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61. 发明专利

OA08617A 未知
公开(公告)号：OA08617A
公开(公告)日：1988-11-30
申请号：OA59144
申请日：1987-06-18
申请人： SCHERING CORP
发明人： HASLANGER MARTIN F , SYBERTZ EDMUND J , NEUSTADT BERNARD R , SMITH ELIZABETH M
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/55 , A61K38/00 , A61K38/22 , A61K38/55 , A61K45/06 , A61P9/12 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/22 , C07C323/25 , C07C323/41 , C07C323/42 , C07C323/56 , C07C323/58 , C07C323/59 , C07C323/60 , C07C325/00 , C07C327/22 , C07C327/32 , C07C329/06 , C07C333/16 , C07D209/14 , C07D209/20 , C07D211/60 , C07D213/83 , C07D233/64 , C07D295/18 , C07D307/54 , C07D307/68 , C07D307/81 , C07D333/24 , C07D333/60 , C07D401/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D487/04 , C07K5/06 , C07K5/062 , C07K5/065 , C07K14/575 , C07K14/81 , A61K37/64 , C07C101/06 , C07C101/08 , C07C149/243
摘要： The method of treating hypertension with neutral metalloendopeptidase (NMEP) inhibitors, NMEP inhibitors in combination with atrial peptides, and NMEP inhibitors in combination with angiotensin converting enzyme inhibitors, as well as pharmaceutical compositions therefor, are disclosed.

62. 发明专利

CA1244041A PROCESS FOR THE PREPARATION OF CIS, ENDO- OCTAHYDROCYCLOPENTA[B]PYRROLE-2-CARBOXYLATE 未知
公开(公告)号：CA1244041A
公开(公告)日：1988-11-01
申请号：CA487583
申请日：1985-07-26
申请人： SCHERING CORP
发明人： GOLD ELIJAH H , NEUSTADT BERNARD R , SMITH ELIZABETH M
IPC分类号： C07K14/81 , C07D209/52 , C07K1/02 , C07K5/02 , C07K5/06 , C07D401/12 , C07D403/12
摘要： Novel process for the preparation of cis,endo-octahydrocyclopenta ¢b!pyrrole-2-carboxylate (IIIa) IIIa wherein R6 is hydroxy, lower alkoxy, lower alkenoxy, dilower alkylamino lower alkoxy, acylamino lower alkoxy, acyloxy lower alkoxy, aryloxy, arylloweralkoxy, amino, lower alkylamino, dilower alkylamino, hydroxyamino, aryllower alkylamino, or substituted aryloxy or substituted aryllower alkoxy wherein the substituent is methyl, halo or methoxy, which comprises catalytic reduction of compound II, II which further may comprise preparing the compound of formula II by the reaction of a halo pyruvate ester (V) V with benzyliminocyclopentane. Compounds IIIa are useful intermediates for the preparation of certain ACE-inhibitors

63. 发明专利

AU7445887A NEUTRAL METALLOENDOPEPTIDASE INHIBITOR 未知
公开(公告)号：AU7445887A
公开(公告)日：1987-12-24
申请号：AU7445887
申请日：1987-06-18
申请人： SCHERING CORP
发明人： HASLANGER MARTIN F , SYBERTZ EDMUND J JR , NEUSTADT BERNARD R , SMITH ELIZABETH M
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/55 , A61K38/00 , A61K38/22 , A61K38/55 , A61K45/06 , A61P9/12 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/22 , C07C323/25 , C07C323/41 , C07C323/42 , C07C323/56 , C07C323/58 , C07C323/59 , C07C323/60 , C07C325/00 , C07C327/22 , C07C327/32 , C07C329/06 , C07C333/16 , C07D209/14 , C07D209/20 , C07D211/60 , C07D213/83 , C07D233/64 , C07D295/18 , C07D307/54 , C07D307/68 , C07D307/81 , C07D333/24 , C07D333/60 , C07D401/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D487/04 , C07K5/06 , C07K5/062 , C07K5/065 , C07K14/575 , C07K14/81 , C07K5/08 , A61K31/66 , C07C153/017 , C07C149/41 , C07F9/65
摘要： The method of treating hypertension with neutral metalloendopeptidase (NMEP) inhibitors, NMEP inhibitors in combination with atrial peptides, and NMEP inhibitors in combination with angiotensin converting enzyme inhibitors, as well as pharmaceutical compositions therefor, are disclosed.

64. 发明专利

AU554362B2 CARBOXYALKYL DIPEPTIDES 未知
公开(公告)号：AU554362B2
公开(公告)日：1986-08-21
申请号：AU7661481
申请日：1981-10-20
申请人： SCHERING CORP
发明人： NEUSTADT BERNARD R , GOLD ELIJAH H , SMITH ELIZABETH M
IPC分类号： C12N9/99 , A61K38/00 , A61P9/12 , A61P43/00 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , A61K37/02
摘要： Disclosed are novel carboxyalkyl dipeptides which are useful as inhibitors of angiotensinconverting enzyme and as antihypertensive agents, having the formula … … and the pharmaceuticallv acceptable salts thereof, wherein R and R are for example hydroxy, lower alkoxy or aryllower-4 alkoxy; R is for example hydrogen, alkyl, lower alkoxy or aryloxy; R and R are the same or different and are hydrogen or lower alkyl; R is for example lower alkyl or phenyl lower alkyl; R and R are selected from hydrogen, lower alkyl and Z, or R and R taken together form a group represented by Q, U, V, Y, D or E wherein … … wherein X and X independent of each other are O, S or CH2, R and R independent of each other are lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl having 3 to 8 carbon atoms, hydroxy lower alkyl or -(CH2)nAr, wherein n is 0, 1. 2 or 3 or R and R taken together form a bridge W, wherein W is a single bond or a methylene bridge or a substituted methylene bridge when at least one of X and X is methylene, or W is an alkylene or substituted alkylene bridge having 2 or 3 carbon atoms; with the proviso that at least one of R and R is Z; … … wherein L is O or S.… The compounds can be prepared according to known methods such as for example by condensation of an aminoacid XXI with an aminoacid XVII … …

65. 发明专利

AT20469T 未知
公开(公告)号：AT20469T
公开(公告)日：1986-07-15
申请号：AT81108348
申请日：1981-10-15
申请人： SCHERING CORP
发明人： NEUSTADT BERNARD R , GOLD ELIJAH H , SMITH ELIZABETH M
IPC分类号： C12N9/99 , A61K38/00 , A61P9/12 , A61P43/00 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , A61K37/02
摘要： Disclosed are novel carboxyalkyl dipeptides which are useful as inhibitors of angiotensinconverting enzyme and as antihypertensive agents, having the formula … … and the pharmaceuticallv acceptable salts thereof, wherein R and R are for example hydroxy, lower alkoxy or aryllower-4 alkoxy; R is for example hydrogen, alkyl, lower alkoxy or aryloxy; R and R are the same or different and are hydrogen or lower alkyl; R is for example lower alkyl or phenyl lower alkyl; R and R are selected from hydrogen, lower alkyl and Z, or R and R taken together form a group represented by Q, U, V, Y, D or E wherein … … wherein X and X independent of each other are O, S or CH2, R and R independent of each other are lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl having 3 to 8 carbon atoms, hydroxy lower alkyl or -(CH2)nAr, wherein n is 0, 1. 2 or 3 or R and R taken together form a bridge W, wherein W is a single bond or a methylene bridge or a substituted methylene bridge when at least one of X and X is methylene, or W is an alkylene or substituted alkylene bridge having 2 or 3 carbon atoms; with the proviso that at least one of R and R is Z; … … wherein L is O or S.… The compounds can be prepared according to known methods such as for example by condensation of an aminoacid XXI with an aminoacid XVII … …

66. 发明专利

DE3360065D1 CARBOXYALKYL DIPEPTIDES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：DE3360065D1
公开(公告)日：1985-03-28
申请号：DE3360065
申请日：1983-03-02
申请人： SCHERING CORP
发明人： SMITH ELIZABETH M , WITKOWSKI JOSEPH T , DOLL RONALD J , GOLD ELIJAH H , NEUSTADT BERNARD R , YEHASKEL ALBERT S
IPC分类号： A61K38/00 , C07K5/02 , C07K5/068 , C07K5/06 , A61K37/02

67. 发明专利

ZA8301844B CARBOXYALKYL DIPEPTIDES,PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：ZA8301844B
公开(公告)日：1984-06-27
申请号：ZA8301844
申请日：1983-03-16
申请人： SCHERING CORP
发明人： SMITH ELIZABETH M , NEUSTADT BERNARD R , WITKOWSKI JOSEPH T , YEHASKEL ALBERT S , DOLL RONALD J , GOLD ELIJAH H
IPC分类号： A61K20060101 , C07C20060101 , C07D20060101 , A61K , C07C , C07D

68. 发明专利

ZA8107261B CARBOXYALKYL DIPEPTIDES,PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：ZA8107261B
公开(公告)日：1982-09-29
申请号：ZA8107261
申请日：1981-10-20
申请人： SCHERING CORP
发明人： NEUSTADT BERNARD R , GOLD ELIJAH H , SMITH ELIZABETH M
IPC分类号： C07D209/44 , A61K38/00 , A61K38/55 , A61P9/12 , C07D209/52 , C07D215/48 , C07D225/02 , C07D267/22 , C07D339/08 , C07D491/048 , C07D491/052 , C07D491/113 , C07D495/10 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C12N9/99 , C07C , A61K
CPC分类号： C07K5/0222 , A61K38/00 , C07K5/022

69. 发明专利

NO813546L 未知
公开(公告)号：NO813546L
公开(公告)日：1982-04-26
申请号：NO813546
申请日：1981-10-21
申请人： SCHERING CORP
发明人： NEUSTADT BERNARD R , GOLD ELIJAH H , SMITH ELIZABETH M
IPC分类号： C12N9/99 , A61K38/00 , A61P9/12 , A61P43/00 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C07C
摘要： Disclosed are novel carboxyalkyl dipeptides which are useful as inhibitors of angiotensinconverting enzyme and as antihypertensive agents, having the formula … … and the pharmaceuticallv acceptable salts thereof, wherein R and R are for example hydroxy, lower alkoxy or aryllower-4 alkoxy; R is for example hydrogen, alkyl, lower alkoxy or aryloxy; R and R are the same or different and are hydrogen or lower alkyl; R is for example lower alkyl or phenyl lower alkyl; R and R are selected from hydrogen, lower alkyl and Z, or R and R taken together form a group represented by Q, U, V, Y, D or E wherein … … wherein X and X independent of each other are O, S or CH2, R and R independent of each other are lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl having 3 to 8 carbon atoms, hydroxy lower alkyl or -(CH2)nAr, wherein n is 0, 1. 2 or 3 or R and R taken together form a bridge W, wherein W is a single bond or a methylene bridge or a substituted methylene bridge when at least one of X and X is methylene, or W is an alkylene or substituted alkylene bridge having 2 or 3 carbon atoms; with the proviso that at least one of R and R is Z; … … wherein L is O or S.… The compounds can be prepared according to known methods such as for example by condensation of an aminoacid XXI with an aminoacid XVII … …

70. 发明专利

BRPI0807547A2 未知
公开(公告)号：BRPI0807547A2
公开(公告)日：2014-06-17
申请号：BRPI0807547
申请日：2008-02-20
申请人： SCHERING CORP , STRICKLAND COREY , SMITH ELIZABETH M , STAMFORD ANDREW , GREENLEE WILLIAM J , ROBERT D MAZZOLA JR , CALDWELL JOHN
发明人： ZHU ZHAONING , STRICKLAND COREY , SMITH ELIZABETH M , STAMFORD ANDREW , GREENLEE WILLIAM J , MAZZOLA ROBERT D , CALDWELL JOHN , CUMMING JARED N , WANG LINGYAN , WU YUSHENG , ISERLOH ULRICH , LIU XIAOXIANG , HUANG YING , LI GUOQING , PAN JIANPING , MISIASZEK JEFFREY A , GUO TAO , LE THUY X H , SAIONZ KURT W , LAI GAIFA , DUO JINGQI , QU CHUANXING , SHAO YUEFEI , BABU SURESH D , HUNTER RACHAEL C , MORRIS MICHELLE L , GU HUIZHONG , QIAN GANG , TADESSE DAWIT
IPC分类号： C07D233/88 , A61K31/513 , A61P25/28 , C07D239/22 , C07D401/06 , C07D401/10 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

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