公开(公告)号：EP1379493A2

公开(公告)日：2004-01-14

申请号：EP02723329.5

申请日：2002-03-21

申请人： Eli Lilly and Company

发明人： BEAVERS, Lisa, Selsam ,  GADSKI, Robert, Alan ,  HIPSKIND, Philip, Arthur ,  LINDSLEY, Craig, William ,  LOBB, Karen, Lynn ,  NIXON, James, Arthur ,  PICKARD, Richard, Todd ,  SCHAUS, John, Mehnert ,  TAKAKUWA, Takako ,  WATSON, Brian, Morgan

IPC分类号： C07C217/58 ,  A61K31/395 ,  A61K31/131 ,  A61P3/00 ,  A61P25/00 ,  C07D295/08 ,  C07D295/12 ,  C07C217/20 ,  C07C311/05 ,  C07C311/13 ,  C07C311/18 ,  C07C237/08 ,  C07D295/14 ,  C07C217/74 ,  C07C271/34 ,  C07C323/62 ,  C07C271/24 ,  C07C233/73 ,  C07C237/32 ,  C07C311/17 ,  C07C409/12

CPC分类号： C07D207/27 ,  C07B2200/07 ,  C07C217/20 ,  C07C217/58 ,  C07C217/74 ,  C07C233/73 ,  C07C237/08 ,  C07C237/32 ,  C07C271/24 ,  C07C271/34 ,  C07C311/05 ,  C07C311/09 ,  C07C311/11 ,  C07C311/18 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/09 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/26 ,  C07D213/38 ,  C07D215/20 ,  C07D217/06 ,  C07D217/08 ,  C07D217/24 ,  C07D231/04 ,  C07D231/12 ,  C07D233/36 ,  C07D233/56 ,  C07D235/14 ,  C07D241/44 ,  C07D243/08 ,  C07D249/08 ,  C07D295/088 ,  C07D295/096 ,  C07D295/13 ,  C07D295/15 ,  C07D307/12 ,  C07D307/14 ,  C07D307/46 ,  C07D333/34 ,  C07D401/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D487/04

摘要： The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereofwhich have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor -related diseases.

摘要翻译： 本发明公开了具有选择性组胺-H 3受体拮抗剂活性的式（I）的新型取代芳基烷基胺化合物或其药学上可接受的盐以及其制备方法。 在另一个实施方案中，本发明公开了包含这种环胺的药物组合物以及使用它们治疗肥胖症和其他组胺H3受体相关疾病的方法。

公开(公告)号：EP1868991B1

公开(公告)日：2014-07-30

申请号：EP06758217.1

申请日：2006-03-28

申请人： ELI LILLY AND COMPANY

发明人： HIPSKIND, Philip, Arthur ,  TAKAKUWA, Takako ,  JESUDASON, Cynthia, Darshini ,  GADSKI, Robert, Alan ,  HORNBACK, William, Joseph ,  PICKARD, Richard, Todd ,  BEAVERS, Lisa, Selsam

IPC分类号： C07D207/09 ,  C07D401/06 ,  A61K31/4025 ,  A61P3/04

CPC分类号： C07D207/09 ,  C07D401/06

公开(公告)号：EP1904442B1

公开(公告)日：2011-09-07

申请号：EP06774260.1

申请日：2006-06-28

申请人： ELI LILLY AND COMPANY

发明人： BEAVERS, Lisa, Selsam ,  FINLEY, Don, Richard ,  GADSKI, Robert, Alan ,  HIPSKIND, Philip, Arthur ,  HORNBACK, William, Joseph ,  JESUDASON, Cynthia, Darshini ,  PICKARD, Richard, Todd ,  TAKAKUWA, Takako ,  VAUGHT, Grant, Mathews

IPC分类号： C07D207/09 ,  C07D403/12 ,  C07D401/12 ,  A61K31/4025 ,  A61P3/04 ,  A61P25/28

CPC分类号： C07D207/09 ,  C07D401/12 ,  C07D403/12

摘要： The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I)

公开(公告)号：EP1735278B1

公开(公告)日：2010-01-06

申请号：EP05730691.2

申请日：2005-03-25

申请人： ELI LILLY AND COMPANY

发明人： BEAVERS, Lisa, Selsam ,  FINLEY, Don, Richard ,  FINN, Terry, Patrick Eli Lilly and Company ,  GADSKI, Robert, Alan ,  HIPSKIND, Philip, Arthur ,  HORNBACK, William, Joseph ,  JESUDASON, Cynthia, Darshini ,  PICKARD, Richard, Todd ,  TAKAKUWA, Takako ,  VAUGHT, Grant, Mathews

IPC分类号： C07D207/09 ,  C07D401/10 ,  C07D413/10 ,  C07D403/10 ,  C07D405/10 ,  A61K31/00 ,  A61K31/4025 ,  A61P25/00 ,  A61P3/04

CPC分类号： C07D207/09 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D413/10 ,  C07D471/04

摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases

公开(公告)号：EP1786790A1

公开(公告)日：2007-05-23

申请号：EP05773290.1

申请日：2005-07-14

申请人： ELI LILLY AND COMPANY

发明人： BEAVERS, Lisa, Selsam ,  BOULET, Serge, Louis ,  FINN, Terry, Patrick,Addex Pharmaceuticals SA ,  GADSKI, Robert, Alan ,  HORNBACK, William, Joseph ,  JESUDASON, Cynthia, Darshini ,  PICKARD, Richard, Todd ,  STEVENS, Freddie, Craig ,  VAUGHT, Grant, Matthews

IPC分类号： C07D263/32 ,  C07D333/38 ,  C07D277/22 ,  A61K31/422 ,  A61P25/00

CPC分类号： C07D413/14 ,  C07D263/32 ,  C07D413/06 ,  C07D417/14

摘要： The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently -(C1-C7) alkyl(optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence -H, -halogen, or -CH3.

公开(公告)号：EP1756051A1

公开(公告)日：2007-02-28

申请号：EP05754884.4

申请日：2005-05-24

申请人： ELI LILLY AND COMPANY

发明人： BEAVERS, Lisa, Selsam ,  GADSKI, Robert, Alan ,  JESUDASON, Cynthia, Darshini ,  PICKARD, Richard, Todd ,  STEVENS, Freddie, Craig

IPC分类号： C07D207/09 ,  C07D401/12 ,  C07D403/12 ,  A61K31/4025 ,  A61P3/04 ,  A61P25/00

CPC分类号： C07D207/09 ,  C07D401/12 ,  C07D403/12 ,  Y02E60/36

摘要： The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist 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 these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.