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1. 发明授权

US09359376B2 Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds 有权
标题翻译：取代的甲基甲酰基试剂及其使用方法来改变化合物的物理化学和/或药代动力学性质
公开(公告)号：US09359376B2
公开(公告)日：2016-06-07
申请号：US14110373
申请日：2012-04-09
申请人： Sundeep Dugar , Dinesh Mahajan , Frank Peter Hollinger
发明人： Sundeep Dugar , Dinesh Mahajan , Frank Peter Hollinger
IPC分类号： C07D307/77 , C07D305/00 , C07D413/00 , C07D405/00 , C07D495/14 , C07D401/14 , C07D405/14 , C07D213/80 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04 , C07D487/22 , C07D491/22 , C07D295/20 , C07D305/14 , C07D213/803 , C07D491/147
CPC分类号： C07D495/14 , C07D213/80 , C07D213/803 , C07D213/81 , C07D213/82 , C07D295/20 , C07D305/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D471/04 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22
摘要： The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
摘要翻译：本发明涉及合成和应用新的手性/非手性取代的甲酰甲酰基试剂以改性药物和/或生物活性物质，以改变未经修饰的原始药剂的所得化合物的物理化学，生物学和/或药代动力学性质。

2. 发明授权

US09328071B2 Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals 有权
公开(公告)号：US09328071B2
公开(公告)日：2016-05-03
申请号：US14314780
申请日：2014-06-25
申请人： SANOFI
发明人： Matthias Schaefer , Josef Pernerstorfer , Dieter Kadereit , Hartmut Strobel , Werngard Czechtizky , L. Charlie Chen , Alena Safarova , Aleksandra Weichsel , Marcel Patek
IPC分类号： C07C237/38 , C07D333/38 , C07D213/82 , C07C235/54 , C07C235/62 , C07C235/84 , C07C317/22 , C07C317/46 , C07C323/62 , C07C255/54 , C07C255/57 , C07C255/58 , C07D207/08 , C07D213/81 , C07C307/10 , C07C309/73 , C07C311/08 , C07C323/12 , C07C323/19 , C07D207/09 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/68 , C07D213/74 , C07D213/75 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/84 , C07D235/12 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D333/16 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D471/08 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C319/20 , C07C323/42
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

3. 发明授权

US08957212B2 Photobase generator 有权
标题翻译：光源发生器
公开(公告)号：US08957212B2
公开(公告)日：2015-02-17
申请号：US13132216
申请日：2009-12-01
申请人： Ayako Kuramoto , Motoshige Sumino , Nobuhiko Sakai
发明人： Ayako Kuramoto , Motoshige Sumino , Nobuhiko Sakai
IPC分类号： C07D295/205 , C07C271/24 , C07C271/12 , C07C50/18 , C07D233/60 , C07D295/192 , C07D211/46 , B01J19/08 , C07D211/44 , C07D295/20
CPC分类号： C07D211/44 , C07C271/12 , C07C271/24 , C07C2601/14 , C07C2603/24 , C07D211/46 , C07D233/60 , C07D295/20 , C07D295/205
摘要： There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branched or acyclic alkyl group having 1 to 10 carbon atoms).
摘要翻译：旨在提供当用长波长光（活性能量射线）照射时产生碱的新型化合物，含有该化合物的光碱产生剂和光碱产生方法，本发明涉及由通式 [1]一种含有这些化合物的光碱产生剂和光碱产生方法（其中，Ar表示选自由蒽基，蒽醌基和芘基组成的组中的特定结构的基团中的任一个; R 1和R 2各自独立地表示氢原子或碳原子数为1〜10的直链状，支链状或环状的烷基，或者表示可以与氮原子一起形成含氮原子的脂环式或含有氮原子的芳香环的烷基它们被结合，其中具有3至8个碳原子的环可以具有取代基，R 3和R 4各自独立地表示氢 tom，具有1至10个碳原子的直链，支链或无环烷基）。

4. 发明申请

US20140100210A1 GUANIDINE COMPOUND 审中-公开
标题翻译：胍基化合物
公开(公告)号：US20140100210A1
公开(公告)日：2014-04-10
申请号：US14099131
申请日：2013-12-06
申请人： Astellas Pharma Inc.
发明人： Kousei YOSHIHARA , Daisuke SUZUKI , Susumu YAMAKI , Hiroyoshi YAMADA , Hisashi MIHARA , Norio SEKI
IPC分类号： C07D405/12 , C07D267/10 , C07D401/04 , C07D239/48 , C07D239/42 , C07D213/74
CPC分类号： C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
摘要： [Problem]The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.[Means for Solution]The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
摘要翻译： [问题]本发明提供了作为药物组合物的活性成分，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物有用的化合物。 [解决方案]本发明人对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性并且可用于预防和/或治疗VAP-1相关疾病，特别是糖尿病性肾病或糖尿病性黄斑水肿，从而完成本发明。此外，本发明涉及包含本发明的化合物或其盐和赋形剂的药物组合物，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物。

5. 发明申请

US20130274476A1 CONFORMATIONALLY RESTRICTED UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE 审中-公开
标题翻译：可溶性环氧化物水解物的一致的限制性尿素抑制剂
公开(公告)号：US20130274476A1
公开(公告)日：2013-10-17
申请号：US13918837
申请日：2013-06-14
申请人： The Regents of the University of California
发明人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless, JR.
IPC分类号： C07D211/58
CPC分类号： C07D211/58 , C07D209/08 , C07D211/26 , C07D211/96 , C07D213/40 , C07D235/30 , C07D295/20 , C07D295/205 , C07D401/06 , C07D401/12 , C07D487/18 , C12Q1/34
摘要： Inhibitors of the soluble epoxide exemplary hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要翻译：提供了可溶性环氧化物示例性水解酶（sEH）的抑制剂，其包含多个药效团并且可用于治疗疾病。

6. 发明申请

US20130203733A1 COMPOSITIONS AND METHODS FOR MODULATING INTERACTION BETWEEN POLYPEPTIDES 审中-公开
标题翻译：用于调节多肽之间相互作用的组合物和方法
公开(公告)号：US20130203733A1
公开(公告)日：2013-08-08
申请号：US13723101
申请日：2012-12-20
申请人： The General Hospital Corporation , Massachusetts Institute of Technology
发明人： Aleksey G. Kazantsev , Anne B. Young , David E. Housman , Steven M. Hersch
IPC分类号： C07D223/02 , C07D217/24 , C07C311/44 , C07D209/80 , C07D333/36 , C07D295/20 , C07D215/40
CPC分类号： C07C311/46 , A61K31/21 , A61K31/277 , A61K31/4015 , A61K31/445 , C07C311/44 , C07C2601/16 , C07D209/56 , C07D209/80 , C07D215/40 , C07D215/42 , C07D217/24 , C07D221/06 , C07D223/02 , C07D295/20 , C07D295/26 , C07D333/36 , C07D333/38 , C07D401/06
摘要： The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
摘要翻译：本发明部分基于我们进行的测定，其显示了可用于治疗或预防以一种蛋白质与另一种蛋白质的异常或不期望的结合为特征的疾病的化合物。

7. 发明授权

US08404747B2 Compositions and methods for modulating interaction between polypeptides 有权
标题翻译：用于调节多肽之间相互作用的组合物和方法
公开(公告)号：US08404747B2
公开(公告)日：2013-03-26
申请号：US11076093
申请日：2005-03-07
申请人： Aleksey G. Kazantsev , Anne B. Young , David E. Housman , Steven Hersch
发明人： Aleksey G. Kazantsev , Anne B. Young , David E. Housman , Steven Hersch
IPC分类号： A61K31/445 , A61K31/4015 , A61K31/21 , A61K31/277
CPC分类号： C07C311/46 , A61K31/21 , A61K31/277 , A61K31/4015 , A61K31/445 , C07C311/44 , C07C2601/16 , C07D209/56 , C07D209/80 , C07D215/40 , C07D215/42 , C07D217/24 , C07D221/06 , C07D223/02 , C07D295/20 , C07D295/26 , C07D333/36 , C07D333/38 , C07D401/06
摘要： The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
摘要翻译：本发明部分基于我们进行的测定，其显示可用于治疗或预防以一种蛋白质与另一种蛋白质的异常或不期望的结合为特征的疾病的化合物。

8. 发明申请

US20120046292A1 DIACYLETHYLENEDIAMINE COMPOUND 审中-公开
标题翻译：二乙烯基胺化合物
公开(公告)号：US20120046292A1
公开(公告)日：2012-02-23
申请号：US13263258
申请日：2010-04-19
申请人： Tomoaki Kawano , Yasuhiro Yonetoku , Takeshi Hanazawa , Takahiro Nigawara , Hiroki Fukudome , Hiroshi Moritani
发明人： Tomoaki Kawano , Yasuhiro Yonetoku , Takeshi Hanazawa , Takahiro Nigawara , Hiroki Fukudome , Hiroshi Moritani
IPC分类号： A61K31/197 , C07D307/79 , A61K31/343 , A61P3/04 , A61K31/495 , C07D239/42 , A61K31/498 , A61K31/5375 , C07C229/38 , C07D295/155
CPC分类号： C07D207/06 , C07B2200/05 , C07C233/62 , C07C235/46 , C07C235/50 , C07C235/84 , C07C237/34 , C07C255/46 , C07C271/20 , C07C275/26 , C07C275/28 , C07C307/06 , C07C311/51 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/18 , C07C2602/42 , C07C2602/44 , C07D209/08 , C07D209/42 , C07D209/44 , C07D211/16 , C07D211/18 , C07D211/32 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/60 , C07D211/62 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/54 , C07D217/02 , C07D217/06 , C07D217/26 , C07D231/14 , C07D231/22 , C07D239/28 , C07D239/42 , C07D241/04 , C07D241/42 , C07D257/04 , C07D263/32 , C07D263/34 , C07D263/48 , C07D271/06 , C07D271/10 , C07D275/02 , C07D277/20 , C07D277/56 , C07D277/68 , C07D295/14 , C07D295/155 , C07D295/18 , C07D295/20 , C07D295/205 , C07D307/79 , C07D309/06 , C07D317/46 , C07D317/72 , C07D319/18 , C07D333/38 , C07D333/54 , C07D333/68 , C07D333/70 , C07D409/12 , C07D451/02 , C07D495/04
摘要： [Problem]A compound which is useful as an anti-obesity agent is provided.[Means for Solution]The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.
摘要翻译： [问题]提供了可用作抗肥胖剂的化合物。 [解决方案]本发明人研究了具有DGAT1抑制作用的化合物，其有希望作为用于治疗肥胖，II型糖尿病，脂肪肝和与这些疾病相关的疾病的药物组合物的活性成分，以及作为结果发现本发明的二酰亚乙基二胺化合物具有优异的DGAT1抑制作用，从而完成了本发明。也就是说，本发明的二酰亚胺二胺化合物具有DGAT1抑制作用，因此可以用作预防和/或治疗肥胖，II型糖尿病，脂肪肝和与这些疾病相关的疾病的药剂。

9. 发明申请

US20100004261A1 PIPERAZINYL AND PIPERIDINYL UREAS AS MODULATORS OF FATTY ACID AMIDE HYDROLASE 有权
标题翻译：作为脂肪酸酰胺水解酶的调节剂的哌嗪和哌啶酸
公开(公告)号：US20100004261A1
公开(公告)日：2010-01-07
申请号：US12557650
申请日：2009-09-11
申请人： Richard Apodaca , J. Guy Breitenbucher , Kanaka Pattabiraman , Mak Seierstad , Wei Xiao
发明人： Richard Apodaca , J. Guy Breitenbucher , Kanaka Pattabiraman , Mak Seierstad , Wei Xiao
IPC分类号： A61K31/496 , C07D401/12 , C07D401/14 , C07D417/14 , A61P25/00 , A61P25/22 , A61P29/00 , A61P3/00 , A61P25/28 , A61P25/08 , A61P1/00 , A61P27/02 , A61P25/16 , A61P27/06 , A61P31/18 , A61P31/00 , A61P19/02 , A61P9/00 , A61P9/12 , A61P35/00 , A61P11/00 , A61P15/00 , A61P15/04 , A61P17/04
CPC分类号： C07D295/195 , C07D207/335 , C07D209/08 , C07D209/14 , C07D209/82 , C07D211/16 , C07D213/38 , C07D213/56 , C07D213/61 , C07D213/75 , C07D215/12 , C07D215/18 , C07D239/42 , C07D241/42 , C07D295/20 , C07D295/215 , C07D307/79 , C07D307/81 , C07D317/46 , C07D317/58 , C07D319/16 , C07D319/18 , C07D333/58 , C07D333/60 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
摘要翻译：某些哌嗪基和哌啶基脲化合物可用作FAAH抑制剂。此类化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法。因此，可以施用化合物以治疗例如焦虑，疼痛，炎症，睡眠障碍，进食障碍或运动障碍（例如多发性硬化症）。

10. 发明申请

US20060173184A1 Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase 有权
公开(公告)号：US20060173184A1
公开(公告)日：2006-08-03
申请号：US11321710
申请日：2005-12-29
申请人： Richard Apodaca , J. Breitenbucher , Kanaka Pattabiraman , Mark Seierstad , Wei Xiao
发明人： Richard Apodaca , J. Breitenbucher , Kanaka Pattabiraman , Mark Seierstad , Wei Xiao
IPC分类号： C07D403/02
CPC分类号： C07D295/195 , C07D207/335 , C07D209/08 , C07D209/14 , C07D209/82 , C07D211/16 , C07D213/38 , C07D213/56 , C07D213/61 , C07D213/75 , C07D215/12 , C07D215/18 , C07D239/42 , C07D241/42 , C07D295/20 , C07D295/215 , C07D307/79 , C07D307/81 , C07D317/46 , C07D317/58 , C07D319/16 , C07D319/18 , C07D333/58 , C07D333/60 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

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