317829-98-4

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 317365-33-6 1-(benzyloxycarbonyl)-2-hydroxymethyl-4-(tert-butyloxycarbonyl)-piperazine 
• 529516-61-8 O₁-benzyl O₄-tert-butyl (2S)-2-(hydroxymethyl)piperazine-1,4-dicarboxylate 
• 314741-40-7 (3S)-3-(hydroxymethyl)-1-piperazinecarboxylic acid 1,1-dimethylethyl ester 
• 128019-59-0 piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 
• 126937-41-5 1-(benzyloxycarbonyl)-4-(tert-butoxycarbonyl)-2-piperazinecarboxylic acid 
• 301673-16-5 tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate 
• 501-53-1 benzyl chloroformate 
• 181955-79-3 N,N'-di-tert-butyloxycarbonylpiperazine-2-carboxylic acid 
• 143540-05-0 2-hydroxymethylpiperazine-1,4-dicarboxylic acid di-tert-butyl ester 
• 935544-47-1 tert-butyl 3-oxotetrahydro-1H-oxazolo[3,4-a]pyrazine-7(3H)-carboxylate 

Downstream Products

• 935544-55-1 1-benzyl 4-tert-butyl 2-vinylpiperazine-1,4-dicarboxylate 

Relevant academic research and scientific papers

HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS

Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

COMBINATION OF HEPATITIS B VIRUS (HBV) VACCINES AND DIHYDROPYRIMIDINE DERIVATIVES AS CAPSID ASSEMBLY MODULATORS

Therapeutic combinations of hepatitis B virus (HBV) vaccines and capsid assembly modulators (CAMs), such as dihydropyrimidine derivatives are described. Methods of inducing an immune response against HBV or treating an HBV-induced disease, particularly in individuals having chronic HBV infection, using the disclosed therapeutic combinations are also described.

BICYCLIC OGA INHIBITOR COMPOUNDS

The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and

CHEMOKINE CXCR4 RECEPTOR MODULATORS AND USES RELATED THERETO

The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. The receptor modulators can be formulated to form pharmaceutical compositions comprising the disclosed compounds or pharmaceutically acceptable salts or prodrugs thereof. The compositions may be used for managing CXCR4 related conditions, typically prevention or treatment of viral infections abnormal cellular proliferation, retinal degeneration, inflammatory diseases, or as an immunostimulant or immunosuppressant or for managing cancer and may be administered with another active ingredient such as an antiviral agent or chemotherapeutic agent.

COMPOUNDS FOR USE IN THE TREATMENT OF KINETOPLASTID INFECTION

The present invention relates to a class of novel heterocyclic compounds, to pharmaceutical compositions comprising the compounds and their use in the treatment of kinetoplastid infections.

PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS

The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS

The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

Discovery of novel N-aryl piperazine CXCR4 antagonists

A novel series of CXCR4 antagonists with substituted piperazines as benzimidazole replacements is described. These compounds showed micromolar to nanomolar potency in CXCR4-mediated functional and HIV assays, namely inhibition of X4 HIV-1IIIB virus in MAGI-CCR5/CXCR4 cells and inhibition of SDF-1 induced calcium release in Chem-1 cells. Preliminary SAR investigations led to the identification of a series of N-aryl piperazines as the most potent compounds. Results show SAR that indicates type and position of the aromatic ring, as well as type of linker and stereochemistry are significant for activity. Profiling of several lead compounds showed that one (49b) reduced susceptibility towards CYP450 and hERG, and the best overall profile when considering both SDF-1 and HIV potencies (6-20 nM).

An orthogonal protection strategy for the synthesis of 2-substituted piperazines

Tetrahydro-1H-oxazolo[3,4-a]pyrazin-3(5H)-ones are readily prepared from the bis-carbamate protected piperazine-2-carboxylic acids and serve as orthogonally protected piperazines from which a variety of 2-substituted piperazines can be prepared. Sodium benzylate and sodium phenoxides react at the C-5 carbon of the oxazolidinone to yield 2-(benzyloxymethyl)piperazines and 2-(phenoxymethyl)piperazines, respectively. The tetrahydro-1H-oxazolo[3,4-a]pyrazin-3(5H)-ones also provide convenient scaffolds from which 2-benzyl- and 2-phenethylpiperazines are prepared.

NOVEL PIPERAZINES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF

Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are phannaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.