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1. 发明公开

EP1644346A1 CYCLIC SULFONAMIDES FOR INHIBITION OF GAMMA-SECRETASE 审中-公开
标题翻译：磺胺类药物循环于抑制γ分泌
公开(公告)号：EP1644346A1
公开(公告)日：2006-04-12
申请号：EP04731671.6
申请日：2004-05-07
申请人： MERCK SHARP & DOHME LTD.
发明人： DINNELL, Kevin , HARRISON, Timothy , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
IPC分类号： C07D285/16 , C07D513/04 , C07D279/02 , A61K31/5415
CPC分类号： C07D279/02
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.

2. 发明授权

EP0942732B1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING MOVEMENT DISORDERS 无效
标题翻译： NK-1受体拮抗剂的运动障碍的治疗中的用途
公开(公告)号：EP0942732B1
公开(公告)日：2004-11-17
申请号：EP97952024.4
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LTD.
发明人： BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
IPC分类号： A61K31/535 , A61K31/445
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 antagonist for the manufacture of a medicament for oral administration for the treatment or prevention of movement disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.

3. 发明公开

EP0942729A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING STRESS DISORDERS 无效
标题翻译： NK-1受体拮抗剂的FOR应激障碍的治疗中的用途
公开(公告)号：EP0942729A1
公开(公告)日：1999-09-22
申请号：EP97952020.0
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LTD.
发明人： BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
IPC分类号： A61K31 , A61K45 , A61P25 , C07D211 , C07D265 , C07D413 , C07D491
CPC分类号： A61K31/661 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.

4. 发明公开

EP0941093A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING MAJOR DEPRESSIVE DISORDERS WITH ANXIETY 无效
标题翻译： NK-1受体拮抗剂的重症抑郁症的治疗用途，焦虑各国伴随
公开(公告)号：EP0941093A1
公开(公告)日：1999-09-15
申请号：EP97952021.0
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LTD.
发明人： BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
IPC分类号： A61K31 , A61K45 , A61P25 , A61P43 , C07D211 , C07D265 , C07D413 , C07D491
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising the same.

5. 发明公开

EP0737192A1 SUBSTITUTED MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 失效
标题翻译：取代的吗啉及其作为药物
公开(公告)号：EP0737192A1
公开(公告)日：1996-10-16
申请号：EP95904621.0
申请日：1994-12-23
申请人： MERCK SHARP & DOHME LTD.
发明人： BAKER, Raymond , HARRISON, Timothy , MACLEOD, Angus, Murray , OWENS, Andrew, Pate , SEWARD, Eileen, Mary , SWAIN, Christopher, John , TEALL, Martin, Richard
IPC分类号： C07D487 , A61K31 , A61P1 , A61P25 , A61P29 , A61P43 , C07D413 , C07D417 , C07F9
CPC分类号： C07D413/06 , C07D413/14 , C07F9/6533 , C07F9/65583
摘要： The present invention relates to compounds of formula (I), wherein R1 is hydrogen, halogen, C¿1-6¿ alkyl, C¿1-6? alkoxy, CF3, NO2, CN, SR?a, SORa, SO¿2Ra, CO2R?a, CONRaRb, C¿2-6 alkenyl, C2-6 alkynyl or C1-4 alkyl substituted by C1-4 alkoxy, where R?a and Rb¿ are hydrogen or C¿1-4? alkyl; R?2¿ is hydrogen, halogen, C¿1-6? alkyl, C1-6 alkoxy substituted by C1-4 alkoxy or CF3; R?3¿ is hydrogen, halogen or CF¿3; R?4 is selected from the definitions of R1; R5 is selected from the definitions of R2; R6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by =O, =S or a C¿1-4? alkyl group, and optionally substituted by an aminoalkyl group; R?9a and R9b¿ are hydrogen or C¿1-4? alkyl, or R?9a and R9b¿ are joined to form a C¿5-7? ring; X is C1-4 alkylene optionally substituted by oxo; and Y is a C1-4 alkyl group optionally substituted by hydroxyl; with the proviso that if Y is C1-4 alkyl, R?6¿ is substituted at least by an aminoalkyl group; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

6. 发明授权

EP0600952B1 AZACYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 失效
标题翻译：氮杂环化合物的方法，FOR THEIR和药物制剂含有它们的
公开(公告)号：EP0600952B1
公开(公告)日：1996-04-17
申请号：EP92917251.8
申请日：1992-08-13
申请人： MERCK SHARP & DOHME LTD.
发明人： BAKER, Raymond , HARRISON, Timothy , SWAIN, Christopher, John , WILLIAMS, Brian, John
IPC分类号： C07D207/12 , C07D211/42 , C07D211/74 , C07D205/04 , C07D409/04 , A61K31/40 , A61K31/445 , A61K31/395
CPC分类号： C07D401/04 , C07D205/04 , C07D207/12 , C07D211/42 , C07D211/76 , C07D409/04
摘要： Compounds of formula (I), and salts and prodrugs thereof wherein n is 1, 2 or 3; X represents O or S; R1 represents optionally substituted phenyl; R2 represents aryl, heteroaryl, benzhydryl, or benzyl; R?4 and R5¿ each independently represent H, halo, CH¿2OR?9, C1-6alkyl, oxo, CO2R10 or CONR?10R11; R8¿ represents H, COR9, CO2R10 or optionally substituted C¿1-6?alkyl; R?9¿ represents H, C¿1-6?alkyl or phenyl; and R?10 and R11¿ each independently represent H or C¿1-6?alkyl; are tachykinin antagonists. They and compositions thereof are useful in medicine.

7. 发明公开

EP0666856A1 4-ARYLMETHYLOXYMETHYL PIPERIDINES AS TACHYKININ ANTAGONISTS 失效
标题翻译： 4- AKYLMETHYLOXYMETHYL PIPERIDINE拮抗剂作为速激肽。
公开(公告)号：EP0666856A1
公开(公告)日：1995-08-16
申请号：EP93923630.0
申请日：1993-10-27
申请人： MERCK SHARP & DOHME LTD.
发明人： HARRISON, Timothy , MACLEOD, Angus Murray, 24 Abbotts Way , STEVENSON, Graeme Irvine , WILLIAMS, Brian John
IPC分类号： C07D211 , A61K31 , A61P1 , A61P9 , A61P11 , A61P13 , A61P15 , A61P25 , A61P29 , A61P35 , A61P37 , A61P43 , C07D207 , C07D213 , C07D401 , C07D413 , C07D417 , C07D521
CPC分类号： C07D207/08 , C07D211/22 , C07D211/96 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D413/06 , C07D417/06
摘要： Compounds of formula (I) wherein m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; X represents O or S; R1 represents phenyl optionally substituted by 1, 2 or 3 groups selected from C¿1-6?alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, -OR?a, SRa, SORa, SO¿2R?a, -NRaRb, -NRaCORb, -NRaCO¿2Rb, -CO2Ra or -CONRaRb, where R?a and Rb¿ each independently represent H, C¿1-6?alkyl, phenyl or trifluoromethyl; R?2¿ represents phenyl optionally substituted by 1, 2 or 3 groups selected from C¿1-6?alkyl, C2-6alkenyl, C2-6alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, -OR?a, SRa, SORa, SO¿2R?a, -NRaRb, -NRaCORb, -NRaCO¿2Rb, -CO2Ra or -CONRaRb, where R?a and Rb¿ are as previously defined; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each heteroaryl and each phenyl moiety of benzyl and benzhydryl may be substituted by C¿1-6?alkyl, C1-6alkoxy, halo or trifluoromethyl; and R?3¿ represents H, COR9, CO2R10, COCONR10R11, COCO¿2?R?10, SO¿2R?15, CONR10SO¿2R15, C1-6alkyl optionally substituted by a group selected from (CO2R?10, CONR10R11¿, hydroxy, cyano, COR?9, NR10R11¿, C(NOH)NR10R11, CONHphenyl(C¿1-4?alkyl), COCO2R?10¿, COCONR?10R11, SO¿2R?15, CONR10SO¿2R15 and phenyl optionally substituted by one or more substituents selected from C¿1-6?alkyl, C1-6alkoxy, halo and trifluoromethyl), Y-R?8¿ or CO-Z-(CH¿2?)q-R?12; R4, R5, R6 and R7¿ each independently represent H or C¿1-6?alkyl; R?8¿ represents an optionally substituted aromatic heterocycle; R9 represents H, C¿1-6?alkyl or phenyl; R?10 and R11¿ each independently represent H or C¿1-6?alkyl; R?12¿ represents NR13R14 or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; R?13 and R14¿ each independently represent H, C¿1-6?alkyl, phenyl optionally substituted by one or more of C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl or phenylC1-4alkyl optionally substituted in the phenyl ring by one or more of C1-6alkyl, C1-6alkoxy, halo or trifluoromethyl; R?15¿ represents C¿1-6?alkyl, trifluoromethyl or phenyl optionally substituted by one or more substituents selected from C1-6alkyl, C1-6alkoxy, halo and trifluoromethyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which way optionally be substituted by oxo; Z represents CH2, O, S or NR?10¿; and q represents 0, 1, 2, 3, 4, 5 or 6 and their salts are useful as tachykinin antagonists.

8. 发明授权

EP1888050B1 cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid for the treatment of cancer 有权转让
标题翻译：顺式-4 - （2,5-二氟苯基）cyclohexanepropansäure[（4-氯苯基）磺酰基] -4- Behandlug癌症
公开(公告)号：EP1888050B1
公开(公告)日：2012-03-21
申请号：EP06727202.1
申请日：2006-05-16
申请人： MERCK SHARP & DOHME LTD.
发明人： LEWIS, Huw David , HARRISON, Timothy , SHEARMAN, Mark Steven
IPC分类号： A61K31/10 , A61P35/00 , A61P35/02
CPC分类号： A61K31/10
摘要： Sulphones of formula (I) are disclosed for use in treatment of cancer.

9. 发明授权

EP1748982B1 (4, 5, 6, 7-TETRAHYDRO-1-H-INDOL-7-YL) ACETIC ACID DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE 有权
标题翻译：（4,5,6,7-四氢-1H-吲哚-7-基）乙酸衍生物用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1748982B1
公开(公告)日：2009-07-29
申请号：EP05740478.2
申请日：2005-05-06
申请人： MERCK SHARP & DOHME LTD.
发明人： BETTATI, Michela , CHURCHER, Ian , DOUGHTY, Victoria Alexandra , HARRISON, Timothy , NIZI, Emmanuela , SMITH, Adam
IPC分类号： C07D209/08 , C07D409/04 , C07D231/56 , A61K31/403 , A61P25/28
CPC分类号： C07D209/08 , C07D209/02 , C07D209/10 , C07D231/56 , C07D409/04
摘要： Compounds of formula: (I); are disclosed. The compounds are useful in treating or preventing diseases associated with deposition of Aβ in the brain.

10. 发明公开

EP1888051A2 SULPHONAMIDO-SUBSTITUTED CYCLOHEXYL SULPHONES FOR TREATMENT OF CANCER 审中-公开
标题翻译：磺酰胺取代的环己基磺基琥珀酸酯治疗癌症
公开(公告)号：EP1888051A2
公开(公告)日：2008-02-20
申请号：EP06744311.9
申请日：2006-05-16
申请人： MERCK SHARP & DOHME LTD.
发明人： LEWIS, Huw David , HARRISON, Timothy , SHEARMAN, Mark Steven
IPC分类号： A61K31/10 , A61P35/02 , A61P35/00
CPC分类号： A61K31/10
摘要： Compounds of formula (I) are disclosed for treatment of cancer.
摘要翻译：公开式（I）化合物用于治疗癌症。

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