- Preparation method of 2-amino-2-(1-methyl-4-piperidyl)ethanol
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The invention discloses a preparation method of 2-amino-2-(1-methyl-4-piperidyl) ethanol. The preparation method comprises the following steps: reacting 2-methyl-2-propyl-4-(1-amino-2-methoxy-2-oxoethyl)-1-piperidinecarboxylate (a compound II) with benzyl bromide under the action of an alkali 1 to generate a compound III; dissolving the compound III in an organic solvent, and generating a compound IV under the action of a reducing agent; and removing benzyl from the compound IV under the action of a catalyst/hydrogen to generate a compound I.
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Paragraph 0062-0065
(2021/07/24)
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- Compound, pharmaceutically acceptable salt thereof and medical application thereof
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The invention belongs to the field of medicines, and particularly relates to a compound shown as a formula I or medicinal salt thereof. The invention also relates to application of the compound or themedicinal salt thereof in selectively inhibiting LF activity, resisting anthrax toxin toxicity and preventing or treating anthracnose.
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Paragraph 0235-0240
(2020/07/24)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS FOR TREATING HEPATITIS C VIRAL INFECTION
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Tetracyclic heterocycle compounds of formula (I) and pharmaceutically acceptable salts thereof are provided, wherein A, A', G, R1, R15, U, V, V', W, W, X, X', Y and Y' are as defined in the invention. The pharmaceutical compositions comprising these compounds and the use of the compounds for treating hepatitis C virus (HCV) infection are also provided.
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Page/Page column 67-68
(2012/04/17)
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- TETRACYCLIC INDOLE DERIVATIVES FOR TREATING HEPATITIS C VIRUS INFECTION
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Tetracyclic indole derivatives of formula (I), pharmaceutically acceptable salts and the pharmaceutical compositions thereof are provided, wherein A, A', G, R1, R15, U, V, V, W, W, X, X', Y, Y' are as defined in the invention. Use of these derivatives for treating hepatitis C virus (HCV) infection is also provided.
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Page/Page column 85-86
(2012/04/17)
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- TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Tetracyclic Indole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprisingat least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing HCV infection in a patient.
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Page/Page column 74-75
(2012/04/17)
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- FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', B, G, R1, U, V, W, W', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
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Page/Page column 74
(2012/05/04)
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- FUSED TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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The present invention discloses novel Fused Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', W, W', X, X', Y and Y' are as defined herein. The present invention also discloses compositions comprising at least one Fused Tetracyclic Heterocycle Compound, and methods of using the Fused Tetracyclic Heterocycle Compounds for treating or preventing HCV infection in a patient.
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- FUSED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
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Page/Page column 96; 97
(2011/08/04)
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- ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C
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The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56
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Page/Page column 79-80
(2010/12/26)
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- ANTIVIRAL COMPOUNDS COMPOSED OF THREE ALIGNED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C
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The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
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Page/Page column 44
(2010/12/26)
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- Discovery of Potent, Selective, and Orally Active Carboxylic Acid Based Inhibitors of Matrix Metalloproteinase-13
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The matrix metalloproteinase enzyme MMP-13 plays a key role in the degradation of type II collagen in cartilage and bone in osteoarthritis (OA). An effective MMP-13 inhibitor would therefore be a novel disease modifying therapy for the treatment of arthritis. Our efforts have resulted in the discovery of a series of carboxylic acid inhibitors of MMP-13 that do not significantly inhibit the related MMP-1 (collagenase-1) or tumor necrosis factor-α (TNF-α) converting enzyme (TACE). It has previously been suggested (but not proven) that inhibition of the latter two enzymes could lead to side effects. A promising carboxylic acid lead 9 was identified and a convergent synthesis developed. This paper describes the optimization of 9 and the identification of a compound 24f for further development. Compound 24f is a subnanomolar inhibitor of MMP-13 (IC50 value 0.5 nM and Ki of 0.19 nM) having no activity against MMP-1 or TACE (IC50 of >10000 nM). Furthermore, in a rat model of MMP-13-induced cartilage degradation, 24f significantly reduced proteoglycan release following oral dosing at 30 mg/kg (75% inhibition, p 0.05) and at 10 mg/kg (40% inhibition, p 0.05).
- Monovich, Lauren G.,Tommasi, Ruben A.,Fujimoto, Roger A.,Blancuzzi, Vincent,Clark, Kirk,Cornell, Wendy D.,Doti, Robert,Doughty, John,Fang, James,Farley, David,Fitt, John,Ganu, Vishwas,Goldberg, Ronald,Goldstein, Robert,Lavoie, Stacey,Kulathila, Raviraj,Macchia, William,Parker, David T.,Melton, Richard,O'Byrne, Elizabeth,Pastor, Gary,Pellas, Theodore,Quadros, Elizabeth,Reel, Noela,Roland, Dennis M.,Sakane, Yumi,Singh, Hem,Skiles, Jerry,Somers, Joseph,Toscano, Karen,Wigg, Andrew,Zhou, Siyuan,Zhu, Lijuan,Shieh, Wen-Chung,Xue, Song,McQuire, Leslie W.
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experimental part
p. 3523 - 3538
(2010/03/30)
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- Certain azacycloalkyl substituted acetic acid derivatives
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Compounds of the formula (I) wherein R represents OH or NHOH; R1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic ac
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- Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases
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A novel series of carboxylic acids containing a substituted piperidine were synthesized and tested for inhibition of selected matrix metalloproteinases. Multiple analogues prepared based on this novel design were found to inhibit the target MMPs (MMP-2,-3
- Pikul,Ohler,Ciszewski,Laufersweiler,Almstead,De,Natchus,Hsieh,Janusz,Peng,Branch,King,Taiwo,Mieling
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p. 2499 - 2502
(2007/10/03)
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- An enantioselective synthesis of (R)-4-piperidinylglycine
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An efficient process for the synthesis of (R)-N-t-Boc-4-piperidinylglycine 8a, an unnatural amino acid, via enantioselective rhodium-catalyzed hydrogenation of the Cbz-enamide 5a is described. Subsequent deprotection of 8a affords unprotected (R)-4-piperi
- Shieh, Wen-Chung,Xue, Song,Reel, Noela,Wu, Raeann,Fitt, John,Repic, Oljan
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p. 2421 - 2425
(2007/10/03)
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