- LIPID NANOPARTICLE COMPOSITION
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Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination.
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Paragraph 00477
(2021/10/15)
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- Material for adsorbing hexamethyldisiloxane
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TiO2 as a photocatalytic material having excellent performance has the most practical prospects in the field of organic waste gas treatment. Hexamethyldisiloxane is a commonly used solvent with high volatility. When TiO2 photocatalytic treatment is perfor
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Paragraph 0012
(2019/10/01)
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- Design, synthesis, and biological evaluation of radioiodinated benzo[d]imidazole-quinoline derivatives for platelet-derived growth factor receptor β (PDGFRβ) imaging
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Several malignant tumors and fibrotic diseases are associated with PDGFRβ overexpression and excessive signaling, making this receptor attractive for molecular targeting and imaging approaches. A series of benzo[d]imidazole-quinoline derivatives were designed and synthesized to develop radioiodinated compounds as PDGFRβ-specific imaging probes. The structure activity relationship (SAR) evaluation of the designed compounds was performed. Among them, 2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]-8-(piperazin-1-yl)quinoline (5a) and 4-{2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}morpholine (5d) exhibited a relatively high PDGFRβ-TK inhibitory potency, whereas iodinated 5a derivative 5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]-8-(piperazin-1-yl)quinoline (8) exhibited a superior inhibitory potency as PDGFRβ inhibitor than iodinated 5d derivative 4-{5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}morpholine (11). Furthermore, [125I]8 and [125I]11 were synthesized and evaluated for PDGFRβ radioligand ability, both in vitro and in vivo. Cellular uptake experiments showed that [125I]8 had a higher uptake in BxPC3-luc cells as PDGFRβ-positive cells than [125I]11. Incubation of [125I]8 after pretreatment of PDGFRβ ligands significantly reduced the uptake of [125I]8. In biodistribution experiments using tumor-bearing mice, [125I]8 accumulation in the tumor 1 h postinjection was higher than that of the benzo[d]imidazol-quinoline derivative [125I]IIQP, used in our previous research. These results indicate that [125I]8 could be a promising PDGFRβ imaging agent. Although its clinical application requires further structural modifications, the results obtained in this research may be useful for the development of PDGFRβ-specific radioligands.
- Effendi, Nurmaya,Mishiro, Kenji,Takarada, Takeshi,Yamada, Daisuke,Nishii, Ryuichi,Shiba, Kazuhiro,Kinuya, Seigo,Odani, Akira,Ogawa, Kazuma
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p. 383 - 393
(2019/01/04)
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- POLYCYCLIC COMPOUNDS AS INHIBITORS OF BRUTON'S TYROSINE KINASE
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The present disclosure is directed to compounds of Formula (I) as Bruton's kinase inhibitors and their preparation, as well as compositions comprising compounds of Formula (I).
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Page/Page column 103; 123
(2017/07/06)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
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Provided are therapeutically active compounds and the use in manufacture of medicaments for treating a cancer characterized by the presence of a mutant allele of IDH1.
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Page/Page column 64; 65
(2015/02/19)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 64
(2015/02/19)
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- COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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The present invention relates to compounds of formula I: in which n, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a pro
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Paragraph 00217; 00218
(2015/02/25)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column
(2015/03/31)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column
(2015/02/19)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 48-49
(2013/07/31)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 63; 64
(2013/07/31)
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- Synthesis and structure-activity relationship studies on novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione derivatives as anticonvulsant agents
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A series of novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5] decane-2,4-dione derivatives 7-36 was synthesized and their pharmacological activity was determined with the objective to better understand their structure-activity relationship for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) test and their neurotoxic effects were determined by rotarod test. Majority of the compounds were active in MES tests. Compounds 24, 27, and 34 showed a significant and protective effect on seizure, when compared with standard drug phenytoin. The compounds having amide bond showed moderate protective effect on MES induced seizures compared to sulfonamide.
- Madaiah,Prashanth,Revanasiddappa,Veeresh
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p. 2633 - 2644
(2013/07/26)
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- THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column
(2013/07/31)
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- Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket
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The synthesis of novel coumarins bearing on the lateral side chain in the 3-position an amine or a guanidine group is described. In vitro evaluation highlighted 14d which possesses a meta aniline side chain as a very potent THR inhibitor. Surprisingly, the introduction of a guanidine moiety always led to a decrease in THR inhibiting properties. We, thus, used docking experiments to rationalize the SAR in the series. This study showed the crucial role of a conserved water molecule in the specificity pocket of THR during docking simulation in order to explain the inactivity of guanidine derivatives.
- Frederick, Raphael,Charlier, Caroline,Robert, Severine,Wouters, Johan,Masereel, Bernard,Pochet, Lionel
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p. 2017 - 2021
(2007/10/03)
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- INHIBITORS OF PHOSPHODIESTERASE TYPE-IV
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The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
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Page/Page column 72
(2010/02/11)
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- 4-AMINO-5-PHENYL-7-CYCLOHEXYL-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES
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The invention relates to new 4-amino-5-phenyl-7-cyclohexyl-pyrrolo[2,3-d] pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in comb
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- Substituted quinazolinone compounds
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A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variab
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- Optically active 1,4-dihydropyridine compounds as bradykinin antagonists
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This invention provides a compound of the formula (I): and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; R1 and R2 are independently C1-4 alkyl; R3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group sele
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- TOCOLYTIC OXYTOCIN RECEPTOR ANTAGONISTS
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This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery. A typical compound is as follows: STR1
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- Ornithine decarboxylase inhibiting cyclic aminooxy compounds
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Compounds of formula (I): H2 N--(CH2)n --A--(CH2)m --O--NH2 and salts thereof are described in which the radical A is C3 -C6 cycloalkylene; n is 0 or 1 and, independen
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- MUSCARINE ANTAGONISTS
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Compounds, 1,3-dihydro-1-{1-[piperidin-4-yl]piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
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- Amine derivatives and process for producing the same
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An amine derivative having a liquid crystal property over a wide temperature range and a process for production thereof are disclosed, the amine derivative being represented by formula (I) STR1 wherein A represents STR2 X1 and X2, which may be the same or different, each represents STR3 Y represents --O-- or STR4 R1 and R3, which may be the same or different, each represents a straight chain or branched chain alkyl group having 1 to 18 carbon atoms; R2 represents a hydrogen atom or a methyl group; m and n each represents 0 or 1; and p and q each represents 1 or 2, provided that p and q are 1 when n is 0, and p and q are not 2 at the same time when n is 1.
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