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1. 发明申请

US20180290976A1 LSD1 INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：US20180290976A1
公开(公告)日：2018-10-11
申请号：US15567978
申请日：2016-04-22
申请人： Constellation Pharmaceuticals, Inc.
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Côté , Martin Duplessis , Victor S. Gehling , Jean-Christophe Harmange , Rishi G. Vaswani
IPC分类号： C07D211/26 , C07D211/58 , C07C211/40 , C07D213/38 , C07C229/10 , C07D213/73 , C07C255/58 , C07D211/76 , C07D401/06 , C07C215/42 , C07C233/41 , C07C217/08 , C07C237/06 , C07D295/195 , C07C229/38 , C07C255/30 , C07D213/69 , C07D305/06
CPC分类号： C07D211/26 , A61P35/00 , C07B2200/07 , C07C211/09 , C07C211/36 , C07C211/40 , C07C215/14 , C07C215/42 , C07C215/44 , C07C217/08 , C07C229/10 , C07C229/38 , C07C229/46 , C07C233/41 , C07C237/06 , C07C255/24 , C07C255/30 , C07C255/58 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/44 , C07D205/12 , C07D207/32 , C07D211/22 , C07D211/36 , C07D211/58 , C07D211/76 , C07D213/38 , C07D213/64 , C07D213/69 , C07D213/73 , C07D215/44 , C07D239/30 , C07D263/32 , C07D295/195 , C07D305/06 , C07D309/20 , C07D317/28 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D417/06
摘要： Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.

2. 发明申请

US20160369087A1 EPOXY-AMINE ADDUCT, RESIN COMPOSITION, SIZING AGENT, CARBON FIBER COATED WITH SIZING AGENT, AND FIBER-REINFORCED COMPOSITE MATERIAL 审中-公开
公开(公告)号：US20160369087A1
公开(公告)日：2016-12-22
申请号：US15191041
申请日：2016-06-23
申请人： DAICEL CORPORATION
发明人： Masanori SAKANE
IPC分类号： C08K5/17 , C08J5/24 , C07C215/44 , C08J5/06
CPC分类号： C08K5/17 , C07C215/44 , C07C2601/14 , C07D303/36 , C08G59/1477 , C08G59/184 , C08G59/24 , C08J5/06 , C08J5/24 , C08J2363/02 , Y10T428/2918
摘要： Provided is an epoxy-amine adduct that offers high reactivity, contributes to better adhesion between a resin and a reinforcing fiber in a fiber-reinforced composite material, and can be easily blended with another component such as a resin. The epoxy-amine adduct has two or more amino groups per molecule and is obtained by a reaction of an epoxy compound (A) having two or more alicyclic epoxy groups per molecule with an amine compound (B) having two or more amino groups per molecule. The epoxy compound (A) is preferably a compound represented by Formula (a):

3. 发明申请

US20150329491A1 FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：氟化合物及其药物用途
公开(公告)号：US20150329491A1
公开(公告)日：2015-11-19
申请号：US14484666
申请日：2014-09-12
申请人： JAPAN TOBACCO INC.
发明人： Takahisa MOTOMURA , Hironobu NAGAMORI , Koichi SUZAWA , Hirotsugu ITO , Toru MORITA , Satoru KOBAYASHI , Hisashi SHINKAI
IPC分类号： C07D231/12
CPC分类号： C07D205/04 , A61K31/045 , A61K31/05 , A61K31/085 , A61K31/10 , A61K31/121 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/192 , A61K31/235 , A61K31/277 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4523 , A61K31/5375 , C07C35/52 , C07C39/42 , C07C43/23 , C07C43/253 , C07C49/83 , C07C59/56 , C07C59/72 , C07C65/17 , C07C69/712 , C07C69/732 , C07C69/76 , C07C215/44 , C07C215/70 , C07C217/20 , C07C233/18 , C07C233/25 , C07C235/42 , C07C235/66 , C07C255/12 , C07C255/53 , C07C259/10 , C07C271/16 , C07C271/30 , C07C311/04 , C07C317/22 , C07C2603/18 , C07D207/04 , C07D211/06 , C07D213/30 , C07D213/56 , C07D231/12 , C07D239/26 , C07D249/08 , C07D257/04 , C07D263/32 , C07D271/06 , C07D271/10 , C07D275/02 , C07D295/08 , C07D295/18 , C07D295/192 , C07D333/22 , C07D401/06 , C07D401/12 , C07D403/12 , C07F7/081
摘要： The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
摘要翻译：本发明提供了用于预防或治疗糖尿病，糖尿病并发症，胰岛素抵抗综合征，代谢综合征，高血糖症，血脂异常，动脉粥样硬化，心力衰竭，心肌病，心肌缺血，脑缺血，脑中风，肺动脉高压，高乳酸血症，线粒体疾病，线粒体性脑病或癌症，即PDHK抑制剂等。由下式[I]表示的化合物或其药学上可接受的盐或其溶剂化物：其中每个符号如说明书中所定义。

4. 发明授权

US09073819B2 Compositions, methods of use, and methods of treatment 有权
标题翻译：组合物，使用方法和治疗方法
公开(公告)号：US09073819B2
公开(公告)日：2015-07-07
申请号：US14128310
申请日：2012-06-29
申请人： Jahanshah Amin , Kirpal S. Bisht , Meghanath Gali
发明人： Jahanshah Amin , Kirpal S. Bisht , Meghanath Gali
IPC分类号： A61K31/357 , C07C215/44 , C07D317/72 , C07C211/40 , C07C217/52 , C07C325/02 , C07C251/20 , C07C251/44 , C07C323/30
CPC分类号： C07C215/44 , C07C211/40 , C07C217/52 , C07C251/20 , C07C251/44 , C07C323/30 , C07C325/02 , C07C2601/14 , C07D317/72
摘要： Embodiments of the present disclosure provide compositions including ketamine analogs, salts, and disalts, pharmaceutical compositions including ketamine analogs, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
摘要翻译：本公开的实施方案提供了包含氯胺酮类似物，盐和糖的组合物，包括氯胺酮类似物，盐或糖的药物组合物，治疗病症或疾病的方法，使用组合物或药物组合物的治疗方法等。

5. 发明授权

US09034868B2 Inhibitors of the shiga toxins trafficking through the retrograde pathway 有权
标题翻译：通过逆行通路抑制志贺毒素的运输
公开(公告)号：US09034868B2
公开(公告)日：2015-05-19
申请号：US14083690
申请日：2013-11-19
申请人： Commissariat A L'Energie Atomique Et Aux Ene Alt. , Institut Curie , Centre National De La Recherche Scientifique
发明人： Daniel Gillet , Julien Barbier , Ludger Johannes , Bahne Stechmann , Siau-Kun Bai
IPC分类号： C07D243/12 , C07D243/24 , C07D487/04 , A61K31/167 , A61K31/341 , A61K31/5513 , C07C211/27 , C07C215/10 , C07C215/42 , C07C215/44 , C07C217/16 , C07C217/58 , C07C229/14 , C07C229/22 , C07C229/38 , C07C229/48 , C07C233/06 , C07C233/65 , C07C237/40 , C07C251/24 , C07C271/56 , C07C275/28 , C07D209/14 , C07D213/38 , C07D215/12 , C07D233/10 , C07D233/58 , C07D233/61 , C07D235/08 , C07D249/06 , C07D307/42 , C07D317/58 , C07D317/62 , C07D317/66 , C07D333/20 , C07D401/04 , C07D453/02 , C07D471/08
CPC分类号： C07D453/02 , A61K31/167 , A61K31/341 , A61K31/5513 , C07C211/27 , C07C211/38 , C07C215/10 , C07C215/42 , C07C215/44 , C07C217/16 , C07C217/58 , C07C229/14 , C07C229/22 , C07C229/38 , C07C229/48 , C07C233/06 , C07C233/58 , C07C233/65 , C07C237/40 , C07C251/24 , C07C271/56 , C07C275/28 , C07C317/14 , C07C335/02 , C07C2601/08 , C07C2602/46 , C07C2603/74 , C07D209/14 , C07D213/38 , C07D215/12 , C07D233/10 , C07D233/58 , C07D233/61 , C07D233/64 , C07D235/08 , C07D243/12 , C07D243/24 , C07D245/06 , C07D249/06 , C07D307/42 , C07D307/52 , C07D317/46 , C07D317/58 , C07D317/62 , C07D317/66 , C07D333/20 , C07D401/04 , C07D451/02 , C07D471/08 , C07D487/04 , Y02A50/471 , Y02A50/473
摘要： The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.
摘要翻译：本发明涉及通式（I）和（II）的化合物在制备用于预防和/或治疗志贺毒素和相关毒素引起的疾病的药物中的应用。

6. 发明授权

US08829196B2 TRPA1 antagonists 有权
标题翻译： TRPA1拮抗剂
公开(公告)号：US08829196B2
公开(公告)日：2014-09-09
申请号：US13499844
申请日：2010-09-28
申请人： Mark T. Bilodeau , Melissa Egbertson , Ahren Green , John C. Hartnett , Yiwei Li
发明人： Mark T. Bilodeau , Melissa Egbertson , Ahren Green , John C. Hartnett , Yiwei Li
IPC分类号： C07D215/38 , C07C215/20 , C07C211/34 , C07C25/02 , A61K31/133
CPC分类号： C07C215/20 , A61K31/133 , C07C25/02 , C07C211/34 , C07C215/44 , C07C255/58 , C07C2602/10 , C07D215/38 , C07D215/44 , C07D311/74 , C07D311/76 , C07D405/04 , C07D405/06
摘要： The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.
摘要翻译：本发明涉及调节至少一种TRP家族成员的组合物和方法。具体地说，本发明涉及新型TRPA1拮抗剂及其用于治疗慢性炎性和神经性疼痛等疼痛的用途。可以调节一种或多种TRPA1功能的化合物在许多方面是有用的，包括但不限于维持钙稳态; 维持钠稳态; 调节细胞内钙含量; 调节膜极化（膜电位）; 调节阳离子水平; 和/或治疗或预防与钙稳态相关的疾病，病症或病症，钠稳态，钙或钠血管平衡，或膜极化/超极化（包括低钠和过度兴奋性）和/或治疗或预防与疾病，病症或病症相关与TRPA1表达或功能调节或失调。本发明还涉及拮抗TRPA1的功能和一种或多种另外的TRP通道的功能的方法和组合物。

7. 发明申请

US20140066409A1 CYCLOHEXANE COMPOUNDS AND THEIR USE AS ANTIBIOTICS 有权
标题翻译：环己烷化合物及其作为抗生素的用途
公开(公告)号：US20140066409A1
公开(公告)日：2014-03-06
申请号：US13990801
申请日：2011-12-13
申请人： UNIVERSITÄT KONSTANZ , RHEINISCHE FRIEDRICH-WILHELMS UNIVERSITÄT BONN
发明人： Günter Mayer , Christina Elsbeth Luense , Valentin Wittmann , Magnus S. Schmidt
IPC分类号： C07F9/44 , C07C215/44
CPC分类号： C07F9/44 , A61K31/13 , A61K31/66 , C07C211/25 , C07C215/42 , C07C215/44 , C07C233/23 , C07C2601/14 , C07F9/117 , C07F9/5304
摘要： The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as an antibiotic.
摘要翻译：本发明涉及根据通式（I）的化合物，包含根据通式（I）的化合物的药物组合物以及用于治疗细菌感染，特别是用作抗生素的化合物的用途。

8. 发明申请

US20130116453A1 ORDERED MESOPOROUS TITANOSILICATE AND THE PROCESS FOR THE PREPARATION THEREOF 有权
标题翻译：订购的多酯钛酸酯及其制备方法
公开(公告)号：US20130116453A1
公开(公告)日：2013-05-09
申请号：US13811235
申请日：2011-07-20
申请人： Srinivas Darbha , Anuj Kumar
发明人： Srinivas Darbha , Anuj Kumar
IPC分类号： B01J21/06 , C07C215/70 , C07C249/04 , C07C215/68 , C07D301/19 , C07C37/60
CPC分类号： B01J21/063 , B01J29/89 , C01B37/005 , C07B2200/09 , C07C37/60 , C07C213/04 , C07C215/68 , C07C215/70 , C07C249/04 , C07C2601/14 , C07D301/14 , C07D301/19 , C07C39/14 , C07C251/44 , C07C215/44 , C07C215/16
摘要： The invention discloses three-dimensional, ordered, mesoporous titanosilicates wherein the Ti is in a tetrahedral geometry and exclusively substituted for Si in the silica framework. Such titanosilicates find use as catalysts for epoxidation, hydroxylation, C—H bond oxidation, oxidation of sulfides, aminolysis of epoxide and amoximation, with approx. 100% selectivity towards the products.
摘要翻译：本发明公开了三维有序的中孔钛硅酸盐，其中Ti是四面体几何形状，并且仅在二氧化硅框架中代替Si。这种钛硅酸盐可用作环氧化，羟基化，C-H键氧化，硫化物氧化，环氧化物的氨解和氨肟化的催化剂。对产品的100％选择性。

9. 发明授权

US08329676B2 Cycloalkane-containing sphingosine 1-phosphate agonists 有权
标题翻译：含环烷烃的鞘氨醇1-磷酸激动剂
公开(公告)号：US08329676B2
公开(公告)日：2012-12-11
申请号：US12834884
申请日：2010-07-12
申请人： Kevin R. Lynch , Timothy L. Macdonald
发明人： Kevin R. Lynch , Timothy L. Macdonald
IPC分类号： A61K31/661 , A61K31/133 , C07F9/09 , C07C215/44
CPC分类号： C07D207/22 , C07C215/44 , C07D207/14 , C07D231/04 , C07D275/03 , C07D307/22 , C07F9/094 , C07F9/3882 , C07F9/547
摘要： The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type, which alter lymphocyte trafficking. The compounds of the invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.
摘要翻译：本发明提供了鞘氨醇-1-磷酸类似物，其是一种或多种S1P受体，特别是S1P1受体类型的有效和选择性激动剂，其改变淋巴细胞运输。本发明的化合物包括具有磷酸酯部分的化合物以及具有水解抗性的磷酸酯替代物如膦酸盐，α-取代的膦酸盐和磷酸三乙酯的化合物。

10. 发明申请

US20120283249A1 Novel compounds which have a protective activity with respect to the action of toxins and of viruses with an intracellular mode of action 审中-公开
标题翻译：对毒素和具有细胞内作用模式的病毒的作用具有保护作用的新型化合物
公开(公告)号：US20120283249A1
公开(公告)日：2012-11-08
申请号：US12999576
申请日：2009-06-17
申请人： Roman Lopez , Séverine Hebbe , Daniel Gillet , Julien Barbier
发明人： Roman Lopez , Séverine Hebbe , Daniel Gillet , Julien Barbier
IPC分类号： A61K31/137 , C07C211/29 , C07C215/50 , C07C217/58 , C07C229/38 , A61K31/24 , C07D213/38 , A61K31/4402 , A61K31/4406 , A61K31/4409 , C07D307/52 , A61K31/341 , C07D333/20 , A61K31/381 , C07D233/64 , A61K31/417 , C07D215/12 , A61K31/47 , C07D451/02 , A61K31/46 , C07D243/24 , A61K31/5513 , C07D243/12 , A61K31/551 , C07D487/04 , A61K31/138 , A61K31/166 , A61K31/18 , A61P39/02 , A61P31/12 , C07C211/27
CPC分类号： C07D453/02 , A61K31/167 , A61K31/341 , A61K31/5513 , C07C211/27 , C07C211/38 , C07C215/10 , C07C215/42 , C07C215/44 , C07C217/16 , C07C217/58 , C07C229/14 , C07C229/22 , C07C229/38 , C07C229/48 , C07C233/06 , C07C233/58 , C07C233/65 , C07C237/40 , C07C251/24 , C07C271/56 , C07C275/28 , C07C317/14 , C07C335/02 , C07C2601/08 , C07C2602/46 , C07C2603/74 , C07D209/14 , C07D213/38 , C07D215/12 , C07D233/10 , C07D233/58 , C07D233/61 , C07D233/64 , C07D235/08 , C07D243/12 , C07D243/24 , C07D245/06 , C07D249/06 , C07D307/42 , C07D307/52 , C07D317/46 , C07D317/58 , C07D317/62 , C07D317/66 , C07D333/20 , C07D401/04 , C07D451/02 , C07D471/08 , C07D487/04 , Y02A50/471 , Y02A50/473
摘要： The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
摘要翻译：本发明的主题是芳族胺，亚胺，氨基金刚烷和苯并二氮杂衍生物的化合物的新型家族，包含其的药物及其作为具有细胞内活性的毒素的毒性作用的抑制剂的用途，例如蓖麻毒素以及使用内源化途径感染细胞的病毒。

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