- Busulfan drug intermediate 1,4 bis-methyl sulfonate butyl diester synthetic method
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A busulfan drug intermediate 1,4-bis-methyl sulfonate butyl diester synthetic method comprises the following steps: 0.15mol of 1,4-butanediol and 150-170ml of triethylamine are added into a reaction vessel, solution temperature is reduced to 3-5 DEG C, stirring speed is controlled at 130-160rpm, 0.36-0.38mol of methanesulfonic acid amine is slowly dropwise added, after the completion of the dropwise addition, the solution temperature is raised to 35-40 DEG C, the solution is stirred for 3-4h, solution temperature is reduced to 15-20 DEG C, a solid is precipitated, and the solid is filtered, washed with a saline solution, dehydrated with a dehydrating agent, and recrystallized in cyclohexane to obtain a white solid of 1,4-bis-methyl sulfonate butyl diester; and the saline solution in the step is any one of sodium nitrate and potassium sulphate.
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Paragraph 0014; 0015
(2016/10/10)
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- BIVALENT BROMODOMAIN LIGANDS, AND METHODS OF USING SAME
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Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins. For example, in one aspect, a bivalent compound or a pharmaceutically acceptable salt, stereoisomer, metabolite, or hydrate thereof is provided. In another aspect, a method of treating a disease associated with a protein having tandem bromodomains in a patient in need thereof is provided. The method comprises administering to the patient the bivalent compound as described.
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Paragraph 00357-00361
(2015/06/11)
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- DITHIOAMINE REDUCING AGENTS
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Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins.
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Page/Page column
(2013/08/28)
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- PROCESS FOR PRODUCTION OF BIS-QUATERNARY AMMONIUM SALT, AND NOVEL INTERMEDIATE
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Object To provide a method for producing a bis-quaternary ammonium salt efficiently and a novel synthetic intermediate thereof. Solution The present invention relates to a method for producing a bis-quaternary ammonium salt represented by a general formula [3] which comprises reacting a disulfonic acid ester represented by a general formula [1] (in the formula, definitions of two R1's and T are as described in claim 1) with a tertiary amine represented by a general formula [2] (in the formula, definitions of R3 to R5 are as described in claim 1), and a disulfonic acid ester represented by a general formula [1′] (in the formula, two R16's represent independently a halogen atom or a C1-C3 fluoroalkyl group, and two m's represent independently an integer of 1 to 5).
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Page/Page column 16
(2012/06/01)
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- Synthesis of C3- and C2-symmetric tris- and bis-sulfoxide ligands by asymmetric oxidation
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A series of tris- and bis-sulfoxides were synthesized by multiple asymmetric oxidation of the corresponding sulfides. High enantioselectivities were obtained based on Horeau-type amplification of selectivity. Naphthyl-substituted sulfoxides allowed for higher selectivity and greater ease of purification. These sulfoxides were tested as ligands in rhodium-catalyzed olefin hydroacylation and 1,4-addition of phenyl boronic acid to 2-cyclohexen-1-one. While no enantioinduction was observed in hydroacylation, up to 80% ee was obtained for a tris-sulfoxide and a bis-sulfoxide ligand in the 1,4-addition. Bis-sulfoxides with flexible backbones gave lower and inversed enantioselectivity, suggesting backbone rigidity plays a key role in enantioinduction.
- Dornan, Peter K.,Leung, Priscilla L.,Dong, Vy M.
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experimental part
p. 4378 - 4384
(2011/08/04)
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- POLYMERS PREPARED FROM MIXTURES OF MULTIFUNCTIONAL N-VINYLFORMAMIDE AND HYBRID REACTIVE N-VINYLFORMAMIDE CROSSLINKING MONOMER MOIETIES AND USES THEREOF
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The present invention provides polymers resulting from polymerization of at least one reactive vinyl monomer moiety and a multifunctional N-vinylformamide crosslinking moiety; polymers resulting from polymerization of at least one reactive vinyl monomer moiety and a hybrid N-vinylformamide crosslinking moiety having at least one N-vinylformamide functionality and at least one other reactive vinyl functionality; polymers resulting from polymerization of at least one hybrid reactive N-vinylformamide monomer moiety having one N-vinylformamide functionality and at least one other reactive non-vinyl functionality and a multifunctional N-vinylformamide crosslinking moiety; and polymers resulting from polymerization of at least one hybrid reactive N-vinylformamide monomer moiety having one N-vinylformamide functionality and at least one other reactive non-vinyl functionality and a hybrid N-vinylformamide crosslinking moiety having at least one N-vinylformamide functionality and at least one other reactive vinyl functionality. The invention further provides a wide variety of compositions comprising the novel crosslinked polymers.
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Page/Page column 18-19
(2011/08/03)
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- THERAPEUTIC FOR HEPATIC CANCER
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A novel pharmaceutical composition for treating or preventing hepatocellular carcinoma and a method of treatment are provided. A pharmaceutical composition for treating or preventing liver cancer is obtained by combining a chemotherapeutic agent with an anti-glypican 3 antibody. Also disclosed is a pharmaceutical composition for treating or preventing liver cancer which comprises as an active ingredient an anti-glypican 3 antibody for use in combination with a chemotherapeutic agent, or which comprises as an active ingredient a chemotherapeutic agent for use in combination with an anti-glypican 3 antibody. Using the chemotherapeutic agent and the anti-glypican 3 antibody in combination yields better therapeutic effects than using the chemotherapeutic agent alone, and mitigates side effects that arise from liver cancer treatment with the chemotherapeutic agent.
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- Anti-Claudin 3 Monoclonal Antibody and Treatment and Diagnosis of Cancer Using the Same
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Monoclonal antibodies that bind specifically to Claudin 3 expressed on cell surface are provided. The antibodies of the present invention are useful for diagnosis of cancers that have enhanced expression of Claudin 3, such as ovarian cancer, prostate cancer, breast cancer, uterine cancer, liver cancer, lung cancer, pancreatic cancer, stomach cancer, bladder cancer, and colon cancer. The present invention provides monoclonal antibodies showing cytotoxic effects against cells of these cancers. Methods for inducing cell injury in Claudin 3-expressing cells and methods for suppressing proliferation of Claudin 3-expressing cells by contacting Claudin 3-expressing cells with a Claudin 3-binding antibody are disclosed. The present application also discloses methods for diagnosis or treatment of cancers.
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- Substituted Sulfonamide Compounds
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Substituted sulfonamide compounds corresponding to the formula I wherein m, n, p, Q, R1, R2, R3, R4, X, Y and Z have the respective meanings defined herein, pharmaceutical compositions containing such compounds, a process for their preparation, and the use of such compounds for the treatment and/or inhibition of pain and other conditions mediated by bradykinin receptor 1 (B1R) and/or bradykinin receptor 2 (B2R).
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Page/Page column 41
(2009/07/25)
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- SUBSTITUTED SULFONAMIDE DERIVATIVES
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The invention relates to substituted sulfonamide derivatives of the general formula (I'); processes for their preparation, medicaments containing these compounds, and the use of substituted sulfonamide derivatives for the preparation of medicaments
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Page/Page column 122
(2009/08/16)
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- Rationally-designed S-chiral bissulfinamides as highly enantioselective organocatalysts for reduction of ketimines
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We recently reported the first example of S-chiral organocatalysts, that are highly efficient and enantioselective in substoichometric amounts, and which use a chiral monosulfinamide group as Lewis base to activate trichlorosilane (HSiCl3) to reduce N-arylketimines. Aplausible mechanism involving two molecules of the monosulfinamde catalyst for the activation of HSiCl 3 prompted us to design S-chiral bissulfinamides as new catalysts. We herein describe our findings that an easily prepared S-chiral bissulfinamide bearing a five-methylene linkage not only inherited the excellent substrate generality from the monosulfinamide catalysts, but also exhibited further improved enantioselectivity.
- Pei, Dong,Zhang, Yu,Wei, Siyu,Wang, Meng,Sun, Jian
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supporting information; experimental part
p. 619 - 623
(2009/04/21)
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- The synthesis of deuterium-labeled spermine, N1 -acetylspermine and N1-acetylspermidine
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The synthesis of deuterium-labeled spermine, N1-acetylspermine and N1-acetylspermidine is reported. 1,1,3,3-2H 4-N1-Acetylspermine hydrochloride, 1,1,3,3- 2H4-N1-acetylspermidine hydrochloride and 1,1,3,3,10,10,12,12-2H8-spermine dihydrochloride were obtained in seven, four and three steps, respectively. All the syntheses were carried out by simple protection and deprotection steps from commonly used selective protecting reagents. These deuterium-labeled compounds can be used as mechanistic probes of polyamine oxidizing enzymes. Copyright
- Gawandi, Vijay,Fitzpatrick, Paul F.
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p. 666 - 670
(2008/02/10)
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- Method and compositions for the treatment of pruritus
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A composition for treating pruritus, comprising a compound selected from the group consisting of opioid receptor antagonists, opioid receptor agonists/antagonists, and pharmaceutically acceptable salts thereof, and a compound useful in treating the cause of the pruritus. This invention also relates to a method of treating pruritus using such compositions, and a method for preparing these compositions.
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- Method of treating nausea and vomiting with certain substituted-phenylalkylamino (and aminoacid) derivatives and other serotonin depleting agents
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A method for the treatment of emesis in a mammal, which method comprises administering to said mammal an emesis inhibiting amount of a compound which depletes serotonin in the brain of mammals; among which are compounds having the formula: STR1 wherein, R is selected from hydrogen, loweralkyl, trifluoromethyl, carboxyl, or loweralkoxycarbonyl; R1 and R2 are hydrogen or loweralkyl; Z is trifluoromethyl or halogen; the optical isomers and pharmaceutically acceptable salts thereof; two of the preferred compounds of the invention are fenfluramine and norfenfluramine.
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- Preparation and (31)P nuclear magnetic resonance studies of chiral phosphines
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The reaction of Li metal with alkyldiphenylphosphines generates the alkylphenylphosphide anions, which can undergo subsequent reactions with alkyl halides to give chiral phosphines (RR'R''P).The (31)P nmr chemical shifts have been measured for these phosphines, and show greater deviations from the values predicted by the first order additivity model than do those of more symmetrical phosphines (i.e., R3P and R2R'P).The shifts for these chiral molecules, and for a wide range of other phosphines, can be accurately predicted using a second order pairwise additivity scheme.The dependence of the observed and calculated chemical shifts upon electronegativity and steric factors is discussed.
- Payne, Nicholas C.,Stephan, Douglas W.
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