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1. 发明申请

WO2008041090A1 MALANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONIST PYRIDINONES 审中-公开
标题翻译：马来浓浓度HORMONE受体-1拮抗剂吡啶酮
公开(公告)号：WO2008041090A1
公开(公告)日：2008-04-10
申请号：PCT/IB2007/002886
申请日：2007-09-24
申请人： PFIZER LIMITED , ARMOUR, Duncan, Robert , GALAN, Sebastien, Rene, Gabriel , LANE, Charlotte, Alice, Louise , LANSDELL, Mark, Ian , MILLS, James, Edward, John , SCIAMMETTA, Nunzio , STUPPLE, Paul, Anthony
发明人： ARMOUR, Duncan, Robert , GALAN, Sebastien, Rene, Gabriel , LANE, Charlotte, Alice, Louise , LANSDELL, Mark, Ian , MILLS, James, Edward, John , SCIAMMETTA, Nunzio , STUPPLE, Paul, Anthony
IPC分类号： C07D213/74 , C07D487/04 , A61K31/4412 , A61P3/04
CPC分类号： C07D213/74 , C07D487/04
摘要： The present invention provides for MCHR1 antagonist compounds of formula (I), and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein the substituents are as defined herein, and the pharmaceutically acceptable salts, solvates and prodrugs thereof, which are useful in treating diseases or conditions wherein antagonism of the MCHR1 receptor is beneficial.
摘要翻译：本发明提供式（I）的MCHR1拮抗剂化合物及其药学上可接受的盐，溶剂合物和前药，其中取代基如本文所定义，及其药学上可接受的盐，溶剂合物和前药，其可用于治疗疾病或其中MCHR1受体拮抗作用有益的条件。

2. 发明申请

WO2007015162A1 PIPERIDINOYL-PYRROLIDINE AND PIPERIDINOYL-PIPERIDINE COMPOUNDS 审中-公开
标题翻译：哌啶二吡咯烷和哌啶二酚哌啶化合物
公开(公告)号：WO2007015162A1
公开(公告)日：2007-02-08
申请号：PCT/IB2006/002151
申请日：2006-07-26
申请人： PFIZER LIMITED , ANDREWS, Mark, David , BROWN, Alan, Daniel , FRADET, David, Sebastien , LANSDELL, Mark, Ian
发明人： ANDREWS, Mark, David , BROWN, Alan, Daniel , FRADET, David, Sebastien , LANSDELL, Mark, Ian
IPC分类号： C07D401/06 , C07D405/14 , A61K31/454 , A61K31/4545 , A61P3/04 , A61P15/00
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention relates to a class of compounds of general formula (I) and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R 6 , R 7 and R 10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
摘要翻译：本发明涉及一类通式（I）的化合物及其盐，水合物，溶剂合物，多晶型物和前药，其中n，R 6，R 7和R 7 特别是式（I）的MCR4激动剂化合物在药物中的用途，特别是用于治疗性功能障碍和肥胖症的中间体在其合成中的用途以及含有他们。

3. 发明申请

WO2007096763A3 MELANOCORTIN TYPE 4 RECEPTOR AGONIST PIPERIDINOYLPYRROLIDINES 审中-公开
公开(公告)号：WO2007096763A3
公开(公告)日：2007-08-30
申请号：PCT/IB2007/000456
申请日：2007-02-19
申请人： PFIZER LIMITED , ANDREWS, Mark, David , BROWN, Alan, Daniel , LANSDELL, Mark, Ian , SUMMERHILL, Nicholas, William
发明人： ANDREWS, Mark, David , BROWN, Alan, Daniel , LANSDELL, Mark, Ian , SUMMERHILL, Nicholas, William
IPC分类号： C07D401/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I), wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.

4. 发明申请

WO2004111003A1 AMIDE DERIVATIVES AS SELECTIVE SEROTONIN RE-UPTAKE INHIBITORS 审中-公开
标题翻译：作为选择性丝氨酸重新吸收抑制剂的酰胺衍生物
公开(公告)号：WO2004111003A1
公开(公告)日：2004-12-23
申请号：PCT/IB2004/001915
申请日：2004-06-04
申请人： PFIZER LIMITED , PFIZER INC. , ANDREWS, Mark, David , BROWN, Alan, Daniel , FRADET, David, Sebastien , GORDON, David, William , LANSDELL, Mark, Ian , MACKENNY, Malcolm, Christian
发明人： ANDREWS, Mark, David , BROWN, Alan, Daniel , FRADET, David, Sebastien , GORDON, David, William , LANSDELL, Mark, Ian , MACKENNY, Malcolm, Christian
IPC分类号： C07D211/58
CPC分类号： C07D401/12 , C07D207/14 , C07D211/58
摘要： The present invention relates to compounds of formula (I), wherein R 1 is selected from: (a) (C 1 -C 6 )alkyl, optionally substituted by 1-3 substituents, each independently selected from: (i) CF 3 , OH, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 1 -C 6 )alkoxy and halo; (ii) Phenyl, optionally fused with phenyl or cyclohexyl, said phenyl or fused phenyl optionally substituted with 1-3 groups selected from (C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl ester, OH and halo; and (b) (C 3 -C 6 )cycloalkyl, optionally fused with (C 5 -C 7 )cycloalkyl, said cycloalkyl or fused cycloalkyl optionally substituted by OH, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy and halo. R 2 is Phenyl, optionally fused to (C 4 -C 6 )cycloalkyl, phenyl or pyridyl, said phenyl or fused phenyl moiety optionally substituted with 1-3 groups each independently selected from (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo and OH. n is 1 to 2 and pharmaceutically acceptable salts, solvates or polymorphs thereof; With the proviso that when n is 2 and R 1 is 2-(3,4-dimethoxylphenyl)-1-ethyl, 3,3diphemyl-1-propyl or 2,4-difluorophenyl, then R 2 cannot be 4-trifluoromethoxyphenyl, 2,4,6-trimethoxyphenyl, 4-acetoxyphenyl or 2,4-difluorophenyl; which are a class of selective serotonin re-uptake inhibitors (SSRIs).
摘要翻译：本发明涉及式（I）化合物，其中R 1选自：（a）任选被1-3个取代基取代的（C 1 -C 6）烷基，各自独立地选自：（i）CF 3，OH ，（C 1 -C 6）烷基，（C 3 -C 6）环烷基，（C 1 -C 6）烷氧基和卤素; （ii）苯基，任选地与苯基或环己基稠合，所述苯基或稠合苯基任选被1-3个选自（C 1 -C 6）烷基，（C 1 -C 6）烷基酯，OH和卤素的基团取代; 任选地与（C 5 -C 7）环烷基稠合的所述环烷基或任选被OH，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基和卤素取代的稠合环烷基。 R 2是苯基，任选地与（C 1 -C 6）环烷基，苯基或吡啶基稠合，所述苯基或稠合苯基部分任选被1-3个基团独立地选自（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，卤素和OH。 n为1〜2及其药学上可接受的盐，溶剂合物或多晶型物; 条件是当n为2且R 1为2-（3,4-二甲氧基苯基）-1-乙基，3,3,6-二甲基-1-丙基或2,4-二氟苯基时，则R 2不能为 4-三氟甲氧基苯基，2,4,6-三甲氧基苯基，4-乙酰氧基苯基或2,4-二氟苯基; 其是一类选择性5-羟色胺再摄取抑制剂（SSRI）。

5. 发明申请

WO2006064351A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006064351A2
公开(公告)日：2006-06-22
申请号：PCT/IB2005/003791
申请日：2005-12-08
申请人： PFIZER LIMITED , ANDREWS, Mark, David , BROWN, Alan, Daniel , FISH, Paul, Vincent , FRAY, Michael, Jonathan , LANSDELL, Mark, Ian , RYCKMANS, Thomas , STOBIE, Alan , VAKENHUT, Florian , GRAY, David, Lawrence, Firman
发明人： ANDREWS, Mark, David , BROWN, Alan, Daniel , FISH, Paul, Vincent , FRAY, Michael, Jonathan , LANSDELL, Mark, Ian , RYCKMANS, Thomas , STOBIE, Alan , VAKENHUT, Florian , GRAY, David, Lawrence, Firman
IPC分类号： C07D207/34 , C07D401/12 , C07D211/58 , A61K31/40 , A61P13/00 , A61P25/24 , A61P29/00
CPC分类号： C07D207/14 , C07D211/58 , C07D401/12
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 is H, C 1-6 alkyl, -C(A)Y, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C l-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; Y is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; aryl is independently selected from phenyl, naphthyl, anthracyl or phenanthryl; het is independently selected from an aromatic or non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R 2 is aryl 1 or het 1 , each optionally substituted; aryl 1 is independently selected from phenyl, naphthyl, anthracyl, phenanthryl, or indanyl; het 1 is an aromatic 5 to 10 membered heterocyclic ring system which contains at least one N, O or S heteroatom, optionally containing an aryl group; R 3 is H, C 1-8 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, C 1-8 alkylSC 1-8 alkyl, het 3 , or het 3 -C 1-4 alkyl, wherein the alkyl, cycloalkyl and het 3 groups are each optionally substituted; het 3 is a non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; or R 3 is (CH 2 ) a , K, wherein a' is 0, 1 or 2 and K is a group selected from: Formula (i) wherein: Z is O, S, NR 12 , (CH 2 ) V or a bond; a is 1, 2, 3 or 4; b is 1, 2 or 3; v is 1 or 2; R 10 and R 11 are each independently H or C 1-4 alkyl; R 12 is H, C 1-6 alkyl, C(O)C 1-6 alkyl, SO 2 -C 1-6 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula(iii) wherein: c is 1, 2, 3 or 4; d is 1, 2 or 3; e is 1 or 2; and R 30 is H or C 1-4 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: f is 0, 1, 2 or 3; L is SO, SO 2 or NR 40 ; and R 40 is H, C 1-6 alkyl, C(O)C 1-6 alkyl, SO 2 -C 1-6 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (v) wherein: g is 0, 1, 2 or 3; and R 50 is H, C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCHF 2 , OCF 3, SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; and Formula (vi) CH(cyclopropane) 2 ; X is a covalent bond, C 1-8 alkyl or C 3-8 cycloalkyl, wherein if X is C 3-8 cycloalkyl, then R 2 -X may form a fused aryl-cycloalkyl ring system; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre.
摘要翻译：式（I）化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1是H，C 1-6烷基，-C（A）Y C 3-8环烷基，芳基，苯基，芳基-C 1-4烷基或叔-C 1-4烷基，其中环烷基，芳基或苯基基团任选被取代; A是S或O; Y是H，C 1-6烷基，芳基，苯基，芳基-C 1-4烷基或叔丁基C 1-4烷基 ; 芳基独立地选自苯基，萘基，蒽基或菲基; 独立地选自芳族或非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5-或6-元碳环基团或第二4- 含有至少一个N，O或S杂原子的5-或6-元杂环; R 2是每个任选被取代的芳基1或1或1; 芳基1独立地选自苯基，萘基，蒽基，菲基或茚满基; 包含至少一个任选含有芳基的N，O或S杂原子的芳族5至10元杂环系统; R 3是H，C 1-8烷基，C 3-8环烷基，C 3-8环烷基 C 1-6烷基，C 1-8烷基，C 1-6烷基，H 3或H 3 其中烷基，环烷基和叔丁基各自任选被取代; 它是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5-或6-元碳环基团或含有至少一个N，O或S杂原子的第二个4-，5-或6-元杂环; 或R 3是（CH 2）2，...，

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