104103-16-4Relevant articles and documents
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Paragraph 0426, (2021/04/02)
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
PYRAZOLE-OXAZOLIDINONE COMPOUND FOR ANTI-HEPATITIS B VIRUS
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Paragraph 0270; 0273-0274, (2019/06/07)
The present invention discloses a pyrazole-oxazolidinone compound having anti-hepatitis B virus activity, which has the structure of formula (I), wherein each variable is as defined herein.
Synthesis and Evaluation of Orexin-1 Receptor Antagonists with Improved Solubility and CNS Permeability
Perrey, David A.,Decker, Ann M.,Zhang, Yanan
, p. 587 - 602 (2018/03/27)
Orexins are hypothalamic neuropeptides playing important roles in many functions including the motivation of addictive behaviors. Blockade of the orexin-1 receptor has been suggested as a potential strategy for the treatment of drug addiction. We have previously reported OX1 receptor antagonists based on the tetrahydroisoquinoline scaffold with excellent OX1 potency and selectivity; however, these compounds had high lipophilicity (clogP > 5) and low to moderate solubility. In an effort to improve their properties, we have designed and synthesized a series of analogues where the 7-position substituents known to favor OX1 potency and selectivity were retained, and groups of different nature were introduced at the 1-position where substitution was generally tolerated as demonstrated in previous studies. Compound 44 with lower lipophilicity (clogP = 3.07) displayed excellent OX1 potency (Ke = 5.7 nM) and selectivity (>1,760-fold over OX2) in calcium mobilization assays. In preliminary ADME studies, 44 showed excellent kinetic solubility (>200 μM), good CNS permeability (Papp = 14.7 × 10-6 cm/sec in MDCK assay), and low drug efflux (efflux ratio = 3.3).
NOVEL BENZAMIDE DERIVATIVES AS MODULATORS OF THE FOLLICLE STIMULATING HORMONE
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Page/Page column 122, (2008/12/04)
The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1 nare defined as in formula I; invention compounds are modulators of follicle-stimulating hormone - ("FSH") which are useful for male and female contraception as well as other disorders modulated by FSH receptor.
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors
Choi, Seoung-Ryoung,Pradhan, Anupam,Hammond, Nicholas L.,Chittiboyina, Amar G.,Tekwani, Babu L.,Avery, Mitchell A.
, p. 3841 - 3850 (2008/02/11)
Plasmodium falciparum lactate dehydrogenase (pfLDH) is a key enzyme for energy generation of malarial parasites and is a potential antimalarial chemotherapeutic target. It is known that the oxamate moiety, a pyruvate analog, alone shows higher inhibition
Thienopyrimidines useful as Aurora kinase inhibitors
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Page/Page column 94, (2008/06/13)
The present invention provides compounds having the formula: wherein R1, R2, X1, X2, L1, L2, Y and Z are as defined in classes and subclasess herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.
ALPHA-4 INTEGRIN MEDIATED CELL ADHESION INHIBITORS FOR THE TREATMENT OR PREVENTION OF INFLAMMATORY DISEASES
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Page/Page column 40-41, (2010/02/13)
The present invention relates to novel compounds of formula (I), processes for their preparation, compositions comprising them and their use in the treatment or prevention of diseases capable of being modulated by the inhibition of cell adhesion.
4-(METHYL SULFONYL AMINO) PHENYL ANALOGUES AS VANILLOID ANTAGONIST SHOWING EXCELLENT ANALGESIC ACTIVITY AND THE PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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Page 23; 67, (2010/02/10)
The present invention relates to novel 4-(methylsulfonylamino) phenyl analogue as a potent vanilloid receptor antagonist and the pharmaceutical compositions comprising the same. The inventive compound can be useful for analgesics to prevent, alleviate or treat pain diseases or inflammatory disease comprising pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease and urgent urinary incontinence.
Reactions of Organic Anions, 147.- Simple and General Synthesis of Hydroxy- and Methoxyindoles via Vicarious Nucleophilic Substitution of Hydrogen
Makosza, Mieczyslaw,Danikiewicz, Witold,Wojciechowski, Krzysztof
, p. 203 - 208 (2007/10/02)
A simple synthesis of 4-, 5-, 6-, and 7-hydroxy- and -methoxyindoles via cyanoalkylation of O-protected nitrophenols by vicarious nucleophilic substitution of hydrogen, followed by catalytic hydrogenation of the (2-nitroaryl)acetonitriles obtained is described.
