198627-86-0

Usage

Uses

Used in Pharmaceutical Research and Drug Development:
1-(3-HYDROXY-PHENYL)-PIPERAZINE-4-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a building block for the synthesis of various biologically active compounds due to its versatile chemical structure and potential to be modified for specific therapeutic targets.
Used in Central Nervous System Stimulation:
In the field of neuroscience and neurology, 1-(3-HYDROXY-PHENYL)-PIPERAZINE-4-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a central nervous system stimulant, leveraging its ability to enhance cognitive function and treat certain neurological conditions.
Used in Psychiatric Disorders Treatment:
1-(3-HYDROXY-PHENYL)-PIPERAZINE-4-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a potential therapeutic agent for the treatment of psychiatric disorders, given its pharmacological profile that may address specific symptoms or underlying mechanisms of these conditions.
Used in Anti-inflammatory and Analgesic Applications:
In the medical and pharmaceutical industries, 1-(3-HYDROXY-PHENYL)-PIPERAZINE-4-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a potential anti-inflammatory and analgesic agent, due to its capacity to reduce inflammation and alleviate pain, which is crucial for managing various conditions and diseases.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 59817-32-2 3-(piperazin-1-yl)phenol 
• 16015-71-7 4-(3-methoxyphenyl)piperazine 
• 107623-21-2 1-(benzyloxy)-3-iodobenzene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 862261-23-2 4-(3-triisopropylsilanyloxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 571202-87-4 3-bromophenyl triisopropylsilyl ether 

Downstream Products

• 540752-86-1 4-(3-trifluoromethanesulfonyloxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1215221-41-2 4-{3-[6-propyl-4-(3-trifluoromethyl-5,6-dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazine-7-yl)-thieno[2,3-d]pyrimidin-2-yloxy]-phenyl}-piperazine-1-carboxylic acid t-butyl ester 
• 89989-06-0 1-(3-ethoxyphenyl)piperazine 
• 1261576-81-1 (4-chloro-N-(naphthalen-1-ylmethyl)-5-(3-(piperazin-1-yl) phenoxy)thiophene-2-sulfonamide) 
• 1265157-04-7 1-(3-(2-fluoroethoxy)phenyl)piperazine 
• 1417454-08-0 C₂₁H₂₇N₃O₃ 
• 1417454-24-0 C₂₆H₃₅N₃O₅ 
• 1380753-90-1 2-(3-(3-(4-(tert-butoxycarbonyl)piperazin-1-yl)phenoxy)azetidin-1-yl)-5-chloronicotinic acid 
• 1380754-68-6 methyl 4-(1-(5-chloro-2-(3-(3-(piperazin-1-yl)phenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate 
• 1380754-72-2 tert-butyl 4-(3-((1-(5-chloro-3-((1-(4-(methoxycarbonyl)phenyl)cyclopropyl)carbamoyl)pyridin-2-yl)azetidin-3-yl)oxy)phenyl)piperazine-1-carboxylate 
• 1380750-73-1 4-(1-(5-chloro-2-(3-(3-(piperazin-1-yl)phenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoic acid 
• 1261576-78-6 tert-butyl 4-(3-(3-chloro-5-(N-(4-methoxybenzyl)-N-(naphthalen-1-ylmethyl)sulfamoyl)thiophen-2-yloxy)phenyl)piperazine-1-carboxylate 
• 1261576-80-0 C₃₀H₃₂ClN₃O₅S₂ 
• 882695-43-4 4-[3-(2,2,2-Trifluoro-ethoxy)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight ‘molecular budget’

Structure-based led optimisation of orally active reversible Methionine Aminopeptidase-2 (MetAP-2) inhibitors utilising a ‘molecular budget’ medicinal chemistry strategy is described. The key physicochemical parameters of target molecules (cLogP, molecula

PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS

The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(═N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, endometriosis and migraine.

PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS

The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is -O-, -O(C1-C3 alkyl)-; -(C1-C3 alkyl)O-; -C(O)-; -C(=N-O(C1-C3 alkyl))-; -NH- or -NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, -NH(C1-C3alkyl)-; -N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is convalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid artrhritis, cancer, endometriosis and migraine.

FUSED HETEROCYCLIC COMPOUND

The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.

Synthesis of novel WAY 100635 derivatives containing a norbornene group and radiofluorination of [18F]AH1.MZ as a serotonin 5-HT1A receptor antagonist for molecular imaging

5-HT1A receptors are involved in a variety of psychiatric disorders and in vivo molecular imaging of the 5-HT1A status represents an important approach to analyze and treat these disorders. We report herein the synthesis of three new

FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS

The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is -H, -OH, -O-R7, -N(H) -R8, -N (H) - (CH2) n-NH2, -N(R9) (R10), or a piperazine cation; R2 is either covalently bound to R9, or is -H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, -H, -OH, alkyl, or when Z is nitrogen R3 is =O; R4 is, inter alia, -H, -OH, or -R11NH2; R5 is, inter alia, -H, -OH, or -R12NH2, and R6 is either is covalently bound to R10 or is -H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.

Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands

A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H4 receptor.

KINASE MODULATORS AND METHODS OF USE

The present invention relates to compounds of the Formula I and II wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.

2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs as adenosine A2A antagonists: The successful reduction of hERG activity. Part 2

The structure-activity relationship (SAR) exploration using 2-(2-furanyl)-7-phenyl[1,2,4]triazolo-[1,5-c]pyrimidin-5-amine (1) as a template led to the identification of a novel class of potent and selective adenosine A2A receptor (AR) antagoni

SUBSTITUTED PIPERAZINES, (1,4) DIASZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS

The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.