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3. 发明申请

WO2005047279A8 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：用作治疗疼痛的VANILLOID-1受体拮抗剂的含有NITRUTED的含六聚氨基甲酰胺的氨基酸
公开(公告)号：WO2005047279A8
公开(公告)日：2006-08-10
申请号：PCT/GB2004004719
申请日：2004-11-09
申请人： MERCK SHARP & DOHME , HOLLINGWORTH GREGORY JOHN , JONES A BRIAN , MCIVER EDWARD GILES , MOYES CHRISTOPHER RICHARD , ROGERS LAUREN
发明人： HOLLINGWORTH GREGORY JOHN , JONES A BRIAN , MCIVER EDWARD GILES , MOYES CHRISTOPHER RICHARD , ROGERS LAUREN
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, hydroxyC 1- 4 a
摘要翻译：本发明提供式（I）化合物：YJ-NH-Z其中：Y是喹啉或异喹啉，其任选地被一个或两个独立地选自羟基，卤素，卤代C 1-4的取代基取代。烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选地被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，，C 3-5环烷基，C 1-4烷氧基，羟基C 1-4 - ， -

4. 发明专利

AT390421T 未知
公开(公告)号：AT390421T
公开(公告)日：2008-04-15
申请号：AT03775557
申请日：2003-11-14
申请人： MERCK SHARP & DOHME
发明人： BLURTON PETER , BURKAMP FRANK , FLETCHER STEPHEN ROBERT , HOLLINGWORTH GREGORY JOHN , JONES A BRIAN , MCIVER EDWARD GILES , MOYES CHRISTOPHER RICHARD , ROGERS LAUREN
IPC分类号： C07D401/12 , A61K31/4709 , A61K31/4725 , A61P29/00 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04

5. 发明专利

CA2545384A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 未知
公开(公告)号：CA2545384A1
公开(公告)日：2005-05-26
申请号：CA2545384
申请日：2004-11-09
申请人： MERCK SHARP & DOHME
发明人： MOYES CHRISTOPHER RICHARD , ROGERS LAUREN , MCIVER EDWARD GILES , JONES BRIAN A , HOLLINGWORTH GREGORY JOHN
IPC分类号： C07D401/04 , A61K31/4725 , A61P43/00 , C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1- 4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alky l, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1- 4alkyl, cyano, hydroxy, C1 - 4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)pQ, NR2R3, - (CH2)pNR2R3 and -O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted wi th one or two substituents independently selected from halogen, haloC1-4alkyl, C1- 4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five- membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-member ed heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alkyl; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3, together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3 ; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.

6. 发明专利

AU2003283581A1 AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 未知
公开(公告)号：AU2003283581A1
公开(公告)日：2004-06-15
申请号：AU2003283581
申请日：2003-11-14
申请人： MERCK SHARP & DOHME
发明人： MCIVER EDWARD GILES , MOYES CHRISTOPHER RICHARD , ROGERS LAUREN , BLURTON PETER , BURKAMP FRANK , FLETCHER STEPHEN ROBERT , HOLLINGWORTH GREGORY JOHN , JONES A BRIAN
IPC分类号： A61P29/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04 , A61K31/4709 , A61K31/4725

7. 发明专利

AT402166T 未知
公开(公告)号：AT402166T
公开(公告)日：2008-08-15
申请号：AT04731058
申请日：2004-05-04
申请人： MERCK SHARP & DOHME
发明人： BLURTON PETER , BURKAMP FRANK , FLETCHER STEPHEN ROBERT , JONES BRIAN A , MCIVER EDWARD GILES
IPC分类号： C07D401/04 , A61K31/502 , A61K31/5025 , C07D403/04 , C07D471/04

8. 发明专利

PE20050577A1 AMINO HETEROCICLOS DE SEIS MIEMBROS QUE CONTIENEN NITROGENO SUSTITUIDO COMO ANTAGONISTAS DEL RECEPTOR 1 VAINILLOIDE 未知
公开(公告)号：PE20050577A1
公开(公告)日：2005-08-25
申请号：PE2004001086
申请日：2004-11-08
申请人： MERCK SHARP & DOHME , MERCK & CO INC
发明人： HOLLINGWORTH GREGORY JOHN , MCIVER EDWARD GILES , JONES A BRIAN , ROGERS LAUREN , MOYES CHRISTOPHER RICHARD , CAI DONGWEI
IPC分类号： A61K31/497 , A61K31/501 , A61K31/506 , A61P43/00 , C07D401/04 , C07D401/14
摘要： SE REFIERE A UN COMPUESTO DE FORMULA Y-J-NH-Z DONDE Y ES QUINOLINA, ISOQUINOLINA OPCIONALMENTE SUSTITUIDO CON UNO O DOS SUTITUYENTES SELECCIONADOS ENTRE HALOGENO, HALOALQUILO C1-C4, ALQUILO C1-C4, ALCOXI C1-C4, ENTRE OTROS; J ES PIRIDINA, PIRIDAZINA, PIRAZINA, PIRIMIDINA, TRIAZINA SUSTITUIDOS CON HALO, HALOALQUILO C1-C4, ALQUILO C1-C4, ENTRE OTROS DONDE J SE SUSTITUYE EN LAS POSICIONES meta UNA RESPECTO A LA OTRA MEDIANTE NH E Y; Z ES FENILO, PIRIDILO SUSTITUIDO CON HALOGENO, HALOALQUILO C1-C4, ALQUILO C1-C4, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 4-QUINOLIN-8-IL-N-[4-TRIFLUOROMETILFENIL]PIRIMIDIN-2-AMINA, 6-QUINOLIN-8-IL-N-[4-TRIFLUOROMETILFENIL]PIRAZIN-2-AMINA, 5-QUINOLIN-8-IL-N-[4-TRIFLUOROMETILFENIL]PIRIDAZIN-3-AMINA, 6-QUINOLIN-8-IL-N-[4-TRIFLUOROMETILFENIL]PIRIMIDIN-4-AMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS MENCIONADOS SON ANTANTAGONISTAS DEL RECEPTOR 1 VAINILLOIDE Y SON UTILES PARA EL TRATAMIENTO DE DOLOR, ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA (EPOC)

9. 发明专利

AU2004236014A1 Substituted-1-phthalazinamines as VR-1 antagonists 未知
公开(公告)号：AU2004236014A1
公开(公告)日：2004-11-18
申请号：AU2004236014
申请日：2004-05-04
申请人： MERCK SHARP & DOHME
发明人： MCIVER EDWARD GILES , BLURTON PETER , FLETCHER STEPHEN ROBERT , JONES BRIAN A , BURKAMP FRANK
IPC分类号： C07D401/04 , C07D403/04 , C07D471/04 , A61K31/502 , A61K31/5025

10. 发明专利

AT519740T 未知
公开(公告)号：AT519740T
公开(公告)日：2011-08-15
申请号：AT06808732
申请日：2006-11-03
申请人： MERCK SHARP & DOHME
发明人： BURKAMP FRANK , CHECKSFIELD GRAHAM DAVID , FLETCHER STEPHEN ROBERT , LEWIS STEPHEN , MCIVER EDWARD GILES , OAKLEY PAUL JOSEPH , TEALL MARTIN RICHARD
IPC分类号： C07D209/30 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.

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