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1. 发明申请

WO2004110995A1 N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译： N-吡咯烷-3-基酰胺衍生物作为丝氨酸蛋白酶和肾上腺素再摄取抑制剂
公开(公告)号：WO2004110995A1
公开(公告)日：2004-12-23
申请号：PCT/IB2004/001943
申请日：2004-06-07
申请人： PFIZER LIMITED , PFIZER INC. , FISH, Paul, Vincent , FRAY, Michael, Jonathan , LOVERING, Deborah, Jane , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
发明人： FISH, Paul, Vincent , FRAY, Michael, Jonathan , LOVERING, Deborah, Jane , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
IPC分类号： C07D207/14
CPC分类号： C07D207/14
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(X)Y, C 3 _ 8 cycloalkyl, aryl, het, aryl-C l _ 4 alkyl or het-C l _ 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1_ 8 allkyl, C 1 _ 8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C l _ 6 alkyl, C 1 _ 4 alkoxy-C 1 _ 6 alkyl and C1_ 4 alkyl-S-C 1 _ 4 alkyl; R 2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C 1 _ 8 alkyl, C 1 _ 8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF3, hydroxy-C 1 _ 6 alkyl, C1_4alkoxy-C 1 _ 6 alkyl and C1_ 4 alkyl-S-C 1 _ 4 alkyl; R 3 is C 1 _ 6 alkyl, C 3 _ 8 cycloalkyl, C 3 _ 8 cycloalkyl-C 1 _ 6 alkyl, aryl, het, aryl-C l _ 4 alkyl or het-C 1 _ 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1 _ 6 alkyl, C 1 _ 6 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1 _ 6 alkyl, C 1 _ 4 alkoxy - C 1 _ 6 alkyl and C 1 _ 4 alkyl-SC 1 _ 4 alkyl; X is S or O; Y is H, C 1 _ 6 alkyl, aryl, het, aryl-C 1 _ 4 alkyl or het-C 1 _ 4 alkyl; 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 center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
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（X）Y，C 3-8环烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基的取代基取代; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基的取代基取代; R 3是C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂芳基，C 1-4烷基或叔丁基C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。

2. 发明申请

WO2005068447A1 PIPERAZINE DERIVATIVES WHICH EXHIBIT ACTIVITY AS SEROTONIN AND NORADRENALINE RE-UPATKE INHIBITORS 审中-公开
标题翻译：作为丝氨酸和肾上腺素复制抑制剂的展示活性的哌嗪衍生物
公开(公告)号：WO2005068447A1
公开(公告)日：2005-07-28
申请号：PCT/IB2005/000016
申请日：2005-01-03
申请人： PFIZER LIMITED , PFIZER INC. , BISH, Gerwyn , BROWN, Alan, Daniel , FISH, Paul, Vincent , FRAY, Michael, Jonathan , STOBIE, Alan , WAKENHUT , Florian , WHITLOCK, Gavin, Alistair
发明人： BISH, Gerwyn , BROWN, Alan, Daniel , FISH, Paul, Vincent , FRAY, Michael, Jonathan , STOBIE, Alan , WAKENHUT , Florian , WHITLOCK, Gavin, Alistair
IPC分类号： C07D295/08
CPC分类号： C07D295/205 , C07D249/18 , C07D295/073 , C07D295/096
摘要： A compound of formula (I), wherein R 1 is H; R 2 is aryl, het, C 3-8 cycloalkyl, C 1-6 alkyl, (CH 2 ) z aryl or R 4 , wherein each of the cycloalkyl, aryl, het and R 4 groups is optionally substituted by at least one substituent independently selected from C 1-6 alkyl, C 1-6 alkoxy, OH, halo, CF 3 , OCF 3, OCHF 2 , O(CH 2 ) y CF 3 , CN, CONH 2 , CON(H)C 1-6 alkyl, CON(C 1-6 alkyl) 2 , hydroxy-C 1-6 alkyl, C l-4 alkoxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-4 alkoxy, SCF 3 , C 1-6 alkyISO 2 , C 1-4 alkyl-S-C l-4 alkyl, C 1-4 alkyl-S-, C 1-4 alkyINR 10 R 11 and NR 10 R 11 ; or R 1 and R 2 , together with the carbon atom to which they are bound, form a 5- or 6-membered carbocycle or a 5- or 6-membered heterocycle containing at least one N, O or S heteroatom; R 3 is aryl, het or R 4 , each optionally substituted by at least one substituent independently selected from C 1-6 alkyl, C 1-6 alkoxy, het, OH, halo, CF 3 , OCF 3 , OCHF 2 , O(CH 2 ) y CF 3 , CN, CONH 2 , CON(H)C 1-6 alkyl, CON(C 1-6 alkyl) 2 , hydroxy-C l-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-4 alkoxy, SCF 3 , C 1-6 alkyISO 2 , C 1-4 alkyl-S-C 1-4 alkyl, C 1-4 alkyl-S-, C 1-4 alkylNR 10 R 11 and NR 10 R 11 ; R 4 is a phenyl group fused to a 5- or 6 membered carbocycle, or a phenyl group fused to a 5- or 6-membered heterocycle containing at least one N, O or S heteroatom; R 5 is H or C 1- 6 alkyl; R 10 and R 11 are the same or different and are independently H or C 1-4 alkyl; A is a C 1-3 alkylene chain which is optionally substituted by OH, C 1-4 alkyl or C 1-4 alkoxy; x is an integer from 1 to 3; y is 1 or 2; z is an integer from 1 to 3; aryl is phenyl, naphthyl, anthracyl or phenanthryl; and het is 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 carbocycle or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom.
摘要翻译：式（I）的化合物，其中R 1是H; R 2是芳基，叔丁基，C 3-8环烷基，C 1-6烷基，（CH 2）z芳基或R 4，其中环烷基，芳基，杂环基和R 4基团中的每一个任选被至少一个取代基独立选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，OCHF 2，O（CH 2）y CF 3，CN，CONH 2，CON（H）C 1-6烷基，CON（C 1-6烷基）2，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基，C 1-4烷氧基-C 1-4烷氧基，SCF 3，C 1-6烷氧基SO 2，C 1-4烷基-S C 1-4烷基，C 1-4烷基-S-，C 1-4烷基， 11>和NR 10 R 11; 或R 1和R 2与它们所连接的碳原子一起形成5-或6-元碳环或含有至少一个N，O或S杂原子的5-或6-元杂环 ; R 3是芳基，杂环或R 4，各自任选被至少一个独立地选自C 1-6烷基，C 1-6烷氧基，羟基，OH，卤素，CF 3，OCF 3，OCHF 2，O（CH 2），CN，CONH 2，CON（H）C 1-6烷基，CON（C 1-6烷基）2，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基，C 1-4烷氧基-C 1-4烷氧基，SCF 3，C 1-6烷氧基， C 1-4烷基-S-C 1-4烷基，C 1-4烷基-S-，C 1-4烷基NR 10 R 11和NR 10 R 11; R 4是与5或6元碳环稠合的苯基或与含有至少一个N，O或S杂原子的5或6元杂环稠合的苯基; R 5是H或C 1-6烷基; R 10和R 11相同或不同，独立地为H或C 1-4烷基; A是任选被OH，C 1-4烷基或C 1-4烷氧基取代的C 1-3亚烷基; x是1至3的整数; y为1或2; z为1〜3的整数; 芳基为苯基，萘基，蒽基或菲基; 并且其是含有至少一个N，O或S杂原子的芳族或非芳香族4-，5-或6-元杂环，任选地与5或6元碳环或者第二个4-，或含有至少一个N，O或S杂原子的6元杂环。

3. 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，...，

4. 发明申请

WO2003076427A1 QUINAZOLINE COMPOUNDS USEFUL IN THERAPY 审中-公开
标题翻译：喹唑啉化合物有用于治疗
公开(公告)号：WO2003076427A1
公开(公告)日：2003-09-18
申请号：PCT/IB2003/000998
申请日：2003-03-05
申请人： PFIZER LIMITED , PFIZER INC. , BLAGG, Julian , FRAY, Michael, Jonathan , LEWIS, Mark, Llewellyn , MATHIAS, John, Paul , STEFANIAK, Mark, Henryk , STOBIE, Alan
发明人： BLAGG, Julian , FRAY, Michael, Jonathan , LEWIS, Mark, Llewellyn , MATHIAS, John, Paul , STEFANIAK, Mark, Henryk , STOBIE, Alan
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D471/04 , C07D487/04
摘要： Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R 1 represents C 1-4 alkyl; R 2 represents halo, C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyloxy, -S O2 (C1-4 alkyl), optionally substituted C 1-4 alkyloxy, Het or -OHet; R 3 represents a bicyclic group of the formula wherein X and Yare selected from C and N, provided that at least one is C; Ring A together with X and Y represents a 5- or 6-membered aromatic, ring containing 0, l, 2 or 3 nitrogen atoms in the ring; n is ), 1 or 2 L represents a direct link, C 1-4 alkylene or C 1-4 alkoxyalkylene; R 4 represents H, -NR 5 R 6 , C 3-6 cycloalkyl, -OR 7 , Het 1 or Het 4 ; R 5 and R 6 are independently selected from H, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-4 alkylene, -S O2 (C 1-4 alkyl) and optionally substituted C 1-4 alkyl. R 7 is selected from H, C 1-4 alkyl, C 1-4 alkoxyalkyl, C 3-6 cycloalkyl, Het 2 and C 1-4 alkyl-Het 3 ; R 8 is H or C 1-4 alkyl; Het, Het 1 , Het 2 and Het 3 independently represent an optionally substituted 4 to 7 membered saturated heterocyclic group which may be mono- or bi-cyclic and which contains one or more heteroatoms selected from N, O or S; Het 4 represents an optionally substituted 5 or 6 membered unsaturated heterocyclic group containing one or more heteroatoms selected from N, O or S; R 9 is H or C 1-4 alkyl; R 10 and R 11 are independently selected from H and C 1-4 alkyl; are useful in the treatment of hypertension, myocardial infarction, male erectile dysfunction (MED), hyperlipidaemia, cardiac arrhythmia, glaucoma and benign prostatic hyperplasia (BPH). They also find utility in the treatment of female sexual arousal dysfunction (FSAD).
摘要翻译：式（I）化合物或其药学上可接受的盐或溶剂合物，其中R 1表示C 1-4烷基; R 2表示卤素，C 1-4烷基，C 3-6环烷基，C 3-6环烷氧基，-SO 2（C 1-4烷基），任选取代的C 1-4烷氧基，Het或-OHet; R3表示下式的双环基团，其中X和Yare选自C和N，条件是至少一个是C; 环A与X和Y表示在环中含有0,1,2或3个氮原子的5-或6-元芳族环; n是），1或2 L表示直链，C 1-4亚烷基或C 1-4烷氧基亚烷基; R4表示H，-NR5R6，C3-6环烷基，-OR7，Het1或Het4; R 5和R 6独立地选自H，C 3-6环烷基，C 3-6环烷基-C 1-4亚烷基，-SO 2（C 1-4烷基）和任选取代的C 1-4烷基。 R 7选自H，C 1-4烷基，C 1-4烷氧基烷基，C 3-6环烷基，Het 2和C 1-4烷基-Het 3; R8是H或C1-4烷基; Het，Het1，Het2和Het3独立地表示任选取代的4至7元饱和杂环基团，其可以是单环或双环的并且含有一个或多个选自N，O或S的杂原子; Het4表示含有一个或多个选自N，O或S的杂原子的任选取代的5或6元不饱和杂环基; R9is H或C1-4烷基; R 10和R 11独立地选自H和C 1-4烷基; 可用于治疗高血压，心肌梗塞，男性勃起功能障碍（MED），高脂血症，心律失常，青光眼和良性前列腺增生（BPH）。它们也可用于治疗女性性唤醒功能障碍（FSAD）。

5. 发明授权

EP1047665B1 MATRIX METALLOPROTEASE INHIBITORS 有权
标题翻译：基质金属蛋白酶
公开(公告)号：EP1047665B1
公开(公告)日：2003-10-22
申请号：EP98966429.7
申请日：1998-12-23
申请人： Pfizer Limited , PFIZER INC.
发明人： FRAY, Michael, Jonathan , DICKINSON, Roger, Peter , DACK, Kevin, Neil
IPC分类号： C07C237/22 , C07C259/06 , A61K31/16
CPC分类号： C07D213/75 , C07B2200/07 , C07C237/22 , C07C259/06 , C07C259/18 , C07C2602/08 , C07D317/34 , Y02P20/55
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors.

6. 发明公开

EP1047665A1 MATRIX METALLOPROTEASE INHIBITORS 有权
标题翻译： MATRIXMETALLOPROTEINASEINHIBITOREN
公开(公告)号：EP1047665A1
公开(公告)日：2000-11-02
申请号：EP98966429.7
申请日：1998-12-23
申请人： Pfizer Limited , PFIZER INC.
发明人： FRAY, Michael, Jonathan , DICKINSON, Roger, Peter , DACK, Kevin, Neil
IPC分类号： C07C237/22 , C07C259/06 , A61K31/16
CPC分类号： C07D213/75 , C07B2200/07 , C07C237/22 , C07C259/06 , C07C259/18 , C07C2602/08 , C07D317/34 , Y02P20/55
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的盐，或任一实体的溶剂化物，其中取代基具有本文所述的值，可用作基质金属蛋白酶（MMP）抑制剂

7. 发明公开

EP0835252A1 TRIAZOLE ANTIFUNGAL AGENTS 失效
标题翻译：三唑含抗真菌药
公开(公告)号：EP0835252A1
公开(公告)日：1998-04-15
申请号：EP96921941.0
申请日：1996-06-05
申请人： Pfizer Research and Development Company, N.V./S.A. , Pfizer Limited
发明人： BELL, Andrew, Simon , FRAY, Michael, Jonathan , MARCHINGTON, Alan, Patrick , RICHARDSON, Kenneth , STEPHENSON, Peter, Thomas , WHITTLE, Peter, John
IPC分类号： C07D249 , A61K31 , A61K47 , A61P31 , C07D401 , C07D403 , C07D413 , C07D417 , C07D521
CPC分类号： C07D231/12 , A61K47/6951 , B82Y5/00 , C07D233/56 , C07D249/08
摘要： An antifungal agent of formula (I) or a pharmaceutically acceptable salt thereof, where Ar is a phenyl group substituted by 1 to 3 substituents each independently selected from halo and CF3; and X is a group of formula (a), (b), (c), or (d) wherein Z is H or F, and in which Het is a 5-membered nitrogen-containing aromatic heterocyclic group optionally containing an oxygen or sulfur atom and attached to the phenyl, pyridyl or pyrimidinyl group by a carbon or nitrogen atom and optionally substituted by 1 to 3 substituents each independently selected from halo; C1-C4 alkyl; (C1-C4 alkoxy)methyl; 2-(C1-C4 alkoxy)ethoxymethyl; 2-hydroxyethoxymethyl; cyanomethyl; -NR1R2 or -CH¿2?CONR?1R2¿ where R?1 and R2¿ are each independently H or C¿1?-C4 alkyl; phenylthio or phenyl-(C1 or C2 alkyl) in both of which said phenyl group is optionally substituted by halo, trifluoromethyl or C1-C4 alkyl; -NHCO(C1-C4 alkyl); -NHSO2(C1-C4 alkyl); -NHCONR?1R2¿ where R?1 and R2¿ are as defined above; mercapto; and -S(O)¿n?(C1-C4 alkyl) where n is 0, 1 or 2.

8. 发明公开

EP0783495A1 QUINOXALINE DERIVATIVES USEFUL IN THERAPY 失效
标题翻译：喹诺酮衍生物可用于治疗
公开(公告)号：EP0783495A1
公开(公告)日：1997-07-16
申请号：EP95932021.0
申请日：1995-09-08
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： FRAY, Michael, Jonathan , MOWBRAY, Charles, Eric , STOBIE, Alan
IPC分类号： C07D , A61K31 , A61P25 , C07D241 , C07D401 , C07D403 , C07D405 , C07D413
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I), wherein A represents N or CH; R?1 and R2¿ independently represent C¿1-4? alkyl, halo or CF3; R?3¿ represents C¿1-4? alkyl (optionally substituted), C3-7 cycloalkyl, CF3 or aryl; and R?4¿ represents H, C¿3-7? cycloalkyl or C1-6 alkyl (optionally substituted); and their pharmaceutically acceptable derivatives; are useful in the treatment of, inter alia, neurodogenerative disorders.
摘要翻译：式（I）化合物，其中A代表N或CH; R 1和R 2'独立地代表C 1-4- 烷基，卤素或CF 3; R？3代表C？1-4？烷基（任选取代的），C 3-7环烷基，CF 3或芳基; R 4表示H，C 3-7 - 环烷基或C 1-6烷基（任选取代的）; 和它们的可药用衍生物; 尤其用于治疗神经变性疾病。

9. 发明授权

EP0835252B1 TRIAZOLE ANTIFUNGAL AGENTS 失效
标题翻译：三唑含抗真菌药
公开(公告)号：EP0835252B1
公开(公告)日：2003-07-30
申请号：EP96921941.9
申请日：1996-06-05
申请人： Pfizer Research and Development Company, N.V./S.A. , Pfizer Limited
发明人： BELL, Andrew, Simon , FRAY, Michael, Jonathan , MARCHINGTON, Alan, Patrick , RICHARDSON, Kenneth , STEPHENSON, Peter, Thomas , WHITTLE, Peter, John
IPC分类号： C07D403/10 , C07D401/14 , C07D403/14 , C07D413/10 , C07D417/10 , C07D249/08 , A61K31/41
CPC分类号： C07D231/12 , A61K47/6951 , B82Y5/00 , C07D233/56 , C07D249/08

10. 发明授权

EP0783495B1 QUINOXALINE DERIVATIVES USEFUL IN THERAPY 失效
标题翻译：喹喔啉和它们的治疗用途
公开(公告)号：EP0783495B1
公开(公告)日：2002-02-27
申请号：EP95932021.9
申请日：1995-09-08
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： FRAY, Michael, Jonathan , MOWBRAY, Charles, Eric , STOBIE, Alan
IPC分类号： C07D241/44 , C07D401/12 , C07D403/12 , C07D405/12
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I), wherein A represents N or CH; R?1 and R2¿ independently represent C¿1-4? alkyl, halo or CF3; R?3¿ represents C¿1-4? alkyl (optionally substituted), C3-7 cycloalkyl, CF3 or aryl; and R?4¿ represents H, C¿3-7? cycloalkyl or C1-6 alkyl (optionally substituted); and their pharmaceutically acceptable derivatives; are useful in the treatment of, inter alia, neurodogenerative disorders.

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