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1. 发明申请

WO0132632A3 PHARMACEUTICALLY ACTIVE 4-SUBSTITUTED PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：药物活性4-取代的吡嗪衍生物
公开(公告)号：WO0132632A3
公开(公告)日：2001-11-08
申请号：PCT/US0026261
申请日：2000-10-19
申请人： LILLY CO ELI , AMBLER SAMANTHA JAYNE , BAKER STEPHEN RICHARD , CLARK BARRY PETER , COLEMAN DARRELL STEPHEN , FOGLESONG ROBERT JAMES , GOLDSWORTHY JOHN , JAGDMANN GUNNAR ERIK JUNIOR , JOHNSON KIRK WILLIS , KINGSTON ANN ELIZABETH , OWTON WILLIAM MARTIN , SCHOEPP DARRYLE DARWIN , HONG JIAN ERIC , SCHKERYANTZ JEFFREY MICHAEL , VANNIEUWENHZE MICHAEL SCOTT , ZIA EBRAHIMI MOHAMMAD SADEGH
发明人： AMBLER SAMANTHA JAYNE , BAKER STEPHEN RICHARD , CLARK BARRY PETER , COLEMAN DARRELL STEPHEN , FOGLESONG ROBERT JAMES , GOLDSWORTHY JOHN , JAGDMANN GUNNAR ERIK JUNIOR , JOHNSON KIRK WILLIS , KINGSTON ANN ELIZABETH , OWTON WILLIAM MARTIN , SCHOEPP DARRYLE DARWIN , HONG JIAN ERIC , SCHKERYANTZ JEFFREY MICHAEL , VANNIEUWENHZE MICHAEL SCOTT , ZIA-EBRAHIMI MOHAMMAD SADEGH
IPC分类号： C07D239/46 , C07D239/94 , C07D239/95 , C07D403/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , A61K31/517 , A61P25/18
CPC分类号： C07D239/47 , C07D239/94 , C07D239/95 , C07D403/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to the use of certain 4-substituted pyrimidine derivatives as mGluR1 antagonists, to novel 4-substituted pyrimidine derivatives, to pharmaceutical formulations comprising 4-substituted pyrimidine derivatives, to a process for preparing 4-substituted pyrimidine derivatives and to intermediates useful in the preparation of 4-substituted pyrimidine derivatives.
摘要翻译：本发明涉及一种4-取代的嘧啶衍生物作为mGluR1拮抗剂，新颖的4-取代的嘧啶衍生物，包含4-取代的嘧啶衍生物的药物制剂，用于制备4-取代的嘧啶衍生物的方法和中间体有用在制备4-取代的嘧啶衍生物时。

2. 发明专利

LT2912041T TETRAHIDROPIROLTIAZINO DARINIAI KAIP BACE SLOPIKLIAI 未知
公开(公告)号：LT2912041T
公开(公告)日：2017-03-10
申请号：LT13785730
申请日：2013-10-17
申请人： LILLY CO ELI
发明人： MARTIN FIONNA MITCHELL , MERGOTT DUSTIN JAMES , OWTON WILLIAM MARTIN
IPC分类号： C07D513/04 , A61K31/542 , A61P25/28

3. 发明专利

CA2536107A1 SUBSTITUTED PIPERAZINES OF AZEPINES, OXAZEPINES, AND THIAZEPINES 未知
公开(公告)号：CA2536107A1
公开(公告)日：2005-03-24
申请号：CA2536107
申请日：2004-09-07
申请人： LILLY CO ELI
发明人： OWTON WILLIAM MARTIN , MARTIN FIONNA MITCHELL , TUPPER DAVID EDWARD , SCHAUS JOHN MEHNERT , ROCCO VINCENT PATRICK , HE JOHN XIAOQIANG
IPC分类号： C07D513/04 , A61K31/55 , A61K31/554 , A61P25/18 , A61P25/24 , C07D417/04 , C07D495/04
摘要： Described herein are antipyschotic compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; R 1 is hydrogen, (C 1-6 ) fluoroalkyl, (C 3-6 ) cycloalkyl, or (C 1-4 ) alkyl, wherein the (C 1-4 ) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH 2 CH 2 OH, -CN, imidazolidin-2-one, phenyl, or tetrazole wherein tetrazole is unsubstituted or substituted with (C 1-4 ) alkyl; R 2 is H, halogen, (C 1-6 ) fluoroalkyl, (C 3-6 ) cycloalkyl, OR 6 , SR 6 , NO 2 , CN, COR 6 , C(O)OR 6 , C(OH)R 6 , CONR 7 R 8 , phenyl or (C 1-6 ) alkyl, wherein the (C 1-6 ) alkyl is unsubstituted or substituted with a hydroxy; R 3 is hydrogen, (C 1-6 )fluoroalkyl , (C 3-6 ) cycloalkyl, (C 2-6 ) alkenyl, phenyl, monocyclic heteroaromatic, bicyclic heteroaromatic, or (C 1-4 )alkyl wherein (C 1-4 ) alkyl is unsubstituted or substituted with a phenyl; R 4 and R 5 are independently selected from hydrogen, halogen, (C 1-6 ) alkyl, (C 1-6 ) fluoroalkyl, OR 9 , SR 9 , NO 2 , CN, or COR 9 ; R 6 is hydrogen, (C 1-6 ) fluoroalkyl, or (C 1-6 ) alkyl; R 7 and R 8 are independently hydrogen, or (C 1-6 ) alkyl; R 9 is hydrogen, (C 1-6 ) fluoroalkyl, (C 1-6 ) alkyl; Alk is (C 1-4 ) alkylene unsubstituted or substituted with a hydroxy; Y is oxygen, sulfur, SO 2 , or a bond; X is CH 2 , C-O, S, O, or SO 2 ; Z is hydrogen, halogen, (C 1-6 ) alkyl, (C 1-6 )fluoroalkyl, -OH, (C 1-6 ) alkoxy, (C 1-6 ) fluoroalkoxy, (C 1-6 ) alkylthio, (C 1-6 ) acyl, (C 1-4 )alkylsulfonyl, -OCF 3 , -NO 2 , -CN, carboxamido which may be substituted on the nitrogen by one or two (C 1-4 ) alkyl groups, and -NH 2 in which one of the hydrogens may be replaced by a (C 1-4 ) alkyl group and the other hydrogen may be replaced by either a (C 1-4 ) alkyl group, a (C 1-6 ) acyl group, or a (C 1-4 ) alkylsulfonyl group; the phenyl of R 1 , R 2 or R 3 is independently unsubstituted or substituted with one to three substituents independently selected from Z; the monocyclic heteroaromatic of R 3 is unsubstituted or substituted with one to three substituents independently selected from Z; the bicyclic heteroaromatic of R 3 is unsubstituted or substituted with one to three substituents independently selected from Z; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D 2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).

4. 发明专利

ES2204932T3 未知
公开(公告)号：ES2204932T3
公开(公告)日：2004-05-01
申请号：ES95306253
申请日：1995-09-07
申请人： LILLY CO ELI
发明人： GILMORE JEREMY , GALLAGHER PETER THADDEUS , MILES MARTIN VICTOR , OWTON WILLIAM MARTIN , SMITH COLIN WILLIAM
IPC分类号： C07D403/04 , A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/425 , A61K31/455 , A61K31/47 , A61P1/00 , A61P1/08 , A61P3/04 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/00 , C07D413/06 , C07D471/04 , C07D487/04 , A61K31/435
摘要： A pharmaceutical compound of the formula in which R and R are each halo, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy, optionally substituted phenyl, optionally substituted naphthyl or optionally substituted heteroaryl, R and R are each hydrogen or C1-6 alkyl, R and R are each hydrogen, halo, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy, optionally substituted phenyl, optionally substituted naphthyl or optionally substituted heteroaryl, R is hydrogen, C1-6 alkyl, optionally substituted phenyl, optionally substituted naphthyl, optionally substituted heteroaryl, optionally substituted phenyl-C1-6 alkyl or -CO2R where R is an ester group, m and p are each 0, 1, 2, 3 or 4, n is 1, 2, 3 or 4, Z is where R and R are each hydrogen, C1-6 alkyl or optionally substituted phenyl-C1-6 alkyl, X is oxygen or sulphur, and Y is where R and R are each hydrogen, C1-6 alkyl, trifluoromethyl, optionally substituted phenyl, optionally substituted naphthyl or optionally substituted heteroaryl; and salts and solvates thereof. The compounds of the invention are indicated for use in the treatment of diseases of the central nervous system. They are active in tests that indicate serotonergic modulation.

5. 发明专利

AT204273T 未知
公开(公告)号：AT204273T
公开(公告)日：2001-09-15
申请号：AT96309200
申请日：1996-12-17
申请人： LILLY CO ELI
发明人： GALLAGHER PETER THADDEUS , MANOR , OWTON WILLIAM MARTIN , SMITH COLIN WILLIAM
IPC分类号： A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/55 , A61P1/00 , A61P1/08 , A61P3/04 , A61P9/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/30 , C07D209/34 , C07D209/38 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： A pharmaceutical compound of the formula in which R and R are each hydrogen, C1-4 alkyl, C1-4 alkoxy, HO-C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, C1-4 alkylthio, halo or phCR'R"- where Ph is optionally substituted phenyl and R' and R" are each hydrogen or C1-4 alkyl, or R and R together with the carbon atom to which they are attached form a C3-6 cycloalkyl group, R , R and R are each hydrogen, halo, nitro, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkyl-CO-, C1-4 alkyl-S(O)m-where m is 0, 1 or 2, R'R"N-SO2-, -COOR', -CONR'R", -NR'R", -N(OR')COOR", -COR', -NHSO2R', where R' and R" are each hydrogen or C1-4 alkyl, R and R are each hydrogen or C1-4 alkyl, and n is 1 to 6, X is oxygen or sulphur, W is where p is 4 to 7, and q and r are each 1 to 3, Y is &rdurule& CO or -CH(OH)-, and Z is optionally substituted phenyl or optionally substituted heteroaryl; and salts and esters thereof.

6. 发明专利

DE69703413T2 未知
公开(公告)号：DE69703413T2
公开(公告)日：2001-03-15
申请号：DE69703413
申请日：1997-06-25
申请人： LILLY CO ELI
发明人： GALLAGHER PETER THADDEUS , MILES MARTIN VICTOR , OWTON WILLIAM MARTIN , SMITH COLIN WILLIAM
IPC分类号： A61K31/4427 , A61K31/445 , A61P25/00 , C07D401/06 , C07D407/14 , C07D413/14

7. 发明专利

PE04672000A1 DERIVADO DE INDOL UTIL COMO INHIBIDOR DE SEROTONINA 未知
公开(公告)号：PE04672000A1
公开(公告)日：2000-06-05
申请号：PE00038199
申请日：1999-05-10
申请人： LILLY CO ELI
发明人： GALLAGHER PETER THADDEUS , MILES MARTIN VICTOR , SMITH COLIN WILLIAM , FAIRHURST JOHN , OWTON WILLIAM MARTIN
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61P1/00 , A61P1/08 , A61P3/04 , A61P9/00 , A61P9/12 , A61P15/10 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P43/00 , C07D401/14
CPC分类号： C07D401/14
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE n ES 1-6; m ES 1-2; p ES 1-2; R1 Y R2 SON H, ALQUILO C1-C4, ALCOXI C1-C4, OH-ALQUILO C1-C4, HALO, FENILO OPCIONALMENTE SUSTITUIDO, FENIL-ALQUILO C1-C4, ENTRE OTROS; O R1 Y R2 FORMAN UN CICLOALQUILO C3-C6, >C=O, C=NOR`; R' ES H, ALQUILO C1-C4; R3, R4 Y R5 SON H, HALO, NITRO, ALQUILO C1-C4, ALCOXI C1-C4, CO-ALQUILO C1-C4, R'R''N-SO2-, -COOR', -CONR'R'', -NR'R'', ENTRE OTROS; R' Y R'' SON H, ALQUILO C1-C4; R6 Y R7 SON H, ALQUILO C1-C4; X ES O, S; EL FLUOR ESTA UNIDO EN LAS POSICIONES 6 o 7. EL COMPUESTO I TIENE AFINIDAD SELECTIVA PARA LOS RECEPTORES DE 5HT SIENDO UN MODULADOR SEROTONERGICO UTIL PARA EL TRATAMIENTO DE TRASTORNOS DEL SISTEMA NERVIOSO CENTRAL

8. 发明专利

CA2330796A1 INDOLE DERIVATIVES AS 5-HT2A LIGANDS AND AS SEROTONINE REUPTAKE INHIBITORS 未知
公开(公告)号：CA2330796A1
公开(公告)日：1999-11-18
申请号：CA2330796
申请日：1999-05-11
申请人： LILLY CO ELI
发明人： GALLAGHER PETER THADDEUS , FAIRHURST JOHN , SMITH COLIN WILLIAM , OWTON WILLIAM MARTIN , MILES MARTIN VICTOR
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61P1/00 , A61P1/08 , A61P3/04 , A61P9/00 , A61P9/12 , A61P15/10 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P43/00 , C07D401/14 , A61K31/40
摘要： Pharmaceutical compounds of formula (I) in which n is 1 to 6, m is 1 or 2 an d p is 1 or 2, R1 and R2 are each hydrogen, C1-4 alkyl, C1-4 alkoxy, HO-C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, C1-4 alkythio, halo, optionally substituted phenyl, optionally substituted phenyl-C1-4 alkyl, or R1 and R2 together with the carbon atom to which they are attached form a C3-6 cycloalkyl group, C=O , C=NOR' where R' is hydrogen or C1-4 alkyl, R3, R4 and R5 are each hydrogen, halo, nitro, C1-4 alkyl, C1-4 alkoxy, C1-4 alkyl-CO-, where m is 0, 1 or 2, R'R''N-SO2-, -COOR', -CONR'R'', -NR'R''-N(OR')COOR'', -COR', -NHSO2R', where R' and R'' are each hydrogen or C1-4 alkyl, R6 and R7 are each hydrogen or C 1- 4 alkyl, X is oxygen or sulphur, the dotted line represents an optional doub le bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.

9. 发明专利

DE69319262T2 未知
公开(公告)号：DE69319262T2
公开(公告)日：1998-11-12
申请号：DE69319262
申请日：1993-02-17
申请人： LILLY CO ELI
发明人： BRUNAVS MICHAEL , DELL COLIN PETER , GALLAGHER PETER THADDEUS , OWTON WILLIAM MARTIN , SMITH COLIN WILLIAM
IPC分类号： A61K31/352 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/35 , A61K31/4433 , A61P1/16 , A61P3/10 , A61P9/10 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D311/92 , C07D405/04 , C07D407/04 , C07D409/04 , C07D409/14 , C07D405/12
摘要： Pharmaceutical compounds of the formula in which n is 0, 1 or 2 and R is attached at any of the positions 7, 8, 9 or 10, and each R is halo, carboxy, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, hydroxy-C1-4 alkyl, hydroxy-C1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, -COOR where R is an ester group, -COR , -CONR R or -NR R where R and R are each hydrogen or C1-4 alkyl; R is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R is furanyl optionally substituted with C1-4 alkyl; R is nitrile, carboxy, -COOR where R is an ester group, or -CONR R where R and R are each hydrogen or C1-4 alkyl; and R is -NR R , -NR COR , -N(COR )2 or -N=CHOCH2R where R and R are each hydrogen or C1-4 alkyl optionally substituted with carboxy, -N=CH-NR R where R is hydrogen or C1-4 alkyl and R is C1-4 alkyl, optionally substituted phenyl or optionally substituted heteroaryl, where X is C2-4 alkylene, or -NHSO2R where R is C1-4 alkyl, trifluoromethyl or optionally substituted phenyl; and salts thereof.

10. 发明专利

SI2912041T1 DERIVATI TETRAHIDROPIROLOTIAZINA KOT INHIBITORJI BETA SEKRETAZE (BACE) 未知
公开(公告)号：SI2912041T1
公开(公告)日：2017-02-28
申请号：SI201330463
申请日：2013-10-17
申请人： LILLY CO ELI
发明人： MARTIN FIONNA MITCHELL , MERGOTT DUSTIN JAMES , OWTON WILLIAM MARTIN
IPC分类号： C07D513/00 , A61K31/00 , A61P25/00

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