- PKB inhibitor
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The invention provides a PKB inhibitor, particularly relates to a compound shown as a formula I or a pharmaceutically acceptable salt thereof. The invention further provides a preparation method of the compound.
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Paragraph 0123; 0124; 0125; 0126
(2021/03/13)
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- THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
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The invention provides compounds having the general Formula (I); and pharmaceutically acceptable salts thereof; wherein the variables RA, RAA, subscript n, subscript q, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
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Page/Page column 239
(2016/01/25)
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- In-Depth Assessment of the Palladium-Catalyzed Fluorination of Five-Membered Heteroaryl Bromides
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A thorough investigation of the challenging Pd-catalyzed fluorination of five-membered heteroaryl bromides is presented. Crystallographic studies and density functional theory (DFT) calculations suggest that the challenging step of this transformation is
- Milner, Phillip J.,Yang, Yang,Buchwald, Stephen L.
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supporting information
p. 4775 - 4780
(2015/10/28)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 37
(2010/09/03)
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- IMIDAZO[1,2-a]PYRIDINES AND IMIDAZO[1,2-b]PYRIDAZINES AS MARK INHIBITORS
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The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 31
(2010/08/08)
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- PYRAZOLO[1,5-A]PYRIDINES AS MARK INHIBITORS
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The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 45
(2010/04/03)
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- PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES
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Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
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Page/Page column 89; 26
(2009/03/07)
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- INTEGRASE INHIBITORS 3
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The present invention provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Compounds of formula (I) are also provided.
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Page/Page column 57
(2008/06/13)
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- Compounds and compositons for treating C1s-mediated diseases and conditions
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Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
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- Design and Synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors
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A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of a variety of substituents at the thiophene 5-position. The 5-alkyl substituted and unsubstituted thiophenes were prepared using organolithium chemistry. Heteroatom substituents were introduced at the 5-position using a novel displacement reaction of 5-methylsulfonylthiophenes and the corresponding oxygen or sulfur anions. Small alkyl group substitution at the 5-position provided inhibitors equipotent with 3 but possessing improved solubility.
- Rudolph,Illig, Carl R.,Subasinghe, Nalin L.,Wilson, Kenneth J.,Hoffman, James B.,Randle, Troy,Green, David,Molloy, Chris J.,Soll, Richard M.,Lewandowski, Frank,Zhang, Marie,Bone, Roger,Spurlino, John C.,Deckman, Ingrid C.,Manthey, Carl,Sharp, Celia,Maguire, Diane,Grasberger, Bruce L.,DesJarlais, Renee L.,Zhou, Zhao
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p. 491 - 495
(2007/10/03)
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- Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
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The present invention is directed to compounds of Formula I: wherein X is O, S or NR7and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
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