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No. Publication Number Title Publication/Patent Number Publication/Patent Number Publication Date Publication Date
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1
US2021023029A1
EDASALONEXENT DOSING REGIMEN FOR TREATING MUSCULAR DYSTROPHY
Publication/Patent Number: US2021023029A1 Publication Date: 2021-01-28 Application Number: 16/761,783 Filing Date: 2018-11-05 Inventor: Nichols, Andrew J.   Perlman, Michael   Assignee: Catabasis Pharmaceuticals, Inc.   IPC: A61K31/166 Abstract: The invention provides methods and compositions for treating a muscular dystrophy, e.g., Duchenne muscular dystrophy (DMD), in a subject, with a fatty acid acetylated salicylate, e.g., edasalonexent, effective to achieve a threshold plasma concentration of the fatty acid acetylated salicylate in the subject, e.g., a threshold plasma concentration of at least about 20 ng/ml for least 12 hours in a 24 hour period.
2
EP3784226A1
AMIDE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS AND METHODS OF TREATMENT
Publication/Patent Number: EP3784226A1 Publication Date: 2021-03-03 Application Number: 19791620.8 Filing Date: 2019-04-24 Inventor: Wang, Tong   Gately, Stephen   Assignee: TRANSLATIONAL DRUG DEVELOPMENT LLC   IPC: A61K31/166
3
CN112367982A
作为激酶抑制剂的酰胺化合物、组合物和治疗方法
Public
Publication/Patent Number: CN112367982A Publication Date: 2021-02-12 Application Number: 201980041940.6 Filing Date: 2019-04-24 Inventor: T·王   S·盖特利   Assignee: 转化药物开发有限责任公司   IPC: A61K31/166 Abstract: 本公开涉及某些酰胺和杂环化合物。本公开还涉及这些化合物抑制Rho相关蛋白激酶和治疗疾病的用途,所述疾病包括自身免疫性疾病、移植物抗宿主病(GVHD)、炎症、心血管疾病、中枢神经系统疾病和肿瘤性疾病。
4
CN112218627A
前药及其在医学上的应用
Public
Publication/Patent Number: CN112218627A Publication Date: 2021-01-12 Application Number: 201980036567.5 Filing Date: 2019-05-29 Inventor: 阿恩·海耶里克   苏菲·德舒梅克   索菲·蒂奥洛伊   多米尼克·瑟萨戈   菲力浦·朗班   Assignee: 康维尔特制药有限公司   IPC: A61K31/166 Abstract: 本发明涉及作为靶向肿瘤的细胞毒性剂的含氮芥取代的哌嗪甲酰胺及其相应的药学上可接受的盐,及其单独使用或与其它癌症疗法联合使用的方法。
5
US2021077487A1
PHARMACEUTICAL COMPOSITION CONTAINING HDAC6 INHIBITOR AS ACTIVE INGREDIENT FOR PREVENTION OR TREATMENT OF ITCHING
Publication/Patent Number: US2021077487A1 Publication Date: 2021-03-18 Application Number: 16/961,302 Filing Date: 2018-11-15 Inventor: Jang, Jun Ho   Yoon, Jeong Ah   Assignee: BNH RESEARCH CO.,LTD.   IPC: A61K31/505 Abstract: The present invention relates to a pharmaceutical composition containing an HDAC6 inhibitor as an active ingredient for prevention or treatment of itching. The present invention provides a novel pharmaceutical composition containing, as an active ingredient, an inhibitor for inhibiting an HDAC6 enzyme, and thus can effectively inhibit and treat itching caused by trypsin, tryptase, histamine, antimycin A, chloroquine, or the like.
6
US2021093605A1
METHODS FOR TREATMENT OF CLOSTRIDIUM DIFFICILE INFECTIONS
Publication/Patent Number: US2021093605A1 Publication Date: 2021-04-01 Application Number: 16/948,227 Filing Date: 2020-09-09 Inventor: Janda, Kim D.   Assignee: The Scripps Research Institute   IPC: A61K31/277 Abstract: In this study, we capitalized on the antimicrobial property and low oral bioavailability of known salicylanilide anthelmintics (closantel, rafoxanide, niclosamide, oxyclozanide) to target the gut pathogen. The anthelmintics displayed excellent potency against C. difficile strains 630 and 4118 (with MIC values as low as 0.06-0.13 μg/mL for rafoxanide) via a membrane depolarization mechanism. Interestingly, closantel, rafoxanide and compound 8 were bactericidal against logarithmic- and stationary-phase cultures of the BI/NAP1/027 strain 4118. Further evaluation of the salicylanilides showed their preferential activity against Gram-positive over Gram-negative bacteria. Moreover, the salicylanilides were non-hemolytic and were non-toxic to mammalian cell lines HepG2 and HEK 293T/17 within the range of their in vitro MICs and MBCs. The salicylanilide anthelmintics exhibit desirable bactericidal and pharmacokinetic properties and are amenable to repositioning as anti-C. difficile agents.
7
US10894837B2
MMP9 inhibitors and uses thereof in the prevention or treatment of a depigmenting disorder
Publication/Patent Number: US10894837B2 Publication Date: 2021-01-19 Application Number: 16/469,665 Filing Date: 2017-12-15 Inventor: Boniface, Katia   Seneschal, Julien   Boukhedouni, Nesrine   Jacquemin, Clement   Bernard, Francois-xavier   Assignee: UNIVERSITÉ DE BORDEAUX   INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)   CENTRE HOSPITALIER UNIVERSITAIRE DE BORDEAUX   IPC: A61P17/00 Abstract: The invention relates to the field of therapy, in particular dermatology. Inventors herein identify for the first time inhibitors of matrix metalloproteinase-9 (MMP9) as active molecules for use for preventing, treating or alleviating skin depigmenting disorders in a subject in need thereof, and describe compositions and kits comprising such inhibitors as well as uses thereof. Inventors further describe a method for screening pharmaceutically active molecules suitable for preventing, treating or alleviating a depigmenting disorder as well as methods for evaluating the efficacy of a depigmenting disorder treatment involving an inhibitor of MMP9 or for monitoring the course of depigmenting disorder in a subject exposed to such a treatment.
8
EP3759076A1
CRYSTALLINE FORM II OF DAROLUTAMIDE
Publication/Patent Number: EP3759076A1 Publication Date: 2021-01-06 Application Number: 19706651.7 Filing Date: 2019-02-25 Inventor: Adamer, Verena   Martin, Nolwenn   Thaler, Andrea   Werner, Veronika   Raneburger, Johannes   Schwarz, Franz Xaver   Legen, Igor   Jereb, Rebeka   Assignee: Sandoz AG   IPC: C07D231/14
9
US2021040265A1
CHEMICAL COMPOSITIONS WITH ANTIMICROBIAL FUNCTIONALITY
Publication/Patent Number: US2021040265A1 Publication Date: 2021-02-11 Application Number: 17/072,771 Filing Date: 2020-10-16 Inventor: Fevre, Mareva B.   Hedrick, James L.   Park, Nathaniel H.   Piunova, Victoria A.   Tan, Pang Kern Jeremy   Yang, Chuan   Yang, Yi Yan   Assignee: International Business Machines Corporation   AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH   IPC: C08G73/02 Abstract: Techniques regarding killing of a pathogen with one or more ionene compositions having antimicrobial functionality are provided. For example, one or more embodiments can comprise a method, which can comprise contacting a Mycobacterium tuberculosis microbe with a chemical compound. The chemical compound can comprise an ionene unit. Also, the ionene unit can comprise a cation distributed along a molecular backbone. The ionene unit can have antimicrobial functionality. The method can further comprise electrostatically disrupting a membrane of the Mycobacterium tuberculosis microbe in response to the contacting.
10
US2021015800A1
CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
Publication/Patent Number: US2021015800A1 Publication Date: 2021-01-21 Application Number: 17/032,626 Filing Date: 2020-09-25 Inventor: Arasappan, Ashok   Basile, Anthony S.   Bueters, Tjerk Johannes Helena   Eagan, Michael F.   Kim, Nancy Dohee   Marshall, Fiona Hamilton   Mukai, Yuki   Struyk, Arie   Uslaner, Jason Martin   Assignee: Merck Sharp & Dohme Corp.   IPC: A61K31/439 Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGuR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGuR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
11
CN107427431B
包含5-金刚烷-1-基-N-(2,4-二羟基苄基)-2,4-二甲氧基苯甲酰胺的抗氧化或抗老化组合物
Grant
Publication/Patent Number: CN107427431B Publication Date: 2021-04-13 Application Number: 201680020251.3 Filing Date: 2016-03-29 Inventor: 朱泳协   白兴洙   黄晶俄   李海光   金容震   申洪柱   李存恒   Assignee: 株式会社爱茉莉太平洋   IPC: A61K8/42 Abstract: 本说明书中公开的5‑金刚烷‑1‑基‑N‑(2,4‑二羟基苄基)‑2,4‑二甲氧基苯甲酰胺可以表现出优异的抗氧化和抗老化效果,同时不具有毒性。例如,所述组合物通过清除自由基或抑制MMP‑1的表达而表现出优异的抗氧化和抗老化效果。
12
US10898461B2
Salts of 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl) phenoxy]ethyli-1-benzofuran-2-carboxamide, related crystalline forms, method for preparing the same and pharmaceutical compositions containing the same
Publication/Patent Number: US10898461B2 Publication Date: 2021-01-26 Application Number: 16/676,911 Filing Date: 2019-11-07 Inventor: Gaillard, Marina   Letellier, Philippe   Assignee: Pharmacyclics LLC   IPC: A61K31/343 Abstract: Described herein are salts of 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofuran-2-carboxamide, in particular that of formula (I): wherein HA is naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, oxalic acid, benzenesulfonic acid, or sulfuric acid, or hydrates thereof, and crystalline forms thereof characterized by the powder X-ray diffraction diagram and the 13C CP/MAS NMR solid state spectrum. Also described are compositions, methods of use and preparation thereof.
13
US2021093590A1
NASAL FORMULATIONS OF METOCLOPRAMIDE
Publication/Patent Number: US2021093590A1 Publication Date: 2021-04-01 Application Number: 17/100,664 Filing Date: 2020-11-20 Inventor: D'onofrio, Matthew J.   Gonyer, David A.   Shah, Shirish A.   Madden, Stuart J.   Assignee: Evoke Pharma, Inc.   IPC: A61K31/166 Abstract: Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof.
14
US10919934B2
Compositions and methods for managing respiratory conditions
Publication/Patent Number: US10919934B2 Publication Date: 2021-02-16 Application Number: 16/922,564 Filing Date: 2020-07-07 Inventor: Koval, Michael   Schlingmann, Barbara   Assignee: Emory University   IPC: C07K7/06 Abstract: This disclosure relates to compositions for use in managing respiratory distress and related disorders. In certain embodiments, the disclosure relates to methods of treating or preventing respiratory distress comprising administering an effective amount of a pharmaceutical composition comprising peptides or agents disclosed herein to a subject in need thereof. In certain embodiments, the peptides or agents decrease the concentration of claudin-5 in cells and tissues of the lungs.
15
CN112368263A
二肽基酮酰胺间甲氧基苯基衍生物及其用途
Public
Publication/Patent Number: CN112368263A Publication Date: 2021-02-12 Application Number: 201980044841.3 Filing Date: 2019-05-03 Inventor: 赫苏斯·列那斯卡尔沃   米丽亚姆·劳尤伊科帕斯托   乌奈·埃莱斯卡诺多奈尔   恩里克·巴斯克斯塔泰   玛尔塔·梅尔加雷霍迪亚兹   玛尔塔·伊莎贝尔·巴兰科盖拉多   伊娃·马·梅迪纳福恩特斯   Assignee: 兰德施泰纳根梅德公司   IPC: C07C235/82 Abstract: 本发明涉及二肽基酮酰胺间甲氧基苯基衍生物及它们在治疗与升高的钙蛋白酶活性相关的疾病和状况中的用途,所述疾病和状况例如由梗塞、具有或没有再灌注的局部缺血引起的心脏损伤;神经退行性紊乱;疟疾;糖尿病肾病;由HIV病毒诱导的神经毒性;癌症;以及纤维化疾病。
16
US2021053909A1
NOVEL ANTIMICROBIAL COMPOUND AND USE THEREOF
Publication/Patent Number: US2021053909A1 Publication Date: 2021-02-25 Application Number: 17/092,949 Filing Date: 2020-11-09 Inventor: Kim, Won Gon   Kim, Hyun Ju   Kim, Yu Jin   Cho, Kyung Yun   Assignee: Korea Research Institute of Bioscience and Biotechnology   IPC: C07C233/75 Abstract: The present invention relates to: coralmycin A and B, which are novel compounds exhibiting antimicrobial activity, an isomer thereof, a derivative thereof or a pharmaceutically acceptable salt thereof; a microorganism of the genus Corallococcus producing the same; and an antimicrobial use thereof. The coralmycin A and B have very strong antimicrobial activity against antibiotic-resistant bacteria such as MRSA, QRSA, VRE, VISA, etc.; Acinetobacter baumannii, which is a multidrug-resistant microorganism; and also against gram-positive microorganisms and gram-negative microorganisms. Therefore, the present invention can be very useful for prevention, treatment and alleviation of various microbial infections, and thus can be widely applied to the medical supply, quasi-drug, food, and feed industries.
17
US2021024457A1
DIAMIDE ANTIMICROBIAL AGENTS
Publication/Patent Number: US2021024457A1 Publication Date: 2021-01-28 Application Number: 16/937,933 Filing Date: 2020-07-24 Inventor: Basu, Amit   Reid, Christopher W.   Iwasaki, Nola Camille   Prete, Joseph   Assignee: BROWN UNIVERSITY   BRYANT UNIVERSITY   IPC: C07C233/92 Abstract: This invention is directed to compounds of Formula (I) pharmaceutically acceptable salts, esters, and prodrugs thereof, to their preparation, to pharmaceutical compositions comprising compounds of Formula I, and to their uses as antimicrobial agents.
18
US2021023183A1
METHODS FOR TREATING AND PREVENTING NEUTROPHIL-DERIVED NET TOXICITY AND THROMBOSIS
Publication/Patent Number: US2021023183A1 Publication Date: 2021-01-28 Application Number: 17/061,624 Filing Date: 2020-10-02 Inventor: Wagner, Denisa D.   Fuchs, Tobias A.   De, Meyer Simon   Martinod, Kimberly   Brill, Alexander   Thomas, Grace M.   Assignee: CHILDREN'S MEDICAL CENTER CORPORATION   IPC: A61K38/46 Abstract: Embodiments of the technology described herein are based upon the discoveries that neutrophil extracellular traps (NETs) provide a stimulus for thrombus formation and that NETs are present in stored blood products. Accordingly, some embodiments relate to methods of treating and preventing toxicity of NETs and thrombosis caused by NETs. Additional embodiments are directed towards methods of treating stored blood products to prevent transfusion-related injuries.
19
CN112315933A
一种溶解度高的包衣片剂
Substantial Examination
Publication/Patent Number: CN112315933A Publication Date: 2021-02-05 Application Number: 202011047866.X Filing Date: 2020-09-29 Inventor: 蒋锋   周健   张春洁   扶文君   陆光玮   Assignee: 江苏鹏鹞药业有限公司   IPC: A61K9/36 Abstract: 本发明公开了一种溶解度高的包衣片剂,包括主药片剂及包覆在主要片剂外周的一层包衣,所述包衣由二氧化钛、硬脂酸镁羟丙基甲基纤维素和玉米油组成。本发明采用二氧化钛代替滑石粉,一方面可以防止药物颗粒的黏连,另一反面不会影响包衣的酸碱性,使药品可以顺利进入肠道;采用硬脂酸镁羟丙基甲基纤维素作为包衣的另一主要材料,可以有效提高包衣在肠道内的溶解度,使药品更易被吸收。
20
EP3758689A1
METHODS OF PREVENTING AND TREATING HYPOGLYCEMIA IN TYPE 1 AND TYPE 2 DIABETES PATIENTS
Publication/Patent Number: EP3758689A1 Publication Date: 2021-01-06 Application Number: 19759952.5 Filing Date: 2019-02-28 Inventor: Harp, Joyce B.   Assignee: Ferox Therapeutics LLC   IPC: A61K31/075
Total 500 pages