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1. 发明公开

EP1319659A4 PYRIDAZINONES AND TRIAZINONES AND MEDICINAL USE THEREOF 有权
标题翻译：哒嗪三嗪酮及其应用的药用
公开(公告)号：EP1319659A4
公开(公告)日：2005-08-10
申请号：EP01970120
申请日：2001-09-17
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： C07D237/14 , C07D237/24 , C07D401/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D237/04 , A61K31/50 , A61P25/00 , C07D401/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14
CPC分类号： C07D237/24 , C07D237/14 , C07D401/04 , C07D491/04
摘要： Provided are novel compounds exhibiting excellent inhibitory activities against AMPA receptor and/or kainate receptor, i.e., compounds of the general formula (I), salts thereof, or hydrates of both wherein A?1, A2 and A3¿ are each independently C¿3-8? cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonoaromatic heterocyclic group, a C6-14 aromatic carbocyclic group, or a 5- to 14-membered aromatic heterocyclic group, any of which may be substituted; Q is O, S, or NH; Z is C or N; X?1, X2 and X3¿ are each independently a single bond, optionally substituted C¿1-6? alkylene, optionally substituted C2-6 alkenylene, optionally substituted C2-6 alkynylene, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, or the like; R?1 and R2¿ are each independently hydrogen or optionally substituted C¿1-6? alkyl, or alternatively R?1 and R2¿ may be united in such a way that CR2-ZR1 forms C=C; and R3 is hydrogen, optionally substituted C¿1-6? alkyl, or the like, or alternatively R?3¿ may unite with any atom on the ring A1 or A3 to form together with the atom an optionally substituted C¿5-8? carbocycle or an optionally substituted 5- to 8-membered heterocycle.

2. 发明公开

EP1020445A4 FUSED PYRIDINE DERIVATIVES 有权
标题翻译：简明吡啶
公开(公告)号：EP1020445A4
公开(公告)日：2001-06-20
申请号：EP98945593
申请日：1998-10-02
申请人： EISAI CO LTD
发明人： UENO KOHSHI , SASAKI ATSUSHI , KAWANO KOKI , OKABE TADASHI , KITAZAWA NORITAKA , TAKAHASHI KEIKO , YAMAMOTO NOBORU , SUZUKI YUICHI , MATSUNAGA MANABU , KUBOTA ATSUHIKO
IPC分类号： C07D217/22 , C07D217/24 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/14 , C07D413/10 , C07D417/04 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/10 , C07D495/04 , C07D217/14 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , C07D217/16 , C07D217/18 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/10 , C07D417/14
CPC分类号： C07D401/04 , C07D217/22 , C07D217/24 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/14 , C07D413/10 , C07D417/04 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/10 , C07D495/04
摘要： Clinically highly useful drugs having an antagonism to serotonin, in particular, central muscle relaxing drugs for treating, ameliorating or preventing spastic paralysis or ameliorating myotonia and comprising fused pyridine derivatives represented by general formula (I), pharmacologically acceptable salts thereof or hydrates of either (I) or (1), wherein the ring A represents a benzene, pyridine, thiophene or furan ring; and B represents (2).

3. 发明公开

EP0976732A4 1,4-SUBSTITUTED CYCLIC AMINE DERIVATIVES 失效
标题翻译： 1,4-取代环胺衍生物
公开(公告)号：EP0976732A4
公开(公告)日：2000-06-14
申请号：EP98911137
申请日：1998-03-31
申请人： EISAI CO LTD
发明人： KITAZAWA NORITAKA , UENO KOHSHI , TAKAHASHI KEIKO , KIMURA TEIJI , SASAKI ATSUSHI , KAWANO KOKI , OKABE TADASHI , KOMATSU MAKOTO , MATSUNAGA MANABU , KUBOTA ATSUHIKO
IPC分类号： C07D211/22 , A61K31/135 , A61P21/02 , C07D211/26 , C07D211/74 , C07D217/02 , C07D217/04 , C07D221/04 , C07D295/08 , C07D295/10 , C07D295/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/14 , C07D491/04 , C07D491/056 , C07D513/04 , C07D521/00 , A61K31/44 , C07D295/12
CPC分类号： C07D231/12 , C07D211/26 , C07D211/74 , C07D217/04 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D491/04 , C07D513/04
摘要： Novel 1,4-substituted cyclic amine derivatives which have serotonin antagonism and serve as drugs having high clinical usefulness, especially an agent for the remedy/alleviation/prevention of spastic paralysis or a central muscle relaxant for alleviating myotonia. The derivatives are represented by general formula (I) or pharmacologically acceptable salts thereof, wherein A, B, C, D, T, Y, and Z each represents a methine group or a nitrogen atom; R?1, R2, R3, R4, and R5¿ each represents a substituent; n is an integer of 0 to 3; m is an integer of 0 to 6; and p is an integer of 1 to 3.

4. 发明公开

EP1300396A4 1,2-DIHYDROPYRIDINE COMPOUNDS, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF 有权转让
标题翻译： 1,2-二氢吡啶，PROCESS FOR PRODUCING及其用途
公开(公告)号：EP1300396A4
公开(公告)日：2005-06-15
申请号：EP01936920
申请日：2001-06-08
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , UENO KOHSHI , KAWANO KOKI , NORIMINE YOSHIHIKO , ITO KOICHI , HANADA TAKAHISA , UENO MASATAKA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , URAWA YOSHIO , NAKA HIROYUKI , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： A61K20060101 , A61P20060101 , A61P1/08 , A61P9/10 , A61P13/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/06 , C07F7/18 , C07D213/71 , A61K31/44
CPC分类号： C07F7/1856 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/06
摘要： Provided are novel compounds exhibiting excellent inhibitory activities against AMPA receptor and/or kainite receptor, specifically compounds of the general formula (I), salts of the same, or hydrates of both, wherein Q is NH, O, or S; and R?1, R2, R3, R4 and R5¿ are each independently hydrogen, halogeno, C¿1-6? alkyl, or a group of the general formula: -X-A (wherein X is a single bond, optionally substituted C1-6 alkylene, or the like; and A is, e.g., a C6-14 aromatic carbocyclic group or a 5- to 14-membered aromatic heterocyclic group, any of which may be optionally substituted).

5. 发明公开

EP1153922A4 HETERODIAZINONE DERIVATIVES 有权
标题翻译： HETERODIAZINON衍
公开(公告)号：EP1153922A4
公开(公告)日：2002-05-15
申请号：EP00902953
申请日：2000-02-15
申请人： EISAI CO LTD
发明人： ITO KOICHI , KITAZAWA NORITAKA , NAGATO SATOSHI , KAJIWARA AKIHARU , FUKUSHIMA TATSUTO , HATAKEYAMA SHINJI , HANADA TAKAHISA , UENO MASATAKA , UENO KOHSHI , KAWANO KOKI
IPC分类号： A61K31/53 , A61K31/5395 , A61K31/549 , A61P25/00 , C07D249/12 , C07D271/10 , C07D271/113 , C07D285/16 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D253/06 , C07D273/04 , C07D285/18
CPC分类号： C07D271/113 , A61K31/53 , A61K31/5395 , A61K31/549 , C07D249/12 , C07D285/16 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： Heterodiazinone derivatives represented by general formula (1 ), pharmacologically acceptable salts of the same, or hydrates of both, exhibiting 2-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonism wherein A is O, S or NR3 (wherein R3 is hydrogen or lower alkyl); R?1 and R2¿ are each independently optionally substituted (hetero)aryl or the like; and R?4 and R5¿ are each independently hydrogen, hydroxyl, halogeno, cyano, nitro, lower alkyl, (hetero)aryl, or the like.
摘要翻译：由通式（1）表示的异二嗪酮衍生物，其药理学上可接受的盐或两者的水合物显示2-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗作用，其中A是O，S 或NR 3（其中R 3是氢或低级烷基）; R 1和R 2'各自独立地为任选取代的（杂）芳基等; R 4和R 5各自独立地为氢，羟基，卤素，氰基，硝基，低级烷基，（杂）芳基等。

6. 发明专利

CA2362385C HETERODIAZINON COMPOUND 未知
公开(公告)号：CA2362385C
公开(公告)日：2009-08-11
申请号：CA2362385
申请日：2000-02-15
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KITAZAWA NORITAKA , KAWANO KOKI , HANADA TAKAHISA , ITO KOICHI , HATAKEYAMA SHINJI , FUKUSHIMA TATSUTO , UENO KOHSHI , UENO MASATAKA , KAJIWARA AKIHARU
IPC分类号： C07D413/04 , A61K31/53 , A61K31/5395 , A61K31/549 , A61P25/00 , A61P25/28 , C07D249/12 , C07D271/10 , C07D271/113 , C07D273/04 , C07D285/16 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a novel compound having an excellent 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, particularly a therapeutic, preventing and ameliorating action useful for cerebral ischemia, cerebrospinal injuries, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's chorea, epilepsy, pain, spastic paralysis, multiple sclerosis etc. That is, the present invention provides a heterodiazinon compound represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. (see formula I) Wherein A represents an oxygen atom, a sulfur atom or a group represented by the formula >NR3 (wherein R3 represents hydrogen atom or a lower alkyl group); R1 and R2 are the same as or different from each other and each represents an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted aralkyl group, an optionally substituted heteroaryl alkyl group, an optionally substituted aryl alkenyl group, an optionally substituted heteroaryl alkenyl group, an optionally substituted piperidyl group, an optionally substituted piperazinyl group; a morpholinyl group, an optionally substituted lower cycloalkyl group, a tetrahydrofuranyl group, a tetrahydropyranyl group, an adamantyl group, an optionally substituted amino group or an optionally substituted amide group; and R4 and R5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, an aryl group or a heteroaryl group, provided that the compounds represented by the following formula (II): (see formula II) (wherein R11 and R12 are the same as or different from each other and each represents hydrogen atom, fluorine, chlorine, bromine, iodine, a C1-C2 fluoroalkyl group, a C1-C2 chloroalkyl group, a C1-C2 bromoalkyl group, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C7-C9 aralkyl group, phenyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a C1-C6 alkylsulfinyl group, a C7-C9 aralkoxy group, phenoxy group, phenylthio group, phenylsulfonyl group, alkali metal carboxylate C2-C5 alkoxycarbonyl group or a group represented by the formula -N(R15)R16 (wherein R15 and R16 are the same as or different from each other and each represents hydrogen atom or a C1-C2 alkyl group); and R13 and R14 are the same as or different from each other and each represents a C1-4 alkylsulfonyl group, nitro group, a group represented by the formula -OCH n X3-n (wherein Xrepresents fluorine, chlorine, bromine or iodine; and n is any of integers 1 to 3) or a group having the same meanings as the definitions of R11 and R12) are excluded.

7. 发明专利

FI113172B 未知
公开(公告)号：FI113172B
公开(公告)日：2004-03-15
申请号：FI951417
申请日：1995-03-24
申请人： EISAI CO LTD
发明人： AKASAKA KOZO , YONAGA MASAHIRO , KAJIWARA AKIHARU , HIGURASHI KUNIZO , UENO KOHSHI , NAGATO SATOSHI , KOMATSU MAKOTO , KITAZAWA NORITAKA , UENO MASATAKA , YAMANISHI YOSHIHARU , MACHIDA YOSHISMASA , KOMATSU YUKI , SHIMOMURA NAOYUKI , MINAMI NORIO , SHIMIZU TOSHIKAZU , NAGOKA ATSUSHI
IPC分类号： C07D295/03 , A61K31/495 , A61P25/18 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/04 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/18 , C07D295/116 , C07D213/36
摘要： A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R represents a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group, a lower alkoxyalkyl group, a lower alkoxyalkoxy group, an aryl group, an aralkyl group, a heteroaryl group, a heteroarylalkyl group, a halogenated heteroarylalkyl group, a cyano lower alkyl group, a hydroxy lower alkyl group, an amino lower alkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, a cyano group, a formyl group, a lower acyl group, an aralkylcarbonyl group, a cycloether group, an alkenyl group, an alkynyl group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower alkylaminosulfonyl group, an arylaminosulfonyl group, a lower alkylsulfonylamino group, a halogenated lower alkylsulfonylamino group or an arylsulfonylamino group; R and R may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group or a cyano group; R represents a hydrogen atom or a halogen atom; R represents a hydrogen atom, a lower alkyl group, a halogenated lower alkyl group, a hydroxy lower alkyl group, a lower alkoxycarbonyl group or an aryloxycarbonyl group; and n is 0 or an integer of 1 to 3, which exhibits dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis.

8. 发明专利

HU0303398A2 1,2-DIHYDROPYRIDINE COMPOUNDS, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 未知
公开(公告)号：HU0303398A2
公开(公告)日：2004-03-01
申请号：HU0303398
申请日：2001-06-08
申请人： EISAI CO LTD
发明人： AMINO HIROYUKI , GROOM ANTHONY JOHN , HANADA TAKAHISA , HATAKEYAMA SHINJI , ITO KOICHI , KAWANO KOKI , NAGATO SATOSHI , NAKA HIROYUKI , NORIMINE YOSHIHIKO , OGO MAKOTO , RIVERS LEANNE , SMITH TERENCE , UENO KOHSHI , UENO MASATAKA , URAWA YOSHIO
IPC分类号： A61K20060101 , A61P20060101 , A61P1/08 , A61P9/10 , A61P13/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/06 , C07F7/18
摘要： The present invention provides compounds represented by the formula: or a salt thereof, wherein, each A 1a and A 3a are the same as or different from each other and each indicates an optionally substituted C 6-14 aromatic hydrocarbocyclic group or 5 to 14-membered aromatic heterocyclic group; and W represents a halogen atom. The compounds are intermediates for the preparation of inhibitors of the AMPA receptor.

9. 发明专利

NO20031232L 未知
公开(公告)号：NO20031232L
公开(公告)日：2003-05-19
申请号：NO20031232
申请日：2003-03-17
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： C07D237/14 , C07D237/24 , C07D401/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D237/04
摘要： The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, A , A and A are independent of each other and each represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X , X and X are independent of each other and each represents a single bond, an optionally substituted C1-6 alkylene group, an optionally substituted C2-6 alkenylene group, an optionally substituted C2-6 alkynylene group, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, etc.; R and R are independent of each other and each represents a hydrogen atom or an optionally substituted C1-6 alkyl group, or R and R may be bound together such that CR -ZR forms C=C; and R represents a hydrogen atom or an optionally substituted C1-6 alkyl group etc., or may be bound to any atom in A or A to form, together with the atom, an optionally substituted C5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

10. 发明专利

ES2184772T3 未知
公开(公告)号：ES2184772T3
公开(公告)日：2003-04-16
申请号：ES95104208
申请日：1995-03-22
申请人： EISAI CO LTD
发明人： AKASAKA KOZO , YONAGA MASAHIRO , KAJIWARA AKIHARU , HIGURASHI KUNIZO , UENO KOHSHI , NAGATO SATOSHI
IPC分类号： C07D295/03 , A61K31/495 , A61P25/18 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/04 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/18 , C07D213/36 , C07D295/20 , C07D295/06 , C07D295/14 , C07D295/12 , C07D295/08 , C07D319/14 , C07D213/74 , C07D295/22
摘要： A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R represents a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group, a lower alkoxyalkyl group, a lower alkoxyalkoxy group, an aryl group, an aralkyl group, a heteroaryl group, a heteroarylalkyl group, a halogenated heteroarylalkyl group, a cyano lower alkyl group, a hydroxy lower alkyl group, an amino lower alkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, a cyano group, a formyl group, a lower acyl group, an aralkylcarbonyl group, a cycloether group, an alkenyl group, an alkynyl group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower alkylaminosulfonyl group, an arylaminosulfonyl group, a lower alkylsulfonylamino group, a halogenated lower alkylsulfonylamino group or an arylsulfonylamino group; R and R may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group or a cyano group; R represents a hydrogen atom or a halogen atom; R represents a hydrogen atom, a lower alkyl group, a halogenated lower alkyl group, a hydroxy lower alkyl group, a lower alkoxycarbonyl group or an aryloxycarbonyl group; and n is 0 or an integer of 1 to 3, which exhibits dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis.

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