352437-09-3

Usage

Uses

Used in Pharmaceutical Industry:
4-(4-BROMO-PHENYL)-PIPERAZINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER is used as a reagent for the synthesis of dual Bcl-2/Bcl-xL inhibitors. These inhibitors are of significant interest in the field of oncology, as they target the Bcl-2 family of proteins, which play a critical role in regulating apoptosis (programmed cell death). By inhibiting these proteins, the compound can potentially promote apoptosis in cancer cells, leading to the development of more effective cancer treatments.

InChI:InChI=1/C15H21BrN2O2/c1-15(2,3)20-14(19)18-10-8-17(9-11-18)13-6-4-12(16)5-7-13/h4-7H,8-11H2,1-3H3

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 66698-28-0 1-(4-bromophenyl)piperazine 
• 821-48-7 bis-(2-chloroethyl)amine hydrochloride 
• 106-40-1 4-bromo-aniline 
• 106-37-6 1.4-dibromobenzene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 589-87-7 1,4-bromoiodobenzene 
• 5467-74-3 4-Bromophenylboronic acid 
• 77278-40-1 tert-butyl 4-(benzoyloxy)piperazine-1-carboxylate 
• 183677-71-6 2-(4-bromophenyl)-5,5-dimethyl-1,3,2-dioxaborinane 

Downstream Products

• 1190962-22-1 tert-butyl 4-(4-(spiro[chromeno[3,4-d]pyrimidine-5,1'-cyclohexane]-3-ylamino)phenyl)-piperazine-1-carboxylate 
• 457613-78-4 4-(4-(tert-butoxycarbonyl)piperazin-1-yl)phenylboronic acid 
• 1228187-44-7 tert-butyl 4-(4'-methylbiphenyl-4-yl)piperazine-1-carboxylate 
• 1233959-10-8 tert-butyl 4-(4-styrylphenyl)piperazine-1-carboxylate 
• 1616558-18-9 C₂₂H₃₅N₃O₄S 
• 1616557-88-0 C₁₈H₂₇N₃O₃ 
• 912369-50-7 1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]piperazine 

Relevant academic research and scientific papers

MONOACYLGLYCEROL LIPASE INHIBITORS

Provided are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof: Also provided are compositions comprising compounds of formula (I). The compounds and compositions are also provided for use as medicaments, for example as medicaments useful in the treatment of a condition modulated by monoacylglycerol lipase (MAGL). Also provided are the use of compounds and compositions for the inhibition of monoacylglycerol lipase (MAGL).

COMPOUND SIMULTANEOUSLY INHIBITING LSD1 AND HDAC TARGETS AND APPLICATION THEREOF

A compound having a general structural formula as shown in Formula I: X-AB-Y (Formula I); in the above Formula I, X is selected from any one of -CO2H, -CONHZ, -CH=CH-CO2H, -CH=CH-CONHZ, wherein Z is selected from any one of substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted aryl, and hydroxyl; Y = -NR1R2, wherein NR1R2 is a substituted or unsubstituted 3- to 9-membered nitrogen-containing heterocycloalkyl; A and B are each independently selected from substituted or unsubstituted phenylene, substituted or unsubstituted azaphenylene. The compound or corresponding pharmaceutical salt thereof can inhibit LSD1 and HDAC target proteins at the same time, thus inhibit the proliferation of many kinds of tumor cells and have good antitumor effect.

POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES

The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.

RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.

ANTI-PAIN COMPOUND AND PREPARATION METHOD THEREFOR

Disclosed are a compound represented by the general Formula (I), or a stereisomer, tautomer, derivative, prodrug or pharmaceutically acceptable salt thereof, and a method for preparing the compound and use of the compound in manufacture of a medicament for treating a neuropathic pain and/or neuropathic pain syndrome or a medicament for combating an inflammation: wherein R1 is selected from hydrogen, halogen, alkyl, cyano and haloalkyl, R2 and R3 are independently selected from hydrogen, halogen, alkyl, haloalkyl and nitro, and R1, R2 and R3 are not hydrogen at the same time; furthermore, when either R2 or R3 is nitro or halogen, the other two of R1, R2 and R3 are not hydrogen at the same time. The compound has good effects in treating a neuropathic pain and/or neuropathic pain syndrome and good effects in combating an inflammation, and has not side effects such as addiction.

METHODS FOR TREATING PATIENTS WITH CANCER HAVING DEFECTS IN CYCLIN D REGULATION

The present disclosure relates to methods of treating cancer comprising administering Parkin ligase activator or a pharmaceutically acceptable salt thereof to a subject who has a mutant form of a protein in the Rb checkpoint pathway. The Parkin ligase activator includes triazole compounds, such as compounds of formula (I), and pharmaceutically acceptable salts thereof as disclosed herein. R1, R2, R3, M1, M2, M3, L1, L2, and L3 are as defined herein.

Substituted piperazine compounds and method and use thereof

The invention relates to a new piperazine compound and a drug composition comprising the compound, which are used for inhibiting 5-hydroxytryptamine reuptake and/or agonizing 5-HT1A receptors. The invention also relates to methods for preparing the compou

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES

The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

METALLOENZYME INHIBITOR COMPOUNDS

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.