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    • 1. 发明授权
      US07375248B2 Inhibitors of matrix metalloproteinase 失效
    • Inhibitors of matrix metalloproteinase
    • US07375248B2
    • 2008-05-20
    • US10561055
    • 2004-06-16
    • Ian Holmes , Stephen Paul Watson
    • Ian Holmes , Stephen Paul Watson
    • C07C315/00 , C07C229/00 , A01N37/34 , A01N37/12
    • C07D213/42 , C07C311/08
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 3. 发明授权
      US07476759B2 Matrix metalloproteinase inhibitors 失效
    • Matrix metalloproteinase inhibitors
    • 基质金属蛋白酶抑制剂
    • US07476759B2
    • 2009-01-13
    • US10569812
    • 2004-08-12
    • Ian Holmes , Stephen Paul Watson
    • Ian Holmes , Stephen Paul Watson
    • C07C229/00 , C07C255/00 , A01N47/00 , A01N37/12 , A01N37/44
    • C07C235/78 , C07C233/51 , C07C235/34 , C07C255/57 , C07C2601/14 , C07D209/08 , C07D333/24
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 4. 发明授权
      US07250439B2 Matrix metalloproteinase inhibitors 失效
    • Matrix metalloproteinase inhibitors
    • 基质金属蛋白酶抑制剂
    • US07250439B2
    • 2007-07-31
    • US10559600
    • 2004-06-01
    • Simon Gaines , Ian Peter Holmes , Stephen Paul Watson
    • Simon Gaines , Ian Peter Holmes , Stephen Paul Watson
    • A61K31/40 , C07D209/46 , C07C315/00 , C07C229/00
    • 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
    • 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.
    • 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＆lt; 9＆gt; 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 5. 发明授权
      US07601729B2 Matrix metalloproteinase inhibitors 失效
    • Matrix metalloproteinase inhibitors
    • US07601729B2
    • 2009-10-13
    • US10571443
    • 2004-09-10
    • Simon Gaines , Ian Peter Holmes , Stephen Lewis Martin , Stephen Paul Watson
    • Simon Gaines , Ian Peter Holmes , Stephen Lewis Martin , Stephen Paul Watson
    • A61K31/513 , A61K31/4035 , C07D409/02 , C07D403/02
    • C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
    • 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).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      US20080227858A1 Inhibitors of matrix metalloproteinase 审中-公开
    • Inhibitors of matrix metalloproteinase
    • US20080227858A1
    • 2008-09-18
    • US12122954
    • 2008-05-19
    • Ian Holmes , Stephen Paul Watson
    • Ian Holmes , Stephen Paul Watson
    • A61K31/277 , A61K31/195 , C07C311/30
    • C07D213/42 , C07C311/08
    • 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 OR6NR6R7 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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