- SPIRO-LACTAM COMPOUNDS AND METHODS OF TREATING VIRAL INFECTIONS USING THE SAME
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Disclosed are compounds, and pharmaceutically acceptable salts thereof, that can ameliorate or treat a viral infection in a subject in need thereof. The disclosure also includes conjugates of such compounds with a protease.
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Page/Page column 86; 87
(2021/12/28)
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- TRICYCLIC PYRIDONES AND PYRIMIDONES
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A compound of Formula (I) is provided: (I) where the variables are defined herein.
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Paragraph 0723; 0733-0735
(2021/06/26)
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- ΒETA-CATENIN AND B-CELL LYMPHOMA 9 (BCL9) INHIBITORS
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Disclosed are inhibitors for the β-catenin/BCL9 interaction. The inhibitors are selective for β-catenin/BCL9 over β-catenin/cadherin interactions. Methods of using the disclosed compounds to treat cancer are also disclosed.
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Page/Page column 58; 74
(2020/05/21)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 30; 31
(2018/03/01)
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- HETEROCYCLIC COMPOUND
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The problem of the present invention is to provide a compound having a superior RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like. The present invention relates to a compound represented by the formula (I): [wherein each symbol is as described in the DESCRIPTION] or a salt thereof, which has an RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like.
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Paragraph 0479
(2017/08/01)
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- Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R6, X, Y, W and n are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0527; 0528; 0529
(2015/11/02)
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- Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain
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Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of α-synuclein in Lewy bodies, which are one of the hallmarks of Parkinson's disease neuropathology. Potent, selective, brain-penetrant inhibitors of Plk
- Aubele, Danielle L.,Hom, Roy K.,Adler, Marc,Galemmo, Robert A.,Bowers, Simeon,Truong, Anh P.,Pan, Hu,Beroza, Paul,Neitz, R. Jeffrey,Yao, Nanhua,Lin, May,Tonn, George,Zhang, Heather,Bova, Michael P.,Ren, Zhao,Tam, Danny,Ruslim, Lany,Baker, Jeanne,Diep, Linnea,Fitzgerald, Kent,Hoffman, Jennifer,Motter, Ruth,Fauss, Donald,Tanaka, Pearl,Dappen, Michael,Jagodzinski, Jacek,Chan, Wayman,Konradi, Andrei W.,Latimer, Lee,Zhu, Yong L.,Sham, Hing L.,Anderson, John P.,Bergeron, Marcelle,Artis, Dean R.
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supporting information
p. 1295 - 1313
(2013/08/23)
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- PTERIDINONES AS INHIBITORS OF POLO - LIKE KINASE
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The present invention provides compounds having a structure according to Formula (I) or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
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Page/Page column 92; 93
(2011/07/09)
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- SATURATED BICYCLIC HETEROCYCLIC DERIVATIVES AS SMO ANTAGONISTS
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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smoantagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.
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Page/Page column 44
(2010/04/06)
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- 4-ACYL-PIPERAZINES AS ANTI-VIRAL AGENTS
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Anti-viral agents of Formula (I) wherein: A represents hydroxy or -NH2; D represents aryl or heteroaryl; E represents hydrogen, straight or branched chain C1-6alkyl, -CO2R1, -C(O)R1a, -C(O)NR2/s
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Page/Page column 17
(2008/06/13)
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- The relationship between physicochemical properties, in vitro activity and pharmacokinetic profiles of analogues of diamine-containing efflux pump inhibitors
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Following the optimization of diamine-containing efflux pump inhibitors with respect to in vitro potentiation activity, in vivo stability and acute toxicity, we addressed the question of how to control the pharmacokinetic properties of the series. Upon in
- Watkins, William J.,Landaverry, Yakira,Leger, Roger,Litman, Renee,Renau, Thomas E.,Williams, Nicole,Yen, Rose,Zhang, Jason Z.,Chamberland, Suzanne,Madsen, Deidre,Griffith, David,Tembe, Vrushali,Huie, Keith,Dudley, Michael N.
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p. 4241 - 4244
(2007/10/03)
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- Src kinase inhibitor compounds
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Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
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- Heterocyclic substituted aniline calcium channel blockers
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The present invention provides compounds that block calcium channels having the Formula I shown below. STR1The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.
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- Inhibitors of farnesyl-protein transferase
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The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras. The compounds of formula A are representative of the compounds of the present invention: STR1
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