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1. 发明授权

US08247610B2 Amine linked modulators of γ-secretase 有权
标题翻译： γ-分泌酶的胺连接调节剂
公开(公告)号：US08247610B2
公开(公告)日：2012-08-21
申请号：US12253444
申请日：2008-10-17
申请人： Chih Yung Ho , Yan Zhang , Umar S. M. Maharoof , John Harrison , Jeremy Major , Svenja Burckhardt , Alison Jones
发明人： Chih Yung Ho , Yan Zhang , Umar S. M. Maharoof , John Harrison , Jeremy Major , Svenja Burckhardt , Alison Jones
IPC分类号： C07C211/00 , C07D213/72 , C07D213/00 , A61K31/135 , A61K31/44
CPC分类号： C07C229/42 , C07C229/34 , C07C255/58 , C07C2602/10 , C07D209/08 , C07D213/74 , C07D215/06 , C07D215/12 , C07D215/38 , C07D217/04
摘要： The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
摘要翻译：本发明涉及如下所示的式I化合物，其中A，X，Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9的定义在说明书中提供。式I化合物可用于治疗与γ-分泌酶活性相关的疾病，包括阿尔茨海默氏病。

2. 发明授权

US08252935B2 Piperidinyl and piperazinyl modulators of γ-secretase 有权
标题翻译： γ-分泌酶的哌啶基和哌嗪基调节剂
公开(公告)号：US08252935B2
公开(公告)日：2012-08-28
申请号：US12251521
申请日：2008-10-15
申请人： Chih Yung Ho , Yan Zhang , Umar S. M. Maharoof , Jeremy Major , John Harrison
发明人： Chih Yung Ho , Yan Zhang , Umar S. M. Maharoof , Jeremy Major , John Harrison
IPC分类号： C07D211/08 , C07D237/00 , A61K31/497 , A61K31/445
CPC分类号： C07D295/155 , C07D211/18 , C07D211/38 , C07D241/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D417/06
摘要： The present invention relates to compounds of Formula I as shown below, wherein the definitions of Het, R0, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
摘要翻译：本发明涉及如下所示的式I化合物，其中Het，R0，R1R2，R3，R4，R5，R6，R7，R8和R9的定义在说明书中提供。式I化合物可用于治疗与γ-分泌酶活性相关的疾病，包括阿尔茨海默氏病。

3. 发明授权

US07557244B2 Substituted biphenyl carboxylic acids and derivatives thereof 失效
标题翻译：取代的联苯羧酸及其衍生物
公开(公告)号：US07557244B2
公开(公告)日：2009-07-07
申请号：US11737938
申请日：2007-04-20
申请人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernadez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Chih Yung Ho , Yan Zhang
发明人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernadez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Chih Yung Ho , Yan Zhang
IPC分类号： C07C321/00 , C07C229/00 , C07C59/00 , C07D249/08 , A01N43/64 , A01N37/10
CPC分类号： C07C229/42 , C07C59/68
摘要： The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有以下给出的X，Y，R 1，R 2，R 3，R 4，R 9和R 10的定义的通式（I）的化合物和/或其盐或酯。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

4. 发明授权

US08106236B2 Triaryl compounds and derivates thereof 有权
标题翻译：三芳基化合物及其衍生物
公开(公告)号：US08106236B2
公开(公告)日：2012-01-31
申请号：US11737475
申请日：2007-04-19
申请人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Yan Zhang , Chih Yung Ho
发明人： Francis Wilson , Alison Reid , Valerie Reader , Richard John Harrison , Mihiro Sunose , Remedios Hernandez-Perni , Jeremy Major , Cyrille Boussard , Kathryn Smelt , Jess Taylor , Adeline LeFormal , Andrew Cansfield , Svenja Burckhardt , Yan Zhang , Chih Yung Ho
IPC分类号： C07C63/00
CPC分类号： C07D257/04 , C07C51/09 , C07C57/38 , C07C57/58 , C07C59/56 , C07C59/64 , C07C63/331 , C07C69/65
摘要： The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, R10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof.Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有以下给出的X，Y，R 1，R 2，R 3，R 4，R 9，R 10的定义的通式（I）的化合物及其溶剂化物，水合物，酯和药学上可接受的盐。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

5. 发明授权

US08692017B2 Carbon linked modulators of gamma-secretase 失效
标题翻译： γ-分泌酶的碳连接调节剂
公开(公告)号：US08692017B2
公开(公告)日：2014-04-08
申请号：US12253264
申请日：2008-10-17
申请人： Chih Yung Ho , Yan Zhang , Svenja Burckhardt , Alison Jones
发明人： Chih Yung Ho , Yan Zhang , Svenja Burckhardt , Alison Jones
IPC分类号： C07C63/33 , A01N43/40 , A61K31/435
CPC分类号： C07C59/88 , C07C57/42 , C07C57/58 , C07C57/60 , C07C59/56 , C07C255/57 , C07D213/61
摘要： The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
摘要翻译：本发明涉及如下所示的式I化合物，其中A，X，R 1，R 3，R 4，R 5，R 6，R 7，R 8和R 9的定义在说明书中提供。式I化合物可用于治疗与γ-分泌酶活性相关的疾病，包括阿尔茨海默氏病。

6. 发明授权

US07795440B2 N-substituted tricyclic 1-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders 有权
标题翻译： N-取代的三环1-氨基吡唑作为治疗细胞增殖性疾病的抑制剂
公开(公告)号：US07795440B2
公开(公告)日：2010-09-14
申请号：US11657912
申请日：2007-01-25
申请人： Chih Yung Ho , Bengt Anders Brunmark , Stuart Emanuel , Robert A. Galemmo, Jr. , Dana L. Johnson , Donald W. Ludovici , Umar Maharoof , Jay M. Mei , Jan L. Sechler , Eric D. Strobel , Robert W. Tuman , Hwa Kwo Yen
发明人： Chih Yung Ho , Bengt Anders Brunmark , Stuart Emanuel , Robert A. Galemmo, Jr. , Dana L. Johnson , Donald W. Ludovici , Umar Maharoof , Jay M. Mei , Jan L. Sechler , Eric D. Strobel , Robert W. Tuman , Hwa Kwo Yen
IPC分类号： A61K31/416 , A61K31/4439 , C07D401/12
CPC分类号： C07F9/65038 , C07D231/54 , C07D231/56 , C07D233/64 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D491/04 , C07D495/04
摘要： The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell proliferative disorders.
摘要翻译：本发明涉及可用作血小板衍生生长因子受体（PDGF-R）激酶抑制剂的N-取代三环3-氨基吡唑衍生物，以及制备所述衍生物的方法。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如肿瘤和其它细胞增殖性疾病的病症的方法。

7. 发明授权

US07091378B2 Preparation of hydroxamic acids from esters in solution and on the solid phase 有权
标题翻译：从溶液中和固相上的酯制备异羟肟酸
公开(公告)号：US07091378B2
公开(公告)日：2006-08-15
申请号：US10885277
申请日：2004-07-06
申请人： Chih Yung Ho , Eric David Strobel
发明人： Chih Yung Ho , Eric David Strobel
IPC分类号： C07C259/06 , C07C259/08 , C07C259/10
CPC分类号： C07C259/06 , C07C259/10 , C07C303/40 , C07C311/29 , C07D209/42 , C07D217/26
摘要： The present invention provides a novel method for the formation of hydroxamic acids comprising reacting under suitable conditions an ester with hydroxylamine in the presence of cyanide anion.
摘要翻译：本发明提供了形成异羟肟酸的新方法，包括在合适的条件下在氰化物阴离子存在下使酯与羟胺反应。

8. 发明授权

US08530655B2 HIV replication inhibiting pyrimidines 有权
公开(公告)号：US08530655B2
公开(公告)日：2013-09-10
申请号：US13177188
申请日：2011-07-06
申请人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
发明人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D401/12 , C07D403/12 , A61K31/506 , A61P31/18
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

9. 发明授权

US06878717B2 HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶
公开(公告)号：US06878717B2
公开(公告)日：2005-04-12
申请号：US09430966
申请日：1999-11-01
申请人： Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： C07D239/47 , A61K20060101 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/551 , A61K31/5513 , A61K31/675 , A61K31/715 , A61P31/18 , C07D20060101 , C07D239/42 , C07D239/46 , C07D239/48 , C07D239/50 , C07D239/80 , C07D401/12 , C07D403/12
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=-a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
摘要翻译：本发明涉及下式化合物的用途：N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中-a 1 = -a 2 -a 3 = a < 与所连接的乙烯基形成苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; n为0〜4; 并在可能的情况下5; R 1是氢，芳基，甲酰基，C 1-6烷基羰基，C 1-6烷基，C 1-6烷氧基羰基，取代的C 1-6烷基或取代的C 1-6烷氧基C 1-6烷基羰基; 每个R 2独立地是羟基，卤素，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 3-7环烷基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或二（ C 1-6烷基）氨基，多卤代甲基，多卤甲氧基，多卤代甲硫基，-S（= O）p R 6，-NH-S（= O）p R 6，-C（= O）R 6， NHC（= O）H，-C（= O）NHNH 2，-NHC（= O）R 6，-C（= NH）R 6或5元杂环; p为1或2; L是任选取代的C 1-10烷基，C 2-10烯基，C 2-10炔基或C 3-7环烷基; 或L是-X-R 3，其中R 3是任选取代的苯基，吡啶基，嘧啶基，吡嗪基或哒嗪基; X是-NR 1 - ， - NH-NH-，-N = N-，-O-，-C（= O） - ， - CHOH-，-S-，-S（= O） - 或 - S（= O）2-; Q是氢，C 1-6烷基，卤素，多卤代-C 1-6烷基或任选取代的氨基; Y表示羟基，卤素，C 3-7环烷基，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或二（C 1-6烷基）氨基，多卤甲基，多卤甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O） -C（= O）NHNH

10. 发明授权

US06197779B1 HIV inhibiting pyrimidine derivative 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US06197779B1
公开(公告)日：2001-03-06
申请号：US09276360
申请日：1999-03-25
申请人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： A61K31506
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
摘要翻译：本发明涉及N-氧化物，其药学上可接受的加成盐和立体化学异构形式的化合物的用途，其中A是CH，CR 4或N; n为0〜4; Q是氢或-NR1R2; R1和R2选自氢，羟基，C1-12烷基，C1-12烷氧基，C1-12烷基羰基，C1-12烷氧基羰基，芳基，氨基，一或二（C1-12烷基）氨基，单或二（C1-12烷基）其中每个C 1-12烷基可以任选被取代; 或R 1和R 2可以一起形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-12烷基）氨基C 1-4亚烷基; R 3是氢，芳基，C 1-6烷基羰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基。 R4为羟基，卤素，任选取代的C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基，三卤代甲基，三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基，C 3-10烯基，C 3-10炔基，C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7，其中R6和R7是任选取代的苯基; X1和X2是-NR3-，-NH-NH-，-N = N-，-O - ， - S - ， - S（= O） - 或-S（= O） Alk是C1-4烷二基; 芳基是取代的苯基; Het是任选取代的脂族或芳族杂环基; 用于制造用于治疗患有HIV（人类免疫缺陷病毒）感染的受试者的药物。它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的组合物。

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