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1. 发明申请

WO2016060564A1 BODY SCULPTING 审中-公开
标题翻译：身体雕刻
公开(公告)号：WO2016060564A1
公开(公告)日：2016-04-21
申请号：PCT/NL2015/050722
申请日：2015-10-14
申请人： BRAINS ONLINE HOLDING B.V. ET ALL , RIJKSUNIVERSITEIT GRONINGEN
发明人： CREMERS , Thomas , FLIK, Gunnar , FRIJLINK, Henderik Willem , WOERDENBAG, Herman Johan
IPC分类号： A61K31/23 , A61P3/04 , C07C219/30 , A61K9/00 , A61K9/06
CPC分类号： A61K8/37 , A61K8/41 , A61K9/0014 , A61K9/06 , A61K31/00 , A61K31/137 , A61K31/22 , A61K31/23 , A61K47/32 , A61K2800/74 , A61Q19/06 , C07C219/30
摘要： The invention pertains to a pharmaceutical composition for topical administration, comprising a prodrug for an agonist and/or an antagonist for an adrenergic receptor, wherein the prodrug has an octanol/water partition coefficient of at least 0, for use in a method of shaping a mammalian body by modulation of subcutaneous fat tissue. The invention further pertains to cosmetic and therapeutic application of such prodrugs, such as their use in methods of shaping a mammalian body by locally modulating subcutaneous fat tissue. The invention also pertains to the prodrugs themselves, as well as to methods of making these prodrugs.
摘要翻译：本发明涉及用于局部给药的药物组合物，其包含用于肾上腺素能受体的激动剂和/或拮抗剂的前体药物，其中前药具有至少为0的辛醇/水分配系数，用于成型方法哺乳动物身体通过调节皮下脂肪组织。本发明还涉及这些前药的美容和治疗应用，例如它们用于通过局部调节皮下脂肪组织来形成哺乳动物体的方法。本发明还涉及前药本身，以及制备这些前药的方法。

2. 发明申请

WO1994008943A1 2-AMINO-1,3-PROPANEDIOL COMPOUND AND IMMUNOSUPPRESSANT 审中-公开
标题翻译： 2-氨基-1,3-丙二醇化合物和免疫抑制剂
公开(公告)号：WO1994008943A1
公开(公告)日：1994-04-28
申请号：PCT/JP1993001515
申请日：1993-10-18
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , TAITO CO., LTD. , FUJITA, Tetsuro , SASAKI, Shigeo , YONETA, Masahiko , MISHINA, Tadashi , ADACHI, Kunitomo , CHIBA, Kenji
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , TAITO CO., LTD.
IPC分类号： C07C215/10
CPC分类号： C07D207/325 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07C2601/08 , C07C2601/14 , C07D207/06 , C07D207/09 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D231/12 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20
摘要： A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient. In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R , R , R and R , which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl. The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields.
摘要翻译：由通式（I）表示的2-氨基-1,3-丙二醇化合物或其药学上可接受的盐，和含有该活性成分的免疫抑制剂。在所述式中，R代表任选取代的直链或支链碳链，任选取代的芳基或任选取代的环烷基; 和R 2，R 3，R 4和R 5彼此可以相同或不同，表示每个氢，烷基，芳烷基，酰基或烷氧基羰基。该化合物是免疫抑制剂，可用作作为器官或骨髓移植排斥反应的抑制剂，作为自身免疫疾病等的预防或补救剂，或医药领域的试剂。

3. 发明申请

WO1994007842A1 OLEAGINOUS COMPOSITIONS 审中-公开
标题翻译：含油组合物
公开(公告)号：WO1994007842A1
公开(公告)日：1994-04-14
申请号：PCT/EP1993002739
申请日：1993-10-05
申请人： EXXON CHEMICAL PATENTS INC. , JACKSON, Graham , KENWARD, Rachel, Evelyn, Mary , BROOKE, Barbara, Catherine
发明人： EXXON CHEMICAL PATENTS INC.
IPC分类号： C07C215/48
CPC分类号： C10L1/2225 , C07C215/50 , C07C219/30 , C07C221/00 , C07C223/02 , C07C229/38 , C07C255/59 , C07C323/32 , C10L1/143 , C10L1/1641 , C10L1/165 , C10L1/195 , C10L1/1963 , C10L1/1966 , C10L1/1973 , C10L1/1985 , C10L1/22 , C10L1/2222 , C10L1/224 , C10L1/2286 , C10L1/231 , C10L1/232 , C10L1/238 , C10L1/2412 , C10L1/2418 , C10L1/2431 , C10L1/2437 , C10L1/245 , C10M133/08 , C10M2215/04 , C10M2215/042 , C10M2215/062 , C10M2215/22 , C10M2215/221 , C10M2215/225 , C10M2215/226 , C10M2215/26 , C10M2215/30 , C10M2219/084 , C10M2219/086 , C10M2219/10 , C10M2219/102 , C10M2219/104 , C10M2219/106 , C10N2240/02 , C10N2240/08 , C10N2240/10 , C10N2240/101 , C10N2240/102 , C10N2240/103 , C10N2240/104 , C10N2240/106 , C10N2270/02
摘要： Compounds of formula (I) are useful as addivitives in oleaginous compositions, wherein B represents an aromatic system, A represents a hydrocarbyl group, R1 and R2 are the same or are different and each independently is an aliphatic hydrocarbyl group containing 10-40 carbon atoms, provided that one of R1 and R2 may represent hydrogen; z is at least 1 and wherein the aromatic system carries at least one substituent group which is an activating group for the ring system or a derivative of an activating group.
摘要翻译：式（I）化合物可用作油性组合物中的添加剂，其中B表示芳族体系，A表示烃基，R1和R2相同或不同，并且各自独立地为含有10-40个碳原子的脂族烃基条件是R 1和R 2中的一个可以表示氢; z至少为1，并且其中芳族体系带有至少一个取代基，其为环系统的活化基团或活化基团的衍生物。

4. 发明申请

WO2012102875A2 ANALGESIC COMPOUNDS, METHODS, AND FORMULATIONS 审中-公开
标题翻译：镇痛化合物，方法和制剂
公开(公告)号：WO2012102875A2
公开(公告)日：2012-08-02
申请号：PCT/US2012021181
申请日：2012-01-13
申请人： LILLY CO ELI , DEFAUW JEAN MARIE , HOLMSTROM SCOTT DALE , CHEN SHUHUI , ZHANG YANG , WU WENTAO , PENG XIAN , MA YUJUAN , LU LUN
发明人： DEFAUW JEAN MARIE , HOLMSTROM SCOTT DALE , CHEN SHUHUI , ZHANG YANG , WU WENTAO , PENG XIAN , MA YUJUAN , LU LUN
IPC分类号： C07C217/54
CPC分类号： C07C215/64 , C07C217/74 , C07C219/28 , C07C219/30 , C07C2602/20 , C07C2602/42 , C07C2602/44 , C07C2602/50
摘要： Provided are analgesic compounds, and salts thereof, of formula: ( I ) wherein A is: ( A ) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.
摘要翻译：提供下式的镇痛化合物及其盐：（I）其中A是：（A）另外，提供了使用上述化合物的药物制剂和使用方法。

5. 发明申请

WO2012100423A1 ANALGESIC COMPOUNDS, METHODS, AND FORMULATIONS 审中-公开
标题翻译：分析化合物，方法和制剂
公开(公告)号：WO2012100423A1
公开(公告)日：2012-08-02
申请号：PCT/CN2011/070706
申请日：2011-01-27
申请人： ELI LILLY AND COMPANY , DEFAUW, Jean Marie , HOLMSTROM, Scott Dale , CHEN, Shuhui , ZHANG, Yang , WU, Wentao , PENG, Xian , MA, Yujuan , LU, Lun
发明人： DEFAUW, Jean Marie , HOLMSTROM, Scott Dale , CHEN, Shuhui , ZHANG, Yang , WU, Wentao , PENG, Xian , MA, Yujuan , LU, Lun
IPC分类号： C07C215/46 , C07C217/54 , A61K31/135 , A61K31/137 , A61P25/04 , A61P25/24
CPC分类号： C07C215/64 , C07C217/74 , C07C219/28 , C07C219/30 , C07C2602/20 , C07C2602/42 , C07C2602/44 , C07C2602/50
摘要： Provided are compounds, and salts thereof, of formula (I): wherein (A) is R 1 is hydrogen, C 1 -C 5 alkyl, C 1 -C 5 alkoxy, C 1 -C 5 haloalkyl, C 1 -C 5 alkanol, -(C 1 -C 5 alkyl)phenyl, or phenyl, or a group of the formula -C(O)-R 12 , where R 12 may be C 1 -C 5 alkyl, C 1 -C 5 alkoxy, C 1 -C 5 haloalkyl, C 1 -C 5 alkanol, -(C 1 -C 5 alkyl)phenyl, or phenyl; R 2 and R 3 are independently hydrogen, C 1 -C 5 alkyl, C 1 -C 5 alkoxy, halogen, C 1 -C 5 haloalkyl, or C 1 -C 5 haloalkoxy; R 4 and R 5 are independently hydrogen, C 1 -C 5 alkyl, or -(C 1 -C 5 alkyl)phenyl; R 6 is hydrogen, hydroxy, or is absent; R 7 is hydrogen; R 8 and R 9 are independently hydrogen or methyl; R 10 is hydrogen; R 11 is hydrogen or C 1 -C 5 alkyl; or R 7 and R 10 combine to form -CH 2 - or -(CH 2 ) 2 -; or R 8 and R 9 combine to form a cyclopropyl group with the carbon to which they are attached; or R 10 and R 11 combine to form -CH 2 - or -(CH 2 ) 3 -. Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.
摘要翻译：提供式（I）的化合物及其盐：其中（A）是R 1是氢，C 1 -C 5烷基，C 1 -C 5烷氧基，C 1 -C 5卤代烷基，C 1 -C 5链烷醇， - （C 1 -C 5烷基）苯基或苯基，或式-C（O）-R12的基团，其中R12可以是C1-C5烷基，C1-C5烷氧基，C1-C5卤代烷基，C1-C5链烷醇， - （C1-C5烷基）苯基或苯基; R2和R3独立地是氢，C1-C5烷基，C1-C5烷氧基，卤素，C1-C5卤代烷基或C1-C5卤代烷氧基; R4和R5独立地是氢，C1-C5烷基或 - （C1-C5烷基）苯基; R6是氢，羟基或不存在; R7是氢; R8和R9独立地是氢或甲基; R10是氢; R11是氢或C1-C5烷基; 或R 7和R 10结合形成-CH 2 - 或 - （CH 2）2 - ; 或R 8和R 9结合形成与它们所连接的碳的环丙基; 或R 10和R 11结合形成-CH 2 - 或 - （CH 2）3 - 。另外，提供使用上述化合物的药物制剂和使用方法。

6. 发明申请

WO03032969B1 ANTI-GLYCATION AGENTS FOR PREVENTING AGE-, DIABETES-, AND SMOKING-RELATED COMPLICATIONS 审中-公开
标题翻译：用于预防年龄，糖尿病和吸烟相关并发症的抗糖化剂
公开(公告)号：WO03032969B1
公开(公告)日：2003-10-16
申请号：PCT/CA0201552
申请日：2002-10-15
申请人： CA NAT RESEARCH COUNCIL , YEBOAH FAUSTINUS , KONISHI YASUO , CHO SUNG JU , LERTVORACHON JITTIWUD , KIYOTA TAIRA , TOMASZ POPEK
发明人： YEBOAH FAUSTINUS , KONISHI YASUO , CHO SUNG JU , LERTVORACHON JITTIWUD , KIYOTA TAIRA , TOMASZ POPEK
IPC分类号： A61K31/00 , A61K31/04 , A61K31/137 , A61K31/195 , A61K31/222 , A61K31/345 , A61K31/352 , A61K31/4164 , A61K31/4168 , A61K31/47 , A61K31/65 , A61P3/10 , A61P9/10 , A61P13/12 , A61P25/02 , C07C219/30
CPC分类号： A61K31/47 , A61K31/00 , A61K31/04 , A61K31/137 , A61K31/195 , A61K31/222 , A61K31/345 , A61K31/352 , A61K31/4164 , A61K31/4168 , A61K31/65 , C07C219/30
摘要： The invention provides new inhibitors of protein glycation, identified from compound libraries by a high throughput screening assay. The anti-glycation agents so identified are characterized by a variety of chemical structures and are useful for the prevention or treatment of age-, diabetes-, and smoking-related complications, including neuropathy, nephropathy, ocular pathologies, or the loss of mechanical properties of collagenous tissues. Among compounds identified as having the anti-glycation activity, of special interest are epinephrine and its analogs, in particular D-epinephrine and its analogs, which are particularly useful for the prevention or treatment of age-, diabetes-, and smoking-related ocular pathologies.
摘要翻译：本发明提供了蛋白质糖化的新型抑制剂，其通过高通量筛选测定从化合物文库中鉴定。如此鉴定的抗糖化剂的特征在于各种化学结构，并且可用于预防或治疗与年龄，糖尿病和吸烟有关的并发症，包括神经病，肾病，眼病，或机械性能的丧失的胶原组织。在鉴定为具有抗糖化活性的化合物中，特别感兴趣的是肾上腺素及其类似物，特别是D-肾上腺素及其类似物，其特别用于预防或治疗年龄，糖尿病和吸烟相关的眼睛病症。

7. 发明申请

WO2003103650A1 WIRKSTOFFSALZE UND ESTER VON 1-DIMETHYLAMINO-3-(3-METHOXY-PHENYL)-2-METHYL-PENTAN-3-OL UND 3-(3-DIMETHYLAMINO-1-ETHYL-1-HYDROXY-2-METHYL-PROPYL)-PHENOL 审中-公开
标题翻译：活性物质的盐和1-二甲基氨基-3-（3-甲氧基 - 苯基）-2-甲基戊-3-醇和3-的酯（3-二甲基氨基-1-乙基-1-羟基-2-甲基 - 丙基） - 苯酚
公开(公告)号：WO2003103650A1
公开(公告)日：2003-12-18
申请号：PCT/EP2003/005971
申请日：2003-06-06
申请人： GRÜNENTHAL GMBH , HOLENZ, Jörg , BUSCHMANN, Helmut
发明人： HOLENZ, Jörg , BUSCHMANN, Helmut
IPC分类号： A61K31/13
CPC分类号： C07D231/38 , A61K45/06 , C07C51/418 , C07C59/48 , C07C59/68 , C07C215/62 , C07C217/72 , C07C219/30 , C07C229/42 , C07D209/28 , C07D231/28 , C07D231/34 , C07D417/12
摘要： Die Erfindung betrifft Wirkstoffsalze und Ester von 1-Dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol und 3-(3-Dimethylamino-1-ethyl-1-hydroxy-2-methyl-propyl)-phenol, Verfahren zu deren Herstellung, deren Verwendung zur Herstellung eines Arzneimittels zur Behandlung von vermehrtem Harndrang bzw. Harninkontinenz sowie entsprechende Arzneimittel und Verfahren zur Behandlung von vermehrtem Harndrang bzw. Harninkontinenz.
摘要翻译：本发明涉及活性化合物的盐和1-二甲基氨基-3-（3-甲氧基 - 苯基）-2-甲基 - 戊-3-醇和3-（3-二甲基氨基-1-乙基-1-羟基-2-甲基的酯丙基） - 苯酚，它们的制备方法，其用于制备药物用于治疗升高尿急或尿失禁，以及相应的药物和方法用于治疗增加尿急或尿失禁的用途。

8. 发明申请

WO2003032969A2 ANTI-GLYCATION AGENTS FOR PREVENTING AGE-, DIABETES-, AND SMOKING-RELATED COMPLICATIONS 审中-公开
标题翻译：用于预防年龄，糖尿病和吸烟相关并发症的抗糖化剂
公开(公告)号：WO2003032969A2
公开(公告)日：2003-04-24
申请号：PCT/CA2002/001552
申请日：2002-10-15
申请人： NATIONAL RESEARCH COUNCIL OF CANADA , YEBOAH, Faustinus , KONISHI, Yasuo , CHO, Sung, Ju , LERTVORACHON, Jittiwud , KIYOTA, Taira , TOMASZ, Popek
发明人： YEBOAH, Faustinus , KONISHI, Yasuo , CHO, Sung, Ju , LERTVORACHON, Jittiwud , KIYOTA, Taira , TOMASZ, Popek
IPC分类号： A61K31/137
CPC分类号： A61K31/47 , A61K31/00 , A61K31/04 , A61K31/137 , A61K31/195 , A61K31/222 , A61K31/345 , A61K31/352 , A61K31/4164 , A61K31/4168 , A61K31/65 , C07C219/30
摘要： The invention provides new inhibitors of protein glycation, identified from compound libraries by a high throughput screening assay. The anti-glycation agents so identified are characterized by a variety of chemical structures and are useful for the prevention or treatment of age-, diabetes-, and smoking-related complications, including neuropathy, nephropathy, ocular pathologies, or the loss of mechanical properties of collagenous tissues. Among compounds identified as having the anti-glycation activity, of special interest are epinephrine and its analogs, in particular D-epinephrine and its analogs, which are particularly useful for the prevention or treatment of age-, diabetes-, and smoking-related ocular pathologies.
摘要翻译：本发明提供了蛋白质糖化的新型抑制剂，其通过高通量筛选测定从化合物文库中鉴定。如此鉴定的抗糖化剂的特征在于各种化学结构，并且可用于预防或治疗与年龄，糖尿病和吸烟有关的并发症，包括神经病，肾病，眼病，或机械性能的丧失的胶原组织。在鉴定为具有抗糖化活性的化合物中，特别感兴趣的是肾上腺素及其类似物，特别是D-肾上腺素及其类似物，其特别用于预防或治疗年龄，糖尿病和吸烟相关的眼睛病理。

9. 发明申请

WO00027799A1 NEW ESTERS DERIVED FROM SUBSTITUTED PHENYL-CYCLOHEXYL COMPOUNDS 审中-公开
标题翻译：从取代的苯基环己基化合物衍生的新产品
公开(公告)号：WO00027799A1
公开(公告)日：2000-05-18
申请号：PCT/ES1999/000352
申请日：1999-11-04
IPC分类号： A61K31/235 , A61K31/24 , A61K31/407 , A61P25/04 , C07B53/00 , C07C213/06 , C07C219/28 , C07C219/30 , C07C231/12 , C07C233/11 , C07C269/06 , C07C271/44 , C07D207/337 , C07D487/04 , C07C219/26
CPC分类号： C07C271/44 , C07B2200/07 , C07C219/28 , C07C219/30 , C07C2601/14 , C07C2601/16 , C07D487/04
摘要： New esters derived from substituted phenyl-cyclohexyl compounds, derived from tramadol, process for obtaining such esters and use of said compounds for the fabrication of a medicament having analgesic properties. These new products having the general formula (I) have an analgesic activity which is higher than that of tramadol, a lesser toxicity and longer duration of activity.
摘要翻译：衍生自衍生自曲马多的取代的苯基 - 环己基化合物的新酯，用于获得这些酯的方法和所述化合物用于制备具有镇痛特性的药物的用途。具有通式（I）的这些新产品具有高于曲马多的镇痛活性，毒性小，活性持续时间更长。

10. 发明申请

WO1991019693A1 ESTERS AND CYCLIC DIESTERS OF 4-HYDROXY-1,3-BENZENEDIMETHANOL AND COMPOSITIONS AND METHODS EMPLOYING SUCH COMPOUNDS 审中-公开
标题翻译： 4-羟基-1,3-苯二甲酰胺及其组合物的酯和循环系统及其使用方法
公开(公告)号：WO1991019693A1
公开(公告)日：1991-12-26
申请号：PCT/US1991003966
申请日：1991-06-11
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , BLYTHIN, David, J. , SHUE, Ho-Jane , GANGULY, Ashit
IPC分类号： C07C219/30
CPC分类号： C07D491/04 , C07C217/46 , C07C217/70 , C07C219/30 , C07D321/00 , C07D495/04
摘要： Novel compounds selected from the group consisting of: (A) compounds of formula I(1), wherein: one of R and R represents the group (a) and the other represents hydrogen or R CO-; R represents C1 to C6-alkyl or the group -(CH2)n-Z-(CH2)m-Ar; Z represents O, S or -CH2-; n represents an integer of 1 to 8; m represents zero or an integer of 1 to 8; R is C1 to C10 alkyl, C3 to C8 cycloalkyl, aryl, heteroaryl, -N(R R ), or R O-; R , R , R , and R are each independently selected from hydrogen, C1 to C6 alkyl and Ar ; R and R are each independently C1-C8 alkyl; Ar and Ar are each independently selected from the group consisting of phenyl or substituted phenyl, (B) compounds of formula I(2), wherein: R represents C1 to C6-alkyl or the group -(CH2)n-Z-(CH2)m-Ar ; Ar is selected from the group consisting of phenyl, substituted phenyl, or phenyl optionally substituted by two adjacent groups which together form an additional benzenoid ring; ring Q represents one of the rings Q1, Q2, Q3 or Q4, and pharmaceutically acceptable acid addition salts thereof are described. These compounds possess favorable properties for the treatment of asthma and all types of chronic, obstructionary bronchopulmonary diseases.
摘要翻译：选自以下的新型化合物：（A）式I（1）化合物，其中：R 1和R 2之一表示（a）基团，另一个表示氢或R 7 CO - ; R 5表示C 1 -C 6烷基或基团 - （CH 2）n-Z-（CH 2）m -Ar; Z表示O，S或-CH 2 - ; n表示1〜8的整数， m表示0或1〜8的整数， R 7是C 1至C 10烷基，C 3至C 8环烷基，芳基，杂芳基，-N（R 9 R 10）或R 11 O-; R 3，R 4，R 9和R 10各自独立地选自氢，C 1至C 6烷基和Ar 1; R 6和R 11各自独立地为C 1 -C 8烷基; Ar和Ar 1各自独立地选自苯基或取代的苯基，（B）式I（2）的化合物，其中：R 5a表示C1至C6-烷基或基团 - （CH2） NZ-（CH 2）M-的Ar <2>; Ar 2选自苯基，取代的苯基或任选被两个相邻基团取代的苯基，它们一起形成另外的苯环; 环Q表示环Q1，Q2，Q3或Q4中的一个，并且其药学上可接受的酸加成盐被描述。这些化合物具有治疗哮喘和所有类型的慢性阻塞性支气管肺疾病的有利性质。

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