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81. 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 … …

82. 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.

83. 发明专利

AT495154T 未知
公开(公告)号：AT495154T
公开(公告)日：2011-01-15
申请号：AT05010936
申请日：2000-05-01
申请人： SCHERING CORP
发明人： BAROUDY BAHIGE M , CLADER JOHN W , JOSIEN HUBER B , MCCOMBIE STUART W , MCKITTRICK BRIAN A , MILLER MICHAEL W , NEUSTADT BERNARD R , PALANI ANANDAN , STEENSMA RUO , TAGAT JAYARAM R , VICE SUSAN F , LAUGHLIN MARK A , SMITH ELIZABETH M , GILBERT ERIC , LABROLI MARC A
IPC分类号： C07D211/58 , C07D401/04 , A61K31/496 , A61K31/497 , A61K31/506 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/00 , A61P37/08 , A61P43/00 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , G01F1/46
摘要： The use is described of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R 1 is hydrogen or alkyl; R 2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R 3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R 4 , R 5 and R 7 are hydrogen or alkyl; R 6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

84. 发明专利

DE602006018456D1 HERSTELLUNG UND VERWENDUNG VON VERBINDUNGEN ALS ASPARTYLPROTEASEHEMMER 未知
公开(公告)号：DE602006018456D1
公开(公告)日：2011-01-05
申请号：DE602006018456
申请日：2006-06-12
申请人： SCHERING CORP
发明人： MCKITTRICK BRIAN , ZHU ZHAONING , STAMFORD ANDREW , SMITH ELIZABETH M
IPC分类号： C07D251/10 , A61K31/53 , A61P9/00

85. 发明专利

DE602006017073D1 未知
公开(公告)号：DE602006017073D1
公开(公告)日：2010-11-04
申请号：DE602006017073
申请日：2006-06-12
申请人： SCHERING CORP
发明人： ZHU ZHAONING , MCKITTRICK BRIAN , STAMFORD ANDREW W , HUANG YING , SMITH ELIZABETH M
IPC分类号： C07D487/04 , A61K31/395 , A61P9/00 , A61P25/00 , A61P25/28 , A61P31/18 , C07D498/04

87. 发明专利

CA2353063C BENZIMIDAZOLE COMPOUNDS THAT ARE VITRONECTIN RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2353063C
公开(公告)日：2009-06-16
申请号：CA2353063
申请日：1999-11-29
申请人： SCHERING CORP
发明人： NEUSTADT BERNARD R , SMITH ELIZABETH M
IPC分类号： C07D235/14 , C07D235/16 , A61K31/4184 , A61P9/10 , A61P19/10 , A61P27/02 , A61P35/00 , A61P43/00 , C07D235/10 , C07D405/12
摘要： The present invention provides compounds having formula (I) wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with th e proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y' each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, -CF3, and -C(O)OH; R1, R2, R3 and R4 are H or specified substituents; R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from H or C1-C3 alkyl; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Al so provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.

88. 发明专利

AU2003210865B2 Gamma secretase inhibitors 未知
公开(公告)号：AU2003210865B2
公开(公告)日：2008-01-31
申请号：AU2003210865
申请日：2003-02-05
申请人： PHARMACOPEIA INC , SCHERING CORP
发明人： ASBEROM THEODROS , SMITH ELIZABETH M , PISSARNITSKI DMITRI A , CLADER JOHN W , GUO TAO , JOSIEN HUBERT B , HOBBS DOUGLAS W
IPC分类号： C07D491/113 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P25/18 , A61P25/28 , A61P43/00 , C07D211/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, -X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R 3 and each R 3A are independently H, or alkyl; R 11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

90. 发明专利

AU2006259574A1 The preparation and use of compounds as aspartyl protease inhibitors 未知
公开(公告)号：AU2006259574A1
公开(公告)日：2006-12-28
申请号：AU2006259574
申请日：2006-06-12
申请人： SCHERING CORP
发明人： SMITH ELIZABETH M , STAMFORD ANDREW , ZHU ZHAONING , MCKITTRICK BRIAN
IPC分类号： A61K31/53 , A61P9/00 , C07D251/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond; X is -N(R 1 )- or -C(R 6 )(R 7 )-; Y is -S(O) 2 -, -C(=O)-, or -C(R 6' R 7' )-; ------ is a single or double bond and R, R 1 , R 2 , R 3 , R 4 , R 3' , R 4' , R 5 , R 6 , R 6' , R 7 and R 7' are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method 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 antagonist.

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