- N-methyl-D-aspartate receptor modulators and methods of making and using same
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Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 67; 68; 69
(2018/06/25)
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- Telaprevir intermediate preparation method
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The invention relates to a preparation method of cyclopentane [c] pyrrole compound (formula I), and the method comprises following steps: taking 3-diaza-bicyclo [3.3.0] octane as the raw material, and then subjecting the raw material to cyanation, hydrolysis and esterification reactions so as to obtain the target product. The preparation method has the advantages of simple and easy operation, high yield, high product purity, and suitability for industrial production.
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- Amide derivative, preparation method of amide derivative, and application of amide derivative to pharmacy
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The invention provides an amide derivative, a preparation method of the amide derivative, and application of the amide derivative to pharmacy. The amide derivative compound is selected from one of the following structures. The compound can be used for preparing medicines in the fields of local anaesthesia or analgesia. (The formulas are as shown in the description).
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Paragraph 0110; 0126; 0127; 0128; 0129; 0130
(2017/08/30)
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- A process for the preparation of intermediates telaprevir
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The invention provides a telaprevir intermediate preparation method. The telaprevir intermediate preparation method comprises the following steps: (1) synthesizing (3aR, 6aS)-1,3a,4,5,6,6a-hexahydrocyclopentapyrrol; (2) synthesizing (3aR, 6aS)-octahydrocyclopentapyrrol-1-sodium sulfate; (3) synthesizing (3aR, 6aS)- octahydrocyclopentapyrrol-1-cyanogen; (4) synthesizing (3aR, 6aS)- octahydrocyclopentapyrrol-1-carboxylic acid; (5) synthesizing (3aR, 6aS)-2-Boc octahydrocyclopentapyrrol-1-carboxylic acid; (6) synthesizing (1s, 3aR, 6aS)-2-Boc octahydrocyclopentapyrrol-1-carboxylic acid; (7) synthesizing (1s, 3aR, 6aS)-2-Boc octahydrocyclopentapyrrol-1-carboxylic acid ethyl ester salt. The telaprevir intermediate preparation method is reasonable in process, low in cost and simple and convenient to operate, reagents are inexpensive and easy to obtain, and the control on reaction is easy.
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- Preparation method for bicyclic pyrrolidine intermediate of telaprevir
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The invention discloses a preparation method for a bicyclic pyrrolidine intermediate of telaprevir. The intermediate is (1S,3alphaR,6alphaS)-octahydrocyclopenta[c]pyrrole-1-carboxylic acid-ethyl ester hydrochloride. The preparation method comprises the following steps: (1) with 3-azabicyclo[3.3.0]octane hydrochloride as a raw material, carrying out Boc2O protection under the action of inorganic base so as to obtain an intermediate 1; (2) dissolving the intermediate 1 in an organic solvent, adding chiral organic ligand, carrying out a reaction with lithium alkyl at -70 DEG C for 2 h under the protection of nitrogen and introducing dry carbon dioxide so as to obtain an intermediate 2; and (3) adding the intermediate 2 into a saturated hydrogen chloride ethanol solution and carrying out a heating reflux reaction for 3 h so as to obtain the target compound. The preparation method provided by the invention has the advantages of short synthesis route, low cost, high product yield and optical purity and easiness in realization of large-scale production.
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Paragraph 0020; 0032
(2017/01/17)
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- Process for the preparation of a viral protease inhibitor and its intermediates
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Process for the preparation of a viral protease inhibitor and intermediates useful in its preparation.
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- Stereoselective lithiation and carboxylation of Boc-protected bicyclopyrrolidine: Synthesis of a key building block for HCV protease inhibitor telaprevir
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A stereoselective process for the manufacture of bicyclopyrrolidine 7 to 2 has been developed. The process utilizes a stereoselective lithiation/carboxylation sequence. The achiral diamine ligand DPBP induces excellent diastereocontrol, and resolution with (S)-THNA provides the corresponding salt of 8 in high er and dr. Subsequent processing of 8 gives 2 as the oxalate salt in an overall yield of 27% from 7 (based on total molar charge of 7). Compound 2 was obtained with high chemical and chiral purities. The process was successfully demonstrated on >100 kg scale.
- Tanoury, Gerald J.,Chen, Minzhang,Dong, Yong,Forslund, Raymond,Jurkauskas, Valdas,Jones, Andrew D.,Belmont, Daniel
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p. 1234 - 1244
(2014/12/10)
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- PROCESS FOR THE PREPARATION OF A VIRAL PROTEASE INHIBITOR AND INTERMEDIATES THEREOF
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Process for the preparation of a viral protease inhibitor and intermediates useful in its preparation.
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- SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to compounds that can modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
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Page/Page column 142
(2013/08/28)
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- PROCESS FOR THE PREPARATION OF A VIRAL PROTEASE INHIBITOR AND ITS INTERMEDIATES
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The application describes a process for the preparation of a compound of formula (II) useful for the preparation of a viral protease inhibitor. Intermediates of the process are also claimed.
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Page/Page column 20
(2013/08/28)
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- Kallikrein 7 modulators
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The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
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Page/Page column 101
(2010/10/19)
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- Enantioselective biocatalytic oxidative desymmetrization of substituted pyrrolidines
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"Chemical Equation Presented" Center stage: Additions of nitrogen-centered radicals to cyanamide compounds provided the first radical synthesis of aromatic polycyclic guanidine derivatives (see scheme). Modular assembly of the substrates allows for a rapid increase of the molecular complexity of scaffolds, which have potential applications for medicinal chemistry.
- Koehler, Valentin,Bailey, Kevin R.,Znabet, Anass,Raftery, James,Helliwell, Madeleine,Turner, Nicholas J.
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supporting information; experimental part
p. 2182 - 2184
(2010/06/18)
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- TERTIARY AMINE SUBSTITUTED PEPTIDES USEFUL AS INHIBITORS OF HCV REPLICATION
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The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
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Page/Page column 17
(2010/12/18)
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- Processes and intermediates
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The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
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Page/Page column 42
(2010/11/26)
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