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1. 发明申请

US20100160280A1 AMINOPYRIDINE AND CARBOXYPYRIDINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS 有权
标题翻译：氨基吡啶和羧基吡啶化合物作为磷酸二酯酶10抑制剂
公开(公告)号：US20100160280A1
公开(公告)日：2010-06-24
申请号：US12639931
申请日：2009-12-16
申请人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael Frohn , Paul Harrington , Essa Hu , Matthew R. Kaller , Roxanne Kunz , Stephanie J. Mercede , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Christopher M. Tegley , Guomin Yao
发明人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael Frohn , Paul Harrington , Essa Hu , Matthew R. Kaller , Roxanne Kunz , Stephanie J. Mercede , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Christopher M. Tegley , Guomin Yao
IPC分类号： A61K31/397 , C07D213/22 , A61K31/444 , C07D213/62 , C07D413/14 , A61K31/5377 , C07D401/02 , A61K31/506 , C07D403/14 , A61K31/4545 , A61K31/496 , C07D267/10 , A61K31/553 , C07D243/08 , A61K31/551 , A61P25/00
CPC分类号： C07D401/04 , C07D213/74 , C07D213/84 , C07D401/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5，R6，R7，X1，X2，X3，X4，X5，X6，X7，X8和Y为如说明书中所定义; 或其药学上可接受的盐，其中环A，m，n，y，R2，R3，R4，R5，R6，R7，R8，R9，X1，X2和环A如说明书中所定义; 和其药学上可接受的盐，其中m，n，y，R2，R3，R4，R5，R6，R7，R9，X1，X2和环A如说明书中所定义; 含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖型糖尿病，精神分裂症，双相情感障碍，强迫症等。

2. 发明授权

US08637500B2 Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors 有权
标题翻译：氨基吡啶和羧基吡啶化合物作为磷酸二酯酶10抑制剂
公开(公告)号：US08637500B2
公开(公告)日：2014-01-28
申请号：US12639931
申请日：2009-12-16
申请人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Essa Hu Harrington , Matthew R. Kaller , Roxanne K. Kunz , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Guomin Yao
发明人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Essa Hu Harrington , Matthew R. Kaller , Roxanne K. Kunz , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Guomin Yao
IPC分类号： A61K31/551 , A61K31/553 , A61K31/5377 , A61K31/497 , C07D243/08 , C07D267/10 , C07D401/12 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , C07D213/74 , C07D213/84 , C07D401/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5，R6，R7，X1，X2，X3，X4，X5，X6，X7，X8和Y为如说明书中所定义; 或其药学上可接受的盐，其中环A，m，n，y，R2，R3，R4，R5，R6，R7，R8，R9，X1，X2和环A如说明书中所定义; 和其药学上可接受的盐，其中m，n，y，R2，R3，R4，R5，R6，R7，R9，X1，X2和环A如说明书中所定义; 含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

3. 发明申请

US20130079325A1 PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS 有权
标题翻译：吡啶和吡嗪衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：US20130079325A1
公开(公告)日：2013-03-28
申请号：US13676826
申请日：2012-11-14
申请人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
发明人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
IPC分类号： C07D413/14 , C07D401/14 , C07D401/12
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00
摘要： Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

4. 发明授权

US08318718B2 Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors 有权
标题翻译：吡啶和嘧啶衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：US08318718B2
公开(公告)日：2012-11-27
申请号：US12619573
申请日：2009-11-16
申请人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
发明人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
IPC分类号： A61K31/4439 , A61K31/437 , A61K31/52 , A61K31/5377 , A61K31/55 , A61K31/397 , C07D401/12 , C07D471/04 , C07D473/00 , C07D413/14 , C07D401/14 , A61P25/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00
摘要： Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

5. 发明申请

US20110306588A1 HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS 有权
标题翻译：作为PDE10抑制剂的异氟醚化合物
公开(公告)号：US20110306588A1
公开(公告)日：2011-12-15
申请号：US13106718
申请日：2011-05-12
申请人： Jennifer R. Allen , Daniel B. Horne , Essa Hu , Matthew R. Kaller , Holger Monenschein , Thomas T. Nguyen , Andreas Reichelt , Robert M. Rzasa
发明人： Jennifer R. Allen , Daniel B. Horne , Essa Hu , Matthew R. Kaller , Holger Monenschein , Thomas T. Nguyen , Andreas Reichelt , Robert M. Rzasa
IPC分类号： A61K31/497 , C07D413/14 , C07D491/107 , A61K31/5377 , A61K31/55 , A61K31/553 , A61K31/551 , A61K31/498 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/00 , A61P25/14 , A61P25/24 , A61P25/30 , C07D401/14
CPC分类号： C07D491/107 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/10
摘要： Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：杂环氧基杂环基化合物和含有它们的组合物，以及这些化合物的制备方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，亨廷顿舞蹈病，双相情感障碍，强迫症等。

6. 发明授权

US08497265B2 Heteroaryloxyheterocyclyl compounds as PDE10 inhibitors 有权
标题翻译：杂环氧基杂环化合物作为PDE10抑制剂
公开(公告)号：US08497265B2
公开(公告)日：2013-07-30
申请号：US13106718
申请日：2011-05-12
申请人： Jennifer R. Allen , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Holger Monenschein , Thomas T. Nguyen , Andreas Reichelt , Robert M. Rzasa
发明人： Jennifer R. Allen , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Holger Monenschein , Thomas T. Nguyen , Andreas Reichelt , Robert M. Rzasa
IPC分类号： C07D241/18 , C07D413/14 , C07D401/14 , A61K31/5355 , A61K31/497 , A61P3/04 , A61P3/10 , A61P25/18
CPC分类号： C07D491/107 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/10
摘要： Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：杂环氧基杂环基化合物和含有它们的组合物，以及这些化合物的制备方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，亨廷顿舞蹈病，双相情感障碍，强迫症等。

7. 发明授权

US08778941B2 TRPM8 antagonists and their use in treatments 有权
公开(公告)号：US08778941B2
公开(公告)日：2014-07-15
申请号：US13529880
申请日：2012-06-21
申请人： James Brown , Jian J. Chen , Vijay Keshav Gore , Scott Harried , Daniel B. Horne , Matthew R. Kaller , Qingyian Liu , Holger Monenschein , Thomas T. Nguyen , Nobuko Nishimura , Wenge Zhong
发明人： James Brown , Jian J. Chen , Vijay Keshav Gore , Scott Harried , Daniel B. Horne , Matthew R. Kaller , Qingyian Liu , Holger Monenschein , Thomas T. Nguyen , Nobuko Nishimura , Wenge Zhong
IPC分类号： C07D401/14 , C07D213/75 , C07D213/40 , C07D405/12 , C07D413/12
CPC分类号： C07D213/53 , C07C275/30 , C07D213/40 , C07D213/75 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

8. 发明申请

US20130157996A1 TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS 有权
标题翻译： TRPM8拮抗剂及其在治疗中的应用
公开(公告)号：US20130157996A1
公开(公告)日：2013-06-20
申请号：US13529860
申请日：2012-06-21
申请人： Kaustav Biswas , James Brown , Jian J. Chen , Vijay Keshav Gore , Scott Harried , Daniel B. Horne , Matthew R. Kaller , Qingyian Liu , Vu Van Ma , Holger Monenschein , Thomas T. Nguyen , David J. St. Jean, JR. , Chester Chenguang Yuan , Wenge Zhong
发明人： Kaustav Biswas , James Brown , Jian J. Chen , Vijay Keshav Gore , Scott Harried , Daniel B. Horne , Matthew R. Kaller , Qingyian Liu , Vu Van Ma , Holger Monenschein , Thomas T. Nguyen , David J. St. Jean, JR. , Chester Chenguang Yuan , Wenge Zhong
IPC分类号： C07D498/04 , C07D401/14 , C07D213/81 , C07D487/04 , C07D413/12 , C07D401/12 , C07D471/04
CPC分类号： C07D213/82 , C07D213/40 , C07D213/61 , C07D213/81 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D498/04
摘要： Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
摘要翻译：式I的化合物可用作TRPM8的拮抗剂。这些化合物可用于治疗多种TRPM8介导的病症和病症，并且可用于制备用于治疗这种病症和病症的药物和药物组合物。这些疾病的实例包括但不限于偏头痛和神经性疼痛。式I的化合物具有以下结构：其中本文提供变量的定义。

9. 发明授权

US07162108B2 Planar lightwave circuit variable optical attenuator 有权
标题翻译：平面光波电路可变光衰减器
公开(公告)号：US07162108B2
公开(公告)日：2007-01-09
申请号：US11015223
申请日：2004-12-17
申请人： Anca L. Sala , Duncan W. Harwood , Barthelemy Fondeur , Anantharaman Vaidyanathan , Robert J. Brainard , Sanjay M. Thekdi , Thomas T. Nguyen , Ian Hutagalung
发明人： Anca L. Sala , Duncan W. Harwood , Barthelemy Fondeur , Anantharaman Vaidyanathan , Robert J. Brainard , Sanjay M. Thekdi , Thomas T. Nguyen , Ian Hutagalung
IPC分类号： G02F1/01 , G02F1/035 , G02F1/00 , G02B26/00 , G02B6/26 , G02B6/42
CPC分类号： G02F1/0147 , G02B6/12007 , G02B6/266 , G02F1/21 , G02F2001/0113 , G02F2001/212 , G02F2203/06
摘要： The invention relates to a variable optical attenuator constructed as a Mach Zehnder planar lightwave circuit, particularly including a channel waveguide support structure for heat isolation and stress relief to reduce polarization dependent loss (PDL) and power consumption in the device. Power reduction trenches comprise longitudinal segments having small stress relief pillars of cladding material left in between them in the etching process. The waveguides of the MZI are supported by a main pillar structure and integral stress relief pillars which remain after removal of the trenches. The waveguide is surrounded by air on three sides for improved heat isolation. The performance of the present invention shows substantial improvement in PDL and extinction ratio over the prior art continuous trench design, and also, to a smaller degree, over the case where power reduction trenches are not used at all. Segmented trenches appear to allow for the lowest stress on the two waveguide arms of all the cases including no trench and trenched devices.
摘要翻译：本发明涉及一种构成马赫曾德平面光波回路的可变光衰减器，特别是包括用于隔热和应力释放的通道波导支撑结构，以减少器件中的偏振相关损耗（PDL）和功耗。功率减小沟槽包括在蚀刻工艺中在它们之间具有小的应力消除柱的包层材料的纵向段。 MZI的波导由主柱结构和消除沟槽后保留的积分应力消除柱支撑。波导三面被空气包围，以改善热隔离。与现有技术的连续沟槽设计相比，本发明的性能显示出PDL和消光比的显着改善，并且在更少的程度上，在完全不使用功率降低沟槽的情况下。分段沟槽似乎允许在所有情况下的两个波导臂上的最小应力，包括没有沟槽和沟槽的器件。

10. 发明授权

US5773420A Acylated benzylglycosides as inhibitors of smooth muscle cell proliferation 失效
标题翻译：酰化苄基甘氨酸作为平滑肌细胞增殖的抑制剂
公开(公告)号：US5773420A
公开(公告)日：1998-06-30
申请号：US531142
申请日：1995-10-20
申请人： Thomas T. Nguyen , John W. Ellingboe
发明人： Thomas T. Nguyen , John W. Ellingboe
IPC分类号： C07H15/203 , A61K31/70 , C07H17/00
CPC分类号： C07H15/203
摘要： This invention relates to acylated benzylglycosides and a method for their use as smooth muscle cell proliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterize by excessive smooth muscle proliferation, such as restenosis. The acylated benzylglycosides of this invention are those of formula I, below: ##STR1## wherein X is ##STR2## R.sup.1 is H, alkyl having 1 to 6 carbon atoms, chloro, bromo, or alkoxy having 1 to 6 carbon atoms; R.sup.2 is H, an acyl group having 1 to 6 carbon atoms, phenylsulfonyl, or substituted phenylsulfonyl; and R.sup.3 is an acyl group having 1 to 8 carbon atoms, benzoyl, substituted benzoyl, alkylsulfonyl having 1 to 6 carbon atoms, phenylsulfonyl, or substituted phenylsulfonyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are each, independently, an acyl group having 1 to 6 carbon atoms; and R.sup.10 and R.sup.11 are each, independently, an acyl group having 1 to 6 carbon atoms, or the R.sup.10 and R.sup.11 groups on the 4' and 6' positions of the maltose or the 4 and 6 positions of the glucose form an isopropylidene group; or pharmaceutically acceptable salts thereof. R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are each, independently, an acyl group having 1 to 6 carbon atoms; and R.sup.10 and R.sup.11 are each, independently, an acyl group having 1 to 6 carbon atoms, or the R.sup.10 and R.sup.11 groups on the 4' and 6' positions of the maltose or the 4 and 6 positions of the glucose form an isopropylidene group; or a pharmaceutically acceptable salt thereof a pharmaceutically acceptable agent.
摘要翻译：本发明涉及酰化苄基鹅糖苷及其作为平滑肌细胞增殖抑制剂和作为用于治疗以过度平滑肌增生为特征的疾病和病症如再狭窄的治疗组合物的方法。本发明的酰化苄基鹅糖苷是下式I的化合物：其中X是R或R 1是H，具有1-6个碳原子的烷基，氯，溴或具有1-6个碳原子的烷氧基碳原子 R2是H，具有1-6个碳原子的酰基，苯基磺酰基或取代的苯基磺酰基; 并且R 3是具有1至8个碳原子的酰基，苯甲酰基，取代的苯甲酰基，具有1至6个碳原子的烷基磺酰基，苯基磺酰基或取代的苯基磺酰基; R4，R5，R6，R7，R8和R9各自独立地为具有1至6个碳原子的酰基; R10和R11各自独立地为具有1至6个碳原子的酰基，或麦芽糖4'和6'位上的R 10和R 11基团或葡萄糖的4和6位形成异丙叉基; 或其药学上可接受的盐。 R4，R5，R6，R7，R8和R9各自独立地为具有1至6个碳原子的酰基; R10和R11各自独立地为具有1至6个碳原子的酰基，或麦芽糖4'和6'位上的R 10和R 11基团或葡萄糖的4和6位形成异丙叉基; 或其药学上可接受的盐是药学上可接受的试剂。

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