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公开(公告)号：EP2016071B1
公开(公告)日：2013-07-24
申请号：EP07761237.2
申请日：2007-04-25
Applicant: ELI LILLY AND COMPANY
Inventor： LI, Renhua , WALLACE, Owen, Brendan , XU, Yanping
IPC: C07D401/14 , A61P3/10 , A61K31/4545
CPC classification number: C07D401/14
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公开(公告)号：EP2021337B1
公开(公告)日：2010-01-13
申请号：EP07761186.1
申请日：2007-04-24
Applicant: ELI LILLY AND COMPANY
Inventor： WALLACE, Owen, Brendan , LI, Renhua , MABRY, Thomas, Edward , WINNEROSKI, Leonard, Larry, Jr. , XU, Yanping
IPC: C07D401/12 , C07D207/26 , A61K31/4015 , A61K31/4025 , A61P3/10
CPC classification number: C07D207/26 , C07D207/27 , C07D401/02 , C07D401/10 , C07D401/14
Abstract: The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11Beta-HSD type 1 activity. X-17377
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3.发明授权SELECTIVE ESTROGEN RECEPTOR MODULATORS CONTAINING A PHENYLSULFONYL GROUP 有权选择性雌激素受体调节剂，AN苯磺酰基CONTAIN
公开(公告)号：EP1530470B1
公开(公告)日：2009-06-10
申请号：EP03765254.2
申请日：2003-07-16
Applicant: ELI LILLY AND COMPANY
Inventor： DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , JONES, Scott, Alan , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan , FONG, Kin, Chiu , HUMMEL, Conrad, Wilson , LEWIS, Geroge, Sal
IPC: A61K31/4453 , A61P5/32 , C07D295/08 , C07D333/56 , C07D333/72 , C07D295/12 , C07D333/64
CPC classification number: C07D295/088 , C07D295/13 , C07D333/56 , C07D333/64 , C07D333/72 , C07D409/02
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
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4.发明授权SELECTIVE ESTROGEN RECEPTOR MODULATORS CONTAINING A PHENYLSULFONYL GROUP 有权选择性雌激素受体调节剂，AN苯磺酰基CONTAIN
公开(公告)号：EP1530470B9
公开(公告)日：2010-04-07
申请号：EP03765254.2
申请日：2003-07-16
Applicant: ELI LILLY AND COMPANY
Inventor： DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , JONES, Scott, Alan , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan , FONG, Kin, Chiu , HUMMEL, Conrad, Wilson , LEWIS, Geroge, Sal
IPC: A61K31/4453 , A61P5/32 , C07D295/08 , C07D333/56 , C07D333/72 , C07D295/12 , C07D333/64
CPC classification number: C07D295/088 , C07D295/13 , C07D333/56 , C07D333/64 , C07D333/72 , C07D409/02
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
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5.发明授权SELECTIVE NOREPINEPHRINE REUPTAKE INHIBITORS FOR THE TREATMENT OF HOT FLASHES 有权选择性去甲肾上腺素再摄取抑制剂潮热的治疗
公开(公告)号：EP1729754B1
公开(公告)日：2008-07-02
申请号：EP04811076.1
申请日：2004-12-01
Applicant: ELI LILLY AND COMPANY
Inventor： ALLEN, Albert, John , HEMRICK-LUECKE, Susan , SUMNER, Calvin, Russell , WALLACE, Owen, Brendan
IPC: A61K31/5375 , A61K31/5377 , A61P15/12
CPC classification number: A61K31/138 , A61K31/40 , A61K31/4025 , A61K31/439 , A61K31/445 , A61K31/4468 , A61K31/4704 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K31/5415
Abstract: Selective norepinephrine reuptake inhibitors are useful for the prevention or treatment of hot flashes, vasomotor symptoms, impulse control disorders or personality change due to a general medical condition.
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6.发明公开PENTACYCLIC OXEPINES AND DERIVATIVES THEREOF, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权五环oxepins及其衍生物，PROCESS FOR THEIR和药物组合物含
公开(公告)号：EP1551822A2
公开(公告)日：2005-07-13
申请号：EP03765456.3
申请日：2003-07-18
Applicant: ELI LILLY AND COMPANY
Inventor： HINKLIN, Ronald, Jay , WALLACE, Owen, Brendan
IPC: C07D313/00
CPC classification number: C07D409/10 , C07D313/06 , C07D313/10 , C07D333/56 , C07D495/04
Abstract: The present invention provides a compound of the formula (I) wherein R1 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), -OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is -S- or -HC=CH-; G is -O-, -S-, -SO-, SO2, or -N(R5)-, wherein R5 is -H or C1-C4 alkyl; and Y is -O-, -S-, -NH-, -NMe-, or -CH2-; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
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7.发明授权
公开(公告)号：EP1401446B1
公开(公告)日：2005-02-09
申请号：EP02746309.0
申请日：2002-05-09
Applicant: ELI LILLY AND COMPANY
Inventor： WALLACE, Owen, Brendan
IPC: A61K31/4709 , A61P15/12
CPC classification number: A61K31/4709
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8.发明公开2-SUBSTITUTED 1,2,3,4-TETRAHYDROQUINOLINES AND DERIVATIVES THEREOF, COMPOSITIONS AND METHODS 有权2-取代1,2,3,4-四HYDRO CHINO LINE及其衍生物，组合物和方法
公开(公告)号：EP1395563A1
公开(公告)日：2004-03-10
申请号：EP02746308.2
申请日：2002-05-09
Applicant: ELI LILLY AND COMPANY
Inventor： WALLACE, Owen, Brendan
IPC: C07D215/20 , A61K31/47 , A61P5/30
CPC classification number: C07D215/38 , C07D215/20
Abstract: The current invention provides novel 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof of the formula (I) (A); pharmaceutical compositions thereof, optionally in combination with estrogen or progestin; methods for inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
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9.发明授权SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS 有权用于治疗血管舒缩症状，雌激素受体的选择性调节剂
公开(公告)号：EP1709021B1
公开(公告)日：2010-08-04
申请号：EP05704874.6
申请日：2005-01-18
Applicant: ELI LILLY AND COMPANY
Inventor： DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan
IPC: C07D295/08 , C07D311/78 , C07D335/04 , C07D221/18 , A61K31/4453 , A61K31/4523 , A61K31/55 , A61P15/12
CPC classification number: C07D295/088 , C07D221/18 , C07D311/78 , C07D335/04
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
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10.发明公开BIPHENYL AMIDE LACTAM DERIVATIVES AS INHIBITORS OF 11- BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权Biphenylamide - 内酰胺衍生物作为11-β羟类固醇脱氢酶1抑制剂
公开(公告)号：EP2016047A1
公开(公告)日：2009-01-21
申请号：EP07760877.6
申请日：2007-04-19
Applicant: ELI LILLY AND COMPANY
Inventor： AICHER, Thomas, Daniel , CHEN, Zhaogen , HINKLIN, Ronald, Jay , HITE, Gary, Alan , KRASUTSKY, Alexei, Pavlovych , LI, Renhua , MCCOWAN, Jefferson, Ray , SAEED, Ashraf , SNYDER, Nancy, June , TOTH, James, Lee , WALLACE, Owen, Brendan , WINNEROSKI, JUNIOR, Leonard, Larry , XU, Yanping , YORK, Jeremy, Schulenburg
IPC: C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D498/04 , A61P3/10 , A61K31/4015
CPC classification number: C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
Abstract: The present invention discloses novel compounds of Formula I: possessing 11 ß-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ß -HSD type 1 activity.
