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1. 发明专利

ZA200705071B Heterocyclic aspartyl protease inhibitors 未知
公开(公告)号：ZA200705071B
公开(公告)日：2008-11-26
申请号：ZA200705071
申请日：2007-06-12
申请人： SCHERING CORP , PHARMACOPEIA INC
发明人： ZHAONING ZHU , ZHONG-YUE SUN , VOIGT JOHANNES H , SMITH ELIZABETH M , GREENLEE WILLIAM J , JOHN CALDWELL , LINGYAN WANG , ULRICH ISERLOH , LE THUY X H , BABU SURESH D , MORRIS MICHELLE L , GANG QIAN , BRIAN MCKITTRICK , YE YUANZAN C , COREY STRICKLAND , ANDREW STAMFORD , ROBERT MAZZOLA , JARED CUMMING , YUSHENG WU , TAO GUO , SAIONZ KURT W , HUNTER RACHAEL C , HUIZHONG GU , DAWIT TADESSE
IPC分类号： A61K20090101 , C07D20090101
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 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.

2. 发明专利

MY144104A HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 未知
公开(公告)号：MY144104A
公开(公告)日：2011-08-15
申请号：MYPI20052623
申请日：2005-06-09
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
发明人： ZHAONING ZHU , ROBERT MAZZOLA , CALDWELL JOHN P , CUMMING JARED N , LINGYAN WANG , YUSHENG WU , ULRICH ISERLOH , TAO GUO , LE THUY X H , SAIONZ KURT W , BABU SURESH D , MCKITTRICK BRIAN A , HUNTER RACHAEL C , MORRIS MICHELLE L , HUIZHONG GU , GANG QIAN , DAWIT TADESSE , ZHONG-YUE SUN , YE YUANZAN C , VOIGT JOHANNES H , COREY STRICKLAND , SMITH ELIZABETH M , STAMFORD ANDREW W , GREENLEE WILLIAM J
IPC分类号： A61K31/4168
摘要： DISCLOSED ARE COMPOUNDS OF THE FORMULA &Igr;,OR A STEREOISOMER, TAUTOMER, OR PHARMACEUTICALLY ACCEPTABLE SALT OR SOLVATE THEREOF, WHEREIN W IS A BOND, -C(=S)-, -S(O)-, -S(O)₂-, -C(=O)-, -O-, -C(R⁶)(R⁷)-, -N(R⁵)- OR -C(=N(R⁵))-; X IS -O-, -N(R⁵)- OR -C(R⁶)(R⁷) -; PROVIDED THAT WHEN X IS -O-, U IS NOT -O-,-S(O)-, -S(0)₂-, -C(=O)- OR -C(=NR⁵)-; U IS A BOND, -S(O)-, -S(O)₂-, -C(O)-, -O-, -P(O)(OR¹⁵)-, -C(=NR⁵)-, -(C(R⁶) (R ⁷) )B- OR -N(R⁵)-; WHEREIN B IS 1 OR 2; PROVIDED THAT WHEN W IS -S(O)-. -S(O)₂-, -O-,OR-N(R⁵) - U IS NOT -S(O)-, -S(O)₂-, -O-, OR -N(R⁵)-; PROVIDED THAT WHEN X IS - N(R⁵)- AND W IS -S(O)-, -S(O)₂-, -O-, OR -N(R⁵)-, THEN U IS NOT A BOND; AND R¹, R², R³, R⁴, R⁵, R⁶, AND R⁷ ARE AS DEFINED IN THE SPECIFICATION; AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUNDS OF FORMULA 1. 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 &Igr; IN COMBINATION WITH A CHOLINESTERASE INHIBITOR OR A MUSCARINIC M₁ AGONIST OR M₂ ANTAGONIST.

3. 发明专利

ZA200601101B Cyclic amine BACE-1 inhibitors having a heterocyclic substituent 未知
公开(公告)号：ZA200601101B
公开(公告)日：2007-05-30
申请号：ZA200601101
申请日：2006-02-07
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
发明人： CUMMING JARED N , GOUQING LI , ANDREW STAMFORD , VOIGT JOHANNES H , JIANPING PAN , HOBBS DOUGLAS W , LOWRIE JEFFREY F , YING HUANG , ULRICH ISERLOH , COREY STRICKLAND , YUSHENG WU , TAO GUO , LE THUY X H
IPC分类号： C07D20090101 , C07D207/26 , C07D207/277 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R 14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I. Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

4. 发明专利

ZA200604833B Heterocyclic aspartyl protease inhibitors 未知
公开(公告)号：ZA200604833B
公开(公告)日：2007-03-28
申请号：ZA200604833
申请日：2006-06-12
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY INC
发明人： ZHAONING ZHU , BRIAN MCKITTRICK , ZHONG-YUE SUN , YE YUANZAN C , VOIGT JOHANNES H , COREY STRICKLAND , SMITH ELIZABETH M , ANDREW STAMFORD , GREENLEE WILLIAM J , YUSHENG WU , ULRICH ISERLOH , ROBERT MAZZOLA , JOHN CALDWELL , JARED CUMMING , LINGYAN WANG , TAO GUO , LE THUY X H , SAIONZ KURT W , BABU SURESH D , RACHAEL HUNTER
IPC分类号： A61K20090101 , C07D20090101 , C07D233/88 , C07D235/02 , C07D239/22 , C07D271/06 , C07D271/07 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, 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.

5. 发明专利

CO5160344A1 INHIBIDORES DE TRANSFERASA DE PROTEINA FARNESILO 未知
公开(公告)号：CO5160344A1
公开(公告)日：2002-05-30
申请号：CO99078838
申请日：1999-12-16
申请人： SCHERING CORP
发明人： TAVERAS ARTHUR G , DOLL RONALD J , COOPER ALAN B , GUZI TIMOTHY , MALLAMS DINANATTH F ALAN K , GIRIJA VALLABHAN VIYYOOR M , COREY STRICKLAND , KELLY JOSEPH M , JIANPING CHAO
IPC分类号： A61K31/44 , A61K31/445 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00
摘要： Un compuesto de fórmula : o una sal farmacéuticamente aceptable o solvato del mismo donde:uno de a, b, c y d representan N o N+O, y los grupos restantes 1, b, c y d representan CR1 o CR2; o cada uno de a, b, c y d están independientemente seleccionados de CR1 o CR2; cada R1 y cada R2 está independientemente seleccionada de H, halo, -CF3, -OR10, -COR10, -SR10, -S(O)tR11 (donde t es 0,1 ó 2), -N(R10)2, -NO2, -OC(O)R10, -CO2R10, -OCO2R11, -CN, -NR10COOR11, -SR11C(O)OR11, -SR11N(R75)2 (con la condición de que R11 en -SR11N(R75)2 no sea -CH2-) donde cada R75 está independientemente seleccionada de H o -C(O)OR11, benzotriazol-1-iloxi, tetrazol-5-iltio, o tetrazol-5-iltio substituido, alquinilo, alquenilo o alquilo, estando dicho grupo alquilo o alquenilo opcionalmente substituido con halo, -OR10 o -CO2R10;R3 y R4 son igualmente o diferentes y cada uno independientemente representa H, cualquiera de los substituyentes de R1 y R2, o R3 y R4 tomados conjuntamente representan un anillo fusionado C5-C7 saturado o insaturado con el anillo benceno (Anillo III);R5, R6, y R7 cada uno independientemente representan H, -CF3, -COR10, aIquilo o arilo, estando dicho alquilo o arilo están opcionalmente substituidos con -OR10, -SR10, -S(O)tR11, -NR10COOR11, -N(R10)2, -NO2, -COR10, -OCOR10, -OCO2R11, -CO2R10, OPO3R10, o R5 se combina con R5 para representar =O o =S;con la condición de que para los grupos -OR10, -SR10, y -N(R10)2 R10 no sea H;R10 representa H, alquilo, arilo, o aralquilo;R11 representa alquilo o arilo;X representa N, CH o C, y cuando X es C, está presente el enlace opcional (representado por la línea de puntos) con el átomo de carbono 11, y cuando X es CH, está ausente el enlace opcional (representado por la linea de puntos) con el átomo de carbón 11;la línea de puntos entre los átomos de carbono 5 y 6 representa un enlace opcional, de manera que cuando está presente un doble enlace, A y B representan independientemente -R10, halo, -OR11, -OCO2R11 o -OC(O)R10, y cuando no está presente ningún doble enlace entre los átomos de carbono 5 y 6, ...

6. 发明专利

ZA200601097B Cyclic amine BACE-1 inhibitors having a benzamine substituent 未知
公开(公告)号：ZA200601097B
公开(公告)日：2007-05-30
申请号：ZA200601097
申请日：2006-02-07
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
发明人： CUMMING JARED N , ANDREW STAMFORD , VOIGT JOHANNES H , YING HUANG , SAMUEL CHACKALAMANNIL , HOBBS DOUGLAS W , LOWRIE JEFFREY F , BABU SURESH D , ULRICH ISERLOH , COREY STRICKLAND , YUSHENG WU , YAN XIA , TAO GUO , LE THUY X H , SAIONZ KURT W
IPC分类号： A61K20090101 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , C07D20090101 , C07D207/09 , C07D211/26 , C07D217/18 , C07D241/04 , C07D243/08 , C07D401/06 , C07D403/12 , C07D403/14 , C07D413/06 , C07F20090101 , C07F9/38
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &bgr;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

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