- Discovery of 2H-chromone-4-one based sulfonamide derivatives as potent retinoic acid receptor-related orphan receptor γt inverse agonists
-
Retinoic acid receptor related orphan receptor γt (RORγt), identified as the essential functional regulator of IL-17 producing Th17 cells, is an attractive drug target for treating autoimmune diseases. Starting from the reported GSK2981278 (Phase II), we structurally modified and synthesized a series of 2H-chromone-4-one based sulfonamide derivatives as novel RORγt inverse agonists, which significantly improved their human metabolic stabilities while maintaining a potent RORγt inverse agonist profile. Efforts in reducing the lipophilicity and improving the LLE values led to the discovery of c9, which demonstrated potent RORγt inverse agonistic activity and consistent metabolic stability. During in vivo studies, oral administration of compound c9 exhibited a robust and dose-dependent inhibition of IL-17A cytokine expression and significantly lessened the skin inflammatory symptoms in the mouse imiquimod-induced skin inflammation model. Docking analysis of the binding mode revealed that c9 can suitably occupy the active pocket, and the introduction of the morpholine pyridine group can interact with Leu396, His479, and Cys393. Thus, compound c9 was selected as a preclinical compound for treating Th17-driven autoimmune diseases.
- Assani, Israa,Chen, Lei,Huang, Ri-Zhen,Jin, Qiu,Kang, Yang-yang,Li, Yan,Liao, Zhi-Xin,Lv, Shen-Min,Su, Mei,Sun, Bo,Wang, Chun-Gu,Wang, De-Zhong,Wang, Jia-Wei,Wang, Mu-Xuan,Wu, Xian-Zhi,Zhao, Shi-Feng
-
-
- COMPOUNDS AND USES THEREOF
-
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
- -
-
-
- COMPOUNDS AND USES THEREOF
-
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
- -
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Page/Page column 71
(2021/08/06)
-
- Palladium-Catalyzed Tandem Carbonylative Diels-Alder Reaction for Construction of Bridged Polycyclic Skeletons
-
A palladium-catalyzed tandem carbonylative lactonization and Diels-Alder cycloaddition reaction between aldehyde-tethered benzylhalides and alkenes has been developed. A range of alkenes and aldehyde-tethered benzylhalides bearing different substituents can be successfully transformed into the corresponding bridged polycyclic compounds in good yields. This strategy provides a unique approach to complex lactone-containing bridged polycyclic compounds.
- Wang, Siyuan,Zhou, Yangkun,Huang, Hanmin
-
p. 2125 - 2129
(2021/04/05)
-
- Copper-promoted direct amidation of isoindolinone scaffolds by sodium persulfate
-
Isoindolinones are ubiquitous structural motifs in natural products and pharmaceuticals. Establishing an efficient method for structural modification of isoindolinones could significantly facilitate new drug development. Herein, we describe copper-promoted direct amidation of isoindolinone scaffolds mediated by sodium persulfate. The method exhibits mild reaction conditions and high site-selectivity, and enables the structural modification of the drug indobufen ester with various amides with yields of 49 to 98%. It is also gram-scalable. Additionally, the reaction mechanism appears to involve a radical and a carbocationic pathway.
- Lai, Huifang,Lin, Jin,Xu, Jiexin,Zha, Daijun
-
p. 7621 - 7626
(2021/09/22)
-
- Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase
-
Aberrant activity of the histone methyltransferase polycomb repressive complex 2 (PRC2) has been linked to several cancers, with small-molecule inhibitors of the catalytic subunit of the PRC2 enhancer of zeste homologue 2 (EZH2) being recently approved fo
- Bagal, Sharan K.,Barton, Peter,Bloecher, Andrew,Borodovsky, Alexandra,Code, Erin,Fillery, Shaun M.,Gregson, Clare,Hsu, Jessie Hao-Ru,Kawatkar, Sameer P.,Li, Chengzhi,Longmire, David,Nai, Youfeng,Nash, Samuel C.,O' Donovan, Daniel H.,Pike, Andrew,Pike, Kurt G.,Rawlins, Phillip B.,Read, Jon A.,Robinson, James,Shen, Minhui,Tang, Jia,Wang, Peng,Williamson, Beth,Woods, Haley
-
p. 17146 - 17183
(2021/12/06)
-
- Photocatalytic continuous bromination method
-
The invention provides a photocatalytic continuous bromination method. The method comprises the following steps: carrying out a first-stage photocatalytic continuous bromination reaction on a materialcontaining an aromatic substrate with a structural general formula I and a bromination reagent in a first continuous illumination reactor to form a first continuous system; overflowing the obtained first continuous system into a second continuous illumination reactor for a second-stage photocatalytic continuous bromination reaction to form a second continuous system; and purifying the second continuous system, wherein the structural general formula I is shown in the specification, R is selected from any one of carboxyl, ester group, NO2, CN, C1 to C8 alkyl and alkoxy, and R1 is C1 to C8 alkyl; n is 1 or 2; X is N or C, and the bromination reagent is Nbromo succinimide or dibromohydantoin. According to the bromination reagent, the selectivity of a product is improved, so the yield of the product is improved; the photocatalytic continuous bromination reaction of the two stages effectively relieves the reaction heat accumulation, and enhances the yield of the target product.
- -
-
Paragraph 0062-0063
(2021/04/03)
-
- ISOINDOLIN-1-ON DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE COMPONENT FOR PREVENTING OR TREATING CANCER
-
The present invention relates to an isoindolin-1-one derivative, a method for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating cancer, wherein the isoindolin-1-one derivative exhib
- -
-
Paragraph 0104-0106
(2021/06/25)
-
- COMPOUNDS AND USES THEREOF
-
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
- -
-
Page/Page column 31
(2021/08/06)
-
- COMPOUNDS
-
This disclosure relates to compounds of formula (I), which are modulators of STING. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods of using compounds of formula (I) in the treatment or prevention of diseases
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Page/Page column 105
(2021/06/26)
-
- COMPOUNDS AND USES THEREOF
-
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
- -
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Paragraph 0155-0157
(2021/07/30)
-
- One-pot method to construct isoindolinones and its application to the synthesis of DWP205109 and intermediate of Lenalidomide
-
Herein a practical and efficient system for concise synthesis of isoindolinones is described by using substituted methyl 2-(halomethyl)benzoates and substituted amines. Structurally various methyl 2-(halomethyl)benzoates and amines were transformed into isoindolinones 80–99% yield and purity in catalyst-free and solvent-free conditions. The method has a wide substrate scope. The synthetic utility of the one-pot reaction was demonstrated by the concise syntheses of Lenalidomide intermediate and DWP205190.
- Liu, Jinbiao,Lu, Bowei,Lu, Junrui,Wang, Hongbo,Xie, Zhiqiang,Zhong, Kaikai
-
supporting information
(2021/06/07)
-
- NOVEL PIPERIDINE-2,6-DIONE DERIVATIVE AND USE THEREOF
-
The present disclosure relates to a novel piperidine-2,6-dione derivative and a use thereof and, more specifically, to a piperidine-2,6-dione derivative compound having a structure of a thalidomide analog. A compound of chemical formula 1 according to the present disclosure specifically binds with CRBN protein, and is involved in functions thereof. Therefore, the compound of the present disclosure can be favorably used in the prevention or treatment of leprosy, chronic graft versus host disease, an inflammatory disease, or cancer, which are caused by actions of CRBN protein.
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-
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- PFKFB3 INHIBITORS AND THEIR USES
-
This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventiions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.
- -
-
-
- COMPOUNDS AND USES THEREOF
-
The present invention relates to methods and compositions for the treatment of BAF-related disorders such as cancers and viral infections.
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-
Page/Page column 357
(2020/08/22)
-
- BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
-
The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
- -
-
Paragraph 0713; 0714; 0715
(2020/05/21)
-
- Aminopyrazine/pyridine compound and preparation method and application thereof
-
The invention discloses an aminopyrazine/pyridine compound and a preparation method and application thereof. Particularly, a pyrazine/pyridylamine compound shown as a general formula I, or pharmaceutically acceptable salt thereof, or enantiomer, diastereoisomer, tautomer, solvate, polymorphic substance or prodrug thereof, a preparation method thereof and application in pharmacy are disclosed, andthe definition of each group is shown in the specification.
- -
-
Paragraph 0158-0160
(2020/05/05)
-
- BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
-
The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
- -
-
Paragraph 0483-0485; 0507-0509
(2020/08/28)
-
- Synthesis and Broad Antiviral Activity of Novel 2-aryl-isoindolin-1-ones towards Diverse Enterovirus A71 Clinical Isolates
-
Enterovirus 71 (EV-A71) is the main causative pathogen of childhood hand, foot and mouth disease. Effective medicine is currently unavailable for the treatment of this viral disease. Using the fragment-hopping strategy, a series of 2-aryl-isoindolin-1-one compounds were designed, synthesized and investigated for their in vitro antiviral activity towards multiple EV-A71 clinical isolates (H, BrCr, Shenzhen98, Jiangsu52) in Vero cell culture in this study. The structure–activity relationship (SAR) studies identified 2-phenyl-isoindolin-1-ones as a new potent chemotype with potent antiviral activity against EV-A71. Ten out of the 24 tested compounds showed significant antiviral activity (EC50 50) values in the range of 1.23–1.76 μM. Moreover, the selectivity indices of A3 and A4 were significantly higher than those of the reference compound, pirodavir. The western blotting experiment indicated that the viral VP1 was significantly decreased at both the protein and RNA level in a dose-dependent manner following treatment with compound A3. Moreover, compound A3 inhibited the viral replication by acting on the virus entry stage. In summary, this study led to the discovery of 2-aryl-isoindolin-1-ones as a promising scaffold with potent anti-EV-A71 activities, which deserves further in-depth studies.
- Wang, Yixuan,Wang, Huiqiang,Jiang, Xinbei,Jiang, Zhi,Guo, Tingting,Ji, Xingyue,Li, Yanping,Li, Yuhuan,Li, Zhuorong
-
-
- Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors
-
Dipeptidyl Peptidase-IV (DPP-4) is a validated therapeutic target for type 2 diabetes. Aiming to interact with both residues Try629 and Lys554 in S2′ site, a series of novel uracil derivatives 1a–l and 2a–i incorporating benzoic acid moieties at the N3 position were designed and evaluated for their DPP-4 inhibitory activity. Structure-activity relationships (SAR) study led to the identification of the optimal compound 2b as a potent and selective DPP-4 inhibitor (IC50 = 1.7 nM). Docking study revealed the additional salt bridge formed between the carboxylic acid and primary amine of Lys554 has a key role in the enhancement of the activity. Furthermore, compound 2b exhibited no cytotoxicity in human hepatocyte LO2 cells up to 50 μM. Subsequent in vivo evaluations revealed that the ester of 2b robustly improves the glucose tolerance in normal mice. The overall results have shown that compound 2b has the potential to a safe and efficacious treatment for T2DM.
- Huang, Junli,Deng, Xiaoyan,Zhou, Siru,Wang, Na,Qin, Yujun,Meng, Liuwei,Li, Guobao,Xiong, Yuhua,Fan, Yating,Guo, Ling,Lan, Danni,Xing, Junhao,Jiang, Weizhe,Li, Qing
-
p. 644 - 654
(2019/01/14)
-
- Rapid generation of novel benzoic acid–based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study
-
A series of novel xanthine derivatives 2a-l incorporating benzoic acid moieties were rapidly generated by using strategy of scaffold-hopping from our previously reported scaffold uracil to xanthine, a scaffold of approved drug linagliptin. After systematic structure-activity relationship (SAR) study around benzoic acid moieties, 5 novel DPP-4 inhibitors with low picomolar potency range (IC50 50 value of 0.1 nM for DPP-4, showed 22-fold improvement in inhibitory activity compared to lead compound uracil 1, its activity was 45-fold more potent than alogliptin. 2e, 2f, 2i and 2k were selected for pharmacokinetic evaluation, and 2f and 2i showed the better pharmacokinetic profiles after iv administration, but poor oral bioavailability. To improve the oral pharmacokinetic profile, prodrug design approach was performed around 2f and 2i. Esters of 2f and 2i were synthesized and evaluated for stability, toxicity and pharmacokinetics. Compound 3e, the methyl ester of compound 2f, was identified to demonstrate good stability, low toxicity and improved oral bioavailability, with 3-fold higher blood concentration compared to 2f in rats. The following in vivo evaluations revealed 3e provided a sustained pharmacodynamics effect for 48h, and robustly improved glucose tolerance in normal ICR and db/db mice in dose-dependent manner. Chronic treatments investigations demonstrated that 3e achieved more beneficial effects on fasting blood glucose levels and glucose tolerance than alogliptin in type 2 diabetic db/db mice. The overall results have shown that compound 3e has the potential to efficacious, safety and long-acting treatment for T2DM.
- Li, Qing,Meng, Liuwei,Zhou, Siru,Deng, Xiaoyan,Wang, Na,Ji, Yi,Peng, Yichun,Xing, Junhao,Yao, Gongmei
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p. 509 - 523
(2019/07/25)
-
- ASK1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
-
The present disclosure relates to a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.
- -
-
Paragraph 0233
(2020/01/02)
-
- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF RAS AND METHODS OF USE THEREOF
-
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R", Q, W, X, Y, Z, n1, n2and '--" are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also disclosed.
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Page/Page column 144
(2018/04/21)
-
- HETEROCYCLIC COMPOUND
-
The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerati
- -
-
Paragraph 0263
(2018/06/07)
-
- 6-PYRIMIDIN-ISOINDOLE DERIVATIVE AS ERK1/2 INHIBITOR
-
This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1 -oxo-2,3-dihydro-1 H-isoindol-2-yl)-N-[(1 S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compoun
- -
-
Page/Page column 70; 71
(2018/11/22)
-
- Preparation method for 5-bromoisoindoline hydrochloride
-
The invention provides a preparation method for 5-bromoisoindoline hydrochloride. The method comprises the following steps: firstly esterifying 5-bromine-2-methyl benzoic acid, and then brominating methyl NBS, cyclizing and reducing with borane, thereby o
- -
-
-
- Synthesis, computational, and spectroscopic analysis of tunable highly fluorescent BN-1,2-azaborine derivatives containing the N-BOH moiety
-
Nine new polycyclic aromatic BN-1,2-azaborine analogues containing the N-BOH moiety were synthesized using a convenient two-step, one-pot procedure. Characterization of the prepared compounds show the luminescence wavelength and the quantum yields of the azaborines were tunable by controlling the power and location of the donor and acceptor substituents on the chromophore. UV-visible spectroscopy and density functional theory (DFT) computations revealed that the addition of electron-donating moieties to the isoindolinone hemisphere raised the energy of the HOMO, resulting in the reduction of the HOMO-LUMO gap. The addition of an electron-accepting moiety to the isoindolinone hemisphere and an electron-donating group to the boronic acid hemisphere decreased the HOMO-LUMO gap considerably, leading to emission properties from partial intramolecular charge transfer (ICT) states. The combined effect of an acceptor on the isoindolinone side and a donor on the boronic acid side (strong acceptor-π-donor) gave the most red-shifted absorption. The polycyclic aromatic BN-1,2-azaborines emitted strong fluorescence in solution and in the solid-state with the largest red-shifted emission at 640 nm and a Stokes shift of Δλ = 218 nm, or Δν = 8070 cm-1.
- Saint-Louis, Carl Jacky,Shavnore, Renée N.,McClinton, Caleb D. C.,Wilson, Julie A.,Magill, Lacey L.,Brown, Breanna M.,Lamb, Robert W.,Webster, Charles Edwin,Schrock, Alan K.,Huggins, Michael T.
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p. 10172 - 10183
(2017/12/26)
-
- HETEROCYCLIC COMPOUND
-
The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases, Charcot-Marie-Tooth disease and the like, and a pharmaceutical composition comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
- -
-
Paragraph 1076-1077
(2017/02/09)
-
- ISOINDOLINE-1-ONE DERIVATIVES AS CHOLINERGIC MUSCARINIC M1 RECEPTOR POSITIVE ALLOESTERIC MODULATOR ACTIVITY FOR THE TREATMENT OF ALZHEIMERS DISEASE
-
The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. (I) wherein each symbol is as described in the specification, or a salt thereof.
- -
-
Paragraph 0332
(2015/11/10)
-
- Series of structural and functional models for the ES (enzyme-substrate) complex of the Co(II)-containing quercetin 2,3-dioxygenase
-
A series of mononuclear CoII-flavonolate complexes [Co IILR(fla)] (LRH = 2-{[bis(pyridin-2-ylmethyl) amino]methyl}-p/m-R-benzoic acid; R = p-OMe (1), p-Me (2), m-Br (4), and m-NO2 (5); fla = flavonolate) were designed and synthesized as structural and functional models for the ES (enzyme-substrate) complexes to mimic the active site of the Co(II)-containing quercetin 2,3-dioxygenase (Co-2,3-QD). The metal center Co(II) ion in each complex shows a similar distorted octahedral geometry. The model complexes display high enzyme-type dioxygenation reactivity (oxidative O-heterocyclic ring opening of the coordinated substrate flavonolate) at low temperature, presumably due to the attached carboxylate group in the ligands. The reactivity exhibits a substituent group dependent order of -OMe (1) > -Me (2) > -H (3)14b > -Br (4) > -NO2 (5), and the Hammett plot is linear (ρ = -0.78). This can be explained as the electronic nature of the substituent group in the ligands may influence the conformation and redox potential of the bound flavonolate and finally bring different reactivity. The structures, properties, and reactivity of the model complexes show some dependence on the substituent group in the supporting model ligands, and there is some relationship among them. This study is the first example of a series of structural and functional ES models of Co-2,3-QD, with focus on the effects of the electronic nature of substituted groups and the carboxylate group of the ligands to the dioxygenation reactivity, that will provide important insights into the structure-property-reactivity relationship and the catalytic role of Co-2,3-QD.
- Sun, Ying-Ji,Huang, Qian-Qian,Zhang, Jian-Jun
-
p. 2932 - 2942
(2014/04/03)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE
-
This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
- -
-
-
- Ep1 receptor ligands
-
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation,
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-
-
- EP1 RECEPTOR LIGANDS
-
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 70
(2013/03/28)
-
- INHIBITORS OF DIACYLGLYCEROL ACYL TRANSFERASE
-
The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
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-
-
- Synthesis of N-methyl-6-heterocyclic-1-oxoisoindoline derivatives by microwave assisted buchwald-hartwig amination
-
An rapid and efficient microwave assisted Pd(II) catalyzed protocol for the preparation of N-methyl-6-heterocyclic-1-oxoisoindoline derivatives by Buchwald-Hartwig amination with an overall yield 68-85% has been described.
- Kishor Kumar,Vijay Kumar,Naik, Nagaraja
-
scheme or table
p. 1108 - 1113
(2012/06/15)
-
- MODULATORS OF ATP-BINDING CASSETTE-TRANSPORTERS
-
Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (""ABC"") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (""CFTR""). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
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-
-
- ANTI-VIRAL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE
-
Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses.
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-
-
- 2-METHYLMORPHOLINE PYRIDO-, PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS
-
There is provided a compound of Formula (I), or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula (1), and the use of a compound of Formula (1) as a medicament and in the treatment of cancer
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Page/Page column 116-117
(2008/06/13)
-
- Synthetic strategies to derivatizable triphenylamines displaying high two-photon absorption
-
(Chemical Equation Presented) A versatile synthetic strategy to access a set of highly fluorescent π-conjugated triphenylamines bearing a functional linker at various positions on one phenyl ring is described. These compounds were designed for large two-photon absorption (2PA) and in particular for labeling of biomolecules. The monoderivatized trisformylated or trisiodinated intermediates described herein allow introduction of a large variety of electron-withdrawing groups required for large 2PA as well as a panel of chemical functions suitable for coupling to biomolecules. The monoderivatized three-branched compounds and in particular the benzothiazole (TP-3Bz) series show remarkable linear (high extinction coefficients and high quantum yield) and nonlinear (high 2-photon cross sections) optical properties. Interestingly the presence of functional side chains does not disturb the two-photon absorption. Finally, monoderivatized two-branched derivatives also appear to be valuable candidates. Altogether the good optical properties of the new derivatizable π-conjugated TPA combined with their small size and their compatibility with bioconjugation protocols suggest that they represent a new chemical class of labels potentially applicable for the tracking of biomolecules using two-photon scanning microscopy.
- Lartia, Remy,Allain, Clemence,Bordeau, Guillaume,Schmidt, Falk,Fiorini-Debuisschert, Celine,Charra, Fabrice,Teulade-Fichou, Marie-Paule
-
p. 1732 - 1744
(2008/09/18)
-
- ISOINDOLE DERIVATIVES
-
This invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, a process of making these compounds, pharmaceutical compositions containing one or more of these compounds or their salts, and their use for the treatment of schizophrenia, bipolar disorder, or other central nervous system disorders.
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Page/Page column 38
(2010/11/30)
-
- Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase
-
The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene-5,4′-imidazol]-5′(1′H)-one compound of formula I Also provided are methods and compositions for the inhibition of β-secretase (BACE) and the treatment of β-amyloid deposits and neurofibrillary tangles.
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Page/Page column 8; 10
(2008/06/13)
-
- NOVEL 2-(1-AZA-BICYCLO[2.2.2]OCT-3-yl)-2,3-DIHYDROISOINDOL-l-ONE/5,6-DIHYDRO-FURO[2,3-c]PYRROL-4ONE DERIVATIVES LIGANDS FOR ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR
-
This invention encompasses nicotinic acetylcholine receptor-reactive compounds in accord with formula (I) Wherein: D represents O; E represents CH2, NH, O or S; n is 1 or 2 and stereoisomers, enantiomers, in vivo-hydrolysable precursors and pharmaceutically-acceptable salts of such compounds, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them, uses of them as medicaments, uses of them in the manufacture of medicaments and uses of them for diagnostic and analytic purposes.
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Page/Page column 13; 16
(2008/06/13)
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS
-
The present invention relates to a selective estrogen receptor modulators of formula I (I); or a pharmaceutical acid addition salt thereof; and of formula II (II); or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
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Page/Page column 27-28
(2010/02/13)
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- Dibenz[b,e]oxepin compounds
-
Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
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-