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1. 发明授权

KR790000197B1 PROCESS FOR PREPARING N-SUBSTITUTED CYCLOSERINES 失效
公开(公告)号：KR790000197B1
公开(公告)日：1979-04-04
申请号：KR740003147
申请日：1974-07-24
申请人： MERCK & CO INC
发明人： JENSEN N P
摘要： Substituted D-4-amino-3-isoxazolidinone(I, R = H or Me group, X, Y, Z = H or alkyl group) were prepd. by condensation of 2.4-pentanedione (II) or its 3-methyl deriv. with D-4-amino-3-isoxazolidinone(III) or its 5-methyl deriv. Thus, II was reacted with III for 40-48 hr at room temp. to give I, which was treated with NaOH or aq. CaO to give the corresponding Na or Ca salts.

2. 发明专利

SE7608037L 未知
公开(公告)号：SE7608037L
公开(公告)日：1977-01-30
申请号：SE7608037
申请日：1976-07-14
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： A61K31/435 , A61P17/00 , A61P29/00 , C07C63/72 , C07C205/57 , C07D213/73 , C07D498/04
摘要： 1497985 Oxazolo[4,5-b]pyridines MERCK & CO Inc 26 July 1976 [29 July 1975] 31065/76 Heading C2C The invention comprises compounds of formula wherein R is H, halogen or C 1-5 alkyl or alkoxy, R 1 is H or C 1-5 alkyl, and n is 3, 4 or 5. In examples, these compounds are prepared by (a) condensing a corresponding 2-amino-3-hydroxypyridine with an appropriate indone-tetrahydronaphthalene- or benzocycloheptene-derived carboxylic acid, or (b) forming the analogue in which R is OH by splitting the methyl ether (R = OMe), followed by etherification to give a different ether. Starting materials otherwise prepared are amino- and nitro-indane (or tetrahydronaphthalene) carboxylic acids. Therapeutic compositions having antiinflammatory activity comprise compounds of the above formula, and may be administered topically.

3. 发明专利

NO742622L 未知
公开(公告)号：NO742622L
公开(公告)日：1975-03-03
申请号：NO742622
申请日：1974-07-18
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： C07D261/02 , A61K31/42 , A61P31/04 , C07D261/04 , C07D85/12
摘要： Stabilized cycloserine compositions, having enhanced stability, and effective in releasing cycloserine compounds in vivo, are prepared by reacting D-4-amino-3-isoxazolidinone or its 5-methyl derivative with 2,4-pentanedione or alkyl-substituted-2,4-pentanedione to form the corresponding N-substituted-cycloserine compound in which one of the hydrogens attached to the primary amino group is replaced by 1-methyl-3-oxo-1-butenyl or an alkyl substituted-1-methyl-3-oxo-1-butenyl grouping. These D-4-(1'-methyl-3'-oxo-1'-butenyl or alkyl-substituted-1'-methyl-3'-oxo-1'-butenyl)amino-3-isoxazolidinones or 5-methyl derivative thereof, which may also be referred to as N-(1-methyl-3-oxo-1-butenyl or alkyl-substituted-1-methyl-3-oxo-1-butenyl)-derivative of cycloserine or methyl-cycloserine, as well as their pharmacologically acceptable salts, are remarkably stable on storage as well as upon oral administration, and are extremely effective in releasing in vivo the cycloserine compound containing the free primary amino grouping.

4. 发明专利

AU505159B2 OXAZOLO (4,5-B) PYRIDINE 未知
公开(公告)号：AU505159B2
公开(公告)日：1979-11-08
申请号：AU1605276
申请日：1976-07-20
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： A61K31/435 , A61P17/00 , A61P29/00 , C07C63/72 , C07C205/57 , C07D213/73 , C07D498/04 , C07C101/70 , C07C101/50
摘要： 1497985 Oxazolo[4,5-b]pyridines MERCK & CO Inc 26 July 1976 [29 July 1975] 31065/76 Heading C2C The invention comprises compounds of formula wherein R is H, halogen or C 1-5 alkyl or alkoxy, R 1 is H or C 1-5 alkyl, and n is 3, 4 or 5. In examples, these compounds are prepared by (a) condensing a corresponding 2-amino-3-hydroxypyridine with an appropriate indone-tetrahydronaphthalene- or benzocycloheptene-derived carboxylic acid, or (b) forming the analogue in which R is OH by splitting the methyl ether (R = OMe), followed by etherification to give a different ether. Starting materials otherwise prepared are amino- and nitro-indane (or tetrahydronaphthalene) carboxylic acids. Therapeutic compositions having antiinflammatory activity comprise compounds of the above formula, and may be administered topically.

5. 发明专利

SE407578B 未知
公开(公告)号：SE407578B
公开(公告)日：1979-04-02
申请号：SE7311178
申请日：1973-08-16
申请人： MERCK & CO INC
发明人： SHEN T-Y , JENSEN N P
IPC分类号： A61K31/685 , A61P25/04 , A61P29/00 , B01J25/00 , C07B61/00 , C07F9/22 , C07F9/26 , C07F9/572 , C07F9/58 , C07F9/655 , C07F9/6553

6. 发明专利

NO742622A 未知
公开(公告)号：NO742622A
公开(公告)日：1975-03-03
申请号：NO742622
申请日：1974-07-18
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： C07D261/02 , A61K31/42 , A61P31/04 , C07D261/04 , C07D85/12
CPC分类号： C07D261/04

7. 发明专利

DK383374A 未知
公开(公告)号：DK383374A
公开(公告)日：1975-04-01
申请号：DK383374
申请日：1974-07-17
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： C07D261/02 , A61K31/42 , A61P31/04 , C07D261/04 , C07D85/12
摘要： Stabilized cycloserine compositions, having enhanced stability, and effective in releasing cycloserine compounds in vivo, are prepared by reacting D-4-amino-3-isoxazolidinone or its 5-methyl derivative with 2,4-pentanedione or alkyl-substituted-2,4-pentanedione to form the corresponding N-substituted-cycloserine compound in which one of the hydrogens attached to the primary amino group is replaced by 1-methyl-3-oxo-1-butenyl or an alkyl substituted-1-methyl-3-oxo-1-butenyl grouping. These D-4-(1'-methyl-3'-oxo-1'-butenyl or alkyl-substituted-1'-methyl-3'-oxo-1'-butenyl)amino-3-isoxazolidinones or 5-methyl derivative thereof, which may also be referred to as N-(1-methyl-3-oxo-1-butenyl or alkyl-substituted-1-methyl-3-oxo-1-butenyl)-derivative of cycloserine or methyl-cycloserine, as well as their pharmacologically acceptable salts, are remarkably stable on storage as well as upon oral administration, and are extremely effective in releasing in vivo the cycloserine compound containing the free primary amino grouping.

8. 发明专利

SE7409378L 未知
公开(公告)号：SE7409378L
公开(公告)日：1975-02-03
申请号：SE7409378
申请日：1974-07-18
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： C07D261/02 , A61K31/42 , A61P31/04 , C07D261/04 , C07D85/12 , C07D261/12
摘要： Stabilized cycloserine compositions, having enhanced stability, and effective in releasing cycloserine compounds in vivo, are prepared by reacting D-4-amino-3-isoxazolidinone or its 5-methyl derivative with 2,4-pentanedione or alkyl-substituted-2,4-pentanedione to form the corresponding N-substituted-cycloserine compound in which one of the hydrogens attached to the primary amino group is replaced by 1-methyl-3-oxo-1-butenyl or an alkyl substituted-1-methyl-3-oxo-1-butenyl grouping. These D-4-(1'-methyl-3'-oxo-1'-butenyl or alkyl-substituted-1'-methyl-3'-oxo-1'-butenyl)amino-3-isoxazolidinones or 5-methyl derivative thereof, which may also be referred to as N-(1-methyl-3-oxo-1-butenyl or alkyl-substituted-1-methyl-3-oxo-1-butenyl)-derivative of cycloserine or methyl-cycloserine, as well as their pharmacologically acceptable salts, are remarkably stable on storage as well as upon oral administration, and are extremely effective in releasing in vivo the cycloserine compound containing the free primary amino grouping.

9. 发明专利

BE769232A 未知
公开(公告)号：BE769232A
公开(公告)日：1971-12-29
申请号：BE769232
申请日：1971-06-29
申请人： MERCK & CO INC
发明人： SHEN T-Y , FORDICE M W , RUYLE W V , JENSEN N P
IPC分类号： A23K1/16 , C07D213/53 , C07D233/92 , C07D233/95 , C07D277/28 , C07D307/54 , C07D307/68 , C07D333/22 , C07C , A61K

10. 发明专利

YU37160B PROCESS FOR OBTAINING N-SUBSTITUTED CYCLOSERINES 未知
公开(公告)号：YU37160B
公开(公告)日：1984-08-31
申请号：YU205374
申请日：1974-07-23
申请人： MERCK & CO INC
发明人： JENSEN N P
IPC分类号： C07D261/02 , A61K31/42 , A61P31/04 , C07D261/04 , A61K31/34
摘要： Stabilized cycloserine compositions, having enhanced stability, and effective in releasing cycloserine compounds in vivo, are prepared by reacting D-4-amino-3-isoxazolidinone or its 5-methyl derivative with 2,4-pentanedione or alkyl-substituted-2,4-pentanedione to form the corresponding N-substituted-cycloserine compound in which one of the hydrogens attached to the primary amino group is replaced by 1-methyl-3-oxo-1-butenyl or an alkyl substituted-1-methyl-3-oxo-1-butenyl grouping. These D-4-(1'-methyl-3'-oxo-1'-butenyl or alkyl-substituted-1'-methyl-3'-oxo-1'-butenyl)amino-3-isoxazolidinones or 5-methyl derivative thereof, which may also be referred to as N-(1-methyl-3-oxo-1-butenyl or alkyl-substituted-1-methyl-3-oxo-1-butenyl)-derivative of cycloserine or methyl-cycloserine, as well as their pharmacologically acceptable salts, are remarkably stable on storage as well as upon oral administration, and are extremely effective in releasing in vivo the cycloserine compound containing the free primary amino grouping.

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