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71. 发明申请

US20160185722A1 METHOD FOR PRODUCING META-XYLYLENEDIAMINES AND METHOD FOR PRODUCING BISAMIDE COMPOUND 有权
标题翻译：用于生产甲基二硅氧烷的方法和用于生产双胺化合物的方法
公开(公告)号：US20160185722A1
公开(公告)日：2016-06-30
申请号：US14903262
申请日：2014-08-11
申请人： MITSUI CHEMICALS, INC.
发明人： Kouya KOJIMA , Hidetaka TSUKADA , Mamoru TAKASHINA , Chitoshi SHIMAKAWA , Naoyuki KAKINUMA
IPC分类号： C07D209/48 , C07C209/62
CPC分类号： C07D209/48 , C07C209/62 , C07C211/27
摘要： A method for producing meta-xylylenediamines includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound having a primary amide group or a secondary amide group are allowed to react in the presence of an acidic liquid, a dehalogenation step in which the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom, and a deprotection step in which the primary amide group or the secondary amide group derived from the amide compound is converted to an amino group. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 16; the acidic liquid has an inorganic acid concentration of more than 80 mass %; and the reaction temperature is more than 40° C.
摘要翻译：一种生产间二甲苯二胺的方法包括一种反应步骤，其中使单卤代苯，甲醛和具有伯酰胺基或仲酰胺基的酰胺化合物在酸性液体存在下反应，其中脱卤步骤衍生自单卤代苯的卤素原子被氢原子取代，其中将来自酰胺化合物的伯酰胺基或仲酰胺基转化为氨基的脱保护步骤。在反应步骤中，酸性液体含有无机酸，无机酸相对于单卤代苯的当量比大于16; 酸性液体的无机酸浓度大于80质量％反应温度大于40℃。

72. 发明申请

US20160122292A1 BASE GENERATOR, BASE-REACTIVE COMPOSITION CONTAINING SAID BASE GENERATOR, AND BASE GENERATION METHOD 审中-公开
标题翻译：基站发生器，含有基站发生器的基板反应组合物和基站生成方法
公开(公告)号：US20160122292A1
公开(公告)日：2016-05-05
申请号：US14901525
申请日：2014-06-25
申请人： WAKO PURE CHEMICAL INDUSTRIES, LTD. , TOKYO UNIVERSITY OF SCIENCE FOUNDATION
发明人： Nobuhiko SAKAI , Kosuke YANABA , Koji ARIMITSU
IPC分类号： C07C279/26 , G03F7/004 , C07C65/28 , C07D209/48 , C07C59/84 , C07D311/86
CPC分类号： C07C279/26 , B01J19/123 , B01J19/127 , B01J19/128 , C07C59/84 , C07C65/28 , C07C2601/14 , C07C2603/24 , C07D209/48 , C07D311/86 , G03F7/0045
摘要： It is a subject of the present invention to provide a base generator which has high solubility to general-purpose organic solvents, can dissolve directly into a base-reactive compound, such as an epoxy-based compound, further is provided with both performance of high heat resistance and low nucleophilicity, and generates a strong base, a base-reactive composition comprising the base generator and a base-reactive compound, as well as a method for generating a base, etc.The present invention relates to a compound represented by the general formula (A), a base generator comprising the compound, a base-reactive composition which comprises the base generator and a base-reactive compound, as well as a method for generating a base, etc. (wherein R1 to R5 each independently represent a hydrogen atom; an alkyl group; an aryl group which may have a substituent; or an arylalkyl group which may have a substituent, R6 represents a hydrogen atom; an alkyl group which may have a substituent; an alkenyl group; an alkynyl group; an aryl group which may have a substituent; or an arylalkyl group which may have a substituent, R7 represents a hydrogen atom; an alkyl group which may have an amino group; an aryl group which may have a substituent; or an arylalkyl group which may have a substituent, and Z− represents an anion derived from a carboxylic acid having a specific structure.)
摘要翻译：本发明的主题是提供一种对通用有机溶剂具有高溶解度的碱发生剂，可以直接溶解在诸如环氧基化合物的碱反应性化合物中，还具有高的性能耐碱性和低亲核性，并且产生强碱，包含碱产生剂和碱反应性化合物的碱反应性组合物，以及产生碱的方法等。本发明涉及由通式（A），包含该化合物的碱发生剂，包含碱发生剂和碱反应性化合物的碱反应性组合物，以及产生碱的方法等（其中R 1至R 5各自独立地表示氢原子;烷基;可具有取代基的芳基;或可具有取代基的芳烷基，R6表示氢原子;可具有取代基的烷基;可具有取代基的烷基甲基炔基; 可以具有取代基的芳基; 或可具有取代基的芳基烷基，R7表示氢原子; 可以具有氨基的烷基; 可以具有取代基的芳基; 或可以具有取代基的芳烷基，Z-表示衍生自具有特定结构的羧酸的阴离子。）

73. 发明授权

US09296689B2 Substituted isoindoline-1,3-dione derivatives 有权
标题翻译：取代的异二氢吲哚-1,3-二酮衍生物
公开(公告)号：US09296689B2
公开(公告)日：2016-03-29
申请号：US14490859
申请日：2014-09-19
申请人： Concert Pharmaceuticals, Inc.
发明人： Julie F. Liu
IPC分类号： C07D209/48 , C07D207/404 , C07D209/46 , C07D405/12 , C07B59/00
CPC分类号： C07D209/48 , C07B59/002 , C07B2200/05 , C07D207/404 , C07D209/46 , C07D405/12
摘要： This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogs of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
摘要翻译：本发明涉及新的取代的异二氢吲哚-1,3-二酮衍生物及其药学上可接受的盐。更具体地，本发明涉及作为去甲生物的类似物的新的取代的异二氢吲哚-1,3-二酮衍生物。本发明还提供了包含本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用去甲苯磺酸酯有益治疗的疾病和病症的方法中的用途。

74. 发明申请

US20160067257A1 SCREENING METHOD AND COMPOUNDS FOR MODULATING TELOMERASE ACTIVITY 审中-公开
标题翻译：筛选方法和化合物用于调节TELOMERASE活性
公开(公告)号：US20160067257A1
公开(公告)日：2016-03-10
申请号：US14945682
申请日：2015-11-19
申请人： The Wistar Institute
发明人： Emmanuel Skordalakes
IPC分类号： A61K31/5375 , A61K31/513 , A61K45/06 , C07D209/48 , A61K31/4035 , A61K31/4184 , A61K31/4409 , A61K31/4406 , A61K31/166 , A61K31/165 , A61K31/341 , C07D403/12 , A61K31/381
CPC分类号： A61K31/5375 , A61K31/165 , A61K31/166 , A61K31/341 , A61K31/381 , A61K31/4035 , A61K31/4184 , A61K31/4406 , A61K31/4409 , A61K31/513 , A61K45/06 , C07C43/174 , C07D209/48 , C07D401/12 , C07D403/12 , C07D413/12 , C12Q1/48 , G01N2333/91245
摘要： The present invention embraces methods for identifying compounds that modulate the activity of telomerase. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the TRBD, “thumb,” “finger,” and/or “palm” domain; or FP-pocket, PT-pocket or Th-pocket of telomerase and testing the compound for its ability to modulate the activity of telomerase. Compounds selected for interacting with the T-pocket or Fingers-Palm pocket of telomerase are also provided.
摘要翻译：本发明包括用于鉴定调节端粒酶活性的化合物的方法。通过设计或筛选与TRBD，“拇指”，“手指”和/或“手掌”结构域的至少一个氨基酸残基结合的化合物来鉴定本发明化合物; 或FP-pocket，PT-pocket或Th-pocket端粒酶，并测试该化合物调节端粒酶活性的能力。还提供了选择用于与端粒酶的T形口袋或手指 - 棕榈袋相互作用的化合物。

75. 发明申请

US20160052927A1 USE OF ORGANIC OXYIMIDES AS FLAME RETARDANT FOR PLASTIC MATERIALS AND ALSO FLAME-RETARDANT PLASTIC MATERIAL COMPOSITION AND MOULDED PARTS PRODUCED THEREFROM 审中-公开
标题翻译：有机氧化物作为塑料材料阻燃剂的使用，还有阻燃塑料材料组合物及其生产的成型零件
公开(公告)号：US20160052927A1
公开(公告)日：2016-02-25
申请号：US14779849
申请日：2014-03-24
申请人： FRAUNHOFER-GESELLSCHAFT ZUR FÖRDERUNG DER ANGEWANDTEN FORSCHUNG E.V.
发明人： Rudolf PFAENDNER , Elke METZSCH-ZILLINGEN , Maria STEC
IPC分类号： C07D487/04 , C07D207/46 , C07D221/14 , C09D123/12 , C07D209/48
摘要： The present invention relates to the use of organic oxy imides as flame retardants for plastics. According to the present invention, a flame-retardant plastics composition is likewise specified, including an oxy imide as flame retardant. Additionally specified are mouldings produced from an inventive flame-retardant polymer composition.
摘要翻译：本发明涉及有机氧化亚胺作为塑料阻燃剂的用途。根据本发明，同样规定了阻燃塑料组合物，包括作为阻燃剂的氧酰亚胺。另外指定的是由本发明的阻燃聚合物组合物制备的模制品。

76. 发明申请

US20160046570A1 N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES 审中-公开
标题翻译： N-羟基甲酰胺和N-羟基-N-亚磺酰胺衍生物
公开(公告)号：US20160046570A1
公开(公告)日：2016-02-18
申请号：US14927658
申请日：2015-10-30
申请人： The Johns Hopkins University , Cardioxyl Pharmaceuticals, Inc.
发明人： John P. Toscano , Art Sutton , Vincent Jacob Kalish , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost
IPC分类号： C07C311/48 , C07D295/195 , C07D309/12 , C07D211/46 , C07D317/30 , C07D241/04 , C07D401/04 , C07D413/04 , C07D211/58 , C07D207/06 , C07D211/62 , C07D213/59 , C07D233/38 , C07D241/08 , C07D209/48 , C07D207/16 , C07D333/34 , C07D307/82 , C07D213/71 , C07C317/32 , C07C311/51
CPC分类号： C07C311/48 , C07C311/51 , C07C317/14 , C07C317/32 , C07C2601/14 , C07D207/06 , C07D207/16 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/62 , C07D213/40 , C07D213/46 , C07D213/59 , C07D213/71 , C07D213/74 , C07D233/38 , C07D241/04 , C07D241/08 , C07D295/192 , C07D295/195 , C07D295/205 , C07D307/82 , C07D309/12 , C07D317/30 , C07D333/34 , C07D401/04 , C07D413/04
摘要： The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
摘要翻译：本发明提供某些N-酰氧基亚磺酰胺和N-羟基-N-酰基磺酰胺衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及使用这些化合物或药物组合物的方法。特别地，本发明提供了使用这些化合物或药物组合物治疗，预防或延缓疾病或病症发作和/或发展的方法。在一些实施方案中，疾病或病症选自心血管疾病，缺血，再灌注损伤，癌性疾病，肺动脉高压和对硝酰基治疗有反应的病症。

77. 发明申请

US20160031837A1 COMPOUNDS FOR INDUCING PROLIFERATION AND DIFFERENTIATION OF CELLS, AND METHODS OF USE THEREOF 审中-公开
标题翻译：用于诱导细胞增殖和分化的化合物及其使用方法
公开(公告)号：US20160031837A1
公开(公告)日：2016-02-04
申请号：US14772284
申请日：2014-03-14
申请人： THE BROAD INSTITUTE, INC. , MASSACHUSETTS INSTITUTE OF TECHNOLOGY
发明人： Sangeeta Bhatia , Jing Shan , Michelle Palmer , Nathan Ross
IPC分类号： C07D263/24 , A61K31/4174 , A61K31/4409 , C07D213/75 , A01K67/027 , C07D209/88 , A61K31/137 , C07C211/32 , A61K31/4035 , C07D209/48 , A61K35/407 , A61K31/403
CPC分类号： C07D263/24 , A01K67/0278 , A01K2227/105 , A01K2267/0331 , A61K31/137 , A61K31/403 , A61K31/4035 , A61K31/4174 , A61K31/4409 , A61K35/407 , C07C211/32 , C07D209/48 , C07D209/88 , C07D213/75 , C12N5/067 , C12N2501/02 , C12N2501/115 , C12N2501/12 , C12N2501/155 , C12N2501/16 , C12N2501/237 , C12N2501/999 , C12N2503/02 , C12N2506/45 , C12N2533/90 , Y02A50/387 , Y02A50/463
摘要： The present invention provides methods of inducing proliferation of and/or differentiating cells comprising contacting cells with compounds within the methods of the invention. The present invention further provides cells obtainable by the methods of the invention. Liver disease affects more than 500 million people worldwide. Organ transplantation is the gold standard for treatment of liver failure, but organ shortages are acute.
摘要翻译：本发明提供诱导和/或分化细胞增殖的方法，包括在本发明的方法中使细胞与化合物接触。本发明还提供可通过本发明的方法获得的细胞。肝病影响全球5亿多人。器官移植是治疗肝衰竭的黄金标准，但器官短缺是急性的。

78. 发明申请

US20150361037A1 ACYLGUANIDINES FOR TREATING OSTEOARTHRITIS 有权
标题翻译：用于治疗OSTEOARTHRITIS的ACYLGUANIDINES
公开(公告)号：US20150361037A1
公开(公告)日：2015-12-17
申请号：US14760765
申请日：2013-12-16
申请人： MERCK PATENT GMBH
发明人： Christos TSAKLAKIDIS , Markus KLEIN , Paul CZODROWSKI
IPC分类号： C07C279/22 , A61K31/19 , A61K31/165 , C07D209/48 , A61K31/4035 , C07C311/46 , A61K31/18 , A61K31/277 , C07D213/58 , A61K31/4409 , A61K31/4402 , C07D257/04 , A61K31/41 , C07D323/02 , A61K31/36 , C07D307/68 , A61K31/341 , C07D333/24 , A61K31/381 , A61K31/44 , C07D309/14 , A61K31/351 , C07D211/98 , A61K31/4468 , C07D309/06 , C07D335/02 , A61K31/382 , C07D333/28 , C07D213/61 , C07D207/12 , A61K31/4015 , A61K31/401 , C07D295/15 , A61K31/5375 , A61K31/216 , C07D271/10 , A61K31/4245 , C07D285/06 , A61K31/433 , C07D233/58 , A61K31/4164 , C07D249/08 , A61K31/4196 , C07D231/12 , C07C277/08 , C07C53/18
CPC分类号： C07C279/22 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/36 , A61K31/381 , A61K31/382 , A61K31/401 , A61K31/4015 , A61K31/4035 , A61K31/41 , A61K31/4164 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4468 , A61K31/5375 , C07C53/18 , C07C277/08 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D207/16 , C07D207/267 , C07D207/273 , C07D209/48 , C07D211/58 , C07D211/98 , C07D213/40 , C07D213/56 , C07D213/58 , C07D213/61 , C07D231/12 , C07D233/58 , C07D233/61 , C07D249/08 , C07D257/04 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/28 , C07D285/06 , C07D295/15 , C07D307/68 , C07D309/06 , C07D309/14 , C07D317/58 , C07D317/60 , C07D323/02 , C07D333/20 , C07D333/24 , C07D333/28 , C07D335/02
摘要： The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.
摘要翻译：本发明涉及式（I）化合物，特别涉及包含至少一种式I化合物的药物，其用于治疗和/或预防触发组织蛋白酶D的生理和/或病理生理条件涉及，特别是用于治疗和/或预防骨关节炎，创伤性软骨损伤，关节炎，疼痛，异常性疼痛或痛觉过敏。

79. 发明授权

US09169276B2 Ethynylphenylamidine compound or salt thereof, method for producing same, and fungicide for agricultural and horticultural use 有权
标题翻译：乙炔基苯脒化合物或其盐，其制备方法和用于农业和园艺用途的杀真菌剂
公开(公告)号：US09169276B2
公开(公告)日：2015-10-27
申请号：US14253109
申请日：2014-04-15
申请人： OTSUKA AGRITECHNO CO., LTD.
发明人： Satoru Masumoto , Hitoshi Mutsutani , Sachi Kimura
IPC分类号： C07C211/45 , C07C211/51 , C07C211/52 , C07F7/10 , A01N37/52 , A01N43/10 , A01N43/38 , A01N43/40 , A01N47/42 , A01N55/00 , C07C257/10 , C07C257/12 , C07D209/48 , C07D213/58 , C07D333/20 , C07F7/08 , A01N33/00 , C07C215/68 , C07C275/12 , C07C335/32 , C07F7/18
CPC分类号： C07F7/10 , A01N33/00 , A01N37/52 , A01N43/10 , A01N43/38 , A01N43/40 , A01N47/42 , A01N55/00 , C07C211/45 , C07C211/52 , C07C215/68 , C07C257/10 , C07C257/12 , C07C275/12 , C07C335/32 , C07C2601/14 , C07D209/48 , C07D213/58 , C07D333/20 , C07F7/081 , C07F7/1804
摘要： An object of the present invention is to provide a novel fungicide having an excellent fungicidal activity. The compound used as the fungicide of the present invention is an ethynylphenylamidine compound or a salt thereof, the compound being represented by Formula (1): wherein R1 and R2 are each hydrogen or C1-12 alkyl, or R1 and R2 may be bonded together to form C1-7 alkylene; R3 is hydrogen or C1-4 alkylthio; R4, R5, R6, and R7 are each hydrogen, halogen, etc.; and R8 is hydrogen, C1-20 alkyl, C3-8 cycloalkyl, C1-4 haloalkyl, phenyl, a heterocyclic group, or —(CH2)n-Si(R9)(R10)(R11) wherein R9, R10, and R11 are each C1-6 alkyl, and n is an integer of 0 or 1.
摘要翻译：本发明的目的是提供一种具有优异杀真菌活性的新型杀真菌剂。用作本发明的杀真菌剂的化合物是乙炔基苯脒化合物或其盐，该化合物由式（1）表示：其中R 1和R 2各自为氢或C 1-12烷基，或者R 1和R 2可以结合在一起以形成C 1-7亚烷基; R3是氢或C1-4烷硫基; R4，R5，R6和R7各自为氢，卤素等; 或R 8为氢，C 1-20烷基，C 3-8环烷基，C 1-4卤代烷基，苯基，杂环基或 - （CH 2）n -Si（R 9）（R 10）（R 11）其中R 9，R 10和R 11 各为C 1-6烷基，n为0或1的整数。

80. 发明授权

US09079877B2 Process for preparing chiral compounds 有权
标题翻译：制备手性化合物的方法
公开(公告)号：US09079877B2
公开(公告)日：2015-07-14
申请号：US14135753
申请日：2013-12-20
申请人： Pfizer Inc.
发明人： David W Bauer , Padraig M O'Neill , Timothy J Watson , Shanghui Hu
IPC分类号： C07D405/06 , C07D209/48 , C07D319/08 , C12P7/62 , C12P13/00 , C12P13/02 , C12P17/10
CPC分类号： C07D405/06 , C07D209/48 , C07D319/08 , C12P7/62 , C12P13/001 , C12P13/02 , C12P17/10
摘要： The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.
摘要翻译：本发明涉及用于制备手性化合物的2-脱氧核糖-5-磷酸醛缩酶（DERA）化学酶法。

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