40004-08-8

Usage

Uses

1. Used in Pharmaceutical Industry:
1-(Ethoxycarbonylmethyl)piperazine is used as a chemical intermediate for the preparation of aralkylpiperazineand aryl-substituted hydrazines, particularly benzylpiperazineacetyl hydrazones of hydroxyaryl aldehydes. These compounds serve as selective inducers of apoptosis and activators of procaspases, making them potential candidates for use as anticancer agents.
2. Used in Anticancer Applications:
In the field of oncology, 1-(Ethoxycarbonylmethyl)piperazine plays a crucial role in the development of novel anticancer agents. The hydrazine derivatives synthesized using 1-(Ethoxycarbonylmethyl)piperazine have the potential to induce apoptosis and activate procaspases, which are essential for the initiation of programmed cell death in cancer cells. This makes them valuable in the fight against various types of cancer.
3. Used in Chemical Synthesis:
As a versatile chemical intermediate, 1-(Ethoxycarbonylmethyl)piperazine can be utilized in the synthesis of a wide range of chemical compounds, including those with potential applications in various industries such as pharmaceuticals, agrochemicals, and materials science.

InChI:InChI=1/C8H16N2O2/c1-2-12-8(11)7-10-5-3-9-4-6-10/h9H,2-7H2,1H3

Upstream product

• 110-85-0 piperazine 
• 105-36-2 ethyl bromoacetate 
• 105-39-5 chloroacetic acid ethyl ester 
• 209667-59-4 tert-butyl 4-(2-ethoxy-2-oxoethyl)piperazine-1-carboxylic acid 

Downstream Products

• 24637-27-2 Piperazino-essigsaeure-hydrazid 
• 374776-43-9 4-(2-ethoxy-5-(4-(ethoxycarbonylmethyl)piperazinylsulfonyl)benzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 374776-44-0 4-(5-(4-(ethoxycarbonylmethyl)piperazinylsulfonyl)-2-n-propoxybenzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 336191-54-9 4-nitrophenyl 4-(2-ethoxy-2-oxoethyl)-1-piperazine carboxylate 
• 861712-01-8 [4-(2,2,5,5-tetramethylpyrrolidin-1-oxyl-3-carbonyl)piperazin-1-yl]acetic acid ethyl ester 
• 864442-44-4 ethyl 2-(4-benzoylpiperazin-1-yl)acetate 
• 229341-11-1 C₃₁H₂₉Cl₃N₄O₄S 
• 209667-59-4 tert-butyl 4-(2-ethoxy-2-oxoethyl)piperazine-1-carboxylic acid 
• 209667-67-4 1-t-butoxycarbonyl-4-phenyl-4-((4-carboethoxymethylpiperazin-1-yl)carboxamido)piperidine 
• 209667-50-5 1-benzyl-4-(pyrid-3-yl)-4-((4-carboethoxymethylpiperazin-1-yl)carboxamido)piperidine 
• 55829-24-8 {4-[cyano-(3,4-dimethoxy-phenyl)-methyl]-piperazin-1-yl}-acetic acid ethyl ester 
• 23173-76-4 ethyl 2-(4-benzylpiperazin-1-yl)acetate 
• 2387-23-7 1,3-Dicyclohexylurea 
• 1239204-48-8 ethyl 2-(4-(4-sulfamoylbenzyl)piperazin-1-yl)acetate 

Relevant academic research and scientific papers

Fused ring compound, pharmaceutical composition containing fused ring compound, and preparation method and application of fused ring compound

The present invention relates to a fused ring compound as shown in Formula (I-A) or Formula (I-B) which is described in the specification, a pharmaceutical composition comprising the same, a preparation method and an application in the prevention or treatment of diseases or conditions associated with RET activity.

Prescreening of Nicotine Hapten Linkers in Vitro To Select Hapten-Conjugate Vaccine Candidates for Pharmacokinetic Evaluation in Vivo

Since the demonstration of nicotine vaccines as a possible therapeutic intervention for the effects of tobacco smoke, extensive effort has been made to enhance nicotine specific immunity. Linker modifications of nicotine haptens have been a focal point for improving the immunogenicity of nicotine, in which the evaluation of these modifications usually relies on in vivo animal models, such as mice, rats or nonhuman primates. Here, we present two in vitro screening strategies to estimate and predict the immunogenic potential of our newly designed nicotine haptens. One utilizes a competition enzyme-linked immunoabsorbent assay (ELISA) to profile the interactions of nicotine haptens or hapten-protein conjugates with nicotine specific antibodies, both polyclonal and monoclonal. Another relies on computational modeling of the interactions between haptens and amino acid residues near the conjugation site of the carrier protein to infer linker-carrier protein conjugation effect on antinicotine antibody response. Using these two in vitro methods, we ranked the haptens with different linkers for their potential as viable vaccine candidates. The ELISA-based hapten ranking was in an agreement with the results obtained by in vivo nicotine pharmacokinetic analysis. A correlation was found between the average binding affinity (IC50) of the haptens to an anti-Nic monoclonal antibody and the average brain nicotine concentration in the immunized mice. The computational modeling of hapten and carrier protein interactions helps exclude conjugates with strong linker-carrier conjugation effects and low in vivo efficacy. The simplicity of these in vitro screening strategies should facilitate the selection and development of more effective nicotine conjugate vaccines. In addition, these data highlight a previously under-appreciated contribution of linkers and hapten-protein conjugations to conjugate vaccine immunogenicity by virtue of their inclusion in the epitope that binds and activates B cells.

Tankyrase inhibitor

The invention belongs to the technical field of medicines and particularly relates to a tankyrase inhibitor represented by a general formula (I) shown in the description and pharmaceutically acceptable salts, esters, solvates or stereoisomers thereof, wherein R1, R2, R3, m, n, Z, L, Q, A, X1, X2 and Y are as defined in the description. The invention further relates to a preparation method for the compounds, pharmaceutical preparations and pharmaceutical compositions containing the compounds and application of the compound and the pharmaceutically acceptable salts, esters, solvates or stereoisomers thereof in preparation of drugs for treating and/or preventing tankyrase mediated cancers and related diseases.

BIARYL DERIVATIVE AS GPR120 AGONIST

The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

Removal of metabolic liabilities enables development of derivatives of procaspase-activating compound 1 (PAC-1) with improved pharmacokinetics

Procaspase-activating compound 1 (PAC-1) is an o-hydroxy-N-acylhydrazone that induces apoptosis in cancer cells by chelation of labile inhibitory zinc from procaspase-3. PAC-1 has been assessed in a wide variety of cell culture experiments and in vivo models of cancer, with promising results, and a phase 1 clinical trial in cancer patients has been initiated (NCT02355535). For certain applications, however, the in vivo half-life of PAC-1 could be limiting. Thus, with the goal of developing a compound with enhanced metabolic stability, a series of PAC-1 analogues were designed containing modifications that systematically block sites of metabolic vulnerability. Evaluation of the library of compounds identified four potentially superior candidates with comparable anticancer activity in cell culture, enhanced metabolic stability in liver microsomes, and improved tolerability in mice. In head-to-head experiments with PAC-1, pharmacokinetic evaluation in mice demonstrated extended elimination half-lives and greater area under the curve values for each of the four compounds, suggesting them as promising candidates for further development.

FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS

The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

DESIGN, SYNTHESIS AND EVALUATION OF PROCASPASE ACTIVATING COMPOUNDS AS PERSONALIZED ANTI-CANCER DRUGS

Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.

COMPOSITIONS AND METHODS INCLUDING CELL DEATH INDUCERS AND PROCASPASE ACTIVATION

Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.

COMPOSITIONS OF NOVEL OPIOID COMPOUNDS AND METHOD OF USE THEREOF

Diarylmethylpiperazine compounds are described, which are useful as mu and/or delta receptor opioid compounds, without central side effects. Pharmaceutical compositions containing such compounds are variously useful for peripheral or non-centrally mediated indications, including peripherally mediated and neuropathic pain, urogenital tract disorders, overactive bladder, urinary incontinence, sexual disorders, premature ejaculation, cough, lung edema, cardiac disorders, cardioprotection, gastro-intestinal disorders, diarrhea, irritable bowl syndrome, functional distention, immuno-modulation and anti-tumor activity.

PYRAZOLE COMPOUNDS

Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted Cl-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or Cl-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r (Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -S02-, -C(=O)O-, -OC(=O)-, -NW-, -C(=O)NRA-, -NRAC(=O)-, -SO2NRA- , or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.