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1. 发明申请

WO2006069153A2 VITAMIN D RECEPTOR MODULATORS 审中-公开
标题翻译：维生素D受体调节剂
公开(公告)号：WO2006069153A2
公开(公告)日：2006-06-29
申请号：PCT/US2005/046360
申请日：2005-12-19
申请人： ELI LILLY AND COMPANY , GOSSETT, Lynn, Stacy , LOPEZ, Jose, Eduardo , WARSHAWSKY, Alan, M. , YEE, Ying, Kwong
发明人： GOSSETT, Lynn, Stacy , LOPEZ, Jose, Eduardo , WARSHAWSKY, Alan, M. , YEE, Ying, Kwong
IPC分类号： C07C65/40 , C07C65/24 , A61K31/165 , A61K31/19 , A61P3/14
CPC分类号： C07C235/42 , C07C65/24 , C07C65/40 , C07C217/80 , C07C271/30
摘要： The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, Z P , L P1 , L P2 L NP , RP 3 , RN, and Z NP are defined herein, their preparation, pharmaceutical compositions, and methods of use.
摘要翻译：本发明涉及式（I）的新型非异构体苯基 - 萘化合物：其中R，R 1，R L，R 1，L，P 1，本文定义了本文中定义的本文所述的其制备方法，药物组合物和/或制备方法使用方法。

2. 发明申请

WO2007087488A3 INDOLE SULFONAMIDE MODULATORS OF PROGESTERONE RECEPTORS 审中-公开
公开(公告)号：WO2007087488A3
公开(公告)日：2007-08-02
申请号：PCT/US2007/060626
申请日：2007-01-17
申请人： ELI LILLY AND COMPANY , BLEISCH, Thomas, John , CLARKE, Christian, Alexander , DODGE, Jeffrey, Alan , JONES, Scott, Alan , LOPEZ, Jose, Eduardo , LUGAR, Charles, Willis, III , MUEHL, Brian, Stephen , RICHARDSON, Timothy, Ivo , YEE, Ying, Kwong , YU, Kuo-long
发明人： BLEISCH, Thomas, John , CLARKE, Christian, Alexander , DODGE, Jeffrey, Alan , JONES, Scott, Alan , LOPEZ, Jose, Eduardo , LUGAR, Charles, Willis, III , MUEHL, Brian, Stephen , RICHARDSON, Timothy, Ivo , YEE, Ying, Kwong , YU, Kuo-long
IPC分类号： C07D209/10 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/24 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , A61K31/404 , A61P35/00
摘要： Compounds of Formula (I), wherein n is 1 or 2, and R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, their preparation, pharmaceutical compositions, and methods of use are disclosed.

3. 发明申请

WO2004093872A1 3-OXO-1, 3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS 审中-公开
标题翻译： 3-氧代-1,3-二氢吲哚-2-羧酸酰胺衍生物作为磷脂酶抑制剂
公开(公告)号：WO2004093872A1
公开(公告)日：2004-11-04
申请号：PCT/US2004/006092
申请日：2004-03-25
申请人： ELI LILLY AND COMPANY , EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
发明人： EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
IPC分类号： A61K31/416
CPC分类号： C07D231/56 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C 5 -C 13 alky1;:C,-C, 2 haloalkyl, C 4 C,2alkenyl, C 4 -C 12 alkynyl, or C,- C5alkylcycloalkyl, C3-C8cycloalkyl, C, C 5 alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with onf to three substituents independently selected from C,-C 8 a)kyl, C,-C 8 haloalkyl,`C 2 -C B alkenyl, C2-C 8 a)kynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (C}12) m 000C,-Csalkyl, (CH2) m NR a R b , and C,C 4 alkylcycloalkyl; wherein Wand R b are independently selected from hydrogen, C,C B alkyl, C 2 -C B alkenyl, C 2 -C B alkynyl, and C,- C5alkylcycloalkyl; R 2 is hydrogen; R3, R4 , R5, and R6, are independently selected from hydrogen, C,-C 12 alkyl, C 2 C,2haloalkyl, C2-C,2 alkenyl, C 2 -C 12 alkynyl, C,-C t2 alkylaryl, C,-C 12 alkylcyclohexyl, C, C 12 alkylcyclopentyl, C,-C 1z alkylheterocyclic, (CH2) m 000H, (CH2) m C0(C,-C,o)alkyl, (CH 2 ) m COO(C,-C, o )alkyl, (CH2) m COO(C,-C, o )alkylaryl, C,-C, o alkylamino, halo, (CH 2 ) m CONH 2 , (CH 2 ) r CONRaR b , phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from C B alkyl, C,-C B haloalkyl, C 2 -C B alkenyl, C Z C B alkynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (CH2) m 000C,-Csalkyl, and C,-C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,-C lo alkyl, C,C, o haloalkyl, C 2 -C, o alkenyl, C 2 -C, o alkynyl, C,-C 6 alkylaryl, C,-C 6 alkylcyclohexyl, C - C 6 aikylcyclopentyl, C,-C 6 alkylheterocyclic, or aryl; or a pharmaceutically acceptable sal lvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.
摘要翻译：本发明提供式I（1）的化合物，其中： R 5选自C 5 -C 13烷基; C 1 -C 2卤代烷基，C 4 -C 2烯基，C 4 -C 12炔基或C 1 -C 5烷基环烷基，C 3 -C 8环烷基，C 5 C 5烷基杂环和芳基，其中环烷基，环烯基，杂环和芳基取代基任选被至少三个独立地选自C 1 -C 8烷基，C 1 -C 8卤代烷基，C 2 -C 12链烯基，C 2 -C 8α-炔基，苯基，苄基，羟基，C - C5烷氧基，（C）12）m000C，-Cs烷基，（CH2）mNRaRb和C，C4烷基环烷基; 其中W 1和R 2独立地选自氢，C 1 -C 8烷基，C 2 -C 12链烯基，C 2 -C 12炔基和C 1 -C 5烷基环烷基; R2是氢; R 3，R 4，R 5和R 6独立地选自氢，C 1 -C 12烷基，C 2 C 2卤代烷基，C 2 -C 2烯基，C 2 -C 12炔基，C 1 -C 12烷基芳基，C 1 -C 12烷基环己基，C 12 C 12烷基环戊基，C ，（CH 2）m COO（C 1 -C 6）烷基，（CH 2）m COO（C 1 -C 10）烷基，（CH 2）m COO（C 1 -C 6）烷基芳基，C 1 -C 8烷基氨基，卤素，（CH 2）m CONH 2，（CH 2）r CONR a R b，苯基或芳基，其中每个苯基或芳基任选地被一至三个独立地选自C烷基，C C 1 -C 6烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，并且其中m为0,1,2或3; R 7选自氢，C 1 -C 4烷基，C，C，卤代烷基，C 2 -C，链烯基，C 2 -C 6炔基，C 1 -C 6烷基芳基，C 1 -C 6烷基环己基，C 1 -C 6烷基环戊基，C 1 -C 6烷基环戊基， C6烷基杂环或芳基; 或其药学上可接受的盐酸盐以及用于抑制肝脂肪酶和/或内皮脂肪酶活性用于治疗，改善或预防肝脂肪酶和/或内皮脂肪酶介导的疾病的用途。

4. 发明申请

WO2004094394A1 BENZISOTHIAZOL-3-ONE-CARBOXYLIC ACID AMIDES AS PHOSPHOLIPASE INHIBITORS 审中-公开
标题翻译：苯并噻唑-3-酮羧酸作为磷脂酶抑制剂
公开(公告)号：WO2004094394A1
公开(公告)日：2004-11-04
申请号：PCT/US2004/006094
申请日：2004-03-25
申请人： ELI LILLY AND COMPANY , EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
发明人： EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
IPC分类号： C07D275/04
CPC分类号： C07D275/04 , C07D417/12
摘要： A novel class of benzisothiazole-3(2H)-one compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases. (I)
摘要翻译：公开了一类新的苯并异噻唑-3（2H） - 酮化合物，同时使用这些化合物抑制肝脂肪酶和/或内皮脂肪酶活性，用于治疗，改善或预防肝脂肪酶和/或内皮脂肪酶介导的疾病。（一世）

5. 发明申请

WO2004094393A1 PHOSPHOLIPASE INHIBITORS 审中-公开
标题翻译：磷脂抑制剂
公开(公告)号：WO2004094393A1
公开(公告)日：2004-11-04
申请号：PCT/US2004/006095
申请日：2004-03-25
申请人： ELI LILLY AND COMPANY , EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
发明人： EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
IPC分类号： C07D261/20
CPC分类号： C07D261/20
摘要： A novel class of 3-oxo-3 H -benzo[ d ]isoxazole carboxamide compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases.
摘要翻译：公开了一类新的3-氧代-3H-苯并[d]异恶唑甲酰胺化合物，同时使用这些化合物抑制肝脂肪酶和/或内皮脂肪酶活性用于治疗，改善或预防肝脂肪酶和/或内皮脂肪酶介导的疾病。

6. 发明申请

WO2003035629A1 THIOPENE- AMD THIAZOLESULFONAMIDES AS ANTINEOPLASTIC AGENTS 审中-公开
标题翻译：作为抗肿瘤药物的噻托蒽醌化合物
公开(公告)号：WO2003035629A1
公开(公告)日：2003-05-01
申请号：PCT/US2002/031568
申请日：2002-10-15
申请人： ELI LILLY AND COMPANY , DE DIOS, Alfonso , GROSSMAN, Cora, Sue , HIPSKIND, Philip, Arthur , LIN, Ho-Shen , LOBB, Karen, Lynn , LOPEZ DE URALDE GARMENDIA, Beatriz , LOPEZ, Jose, Eduardo , MADER, Mary, Margaret , RICHETT, Michael, Enrico , SHIH, Chaun
发明人： DE DIOS, Alfonso , GROSSMAN, Cora, Sue , HIPSKIND, Philip, Arthur , LIN, Ho-Shen , LOBB, Karen, Lynn , LOPEZ DE URALDE GARMENDIA, Beatriz , LOPEZ, Jose, Eduardo , MADER, Mary, Margaret , RICHETT, Michael, Enrico , SHIH, Chaun
IPC分类号： C07D277/36
CPC分类号： C07D277/36 , C07D333/34 , C07D333/38
摘要： The present invention provides antineoplastic compounds of the formula (I).
摘要翻译：本发明提供式（I）的抗肿瘤化合物。

7. 发明公开

EP1836151A2 VITAMIN D RECEPTOR MODULATORS 有权
标题翻译：维生素D受体的调节剂
公开(公告)号：EP1836151A2
公开(公告)日：2007-09-26
申请号：EP05854992.4
申请日：2005-12-19
申请人： ELI LILLY AND COMPANY
发明人： GOSSETT, Lynn, Stacy , LOPEZ, Jose, Eduardo , WARSHAWSKY, Alan, M. , YEE, Ying, Kwong
IPC分类号： C07C65/40 , C07C65/24 , A61K31/165 , A61K31/19 , A61P3/14
CPC分类号： C07C235/42 , C07C65/24 , C07C65/40 , C07C217/80 , C07C271/30
摘要： The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, ZP, LP1, LP2 LNP, RP3, RN, and ZNP are defined herein, their preparation, pharmaceutical compositions, and methods of use.

8. 发明公开

EP1305323A1 CHROMOGENIC COMPOUND 审中-公开
标题翻译： CHROMOGENVERBINDUNG
公开(公告)号：EP1305323A1
公开(公告)日：2003-05-02
申请号：EP00948748.9
申请日：2000-07-25
申请人： ELI LILLY AND COMPANY
发明人： EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , HARPER, Richard, Waltz , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , RICHETT, Michael, Enrico
IPC分类号： C07F9/10 , C07F9/09 , C07F9/14 , C12Q1/44
CPC分类号： C12Q1/44 , C07F9/091 , C07F9/10 , C07F9/14
摘要： This application relates to a novel compound of formula I, as defined herein, processes and intermediates for its preparation and the use of the compound of formula I as a substrate for a pharmaceutical screen.

9. 发明授权

EP1836151B1 VITAMIN D RECEPTOR MODULATORS 有权
标题翻译：维生素D受体的调节剂
公开(公告)号：EP1836151B1
公开(公告)日：2009-04-01
申请号：EP05854992.4
申请日：2005-12-19
申请人： ELI LILLY AND COMPANY
发明人： GOSSETT, Lynn, Stacy , LOPEZ, Jose, Eduardo , WARSHAWSKY, Alan, M. , YEE, Ying, Kwong
IPC分类号： C07C65/40 , C07C65/24 , A61K31/165 , A61K31/19 , A61P3/14
CPC分类号： C07C235/42 , C07C65/24 , C07C65/40 , C07C217/80 , C07C271/30
摘要： The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, Z P , L P1 , L P2 L NP , RP 3 , RN, and Z NP are defined herein, their preparation, pharmaceutical compositions, and methods of use.

10. 发明公开

EP1610779A1 3-OXO-1,3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS 有权
标题翻译： 3-氧代-1,3-二氢 - 吲唑-2-羧酰胺衍生物作为抑制剂磷脂酶
公开(公告)号：EP1610779A1
公开(公告)日：2006-01-04
申请号：EP04723448.9
申请日：2004-03-25
申请人： ELI LILLY AND COMPANY
发明人： EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
IPC分类号： A61K31/416 , C07D231/56 , C07C275/26 , A61P3/06
CPC分类号： C07D231/56 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C5-C13alky1;:C,-C,2haloalkyl, C4C,2alkenyl, C4-C12alkynyl, or C,- C5alkylcycloalkyl, C3-C8cycloalkyl, C, C5alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with onf to three substituents independently selected from C,-C8a)kyl, C,-C8haloalkyl,`C2-CBalkenyl, C2-C8a)kynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (C}12)m000C,-Csalkyl, (CH2)mNRaRb, and C,C4alkylcycloalkyl; wherein Wand Rb are independently selected from hydrogen, C,CBalkyl, C2-CBalkenyl, C2-CBalkynyl, and C,- C5alkylcycloalkyl; R2 is hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,-C12alkyl, C2C,2haloalkyl, C2-C,2 alkenyl, C2-C12alkynyl, C,-Ct2alkylaryl, C,-C12alkylcyclohexyl, C, C12alkylcyclopentyl, C,-C1zalkylheterocyclic, (CH2)m000H, (CH2)mC0(C,-C,o)alkyl, (CH2)m COO(C,-C,o)alkyl, (CH2)mCOO(C,-C,o)alkylaryl, C,-C,oalkylamino, halo, (CH2)mCONH2, (CH2)rCONRaRb, phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from CBalkyl, C,-CBhaloalkyl, C2-CBalkenyl, CZ CBalkynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (CH2)m000C,-Csalkyl, and C,-C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,-Cloalkyl, C,C,ohaloalkyl, C2-C,oalkenyl, C2-C,oalkynyl, C,-C6alkylaryl, C,-C6alkylcyclohexyl, C - C6aikylcyclopentyl, C,-C6alkylheterocyclic, or aryl; or a pharmaceutically acceptable sal lvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.

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