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1. 发明申请

WO2007039389A1 ISOXAZOLO DERIVATIVES AS GABA A ALPHA5 INVERSE AGONISTS 审中-公开
标题翻译： ISOXAZOLO衍生物作为GABA ALPHA5反相激动剂
公开(公告)号：WO2007039389A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066094
申请日：2006-09-07
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , HENNER, Knust , NETTEKOVEN, Matthias , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , HENNER, Knust , NETTEKOVEN, Matthias , THOMAS, Andrew
IPC分类号： C07D413/14 , C07D413/06 , C07D451/06 , A61P25/28 , A61K31/42
CPC分类号： C07D413/14 , C07D413/06 , C07D451/06
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula (I) wherein R 1 is hydrogen, halogen, lower alkoxy, phenyloxy or benzyloxy; R 2 is lower alkyl, (CH2)n-O-lower alkyl or phenyl; R 3 is hydrogen or lower alkyl; R 4 /R 5 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkynyl or -(CHR)n-aryl, unsubstituted or substituted by halogen, lower alkyl or lower alkoxy, -(CH 2 ) n -non aromatic heterocyclic ring, unsubstituted or substituted by one or two lower alkyl groups, -(CH 2 ) n -aromatic heterocyclic rings -(CR 2 ) n -cycloalkyl, unsubstituted or substituted by one to three substituents, selected from the group consisting of hydroxy or lower alkyl, -(CHR) n -O-lower alkyl, -(CR 2 ) n -OH, -(CHR) n -NR’R", or R 4 /R 5 form together with the N-atom to which they are attached the ring - 8-aza-bicyclo[3.2.1] octane, substituted by hydroxy, or - 3,4-dihydro- l H -isoquinoline, or - a non aromatic heterocyclic ring, unsubstituted or substituted by one or two substituents, selected from the group consisting of C(O)O-lower alkyl, lower alkyl, lower alkyl substituted by halogen, cycloalkyl, hydroxy, halogen, N(R)C(O)-lower alkyl, -(CΗ 2 ) n -O-lower alkyl, or by an aromatic heterocyclic ring; R is hydrogen, hydroxy, or lower alkyl, wherein R may be the same or different in case of R 2 ; R’/R" are independently from each other hydrogen or lower alkyl; n is O, 1, 2, 3 or 4; m is 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA Aα5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）的芳基 - 异恶唑-4-羰基 - 吡咯-2-羧酸酰胺衍生物，其中R 1是氢，卤素，低级烷氧基，苯氧基或苄氧基; R 2是低级烷基，（CH 2）n -O-低级烷基或苯基; R 3是氢或低级烷基; R 4和R 5彼此独立地为氢，低级烷基，被卤素取代的低级烷基，低级炔基或 - （CHR）n - 芳基，未取代或被卤素，低级烷基或低级烷氧基， - 未被取代或被一个或两个低级烷基取代的 - （CH 2 N 2）n - 芳族杂环， - （CH

2. 发明申请

WO2007042420A1 ISOXAZOLE DERIVATIVES 审中-公开
标题翻译：异佛唑衍生物
公开(公告)号：WO2007042420A1
公开(公告)日：2007-04-19
申请号：PCT/EP2006/066959
申请日：2006-10-02
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
IPC分类号： C07D413/06 , C07D413/14 , A61K31/41 , A61P25/00
CPC分类号： C07D413/14
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula (I) wherein R 1 is hydrogen, lower alkyl or aryl; R 2 is lower alkyl; R 3 is hydrogen or halogen; R 4 /R 5 is independently from each other hydrogen, lower alkyl, lower alkinyl, -(CH 2 )n-cycloalkyl, -(CH 2 ) n -heteroaryl, -(CH 2 ) n -heterocyclyl or -(CH 2 ) n -OH; n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA α 5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1是氢，低级烷基或芳基; R 2是低级烷基; R 3是氢或卤素; R 4和R 5彼此独立地为氢，低级烷基，低级炔基， - （CH 2 CH 2）n - 环烷基， - （（CH 2）n - 杂环基， - （CH 2）n - 杂环基或 - （CH 2）n - 2 ）_{名词 -OH; n为0,1,2或3; 和其药学上可接受的酸加成盐。已经发现，这类化合物显示出对GABA 5受体结合位点的高亲和力和选择性，并且可以用作认知增强剂或用于治疗诸如阿尔茨海默病的认知障碍。}

3. 发明申请

WO2007054444A3 3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES 审中-公开
公开(公告)号：WO2007054444A3
公开(公告)日：2007-05-18
申请号：PCT/EP2006/067879
申请日：2006-10-27
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
IPC分类号： C07D413/06 , C07D413/14 , A61K31/42 , A61P25/28
摘要： The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, hydroxy, lower alkoxy, OCF3, -OCH2-R, R3 is hydrogen or lower alkoxy; or R2 and R3 form together with the carbon atom to which they are attached a ring with -CH=CH-CH=-CH-; R is aryl or heteroaryl, optionally substituted by halogen or lower alkyl, or is C(O)NH-lower alkyl, or is -C(O)-heteroaryl, wherein the heteroaryl group is optionally substituted by lower alkyl or phenyl, and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A cc5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

4. 发明申请

WO2008148688A1 PROLINAMIDE-TETRAZOLE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK3受体拮抗剂的丙酰胺 - 四唑衍生物
公开(公告)号：WO2008148688A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056587
申请日：2008-05-29
申请人： F. HOFFMANN-LA ROCHE AG , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D403/12 , A61K31/496 , A61P25/00
CPC分类号： C07D403/12
摘要： The present invention relates to a compound of formula (I) : wherein R 1 is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms; R 2 is hydrogen or halogen; R 3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen; n is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）化合物：其中R 1是环烷基或未被取代或被一个或两个卤原子取代的苯基; R2是氢或卤素; R3是氢，CN，低级烷氧基，低级烷基或卤素; n为0,1或2; 或其药学上合适的酸加成盐。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

5. 发明申请

WO2008148689A1 PROLINAMIDE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：丙酰胺衍生物作为NK3拮抗剂
公开(公告)号：WO2008148689A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056589
申请日：2008-05-29
申请人： F. HOFFMANN-LA ROCHE AG , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/16 , C07D401/06 , C07D487/10 , A61P25/16 , A61P25/18 , A61K31/401
CPC分类号： C07D207/16 , C07D401/06 , C07D471/10
摘要： The present invention relates to a compound of formula (I) wherein R 1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, or lower alkoxy substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 , R 4 form together with the N-atom to which they are attached a non aromatic heterocyclic group, selected from R 5 is hydrogen or halogen; R 6 is phenyl, unsubstituted or substituted by cyano, halogen, lower alkyl, lower alkoxy, CF 3 , -(CH 2 ) 2 O-lower alkyl, C(O)-lower alkyl or C(O)O-lower alkyl, or is pyridinyl, unsubstituted or substituted by CF 3 , or is -C(O)-phenyl; R 7 is hydrogen or lower alkoxy; R 8 is phenyl, lower alkyl or -C(O)O-lower alkyl; R 9 is hydrogen or S(O) 2 -lower alkyl; R 10 is hydrogen or cycloalkyl; X is -CH 2 - or -C(O)-; p is 1 or 2; n is 1, 2 or 3; o is 1 or 2; or to a pharmaceutically suitable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）化合物，其中R 1为氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基或被卤素取代的低级烷氧基; R2是氢或低级烷基; R3，R4与它们所连接的N-原子一起形成非芳族杂环基，选自R5是氢或卤素; R 6为未取代或被氰基，卤素，低级烷基，低级烷氧基，CF 3， - （CH 2）2 O-低级烷基，C（O） - 低级烷基或C（O）O-低级烷基取代或被吡啶基取代的苯基，未取代或被CF 3取代，或为-C（O） - 苯基; R7是氢或低级烷氧基; R8是苯基，低级烷基或-C（O）O-低级烷基; R9是氢或S（O）2-低级烷基; R 10是氢或环烷基; X是-CH 2 - 或-C（O） - ; p为1或2; n为1,2或3; o是1或2; 或其药学上合适的酸加成盐，其是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

6. 发明申请

WO2008081012A1 SPIROPIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：作为NK3拮抗剂的螺吡啶衍生物
公开(公告)号：WO2008081012A1
公开(公告)日：2008-07-10
申请号：PCT/EP2008/050005
申请日：2008-01-02
申请人： F. HOFFMANN-LA ROCHE AG , CAROON, Joanie Marie , DILLON, Michael Patrick , HAN, Bo , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
发明人： CAROON, Joanie Marie , DILLON, Michael Patrick , HAN, Bo , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
IPC分类号： C07D498/10 , A61K31/537 , A61P25/00
CPC分类号： C07D498/10
摘要： The present invention relates to a compound of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is lower alkyl, lower hydroxyalkyl or -(CHR 5 ) x -A; R 5 is hydrogen, lower alkyl or lower hydroxyalkyl, or is heteroaryl optionally substituted by lower alkyl; A is cycloalkyl, aryl, heterocyclyl or heteroaryl, which rings are optionally substituted one or more R 6 , wherein R 6 is lower alkyl, lower alkoxy, lower alkylsulfonyl, cyano, halogen, lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or is aryl, heterocyclyl or heteroaryl optionally substituted by lower alkyl or is cycloalkyl optionally substituted by lower alkyl; x is 0, 1, 2 or 3; or R 1 , R 2 may form together with the N-atom heterocyclyl or heteroaryl, which rings are optionally substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, lower alkylsulfonyl, halogen, cycloalkyl, benzyl or aryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; R 7 is hydrogen, halogen or lower alkyl; m is 1 or 2; when m is 2, R 3 may be the same or not; n is 1 or 2; o is 1 or 2; when o is 2, R 7 may be the same or not; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及其中R 1为氢或低级烷基的式（I）化合物; R 2是低级烷基，低级羟基烷基或 - （CHR 5 O）x -A; R 5为氢，低级烷基或低级羟烷基，或为任选被低级烷基取代的杂芳基; A是环烷基，芳基，杂环基或杂芳基，该环任选被一个或多个R 6取代，其中R 6是低级烷基，低级烷氧基，低级烷基磺酰基，氰基，卤素，被卤素取代的低级烷基或被卤素取代的低级烷氧基，或被任选被低级烷基取代的芳基，杂环基或杂芳基或任选被低级烷基取代的环烷基; x为0,1,2或3; 或R 1，R 2可以与N-原子杂环基或杂芳基一起形成，该环任选被一个或多个选自以下的取代基取代：低级烷基低级烷氧基，低级烷基磺酰基，卤素，环烷基，苄基或芳基; R 3是氢或卤素; R 4是氢或低级烷基; R 7是氢，卤素或低级烷基; m为1或2; 当m为2时，R 3可以相同或不相同; n为1或2; o是1或2; 当o为2时，R 7可以相同或不相同; 或其药学上适合的酸加成盐。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

7. 发明申请

WO2013068306A1 [1, 2, 3] TRIAZOLO [4, 5 -D] PYRIMIDINE DERIVATIVES AS AGONISTS OF THE CANNABINOID RECEPTOR 2 审中-公开
标题翻译： [1,2,3]三唑并[4,5-D]吡啶衍生物作为CANNABINOID受体2的激动剂
公开(公告)号：WO2013068306A1
公开(公告)日：2013-05-16
申请号：PCT/EP2012/071788
申请日：2012-11-05
申请人： F. HOFFMANN-LA ROCHE AG , ADAM, Jean-Michel , BISSANTZ, Caterina , GRETHER, Uwe , KIMBARA, Atsushi , NETTEKOVEN, Matthias , ROEVER, Stephan , ROGERS-EVANS, Mark
发明人： ADAM, Jean-Michel , BISSANTZ, Caterina , GRETHER, Uwe , KIMBARA, Atsushi , NETTEKOVEN, Matthias , ROEVER, Stephan , ROGERS-EVANS, Mark
IPC分类号： C07D487/04 , A61K31/519 , A61P3/10 , A61P9/10 , A61P27/06
CPC分类号： C07D487/04 , A61K9/0019 , A61K9/2054 , A61K9/4866 , A61K31/519 , A61K47/10 , C07D491/107
摘要： The invention relates to a compound of formula (I), wherein A, R 1 and R 2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament as agonists of the cannabinoid receptor 2.
摘要翻译：本发明涉及式（I）化合物，其中A，R 1和R 2如描述和权利要求中所定义。式（I）化合物可以用作大麻素受体2的激动剂的药物。

8. 发明申请

WO2012093109A1 PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK3拮抗剂
公开(公告)号：WO2012093109A1
公开(公告)日：2012-07-12
申请号：PCT/EP2012/050034
申请日：2012-01-03
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D413/10 , A61K31/4025 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D407/06 , C07D413/10
摘要： The invention relates to compounds of formula (I) wherein R 1 is (A), or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl; X is NR or O; R is C(O)-lower alkyl, -C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl; wherein R 2 and R 4 are not simultaneously hydrogen or lower alkyl; R 5 is lower alkyl; R 6 halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O) 2 -lower alkyl or cyano; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）化合物，其中R 1为（A），或为苯基，吡啶基或哒嗪基，其中苯基，吡啶基和哒嗪基可任选被氰基，低级烷基，卤素取代的苯基，低级烷基取代 [1,2,4]恶二唑-3-基或2-氧代 - 哌啶-1-基; X是NR或O; R是C（O） - 低级烷基，被低级烷基，环烷基或苯基，吡啶基或哒嗪基取代的-C（O） - 环烷基，其中苯基，吡啶基和哒嗪基可以任选地被低级烷基，低级烷氧基，氰基， -C（O） - 低级烷基，卤素或被卤素取代的低级烷基; R2是氢或低级烷基; R3是氢，卤素，氰基，被卤素取代的低级烷基或低级烷基; R4是氢或低级烷基; 其中R2和R4不同时为氢或低级烷基; R5是低级烷基; R 6卤素，羟基，低级烷基，低级烷氧基，被卤素取代的低级烷基，S（O）2 - 低级烷基或氰基; 或其药学上合适的酸加成盐。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

9. 发明申请

WO2011012602A1 PIPERIDINE DERIVATIVES AND THEIR USE TO TREAT OBESITY, DIABETES, DYSLIPIDEMIA AND ATHEROSCLEROSIS 审中-公开
标题翻译：哌啶衍生物及其用于治疗肥胖，糖尿病，DYSLIPIDEMIA和ATHEROSCLEROSIS的用途
公开(公告)号：WO2011012602A1
公开(公告)日：2011-02-03
申请号：PCT/EP2010/060854
申请日：2010-07-27
申请人： F. HOFFMANN-LA ROCHE AG , ACKERMANN, Jean , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , WERTHEIMER, Stanley
发明人： ACKERMANN, Jean , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , WERTHEIMER, Stanley
IPC分类号： C07D211/44 , C07D211/58 , C07D409/12 , A61K31/435 , A61K31/44 , A61K31/4436 , A61P3/00
CPC分类号： C07D211/44 , C07D211/58 , C07D409/12
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A 1 , A 2 , R 1 , R 2 , R 3 and R 4 have the significance given in claim 1.
摘要翻译：式（I）化合物及其药学上可接受的盐可以以药物组合物的形式使用，其中A1，A2，R1，R2，R3和R4具有权利要求1中给出的含义。

10. 发明申请

WO2010130665A1 AZACYCLIC SPIRODERIVATIVES AS HSL INHIBITORS 审中-公开
标题翻译： AZACYCLIC螺旋体作为HSL抑制剂
公开(公告)号：WO2010130665A1
公开(公告)日：2010-11-18
申请号：PCT/EP2010/056307
申请日：2010-05-10
申请人： F. HOFFMANN-LA ROCHE AG , ACKERMANN, Jean , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , SCHULZ-GASCH, Tanja , WERTHEIMER, Stanley
发明人： ACKERMANN, Jean , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , SCHULZ-GASCH, Tanja , WERTHEIMER, Stanley
IPC分类号： C07D471/10 , A61K31/438 , A61P3/00
CPC分类号： C07D471/10
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein n, m, A, R 1 and R 2 have the significance given in claim 1. The compounds are useful as HSL inhibitors for the treatment of diabetes dyslipidemia, atherosclerosis and obesity.
摘要翻译：式（I）化合物及其药学上可接受的盐可以以药物组合物的形式使用，其中n，m，A，R 1和R 2具有权利要求1中给出的含义。该化合物可用作HSL抑制剂治疗糖尿病血脂异常，动脉粥样硬化和肥胖。

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