专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-2021386068-A1 优先权日:2018-11-07 标题 :Compositions comprising pyridine carboxylate herbicides and very long chain fatty acid (vlcfa) synthesis inhibitor herbicides 发明人:KISTER JEREMY; SATCHIVI NORBERT M 权利人:CORTEVA AGRISCIENCE LLC 摘要:Disclosed herein are compositions comprising (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof and (b) a VLCFA synthesis inhibitor herbicide. Also disclosed herein are methods of controlling undesirable vegetation, comprising applying to vegetation or an area adjacent the vegetation or applying in soil or water to control the emergence or growth of vegetation (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof, and (b) a VLCFA synthesis inhibitor herbicide.
专利号:US-2021352899-A1 优先权日:2018-11-07 标题 :Compositions comprising pyridine carboxylate herbicides and fatty acid and lipid synthesis inhibitor herbicides 发明人:KISTER JEREMY; SATCHIVI NORBERT M 权利人:CORTEVA AGRISCIENCE LLC 摘要:Disclosed herein are compositions comprising (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof and (b) a fatty acid and lipid synthesis inhibitor (FA/LSI) herbicide, an agriculturally acceptable salt or ester thereof, or mixtures thereof. Also disclosed herein are methods of controlling undesirable vegetation, comprising applying to vegetation or an area adjacent the vegetation or applying in soil or water to control the emergence or growth of vegetation (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof and (b) a fatty acid and lipid synthesis inhibitor (FA/LSI) herbicide, an agriculturally acceptable salt or ester thereof, or mixtures thereof.
专利号:BR-102013018473-B1 优先权日:2012-07-24 标题 :HERBICIDAL COMPOSITIONS COMPENDIENT 4-AMINO-3-CHLORO-5-FLUORO-6- (4-CHLORO-2-FLUORO-3-ETOXYPHENYL) PYRIDINE-2-CARBOXYLIC ACID OR A DERIVATIVE OF THE SAME AND HERBICIDES INHIBITING THE SYNTHESIS OF VLCFA AND SYNTHESIS OF GRAIN ACID / LIPID, AND METHOD FOR UNDESIRABLE VEGETATION CONTROL
1: Kaplan V, Hasanoglu Erbasar GN, Cigerim L, Altay Turgut H, Cerit A. Effect of St. John's wort oil and olive oil on the postoperative complications after third molar surgery: randomized, double-blind clinical trial. Clin Oral Investig. 2020 Oct 15. doi: 10.1007/s00784-020-03639-0. Epub ahead of print. 67(11):1624-1642. English. doi: 10.1007/s12630-020-01792-4. Epub 2020 Aug 20. 12(7):657. doi: 10.3390/pharmaceutics12070657. 5: Ahmed MG, Adinarayana S. Formulation Design of Hydrocortisone Films for the Treatment of Aphthous Ulcers. Turk J Pharm Sci. 2019 Sep;16(3):348-355. doi: 10.4274/tjps.galenos.2018.75046. Epub 2019 Jul 10. 6: Surboyo MDC, Mahdani FY, Ernawati DS, Sarasati A, Rezkita F. The Macrophage Responses during Diabetic Oral Ulcer Healing by Liquid Coconut Shell Smoke: An Immunohistochemical Analysis. Eur J Dent. 2020 Jul;14(3):410-414. doi: 10.1055/s-0040-1712776. Epub 2020 May 24.
合成参考文献
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