- OXADIAZINE COMPOUNDS AND METHODS OF USE THEREOF
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The present disclosure relates to oxadiazine compounds, pharmaceutical compositions comprising an effective amount of an oxadiazine compound and methods for using an oxadiazine compound in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of an oxadiazine compound.
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- 5 - thiazole amides and biological applications
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The invention relates to a 5-thiazole amide compound and biology application thereof. The 5-thiazole amide compound has a general formula (I) described in the specification and is used for targeting an AKT/PKB kinase (ATP binding site). Experiments prove that a thiazole amide AKT inhibitor can remarkably inhibit the activity of the AKT kinase in vitro and has strong proliferation inhibition function on various tumor cells with high AKT activity, which indicate that the 5-thiazole amide compound can be used for preparing drugs for resisting tumors.
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- Solution-phase parallel synthesis of ruxolitinib-derived Janus kinase inhibitors via copper-catalyzed azide-alkyne cycloaddition
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A solution-phase parallel synthesis of triazole-derived ruxolitinib analogues was developed in the current study. The method employs copper-catalyzed azide-alkyne cycloaddition to build up the central triazole template. Product isolation by precipitation
- Gehringer, Matthias,Forster, Michael,Laufer, Stefan A.
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- New thiazole carboxamides as potent inhibitors of Akt kinases
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A new series of 2-substituted thiazole carboxamides were identified as potent pan inhibitors against all three isoforms of Akt (Akt1, Akt2 and Akt3) by systematic optimization of weak screening hit N-(1-amino-3-phenylpropan-2-yl)- 2-phenylthiazole-5-carboxamide (1). One of the most potent compounds, 5m, inhibited the kinase activities of Akt1, Akt2 and Akt3 with IC50 values of 25, 196 and 24 nM, respectively. The compound also potently inhibited the phosphorylation of downstream MDM2 and GSK3β proteins, and displayed strongly antiproliferative activity in prostate cancer cells. The inhibitors might serve as lead compounds for further development of novel effective anticancer agents.
- Chang, Shaohua,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Cao, Xianwen,Li, Honglin,Tu, Zhengchao,Lu, Xiaoyun,Ren, Xiaomei,Ding, Ke
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p. 1208 - 1212
(2012/03/11)
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- CHEMICAL COMPOUNDS
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There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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- 3-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
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Page/Page column 120
(2010/04/06)
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- MTOR KINASE INHIBITORS FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE MTOR/P13K/AKT PATHWAY
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Provided herein are Heteroaryl Compounds having the following structure: R2 N (I) or (II) wherein R1 -R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
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Page/Page column 125
(2010/06/17)
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- PYRROLOPYRIDINES AS KINASE INHIBITORS
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Compounds of Formula (I) are useful for inhibition of CHKl and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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- 2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10
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This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R1, R2, R4. Ar and Het are as defined herein. The invention also relates to methods of using the compound of for
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Page/Page column 128-129
(2009/11/29)
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- 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
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Page/Page column 36-37
(2009/12/23)
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- Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors
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A pyrrolopyridinyl thiophene carboxamide 7 was discovered as a tractable starting point for a lead optimization effort in an AKT kinase inhibition program. SAR studies aided by a co-crystal structure of 7 in AKT2 led to the identification of AKT inhibitor
- Seefeld, Mark A.,Rouse, Meagan B.,McNulty, Kenneth C.,Sun, Lihui,Wang, Jizhou,Yamashita, Dennis S.,Luengo, Juan I.,Zhang, ShuYun,Minthorn, Elisabeth A.,Concha, Nestor O.,Heerding, Dirk A.
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scheme or table
p. 2244 - 2248
(2009/12/07)
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- NOVEL COMPOUNDS
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The present invention relates to compounds of formula (I): and processes for preparing them, compositions containing them and their use in treating diseases relating to inappropriate c-Met activity.
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Page/Page column 50-51
(2008/12/05)
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- COMPOUNDS
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Invented are novel azaindole 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
(2008/06/13)
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- INHIBITORS OF Akt ACTIVITY
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Invented are novel thiophene 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 54
(2010/11/27)
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- KINASE INHIBITORS
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The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I, II, or III or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, I II III wherein X, R1, R2, R3, R31, n, and m have the meaning defined in the claims. In particular, the present invention relates more specifically to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
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Page/Page column 50
(2008/06/13)
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- 2-OXO-1-PYRROLIDINE DERIVATIVES
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The present invention concerns 2-oxo-1 -pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
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- Certain substituted ureas, as modulators of kinase activity
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Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity
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Page/Page column 18
(2010/11/24)
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- Concise and Efficient Synthesis of 4-Fluoro-1H-pyrrolo[2,3-b]pyridine
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(Equation presented) Two routes describing the preparation of 4-fluoro-1H-pyrrolo[2,3-b]pyridine (4a) from 1H-pyrrolo[2,3-b]pyridine N-oxide (1) are presented. Regioselective fluorination was achieved using either the Balz-Schiemann reaction or lithium-halogen exchange.
- Thibault, Carl,L'Heureux, Alexandre,Bhide, Rajeev S.,Ruel, Rejean
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p. 5023 - 5025
(2007/10/03)
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