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1. 发明公开

EP1824817A1 ARYLSULFONYLNAPHTHALENE DERIVATIVES AS 5HT2A ANTAGONISTS 有权
标题翻译：作为5HT2A拮抗剂的芳基磺酰基萘乙烯衍生物
公开(公告)号：EP1824817A1
公开(公告)日：2007-08-29
申请号：EP05813608.6
申请日：2005-11-28
申请人： MERCK SHARP & DOHME LTD.
发明人： CHAMBERS, Mark, Stuart , CURTIS, Neil, Roy , GANCIA, Emanuela , GILLIGAN, Myra , HUMPHRIES, Alexander, Charles , LADDUWAHETTY, Tamara , MAXEY, Robert, James , MERCHANT, Kevin, John
IPC分类号： C07C317/14 , C07D213/71 , C07D215/36 , C07D471/02 , C07D241/12 , A61K31/10 , A61K31/275 , A61K31/4409 , A61K31/47 , A61P25/00
CPC分类号： C07D401/12 , C07C311/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/42 , C07C317/44 , C07C323/65 , C07C2601/04 , C07D213/61 , C07D213/64 , C07D213/70 , C07D215/36 , C07D215/60 , C07D233/64 , C07D241/12 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D271/10 , C07D277/26 , C07D333/34 , C07D471/04 , C07D473/38
摘要： Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译：式（I）化合物是有效的和选择性的5-HT 2A拮抗剂，可用于治疗CNS的各种不利病症。

2. 发明授权

EP1511748B1 8-FLUORIMIDAZO(1,2-A)PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 有权
标题翻译： 8-氟咪唑（1,2-A）吡啶衍生物通常将GABA受体作为配体
公开(公告)号：EP1511748B1
公开(公告)日：2006-08-09
申请号：EP03732655.0
申请日：2003-05-23
申请人： MERCK SHARP & DOHME LTD.
发明人： BLACKABY, Wesley, Peter , CASTRO PINEIRO, Jose, Luis , GOODACRE, Simon, Charles , HALLETT, David, James , HUMPHRIES, Alexander, Charles , JONES, Philip , MERCHANT, Kevin, John , READER, Michael
IPC分类号： C07D471/04 , A61K31/505 , A61P25/28
CPC分类号： C07D471/04
摘要： A class of 8-fluoroimidazo[1,2-a]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

3. 发明授权

EP0986562B1 SUBSTITUTED 1,2,4-TRIAZOLO 3,4-A]PHTHALAZINE DERIVATIVES AS GABA ALPHA 5 LIGANDS 失效
标题翻译：取代的1,2,4-三唑并[3,4，-A]酞嗪衍生物作为GABA-ALPHA 5个配体
公开(公告)号：EP0986562B1
公开(公告)日：2002-08-07
申请号：EP98920635.4
申请日：1998-05-06
申请人： MERCK SHARP & DOHME LTD.
发明人： CARLING, William, Robert , LADDUWAHETTY, Tamara , MACLEOD, Angus, Murray , MERCHANT, Kevin, John , MOORE, Kevin, William , STERNFELD, Francine , STREET, Leslie, Joseph
IPC分类号： C07D487/04 , A61K31/50
CPC分类号： C07D487/04
摘要： A compound of formula (I) wherein R1 is hydrogen, halogen or CN or a group CF¿3?, OCF3, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy, each of which groups is unsubstituted or substituted with one or two halogen atoms or with a pyridyl or phenyl ring each of which rings may be unsubstituted or independently substituted by one or two halogen atoms or nitro, cyano, amino, methyl or CF3 groups; R?2¿ is hydrogen, halogen or CN or a group CF¿3?, OCF3, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy each of which groups is unsubstituted or substituted with one or two halogen atoms; L is O, S, or NR?n¿ where Rn is H, C¿1-6?alkyl or C3-6cycloalkyl; X is a five or six-membered optionally substituted heterocycle; Y is optionally branched C1-4alkylidene optionally substituted by an oxo group or Y is a group (CH2)jO wherein the oxygen atom is nearest the group X and j is 2, 3 or 4; Z is a five or six-membered optionally substituted heterocycle; or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising it, its use in medical treatment, processes for producing it and intermediates used in those processes are disclosed.

4. 发明公开

EP1511748A1 8-FLUORIMIDAZO(1,2-A)PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 有权
标题翻译： 8-氟咪唑（1,2-A）吡啶衍生物通常将GABA受体作为配体
公开(公告)号：EP1511748A1
公开(公告)日：2005-03-09
申请号：EP03732655.0
申请日：2003-05-23
申请人： MERCK SHARP & DOHME LTD.
发明人： BLACKABY, Wesley, Peter , CASTRO PINEIRO, Jose, Luis , GOODACRE, Simon, Charles , HALLETT, David, James , HUMPHRIES, Alexander, Charles , JONES, Philip , MERCHANT, Kevin, John , READER, Michael
IPC分类号： C07D471/04 , A61K31/505 , A61P25/28
CPC分类号： C07D471/04
摘要： A class of 8-fluoroimidazo[1,2-a]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

5. 发明公开

EP0986562A1 SUBSTITUTED 1,2,4-TRIAZOLO 3,4-A]PHTHALAZINE DERIVATIVES AS GABA ALPHA 5 LIGANDS 失效
标题翻译：取代的1,2,4-三唑并[3,4，-A]酞嗪衍生物作为GABA-ALPHA 5个配体
公开(公告)号：EP0986562A1
公开(公告)日：2000-03-22
申请号：EP98920635.4
申请日：1998-05-06
申请人： MERCK SHARP & DOHME LTD.
发明人： CARLING, William, Robert , LADDUWAHETTY, Tamara , MACLEOD, Angus, Murray , MERCHANT, Kevin, John , MOORE, Kevin, William , STERNFELD, Francine , STREET, Leslie, Joseph
IPC分类号： C07D487/04 , A61K31/50
CPC分类号： C07D487/04
摘要： A compound of formula (I) wherein R1 is hydrogen, halogen or CN or a group CF¿3?, OCF3, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy, each of which groups is unsubstituted or substituted with one or two halogen atoms or with a pyridyl or phenyl ring each of which rings may be unsubstituted or independently substituted by one or two halogen atoms or nitro, cyano, amino, methyl or CF3 groups; R?2¿ is hydrogen, halogen or CN or a group CF¿3?, OCF3, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy each of which groups is unsubstituted or substituted with one or two halogen atoms; L is O, S, or NR?n¿ where Rn is H, C¿1-6?alkyl or C3-6cycloalkyl; X is a five or six-membered optionally substituted heterocycle; Y is optionally branched C1-4alkylidene optionally substituted by an oxo group or Y is a group (CH2)jO wherein the oxygen atom is nearest the group X and j is 2, 3 or 4; Z is a five or six-membered optionally substituted heterocycle; or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising it, its use in medical treatment, processes for producing it and intermediates used in those processes are disclosed.

6. 发明公开

EP0861245A1 PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES 失效
标题翻译：哌啶和四氢吡啶衍生物
公开(公告)号：EP0861245A1
公开(公告)日：1998-09-02
申请号：EP96938351.0
申请日：1996-11-14
申请人： MERCK SHARP & DOHME LTD.
发明人： CHAMBERS, Mark, Stuart , HOBBS, Sarah, Christine , LADDUWAHETTY, Tamara , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
IPC分类号： C07D401 , C07D413 , C07D521
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D413/14
摘要： A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1Dα receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT1Dα receptor subtype relative to the 5-HT1Dβ subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.

7. 发明公开

EP0775140A1 SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 失效
标题翻译：螺取代的氮杂双环衍生物及其治疗用途
公开(公告)号：EP0775140A1
公开(公告)日：1997-05-28
申请号：EP95927861.0
申请日：1995-08-07
申请人： MERCK SHARP & DOHME LTD.
发明人： LADDUWAHETTY, Tamara , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MERCHANT, Kevin, John
IPC分类号： A61K31 , A61P1 , A61P11 , A61P25 , A61P29 , A61P37 , A61P43 , C07D471
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C1-6alkyl, C1-6alkoxy, hydroxy, halogen, cyano, trifluoromethyl, SO2C1-6alkyl, NR?aRb, NRaCORb¿ or CONRaRb, where R?a and Rb¿ are each H, C¿1-6?alkyl, phenyl or trifluoromethyl; R?1¿ represents phenyl optionally substituted by 1, 2 or 3 of C¿1-6?alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, -O(CH2)pO- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR?a, SRa, SORa, SO¿2R?a, NRaRb, NRaCORb, NRaCO¿2R?b, CORa, CO¿2Ra or CONRaRb; naphthyl; benzhydryl; or benzyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C¿1-6?alkyl, C1-6alkoxy, halogen or trifluoromethyl; R?2¿ represents hydrogen, a substituent as defined for R1 or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C¿1-6?alkyl, C1-6alkoxy, halogen or trifluoromethyl; R?3 and R4¿ are each H or C¿1-6?alkyl or R?3 and R4¿ together are linked so as to form a C¿1-3?alkylene chain; R?5¿ represents H, C¿1-6?alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenylC1-4alkyl, CO2R?a, CONRaRb, SORa¿ or SO¿2R?a, wherein the phenyl moiety may be substituted by C¿1-6?alkyl, C1-6alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represent =O; and Z represents a bond, O, S, SO, SO2, NR?6¿, or -(CR6R6)- where R6 is H or C¿1-6?alkyl; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

8. 发明公开

EP0711281A1 4-PHENYL-4-PHENYLPROPYL(ENYL)-PIPERIDINES AS TACHYKININ ANTAGONISTS 失效
标题翻译： 4-苯基-4-苯基丙基（环烯基） - 哌啶ALS TACHYKININ-ANTAGONISTEN
公开(公告)号：EP0711281A1
公开(公告)日：1996-05-15
申请号：EP94921065.0
申请日：1994-07-21
申请人： MERCK SHARP & DOHME LTD.
发明人： MACLEOD, Angus, Murray , MERCHANT, Kevin, John , STEVENSON, Graeme, Irvine
IPC分类号： A61K31 , A61P1 , A61P25 , A61P29 , A61P43 , C07D211 , C07D401
CPC分类号： C07D401/06 , C07D211/18 , C07D211/22 , C07D211/32
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R?4, R5, R6 and R7¿; 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; R1 represents optionally substituted phenyl; R2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R3 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 optionally substituted phenyl), Y-R8 or CO-Z-(CH¿2?)q-R?12; R4 and R5¿ each independently represent H, C¿1-6?alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, hydroxy or C1-6alkoxy, or R?4 and R5¿ together form a group =0; R?6 and R7¿ each independently represents H, C¿1-6?alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, hydroxy or C1-6alkoxy or R?6 and R7¿ together form a group =0; R8 represents an optionally substituted aromatic heterocycle; R9 represents H, C¿1-6?alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, or phenyl; R?10 and R11¿ each independently represent H, C¿1-6?alkyl, C3-6cycloalkyl or C3-5cycloalkylmethyl; 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, C3-6cycloalkyl, C3-5cycloalkylmethyl, optionally substituted phenyl or phenylC1-4alkyl; R?15¿ represents C¿1-6?alkyl, C3-6cycloalkyl, C3-5cycloalkylmethyl, trifluoromethyl or optionally substituted phenyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which may optionally be substituted by oxo; Z represents CH2, O, S or NR?10¿; and q represents 0, 1, 2, 3, 4, 5 or 6. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.

9. 发明授权

EP1824817B1 ARYLSULFONYLNAPHTHALENE DERIVATIVES AS 5HT2A ANTAGONISTS 有权
标题翻译：亚油酸磷酸盐酸盐5HT2A拮抗剂
公开(公告)号：EP1824817B1
公开(公告)日：2009-02-04
申请号：EP05813608.6
申请日：2005-11-28
申请人： MERCK SHARP & DOHME LTD.
发明人： CHAMBERS, Mark, Stuart , CURTIS, Neil, Roy , GANCIA, Emanuela , GILLIGAN, Myra , HUMPHRIES, Alexander, Charles , LADDUWAHETTY, Tamara , MAXEY, Robert, James , MERCHANT, Kevin, John
IPC分类号： C07C317/14 , C07D213/71 , C07D215/36 , C07D471/02 , C07D241/12 , A61K31/10 , A61K31/275 , A61K31/4409 , A61K31/47 , A61P25/00
CPC分类号： C07D401/12 , C07C311/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/42 , C07C317/44 , C07C323/65 , C07C2601/04 , C07D213/61 , C07D213/64 , C07D213/70 , C07D215/36 , C07D215/60 , C07D233/64 , C07D241/12 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D271/10 , C07D277/26 , C07D333/34 , C07D471/04 , C07D473/38
摘要： Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译：式（I）化合物是有效和选择性的5-HT2A拮抗剂，可用于治疗CNS的多种不利条件。

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