序号 | 专利名 | 申请号 | 申请日 | 公开(公告)号 | 公开(公告)日 | 发明人 |
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81 | SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIITORS | EP12823540.5 | 2012-08-15 | EP2744330B1 | 2020-07-15 | VANKAYALAPATI, Hariprasad; SORNA, Venkataswamy; WARNER, Steve, L.; BEARSS, David, J.; SHARMA, Sunil; STEPHENS, Bret |
82 | SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIITORS | EP12823540 | 2012-08-15 | EP2744330A4 | 2015-03-25 | VANKAYALAPATI HARIPRASAD; SORNA VENKATASWAMY; WARNER STEVE L; BEARSS DAVID J; SHARMA SUNIL; STEPHENS BRET |
In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | ||||||
83 | SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIITORS | EP12823540.5 | 2012-08-15 | EP2744330A1 | 2014-06-25 | VANKAYALAPATI, Hariprasad; SORNA, Venkataswamy; WARNER, Steve, L.; BEARSS, David, J.; SHARMA, Sunil; STEPHENS, Bret |
In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | ||||||
84 | HYDRAZINMODIFIZIERTE MATRICES, IHRE VERWENDUNG IN VERFAHREN ZUR ISOLIERUNG VON BIOMOLEKÜLEN | EP09711574.5 | 2009-02-20 | EP2255000A1 | 2010-12-01 | FABIS, Roland; HIMMELREICH, Ralf |
The invention relates to novel functionalized matrices or matrix materials comprising structures of general formula Carrier — Linker — Spacer — NR 3 — NR 1R 2 (I), methods for the production thereof, and the use thereof for isolating biomolecules. | ||||||
85 | AMINOBUTANOIC ACID DERIVATIVES | EP98947771 | 1998-09-07 | EP1024134A4 | 2003-05-14 | TAKAHASHI KANJI; SUGIURA TSUNEYUKI |
Aminobutanoic acid derivatives represented by general formula (I) and salts thereof (wherein each symbol is as defined in the description). The derivatives inhibit matrix metalloproteinases and are therefore useful for the prevention and/or treatment of rheumatism, osteoarthritis, pathologic bone resorption, osteoporosis, periodontal diseases, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatic cirrhosis, corneal injury, diseases due to metastasis and infiltration of cancer cells or proliferation thereof, autoimmune diseases (such as Crohn's disease and Sjögren's disease), diseases due to transmigration of white blood cells or infiltration thereof, neovascularization, multiple sclerosis, aortic aneurysm, endometritis and so on. | ||||||
86 | Radiohalogenated compounds for site specific labeling | EP89401557.7 | 1989-06-06 | EP0348261A1 | 1989-12-27 | Coughlin, Daniel James; Belinka, Benjamin A.; Alvarez, Vernon Leon |
Radiohalogenated compounds which are useful as intermediates for preparing radiohalogenated antibody conjugates in which the radiohalogenated compound is site specifically attached to an oxidized carbohydrate moiety of an antibody or antibody fragment are disclosed. Methods for making the compounds and the antibody conjugates as well as methods of use of the same are also disclosed. |
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87 | METHOD FOR PREPARING AND METHOD FOR REPAIRING DEFECTS OF COVALENT ORGANIC FRAMEWORK MATERIAL | EP18940484.1 | 2018-11-19 | EP3862341A1 | 2021-08-11 | WANG, Wenjun; WANG, Song; LIU, Pingwei; LI, Bogeng |
The present invention relates to a method for preparing a covalent organic framework (COF) materials - a reversible polycondensation/termination method, the COF materials prepared by the method have high crystallinity, high specific surface area, regular and controllable morphology. The present invention also relates to a method for repairing defects of COF materials - reversible degradation-recombination, the method can eliminate defects of existing COF materials, thereby increasing the crystallinity and specific surface area of COF materials and improving their morphological characteristics. |
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88 | DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES | EP12779616.7 | 2012-04-27 | EP2704568A1 | 2014-03-12 | ALI, Amjad; LO, Michael, Man-Chu; YAN, Lin |
The present invention includes diazeniumdiolate cyclohexyl derivatives, such as a compound having the structure of formula (I) wherein R 1-R 13 are as defined herein, including various pharmaceutically acceptable salts and hydrates thereof, and pharmaceutical formulations comprising the diazeniumdiolate cyclohexyl derivatives. The invention also includes a method for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy, comprising administering a compounds of the invention to a patient having such a condition, or being at risk to having such condition. | ||||||
89 | COMPOSITIONS AND METHODS TO CONTROL FUNGAL PATHOGENS | EP09789561.9 | 2009-04-01 | EP2413695A1 | 2012-02-08 | PEARSON, Norman; ROSS, Ronald; EHR, Robert |
Disclosed herein are acylhydrazone and semicarbazones derivatives of aldehydes and ketones that may act to attract plant pathogenic zoospores and methods of using these compounds. These compounds include the compound according to Formula 1 : wherein: X is selected from the group consisting of: (CH 2) n, 1,3-phenylene and 1,4-phenylene; R1 is selected from the group consisting of iso-butyl, sec -butyl and tert-butyl- CH 2; R 2 is hydrogen or methyl; and n is equal to 0-25. Upon exposure to water, these compounds release aldehydes or ketones that may attract zoospores. These compounds can be combined with fungicides to form fungicidal formulations that are especially effective against oomycete producing fungal pathogens. | ||||||
90 | HALOGENATED 2-AMINO-4, 5 HEPTENOIC ACID DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS | EP01927026 | 2001-04-13 | EP1272455A4 | 2005-07-27 | HANSEN DONALD W JR; WEBBER RONALD KEITH; AWASTHI ALOK K; MANNING PAMELA T; SIKORSKI JAMES A |
91 | HALOGENATED 2-AMINO-4, 5 HEPTENOIC ACID DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS | EP01927026.3 | 2001-04-13 | EP1272455A1 | 2003-01-08 | HANSEN, Donald, W., Jr.; WEBBER, Ronald, Keith; AWASTHI, Alok, K.; MANNING, Pamela, T.; SIKORSKI, James, A. |
The present invention contains halogenated 2-amino-4, 5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors. | ||||||
92 | FLUORINATED COMPOUND AND USE THEREOF | EP95934279 | 1995-10-12 | EP0786451A4 | 1998-12-30 | YAMANA M; HONDA Y |
A fluorinated polyether compound represented by the following general formula (1): X-(Rf1)-(CF2)x-(CH2)y-{CHR-CH2}z1-Y1-Z1 or (1'): Z2-Y2-{CH2-CHR}z2-(CH2)y-(CF2)x-(Rf2)-(CF2)x-(CH2)y-{CHR-CH2}z3-Y3-Z3, a lubricating oil, and a magnetic recording medium containing the oil, wherein Rf1 and Rf2 represent each a fluorinated polyether group, perfluoroalkyl group or perfluoroalkenyl group; and Z1, Z2 and Z3 represent each a member selected from among groups containing organic free radicals represented by formulae (5) to (7). | ||||||
93 | Radiohalogenated compounds for site specific labeling | EP89401557.7 | 1989-06-06 | EP0348261B1 | 1993-12-15 | Coughlin, Daniel James; Belinka, Benjamin A.; Alvarez, Vernon Leon |
94 | Insecticidal N'-substituted-N-alkylcarbonyl-N'-acylhydrazines and N'-substituted -N-acyl-N'-alkylcarbonyl hydrazines | EP89306052.5 | 1989-06-15 | EP0347216B1 | 1993-09-01 | Hsu, Adam Chi-Tung; Le, Dat Phat; Murphy, Raymond August; Weinstein, Barry |
95 | IMPROVED SYNTHESIS OF OTVICICLIB | EP22199174.8 | 2022-09-30 | EP4345102A1 | 2024-04-03 | HUBER, Lukas A.; GSTACH, Hubert; MASTALIR, Matthias; LEBAN, Johann |
The present invention relates to an improved synthesis of Otviciclib (N-{4-[1-(2,6-Dichloro-4-sulfamoyl-phenyl)-3-dimethylamino-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-ylmethyl]-phenyl}-2-diethylamino-acetamide) and its derivatives, and furthermore relates to intermediates useful in this synthesis. |
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96 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE | EP13794428.6 | 2013-05-15 | EP2852570A2 | 2015-04-01 | KANDULA, Mahesh |
The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammatory bowel disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria. | ||||||
97 | DIVALENT HYDRAZIDE COMPOUND CONJUGATES FOR INHIBITING CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR | EP09755506.4 | 2009-04-03 | EP2288592A2 | 2011-03-02 | VERKMAN, Alan, S.; SONAWANE, Nitin, D. |
Provided herein are divalent hydrazide-polyethylene glycol conjugates that inhibit the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR). The conjugates described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. | ||||||
98 | N,N-DINITRAMIDE SALTS AS SOLUBILIZING AGENTS FOR BIOLOGICALLY ACTIVE AGENTS | EP02756424 | 2002-07-09 | EP1417153A4 | 2005-01-05 | BOTTARO JEFFREY C; PETRIE MARK A; PENWELL PAUL E; BOMBERGER DAVID C |
99 | ARYLHYDRAZONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS | EP96933116 | 1996-09-13 | EP0881878A4 | 2004-08-04 | LAM KELVIN T; POWERS DAVID G |
100 | N,N-DINITRAMIDE SALTS AS SOLUBILIZING AGENTS FOR BIOLOGICALLY ACTIVE AGENTS | EP02756424.4 | 2002-07-09 | EP1417153A1 | 2004-05-12 | BOTTARO, Jeffrey, C.; PETRIE, Mark, A.; PENWELL, Paul, E.; BOMBERGER, David, C. |
A method is provided for enhancing the solubility of an ionizable compound in a lipophilic medium by admixing the compound with an effective solubility-enhancing amount of an N,N-dinitramide salt. The ionizable compound, upon ionization, gives rise to a biologically active cationic species that ionically associates with the N,N-dinitramide anion N(NO2)2 following admixture with the N,N-dinitramide salt. The biologically active cationic species may be a pharmacologically active cation, in which case the method is useful for enhancing the penetration of the blood-brain barrier by the pharmacologically active cation. In other embodiments, the ionizable compounds are medical imaging or diagnostic agents, or agricultural agents such as pesticides. Salts of biologically active cations and N,N-dinitramide ion are also provided as novel compositions of matter. |