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1. 发明专利

CA2278779A1 SUBSTITUTED AMINO BICYCLIC-.BETA.-LACTAM PENAM AND CEPHAM DERIVATIVES AS CYSTEINE PROTEASE INHIBITORS 未知
公开(公告)号：CA2278779A1
公开(公告)日：1998-07-30
申请号：CA2278779
申请日：1998-01-22
申请人： SYNPHAR LAB INC
发明人： ZHOU NIAN E , GUO DEQI , MICETICH RONALD G , SINGH RAJESHWAR
IPC分类号： C12N9/99 , A61K31/43 , A61K31/431 , A61K31/545 , A61K31/546 , A61P9/02 , A61P9/10 , A61P11/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/12 , A61P29/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P33/06 , A61P35/00 , A61P35/04 , A61P43/00 , C07D499/00 , C07D499/06 , C07D499/40 , C07D499/897 , C07D501/00 , C07D501/08 , C07D501/14 , C07D501/20 , C07K5/06 , C07K5/08 , A61K38/55
摘要： The present invention provides substituted amino bicyclic-.beta.-lactam penam derivatives and substituted amino bicyclic-.beta.-lactam cepham derivatives and their diastereoisomers of general formula (I) as well as compositions containing such compounds, methods of making such compounds, and methods of using such compounds which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis, muscular dystrophy, myocardial infarction, pulmonary emphysema, septic shock, cerebral ischemia, decreased memory function, Alzheimer, cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections and viral infections. In said formula, R is a peptidyl residue of a single natural .alpha.-amino acid selected from a specific group of natural .alpha.-amino acids or a peptidyl residue of a single non-natural amino acid selected from a specified group of non-natural amino acids, in which natural or non-natural peptidyl residue the terminal NH2 group is unsubstituted or substituted once or twice with group R4; wherein R4 is selected from the group consisting of -COOR5, -COR5, -SO2R5, and -COR6; R5 is selected from the group consisting of (i) a C1-C6 alkyl group, (ii) a C2C6 alkenyl group, (iii) a C2-C6 alkenyl group, (iv) a C3-C6 cycloalkyl group, (v) a phenyl group, (vi) a naphthyl group, and (vii) a monocyclic or bicyclic heterocyclic group, which group (i), (ii), (iii), (iv), (v), (vi) or (vii) is unsubstituted or substituted; R6 is an amino group which is unsubstituted or substituted at least once with a C1-C6 alkyl group which is unsubstituted or substituted; R1 is selected from the group consisting of hydrogen, hydroxy, carboxy, -COOR5, -OR7-, -CONHR7, and C1-C6 alkyl, in which the C1-C6 alkyl is unsubstituted or substituted; wherein R7 is selected from the group consisting of: (i) C1-C6 alkyl which is unsubstituted or substituted, (ii) C2-C4 alkenyl which is unsubstitued or substituted, (iii) C2-C4 alkynyl, (iv) C3-C6 cycloalkyl, (v) phenyl which is unsubstituted or substituted, and (vi) a heterocycle which is monocyclic or bicyclic having 1, 2 or 3 heteroatoms selected from the group consisting of N, S, O; R2 and R3 are independently hydrogen or C1-C3 alkyl which is unsubstituted or substituted; n is 0, 1 or 2; and n1 is 0 or 1.

2. 发明专利

CA2266639A1 3,4-DISUBSTITUTED AZETIDIN-2-ONE DERIVATIVES USEFUL AS CYSTEINE PROTEINASE REGULATORS 未知
公开(公告)号：CA2266639A1
公开(公告)日：1998-03-26
申请号：CA2266639
申请日：1997-09-22
申请人： SYNPHAR LAB INC
发明人： GUO DEQI , MICETICH RONALD G , ZHOU NIAN E , SINGH RAJESHWAR
IPC分类号： A61K38/00 , A61P3/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/12 , A61P29/00 , A61P31/12 , A61P33/00 , A61P33/06 , A61P35/04 , C07D205/085 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/08 , A61K31/395
摘要： The present invention is based on the discovery that certain 3,4-disubstituted-azetidin-2-one derivatives exhibit excellent cysteine proteinase inhibitory activity which can be used for treatment of different diseases such as muscular dystrophy, myocardial infarction, bone resorption, arthritis, cancer metastatis, pulmonary emphysema, septic shock, cerebral ischemia, memory function, Alzheimer and cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections, and viral infections. In accordance with the present invention, there is provided a 3,4-disubstituted-azetidin-2-one derivatives of formula (I), wherein R1, R2 and R3 are as defined herein, or a pharmaceutically acceptable salt thereof.

3. 发明专利

ZA9500106B Novel 3-(substituted methyl)-4-oxa-1-azabicyclo[3.2.0] heptan-7-one derivatives useful as antitumor agents 未知
公开(公告)号：ZA9500106B
公开(公告)日：1996-02-07
申请号：ZA9500106
申请日：1995-01-09
申请人： TAIHO PHARMACEUTICAL CO LTD , SYNPHAR LAB INC
发明人： SINGH RAJESHWAR , YAMASHITA TOMOHIRO , FIAKPUI CHARLES , THOMAS GEORGE , HA CHAN , MATSUMOTO HIROSHI , OTANI TOSHIO , OIE SHINJI , MICETICH RONALD
IPC分类号： A61K31/42 , A61P35/00 , C07D503/00 , A61K
CPC分类号： C07D503/00 , Y02P20/55

4. 发明专利

FI950101A 未知
公开(公告)号：FI950101A
公开(公告)日：1995-03-07
申请号：FI950101
申请日：1995-01-09
申请人： SYNPHAR LAB INC , TAIHO PHARMACEUTICAL CO LTD
发明人： SINGH RAJESHWAR , YAMASHITA TOMOHIRO , TEMPEST MARK , MATSUMOTO HIROSHI , OTANI TOSHIO , OIE SHINJI , MICETICH RONALD
IPC分类号： C07D503/00 , A61K31/42 , A61P35/00 , A61K

6. 发明专利

FI932596A0 未知
公开(公告)号：FI932596A0
公开(公告)日：1993-06-07
申请号：FI932596
申请日：1993-06-07
申请人： SYNPHAR LAB INC
发明人： SINGH RAJESHWAR , SINGH INDER PAL , THOMAS GEORGE , SINGH MAYA PRAKASH , MICETICH RONALD GEORGE , FATHI-AFSHAR RAKHSHANDEH , DOERKSEN THOMAS ROGER
IPC分类号： A61K31/435 , A61K31/47 , A61P31/04 , C07D401/14 , C07D471/04 , C07D498/06 , C07D521/00 , C07D

7. 发明专利

NO932033A 未知
公开(公告)号：NO932033A
公开(公告)日：1993-06-03
申请号：NO932033
申请日：1993-06-03
申请人： SYNPHAR LAB INC
发明人： SINGH RAJESHWAR , SINGH INDER PAL , THOMAS GEORGE , SINGH MAYA PRAKASH , MICETIC RONALD GEORGE , FATHI-AFSHAR , EDMONTON AB
IPC分类号： A61K31/435 , A61K31/47 , A61P31/04 , C07D401/14 , C07D471/04 , C07D498/06 , C07D521/00 , C07D498/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D471/04

8. 发明专利

ZA919601B 7-SUBSTITUTED-6-FLUORO-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID COMPOUNDS USEFUL AS ANTIBACTERIAL AGENTS 未知
公开(公告)号：ZA919601B
公开(公告)日：1992-10-28
申请号：ZA919601
申请日：1991-12-05
申请人： SYNPHAR LAB INC
发明人： SINGH RAJESHWAR , RAJESHWAR SINGH , SINGH INDER PAL , INDER PAL SINGH , THOMAS GEORGE , GEORGE THOMAS
IPC分类号： A61K31/435 , A61K31/47 , A61P31/04 , C07D401/14 , C07D471/04 , C07D498/06 , C07D521/00 , C07D , A61K

9. 发明专利

NO305479B1 未知
公开(公告)号：NO305479B1
公开(公告)日：1999-06-07
申请号：NO932033
申请日：1993-06-03
申请人： SYNPHAR LAB INC
发明人： SINGH RAJESHWAR , SINGH INDER PAL , THOMAS GEORGE , SINGH MAYA PRAKASH , MICETICH RONALD GEORGE , FATHI-AFSHAR RAKHSHANDEH , DOERKSEN THOMAS ROGER
IPC分类号： A61K31/435 , A61K31/47 , A61P31/04 , C07D401/14 , C07D471/04 , C07D498/06 , C07D521/00

10. 发明专利

CA2266849A1 4-SUBSTITUTED-3-(2-AMINO-2-CYCLOALKYL METHYL)-ACETAMIDO AZETIDIN-2-ONE DERIVATIVES AS CYSTEINE PROTEINASE REGULATORS 未知
公开(公告)号：CA2266849A1
公开(公告)日：1998-03-26
申请号：CA2266849
申请日：1997-09-23
申请人： SYNPHAR LAB INC , CA NAT RESEARCH COUNCIL
发明人： SINGH RAJESHWAR , ZHOU NIAN E , MICETICH RONALD G , PURISIMA ENRICO O
IPC分类号： A61K38/55 , A61K31/00 , A61K38/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/12 , A61P29/00 , A61P31/04 , A61P31/10 , A61P33/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07K5/06 , C07K5/065 , A61K38/05
摘要： In accordance with the present invention, there are provided 4-substituted-3- (2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives of formula (I), wherein n is 1, 2 or 3; in which R1, R2 and R3 are as defined herein, and salts thereof, which exhibit excellent cysteine proteinase inhibitory activity and which can be used for treatment of different diseases such as muscular dystrophy, myocardial infarction, bone resorption, arthritis, cancer metastasis, pulmonary emphysema, septic shock, cerebral ischemia, memory function, Alzheimer and cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections, and viral infections.

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