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公开(公告)号:US5703240A
公开(公告)日:1997-12-30
申请号:US612843
申请日:1996-03-21
申请人: Duncan Robert Armour , Brian Evans , David Middlemiss , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson
发明人: Duncan Robert Armour , Brian Evans , David Middlemiss , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/56 , C07D401/10 , C07D401/12
CPC分类号: C07D401/12
摘要: The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group; R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sup.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group; R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译: PCT No.PCT / EP94 / 03129 Sec。 371日期1996年3月21日 102(e)1996年3月21日PCT PCT 1994年9月20日PCT公布。 第WO95 / 08549号公报 日期:1995年3月30日本发明涉及式(I)的哌啶衍生物其中R 1为C 1-4烷氧基; R 2是氢或卤素原子; R 4和R 5可各自独立地表示氢或卤素原子,或C 1-4烷基,C 1-4烷氧基或三氟甲基; R6是氢原子,C1-4烷基,(CH2)环丙基,-S(O)nC1-4烷基,苯基,NR7R8,CH2C(O)CF3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0,1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。
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公开(公告)号:US5843966A
公开(公告)日:1998-12-01
申请号:US899190
申请日:1997-07-23
申请人: Duncan Robert Armour , Brian Evans , David Middlemiss , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin
发明人: Duncan Robert Armour , Brian Evans , David Middlemiss , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/56 , C07D401/10 , C07D401/12
CPC分类号: C07D401/12
摘要: The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group; R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sub.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group; R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译: 本发明涉及式(I)的哌啶衍生物其中R 1为C 1-4烷氧基; R 2是氢或卤素原子; R 4和R 5可各自独立地表示氢或卤素原子,或C 1-4烷基,C 1-4烷氧基或三氟甲基; R6是氢原子,C1-4烷基,(CH2)环丙基,-S(O)nC1-4烷基,苯基,NR7R8,CH2C(O)CF3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0,1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。
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公开(公告)号:US07601729B2
公开(公告)日:2009-10-13
申请号:US10571443
申请日:2004-09-10
IPC分类号: A61K31/513 , A61K31/4035 , C07D409/02 , C07D403/02
CPC分类号: C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH═CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1′ each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl; R7 and R8 each independently represent H, halo, C1-6 alkyl or C1-4 alkylaryl; R9 and R10 each independently represents H, C1-6 alkyl optionally substituted by halo, cyano, OR11 or NR6R11, C1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR6R11, OR11 or, together with the N to which they are attached, R9 and R10 form a heterocyclic group: R11 represents H, C1-6 alkyl, C1-4 alkylaryl or COR5; R12 and R13 each independently represent H, C1-3 alkyl, C1-3 alkylaryl or C1-3 alkylheteroaryl or, together with the functionality to which they are attached, R12 and R13 form a heterocyclic group: R14 and R15 each independently represent H, C1-6 alkyl, C1-4 alkylaryl or C1-4 alkylheteroaryl or together with the functionality to which they are attached R14 and R15 form a heterocyclic or fused heterocyclic group; and physiologically functional derivatives thereof, corresponding processes for preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs).
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公开(公告)号:US07375248B2
公开(公告)日:2008-05-20
申请号:US10561055
申请日:2004-06-16
申请人: Ian Holmes , Stephen Paul Watson
发明人: Ian Holmes , Stephen Paul Watson
IPC分类号: C07C315/00 , C07C229/00 , A01N37/34 , A01N37/12
CPC分类号: C07D213/42 , C07C311/08
摘要: Compounds of formula (I): wherein R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR4, OCR4R5, CR4R5O, or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents COR3 or N(OR8)COR9; R2 represents SO2R10 or SO2NR10R11; R3 represents OR6, NR6R7 or NR6OH; R4 and R5 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R6 and R7 each independently represents H, C1-6 alkyl, or C1-6 alkyl substituted with one or more heteroaryl groups, or R6 and R7 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; R8 and R9 each independently represents H or C1-6 alkyl; R10 and R11 each independently represents H or C1-6 alkyl; and and physiologically functional derivatives thereof, with the exception of N-(ethoxycarbonyl)-N-[4-(1H-tetrazol-1-yl)phenyl]glycine, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metalloproteinase enzymes (MMPs) are described.
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公开(公告)号:US08263602B2
公开(公告)日:2012-09-11
申请号:US12266767
申请日:2008-11-07
IPC分类号: A61K31/505 , A61K31/405
CPC分类号: C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要: The present invention relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).
摘要翻译: 本发明涉及式(I)的化合物或其药学上可接受的盐,相应的制备方法,用作基质金属蛋白酶(MMPs)抑制剂的药物制剂和方法。
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公开(公告)号:US20110065725A1
公开(公告)日:2011-03-17
申请号:US12922101
申请日:2009-03-16
IPC分类号: A61K31/4192 , C07D401/12 , A61K31/4439 , C07D403/12 , A61K31/497 , C07D249/06 , A61K31/506 , C07D401/04 , A61P25/00 , A61P25/30
CPC分类号: C07D249/06 , C07D401/04 , C07D401/12 , C07D403/12
摘要: The invention relates to triazole amide derivatives of formula (I) for use in therapy, in particular for treating diseases and conditions mediated by antagonism of the mGluR5 receptor, in particular substance related disorders. The invention also relates to certain novel derivatives. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
摘要翻译: 本发明涉及式(I)的三唑酰胺衍生物,其用于治疗,特别是用于治疗由mGluR5受体的拮抗作用介导的疾病和病症,特别是与物质有关的疾病。 本发明还涉及某些新型衍生物。 此外,本发明涉及含有衍生物的组合物及其制备方法。
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公开(公告)号:US07476759B2
公开(公告)日:2009-01-13
申请号:US10569812
申请日:2004-08-12
申请人: Ian Holmes , Stephen Paul Watson
发明人: Ian Holmes , Stephen Paul Watson
IPC分类号: C07C229/00 , C07C255/00 , A01N47/00 , A01N37/12 , A01N37/44
CPC分类号: C07C235/78 , C07C233/51 , C07C235/34 , C07C255/57 , C07C2601/14 , C07D209/08 , C07D333/24
摘要: Compounds of Formula (I): wherein: R1 is optionally substituted —C4-12 alkyl, —C2-10alkylcycloalkyl, —C2-6alkylheterocycloalkyl, —C2-6alkylaryl, optionally substituted 5- or 6-membered aryl or heteroaryl with the proviso that R2 in not pyridinyl; Z is a bond, CH2, O, S, SO, SO2, NR4, OCR4R5 or CR4R5O; or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q is an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X is COR3; R2 is CONH2, CO2H, CO2R7, SO2R7 or SO2NR8R9, with the proviso that R2 is not CO2R7, when X is CONH2; R3 is OR6 or NR8R9; R4 and R5 each independently is H, C1-6 alkyl or C1-4 alkylaryl; R6 is H or C1-6 alkyl; R7 is C1-6 alkyl; and R8 and R9 each independently is H or C1-6 alkyl; or R8 and R9 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; or physiologically functional derivatives thereof, with the proviso that formula (I) compounds are not: [3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid and 3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid diethyl ether; butanedioic acid [3-methoxy-4-(phenylmethoxy)phenyl]; or butanedioic acid [4-(phenylmethoxy)phenyl]; and with the proviso that when R1 is C4-12alkyl, Z is other than a bond, O or CH2; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.
摘要翻译: 式(I)的化合物:其中:R 1是任选取代的C 1-4-12烷基,-C 2-10烷基环烷基,-C 2-6烷基杂环烷基,-C 2-6烷基芳基,任选取代的5-或6-元芳基或杂芳基,条件是R 2 非吡啶基; Z是键,CH2,O,S,SO,SO2,NR4,OCR4R5或CR4R5O; 或Z,R 1和Q一起形成任选取代的稠合三环基团; Q是任选取代的5或6元芳基或杂芳基环; X是COR3; R2是CONH2,CO2H,CO2R7,SO2R7或SO2NR8R9,条件是当X是CONH2时,R2不是CO2R7; R3是OR6或NR8R9; R 4和R 5各自独立地为H,C 1-6烷基或C 1-4烷基芳基; R6是H或C1-6烷基; R7是C1-6烷基; 且R 8和R 9各自独立地为H或C 1-6烷基; 或R 8和R 9与它们所连接的氮原子一起形成5-或6-元环,其可任选地包括1个或多个选自O,S和N的其它杂原子; 或其生理功能衍生物,条件是式(I)化合物不是:[3-(乙酰氨基)-4-环己基苯基]丁二酸和3-(乙酰氨基)-4-环己基苯基]丁二酸二乙醚; 丁二酸[3-甲氧基-4-(苯基甲氧基)苯基]; 或丁二酸[4-(苯基甲氧基)苯基]; 并且条件是当R 1为C 4-12烷基时,Z不是键O或CH 2; 和其生理功能衍生物,其制备方法,含有它们的药物制剂及其作为基质金属蛋白酶(MMP)抑制剂的用途。
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公开(公告)号:US07250439B2
公开(公告)日:2007-07-31
申请号:US10559600
申请日:2004-06-01
IPC分类号: A61K31/40 , C07D209/46 , C07C315/00 , C07C229/00
CPC分类号: C07D307/91 , C07C17/16 , C07C59/48 , C07C59/54 , C07C59/56 , C07C59/68 , C07C59/90 , C07C205/56 , C07C233/54 , C07C255/57 , C07C323/62 , C07C2603/18 , C07D277/04 , C07C22/04
摘要: Compounds of formula (I): wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR5 or CR6 R7; Y represents CHOH, CHSH, NOR8, CNR8 or CNOR8; Z represents a bond, CR10R11, O, S, SO, SO2, NR10, OCR10R11, CR10R11 O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R1, R1′, R3 and R3′ each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R2 represents CO2R8, CONR5OR9 or NR5COR9; R4 represents optionally substituted 5- or 6-membered aryl or heteroaryl; R5 represents H or C1-3 alkyl; R6 and R7 each independently represents H, C1-3 alkyl or halo; R8 represents H or C1-2 alkyl; R9 represents H or C1-3 alkyl; R10 and R11 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metalloproteinase enzymes (MMPs) are described.
摘要翻译: 式(I)的化合物:其中:Q表示任选取代的5或6元芳基或杂芳基环; X表示O,S,NR 5或CR 6 R 7; Y代表CHOH,CHSH,NOR 8,CNR 8或CNOR 8; Z表示键,CR 10,O,S,SO,SO 2,NR 10, OCR 10,10,11,10,10,10或10,R 4,R 4, 和Q一起形成任选取代的稠合三环基团; R 1,R 1,R 3,R 3和R 3'各自独立地表示H,C 1, 1-6烷基或C 1-4烷基芳基; R 2表示CO 2 R 8,CONR 5或9或NR 9, 9< 9> R 4表示任选取代的5或6元芳基或杂芳基; R 5表示H或C 1-3烷基; R 6和R 7各自独立地表示H,C 1-3烷基或卤素; R 8表示H或C 1-12烷基; R 9表示H或C 1-3烷基; R 10和R 11各自独立地表示H,C 1-6烷基或C 1-4烷基芳基; 和其生理功能衍生物,其制备方法,含有它们的药物制剂及其作为基质金属蛋白酶(MMP)抑制剂的用途。
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公开(公告)号:US08343986B2
公开(公告)日:2013-01-01
申请号:US12551892
申请日:2009-09-01
IPC分类号: A61K31/505 , A61K31/403 , C07D209/36 , C07D239/70 , A61P37/02
CPC分类号: C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metalloproteinase enzymes (MMPs).
摘要翻译: 本发明涉及式(I)的化合物:其药学上可接受的盐,相应的制备方法,用作基质金属蛋白酶抑制剂(MMP)的药物制剂和方法。
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公开(公告)号:US20090082377A1
公开(公告)日:2009-03-26
申请号:US12266767
申请日:2008-11-07
IPC分类号: A61K31/513 , A61K31/4035
CPC分类号: C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要: The present invention relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).
摘要翻译: 本发明涉及式(I)的化合物或其药学上可接受的盐,相应的制备方法,用作基质金属蛋白酶(MMPs)抑制剂的药物制剂和方法。
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