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1. 发明授权

US4342766A Novel dihydro-as-triazino[5,6-c]quinoline derivatives and a process for the preparation thereof 失效
标题翻译：新型二氢 - 三嗪并[5,6-c]喹啉衍生物及其制备方法
公开(公告)号：US4342766A
公开(公告)日：1982-08-03
申请号：US254763
申请日：1981-04-16
申请人： Edit Berenyi nee Poldermann , Peter Gorog , Katalin Grasser , Ibolya Kosoczky , Agnes Koracs nee Palotay , Lujza Petocz
发明人： Edit Berenyi nee Poldermann , Peter Gorog , Katalin Grasser , Ibolya Kosoczky , Agnes Koracs nee Palotay , Lujza Petocz
IPC分类号： A61K31/4745 , A61K31/53 , A61P23/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P29/00 , C07D471/04 , A61K31/395
CPC分类号： C07D471/04
摘要： New compounds are disclosed of the formulae ##STR1## or pharmaceutically effective salts thereof, wherein R is hydrogen, C.sub.1-12 alkyl, or R is phenyl or phenyl-C.sub.1 to C.sub.4 alkyl wherein the phenyl can be substituted with 1 to 3 halogen, C.sub.1 to C.sub.4 alkyl, or C.sub.1 to C.sub.4 alkoxy substituents; andX.sub.1, X.sub.2 and X.sub.3 are hydrogen, C.sub.1 to C.sub.6 alkanoyl, or C.sub.1 to C.sub.6 haloalkanoyl; and where X.sub.1 is hydrogen, X.sub.2 and X.sub.3 are not simultaneously hydrogen. The compounds possess antiphlogistic, analgesic, anticonvulsive, or tranquilizing properties.
摘要翻译：公开了新的化合物或其药学有效盐，其中R是氢，C 1-12烷基或R是苯基或苯基-C 1至C 4烷基，其中苯基可被1至3个卤素取代，C 1 至C 4烷基或C 1至C 4烷氧基取代基; 且X 1，X 2和X 3为氢，C 1至C 6烷酰基或C 1至C 6卤代烷酰基; 并且其中X1为氢，X2和X3不同时为氢。该化合物具有消炎，镇痛，抗惊厥或镇静作用。

2. 发明授权

US4871846A Process for the preparation of condensed as-triazine derivatives 失效
标题翻译：缩合的三嗪衍生物的制备方法
公开(公告)号：US4871846A
公开(公告)日：1989-10-03
申请号：US43600
申请日：1987-04-28
申请人： Sandor Batori , Gyorgy Hajos , Andras Messmer , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly
发明人： Sandor Batori , Gyorgy Hajos , Andras Messmer , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly
IPC分类号： C07D215/12 , C07D215/58 , C07D217/16 , C07D217/18 , C07D471/04
CPC分类号： C07D471/04 , C07D215/58 , C07D217/18
摘要： A process for the preparation of condensed as-triazinium derivatives of the formula I ##STR1## and isomers thereof, wherein R.sub.1 inter alia is an alkyl group, R.sub.2 inter alia is hydrogen or an alkyl group and R.sub.3 is hydrogen and where Z is a group of the formula a or b ##STR2## which comprises reacting a compound of the formula II ##STR3## where Y is a group of the formula c or d ##STR4## with a compound of the formula IIaNH.sub.2 --CO--R.sub.2 (IIa)in the presence of a dehydrating agent. The advantage of the process is that it consists of fewer reaction steps and provides higher yields than the known methods. The compounds of formula I are pharmaceutically active known derivatives.
摘要翻译：一种制备式I（I）的缩合的三嗪鎓衍生物及其异构体的方法，其中R1特别是烷基，R 2特别是氢或烷基，R 3是氢，并且其中Z 是式a或b的基团（a）（b），其包括使式II的化合物（II）其中Y是式c的基团或d （c）在脱水剂存在下，用式IIa NH 2 -CO-R 2（IIa）化合物与（d）化合物反应。该方法的优点在于其由较少的反应步骤组成，并提供比已知方法更高的产率。式I的化合物是药学活性的已知衍生物。

3. 发明授权

US4753938A Condensed as-triazine derivatives 失效
标题翻译：浓缩的三嗪衍生物
公开(公告)号：US4753938A
公开(公告)日：1988-06-28
申请号：US787704
申请日：1985-10-15
申请人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
发明人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/53 , A61P9/06 , A61P25/02 , A61P25/24 , A61P29/00 , A61P43/00 , C07D471/04 , C07D253/08
CPC分类号： C07D471/04
摘要： The invention relates to new compounds of the general Formula I ##STR1## and isomers thereof wherein R.sub.1 is C.sub.1-10 alkyl, C.sub.3-6 cycloalkyl or phenyl, naphthyl or phenyl-(C.sub.1-4 alkyl), wherein the aryl ring of the three latter groups may optionally bear one or more halogen, nitro, trifluoromethyl, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.2 stands for hydrogen, halogen, hydroxy, oxo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or naphthyl, wherein the two latter groups may optionally bear one or more halogen, nitro, trifluoromethyl, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.3 represents hydrogen, hydroxy or C.sub.1-4 alkoxy;Z is buta-1,3-dienyl or a group of the general Formula (a) ##STR2## or (b) ##STR3## and X is hydrogen or halogen.The compounds of the general Formula I possess useful pharmacological properties, particularly antidepressant and antiarrhythmial effect.
摘要翻译：本发明涉及通式I（I）的新化合物及其异构体，其中R 1为C 1-10烷基，C 3-6环烷基或苯基，萘基或苯基 - （C 1-4烷基），其中芳基环三个后面的基团可任选地带有一个或多个卤素，硝基，三氟甲基，氨基，羟基，C 1-4烷基和/或C 1-4烷氧基取代基; R2代表氢，卤素，羟基，氧代，C1-4烷基，C1-4烷氧基，苯基或萘基，其中后两个基团可任选地具有一个或多个卤素，硝基，三氟甲基，氨基，羟基，C 1-4烷基和/或C 1-4烷氧基取代基; R3表示氢，羟基或C1-4烷氧基; Z是丁-1,3-二烯基或通式（a）的基团（a）或（b）图像（b），X是氢或卤素。通式I的化合物具有有用的药理学特性，特别是抗抑郁药和抗心律失常作用。

4. 发明授权

US4665083A Iminothiazolidine derivatives 失效
标题翻译：亚氨基噻唑烷衍生物
公开(公告)号：US4665083A
公开(公告)日：1987-05-12
申请号：US726867
申请日：1985-04-25
申请人： Karoly Lempert , Gyula Hornyak , Ferenc Bartha , Gabor Doleschall , Jozsef Fetter , Jozsef Nyitrai , Gyula Simig , Karoly Zauer , Peter Huszthy , Antal Feller , Lujza Petocz , Eniko Szirt , Katalin Grasser , Edit Berenyi , Zsuzsanna Orr , Etelka Pjeczka
发明人： Karoly Lempert , Gyula Hornyak , Ferenc Bartha , Gabor Doleschall , Jozsef Fetter , Jozsef Nyitrai , Gyula Simig , Karoly Zauer , Peter Huszthy , Antal Feller , Lujza Petocz , Eniko Szirt , Katalin Grasser , Edit Berenyi , Zsuzsanna Orr , Etelka Pjeczka
IPC分类号： A61K31/425 , A61K31/426 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/26 , C07D277/12 , C07D277/18
CPC分类号： C07D277/18
摘要： The invention relates to novel iminothiazolidine derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.3 represent, independently from each other, hydrogen or lower alkyl group,R.sup.3 is nitro or amino group,R stands for halo, lower alkyl, haloalkyl, nitro, amino, hydroxy, lower alkoxy, carboxy or lower alkoxycarbonyl group, andn is 0, 1 or 2,and pharmaceutically acceptable acid addition salts thereof.The iminothiazolidine derivatives of the formula (I) possess valuable antidepressant, antiparkinsonic, antiepileptic and spasmolytic activities.
摘要翻译：本发明涉及式（I）的新型亚氨基噻唑烷衍生物，其中R 1和R 3彼此独立地表示氢或低级烷基，R 3是硝基或氨基，R代表卤素，低级烷基，卤代烷基，硝基，氨基，羟基，低级烷氧基，羧基或低级烷氧基羰基，n为0,1或2及其药学上可接受的酸加成盐。式（I）的亚氨基噻唑烷衍生物具有有价值的抗抑郁药，抗帕金森病，抗癫痫和解痉作用。

5. 发明授权

US4259257A 1-Phenyl-2-amino-1,3-propanediol-N-aryloxyalkyl derivatives 失效
标题翻译： 1-苯基-2-氨基-1,3-丙二醇-N-芳氧基烷基衍生物
公开(公告)号：US4259257A
公开(公告)日：1981-03-31
申请号：US73563
申请日：1979-09-07
申请人： Laszlo Levai , Gabor Fazekas , Lujza Petocz , Katalin Grasser
发明人： Laszlo Levai , Gabor Fazekas , Lujza Petocz , Katalin Grasser
IPC分类号： A61K31/135 , A61K20060101 , A61K31/13 , A61K31/137 , A61P11/04 , A61P21/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P29/00 , B01J23/00 , B01J23/40 , B01J25/00 , C07B61/00 , C07C20060101 , C07C67/00 , C07C213/00 , C07C215/36 , C07C93/06
CPC分类号： C07C51/353
摘要： The invention relates to novel 1-phenyl-2-amino-1,3-propanediol-N-alkyl derivatives having the general formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl having from 1 to 8 carbon atoms or phenoxymethyl, andR.sub.2 is hydrogen, alkyl having from 1 to 8 carbon atoms or 2,2-diphenylethyl,with the proviso that if R.sub.1 is phenoxymethyl then R.sub.2 may stand only for methyl, and if R.sub.2 is 2,2-diphenylethyl then R.sub.1 may stand only for hydrogen, and its isomers and pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The novel 1-phenyl-2-amino-1,3-propanediol-N-alkyl derivatives having the general formula I possess significant anti-anginose activity and show several other biological activities.
摘要翻译：本发明涉及具有通式I（I）的新颖的1-苯基-2-氨基-1,3-丙二醇-N-烷基衍生物，其中R 1是氢，具有1至8个碳原子的烷基或苯氧基甲基，并且R 2是氢，具有1至8个碳原子的烷基或2,2-二苯基乙基，条件是如果R 1是苯氧基甲基，那么R 2可以仅仅是甲基，并且如果R 2是2,2-二苯基乙基，那么R 1可以仅仅是氢及其异构体和药学上可接受的盐。此外，本发明涉及一种制备这些化合物的方法。具有通式I的新型1-苯基-2-氨基-1,3-丙二醇-N-烷基衍生物具有显着的抗焦虑作用，并显示出其它几种生物活性。

6. 发明授权

US4077999A Novel oxime ethers 失效
标题翻译：新型肟醚
公开(公告)号：US4077999A
公开(公告)日：1978-03-07
申请号：US749399
申请日：1976-12-10
申请人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Katalin Grasser , Eniko Szirt nee Kiszelly , Ibolya Kosoczky , Lujza E. Petocz
发明人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Katalin Grasser , Eniko Szirt nee Kiszelly , Ibolya Kosoczky , Lujza E. Petocz
IPC分类号： C07C251/58 , C07D295/088 , C07C131/02 , C07C131/04
CPC分类号： C07D295/088 , C07C251/58 , C07C2101/08 , C07C2101/16 , C07C2101/18
摘要： The invention relates to novel oxime ethers of the formula I ##STR1## wherein R stands for a phenyl group which may be substituted by a halogen atom or by one or more C.sub.1 -C.sub.4 alkoxy, hydroxyl, nitro or di(C.sub.1 -C.sub.3 alkyl)amino groups,R.sup.1 and R.sup.2 denote each a hydrogen atom or together a valence bond,A denotes a C.sub.2 -C.sub.4 straight or branched-chain alkylene group,N denotes an integer from 3 to 10, andR.sup.3 and R.sup.4 denote a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, furthermore to acid addition salts and quaternary ammonium salts thereof. These new compounds are biologically active, and possess primarily local analgesic, spasmolytic, nicotine-lethality inhibiting, tetrabenazine-antagonistic and tetra-cor-spasm inhibiting effects.
摘要翻译：本发明涉及式I（I）的新型肟醚，其中R代表可被卤素原子取代的苯基或一个或多个C 1 -C 4烷氧基，羟基，硝基或二（C1- C 3烷基）氨基，R 1和R 2各自表示氢原子或价键一起，A表示C 2 -C 4直链或支链亚烷基，N DENOTES AN INTEGER为3〜10，R 3和R 4表示氢原子或C1-C4烷基，此外还涉及其酸加成盐和季铵盐。这些新化合物具有生物活性，主要具有局部镇痛，解痉，尼古丁致死抑制，四苯并嗪拮抗和四痉挛抑制作用。

7. 发明授权

US4395413A Oxime ethers and pharmaceutical compositions containing the same 失效
标题翻译：肟醚和含有它的药物组合物
公开(公告)号：US4395413A
公开(公告)日：1983-07-26
申请号：US162674
申请日：1980-06-24
申请人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly , Peter Gorog
发明人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly , Peter Gorog
IPC分类号： A61K31/15 , A61K31/495 , A61P25/04 , C07C67/00 , C07C239/00 , C07C249/10 , C07C251/58 , C07D295/02 , C07D295/088 , C07D295/08
CPC分类号： C07D295/088 , Y10S514/926 , Y10S514/927
摘要： The invention relates to novel oxime ethers of the general formula /I/ and acid addition salts and quaternary ammonium derivatives thereof, ##STR1## wherein A represents a C.sub.2-6 straight or branched alkylene chain,R and R.sup.1 each represent a C.sub.1-6 alkyl group or they form together with the adjacent nitrogen atom a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further hetero atom, i.e. an oxygen, sulfur or nitrogen atom, and said ring may be optionally substituted by a C.sub.1-3 alkyl, phenyl or benzyl group,R.sup.2 and R.sup.3 each denote a hydrogen atom or together form a valency bond,R.sup.4 denotes a C.sub.1-10 alkyl or C.sub.2-10 alkenyl group, andn denotes an integer from 3 to 7.The compounds of the general formula /I/ are prepared according to the invention by reacting a cycloalkane derivative of the general formula /II/ ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and n have the same meaning as above, whereasY denotes an oxygen or sulphur atom or a .dbd.N--OH group with an aminoalkyl derivative of the general formula /III/ ##STR3## wherein R, R.sup.1 and A have the same meaning as stated above andZ means a halogen atom or a H.sub.2 N--O-- group or a salt thereof in the presence of a basic condensing agent.The new compounds of the general formula /I/ possess valuable nicotine-lethality inhibiting, local anaesthetic, analgesic effects, which are, in case of certain compounds, complemented by anti-hypertensive, maximum electroshock and tetracorspasm inhibiting, ulcus inhibiting and motility inhibiting effects, and can be applied to advantage in the therapy.
摘要翻译：本发明涉及通式I I的新型肟醚及其酸加成盐和季铵衍生物，其中A表示C2-6直链或支链亚烷基链，R和R1各自表示C1 -6烷基，或者它们与相邻的氮原子一起与含有4至7个碳原子的杂环和任选的另外的杂原子（即氧，硫或氮原子）一起形成，并且所述环可以任选地被C 1-3 烷基，苯基或苄基，R2和R3各自表示氢原子或一起形成价键，R4表示C1-10烷基或C2-10烯基，n表示3至7的整数。根据本发明通过使通式/ II / IMAGE / II /的环烷烃衍生物与其中R2，R3，R4和n具有与上述相同的含义反应制备通式/ I / I，而Y表示氧或硫原子或a =具有氨基烷基衍生物的N-OH基团通式/ III / / III /其中R，R 1和A具有与上述相同的含义，Z表示在碱性缩合剂存在下的卤素原子或H 2 N-O-基或其盐。新型化合物/ I /具有有价值的尼古丁杀伤力抑制，局部麻醉，止痛作用，在某些化合物的情况下，补充有抗高血压，最大电休克和四疣抑制作用，抑制溃疡和运动抑制作用，并且可以在治疗中有利地应用。

8. 发明授权

US4208410A Dibenzo[d,g][1,3,6]dioxazocine derivatives 失效
标题翻译：二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物
公开(公告)号：US4208410A
公开(公告)日：1980-06-17
申请号：US927934
申请日：1978-07-25
申请人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
发明人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
IPC分类号： A61K31/553 , C07D273/00 , C07D273/01 , C07D267/22 , A61K31/395
CPC分类号： C07D273/00 , Y10S514/818
摘要： This invention relates to novel dibenzo[d,g][1,3,6]dioxazocine derivatives represented by the general formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, cyano or trifluoromethyl,Y stands for hydrogen or a group of formula ##STR2## wherein A stands for a straight or branched chained alkylene having from 2 to 5 carbon atoms andR.sub.3 and R.sub.4 independently stand for an alkyl having from 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the nitrogen atom they are attached to and optionally together with a further nitrogen atom or with an additional oxygen atom may form a five- or six-membered heterocyclic ring optionally substituted with an alkyl having from 1 to 4 carbon atoms,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.The above compounds possess valuable pharmaceutical properties, for instance they are effective local anaesthetics and can be used for treating Parkinson syndrome.
摘要翻译：本发明涉及由通式I（I）表示的新的二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物，其中R 1和R 2独立地表示氢，卤素，氰基或三氟甲基，Y代表氢或一组式（I）其中A代表具有2至5个碳原子的直链或支链链状亚烷基，R3和R4独立代表具有1至4个碳原子的烷基，或R3和R4与氮原子一起它们与另外的氮原子或与另外的氧原子连接并且可选地与另外的氧原子连接的原子可以形成任选被具有1至4个碳原子的烷基取代的五元或六元杂环，及其药学上可接受的酸加成盐由无机或有机酸形成。上述化合物具有有价值的药物性质，例如它们是有效的局部麻醉剂，并且可用于治疗帕金森综合征。

9. 发明授权

US4621101A Pharmaceutical compositions with antianginal activity 失效
标题翻译：具有抗心绞痛活性的药物组合物
公开(公告)号：US4621101A
公开(公告)日：1986-11-04
申请号：US751623
申请日：1985-07-02
申请人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Zsuzsanna Orr
发明人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Zsuzsanna Orr
IPC分类号： A61K31/15 , A61P43/00 , C07C251/38
CPC分类号： C07C251/58 , C07C2101/14 , C07C2101/18
摘要： The invention relates to pharmaceutical compositions possessing valuable antianginal activity. These compositions show higher activity and more favorable therapeutic indices than the reference compound Prenylamine. Preparation of different kinds of pharmaceutical compositions, such as tablets, dragees, capsules and injectable solutions, containing compounds of general formula (I) ##STR1## or their acid addition salts as active ingredients, is disclosed, wherein in formula (I)R is phenyl or 4-chlorophenyl;R.sup.1 and R.sup.2 each represent hydrogen, methyl or isopropyl;R.sup.3 and R.sup.4 are hydrogen, or together form a chemical bond;n is an integer from 4 to 6;A means trimethylene, if n is 4 or 6; or ethylene, if n is 5.
摘要翻译：本发明涉及具有有价值的抗心绞痛活性的药物组合物。这些组合物显示比参考化合物Prenylamine更高的活性和更有利的治疗指数。公开了含有通式（I）化合物或其酸加成盐作为活性成分的不同种类的药物组合物如片剂，硫化物，胶囊和可注射溶液的制备，其中在式（I）中R是苯基或4-氯苯基; R1和R2各自表示氢，甲基或异丙基; R3和R4是氢，或一起形成化学键; n为4-6的整数; 如果n为4或6，则表示三亚甲基; 或乙烯，如果n为5。

10. 发明授权

US4727074A 2-(phenylmethylene)-1-(diaminoalkoxy) cycloalkanes and their pharmaceutical uses 失效
标题翻译： 2-（苯基亚甲基）-1-（二氨基烷氧基）环烷烃及其药物用途
公开(公告)号：US4727074A
公开(公告)日：1988-02-23
申请号：US578286
申请日：1984-02-08
申请人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
发明人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61P9/06 , A61P23/00 , A61P25/04 , C07C67/00 , C07C239/00 , C07C251/44 , C07C251/58 , C07D295/088 , A61K31/495 , A61K31/205 , C07C131/02
CPC分类号： C07D295/088
摘要： The invention relates to selected stereoisomers having the E, E or E, Z configuration and within the Formula (I) ##STR1## wherein N is 2-4, A is alkylene or 2 or 3 carbon atoms, R is phenyl or substituted phenyl and R.sup.1 and R.sup.2 are lower alkyl, or, together with the carbon to which attached, form a heterocyclic ring; and pharmaceutically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions comprising the same.The compounds of the general formula (I) can be used in therapy due to their narcosis potentiating, analgesic and antiarrhythmial effect.
摘要翻译：本发明涉及具有E，E或E，Z构型的选定的立体异构体，并且在其中N为2-4的式（I）中，A为亚烷基或2或3个碳原子，R为苯基或取代的苯基，R 1和R 2为低级烷基，或与连接的碳一起形成杂环; 及其药学上可接受的酸加成盐，其制备方法和包含其的药物组合物。通式（I）的化合物可以用于治疗，因为它们具有麻醉增效，止痛和抗心律失常作用。

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