167832-26-0Relevant articles and documents
Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators
Hirose, Wataru,Kato, Yoshihiro,Natsutani, Itaru,Takata, Makoto,Kitaichi, Maiko,Imai, Satoki,Hayashi, Shun,Arai, Yukiyo,Hoshino, Kohei,Yoshida, Kohzo
, p. 4331 - 4335 (2017/09/12)
We describe here the design, synthesis and characterization of a series of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as metabotropic glutamate receptor (mGluR) 5 negative allosteric modulators (NAMs). Optimization of the substituents led to the identifica
2-(AZAINDOL-2-YL)BENZIMIDAZOLES AS PAD4 INHIBITORS
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Paragraph 0446; 0447; 0448; 0449; 0450, (2015/07/02)
Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl;R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy;R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl;R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl;A is C—R5 or N;B is C—R6 or N;D is C—R7 or N;with the proviso that at least one of A, B, and D, is N;R5 is hydrogen or C1-6alkyl;R6 is hydrogen or C1-6alkyl;R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy;R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen;R9 is hydrogen or hydroxy;R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
BETA-LACTAMASE INHIBITORS
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, (2014/10/04)
Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Paragraph 0724; 0725, (2014/07/23)
The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
2 - (AZAINDOL- 2 -YL) BENZ IMIDAZOLES AS PAD4 INHIBITORS
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, (2014/02/16)
Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O-, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C-R5 or N; B is C-R6 or N; D is C-R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
Structure guided optimization, in vitro activity, and in vivo activity of pan-PIM kinase inhibitors
Burger, Matthew T.,Han, Wooseok,Lan, Jiong,Nishiguchi, Gisele,Bellamacina, Cornelia,Lindval, Mika,Atallah, Gordana,Ding, Yu,Mathur, Michelle,Mcbride, Chris,Beans, Elizabeth L.,Muller, Kristine,Tamez, Victoriano,Zhang, Yanchen,Huh, Kay,Feucht, Paul,Zavorotinskaya, Tatiana,Dai, Yumin,Holash, Jocelyn,Castillo, Joseph,Langowski, John,Wang, Yingyun,Chen, Min Y.,Garcia, Pablo D.
supporting information, p. 1193 - 1197 (2014/01/06)
Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM Kis 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described.
BRUTON'S TYROSINE KINASE INHIBITORS
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, (2011/04/14)
The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
Heterocyclic Kinase Inhibitors
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Page/Page column 11, (2011/08/22)
New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
INHIBITORS OF JAK
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Page/Page column 76, (2011/04/18)
The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
CHEMICAL COMPOUNDS 251
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Page/Page column 174, (2011/10/02)
The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.