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1. 发明申请

US20140357623A1 NEW ENZYME INHIBITOR COMPOUNDS 有权
公开(公告)号：US20140357623A1
公开(公告)日：2014-12-04
申请号：US14344417
申请日：2011-09-14
申请人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
发明人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

2. 发明申请

US20080221060A1 Therapeutic Compounds 审中-公开
公开(公告)号：US20080221060A1
公开(公告)日：2008-09-11
申请号：US10598520
申请日：2005-03-04
申请人： Martyn Pritchard , Jacqueline Ouzman , Edward Savory , Giles Brown
发明人： Martyn Pritchard , Jacqueline Ouzman , Edward Savory , Giles Brown
IPC分类号： A61K31/70 , C07H19/16 , A61P35/00
CPC分类号： C07H19/16
摘要： Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X=OH, R2=NH2, R5=CH2OH, R6=H, R1 is C5-C6 alkoxy, OCH2Cyclopropyl, O-(2,2,3,3-tetrafluoro-cycloButyl), phenoxy, substituted phenoxy, OCH2CH2OH, or OCH2CHF2, (5-indanyl)oxy, C1, C2, C5, or C6 alkylamino, (R) or (S)-sec-Butylamino, C5 or C6 cycloalkylamino, exo-norbornane amino, (N-methyl, N-isoamylamino), phenylamino, phenylamino with either methoxy or fluoro substituents, a C2 sulfone group, a C2 alkyl group, a cyano group, a CONH2 group, or 3,5-dimethylphenyl; or when X=H, R2=NH2, R5=CH2OH, R6=H, R1 is n-hexyloxy; or (II) when X=OH, R1=H, R5=CH2OH, R6=H, R2 is NMe2, N-(2-isopentenyl), piperazinyl, (N-Me, N-benzyl), (N-Me, N—CH2Ph(3-Br)), (N-Me, N—CH2Ph(3-CF3)), or (N-Me, N-(2-methoxyethyl)), or OCH2Cyclopentyl; or (III) when X=OH, R5=CONHR3, R6=H: R1 is H, R3 is an isopropyl group, and R2 is either NH2 or a methylamino group (NHMe) or an isoamyl group (CH2CH2CHMe2); or R1 is H, R3 is H, and R2 is NH2; or R1 is OMe, R3 is Ph, and R2 is NH2; or R1 is NHCH2CH2CH2CH2CH2Me, R3 is CH2CH2CH2Me, and R2 is NH2; or (IV) when X=OH, R1=H, R2=NH2, R5=CH2NHCOR4, R6=H, R1 is n-propyl or NHCH2CH3; or (V) when X=OH, R5=CH2OH, R6=H: R1 is NHCyclohexyl when R2 is NMe2; or R1 is OMe when R2 is NHBenzyl; or (VI) when X=OH, R2=NH2, R5=CH2OH, R6=Me, R1 is NHCyclohexyl or NHCyclopentyl.

3. 发明授权

US09150574B2 Enzyme inhibitor compounds 有权
公开(公告)号：US09150574B2
公开(公告)日：2015-10-06
申请号：US14344417
申请日：2011-09-14
申请人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
发明人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
IPC分类号： C07D471/02 , A61K31/55 , C07D471/04
CPC分类号： C07D471/04
摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

4. 发明申请

US20110195992A1 NEW COMPOUNDS II 失效
标题翻译：新化合物II
公开(公告)号：US20110195992A1
公开(公告)日：2011-08-11
申请号：US13062366
申请日：2009-09-16
申请人： Edward Savory , Iain Simpson
发明人： Edward Savory , Iain Simpson
IPC分类号： A61K31/437 , C07D471/04 , A61P19/02 , A61P29/00 , A61P1/04 , A61P25/00 , A61P25/28 , A61P11/00 , A61P17/06 , A61P17/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P1/16
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as such as inflammatory diseases and immune disorders.
摘要翻译：本发明涉及作为SSAO活性抑制剂的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，几何异构体，互变异构体，旋光异构体或N-氧化物。本发明还涉及包含这些化合物的药物组合物和这些化合物用于治疗其中SSAO活性的抑制是有益的医学病症的用途，例如炎性疾病和免疫疾病。

5. 发明申请

US20080076776A1 Therapeutic compounds 失效
标题翻译：治疗化合物
公开(公告)号：US20080076776A1
公开(公告)日：2008-03-27
申请号：US11823377
申请日：2007-06-26
申请人： Michael Higginbottom , Edward Savory , Giles Brown , Viet-Anh Horgan , Emma Chapman
发明人： Michael Higginbottom , Edward Savory , Giles Brown , Viet-Anh Horgan , Emma Chapman
IPC分类号： A61K31/497 , A61K31/52 , A61P43/00 , C07D487/00
CPC分类号： C07H19/16
摘要： Compounds of formula (I) below are disclosed. Their use as medicaments is described, in particular for the treatment of pain or inflammation: wherein: when X═Y=Z=OH, R1 is OCH2CF2CF3, phenoxy (substituted with 3-(4-trifluoromethylphenyl), 3,4-dichloro, (3-trifluoromethyl,4-fluoro), (3-trifluoromethyl,4-chloro), (3-chloro, 4-cyano), or 3,5-bis(trifluoromethyl)), 1-piperazinyl(4-(3,4-dichlorophenyl)), phenyl (substituted with 3,4-dichloro, 3,5-difluoro, 3,5-bis(trifluoromethyl) or 3,4,5-trifluoro) or 2-benzofuranyl; or when X═Y═OH and Z=OMe, R1 is OCH3, OCH2CHF2, OCH2cyclopentyl, O-(2,5-difluorophenyl) or (S)-sec-butylamino; or when X═H and Y=Z=OH, R1 is n-hexylamino or cyclopentylamino; or when (IV) X=Z=OH and Y═H, R1 is cyclopentylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了下式（I）的化合物。描述了其作为药物的用途，特别是用于治疗疼痛或炎症：其中：当XY = Z = OH时，R 1是OCH 2 2 CF 2 CF 3，苯氧基（被3-（4-三氟甲基苯基），3,4-二氯，（3-三氟甲基，4-氟），（3-三氟甲基，4-氯）），（3-氯，4-氰基）或3,5-双（三氟甲基）），1-哌嗪基（4-（3,4-二氯苯基）），苯基（被3,4-二氯，或三氟甲基或3,4,5-三氟）或2-苯并呋喃基; 或当XY-OH和Z = OMe时，R 1是OCH 3，OCH 2 CHF 2，OCH 环戊基，O-（2,5-二氟苯基）或（S） - 仲丁基氨基; 或当X-H和Y = Z = OH时，R 1是正己基氨基或环戊基氨基; 或当（IV）X = Z = OH和Y-H时，R 1是环戊基氨基; 或其药学上可接受的盐。

6. 发明授权

US08569338B2 Methods of using 4, 5, 6, 7-tetrahydroimidazo-[4,5-c]pyridine compounds 有权
标题翻译：使用4,5,6,7-四氢咪唑并[4,5-c]吡啶化合物的方法
公开(公告)号：US08569338B2
公开(公告)日：2013-10-29
申请号：US13567146
申请日：2012-08-06
申请人： Edward Savory , Michael Higginbottom , Kathryn Oliver , Viet-Anh Anne Horgan
发明人： Edward Savory , Michael Higginbottom , Kathryn Oliver , Viet-Anh Anne Horgan
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437
摘要： The present invention relates to a method for the treatment or prevention of inflammation, an inflammatory disease, an immune or an autoimmune disorder, which comprises administering to a mammal in need of such treatment an effective amount of a compound compound of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity.
摘要翻译：本发明涉及治疗或预防炎症，炎性疾病，免疫或自身免疫性疾病的方法，其包括向需要这种治疗的哺乳动物施用有效量的式（I）化合物和其药学上可接受的盐，溶剂化物，水合物，几何异构体，互变异构体，光学异构体或N-氧化物，其是SSAO活性的抑制剂。

7. 发明申请

US20130102587A1 New Enzyme Inhibitor Compounds 有权
标题翻译：新型酶抑制剂化合物
公开(公告)号：US20130102587A1
公开(公告)日：2013-04-25
申请号：US13634732
申请日：2011-03-14
申请人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
发明人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
IPC分类号： C07D471/04 , C07D491/08 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D491/08 , C07D498/08 , C07D519/00
摘要： Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.
摘要翻译：公开了抑制SSAO酶活性的化合物。还公开了包含这些化合物的药物组合物以及这些化合物在治疗或预防其中抑制SSAO活性有益的医学病症中的用途，例如炎性疾病，免疫疾病和抑制肿瘤生长。

8. 发明申请

US20080009461A1 Therapeutic compounds 失效
标题翻译：治疗化合物
公开(公告)号：US20080009461A1
公开(公告)日：2008-01-10
申请号：US11823191
申请日：2007-06-26
申请人： Edward Savory
发明人： Edward Savory
IPC分类号： A61K31/7076 , A61P19/02 , A61P25/04 , A61P29/00 , C07H19/167
CPC分类号： C07D473/18
摘要： The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2′-methoxy adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.
摘要翻译：本发明涉及通过使用2'-甲氧基腺苷前药改善腺苷类似物的口服药物吸收的方法以及这些前药用作药物的方法。本发明还涉及作为腺苷受体激动剂的前药的化合物及其作为治疗化合物，特别是作为镇痛或抗炎化合物或作为疾病改善抗风湿药物（DMARD）的用途的方法，使用这些化合物治疗或改善疼痛或炎症。

9. 发明授权

US09227967B2 Inhibitor compounds of semicarbazide-sensitive amine oxidases 有权
标题翻译：氨基脲敏感性胺氧化酶抑制剂化合物
公开(公告)号：US09227967B2
公开(公告)日：2016-01-05
申请号：US13634732
申请日：2011-03-14
申请人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
发明人： David Evans , Allison Carley , Alison Stewart , Michael Higginbottom , Edward Savory , Iain Simpson , Marianne Nilsson , Martin Haraldsson , Erik Nordling , Tobias Koolmeister
IPC分类号： C07D471/04 , C07D487/04 , C07D498/08 , C07D519/00 , C07D491/08
CPC分类号： C07D471/04 , C07D487/04 , C07D491/08 , C07D498/08 , C07D519/00
摘要： Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
摘要翻译：公开了抑制SSAO酶活性的化合物。还公开了包含这些化合物的药物组合物以及这些化合物在治疗或预防其中抑制SSAO活性有益的医学病症中的用途，例如炎性疾病，免疫疾病和抑制肿瘤生长。

10. 发明申请

US20080027081A1 Therapeutic compounds 失效
标题翻译：治疗化合物
公开(公告)号：US20080027081A1
公开(公告)日：2008-01-31
申请号：US11823335
申请日：2007-06-26
申请人： Edward Savory
发明人： Edward Savory
IPC分类号： A61K31/52 , A61P19/00 , A61P25/00 , A61P29/00 , C07D473/00
CPC分类号： A61K31/7076 , C07H19/167 , Y02A50/411
摘要： The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2′,3′-methylidene acetal adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.
摘要翻译：本发明涉及通过使用2'，3'-亚甲基缩醛腺苷前药改善腺苷类似物的口服药物吸收的方法，以及这些前药用作药物的方法。本发明还涉及作为腺苷受体激动剂的前药的化合物及其作为治疗化合物，特别是作为镇痛或抗炎化合物或作为疾病改善抗风湿药物（DMARD）的用途的方法，使用这些化合物治疗或改善疼痛或炎症。

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