- Inhibition of 3D colon cancer stem cell spheroids by cytotoxic RuII-p-cymene complexes of mesalazine derivatives
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The Ru(ii) complex of an imidazole-mesalazine Schiff base is a unique example showing growth inhibition of 3D-colon cancer stem cell spheroids and bulk colon cancer cells at lower dosage than salinomycin or oxaliplatin. Unlike oxaliplatin which increases
- Acharya, Sourav,Ghosh, Subhashis,Maji, Moumita,Mukherjee, Arindam,Parambil, Ajmal Roshan Unniram,Singh, Sandeep
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Read Online
- PYROPTOSIS-INDUCED IMMUNOTHERAPY
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Pyroptosis-induced immunotherapy is effected by activating a pore-forming, pyrpotogenic molecule, wherein the activating induces tumor cell pryoptosis and causes tumor regression by T-cell mediated anti-tumor immunity.
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Paragraph 041; 074
(2021/03/05)
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- EIF4E INHIBITORS AND USES THEREOF
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The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
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Paragraph 00506; 00520
(2021/09/11)
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- MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
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Paragraph 00308-00310
(2021/12/08)
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- Synthesis and biological evaluation of salicylic acid analogues of celecoxib as a new class of selective cyclooxygenase-1 inhibitor
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A series of salicylic acid analogues of celecoxib where the phenylsulfonamide moiety in the structure of celecoxib is replaced by salicylic acid moiety was synthesized and tested for in vitro cyclooxygenase (COX)-1 and COX-2 enzyme inhibition. Among the series, 5-substituted-2-hydroxy-benzoic acid analogues (7a–7h) generally showed better inhibitory activities on both enzymes than 4-substituted-2-hydroxy-ben-zoic acid analogues (12a–12h). In particular, the chloro analogue 7f which had the highest inhibitory effect (IC50=0.0057μM) to COX-1 with excellent COX-1 selectivity (SI=768) can be classified as a new potent and selective COX-1 inhibitor. The high inhibitory potency of 7f was rationalized through the docking simulation of this analogue in the active site of COX-1 enzyme.
- Yoon, Sung-Hwa,Cho, Duk-Yeon,Choi, Seoung-Ryoung,Lee, Joo-Young,Choi, Dong-Kug,Kim, Eunha,Park, Ju-Young
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p. 1230 - 1238
(2021/09/06)
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- A bioorthogonal system reveals antitumour immune function of pyroptosis
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Bioorthogonal chemistry capable of operating in live animals is needed to investigate biological processes such as cell death and immunity. Recent studies have identified a gasdermin family of pore-forming proteins that executes inflammasome-dependent and
- Ding, Jingjin,Gao, Wenqing,Huang, Huanwei,Liu, Zhibo,Shao, Feng,Wang, Chunhong,Wang, Qinyang,Wang, Yupeng,Zhou, Xuehan
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- Carbonyl Sulfide (COS) Donor Induced Protein Persulfidation Protects against Oxidative Stress
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The emergence of hydrogen sulfide (H2S) as an important signalling molecule in redox biology with therapeutic potential has triggered interest in generating this molecule within cells. One strategy that has been proposed is to use carbonyl sulfide (COS) as a surrogate for hydrogen sulfide. Small molecules that generate COS have been shown to produce hydrogen sulfide in the presence of carbonic anhydrase, a widely prevalent enzyme. However, other studies have indicated that COS may have biological effects which are distinct from H2S. Thus, it would be useful to develop tools to compare (and contrast) effects of COS and H2S. Here we report enzyme-activated COS donors that are capable of inducing protein persulfidation, which is symptomatic of generation of hydrogen sulfide. The COS donors are also capable of mitigating stress induced by elevated reactive oxygen species. Together, our data suggests that the effects of COS parallel that of hydrogen sulfide, laying the foundation for further development of these donors as possible therapeutic agents.
- Chauhan, Preeti,Gupta, Kavya,Ravikumar, Govindan,Saini, Deepak K.,Chakrapani, Harinath
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supporting information
p. 4717 - 4724
(2019/11/03)
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- Synthesis, characterization, and cytotoxic evaluation of some newly substituted diazene candidates
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A series of azocompounds containing methyl salicylate 4a-k and 1-naphthyl moiety 6-8 was synthesized and tested as anticancer agents. Nitrosation of methyl 5-amino-2-hydroxybenzoate or 1-aminonaphthalene by using NaNO2 in the presence of HCl af
- El-Naggar, Mohamed,El-Shorbagi, Abdel-Nasser,Elnaggar, Dina H.,Amr, Abd El-Galil E.,Al-Omar, Mohamed A.,Elsayed, Elsayed A.
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- Fe-Catalyzed Amination of (Hetero)Arenes with a Redox-Active Aminating Reagent under Mild Conditions
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A novel and efficient Fe-catalyzed direct C?H amination (NH2) of arenes is reported using a new redox-active aminating reagent. The reaction is simple, and can be performed under air, mild, and redox-neutral conditions. This protocol has a broad substrate scope and could be used in the late-stage modification of bioactive compounds. Mechanistic studies demonstrate that a radical pathway could be involved in this transformation.
- Liu, Jianzhong,Wu, Kai,Shen, Tao,Liang, Yujie,Zou, Miancheng,Zhu, Yuchao,Li, Xinwei,Li, Xinyao,Jiao, Ning
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supporting information
p. 563 - 567
(2017/01/18)
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- 4-substituted pyridine-2-formamide compound, preparation method thereof and application
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The invention discloses a 4-substituted pyridine-2-formamide compound, a preparation method thereof and an application. The 4-substituted pyridine-2-formamide compound has a structure as shown in a formula I, and the chemical name of the compound is 4-{4-[3-(4-chlorine-3-trifluoromethyl-phenyl)-ureide]-3-carboxyl phenoxy}-N-picoline-2-carboxylic methylamine. According to the preparation method of the 4-substituted pyridine-2-formamide compound, 4-chlorine-2-picolinic acid serves as an initial raw material, and the compound in the formula I is prepared by acylating chlorination, amination, substitution reaction and condensation reaction. The 4-substituted pyridine-2-formamide compound retains a Sorafenib efficacy structure, 5-aminosalicylic acid or aminosalicylic acid ester achieving a positive pharmacological function in the metabolic process replaces p-aminophenol with large toxic and side effects, efficacy can be improved, and the toxic and side effects are reduced.
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Paragraph 0059-0063
(2018/03/28)
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- Calcium Coordination Solids for pH-Triggered Release of Olsalazine
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Calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H4olz), an anti-inflammatory compound used for treatment of ulcerative colitis. The materials include one-dimensional Ca(H2olz)?4 H2O chains, two-dimensional Ca(H2olz)?2 H2O sheets, and a three-dimensional metal-organic framework Ca(H2olz)?2DMF (DMF=N,N-dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H2olz) phase when exposed to aqueous HCl. The compounds Ca(H2olz)?x H2O (x=0, 2, 4) were each pressed into pellets and exposed to simulated gastrointestinal fluids to mimic the passage of a pill from the acidic stomach to the pH-neutral intestines. All three calcium materials exhibited a delayed release of olsalazine relative to Na2(H2olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.
- Levine, Dana J.,Gonzalez, Miguel I.,Legendre, Christina M.,Run?evski, Tom?e,Oktawiec, Julia,Colwell, Kristen A.,Long, Jeffrey R.
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supporting information
p. 1739 - 1742
(2017/11/15)
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- Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase
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Through structure-based virtual screening and subsequent activity assays of selected natural products, Lavendustin B was previously identified as an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF/p75). In order to improve the inhibitory potency we have employed in silico-based approaches. Particularly, a series of new analogues was designed and docked into the LEDGF/p75 binding pocket of HIV-1 IN. To identify promising leads we used the Molecular Mechanics energies combined with the Generalized Born and Surface Area continuum solvation (MM-GBSA) method, molecular dynamics simulations and analysis of hydrogen bond occupancies. On the basis of these studies, six analogues of Lavendustine B, containing the benzylamino-hydroxybenzoic scaffold, were selected for synthesis and structure activity-relationship (SAR) studies. Our results demonstrated a good correlation between computational and experimental data, and all six analogues displayed an improved potency for inhibiting IN binding to LEDGF/p75 in?vitro to respect to the parent compound Lavendustin B. Additionally, these analogs show to inhibit weakly LEDGF/p75-independent IN catalytic activity suggesting a multimodal allosteric mechanism of action. Nevertheless, for the synthesized compounds similar profiles for HIV-1 inhibition and cytoxicity were highlighted. Taken together, our studies elucidated the mode of action of Lavendustin B analogs and provided a path for their further development as a new promising class of HIV-1 integrase inhibitors.
- Agharbaoui, Fatima E.,Hoyte, Ashley C.,Ferro, Stefania,Gitto, Rosaria,Buemi, Maria Rosa,Fuchs, James R.,Kvaratskhelia, Mamuka,De Luca, Laura
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p. 673 - 683
(2016/08/12)
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- Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold
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A series of compounds possessing 2-(3-phenyl)ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and HepG2 cell lines using Sorafenib as the positive control. Compounds 6i showed a good to moderate inhibition on VEGFR-2 and PI3Kα which was proved by further molecular docking study. This study suggests that compound 6i is a potential dual inhibitor of VEGFR-2 and PI3Kα and is applicable for further investigation.
- Li, Lin,Zhang, Cun-Long,Song, Hong-Rui,Tan, Chun-Yan,Ding, Huai-Wei,Jiang, Yu-Yang
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supporting information
p. 1 - 6
(2016/01/25)
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- 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
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Paragraph 0401; 0402; 0403
(2014/06/23)
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- COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC DISORDERS AND SYNTHESIS OF THE SAME
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The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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Page/Page column 120
(2014/10/18)
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- NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS
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Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.
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Paragraph 0343; 0344
(2014/03/24)
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- ARYLOXY PHENOXY ACRYLIC COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT
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The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity no
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Paragraph 0146; 0147; 0148; 0167; 0168; 0169
(2013/09/26)
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- DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
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Paragraph 0841
(2013/04/10)
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- DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
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Page/Page column 190
(2013/04/13)
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- HETEROCYCLIC COMPOUNDS
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The present invention relates to novel pyrimidine class of compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions containing them and their use in medicine.
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Page/Page column 32
(2013/04/25)
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- Application of new photolabile protecting groups as photocleavable joints of block copolymers
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New photoresponsive block copolymers (BCPs) have been developed by incorporating photocleavable units. These photocleavable units are derived from robust photolabile protecting groups (PPGs); UV irradiation cleaves the BCPs and releases a well-defined chemically active functional group at the cleaved end of a PS polymer. The Royal Society of Chemistry 2013.
- Lu, Wenya,Tian, Chong,Thogaripally, Punith,Hu, Jun,Wang, Pengfei
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p. 9636 - 9638
(2013/10/08)
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- Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as Hypoxia-Inducible Factor (HIF) 1α inhibitors
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A series of (E)-phenoxyacrylic amide derivatives were synthesized and evaluated as hypoxia inducible factor (HIF) 1α inhibitors. The present structure-activity relationship study on this series identified the morpholinoethyl containing ester 4p as a potent inhibitor of HIF-1α under hypoxic conditions (IC50 = 0.12 μM in a cell-based HRE reporter assay) in HCT116 cells. The representative compound 4p suppressed hypoxia-induced HIF-1α accumulation and targeted gene expression in a dose-dependent manner. The effect of HIF-1α inhibition by 4p was further demonstrated by its inhibitory activity on in vitro tube formation and migration of cells, which may be valuable for development of novel therapeutics for cancer and tumor angiogenesis.
- Naik, Ravi,Won, Misun,Kim, Bo-Kyung,Xia, Yan,Choi, Hyun Kyung,Jin, Guanghai,Jung, Youngjin,Kim, Hwan Mook,Lee, Kyeong
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supporting information
p. 10564 - 10571
(2013/02/22)
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- Biaryl analogues of teriflunomide as potent DHODH inhibitors
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The structure-activity relationships of a novel series of biaryl dihydroorotate dehydrogenase (DHODH) inhibitors related to teriflunomide are disclosed. These biaryl derivatives were the result of structure-based design and proved to be potent DHODH inhibitors which in addition showed good antiproliferative activities on peripheral blood mononuclear cells and good efficacies in vivo in the rat adjuvant-induced-arthritis model.
- Erra, Montse,Moreno, Imma,Sanahuja, Jordi,Andres, Miriam,Reinoso, Raquel F.,Lozoya, Estrella,Pizcueta, Pilar,Godessart, Nuria,Castro-Palomino, Julio Cesar
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p. 7268 - 7272
(2012/02/04)
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- Development of trityl-based photolabile hydroxyl protecting groups
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A series of trityl-based photolabile hydroxyl protecting groups have been examined. These PPGs evolve from the traditional acid-labile trityl protecting group with proper electron-donating substituents. Structure-reactivity relationships have been explored. A m-dimethylamino group is crucial to achieve high photochemical deprotection efficiency. The o-hydroxyl group in 8 greatly improves the yield of the photochemical deprotection reaction, compared with the corresponding o-methoxyl-substituted counterpart 7. However, comparison between the photoreactions of 9 and 11 does not show similar structural relevance. The PPG in ether 1 (i.e., DMATr group) is structurally simple and easy to prepare and install. Its deprotection can be successfully carried out with irradiation of sunlight without requirement of photochemical devices.
- Zhou, Lei,Yang, Haishen,Wang, Pengfei
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experimental part
p. 5873 - 5881
(2011/10/02)
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- Syntheses of 1,2,3-triazolyl salicylamides with inhibitory activity on lipopolysaccharide-induced nitric oxide production
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A 28-membered 1,2,3-triazolyl salicylamide library was synthesized via a Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition and evaluated for their abilities to inhibit NO production in LPS-activated RAW264.7 macrophage cells. Among 28 analogues, 29g showed a significant inhibitory activity (IC 50 = 12.8 μM). The inhibitory effects of 29g on LPS-mediated NO production in macrophage cells appeared to be associated with the suppression of iNOS expression.
- Yoon, Jieun,Cho, Lan,Lee, Sang Kook,Ryu, Jae-Sang
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supporting information; experimental part
p. 1953 - 1957
(2011/05/02)
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- LIPOIC ACID ACYLATED SALICYLATE DERIVATIVES AND THEIR USES
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The invention relates to lipoic acid acylated salicylate derivatives; compositions comprising an effective amount of a lipoic acid acylated salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of
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Page/Page column 30
(2011/04/24)
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- Multitarget Compounds Active at a PPAR and Cannabinoid Receptor
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There is a need for pharmaceutical compounds which have activity at, at least one of a PPAR and a cannabinoid receptor. Thus there are provided such compounds, wherein the compound comprises: a PPAR pharmacophore and a cannabinoid pharmacophore linked together by a moiety comprising a fused bicyclic ring comprising a five membered ring fused with a six membered ring or a six membered ring fused with a six membered ring; wherein the cannabinoid pharmacophore comprises the fused bicyclic ring; and the PPAR pharmacophore comprises a salicylic acid, alkoxybenzylacetic acid or a alkoxyphenylacetic acid functionality; and wherein the PPAR pharmacophore is linked to the bicyclic ring of the cannabinoid pharmacophore through a linker comprising an amine or an amide functional group.
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Page/Page column 50
(2011/04/13)
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- Mizoroki-heck reactions with 4-phenoldiazonium salts
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Significantly better yields were achieved in Mizoroki-Heck reactions using 4-phenoldiazonium salts instead of their O-alkylated analogues under otherwise identical conditions. We found that a one-flask deacetylation-diazotation- precipitation sequence starting from paracetamol or acetanilides derived thereof provides a convenient access to the required diazonium tetrafluoroborates. The utility of these arylating agents in palladium-catalyzed C-C bond forming reactions was demonstrated for a one-flask-synthesis of the heterocyclic core of the drug aripiprazole. Notably, the diazonium salt formation from an acetanilide could be combined with two Pd-catalyzed steps in a one-flask sequence, without any exchange of solvents or isolation of intermediates.
- Schmidt, Bernd,Hoelter, Frank,Berger, Rene,Jessel, Soenke
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supporting information; experimental part
p. 2463 - 2473
(2010/12/25)
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- Structure-based design, synthesis and biological evaluation of new N-carboxyphenylpyrrole derivatives as HIV fusion inhibitors targeting gp41
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A new series of N-carboxyphenylpyrrole ligands were designed using GeometryFit based on an X-ray crystal structure of gp41. The synthesized ligands showed significant inhibitory activities against HIV gp41 6-helix bundle formation, HIV-1 mediated cell-cel
- Wang, Yong,Lu, Hong,Zhu, Qiang,Jiang, Shibo,Liao, Yun
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scheme or table
p. 189 - 192
(2010/04/02)
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- A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly
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Lavendustin-mimetic small molecules modifying the linker -CH 2-NH- with an 1,2,3-triazole ring have been synthesized via a click chemistry. Two pharmacophoric fragments of lavendustin were varied to investigate chemical space and the auxophoric -CH2-NH- was altered to an 1,2,3-triazole for rapid click conjugation. The small molecules were evaluated against HCT116 colon cancer and CCRF-CEM leukemia cell lines. Among 28 analogues, 3-phenylpropyl ester 26b inhibited CCRF-CEM leukemia cell growth with GI50 value of 0.9 μM.
- Yoon, Jieun,Ryu, Jae-Sang
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supporting information; experimental part
p. 3930 - 3935
(2010/08/20)
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- FATTY ACID ACETYLATED SALICYLATES AND THEIR USES
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The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.
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Page/Page column 113-114
(2010/03/04)
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- Photolabile carbonyl protecting group: A new tool for light-controlled release of anticancer agents
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A new type of photolabile carbonyl-protecting group was utilized in releasing anticancer agents upon irradiation at 350 nm in an aqueous environment.
- Wang, Pengfei,Mondal, Mukulesh,Wang, Yun
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scheme or table
p. 2055 - 2058
(2009/09/06)
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- Salicylate-urea-based soluble epoxide hydrolase inhibitors with high metabolic and chemical stabilities
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We investigated N-adamantyl-N′-phenyl urea derivatives as simple sEH inhibitors. Salicylate ester derivatives have high inhibitory activities against human sEH, while the free benzoic acids are less active. The methyl salicylate derivative is a potent sEH inhibitor, which also has high metabolic and chemical stabilities; suggesting that such inhibitors are potential lead molecule for bioactive compounds acting in vivo.
- Kasagami, Takeo,Kim, In-Hae,Tsai, Hsing-Ju,Nishi, Kosuke,Hammock, Bruce D.,Morisseau, Christophe
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supporting information; experimental part
p. 1784 - 1789
(2009/12/03)
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- Sequential removal of photolabile protecting groups for carbonyls with controlled wavelength
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(Chemical Equation Presented) A group of robust and easy-to-make photolabile protecting groups (PPGs) for carbonyl compounds has been developed. Sequential removal of different PPGs is achieved via control of irradiation wavelength.
- Wang, Pengfei,Wang, Yun,Hu, Huayou,Spencer, Cierra,Liang, Xing,Pan, Lurong
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p. 6152 - 6157
(2008/12/22)
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- Process for the preparation of aromatic azo-compounds
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The present invention relates to a process for the preparation of aromatic azo-compounds, in particular 3,3′-azo-bis(6-hydroxybenzoic acid) (olsalazine) and its salts and derivatives.
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- PYRROLE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine, in particular their use in the treatment of prostaglandin mediated diseases such as pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
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- Identification of urinary metabolites of ecabapide in rat
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14C-Ecabapide, 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]methyl]amino-N-methyl[14 C]benzamide, was dosed orally to rat (100 mg/kg). Within 48 h after dosing, 36.7 ± 5.4 and 55.7 ± 11.8% of the administered radioactivity was recovered from urine and faeces respectively. The unchanged drug was the major compound excreted in the urine and accounted for 37% of the urinary radioactivity. Seven urinary metabolites were purified by preparative hplc and their structures were elucidated by mass and 1H-nmr spectrometry. The major metabolic pathway of ecabapide was found to be the formation of 3-amino-N-methylbenzamide produced by N-dealkylation of the secondary amine at the 3-position of the benzamide moiety followed by acetylation. Further metabolic pathways of the N-methylbenzamide moiety were N-demethylation via the carbinolamine derivatives, and/or aromatic hydroxylation followed by glucuronidation.
- Fujimaki,Hosokami,Ono
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p. 501 - 510
(2007/10/03)
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- SUBSTITUTED-4-THIAZOLIDINONE DERIVATIVES
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Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin
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- Benzoic acid derivatives and use thereof
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A pharmaceutical composition for use in the treatment of psoriasis comprises 4-aminosalicylic acid (4-ASA) or 5-aminosalicylic acid (5-ASA) or a functional derivative thereof, said pharmaceutical composition being in a form suitable for topical administration. Furthermore, 4- or 5-ASA or a functional derivative thereof are used for the manufacture of pharmaceutical compositions for treating psoriasis, atopic dermatitis, allergic dermatitis, contact dermatitis, seborrhoic dermatitis, or acne diseases. The derivatives have the formulae: STR1 where W is COOX, wherein X is H, Li, Na, K, Mg0.5, Ca0.5, Zn0.5, Al0.33, Fe(II)0.5, Fe(III)0.33, NH4, NH3 R1, NH2 R12, NHR13, NR14, or R1, where R1 is substituted or unsubstituted C1-6 -alkyl, aryl-C1-4 -alkyl, or heteroaryl-C1-4 -alkyl; or COX, where X is NR1 R1', where R1' has the same meaning as R1 defined above and R1 and R1' may be identical or different; Y is H or R1 CO, where R1 is defined as above; Z1 and Z2, which may be identical or non-identical are H, R1 or R1 CO, where R1 is defined as above, or Z1 and Z2 represent R2, where R2 is substituted or unsubstituted C1-6 -alkylidene or aryl-C1-6 -alkylidene, or heteroaryl-C1-6 -alkylidene, or Z1, Z2 together with the nitrogen atom to which they are attached may represent a 3 to 7 membered saturated or unsaturated heterocyclic ring, or may represent a group of the formula --N=N--R3 where R3 is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.
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- Protease inhibitors
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This invention relates to methods of preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation by administering compounds, some of which are novel, of the formula: STR1 or their pharmacologically acceptable salts.
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- 1,3,5- Or 1,3,6-naphthalenetriyltris(sulfonylimino)aryl acids and salts
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1,3,5- or 1,3,6-naphthalenetriyltris(sulfonylimino)aryl acids and salts, useful as complement inhibitors, and 1,3,5- or 1,3,6-naphthalenetriyltris(sulfonylimino)aryl acid esters which are intermediates, and the method for their preparation.
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