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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
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.

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.

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.

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.
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