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111. 发明申请

WO2007039470A1 4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 审中-公开
标题翻译： 4-苯基-6-取代的嘧啶-2-羰基衍生物
公开(公告)号：WO2007039470A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066562
申请日：2006-09-21
申请人： N.V. ORGANON , RANKOVIC, Zoran , CAI, Jiaqiang
发明人： RANKOVIC, Zoran , CAI, Jiaqiang
IPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/36 , C07D403/04 , C07D401/04 , C07D403/12 , C07D401/12 , A61K31/505 , A61K31/506 , A61P19/10 , A61P9/10
CPC分类号： C07D239/34 , C07D239/36 , C07D239/38 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12
摘要： The invention relates to 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula (I) wherein R represents 1-3 optional substituents independently selected from (C 1-4 )- alkyl (optionally substituted with one or more halogens), (C 1-4 )alkyloxy (optionally substituted with one or more halogens) and halogen; X is NR 1 , O or S; R 1 is H or (C 1-4 )alkyl; Y is (C 1-4 )alkyl, benzyl or (C 2-6 )alkyl, substituted with a group selected from OH, (C 1-4 )alkyloxy, NR 2 R 3 , a 4-8 membered saturated heterocyclic ring comprising 1 or 2 heteroatoms selected from O, S and NR 4 , and a 5 or 6-membered aromatic heterocyclic group comprising 1-4 N atoms; or R 1 and Y form together with the nitrogen to which they are bonded a 5-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S, NR 4 and NO; the ring being optionally substituted with NR 2 R 3 or with 1 to 4 (C 1-3 )alkyl groups; R 2 and R 3 are independently H or (C 1-4 )alkyl; or R 2 and R 3 form together with the nitrogen to which they are bonded a 4-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S and NR 4 ; R 4 is H, (C 1-6 )alkyl,(C 3-6 ) cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl, (C 1-4 )alkyloxy-(C 1-4 )alkyl, benzyl, amido- (C 1-4 )alkyl, (C 1-6 )alkyloxycarbonyl(C 1-4 )alkyl or carboxy(C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the preparation of a medicament for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.
摘要翻译：本发明涉及具有式（I）的4-苯基-6-取代 - 嘧啶-2-甲腈衍生物，其中R表示1-3个任选的取代基，其独立地选自（C 1-4 - ） - 烷基（任选被一个或多个卤素取代），（C 1-4烷基）烷氧基（任选被一个或多个卤素取代）和卤素; X是NR 1，O或S; R 1是H或（C 1-4烷基）烷基; Y是（C 1-4 - ）烷基，苄基或被选自OH，（C 1-4）烷基的（C 1-6）烷基取代的（C 1-6 - NR 3 R 3，含有1或2个选自O，S和NR 4的杂原子的4-8元饱和杂环和含有1-4个N原子的5或6元芳族杂环基; 或R 1和Y与它们所键合的氮一起形成5-8元饱和杂环，任选地包含另外的选自O，S，NR 4的杂原子 >和NO; 该环任选地被NR 2 R 3 3或与1至4个（C 1-3 - ）烷基取代; R 2和R 3独立地是H或（C 1-4烷基）烷基; 或R 2和R 3 3与它们所连接的氮一起形成4-8元饱和杂环，任选地包含另外的选自O，S的杂原子和 NR _{4 ; R 4是H，（C 1-6）烷基，（C 3-6）环烷基，（C 3-6）（C 1-4）烷基，（C 1-4烷基）烷氧基 - （C 1-4 - ）烷基，苄基，酰氨基 - （C 1-4 - ）烷基，（C 1-6 - ）烷氧基羰基（C 1-4 - ）烷基或羧基（C _{1-4 ）烷基; 或其药学上可接受的盐，包含其的药物组合物，以及这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物在制备用于治疗组织蛋白酶K和组织蛋白酶的药物中的用途 S相关疾病，例如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛。}}

112. 发明申请

WO2006117368A1 4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES THE TREATMENT OF INFERTILITY 审中-公开
标题翻译： 4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物治疗感染
公开(公告)号：WO2006117368A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061972
申请日：2006-05-02
申请人： N.V. ORGANON , GRIMA POVEDA, Pedro, Manuel , KARSTENS, Willem, Frederik, Johan , TIMMERS, Cornelis, Marius
发明人： GRIMA POVEDA, Pedro, Manuel , KARSTENS, Willem, Frederik, Johan , TIMMERS, Cornelis, Marius
IPC分类号： A61K31/47 , C07D215/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/4709 , A61P5/24
CPC分类号： C07D401/12 , C07D215/20 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R 2 , R 3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R 4 is phenyl or (2-5C)- heteroaryl, both substituted with R 7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l-4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
摘要翻译：本发明涉及式I式I的4-苯基-5-氧代-1,2,4,5,6,7,8-六氢喹啉衍生物或其药学上可接受的盐，其中R 1〜是（1-6C）烷基，（2-6C）烯基或（2-6C）芳基; （2-4C）链烯基，（2-4C） - 炔基，（1-4C）环烷基，（1-4C）烷基，（1-4C）（3-4C）烯氧基或（3-4C）炔氧基; R 4是苯基或（2-5C） - 杂芳基，两者均被R 7取代，并且任选地在（杂）芳环上取代有一个或多个选自羟基的取代基，氨基，卤素，硝基，三氟甲基，氰基，（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基和（二）（1-4C）烷基氨基。本发明还涉及包含所述衍生物的药物组合物，以及这些4-苯基-5-氧代-1,2,5,6,7,8-六氢 - 喹啉衍生物在治疗中的用途，更具体地说，治疗不育症

113. 发明申请

WO2006117023A1 DIHYDROPYRIDINE DERIVATIVES 审中-公开
标题翻译：二氢吡啶衍生物
公开(公告)号：WO2006117023A1
公开(公告)日：2006-11-09
申请号：PCT/EP2005/052042
申请日：2005-05-04
申请人： N.V. ORGANON , VAN STRATEN, Nicole, Corine, Renee , GERRITSMA, Gerritdina, Geziena , VAN DER VEEN, Lars, Anders
发明人： VAN STRATEN, Nicole, Corine, Renee , GERRITSMA, Gerritdina, Geziena , VAN DER VEEN, Lars, Anders
IPC分类号： C07D215/54 , A61K31/47 , A61P5/06
CPC分类号： C07D215/54
摘要： The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, (1-5C)heteroaryl R 2 , R 3 are independently (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (24C)alkenyloxy, (2-4C)alkynyloxy, halogen X is SO 2 , CH 2 , C(O) or X is absent R 4 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (3-6C)cycloalkenyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl, (2-6C)heterocycloalkyl(14C)alkyl, (6-1 OC)aryl, (6-10C)aryl(1-4C)alkyl, (1-9C)heteroaryl or (1-9C)heteroaryl(14C)alkyl. The compounds are useful for the treatment of fertility disorders.
摘要翻译：本发明涉及具有通式（I）的二氢吡啶衍生物或其药学上可接受的盐，其中R 1为（1-6C）烷基，（2-6C）烯基，（2-6C）炔基，苯基，（1-5C）杂芳基R 2，R 3，R 3独立地为（1-4C）烷基，（2-4C）烯基，（2-4C）炔基，（1-4C）烷氧基，（24C）烯氧基，（2-4C）炔氧基，卤素X是SO 2，CH 2，C（O）或 X不存在R 4是（1-6C）烷基，（2-6C）烯基，（2-6C）炔基，（3-6C）环烷基，（3-6C）环烯基，（3 -6C）环烷基（1-4C）烷基，（2-6C）杂环烷基，（2-6C）杂环烷基（14C）烷基，（6-1C）芳基，（6-10C）芳基（1-4C）烷基，（1-9C）杂芳基或（1-9C）杂芳基（14C）烷基。该化合物可用于治疗生育障碍。

114. 发明申请

WO2006082184A3 CONJUGATES OF A POLYPEPTIDE AND A PENTASACCHARIDE 审中-公开
公开(公告)号：WO2006082184A3
公开(公告)日：2006-08-10
申请号：PCT/EP2006/050551
申请日：2006-01-31
申请人： N.V. ORGANON , BOS, Ebo, Sybren , DE KORT, Martin , SMIT, Meertinus, Jan , VAN BOECKEL, Constant, Adriaan, Anton
发明人： BOS, Ebo, Sybren , DE KORT, Martin , SMIT, Meertinus, Jan , VAN BOECKEL, Constant, Adriaan, Anton
IPC分类号： A61K47/48
摘要： The present invention relates to conjugates of a polypeptide and an oligosaccharide, wherein the polypeptide is conjugated to at least one oligosaccharide-spacer residue, the oligosaccharide being a synthetic sulfated oligosaccharide comprising 4-18 monosaccharide units and per se having affinity to antithrombin III and the spacer being a bond or an essentially pharmacologically inactive flexible linking residue, or a pharmaceutically acceptable salt thereof. The conjugates of the invention have improved pharmacokinetic properties when compared to the original polypeptides (i.e. the corresponding non-conjugated polypeptides per se).

115. 发明申请

WO2011061318A1 HETEROCYLIC COMPOUNDS AS ANTAGONISTS OF THE OREXIN RECEPTORS 审中-公开
标题翻译：杂环化合物作为OREXIN受体的拮抗剂
公开(公告)号：WO2011061318A1
公开(公告)日：2011-05-26
申请号：PCT/EP2010/067904
申请日：2010-11-22
申请人： N.V. ORGANON , BINGHAM, Matilda Jane , DUNBAR, Neil Andrew , HUGGETT, Margaret Jean , WISHART, Grant
发明人： BINGHAM, Matilda Jane , DUNBAR, Neil Andrew , HUGGETT, Margaret Jean , WISHART, Grant
IPC分类号： C07D217/26 , C07D401/06 , C07D471/04 , A61K31/4375 , A61K31/4725 , A61K31/55
CPC分类号： C07D217/26 , A61K31/4375 , A61K31/4725 , A61K31/55 , C07D401/06 , C07D471/04
摘要： The present invention relates to a heterocyclic derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.
摘要翻译：本发明涉及式（I）的杂环衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含所述杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防受食欲调节如睡眠障碍影响的疾病或疾病。

116. 发明申请

WO2011051490A2 HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO2011051490A2
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066584
申请日：2010-11-02
申请人： N.V. ORGANON , ADAM, Julia , GILLESPIE, Jonathan , LAATS, Steven , MACLEAN, John Kinnaird Ferguson , McARTHUR, Duncan Robert
发明人： ADAM, Julia , GILLESPIE, Jonathan , LAATS, Steven , MACLEAN, John Kinnaird Ferguson , McARTHUR, Duncan Robert
IPC分类号： C07D401/10
CPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10
摘要： The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
摘要翻译：本发明涉及式（I）的杂环衍生物或其药学上可接受的盐或溶剂化物，其中变量如说明书中所定义。本发明进一步涉及包含所述杂环衍生物的药物组合物，并涉及它们在治疗中的应用，例如治疗或预防由谷氨酸功能障碍如精神分裂症和广泛性焦虑症所介导的障碍。

117. 发明申请

WO2011009922A1 APPARATUS AND METHOD OF PRESERVING MUCOSA 审中-公开
标题翻译：装置和保存MUCOSA的方法
公开(公告)号：WO2011009922A1
公开(公告)日：2011-01-27
申请号：PCT/EP2010/060657
申请日：2010-07-22
申请人： N.V. ORGANON , GIJTENBEEK, Adolph Bartholomeus , VAN TUIJN, Harry , PLOEGMAKERS, Marinus Johannes Gerardus Maria
发明人： GIJTENBEEK, Adolph Bartholomeus , VAN TUIJN, Harry , PLOEGMAKERS, Marinus Johannes Gerardus Maria
IPC分类号： A22C5/00 , A22B7/00
CPC分类号： A22C5/00 , A22B7/008 , A23V2002/00 , B01F7/021 , B01F7/04 , B01F15/00772 , B01F15/00785 , A23V2200/10
摘要： A mixing apparatus (1) for mixing slaughter offal with a preservative agent, the apparatus comprising an offal collection tank (3) with a bottom (4) provided w ith a discharge opening (5) connectable to a closable discharge, an agitator (8) extending into the offal collection tank, and a pump unit (9) operatively connectable to the discharge, wherein the apparatus further comprises a preservative reservoir (7) mounted on top of the collection tank (3). A collection and preservation system is provided, wherein the addition of preservation agent can be strictly controlled, can easily and quickly be installed and connected when it is to be used. After use, the system is easily removed and cleaned.
摘要翻译：一种用于将屠宰内脏与防腐剂混合的混合装置（1），该装置包括具有底部（4）的内脏收集罐（3），所述底部收集罐具有可连接到可关闭排放物的排出口（5），搅拌器）和可操作地连接到所述排放口的泵单元（9），其中所述装置还包括安装在所述收集罐（3）的顶部上的防腐剂储存器（7）。提供收集和保存系统，其中可以严格控制添加保存剂，并且可以在使用时容易且快速地安装和连接。使用后，系统很容易拆卸和清洁。

118. 发明申请

WO2010100056A2 ANTIBODIES AGAINST A PROLIFERATING INDUCING LIGAND (APRIL) 审中-公开
标题翻译：抗增生诱导配偶（APRIL）抗体
公开(公告)号：WO2010100056A2
公开(公告)日：2010-09-10
申请号：PCT/EP2010/052254
申请日：2010-02-23
申请人： STICHTING TOP INSTITUTE PHARMA , N.V. ORGANON , VRIJE UNIVERSITEIT MEDISCH CENTRUM , ACADEMISCH MEDISCH CENTRUM , RIJKSUNIVERSITEIT GRONINGEN , ACADEMISCH ZIEKENHUIS GRONINGEN , PEPSCAN HOLDING N.V. , MEDEMA, Jan, Paul , EENENNAAM, VAN, Hans , GUADAGNOLI, Marco , KIMBERLEY, Fiona, Clare , PHAN, Uyen, Truong
发明人： MEDEMA, Jan, Paul , EENENNAAM, VAN, Hans , GUADAGNOLI, Marco , KIMBERLEY, Fiona, Clare , PHAN, Uyen, Truong
IPC分类号： A61K39/395
CPC分类号： C07K16/2878 , A61K2039/505 , C07K16/241 , C07K16/2875 , C07K2317/34 , C07K2317/73 , C07K2317/76 , C07K2317/92 , C07K2319/30 , C07K2319/32 , G01N33/6863
摘要： The present invention relates to a binding compound which binds to human APRIL. More specifically the invention provides, compositions of anti-APRIL specific antibodies and methods to use such antibodies in modulating the biological activity APRIL, particularly in inflammatory diseases, inhibition of cell proliferation and cancer.
摘要翻译：本发明涉及结合人APRIL的结合化合物。更具体地，本发明提供了抗APRIL特异性抗体的组合物和使用这种抗体调节生物活性APRIL，特别是炎性疾病，抑制细胞增殖和癌症的方法。

119. 发明申请

WO2010091009A1 ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLE-3-CARBOXAMIDE衍生物
公开(公告)号：WO2010091009A1
公开(公告)日：2010-08-12
申请号：PCT/US2010/022869
申请日：2010-02-02
申请人： N.V. ORGANON , PHARMACOPEIA, LLC , PALIN, Ronald , RATCLIFFE, Paul, David , KULTGEN, Steven, G. , HO, Koc-Kan , ROUGHTON, Andrew, Laird , OHLMEYER, Michael
发明人： PALIN, Ronald , RATCLIFFE, Paul, David , KULTGEN, Steven, G. , HO, Koc-Kan , ROUGHTON, Andrew, Laird , OHLMEYER, Michael
IPC分类号： C07D261/18 , C07D413/06 , C07D413/12 , A61P25/00 , A61K31/42 , A61K31/422 , A61K31/45 , A61K31/4468 , A61K31/4453 , A61K31/4439 , A61K31/5377
CPC分类号： C07D261/18 , C07D413/06 , C07D413/12
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
摘要翻译：本发明涉及具有通式I的异恶唑-3-甲酰胺衍生物或其药学上可接受的盐，其涉及包含该异构体的药物组合物，以及所述异恶唑-3-甲酰胺衍生物用于治疗TRPV1介导的急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎性疼痛，呼吸系统疾病和下尿路疾病。

120. 发明申请

WO2010063721A1 1- (BIPHENYL-4-YLMETHYL) IMIDAZOLIDINE-2, 4-DIONE DERIVATIVES AND THEIR USE AS CB2 RECEPTOR AGONISTS 审中-公开
标题翻译： 1-（二苯基-4-甲基）咪唑烷-2,4-二酮衍生物及其作为CB2受体激动剂的用途
公开(公告)号：WO2010063721A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/066156
申请日：2009-12-01
申请人： N.V. ORGANON , VAN DER STELT, Marcelis , CALS, Joseph, Maria, Gerardus, Barbara
发明人： VAN DER STELT, Marcelis , CALS, Joseph, Maria, Gerardus, Barbara
IPC分类号： C07D233/74 , C07D401/10 , A61K31/454 , A61K31/5375 , A61K31/54 , A61P25/04
CPC分类号： C07D233/74 , C07D401/10
摘要： The invention relates to A 1 -(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula (I) wherein R 1 is H, (C 1-6 )alkyl (optionally substituted with oxo, OR 4 , COOR 5 , halogen or CN), (C 2-6 )alkenyl, (C 2-6 )alkynyl, (C 3-6 )cycloalkyl or (C 3-6 )cycloalkyl(C 1-3 )alkyl; R 2 and R 2 ' are independently H or (C 1-3 )alkyl; or R 2 and R 2 ' form together with the carbon atom to which they are bound a (C 3-5 )cycloalkyl group;R 3 represents H or 1 to 4 F substituents; Y represents Formula (II) or NR 8 R 9 ; X represents CHR 6 , CF 2 , O, S, SO or SO 2 ; R 4 and R 5 are (C 1-6 )alkyl; R 6 is H, OR 7 or CN; R 7 is (C 1-3 )alkyl; R 8 is (C 5-7 )cycloalkyl comprising a heteroatom selected from O, S, SO and SO 2 ; R 9 is H or (C 1-4 )alkyl; o and m represent the ortho or meta position of the substituent Y-CH 2 ; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1 -(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives as CB2 receptor agonists in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式（I）的通式（I）的1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物，其中R 1为H，（C 1-6）烷基（任选被氧代取代，OR 4，COOR 5，卤素或CN），（C2-6）烯基，（C2-6）炔基，（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基; R2和R2'独立地为H或（C1-3）烷基; 或R 2和R 2'与它们所连接的碳原子一起形成（C 3-5）环烷基; R 3表示H或1至4 F取代基; Y表示式（II）或NR8R9; X表示CHR6，CF2，O，S，SO或SO2; R4和R5是（C1-6）烷基; R6是H，OR7或CN; R7是（C1-3）烷基; R8是包含选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; o和m表示取代基Y-CH 2的邻位或间位; 或其药学上可接受的盐; 以及所述1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物作为CB 2受体激动剂用于治疗疼痛的用途，例如手术前疼痛，慢性疼痛，神经性疼痛，癌症与多发性硬化相关的疼痛和疼痛和痉挛状态。

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