- BRAF DEGRADERS
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Present invention provides compounds that cause specifically the degradation of BRAF. The present compounds are useful for the treatment of various cancers.
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Page/Page column 155-156
(2022/02/06)
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- COMPOUNDS FOR TARGETED DEGRADATION OF BRD9
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BRD9 protein degradation compounds or pharmaceutically acceptable salts thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.
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Page/Page column 437-439; 471
(2021/09/11)
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- 2,4-dibasic miazines compound
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The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.
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- COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
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The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
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Paragraph 175; 176
(2015/03/28)
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- PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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Page/Page column 37
(2014/01/17)
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- Structure-activity relationships of new cyanothiophene inhibitors of the essential peptidoglycan biosynthesis enzyme MurF
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Peptidoglycan is an essential component of the bacterial cell wall, and enzymes involved in its biosynthesis represent validated targets for antibacterial drug discovery. MurF catalyzes the final intracellular peptidoglycan biosynthesis step: the addition of D-Ala-D-Ala to the nucleotide precursor UDP-MurNAc-L-Ala-γ-D-Glu-meso-DAP (or L-Lys). As MurF has no human counterpart, it represents an attractive target for the development of new antibacterial drugs. Using recently published cyanothiophene inhibitors of MurF from Streptococcus pneumoniae as a starting point, we designed and synthesized a series of structurally related derivatives and investigated their inhibition of MurF enzymes from different bacterial species. Systematic structural modifications of the parent compounds resulted in a series of nanomolar inhibitors of MurF from S. pneumoniae and micromolar inhibitors of MurF from Escherichia coli and Staphylococcus aureus. Some of the inhibitors also show antibacterial activity against S. pneumoniae R6. These findings, together with two new co-crystal structures, represent an excellent starting point for further optimization toward effective novel antibacterials.
- Hrast, Martina,Turk, Samo,Sosi?, Izidor,Knez, Damijan,Randall, Christopher P.,Barreteau, Hélène,Contreras-Martel, Carlos,Dessen, Andréa,O'Neill, Alex J.,Mengin-Lecreulx, Dominique,Blanot, Didier,Gobec, Stanislav
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- 2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS
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The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
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Page/Page column 18
(2011/02/15)
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- Pyrrolopyrimidine Compounds and Their Uses
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The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.
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Page/Page column 45
(2009/12/28)
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- HYDRAZIDE COMPOUNDS AS THYROID HORMONE RECEPTOR MODULATORS AND USES THEREOF
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A method of identification of compounds that modulate thyroid hormone activity, and the use of such compounds and compositions thereof for such purposes are disclosed. The compounds may be selected from the group consisting of: The compounds may be prepar
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- ANTIFUNGAL AGENTS
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Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: Rl, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
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Page/Page column 54-55
(2008/06/13)
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- DIAMINOPYRIMIDINECARBOXA MIDE DERIVATIVE
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A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
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Page/Page column 20
(2008/06/13)
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- 4-Piperidinylimino: A Nearly Linear Head-to-Tail Linking Group for Dipolar Chromophores
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Linkage of the p-aminobenzaldimine and p-nitroaniline chromophores through a piperidine ring gives a compound whose dipole moment is almost exactly the sum of the moments of the constituent chromophores.
- Katz, H. E.,Lavell, W. T.
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p. 2282 - 2284
(2007/10/02)
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- Pyrimidinedione compounds, method of producing the same and antiarrythmic agents containing the same
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A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain containing at least two nitrogen atoms. The pyrimidinedione derivative is useful for a medical treatment of cardiac arrhythmias.
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- Spiro-benzodiazepine-4,4'-piperidine>derivatives as Potential Nootropic Agents: A Simple One-Pot Synthesis
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Some derivatives of a new heterocyclic ring, spiro-benzodiazepine-4,4'-piperidine>, have been obtained in very good yields by a simple one-pot reaction using 1-(2-aminomethylphenyl)-1H-pyrrole and 1-substituted 4-oxopiperidines as t
- Massa, S.,Mai, A.,Artico, M.
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p. 3537 - 3545
(2007/10/02)
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