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1. 发明申请

WO2002071827A2 RETINOID X RECEPTOR MODULATORS 审中-公开
标题翻译： RETINOID X受体调节剂
公开(公告)号：WO2002071827A2
公开(公告)日：2002-09-19
申请号：PCT/US2002/008292
申请日：2002-03-14
申请人： ELI LILLY AND COMPANY , LIGAND PHARMACEUTICALS INCORPORATED , GARDINIER, Kevin, Matthew , GERNERT, Douglas, Linn , GRESE, Timothy, Alan , NEEL, David, Andrew , MAPES, Christopher, M. , MICHELLYS, Pierre-Yves , BOEHM, Marcus, F.
发明人： GARDINIER, Kevin, Matthew , GERNERT, Douglas, Linn , GRESE, Timothy, Alan , NEEL, David, Andrew , MAPES, Christopher, M. , MICHELLYS, Pierre-Yves , BOEHM, Marcus, F.
IPC分类号： A61K31/343 , A61K31/381 , A61K31/405 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/4365 , A61K31/437 , A61K31/47 , A61K31/472 , A61K38/17 , A61K45/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/40 , A61P9/00 , A61P9/10 , A61P13/08 , A61P13/10 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P37/08 , A61P43/00 , C07D209/12 , C07D209/18 , C07D215/14 , C07D217/16 , C07D231/56 , C07D261/20 , C07D307/80 , C07D307/85 , C07D333/56 , C07D333/60 , C07D333/70 , C07D471/04 , C07D495/04
CPC分类号： C07D261/20 , C07D209/12 , C07D215/14 , C07D217/16 , C07D231/56 , C07D307/80 , C07D307/85 , C07D333/56 , C07D333/60 , C07D333/70 , C07D471/04 , C07D495/04
摘要： The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.
摘要翻译：本发明涉及由结构式（I）表示的化合物及其药学上可接受的盐，溶剂合物和水合物：（I）。本发明还涉及由结构式（I）表示的药物组合物，使用方法和制备化合物的方法及其药学上可接受的盐，溶剂合物和水合物。

2. 发明申请

WO2006066174A1 THIAZOLOPYRIDINONE DERIVATES AS MCH RECEPTOR ANTAGONISTS 审中-公开
标题翻译：噻唑吡啶酮作为MCH受体拮抗剂
公开(公告)号：WO2006066174A1
公开(公告)日：2006-06-22
申请号：PCT/US2005/045866
申请日：2005-12-16
申请人： ELI LILLY AND COMPANY , AMEGADZIE, Albert, Kudzovi , BECK, James, Peter , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , RUBLE, James, Craig , SAVIN, Kenneth, Allen , WAKEFIELD, Brian, David
发明人： AMEGADZIE, Albert, Kudzovi , BECK, James, Peter , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , RUBLE, James, Craig , SAVIN, Kenneth, Allen , WAKEFIELD, Brian, David
IPC分类号： C07D513/04 , A61K31/435 , A61P3/00
CPC分类号： C07D513/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R 1 , q, p, R 2 , t, Ar 1 , L 1 , R 3 and R 4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物; 其中w，R 1，q，p，R 2，t，Ar 1，L 1，R 或其药学上可接受的盐，溶剂化物或对映异构体可用于治疗，预防或改善与肥胖症和相关疾病相关的症状。

3. 发明申请

WO2005000821A1 TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译： TACHYKININ受体拮抗剂
公开(公告)号：WO2005000821A1
公开(公告)日：2005-01-06
申请号：PCT/US2004/015579
申请日：2004-06-03
申请人： ELI LILLY AND COMPANY , AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HIPSKIND, Philip, Arthur , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , SAVIN, Kenneth, Allen , THRASHER, Kenneth, Jeff , BOYD, Steven, A.
发明人： AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HIPSKIND, Philip, Arthur , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , SAVIN, Kenneth, Allen , THRASHER, Kenneth, Jeff , BOYD, Steven, A.
IPC分类号： C07D233/90
CPC分类号： C07D401/04 , C07D249/04 , C07D249/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/12 , C07D487/04
摘要： The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
摘要翻译：本发明涉及式（I）的选择性NK-1受体拮抗剂或其药学上可接受的盐，用于治疗与过速速激肽相关的疾病。

4. 发明申请

WO2008076562A1 5- [4- (AZETIDIN-3-YL0XY) -PHENYL] -2-PHENYL-5H-THIAZ0L0 [5,4-C] PYRIDIN-4-0NE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 5- [4-（AZETIDIN-3-YL0XY） - 苯基] -2-苯基-5H-噻唑并[5,4-C]吡啶-4-羟基衍生物及其作为MCH受体拮抗剂的用途
公开(公告)号：WO2008076562A1
公开(公告)日：2008-06-26
申请号：PCT/US2007/084812
申请日：2007-11-15
申请人： ELI LILLY AND COMPANY , GARDINIER, Kevin, Matthew , GARMENE, David, Joseph , HEMBRE, Erik, James , BRUNAVS, Michael , SZEKERES, Helen, Jane
发明人： GARDINIER, Kevin, Matthew , GARMENE, David, Joseph , HEMBRE, Erik, James , BRUNAVS, Michael , SZEKERES, Helen, Jane
IPC分类号： C07D513/04 , A61K31/437
CPC分类号： C07D513/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein "-----" is absent or is optionally a bond; q is 1 or 2; R 1 is independently selected from hydrogen, -C 1 -C 2 alkyl, halo, hydroxy, -C 1 -C 2 haloalkyl, -C 1 -C 3 alkoxy, cyano, -O-C 3 -C 4 cycloalkyl, and -OC 1 -C 2 haloalkyl; R 2 is selected from the group consisting of hydrogen, -C 1 -C 3 alkyl, hydroxy, -C 1 -C 3 alkoxy, cyano, -C 1 -C 2 haloalkyl, -OC 1 -C 2 haloalkyl, and halo; R 3 is selected from the group consisting of hydrogen, -C 1 -C 4 alkyl, -C 2 -C 4 haloalkyl, -C 2 -C 4 alkylOH, -C 3 -C 6 cycloalkyl, -CH 2 C 3 -C 6 cyxloalkyl, -C 2 -C 4 alkyl-O-C 1 -C 4 alkyl, -C(O)C 1 -C 4 alkyl, -C(O)C 1 -C 4 haloalkyl, -CH 2 -thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C 1 -C 2 alkyl, and -C 1 -C 2 haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof,, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.
摘要翻译：本发明涉及式I的黑色素浓缩激素拮抗剂化合物：其中“-----”不存在或任选地是键; q为1或2; R 1独立地选自氢，-C 1 -C 2烷基，卤素，羟基，-C 1 H 2 -C≡2卤代烷基，-C 1 -C 3烷氧基，氰基，-OC 3-C≡C- 亚烷基环烷基和-OC 1 -C 2卤代烷基; R 2选自氢，-C 1 -C 3 - 烷基，羟基，-C 1 -C 4烷基， C 1 -C 3烷氧基，氰基，-C 1 -C 2卤代烷基，-OC 1 -C 卤代烷基和卤素; R 3选自氢，-C 1 -C 4烷基，-C 2 -C 4烷基， -C 4卤代烷基，-C 2 -C 4烷基OH，-C 3 -C 6 -CH 2 C 3 -C 6环烷基，-C 2 -C 3环烷基，-CH 2 C 3 -C 6环烷基， -C（O）C 1 -C 4烷基-C 1 -C 4烷基，-C（O）C 1 -C 4烷基， -C（O）C 1 -C 4卤代烷基，-CH 2 - 噻唑，苯基，苄基，四氢噻喃基和四氢吡喃基，其中环烷基，四氢噻喃基，四氢吡喃基和噻唑基任选被一个或两个独立地选自卤素，羟基，C 1 -C 2 - 烷基和-C 1 -C 2 -C 2卤代烷基; 或其药学上可接受的盐，对映异构体，非对映体或其混合物，其可用于治疗，预防或改善与肥胖症和相关疾病相关的症状。

5. 发明申请

WO2005066126A1 CB1 MODULATOR COMPOUNDS 审中-公开
标题翻译： CB1调节剂化合物
公开(公告)号：WO2005066126A1
公开(公告)日：2005-07-21
申请号：PCT/US2004/039763
申请日：2004-12-13
申请人： ELI LILLY AND COMPANY , ALLEN, Jennifer, Rebecca , AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , GREGORY, George, Stuart , HITCHCOCK, Steven, Andrew , HOOGESTRAAT, Paul, J. , JONES, Winton, Dennis, Junior , SMITH, Daryl, Lynn
发明人： ALLEN, Jennifer, Rebecca , AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , GREGORY, George, Stuart , HITCHCOCK, Steven, Andrew , HOOGESTRAAT, Paul, J. , JONES, Winton, Dennis, Junior , SMITH, Daryl, Lynn
IPC分类号： C07D209/08
CPC分类号： C07D209/10 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/40 , C07D209/42 , C07D209/96 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D417/04 , C07D471/04 , C07D471/10 , C07D491/10
摘要： Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
摘要翻译：公开了结构式（I）的新型化合物。作为大麻素-1（CB1）受体的调节剂，这些化合物可用于治疗，预防和抑制由CB1受体介导的疾病。因此，本发明的化合物可用于治疗，预防和抑制精神病，记忆缺陷，认知障碍，偏头痛，神经病，神经炎症性疾病（例如，多发性硬化症，吉兰巴利综合症和炎性后遗症病毒性脑炎），脑血管意外，头部创伤，焦虑障碍，压力，癫痫，帕金森病和精神分裂症。这些化合物也可用于治疗药物滥用障碍，特别是鸦片剂，酒精和尼古丁。所述化合物还可用于治疗与过量食物摄入和与其相关的并发症相关的肥胖或进食障碍。

6. 发明申请

WO2007146759A2 NOVEL MCH RECEPTOR ANTAGONISTS 审中-公开
标题翻译：新生儿受体拮抗剂
公开(公告)号：WO2007146759A2
公开(公告)日：2007-12-21
申请号：PCT/US2007/070668
申请日：2007-06-08
申请人： ELI LILLY AND COMPANY , AMEGADZIE, Albert, Kudzovi , DAO, Yen , GARDINIER, Kevin, Matthew , GARMENE, David, Joseph , GREEN, Steven, James , HEMBRE, Erik, James , LU, Jianliang , SPINAZZE, Patrick, Gianpietro
发明人： AMEGADZIE, Albert, Kudzovi , DAO, Yen , GARDINIER, Kevin, Matthew , GARMENE, David, Joseph , GREEN, Steven, James , HEMBRE, Erik, James , LU, Jianliang , SPINAZZE, Patrick, Gianpietro
IPC分类号： C07D495/04 , A61K31/4365 , A61P3/04
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R 1 , R a , R b , R 2 , L 1 , R 3 , R 4 and R 5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物：其中R 1，R 2，R b，R b， SUP> 2，L 1，R 3，R 4和R 5定义如上所述。，或其可用于治疗，肥胖症和相关疾病的药学上可接受的盐，对映异构体，非对映体或非对映体的混合物。

7. 发明申请

WO2007146758A2 NOVEL MCH RECEPTOR ANTAGONISTS 审中-公开
标题翻译：新生儿受体拮抗剂
公开(公告)号：WO2007146758A2
公开(公告)日：2007-12-21
申请号：PCT/US2007/070662
申请日：2007-06-08
申请人： ELI LILLY AND COMPANY , ARNOLD, Macklin, Brian , DAO, Yen , GARDINIER, Kevin, Matthew , GARMENE, David, Joseph , GREEN, Steven, James , HEMBRE, Erik, James , LU, Jianliang
发明人： ARNOLD, Macklin, Brian , DAO, Yen , GARDINIER, Kevin, Matthew , GARMENE, David, Joseph , GREEN, Steven, James , HEMBRE, Erik, James , LU, Jianliang
IPC分类号： C07D495/04 , A61K31/4365 , A61P3/04
CPC分类号： C07D495/04
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R 1 , R a , R b , R 2 , L 1 , R 3 , R 4 and R 5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
摘要翻译：本发明涉及式（I）的黑色素浓缩激素拮抗剂化合物：其中R 1，R 2，R b，R b， SUP> 2，L 1，R 3，R 4和R 5定义如上所述。，或其可用于治疗，肥胖症和相关疾病的药学上可接受的盐，对映体，非对映异构体或非对映异构体的混合物。

8. 发明申请

WO2006066173A3 NOVEL MCH RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006066173A3
公开(公告)日：2006-06-22
申请号：PCT/US2005/045864
申请日：2005-12-16
申请人： ELI LILLY AND COMPANY , BECK, James, Peter , WAKEFIELD, Brian, David , CORDIER, Frederic, Laurent , DOMINGUEZ-MANZANARES, Esteban , GARDINIER, Kevin, Matthew , GREENEN, Peter, Michael , SAVIN, Kenneth, Allen
发明人： BECK, James, Peter , WAKEFIELD, Brian, David , CORDIER, Frederic, Laurent , DOMINGUEZ-MANZANARES, Esteban , GARDINIER, Kevin, Matthew , GREENEN, Peter, Michael , SAVIN, Kenneth, Allen
IPC分类号： C07D417/04 , C07D417/14 , C07D277/82 , C07D263/58 , C07D413/04 , C07D277/68 , C07D413/12 , A61K31/435 , A61K31/495 , A61K31/41 , A61P3/04 , A61P3/06 , A61P3/10
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein Ar 1 , L 1 , R 1 , q, X, R 2 , R 3 , R 4 , and R 5 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.

9. 发明申请

WO2003091227A1 TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译： TACHYKININ受体拮抗剂
公开(公告)号：WO2003091227A1
公开(公告)日：2003-11-06
申请号：PCT/US2003/010682
申请日：2003-04-22
申请人： ELI LILLY AND COMPANY , AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HONG, Jian, Eric , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , REMICK, David, Michael , ROBERTSON, Michael, Alan , SAVIN, Kenneth, Allen
发明人： AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HONG, Jian, Eric , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , REMICK, David, Michael , ROBERTSON, Michael, Alan , SAVIN, Kenneth, Allen
IPC分类号： C07D249/06
CPC分类号： C07D249/06 , C07D249/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14
摘要： The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
摘要翻译：本发明涉及式（I）的选择性NK-1受体拮抗剂; 或其药学上可接受的盐，用于治疗与过速的速激肽相关的病症。

10. 发明申请

WO2003091226A1 TRIAZOLE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为TACHYKININ受体拮抗剂的三唑衍生物
公开(公告)号：WO2003091226A1
公开(公告)日：2003-11-06
申请号：PCT/US2003/010681
申请日：2003-04-22
申请人： ELI LILLY AND COMPANY , AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HONG, Jian, Eric , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , REMICK, David, Michael , ROBERTSON, Michael, Alan , SAVIN, Kenneth, Allen
发明人： AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HONG, Jian, Eric , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , REMICK, David, Michael , ROBERTSON, Michael, Alan , SAVIN, Kenneth, Allen
IPC分类号： C07D249/06
CPC分类号： C07D401/04 , C07D249/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D487/04
摘要： This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparation and intermediates therefor. (I) wherein: D is a C 1 -C 3 alkane-diyl; R 1 is phenyl, which is optionally substituted with one to three substitutents indpendently selected from the group consisting of halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, cyano, difluoromethyl, trifluoromethyl, and trifluoromethoxy; R 4 is a radical selected from the group consisting of: (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH)
摘要翻译：本申请涉及式（I）化合物或其药学上可接受的盐，其药物组合物及其作为速激肽受体NK-1亚型抑制剂的用途，以及其制备方法及其中间体。（I）其中：D是C1-C3烷烃二基; R 1是苯基，其任选地被一至三个独立地选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氰基，二氟甲基，三氟甲基和三氟甲氧基的取代基取代; （IA），（IB），（IC），（ID），（IE），（IF），（IG），（IH）

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