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21. 发明专利

AU2006214380A1 Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity 未知
公开(公告)号：AU2006214380A1
公开(公告)日：2006-08-24
申请号：AU2006214380
申请日：2006-02-14
申请人： PHARMACOPEIA INC , SCHERING CORP
发明人： SHANKAR BANDARPALLE B , ROSENBLUM STUART B , YU WENSHENG , WONG MICHAEL K C , DONG GUIZHEN , MCGUINNESS BRIAN F , SHAO YUEFEI , KOZLOWSKI JOSEPH A , ZENG QINGBEI , BALDWIN JOHN J , HOBBS DOUGLAS W , JIANG YUEHENG , KIM SEONG HEON , ZAWACKI LISA GUISE , ANILKUMAR GOPINADHAN N , SHIH NENG-YANG
IPC分类号： C07D401/12 , A61K31/445 , A61K31/495 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

22. 发明专利

ZA200403685B Cannabinoid receptor ligands. 未知
公开(公告)号：ZA200403685B
公开(公告)日：2005-05-23
申请号：ZA200403685
申请日：2004-05-13
申请人： SCHERING CORP
发明人： FRIARY RICHARD J , SHANKAR BANDARPALLE B , ZHOU GUOWEL , SHIH NENG-YANG , CHEN LEI , KOZLOWSKI JOSEPH A , WONG MICHAEL K C , LAVEY BRIAN J , TONG LING , SHU YOUHENG
IPC分类号： A61K31/445 , A61K31/4535 , A61K31/454 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/08 , C07D211/26 , C07D211/96 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D
摘要： There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.

23. 发明专利

PE07542004A1 LIGANDOS DE RECEPTORES CANABINOIDES 未知
公开(公告)号：PE07542004A1
公开(公告)日：2004-11-20
申请号：PE0007742003
申请日：2003-08-05
申请人： SCHERING CORP
发明人： KOZLOWSKI JOSEPH A , LAVEY BRIAN J , RIZVI RAZIA K , SHANKAR BANDARPALLE B , WONG MICHAEL K , SPITLER JAMES M , TONG LING , WOLIN RONALD L , SHIH NENG-YANG
IPC分类号： C07D295/08 , A61K31/12 , A61K31/137 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/235 , A61K31/277 , A61K31/381 , A61K31/4164 , A61K31/44 , A61K31/4402 , A61K31/495 , A61K31/5375 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/00 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C31/24 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C323/40 , C07C323/41 , C07C323/56 , C07C323/65 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/36 , C07D233/42 , C07D233/84 , C07D239/38 , C07D295/18 , C07D295/20 , C07D307/64 , C07D333/20 , C07D333/34 , C07D333/38
CPC分类号： C07D213/70 , C07C31/24 , C07C317/22 , C07C317/32 , C07C317/36 , C07C317/44 , C07C323/41 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/36 , C07D233/42 , C07D233/84 , C07D239/38 , C07D307/64 , C07D333/20 , C07D333/34 , C07D333/38
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES H, ALQUILO, HALOALQUILO C1-C6, CICLOALQUILO, ENTRE OTROS; R2 ES H, ALQUILO C1-C6; R3 ES 1-3 SUSTITUYENTES COMO H, ALQUILO C1-C6, F, CF3, ENTRE OTROS; R4 ES H, ALQUILO C1-C6, ALCOXI C1-C6, ENTRE OTROS; R5 ES H, ALQUILO C1-C6; R6 ES H, ALQUILO C1-C6; O R5 Y R6 JUNTO AL CARBONO AL QUE SE UNEN FORMAN UN CARBONILO; L1 ES -C(R2)2-, -C(0)-, -CHOR2-, ENTRE OTROS; L2 ES UN ENLACE COVALENTE, X ES H, HALOGENO, CF3, ENTRE OTROS; Z E Y SON CADA UNO UN ENLACE COVALENTE, -CH2, -SO2, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON LIGANDOS DE RECEPTORES CANABINOIDES (CB2) CON ACTIVIDAD ANTIINFLAMATORIA E INMUNOMODULADORA

24. 发明专利

CA2519401A1 CANNABINOID RECEPTOR LIGANDS 未知
公开(公告)号：CA2519401A1
公开(公告)日：2004-10-07
申请号：CA2519401
申请日：2004-03-18
申请人： SCHERING CORP
发明人： SHANKAR BANDARPALLE B , RIZVI RAZIA K , KOZLOWSKI JOSEPH A , SHIH NENG-YANG
IPC分类号： C07C317/14 , C07C317/22 , C07C317/36 , C07D209/30 , C07D211/54 , C07D213/71 , C07D213/80 , C07D213/89 , C07D239/38 , C07D295/205 , C07D307/64 , C07D333/34 , C07D401/12 , C07D405/12 , C07D493/08 , A61K31/10 , C07D413/12 , A61K31/136 , C07D307/82
摘要： There are disclosed compounds of the formula (I) a pharmaceutically acceptab le salt or solvate of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.

25. 发明专利

CA2494827A1 CANNABINOID RECEPTOR LIGANDS 未知
公开(公告)号：CA2494827A1
公开(公告)日：2004-02-19
申请号：CA2494827
申请日：2003-08-05
申请人： SCHERING CORP
发明人： SHIH NENG-YANG , TONG LING , SPITLER JAMES M , WOLIN RONALD , KOZLOWSKI JOSEPH A , SHANKAR BANDARPALLE B , RIZVI RAZIA K , LAVEY BRIAN J , WONG MICHAEL K
IPC分类号： C07D295/08 , A61K31/12 , A61K31/137 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/235 , A61K31/277 , A61K31/381 , A61K31/4164 , A61K31/44 , A61K31/4402 , A61K31/495 , A61K31/5375 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/10 , A61P21/04 , A61P25/00 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C31/24 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C323/40 , C07C323/41 , C07C323/56 , C07C323/65 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/36 , C07D233/42 , C07D233/84 , C07D239/38 , C07D295/18 , C07D295/20 , C07D307/64 , C07D333/20 , C07D333/34 , C07D333/38 , C07C29/12
摘要： The invention relates to compounds of the formula, a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity . Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.

28. 发明专利

PE20030720A1 LIGANDOS DE LOS RECEPTORES DE LOS CANNABINOIDES 未知
公开(公告)号：PE20030720A1
公开(公告)日：2003-08-29
申请号：PE2002001100
申请日：2002-11-13
申请人： SCHERING CORP
发明人： SHIH NENG-YANG , KOZLOWSKI JOSEPH A , FRIARY RICHARD J , SHANKAR BANDARPALLE B , WONG MICHAEL K C , CHEN LEI , SHU YOUHENG , ZHOU GUOWEI , TONG LING , LAVEY BRIAN J
IPC分类号： A61K31/445 , A61K31/4535 , A61K31/454 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/08 , C07D209/04 , C07D211/26 , C07D211/96 , C07D213/62 , C07D213/89 , C07D239/10 , C07D307/34 , C07D333/34 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： SE REFIERE A LIGANDOS DE LOS RECEPTORES DE CANNABINOIDES DE FORMULA I DONDE L1 ES UN ENLACE COVALENTE, -CH2-, -C(O), -C(O)O-, SO2, -S-, ENTRE OTROS; L2 ES -CH2-, -C(H)(ALQUIL)-, -C(ALQUIL)2-, -C(O)-, -SO-, ENTRE OTROS; L3 ES UN ENLACE COVALENTE, -C(O)-, -S(O2)-; R1 ES H, HALOGENO, ALQUILO, HALOALQUILO, CICLOALQUILO, CICLOALQUILALQUILO, HETEROCICLILALQUILO, -CHR7-, ENTRE OTROS; CON LA CONDICION DE QUE CUANDO R1 ES HALO, L1 ES UN ENLACE COVALENTE, CUANDO R1 ES -NHR7, L1 ES UN ENLACE COVALENTE, -CH2-, -C(O)-, SO2, -SO-, ENTRE OTROS; R2 ES H, OH, HALO, -CF3, ALCOXI, ALQUILO, ENTRE OTROS; R3 Y R4 SON H, ALQUILO; R3 Y R4 TOMADOS CONJUNTAMENTE FORMAN UN GRUPO CARBONILO ES DECIR C(=O); R5 ES H, ALQUILO; R6 ES H, ALQUILO, HALOALQUILO, CICLOALQUILO, NHR7, N(R7)2, ARILO, HETEROARILO, ENTRE OTROS; R7 ES H, ALQUILO, HALOALQUILO, CICLOALQUILO, HETEROCICLILALQUILO, ENTRE OTROS; A ES FENILO, NAFTILO, PIRIDILO, TIENILO, TIAZOLILO, INDOLILO, QUINOLILO, ISOQUINOLILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS PRESENTAN UNA ACTIVIDAD ANTIINFLAMATORIA E INMUNOMODULADORA

29. 发明专利

NO964008L 未知
公开(公告)号：NO964008L
公开(公告)日：1996-11-22
申请号：NO964008
申请日：1996-09-24
申请人： SCHERING CORP
发明人： KIRKUP MICHAEL P , DUGAR SUNDEEP , SHANKAR BANDARPALLE B
IPC分类号： A61K31/395 , A61K31/397 , A61P3/06 , A61P9/10 , C07B53/00 , C07C227/32 , C07C229/34 , C07C311/06 , C07C311/19 , C07C311/37 , C07C319/20 , C07C323/62 , C07D205/08
摘要： Substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 is R3-substituted aryl; Ar2 is R4-substituted aryl; Ar3 is R5-substituted aryl; Y and Z are independently -CH2-, -CH(lower alkyl)- or -C(dilower alkyl)-; A is -O-, -S-, -S(O)- or -S(O)2-; R1 is -OR6, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R2 is hydrogen, lower alkyl or aryl; or R1 and R2 together are =O; q is 1, 2 or 3; p is 0, 1,2, 3 or 4; R5 is 1-3 substitutes independently selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR9, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2-lower alkyl, -NR6SO2-aryl, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2-alkyl, S(O)0-2-aryl, -O(CH2)1-10-COOR6, -O(CH2)0-10CONR6R7, o-halogeno, m-halogeno, o-lower alkyl, m-lower alkyl, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R3 and R4 are 1-3 substituents independently selected from R5, hydrogen, p-lower alkyl, aryl, -NO2, CF3 and p-halogeno; R6, R7 and R8 are hydrogen, lower alkyl, aryl or aryl-substituted lower alkyl; and R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, pharmaceutical compositions containing them, the combination of a substituted azetidinone and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis, novel intermediates and methods for preparing said intermediates.

30. 发明专利

FI963817A 未知
公开(公告)号：FI963817A
公开(公告)日：1996-09-25
申请号：FI963817
申请日：1996-09-25
申请人： SCHERING CORP
发明人： KIRKUP MICHAEL P , DUGAR SUNDEEP , SHANKAR BANDARPALLE B
IPC分类号： A61K31/395 , A61K31/397 , A61P3/06 , A61P9/10 , C07B53/00 , C07C227/32 , C07C229/34 , C07C311/06 , C07C311/19 , C07C311/37 , C07C319/20 , C07C323/62 , C07D205/08 , C07D
摘要： Substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 is R3-substituted aryl; Ar2 is R4-substituted aryl; Ar3 is R5-substituted aryl; Y and Z are independently -CH2-, -CH(lower alkyl)- or -C(dilower alkyl)-; A is -O-, -S-, -S(O)- or -S(O)2-; R1 is -OR6, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R2 is hydrogen, lower alkyl or aryl; or R1 and R2 together are =O; q is 1, 2 or 3; p is 0, 1,2, 3 or 4; R5 is 1-3 substitutes independently selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR9, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2-lower alkyl, -NR6SO2-aryl, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2-alkyl, S(O)0-2-aryl, -O(CH2)1-10-COOR6, -O(CH2)0-10CONR6R7, o-halogeno, m-halogeno, o-lower alkyl, m-lower alkyl, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R3 and R4 are 1-3 substituents independently selected from R5, hydrogen, p-lower alkyl, aryl, -NO2, CF3 and p-halogeno; R6, R7 and R8 are hydrogen, lower alkyl, aryl or aryl-substituted lower alkyl; and R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, pharmaceutical compositions containing them, the combination of a substituted azetidinone and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis, novel intermediates and methods for preparing said intermediates.

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