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1. 发明申请

US20150320044A1 (HETERO) ARYLACRYLAMIDES FOR THE CONTROL OF ECTOPARASITES 有权
标题翻译：（HETERO）用于控制ECTOPARASITES的ARYLACRYLAMIDES
公开(公告)号：US20150320044A1
公开(公告)日：2015-11-12
申请号：US14649268
申请日：2013-12-20
申请人： Emilie DUPONT , Noëlle GAUVRY , Steve NANCHEN , Chikako OGAWA , Chouaib TAHTAOUI , Novartis Tiergesundheit AG
发明人： Emilie Dupont , Noelle Gauvry , Steve Nanchen , Chikako Ogawa , Chouaib Tahtaoui
IPC分类号： A01N37/34 , A01N37/18 , C07C255/48 , C07D213/40 , A01N43/40 , C07D307/52 , A01N43/08 , A01N43/20 , C07D305/06 , C07D331/04 , C07D309/14 , A01N43/16 , C07D213/75 , A01N43/44 , A01N43/36 , A01N43/80 , C07D207/273 , C07D205/04 , C07D261/04 , C07C233/66
CPC分类号： A01N37/34 , A01N37/18 , A01N37/30 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/20 , A01N43/36 , A01N43/40 , A01N43/42 , A01N43/44 , A01N43/80 , A01N47/16 , C07C233/65 , C07C233/66 , C07C233/69 , C07C237/22 , C07C255/29 , C07C255/46 , C07C255/48 , C07C327/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D205/04 , C07D207/273 , C07D213/40 , C07D213/75 , C07D215/48 , C07D261/04 , C07D295/192 , C07D305/06 , C07D305/08 , C07D307/52 , C07D307/79 , C07D309/14 , C07D331/04 , C07D333/38 , C07D333/72 , C07D409/12
摘要： The present invention relates to new compounds of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
摘要翻译：本发明涉及新的式（I）化合物，其中变量具有如权利要求中所示的含义; 以自由形式和盐形式; 和任选的其对映体和几何异构体。式（I）化合物可用于控制脊椎动物内和寄生虫上的寄生虫，特别是外寄生虫。

2. 发明申请

US20150157601A1 SUBSTITUTED 2-[2-(PHENYL) ETHYLAMINO] ALKANEAMIDE DERIVATIVES AND THEIR USE AS SODIUM AND/OR CALCIUM CHANNEL MODULATORS 有权
公开(公告)号：US20150157601A1
公开(公告)日：2015-06-11
申请号：US14615227
申请日：2015-02-05
申请人： NEWRON PHARMACEUTICALS S.P.A.
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/381 , A61K31/165
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R1, R2, R3, R′3 R4, R5, R6, R7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

3. 发明授权

US09051240B2 Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators 有权
标题翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物及其作为钠和/或钙通道调节剂的用途
公开(公告)号：US09051240B2
公开(公告)日：2015-06-09
申请号：US13794555
申请日：2013-03-11
申请人： Newron Pharmaceuticals S.P.A.
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/165 , C07C237/08 , C07C233/05 , C07C233/65 , A61P25/00 , C07C237/20 , C07C317/28 , C07C323/25 , C07C327/42 , C07D295/182 , A61K31/381 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07D207/16 , C07D333/20 , C07C321/26 , C07C327/44
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
摘要翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物，其药学上可接受的盐和含有它们的药物组合物可用作用于预防，减轻和治愈其中上述机制发挥病理作用的病症的钠和/或钙通道调节剂。这些化合物可能特别可用于预防，减轻和治愈例如神经，认知，精神，炎症，泌尿生殖和胃肠道疾病。

4. 发明申请

US20130289083A1 IDO Inhibitors 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：US20130289083A1
公开(公告)日：2013-10-31
申请号：US13801268
申请日：2013-03-13
申请人： NewLink Genetics Corporation
发明人： Mario Mautino , Firoz Jaipuri , Agnieszka Marcinowicz-Flick , Tanay Kesharwani , Jesse Waldo
IPC分类号： C07D333/56 , C07D307/80 , C07D277/64
CPC分类号： C07D333/56 , A61K31/138 , A61K31/506 , C07C259/06 , C07C311/48 , C07C327/44 , C07C327/48 , C07C333/20 , C07D209/14 , C07D209/18 , C07D213/40 , C07D215/26 , C07D253/07 , C07D261/20 , C07D263/22 , C07D277/36 , C07D277/64 , C07D279/06 , C07D307/80 , C07D307/81 , C07D333/58 , C07D333/60 , C07D335/06 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12 , Y02A50/409 , Y02A50/465
摘要： Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunsupression associated with an infectious disease, e.g., HIV-1 infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
摘要翻译：目前提供的是（a）调节吲哚胺2,3-双加氧酶的活性的方法，包括使吲哚胺2,3-双加氧酶与调节有效量的化合物接触，如本文所述的一个方面所述; （b）在有需要的受试者中治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （c）治疗受抑于吲哚胺-2,3-双加氧酶的酶活性的医学病症，包括给予有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （d）增强抗癌治疗的有效性，包括给予本文所述方面之一所述的抗癌剂和化合物; （e）治疗与癌症相关的肿瘤特异性免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; 和（f）治疗与感染性疾病例如HIV-1感染相关的免疫抑制，包括给予有效的吲哚胺2,3-双加氧酶抑制量的化合物，如本文所述方面之一所述。

5. 发明申请

US20130231478A1 Novel Intermediate for Preparing Tapentadol or Analogues Thereof 有权
标题翻译：制备他喷他多或其类似物的新型中间体
公开(公告)号：US20130231478A1
公开(公告)日：2013-09-05
申请号：US13884810
申请日：2011-07-29
申请人： Ziao Xu , Yuanhai Zhao , Degang Li , Xiaoxiang Li
发明人： Ziao Xu , Yuanhai Zhao , Degang Li , Xiaoxiang Li
IPC分类号： C07D295/192 , C07C69/734 , C07C327/28 , C07C69/732 , C07C327/44 , C07C235/34 , C07C51/60 , C07C255/36 , C07C253/14 , C07D211/16 , C07C67/08 , C07C231/02 , C07C233/11 , C07C237/20 , C07C255/37 , C07C213/02 , C07C59/48
CPC分类号： C07D295/192 , C07C41/22 , C07C41/26 , C07C51/367 , C07C51/60 , C07C59/48 , C07C59/64 , C07C67/08 , C07C69/732 , C07C69/734 , C07C213/00 , C07C213/02 , C07C213/10 , C07C231/02 , C07C233/11 , C07C235/34 , C07C237/20 , C07C253/14 , C07C255/36 , C07C255/37 , C07C327/22 , C07C327/28 , C07C327/44 , C07D211/16 , C07D295/185 , C07C59/60 , C07C43/23 , C07C43/225 , C07C215/54
摘要： The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
摘要翻译：本发明公开了一种制备他喷他多及其类似物的新型中间体，其结构式如式I或II所示，其定义为说明书。本发明进一步公开了一种制备新型中间体的方法以及用于制备他喷他多和其类似物的中间体。本发明可显着提高他喷他多的产品产量和质量，降低生产成本，简化生产工艺。制备工艺环保，更适合工业生产要求。

6. 发明申请

US20110105618A1 NOVEL MODULATORS OF PROTEIN KINASE SIGNALING 有权
标题翻译：蛋白激酶信号的新型调节剂
公开(公告)号：US20110105618A1
公开(公告)日：2011-05-05
申请号：US12995669
申请日：2009-06-07
申请人： Hadas Reuveni , Alexander Levitzki , Revital Sasson , Andre C. B. Lucassen
发明人： Hadas Reuveni , Alexander Levitzki , Revital Sasson , Andre C. B. Lucassen
IPC分类号： A61K31/165 , C07C327/12 , C12N5/00 , A61P35/00
CPC分类号： C07D277/36 , C07C327/44
摘要： The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.
摘要翻译：本发明提供了作为蛋白激酶（PK）和受体激酶（RK）信号转导调节剂的新的酪氨酸磷酸化酶衍生物。本发明进一步提供其制备方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物的方法，特别是用于预防和治疗PK和RK相关疾病如代谢，炎症，纤维化和细胞增殖性疾病的化学治疗剂，特别是癌症。

7. 发明申请

US20110053941A1 IDO Inhibitors 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：US20110053941A1
公开(公告)日：2011-03-03
申请号：US12744860
申请日：2008-12-01
申请人： Mario Mautino , Firoz Jaipuri , Agnieszka Marcinowicz-Flick , Tanay Kesharwani , Jesse Waldo , Steven James Collier
发明人： Mario Mautino , Firoz Jaipuri , Agnieszka Marcinowicz-Flick , Tanay Kesharwani , Jesse Waldo , Steven James Collier
IPC分类号： A61K31/5375 , A61P37/00 , A61K31/135 , C07D209/14 , A61K31/4045 , A61K31/404 , C07D403/12 , C07D401/12 , A61K31/4709 , C07D405/12 , C07D413/12 , A61K31/423 , C07C333/04 , A61K31/27 , C07D213/53 , A61K31/4406 , A61K31/4402 , A61K31/36 , A61K31/381 , A61K31/47 , A61K31/357 , A61K31/428 , A61K31/505
CPC分类号： C07D333/56 , A61K31/138 , A61K31/506 , C07C259/06 , C07C311/48 , C07C327/44 , C07C327/48 , C07C333/20 , C07D209/14 , C07D209/18 , C07D213/40 , C07D215/26 , C07D253/07 , C07D261/20 , C07D263/22 , C07D277/36 , C07D277/64 , C07D279/06 , C07D307/80 , C07D307/81 , C07D333/58 , C07D333/60 , C07D335/06 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12 , Y02A50/409 , Y02A50/465
摘要： Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
摘要翻译：目前提供的是（a）调节吲哚胺2,3-双加氧酶的活性的方法，包括使吲哚胺2,3-双加氧酶与调节有效量的化合物的接触，如本文所述的一个方面所述; （b）在有需要的受试者中治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （c）治疗受抑于吲哚胺-2,3-双加氧酶的酶活性的医学病症，包括给予有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （d）增强抗癌治疗的有效性，包括给予本文所述方面之一所述的抗癌剂和化合物; （e）治疗与癌症相关的肿瘤特异性免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （f）治疗与感染性疾病例如HIV-1感染相关的免疫抑制，包括给予有效的吲哚胺2,3-双加氧酶抑制量的化合物，如本文所述方面之一所述。

8. 发明申请

US20060264480A1 Novel thiocarbamic acid derivatives and the pharmaceutical compositions containing the same 审中-公开
公开(公告)号：US20060264480A1
公开(公告)日：2006-11-23
申请号：US11373828
申请日：2006-03-13
申请人： Young Suh , Uh Oh , Hee Kim , Jee Lee , Hyeung Park , Young Park , Jung Yi
发明人： Young Suh , Uh Oh , Hee Kim , Jee Lee , Hyeung Park , Young Park , Jung Yi
IPC分类号： A61K31/44 , A61K31/4172 , A61K31/405 , A61K31/277 , C07D213/57 , C07D213/53 , C07D213/00 , C07D233/61
CPC分类号： C07D333/20 , A61K31/165 , A61K31/17 , A61K31/175 , C07C271/12 , C07C311/08 , C07C327/44 , C07C333/04 , C07C333/08 , C07C335/12 , C07D209/08 , C07D213/40 , C07D213/73 , C07D213/75 , C07D213/79
摘要： The present invention relates to an antagonist against vanilloid receptor and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fevescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

9. 发明授权

US07105545B2 N-p-propargyloxyphenethyl-thioacetic acid amides 失效
标题翻译： N-对 - 丙酰氧基苯乙基 - 硫代乙酰胺
公开(公告)号：US07105545B2
公开(公告)日：2006-09-12
申请号：US10472577
申请日：2002-04-02
申请人： Walter Kunz , Clemens Lamberth , Fredrik Cederbaum , Martin Zeller
发明人： Walter Kunz , Clemens Lamberth , Fredrik Cederbaum , Martin Zeller
IPC分类号： A01N43/40 , A01N43/06 , A01N43/08 , A01N37/44 , A01N37/18
CPC分类号： C07C327/44 , A01N37/36 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/30 , A01N43/32 , A01N43/40 , A01N43/54
摘要： The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkynylsulfonyl or a group —O—CO—R11, —O—CO—O—R11 or —O—CO—CO—O—R11 wherein R11 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi
摘要翻译：本发明涉及通式（I）的N-炔丙氧基 - 苯乙基硫代乙酰胺衍生物，其包括其旋光异构体和这些异构体的混合物，其中R 1是氢，烷基，环烷基或任选取代的芳基，R 2和R 3各自独立地是氢或烷基，R 4是烷基，烯基或炔基，R 5， R 6，R 7，R 8和R 8各自独立地为氢或烷基，R 9为氢，任选取代的烷基，任选取代的烯基或任选取代的炔基，R 10是任选取代的芳基或任选取代的杂芳基，Z是羟基，任选取代的芳氧基，任选取代的烷氧基，任选取代的炔氧基，任选地取代的芳硫基，任选取代的烷硫基，任选取代的炔硫基，任选取代的烷基亚磺酰基，任选取代的烯基亚磺酰基，任选的取代的炔基亚磺酰基，任选取代的烷基磺酰基，任选取代的链烯基磺酰基，任选取代的炔基磺酰基或基团-O-CO-R 11，-O-CO-OR 11或-O- 其中R 11是氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂芳基。这些化合物具有有用的植物保护性质，并且可有利地用于农业实践中以控制或防止由植物病原微生物特别是真菌侵染植物

10. 发明授权

US06890932B2 Anthranilic acid derivative 失效
标题翻译：邻氨基苯甲酸衍生物
公开(公告)号：US06890932B2
公开(公告)日：2005-05-10
申请号：US10355125
申请日：2003-01-31
申请人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
发明人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
IPC分类号： C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07D207/08 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/092 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12 , A61K31/435 , A01N43/40 , C07D213/00 , C07D213/63
CPC分类号： C07D207/08 , C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/28 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/088 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12
摘要： The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
摘要翻译：本发明涉及由下式（1）或下式（2）表示的邻氨基苯甲酸衍生物或其药理学上允许的盐或溶剂合物。

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