- METHODS OF EXTENDING LIFESPAN BY ADMINISTERING FERROPTOSIS INHIBITORS
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Provided herein is a method of extending the lifespan of an organism comprising administering to the organism an effective amount of a ferroptosis inhibitor. Also provided are compositions for extending lifespan comprising ferroptosis inhibitors.
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Paragraph 237; 251
(2022/02/05)
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- PYRIDOPYRIMIDINES AND METHODS OF THEIR USE
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Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.
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Page/Page column 57; 58
(2021/12/28)
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- ION CHANNEL INHIBITOR COMPOUNDS FOR CANCER TREATMENT
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The present invention concerns a compound of following general formula (I): where: either R is an R1 group and R′ is an -A1-Cy1 group, or R is an -A1-Cy1 group and R′ is an R1 group, R1 particularly being H or (C1-C6)alkyl group;A1 being an —NH— radical or —NH—CH2— radical;Cy1 particularly being a phenyl group,A is a fused (hetero)aromatic ring having 5 to 7 atoms, for use for treating cancer.
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Paragraph 0215; 0216
(2021/01/25)
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- HETEROAROMATIC AND HETEROBICYCLIC AROMATIC DERIVATIVES FOR THE TREATMENT OF FERROPTOSIS-RELATED DISORDERS
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The present application discloses heteroaromatic and heterobicyclic aromatic derivative compounds and compositions, and methods for treating ferroptosis-related disorders and diseases in patients using the compounds and compositions as disclosed herein.
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Paragraph 0248
(2020/09/27)
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- Pyrimidine derivatives, preparation method therefor and application of pyrimidine derivatives
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The invention belongs to the field of drug synthesis and relates to novel pyrimidine derivatives, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, preparation methods of thenovel pyrimidine derivatives and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof and use of the novel pyrimidine derivatives and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof in preparation of therapeutic agents, particularly PAK inhibitors. The derivatives disclosed by the invention are represented by a general formula (I) or (II), wherein each substituent is as defined in claims.
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Paragraph 0150; 0151; 0155; 0156; 0177; 0178
(2018/03/26)
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- Synthesis and structure-activity relationship of: N 4-benzylamine- N 2-isopropyl-quinazoline-2,4-diamines derivatives as potential antibacterial agents
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A series of N4-benzylamine-N2-isopropyl-quinazoline-2,4-diamine derivatives has been synthesized and tested for antibacterial activity against five bacterial strains. Twelve different substituents on the N4-benzylamine group have been investigated along with replacement of the quinazoline core (with either a benzothiophene or regioisomeric pyridopyrimidine ring systems). In order to develop structure activity relationships, all derivatives were tested for their antibacterial activities against Escherichia coli and Staphylococcus aureus via Kirby-Bauer assays and minimum inhibitory concentration assays. Eight of the most potent compounds against S. aureus and E. coli were also screened against one strain of methicillin-resistant S. aureus (MRSA), Staphylococcus epidermidis and Salmonella typhimurium to further examine their antibacterial activities. Lead compound A5 showed good activities with MICs of 3.9 μg mL-1 against E. coli, S. aureus and S. epidermidis and 7.8 μg mL-1 against MRSA. Selected front runners were also screened for their DMPK properties in vitro to assess their potential for further development.
- Jiang, Zhengyun,Hong, W. David,Cui, Xiping,Gao, Hongcan,Wu, Panpan,Chen, Yingshan,Shen, Ding,Yang, Yang,Zhang, Bingjie,Taylor, Mark J.,Ward, Stephen A.,O'Neill, Paul M.,Zhao, Suqing,Zhang, Kun
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p. 52227 - 52237
(2017/11/22)
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- Application of quinazoline and pyrido[3,2-: D] pyrimidine templates to design multi-targeting agents in Alzheimer's disease
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A quinazoline and pyrido[3,2-d]pyrimidine based compound library was designed, synthesized and evaluated as multi-targeting agents aimed at Alzheimer's disease (AD). The SAR studies identified compound 8h (8-chloro-N2-isopropyl-N4-ph
- Mohamed, Tarek,Mann, Mandeep K.,Rao, Praveen P. N.
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p. 22360 - 22368
(2017/07/10)
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- 2,4-quinazolinediamine derivatives, and preparation method and application thereof
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The invention discloses 2,4-quinazolinediamine derivatives, and a preparation method and application thereof, belonging to the field of medicines and preparation and application thereof. The 2,4-quinazolinediamine derivatives comprises compounds as shown in a formula (I) which is described in the specification and a solvate, hydrate, tautomer and pharmaceutically acceptable salt thereof. Test results show that the 2,4-quinazolinediamine derivatives have strong Wolbachia resisting activity; and in the derivatives, 2-isopropylamido substitution has good effect, and compounds with better Wolbachia resisting activity can be obtained by changing a 4-amido group. The compounds have activity in resisting plasmodia, Wolbachia and bacteria.
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Paragraph 0185; 0188; 0189
(2017/04/18)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Paragraph 00651
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Page/Page column 145
(2012/05/21)
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- Solvent-free or low-solvent large-scale preparation of chloropyrimidine and analogues
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Chloropyrimidine or other N-containing aromatic heterocyclic analogues can be efficiently prepared from the corresponding hydroxylated precursors under solvent-free or low-solvent conditions with equimolar or less chlorinating reagents. This high-yielding protocol allows successful preparations of multigram and kilogram batches of these important synthetic intermediates.
- Sun, Zhihua,Wang, Han,Wen, Kun,Li, Ya,Fan, Erkang
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experimental part
p. 4149 - 4153
(2011/07/07)
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- 4-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES
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This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune deseases, inflammatory disorders, multiple sclerosis and other deseases like cancers.
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Page/Page column 61
(2010/04/27)
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- The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
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We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.
- Malagu, Karine,Duggan, Heather,Menear, Keith,Hummersone, Marc,Gomez, Sylvie,Bailey, Christine,Edwards, Peter,Drzewiecki, Jan,Leroux, Frederic,Quesada, Mar Jimenez,Hermann, Gesine,Maine, Stephanie,Molyneaux, Carrie-Anne,Le Gall, Armelle,Pullen, James,Hickson, Ian,Smith, Lisa,Maguire, Sharon,Martin, Niall,Smith, Graeme,Pass, Martin
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scheme or table
p. 5950 - 5953
(2010/07/05)
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- Compounds
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Compounds of formula l: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to
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Page/Page column 13
(2008/06/13)
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- Efficient access to novel mono- and disubstituted pyrido[3,2-d]pyrimidines
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New mono- and disubstituted pyrido[3,2-d]pyrimidines were synthesized starting from the corresponding 2,4-dichloro derivative through SNAr and palladium-catalyzed reactions. SNAr and palladium-catalyzed hydro-deshalogenation occurred
- Tikad, Abdellatif,Routier, Sylvain,Akssira, Mohamed,Leger, Jean-Michel,Jarry, Christian,Guillaume, Gérald
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p. 1938 - 1942
(2008/02/08)
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