- 6-5 FUSED RINGS AS C5a INHIBITORS
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The present disclosure provides, inter alia, Compounds of Formula (I) (I) or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
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Paragraph 0266
(2019/01/05)
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- AMINE-SUBSTITUTED ARYL OR HETEROARYL COMPOUNDS AS EHMT1 AND EHMT2 INHIBITORS
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The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
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Paragraph 0497-0499
(2017/11/10)
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- Effective combinatorial immunotherapy for castration-resistant prostate cancer
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A significant fraction of patients with advanced prostate cancer treated with androgen deprivation therapy experience relapse with relentless progression to lethal metastatic castration-resistant prostate cancer (mCRPC). Immune checkpoint blockade using a
- Lu, Xin,Horner, James W.,Paul, Erin,Shang, Xiaoying,Troncoso, Patricia,Deng, Pingna,Jiang, Shan,Chang, Qing,Spring, Denise J.,Sharma, Padmanee,Zebala, John A.,Maeda, Dean Y.,Wang, Y. Alan,Depinho, Ronald A.
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p. 728 - 732
(2017/05/01)
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- 2- [5- [N- (4 -FLUOROPHENYL) CARBAMOYL] PYRIMIDIN- 2 - YLSULFANYLMETHYL] -4- (TRIFLUOROMET HOXY) PHENYL] BORONIC ACID
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There is disclosed a pyrimidinecarboxamide compound useful as a pharmaceutical agent, synthetic processes, and pharmaceutical compositions which include the pyrimidinecarboxamide compound. More specifically, there is disclosed a CXCRl/2 inhibitor useful f
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Paragraph 0125
(2015/02/25)
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- HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and tr
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Page/Page column 24
(2011/07/06)
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- Organic compounds
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.
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Page/Page column 30
(2009/05/29)
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- Inhibitors of NF-kappaB and AP-1 gene expression: SAR studies on the pyrimidine portion of 2-chloro-4-trifluoromethylpyrimidine-5-[N-(3', 5'-bis(trifluoromethyl)phenyl)carboxamide].
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We investigated the structure-activity relationship studies of N-[3, 5-bis(trifluoromethyl)phenyl][2-chloro-4-(trifluoromethyl)pyrimidin-5 -yl]carboxamide (1), an inhibitor of transcription mediated by both NF-kappaB and AP-1 transcription factors, with the goal of improving its potential oral bioavailability. Compounds were examined for cell-based activity, were fit to Lipinski's rule of 5, and were examined for potential gastrointestinal permeability using the intestinal epithelial cell line, Caco-2. Selected groups were substituted at the 2-, 4-, and 5-positions of the pyrimidine ring using solution-phase combinatorial methodology. The introduction of a fluorine in the place of 2-chlorine of 1 resulted in a compound with comparable activity. However, other substitutions at the 2-position resulted in a loss of activity. The trifluoromethyl group at the 4-position could be replaced with a methyl, ethyl, chlorine, or phenyl without a substantial loss of activity. The carboxamide group at the 5-position is critical for activity. If it was moved to the 6-position, the activity was lost. The 2-methyl analogue of 1 (81) showed comparable in vitro activity and improved Caco-2 permeability compared to 1.
- Palanki,Erdman,Gayo-Fung,Shevlin,Sullivan,Goldman,Ransone,Bennett,Manning,Suto
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p. 3995 - 4004
(2007/10/03)
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- Organomanganese(II) Reagents in the Synthesis of 5-Pyrimidinyl Ketones
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Substituted alkyl 5-pyrimidinyl ketones were formed from acid chlorides of pyrimidine-5-carboxylic acids and alkylmanganese(II) iodides.The corresponding alcohols were also formed in the case of sterically less requiring organomanganese reagents and the a
- Arukwe, Joseph,Undheim, Kjell
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p. 764 - 767
(2007/10/02)
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