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1. 发明授权

US5086170A Process for the preparation of azabicyclo compounds 失效
标题翻译：制备亚硫酸化合物的方法
公开(公告)号：US5086170A
公开(公告)日：1992-02-04
申请号：US633289
申请日：1990-12-24
申请人： Abdul B. N. Luheshi , Robert K. Smalley , Peter D. Kennewell , Robert Westwood
发明人： Abdul B. N. Luheshi , Robert K. Smalley , Peter D. Kennewell , Robert Westwood
IPC分类号： A61K31/397 , A61K31/41 , A61K31/415 , A61K31/42 , A61P29/00 , A61P37/00 , C07D487/04 , C07D498/04 , C07D507/02
CPC分类号： C07D487/04
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and hydroxyalkyl of 1 to 5 carbon atoms and amino, n is an integer from 1 to 3, X and X.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the carbon atom to which they are attached are ##STR2## Y is --O-- or --S--, R.sub.3 is alkyl of 1 to 3 carbon atoms or aryl of 6 to 8 carbon atoms, ##STR3## is selected from the group consisting of ##STR4## R.sub.4 and R.sub.5 are individually aryl unsubstituted or substituted with at least one member of the group consisting of halogen, --NO.sub.2 and alkyl and alkoxy of 1 to 3 carbon atoms and non-toxic, pharmaceutically acceptable salts thereof with acids and bases having cyclooxygenase inhibiting and antibiotic acitvity.

2. 发明授权

US4472400A Triazoloquinazolones having antihistaminic and bronchospasmolytic activity 失效
标题翻译：具有抗组胺和支气管扩张活性的三氮唑喹唑啉酮
公开(公告)号：US4472400A
公开(公告)日：1984-09-18
申请号：US420798
申请日：1982-09-21
申请人： Wilfred R. Tully , Robert Westwood , David A. Rowlands , Stephen Clements-Jewery
发明人： Wilfred R. Tully , Robert Westwood , David A. Rowlands , Stephen Clements-Jewery
IPC分类号： A61K31/505 , A61K31/535 , A61K31/55 , A61P11/08 , A61P43/00 , C07D239/95 , C07D239/96 , C07D487/04
CPC分类号： C07D487/04 , C07D239/95 , C07D239/96
摘要： Novel triazoloquinazolones of the formula ##STR1## wherein R and R' are individually selected from the group consisting of hydrogen, halogen, nitro and alkyl and alkoxy of 1 to 3 carbon atoms, Y is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 4 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms, B is an alkylene of 1 to 3 carbon atoms, X is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms, aralkyl of 7 to 8 carbon atoms, aminoalkyl of 2 to 4 carbon atoms, mono- and dialkylaminoalkyl with each alkyl having 2 to 4 carbon atoms, piperidinoalkyl of 1 to 4 alkyl carbon atoms, morpholinoalkyl of 1 to 4 alkyl carbon atoms and piperazinylalkyl of 1 to 4 alkyl carbon atoms or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached form a saturated mono- or bicyclic heterocyclic ring with 4 to 8 carbon atoms optionally substituted with 1 to 2 methyls and optionally containing in the ring a heteroatom selected from --O--, --S-- and ##STR3## and R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, hydroxyalkyl of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and their preparation and intermediates.
摘要翻译：新颖的式（I）的三唑并喹唑酮其中R和R'分别选自氢，卤素，硝基和1至3个碳原子的烷基和烷氧基，Y选自1至 6个碳原子，2至4个碳原子的烯基，3至8个碳原子的环烷基，6至8个碳原子的芳基和7至8个碳原子的芳烷基，B是1至3个碳原子的亚烷基，选择X 来自由 R 1和R 2组成的组分别选自氢，1至6个碳原子的烷基，3至8个碳原子的环烷基，6至8个碳原子的芳基，7至8个的芳烷基碳原子数2〜4个的氨基烷基，碳原子数2〜4的烷基的单烷氧基氨基烷基和二烷基氨基烷基，1〜4个碳原子的哌啶子基烷基，1〜4个的烷基碳原子的吗啉代烷基，1〜4个碳原子的哌嗪基烷基原子或R1和R2与它们一起的氮一起重新连接形成具有4至8个碳原子的饱和单环或双环杂环，任选被1至2个甲基取代，并且任选地在环中含有选自-O - ， - S-和的杂原子，并且R 3选自由氢，1〜3个碳原子的烷基，1〜3个碳原子的羟基烷基，2〜5个碳原子的烷氧基羰基，6〜8个碳原子的芳基和7〜8个碳原子的芳烷基组成的组及其无毒的，具有抗组胺和支气管痉挛分解活性的药学上可接受的酸加成盐及其制备和中间体。

3. 发明授权

US08884001B2 Preparation of intermediates useful in the synthesis of 2′-cyano-2′-deoxy-N4-palmi-toyl-1-β-D-arabinofuranosylcytosine 有权
标题翻译：制备可用于合成2'-氰基-2'-脱氧-N4-棕榈酰-1-基 - D-阿拉伯呋喃糖基胞嘧啶的中间体
公开(公告)号：US08884001B2
公开(公告)日：2014-11-11
申请号：US12991582
申请日：2009-05-08
申请人： Gavin Wood , Robert Westwood , Tsuyoshi Murofushi , Eiji Numagami , Takashi Takita
发明人： Gavin Wood , Robert Westwood , Tsuyoshi Murofushi , Eiji Numagami , Takashi Takita
IPC分类号： C07H19/06 , C07F7/08
CPC分类号： C07F7/0838
摘要： The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2′ into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2′-cyano-2′-deoxy-N4-palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
摘要翻译：本发明涉及一种制备式682-4化合物的方法，所述方法包括以下步骤：（i）将式682-1化合物转化为式682-2化合物; （ii）将所述式682-2'化合物转化为式682-3化合物; 和（iii）将所述式682-3化合物转化为式682-4化合物。本发明的其它方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-基 - D-阿糖呋喃糖基胞嘧啶的用途，嘧啶核苷在治疗中是有用的和/或预防癌症。

4. 发明申请

US20100035870A1 Pyrimidin-4-yl-3, 4-Dihydro-2H-Pyrrolo[1,2A] Pyrazin-1-one Compounds 有权
标题翻译：嘧啶-4-基-3,4-二氢-2H-吡咯并[1,2A]吡嗪-1-酮化合物
公开(公告)号：US20100035870A1
公开(公告)日：2010-02-11
申请号：US12083534
申请日：2006-10-09
申请人： Stuart Jones , Robert Westwood , Mark Thomas , Janice McLachlan , Kenneth Duncan , Fred Scaerou , Daniella I. Zheleva
发明人： Stuart Jones , Robert Westwood , Mark Thomas , Janice McLachlan , Kenneth Duncan , Fred Scaerou , Daniella I. Zheleva
IPC分类号： A61K31/506 , C07D487/04 , A61K31/538 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P35/02 , A61P19/02 , A61P11/00 , A61P31/12 , C12Q1/48 , G01N33/53 , A61P25/00 , A61P25/28 , A61P17/14 , A61P3/10 , A61P27/02
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR11, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH═CH; X is a hydrocarbyl group optionally substituted by one or more R12 groups; R10 and R11 are each independently II or alkyl; R1-R4 are each independently II or (CII2)mR12, where m is O, 1, 2, or 3; each R12 is independently (CH2)aR16, where each R16 is independently selected from O(CH2)bR13, R13, COR13, COOR13, CN, CONR13R14, NR13R14, NR13COR14, SR13, SOR13, SO2R13, NR13SO2R14, SO2OR13, SO2NR13R14, halogen, CF3, and NO2, and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R13 and R14 are each independently H or (CH2)nR15, where n is 0, 1, 2, or 3; and each R15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO— alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy, wherein said alkyl and alkoxy groups may be further substituted by one or more OH groups. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula I, and the use of compounds of formula (I) in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为NR11，NHCO，NHSO2，NHCH2，CH2，CH2CH2或CH-CH; X是任选被一个或多个R 12基团取代的烃基; R 10和R 11各自独立地为II或烷基; R1-R4各自独立地为II或（CII2）mR12，其中m为0,1,2或3; 每个R 12独立地为（CH 2）a R 16，其中每个R 16独立地选自O（CH 2）b R 13，R 13，COR 13，COOR 13，CN，CONR 13 R 14，NR 13 R 14，NR 13 COR 14，SR 13，SOR 13，SO 2 R 13，NR 13 SO 2 R 14，SO 2 R 13，SO 2 NR 13 R 14， CF 3和NO 2，并且其中每个a是0,1,2或3，b是0,1,2或3; R 13和R 14各自独立地为H或（CH 2）n R 15，其中n为0,1,2或3; 并且每个R 15独立地选自烷基，环烷基，杂芳基，芳烷基，芳基和杂环烷基，其各自可以任选被一个或多个选自卤素，OH，CN，COO-烷基，芳烷基，SO 2 - 烷基，SO 2 - 芳基，COOH，CO-烷基，CO-芳基，NH 2，NH-烷基，N（烷基）2，CF 3，烷基和烷氧基，其中所述烷基和烷氧基可进一步被一个或多个OH基取代。本发明的其它方面涉及包含式I化合物的药物组合物，以及式（I）化合物在制备用于治疗多种病症（包括增殖性病症，病毒性疾病，中风等）的药物中的用途。

5. 发明授权

US5371099A Phenyl carboxamide isoxazoles 失效
标题翻译：苯基甲酰胺异恶唑
公开(公告)号：US5371099A
公开(公告)日：1994-12-06
申请号：US54893
申请日：1993-04-28
申请人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
发明人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
IPC分类号： A61K31/42 , A61P29/00 , C07C235/78 , C07C235/80 , C07C255/60 , C07C323/41 , C07D207/06 , C07D261/18 , C07D295/145 , C07D261/08 , C07D261/12
CPC分类号： C07D295/145 , C07C235/80 , C07C255/60 , C07C323/41 , C07D261/18 , C07C2101/02
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 3 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, R.sub.3 is --COOR.sub.6, R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.4 is selected from the group consisting of halogen, --CN, --NO.sub.2, --SCH.sub.3, alkylcarbonyl of 1 to 6 alkyl carbon atoms, --CX.sub.3, --WCX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --W--(CX.sub.2).sub.n --CX.sub.3, and --W--(CH.sub.2).sub.n --CX.sub.3, X is halogen, W is --O-- or --S--, n is 1, 2 or 3, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms and their salts with non-toxic pharmaceutically acceptable bases with the proviso that if R.sub.2 is alkyl of 1 to 3 carbon atoms, R.sub.1 is hydrogen and R.sub.4 is selected from the group consisting of halogen, --CX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --OCX.sub.3, --O--(CX.sub.2).sub.n --CX.sub.3, and --O--(CH.sub.2).sub.n --CX.sub.3, X is halogen and n is 1, 2 or 3, R.sub.5 cannot be hydrogen having anti-inflammatory activity and their preparation and intermediates.
摘要翻译：选自下式的化合物的化合物其中R 1为氢或1至3个碳原子的烷基，R 2为1至3个碳原子的烷基或3至6个碳原子的环烷基，R 3为 -COOR 6，R 6是氢或1至3个碳原子的烷基，R 4选自卤素，-CN，-NO 2，-SCH 3，1至6个烷基碳原子的烷基羰基，-CX 3，-WCX 3，（CH 2）n -CX 3， - （CX 2）n -CX 3，-W-（CX 2）n -CX 3和-W-（CH 2）n -CX 3，X是卤素，W是-O-或-S-， n为1,2或3，R5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基及其与无毒的药学上可接受的碱的盐，条件是如果R2为 1至3个碳原子的烷基，R1是氢，R4选自卤素，-CX3， - （CH2）n -CX3， - （CX2）n -CX3，-OCX3，-O-（CX2） n -CX3和-O-（CH2）n -CX3，X是卤素，n是1,2或3，R5不能是具有抗炎活性的氢及其制备和中间体。

6. 发明授权

US08497291B2 Crystalline pyrimidine nucleoside derivative suspensions in capsules 有权
标题翻译：胶囊中的结晶嘧啶核苷衍生物悬浮液
公开(公告)号：US08497291B2
公开(公告)日：2013-07-30
申请号：US12097912
申请日：2006-12-22
申请人： Robert Westwood , Alistair Selkirk
发明人： Robert Westwood , Alistair Selkirk
IPC分类号： A01N43/80 , A61K31/42 , A61K9/64
CPC分类号： A61K9/4808 , A61K9/4866 , A61K31/513
摘要： The present invention relates to a pharmaceutical formulation which comprises (i) a capsule, and (ii) a core comprising crystalline 2′-cyano-2′-deoxy-N4-palmitoyl-1-β-D-arabinofuranosylcytosine and a liquid carrier.
摘要翻译：本发明涉及一种药物制剂，其包含（i）胶囊和（ii）包含结晶的2'-氰基-2'-脱氧-N4-棕榈酰基-1-β-D-阿拉伯呋喃糖基胞嘧啶的核心和液体载体。

7. 发明授权

US5476866A Isoxazoles 失效
标题翻译：异恶唑
公开(公告)号：US5476866A
公开(公告)日：1995-12-19
申请号：US293840
申请日：1994-08-22
申请人： Elizabeth A. Kuo , Robert Westwood
发明人： Elizabeth A. Kuo , Robert Westwood
IPC分类号： A61K31/42 , A61P19/02 , A61P29/00 , A61P35/00 , C07D261/18 , C07D263/30
CPC分类号： C07D261/18
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is cycloalkyl of 3 to 6 carbon atoms; R.sub.4 is selected from the group consisting of halogen, nitrile, nitro, --SCH.sub.3, -alkylcarbonyl of 1 to 6 carbon atoms, cycloalkylcarbonyl of 3 to 6 carbon atoms, --CX.sub.3, --WCX.sub.3, --(CH.sub.2).sub.n CX.sub.3, --(CX.sub.2).sub.n CX.sub.3, --W(CX.sub.2).sub.n CX.sub.3 and a --W(CH.sub.2).sub.n CX.sub.3, in which X is halogen, W is oxygen or sulfur, and n is 1, 2 or 3; and R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms; with the proviso that if R.sub.5 is hydrogen, R.sub.4 is not --SCH.sub.3 or --CF.sub.3 and their non-toxic pharmaceutically acceptable salts having anti-prolifera-tive, anti-inflammatory and anti-tumor activity.
摘要翻译：选自下式的化合物的化合物其中R 1是氢或1至3个碳原子的烷基; R 2是3至6个碳原子的环烷基; R 4选自卤素，腈，硝基，-SCH 3 - 具有1至6个碳原子的烷基羰基，3至6个碳原子的环烷基羰基，-CX 3，-WCX 3， - （CH 2）n CX 3， - （CX 2） nCX3，-W（CX2）nCX3和-W（CH2）nCX3，其中X是卤素，W是氧或硫，n是1,2或3; 并且R 5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基; 条件是如果R5是氢，R4不是-SCH3或-CF3及其无毒的药学上可接受的盐，其具有抗增殖，抗炎和抗肿瘤活性。

8. 发明授权

US5059596A Azabicyclo compounds 失效
标题翻译：偶氮化合物
公开(公告)号：US5059596A
公开(公告)日：1991-10-22
申请号：US465031
申请日：1990-01-16
申请人： Abdul B. N. Luheshi , Robert K. Smalley , Peter D. Kennewell , Robert Westwood
发明人： Abdul B. N. Luheshi , Robert K. Smalley , Peter D. Kennewell , Robert Westwood
IPC分类号： A61K31/397 , A61K31/41 , A61K31/415 , A61K31/42 , A61P29/00 , A61P37/00 , C07D487/04 , C07D498/04 , C07D507/02
CPC分类号： C07D487/04
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and hydroxyalkyl of 1 to 5 carbon atoms and amino, n is an integer from 1 to 3, X and X.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the carbon atom to which they are attached are >C.dbd.O Y is --O-- or --S--, R.sub.3 is alkyl of 1 to 3 carbon atoms or aryl of 6 to 8 carbon atoms, ##STR2## is selected from the group consisting of ##STR3## R.sub.4 and R.sub.5 are individually aryl unsubstituted or substituted with at least one member of the group consisting of halogen, --NO.sub.2 and alkyl and alkoxy of 1 to 3 carbon atoms and non-toxic, pharmaceutically acceptable salts thereof with acids and bases having cyclooxygenase inhibiting and antibiotic activity.
摘要翻译：选自下式的化合物的化合物：其中R 1和R 2分别选自氢，1至5个碳原子的烷基和羟烷基和氨基，n是1至3的整数 X和X 1分别选自氢和1〜3个碳原子的烷基，或者与它们所连接的碳原子一起被连在一起，C = OY是-O-或-S-，R3是烷基 1至3个碳原子的芳基或6至8个碳原子的芳基，选自由以下组成的组：R 4和R 5各自独立地为未取代的芳基或被至少一个选自卤素， NO 2和具有1至3个碳原子的烷基和烷氧基以及其具有环氧合酶抑制和抗生素活性的酸和碱的无毒的药学上可接受的盐。

9. 发明授权

US4794122A Novel benzimidazolyl-thiomethyl-benzothiazoles 失效
标题翻译：新型苯并咪唑基 - 硫代甲基 - 苯并噻唑
公开(公告)号：US4794122A
公开(公告)日：1988-12-27
申请号：US57758
申请日：1987-06-03
申请人： Stephen Clements-Jewery , Peter D. Kennewell , Robert Westwood
发明人： Stephen Clements-Jewery , Peter D. Kennewell , Robert Westwood
IPC分类号： A61K31/425 , A61P29/00 , A61P37/08 , C07D417/12
CPC分类号： C07D417/12
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-allergic and anti-inflammatory properties.
摘要翻译：选自下式的化合物的化合物其中R 1，R 2和R 3分别选自氢，卤素和1至6个碳原子的烷基和烷氧基，并且它们的无毒，具有抗过敏和抗炎特性的药学上可接受的酸加成盐。

10. 发明授权

US4751233A 8[2-(imidazolyl)thio] and 8[2-(thiazolyl)thio]-5,6,7,8-tetrahydroquinolines, and anti-allergic use thereof 失效
标题翻译： 8 [2-（咪唑基）硫基]和8 [2-（噻唑基）硫基] -5,6,7,8-四氢喹啉和其抗过敏用途
公开(公告)号：US4751233A
公开(公告)日：1988-06-14
申请号：US833853
申请日：1986-02-26
申请人： Stephen Clements-Jewery , Peter D. Kennewell , Robert Westwood
发明人： Stephen Clements-Jewery , Peter D. Kennewell , Robert Westwood
IPC分类号： A61K31/47 , A61K31/505 , A61P11/08 , A61P37/08 , C07D401/12 , C07D413/12 , C07D417/12 , C07D403/14 , A61K31/415 , A61K31/425
CPC分类号： C07D401/12 , C07D413/12 , C07D417/12
摘要： Novel 8-thiotetrahydroquinolines of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## Alk is alkyl of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are Alk individually selected from the group consisting of hydrogen and aryl or taken together with the carbon atoms to which they are attached form a phenyl optionally substituted with at least one member of the group consisting of alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, halogen, ##STR3## and Alk' is alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antiallergic activity and their preparation.
摘要翻译：新颖的具有式（I）的8-硫代四氢喹啉，其中X选自由下列组成的组：Alk是1至6个碳原子的烷基，R 1和R 2是分别选自氢和芳基或被取代的烷基与它们所连接的碳原子一起形成任选被至少一个由1-6个碳原子的烷基，烷氧基和烷硫基组成的组的卤素取代的苯基，卤素，Alk'是1至 6个碳原子及其无毒，药学上可接受的具有抗过敏活性的酸加成盐及其制备。

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