1152111-14-2Relevant articles and documents
Composition and orientation of the core region of novel HIV-1 entry inhibitors influences metabolic stability
Cocklin, Simon,Karadsheh, Rama,Meuser, Megan E.
, (2020/03/26)
Fostemsavir/temsavir is an investigational HIV-1 entry inhibitor currently in late-stage clinical trials. Although it holds promise to be a first-in-class Env-targeted entry inhibitor for the clinic, issues with bioavailability relegate its use to salvage
PYRIDINE-3-SULFONAMIDE COMPOUNDS AS PI3-KINASE INHIBITORS
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Page/Page column 92, (2019/02/13)
The invention is directed to compounds of formula (I) and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity.
TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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Paragraph 00321, (2019/07/13)
The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
Amino pyrimidine compound and preparation method and application thereof
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Paragraph 0165; 0168; 0169; 0170, (2018/11/22)
The invention relates to an amino pyrimidine compound and a preparation method and application thereof. The amino pyrimidine compound has a structure as shown in a formula I. The formula is shown in the description. The compound is an inhibitor of an epidermal growth factor receptor (EGFR) kinase. The invention further relates to a medicine composition comprising the compound, a preparation methodand application thereof in preparation of anti-tumor medicines.
BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION
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Paragraph 0132, (2017/02/24)
The present invention relates to certain bis-heteroaryl compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto- temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
Quinazolinone PARP-1 inhibitors, medicinal composition containing inhibitors, and antitumor use of inhibitors
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Paragraph 0218; 0219; 0220, (2016/10/08)
The invention discloses quinazolinyl-2,4(1H,3H)-dione PARP-1 inhibitors, and a preparation method, a medicinal composition and a use thereof. The invention concretely relates to quinazolinyl-2,4(1H,3H)-dione derivatives represented by general formula I, a medicinal salt and a preparation method thereof, a composition containing one or more of the compounds, and a use of the compounds in the preparation of tumor prevention and/or treatment medicines.
Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer
Johnson, James K.,Skoda, Erin M.,Zhou, Jianhua,Parrinello, Erica,Wang, Dan,O'Malley, Katherine,Eyer, Benjamin R.,Kazancioglu, Mustafa,Eisermann, Kurtis,Johnston, Paul A.,Nelson, Joel B.,Wang, Zhou,Wipf, Peter
supporting information, p. 785 - 790 (2016/08/24)
After a high-throughput screening campaign identified thioether 1 as an antagonist of the nuclear androgen receptor, a zone model was developed for structure-activity relationship (SAR) purposes and analogues were synthesized and evaluated in a cell-based luciferase assay. A novel thioether isostere, cyclopropane (1S,2R)-27, showed the desired increased potency and structural properties (stereospecific SAR response, absence of a readily oxidized sulfur atom, low molecular weight, reduced number of flexible bonds and polar surface area, and drug-likeness score) in the prostate-specific antigen luciferase assay in C4-2-PSA-rl cells to qualify as a new lead structure for prostate cancer drug development.
5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS
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Paragraph 0196, (2016/07/27)
The present invention discloses compounds according to Formula (I), wherein R, R2, R3a, R3b, and Cy are as defined herein. The present invention discloses compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same and methods for the prophylaxis and/or treatment of inflammatory conditions and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis.
NOVEL COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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Paragraph 2035; 2036, (2015/10/05)
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.
NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USES
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Paragraph 0558-0559, (2014/10/29)
The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.