- Intermediate for preparing medetomidine and its preparation method and use
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The invention provides an intermediate for preparing medetomidine. The intermediate is a compound shown in the formula (I). The invention also provides a preparation method of the intermediate, and ause of the intermediate in the preparation of medetomidine. The compound shown in the formula (I) is used for preparation of medetomidine so that the raw material is cheap and easy to obtain, synthesis processes are simple, the reaction cycle is short, the environmental pollution is avoided, operation is simple, the harsh reaction conditions are avoided, the operation and post-treatment are simple, the yield and the product purity are high, the intermediate in each step is a solid and is easy to purify, a production cost is low, and the intermediate is suitable for industrial large-scale production and conforms to the principle of green chemistry.
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Paragraph 0094-0096
(2018/08/03)
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- PREPARATION METHOD OF DEXMEDETOMIDINE INTERMEDIATE
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The present invention discloses a preparation method of 2,3-dimethyl phenyl-1-trityl-imidazole-4-ketone. In accordance with this method, imidazole-4-ethyl formate is used as a raw material; ethyl formate is used for amino protection, 1-trityl-1H-imidazole
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Paragraph 0024
(2016/10/11)
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- Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
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A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ray crystallography of inhibitors bound to reverse transcriptase, including a structure of the Y188L RT protein, was used extensively to help identify and optimize the key hydrogen-bonding motif. This led directly to the design of compound 43 that exhibits remarkable antiviral activity (EC50 1 nM) against a wide range of NNRTI-resistant viruses and a favorable pharmacokinetic profile across multiple species.
- Chong, Pek,Sebahar, Paul,Youngman, Michael,Garrido, Dulce,Zhang, Huichang,Stewart, Eugene L.,Nolte, Robert T.,Wang, Liping,Ferris, Robert G.,Edelstein, Mark,Weaver, Kurt,Mathis, Amanda,Peat, Andrew
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supporting information
p. 10601 - 10609
(2013/02/23)
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- IMIDAZOLE CARBOXAMIDES
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The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same.
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Page/Page column 17
(2010/02/17)
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- THIA-TRIAZA-CYCLOPENTAZULENES AS PI3-KINASES INHIBITORS FOR THE TREATMENT OF CANCER
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The present invention encompasses compounds of general formula (1) wherein 5 R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and th
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Page/Page column 29-30
(2010/11/05)
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- NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
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Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
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Page/Page column 21
(2009/02/11)
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
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Page/Page column 105
(2009/01/24)
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- Amide substituted xanthine derivatives
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The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
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- Novel farnesyl protein transferase inhibitors as antitumor agents
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Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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- AMIDE SUBSTITUTED XANTHINE DERIVATIVES WITH GLUCONEOGENESIS MODULATING ACTIVITY
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The present invention is a 1,3,8 substituted xanthine derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (I) and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
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- Development of orally active nonpeptidic inhibitors of human neutrophil elastase
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5-Amino-2-phenylpyrimidin-6-ones, some of their desamino derivatives, and miscellaneous derivatives were synthesized and biologically evaluated on both in vitro activity and oral activity in an acute hemorrhagic assay. These compounds contained an α-keto-1,3,4-oxadiazole moiety to bind covalently to the Ser-195 hydroxy group of human neutrophil elastase (HNE). Among those tested, compounds 11a-c,e,i-l(F), 11d,e,k(H), 21d,e,k(F), and 21d,e(H) showed a good oral profile. RS-Mixture 3(H) was selected for clinical evaluation based on its oral potency, duration of action, enzyme selectivity, safety profile, and ease of synthesis. Structure -activity relationships (SARs) are discussed.
- Ohmoto,Yamamoto,Okuma,Horiuchi,Imanishi,Odagaki,Kawabata,Sekioka,Hirota,Matsuoka,Nakai,Toda,Cheronis,Spruce,Gyorkos,Wieczorek
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p. 1268 - 1285
(2007/10/03)
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- Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.
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All previously reported CAAX-based farnesyltransferase inhibitors contain a thiol functionality. We report that attachment of the 4-imidazolyl group, via 1-, 2-, or 3-carbon alkyl or alkanoyl spacers, to Val-Tic-Met or tLeu-Tic-Gln provides potent FT inhibitors. (R*)-N-[[1,2,3,4-Tetrahydro-2-[N-[2-(1H-imidazol-4-yl)ethyl] -L-valyl]-3-isoquinolinyl]carbonyl]-L-methionine ([imidazol- 4-yl-ethyl]-Val-Tic-Met), with FT IC50 = 0.79 nM, displayed potent cell activity in the absence of prodrug formation (SAG EC50 = 3.8 muM).
- Hunt, John T.,Lee, Ving G.,Leftheris, Katerina,Seizinger, Bernd,Carboni, Joan,et al.
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p. 353 - 358
(2007/10/03)
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