3138-88-3

Usage

Uses

Used in Organic Synthesis:
(2R,5S)-1-Benzyl-2,5-Dimethyl-Piperazine is utilized as an intermediate in organic synthesis for the creation of various chemical compounds. Its unique structure allows for the development of new molecules with potential applications across different industries.
Used in Pharmaceutical Research:
In the pharmaceutical industry, (2R,5S)-1-Benzyl-2,5-Dimethyl-Piperazine serves as a valuable intermediate for the research and development of new drugs. Its structural features may contribute to the discovery of novel therapeutic agents with improved efficacy and safety profiles.
Used in Drug Development:
(2R,5S)-1-Benzyl-2,5-Dimethyl-Piperazine holds promise in the development of new drugs, potentially leading to advancements in medicinal chemistry. Its role in this process is to facilitate the synthesis of drug candidates that may address unmet medical needs or offer alternative treatment options.
Used in Material Science:
Although not explicitly mentioned in the provided materials, the compound's potential applications in material science could be explored, given its unique chemical structure. This may include the development of new materials with specific properties for use in various applications, such as coatings, adhesives, or polymers.

InChI:InChI=1/C13H20N2/c1-11-9-15(12(2)8-14-11)10-13-6-4-3-5-7-13/h3-7,11-12,14H,8-10H2,1-2H3/t11-,12+/m1/s1

Upstream product

• 100-39-0 benzyl bromide 
• 2815-34-1 2,5-dimethyl-piperazine 
• 3138-88-3 (+/-)-trans-2,5-dimethyl-4-benzyl-piperazine 
• 3744-87-4 Boc-(R)-Ala 
• 31022-10-3 N-benzyl-L-alanine methyl ester 
• 75-36-5 acetyl chloride 
• 200731-31-3 HATU 
• 3138-88-3 C₁₃H₂₀N₂ 
• 262295-89-6 (3S,6R)-1-benzyl-3,6-dimethylpiperazine-2,5-dione 
• 95-14-7 1,2,3-Benzotriazole 
• 1122-91-4 4-bromo-benzaldehyde 
• 100-44-7 benzyl chloride 
• 1072102-01-2 (3S,6R)-4-benzyl-3,6-dimethylpiperazine-2,5-dione 
• 159999-80-1 N-benzyl-N-Boc-L-alanine 

Downstream Products

• 216532-43-3 (-)-(2R,5S)-1-benzyl-2,5-dimethylpiperazine 
• 260254-80-6 trans-2R,5S-dimethyl-4-benzyl-piperazine 

Relevant academic research and scientific papers

CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER

[Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)

3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES AS INHIBITORS OF PROTEIN KINASE C

The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ

3-AMINO-PYRROLO[3,4-C] PYRAZOLE- 5 (1H, 4H, 6H) CARBALDEHYDE DERIVATIVES AS PKC INHIBITORS

The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.

(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6- (trifluoromethyl)pyridin-3-yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist

A novel series of trans-N-aryl-2,5-dimethylpiperazine-1-carboxamide derivatives was synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic effects were evaluated. Pharmacological assays indicated that compound 33 was a potent AR antagonist, and subsequent optical resolution provided (+)-(2R,5S)4-[4-cyano-3-(trifluoromethyl)phenyl]-2, 5-dimethyl-N-[6(triflouromethyl)pyridin-3-yl]piperazine-1-carboxamide (33a, YM580) which exhibited the most potent antiandrogenic activity. Unlike bicalutamide, compound 33a decreased the weight of rat ventral prostate in a dose-dependent manner (ED50 = 2.2 mg/kg/day), and induced the maximum antiandrogenic effect, comparable to that of surgical castration, without significantly affecting serum testosterone levels. Compound 33a is a promising clinical candidate for prostate cancer monotherapy.

PIPERAZINE DERIVATIVES AND THEIR USE AS MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION

The present invention provides piperazine derivatives and methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders.

Indole-type derivatives as inhibitors of p38 kinase

The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond;one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent;A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 ?, and each of i and j is independently 0 or 1;as Z3 is NR7 or O;each R3 is independently a noninterfering substituent;n is 0-3;each of L1 and L2 is a linker;each R4 is independently a noninterfering substituent;m is 0-4;Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent;each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3;Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; andthe distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24 ?.

Cyanophenyl derivative

This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.

Indole-type derivatives as inhibitors of p38 kinase

The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.

Indole-based heterocyclic inhibitors of p38α MAP kinase: Designing a conformationally restricted analogue

p38α Mitogen Activated Protein Kinase (MAP kinase) is an intracellular soluble serine threonine kinase. p38α kinase is activated in response to cellular stresses, growth factors and cytokines such as interleukin-1 (IL-1) and tumor necrosis factor alpha (TNF-α). The central role of p38α activation in settings of both chronic and acute inflammation has led efforts to find inhibitors of this enzyme as possible therapies for diseases such as rheumatoid arthritis, where p38α activation is thought to play a causal role. Herein, we report structure-activity relationship studies on a series of indole-based heterocyclic inhibitors that led to the design and identification of a new class of p38α inhibitors.

Anti-inflammatory piperazinyl-benzyl-tetrazole derivatives and intermediates thereof

This invention relates to tetrazoles and their pharmaceutically acceptable salts which are selective agonists for the delta opioid receptor, particularly useful in the treatment of inflammatory diseases such as arthritis, psoriasis, asthma, inflammatory bowel disease, disorders or respiratory function, gastrointestinal disorders such as functional bowel disease and functional GI disorders, of formula (I) wherein R1is H, C2-C6alkanoyl, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, (C3-C7cycloalkyl)-(C1-C4alkyl), (C1-C4alkoxy)-(C1-C4alkyl), carboxy-(C1-C4alkyl), aryl-(C1-C4alkyl) or heteroaryl-(C1-C4alkyl); R2and R3are each independently H or C1-C4alkyl; R4is selected from (i) H, (ii) a group of the formula R6—(CH2)m—Z—(CH2)n—, where m is 0, 1, 2 or 3, n is 1, 2 or 3, Z is a direct link or O, and R6is —CO2H or —CO2(C1-C4alkyl), and (iii) a group of formula (a) where R7is H or C1-C4alkyl; and R5is hydroxy, C1-C4alkoxy or —NHSO2(C1-C4alkyl); with the proviso that when Z is O, m is 1, 2 or 3 and n is 2 or 3.