-
51.发明申请AMIDE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF AND MEDICINAL APPLICATION THEREOF 审中-公开酰胺衍生物及其药学上可接受的盐，其制备方法及药物应用公开(公告)号：US20170037044A1
公开(公告)日：2017-02-09
申请号：US15303704
申请日：2015-03-31
发明人： Xin LI , Wei HE , Xianbo LIU , Bin WANG , Qiyue HU , Fangfang JIN , Qing DONG , Piaoyang SUN
IPC分类号： C07D471/04 , C07D209/10 , C07D231/56 , C07D263/57 , C07D235/18 , C07D209/44 , C07D405/12 , C07D405/14 , C07D401/04 , C07D417/12 , C07D401/12 , C07D413/12
CPC分类号： C07D471/04 , C07C233/47 , C07C233/63 , C07C2601/02 , C07D209/10 , C07D209/44 , C07D231/56 , C07D235/18 , C07D263/57 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof are provided. Specifically, amide derivatives represented by general formula (I) are provided. The amide derivatives represented by general formula (I) can be used as a therapeutic agent, particularly as an inhibitor for microsomal prostaglandin E synthase-1 (mPGES-1), and also to treat and/or prevent diseases or illnesses such as inflammation and/or pain etc. The definition of each substituent group in general formula (I) is the same as the definition in the description.
摘要翻译： 本发明涉及酰胺衍生物及其药学上可接受的盐，其制备方法和药物应用。 具体地说，本发明涉及由通式（I）表示的酰胺衍生物，其制备方法，含有该衍生物的药物组合物及其作为治疗剂的用途，特别是作为微粒体前列腺素E合成酶-1（mPGES-1）抑制剂， 并且用于制备用于治疗和/或预防诸如炎症和/或疼痛等疾病或疾病的药物。通式（I）中每个取代基的定义与描述中的定义相同。
-
52.发明授权公开(公告)号：US09527851B2
公开(公告)日：2016-12-27
申请号：US14365497
申请日：2012-12-19
发明人： Xuejun Zhang , Qing Dong , Bonian Liu , Yaoping Zhu , Xiaotao Li , Jiong Lan
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61K45/06 , C07D471/04 , A61K31/437 , C07D217/06 , C07D221/04 , C07D209/44 , C07D209/52 , C07D403/04
CPC分类号： C07D487/04 , A61K45/06 , C07D209/44 , C07D209/52 , C07D217/06 , C07D221/04 , C07D403/04 , C07D471/04
摘要： The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered heteroaryl ring derivative as represented by formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic method using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in the description.
摘要翻译： 本发明涉及吡咯六元杂芳环衍生物及其制备方法及其药用用途。 具体地说，本发明涉及式（I）所示的新的吡咯六元杂环衍生物及其制备方法，包含该衍生物的药物组合物和使用该衍生物的治疗剂，特别是其用途 作为JAK抑制剂和免疫抑制剂。 式（I）中的基团与描述中的定义相同。
-
53.发明授权Cyclic amide derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase and uses thereof 有权作为11-β-羟基类固醇脱氢酶抑制剂的环状酰胺衍生物及其用途公开(公告)号：US09453014B2
公开(公告)日：2016-09-27
申请号：US14367614
申请日：2012-12-21
发明人： Jagannath Madanahalli Ranganath Rao , Uppala Venkatesham , Jenson George , George Fernand , Sivanageswara Rao Doppalapudi , G R Madhavan , Nagarajan Arumugam , Mohammed Ansari , K Murugavel , Jidugu Pradeep , Sulthan Allavuddeen , K Vijayaramalingam , Hampelingaiah Shiva Prasad , Augustine Michael Raj , S Gnanavel , Ramamoorthy Kottamalai , Naresh M P S Babu , Bommegowda Yadaganahalli Kenchegowda
IPC分类号： C07D471/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D417/12 , C07D417/06 , C07D209/44 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06
CPC分类号： C07D471/04 , C07D209/44 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/12
摘要： The present invention relates amide compounds of formula (I): wherein R1, R1a, Ar, A, B, W1, W2, D, a, b, and c are defined herein, and pharmaceutical acceptable salts thereof. These compounds have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.
-
54.发明申请公开(公告)号：US20160264518A1
公开(公告)日：2016-09-15
申请号：US15067605
申请日：2016-03-11
发明人： Kenneth W Bair , Nicholas Barczak , Bingsong Han , David R. Lancia, JR. , Cuixian Liu , Matthew W Martin , Pui Yee Ng , Aleksandra Rudnitskaya , Jennifer R Thomason , Mary Margaret Zablocki , Xiaozhang Zheng
IPC分类号： C07C259/06 , C07D221/20 , A61K31/438 , A61K31/277 , C07D209/44 , A61K31/4035 , C07D295/155 , A61K31/451 , C07D471/10 , A61K31/435 , C07D487/10 , A61K31/407 , C07D495/10 , A61K31/397 , C07D235/14 , A61K31/4184 , C07C275/38 , C07D233/68 , A61K31/417 , C07D213/56 , A61K31/44 , C07D241/08 , A61K31/495 , C07D417/04 , A61K31/4439 , A61K31/5377 , C07D471/04 , A61K31/185
CPC分类号： C07C259/06 , A61K31/185 , A61K31/277 , A61K31/397 , A61K31/4035 , A61K31/407 , A61K31/417 , A61K31/4184 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/4439 , A61K31/451 , A61K31/495 , A61K31/5377 , C07D207/10 , C07D207/267 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/46 , C07D211/16 , C07D211/58 , C07D213/56 , C07D213/65 , C07D213/75 , C07D213/81 , C07D215/12 , C07D221/20 , C07D231/14 , C07D231/18 , C07D233/36 , C07D233/38 , C07D233/68 , C07D235/14 , C07D235/30 , C07D239/20 , C07D239/22 , C07D241/08 , C07D241/12 , C07D249/18 , C07D257/04 , C07D261/18 , C07D277/56 , C07D295/155 , C07D295/192 , C07D307/68 , C07D317/68 , C07D333/70 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D493/08 , C07D495/10 , C07D498/04 , C07D513/10
摘要： The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
摘要翻译： 本发明涉及可用于治疗癌症和其它疾病和病症的组蛋白脱乙酰酶抑制剂，特别是HDAC8的抑制剂，以及所述抑制剂的合成和应用。
-
公开(公告)号：US20160251351A1
公开(公告)日：2016-09-01
申请号：US15147201
申请日：2016-05-05
申请人： The Broad Institute, Inc. , The General Hospital Corporation d/b/a Massachusetts General Hospital , Massachusetts Institute of Technology
发明人： Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Li-Huei Tsai , Stephen J. Haggarty , Yan-Ling Zhang
IPC分类号： C07D471/04 , A61K31/167 , C07D211/62 , A61K31/445 , C07D295/195 , A61K31/437 , C07D211/34 , C07D209/44 , A61K31/4035 , C07D209/52 , A61K31/403 , C07C237/24 , A61K31/402
CPC分类号： C07D491/107 , A61K31/167 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/397 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4178 , A61K31/437 , A61K31/439 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/519 , A61K31/5377 , C07C211/52 , C07C233/42 , C07C233/43 , C07C233/56 , C07C233/62 , C07C235/82 , C07C237/20 , C07C237/24 , C07C271/28 , C07C275/30 , C07C275/40 , C07C281/06 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/50 , C07D205/04 , C07D205/06 , C07D209/44 , C07D209/52 , C07D211/22 , C07D211/34 , C07D211/62 , C07D213/40 , C07D213/56 , C07D231/04 , C07D237/04 , C07D241/12 , C07D295/185 , C07D295/195 , C07D309/08 , C07D311/04 , C07D311/82 , C07D333/20 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/08 , C07D493/08
摘要： The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R1a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物，溶剂合物或前药，其中U，J，V，X，R 1a，R 2b，R 2c，R 5和t如本文所述。 本发明一般涉及组蛋白脱乙酰酶的抑制剂及其制备和使用方法。 这些化合物可用于促进认知功能和增强学习和记忆形成。 此外，这些化合物可用于治疗，减轻和/或预防各种病症，包括例如神经障碍，记忆和认知功能障碍/损伤，灭绝学习障碍，真菌疾病和感染，炎性疾病，血液疾病和 人类和动物中的肿瘤性疾病。
-
公开(公告)号：US09422332B2
公开(公告)日：2016-08-23
申请号：US14419288
申请日：2013-08-06
IPC分类号： C07D405/06 , C07D409/12 , C07D209/44 , C07K5/083 , C07D217/26 , C07D401/12
CPC分类号： C07K5/0806 , C07D209/44 , C07D217/26 , C07D401/12 , C07D405/06 , C07D409/12
摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, m, n and q are described in this application, and methods of using said compounds in the treatment of cancer.
摘要翻译： 公开了式（I）的化合物或其药学上可接受的盐，其中本申请中描述了R1，R2，R3，m，n和q，以及使用所述化合物治疗癌症的方法。
-
公开(公告)号：US09412955B2
公开(公告)日：2016-08-09
申请号：US14797646
申请日：2015-07-13
IPC分类号： H01L51/54 , C09K11/06 , H01L51/00 , C07D209/44 , C07D401/14 , H01L51/50
CPC分类号： H01L51/0072 , C07D209/44 , C07D401/14 , C09K11/06 , C09K2211/1007 , C09K2211/1018 , C09K2211/1029 , C09K2211/18 , H01L51/0067 , H01L51/0077 , H01L51/5012
摘要： The present invention provides a new class of excited state intramolecular charge transfer (ESIPT) dye compounds based on mono or dihydroxy substituted 1,3-bisiminoisoindole motif and metal complexes containing such compounds as ligands. The present invention also provides OLEDs containing the compound and/or metal complex as the emissive material.
-
公开(公告)号：US20160137601A1
公开(公告)日：2016-05-19
申请号：US14944662
申请日：2015-11-18
IPC分类号： C07D209/44 , C08G65/34 , G01N33/44
CPC分类号： C07D209/44 , C07D403/14 , C08G65/34 , G01N33/442 , G01N33/5306 , G01N33/582
摘要： Method for producing an isoindole derivative, the isoindole derivative obtainable by the methods, a methods for stabilizing an isoindole derivative, and methods for detection and/or quantification of macromolecules.
摘要翻译： 异吲哚衍生物的制造方法，通过该方法得到的异吲哚衍生物，异吲哚衍生物的稳定化方法以及大分子的检测和/或定量方法。
-
59.发明申请NOVEL 3-(4(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING METABOLIC DISEASE INCLUDING SAME AS EFFECTIVE INGREDIENT 有权新型3-（4（苄氧基）苯基）十四烷酸衍生物，其制备方法和用于预防和治疗包括其有效成分的代谢疾病的药物组合物公开(公告)号：US20160024063A1
公开(公告)日：2016-01-28
申请号：US14872745
申请日：2015-10-01
发明人： Jin Yang , Jin Woong Kim , Han Kyu Lee , Jae Hyun Kim , Chang Mo Son , kyu hwan Lee , Hyung-Ho Choi , daehoon Kim , Tae-Young Ha , Jaekeol Rhee
IPC分类号： C07D413/04 , C07C59/90 , C07C59/72 , C07D209/44 , C07D211/70 , C07D295/096 , C07D271/07 , C07D217/04 , C07D295/155 , C07D217/24 , C07D211/14 , C07D215/04 , C07D277/82 , C07D239/28 , C07D213/74 , C07D207/06 , C07C51/373 , C07C51/367 , C07D317/72
CPC分类号： C07D413/04 , C07C51/367 , C07C51/373 , C07C59/72 , C07C59/90 , C07D207/06 , C07D209/44 , C07D211/14 , C07D211/70 , C07D213/74 , C07D213/85 , C07D215/04 , C07D215/06 , C07D217/04 , C07D217/24 , C07D221/20 , C07D239/28 , C07D239/42 , C07D271/07 , C07D277/82 , C07D295/073 , C07D295/096 , C07D295/155 , C07D317/72
摘要： The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.
摘要翻译： 本发明涉及一种新型的3-（4-（苄氧基）苯基）己-4-烯酸衍生物及其制备方法，以及包含其作为预防和治疗代谢性疾病的活性成分的药物组合物。 本发明的新型3-（4-（苄氧基）苯基）己-4-烯酸衍生物，其旋光异构体或其药学上可接受的盐具有优异的活化GPR40蛋白并相应地促进胰岛素分泌，但没有 与其他药物共同给药时的毒性。 也就是说，本发明的新型3-（4-（苄氧基）苯基）己-4-烯酸衍生物，其旋光异构体或其药学上可接受的盐可以与其它药物共同给药， 可以显着地激活GPR40蛋白质，使得包含与活性成分相同的组合物可以有效地用作预防和治疗代谢疾病如肥胖症，I型糖尿病，II型糖尿病，不相容的葡萄糖耐量，胰岛素 高血糖症，高脂血症，高甘油三酯血症，高胆固醇血症，血脂异常，X综合征等。
-
60.发明申请4-CARBOXAMIDO-ISOINDOLINONE DERIVATIVES AS SELECTIVE PARP-1 INHIBITORS 审中-公开作为选择性PARP-1抑制剂的4-CARBOXAMIDO-ISOINDOLINONE衍生物公开(公告)号：US20150274662A1
公开(公告)日：2015-10-01
申请号：US14438410
申请日：2013-10-23
发明人： Gianluca Mariano Enrico Papeo , Mikhail Yurievitch Krasavin , Paolo Orsini , Alessandra Scolaro
IPC分类号： C07D209/44 , C07D401/06 , A61K31/4725 , A61K31/4188 , A61K31/5377 , A61K31/4439 , A61K31/496 , A61K31/4035 , A61K31/454
CPC分类号： C07D209/44 , A61K31/4035 , A61K31/4188 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , C07D209/46 , C07D401/06 , C07D401/14 , C07D403/02 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14
摘要： There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
摘要翻译： 提供取代的4-甲酰氨基 - 异二氢吲哚酮衍生物，其选择性地抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性。 因此，本发明的化合物可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症的疾病。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。
-
-
-
-
-
-
-
-
-
搜索结果
1020 条记录 (耗时 0.06 秒)
