928038-44-2

Usage

Uses

3-Azetidinemethanol Hydrochloride is used in the synthesis of human rhinovirus inhibitors.

InChI:InChI=1/C4H9NO.ClH/c6-3-4-1-5-2-4;/h4-6H,1-3H2;1H

Upstream product

• 72351-36-1 1-diphenylmethyl-3-hydroxymethylazetidine 
• 142253-56-3 3-hydroxymethyl-azetidine-1-carboxylic acid tert-butyl ester 
• 99025-94-2 (1-benzylazetidin-3-yl)methanol 

Downstream Products

• 1016233-36-5 1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl]azetidine-3-methanol 
• 1354791-87-9 (3-(4-((3-(hydroxymethyl)azetidin-1-yl)methyl)phenylthio)azetidin-1-yl)(5-phenyl-1,3,4-oxadiazol-2-yl)methanone 
• 142253-56-3 3-hydroxymethyl-azetidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

RAPIDLY ACCELERATING FIBROSARCOMA PROTEIN DEGRADING COMPOUNDS AND ASSOCIATED METHODS OF USE

Bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-Raf), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds Raf, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS

The present disclosure provides phosphodiesterase 5 (PDE-5) and/or phosphodiesterase 6 (PDE-6) inhibitor compounds and compositions including said compounds. In some embodiments, said compounds are nitrogen oxide (NO) donating PDE-5 and/or -6 inhibitor compounds that include a nitrogen oxide-containing donor substituent attached to a benzenesulfonamide group. The compounds can provide dual functionality for increasing protein kinase G (PKG) activity by inhibiting PDE-5 and PDE-6, and/or stimulating guanylate cyclase (sGC) via donation of nitrogen oxide (NO) from the donor substituent of the compound. The present disclosure also provides methods of using said compounds and compositions for inhibiting PDE-5 and/or -6 and increasing activity of protein kinase G (PKG). The compounds and compositions find use in therapeutic applications including in the treatment of a variety of eye diseases. For example, the subject compounds may be used as a therapeutic agent for glaucoma, age-related macular degeneration (AMD), diabetic retinopathy (DR), xerophthalmia, cataracts or uveitis.

SELECTIVE MODULATORS OF MUTANT LRRK2 PROTEOLYSIS AND ASSOCIATED METHODS OF USE

Bifunctional compounds, which find utility as modulators of non-receptor Leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

SOMATOSTATIN MODULATORS AND USES THEREOF

Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

MODIFIED COMPOUND OF ANDROGRAPHOLIDE

The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.

As the NS4B inhibitor benzofuran analogs (by machine translation)

The present invention discloses a kind of as NS4B benzofuran analogue inhibitors, in particular to the formula (I) below or a pharmaceutically acceptable salt thereof. (by machine translation)

Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders

To try and generate broad spectrum human rhinovirus VP1 inhibitors with more attractive physicochemical, DMPK and safety profiles, we explored the current SAR of known VP1 compounds. This lead to the identification of specific structural regions where reduction in polarity can be achieved, so guiding chemistry to analogues with significantly superior profiles to previously reported inhibitors.

PYRIDINE OR PYRIMIDINE DERIVATIVE HAVING EXCELLENT CELL GROWTH INHIBITION EFFECT AND EXCELLENT ANTI-TUMOR EFFECT ON CELL STRAIN HAVING AMPLIFICATION OF HGFR GENE

A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen.

AZETIDINE ANALOGUES OF NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS

Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH2OH, CH2OQ and CH2SQ; Y and Z are each independently selected from hydrogen, halogen, CH2OH, CH2OQ, CH2SQ, SQ, OQ and Q; Q is an alkyl, aralkyl or aryl group each of which may be optionally substituted with one or more substituents selected from hydroxy, halogen, methoxy, amino, or carboxy; R1 is a radical of the formula (II) or R1 is a radical of the formula (III) A is selected from N, CH and CR2, where R2 is selected from halogen, alkyl, aralkyl, aryl, OH, NH2, NHR3, NR3R4 and SR5, where R3, R4 and R5 are each alkyl, aralkyl or aryl groups optionally substituted with hydroxy or halogen, and where R2 is optionally substituted with hydroxy or halogen when R2 is alkyl, aralkyl or aryl; B is selected from hydroxy, NH2, NHR6, SH, hydrogen and halogen, where R6 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; D is selected from hydroxy, NH2, NHR7, hydrogen, halogen and SCH3, where R7 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; E is selected from N and CH; G is a C1-4 saturated or unsaturated alkyl group optionally substituted with hydroxy or halogen, or G is absent; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof.

TAXANE COMPOUND WITH AZETIDINE RING STRUCTURE

A compound represented by the general formula (1) [X1 and X2 represent hydrogen atom, a halogen atom, hydroxyl group and the like, R1 represents a phenyl group, R2 represents an alkyl group, an alkenyl group, or