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1. 发明授权

US08178549B2 Azabicyclo [3. 1. O] hexyl derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂双环[3。 O]己基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US08178549B2
公开(公告)日：2012-05-15
申请号：US12680785
申请日：2008-10-01
申请人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
发明人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
IPC分类号： C07D403/14 , C07D413/14 , A61K31/513
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷基， 4烷氧基和SF5; n为1或2; 它们在治疗中的用途，作为多巴胺D3受体的调节剂，例如。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

2. 发明申请

US20100210672A1 AZABICYCLO [3. 1. O] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：US20100210672A1
公开(公告)日：2010-08-19
申请号：US12680785
申请日：2008-10-01
申请人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
发明人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
IPC分类号： A61K31/506 , C07D403/14 , A61P25/18 , A61P25/30
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: whereinR1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷基， 4烷氧基和SF5; n为1或2; 它们在治疗中的用途，作为多巴胺D3受体的调节剂，例如。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

3. 发明申请

US20090326011A1 AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZAB I CYCLO [3。 1。 0] HEXANE衍生物作为DOPAMIN D3受体调节剂
公开(公告)号：US20090326011A1
公开(公告)日：2009-12-31
申请号：US11917352
申请日：2006-06-13
申请人： Luca Arista , Francesca Cardullo , Anna Checchia , Dieter Hamprecht , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Francesca Cardullo , Anna Checchia , Dieter Hamprecht , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/4439 , A61K31/41 , A61K31/427 , A61K31/4164 , A61K31/403 , A61K31/4025 , C07D417/14 , C07D417/12 , C07D403/12 , C07D209/52
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.
摘要翻译：本文公开了式（I）的化合物，其中G和Q是杂芳族基团。这些化合物可用于治疗精神病或精神病状，药物滥用，早泄或认知障碍。

4. 发明申请

US20090192194A1 Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them 审中-公开
标题翻译：环胺衍生物，其制备方法以及含有它们的药物组合物
公开(公告)号：US20090192194A1
公开(公告)日：2009-07-30
申请号：US11869945
申请日：2007-10-10
申请人： Giuseppe Alvaro , Luca Arista , Francesca Cardullo , Lucilla D'Adamo , Aldo Feriani , Riccardo Giovannini , Catia Seri
发明人： Giuseppe Alvaro , Luca Arista , Francesca Cardullo , Lucilla D'Adamo , Aldo Feriani , Riccardo Giovannini , Catia Seri
IPC分类号： A61K31/445 , C07D401/02 , C07D211/22 , A61P25/22
CPC分类号： C07D405/04 , C07D211/34 , C07D405/12
摘要： A compound of formula (I) wherein R is a radical selected from in which R7 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; p is an integer from 0 to 3; R1 is hydrogen, halogen, cyano, C2-4 alkenyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 is hydrogen or C1-4 alkyl; R3 and R4 independently are hydrogen, C1-4 alkyl or R3 together with R4 is C3-7 cycloalkyl; R5 is phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl or R5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl; R6 is hydrogen or (CH2)qR8; R8 is hydrogen, C3-7 cycloalkyl, C1-4 alkoxy, amine, C1-4 alkylamine, (C1-4 alkyl)2amine, OC(O)NR9R10 or C(O)NR9R10; R9 and R10 independently are hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m is zero or 1; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof; processes for their preparation to pharmaceutical compositions containing them and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
摘要翻译：式（I）化合物，其中R为选自其中R 7为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基的基团; p是0至3的整数; R 1是氢，卤素，氰基，C 2-4链烯基，任选地被卤素，氰基或C 1-4烷氧基取代的C 1-4烷基; R2是氢或C1-4烷基; R3和R4独立地是氢，C1-4烷基或R3与R4一起是C3-7环烷基; R5是被1-3个独立地选自三氟甲基，C1-4烷基，氰基，C1-4烷氧基，三氟甲氧基，卤素或（SO）rC1-4烷基取代的苯基，被1至3个独立地选自三氟甲基， C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或（SO）r C 1-4烷基，被1至3个独立地选自三氟甲基，C 1-4烷基，氰基的1-3元基团取代的9至10元稠合双环杂环基，C 1-4烷氧基，三氟甲氧基，卤素或（SO）rC 1-4烷基或R 5是被1-3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或（SO）rC 1-4烷基; R6是氢或（CH2）qR8; R 8为氢，C 3-7环烷基，C 1-4烷氧基，胺，C 1-4烷基胺，（C 1-4烷基）2胺，OC（O）NR 9 R 10或C（O）NR 9 R 10; R9和R10独立地是氢，C1-4烷基或C3-7环烷基; m为零或1; n为1或2; q是1至4的整数; r为1或2; 或其药学上可接受的盐和溶剂化物; 其制备方法用于含有它们的药物组合物及其用于治疗由速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。

5. 发明申请

US20060058348A1 N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors 审中-公开
标题翻译： N-苄基-3-苯基-3-杂环基 - 丙酰胺化合物作为速激肽和/或5-羟色胺再摄取抑制剂
公开(公告)号：US20060058348A1
公开(公告)日：2006-03-16
申请号：US10521159
申请日：2003-07-02
申请人： Giuseppe Alvaro , Francesca Cardullo , Lucilla D'Adamo , Elisabeth Piga , Catia Seri
发明人： Giuseppe Alvaro , Francesca Cardullo , Lucilla D'Adamo , Elisabeth Piga , Catia Seri
IPC分类号： C07D211/26 , A61K31/445
CPC分类号： C07D207/08 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/535 , C07D207/20 , C07D211/34 , C07D211/38 , C07D211/70 , C07D213/56 , C07D265/30
摘要： The present invention relates to heterocyclic derivatives of formula (I) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; R1 represents a 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms, or R1 represents a 4, 5 or 6 membered heterocyclic group, wherein saids 5 or 6 membered heteroaryl or the 4, 5 or 6 membered heterocyclic group may optionally be substituted by one to three substituents, which may be the same or different, selected from (CH2)pR6, wherein p is zero or an integer from 1 to 4 and R6 is selected from: halogen, C1-4alkoxy, C1-4alkyl, C3-7cycloalkyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy, hydroxy, cyano, nitro, trifluoromethyl, carboxy, NH(C1-4 alkyl), N(C1-4 alkyl)2 NH(C3-7 cycloalkyl), N(C1-4 alkyl)(C3-7 cycloalkyl); NH(C1-4alkylOC1-4alkoxy), OC(O)NR7R8, NR8C(O)R7 or C(O)NR7R8; R2 represents hydrogen, or C1-4 alkyl; R3 and R4 independently represent hydrogen, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)qC1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R7 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; L is a single or a double bond; n is an integer from 1 to 3; m is zero or an integer from 1 to 3; q is zero or an integer from 1 to 2; provided that a) when L is a double bond, R1 is not an optionally substituted 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms; b) the group R1 is linked to the carbon atom shown as * via a carbon atom; and c) when the heteroatom contained in the group R1 is substituted, p is not zero; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
摘要翻译：本发明涉及式（I）的杂环衍生物，

6. 发明申请

US20050215495A1 Macrolide antibiotics 审中-公开
标题翻译：大环内酯抗生素
公开(公告)号：US20050215495A1
公开(公告)日：2005-09-29
申请号：US11127701
申请日：2005-05-12
申请人： Sulejman Alihodzic , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzan , Catia Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
发明人： Sulejman Alihodzic , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzan , Catia Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
IPC分类号： A61K31/7048 , A61P31/10 , C07H17/08 , A61K31/7052
CPC分类号： C07H17/08 , A61K9/0019 , A61K9/2018 , Y02P20/55
摘要： The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R1, R2, R3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及式（I）的11,12个γ-内酯酮内酯，其中R 1，R 1，R 2，R 3，3，本文定义其药学上可接受的盐和溶剂化物，以处理其制备及其在治疗或预防人或动物体内的全身或局部细菌感染中的用途。

7. 发明申请

US20100197699A1 I-OXA-3-Azaspiro (4.5) Decan-2-One And 1-OXA-3, 8-Diazaspiro (4.5) Decan-2-One Derivatives For The Treatment of Eating Disorders 审中-公开
标题翻译： I-OXA-3-Azaspiro（4.5）Decan-2-One和1-OXA-3,8-Diazaspiro（4.5）Decan-2-One衍生物用于饮食障碍的治疗
公开(公告)号：US20100197699A1
公开(公告)日：2010-08-05
申请号：US12524038
申请日：2008-01-30
申请人： Jonathan Bentley , Matteo Biagetti , Francesca Cardullo , Thorsten Genski , Silvia Rosalia Kopf , Colin Philip Leslie , Sergio Melotto , Mirco Meniconi , Giancarlo Merlo , Domenica Antonia Pizzi , Catia Seri
发明人： Jonathan Bentley , Matteo Biagetti , Francesca Cardullo , Thorsten Genski , Silvia Rosalia Kopf , Colin Philip Leslie , Sergio Melotto , Mirco Meniconi , Giancarlo Merlo , Domenica Antonia Pizzi , Catia Seri
IPC分类号： A61K31/423 , C07D498/10 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/444 , A61K31/501 , A61K31/497 , A61K31/506 , A61P3/04 , A61P25/24
CPC分类号： C07D498/10 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; W is —CZ1 or nitrogen; Z1 is hydrogen, C1-C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is —CZ1, compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基; 其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; W是-CZ1或氮; Z1是氢，C1-C4烷基; A是可被一个或多个卤素取代的5元杂芳基，吡嗪，嘧啶或喹啉或喹唑啉：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; B是氢或可被一个或多个卤素取代的5-10元芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 是通过任何原子连接的A和B; 条件是当W是-CZ1时，式（I）化合物具有反式立体化学; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

8. 发明申请

US20080269195A1 Compounds Having Affinity For the Dopamine D3 Receptor and Uses Thereof in Medicine 审中-公开
标题翻译：具有多巴胺D3受体亲和力的化合物及其在医学中的应用
公开(公告)号：US20080269195A1
公开(公告)日：2008-10-30
申请号：US11571051
申请日：2005-06-29
申请人： Giorgio Bonanomi , Francesca Cardullo , Federica Damiani , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi
发明人： Giorgio Bonanomi , Francesca Cardullo , Federica Damiani , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi
IPC分类号： A61K31/55 , C07D498/04 , A61P25/30
CPC分类号： C07D513/04
摘要： Compounds of formula (I) or a salt thereof are disclosed: wherein, A, m R1, R2, R3, q, W1, W2, R4 and R5 are as defined in the description. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物或其盐：其中，A，m R 1，R 2，R 3，q， W 1，W 2，R 4和R 5如说明书中所定义。还公开了用于药物中化合物的制备和用途的方法，例如用于治疗精神分裂症或药物依赖性。

9. 发明申请

US20060211636A1 Macrolide Antibiotics 审中-公开
标题翻译：大环内酯抗生素
公开(公告)号：US20060211636A1
公开(公告)日：2006-09-21
申请号：US11422122
申请日：2006-06-05
申请人： Sulejman ALIHODZIC , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzman , Catai Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
发明人： Sulejman ALIHODZIC , Daniele Andreotti , Luca Arista , Stefano Biondi , Francesca Cardullo , Manuela Ciraco , Federica Damiani , Sergio Lociuro , Carla Marchioro , Giancarlo Merlo , Anna Mingardi , Daniela Niccolai , Alfredo Paio , Elisabetta Piga , Alfonso Pozzman , Catai Seri , Luca Tarsi , Silvia Terreni , Jessica Tibasco
IPC分类号： C07H17/08 , A61K31/7048
CPC分类号： C07H17/08 , A61K9/0019 , A61K9/2018 , Y02P20/55
摘要： The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R1, R2, R3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及式（I）的11,12个γ-内酯酮内酯，其中R 1，R 1，R 2，R 3，3，本文定义其药学上可接受的盐和溶剂化物，以处理其制备及其在治疗或预防人或动物体内的全身或局部细菌感染中的用途。

10. 发明申请

US20080167351A1 Compounds Which Potentiate Glutamate Receptor and Uses Thereof in Medicine 失效
标题翻译：增加谷氨酸受体的化合物及其在医学中的应用
公开(公告)号：US20080167351A1
公开(公告)日：2008-07-10
申请号：US11816284
申请日：2006-02-13
申请人： Daniele Andreotti , Luca Arista , Francesca Cardullo , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniele Andreotti , Luca Arista , Francesca Cardullo , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/44 , C07D213/02 , C07C311/01 , A61K31/18 , C07D333/02 , A61K31/381 , A61P25/18
CPC分类号： C07D277/64 , C07D213/42 , C07D213/61 , C07D213/65 , C07D317/58 , C07D333/20
摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及通过新的式（I）化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

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