- TETRAHYDROBENZO-QUINOLINE SULFONAMIDES DERIVATIVE COMPOUNDS
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The present invention relates to tetrahydrobenzo-isoquinoline sulfonamides derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses,
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Page/Page column 12
(2021/07/02)
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- DIHYDROCYCLOPENTA-ISOQUINOLINE-SULFONAMIDE DERIVATIVES COMPOUNDS
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The present invention relates to dihydrocyclopenta-isoquinoline-sulfonamide derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FcεRI receptor.
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Page/Page column 25-26
(2021/07/02)
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- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR
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Disclosed are heterocyclic compounds as inhibitors of FGFR-4 represented by formula (I). Also disclosed is a pharmaceutical composition that includes an inhibitor of FGFR-4. The compounds maybe used to treat diseases mediated with abnormality of FGFR-4 and /or FGF19, such as hepatocellular carcinoma and other forms of cancer.
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Page/Page column 53
(2020/09/03)
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- Heterocyclic compound as FGFR inhibitor, synthesis method and applications thereof
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The present invention discloses a heterocyclic compound as an FGFR inhibitor, and a synthesis method thereof, and applications of the heterocyclic compound in preparation of drugs for treating cancers. According to the present invention, the heterocyclic compound as the FGFR inhibitor or the pharmaceutically acceptable salt thereof has high FGFR inhibitory action, and the pharmaceutical composition prepared from the heterocyclic compound has good anticancer effect and wide application range.
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Paragraph 0071; 0074-0077
(2019/10/01)
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- CONDENSED TRICYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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There is provided compounds of formula I, (I) wherein R1, R2, R3 R4, R5, R6, R7a and R7b have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. CDK8 and/or Haspin kinase) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
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Page/Page column 73
(2017/03/14)
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- COMPOUNDS
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Disclosed are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis(ALS).
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Page/Page column 91; 92
(2017/02/09)
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- 1-(HET)ARYLSULFONYL-(PYRROLIDINE OR PIPERIDINE)-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
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The invention is concerned with the compounds of formula I and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
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Paragraph 01232; 01233; 01234
(2016/09/22)
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- Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors
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NAMPT inhibitors may show potential as therapeutics for oncology. Throughout our NAMPT inhibitor program, we found that exposed pyridines or related heterocyclic systems in the left-hand portion of the inhibitors are necessary pharmacophores for potent cellular NAMPT inhibition. However, when combined with a benzyl group in the center of the inhibitors, such pyridine-like moieties also led to consistent and potent inhibition of CYP2C9. In an attempt to reduce CYP2C9 inhibition, a parallel synthesis approach was used to identify central benzyl group replacements with increased Fsp3. A spirocyclic central motif was thus discovered that was combined with left-hand pyridines (or pyridine-like systems) to provide cellularly potent NAMPT inhibitors with minimal CYP2C9 inhibition. Further optimization of potency and ADME properties led to the discovery of compound 68, a highly potent NAMPT inhibitor with outstanding efficacy in a mouse tumor xenograft model and lacking measurable CYP2C9 inhibition at the concentrations tested.
- Zak, Mark,Yuen, Po-Wai,Liu, Xiongcai,Patel, Snahel,Sampath, Deepak,Oeh, Jason,Liederer, Bianca M.,Wang, Weiru,O'Brien, Thomas,Xiao, Yang,Skelton, Nicholas,Hua, Rongbao,Sodhi, Jasleen,Wang, Yunli,Zhang, Lei,Zhao, Guiling,Zheng, Xiaozhang,Ho, Yen-Ching,Bair, Kenneth W.,Dragovich, Peter S.
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p. 8345 - 8368
(2016/10/03)
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- HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
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The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
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Paragraph 0674; 0675; 0676
(2016/12/01)
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- COMPOUNDS AND METHODS OF USE
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This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.
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Paragraph 0178
(2015/07/16)
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- SODIUM CHANNEL BLOCKERS, PREPARATION METHOD THEREOF AND USE THEREOF
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The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD).
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Page/Page column 56; 57
(2014/05/07)
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- AMIDO-BENZYL SULFONE AND SULFONAMIDE DERIVATIVES
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Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.
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Page/Page column 95; 96
(2013/09/12)
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- Pyrazolopyrrolidine compounds
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The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
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Page/Page column 202
(2013/06/27)
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- BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE
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Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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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Page/Page column 99
(2012/10/08)
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- IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT' OF CANCER
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The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R1 hydrogen, hydroxy, halo, methyl, C1-C2 alkoxy, amino, or rnethylamino; R2 is hydrogen, halo, or cyano; R3 is hydrogen or halo;, R4 is hydrogen, halo, or methyl; provided that at least two of R1, R2, R3, and R4 are hydrogen; R5 is hydrogen, halo, or methyl; or a pharmaceutically acceptable salt thereof.
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Page/Page column 10
(2008/12/06)
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- TRIAZOLYL AMINOPYRIMIDINE COMPOUNDS
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The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
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Page/Page column 23
(2009/01/20)
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- Gram scale synthesis of the glucuronide metabolite of ABT-724
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A gram scale synthesis of the glucuronide metabolite of ABT-724 is reported. Glycosidic coupling between a trichloroacetimidate glucuronyl donor and a Cbz-protected hydroxypyridylpiperazine glycosyl acceptor is the key step in the synthesis, since attempts to directly glucuronicrossed d signate the aglycon, aglycon derivatives, and other truncated glycosyl acceptors were unsuccessful. The route was used to produce 2.1 g of metabolite in eight steps from 2-chloro-5-hydroxypyridine in 21% overall yield.
- Engstrom, Kenneth M.,Daanen, Jerome F.,Wagaw, Seble,Stewart, Andrew Q.
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p. 8378 - 8383
(2007/10/03)
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- SUBSTITUTED BIARYL ANALOGUES
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Substituted biaryl analogues of Formula (I) are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological recep
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Page/Page column 42
(2008/06/13)
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