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1. 发明申请

WO2003084947A1 4,5,6,7-TRETRAHYDROBENZO[B] THIOPHENE DERIVATIVES AND METHODS FOR MEDICAL INTERVENTION AGAINST MYCROBACTERIAL INFECTIONS 审中-公开
标题翻译： 4,5,6,7-三氢苯并[B]噻吩衍生物和用于医疗干预反应性巨噬细胞感染的方法
公开(公告)号：WO2003084947A1
公开(公告)日：2003-10-16
申请号：PCT/EP2003/003697
申请日：2003-04-09
申请人： AXXIMA PHARMACEUTICALS AG , MISSIO, Andrea , BACHER, Gerald , KOUL, Anil , CHOIDAS, Axel
发明人： MISSIO, Andrea , BACHER, Gerald , KOUL, Anil , CHOIDAS, Axel
IPC分类号： C07D333/68
CPC分类号： C07D409/12 , C07D333/66 , C07D333/68 , C07D409/14 , C07D495/04 , C07D495/14
摘要： Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases.
摘要翻译：描述了4,5,6,7-四氢苯并[b]噻吩衍生物及其药学上可接受的盐，这些衍生物用于预防和/或治疗分枝杆菌诱导的感染和机会性感染，以及至少含有一种4,5,6,7-四氢苯并[b]噻吩衍生物和/或其药学上可接受的盐。此外，本发明的用于识别和监测疾病和控制疾病治疗的这些激酶的检测和测定方法。

2. 发明申请

WO2004013633A2 MEDIUM AND METHOD FOR ENRICHING, PURIFYING OR DEPLETING ATP BINDING PROTEINS FROM A POOL OF PROTEINS 审中-公开
标题翻译：从蛋白质池中增殖，净化或减少ATP结合蛋白的培养基和方法
公开(公告)号：WO2004013633A2
公开(公告)日：2004-02-12
申请号：PCT/EP2003/008375
申请日：2003-07-29
申请人： AXXIMA PHARMACEUTICALS AG , GODL, Klaus , MISSIO, Andrea , DAUB, Henrik , STEIN-GERLACH, Matthias , GREFF, Zoltan
发明人： GODL, Klaus , MISSIO, Andrea , DAUB, Henrik , STEIN-GERLACH, Matthias , GREFF, Zoltan
IPC分类号： G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/6803 , G01N2333/91205
摘要： The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-l H -imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8 H -pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1 H -indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-3-(1 H -indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-4-(1-methyl-l H -indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2- a ]-indol-10-yl)-4-(1-methyl-l H -indol -3-y1)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-l-yl-methyl]- N -[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases from a pool of heterogeneous proteins.
摘要翻译：本发明涉及一种培养基和一种富含ATP结合蛋白的方法，蛋白质蛋白酶，来自蛋白质库，如蛋白质组。本发明的培养基包含特异性抑制剂，例如， 4- [4-（4-氟 - 苯基）-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺中的至少一种化合物，2- [4-（2-氨基 - 乙氧基） - 苯基氨基] -6-（2,6-二氯 - 苯基）-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮，2- [1-（3-氨基丙基）-1H-吲哚 -3-基）马来酰亚胺，3- [1-（3-氨基丙基）-1H-吲哚-3-基] -3-（1H-吲哚-3-基） - 马来酰亚胺，3- [1-（3-氨基丙基） -1H-吲哚-3-基] -4-（1-甲基-1H-吲哚-3-基）马来酰亚胺，3-（8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a ] - （1-甲基-1H-吲哚-3-基） - 马来酰胺，[6-（3-氨基 - 丙氧基） - 甲氧基 - 喹唑啉-4-基] - （3- 苯基） - 胺，6-（3-氨基 - 丙氧基）-7-甲氧基 - 喹唑啉-4-基 - （3-氯-4-氟 - 苯基） - 胺，6-（3Amino-丙氧基） - -7-甲氧基 - 喹唑啉-4-基] - （3-溴 - 苯基） - 胺和4- [4-（4-氨基 - 丁基） - 哌嗪-1-基 - 甲基] -N- [4-甲基 - 3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺固定在载体材料上。根据本发明的方法，上述固定化化合物用于选择性地结合来自异质蛋白库的蛋白激酶。

3. 发明申请

WO2005023818A2 HETEROBICYCLIC COMPOUNDS AS PHARMACEUTICALLY ACTIVE AGENTS 审中-公开
标题翻译：作为药物活性剂的杂环化合物
公开(公告)号：WO2005023818A2
公开(公告)日：2005-03-17
申请号：PCT/EP2004/010161
申请日：2004-09-10
申请人： AXXIMA PHARMACEUTICALS AG , KOUL, Anil , KLEBL, Bert , MÜLLER, Gerhard , MISSIO, Andrea , SCHWAB, Wilfried , HAFENBRADL, Doris , NEUMANN, Lars , SOMMER, Marc-Nicola , MÜLLER, Stefan , HOPPE, Edmund , FREISLEBEN, Achim , BACKES, Alexander , HARTUNG, Christian , FELBER, Beatrice , ZECH, Birgit , ENGKVIST, Ola , KERI, György , ÖRFI, Laszlo , BANHEGYI, Peter , GREFF, Zoltan , HORVÁTH, Zoltán , VARGA, Zoltán , MARKO, Péter , PATÓ, Jànos , SZABADKAI, István , SZÉKELYHIDI, Zsolt , WÁCZEK, Frigyes
发明人： KOUL, Anil , KLEBL, Bert , MÜLLER, Gerhard , MISSIO, Andrea , SCHWAB, Wilfried , HAFENBRADL, Doris , NEUMANN, Lars , SOMMER, Marc-Nicola , MÜLLER, Stefan , HOPPE, Edmund , FREISLEBEN, Achim , BACKES, Alexander , HARTUNG, Christian , FELBER, Beatrice , ZECH, Birgit , ENGKVIST, Ola , KERI, György , ÖRFI, Laszlo , BANHEGYI, Peter , GREFF, Zoltan , HORVÁTH, Zoltán , VARGA, Zoltán , MARKO, Péter , PATÓ, Jànos , SZABADKAI, István , SZÉKELYHIDI, Zsolt , WÁCZEK, Frigyes
IPC分类号： C07D495/00
CPC分类号： C07D409/12 , C07D209/42 , C07D333/66 , C07D333/68 , C07D491/04 , C07D493/04 , C07D495/04 , C07D495/10
摘要： Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
摘要翻译：描述了杂双环化合物，例如4,5,6,7-四氢＆shy;苯并[b]噻吩-3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3- C]噻喃＆害羞; 3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸酰胺或苯并[b]噻吩-3-羧酸酰胺及其药学上可接受的盐，其用途这些衍生物用于预防和/或治疗各种疾病，如感染性疾病，包括分枝杆菌和害羞;诱导感染和机会性疾病，朊病毒疾病，免疫性疾病，自身免疫性疾病，双相性和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经退行性疾病和中风，以及含有至少一种杂双环化合物和/或其药学上可接受的盐的组合物。此外，公开了用于合成杂双环化合物的反应程序。

4. 发明申请

WO2004013633A3 METHOD FOR ISOLATING ATP BINDING PROTEINS BY MEANS OF IMMOBOLIZED PROTEIN INHIBITORS 审中-公开
标题翻译：通过免疫蛋白抑制剂分离ATP结合蛋白的方法
公开(公告)号：WO2004013633A3
公开(公告)日：2004-10-28
申请号：PCT/EP0308375
申请日：2003-07-29
申请人： AXXIMA PHARMACEUTICALS AG , GODL KLAUS , MISSIO ANDREA , DAUB HENRIK , STEIN-GERLACH MATTHIAS , GREFF ZOLTAN , KLEBL BERT , ORFI LASZLO , KERI GYOERGY , VARGA ZOLTAN
发明人： GODL KLAUS , MISSIO ANDREA , DAUB HENRIK , STEIN-GERLACH MATTHIAS , GREFF ZOLTAN , KLEBL BERT , ORFI LASZLO , KERI GYOERGY , VARGA ZOLTAN
IPC分类号： A61K38/00 , C07D239/72 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/573 , G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/6803 , G01N2333/91205
摘要： The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-lH-imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1H-indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-3-(1H-indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-lH-indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2-a]-indol-10-yl)-4-(1-methyl-lH-indol -3-y1)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-l-yl-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases (e.g. p38, JNK1, JNK2, CK18, RICK, GAK) from a pool of heterogeneous proteins.
摘要翻译：本发明涉及一种培养基和一种富含ATP结合蛋白的方法，蛋白质蛋白酶，来自蛋白质库，如蛋白质组。本发明的培养基包含特异性抑制剂，例如， 4- [4-（4-氟 - 苯基）-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺中的至少一种化合物，2- [4-（2-氨基 - 乙氧基） - 苯基氨基] -6-（2,6-二氯 - 苯基）-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮，2- [1-（3-氨基丙基）-1H-吲哚 -3-基）马来酰亚胺，3- [1-（3-氨基丙基）-1H-吲哚-3-基] -3-（1H-吲哚-3-基） - 马来酰亚胺，3- [1-（3-氨基丙基） -1H-吲哚-3-基] -4-（1-甲基-1H-吲哚-3-基）马来酰亚胺，3-（8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a ] - （1-甲基-1H-吲哚-3-基） - 马来酰胺，[6-（3-氨基 - 丙氧基） - 甲氧基 - 喹唑啉-4-基] - （3- 苯基） - 胺，6-（3-氨基 - 丙氧基）-7-甲氧基 - 喹唑啉-4-基 - （3-氯-4-氟 - 苯基） - 胺，6-（3Amino-丙氧基） - -7-甲氧基 - 喹唑啉-4-基] - （3-溴 - 苯基） - 胺和4- [4-（4-氨基 - 丁基） - 哌嗪-1-基 - 甲基] -N- [4-甲基 - 3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺固定在载体材料上。根据本发明的方法，上述固定化化合物用于选择性地结合蛋白激酶（例如p38，JNK1，JNK2，CK18，RICK，GAK）从异源蛋白质库中。

5. 发明申请

WO2005105097A3 PYRIDOPYRIMIDINES FOR TREATING INFLAMMATORY AND OTHER DISEASES 审中-公开
公开(公告)号：WO2005105097A3
公开(公告)日：2005-11-10
申请号：PCT/EP2005/051892
申请日：2005-04-27
申请人： GPC BIOTECH AG , DAUB, Henrik , WISSING, Josef , MISSIO, Andrea , KLEBL, Bert
发明人： DAUB, Henrik , WISSING, Josef , MISSIO, Andrea , KLEBL, Bert
IPC分类号： A61K31/513 , A61P29/00 , A61P37/00
摘要： The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R 1 represents -NR 3 R 4 , -SR 3 , -SO-R 3 , -SO 2 -R 3 , -OR 3 ; R 2 , R 3 , and R 4 are independently of each other hydrogen, -(CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR 5 R 6 , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R 5 and R 6 are independently of each other hydrogen, (CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; R 5 and R 6 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R 4 can optionally be -CO-R 3 , -CO-OR 3 , -SO 2 -R 3 , -SO 2 -NR 5 R 6 , -CO-NR 5 R 6 , -CS-NR 5 R 6 , -C(=NH)-R 3 , -C(=NH)-NR 5 R 6 ; R 3 and R 4 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.

6. 发明申请

WO2005105097A2 PYRIDOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物衍生物
公开(公告)号：WO2005105097A2
公开(公告)日：2005-11-10
申请号：PCT/EP2005051892
申请日：2005-04-27
申请人： GPC BIOTECH AG , DAUB HENRIK , WISSING JOSEF , MISSIO ANDREA , KLEBL BERT
发明人： DAUB HENRIK , WISSING JOSEF , MISSIO ANDREA , KLEBL BERT
IPC分类号： A61K31/513 , A61P29/00 , A61P37/00
CPC分类号： A61K31/513
摘要： The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R represents -NR R , -SR , -SO-R , -SO2-R , -OR ; R , R , and R are independently of each other hydrogen, -(CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR R , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R and R are independently of each other hydrogen, (CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; R and R can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R can optionally be -CO-R , -CO-OR , -SO2-R , -SO2-NR R , -CO-NR R , -CS-NR R , -C(=NH)-R , -C(=NH)-NR R ; R and R can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.
摘要翻译：本发明涉及具有通式（I）的吡啶并嘧啶衍生物的用途，其中X表示= NH，= N-酰基，= O或= S; R 1表示-NR 3 R 4，-SR 3，-SO-R 3，-SO 2 -R 3，-OR 3; R 2，R 3和R 4彼此独立地为氢， - （CH 2）n Ph *，杂芳基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基，C 2 C 1-6 - 烯基，C 2 -C 6 - 炔基; 其中环烷基，烷基，烷酰基，烯基，炔基残基可以任选被一个或多个下列基团取代：-NR 5 R 6，苯基，取代的苯基，硫代烷基，烷氧基，羟基，羧基，卤素，环烷基 ; R 5和R 6彼此独立地为氢，（CH 2）n Ph *，杂芳基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基，C 2 -C 6 - 烯基， C6炔基; R 5和R 6可以与它们所连接的氮一起连接，以形成具有3至7个碳原子的环，任选地含有1,2或3个选自氮，氧和硫的杂原子; Ph *表示苯基或取代的苯基; n为0,1,2或3; R 4可以任选地是-CO-R 3，-CO-OR 3，-SO 2 -R 3，-SO 2 -NR 5 R 6，-CO-NR 5， R 6，-C 6 -NR 5 R 6，-C（= NH）-R 3，-C（= NH）-NR 5 R 6; R 3和R 4可以与它们所连接的氮一起连接，以形成具有3-7个碳原子的环，任选地含有1,2或3个选自氮，氧和硫的杂原子; Ar表示苯基，取代的苯基或杂芳基; 用于预防和/或治疗炎性疾病，神经变性疾病，免疫疾病，神经免疫疾病，自身免疫疾病，糖尿病，移植排斥，感染性疾病，朊病毒疾病，心血管疾病和病症的药学上可接受的盐。

7. 发明申请

WO2004016271A1 PYRIMIDONES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：吡咯烷酮作为抗病毒剂
公开(公告)号：WO2004016271A1
公开(公告)日：2004-02-26
申请号：PCT/EP2003/009039
申请日：2003-08-14
申请人： AXXIMA PHARMACEUTICALS AG , 4SC AG , MISSIO, Andrea , HERGET, Thomas , ASCHENBRENNER, Andrea , KRAMER, Bernd , LEBAN, Johann , WOLF, Kristina
发明人： MISSIO, Andrea , HERGET, Thomas , ASCHENBRENNER, Andrea , KRAMER, Bernd , LEBAN, Johann , WOLF, Kristina
IPC分类号： A61K31/513
CPC分类号： C07D239/36 , C07D405/06
摘要： The present invention relates to vinylpyrimidine-2-one derivatives of general formula (I). Furthermore the present invention relates to vinylpyrimidine-2-one derivatives and of general formula (Ia), wherein R 1 to R 6 in formula (I) and in formula (Ia) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
摘要翻译：本发明涉及通式（I）的乙烯基嘧啶-2-酮衍生物。此外，本发明涉及乙烯基嘧啶-2-酮衍生物和通式（Ia），其中式（I）和式（Ia）中的R 1至R 6彼此独立地表示各种不同的取代基包括烷基，芳基，芳烷基，烷基芳基，杂芳基和单官能部分。

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