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1. 发明授权

EP0978514B1 Indazole derivatives as 5-HT1F agonists 有权
标题翻译：吲唑衍生物5-HT1F激动剂
公开(公告)号：EP0978514B1
公开(公告)日：2004-12-15
申请号：EP99305915.3
申请日：1999-07-26
申请人： ELI LILLY AND COMPANY
发明人： Krushinski, Joseph Herman Jr. , Schaus, John Mehnert
IPC分类号： C07D401/04 , A61K31/445 , C07D471/04 , C07D455/02
CPC分类号： C07D455/02 , C07D401/04 , C07D471/04

2. 发明公开

EP1082958A2 5-HT1F agonists in chronic pain 失效
标题翻译： 5-HT1F Agonisten在chronischem Schmerz
公开(公告)号：EP1082958A2
公开(公告)日：2001-03-14
申请号：EP00203526.9
申请日：1997-11-12
申请人： ELI LILLY AND COMPANY
发明人： Filla, Sandra Ann , Schaus, John Mehnert , Phebus, Lee Alan , Johnson, Kirk Willis
IPC分类号： A61K31/00 , A61P25/04
CPC分类号： C07D471/04 , A61K31/00 , A61K31/437 , A61K31/444 , A61K31/4545
摘要： The use of a 5-HT 1F agonist for the manufacture of a medicament for the treatment of chronic pain.
摘要翻译：使用5-HT1F激动剂制造用于治疗慢性疼痛的药物。

3. 发明公开

EP0978514A1 Indazole derivatives as 5-HT1F agonists 有权
标题翻译：吲唑衍生物5-HT1F激动剂
公开(公告)号：EP0978514A1
公开(公告)日：2000-02-09
申请号：EP99305915.3
申请日：1999-07-26
申请人： ELI LILLY AND COMPANY
发明人： Krushinski, Joseph Herman Jr. , Schaus, John Mehnert
IPC分类号： C07D401/04 , A61K31/445 , C07D471/04 , C07D455/02
CPC分类号： C07D455/02 , C07D401/04 , C07D471/04
摘要： The present invention relates to a compound of formula
or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT 1F receptors and inhibiting neuronal protein extravasation in a mammal.
摘要翻译：本发明涉及式的化合物或其药用酸加成盐; 其可用于激活哺乳动物中的5-HT1F受体并抑制神经元蛋白质外渗。

4. 发明公开

EP0590970A1 6-Heterocyclyl-4-amino-1,2,2a,3,4,5-hexahydrobenz CD indoles for treating motion sickness and vomiting 失效
标题翻译： 6-杂环基-4-氨基-1,2,2a，3,4,5-六氢化苯并（CD）吲哚的制备方法，用于在Behandlung von Reisekrankheit und Erbrechen。
公开(公告)号：EP0590970A1
公开(公告)日：1994-04-06
申请号：EP93307745.5
申请日：1993-09-29
申请人： ELI LILLY AND COMPANY
发明人： Booher, Richard Nolan , Flaugh, Michael Edward , Lawhorn, David Ernest , Martinelli, Michael John , Paget, Charles Johnson, Jr. , Schaus, John Mehnert
IPC分类号： C07D403/04 , A61K31/40
CPC分类号： C07D401/04 , A61K31/40 , C07D209/90 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , Y02P20/55
摘要： The use of a compound, or a pharmaceutically acceptable salt thereof, of the formula

wherein:
R¹ is hydrogen, C₁-C₄ alkyl, C₃-C₄ alkenyl, cyclopropylmethyl, aryl (C₁-C₄ alkyl), -(CH₂) n S(C₁-C₄ alkyl), -C(O)R⁴ or -(CH₂) n C(O)NR⁵R⁶;
R² is hydrogen, C₁-C₄ alkyl, cyclopropylmethyl or C₃-C₄ alkenyl;
R³ is hydrogen, C₁-C₄ alkyl or an amino blocking group;
n is 1-4;
R⁴ is hydrogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy or phenyl;
R⁵ and R⁶ are independently hydrogen, C₁-C₄ alkyl, or C₅-C₈ cycloalkyl with the proviso that when one of R⁵ or R⁶ is a cycloalkyl the other is hydrogen;
HET is a tetrazolyl ring, a substituted tetrazolyl ring or an aromatic 5- or 6-membered heterocyclic ring, said ring having from one to three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen, and nitrogen with the proviso that the 6-membered heterocyclic ring can only contain carbon and nitrogen and with the further proviso that the 5-membered ring contains no more than one oxygen or one sulfur but not both oxygen and sulfur; to prepare a medicament for treating emesis or motion sickness; and a compound of the formula above wherein HET is an optionally substituted tetrazolyl ring.
摘要翻译：其中：R 1是氢，C 1 -C 4烷基，C 3 -C 4烯基，环丙基甲基，芳基（C 1 -C 4烷基）， - （ CH2）nS（C1-C4烷基），-C（O）R4或 - （CH2）nC（O）NR5R6; R 2是氢，C 1 -C 4烷基，环丙基甲基或C 3 -C 4烯基; R 3是氢，C 1 -C 4烷基或氨基封端基; n为1-4; R 4是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基或苯基; R 5和R 6独立地是氢，C 1 -C 4烷基或C 5 -C 8环烷基，条件是当R 5或R 6中的一个是环烷基时，另一个是氢; HET是四唑基环，取代的四唑基环或芳族5-或6-元杂环，所述环具有一至三个相同或不同的杂原子，并且选自硫，氧和氮，条件是6元杂环只能含有碳和氮，另外条件是5元环含有不超过一个氧或一个硫，但不含氧和硫; 制备用于治疗呕吐或运动病的药物; 和上式的化合物，其中HET是任选取代的四唑基环。

5. 发明公开

EP0471515A1 Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes and 3-aminothiochromanes 失效
标题翻译：环取代基2-氨基-1,2,3,4-四氢化萘，3-氨基荧烷和3-氨基硫色满。
公开(公告)号：EP0471515A1
公开(公告)日：1992-02-19
申请号：EP91307328.4
申请日：1991-08-09
申请人： ELI LILLY AND COMPANY
发明人： Hoechstetter, Craig Steven , Huser, Diane Lynn , Paget Jr, Charles Johnson , Schaus, John Mehnert , Titus, Robert Daniel
IPC分类号： C07C225/20 , C07D311/58 , C07D335/06 , A61K31/135 , A61K31/35 , A61K31/38
CPC分类号： C07C225/20 , C07C2601/14 , C07C2602/10
摘要： The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor, of the formula

in which R is C₁-C₄ alkyl, C₃-C₄ alkenyl, or cyclopropylmethyl;
R₃ is hydrogen; or
R and R₃ taken together are a divalent group of the formula -CH₂CH₂CH₂-;
R₁ is hydrogen, C₁-C₄ alkyl, C₃-C₄ alkenyl, cyclopropylmethyl, aryl(C₁-C₄-alkyl), -COR₄, -(CH₂) n S(C₁-C₄ alkyl) or -(CH₂) n CONR₅R₆;
n is an integer from 1 to 4;
R₄ is hydrogen, C₁-C₄ alkyl, C₁-C₄ alkoxy, or phenyl;
R₅ and R₆ are independently hydrogen, C₁-C₄ alkyl, or C₃-C₇ cycloalkyl with the proviso that when one of R₅ or R₆ is cycloalkyl the other is hydrogen;
X is -CH₂-, -O-, -S-,

A is

R₂ is C₁-C₈ alkyl, substituted C₁-C₈ alkyl, C₂-C₄ alkenyl, aryl, substituted aryl, aryl(C₁-C₄-alkyl), substituted aryl(C₁-C₄ alkyl), C₃-C₇ cycloalkyl-substituted methyl, or C₃-C₇ cycloalkyl;
and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明提供了新的环取代的2-氨基-1,2,3,4-四氢萘，3-氨基色烷和3-氨基异色满，包括它们相应的亚砜和砜，这些环取代的化合物在5-羟色胺1A 受体，其中R是C 1 -C 4烷基，C 3 -C 4烯基或环丙基甲基; R3是氢; 或R和R 3一起是式-CH 2 CH 2 CH 2 - 的二价基团; R1是氢，C1-C4烷基，C3-C4烯基，环丙基甲基，芳基（C1-C4-烷基），-COR4， - （CH2）nS（C1-C4烷基）或 - （CH2）nCONR5R6; n是1至4的整数; R4是氢，C1-C4烷基，C1-C4烷氧基或苯基; R 5和R 6独立地是氢，C 1 -C 4烷基或C 3 -C 7环烷基，条件是当R 5或R 6中的一个是环烷基时，另一个是氢; X是-CH 2 - ， - O - ， - S - ，CH CH 2 R 2是C 1 -C 8烷基，取代的C 1 -C 8烷基，C 2 -C 4烯基，芳基，取代的芳基，芳基（C 1 -C 4 - 烷基），取代的芳基（C 1 -C 4烷基），C 3 -C 7环烷基取代的甲基或C 3 -C 7环烷基; 及其药学上可接受的酸加成盐。

6. 发明公开

EP0343830A3 Ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes 失效
标题翻译：环取代的2-氨基-1,2,3,4-四氢萘酮
公开(公告)号：EP0343830A3
公开(公告)日：1990-11-28
申请号：EP89304935.3
申请日：1989-05-16
申请人： ELI LILLY AND COMPANY
发明人： Nixon, James Arthur , Pioch, Richard Paul , Schaus, John Mehnert , Titus, Robert Daniel
IPC分类号： C07D295/02 , C07D295/06 , C07D295/08 , C07D295/10 , C07D295/14 , C07D243/08 , A61K31/495 , A61K31/55
CPC分类号： C07D295/155 , C07D243/08 , C07D295/033 , C07D295/073 , C07D295/096 , C07D295/112
摘要： This invention provides ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes which are selective inhibitors of serotonin reuptake.

7. 发明公开

EP0250179A3 BCD tricyclic ergoline part-structure analogues 失效
标题翻译： BCD三环麦角灵部分结构类似物
公开(公告)号：EP0250179A3
公开(公告)日：1989-08-23
申请号：EP87305240.1
申请日：1987-06-12
申请人： ELI LILLY AND COMPANY
发明人： Huser, Diana Lynn , Schaus, John Mehnert
IPC分类号： C07D471/04 , C07D513/04 , C07D498/04 , A61K31/435 , A61K31/505 , C07D215/20 , C07D215/54 , C07D215/22 , C07D215/42 , C07D215/56
CPC分类号： C07D215/233 , C07D215/20 , C07D215/42 , C07D215/54 , C07D471/04 , C07D491/10 , C07D513/04
摘要： 7-or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g ]quinoline, oxazolo[4,5-g]-quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8-or 9-substituted, partially hydrogenated pyrido[2,3-g]-quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1- substituted-decahydroquinolines which are additionally substituted in the 3-or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.
摘要翻译： 7-或8-取代部分氢化的吡唑并[3,4-g]喹啉，噻唑并[4,5-g]喹啉，恶唑并[4,5-g]喹啉和吡咯并[3,4-g]喹啉衍生物和8-或9-取代的部分氢化的吡啶并[2,3-g] - 喹唑啉衍生物是D-2多巴胺激动剂。另外在3-或4-位被取代的6-氧代-1-取代的 - 八氢喹啉和6-氧代-1-取代的 - 十氢喹啉是用于制备多巴胺激动剂的中间体。 4,6-二氧代-1-取代 - 十氢喹啉-3-羧酸酯的缩醛可以合成前述化合物。

8. 发明公开

EP0139393A3 Pyrimido(4,5-g)quinolines, process for their preparation, and pharmaceutical compositions containing them 失效
标题翻译：哌嗪（4,5-G）喹啉，其制备方法和含有它们的药物组合物
公开(公告)号：EP0139393A3
公开(公告)日：1988-01-13
申请号：EP84305684
申请日：1984-08-21
申请人： ELI LILLY AND COMPANY
发明人： Nichols, Cynthia Lynn , Kornfeld, Edmund Carl , Foreman, Mark Mortensen , Schaus, John Mehnert , Huser, Diane Lynn , Booher, Richard Nolan , Wong, David Taiwai
IPC分类号： C07D471/04 , A61K31/505 , C07D239/00 , C07D221/00
CPC分类号： C07D471/04 , C07D215/20 , C07D495/10
摘要： Trans-(±)-2-Amino (or substituted amino)-4-(permissibly-substituted)-6-C 1 -C 3 alkyl (or allyl)-5,5a,-6,7,8,9,9a,10-octahydropyrimido[4,5-g]quinolines, the corresponding trans-(-) and trans-(+)-stereoisomers and salts thereof, useful in treating Parkinson's Syndrome, sexual dysfunction, depression, hypertension, and prolactin related diseases, and intermediates useful for the synthesis thereof, are disclosed. The products are prepared by condensing an appropriate ketone with the appropriately substituted guanidine.

9. 发明公开

EP0171277A3 Improvements in or relating to tricycling quinoline derivatives 失效
标题翻译：关于喹啉衍生物的改进或相关
公开(公告)号：EP0171277A3
公开(公告)日：1987-11-19
申请号：EP85305537
申请日：1985-08-02
申请人： ELI LILLY AND COMPANY
发明人： Schaus, John Mehnert , Whitaker, Nancy Gail Gallick
IPC分类号： C07D471/04 , C07D513/04 , C07D498/04 , C07D231/00 , C07D221/00 , C07D239/00 , C07D277/00 , C07D263/00
CPC分类号： C07D215/227 , C07D307/00 , C07D317/72 , C07D471/04 , C07D491/10 , C07D513/04
摘要： A process for preparing trycyclic quinoline derivatives having dopamine agonist properties by reducing the corresponding lactam precursors.

10. 发明授权

EP0127708B1 Trans-dl-1-alkyl-6-alkoxyoctahydroquinolines 失效
标题翻译：反-dl-1-烷基-6- alkoxyoctahydroquinolines
公开(公告)号：EP0127708B1
公开(公告)日：1987-09-09
申请号：EP83303202.2
申请日：1983-06-03
申请人： ELI LILLY AND COMPANY
发明人： Schaus, John Mehnert , Garbrecht, William Lee
IPC分类号： C07D215/20
CPC分类号： C07D215/20 , C07D471/04

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