiazolidine -4-one. USE:A medicine and active ingredient for anti-platelet-activating factor agent. Useful as a medicine for preventing and treating an induced disease such as allergic disease, circulatory disease or alimentary disease. PREPARATION:For example, an optically active compound expressed by formula II is reacted with a compound expressed by formula III in an organic solvent to close a ring and the resultant mixture of cis isomer and trans isomer is readily separated to cis isomer and trans isomer by conventional separation means to provide the compound expressed by formula I.

5. 发明专利

AU8605382A PENICILLINS AND AZETIDINONES 未知
公开(公告)号：AU8605382A
公开(公告)日：1983-01-20
申请号：AU8605382
申请日：1982-07-15
申请人： SUMITOMO CHEMICAL CO
发明人： SUNAGAWA MAKOTO , MATSUMURA HARUKI , INOUE TAKAAKI , ENOMOTO MASAO
IPC分类号： C07C205/42 , C07D205/08 , C07D205/09 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/32 , C07D211/38 , C07D211/46 , C07D211/48 , C07D211/54 , C07D211/62 , C07D211/70 , C07D211/74 , C07D499/00 , C07D499/88 , C07F9/568 , C07F9/6541 , C07C69/353 , C07C69/75 , C07C79/22 , C07C101/20 , C07C101/72 , C07C143/68 , C07C149/243 , C07C153/017 , C07F9/65

6. 发明专利

CA1338090C THIAZOLIDIN-4-ONE DERIVATIVES AND ACID ADDITION SALTS THEREOF 未知
公开(公告)号：CA1338090C
公开(公告)日：1996-02-27
申请号：CA567319
申请日：1988-05-20
申请人： SUMITOMO PHARMA
发明人： ENOMOTO MASAO , KOJIMA ATSUYUKI , KOMURO YOSHIHIRO , MOROOKA SHIGEAKI , AONO SHUNJI , SANEMITSU YUZURU , MIZUTANI MASATO , TANABE YOU
IPC分类号： C07D417/04 , C07D417/14 , A61K31/44
摘要： Thiazolidin-4-one derivative represented by the following general formula (I) and acid addition salts thereof (I) wherein; R1 and R2 are the same or different and denote each (i) a residue represented by the general formula -A-R4 wherein, A denotes a single bond, C1-C8 alkylene, C2-C8 alkenylene, or C2-C8 alkynylene and R4 denotes hydrogen, C1-C12 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, or C1-C6 haloalkyl, or (ii) a residue represented by the general formula wherein, B denotes a single bond or C1-C6 alkylene, R5 denotes hydrogen, C1-C6 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2; and R3 denotes hydrogen, C1-C2 alkyl, allyl, 2propynyl, or a residue represented by (a) the general formula (CH2)? R6 wherein, R6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C1-C4 alkoxy groups, or a residue represented by the general formula -D-R7 (D denotes oxygen or sulfur and R7 denotes hydrogen, C1-C4 alkyl, or C1-C4 alkanol) and ? denotes an integer of 2 to 4, (b) the general formula ?CH2? CO-E-R8 wherein, E denotes oxygen, sulfur, imino, or C1-C4 alkylimino, R8 denotes hydrogen or C1-C4 alkyl, or -(E-R8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or (c) the general formula - F-R9 wherein, F denotes C2-C6 alkylene and R9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula (R10 denotes hydrogen, C1-C4 alkyl, or C1-C4 alkyl or R10 in combination with R11 denotes a 5- to

7. 发明专利

DE3279647D1 PROCESS OF PREPARING AZETIDINONE COMPOUNDS 未知
公开(公告)号：DE3279647D1
公开(公告)日：1989-06-01
申请号：DE3279647
申请日：1982-07-15
申请人： SUMITOMO PHARMA
发明人： SUNAGAWA MAKOTO , MATSUMURA HARUKI , INOUE TAKAAKI , ENOMOTO MASAO
IPC分类号： A61K31/43 , C07D205/08 , C07D499/00

8. 发明专利

DE3873167D1 未知
公开(公告)号：DE3873167D1
公开(公告)日：1992-09-03
申请号：DE3873167
申请日：1988-05-20
申请人： SUMITOMO PHARMA
发明人： ENOMOTO MASAO , KOJIMA ATSUYUKI , KOMURO YOSHIHIRO , MOROOKA SHIGEAKI , AONO SHUNJI , SANEMITSU YUZURU , MIZUTANI MASATO , TANABE YOU
IPC分类号： C07D417/04 , A61K31/44
摘要： Thiazolidin-4-one derivatives are represented by the following general formula (I) wherein; R and R are the same or different and denote each (i) a residue represented by the general formula -A-R wherein, A denotes a single bond, C1-C8 alkylene, C2-C8 alkenylene, or C2-C8 alkynylene and R denotes hydrogen, C1-C12 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, or C1-C6 haloalkyl, or (ii) a residue represented by the general formula wherein, B denotes a single bond or C1-C6 alkylene, R denotes hydrogen, C1-C6 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n min denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m min denotes an integer of 0 to 2; and R denotes hydrogen, C1-C2 alkyl, allyl, 2-propynyl, or a residue represented by (a) the general formula @@@CH2@ @@R wherein, R denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C1-C4 alkoxy groups, or a residue represented by the general formula -D-R (D denotes oxygen or sulfur and R denotes hydrogen, C1-C4 alkyl, or C1-C4 alkanol) and l denotes an integer of 2 to 4, (b) the general formula @@@CH2@ @@CO-E-R wherein, E denotes oxygen, sulfur, imino, or C1-C4 alkylimino, R denotes hydrogen or C1-C4 alkyl, or -(E-R ) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or (c) the general formula -F-R wherein, F denotes C2-C6 alkylene and R denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula (R denotes hydrogen, C1-C4 alkyl, or C1-C4 alkyl or R in combination with R denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms), with the proviso that, when R is hydrogen and R is methyl, R denotes hydrogen, C1-C2 alkyl, 2-propynyl, or a residue represented by (a) the general formula @@@CH2@ @@R wherein, R denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C1-C4 alkoxy groups, or a residue represented by the general formula -D-R (D denotes oxygen or sulfur and R denotes hydrogen, C1-C4 alkyl, or C1-C4 alkanoyl) and l denotes an integer of 2 to 4, (b) the general formula @@CH2@@ @CO-E-R wherein, E denotes oxygen, sulfur, imino, or C1-C4 alkylimino, denotes hydrogen or C1-C4 alkyl, or -(E-R ) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or (c) the general formula -F-R wherein, F denotes C2-C6 alkylene and R denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula (R denotes hydrogen, C2-C4 alkyl or C1-C4 alkanoyl and R denotes hydrogen or C1-C4 alkyl or R in combination with R denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms. Since these derivatives, and acid addition salts thereof have selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflamation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

9. 发明专利

AT78821T 未知
公开(公告)号：AT78821T
公开(公告)日：1992-08-15
申请号：AT88304583
申请日：1988-05-20
申请人： SUMITOMO PHARMA
发明人： ENOMOTO MASAO , KOJIMA ATSUYUKI , KOMURO YOSHIHIRO , MOROOKA SHIGEAKI , AONO SHUNJI , SANEMITSU YUZURU , MIZUTANI MASATO , TANABE YOU
IPC分类号： A61K31/44 , C07D417/04

10. 发明专利

DE3873167T2 未知
公开(公告)号：DE3873167T2
公开(公告)日：1992-12-03
申请号：DE3873167
申请日：1988-05-20
申请人： SUMITOMO PHARMA
发明人： ENOMOTO MASAO , KOJIMA ATSUYUKI , KOMURO YOSHIHIRO , MOROOKA SHIGEAKI , AONO SHUNJI , SANEMITSU YUZURU , MIZUTANI MASATO , TANABE YOU
IPC分类号： C07D417/04 , A61K31/44
摘要： Thiazolidin-4-one derivatives are represented by the following general formula (I) wherein; R and R are the same or different and denote each (i) a residue represented by the general formula -A-R wherein, A denotes a single bond, C1-C8 alkylene, C2-C8 alkenylene, or C2-C8 alkynylene and R denotes hydrogen, C1-C12 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, or C1-C6 haloalkyl, or (ii) a residue represented by the general formula wherein, B denotes a single bond or C1-C6 alkylene, R denotes hydrogen, C1-C6 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n min denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m min denotes an integer of 0 to 2; and R denotes hydrogen, C1-C2 alkyl, allyl, 2-propynyl, or a residue represented by (a) the general formula @@@CH2@ @@R wherein, R denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C1-C4 alkoxy groups, or a residue represented by the general formula -D-R (D denotes oxygen or sulfur and R denotes hydrogen, C1-C4 alkyl, or C1-C4 alkanol) and l denotes an integer of 2 to 4, (b) the general formula @@@CH2@ @@CO-E-R wherein, E denotes oxygen, sulfur, imino, or C1-C4 alkylimino, R denotes hydrogen or C1-C4 alkyl, or -(E-R ) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or (c) the general formula -F-R wherein, F denotes C2-C6 alkylene and R denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula (R denotes hydrogen, C1-C4 alkyl, or C1-C4 alkyl or R in combination with R denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms), with the proviso that, when R is hydrogen and R is methyl, R denotes hydrogen, C1-C2 alkyl, 2-propynyl, or a residue represented by (a) the general formula @@@CH2@ @@R wherein, R denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C1-C4 alkoxy groups, or a residue represented by the general formula -D-R (D denotes oxygen or sulfur and R denotes hydrogen, C1-C4 alkyl, or C1-C4 alkanoyl) and l denotes an integer of 2 to 4, (b) the general formula @@CH2@@ @CO-E-R wherein, E denotes oxygen, sulfur, imino, or C1-C4 alkylimino, denotes hydrogen or C1-C4 alkyl, or -(E-R ) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or (c) the general formula -F-R wherein, F denotes C2-C6 alkylene and R denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula (R denotes hydrogen, C2-C4 alkyl or C1-C4 alkanoyl and R denotes hydrogen or C1-C4 alkyl or R in combination with R denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms. Since these derivatives, and acid addition salts thereof have selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflamation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

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